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US 2003/0229121 A1Published application
Piperidine CCR-3 receptor antagonists
AssigneeSyntex (U.S.A.) Inc.
InventorsDaisy Joe Du Bois, Denis John Kertesz, Eric Brian Sjogren, David Bernard Smith, Beihan Wang
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Abstract
The invention provides compounds of Formula (I): 1 wherein: R1-R5, A, L, and X have any of the values defined in the specification that are CCR-3 receptor antagonists, pharmaceutical compositions containing them, methods for their use, and methods and intermediates useful for preparing them.
Claims28
A compound of Formula (I):
- 96
- wherein:
- R1 is (C1-C2)alkylene;
- R2 is optionally substituted phenyl;
- R3 is hydrogen, alkyl, acyl, aryl, or arylalkyl;
- ring A is a cycloalkyl, heterocyclyl, or optionally substituted phenyl;
- L is —C(═O)—, —C(═S)—, —SO2—, —C(═O)N(Ra)—, —C(═S) N(Ra)—, —SO2 N(Ra)—, —C(═O)O—, —C(═S)O—, —S(═O)2O—;
- where Ra is hydrogen, alkyl, acyl, aryl, arylalkyl, alkoxycarbonyl, or benzyloxycarbonyl;
- X is absent, —(CR′R″)O—, —(CR′R″)S—,—(CR′R″)NRb— or alkylene;
- where R′ and R″ are independently hydrogen or alkyl, and Rb is hydrogen or alkyl;
- R4 is aryl or heteroaryl;
- and
- R5 is hydrogen or alkyl;
- provided that when R1 is —CH2—, R2 is phenyl, R3 is hydrogen, R5 is hydrogen, A is phenyl, L is —C(═O)NH— and X is absent, then R4 is not 2,5-difluorophenyl;
- or
- prodrugs, individual isomers, racemic and non-racemic mixtures of isomers, and pharmaceutically acceptable salts thereof.
13 more elements
Dependencies are inferred from the claim text.