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Title:
NEW STEROID HAVING SUBSTITUTED THIOETHYL GROUP AT 10-POSITION, ITS PRODUCTION, INTERMEDIATE IN ITS PRODUCTION, ITS USE AS DRUG AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME
Document Type and Number:
Japanese Patent JPH04120091
Kind Code:
A
Abstract:

NEW MATERIAL: A compound of formula I [R is H, an alkyl, an alkenyl, an alkynyl, an acyl, an aryl, etc.; X is O, N-O-R1 (R1 is an alkyl), formula II (RA and RB are each H, a halogen, etc.), (H,H) or formula III; Y is formula III (excluding X), formula IV (RC is H, an alkyl, etc.), formula V ((q) is 1-3); W is H, an alkyl, an alkylthio or an arylthio; Z is H or an alkyl; (n) is 0-2] and its salt.

EXAMPLE: 10β-[2-(Methyltio)ethyl]-estra-4,9(11)-diene-3,17-dione.

USE: The compound exhibits aromatase specific activity and is suitable for use in treatment of hormone-dependent diseases, especially estrogen-dependent diseases.

PROCESS: For example, a compound of formula VI (K and K' are each a protected keto group; Alk is an alkyl) is reduced, and the OH group in the resultant product is converted into SH group, then treated with a reactive derivative of the group R to give a compound of formula VII. Treatment of the product with a deblocking agent gives a corresponding compound of formula I.


Inventors:
JIYANFURANSOWA GUURUBESUTO
DOMINIKU RUSUYUISU
Application Number:
JP41267590A
Publication Date:
April 21, 1992
Filing Date:
December 21, 1990
Export Citation:
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Assignee:
ROUSSEL UCLAF
International Classes:
A61P5/32; A61P43/00; C07J1/00; C07J21/00; C07J31/00; A61K31/565; C07J41/00; (IPC1-7): A61K31/565; C07J1/00; C07J31/00; C07J41/00
Attorney, Agent or Firm:
Motohiro Kurauchi (1 outside)



 
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