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US 2003/0069291 A1Published application
3-heterocyclylpropanohydroxamic acid PCP inhibitors
AssigneePfizer Inc.
InventorsSimon Bailey, Paul Vincent Fish, Kim James, Gavin Alistar Whitlock
Life of this patent
Estimating the term…
Abstract
Compounds of formula (I): 1 and their salts, solvates, hydrates and prodrugs are useful PCP inhibitors, processes for making the same, compositions comprising the same, and methods of treating a PCP-mediated condition or disease using the same.
Claims17
A compound of formula (I):
- 285
- 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, C58 cycloalkenyl or C38 cycloalkyl unsubstituted or substituted by one or more fluorine atoms;
- wherein aryl comprises phenyl unsubstituted or substituted by one or more substituents independently selected from R1, OH, SO2(C1-4 alkyl) and C(O)p(C1-4 alkyl) groups;
- wherein p=0, 1 or 2;
- [HET] is a divalent heterocyclic moiety selected from:
- 286
- wherein Z is H or C1-4 alkyl;
- Y is a mono- or bicyclic unsaturated ring system containing from 5 to IO ring atoms, of which up to 4 of said ring atoms are hetero-atoms independently selected from N, O and S, and said ring system is unsubstituted or substituted by one or more substituents independently selected from ═O, C1-4 alkyl, C1-4 alkoxy, NR1R2, SO2NR1R2, CO2R1, CONR1R2, CH2CO2R1, NR1CO2R2, NR1SO2R2 or het1;
- wherein R1 and R2 are each independently selected from H and C1-4 alkyl unsubstituted or substituted by C1-4 alkoxy;
- wherein het1 is a N-linked 4- to 6-membered mono- or bicyclic heterocycle unsubstituted or containing 1 or 2 further hetero ring atoms independently selected from N and O, which heterocycle is unsubstituted or substituted by one or more substituents independently selected from ═O, C1-4 alkyl, C1-4 alkoxy, NR1R2, SO2NR1R2, CO2R1, CONR1R2, CH2CO2R1, NR1CO2R1, NR1SO2R2 or het2;
- wherein het2 is a N-linked 4- to 6-membered mono- or bicyclic heterocycle unsubstituted or containing 1 or 2 further hetero ring atoms independently selected from N and O;
- and the pharmaceutically acceptable salts, solvates, hydrates and prodrugs thereof.
11 more elements
A compound of formula (II), (III), (IV) or (V):
- 293
- wherein:
- X is C1-6 alkylene or C2-6 alkenylene, unsubstituted or substituted by one or more fluorine atoms;
- R is aryl, C5-8 cycloalkenyl or C3-8 cycloalkyl, unsubstituted or substituted by one or more fluorine atoms;
- wherein aryl comprises phenyl unsubstituted or substituted by one or more substituents independently selected from R1, OH, SO2(C1-4 alkyl) and C(O)p(C1-4 alkyl) groups;
- wherein p=0, 1 or 2;
- L is a suitable leaving group;
- P is a NHO-protecting group;
- P1 is a suitable carboxylic acid protecting group;
- [HET] is a divalent heterocyclic moiety selected from:
- 294
- wherein Z is H or C1-4 alkyl;
- Y is a mono- or bicyclic unsaturated ring system containing from 5 to 10 ring atoms, of which up to 4 of said ring atoms are hetero-atoms independently selected from N, O and S, and said ring system is unsubstituted or substituted by one or more substituents independently selected from ═O, C1-4 alkyl, C1-4 alkoxy, NR1R2, SO2NR1R2, CO2R1, CONR1R2, CH2CO2R1, NR1CO2R2, NR1SO2R2 or het1;
- wherein R1 and R2 are each independently selected from H and C14 alkyl unsubstituted or substituted by C14 alkoxy;
- wherein het1 is a N-linked 4- to 6-membered mono- or bicyclic heterocycle unsubstituted or containing 1 or 2 further hetero ring atoms independently selected from N and O, which heterocycle is unsubstituted or substituted by one or more substituents independently selected from ═O, C1-4 alkyl, C1-4 alkoxy, NR1R2, SO2NR1R2, CO2R1, CONR1R2, CH2CO2R1, NR1CO2R2, NR1SO2R2 or het2;
- wherein het2 is a N-linked 4- to 6-membered mono- or bicyclic heterocycle unsubstituted or containing 1 or 2 further hetero ring atoms independently selected from N and O;
- and the pharmaceutically acceptable salts, solvates, hydrates and prodrugs thereof.
14 more elements
Dependencies are inferred from the claim text.