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US 7,250,440 B2Granted
(Hydroxyphenyl)-1H-indole-3-carbaldehyde oxime derivatives as estrogenic agents
AssigneeWyeth
InventorsRichard Eric Mewshaw, Stephen Marc Bowen, Eric Steven Manas
Life of this patent
Estimating the term…
Abstract
This invention provides estrogen receptor modulators of formula I, having the structure where R1, R2, R3, and R4 are as defined in the specification, or a pharmaceutically acceptable salt thereof.
Claims10
A compound of the formula:
- wherein:
- R1 is hydrogen, lower alkyl, halogen, CN, or lower alkoxy;
- R2 is hydrogen, lower alkyl, or phenyl;
- or
- R1 and R2 together may form a 5-7 membered ring;
- and
- R3, and R4 are each, independently, H, OH, halogen, CN, phenyl, substituted phenyl, lower alkyl or lower alkoxy;
- where said substituted phenyl is substituted with one or more of nitro, cyano, —N(R11)(R12), halo, hydroxy, carboxy, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl, alkoxy, aryloxy, heteroaryloxy, alkylalkoxy, alkoxycarbonyl, alkoxyalkoxy, perfluoroalkyl, perfluoroalkoxy, arylalkyl, alkylaryl, hydroxyalkyl, alkoxyalkyl, alkylthio, —S(O)2—N(R11)(R12), —C(═O)—N(R11)(R12), (R11)(R12)N-alkyl, (R11)(R12)N-alkoxyalky, (R11)(R12)N-alkylaryloxyalkyl, —S(O)s-aryl, or —S(O)s—heteroaryl, where R,11 and R12 are each independently hydrogen or alkyl, and s is 0, 1, or 2;
- or
- a pharmaceutically acceptable salt thereof;
- provided that R1 is lower alkyl or R2 is H or lower alkyl, or R1 and R2 together form a 6-membered ring.
8 more elements
A pharmaceutical composition comprising
- a compound of the formula:
- wherein:
- R1 is hydrogen, lower alkyl, halogen, CN, or lower alkoxy;
- R2 is hydrogen, lower alkyl, or phenyl;
- or
- R1 and R2 together may form a 5-7 membered ring;
- and
- R3, and R4 are each, independently, H, OH, halogen, CN, phenyl, substituted phenyl, lower alkyl or lower alkoxy;
- or
- where said substituted phenyl is substituted with one or more of nitro, cyano, —N(R11)(R12), halo, hydroxy, carboxy, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl, alkoxy, aryloxy, heteroaryloxy, alkylalkoxy, alkoxycarbonyl, alkoxyalkoxy, perfluoroalkyl, perfluoroalkoxy, arylalkyl, alkylaryl, hydroxyalkyl, alkoxyalkyl, alkylthio, —S(O)2—N(R11)(R12), —C(═O)—N(R11)(R12), (R11)(R12)N-alkyl, (R11)(R12)N-alkoxyalky, (R11)(R12)N-alkylaryloxyalkyl, —S(O)s-aryl, or —S(O)s-heteroaryl, where R,11 and R12 are each independently hydrogen or alkyl, and s is 0, 1, or 2;
- or
- a pharmaceutically acceptable salt thereof;
- provided that R1 is lower alkyl or R2 is H or lower alkyl, or R1 and R2 together form a 6-membered ring and
- a pharmaceutical.
11 more elements
Dependencies are inferred from the claim text.