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US 6,645,993 B2Granted
3-heterocyclylpropanohydroxamic acid PCP inhibitors
AssigneeWarner-Lambert Company
InventorsPaul Vincent Fish, Jackie Diane Kendall, Gavin Alistair Whitlock
Life of this patent
Estimating the term…
Abstract
Compounds of formula (I) and their salts, solvates and prodrugs, wherein the substituents have the values mentioned herein, are Procollagen C-Proteinase (PCP) inhibitors and have utility in conditions mediated by PCP.
Claims15
A compound of formula I:
- wherein:
- X is C1-6 alkylene or C2-6 alkenylene, each of which is unsubstituted or substituted by one or more fluorine atoms;
- R is aryl, C3-8 cyclalkyl or C5-8 cycloalkenyl unsubstituted or substituted by one or more fluorine atoms;
- W is N;
- X1 is H or C1-C4 alkyl;
- Y1 is C1-C4 alkyl, unsubstituted or substituted by aryl, or by one or more halogen atoms, with the proviso that when Y1 is methyl, X1 is not H;
- or
- Y1 is aryl;
- or
- Y1 is a mono or bicyclic non-aromatic carbocyclic or heterocyclic moiety containing up to 10 ring atoms and which can include up to 3 ring heteroatoms, independently selected from N, O and S, which ring moiety is unsubstituted or substitued by one or more substituents independently slected from halogen, C1-C4 alkoxy and C1-C4 alkyl unsubstituted or substituted by one or more halogen;
- aryl is a mono or bicyclic aromatic carbocyclic or heterocyclic moiety containing up to 10 ring atoms, and which can include up to 3 ring heteroatoms, independently selected from N, O and S, which ring moiety is unsubstituted or substituted by one or more substitutents, independently selected from hologen, C1-C4 alkoxy and C1-C4 alkyl unsubstituted or substituted by halogen;
- and the pharmaceutically acceptable salts, solvates and prodrugs thereof.
9 more elements
A pharmaceutical composition comprising a therapeutically effective amount of a compound of formula (I):
- wherein:
- X is C1-6 alkylene or C2-6 alkenylene, each at which is unsubstituted or substituted by one or more fluorine atoms;
- R is aryl, C3-8 cycloallcyl or C5-8 cycloalkenyl unsubstituted or substituted by one or more fluorine atoms;
- W is N;
- X1 is H or C1-C4 alkyl;
- Y1 is C1-C4 alkyl, unsubstituted or substituted by aryl, or by one or more halogen atoms, with the proviso that when Y1 is methyl, X1 is not H;
- or
- Y1 is aryl;
- or
- Y1 is a mono or bicyclic non-aromatic carbocyclic or heterocyclic moiety containing up to 10 ring atoms and which can include up to 3 ring heteroatoms, independently selected from N, O and S, which ring moiety is unsubstituted or substituted by one or more substituents independently selected from halogen, C1-C4 alkoxy and C1-C4 alkyl unsubstituted or substituted by one or more halogen;
- aryl is a mono or bicyclic aromatic carbocyclic or heterocyclic moiety containing up to 10 ring atoms, and which can include up to 3 ring heteroatoms, independently selected from N, O and S, which ring moiety is unsubstituted or substituted by one or more substituents, independently selected from halogen, C1-C4 alkoxy and C1-C4 alkyl unsubstituted or substituted by halogen;
- including the salts, solvates and prodrugs thereof;
- and a pharmaceutically acceptable diluent, carrier or adjuvant.
10 more elements
(3R)-6-Cyclohexyl-N-hydroxy-3(3-{[(phenylsulfonyl)amino]carbonyl}-1,2,4-oxadiazol-5-yl)hexanamide and the pharmaceuticaily acceptable salts, solvates and prodrugs thereof.
Dependencies are inferred from the claim text.