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US 2006/0142355 A1Published application
Carboxylic acid peri-substituted bicyclics for occlusive artery disease
AssigneedeCODE Chemistry, Inc.
InventorsJasbir Singh, Mark Gurney, Georgeta Hategan, Peng Yu, David Zembower, Nian Zhou, Alexandre Polozov, Wayne Zeller
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Abstract
Peri-substituted, fused bicyclic ring carboxylic acids useful for the treatment or prophylaxis of a prostaglandin-mediated disease or condition are disclosed. The compounds are of the general formula A representative example is:
Claims33
A compound of formula
- wherein
- A and B represent a pair of fused 5-, 6- or 7-membered rings, said A/B ring system containing from zero to four heteroatoms chosen from nitrogen, oxygen and sulfur and said rings additionally substituted with from zero to four substituents chosen independently from halogen, —OH, loweralkyl, —O-loweralkyl, fluoroloweralkyl, —O-lowerfluoroalkyl, methylenedioxy, ethylenedioxy, alkoxy-loweralkyl, hydroxyloweralkyl, oxo, oxide, —CN, nitro, —S-loweralkyl, amino, loweralkylamino, diloweralkylamino, diloweralkylaminoalkyl, carboxy, carboalkoxy, acyl, carboxamido, loweralkylsulfoxide, acylamino, phenyl, benzyl, spirothiazolidinyl, phenoxy and benzyloxy;
- with the proviso that 3-unsubstituted-2-oxoindoles, 3,4-dihydro-2-oxoquinolines and hexahydro-2-oxo-1H-thieno[3,4-d]imidazoles are excluded;
- a and b represent points of attachment of residues W and Y respectively and a and b are in a peri relationship to one another on said fused A/B ring system;
- d and e represent points of fusion between ring A and ring B in said fused A/B ring system;
- W is a linker comprising from 2 to 8 atoms in a chain;
- Y is a linker comprising from 1 to 8 atoms in a chain;
- M is chosen from aryl, substituted aryl, heterocyclyl, substituted heterocyclyl, C6 to C20 alkyl and substituted C6 to C20 alkyl;
- with the proviso that (E)-3-(4-benzyloxy-1H-indol-3-yl)-acrylic acid is excluded.
6 more elements
A compound of formula
- wherein
- R3and R4 are substituents in either or both rings, chosen independently from hydrogen, halogen, —OH, loweralkyl, —O-loweralkyl, fluoroloweralkyl, —O-lowerfluoroalkyl, methylenedioxy, ethylenedioxy, alkoxy-loweralkyl, hydroxyloweralkyl, oxo, oxide, —CN, nitro, —S-loweralkyl, amino, loweralkylamino, diloweralkylamino, diloweralkylaminoalkyl, carboxy, carboalkoxy, acyl, carboxamido, loweralkylsulfoxide, acylamino, phenyl, benzyl, spirothiazolidinyl, phenoxy and benzyloxy;
- W is a linker comprising from 0 to 8 atoms in a chain;
- Y is a linker comprising from 1 to 8 atoms in a chain;
- and
- M is chosen from aryl, substituted aryl, heterocyclyl, substituted heterocyclyl, C6 to C20 alkyl and substituted C6 to C20 alkyl.
3 more elements
Dependencies are inferred from the claim text.