Title:
STEROID DERIVATIVE
Document Type and Number:
Japanese Patent JP2514778
Kind Code:
B2
Abstract:
PURPOSE: To obtain a new compound, having excellent inhibiting action on testosterone 5α-reductases and low toxicity and useful as a preventing and therapeutic agent for diseases caused by an excess of 5α-dihydrotestosterone, especially prostatic hypertrophy.
CONSTITUTION: This compound is expressed by formula I [R1 is H, 1-6C alkyl etc.; R2 is aryl or 1-6C alkyl or diarylamino substituted with 5- to 6-membered cyclic aryl; R3 is (protected)carboxy or expressed by the formula CONHSO2R4 (R4 is R1 other than H)] and its salt, e.g. 17β-[N-(diphenylmethyl)- carbamoyl]androsta-3,5-diene-3-carboxylic acid. The compound is obtained by reacting a compound expressed by formula II (R5 is carboxy-protecting group) with a di-1-6C alkyl or a diaryl phosphorocyanidate, then hydrolyzing resultant product with a base, providing a compound expressed by formula III, subsequently reacting the prepared compound expressed by formula III with a compound expressed by the formula HNR1R2, affording a compound expressed by formula IV and then hydrolyzing the resultant compound with a base.
Inventors:
KOJIMA KOICHI
KURATA HITOSHI
ISHIBASHI KIMIKI
HORIKOSHI HIROYOSHI
HAMADA TAKAKAZU
KURATA HITOSHI
ISHIBASHI KIMIKI
HORIKOSHI HIROYOSHI
HAMADA TAKAKAZU
Application Number:
JP9284093A
Publication Date:
July 10, 1996
Filing Date:
April 20, 1993
Export Citation:
Assignee:
SANKYO CO
International Classes:
A61K31/56; A61K31/568; C07J1/00; A61K31/575; A61P5/00; A61P13/02; A61P15/00; C07J41/00; C07J43/00; A61K; C07J; (IPC1-7): C07J41/00; A61K31/575
Attorney, Agent or Firm:
Akio Ohno (2 outside)