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Title:
TRIPHENYLETHYLENE COMPOUNDS AS SELECTIVE ESTROGEN RECEPTOR MODULATORS
Document Type and Number:
WIPO Patent Application WO2005033056
Kind Code:
A3
Abstract:
The present invention relates to novel compounds of Formula (I) with a variety of therapeutic uses, more particularly novel prodrugs that are particularly useful for delivering a parent compound for selective estrogen receptor modulation. R<1 >is -C(O)-alkyl, -C(O)-aryl, -C(O)-heteroaryl, -C(O)-cycloalkyl, -C(O)-(CH2)n-NR<4>R<5>, -C(O)-O-alkyl, C(O)-(CH2)n-O-alkyl, -C(O)-(CH2)n-haloalkyl, -C(O)-(CH2)n-heterocylcyl, or -PO 3 H 2; R<4> and R<5> each independently are selected from H and alkyl; and n is 1 to 6.

Inventors:
EADDY III JOHN FRED (US)
HEYER DENNIS (US)
KATAMREDDY SUBBA REDDY (US)
MARTIN MICHAEL TOLAR (US)
MCCLURE MICHAEL SCOTT (US)
RANDHAWA AMARJIT SAB (US)
SAMANO VICENTE (US)
RAY JOHN ALBERT (US)
Application Number:
PCT/US2004/032918
Publication Date:
June 23, 2005
Filing Date:
October 04, 2004
Export Citation:
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Assignee:
SMITHKLINE BEECHAM CORP (US)
EADDY III JOHN FRED (US)
HEYER DENNIS (US)
KATAMREDDY SUBBA REDDY (US)
MARTIN MICHAEL TOLAR (US)
MCCLURE MICHAEL SCOTT (US)
RANDHAWA AMARJIT SAB (US)
SAMANO VICENTE (US)
RAY JOHN ALBERT (US)
International Classes:
A61K31/341; A61K31/381; A61K31/495; C07C59/52; C07C69/017; C07C69/63; C07C69/708; C07C69/732; C07C69/75; C07C69/78; C07C69/96; C07C229/10; C07D211/14; C07D261/18; C07D295/15; C07D307/24; C07D307/54; C07D333/38; C07D333/40; C07F9/12; (IPC1-7): C07D333/38; C07D307/54; C07D261/18; C07D211/14; A61K31/495; A61K31/381; A61K31/341; A61P15/02; A61P19/10; A61P35/00
Domestic Patent References:
WO2001077057A22001-10-18
WO2001077055A22001-10-18
WO2003016270A22003-02-27
WO1992004310A11992-03-19
Other References:
SCANLAN T S ET AL: "Differential SERM activation of the estrogen receptors (ERalpha and ERbeta) at AP-1 sites", CHEMISTRY AND BIOLOGY, CURRENT BIOLOGY, LONDON, GB, vol. 8, no. 5, 2001, pages 427 - 436, XP002220838, ISSN: 1074-5521
WILLSON T M ET AL: "3-Ú4-(1,2-DIPHENYLBUT-1-ENYL)PHENYLACRYLIC ACID: A NON-STEROIDAL ESTROGEN WITH FUCNTIONAL SLECTIVITY FOR BONE OVER UTERUS IN RATS", JOURNAL OF MEDICINAL CHEMISTRY, AMERICAN CHEMICAL SOCIETY. WASHINGTON, US, vol. 37, no. 11, 25 May 1994 (1994-05-25), pages 1550 - 1552, XP002057515, ISSN: 0022-2623
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