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Title:
2-AMINOPHENOXY(THIO)ALKYLCARBONYLAMINO ACID DERIVATIVE, PRODUCTION THEREOF AND 5ALPHA-REDUCTASE INHIBITOR CONTAINING SAID COMPOUND AS ACTIVE INGREDIENT
Document Type and Number:
Japanese Patent JPS62198653
Kind Code:
A
Abstract:

NEW MATERIAL:A compound expressed by formula I (R1 is H, 1W10C alkyl or 1W10C alkoxy; R2 is H or 1W4C alkyl; R3 is H, halogen or 1W4C alkyl; R4 is amino acid residue; A is single bond or unsubstituted or 1W4C alkyl- substituted methylene, ethylene or vinylene; B is 1W4C alkylene, X is O or S).

EXAMPLE: 4-[2-(4-Amyl-3-methylcinnamoyl)aminophenoxy]butanoylglycine.

USE: With inhibitory action on 5α-reductase and useful for preventing and treating diseases caused by excess production of dihydrotestosterone by 5α-reductase, e.g. male pattern alopecia and prostatic hypertrophy.

PREPARATION: A compound expressed by formula II and a compound expressed by the formula H-R4 are subjected to amidation reaction to afford the aimed compound expressed by formula I.


Inventors:
ARAI YOSHINOBU
NAKAI HISAO
TERAJIMA HIROSHI
Application Number:
JP4044486A
Publication Date:
September 02, 1987
Filing Date:
February 27, 1986
Export Citation:
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Assignee:
ONO PHARMACEUTICAL CO
International Classes:
A61K8/00; A61K8/44; A61K31/195; A61K31/215; A61K31/22; A61P13/02; A61P15/00; A61P43/00; A61Q5/00; A61Q7/00; C07C67/00; C07C231/00; C07C231/02; C07C235/20; C07C235/38; C07C235/56; C12N9/99; (IPC1-7): A61K7/06; A61K31/195; C07C102/00; C07C103/78; C12N9/99
Attorney, Agent or Firm:
Kunihisa Oya