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Title:
【発明の名称】新規の抗プロゲステロンとしての21―置換プロゲステロン誘導体
Document Type and Number:
Japanese Patent JP2000509396
Kind Code:
A
Abstract:
A compound having the general formula: in which: R1 is a member selected from the group consisting of —OCH3, —SCH3, —N(CH3)2, —NHCH3, —CHO, —COCH3 and —CHOHCH3; R2 is a member selected from the group consisting of halogen, alkyl, acyl, hydroxy, alkoxy, acyloxy, alkyl carbonate, cypionyloxy, S-alkyl and S-acyl; R3 is a member selected from the group consisting of alkyl, hydroxy, alkoxy and acyloxy; R4 is a member selected from the group consisting of hydrogen and alkyl; and X is a member selected from the group consisting of ═O and ═N—OR5, wherein R5 is a member selected from the group consisting of hydrogen and alkyl. In addition to providing the compounds of Formula I, the present invention provides methods wherein the compounds of Formula I are advantageously used, inter alia, to antagonize endogenous progesterone; to induce menses; to treat endometriosis; to treat dysmenorrhea; to treat endocrine hormone-dependent tumors; to treat uterine fibroids; to inhibit uterine endometrial proliferation; to induce labor; and for contraception.

Inventors:
Kim, Hyun, Kay.
Bry, Richard, Pee.
Lao, Pemmage, N.
Cessac, James, W.
Acosta, Kermy, Kay.
Application Number:
JP53923297A
Publication Date:
July 25, 2000
Filing Date:
April 30, 1997
Export Citation:
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Assignee:
US HEALTH (US)
International Classes:
A61K31/00; A61P5/24; C07J5/00; C07J7/00; C07J9/00; C07J21/00; C07J41/00; C07J51/00; A61K31/57; C07J71/00; (IPC1-7): C07J41/00; A61P5/24; A61K31/57; C07J5/00; C07J7/00; C07J21/00; C07J51/00; C07J71/00
Domestic Patent References:
JPH03505582A1991-12-05
JPS58201800A1983-11-24
JPH05509287A1993-12-22
JPH05509289A1993-12-22
JPH07258080A1995-10-09
Other References:
COUZINET, B., ET AL., DRUGS, vol. 35(3), JPN6008015780, pages 187 - 191, ISSN: 0001016899
WEBB, A.M.C., ET AL., BMJ, vol. 305(6859), JPN6008015783, pages 927 - 931, ISSN: 0001016900
ACOSTA, K., ET AL., J. CHEM. SOC., CHEM. COMMUN., JPN6008064109, pages 1985 - 1986, ISSN: 0001207097
Attorney, Agent or Firm:
Takashi Ishida (4 others)