Title:
17-ALPHA-SUBSTITUTED-11-BETA-SUBSTITUTED-4-ARYL AND 21-SUBSTITUTED 19-NORPREGNA 21-SUBSTITUTED 19-NORPREGNADIENEDIONE AS ANTIPROGESTATIONAL AGENTS
Document Type and Number:
WIPO Patent Application WO2001074840
Kind Code:
A3
Abstract:
The present invention relates, inter alia, to compounds having the general formula (I) in which: R<1> is a member selected from the group consisting of -OCH3 -SCH3, -N(CH3)2, -NHCH3, -NC4H8, -NC5H10, -NC4H8O, -CHO, -CH(OH)CH3, -C(O)CH3, -O(CH2)2N(CH3)2, and -O(CH2)2NC5H10; R<2> is a member selected from the group consisting of hydrogen, halogen, alkyl, acyl, hydroxy, alkoxy (e.g., methoxy, ethoxy, vinyloxy, ethynyloxy, cyclopropyloxy, etc.), acyloxy (e.g., acetoxy, glycinate, etc.), alkylcarbonate, cypionyloxy, S-alkyl, -SCN, S-acyl and -OC(O)R<6>, wherein R<6> is a functional group including, but not limited to, alkyl (e.g., methyl, ethyl, etc.), alkoxy ester (e.g., -CH2OCH3) and alkoxy (-OCH3); R<3> is a member selected from the group consisting of alkyl, hydroxy, alkoxy and acyloxy; R<4> is a member selected from the group consisting of hydrogen and alkyl; and X is a member selected from the group consisting of =0 and =N-OR<5>, wherein R<5> is a member selected from the group consisting of hydrogen and alkyl.The compounds of Formula I antagonize progesterone.
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Inventors:
KIM HYUN K (US)
BLYE RICHARD P (US)
RAO PEMMARAJU N (US)
CESSAC JAMES W (US)
ACOSTA CARMIE K (US)
SIMMONS ANNE MARIE (US)
BLYE RICHARD P (US)
RAO PEMMARAJU N (US)
CESSAC JAMES W (US)
ACOSTA CARMIE K (US)
SIMMONS ANNE MARIE (US)
Application Number:
PCT/US2001/008681
Publication Date:
May 02, 2002
Filing Date:
March 16, 2001
Export Citation:
Assignee:
US GOV HEALTH & HUMAN SERV (US)
KIM HYUN K (US)
BLYE RICHARD P (US)
RAO PEMMARAJU N (US)
CESSAC JAMES W (US)
ACOSTA CARMIE K (US)
SIMMONS ANNE MARIE (US)
KIM HYUN K (US)
BLYE RICHARD P (US)
RAO PEMMARAJU N (US)
CESSAC JAMES W (US)
ACOSTA CARMIE K (US)
SIMMONS ANNE MARIE (US)
International Classes:
A61K31/57; A61K31/575; A61K31/58; A61P5/24; A61P5/36; A61P15/00; A61P15/04; A61P15/18; A61P35/00; C07C401/00; C07J5/00; C07J7/00; C07J9/00; C07J31/00; C07J41/00; C07J43/00; (IPC1-7): C07J41/00; A61K31/57; C07J31/00; C07J7/00; C07J5/00; C07J9/00; A61K31/575; A61P5/36
Domestic Patent References:
| WO1999045022A1 | 1999-09-10 | |||
| WO1997041145A1 | 1997-11-06 | |||
| WO1989012448A1 | 1989-12-28 | |||
| WO2000034306A1 | 2000-06-15 |
Other References:
RAO P N ET AL: "11beta-Substituted 13beta-ethyl gonane derivatives exhibit reversal of antiprogestational activity", STEROIDS: STRUCTURE, FUNCTION, AND REGULATION,US,ELSEVIER SCIENCE PUBLISHERS, NEW YORK, NY, vol. 63, no. 1, 1998, pages 50 - 57, XP004103060, ISSN: 0039-128X
RAO P N ET AL: "New 11beta-aryl-substituted steroids exhibit both progestational and antiprogestational activity", STEROIDS: STRUCTURE, FUNCTION, AND REGULATION,US,ELSEVIER SCIENCE PUBLISHERS, NEW YORK, NY, vol. 63, no. 10, 1 October 1998 (1998-10-01), pages 523 - 530, XP004140834, ISSN: 0039-128X
RAO P N ET AL: "New 11beta-aryl-substituted steroids exhibit both progestational and antiprogestational activity", STEROIDS: STRUCTURE, FUNCTION, AND REGULATION,US,ELSEVIER SCIENCE PUBLISHERS, NEW YORK, NY, vol. 63, no. 10, 1 October 1998 (1998-10-01), pages 523 - 530, XP004140834, ISSN: 0039-128X
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