C07D261/14

PROCESS FOR THE PREPARATION OF OPTICALLY ACTIVE ISOXAZOLINE COMPOUNDS
20170217953 · 2017-08-03 · ·

The present invention relates to a process for the preparation of a compound of formula (I) wherein A.sub.1 and A.sub.2 are C—H, or one of A.sub.1 and A.sub.2 is C—H and the other is N; R.sub.1 is C.sub.1-C.sub.4alkyl, C.sub.1-C.sub.4haloalkyl or C.sub.3-C.sub.6cycloalkyl; each R.sub.2 is independently bromo, chloro, fluoro or trifluoromethyl; R.sub.3 is hydrogen; R.sub.4 is hydrogen, halogen, methyl, halomethyl or cyano; or R.sub.3 and R.sub.4 together form a bridging 1,3-butadiene group; R.sub.5 is chlorodifluoro-methyl or trifluoromethyl; n is 2 or 3; by reacting a compound of formula (II) wherein A.sub.1, A.sub.2, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and n is as defined under formula (I) above, with hydroxylamine, a base and a chiral catalyst, characterized in that the chiral catalyst is a dimeric chiral catalyst of formula (III) wherein R.sub.6, R.sub.7, R.sub.8, R.sub.9, R.sub.10 and X are as defmed in claim 1.

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PROCESS FOR THE PREPARATION OF OPTICALLY ACTIVE ISOXAZOLINE COMPOUNDS
20170217953 · 2017-08-03 · ·

The present invention relates to a process for the preparation of a compound of formula (I) wherein A.sub.1 and A.sub.2 are C—H, or one of A.sub.1 and A.sub.2 is C—H and the other is N; R.sub.1 is C.sub.1-C.sub.4alkyl, C.sub.1-C.sub.4haloalkyl or C.sub.3-C.sub.6cycloalkyl; each R.sub.2 is independently bromo, chloro, fluoro or trifluoromethyl; R.sub.3 is hydrogen; R.sub.4 is hydrogen, halogen, methyl, halomethyl or cyano; or R.sub.3 and R.sub.4 together form a bridging 1,3-butadiene group; R.sub.5 is chlorodifluoro-methyl or trifluoromethyl; n is 2 or 3; by reacting a compound of formula (II) wherein A.sub.1, A.sub.2, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and n is as defined under formula (I) above, with hydroxylamine, a base and a chiral catalyst, characterized in that the chiral catalyst is a dimeric chiral catalyst of formula (III) wherein R.sub.6, R.sub.7, R.sub.8, R.sub.9, R.sub.10 and X are as defmed in claim 1.

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Bisarylsulfonamides useful in the treatment of inflammation and cancer

A compound of formula (I), useful for the treatment of cancer, inflammation and inflammatory disorders, and a pharmaceutical composition containing the compound. ##STR00001##

Bisarylsulfonamides useful in the treatment of inflammation and cancer

A compound of formula (I), useful for the treatment of cancer, inflammation and inflammatory disorders, and a pharmaceutical composition containing the compound. ##STR00001##

TrkA kinase inhibitors, compositions and methods thereof

The present invention is directed to benzyl urea compounds of formula (I) which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence may be useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor Trk-A, Trk-B and/or Trk-C. ##STR00001##

TrkA kinase inhibitors, compositions and methods thereof

The present invention is directed to benzyl urea compounds of formula (I) which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence may be useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor Trk-A, Trk-B and/or Trk-C. ##STR00001##

PHARMACEUTICAL COMPOUND

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 (I): wherein X.sup.1 is selected from C and N; X.sup.3 and X.sup.5 may be the same or different and each is independently selected from C, N, O and S; Y is selected from N and O; Z is selected from C, N and O; each bond represented by a dotted line may independently be a double bond or a single bond, provided that valencies at each ring atom are maintained and provided that the ring Q contains at least one double bond and provided that the atom N has a double bond; R.sup.3 and R.sup.5 may be present or absent and may be the same or different and each is independently selected from H and a substituted or unsubstituted organic group, provided that the number of R.sup.3 groups present is such that the valency of X.sup.3 is maintained, and the number of R.sup.5 groups present is such that the valency of X.sup.5 is maintained; each R.sup.11 and R.sup.12 may be present or absent and may be the same or different and each is independently selected from H and a substituted or unsubstituted organic group, provided that the number of R.sup.11 and R.sup.12 groups present is such that the valency of Z is maintained; R.sup.21 is selected from H and a substituted or unsubstituted organic group; R.sup.22 may be present or absent and is selected from H and a substituted or unsubstituted organic group; and Cy is a cyclic organic group.

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PHARMACEUTICAL COMPOUND

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 (I): wherein X.sup.1 is selected from C and N; X.sup.3 and X.sup.5 may be the same or different and each is independently selected from C, N, O and S; Y is selected from N and O; Z is selected from C, N and O; each bond represented by a dotted line may independently be a double bond or a single bond, provided that valencies at each ring atom are maintained and provided that the ring Q contains at least one double bond and provided that the atom N has a double bond; R.sup.3 and R.sup.5 may be present or absent and may be the same or different and each is independently selected from H and a substituted or unsubstituted organic group, provided that the number of R.sup.3 groups present is such that the valency of X.sup.3 is maintained, and the number of R.sup.5 groups present is such that the valency of X.sup.5 is maintained; each R.sup.11 and R.sup.12 may be present or absent and may be the same or different and each is independently selected from H and a substituted or unsubstituted organic group, provided that the number of R.sup.11 and R.sup.12 groups present is such that the valency of Z is maintained; R.sup.21 is selected from H and a substituted or unsubstituted organic group; R.sup.22 may be present or absent and is selected from H and a substituted or unsubstituted organic group; and Cy is a cyclic organic group.

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HERBICIDAL COMPOUNDS

The present invention relates to a compound of formula (I) wherein: wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9, R.sup.10, R.sup.11 and G are as defined herein; and wherein the compound of formula (I) is optionally present as an agrochemically acceptable salt thereof. These compounds are thought to be suitable for use as herbicides. The invention therefore also relates to a method of controlling weeds, especially grassy monocotyledonous weeds, in crops of useful plants, comprising applying a compound of formula (I), or a herbicidal composition comprising such a compound, to the plants or to the locus thereof.

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HERBICIDAL COMPOUNDS

The present invention relates to a compound of formula (I) wherein: wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.9, R.sup.10, R.sup.11 and G are as defined herein; and wherein the compound of formula (I) is optionally present as an agrochemically acceptable salt thereof. These compounds are thought to be suitable for use as herbicides. The invention therefore also relates to a method of controlling weeds, especially grassy monocotyledonous weeds, in crops of useful plants, comprising applying a compound of formula (I), or a herbicidal composition comprising such a compound, to the plants or to the locus thereof.

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