Title:
MEDICAMENT FOR PREVENTION OF PROSTATIC CARCINOMA BY 17BETA-N-MONO-SUBSTITUTED-CARBAMOYL-4-AZA-5ALPHA-ANDROST-1-EN-3-ONE
Document Type and Number:
Japanese Patent JP2538489
Kind Code:
B2
Abstract:
PURPOSE: To prepare a medicament composed of a new testosterone-5α-reductase inhibiting compd. and useful for the prevention of prostatic carcinoma for patients free from the symptom of prostatic carcinoma.
CONSTITUTION: The objective medicament contg. a compd. of formula I (R1 is H, ethyl or the like; R1 is a 1-12C chain alkyl, cycloalkyl or the like; R' is H or methyl; R" is H or β-methyl; R''' is H, α-methyl or the like) such as 17β-(N-t-butyl-carbamoyl)-4-aza-4-methyl-5α-androst-1-en-3-one or the like. The compd. represented by the formula I is obtd., e.g. by dehydrogenating the compd. represented by formula II, thereafter making the product to react with sodium hydride and alkyl iodide in succession to obtain the compd. represented by formula III, then hydrolyzing this with a strong base, thereafter acidificating it, successively subjecting the product to reflux together with triphenylphosphine and 2,2-dipyridylsulfinde to obtain 2-pyridylthioester represented by the formula IV and subsequently making this compd. to react with primary amine.
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Inventors:
GUREN JEI GOOMURII
ERIZABESU SUTONAA
ERIZABESU SUTONAA
Application Number:
JP32935992A
Publication Date:
September 25, 1996
Filing Date:
December 09, 1992
Export Citation:
Assignee:
MERCK & CO INC
International Classes:
A61K31/58; A61P35/00; C07J73/00; (IPC1-7): C07J73/00; A61K31/58
Domestic Patent References:
JP532693A | ||||
JP4230296A | ||||
JP54145669A | ||||
JP60222497A | ||||
JP3206096A | ||||
JP63192800A | ||||
JP63139195A | ||||
JP61257996A |
Other References:
【文献】国際公開91/12261(WO,A1)
【文献】欧州公開285383(EP,A1)
【文献】欧州公開285383(EP,A1)
Attorney, Agent or Firm:
Yoshio Kawaguchi (2 outside)