Disclosed are compounds of formulae (I), (II), and (II)I: and pharmaceutically acceptable salts thereof, wherein the variables, R, R.sub.1, R.sub.2, R.sub.3, R.sub.101, L, D, Q, Y, X, and Z are defined herein. These compounds are useful for treating Gram-negative bacteria infections. ##STR00001##

Disclosed are compounds of formulae (I), (II), and (II)I: and pharmaceutically acceptable salts thereof, wherein the variables, R, R.sub.1, R.sub.2, R.sub.3, R.sub.101, L, D, Q, Y, X, and Z are defined herein. These compounds are useful for treating Gram-negative bacteria infections. ##STR00001##

The present invention pertains to novel thiocycloheptyne derivatives of general formula (I): and in particular to thiacycloalkynesulfoimine derivatives and their synthesis. The invention also relates to the use of the novel thiocycloheptyne derivatives in coupling reactions with linkers and drugs. The invention further relates to the use of the novel thiocycloheptynes in bioorthogonal (copper-free) click reactions. The invention further pertains to the use of the novel thiocycloheptyne derivatives in the generation of advanced multifunctional drug delivery systems (drug-loaded) nanoparticles.

##STR00001##

The present invention relates to a method for synthesizing a compound of Formula (I) ##STR00001## as defined herein, comprising: (i) activating a compound of Formula (II) ##STR00002## as defined herein, by reacting said compound of Formula (II) with a compound of Formula (III) ##STR00003## as defined herein, in the presence of a base, to obtain a compound of Formula (IV) ##STR00004## as defined herein; and (ii) reacting the compound of Formula (IV) with an electrophile to obtain the compound of Formula (I). The present invention further relates to the organocatalysts used in the described methods and their respective uses.

The present invention relates to a method for synthesizing a compound of Formula (I) ##STR00001## as defined herein, comprising: (i) activating a compound of Formula (II) ##STR00002## as defined herein, by reacting said compound of Formula (II) with a compound of Formula (III) ##STR00003## as defined herein, in the presence of a base, to obtain a compound of Formula (IV) ##STR00004## as defined herein; and (ii) reacting the compound of Formula (IV) with an electrophile to obtain the compound of Formula (I). The present invention further relates to the organocatalysts used in the described methods and their respective uses.

The present invention relates to a compound of formula (I): wherein L is an optionally substituted heterocyclic group excluding unsubstituted monocyclic pyridine groups; wherein a is 0, 1 or 2; wherein R.sup.1 is H or with R.sup.2 is a bond; wherein R.sup.2 is an optionally substituted alkoxy or aryloxy group, or with R.sup.1 forms a bond; wherein R.sup.3 is an optionally substituted alkyl group; and wherein R.sup.4 is CH.sub.2, CMe.sub.2 or O. Such compounds may be used in the treatment or prophylaxis of a disease or condition in which inhibition of acute inflammation and/or promotion of its resolution and/or suppression of fibrosis.

##STR00001##

A compound of formula (I) wherein: M is selected from Mo or W; X is selected from O or NR.sup.5; R.sup.1 and R.sup.2 are independently selected from H, C.sub.1-6 alkyl, and aryl; C.sub.1-6 alkyl and aryl optionally being substituted with one or more of C.sub.1-6 alkyl, C.sub.1-6 alkoxy, and OC.sub.6H.sub.5; R.sup.3 is selected from a nitrogen-containing aromatic heterocycle being bound to M via said nitrogen; and from halogen; R.sup.4 is an aryl oxy group being bound to M via said oxygen of said aryl oxy group; wherein said aryl group Ar of said aryl oxy group is bound to a group Cat such to form a cationic ligand Cat.sup.+-ZArO, wherein Z is either a covalent bond or a linker; R.sup.5 is alkyl or aryl, optionally substituted.

##STR00001##

The present invention is directed to heterocycloalkenyl derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the GPR120 and/or GPR40 receptors. More particularly, the compounds of the present invention are agonists of GPR120 and/or GPR40, useful in the treatment of, for example, obesity, Type II Diabetes Mellitus, dyslipidemia, etc.

Disclosed are compounds of formulae (I), (II), and (II)I: and pharmaceutically acceptable salts thereof, wherein the variables, R, R.sub.1, R.sub.2, R.sub.3, R.sub.101, L, D, Q, Y, X, and Z are defined herein. These compounds are useful for treating Gram-negative bacteria infections. ##STR00001##

Disclosed are compounds of formulae (I), (II), and (II)I: and pharmaceutically acceptable salts thereof, wherein the variables, R, R.sub.1, R.sub.2, R.sub.3, R.sub.101, L, D, Q, Y, X, and Z are defined herein. These compounds are useful for treating Gram-negative bacteria infections. ##STR00001##