Indole derivatives for use in medicine

Abstract

Provided is a tryptophan-2,3-dioxygenase (TDO) and/or indoleamine-2,3-dioxygenase (IDO) inhibitor compound for use in medicine, which compound comprises the following formula: wherein X.sup.1, X.sup.2, X.sup.3, X.sup.4, and X.sup.5 may be the same or different and each is independently selected from C, N and O; each atom having a dotted line may independently have a double bond or a single bond, provided that valencies at each atom are maintained; each R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, and R.sup.7 may be present or absent and may be the same or different and is selected from H and a substituted or unsubstituted organic group, provided that the number of such R groups present is such that the valencies of X.sup.1, X.sup.2, X.sup.3, X.sup.4, and X.sup.5 are maintained; one or two R.sup.6 groups may be present and are selected from H and a substituted or unsubstituted organic group, provided that the number of R.sup.6 groups present is such that the valency of the carbon atom to which they are attached is maintained, and provided that at least one R.sup.6 is an organic group comprising an atom double-bonded to an oxygen atom (preferably a carbonyl group or a sulphonyl group) at an -, -, or -position to the carbon atom to which the R.sup.6 is attached and in which the atom double-bonded to an oxygen atom is also bonded to a hetero-atom. ##STR00001##

Claims

1. A compound of the following formula, or a pharmaceutically acceptable salt thereof: ##STR00132## wherein: each of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 is independently selected from H, halogen, CN, C.sub.1-C.sub.6 alkyl, C.sub.1-C.sub.6 halogenated alkyl, OH, C.sub.1-C.sub.7 alkoxy, OCF.sub.3, C(O)NH.sub.2, C(O)NHMe, NHSO.sub.2Me, NHSO.sub.2Et, NHSO.sub.2Pr, and NHSO.sub.2iPr; R.sup.5 is H; R.sup.7 is selected from H and C.sub.1-C.sub.6 alkyl; R.sup.61 is selected from H and C.sub.1-C.sub.6 alkyl; R.sup.65 is a heterocyclic group selected from pyrazol-1-yl, pyrazol-3-yl, pyrazol-4-yl, pyrazol-5-yl, 1,2,3-triazol-4-yl, 1,2,3-triazol-5-yl, 1,2,4-triazol-1-yl, 1,2,4-triazol-3-yl, 1,2,4-triazol-5-yl, pyridin-2-yl, pyridin-3-yl, pyridin-4-yl, pyrimidin-2-yl, pyrimidin-4-yl, pyrimidin-5-yl, pyrimidin-6-yl, piperidin-1-yl, piperidin-2-yl, piperidin-3-yl, piperidin-4-yl, oxazol-2-yl, oxazol-4-yl, oxazol-5-yl, isoxazol-3-yl, isoxazol-4-yl, isoxazol-5-yl, tetrazol-1-yl, tetrazol-2-yl, and tetrazol-5-yl; each of which is optionally substituted with one to three substituents independently selected from halogen, methyl, ethyl, propyl, C(O)-methyl, S(O).sub.2-methyl and phenyl; and R.sup.63 and R.sup.64 together form a 3-6 membered carbocyclic or heterocyclic ring selected from cyclopropyl, cyclobutyl, cyclopentyl, cyclopentenyl, cyclohexyl, cyclohexenyl, aziridinyl, azetidinyl, pyrrolidinyl, piperidinyl, piperazinyl, oxetanyl, tetrahydrofuranyl and tetrahydropyranyl.

2. The compound according to claim 1, or a pharmaceutically acceptable salt thereof, wherein: each of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 is independently selected from H, halogen, CN, methyl, ethyl, propyl, iso-propyl, n-butyl, iso-butyl, tert-butyl, CF.sub.3, CHF.sub.2, OH, O-methyl, O ethyl, O-propyl, and OCF.sub.3; R.sup.5 is H; R.sup.7 is selected from H and methyl; R.sup.61 is selected from H, methyl, ethyl, propyl and iso-propyl; R.sup.65 is pyrazol-1-yl, pyrazol-3-yl, pyrazol-4-yl, pyrazol-5-yl, 1,2,3-triazol-1-yl, 1,2,3-triazol-4-yl, 1,2,3-triazol-5-yl, 1,2,4-triazol-1-yl, 1,2,4-triazol-3-yl, 1,2,4-triazol-5-yl, oxazol-2-yl, oxazol-4-yl, isoxazol-3-yl, tetrazol-1-yl, tetrazol-2-yl, and tetrazol-5-yl; each of which is optionally substituted with one to three substituents independently selected from halogen, methyl, ethyl, propyl and phenyl; and R.sup.63 and R.sup.64 together form a 3-6 membered saturated carbocyclic or heterocyclic ring selected from cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, aziridinyl, azetidinyl, pyrrolidinyl, piperidinyl, piperazinyl, oxetanyl, tetrahydrofuranyl and tetrahydropyranyl.

3. The compound according to claim 2, or a pharmaceutically acceptable salt thereof, wherein: each of R.sup.1, R.sup.3 and R.sup.4 is independently selected from H, halogen and methyl; R.sup.2 is selected from halogen, CN, methyl, ethyl, propyl, iso-propyl, CF.sub.3, CHF.sub.2, OH, O methyl, O-ethyl, O-propyl and OCF.sub.3; and each of R.sup.5 and R.sup.7 is H.

4. The compound according to claim 3, or a pharmaceutically acceptable salt thereof, wherein R.sup.61 is H.

5. The compound according to claim 4, or a pharmaceutically acceptable salt thereof, wherein: R.sup.65 is a heterocyclic group selected from pyrazol-1-yl, pyrazol-3-yl, pyrazol-4-yl, pyrazol-5-yl, 1,2,4-triazol-1-yl, 1,2,4-triazol-3-yl, 1,2,4-triazol-5-yl, oxazol-4-yl, isoxazol-3-yl, tetrazol-1-yl, tetrazol-2-yl, tetrazol-5-yl; each of which is optionally substituted with one to three substituents independently selected from halogen, methyl, ethyl, propyl, and phenyl; and R.sup.63 and R.sup.64 together form a 3-6 membered carbocyclic or heterocyclic ring selected from cyclopropyl, cyclobutyl, cyclopentyl, and cyclohexyl.

6. The compound according to claim 2, or a pharmaceutically acceptable salt thereof, wherein: each of R.sup.1, R.sup.3, and R.sup.4 is H; R.sup.2 is selected from halogen, CN, methyl, ethyl, CF.sub.3, O-methyl and OCF.sub.3; each of R.sup.5 and R.sup.61 is H; R.sup.7 is H; R.sup.65 is a heterocyclic group selected from pyrazol-1-yl, pyrazol-3-yl, pyrazol-4-yl, pyrazol-5-yl, oxazol-4-yl, isoxazol-3-yl, tetrazol-1-yl, tetrazol-2-yl, and tetrazol-5-yl; each of which is optionally substituted with one to three substituents independently selected from halogen, methyl, ethyl, propyl, and phenyl; and R.sup.63 and R.sup.64 together form a 3-6 membered unsubstituted saturated carbocyclic ring selected from cyclopropyl, cyclobutyl, cyclopentyl, and cyclohexyl.

7. The compound according to claim 1 selected from the following, or a pharmaceutically acceptable salt thereof: ##STR00133## ##STR00134## ##STR00135## ##STR00136## ##STR00137## ##STR00138##

8. A compound according to claim 1, or a pharmaceutically acceptable salt thereof, which compound comprises: an isolated enantiomer, a mixture of two or more enantiomers, a mixture of two or more diastereomers, and/or epimers, a racemic mixture, and/or one or more tautomers of the compound.

9. A pharmaceutical composition comprising a compound of claim 1, or a pharmaceutically acceptable salt thereof.

10. The compound according to claim 1 selected from the following, or a pharmaceutically acceptable salt thereof: ##STR00139## ##STR00140## ##STR00141## ##STR00142## ##STR00143## ##STR00144##

11. The compound according to claim 1 selected from the following, or a pharmaceutically acceptable salt thereof: ##STR00145## ##STR00146## ##STR00147## ##STR00148##

12. The compound according to claim 1 selected from the following, or a pharmaceutically acceptable salt thereof: ##STR00149## ##STR00150##

13. The compound according to claim 2 of the following formula, or a pharmaceutically acceptable salt thereof: ##STR00151##

14. The compound according to claim 2 of the following formula, or a pharmaceutically acceptable salt thereof: ##STR00152##

15. The compound according to claim 2 of the following formula, or a pharmaceutically acceptable salt thereof: ##STR00153##

16. The compound according to claim 2 of the following formula, or a pharmaceutically acceptable salt thereof: ##STR00154##

17. The compound according to claim 2 of the following formula, or a pharmaceutically acceptable salt thereof: ##STR00155##

18. The compound according to claim 2, or a pharmaceutically acceptable salt thereof, wherein: each of R.sup.1, R.sup.3 and R.sup.4 is independently selected from H, methyl, ethyl and halogen; R.sup.2 is selected from H, methyl, ethyl, propyl, O-methyl, O-ethyl, O-propyl, O-isopropyl, OCF.sub.3, CF.sub.3, CHF.sub.2, CN, F, Cl and Br; each of R.sup.5 and R.sup.7 is H; R.sup.61 is selected from H, methyl and ethyl; R.sup.63 and R.sup.64 together form a 3-6 membered saturated carbocyclic or heterocyclic ring selected from cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, aziridinyl, azetidinyl, pyrrolidinyl, piperidinyl, piperazinyl, oxetanyl, tetrahydrofuranyl and tetrahydropyranyl; and R.sup.65 is selected from: pyrazol-1-yl, optionally substituted with methyl, ethyl or propyl; pyrazol-3-yl, optionally substituted with methyl, ethyl or propyl; pyrazol-4-yl, optionally substituted with methyl, ethyl or propyl; and pyrazol-5-yl, optionally substituted with methyl, ethyl or propyl.

19. The compound according to claim 18, wherein: each of R.sup.1, R.sup.3 and R.sup.4 is independently selected from H, methyl and halogen; R.sup.2 is selected from methyl, ethyl, O-methyl, O-ethyl, F, Cl, Br and CN; each of R.sup.5, R.sup.7 and R.sup.61 is H; R.sup.63 and R.sup.64 together form a 3-6 membered saturated carbocyclic ring selected from cyclopropyl, cyclobutyl, cyclopentyl and cyclohexyl; and R.sup.65 is selected from: pyrazol-1-yl, optionally substituted with methyl, ethyl or propyl; pyrazol-3-yl, optionally substituted with methyl, ethyl or propyl; pyrazol-4-yl, optionally substituted with methyl, ethyl or propyl; and pyrazol-5-yl, optionally substituted with methyl, ethyl or propyl.

20. The compound according to claim 18, wherein: each of R.sup.1, R.sup.3 and R.sup.4 is H; R.sup.2 is selected from methyl, ethyl, F, Cl, Br and CN; each of R.sup.5, R.sup.7 and R.sup.61 is H; R.sup.63 and R.sup.64 together form cyclopropyl; and R.sup.65 is selected from: pyrazol-1-yl, optionally substituted with methyl, ethyl or propyl; pyrazol-3-yl, optionally substituted with methyl, ethyl or propyl; and pyrazol-4-yl, optionally substituted with methyl, ethyl or propyl.

21. A compound of the following formula: ##STR00156##

22. A compound of the following formula: ##STR00157##

23. A compound of the following formula: ##STR00158##

24. A compound of the following formula: ##STR00159##

Description

(1) The invention will now be explained in more detail, by way of example only, with reference to the following Figures.

(2) FIG. 1 shows a schematic diagram of tryptophan catabolism along the KP (from The Kynurenine Pathway in Brain Tumour Pathogenesis, Adam et al., 2012, Cancer Res 72:5649-57).

(3) FIG. 2 shows a schematic summary of the involvement of kynurenine in CNS disorders (from The kynurenine pathway as a therapeutic target in cognitive and neurodegenerative disorders, Stone and Darlington. Br. J. Pharmacol. 2013 169(6):1211-27.

(4) The compounds used in the invention will now be described in more detail.

(5) As has been described, the invention relates to a tryptophan-2,3-dioxygenase (TDO) and/or indoleamine-2,3-dioxygenase (IDO) inhibitor compound for use in medicine, which compound comprises the following formula:

(6) ##STR00011##
wherein X.sup.1, X.sup.2, X.sup.3, X.sup.4, and X.sup.5 may be the same or different and each is independently selected from C, N, and O; each atom having a dotted line may independently have a double bond or a single bond, provided that valencies at each atom are maintained; each R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, and R.sup.7 may be present or absent and may be the same or different and is selected from H and a substituted or unsubstituted organic group, provided that the number of such R groups present is such that the valencies of X.sup.1, X.sup.2, X.sup.3, X.sup.4, and X.sup.5 are maintained; one or two R.sup.6 groups may be present and are selected from H and a substituted or unsubstituted organic group, provided that the number of R.sup.6 groups present is such that the valency of the carbon atom to which they are attached is maintained, and provided that at least one R.sup.6 is an organic group comprising an atom double-bonded to an oxygen atom (preferably forming a carbonyl group or a sulphonyl group) at an -, -, or -position to the carbon atom to which the R.sup.6 is attached and in which the atom double-bonded to an oxygen atom is also bonded to a hetero-atom.

(7) All tautomeric forms of the ring system (including the tautomeric forms of the 6-membered ring and the tautomeric forms of the 5-membered ring, and all combinations thereof), are included.

(8) As has been mentioned, this definition includes compounds in which, where there are two R groups attached to the same atom, except for R.sup.5 and R.sup.6, they may together form a group which is double bonded to that atom, such as a carbonyl group (O) or an alkene group (C(R).sub.2) (wherein each R group is the same or different and is H or an organic group, preferably H or a straight or branched C.sub.1-C.sub.6 alkyl group). Accordingly, in some embodiments R.sup.1, R.sup.2, R.sup.3, R.sup.4, and/or R.sup.7 may be a O group, as may R.sup.63, R.sup.64 and/or R.sup.66 in some embodiments discussed below.

(9) As has been mentioned, previously, Dolusic et al. have tested indole compounds to determine their IDO inhibitory activity and that study determined that certain indole compounds with ketone substituents at the 2-position might be useful IDO inhibitors, although marginally. Dolusic et al. concluded that a similar amide compound was not an effective inhibitor as compared with the ketone compounds. However, the inventors have now determined that Dolusic et al. were mistaken about amide compounds in that certain carbonyl compounds with adjacent hetero atoms are highly active. The amide compound in the Dolusic paper (compound REF) is not active and is therefore not claimed by the present invention, which only extends to active compounds. It has however been used as a reference compound in testing compounds of the invention.

(10) In the present context, preferably R.sup.5 and R.sup.7 do not comprise a cyclic group. Typically R.sup.5 and R.sup.7 are selected from H and a substituted or unsubstituted, linear or branched, C.sub.1-C.sub.6 alkyl group (such as methyl (Me), ethyl (Et), propyl (Pr), iso-propyl (i-Pr), n-butyl (n-Bu), iso-butyl (i-Bu), tert-butyl (t-Bu), pentyl and hexyl). More preferably both of R.sup.5 and R.sup.7 are H, or one of R.sup.5 and R.sup.7 is H and the other is Me (e.g. R.sup.5H and R.sup.7=Me, or R.sup.5=Me and R.sup.7H), or both of R.sup.5 and R.sup.7 are Me.

(11) In the above formula, in certain embodiments, when present R.sup.1 and R.sup.4 are both H, or R.sup.1 and R.sup.4 are both not H, or R.sup.1 is not H and R.sup.4 is H, or R.sup.4 is not H and R.sup.1 is H. Furthermore, in certain embodiments when present R.sup.7 is H. Furthermore, in certain embodiments when present R.sup.5 is H. Still further, in certain embodiments, where present R.sup.2 and R.sup.3 are both H, or R.sup.2 and R.sup.3 are both not H, or R.sup.2 is not H and R.sup.3 is H, or R.sup.3 is not H and R.sup.2 is H.

(12) It follows from the formula that X.sup.1, X.sup.2, X.sup.3 and X.sup.4 form a ring together with two C atoms, and all are present such that the ring is a 6-membered ring. This ring has at least one unsaturated bond between the two adjacent C atoms bridging the ring system, but may also have two or three unsaturated bonds, depending upon the bonding between the X atoms. X.sup.1, X.sup.2, X.sup.3 and X.sup.4 are selected from C, N and O. Typically all of X.sup.1, X.sup.2, X.sup.3 and X.sup.4 are C, but alternatively three of X.sup.1, X.sup.2, X.sup.3 and X.sup.4 may be C, two of X.sup.1, X.sup.2, X.sup.3 and X.sup.4 may be C, one of X.sup.1, X.sup.2, X.sup.3 and X.sup.4, may be C or all of X.sup.1, X.sup.2, X.sup.3 and X.sup.4 may be N. In some embodiments one of X.sup.1, X.sup.2, X.sup.3 and X.sup.4, may be N or two of X.sup.1, X.sup.2, X.sup.3 and X.sup.4, may be N. In some embodiments one of X.sup.1, X.sup.2, X.sup.3 and X.sup.4, may be O or two of X.sup.1, X.sup.2, X.sup.3 and X.sup.4, may be O.

(13) X.sup.5 forms a 5-membered ring together with one N atom and three C atoms. The ring has at least one unsaturated bond between the two adjacent C atoms bridging the ring system, but may also have a further unsaturated bond depending upon the bonding at X.sup.5, and depending upon the bonding at the N atom. Thus, in some embodiments there may be a double bond between X.sup.5 and the carbon atom bearing R.sup.6, whilst in other embodiments there may be a double bond between the N atom and the carbon atom bearing R.sup.6. In still further embodiments, the only double bond in the 5-membered ring is the one between the two adjacent C atoms bridging the ring system. Typically X.sup.5 is a C atom, and typically it is double-bonded to the adjacent C-atom. However, in certain embodiments, X.sup.5 is C and is single bonded to the adjacent C atom, or X.sup.5 is N and is double-bonded to the adjacent C atom, or X.sup.5 is N and is single bonded to the adjacent C atom, or X.sup.5 is O and is single bonded to the adjacent C atom.

(14) Thus, in view of the typical embodiments already described, in certain embodiments the invention relates to a compound as defined above, which compound comprises one of the following formulae:

(15) ##STR00012##

(16) In some more preferred embodiments X.sup.5 is C, in which case the compounds have one of the following formulae:

(17) ##STR00013##

(18) In other embodiments X.sup.5 is N, in which case the compounds have one of the following formulae:

(19) ##STR00014##

(20) In other embodiments, X.sup.5 is O, in which case the compounds have one of the following formulae:

(21) ##STR00015##

(22) In further preferred embodiments, the six membered ring is fully unsaturated such that the compounds have one of the following formulae:

(23) ##STR00016##
and when X.sup.5 is C, N or O the following formulae:

(24) ##STR00017##

(25) In still further preferred embodiments, in any of the above formulae, the five-membered ring has at least one double bond, and/or the 6-membered ring is fully unsaturated, and/or all of X.sup.1, X.sup.2, X.sup.3, and X.sup.4 are C or one of X.sup.1, X.sup.2, X.sup.3, and X.sup.4 is N.

(26) More preferred compounds of this type include the following:

(27) ##STR00018##

(28) In these compounds, in certain embodiments, when present R.sup.1 and R.sup.4 are both H, or R.sup.1 and R.sup.4 are both not H, or R.sup.1 is not H and R.sup.4 is H, or R.sup.4 is not H and R.sup.1 is H. Furthermore, in certain embodiments when present R.sup.7 is H. Furthermore, in certain embodiments when present R.sup.5 is H. Still further, in certain embodiments, where present R.sup.2 and R.sup.3 are both H, or R.sup.2 and R.sup.3 are both not H, or R.sup.2 is not H and R.sup.3 is H, or R.sup.3 is not H and R.sup.2 is H.

(29) In all of the embodiments herein, as has been described, R.sup.6 comprises an organic group comprising an atom double-bonded to an oxygen atom (preferably forming a carbonyl group or a sulphonyl group) at an -, -, or -position to the carbon atom to which the R.sup.6 is attached. In this context, the terms -, -, and -position have the common meaning in organic chemistry, that is to say that they refer to the adjacent atom (-) or the next-but-one atom (-), or the next-but-two atom (-). Thus, atom double-bonded to an oxygen atom may be an atom adjacent to the ring carbon to which R.sup.6 is attached, or may be the next-but-one atom to the ring carbon to which R.sup.6 is attached, or may be the next-but-two atom to the ring carbon to which R.sup.6 is attached. The atom double-bonded to an oxygen atom may be any atom common to organic groups (except oxygen and halogen), such as C, S, or P. As has been mentioned, preferably the atom double bonded to the oxygen forms a carbonyl group or a sulphonyl group. In the present compounds, the atom double-bonded to an oxygen atom (or the carbonyl group or sulphonyl group as the case may be) is further attached to an adjacent heteroatom. The adjacent heteroatom in this case may be any heteroatom common to organic groups (i.e. any non-carbon atom common to organic groups) and is typically an atom selected from N, O, S, P, B or Si, although in more preferred embodiments it is N.

(30) The carbonyl group or sulphonyl group may be any carbonyl group or sulphonyl group as long as it is a carbonyl group or a sulphonyl group attached to an adjacent heteroatom. In more preferred embodiments, the heteroatom is a nitrogen atom, and in typical embodiments, R.sup.6 is selected from the following groups:

(31) ##STR00019##
wherein R.sup.61 is selected from H and a substituted or unsubstituted organic group; R.sup.62 is selected from H and a substituted or unsubstituted organic group; X.sup.66 is selected from C, O, N and S (X.sup.66 is preferably C and if more than one X.sup.66 is present, preferably at least one X.sup.66 is C); and if present each R.sup.66 may be the same or different and is selected from H and a substituted or unsubstituted organic group, wherein the number of R.sup.66 present is sufficient to maintain the valency of X.sup.66, in the manner already explained above. The number of X.sup.66 atoms present may determine whether the atom double-bonded to the oxygen atom is -, -, or - to the ring system, and may be selected accordingly. When there are two X.sup.66 atoms present they may be joined by a double bond or a single bond.

(32) In the present context, and in general herein, the part of the structure present in brackets may be repeated the number of times given by the numbers next to the brackets. For example, in the case of (X.sup.66(R.sup.66).sub.2).sub.0,1,2 the X.sup.66(R.sup.66).sub.2 group may be absent, or may be present once: X.sup.66(R.sup.66).sub.2; or may be present twice: X.sup.66(R.sup.66).sub.2X.sup.66(R.sup.66).sub.2; or X.sup.66(R.sup.66)X.sup.66(R.sup.66).

(33) In typical embodiments R.sup.62 comprises a group having the following formula:

(34) ##STR00020##
wherein R.sup.63 and R.sup.64 may be the same or different and are independently selected from H and a substituted or unsubstituted organic group, and wherein R.sup.65 is selected from H and a substituted or unsubstituted organic group. Thus there may be one C(R.sup.63R.sup.64) group, or two such groups or three such groups present between the bicyclic ring system and the R.sup.65 group. When there is one C(R.sup.63R.sup.64) group (most preferred), typically at least one of R.sup.63 and R.sup.64 is not H. More typically R.sup.63 and R.sup.64 together form a 3-6 membered substituted or unsubstituted saturated or unsaturated carbocyclic or heterocyclic ring (such as a cyclopropyl, cyclobutyl, cyclopentyl, cyclopentenyl, cyclohexyl, cyclohexenyl, aziridine, azetidine, pyrrolidine, piperidine, piperazine, oxetane, tetrahydrofuran or tetrahydropyran ring).

(35) When there is more than one C(R.sup.63R.sup.64) group typically at least one of any of the R.sup.63 and R.sup.64 groups present is not H. More typically at least one R.sup.63 and R.sup.64 together form a 3-6 membered substituted or unsubstituted saturated or unsaturated carbocyclic or heterocyclic ring (such as a cyclopropyl, cyclobutyl, cyclopentyl, cyclopentenyl, cyclohexyl, cyclohexenyl, aziridine, azetidine, pyrrolidine, piperidine, piperazine, oxetane, tetrahydrofuran or tetrahydropyran ring). In these compounds the R.sup.63 or R.sup.64 group that is not H, or the 3-6 membered substituted or unsubstituted saturated or unsaturated carbocyclic or heterocyclic ring, may be on any of the C(R.sup.63R.sup.64) groups, including the central one, but is preferably on the C(R.sup.63R.sup.64) group closest to the bicyclic ring system, or on the C(R.sup.63R.sup.64) group next to the R.sup.65 group. When there are two or more R.sup.63 groups, or two or more R.sup.64 groups, each R.sup.63 may be the same or different and each R.sup.64 may be the same or different. In some embodiments R.sup.63 and R.sup.64 may together form a group which is double bonded to the carbon atom to which they are attached (such as a carbonyl group (O) or an alkene group (C(R).sub.2) wherein each R group is the same or different and is H or an organic group, preferably H or a straight or branched C.sub.1-C.sub.6 alkyl group).

(36) Thus, in view of the typical embodiments already described, in certain embodiments the invention relates to a compound as defined above, which compound comprises one or other of the following formulae:

(37) ##STR00021## ##STR00022## ##STR00023##
wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.7, R.sup.61, R.sup.63, R.sup.64, R.sup.65 and R.sup.66 are as defined herein. In these compounds, in certain embodiments, when present R.sup.1 and R.sup.4 are both H, or R.sup.1 and R.sup.4 are both not H, or R.sup.1 is not H and R.sup.4 is H, or R.sup.4 is not H and R.sup.1 is H. Furthermore, in certain embodiments when present R.sup.7 is H. Furthermore, in certain embodiments when present R.sup.5 is H. Still further, in certain embodiments, where present R.sup.2 and R.sup.3 are both H, or R.sup.2 and R.sup.3 are both not H, or R.sup.2 is not H and R.sup.3 is H, or R.sup.3 is not H and R.sup.2 is H.

(38) In further view of the typical embodiments already described, in certain embodiments the invention relates to a compound as defined above, which compound comprises one or other of the following formulae:

(39) ##STR00024## ##STR00025## ##STR00026##
R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.7, R.sup.61, R.sup.63, R.sup.64, R.sup.65 and R.sup.66 are as defined herein. In these compounds, in certain embodiments, when present R.sup.1 and R.sup.4 are both H, or R.sup.1 and R.sup.4 are both not H, or R.sup.1 is not H and R.sup.4 is H, or R.sup.4 is not H and R.sub.1 is H. Furthermore, in certain embodiments when present R.sup.7 is H. Furthermore, in certain embodiments when present R.sup.5 is H. Still further, in certain embodiments, where present R.sup.2 and R.sup.3 are both H, or R.sup.2 and R.sup.3 are both not H, or R.sup.2 is not H and R.sup.3 is H, or R.sup.3 is not H and R.sup.2 is H.

(40) In more preferred embodiments, in certain embodiments the invention relates to a compound as defined above, which compound comprises one or other of the following formulae:

(41) ##STR00027## ##STR00028## ##STR00029##
wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.7, R.sup.61, R.sup.63, R.sup.64, and R.sup.65 are as defined herein. In these compounds, in certain embodiments, when present R.sup.1 and R.sup.4 are both H, or R.sup.1 and R.sup.4 are both not H, or R.sup.1 is not H and R.sup.4 is H, or R.sup.4 is not H and R.sup.1 is H. Furthermore, in certain embodiments when present R.sup.7 is H. Furthermore, in certain embodiments when present R.sup.5 is H. Still further, in certain embodiments, where present R.sup.2 and R.sup.3 are both H, or R.sup.2 and R.sup.3 are both not H, or R.sup.2 is not H and R.sup.3 is H, or R.sup.3 is not H and R.sup.2 is H.

(42) In other embodiments which are less preferred, but not excluded, the invention relates to a compound as defined above, which compound comprises one or other of the following formulae:

(43) ##STR00030## ##STR00031## ##STR00032##
wherein, in these compounds (unlike in the more preferred compounds above) the R.sup.65 is not attached to the rest of the structure via a group of the type C(R.sup.63)(R.sup.64), and wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.7, R.sup.61, and R.sup.65 are otherwise as defined herein. In these compounds, typically R.sup.65 is not a monocyclic heterocyclic group. In these compounds, in certain embodiments, when present R.sup.1 and R.sup.4 are both H, or R.sup.1 and R.sup.4 are both not H, or R.sup.1 is not H and R.sup.4 is H, or R.sup.4 is not H and R.sup.1 is H. Furthermore, in certain embodiments when present R.sup.7 is H. Furthermore, in certain embodiments when present R.sup.5 is H. Still further, in certain embodiments, where present R.sup.2 and R.sup.3 are both H, or R.sup.2 and R.sup.3 are both not H, or R.sup.2 is not H and R.sup.3 is H, or R.sup.3 is not H and R.sup.2 is H.

(44) Although these other embodiments are less preferred, they are slightly more preferred when R.sup.65 comprises a fused ring group attached directly through one of the ring atoms. Thus, in such slightly more preferred compounds, R.sup.65 may typically be selected from:

(45) fused ring systems comprising two or three or more fused rings, which rings may be substituted or unsubstituted, preferably wherein the rings are selected from one, two, or more of the above aromatic groups and aromatic or non-aromatic heterocyclic groups, (e.g. fused ring systems such as naphthalene, anthracene, phenanthrene, phenalene, biphenylene, pentalene, indene, as-indacene, s-indacene, acenaphthylene, fluorene, fluoranthene, acephenanthrylene, azulene, heptalene, indole, indazole, benzimidazole, 4-azaindole, 5-azaindole, 6-azaindole, 7-azaindole, isoindole, 4-azaisoindole, 5-azaisoindole, 6-azaisoindole, 7-azaisoindole, indolizine, 1-azaindolizine, 2-azaindolizine, 3-azaindolizine, 5-azaindolizine, 6-azaindolizine, 7-azaindolizine, 8-azaindolizine, 9-azaindolizine, purine, carbazole, carboline, benzofuran, isobenzofuran, benzothiophene, isobenzothiophene, quinoline, cinnoline, quinazoline, quinoxaline, 5-azaquinoline, 6-azaquinoline, 7-azaquinoline, naphthyridine, isoquinoline, phthalazine, 6-azaisoquinoline, 7-azaisoquinoline, pteridine, chromene, isochromene, acridine, phenanthridine, perimidine, phenanthroline, phenoxazine, xanthene, phenoxanthiin, and/or thianthrene).

(46) In more preferred embodiments, the invention relates to a compound as defined above, which compound comprises one of the following formulae:

(47) ##STR00033##
wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.7, R.sup.61, R.sup.63, R.sup.64, and R.sup.65 are as defined herein, provided that all of X.sup.1, X.sup.2, X.sup.3 and X.sup.4 are C, or one of X.sup.1, X.sup.2, X.sup.3 and X.sup.4 is N and the rest of X.sup.1, X.sup.2, X.sup.3 and X.sup.4 are C, for example:

(48) ##STR00034##
wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.7, R.sup.61, R.sup.63, R.sup.64 and R.sup.65 are as defined herein. In these compounds, in certain embodiments, when present R.sup.1 and R.sup.4 are both H, or R.sup.1 and R.sup.4 are both not H, or R.sup.1 is not H and R.sup.4 is H, or R.sup.4 is not H and R.sup.1 is H. Furthermore, in certain embodiments when present R.sup.7 is H. Furthermore, in certain embodiments when present R.sup.5 is H. Still further, in certain embodiments, where present R.sup.2 and R.sup.3 are both H, or R.sup.2 and R.sup.3 are both not H, or R.sup.2 is not H and R.sup.3 is H, or R.sup.3 is not H and R.sup.2 is H.

(49) In any of the embodiments herein, and in particular in the preferred and more preferred embodiments described above, R.sup.1, R.sup.2, R.sup.3, R.sup.4, and R.sup.7 are preferably independently selected from H and:

(50) a halogen such as F, Cl, Br and I, preferably F and Cl;

(51) CN;

(52) a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 alkyl group such as such as methyl (Me), ethyl (Et), propyl (Pr), iso-propyl (i-Pr), cyclopropyl (cy-Pr), n-butyl (n-Bu), iso-butyl (i-Bu), tert-butyl (t-Bu), pentyl and hexyl, preferably -Me;

(53) a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 halogenated alkyl group (such as CH.sub.2F, CHF.sub.2, CH.sub.2Cl, CH.sub.2Br, CH.sub.2I, CF.sub.3, CCl.sub.3, CBr.sub.3, CI.sub.3, CH.sub.2CF.sub.3, CH.sub.2CCl.sub.3, CH.sub.2CBr.sub.3, and CH.sub.2CI.sub.3), preferably CF.sub.3; and

(54) a substituted or unsubstituted linear or branched C.sub.1-C.sub.7 alkoxy group (such as OMe, OEt, OPr, O-i-Pr, O-n-Bu, O-i-Bu, O-t-Bu, O-pentyl, O-hexyl, OCH.sub.2F, OCHF.sub.2, OCF.sub.3, OCH.sub.2Cl, OCHCl.sub.2, OCCl.sub.3, O-Ph, CH.sub.2OMe, CH.sub.2OEt, CH.sub.2OPr, CH.sub.2OBu, CH.sub.2CH.sub.2OMe, CH.sub.2CH.sub.2CH.sub.2OMe, CH.sub.2CH.sub.2CH.sub.2CH.sub.2OMe, and CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2OMe), preferably OMe;

(55) and R.sup.5 and R.sup.61 are preferably independently selected from H and:

(56) a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 alkyl group (such as methyl (Me), ethyl (Et), propyl (Pr), iso-propyl (i-Pr), n-butyl (n-Bu), iso-butyl (i-Bu), tert-butyl (t-Bu), pentyl and hexyl);

(57) a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 halogenated alkyl group (such as CH.sub.2F, CHF.sub.2, CF.sub.3, CCl.sub.3, CBr.sub.3, CI.sub.3, CH.sub.2CF.sub.3, CH.sub.2CCl.sub.3, CH.sub.2CBr.sub.3, and CH.sub.2CI.sub.3), preferably a linear or branched C.sub.1-C.sub.6 fluorinated alkyl group (such as CH.sub.2F, CHF.sub.2, CF.sub.3, CH.sub.2CH.sub.2F, CH.sub.2CHF.sub.2, and CH.sub.2CF.sub.3); and

(58) a substituted or unsubstituted linear or branched C.sub.2-C.sub.6 alcohol group (such as CH.sub.2CH.sub.2OH, CH.sub.2CH.sub.2CH.sub.2OH, CH(CH.sub.3)CH.sub.2OH, C(CH.sub.3).sub.2OH, CH.sub.2CH.sub.2CH.sub.2CH.sub.2OH, CH(CH.sub.3)CH.sub.2CH.sub.2OH, CH(CH.sub.3)CH(CH.sub.3)OH, CH(CH.sub.2CH.sub.3)CH.sub.2OH, C(CH.sub.3).sub.2CH.sub.2OH, CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2OH, and CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2OH);

(59) and R.sup.61 may further be selected from a substituted or unsubstituted cyclic C.sub.3-C.sub.8 alkyl group (such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl and cyclooctyl);

(60) wherein R.sup.5 is preferably H and R.sup.61 is preferably H;

(61) and R.sup.65 is preferably selected from H and:

(62) a cyclic amine or amido group (such as pyrrolidin-1-yl, pyrrolidin-2-yl, pyrrolidin-3-yl, piperidin-1-yl, piperidin-2-yl, piperidin-3-yl, piperidin-4-yl, piperazin-1-yl, piperazin-2-yl, piperazin-3-yl, morpholin-2-yl, morpholin-3-yl, morpholin-4-yl, 2-keto-pyrrolidinyl, 3-keto-pyrrolidinyl, 2-keto-piperidinyl, 3-keto-piperidinyl, 4-keto-piperidinyl), 2-keto-piperazinyl, and 3-keto-piperazinyl;

(63) a substituted or unsubstituted cyclic C.sub.3-C.sub.8 alkyl group (such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl and cyclooctyl);

(64) a substituted or unsubstituted aromatic group (such as Ph-, 2-F-Ph-, 3-F-Ph-, 4-F-Ph-, 2-Cl-Ph-, 3-Cl-Ph-, 4-Cl-Ph-, 2-Br-Ph-, 3-Br-Ph-, 4-Br-Ph-, 2-I-Ph-, 3-I-Ph, 4-I-Ph-, 2,(3,4,5 or 6)-F.sub.2-Ph-, 2,(3,4,5 or 6)-Cl.sub.2-Ph-, 2,(3,4,5 or 6)-Br.sub.2-Ph-, 2,(3,4,5 or 6)-I.sub.2-Ph-, 2,(3,4,5 or 6)-Me.sub.2-Ph-, 2,(3,4,5 or 6)-Et.sub.2-Ph-, 2,(3,4,5 or 6)-Pr.sub.2-Ph-, 2,(3,4,5 or 6)-Bu.sub.2-Ph-, 2,(3,4,5 or 6)-(CN).sub.2-Ph-, 2,(3,4,5 or 6)-(NO.sub.2).sub.2-Ph-, 2,(3,4,5 or 6)-(NH.sub.2).sub.2-Ph-, 2,(3,4,5 or 6)-(MeO).sub.2-Ph-, 2,(3,4,5 or 6)-(CF.sub.3).sub.2-Ph-, 3,(4 or 5)-F.sub.2-Ph-, 3,(4 or 5)-Cl.sub.2-Ph-, 3,(4 or 5)-Br.sub.2-Ph-, 3,(4 or 5)-I.sub.2-Ph-, 3,(4 or 5)-Me.sub.2-Ph-, 3,(4 or 5)-Et.sub.2-Ph-, 3,(4 or 5)-Pr.sub.2-Ph-, 3,(4 or 5)-Bu.sub.2-Ph-, 3,(4 or 5)-(CN).sub.2-Ph-, 3,(4 or 5)-(NO.sub.2).sub.2-Ph-, 3,(4 or 5)-(NH.sub.2).sub.2-Ph-, 3,(4 or 5)-(MeO).sub.2-Ph-, 3,(4 or 5)-(CF.sub.3).sub.2-Ph-, 2-Me-Ph-, 3-Me-Ph-, 4-Me-Ph-, 2-Et-Ph-, 3-Et-Ph-, 4-Et-Ph-, 2-Pr-Ph-, 3-Pr-Ph-, 4-Pr-Ph-, 2-Bu-Ph-, 3-Bu-Ph-, 4-Bu-Ph-, 2-(CN)-Ph-, 3-(CN)-Ph-, 4-(CN)-Ph-, 2-(NO.sub.2)-Ph-, 3-(NO.sub.2)-Ph-, 4-(NO.sub.2)-Ph-, 2-(NH.sub.2)-Ph-, 3-(NH.sub.2)-Ph-, 4-(NH.sub.2)-Ph-, 2-MeO-Ph-, 3-MeO-Ph-, 4-MeO-Ph-, 2-(NH.sub.2CO)-Ph-, 3-(NH.sub.2CO)-Ph-, 4-(NH.sub.2CO)-Ph-, 2-CF.sub.3-Ph-, 3-CF.sub.3-Ph-, 4-CF.sub.3-Ph-, 2-CF.sub.3O-Ph-, 3-CF.sub.3O-Ph-, and 4-CF.sub.3O-Ph-); and

(65) a saturated or unsaturated, substituted or unsubstituted, heterocyclic group including an aromatic heterocyclic group and/or a non-aromatic heterocyclic group (such as pyrrole-1-yl, pyrrole-2-yl, pyrrole-3-yl, pyrazole-1-yl, pyrazole-3-yl, pyrazole-4-yl, pyrazole-5-yl, imidazole-1-yl, imidazole-2-yl, imidazole-4-yl, imidazole-5-yl, 1,2,3-triazole-1-yl, 1,2,3-triazole-4-yl, 1,2,3-triazole-5-yl, 1,2,4-triazole-1-yl, 1,2,4-triazole-3-yl, 1,2,4-triazole-5-yl, pyridin-2-yl, pyridin-3-yl, pyridin-4-yl, pyridazine-3-yl, pyridazine-4-yl, pyrimidin-2-yl, pyrimidin-4-yl, pyrimidin-5-yl, pyrimidin-6-yl, pyrazine-2-yl, pyrrolidine-1-yl, pyrrolidine-2-yl, pyrrolidine-3-yl, piperidine-1-yl, piperidine-2-yl, piperidine-3-yl, piperidine-4-yl, 2-azapiperidine-1-yl, 2-azapiperidine-3-yl, 2-azapiperidine-4-yl, 3-azapiperidine-1-yl, 3-azapiperidine-2-yl, 3-azapiperidine-4-yl, 3-azapiperidine-5-yl, piperazine-1-yl, piperazine-2-yl, furan-2-yl, furan-3-yl, pyran-2-yl, pyran-3-yl, pyran-4-yl, 2-azapyran-2-yl, 2-azapyran-3-yl, 2-azapyran-4-yl, 2-azapyran-5-yl, 2-azapyran-6-yl, 3-azapyran-2-yl, 3-azapyran-4-yl, 3-azapyran-5-yl, 3-azapyran-6-yl, 4-azapyran-2-yl, 4-azapyran-3-yl, 4-azapyran-4-yl, 4-azapyran-5-yl, 4-azapyran-6-yl, tetrahydrofuran-2-yl, tetrahydrofuran-3-yl, 2-aza-tetrahydrofuran-2-yl, 2-aza-tetrahydrofuran-3-yl, 2-aza-tetrahydrofuran-4-yl, 2-aza-tetrahydrofuran-5-yl, 3-aza-tetrahydrofuran-2-yl, 3-aza-tetrahydrofuran-3-yl, 3-aza-tetrahydrofuran-4-yl, 3-aza-tetrahydrofuran-5-yl, tetrahydropyran-2-yl, tetrahydropyran-3-yl, tetrahydropyran-4-yl, 2-aza-tetrahydropyran-2-yl, 2-aza-tetrahydropyran-3-yl, 2-aza-tetrahydropyran-4-yl, 2-aza-tetrahydropyran-5-yl, 2-aza-tetrahydropyran-6-yl, 3-aza-tetrahydropyran-2-yl, 3-aza-tetrahydropyran-3-yl, 3-aza-tetrahydropyran-4-yl, 3-aza-tetrahydropyran-5-yl, 3-aza-tetrahydropyran-6-yl, morpholine-2-yl, morpholine-3-yl, morpholine-4-yl, thiophen-2-yl, thiophen-3-yl, isothiazole-3-yl, isothiazole-4-yl, isothiazole-5-yl, thiazole-2-yl, thiazole-4-yl, thiazole-5-yl, thiopyran-2-yl, thiopyran-3-yl, thiopyran-4-yl, 2-azathiopyran-2-yl, 2-azathiopyran-3-yl, 2-azathiopyran-4-yl, 2-azathiopyran-5-yl, 2-azathiopyran-6-yl, 3-azathiopyran-2-yl, 3-azathiopyran-4-yl, 3-azathiopyran-5-yl, 3-azathiopyran-6-yl, 4-azathiopyran-2-yl, 4-azathiopyran-3-yl, 4-azathiopyran-4-yl, 4-azathiopyran-5-yl, 4-azathiopyran-6-yl, thiolane-2-yl, thiolane-3-yl, thiane-2-yl, thiane-3-yl, thiane-4-yl, oxazol-2-yl, oxazol-4-yl, oxazol-5-yl, isoxazol-3-yl, isoxazol-4-yl, isoxazol-5-yl, furazan-3-yl, (1,3,4-oxadiazol)-2-yl, (1,3,4-oxadiazol)-5-yl, (1,2,4-oxadiazol)-3-yl, (1,2,4-oxadiazol)-5-yl; and tetrazole-1-yl, tetrazole-2-yl, tetrazole-5-yl); and

(66) fused ring systems comprising two or three or more fused rings, which rings may be substituted or unsubstituted, preferably wherein the rings are selected from one, two, or more of the above aromatic groups and aromatic or non-aromatic heterocyclic groups, (e.g. fused ring systems such as naphthalene, anthracene, phenanthrene, phenalene, biphenylene, pentalene, indene, as-indacene, s-indacene, acenaphthylene, fluorene, fluoranthene, acephenanthrylene, azulene, heptalene, indole, indazole, benzimidazole, 4-azaindole, 5-azaindole, 6-azaindole, 7-azaindole, isoindole, 4-azaisoindole, 5-azaisoindole, 6-azaisoindole, 7-azaisoindole, indolizine, 1-azaindolizine, 2-azaindolizine, 3-azaindolizine, 5-azaindolizine, 6-azaindolizine, 7-azaindolizine, 8-azaindolizine, 9-azaindolizine, purine, carbazole, carboline, benzofuran, isobenzofuran, benzothiophene, isobenzothiophene, quinoline, cinnoline, quinazoline, quinoxaline, 5-azaquinoline, 6-azaquinoline, 7-azaquinoline, naphthyridine, isoquinoline, phthalazine, 6-azaisoquinoline, 7-azaisoquinoline, pteridine, chromene, isochromene, acridine, phenanthridine, perimidine, phenanthroline, phenoxazine, xanthene, phenoxanthiin, and/or thianthrene);

(67) and R.sup.63 and R.sup.64 are preferably independently selected from H and:

(68) a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 alkyl group (such as Me, Et, Pr, i-Pr, n-Bu, i-Bu, t-Bu, pentyl and hexyl);

(69) a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 halogenated alkyl group (such as CH.sub.2F, CHF.sub.2, CH.sub.2Cl, CH.sub.2Br, CH.sub.2I, CF.sub.3, CCl.sub.3 CBr.sub.3, CI.sub.3, CH.sub.2CF.sub.3, CH.sub.2CCl.sub.3, CH.sub.2CBr.sub.3, and CH.sub.2CI.sub.3);

(70) an NH.sub.2 group or a substituted or unsubstituted linear or branched primary secondary or tertiary C.sub.1-C.sub.6 amine group (such as NMeH, NMe.sub.2, NEtH, NEtMe, NEt.sub.2, NPrH, NPrMe, NPrEt, NPr.sub.2, NBuH, NBuMe, NBuEt, CH.sub.2NH.sub.2, CH.sub.2NMeH, CH.sub.2NMe.sub.2, CH.sub.2NEtH, CH.sub.2NEtMe, CH.sub.2NEt.sub.2, CH.sub.2NPrH, CH.sub.2NPrMe, and CH.sub.2NPrEt);

(71) a substituted or unsubstituted cyclic C.sub.3-C.sub.8 alkyl group (such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl and cyclooctyl);

(72) an OH group or a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 alcohol group (such as CH.sub.2OH, CH.sub.2CH.sub.2OH, CH.sub.2CH.sub.2CH.sub.2OH, CH(CH.sub.3)CH.sub.2OH, C(CH.sub.3).sub.2OH, CH.sub.2CH.sub.2CH.sub.2CH.sub.2OH, CH(CH.sub.3)CH.sub.2CH.sub.2OH, CH(CH.sub.3)CH(CH.sub.3)OH, CH(CH.sub.2CH.sub.3)CH.sub.2OH, C(CH.sub.3).sub.2CH.sub.2OH, CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2OH, and CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2OH);

(73) a substituted or unsubstituted cyclic amine or amido group (such as pyrrolidin-2-yl, pyrrolidin-3-yl, piperidin-2-yl, piperidin-3-yl, piperidin-4-yl, piperazin-1-yl, piperazin-2-yl, piperazin-3-yl, morpholin-2-yl, morpholin-3-yl, 2-keto-pyrrolidinyl, 3-keto-pyrrolidinyl, 2-keto-piperidinyl, 3-keto-piperidinyl, 4-keto-piperidinyl), 2-keto-piperazinyl, and 3-keto-piperazinyl;

(74) a substituted or unsubstituted aromatic group (such as Ph-, 2-F-Ph-, 3-F-Ph-, 4-F-Ph-, 2-Cl-Ph-, 3-Cl-Ph-, 4-Cl-Ph-, 2-Br-Ph-, 3-Br-Ph-, 4-Br-Ph-, 2-I-Ph-, 3-I-Ph, 4-I-Ph-, 2,(3,4,5 or 6)-F.sub.2-Ph-, 2,(3,4,5 or 6)-Cl.sub.2-Ph-, 2,(3,4,5 or 6)-Br.sub.2-Ph-, 2,(3,4,5 or 6)4.sub.2-Ph-, 2,(3,4,5 or 6)-Me.sub.2-Ph-, 2,(3,4,5 or 6)-Et.sub.2-Ph-, 2,(3,4,5 or 6)-Pr.sub.2-Ph-, 2,(3,4,5 or 6)-Bu.sub.2-Ph-, 2,(3,4,5 or 6)-(CN).sub.2-Ph-, 2,(3,4,5 or 6)-(NO.sub.2).sub.2-Ph-, 2,(3,4,5 or 6)-(NH.sub.2).sub.2-Ph-, 2,(3,4,5 or 6)-(MeO).sub.2-Ph-, 2,(3,4,5 or 6)-(CF.sub.3).sub.2-Ph-, 3,(4 or 5)-F.sub.2-Ph-, 3,(4 or 5)-Cl.sub.2-Ph-, 3,(4 or 5)-Br.sub.2-Ph-, 3,(4 or 5)-I.sub.2-Ph-, 3,(4 or 5)-Me.sub.2-Ph-, 3,(4 or 5)-Et.sub.2-Ph-, 3,(4 or 5)-Pr.sub.2-Ph-, 3,(4 or 5)-Bu.sub.2-Ph-, 3,(4 or 5)-(CN).sub.2-Ph-, 3,(4 or 5)-(NO.sub.2).sub.2-Ph-, 3,(4 or 5)-(NH.sub.2).sub.2-Ph-, 3,(4 or 5)-(MeO).sub.2-Ph-, 3,(4 or 5)-(CF.sub.3).sub.2-Ph-, 2-Me-Ph-, 3-Me-Ph-, 4-Me-Ph-, 2-Et-Ph-, 3-Et-Ph-, 4-Et-Ph-, 2-Pr-Ph-, 3-Pr-Ph-, 4-Pr-Ph-, 2-Bu-Ph-, 3-Bu-Ph-, 4-Bu-Ph-, 2-(CN)-Ph-, 3-(CN)-Ph-, 4-(CN)-Ph-, 2-(NO.sub.2)-Ph-, 3-(NO.sub.2)-Ph-, 4-(NO.sub.2)-Ph-, 2-(NH.sub.2)-Ph-, 3-(NH.sub.2)-Ph-, 4-(NH.sub.2)-Ph-, 2-MeO-Ph-, 3-MeO-Ph-, 4-MeO-Ph-, 2-(NH.sub.2CO)-Ph-, 3-(NH.sub.2CO)-Ph-, 4-(NH.sub.2CO)-Ph-, 2-CF.sub.3-Ph-, 3-CF.sub.3-Ph-, 4-CF.sub.3-Ph-, 2-CF.sub.3O-Ph-, 3-CF.sub.3O-Ph-, and 4-CF.sub.3O-Ph-);

(75) a substituted or unsubstituted saturated or unsaturated heterocyclic group such as an aromatic heterocyclic group (such as pyridin-2-yl, pyridin-3-yl, pyridin-4-yl, thiophen-2-yl, thiophen-3-yl, pyrimidin-2-yl, pyrimidin-4-yl, pyrimidin-5-yl, pyrimidin-6-yl, tetrazole-1yl, tetrazole-2-yl, tetrazole-5-yl, oxazol-2-yl, oxazol-4-yl, oxazol-5-yl, isoxazol-3-yl, isoxazol-4-yl, isoxazol-5-yl, (1,3,4-oxadiazol)-2-yl, (1,3,4-oxadiazol)-4-yl, (1,3,4-oxadiazol)-5-yl, thiazol-2-yl, thiazol-4-yl, thiazol-5-yl, furan-2-yl, and furan-3-yl); or such as a substituted or unsubstituted saturated heterocyclic group (such as piperidin-2-yl, piperidin-3-yl, piperidin-4-yl, piperazin-1-yl, piperazin-2-yl, piperazin-3-yl, tetrahydrofuran-2-yl, and tetrahydrofuran-3-yl, tetrahydropyran-2-yl, tetrahydropyran-3-yl, tetrahydropyran-4-yl); and

(76) a group where R.sup.63 and R.sup.64 together form a 3-6 membered substituted or unsubstituted saturated or unsaturated carbocyclic or heterocyclic ring (such as a cyclopropyl, cyclobutyl, cyclopentyl, cyclopentenyl, cyclohexyl, cyclohexenyl, aziridine, azetidine, pyrrolidine, piperidine, piperazine, oxetane, tetrahydrofuran or tetrahydropyran ring);

(77) and further preferably one of R.sup.63 and R.sup.64 is not H.

(78) In any of the embodiments herein, and in particular in the preferred and more preferred embodiments described above, it is still more preferred that R.sup.1, R.sup.3, and R.sup.4 are each independently selected from H and F, most preferably H; and/or R.sup.2 is selected from Cl, Br, CN, OMe and OEt; and/or and R.sup.7 is H; and/or R.sup.5 and R.sup.61 are selected from H and C.sub.1-C.sub.6 alkyl, most preferably R.sup.5 and R.sup.61 are both H; and/or R.sup.65 is selected from a substituted or unsubstituted phenyl group, a substituted or unsubstituted pyrazol-4-yl group, a substituted or unsubstituted oxazol-4-yl group, and a substituted or unsubstituted isoxazol-3-yl group; and/or R.sup.63 and R.sup.64 are selected from groups in which R.sup.63 and R.sup.64 together form a 3-6 membered substituted or unsubstituted saturated or unsaturated carbocyclic or heterocyclic ring (such as a cyclopropyl, cyclobutyl, cyclopentyl, cyclopentenyl, cyclohexyl, cyclohexenyl, aziridine, azetidine, pyrrolidine, piperidine, piperazine, oxetane, tetrahydrofuran or tetrahydropyran ring). Furthermore, in certain of these more preferred embodiments R.sup.7 is H. Furthermore, in certain of these more preferred embodiments R.sup.5 is H. Still further, in these more preferred embodiments, R.sup.2 and R.sup.3 are both not H, or R.sup.2 is not H and R.sup.3 is H, or R.sup.3 is not H and R.sup.2 is H.

(79) Some of the more preferred of the R substituents have been discussed above. However, the R substituents referred to in all of the compounds and structures herein will now be described generally and in more detail.

(80) Typically, as has been described, the R substituents in any of the compounds herein, unless otherwise specified, are selected from H and an organic group, and may themselves be substituted or unsubstituted. An organic group may be any group common to organic chemistry, and has already been defined in detail above. In typical embodiments, where present R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.61, R.sup.62, R.sup.63, R.sup.64, R.sup.65 and R.sup.66 are each the same or different, and in some embodiments adjacent and/or proximal groups may form rings, as already mentioned above in detail in respect of R.sup.1-R.sup.7, although in the case of R.sup.5 and R.sup.7 it is preferred if R.sup.5 and R.sup.7 do not form rings and do not comprise rings. For the avoidance of doubt, in any of the compounds herein R.sup.61 may form a ring with an R.sup.66 or with R.sup.63, R.sup.64 or R.sup.65. Similarly R.sup.63 may form a ring with R.sup.64 or R.sup.65, and R.sup.64 may for a ring with R.sup.65. In addition, R.sup.66 may form a ring with another R.sup.66.

(81) In more typical embodiments R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are independently selected from H and a group selected from the following groups:

(82) a halogen (such as F, Cl, Br and I);

(83) a CN group;

(84) a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 alkyl group (such as methyl (Me), ethyl (Et), propyl (Pr), iso-propyl (i-Pr), n-butyl (n-Bu), iso-butyl (i-Bu), tert-butyl (t-Bu), pentyl and hexyl);

(85) a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 alkyl-aryl group (such as CH.sub.2Ph, CH.sub.2(2,3 or 4)F-Ph, CH.sub.2(2,3 or 4)Cl-Ph, CH.sub.2(2,3 or 4)Br-Ph, CH.sub.2(2,3 or 4)I-Ph, CH.sub.2CH.sub.2Ph, CH.sub.2CH.sub.2CH.sub.2Ph, CH.sub.2CH.sub.2CH.sub.2CH.sub.2Ph, CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2Ph, and CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2Ph);

(86) a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 halogenated alkyl group (such as CH.sub.2F, CHF.sub.2, CH.sub.2Cl, CH.sub.2Br, CH.sub.2I, CF.sub.3, CCl.sub.3, CBr.sub.3, CI.sub.3, CH.sub.2CF.sub.3, CH.sub.2CCl.sub.3, CH.sub.2CBr.sub.3, and CH.sub.2CI.sub.3);

(87) an NH.sub.2 group or a substituted or unsubstituted linear or branched primary secondary or tertiary C.sub.1-C.sub.6 amine group (such as NMeH, NMe.sub.2, NEtH, NEtMe, NEt.sub.2, NPrH, NPrMe, NPrEt, NPr.sub.2, NBuH, NBuMe, NBuEt, CH.sub.2NH.sub.2, CH.sub.2NMeH, CH.sub.2NMe.sub.2, CH.sub.2NEtH, CH.sub.2NEtMe, CH.sub.2NEt.sub.2, CH.sub.2NPrH, CH.sub.2NPrMe, and CH.sub.2NPrEt);

(88) a substituted or unsubstituted amino-aryl group (such as NH-Ph, NH-(2,3 or 4)F-Ph, NH-(2,3 or 4)Cl-Ph, NH-(2,3 or 4)Br-Ph, NH-(2,3 or 4)I-Ph, NH-(2,3 or 4)Me-Ph, NH-(2,3 or 4)Et-Ph, NH-(2,3 or 4)Pr-Ph, NH-(2,3 or 4)Bu-Ph, NH-(2,3 or 4)OMe-Ph, NH-(2,3 or 4)OEt-Ph, NH-(2,3 or 4)OPr-Ph, NH-(2,3 or 4)OBu-Ph, NH-2,(3,4,5 or 6)F.sub.2-Ph, NH-2,(3,4,5 or 6)Cl.sub.2-Ph, NH-2,(3,4,5 or 6)Br.sub.2-Ph, NH-2,(3,4,5 or 6)I.sub.2-Ph, NH-2,(3,4,5 or 6)Me.sub.2-Ph, NH-2,(3,4,5 or 6)Et.sub.2-Ph, NH-2,(3,4,5, or 6)Pr.sub.2-Ph, NH-2,(3,4,5 or 6)Bu.sub.2-Ph;

(89) a substituted or unsubstituted cyclic amine or amido group (such as pyrrolidin-1-yl, pyrrolidin-2-yl, pyrrolidin-3-yl, piperidin-1-yl, piperidin-2-yl, piperidin-3-yl, piperidin-4-yl, piperazin-1-yl, piperazin-2-yl, piperazin-3-yl, morpholin-2-yl, morpholin-3-yl, morpholin-4-yl, 2-keto-pyrrolidinyl, 3-keto-pyrrolidinyl, 2-keto-piperidinyl, 3-keto-piperidinyl 4-keto-piperidinyl), 2-keto-piperazinyl, and 3-keto-piperazinyl;

(90) a substituted or unsubstituted cyclic C.sub.3-C.sub.8 alkyl group (such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl and cyclooctyl);

(91) an OH group or a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 alcohol group (such as CH.sub.2OH, CH.sub.2CH.sub.2OH, CH.sub.2CH.sub.2CH.sub.2OH, CH(CH.sub.3)CH.sub.2OH, C(CH.sub.3).sub.2OH, CH.sub.2CH.sub.2CH.sub.2CH.sub.2OH, CH(CH.sub.3)CH.sub.2CH.sub.2OH, CH(CH.sub.3)CH(CH.sub.3)OH, CH(CH.sub.2CH.sub.3)CH.sub.2OH, C(CH.sub.3).sub.2CH.sub.2OH, CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2OH, and CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2OH);

(92) a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 carboxylic acid group (such as COOH, CH.sub.2COOH, CH.sub.2CH.sub.2COOH, CH.sub.2CH.sub.2CH.sub.2COOH, CH.sub.2CH.sub.2CH.sub.2CH.sub.2COOH, and CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2COOH);

(93) a substituted or unsubstituted linear or branched carbonyl group (such as (CO)Me, (CO)Et, (CO)Pr, (CO)iPr, (CO)nBu, (CO)iBu, (CO)tBu, (CO)Ph, (CO)CH.sub.2Ph, (CO)CH.sub.2OH, (CO)CH.sub.2OCH.sub.3, (CO)CH.sub.2NH.sub.2, (CO)CH.sub.2NHMe, (CO)CH.sub.2NMe.sub.2, (CO)-cyclopropyl, (CO)-1,3-epoxypropan-2-yl; (CO)NH.sub.2, (CO)NHMe, (CO)NMe.sub.2, (CO)NHEt, (CO)NEt.sub.2, (CO)-pyrollidine-N-yl, (CO)-morpholine-N-yl, (CO)-piperazine-N-yl, (CO)N-methyl-piperazine-N-yl, (CO)NHCH.sub.2CH.sub.2OH, (CO)NHCH.sub.2CH.sub.2OMe, (CO)NHCH.sub.2CH.sub.2NH.sub.2, (CO)NHCH.sub.2CH.sub.2NHMe, and (CO)NHCH.sub.2CH.sub.2NMe.sub.2;

(94) a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 carboxylic acid ester group (such as COOMe, COOEt, COOPr, COO-i-Pr, COO-n-Bu, COO-i-Bu, COO-t-Bu, CH.sub.2COOMe, CH.sub.2CH.sub.2COOMe, CH.sub.2CH.sub.2CH.sub.2COOMe, and CH.sub.2CH.sub.2CH.sub.2CH.sub.2COOMe);

(95) a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 amide group (such as CONH.sub.2, CONMeH, CONMe.sub.2, CONEtH, CONEtMe, CO-NEt.sub.2, CONPrH, CONPrMe, and CONPrEt);

(96) a substituted or unsubstituted linear or branched C.sub.1-C.sub.7 amino carbonyl group (such as NHCO-Me, NHCO-Et, NHCO-Pr, NHCO-Bu, NHCO-pentyl, NHCO-hexyl, NHCO-Ph, NMe-CO-Me, NMe-CO-Et, NMe-CO-Pr, NMe-CO-Bu, NMe-CO-pentyl, NMe-CO-hexyl, NMe-CO-Ph;

(97) a substituted or unsubstituted linear or branched C.sub.1-C.sub.7 alkoxy or aryloxy group (such as OMe, OEt, OPr, O-i-Pr, O-n-Bu, O-i-Bu, O-t-Bu, O-pentyl, O-hexyl, OCH.sub.2F, OCHF.sub.2, OCF.sub.3, OCH.sub.2Cl, OCHCl.sub.2, OCCl.sub.3, O-Ph, OCH.sub.2-Ph, OCH.sub.2-(2,3 or 4)-F-Ph, OCH.sub.2-(2,3 or 4)-Cl-Ph, CH.sub.2OMe, CH.sub.2OEt, CH.sub.2OPr, CH.sub.2OBu, CH.sub.2CH.sub.2OMe, CH.sub.2CH.sub.2CH.sub.2OMe, CH.sub.2CH.sub.2CH.sub.2CH.sub.2OMe, and CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2OMe);

(98) a substituted or unsubstituted linear or branched aminoalkoxy group (such as OCH.sub.2CH.sub.2NH.sub.2, OCH.sub.2CH.sub.2NHMe, OCH.sub.2CH.sub.2NMe.sub.2, OCH.sub.2CH.sub.2NHEt, and OCH.sub.2CH.sub.2NEt.sub.2;

(99) a substituted or unsubstituted linear or branched sulphonyl group (such as SO.sub.2Me, SO.sub.2Et, SO.sub.2Pr, SO.sub.2iPr, SO.sub.2Ph, SO.sub.2-(2,3 or 4)-F-Ph, SO.sub.2-cyclopropyl, SO.sub.2CH.sub.2CH.sub.2OCH.sub.3;

(100) a substituted or unsubstituted linear or branched sulphonylamino group (such as SO.sub.2NH.sub.2, SO.sub.2NHMe, SO.sub.2NMe.sub.2, SO.sub.2NHEt, SO.sub.2NEt.sub.2, SO.sub.2-pyrrolidine-N-yl, SO.sub.2-morpholine-N-yl, SO.sub.2NHCH.sub.2OMe, and SO.sub.2NHCH.sub.2CH.sub.2OMe);

(101) a substituted or unsubstituted linear or branched aminosulphonyl group (such as NHSO.sub.2Me, NHSO.sub.2Et, NHSO.sub.2Pr, NHSO.sub.2iPr, NHSO.sub.2Ph, NHSO.sub.2-(2,3 or 4)-F-Ph, NHSO.sub.2-cyclopropyl, NHSO.sub.2CH.sub.2CH.sub.2OCH.sub.3);

(102) a substituted or unsubstituted cyclic aminosulphonyl-group (such as N(SO.sub.2)(CH.sub.2).sub.3 and N(SO.sub.2)(CH.sub.2).sub.4);

(103) a substituted or unsubstituted aromatic group (such as Ph-, 2-F-Ph-, 3-F-Ph-, 4-F-Ph-, 2-Cl-Ph-, 3-Cl-Ph-, 4-Cl-Ph-, 2-Br-Ph-, 3-Br-Ph-, 4-Br-Ph-, 2-I-Ph-, 3-I-Ph, 4-I-Ph-, 2,(3,4,5 or 6)-F.sub.2-Ph-, 2,(3,4,5 or 6)-Cl.sub.2-Ph-, 2,(3,4,5 or 6)-Br.sub.2-Ph-, 2,(3,4,5 or 6)-I.sub.2-Ph-, 2,(3,4,5 or 6)-Me.sub.2-Ph-, 2,(3,4,5 or 6)-Et.sub.2-Ph-, 2,(3,4,5 or 6)-Pr.sub.2-Ph-, 2,(3,4,5 or 6)-Bu.sub.2-Ph-, 2,(3,4,5 or 6)-(CN).sub.2-Ph-, 2,(3,4,5 or 6)-(NO.sub.2).sub.2-Ph-, 2,(3,4,5 or 6)-(NH.sub.2).sub.2-Ph-, 2,(3,4,5 or 6)-(MeO).sub.2-Ph-, 2,(3,4,5 or 6)-(CF.sub.3).sub.2-Ph-, 3,(4 or 5)-F.sub.2-Ph-, 3,(4 or 5)-Cl.sub.2-Ph-, 3,(4 or 5)-Br.sub.2-Ph-, 3,(4 or 5)-I.sub.2-Ph-, 3,(4 or 5)-Me.sub.2-Ph-, 3,(4 or 5)-Et.sub.2-Ph-, 3,(4 or 5)-Pr.sub.2-Ph-, 3,(4 or 5)-Bu.sub.2-Ph-, 3,(4 or 5)-(CN).sub.2-Ph-, 3,(4 or 5)-(NO.sub.2).sub.2-Ph-, 3,(4 or 5)-(NH.sub.2)2-Ph-, 3,(4 or 5)-(MeO).sub.2-Ph-, 3,(4 or 5)-(CF.sub.3).sub.2-Ph-, 2-Me-Ph-, 3-Me-Ph-, 4-Me-Ph-, 2-Et-Ph-, 3-Et-Ph-, 4-Et-Ph-, 2-Pr-Ph-, 3-Pr-Ph-, 4-Pr-Ph-, 2-Bu-Ph-, 3-Bu-Ph-, 4-Bu-Ph-, 2-(CN)-Ph-, 3-(CN)-Ph-, 4-(CN)-Ph-, 2-(NO.sub.2)-Ph-, 3-(NO.sub.2)-Ph-, 4-(NO.sub.2)-Ph-, 2-(NH.sub.2)-Ph-, 3-(NH.sub.2)-Ph-, 4-(NH.sub.2)-Ph-, 2-MeO-Ph-, 3-MeO-Ph-, 4-MeO-Ph-, 2-(NH.sub.2CO)-Ph-, 3-(NH.sub.2CO)-Ph-, 4-(NH.sub.2CO)-Ph-, 2-CF.sub.3-Ph-, 3-CF.sub.3-Ph-, 4-CF.sub.3-Ph-, 2-CF.sub.3O-Ph-, 3-CF.sub.3O-Ph-, and 4-CF.sub.3O-Ph-);

(104) a saturated or unsaturated, substituted or unsubstituted, heterocyclic group including an aromatic heterocyclic group and/or a non-aromatic heterocyclic group (such as pyrrole-1-yl, pyrrole-2-yl, pyrrole-3-yl, pyrazole-1-yl, pyrazole-3-yl, pyrazole-4-yl, pyrazole-5-yl, imidazole-1-yl, imidazole-2-yl, imidazole-4-yl, imidazole-5-yl, 1,2,3-triazole-1-yl, 1,2,3-triazole-4-yl, 1,2,3-triazole-5-yl, 1,2,4-triazole-1-yl, 1,2,4-triazole-3-yl, 1,2,4-triazole-5-yl, pyridin-2-yl, pyridin-3-yl, pyridin-4-yl, pyridazine-3-yl, pyridazine-4-yl, pyrimidin-2-yl, pyrimidin-4-yl, pyrimidin-5-yl, pyrimidin-6-yl, pyrazine-2-yl, pyrrolidine-1-yl, pyrrolidine-2-yl, pyrrolidine-3-yl, piperidine-1-yl, piperidine-2-yl, piperidine-3-yl, piperidine-4-yl, 2-azapiperidine-1-yl, 2-azapiperidine-3-yl, 2-azapiperidine-4-yl, 3-azapiperidine-1-yl, 3-azapiperidine-2-yl, 3-azapiperidine-4-yl, 3-azapiperidine-5-yl, piperazine-1-yl, piperazine-2-yl, furan-2-yl, furan-3-yl, pyran-2-yl, pyran-3-yl, pyran-4-yl, 2-azapyran-2-yl, 2-azapyran-3-yl, 2-azapyran-4-yl, 2-azapyran-5-yl, 2-azapyran-6-yl, 3-azapyran-2-yl, 3-azapyran-4-yl, 3-azapyran-5-yl, 3-azapyran-6-yl, 4-azapyran-2-yl, 4-azapyran-3-yl, 4-azapyran-4-yl, 4-azapyran-5-yl, 4-azapyran-6-yl, tetrahydrofuran-2-yl, tetrahydrofuran-3-yl, 2-aza-tetrahydrofuran-2-yl, 2-aza-tetrahydrofuran-3-yl, 2-aza-tetrahydrofuran-4-yl, 2-aza-tetrahydrofuran-5-yl, 3-aza-tetrahydrofuran-2-yl, 3-aza-tetrahydrofuran-3-yl, 3-aza-tetrahydrofuran-4-yl, 3-aza-tetrahydrofuran-5-yl, tetrahydropyran-2-yl, tetrahydropyran-3-yl, tetrahydropyran-4-yl, 2-aza-tetrahydropyran-2-yl, 2-aza-tetrahydropyran-3-yl, 2-aza-tetrahydropyran-4-yl, 2-aza-tetrahydropyran-5-yl, 2-aza-tetrahydropyran-6-yl, 3-aza-tetrahydropyran-2-yl, 3-aza-tetrahydropyran-3-yl, 3-aza-tetrahydropyran-4-yl, 3-aza-tetrahydropyran-5-yl, 3-aza-tetrahydropyran-6-yl, morpholine-2-yl, morpholine-3-yl, morpholine-4-yl, thiophen-2-yl, thiophen-3-yl, isothiazole-3-yl, isothiazole-4-yl, isothiazole-5-yl, thiazole-2-yl, thiazole-4-yl, thiazole-5-yl, thiopyran-2-yl, thiopyran-3-yl, thiopyran-4-yl, 2-azathiopyran-2-yl, 2-azathiopyran-3-yl, 2-azathiopyran-4-yl, 2-azathiopyran-5-yl, 2-azathiopyran-6-yl, 3-azathiopyran-2-yl, 3-azathiopyran-4-yl, 3-azathiopyran-5-yl, 3-azathiopyran-6-yl, 4-azathiopyran-2-yl, 4-azathiopyran-3-yl, 4-azathiopyran-4-yl, 4-azathiopyran-5-yl, 4-azathiopyran-6-yl, thiolane-2-yl, thiolane-3-yl, thiane-2-yl, thiane-3-yl, thiane-4-yl, oxazol-2-yl, oxazol-4-yl, oxazol-5-yl, isoxazol-3-yl, isoxazol-4-yl, isoxazol-5-yl, furazan-3-yl, (1,3,4-oxadiazol)-2-yl, (1,3,4-oxadiazol)-5-yl, (1,2,4-oxadiazol)-3-yl, (1,2,4-oxadiazol)-5-yl; and tetrazole-1-yl, tetrazole-2-yl, tetrazole-5-yl);

(105) fused ring systems comprising two or three or more fused rings, which rings may be substituted or unsubstituted, preferably wherein the rings are selected from one, two, or more of the above aromatic groups and aromatic or non-aromatic heterocyclic groups, (e.g. fused ring systems such as naphthalene, anthracene, phenanthrene, phenalene, biphenylene, pentalene, indene, as-indacene, s-indacene, acenaphthylene, fluorene, fluoranthene, acephenanthrylene, azulene, heptalene, indole, indazole, benzimidazole, 4-azaindole, 5-azaindole, 6-azaindole, 7-azaindole, isoindole, 4-azaisoindole, 5-azaisoindole, 6-azaisoindole, 7-azaisoindole, indolizine, 1-azaindolizine, 2-azaindolizine, 3-azaindolizine, 5-azaindolizine, 6-azaindolizine, 7-azaindolizine, 8-azaindolizine, 9-azaindolizine, purine, carbazole, carboline, benzofuran, isobenzofuran, benzothiophene, isobenzothiophene, quinoline, cinnoline, quinazoline, quinoxaline, 5-azaquinoline, 6-azaquinoline, 7-azaquinoline, naphthyridine, isoquinoline, phthalazine, 6-azaisoquinoline, 7-azaisoquinoline, pteridine, chromene, isochromene, acridine, phenanthridine, perimidine, phenanthroline, phenoxazine, xanthene, phenoxanthiin, and/or thianthrene); and

(106) where there are two R groups attached to the same atom, they may together form a group which is double bonded to that atom, (such as a carbonyl group (O) or an alkene group (C(R).sub.2) wherein each R group is the same or different and is H or an organic group, preferably H or a straight or branched C.sub.1-C.sub.6 alkyl group).

(107) In more typical embodiments R.sup.7 is independently selected from H and a group selected from the following groups:

(108) a halogen (such as F, Cl, Br and I);

(109) a CN group;

(110) a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 alkyl group (such as methyl (Me), ethyl (Et), propyl (Pr), iso-propyl (i-Pr), n-butyl (n-Bu), iso-butyl (i-Bu), tert-butyl (t-Bu), pentyl and hexyl);

(111) a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 alkyl-aryl group (such as CH.sub.2Ph, CH.sub.2(2,3 or 4)F-Ph, CH.sub.2(2,3 or 4)Cl-Ph, CH.sub.2(2,3 or 4)Br-Ph, CH.sub.2(2,3 or 4)I-Ph, CH.sub.2CH.sub.2Ph, CH.sub.2CH.sub.2CH.sub.2Ph, CH.sub.2CH.sub.2CH.sub.2CH.sub.2Ph, CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2Ph, and CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2Ph);

(112) a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 halogenated alkyl group (such as CH.sub.2F, CHF.sub.2, CH.sub.2Cl, CH.sub.2Br, CH.sub.2I, CF.sub.3, CCl.sub.3, CBr.sub.3, CI.sub.3, CH.sub.2CF.sub.3, CH.sub.2CCl.sub.3, CH.sub.2CBr.sub.3, and CH.sub.2CI.sub.3);

(113) an NH.sub.2 group or a substituted or unsubstituted linear or branched primary secondary or tertiary C.sub.1-C.sub.6 amine group (such as NMeH, NMe.sub.2, NEtH, NEtMe, NEt.sub.2, NPrH, NPrMe, NPrEt, NPr.sub.2, NBuH, NBuMe, NBuEt, CH.sub.2NH.sub.2, CH.sub.2NMeH, CH.sub.2NMe.sub.2, CH.sub.2NEtH, CH.sub.2NEtMe, CH.sub.2NEt.sub.2, CH.sub.2NPrH, CH.sub.2NPrMe, and CH.sub.2NPrEt);

(114) a amino-aryl group (such as NH-Ph, NH-(2,3 or 4)F-Ph, NH-(2,3 or 4)Cl-Ph, NH-(2,3 or 4)Br-Ph, NH-(2,3 or 4)I-Ph, NH-(2,3 or 4)Me-Ph, NH-(2,3 or 4)Et-Ph, NH-(2,3 or 4)Pr-Ph, NH-(2,3 or 4)Bu-Ph, NH-(2,3 or 4)OMe-Ph, NH-(2,3 or 4)OEt-Ph, NH-(2,3 or 4)OPr-Ph, NH-(2,3 or 4)OBu-Ph, NH-2,(3,4,5 or 6)F.sub.2-Ph, NH-2,(3,4,5 or 6)Cl.sub.2-Ph, NH-2,(3,4,5 or 6)Br.sub.2-Ph, NH-2,(3,4,5 or 6)I.sub.2-Ph, NH-2,(3,4,5 or 6)Me.sub.2-Ph, NH-2,(3,4,5 or 6)Et.sub.2-Ph, NH-2,(3,4,5, or 6)Pr.sub.2-Ph, NH-2,(3,4,5 or 6)Bu.sub.2-Ph;

(115) an OH group or a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 alcohol group (such as CH.sub.2OH, CH.sub.2CH.sub.2OH, CH.sub.2CH.sub.2CH.sub.2OH, CH(CH.sub.3)CH.sub.2OH, C(CH.sub.3).sub.2OH, CH.sub.2CH.sub.2CH.sub.2CH.sub.2OH, CH(CH.sub.3)CH.sub.2CH.sub.2OH, CH(CH.sub.3)CH(CH.sub.3)OH, CH(CH.sub.2CH.sub.3)CH.sub.2OH, C(CH.sub.3).sub.2CH.sub.2OH, CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2OH, and CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2OH);

(116) a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 carboxylic acid group (such as COOH, CH.sub.2COOH, CH.sub.2CH.sub.2COOH, CH.sub.2CH.sub.2CH.sub.2COOH, CH.sub.2CH.sub.2CH.sub.2CH.sub.2COOH, and CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2COOH);

(117) a substituted or unsubstituted linear or branched carbonyl group (such as (CO)Me, (CO)Et, (CO)Pr, (CO)iPr, (CO)nBu, (CO)iBu, (CO)tBu, (CO)Ph, (CO)CH.sub.2Ph, (CO)CH.sub.2OH, (CO)CH.sub.2OCH.sub.3, (CO)CH.sub.2NH.sub.2, (CO)CH.sub.2NHMe, (CO)CH.sub.2NMe.sub.2, (CO)-cyclopropyl, (CO)-1,3-epoxypropan-2-yl; (CO)NH.sub.2, (CO)NHMe, (CO)NMe.sub.2, (CO)NHEt, (CO)NEt.sub.2, (CO)-pyrollidine-N-yl, (CO)-morpholine-N-yl, (CO)-piperazine-N-yl, (CO)N-methyl-piperazine-N-yl, (CO)NHCH.sub.2CH.sub.2OH, (CO)NHCH.sub.2CH.sub.2OMe, (CO)NHCH.sub.2CH.sub.2NH.sub.2, (CO)NHCH.sub.2CH.sub.2NHMe, and (CO)NHCH.sub.2CH.sub.2NMe.sub.2;

(118) a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 carboxylic acid ester group (such as COOMe, COOEt, COOPr, COO-i-Pr, COO-n-Bu, COO-i-Bu, COO-t-Bu, CH.sub.2COOMe, CH.sub.2CH.sub.2COOMe, CH.sub.2CH.sub.2CH.sub.2COOMe, and CH.sub.2CH.sub.2CH.sub.2CH.sub.2COOMe);

(119) a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 amide group (such as CONH.sub.2, CONMeH, CONMe.sub.2, CONEtH, CONEtMe, CONEt.sub.2, CONPrH, CONPrMe, and CONPrEt);

(120) a substituted or unsubstituted linear or branched C.sub.1-C.sub.7 amino carbonyl group (such as NHCO-Me, NHCO-Et, NHCO-Pr, NHCO-Bu, NHCO-pentyl, NHCO-hexyl, NHCO-Ph, NMe-CO-Me, NMe-CO-Et, NMe-CO-Pr, NMe-CO-Bu, NMe-CO-pentyl, NMe-CO-hexyl, NMe-CO-Ph;

(121) a substituted or unsubstituted linear or branched C.sub.1-C.sub.7 alkoxy or aryloxy group (such as OMe, OEt, OPr, O-i-Pr, O-n-Bu, O-i-Bu, O-t-Bu, O-pentyl, O-hexyl, OCH.sub.2F, OCHF.sub.2, OCF.sub.3, OCH.sub.2Cl, OCHCl.sub.2, OCCl.sub.3, O-Ph, OCH.sub.2-Ph, OCH.sub.2-(2,3 or 4)-F-Ph, OCH.sub.2-(2,3 or 4)-Cl-Ph, CH.sub.2OMe, CH.sub.2OEt, CH.sub.2OPr, CH.sub.2OBu, CH.sub.2CH.sub.2OMe, CH.sub.2CH.sub.2CH.sub.2OMe, CH.sub.2CH.sub.2CH.sub.2CH.sub.2OMe, and CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2OMe);

(122) a substituted or unsubstituted linear or branched aminoalkoxy group (such as OCH.sub.2CH.sub.2NH.sub.2, OCH.sub.2CH.sub.2NHMe, OCH.sub.2CH.sub.2NMe.sub.2, OCH.sub.2CH.sub.2NHEt, and OCH.sub.2CH.sub.2NEt.sub.2;

(123) a substituted or unsubstituted linera or branched sulphonyl group (such as SO.sub.2Me, SO.sub.2Et, SO.sub.2Pr, SO.sub.2iPr, SO.sub.2Ph, SO.sub.2-(2,3 or 4)-F-Ph, SO.sub.2-cyclopropyl, SO.sub.2CH.sub.2CH.sub.2OCH.sub.3;

(124) a substituted or unsubstituted linear or branched sulphonylamino group (such as SO.sub.2NH.sub.2, SO.sub.2NHMe, SO.sub.2NMe.sub.2, SO.sub.2NHEt, SO.sub.2NEt.sub.2, SO.sub.2-pyrrolidine-N-yl, SO.sub.2-morpholine-N-yl, SO.sub.2NHCH.sub.2OMe, and SO.sub.2NHCH.sub.2CH.sub.2OMe);

(125) a substituted or unsubstituted linear or branched aminosulphonyl group (such as NHSO.sub.2Me, NHSO.sub.2Et, NHSO.sub.2Pr, NHSO.sub.2iPr, NHSO.sub.2Ph, NHSO.sub.2-(2,3 or 4)-F-Ph, NHSO.sub.2-cyclopropyl, NHSO.sub.2CH.sub.2CH.sub.2OCH.sub.3).

(126) In more typical embodiments R.sup.1, R.sup.2, R.sup.3, R.sup.4, and R.sup.7 may be selected from more common small organic substituents. It is particularly preferred that at least one of R.sup.1, R.sup.2, R.sup.3, and R.sup.4 is not H. Thus, in certain embodiments R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.7 are independently selected from H and:

(127) a halogen such as F, Cl, Br and I, preferably F and Cl, (more preferably wherein R.sup.2 is selected from Cl and Br, and R.sup.1, R.sup.3, and R.sup.4 are selected from H and F);

(128) CN;

(129) a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 alkyl group such as such as methyl (Me), ethyl (Et), propyl (Pr), iso-propyl (i-Pr), cyclopropyl (cy-Pr), n-butyl (n-Bu), iso-butyl (i-Bu), tert-butyl (t-Bu), pentyl and hexyl, preferably -Me;

(130) a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 halogenated alkyl group (such as CH.sub.2F, CHF.sub.2, CH.sub.2Cl, CH.sub.2Br, CH.sub.2I, CF.sub.3, CCl.sub.3, CBr.sub.3, CI.sub.3, CH.sub.2CF.sub.3, CH.sub.2CCl.sub.3, CH.sub.2CBr.sub.3, and CH.sub.2CI.sub.3), preferably CF.sub.3; and

(131) a substituted or unsubstituted linear or branched C.sub.1-C.sub.7 alkoxy group (such as OMe, OEt, OPr, O-i-Pr, O-n-Bu, O-i-Bu, O-t-Bu, O-pentyl, O-hexyl, OCH.sub.2F, OCHF.sub.2, OCF.sub.3, OCH.sub.2Cl, OCHCl.sub.2, OCCl.sub.3, O-Ph, CH.sub.2OMe, CH.sub.2OEt, CH.sub.2OPr, CH.sub.2OBu, CH.sub.2CH.sub.2OMe, CH.sub.2CH.sub.2CH.sub.2OMe, CH.sub.2CH.sub.2CH.sub.2CH.sub.2OMe, and CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2OMe), preferably OMe or OEt.

(132) In these compounds, and the other compounds herein, in certain embodiments, when present R.sup.1 and R.sup.4 are both H, or R.sup.1 and R.sup.4 are both not H, or R.sup.1 is not H and R.sup.4 is H, or R.sup.4 is not H and R.sup.1 is H. Furthermore, in certain embodiments when present R.sup.7 is H. Furthermore, in certain embodiments when present R.sup.5 is H. Still further, in certain embodiments, where present R.sup.2 and R.sup.3 are both H, or R.sup.2 and R.sup.3 are both not H, or R.sup.2 is not H and R.sup.3 is H, or R.sup.3 is not H and R.sup.2 is H. In these and other embodiments, when one of these groups is not H it is more typically selected from F, Cl, Br, -Me, -MeO and CN. Still further, where present both R.sup.66 may be H or one R.sup.66 may be H or both R.sup.66 are not H. Where there are three or four R.sup.66 groups, all three or four may be H or one, two, three or four may be not H.

(133) In more typical embodiments R.sup.66, may be selected from more common small organic substituents. It is particularly preferred that R.sup.66 is selected from H and:

(134) F;

(135) a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 alkyl group such as such as methyl (Me), ethyl (Et), propyl (Pr), iso-propyl (i-Pr), cyclopropyl (cy-Pr), n-butyl (n-Bu), iso-butyl (i-Bu), tert-butyl (t-Bu), pentyl and hexyl, preferably -Me;

(136) an NH.sub.2 group or a substituted or unsubstituted linear or branched primary secondary or tertiary C.sub.1-C.sub.6 amine group (such as NMeH, NMe.sub.2, NEtH, NEtMe, NEt.sub.2, NPrH, NPrMe, NPrEt, NPr.sub.2, NBuH, NBuMe, NBuEt, CH.sub.2NH.sub.2, CH.sub.2NMeH, CH.sub.2NMe.sub.2, CH.sub.2NEtH, CH.sub.2NEtMe, CH.sub.2NEt.sub.2, CH.sub.2NPrH, CH.sub.2NPrMe, and CH.sub.2NPrEt);

(137) a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 halogenated alkyl group (such as CH.sub.2F, CHF.sub.2, CH.sub.2Cl, CH.sub.2Br, CH.sub.2I, CF.sub.3, CCl.sub.3, CBr.sub.3, CI.sub.3, CH.sub.2CF.sub.3, CH.sub.2CCl.sub.3, CH.sub.2CBr.sub.3, and CH.sub.2CI.sub.3), preferably CF.sub.3;

(138) a substituted or unsubstituted linear or branched C.sub.1-C.sub.7 alkoxy group (such as OMe, OEt, OPr, O-i-Pr, O-n-Bu, O-i-Bu, O-t-Bu, O-pentyl, O-hexyl, OCH.sub.2F, OCHF.sub.2, OCF.sub.3, OCH.sub.2Cl, OCHCl.sub.2, OCCl.sub.3, O-Ph, CH.sub.2OMe, CH.sub.2OEt, CH.sub.2OPr, CH.sub.2OBu, CH.sub.2CH.sub.2OMe, CH.sub.2CH.sub.2CH.sub.2OMe, CH.sub.2CH.sub.2CH.sub.2CH.sub.2OMe, and CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2OMe), preferably OMe; and

(139) where there are two R.sup.66 groups attached to the same atom, they may together form a group which is double bonded to that atom, (such as a carbonyl group (O) or an alkene group (C(R).sub.2) wherein each R group is the same or different and is H or an organic group, preferably H or a straight or branched C.sub.1-C.sub.6 alkyl group).

(140) In these compounds, and the other compounds herein, in certain embodiments, when present R.sub.1 and R.sup.4 are both H, or R.sub.1 and R.sup.4 are both not H, or R.sub.1 is not H and R.sup.4 is H, or R.sup.4 is not H and R.sub.1 is H. Furthermore, in certain embodiments when present R.sup.7 is H. Furthermore, in certain embodiments when present R.sup.5 is H. Still further, in certain embodiments, where present R.sup.2 and R.sup.3 are both H, or R.sup.2 and R.sup.3 are both not H, or R.sup.2 is not H and R.sup.3 is H, or R.sup.3 is not H and R.sup.2 is H. In these and other embodiments, when one of these groups is not H it is more typically selected from F, Cl, Br, -Me, -MeO, OEt and CN. Still further, where present both R.sup.66 may be H or one R.sup.66 may be H or both R.sup.66 are not H.

(141) In more typical embodiments R.sup.5 and R.sup.61 are groups attached to N atoms in the compounds of the invention. In preferred embodiments they are not large groups, nor do they contain hetero atoms attached directly to the N atom. They are typically selected from H and lower alkyl groups, or the like. Thus, in typical embodiments, R.sup.5 and R.sup.61 may be the same or different and may be independently selected from H and:

(142) a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 alkyl group (such as methyl (Me), ethyl (Et), propyl (Pr), iso-propyl (i-Pr), n-butyl (n-Bu), iso-butyl (i-Bu), tert-butyl (t-Bu), pentyl and hexyl);

(143) a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 halogenated alkyl group (such as CH.sub.2F, CHF.sub.2, CF.sub.3, CCl.sub.3, CBr.sub.3, Cl.sub.3, CH.sub.2CF.sub.3, CH.sub.2CCl.sub.3, CH.sub.2CBr.sub.3, and CH.sub.2CI.sub.3), preferably a linear or branched C.sub.1-C.sub.6 fluorinated alkyl group (such as CH.sub.2F, CHF.sub.2, CF.sub.3, CH.sub.2CH.sub.2F, CH.sub.2CHF.sub.2, and CH.sub.2CF.sub.3); and

(144) a substituted or unsubstituted linear or branched C.sub.2-C.sub.6 alcohol group (such as CH.sub.2CH.sub.2OH, CH.sub.2CH.sub.2CH.sub.2OH, CH(CH.sub.3)CH.sub.2OH, C(CH.sub.3).sub.2OH, CH.sub.2CH.sub.2CH.sub.2CH.sub.2OH, CH(CH.sub.3)CH.sub.2CH.sub.2OH, CH(CH.sub.3)CH(CH.sub.3)OH, CH(CH.sub.2CH.sub.3)CH.sub.2OH, C(CH.sub.3).sub.2CH.sub.2OH, CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2OH, and CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2OH).

(145) R.sup.61 may further be selected from a substituted or unsubstituted cyclic C.sub.3-C.sub.8 alkyl group (such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl and cyclooctyl).

(146) More preferably, R.sup.5 is H. Further (independently) preferably R.sup.61 is H. More preferably both R.sup.5 and R.sup.61 are H.

(147) In more typical embodiments R.sup.63, R.sup.64, and R.sup.65 are independently selected from H and a group selected from the following groups:

(148) a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 alkyl group (such as methyl (Me), ethyl (Et), propyl (Pr), iso-propyl (i-Pr), n-butyl (n-Bu), iso-butyl (i-Bu), tert-butyl (t-Bu), pentyl and hexyl);

(149) a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 alkyl-aryl group (such as CH.sub.2Ph, CH.sub.2(2,3 or 4)F-Ph, CH.sub.2(2,3 or 4)Cl-Ph, CH.sub.2(2,3 or 4)Br-Ph, CH.sub.2(2,3 or 4)I-Ph, CH.sub.2CH.sub.2Ph, CH.sub.2CH.sub.2CH.sub.2Ph, CH.sub.2CH.sub.2CH.sub.2CH.sub.2Ph, CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2Ph, and CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2Ph);

(150) a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 halogenated alkyl group (such as CH.sub.2F, CHF.sub.2, CH.sub.2Cl, CH.sub.2Br, CH.sub.2I, CF.sub.3, CCl.sub.3, CBr.sub.3, CI.sub.3, CH.sub.2CF.sub.3, CH.sub.2CCl.sub.3, CH.sub.2CBr.sub.3, and CH.sub.2CI.sub.3);

(151) an NH.sub.2 group or a substituted or unsubstituted linear or branched primary secondary or tertiary C.sub.1-C.sub.6 amine group (such as NMeH, NMe.sub.2, NEtH, NEtMe, NEt.sub.2, NPrH, NPrMe, NPrEt, NPr.sub.2, NBuH, NBuMe, NBuEt, CH.sub.2NH.sub.2, CH.sub.2NMeH, CH.sub.2NMe.sub.2, CH.sub.2NEtH, CH.sub.2NEtMe, CH.sub.2NEt.sub.2, CH.sub.2NPrH, CH.sub.2NPrMe, and CH.sub.2NPrEt);

(152) a substituted or unsubstituted cyclic amine or amido group (such as pyrrolidin-1-yl, pyrrolidin-2-yl, piperidin-1-yl, piperidin-2-yl, piperidin-3-yl, piperidin-4-yl, piperazin-1-yl, piperazin-2-yl, piperazin-3-yl, morpholin-2-yl, morpholin-3-yl, morpholin-4-yl, 2-keto-pyrrolidinyl, 3-keto-pyrrolidinyl, 2-keto-piperidinyl, 3-keto-piperidinyl, 4-keto-piperidinyl, 2-keto-piperazinyl, and 3-keto-piperazinyl);

(153) a substituted or unsubstituted cyclic C.sub.3-C.sub.8 alkyl group (such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl and cyclooctyl);

(154) an OH group or a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 alcohol group (such as CH.sub.2OH, CH.sub.2CH.sub.2OH, CH.sub.2CH.sub.2CH.sub.2OH, CH(CH.sub.3)CH.sub.2OH, C(CH.sub.3).sub.2OH, CH.sub.2CH.sub.2CH.sub.2CH.sub.2OH, CH(CH.sub.3)CH.sub.2CH.sub.2OH, CH(CH.sub.3)CH(CH.sub.3)OH, CH(CH.sub.2CH.sub.3)CH.sub.2OH, C(CH.sub.3).sub.2CH.sub.2OH, CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2OH, and CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2OH);

(155) a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 carboxylic acid group (such as COOH, CH.sub.2COOH, CH.sub.2CH.sub.2COOH, CH.sub.2CH.sub.2CH.sub.2COOH, CH.sub.2CH.sub.2CH.sub.2CH.sub.2COOH, and CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2COOH);

(156) a substituted or unsubstituted linear or branched carbonyl group (such as (CO)Me, (CO)Et, (CO)Pr, (CO)iPr, (CO)nBu, (CO)iBu, (CO)tBu, (CO)Ph, (CO)CH.sub.2Ph, (CO)CH.sub.2OH, (CO)CH.sub.2OCH.sub.3, (CO)CH.sub.2NH.sub.2, (CO)CH.sub.2NHMe, (CO)CH.sub.2NMe.sub.2, (CO)-cyclopropyl, (CO)-1,3-epoxypropan-2-yl; (CO)NH.sub.2, (CO)NHMe, (CO)NMe.sub.2, (CO)NHEt, (CO)NEt.sub.2, (CO)-pyrollidine-N-yl, (CO)-morpholine-N-yl, (CO)-piperazine-N-yl, (CO)N-methyl-piperazine-N-yl, (CO)NHCH.sub.2CH.sub.2OH, (CO)NHCH.sub.2CH.sub.2OMe, (CO)NHCH.sub.2CH.sub.2NH.sub.2, (CO)NHCH.sub.2CH.sub.2NHMe, and (CO)NHCH.sub.2CH.sub.2NMe.sub.2;

(157) a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 carboxylic acid ester group (such as COOMe, COOEt, COOPr, COO-i-Pr, COO-n-Bu, COO-i-Bu, COO-t-Bu, CH.sub.2COOMe, CH.sub.2CH.sub.2COOMe, CH.sub.2CH.sub.2CH.sub.2COOMe, and CH.sub.2CH.sub.2CH.sub.2CH.sub.2COOMe);

(158) a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 amide group (such as CONH.sub.2, CONMeH, CONMe.sub.2, CONEtH, CONEtMe, CONEt.sub.2, CONPrH, CONPrMe, and CONPrEt);

(159) a substituted or unsubstituted aromatic group (such as Ph-, 2-F-Ph-, 3-F-Ph-, 4-F-Ph-, 2-Cl-Ph-, 3-Cl-Ph-, 4-Cl-Ph-, 2-Br-Ph-, 3-Br-Ph-, 4-Br-Ph-, 2-I-Ph-, 3-I-Ph, 4-I-Ph-, 2,(3,4,5 or 6)-F.sub.2-Ph-, 2,(3,4,5 or 6)-Cl.sub.2-Ph-, 2,(3,4,5 or 6)-Br.sub.2-Ph-, 2,(3,4,5 or 6)-I.sub.2-Ph-, 2,(3,4,5 or 6)-Me.sub.2-Ph-, 2,(3,4,5 or 6)-Et.sub.2-Ph-, 2,(3,4,5 or 6)-Pr.sub.2-Ph-, 2,(3,4,5 or 6)-Bu.sub.2-Ph-, 2,(3,4,5 or 6)-(CN).sub.2-Ph-, 2,(3,4,5 or 6)-(NO.sub.2).sub.2-Ph-, 2,(3,4,5 or 6)-(NH.sub.2).sub.2-Ph-, 2,(3,4,5 or 6)-(MeO).sub.2-Ph-, 2,(3,4,5 or 6)-(CF.sub.3).sub.2-Ph-, 3,(4 or 5)-F.sub.2-Ph-, 3,(4 or 5)-Cl.sub.2-Ph-, 3,(4 or 5)-Br.sub.2-Ph-, 3,(4 or 5)-I.sub.2-Ph-, 3,(4 or 5)-Me.sub.2-Ph-, 3,(4 or 5)-Et.sub.2-Ph-, 3,(4 or 5)-Pr.sub.2-Ph-, 3,(4 or 5)-Bu.sub.2-Ph-, 3,(4 or 5)-(CN).sub.2-Ph-, 3,(4 or 5)-(NO.sub.2).sub.2-Ph-, 3,(4 or 5)-(NH.sub.2).sub.2-Ph-, 3,(4 or 5)-(MeO).sub.2-Ph-, 3,(4 or 5)-(CF.sub.3).sub.2-Ph-, 2-Me-Ph-, 3-Me-Ph-, 4-Me-Ph-, 2-Et-Ph-, 3-Et-Ph-, 4-Et-Ph-, 2-Pr-Ph-, 3-Pr-Ph-, 4-Pr-Ph-, 2-Bu-Ph-, 3-Bu-Ph-, 4-Bu-Ph-, 2-(CN)-Ph-, 3-(CN)-Ph-, 4-(CN)-Ph-, 2-(NO.sub.2)-Ph-, 3-(NO.sub.2)-Ph-, 4-(NO.sub.2)-Ph-, 2-(NH.sub.2)-Ph-, 3-(NH.sub.2)-Ph-, 4-(NH.sub.2)-Ph-, 2-MeO-Ph-, 3-MeO-Ph-, 4-MeO-Ph-, 2-(NH.sub.2CO)-Ph-, 3-(NH.sub.2CO)-Ph-, 4-(NH.sub.2CO)-Ph-, 2-CF.sub.3-Ph-, 3-CF.sub.3-Ph-, 4-CF.sub.3-Ph-, 2-CF.sub.3O-Ph-, 3-CF.sub.3O-Ph-, and 4-CF.sub.3O-Ph-);

(160) a saturated or unsaturated, substituted or unsubstituted, heterocyclic group including an aromatic heterocyclic group and/or a non-aromatic heterocyclic group (such as pyrrole-1-yl, pyrrole-2-yl, pyrrole-3-yl, pyrazole-1-yl, pyrazole-3-yl, pyrazole-4-yl, pyrazole-5-yl, imidazole-1-yl, imidazole-2-yl, imidazole-4-yl, imidazole-5-yl, 1,2,3-triazole-1-yl, 1,2,3-triazole-4-yl, 1,2,3-triazole-5-yl, 1,2,4-triazole-1-yl, 1,2,4-triazole-3-yl, 1,2,4-triazole-5-yl, pyridin-2-yl, pyridin-3-yl, pyridin-4-yl, pyridazine-3-yl, pyridazine-4-yl, pyrimidin-2-yl, pyrimidin-4-yl, pyrimidin-5-yl, pyrimidin-6-yl, pyrazine-2-yl, pyrrolidine-1-yl, pyrrolidine-2-yl, pyrrolidine-3-yl, piperidine-1-yl, piperidine-2-yl, piperidine-3-yl, piperidine-4-yl, 2-azapiperidine-1-yl, 2-azapiperidine-3-yl, 2-azapiperidine-4-yl, 3-azapiperidine-1-yl, 3-azapiperidine-2-yl, 3-azapiperidine-4-yl, 3-azapiperidine-5-yl, piperazine-1-yl, piperazine-2-yl, furan-2-yl, furan-3-yl, pyran-2-yl, pyran-3-yl, pyran-4-yl, 2-azapyran-2-yl, 2-azapyran-3-yl, 2-azapyran-4-yl, 2-azapyran-5-yl, 2-azapyran-6-yl, 3-azapyran-2-yl, 3-azapyran-4-yl, 3-azapyran-5-yl, 3-azapyran-6-yl, 4-azapyran-2-yl, 4-azapyran-3-yl, 4-azapyran-4-yl, 4-azapyran-5-yl, 4-azapyran-6-yl, tetrahydrofuran-2-yl, tetrahydrofuran-3-yl, 2-aza-tetrahydrofuran-2-yl, 2-aza-tetrahydrofuran-3-yl, 2-aza-tetrahydrofuran-4-yl, 2-aza-tetrahydrofuran-5-yl, 3-aza-tetrahydrofuran-2-yl, 3-aza-tetrahydrofuran-3-yl, 3-aza-tetrahydrofuran-4-yl, 3-aza-tetrahydrofuran-5-yl, tetrahydropyran-2-yl, tetrahydropyran-3-yl, tetrahydropyran-4-yl, 2-aza-tetrahydropyran-2-yl, 2-aza-tetrahydropyran-3-yl, 2-aza-tetrahydropyran-4-yl, 2-aza-tetrahydropyran-5-yl, 2-aza-tetrahydropyran-6-yl, 3-aza-tetrahydropyran-2-yl, 3-aza-tetrahydropyran-3-yl, 3-aza-tetrahydropyran-4-yl, 3-aza-tetrahydropyran-5-yl, 3-aza-tetrahydropyran-6-yl, morpholine-2-yl, morpholine-3-yl, morpholine-4-yl, thiophen-2-yl, thiophen-3-yl, isothiazole-3-yl, isothiazole-4-yl, isothiazole-5-yl, thiazole-2-yl, thiazole-4-yl, thiazole-5-yl, thiopyran-2-yl, thiopyran-3-yl, thiopyran-4-yl, 2-azathiopyran-2-yl, 2-azathiopyran-3-yl, 2-azathiopyran-4-yl, 2-azathiopyran-5-yl, 2-azathiopyran-6-yl, 3-azathiopyran-2-yl, 3-azathiopyran-4-yl, 3-azathiopyran-5-yl, 3-azathiopyran-6-yl, 4-azathiopyran-2-yl, 4-azathiopyran-3-yl, 4-azathiopyran-4-yl, 4-azathiopyran-5-yl, 4-azathiopyran-6-yl, thiolane-2-yl, thiolane-3-yl, thiane-2-yl, thiane-3-yl, thiane-4-yl, oxazol-2-yl, oxazol-4-yl, oxazol-5-yl, isoxazol-3-yl, isoxazol-4-yl, isoxazol-5-yl, furazan-3-yl, (1,3,4-oxadiazol)-2-yl, (1,3,4-oxadiazol)-5-yl, (1,2,4-oxadiazol)-3-yl, (1,2,4-oxadiazol)-5-yl; and tetrazole-1-yl, tetrazole-2-yl, tetrazole-5-yl);

(161) fused ring systems comprising two or three or more fused rings, which rings may be substituted or unsubstituted, preferably wherein the rings are selected from one, two, or more of the above aromatic groups and aromatic or non-aromatic heterocyclic groups, (e.g. fused ring systems such as naphthalene, anthracene, phenanthrene, phenalene, biphenylene, pentalene, indene, as-indacene, s-indacene, acenaphthylene, fluorene, fluoranthene, acephenanthrylene, azulene, heptalene, indole, indazole, benzimidazole, 4-azaindole, 5-azaindole, 6-azaindole, 7-azaindole, isoindole, 4-azaisoindole, 5-azaisoindole, 6-azaisoindole, 7-azaisoindole, indolizine, 1-azaindolizine, 2-azaindolizine, 3-azaindolizine, 5-azaindolizine, 6-azaindolizine, 7-azaindolizine, 8-azaindolizine, 9-azaindolizine, purine, carbazole, carboline, benzofuran, isobenzofuran, benzothiophene, isobenzothiophene, quinoline, cinnoline, quinazoline, quinoxaline, 5-azaquinoline, 6-azaquinoline, 7-azaquinoline, naphthyridine, isoquinoline, phthalazine, 6-azaisoquinoline, 7-azaisoquinoline, pteridine, chromene, isochromene, acridine, phenanthridine, perimidine, phenanthroline, phenoxazine, xanthene, phenoxanthiin, and/or thianthrene); and

(162) R.sup.63 and R.sup.64 may together form a group which is double bonded to the carbon atom to which they are attached, (such as a carbonyl group (O) or an alkene group (C(R).sub.2) wherein each R group is the same or different and is H or an organic group, preferably H or a straight or branched C.sub.1-C.sub.6 alkyl group).

(163) Whilst in some embodiments R.sup.65 may be H or an organic group, or the more typical groups described above, in preferred embodiments R.sup.65 is selected from: a substituted or unsubstituted, straight or branched chain organic group; and a substituted or unsubstituted cyclic organic group. More typically R.sup.65 comprises a cyclic group. Accordingly, R.sup.65 may be selected from: a substituted or unsubstituted, saturated or unsaturated, aliphatic cyclic group; a substituted or unsubstituted, aromatic cyclic group; a substituted or unsubstituted, saturated or unsaturated, non-aromatic or aromatic, heterocyclic group; and fused ring systems comprising two or more fused rings selected from one or more of the above.

(164) In certain embodiments R.sup.65 is selected from:

(165) a substituted or unsubstituted cyclic amine or amido group (such as pyrrolidin-1-yl, pyrrolidin-2-yl, pyrrolidin-3-yl, piperidin-1-yl, piperidin-2-yl, piperidin-3-yl, piperidin-4-yl, piperazin-1-yl, piperazin-2-yl, piperazin-3-yl, morpholin-2-yl, morpholin-3-yl, morpholin-4-yl, 2-keto-pyrrolidinyl, 3-keto-pyrrolidinyl, 2-keto-piperidinyl, 3-keto-piperidinyl, 4-keto-piperidinyl, 2-keto-piperazinyl, and 3-keto-piperazinyl);

(166) a substituted or unsubstituted cyclic C.sub.3-C.sub.8 alkyl group (such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl and cyclooctyl);

(167) a substituted or unsubstituted aromatic group (such as Ph-, 2-F-Ph-, 3-F-Ph-, 4-F-Ph-, 2-Cl-Ph-, 3-Cl-Ph-, 4-Cl-Ph-, 2-Br-Ph-, 3-Br-Ph-, 4-Br-Ph-, 2-I-Ph-, 3-I-Ph, 4-I-Ph-, 2,(3,4,5 or 6)-F.sub.2-Ph-, 2,(3,4,5 or 6)-Cl.sub.2-Ph-, 2,(3,4,5 or 6)-Br.sub.2-Ph-, 2,(3,4,5 or 6)-I.sub.2-Ph-, 2,(3,4,5 or 6)-Me.sub.2-Ph-, 2,(3,4,5 or 6)-Et.sub.2-Ph-, 2,(3,4,5 or 6)-Pr.sub.2-Ph-, 2,(3,4,5 or 6)-Bu.sub.2-Ph-, 2,(3,4,5 or 6)-(CN).sub.2-Ph-, 2,(3,4,5 or 6)-(NO.sub.2).sub.2-Ph-, 2,(3,4,5 or 6)-(NH.sub.2).sub.2-Ph-, 2,(3,4,5 or 6)-(MeO).sub.2-Ph-, 2,(3,4,5 or 6)-(CF.sub.3).sub.2-Ph-, 3,(4 or 5)-F.sub.2-Ph-, 3,(4 or 5)-Cl.sub.2-Ph-, 3,(4 or 5)-Br.sub.2-Ph-, 3,(4 or 5)-I.sub.2-Ph-, 3,(4 or 5)-Me.sub.2-Ph-, 3,(4 or 5)-Et.sub.2-Ph-, 3,(4 or 5)-Pr.sub.2-Ph-, 3,(4 or 5)-Bu.sub.2-Ph-, 3,(4 or 5)-(CN).sub.2-Ph-, 3,(4 or 5)-(NO.sub.2).sub.2-Ph-, 3,(4 or 5)-(NH.sub.2).sub.2-Ph-, 3,(4 or 5)-(MeO).sub.2-Ph-, 3,(4 or 5)-(CF.sub.3).sub.2-Ph-, 2-Me-Ph-, 3-Me-Ph-, 4-Me-Ph-, 2-Et-Ph-, 3-Et-Ph-, 4-Et-Ph-, 2-Pr-Ph-, 3-Pr-Ph-, 4-Pr-Ph-, 2-Bu-Ph-, 3-Bu-Ph-, 4-Bu-Ph-, 2-(CN)-Ph-, 3-(CN)-Ph-, 4-(CN)-Ph-, 2-(NO.sub.2)-Ph-, 3-(NO.sub.2)-Ph-, 4-(NO.sub.2)-Ph-, 2-(NH.sub.2)-Ph-, 3-(NH.sub.2)-Ph-, 4-(NH.sub.2)-Ph-, 2-MeO-Ph-, 3-MeO-Ph-, 4-MeO-Ph-, 2-(NH.sub.2CO)-Ph-, 3-(NH.sub.2CO)-Ph-, 4-(NH.sub.2CO)-Ph-, 2-CF.sub.3-Ph-, 3-CF.sub.3-Ph-, 4-CF.sub.3-Ph-, 2-CF.sub.3O-Ph-, 3-CF.sub.3O-Ph-, and 4-CF.sub.3O-Ph-); and

(168) a saturated or unsaturated, substituted or unsubstituted, heterocyclic group including an aromatic heterocyclic group and/or a non-aromatic heterocyclic group (such as pyrrole-1-yl, pyrrole-2-yl, pyrrole-3-yl, pyrazole-1-yl, pyrazole-3-yl, pyrazole-4-yl, pyrazole-5-yl, imidazole-1-yl, imidazole-2-yl, imidazole-4-yl, imidazole-5-yl, 1,2,3-triazole-1-yl, 1,2,3-triazole-4-yl, 1,2,3-triazole-5-yl, 1,2,4-triazole-1-yl, 1,2,4-triazole-3-yl, 1,2,4-triazole-5-yl, pyridin-2-yl, pyridin-3-yl, pyridin-4-yl, pyridazine-3-yl, pyridazine-4-yl, pyrimidin-2-yl, pyrimidin-4-yl, pyrimidin-5-yl, pyrimidin-6-yl, pyrazine-2-yl, pyrrolidine-1-yl, pyrrolidine-2-yl, pyrrolidine-3-yl, piperidine-1-yl, piperidine-2-yl, piperidine-3-yl, piperidine-4-yl, 2-azapiperidine-1-yl, 2-azapiperidine-3-yl, 2-azapiperidine-4-yl, 3-azapiperidine-1-yl, 3-azapiperidine-2-yl, 3-azapiperidine-4-yl, 3-azapiperidine-5-yl, piperazine-1-yl, piperazine-2-yl, furan-2-yl, furan-3-yl, pyran-2-yl, pyran-3-yl, pyran-4-yl, 2-azapyran-2-yl, 2-azapyran-3-yl, 2-azapyran-4-yl, 2-azapyran-5-yl, 2-azapyran-6-yl, 3-azapyran-2-yl, 3-azapyran-4-yl, 3-azapyran-5-yl, 3-azapyran-6-yl, 4-azapyran-2-yl, 4-azapyran-3-yl, 4-azapyran-4-yl, 4-azapyran-5-yl, 4-azapyran-6-yl, tetrahydrofuran-2-yl, tetrahydrofuran-3-yl, 2-aza-tetrahydrofuran-2-yl, 2-aza-tetrahydrofuran-3-yl, 2-aza-tetrahydrofuran-4-yl, 2-aza-tetrahydrofuran-5-yl, 3-aza-tetrahydrofuran-2-yl, 3-aza-tetrahydrofuran-3-yl, 3-aza-tetrahydrofuran-4-yl, 3-aza-tetrahydrofuran-5-yl, tetrahydropyran-2-yl, tetrahydropyran-3-yl, tetrahydropyran-4-yl, 2-aza-tetrahydropyran-2-yl, 2-aza-tetrahydropyran-3-yl, 2-aza-tetrahydropyran-4-yl, 2-aza-tetrahydropyran-5-yl, 2-aza-tetrahydropyran-6-yl, 3-aza-tetrahydropyran-2-yl, 3-aza-tetrahydropyran-3-yl, 3-aza-tetrahydropyran-4-yl, 3-aza-tetrahydropyran-5-yl, 3-aza-tetrahydropyran-6-yl, morpholine-2-yl, morpholine-3-yl, morpholine-4-yl, thiophen-2-yl, thiophen-3-yl, isothiazole-3-yl, isothiazole-4-yl, isothiazole-5-yl, thiazole-2-yl, thiazole-4-yl, thiazole-5-yl, thiopyran-2-yl, thiopyran-3-yl, thiopyran-4-yl, 2-azathiopyran-2-yl, 2-azathiopyran-3-yl, 2-azathiopyran-4-yl, 2-azathiopyran-5-yl, 2-azathiopyran-6-yl, 3-azathiopyran-2-yl, 3-azathiopyran-4-yl, 3-azathiopyran-5-yl, 3-azathiopyran-6-yl, 4-azathiopyran-2-yl, 4-azathiopyran-3-yl, 4-azathiopyran-4-yl, 4-azathiopyran-5-yl, 4-azathiopyran-6-yl, thiolane-2-yl, thiolane-3-yl, thiane-2-yl, thiane-3-yl, thiane-4-yl, oxazol-2-yl, oxazol-5-yl, isoxazol-3-yl, isoxazol-4-yl, isoxazol-5-yl, furazan-3-yl, (1,3,4-oxadiazol)-2-yl, (1,3,4-oxadiazol)-5-yl, (1,2,4-oxadiazol)-3-yl, (1,2,4-oxadiazol)-5-yl; and tetrazole-1-yl, tetrazole-2-yl, tetrazole-5-yl); and

(169) fused ring systems comprising two or three or more fused rings, which rings may be substituted or unsubstituted, preferably wherein the rings are selected from one, two, or more of the above aromatic groups and aromatic or non-aromatic heterocyclic groups, (e.g. fused ring systems such as naphthalene, anthracene, phenanthrene, phenalene, biphenylene, pentalene, indene, as-indacene, s-indacene, acenaphthylene, fluorene, fluoranthene, acephenanthrylene, azulene, heptalene, indole, indazole, benzimidazole, 4-azaindole, 5-azaindole, 6-azaindole, 7-azaindole, isoindole, 4-azaisoindole, 5-azaisoindole, 6-azaisoindole, 7-azaisoindole, indolizine, 1-azaindolizine, 2-azaindolizine, 3-azaindolizine, 5-azaindolizine, 6-azaindolizine, 7-azaindolizine, 8-azaindolizine, 9-azaindolizine, purine, carbazole, carboline, benzofuran, isobenzofuran, benzothiophene, isobenzothiophene, quinoline, cinnoline, quinazoline, quinoxaline, 5-azaquinoline, 6-azaquinoline, 7-azaquinoline, naphthyridine, isoquinoline, phthalazine, 6-azaisoquinoline, 7-azaisoquinoline, pteridine, chromene, isochromene, acridine, phenanthridine, perimidine, phenanthroline, phenoxazine, xanthene, phenoxanthiin, and/or thianthrene).

(170) In some preferred embodiments, the invention therefore provides a tryptophan-2,3-dioxygenase (TDO) and/or indoleamine-2,3-dioxygenase (IDO) inhibitor compound for use in medicine, which compound comprises the following formula:

(171) ##STR00035##

(172) wherein X.sup.1, X.sup.2, X.sup.3, X.sup.4, and X.sup.5 may be the same or different and each is independently selected from C, N and O; each atom having a dotted line may independently have a double bond or a single bond, provided that valencies at each atom are maintained; each R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, and R.sup.7 may be present or absent and may be the same or different and is selected from the groups as defined below, provided that the number of such R groups present is such that the valencies of X.sup.1, X.sup.2, X.sup.3, X.sup.4, and X.sup.5 are maintained; one or two R.sup.6 groups may be present and are selected from the groups as defined below, provided that the number of R.sup.6 groups present is such that the valency of the carbon atom to which they are attached is maintained, and provided that at least one R.sup.6 is an organic group comprising an atom double-bonded to an oxygen atom at an -, -, or -position to the carbon atom to which the R.sup.6 is attached and in which the atom double-bonded to an oxygen atom is also bonded to a hetero-atom;

(173) and wherein R.sup.5 and R.sup.7 do not comprise a cyclic group;

(174) and wherein, where present, R.sub.1, R.sup.2, R.sup.3, and R.sup.4 are independently selected from H and a group selected from the following groups:

(175) a halogen (such as F, Cl, Br and I);

(176) a CN group;

(177) a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 alkyl group (such as methyl (Me), ethyl (Et), propyl (Pr), iso-propyl (i-Pr), n-butyl (n-Bu), iso-butyl (i-Bu), tert-butyl (t-Bu), pentyl and hexyl);

(178) a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 alkyl-aryl group (such as CH.sub.2Ph, CH.sub.2(2,3 or 4)F-Ph, CH.sub.2(2,3 or 4)Cl-Ph, CH.sub.2(2,3 or 4)Br-Ph, CH.sub.2(2,3 or 4)I-Ph, CH.sub.2CH.sub.2Ph, CH.sub.2CH.sub.2CH.sub.2Ph, CH.sub.2CH.sub.2CH.sub.2CH.sub.2Ph, CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2Ph, and CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2Ph);

(179) a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 halogenated alkyl group (such as CH.sub.2F, CHF.sub.2, CH.sub.2Cl, CH.sub.2Br, CH.sub.2I, CF.sub.3, CCl.sub.3, CBr.sub.3, CI.sub.3, CH.sub.2CF.sub.3, CH.sub.2CCl.sub.3, CH.sub.2CBr.sub.3, and CH.sub.2CI.sub.3);

(180) an NH.sub.2 group or a substituted or unsubstituted linear or branched primary secondary or tertiary C.sub.1-C.sub.6 amine group (such as NMeH, NMe.sub.2, NEtH, NEtMe, NEt.sub.2, NPrH, NPrMe, NPrEt, NPr.sub.2, NBuH, NBuMe, NBuEt, CH.sub.2NH.sub.2, CH.sub.2NMeH, CH.sub.2NMe.sub.2, CH.sub.2NEtH, CH.sub.2NEtMe, CH.sub.2NEt.sub.2, CH.sub.2NPrH, CH.sub.2NPrMe, and CH.sub.2NPrEt);

(181) a substituted or unsubstituted amino-aryl group (such as NH-Ph, NH-(2,3 or 4)F-Ph, NH-(2,3 or 4)Cl-Ph, NH-(2,3 or 4)Br-Ph, NH-(2,3 or 4)I-Ph, NH-(2,3 or 4)Me-Ph, NH-(2,3 or 4)Et-Ph, NH-(2,3 or 4)Pr-Ph, NH-(2,3 or 4)Bu-Ph, NH-(2,3 or 4)OMe-Ph, NH-(2,3 or 4)OEt-Ph, NH-(2,3 or 4)OPr-Ph, NH-(2,3 or 4)OBu-Ph, NH-2,(3,4,5 or 6)F.sub.2-Ph, NH-2,(3,4,5 or 6)Cl.sub.2-Ph, NH-2,(3,4,5 or 6)Br.sub.2-Ph, NH-2,(3,4,5 or 6)I.sub.2-Ph, NH-2,(3,4,5 or 6)Me.sub.2-Ph, NH-2,(3,4,5 or 6)Et.sub.2-Ph, NH-2,(3,4,5, or 6)Pr.sub.2-Ph, NH-2,(3,4,5 or 6)Bu.sub.2-Ph;

(182) a substituted or unsubstituted cyclic amine or amido group (such as pyrrolidin-1-yl, pyrrolidin-2-yl, pyrrolidin-3-yl, piperidin-1-yl, piperidin-2-yl, piperidin-3-yl, piperidin-4-yl, piperazin-1-yl, piperazin-2-yl, piperazin-3-yl, morpholin-2-yl, morpholin-3-yl, morpholin-4-yl, 2-keto-pyrrolidinyl, 3-keto-pyrrolidinyl, 2-keto-piperidinyl, 3-keto-piperidinyl, 4-keto-piperidinyl, 2-keto-piperazinyl, and 3-keto-piperazinyl);

(183) a substituted or unsubstituted cyclic C.sub.3-C.sub.8 alkyl group (such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl and cyclooctyl);

(184) an OH group or a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 alcohol group (such as CH.sub.2OH, CH.sub.2CH.sub.2OH, CH.sub.2CH.sub.2CH.sub.2OH, CH(CH.sub.3)CH.sub.2OH, C(CH.sub.3).sub.2OH, CH.sub.2CH.sub.2CH.sub.2CH.sub.2OH, CH(CH.sub.3)CH.sub.2CH.sub.2OH, CH(CH.sub.3)CH(CH.sub.3)OH, CH(CH.sub.2CH.sub.3)CH.sub.2OH, C(CH.sub.3).sub.2CH.sub.2OH, CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2OH, and CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2OH);

(185) a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 carboxylic acid group (such as COOH, CH.sub.2COOH, CH.sub.2CH.sub.2COOH, CH.sub.2CH.sub.2CH.sub.2COOH, CH.sub.2CH.sub.2CH.sub.2CH.sub.2COOH, and CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2COOH);

(186) a substituted or unsubstituted linear or branched carbonyl group (such as (CO)Me, (CO)Et, (CO)Pr, (CO)iPr, (CO)nBu, (CO)iBu, (CO)tBu, (CO)Ph, (CO)CH.sub.2Ph, (CO)CH.sub.2OH, (CO)CH.sub.2OCH.sub.3, (CO)CH.sub.2NH.sub.2, (CO)CH.sub.2NHMe, (CO)CH.sub.2NMe.sub.2, (CO)-cyclopropyl, (CO)-1,3-epoxypropan-2-yl; (CO)NH.sub.2, (CO)NHMe, (CO)NMe.sub.2, (CO)NHEt, (CO)NEt.sub.2, (CO)-pyrollidine-N-yl, (CO)-morpholine-N-yl, (CO)-piperazine-N-yl, (CO)N-methyl-piperazine-N-yl, (CO)NHCH.sub.2CH.sub.2OH, (CO)NHCH.sub.2CH.sub.2OMe, (CO)NHCH.sub.2CH.sub.2NH.sub.2, (CO)NHCH.sub.2CH.sub.2NHMe, and (CO)NHCH.sub.2CH.sub.2NMe.sub.2;

(187) a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 carboxylic acid ester group (such as COOMe, COOEt, COOPr, COO-i-Pr, COO-n-Bu, COO-i-Bu, COO-t-Bu, CH.sub.2COOMe, CH.sub.2CH.sub.2COOMe, CH.sub.2CH.sub.2CH.sub.2COOMe, and CH.sub.2CH.sub.2CH.sub.2CH.sub.2COOMe);

(188) a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 amide group (such as CONH.sub.2, CONMeH, CONMe.sub.2, CONEtH, CONEtMe, CONEt.sub.2, CONPrH, CONPrMe, and CONPrEt);

(189) a substituted or unsubstituted linear or branched C.sub.1-C.sub.7 amino carbonyl group (such as NHCO-Me, NHCO-Et, NHCO-Pr, NHCO-Bu, NHCO-pentyl, NHCO-hexyl, NHCO-Ph, NMe-CO-Me, NMe-CO-Et, NMe-CO-Pr, NMe-CO-Bu, NMe-CO-pentyl, NMe-CO-hexyl, NMe-CO-Ph;

(190) a substituted or unsubstituted linear or branched C.sub.1-C.sub.7 alkoxy or aryloxy group (such as OMe, OEt, OPr, O-i-Pr, O-n-Bu, O-i-Bu, O-t-Bu, O-pentyl, O-hexyl, OCH.sub.2F, OCHF.sub.2, OCF.sub.3, OCH.sub.2Cl, OCHCl.sub.2, OCCl.sub.3, O-Ph, OCH.sub.2-Ph, OCH.sub.2-(2,3 or 4)-F-Ph, OCH.sub.2-(2,3 or 4)-Cl-Ph, CH.sub.2OMe, CH.sub.2OEt, CH.sub.2OPr, CH.sub.2OBu, CH.sub.2CH.sub.2OMe, CH.sub.2CH.sub.2CH.sub.2OMe, CH.sub.2CH.sub.2CH.sub.2CH.sub.2OMe, and CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2OMe);

(191) a substituted or unsubstituted linear or branched aminoalkoxy group (such as OCH.sub.2CH.sub.2NH.sub.2, OCH.sub.2CH.sub.2NHMe, OCH.sub.2CH.sub.2NMe.sub.2, OCH.sub.2CH.sub.2NHEt, and OCH.sub.2CH.sub.2NEt.sub.2;

(192) a substituted or unsubstituted linear or branched sulphonyl group (such as SO.sub.2Me, SO.sub.2Et, SO.sub.2Pr, SO.sub.2iPr, SO.sub.2Ph, SO.sub.2-(2,3 or 4)-F-Ph, SO.sub.2-cyclopropyl, SO.sub.2CH.sub.2CH.sub.2OCH.sub.3;

(193) a sulphonylamino group (such as SO.sub.2NH.sub.2, SO.sub.2NHMe, SO.sub.2NMe.sub.2, SO.sub.2NHEt, SO.sub.2NEt.sub.2, SO.sub.2-pyrrolidine-N-yl, SO.sub.2-morpholine-N-yl, SO.sub.2NHCH.sub.2OMe, and SO.sub.2NHCH.sub.2CH.sub.2OMe);

(194) an aminosulphonyl group (such as NHSO.sub.2Me, NHSO.sub.2Et, NHSO.sub.2Pr, NHSO.sub.2iPr, NHSO.sub.2Ph, NHSO.sub.2-(2,3 or 4)-F-Ph, NHSO.sub.2-cyclopropyl, NHSO.sub.2CH.sub.2CH.sub.2OCH.sub.3);

(195) a cyclic aminosulphonyl-group (such as N(SO.sub.2)(CH.sub.2).sub.3 and N(SO.sub.2)(CH.sub.2).sub.4);

(196) an aromatic group (such as Ph-, 2-F-Ph-, 3-F-Ph-, 4-F-Ph-, 2-Cl-Ph-, 3-Cl-Ph-, 4-Cl-Ph-, 2-Br-Ph-, 3-Br-Ph-, 4-Br-Ph-, 2-I-Ph-, 3-I-Ph, 4-I-Ph-, 2,(3,4,5 or 6)-F.sub.2-Ph-, 2,(3,4,5 or 6)-Cl.sub.2-Ph-, 2,(3,4,5 or 6)-Br.sub.2-Ph-, 2,(3,4,5 or 6)-I.sub.2-Ph-, 2,(3,4,5 or 6)-Me.sub.2-Ph-, 2,(3,4,5 or 6)-Et.sub.2-Ph-, 2,(3,4,5 or 6)-Pr.sub.2-Ph-, 2,(3,4,5 or 6)-Bu.sub.2-Ph-, 2,(3,4,5 or 6)-(CN).sub.2-Ph-, 2,(3,4,5 or 6)-(NO.sub.2).sub.2-Ph-, 2,(3,4,5 or 6)-(NH.sub.2).sub.2-Ph-, 2,(3,4,5 or 6)-(MeO).sub.2-Ph-, 2,(3,4,5 or 6)-(CF.sub.3).sub.2-Ph-, 3,(4 or 5)-F.sub.2-Ph-, 3,(4 or 5)-Cl.sub.2-Ph-, 3,(4 or 5)-Br.sub.2-Ph-, 3,(4 or 5)-I.sub.2-Ph-, 3,(4 or 5)-Me.sub.2-Ph-, 3,(4 or 5)-Et.sub.2-Ph-, 3,(4 or 5)-Pr.sub.2-Ph-, 3,(4 or 5)-Bu.sub.2-Ph-, 3,(4 or 5)-(CN)2-Ph-, 3,(4 or 5)-(NO.sub.2).sub.2-Ph-, 3,(4 or 5)-(NH.sub.2).sub.2-Ph-, 3,(4 or 5)-(MeO).sub.2-Ph-, 3,(4 or 5)-(CF.sub.3).sub.2-Ph-, 2-Me-Ph-, 3-Me-Ph-, 4-Me-Ph-, 2-Et-Ph-, 3-Et-Ph-, 4-Et-Ph-, 2-Pr-Ph-, 3-Pr-Ph-, 4-Pr-Ph-, 2-Bu-Ph-, 3-Bu-Ph-, 4-Bu-Ph-, 2-(CN)-Ph-, 3-(CN)-Ph-, 4-(CN)-Ph-, 2-(NO.sub.2)-Ph-, 3-(NO.sub.2)-Ph-, 4-(NO.sub.2)-Ph-, 2-(NH.sub.2)-Ph-, 3-(NH.sub.2)-Ph-, 4-(NH.sub.2)-Ph-, 2-MeO-Ph-, 3-MeO-Ph-, 4-MeO-Ph-, 2-(NH.sub.2CO)-Ph-, 3-(NH.sub.2CO)-Ph-, 4-(NH.sub.2CO)-Ph-, 2-CF.sub.3-Ph-, 3-CF.sub.3-Ph-, 4-CF.sub.3-Ph-, 2-CF.sub.3O-Ph-, 3-CF.sub.3O-Ph-, and 4-CF.sub.3O-Ph-);

(197) a saturated or unsaturated, substituted or unsubstituted, heterocyclic group including an aromatic heterocyclic group and/or a non-aromatic heterocyclic group (such as pyrrole-1-yl, pyrrole-2-yl, pyrrole-3-yl, pyrazole-1-yl, pyrazole-3-yl, pyrazole-4-yl, pyrazole-5-yl, imidazole-1-yl, imidazole-2-yl, imidazole-4-yl, imidazole-5-yl, 1,2,3-triazole-1-yl, 1,2,3-triazole-4-yl, 1,2,3-triazole-5-yl, 1,2,4-triazole-1-yl, 1,2,4-triazole-3-yl, 1,2,4-triazole-5-yl, pyridin-2-yl, pyridin-3-yl, pyridin-4-yl, pyridazine-3-yl, pyridazine-4-yl, pyrimidin-2-yl, pyrimidin-4-yl, pyrimidin-5-yl, pyrimidin-6-yl, pyrazine-2-yl, pyrrolidine-1-yl, pyrrolidine-2-yl, pyrrolidine-3-yl, piperidine-1-yl, piperidine-2-yl, piperidine-3-yl, piperidine-4-yl, 2-azapiperidine-1-yl, 2-azapiperidine-3-yl, 2-azapiperidine-4-yl, 3-azapiperidine-1-yl, 3-azapiperidine-2-yl, 3-azapiperidine-4-yl, 3-azapiperidine-5-yl, piperazine-1-yl, piperazine-2-yl, furan-2-yl, furan-3-yl, pyran-2-yl, pyran-3-yl, pyran-4-yl, 2-azapyran-2-yl, 2-azapyran-3-yl, 2-azapyran-4-yl, 2-azapyran-5-yl, 2-azapyran-6-yl, 3-azapyran-2-yl, 3-azapyran-4-yl, 3-azapyran-5-yl, 3-azapyran-6-yl, 4-azapyran-2-yl, 4-azapyran-3-yl, 4-azapyran-4-yl, 4-azapyran-5-yl, 4-azapyran-6-yl, tetrahydrofuran-2-yl, tetrahydrofuran-3-yl, 2-aza-tetrahydrofuran-2-yl, 2-aza-tetrahydrofuran-3-yl, 2-aza-tetrahydrofuran-4-yl, 2-aza-tetrahydrofuran-5-yl, 3-aza-tetrahydrofuran-2-yl, 3-aza-tetrahydrofuran-3-yl, 3-aza-tetrahydrofuran-4-yl, 3-aza-tetrahydrofuran-5-yl, tetrahydropyran-2-yl, tetrahydropyran-3-yl, tetrahydropyran-4-yl, 2-aza-tetrahydropyran-2-yl, 2-aza-tetrahydropyran-3-yl, 2-aza-tetrahydropyran-4-yl, 2-aza-tetrahydropyran-5-yl, 2-aza-tetrahydropyran-6-yl, 3-aza-tetrahydropyran-2-yl, 3-aza-tetrahydropyran-3-yl, 3-aza-tetrahydropyran-4-yl, 3-aza-tetrahydropyran-5-yl, 3-aza-tetrahydropyran-6-yl, morpholine-2-yl, morpholine-3-yl, morpholine-4-yl, thiophen-2-yl, thiophen-3-yl, isothiazole-3-yl, isothiazole-4-yl, isothiazole-5-yl, thiazole-2-yl, thiazole-4-yl, thiazole-5-yl, thiopyran-2-yl, thiopyran-3-yl, thiopyran-4-yl, 2-azathiopyran-2-yl, 2-azathiopyran-3-yl, 2-azathiopyran-4-yl, 2-azathiopyran-5-yl, 2-azathiopyran-6-yl, 3-azathiopyran-2-yl, 3-azathiopyran-4-yl, 3-azathiopyran-5-yl, 3-azathiopyran-6-yl, 4-azathiopyran-2-yl, 4-azathiopyran-3-yl, 4-azathiopyran-4-yl, 4-azathiopyran-5-yl, 4-azathiopyran-6-yl, thiolane-2-yl, thiolane-3-yl, thiane-2-yl, thiane-3-yl, thiane-4-yl, oxazol-2-yl, oxazol-4-yl, oxazol-5-yl, isoxazol-3-yl, isoxazol-4-yl, isoxazol-5-yl, furazan-3-yl, (1,3,4-oxadiazol)-2-yl, (1,3,4-oxadiazol)-5-yl, (1,2,4-oxadiazol)-3-yl, (1,2,4-oxadiazol)-5-yl; and tetrazole-1-yl, tetrazole-2-yl, tetrazole-5-yl);

(198) fused ring systems comprising two or three or more fused rings, which rings may be substituted or unsubstituted, preferably wherein the rings are selected from one, two, or more of the above aromatic groups and aromatic or non-aromatic heterocyclic groups, (e.g. fused ring systems such as naphthalene, anthracene, phenanthrene, phenalene, biphenylene, pentalene, indene, as-indacene, s-indacene, acenaphthylene, fluorene, fluoranthene, acephenanthrylene, azulene, heptalene, indole, indazole, benzimidazole, 4-azaindole, 5-azaindole, 6-azaindole, 7-azaindole, isoindole, 4-azaisoindole, 5-azaisoindole, 6-azaisoindole, 7-azaisoindole, indolizine, 1-azaindolizine, 2-azaindolizine, 3-azaindolizine, 5-azaindolizine, 6-azaindolizine, 7-azaindolizine, 8-azaindolizine, 9-azaindolizine, purine, carbazole, carboline, benzofuran, isobenzofuran, benzothiophene, isobenzothiophene, quinoline, cinnoline, quinazoline, quinoxaline, 5-azaquinoline, 6-azaquinoline, 7-azaquinoline, naphthyridine, isoquinoline, phthalazine, 6-azaisoquinoline, 7-azaisoquinoline, pteridine, chromene, isochromene, acridine, phenanthridine, perimidine, phenanthroline, phenoxazine, xanthene, phenoxanthiin, and/or thianthrene); and

(199) where there are two R groups attached to the same atom, they may together form a group which is double bonded to that atom, (such as a carbonyl group (O) or an alkene group (C(R).sub.2) wherein each R group is the same or different and is H or an organic group, preferably H or a straight or branched C.sub.1-C.sub.6 alkyl group);

(200) and wherein, where present, R.sup.7 is independently selected from H and a group selected from the following groups:

(201) a halogen (such as F, Cl, Br and I);

(202) a CN group;

(203) a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 alkyl group (such as methyl (Me), ethyl (Et), propyl (Pr), iso-propyl (i-Pr), n-butyl (n-Bu), iso-butyl (i-Bu), tert-butyl (t-Bu), pentyl and hexyl);

(204) a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 halogenated alkyl group (such as CH.sub.2F, CHF.sub.2, CH.sub.2Cl, CH.sub.2Br, CH.sub.2I, CF.sub.3, CCl.sub.3, CBr.sub.3, CI.sub.3, CH.sub.2CF.sub.3, CH.sub.2CCl.sub.3, CH.sub.2CBr.sub.3, and CH.sub.2CI.sub.3);

(205) an NH.sub.2 group or a substituted or unsubstituted linear or branched primary secondary or tertiary C.sub.1-C.sub.6 amine group (such as NMeH, NMe.sub.2, NEtH, NEtMe, NEt.sub.2, NPrH, NPrMe, NPrEt, NPr.sub.2, NBuH, NBuMe, NBuEt, CH.sub.2NH.sub.2, CH.sub.2NMeH, CH.sub.2NMe.sub.2, CH.sub.2NEtH, CH.sub.2NEtMe, CH.sub.2NEt.sub.2, CH.sub.2NPrH, CH.sub.2NPrMe, and CH.sub.2NPrEt);

(206) an OH group or a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 alcohol group (such as CH.sub.2OH, CH.sub.2CH.sub.2OH, CH.sub.2CH.sub.2CH.sub.2OH, CH(CH.sub.3)CH.sub.2OH, C(CH.sub.3).sub.2OH, CH.sub.2CH.sub.2CH.sub.2CH.sub.2OH, CH(CH.sub.3)CH.sub.2CH.sub.2OH, CH(CH.sub.3)CH(CH.sub.3)OH, CH(CH.sub.2CH.sub.3)CH.sub.2OH, C(CH.sub.3).sub.2CH.sub.2OH, CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2OH, and CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2OH);

(207) a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 carboxylic acid group (such as COOH, CH.sub.2COOH, CH.sub.2CH.sub.2COOH, CH.sub.2CH.sub.2CH.sub.2COOH, CH.sub.2CH.sub.2CH.sub.2CH.sub.2COOH, and CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2COOH);

(208) a substituted or unsubstituted linear or branched carbonyl group (such as (CO)Me, (CO)Et, (CO)Pr, (CO)iPr, (CO)nBu, (CO)iBu, (CO)tBu, (CO)CH.sub.2OH, (CO)CH.sub.2OCH.sub.3, (CO)CH.sub.2NH.sub.2, (CO)CH.sub.2NHMe, (CO)CH.sub.2NMe.sub.2, (CO)NH.sub.2, (CO)NHMe, (CO)NMe.sub.2, (CO)NHEt, (CO)NEt.sub.2, (CO)NHCH.sub.2CH.sub.2OH, (CO)NHCH.sub.2CH.sub.2OMe, (CO)NHCH.sub.2CH.sub.2NH.sub.2, (CO)NHCH.sub.2CH.sub.2NHMe, and (CO)NHCH.sub.2CH.sub.2NMe.sub.2;

(209) a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 carboxylic acid ester group (such as COOMe, COOEt, COOPr, COO-i-Pr, COO-n-Bu, COO-i-Bu, COO-t-Bu, CH.sub.2COOMe, CH.sub.2CH.sub.2COOMe, CH.sub.2CH.sub.2CH.sub.2COOMe, and CH.sub.2CH.sub.2CH.sub.2CH.sub.2COOMe);

(210) a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 amide group (such as CONH.sub.2, CONMeH, CONMe.sub.2, CONEtH, CONEtMe, CONEt.sub.2, CONPrH, CONPrMe, and CONPrEt);

(211) a substituted or unsubstituted linear or branched C.sub.1-C.sub.7 amino carbonyl group (such as NHCO-Me, NHCO-Et, NHCO-Pr, NHCO-Bu, NHCO-pentyl, NHCO-hexyl, NMe-CO-Me, NMe-CO-Et, NMe-CO-Pr, NMe-CO-Bu, NMe-CO-pentyl, NMe-CO-hexyl;

(212) a substituted or unsubstituted linear or branched C.sub.1-C.sub.7 alkoxy or aryloxy group (such as OMe, OEt, OPr, O-i-Pr, O-n-Bu, O-i-Bu, O-t-Bu, O-pentyl, O-hexyl, OCH.sub.2F, OCHF.sub.2, OCF.sub.3, OCH.sub.2Cl, OCHCl.sub.2, OCCl.sub.3CH.sub.2OMe, CH.sub.2OEt, CH.sub.2OPr, CH.sub.2OBu, CH.sub.2CH.sub.2OMe, CH.sub.2CH.sub.2CH.sub.2OMe, CH.sub.2CH.sub.2CH.sub.2CH.sub.2OMe, and CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2OMe);

(213) a substituted or unsubstituted linear or branched aminoalkoxy group (such as OCH.sub.2CH.sub.2NH.sub.2, OCH.sub.2CH.sub.2NHMe, OCH.sub.2CH.sub.2NMe.sub.2, OCH.sub.2CH.sub.2NHEt, and OCH.sub.2CH.sub.2NEt.sub.2;

(214) a substituted or unsubstituted linear or branched sulphonyl group (such as SO.sub.2Me, SO.sub.2Et, SO.sub.2Pr, SO.sub.2iPr, SO.sub.2CH.sub.2CH.sub.2OCH.sub.3;

(215) a substituted or unsubstituted linear or branched sulphonylamino group (such as SO.sub.2NH.sub.2, SO.sub.2NHMe, SO.sub.2NMe.sub.2, SO.sub.2NHEt, SO.sub.2NEt.sub.2, SO.sub.2NHCH.sub.2OMe, and SO.sub.2NHCH.sub.2CH.sub.2OMe);

(216) a substituted or unsubstituted linear or branched aminosulphonyl group (such as NHSO.sub.2Me, NHSO.sub.2Et, NHSO.sub.2Pr, NHSO.sub.2iPr, NHSO.sub.2CH.sub.2CH.sub.2OCH.sub.3);

(217) preferably wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, and R.sup.7 are selected from H and:

(218) a halogen such as F, Cl, Br and I, preferably F and Cl, (more preferably wherein R.sup.2 is selected from Cl and Br, and R.sup.1, R.sup.3, and R.sup.4 are selected from H and F);

(219) CN;

(220) a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 alkyl group such as such as methyl (Me), ethyl (Et), propyl (Pr), iso-propyl (i-Pr), cyclopropyl (cy-Pr), n-butyl (n-Bu), iso-butyl (i-Bu), tert-butyl (t-Bu), pentyl and hexyl, preferably -Me;

(221) a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 halogenated alkyl group (such as CH.sub.2F, CHF.sub.2, CH.sub.2Cl, CH.sub.2Br, CH.sub.2I, CF.sub.3, CCl.sub.3, CBr.sub.3, CI.sub.3, CH.sub.2CF.sub.3, CH.sub.2CCl.sub.3, CH.sub.2CBr.sub.3, and CH.sub.2CI.sub.3), preferably CF.sub.3; and

(222) a substituted or unsubstituted linear or branched C.sub.1-C.sub.7 alkoxy group (such as OMe, OEt, OPr, O-i-Pr, O-n-Bu, O-i-Bu, O-t-Bu, O-pentyl, O-hexyl, OCH.sub.2F, OCHF.sub.2, OCF.sub.3, OCH.sub.2Cl, OCHCl.sub.2, OCCl.sub.3, O-Ph, CH.sub.2OMe, CH.sub.2OEt, CH.sub.2OPr, CH.sub.2OBu, CH.sub.2CH.sub.2OMe, CH.sub.2CH.sub.2CH.sub.2OMe, CH.sub.2CH.sub.2CH.sub.2CH.sub.2OMe, and CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2OMe), preferably OMe or OEt;

(223) and wherein, where present, R.sup.5 is independently selected from H and:

(224) a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 alkyl group (such as methyl (Me), ethyl (Et), propyl (Pr), iso-propyl (i-Pr), n-butyl (n-Bu), iso-butyl (i-Bu), tert-butyl (t-Bu), pentyl and hexyl);

(225) a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 halogenated alkyl group (such as CH.sub.2F, CHF.sub.2, CF.sub.3, CCl.sub.3, CBr.sub.3, CI.sub.3, CH.sub.2CF.sub.3, CH.sub.2CCl.sub.3, CH.sub.2CBr.sub.3, and CH.sub.2CI.sub.3), preferably a linear or branched C.sub.1-C.sub.6 fluorinated alkyl group (such as CH.sub.2F, CHF.sub.2, CF.sub.3, CH.sub.2CH.sub.2F, CH.sub.2CHF.sub.2, and CH.sub.2CF.sub.3); and

(226) a unsubstituted linear or branched C.sub.2-C.sub.6 alcohol group (such as CH.sub.2CH.sub.2OH, CH.sub.2CH.sub.2CH.sub.2OH, CH(CH.sub.3)CH.sub.2OH, C(CH.sub.3).sub.2OH, CH.sub.2CH.sub.2CH.sub.2CH.sub.2OH, CH(CH.sub.3)CH.sub.2CH.sub.2OH, CH(CH.sub.3)CH(CH.sub.3)OH, CH(CH.sub.2CH.sub.3)CH.sub.2OH, C(CH.sub.3).sub.2CH.sub.2OH, CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2OH, and CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2OH);

(227) preferably wherein R.sup.5 is H.

(228) In some still further preferred embodiments, the invention therefore provides a tryptophan-2,3-dioxygenase (TDO) and/or indoleamine-2,3-dioxygenase (IDO) inhibitor compound for use in medicine, which compound comprises the following formula:

(229) ##STR00036##

(230) wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.7, R.sup.61, R.sup.63, R.sup.64, and R.sup.65 are as defined below, provided that neither R.sup.5 nor R.sup.7 comprises a cyclic group:

(231) wherein, R.sub.1, R.sup.2, R.sup.3, and R.sup.4 are independently selected from H and a group selected from the following groups:

(232) a halogen (such as F, Cl, Br and I);

(233) a CN group;

(234) a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 alkyl group (such as methyl (Me), ethyl (Et), propyl (Pr), iso-propyl (i-Pr), n-butyl (n-Bu), iso-butyl (i-Bu), tert-butyl (t-Bu), pentyl and hexyl);

(235) a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 alkyl-aryl group (such as CH.sub.2Ph, CH.sub.2(2,3 or 4)F-Ph, CH.sub.2(2,3 or 4)Cl-Ph, CH.sub.2(2,3 or 4)Br-Ph, CH.sub.2(2,3 or 4)I-Ph, CH.sub.2CH.sub.2Ph, CH.sub.2CH.sub.2CH.sub.2Ph, CH.sub.2CH.sub.2CH.sub.2CH.sub.2Ph, CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2Ph, and CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2Ph);

(236) a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 halogenated alkyl group (such as CH.sub.2F, CHF.sub.2, CH.sub.2Cl, CH.sub.2Br, CH.sub.2I, CF.sub.3, CCl.sub.3, CBr.sub.3, CI.sub.3, CH.sub.2CF.sub.3, CH.sub.2CCl.sub.3, CH.sub.2CBr.sub.3, and CH.sub.2CI.sub.3);

(237) an NH.sub.2 group or a substituted or unsubstituted linear or branched primary secondary or tertiary C.sub.1-C.sub.6 amine group (such as NMeH, NMe.sub.2, NEtH, NEtMe, NEt.sub.2, NPrH, NPrMe, NPrEt, NPr.sub.2, NBuH, NBuMe, NBuEt, CH.sub.2NH.sub.2, CH.sub.2NMeH, CH.sub.2NMe.sub.2, CH.sub.2NEtH, CH.sub.2NEtMe, CH.sub.2NEt.sub.2, CH.sub.2NPrH, CH.sub.2NPrMe, and CH.sub.2NPrEt);

(238) a substituted or unsubstituted amino-aryl group (such as NH-Ph, NH-(2,3 or 4)F-Ph, NH-(2,3 or 4)Cl-Ph, NH-(2,3 or 4)Br-Ph, NH-(2,3 or 4)I-Ph, NH-(2,3 or 4)Me-Ph, NH-(2,3 or 4)Et-Ph, NH-(2,3 or 4)Pr-Ph, NH-(2,3 or 4)Bu-Ph, NH-(2,3 or 4)OMe-Ph, NH-(2,3 or 4)OEt-Ph, NH-(2,3 or 4)OPr-Ph, NH-(2,3 or 4)OBu-Ph, NH-2,(3,4,5 or 6)F.sub.2-Ph, NH-2,(3,4,5 or 6)Cl.sub.2-Ph, NH-2,(3,4,5 or 6)Br.sub.2-Ph, NH-2,(3,4,5 or 6)I.sub.2-Ph, NH-2,(3,4,5 or 6)Me.sub.2-Ph, NH-2,(3,4,5 or 6)Et.sub.2-Ph, NH-2,(3,4,5, or 6)Pr.sub.2-Ph, NH-2,(3,4,5 or 6)Bu.sub.2-Ph;

(239) a substituted or unsubstituted cyclic amine or amido group (such as pyrrolidin-1-yl, pyrrolidin-2-yl, pyrrolidin-3-yl, piperidin-1-yl, piperidin-2-yl, piperidin-3-yl, piperidin-4-yl, piperazin-1-yl, piperazin-2-yl, piperazin-3-yl, morpholin-2-yl, morpholin-3-yl, morpholin-4-yl, 2-keto-pyrrolidinyl, 3-keto-pyrrolidinyl, 2-keto-piperidinyl, 3-keto-piperidinyl, 4-keto-piperidinyl, 2-keto-piperazinyl, and 3-keto-piperazinyl);

(240) a substituted or unsubstituted cyclic C.sub.3-C.sub.8 alkyl group (such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl and cyclooctyl);

(241) an OH group or a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 alcohol group (such as CH.sub.2OH, CH.sub.2CH.sub.2OH, CH.sub.2CH.sub.2CH.sub.2OH, CH(CH.sub.3)CH.sub.2OH, C(CH.sub.3).sub.2OH, CH.sub.2CH.sub.2CH.sub.2CH.sub.2OH, CH(CH.sub.3)CH.sub.2CH.sub.2OH, CH(CH.sub.3)CH(CH.sub.3)OH, CH(CH.sub.2CH.sub.3)CH.sub.2OH, C(CH.sub.3).sub.2CH.sub.2OH, CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2OH, and CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2OH);

(242) a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 carboxylic acid group (such as COOH, CH.sub.2COOH, CH.sub.2CH.sub.2COOH, CH.sub.2CH.sub.2CH.sub.2COOH, CH.sub.2CH.sub.2CH.sub.2CH.sub.2COOH, and CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2COOH);

(243) a substituted or unsubstituted linear or branched carbonyl group (such as (CO)Me, (CO)Et, (CO)Pr, (CO)iPr, (CO)nBu, (CO)iBu, (CO)tBu, (CO)Ph, (CO)CH.sub.2Ph, (CO)CH.sub.2OH, (CO)CH.sub.2OCH.sub.3, (CO)CH.sub.2NH.sub.2, (CO)CH.sub.2NHMe, (CO)CH.sub.2NMe.sub.2, (CO)-cyclopropyl, (CO)-1,3-epoxypropan-2-yl; (CO)NH.sub.2, (CO)NHMe, (CO)NMe.sub.2, (CO)NHEt, (CO)NEt.sub.2, (CO)-pyrollidine-N-yl, (CO)-morpholine-N-yl, (CO)-piperazine-N-yl, (CO)N-methyl-piperazine-N-yl, (CO)NHCH.sub.2CH.sub.2OH, (CO)NHCH.sub.2CH.sub.2OMe, (CO)NHCH.sub.2CH.sub.2NH.sub.2, (CO)NHCH.sub.2CH.sub.2NHMe, and (CO)NHCH.sub.2CH.sub.2NMe.sub.2;

(244) a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 carboxylic acid ester group (such as COOMe, COOEt, COOPr, COO-i-Pr, COO-n-Bu, COO-i-Bu, COO-t-Bu, CH.sub.2COOMe, CH.sub.2CH.sub.2COOMe, CH.sub.2CH.sub.2CH.sub.2COOMe, and CH.sub.2CH.sub.2CH.sub.2CH.sub.2COOMe);

(245) a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 amide group (such as CONH.sub.2, CONMeH, CONMe.sub.2, CONEtH, CONEtMe, CONEt.sub.2, CONPrH, CONPrMe, and CONPrEt);

(246) a substituted or unsubstituted linear or branched C.sub.1-C.sub.7 amino carbonyl group (such as NHCO-Me, NHCO-Et, NHCO-Pr, NHCO-Bu, NHCO-pentyl, NHCO-hexyl, NHCO-Ph, NMe-CO-Me, NMe-CO-Et, NMe-CO-Pr, NMe-CO-Bu, NMe-CO-pentyl, NMe-CO-hexyl, NMe-CO-Ph;

(247) a substituted or unsubstituted linear or branched C.sub.1-C.sub.7 alkoxy or aryloxy group (such as OMe, OEt, OPr, O-i-Pr, O-n-Bu, O-i-Bu, O-t-Bu, O-pentyl, O-hexyl, OCH.sub.2F, OCHF.sub.2, OCF.sub.3, OCH.sub.2Cl, OCHCl.sub.2, OCCl.sub.3, O-Ph, OCH.sub.2-Ph, OCH.sub.2-(2,3 or 4)-F-Ph, OCH.sub.2-(2,3 or 4)-Cl-Ph, CH.sub.2OMe, CH.sub.2OEt, CH.sub.2OPr, CH.sub.2OBu, CH.sub.2CH.sub.2OMe, CH.sub.2CH.sub.2CH.sub.2OMe, CH.sub.2CH.sub.2CH.sub.2CH.sub.2OMe, and CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2OMe);

(248) a substituted or unsubstituted linear or branched aminoalkoxy group (such as OCH.sub.2CH.sub.2NH.sub.2, OCH.sub.2CH.sub.2NHMe, OCH.sub.2CH.sub.2NMe.sub.2, OCH.sub.2CH.sub.2NHEt, and OCH.sub.2CH.sub.2NEt.sub.2;

(249) a substituted or unsubstituted linear or branched sulphonyl group (such as SO.sub.2Me, SO.sub.2Et, SO.sub.2Pr, SO.sub.2iPr, SO.sub.2Ph, SO.sub.2-(2,3 or 4)-F-Ph, SO.sub.2-cyclopropyl, SO.sub.2CH.sub.2CH.sub.2OCH.sub.3; a sulphonylamino group (such as SO.sub.2NH.sub.2, SO.sub.2NHMe, SO.sub.2NMe.sub.2, SO.sub.2NHEt, SO.sub.2NEt.sub.2, SO.sub.2-pyrrolidine-N-yl, SO.sub.2-morpholine-N-yl, SO.sub.2NHCH.sub.2OMe, and SO.sub.2NHCH.sub.2CH.sub.2OMe);

(250) an aminosulphonyl group (such as NHSO.sub.2Me, NHSO.sub.2Et, NHSO.sub.2Pr, NHSO.sub.2iPr, NHSO.sub.2Ph, NHSO.sub.2-(2,3 or 4)-F-Ph, NHSO.sub.2-cyclopropyl, NHSO.sub.2CH.sub.2CH.sub.2OCH.sub.3);

(251) a cyclic aminosulphonyl-group (such as N(SO.sub.2)(CH.sub.2).sub.3 and N(SO.sub.2)(CH.sub.2).sub.4);

(252) an aromatic group (such as Ph-, 2-F-Ph-, 3-F-Ph-, 4-F-Ph-, 2-Cl-Ph-, 3-Cl-Ph-, 4-Cl-Ph-, 2-Br-Ph-, 3-Br-Ph-, 4-Br-Ph-, 2-I-Ph-, 3-I-Ph, 4-I-Ph-, 2,(3,4,5 or 6)-F.sub.2-Ph-, 2,(3,4,5 or 6)-Cl.sub.2-Ph-, 2,(3,4,5 or 6)-Br.sub.2-Ph-, 2,(3,4,5 or 6)-I.sub.2-Ph-, 2,(3,4,5 or 6)-Me.sub.2-Ph-, 2,(3,4,5 or 6)-Et.sub.2-Ph-, 2,(3,4,5 or 6)-Pr.sub.2-Ph-, 2,(3,4,5 or 6)-Bu.sub.2-Ph-, 2,(3,4,5 or 6)-(CN).sub.2-Ph-, 2,(3,4,5 or 6)-(NO.sub.2).sub.2-Ph-, 2,(3,4,5 or 6)-(NH.sub.2).sub.2-Ph-, 2,(3,4,5 or 6)-(MeO)2-Ph-, 2,(3,4,5 or 6)-(CF.sub.3).sub.2-Ph-, 3,(4 or 5)-F.sub.2-Ph-, 3,(4 or 5)-Cl.sub.2-Ph-, 3,(4 or 5)-Br.sub.2-Ph-, 3,(4 or 5)-I.sub.2-Ph-, 3,(4 or 5)-Me.sub.2-Ph-, 3,(4 or 5)-Et.sub.2-Ph-, 3,(4 or 5)-Pr.sub.2-Ph-, 3,(4 or 5)-Bu.sub.2-Ph-, 3,(4 or 5)-(CN).sub.2-Ph-, 3,(4 or 5)-(NO.sub.2).sub.2-Ph-, 3,(4 or 5)-(NH.sub.2).sub.2-Ph-, 3,(4 or 5)-(MeO).sub.2-Ph-, 3,(4 or 5)-(CF.sub.3).sub.2-Ph-, 2-Me-Ph-, 3-Me-Ph-, 4-Me-Ph-, 2-Et-Ph-, 3-Et-Ph-, 4-Et-Ph-, 2-Pr-Ph-, 3-Pr-Ph-, 4-Pr-Ph-, 2-Bu-Ph-, 3-Bu-Ph-, 4-Bu-Ph-, 2-(CN)-Ph-, 3-(CN)-Ph-, 4-(CN)-Ph-, 2-(NO.sub.2)-Ph-, 3-(NO.sub.2)-Ph-, 4-(NO.sub.2)-Ph-, 2-(NH.sub.2)-Ph-, 3-(NH.sub.2)-Ph-, 4-(NH.sub.2)-Ph-, 2-MeO-Ph-, 3-MeO-Ph-, 4-MeO-Ph-, 2-(NH.sub.2CO)-Ph-, 3-(NH.sub.2CO)-Ph-, 4-(NH.sub.2CO)-Ph-, 2-CF.sub.3-Ph-, 3-CF.sub.3-Ph-, 4-CF.sub.3-Ph-, 2-CF.sub.3O-Ph-, 3-CF.sub.3O-Ph-, and 4-CF.sub.3O-Ph-);

(253) a saturated or unsaturated, substituted or unsubstituted, heterocyclic group including an aromatic heterocyclic group and/or a non-aromatic heterocyclic group (such as pyrrole-1-yl, pyrrole-2-yl, pyrrole-3-yl, pyrazole-1-yl, pyrazole-3-yl, pyrazole-4-yl, pyrazole-5-yl, imidazole-1-yl, imidazole-2-yl, imidazole-4-yl, imidazole-5-yl, 1,2,3-triazole-1-yl, 1,2,3-triazole-4-yl, 1,2,3-triazole-5-yl, 1,2,4-triazole-1-yl, 1,2,4-triazole-3-yl, 1,2,4-triazole-5-yl, pyridin-2-yl, pyridin-3-yl, pyridin-4-yl, pyridazine-3-yl, pyridazine-4-yl, pyrimidin-2-yl, pyrimidin-4-yl, pyrimidin-5-yl, pyrimidin-6-yl, pyrazine-2-yl, pyrrolidine-1-yl, pyrrolidine-2-yl, pyrrolidine-3-yl, piperidine-1-yl, piperidine-2-yl, piperidine-3-yl, piperidine-4-yl, 2-azapiperidine-1-yl, 2-azapiperidine-3-yl, 2-azapiperidine-4-yl, 3-azapiperidine-1-yl, 3-azapiperidine-2-yl, 3-azapiperidine-4-yl, 3-azapiperidine-5-yl, piperazine-1-yl, piperazine-2-yl, furan-2-yl, furan-3-yl, pyran-2-yl, pyran-3-yl, pyran-4-yl, 2-azapyran-2-yl, 2-azapyran-3-yl, 2-azapyran-4-yl, 2-azapyran-5-yl, 2-azapyran-6-yl, 3-azapyran-2-yl, 3-azapyran-4-yl, 3-azapyran-5-yl, 3-azapyran-6-yl, 4-azapyran-2-yl, 4-azapyran-3-yl, 4-azapyran-4-yl, 4-azapyran-5-yl, 4-azapyran-6-yl, tetrahydrofuran-2-yl, tetrahydrofuran-3-yl, 2-aza-tetrahydrofuran-2-yl, 2-aza-tetrahydrofuran-3-yl, 2-aza-tetrahydrofuran-4-yl, 2-aza-tetrahydrofuran-5-yl, 3-aza-tetrahydrofuran-2-yl, 3-aza-tetrahydrofuran-3-yl, 3-aza-tetrahydrofuran-4-yl, 3-aza-tetrahydrofuran-5-yl, tetrahydropyran-2-yl, tetrahydropyran-3-yl, tetrahydropyran-4-yl, 2-aza-tetrahydropyran-2-yl, 2-aza-tetrahydropyran-3-yl, 2-aza-tetrahydropyran-4-yl, 2-aza-tetrahydropyran-5-yl, 2-aza-tetrahydropyran-6-yl, 3-aza-tetrahydropyran-2-yl, 3-aza-tetrahydropyran-3-yl, 3-aza-tetrahydropyran-4-yl, 3-aza-tetrahydropyran-5-yl, 3-aza-tetrahydropyran-6-yl, morpholine-2-yl, morpholine-3-yl, morpholine-4-yl, thiophen-2-yl, thiophen-3-yl, isothiazole-3-yl, isothiazole-4-yl, isothiazole-5-yl, thiazole-2-yl, thiazole-4-yl, thiazole-5-yl, thiopyran-2-yl, thiopyran-3-yl, thiopyran-4-yl, 2-azathiopyran-2-yl, 2-azathiopyran-3-yl, 2-azathiopyran-4-yl, 2-azathiopyran-5-yl, 2-azathiopyran-6-yl, 3-azathiopyran-2-yl, 3-azathiopyran-4-yl, 3-azathiopyran-5-yl, 3-azathiopyran-6-yl, 4-azathiopyran-2-yl, 4-azathiopyran-3-yl, 4-azathiopyran-4-yl, 4-azathiopyran-5-yl, 4-azathiopyran-6-yl, thiolane-2-yl, thiolane-3-yl, thiane-2-yl, thiane-3-yl, thiane-4-yl, oxazol-2-yl, oxazol-4-yl, oxazol-5-yl, isoxazol-3-yl, isoxazol-4-yl, isoxazol-5-yl, furazan-3-yl, (1,3,4-oxadiazol)-2-yl, (1,3,4-oxadiazol)-5-yl, (1,2,4-oxadiazol)-3-yl, (1,2,4-oxadiazol)-5-yl; and tetrazole-1-yl, tetrazole-2-yl, tetrazole-5-yl);

(254) fused ring systems comprising two or three or more fused rings, which rings may be substituted or unsubstituted, preferably wherein the rings are selected from one, two, or more of the above aromatic groups and aromatic or non-aromatic heterocyclic groups, (e.g. fused ring systems such as naphthalene, anthracene, phenanthrene, phenalene, biphenylene, pentalene, indene, as-indacene, s-indacene, acenaphthylene, fluorene, fluoranthene, acephenanthrylene, azulene, heptalene, indole, indazole, benzimidazole, 4-azaindole, 5-azaindole, 6-azaindole, 7-azaindole, isoindole, 4-azaisoindole, 5-azaisoindole, 6-azaisoindole, 7-azaisoindole, indolizine, 1-azaindolizine, 2-azaindolizine, 3-azaindolizine, 5-azaindolizine, 6-azaindolizine, 7-azaindolizine, 8-azaindolizine, 9-azaindolizine, purine, carbazole, carboline, benzofuran, isobenzofuran, benzothiophene, isobenzothiophene, quinoline, cinnoline, quinazoline, quinoxaline, 5-azaquinoline, 6-azaquinoline, 7-azaquinoline, naphthyridine, isoquinoline, phthalazine, 6-azaisoquinoline, 7-azaisoquinoline, pteridine, chromene, isochromene, acridine, phenanthridine, perimidine, phenanthroline, phenoxazine, xanthene, phenoxanthiin, and/or thianthrene); and

(255) where there are two R groups attached to the same atom, they may together form a group which is double bonded to that atom, (such as a carbonyl group (O) or an alkene group (C(R).sub.2) wherein each R group is the same or different and is H or an organic group, preferably H or a straight or branched C.sub.1-C.sub.6 alkyl group);

(256) and wherein, R.sup.7 is independently selected from H and a group selected from the following groups:

(257) a halogen (such as F, Cl, Br and I);

(258) a CN group;

(259) a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 alkyl group (such as methyl (Me), ethyl (Et), propyl (Pr), iso-propyl (i-Pr), n-butyl (n-Bu), iso-butyl (i-Bu), tert-butyl (t-Bu), pentyl and hexyl);

(260) a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 halogenated alkyl group (such as CH.sub.2F, CHF.sub.2, CH.sub.2Cl, CH.sub.2Br, CH.sub.2I, CF.sub.3, CCl.sub.3, CBr.sub.3, CI.sub.3, CH.sub.2CF.sub.3, CH.sub.2CCl.sub.3, CH.sub.2CBr.sub.3, and CH.sub.2CI.sub.3);

(261) an NH.sub.2 group or a substituted or unsubstituted linear or branched primary secondary or tertiary C.sub.1-C.sub.6 amine group (such as NMeH, NMe.sub.2, NEtH, NEtMe, NEt.sub.2, NPrH, NPrMe, NPrEt, NPr.sub.2, NBuH, NBuMe, NBuEt, CH.sub.2NH.sub.2, CH.sub.2NMeH, CH.sub.2NMe.sub.2, CH.sub.2NEtH, CH.sub.2NEtMe, CH.sub.2NEt.sub.2, CH.sub.2NPrH, CH.sub.2NPrMe, and CH.sub.2NPrEt);

(262) an OH group or a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 alcohol group (such as CH.sub.2OH, CH.sub.2CH.sub.2OH, CH.sub.2CH.sub.2CH.sub.2OH, CH(CH.sub.3)CH.sub.2OH, C(CH.sub.3).sub.2OH, CH.sub.2CH.sub.2CH.sub.2CH.sub.2OH, CH(CH.sub.3)CH.sub.2CH.sub.2OH, CH(CH.sub.3)CH(CH.sub.3)OH, CH(CH.sub.2CH.sub.3)CH.sub.2OH, C(CH.sub.3)2CH.sub.2OH, CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2OH, and CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2OH);

(263) a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 carboxylic acid group (such as COOH, CH.sub.2COOH, CH.sub.2CH.sub.2COOH, CH.sub.2CH.sub.2CH.sub.2COOH, CH.sub.2CH.sub.2CH.sub.2CH.sub.2COOH, and CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2COOH);

(264) a substituted or unsubstituted linear or branched carbonyl group (such as (CO)Me, (CO)Et, (CO)Pr, (CO)iPr, (CO)nBu, (CO)iBu, (CO)tBu, (CO)CH.sub.2OH, (CO)CH.sub.2OCH.sub.3, (CO)CH.sub.2NH.sub.2, (CO)CH.sub.2NHMe, (CO)CH.sub.2NMe.sub.2, (CO)NH.sub.2, (CO)NHMe, (CO)NMe.sub.2, (CO)NHEt, (CO)NEt.sub.2, (CO)NHCH.sub.2CH.sub.2OH, (CO)NHCH.sub.2CH.sub.2OMe, (CO)NHCH.sub.2CH.sub.2NH.sub.2, (CO)NHCH.sub.2CH.sub.2NHMe, and (CO)NHCH.sub.2CH.sub.2NMe.sub.2;

(265) a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 carboxylic acid ester group (such as COOMe, COOEt, COOPr, COO-i-Pr, COO-n-Bu, COO-i-Bu, COO-t-Bu, CH.sub.2COOMe, CH.sub.2CH.sub.2COOMe, CH.sub.2CH.sub.2CH.sub.2COOMe, and CH.sub.2CH.sub.2CH.sub.2CH.sub.2COOMe);

(266) a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 amide group (such as CONH.sub.2, CONMeH, CONMe.sub.2, CONEtH, CONEtMe, CONEt.sub.2, CONPrH, CONPrMe, and CONPrEt);

(267) a substituted or unsubstituted linear or branched C.sub.1-C.sub.7 amino carbonyl group (such as NHCO-Me, NHCO-Et, NHCO-Pr, NHCO-Bu, NHCO-pentyl, NHCO-hexyl, NMe-CO-Me, NMe-CO-Et, NMe-CO-Pr, NMe-COBu, NMe-CO-pentyl, NMe-CO-hexyl;

(268) a substituted or unsubstituted linear or branched aminosulphonyl group (such as NHSO.sub.2Me, NHSO.sub.2Et, NHSO.sub.2Pr, NHSO.sub.2iPr, NHSO.sub.2CH.sub.2CH.sub.2OCH.sub.3);

(269) preferably wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, are selected from H and:

(270) a halogen such as F, Cl, Br and I, preferably F and Cl, (more preferably wherein R.sup.2 is selected from Cl and Br, and R.sup.1, R.sup.3, and R.sup.4 are selected from H and F);

(271) CN;

(272) a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 alkyl group such as such as methyl (Me), ethyl (Et), propyl (Pr), iso-propyl (i-Pr), cyclopropyl (cy-Pr), n-butyl (n-Bu), iso-butyl (i-Bu), tert-butyl (t-Bu), pentyl and hexyl, preferably -Me;

(273) a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 halogenated alkyl group (such as CH.sub.2F, CHF.sub.2, CH.sub.2Cl, CH.sub.2Br, CH.sub.2I, CF.sub.3, CCl.sub.3, CBr.sub.3, CI.sub.3, CH.sub.2CF.sub.3, CH.sub.2CCl.sub.3, CH.sub.2CBr.sub.3, and CH.sub.2CI.sub.3), preferably CF.sub.3; and

(274) a substituted or unsubstituted linear or branched C.sub.1-C.sub.7 alkoxy group (such as OMe, OEt, OPr, O-i-Pr, O-n-Bu, O-i-Bu, O-t-Bu, O-pentyl, O-hexyl, OCH.sub.2F, OCHF.sub.2, OCF.sub.3, OCH.sub.2Cl, OCHCl.sub.2, OCCl.sub.3, O-Ph, CH.sub.2OMe, CH.sub.2OEt, CH.sub.2OPr, CH.sub.2OBu, CH.sub.2CH.sub.2OMe, CH.sub.2CH.sub.2CH.sub.2OMe, CH.sub.2CH.sub.2CH.sub.2CH.sub.2OMe, and CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2OMe), preferably OMe, or OEt;

(275) preferably wherein R.sup.7, is selected from H and:

(276) a halogen such as F and Cl;

(277) CN;

(278) a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 alkyl group such as such as methyl (Me), ethyl (Et), propyl (Pr), iso-propyl (i-Pr), cyclopropyl (cy-Pr), n-butyl (n-Bu), iso-butyl (i-Bu), tert-butyl (t-Bu), pentyl and hexyl, preferably -Me; and

(279) a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 halogenated alkyl group (such as CH.sub.2F, CHF.sub.2, CH.sub.2Cl, CH.sub.2Br, CH.sub.2I, CF.sub.3, CCl.sub.3, CBr.sub.3, CI.sub.3, CH.sub.2CF.sub.3, CH.sub.2CCl.sub.3, CH.sub.2CBr.sub.3, and CH.sub.2CI.sub.3), preferably CF.sub.3;

(280) and wherein, R.sup.5 and R.sup.61 are independently selected from H and:

(281) a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 alkyl group (such as methyl (Me), ethyl (Et), propyl (Pr), iso-propyl (i-Pr), n-butyl (n-Bu), iso-butyl (i-Bu), tert-butyl (t-Bu), pentyl and hexyl);

(282) a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 halogenated alkyl group (such as CH.sub.2F, CHF.sub.2, CF.sub.3, CCl.sub.3, CBr.sub.3, CI.sub.3, CH.sub.2CF.sub.3, CH.sub.2CCl.sub.3, CH.sub.2CBr.sub.3, and CH.sub.2CI.sub.3), preferably a linear or branched C.sub.1-C.sub.6 fluorinated alkyl group (such as CH.sub.2F, CHF.sub.2, CF.sub.3, CH.sub.2CH.sub.2F, CH.sub.2CHF.sub.2, and CH.sub.2CF.sub.3); and

(283) a unsubstituted linear or branched C.sub.2-C.sub.6 alcohol group (such as CH.sub.2CH.sub.2OH, CH.sub.2CH.sub.2CH.sub.2OH, CH(CH.sub.3)CH.sub.2OH, C(CH.sub.3).sub.2OH, CH.sub.2CH.sub.2CH.sub.2CH.sub.2OH, CH(CH.sub.3)CH.sub.2CH.sub.2OH, CH(CH.sub.3)CH(CH.sub.3)OH, CH(CH.sub.2CH.sub.3)CH.sub.2OH, C(CH.sub.3)2CH.sub.2OH, CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2OH, and CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2OH);

(284) and R.sup.61 may further be selected from a substituted or unsubstituted cyclic C.sub.3-C.sub.8 alkyl group (such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl and cyclooctyl);

(285) wherein R.sup.5 is preferably H and R.sup.61 is preferably H;

(286) and wherein R.sup.65 is a cyclic group, which cyclic group is bonded directly through one of its ring atoms to the carbon attached to R.sup.63 and R.sup.64, the cyclic group being selected from:

(287) a cyclic amine or amido group (such as pyrrolidin-2-yl, pyrrolidin-3-yl, piperidin-2-yl, piperidin-4-yl, piperazin-2-yl, piperazin-3-yl, morpholin-2-yl, morpholin-3-yl, 2-keto-pyrrolidinyl, 3-keto-pyrrolidinyl, 2-keto-piperidinyl, 3-keto-piperidinyl, 4-keto-piperidinyl), 2-keto-piperazinyl, and 3-keto-piperazinyl;

(288) a substituted or unsubstituted cyclic C.sub.3-C.sub.8 alkyl group (such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl and cyclooctyl);

(289) a substituted or unsubstituted aromatic group (such as Ph-, 2-F-Ph-, 3-F-Ph-, 4-F-Ph-, 2-Cl-Ph-, 3-Cl-Ph-, 4-Cl-Ph-, 2-Br-Ph-, 3-Br-Ph-, 4-Br-Ph-, 2-I-Ph-, 3-I-Ph, 4-I-Ph-, 2,(3,4,5 or 6)-F.sub.2-Ph-, 2,(3,4,5 or 6)-Cl.sub.2-Ph-, 2,(3,4,5 or 6)-Br.sub.2-Ph-, 2,(3,4,5 or 6)-I.sub.2-Ph-, 2,(3,4,5 or 6)-Me.sub.2-Ph-, 2,(3,4,5 or 6)-Et.sub.2-Ph-, 2,(3,4,5 or 6)-Pr.sub.2-Ph-, 2,(3,4,5 or 6)-Bu.sub.2-Ph-, 2,(3,4,5 or 6)-(CN).sub.2-Ph-, 2,(3,4,5 or 6)-(NO.sub.2).sub.2-Ph-, 2,(3,4,5 or 6)-(NH.sub.2).sub.2-Ph-, 2,(3,4,5 or 6)-(MeO).sub.2-Ph-, 2,(3,4,5 or 6)-(CF.sub.3).sub.2-Ph-, 3,(4 or 5)-F.sub.2-Ph-, 3,(4 or 5)-Cl.sub.2-Ph-, 3,(4 or 5)-Br.sub.2-Ph-, 3,(4 or 5)-I.sub.2-Ph-, 3,(4 or 5)-Me.sub.2-Ph-, 3,(4 or 5)-Et.sub.2-Ph-, 3,(4 or 5)-Pr.sub.2-Ph-, 3,(4 or 5)-Bu.sub.2-Ph-, 3,(4 or 5)-(CN).sub.2-Ph-, 3,(4 or 5)-(NO.sub.2).sub.2-Ph-, 3,(4 or 5)-(NH.sub.2).sub.2-Ph-, 3,(4 or 5)-(MeO).sub.2-Ph-, 3,(4 or 5)-(CF.sub.3).sub.2-Ph-, 2-Me-Ph-, 3-Me-Ph-, 4-Me-Ph-, 2-Et-Ph-, 3-Et-Ph-, 4-Et-Ph-, 2-Pr-Ph-, 3-Pr-Ph-, 4-Pr-Ph-, 2-Bu-Ph-, 3-Bu-Ph-, 4-Bu-Ph-, 2-(CN)-Ph-, 3-(CN)-Ph-, 4-(CN)-Ph-, 2-(NO.sub.2)-Ph-, 3-(NO.sub.2)-Ph-, 4-(NO.sub.2)-Ph-, 2-(NH.sub.2)-Ph-, 3-(NH.sub.2)-Ph-, 4-(NH.sub.2)-Ph-, 2-MeO-Ph-, 4-MeO-Ph-, 2-(NH.sub.2CO)-Ph-, 3-(NH.sub.2CO)-Ph-, 4-(NH.sub.2CO)-Ph-, 2-CF.sub.3-Ph-, 3-CF.sub.3-Ph-, 4-CF.sub.3-Ph-, 2-CF.sub.3O-Ph-, 3-CF.sub.3O-Ph-, and 4-CF.sub.3O-Ph-); and

(290) a saturated or unsaturated, substituted or unsubstituted, heterocyclic group such as an aromatic heterocyclic group and/or a non-aromatic heterocyclic group (such as pyrrole-2-yl, pyrrole-3-yl, pyrazole-3-yl, pyrazole-4-yl, imidazole-2-yl, imidazole-4-yl, 1,2,3-triazole-4-yl, 1,2,3-triazole-5-yl, 1,2,4-triazole-3-yl, 1,2,4-triazole-5-yl, pyridin-2-yl, pyridin-3-yl, pyridin-4-yl, pyridazine-3-yl, pyridazine-4-yl, pyrimidin-2-yl, pyrimidin-4-yl, pyrimidin-5-yl, pyrazine-2-yl, pyrrolidine-2-yl, pyrrolidine-3-yl, piperidine-2-yl, piperidine-3-yl, piperidine-4-yl, 2-azapiperidine-3-yl, 2-azapiperidine-4-yl, 3-azapiperidine-2-yl, 3-azapiperidine-4-yl, 3-azapiperidine-5-yl, piperazine-2-yl, furan-2-yl, furan-3-yl, pyran-2-yl, pyran-3-yl, pyran-4-yl, 2-azapyran-3-yl, 2-azapyran-4-yl, 2-azapyran-5-yl, 2-azapyran-6-yl, 3-azapyran-2-yl, 3-azapyran-4-yl, 3-azapyran-5-yl, 3-azapyran-6-yl, 4-azapyran-2-yl, 4-azapyran-3-yl, 4-azapyran-5-yl, 4-azapyran-6-yl, tetrahydrofuran-2-yl, tetrahydrofuran-3-yl, 2-aza-tetrahydrofuran-3-yl, 2-aza-tetrahydrofuran-4-yl, 2-aza-tetrahydrofuran-5-yl, 3-aza-tetrahydrofuran-2-yl, 3-aza-tetrahydrofuran-4-yl, 3-aza-tetrahydrofuran-5-yl, tetrahydropyran-2-yl, tetrahydropyran-3-yl, tetrahydropyran-4-yl, 2-aza-tetrahydropyran-3-yl, 2-aza-tetrahydropyran-4-yl, 2-aza-tetrahydropyran-5-yl, 2-aza-tetrahydropyran-6-yl, 3-aza-tetrahydropyran-2-yl, 3-aza-tetrahydropyran-4-yl, 3-aza-tetrahydropyran-5-yl, 3-aza-tetrahydropyran-6-yl,morpholine-2-yl, morpholine-3-yl, thiophen-2-yl, thiophen-3-yl, isothiazol-3-yl, isothiazol-4-yl, isothiazol-5-yl, thiazol-2-yl, thiazol-4-yl, thiazol-5-yl, thiopyran-2-yl, thiopyran-3-yl, thiopyran-4-yl, 2-azathiopyran-3-yl, 2-azathiopyran-4-yl, 2-azathiopyran-5-yl, 2-azathiopyran-6-yl, 3-azathiopyran-2-yl, 3-azathiopyran-4-yl, 3-azathiopyran-5-yl, 3-azathiopyran-6-yl, 4-azathiopyran-2-yl, 4-azathiopyran-3-yl, 4-azathiopyran-5-yl, 4-azathiopyran-6-yl, thiolane-2-yl, thiolane-3-yl, thiane-2-yl, thiane-3-yl, thiane-4-yl, oxazol-2-yl, oxazol-4-yl, oxazol-5-yl, isoxazol-3-yl, isoxazol-4-yl, isoxazol-5-yl, furazan-3-yl, (1,3,4-oxadiazol)-2-yl, (1,3,4-oxadiazol)-5-yl, (1,2,4-oxadiazol)-3-yl, (1,2,4-oxadiazol)-5-yl; and tetrazole-5-yl); and

(291) fused ring systems comprising two or three or more fused rings, which rings may be substituted or unsubstituted, preferably wherein the rings are selected from one, two, or more of the above aromatic groups and aromatic or non-aromatic heterocyclic groups, (e.g. fused ring systems such as naphthalene, anthracene, phenanthrene, phenalene, biphenylene, pentalene, indene, as-indacene, s-indacene, acenaphthylene, fluorene, fluoranthene, acephenanthrylene, azulene, heptalene, indole, indazole, benzimidazole, 4-azaindole, 5-azaindole, 6-azaindole, 7-azaindole, isoindole, 4-azaisoindole, 5-azaisoindole, 6-azaisoindole, 7-azaisoindole, indolizine, 1-azaindolizine, 2-azaindolizine, 3-azaindolizine, 5-azaindolizine, 6-azaindolizine, 7-azaindolizine, 8-azaindolizine, 9-azaindolizine, purine, carbazole, carboline, benzofuran, isobenzofuran, benzothiophene, isobenzothiophene, quinoline, cinnoline, quinazoline, quinoxaline, 5-azaquinoline, 6-azaquinoline, 7-azaquinoline, naphthyridine, isoquinoline, phthalazine, 6-azaisoquinoline, 7-azaisoquinoline, pteridine, chromene, isochromene, acridine, phenanthridine, perimidine, phenanthroline, phenoxazine, xanthene, phenoxanthiin, and/or thianthrene);

(292) and wherein R.sup.63 and R.sup.64 are independently selected from H and the following groups provided that one of R.sup.63 and R.sup.64 is not H:

(293) a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 alkyl group (such as Me, Et, Pr, i-Pr, n-Bu, i-Bu, t-Bu, pentyl and hexyl);

(294) a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 halogenated alkyl group (such as CH.sub.2F, CHF.sub.2, CH.sub.2Cl, CH.sub.2Br, CH.sub.2I, CF.sub.3, CCl.sub.3CBr.sub.3, CI.sub.3, CH.sub.2CF.sub.3, CH.sub.2CCl.sub.3, CH.sub.2CBr.sub.3, and CH.sub.2CI.sub.3);

(295) a substituted or unsubstituted linear or branched primary secondary or tertiary C.sub.1-C.sub.6 amine group (such as CH.sub.2NH.sub.2, CH.sub.2NMeH, CH.sub.2NMe.sub.2, CH.sub.2NEtH, CH.sub.2NEtMe, CH.sub.2NEt.sub.2, CH.sub.2NPrH, CH.sub.2NPrMe, and CH.sub.2NPrEt);

(296) a substituted or unsubstituted cyclic C.sub.3-C.sub.8 alkyl group (such as cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl and cyclooctyl);

(297) a substituted or unsubstituted linear or branched C.sub.1-C.sub.6 alcohol group (such as CH.sub.2OH, CH.sub.2CH.sub.2OH, CH.sub.2CH.sub.2CH.sub.2OH, CH(CH.sub.3)CH.sub.2OH, C(CH.sub.3).sub.2OH, CH.sub.2CH.sub.2CH.sub.2CH.sub.2OH, CH(CH.sub.3)CH.sub.2CH.sub.2OH, CH(CH.sub.3)CH(CH.sub.3)OH, CH(CH.sub.2CH.sub.3)CH.sub.2OH, C(CH.sub.3).sub.2CH.sub.2OH, CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2OH, and CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2CH.sub.2OH);

(298) a substituted or unsubstituted cyclic amine or amido group (such as pyrrolidin-2-yl, pyrrolidin-3-yl, piperidin-2-yl, piperidin-3-yl, piperidin-4-yl, piperazin-2-yl, piperazin-3-yl, morpholin-2-yl, morpholin-3-yl, 2-keto-pyrrolidinyl, 3-keto-pyrrolidinyl, 2-keto-piperidinyl, 3-keto-piperidinyl, 4-keto-piperidinyl), 2-keto-piperazinyl, and 3-keto-piperazinyl;

(299) a substituted or unsubstituted aromatic group (such as Ph-, 2-F-Ph-, 3-F-Ph-, 4-F-Ph-, 2-Cl-Ph-, 3-Cl-Ph-, 4-Cl-Ph-, 2-Br-Ph-, 3-Br-Ph-, 4-Br-Ph-, 2-I-Ph-, 3-I-Ph, 4-I-Ph-, 2,(3,4,5 or 6)-F.sub.2-Ph-, 2,(3,4,5 or 6)-Cl.sub.2-Ph-, 2,(3,4,5 or 6)-Br.sub.2-Ph-, 2,(3,4,5 or 6)-I.sub.2-Ph-, 2,(3,4,5 or 6)-Me.sub.2-Ph-, 2,(3,4,5 or 6)-Et.sub.2-Ph-, 2,(3,4,5 or 6)-Pr.sub.2-Ph-, 2,(3,4,5 or 6)-Bu.sub.2-Ph-, 2,(3,4,5 or 6)-(CN).sub.2-Ph-, 2,(3,4,5 or 6)-(NO.sub.2).sub.2-Ph-, 2,(3,4,5 or 6)-(NH.sub.2).sub.2-Ph-, 2,(3,4,5 or 6)-(MeO).sub.2-Ph-, 2,(3,4,5 or 6)-(CF.sub.3).sub.2-Ph-, 3,(4 or 5)-F.sub.2-Ph-, 3,(4 or 5)-Cl.sub.2-Ph-, 3,(4 or 5)-Br.sub.2-Ph-, 3,(4 or 5)-I.sub.2-Ph-, 3,(4 or 5)-Me.sub.2-Ph-, 3,(4 or 5)-Et.sub.2-Ph-, 3,(4 or 5)-Pr.sub.2-Ph-, 3,(4 or 5)-Bu.sub.2-Ph-, 3,(4 or 5)-(CN).sub.2-Ph-, 3,(4 or 5)-(NO.sub.2).sub.2-Ph-, 3,(4 or 5)-(NH.sub.2).sub.2-Ph-, 3,(4 or 5)-(MeO)2-Ph-, 3,(4 or 5)-(CF.sub.3).sub.2-Ph-, 2-Me-Ph-, 3-Me-Ph-, 4-Me-Ph-, 2-Et-Ph-, 3-Et-Ph-, 4-Et-Ph-, 2-Pr-Ph-, 3-Pr-Ph-, 4-Pr-Ph-, 2-Bu-Ph-, 3-Bu-Ph-, 4-Bu-Ph-, 2-(CN)-Ph-, 3-(CN)-Ph-, 4-(CN)-Ph-, 2-(NO.sub.2)-Ph-, 3-(NO.sub.2)-Ph-, 4-(NO.sub.2)-Ph-, 2-(NH.sub.2)-Ph-, 3-(NH.sub.2)-Ph-, 4-(NH.sub.2)-Ph-, 2-MeO-Ph-, 3-MeO-Ph-, 4-MeO-Ph-, 2-(NH.sub.2CO)-Ph-, 3-(NH.sub.2CO)-Ph-, 4-(NH.sub.2CO)-Ph-, 2-CF.sub.3-Ph-, 3-CF.sub.3-Ph-, 4-CF.sub.3-Ph-, 2-CF.sub.3O-Ph-, 3-CF.sub.3O-Ph-, and 4-CF.sub.3O-Ph-);

(300) a substituted or unsubstituted saturated or unsaturated heterocyclic group such as an aromatic heterocyclic group (such as pyridin-2-yl, pyridin-3-yl, pyridin-4-yl, thiophen-2-yl, thiophen-3-yl, pyrimidin-2-yl, pyrimidin-4-yl, pyrimidin-5-yl, pyrimidin-6-yl, tetrazole-5-yl, oxazol-2-yl, oxazol-4-yl, oxazol-5-yl, isoxazol-3-yl, isoxazol-4-yl, isoxazol-5-yl, (1,3,4-oxadiazol)-2-yl, (1,3,4-oxadiazol)-5-yl, (1,3-thiazol)-2-yl, (1,3-thiazol)-4-yl, (1,3-thiazol)-5-yl, furan-2-yl, and furan-3-yl); or such as a substituted or unsubstituted saturated heterocyclic group (such as piperidin-2-yl, piperidin-3-yl, piperidin-4-yl, piperazin-2-yl, piperazin-3-yl, tetrahydrofuran-2-yl, and tetrahydrofuran-3-yl, tetrahydropyran-2-yl, tetrahydropyran-3-yl, tetrahydropyran-4-yl); and

(301) a group where R.sup.63 and R.sup.64 together form a 3-6 membered substituted or unsubstituted saturated or unsaturated carbocyclic or heterocyclic ring (such as a cyclopropyl, cyclobutyl, cyclopentyl, cyclopentenyl, cyclohexyl, cyclohexenyl, aziridine, azetidine, pyrrolidine, piperidine, piperazine, oxetane, tetrahydrofuran or tetrahydropyran ring);

(302) provided that when one of R.sup.63 and R.sup.64 is H and the other is Me, R.sup.65 is not 3-MeO-Ph-, and that when R.sup.65 is -Ph, and one of R.sup.63 and R.sup.64 is H, the other of R.sup.63 and R.sup.64 is not CH(OH)-Ph.

(303) Thus, the present invention provides a TDO or IDO compound for use in medicine, which compound comprises a formula selected from one of the following:

(304) ##STR00037## ##STR00038## ##STR00039## ##STR00040## ##STR00041## ##STR00042## ##STR00043## ##STR00044## ##STR00045## ##STR00046## ##STR00047## ##STR00048## ##STR00049## ##STR00050## ##STR00051## ##STR00052## ##STR00053## ##STR00054## ##STR00055## ##STR00056## ##STR00057## ##STR00058## ##STR00059## ##STR00060## ##STR00061## ##STR00062## ##STR00063## ##STR00064## ##STR00065## ##STR00066## ##STR00067## ##STR00068## ##STR00069## ##STR00070## ##STR00071## ##STR00072## ##STR00073## ##STR00074## ##STR00075## ##STR00076## ##STR00077## ##STR00078## ##STR00079## ##STR00080## ##STR00081## ##STR00082## ##STR00083## ##STR00084## ##STR00085## ##STR00086## ##STR00087## ##STR00088## ##STR00089## ##STR00090## ##STR00091##

(305) In the above compounds, where stereochemistry is indicated at a chiral centre, the invention also includes both of the possible isolated enantiomers and also the racemic mixture. In addition, where a racemic mixture is indicated at a chiral centre (such as by a wavy line) the invention also includes both isolated enantiomers and the racemic mixture. Further, where no stereochemistry is given at a chiral centre the invention also includes both isolated enantiomers and the racemic mixture. Thus, the compounds of the present invention extend to isolated enantiomers, and/or a mixture of two or more enantiomers, and/or a mixture of two or more diastereomers (e.g. where there is more than one chiral centre), and/or a mixture of two or more epimers, and/or racemic mixtures. In addition to this, the above formulae (and all formulae herein) are intended to represent all tautomeric forms equivalent to the corresponding formula.

(306) In the context of the present invention, the medicinal use is not especially limited, provided that it is a use which is facilitated by the TDO and/or the IDO inhibitory effect of the compound. Thus, the compounds of the invention may be for use in any disease, condition or disorder that may be prevented, ameliorated or treated using a TDO and/or IDO inhibitor. Typically this comprises a disease condition and/or a disorder selected from: a cancer, an inflammatory condition, an infectious disease, a central nervous system disease or disorder, coronary heart disease, chronic renal failure, post anaesthesia cognitive dysfunction, a disease condition and/or a disorder relating to female reproductive health including contraception or abortion, and cataracts.

(307) When the disease, condition or disorder is an inflammatory disease, condition or disorder, it is not especially limited, provided that the disease, condition or disorder is one which may be treated, prevented or ameliorated by using a TDO and/or IDO inhibitor. However, typically the inflammatory condition is a condition relating to immune B cell, T cell, dendritic cell, natural killer cell, macrophage, and/or neutrophil dysregulation.

(308) When the disease, condition or disorder is a cancer, it is not especially limited, provided that the cancer is one which may be treated, prevented or ameliorated by using a TDO and/or IDO inhibitor. Thus the cancer may be a cancer selected from: a solid or liquid tumour including cancer of the eye, brain (such as gliomas, glioblastomas, medullablastomas, craniopharyngioma, ependymoma, and astrocytoma), spinal cord, kidney, mouth, lip, throat, oral cavity, nasal cavity, small intestine, colon, parathyroid gland, gall bladder, head and neck, breast, bone, bile duct, cervix, heart, hypopharyngeal gland, lung, bronchus, liver, skin, ureter, urethra, testicles, vagina, anus, laryngeal gland, ovary, thyroid, oesophagus, nasopharyngeal gland, pituitary gland, salivary gland, prostate, pancreas, adrenal glands; an endometrial cancer, oral cancer, melanoma, neuroblastoma, gastric cancer, an angiomatosis, a hemangioblastoma, a pheochromocytoma, a pancreatic cyst, a renal cell carcinoma, Wilms' tumour, squamous cell carcinoma, sarcoma, osteosarcoma, Kaposi sarcoma, rhabdomyosarcoma, hepatocellular carcinoma, PTEN Hamartoma-Tumor Syndromes (PHTS) (such as Lhermitte-Duclos disease, Cowden syndrome, Proteus syndrome, and Proteus-like syndrome), leukaemias and lymphomas (such as acute lymphoblastic leukaemia, chronic lymphocytic leukaemia, acute myelogenous leukaemia, chronic myelogenous leukaemia, hairy cell leukaemia, T-cell prolymphocytic leukemia (T-PLL), large granular lymphocytic leukemia, adult T-cell leukemia, juvenile myelomonocytic leukaemia, Hodgkin lymphoma, non-Hodgkin lymphoma, mantle lymphoma, follicular lymphoma, primary effusion lymphoma, AIDS-related lymphoma, Hodgkin lymphoma, diffuse B cell lymphoma, Burkitt lymphoma, and cutaneous T-cell lymphoma). However, when the compound is an IDO inhibitor, typically (but not exclusively) the cancer is a cancer selected from acute myeloid leukemia (AML), a small-cell lung cancer, a melanoma, an ovarian cancer, a colorectal cancer, a pancreatic cancer, an endometrial cancer, and a skin papilloma. When the compound is a TDO inhibitor, typically (but not exclusively) the cancer is a cancer selected from a glioma, and a hepatocellular carcinoma.

(309) When the disease is an infectious disease, it is not especially limited, provided that the disease is one which may be treated, prevented or ameliorated by using a TDO and/or IDO inhibitor. However, typically the infectious disease is selected from a bacterial infection and a viral infection, preferably a gut infection, sepsis, sepsis induced hypotension, HIV infection and HCV infection.

(310) When the disease, condition or disorder is a central nervous system disease, condition or disorder, it is not especially limited, provided that the disease, condition or disorder is one which may be treated, prevented or ameliorated by using a TDO and/or IDO inhibitor. However, the central nervous system disease, condition or disorder is typically selected from amyotrophic lateral sclerosis (ALS), Huntington's disease, Alzheimer's disease, pain, a psychiatric disorder, multiple sclerosis, Parkinson's disease, and HIV related neurocognitive decline.

(311) When the disease, condition or disorder is one relating to female reproductive health, it is not especially limited provided that the disease, condition or disorder is one which may be treated, prevented or ameliorated by using a TDO and/or IDO inhibitor. In typical embodiments the disease, condition or disorder is selected from gynaecological disorders such as endometriosis. Conditions relating to female reproductive health that are included in the invention include contraception and abortion such that the compounds of the invention may be used as a contraceptive and/or abortive agent.

(312) The present invention also provides a pharmaceutical composition comprising a compound as defined above. Whilst the pharmaceutical composition is not especially limited, typically the composition further comprises a pharmaceutically acceptable additive and/or excipient. In the pharmaceutical composition, the compound as defined above may be present in the form described above, but may alternatively be in a form suitable for improving bioavailability, solubility, and/or activity, and/or may be in a form suitable for improving formulation. Thus, the compound may be in the form of a pharmaceutically acceptable salt, hydrate, acid, ester, or other alternative suitable form. Typically, the composition is for treating a disease, condition or disorder as defined above. In some instances, the compound may be present in the composition as a pharmaceutically acceptable salt, or other alternative form of the compound, in order to ameliorate pharmaceutical formulation.

(313) In some embodiments the pharmaceutical composition is a composition for treating a cancer, further comprising a further agent for treating cancer. The further agent for treating cancer is not especially limited, provided that it affords some utility for cancer treatment. However, typically the further agent for treating cancer is selected from anti-microtubule agents, platinum coordination complexes, alkylating agents, antibiotic agents, topoisomerase II inhibitors, antimetabolites, topoisomerase I inhibitors, hormones and hormone analogues, signal transduction pathway inhibitors, non-receptor tyrosine kinase angiogenesis inhibitors, immunotherapeutic agents, proapoptotic agents and cell cycle signalling inhibitors. An immunotherapeutic agent may consist of but is not limited to an anti-tumour vaccine, an oncolytic virus, an immune stimulatory antibody such as anti-CTLA4, anti-PD1, anti-PDL-1, anti-OX40, anti-41BB, anti-CD27, anti-anti-CD40, anti-LAG3, anti-TIM3, and anti-GITR, a novel adjuvant, a peptide, a cytokine, a chimeric antigen receptor T cell therapy (CAR-T), a small molecule immune modulator, tumour microenvironment modulators, and anti-angiogenic agents.

(314) Further provided by the invention is a method of treating a disease and/or a condition and/or a disorder, which method comprises administering to a patient a compound or a composition as defined above. The method is typically a method for treating any disease condition or disorder mentioned herein. In typical embodiments, the method is a method for treating a cancer. Preferably such a method comprises administering to a patient a compound or a composition as defined above and a further agent for treating cancer as defined above. The compound or composition and the further agent may administered simultaneously, sequentially or separately, depending upon the agents and patients involved, and the type of cancer indicated.

(315) Typically, in all embodiments of the invention, both above and below, the patient is an animal, typically a mammal, and more typically a human.

(316) Further provided by the invention is a method of synthesis of a compound as defined above, which method comprises a step of substituting the substituent (typically an H group) at the 2-position of a substituted or unsubstituted indole or azaindole compound, or a part thereof (typically when an amide or other coupling reaction is performed) with a different substituent, and/or performing a coupling reaction (such as an amide coupling reaction) on a substituent in the 2-position.

(317) In addition to compounds for use in medicine, the present invention, and in particular the synthetic method, provides compounds that were not previously known, such compounds comprising a formula selected from one of the following:

(318) ##STR00092## ##STR00093## ##STR00094## ##STR00095## ##STR00096## ##STR00097## ##STR00098## ##STR00099## ##STR00100## ##STR00101## ##STR00102## ##STR00103## ##STR00104## ##STR00105## ##STR00106## ##STR00107## ##STR00108## ##STR00109## ##STR00110## ##STR00111## ##STR00112## ##STR00113## ##STR00114## ##STR00115## ##STR00116## ##STR00117## ##STR00118## ##STR00119## ##STR00120## ##STR00121## ##STR00122## ##STR00123## ##STR00124## ##STR00125## ##STR00126## ##STR00127##

(319) In some instances, the above formulae (and all formulae herein) are shown in non-stereoisomeric form, in other cases in stereoisomeric form, and in yet further cases shown in a manner to indicate both enantiomers (using a wavy line). For the avoidance of doubt, in the present context a single formula is intended to represent all possible stereoisomers of a particular structure, including all possible isolated enantiomers corresponding to the formula, all possible mixtures of enantiomers corresponding to the formula, all possible mixtures of diastereomers corresponding to the formula, all possible mixtures of epimers corresponding to the formula and all possible racemic mixtures corresponding to the formula. In addition to this, the above formulae (and all formulae herein) are intended to represent all tautomeric forms equivalent to the corresponding formula.

(320) In addition to the above compounds that were not previously known, the present invention, and in particular the synthetic method, provides further compounds comprising a formula selected from one of the following:

(321) ##STR00128##

(322) These compounds have previously been synthesised as racemic mixtures, but not as isolated enantiomers or other mixtures of stereoisomers that are not racemic. Accordingly, the invention extends to such compounds wherein the compound may comprise an isolated enantiomer corresponding to the formula, or may comprise a non-racemic mixture of enantiomers corresponding to the formula, a mixture of diastereomers corresponding to the formula, and/or a mixture of epimers corresponding to the formula.

(323) The invention will now be described in more detail, by way of example only, with reference to the following specific embodiments.

EXAMPLES

(324) Exemplary compounds of the invention were prepared, and tested to determine their effect as TDO and/or IDO inhibitors. These were compared with reference compound REF:

(325) ##STR00129##

(326) Exemplary Syntheses of Compounds of the Invention

(327) As has been mentioned, the compounds of the invention may be synthesised using known coupling reactions, and starting materials that are readily available. Exemplary syntheses of two compounds of the invention are shown below.

(328) Compound 48 was synthesised according to the following route:

(329) ##STR00130##

(330) Compound 141 was synthesised according to the following route:

(331) ##STR00131##

(332) Assays

(333) Two different types of assay were employed: 1. A TDO and IDO biochemical coupled assay which utilised recombinantly produced and purified TDO and IDO enzymes in combination with the enzyme formamidase. This coupled enzyme system allowed conversion of N-formylkynurenine produced by TDO or IDO activity to kynurenine which was then quantified by fluorescence following addition of Erhlich's Reagent. 2. A cell-based assay for detecting the effect of test compounds on kynurenine production in two different cancer cell types. This assay utilised cancer cells which expressed either TDO or IDO and as such was used as a means of testing compound activity at these two enzymes in a cell-based context. The protocols for these are set out below.

(334) TDO Biochemical Assays

(335) 2 M of human TDO protein was pre-incubated for 10 minutes at RT with test compounds in the presence of 50 mM KH.sub.2PO.sub.4, pH 7.0, 0.5 mM EDTA, 0.5 mM EGTA, 0.05% Triton X-100, 20 mM ascorbate, 500 U/ml catalase, 10 M methylene blue at RT in a 384 well plate. 0.05 g/l kynurenine formamidase and 330 M or 178 M L-tryptophan were added and the assays were incubated at room temperature (RT) for 17 min. Assays were stopped and the level of kynurenine was determined by incubation with Ehrlich's reagent to a final concentration of 1.33% at RT for 5 min. Fluorescence intensity was read at 475 nm/530 nm.

(336) IDO Biochemical Assays

(337) 0.17 M of human IDO protein was pre-incubated for 10 min or 120 min at RT with test compounds in the presence of 50 mM KPO.sub.4, pH 7.0, 0.5 mM EDTA, 0.5 mM EGTA, 0.05% Triton X-100, 20 mM ascorbate, 500 U/ml catalase, 10 M methylene blue at RT in a 384 well plate. 0.05 g/l kynurenine formamidase and 45 M or 121 M L-tryptophan (L-Trp) were added and the assays were incubated at RT for 17 min. Assays were stopped and the level of kynurenine was determined by incubation with Ehrlich's reagent to a final concentration of 1.33% at RT for 5 min. Fluorescence intensity was read at 475 nm/530 nm.

(338) TDO and IDO Cell-Based Assays

(339) A172 human glioblastoma (ATCC) were grown in DMEM+2 mM L-glutamine medium supplemented with 10% foetal bovine serum and SKOV-3 ovary adenocarcinoma (ATCC) cells were grown in McCoys 5A+L-glutamax medium supplemented with 15% foetal bovine serum. On the day of assay, cells were detached using trypsin-EDTA (0.25% v/v), re-suspended in assay media (RPMI 1640 phenol red free+L-glutamine supplemented with 10% dialysed foetal bovine serum). A172 cells were seeded at 30K cells per well and SKOV-3 cells at 40K cells per well into 96-well plates containing test samples/vehicle control together with 500 M L-Trp. Cells were then incubated for 48 h at 37 C., 5% CO.sub.2. In SK-OV-3 cells, IFN was also added at 500 ng/ml for the 48 h incubation in order to induce expression of IDO. Plates were centrifuged and the supernatant was removed and incubated for 5 min in the presence of 1% Erhlich's reagent. Kynurenine levels were then quantified by measuring absorbance at 490 nm.

(340) The pIC50 values for a variety of test compounds are shown in Table 1.

(341) TABLE-US-00001 TABLE 1 pIC50 values for the inhibition of IDO (SKOV-3 cells) and TDO (A172 cells) determined for test compounds TDO cellular IDO cellular Compound assay (A172) assay (SKOV3) 1 ++ 2 ++ 3 +++ 4 + ++ 5 + 6 + + 7 +++ 8 + 9 +++ 10 + 11 ++ ++ 12 +++ 13 + 14 ++ 15 ++ +++ 16 + +++ 17 + +++ 18 +++ 19 +++ 20 + 21 ++ 22 + ++ 23 +++ 24 + ++ 25 +++ +++ 26 ++ +++ 27 ++ 28 + 29 + 30 + 31 + 32 ++ 33 ++ 34 +++ 35 + 36 + +++ 37 + 38 + ++ 39 ++ 40 ++ + 41 +++ 42 ++ 43 ++ +++ 44 + +++ 45 + 46 ++ 47 ++ ++ 48 ++ +++ 49 + ++ 50 +++ +++ 51 +++ 52 + + 53 + 54 + 55 + 56 + + 57 + 58 ++ 59 + 60 + + 61 +++ +++ 62 +++ +++ 63 + + 64 ++ ++ 65 +++ 66 ++ 67 ++ + 68 ++ +++ 69 ++ +++ 70 ++ +++ 71 + +++ 72 +++ 73 + 74 + 75 +++ 76 + 77 + +++ 78 + ++ 79 + 80 ++ 81 + 82 +++ +++ 83 +++ 84 ++ +++ 85 ++ ++ 86 +++ +++ 87 + +++ 88 +++ 89 +++ 90 +++ 91 + 92 + +++ 93 + +++ 94 + ++ 95 + 96 + 97 + ++ 98 +++ 99 + +++ 100 ++ +++ 101 + +++ 102 + 103 +++ 104 + ++ 105 +++ 106 + 107 ++ 108 ++ 109 ++ 110 ++ 111 ++ 112 +++ 113 +++ 114 +++ 115 + +++ 116 ++ 117 + ++ 118 + ++ 119 + 120 +++ 121 +++ 122 ++ 123 + ++ 124 +++ 125 + +++ 126 +++ 127 + 128 + +++ 129 ++ 130 ++ 131 +++ 132 + +++ 133 +++ 134 +++ 135 +++ 136 +++ 137 +++ 138 +++ 139 + 140 +++ 141 +++ 142 + +++ 143 + +++ 144 + +++ 145 +++ 146 +++ 147 +++ 148 + +++ 149 +++ 150 ++ +++ 151 +++ 152 ++ 153 +++ 154 + 155 +++ 156 +++ 157 ++ 158 +++ 159 ++ 160 +++ 161 +++ 162 ++ 163 + 164 +++ 165 + 166 + 167 ++ 168 + +++ 169 ++ 170 + +++ 171 +++ 172 + 173 +++ 174 ++ +++ 175 +++ 176 +++ 177 ++ 178 +++ 179 ++ 180 + 181 + 182 +++ 183 + +++ 184 ++ 185 + + 186 +++ 187 + 188 + +++ 189 ++ 190 + 191 +++ 192 + 193 +++ 194 +++ 195 ++ 196 + 197 + 198 +++ 199 +++ 200 +++ 201 + 202 +++ 203 + ++ 204 +++ 205 +++ 206 + 207 + +++ 208 + +++ 209 ++ +++ 210 + +++ 211 + 212 + ++ 213 +++ 214 +++ 215 +++ 216 + 217 +++ 218 + 219 +++ 220 +++ 221 + 222 ++ 223 +++ 224 ++ ++ 225 +++ 226 +++ 227 ++ +++ 228 ++ ++ 229 +++ +++ 230 +++ 231 +++ 232 +++ 233 + 234 ++ +++ 235 +++ 236 +++ 237 ++ 238 +++ 239 + 240 +++ 241 +++ 242 +++ 243 +++ 244 +++ 245 +++ 246 + +++ 247 +++ 248 +++ 249 + +++ 250 +++ 251 +++ 252 +++ 253 +++ 254 +++ 255 + +++ 256 + + 257 +++ 258 +++ 259 +++ 260 + +++ 261 +++ 262 + 263 +++ 264 +++ 265 +++ 266 +++ 267 ++ +++ 268 +++ 269 +++ 270 +++ 271 ++ +++ 272 +++ 273 +++ 274 +++ 275 +++ Key: +++ = pIC.sub.50 5.50 ++ = pIC.sub.50 5.00-<5.50 + = pIC.sub.50 4.50-<5.00 = pIC.sub.50 <4.50

(342) The Table shows that a large number of the test compounds show strong TDO and IDO inhibitory function in cell-based assays. This compares with the REF compound, which scored and on each of the tests, and which is therefore disclaimed in the present invention, since it is not TDO or IDO active.

(343) Biochemical enzyme assays were conducted according to the protocols described above, and the results confirmed the bona fide activity of the compounds as enzyme inhibitors. Compounds 83, 160, 178, 205, 215, 230 and 231 all showed a pIC.sub.50 in the hIDO assay of >5. For example, compound 83 showed a pIC.sub.50 in hIDO of 5.24. This compares with the REF compound, which scored <3.99 and <3.99 on the hTDO and hIDO tests respectively.