Title:
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 JP4260886
Kind Code:
B2
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.
Bry, Richard, Pee.
Lao, Pemmage, N.
Cessac, James, W.
Acosta, Kermy, Kay.
Application Number:
JP53923297A
Publication Date:
April 30, 2009
Filing Date:
April 30, 1997
Export Citation:
Assignee:
THE UNITED STATES OF AMERICA
International Classes:
A61K31/57; A61K31/00; C07J41/00; A61P5/24; A61P15/00; A61P15/04; A61P15/08; C07J5/00; C07J7/00; C07J9/00; C07J21/00; C07J51/00; C07J71/00
Domestic Patent References:
| JP3505582A | ||||
| JP58201800A | ||||
| JP5509287A | ||||
| JP5509289A | ||||
| JP7258080A |
Other References:
COUZINET, B., et al., Drugs, 35(3), pp.187-191 (1988)
WEBB, A.M.C., et al., BMJ, 305(6859), pp.927-931 (1992)
ACOSTA, K., et al., J. Chem. Soc., Chem. Commun., pp.1985-1986 (1994)
WEBB, A.M.C., et al., BMJ, 305(6859), pp.927-931 (1992)
ACOSTA, K., et al., J. Chem. Soc., Chem. Commun., pp.1985-1986 (1994)
Attorney, Agent or Firm:
Takashi Ishida
Fukumoto product
Toshio Toda
Masaya Nishiyama
Higuchi Souji
Fukumoto product
Toshio Toda
Masaya Nishiyama
Higuchi Souji