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Title:
PHARMACEUTICAL COMPOSITION COMPRISING ANTAGONIST OF GONADOTROPIN-RELEASING HORMONE
Document Type and Number:
Japanese Patent JP2000212161
Kind Code:
A
Abstract:

To obtain a new compound useful for treating various sex hormone- related symptoms, especially gonadotropin-releasing hormone derived disorders such as sex hormone-dependent cancers, benign prostatic hyperplasia or uterine myoma.

A compound of formula I [A is a (substituted) 1-6C alkyl or the like; R0 is H, a (substituted) 1-6C alkyl or the like; R1 is a group of formula II (R13 is H, OH or the like; R14, R15 are each H, a 1-6C alkyl or the like) or the like; R2-R7, R9, R9a, R10a are each H, a (substituted) 1-6C alkyl or the like; R8 is a (substituted) 1-6C alkyl or the like; X is N, O or the like; (m) is 0-3], for example, morpholine-4-carboxylic acid 2-(3,5- dimethylphenyl)-3-[2-[4-[4-hydroxyphenyl]butylamino]ethyl]-1H-indol-5-yl ester. The compound of formula I is obtained by treating tryptamine of formula III with N-carboxyphthalimide at a temperature of 20-65°C for 12-48 hr in an inert organic solvent.


Inventors:
GOULET MARK
ASHTON WALLACE T
CHU LIN
FISHER MICHAEL H
WYVRATT MATTHEW J
Application Number:
JP2000036746A
Publication Date:
August 02, 2000
Filing Date:
December 10, 1996
Export Citation:
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Assignee:
MERCK & CO INC
International Classes:
A61K31/40; A61K31/403; A61K31/404; A61K31/4045; A61K31/407; A61K31/41; A61K31/415; A61K31/4155; A61K31/4178; A61K31/4184; A61K31/42; A61K31/422; A61K31/423; A61K31/425; A61K31/427; A61K31/437; A61K31/44; A61K31/4427; A61K31/443; A61K31/4439; A61K31/445; A61K31/454; A61K31/495; A61K31/496; A61K31/505; A61K31/506; A61K31/513; A61K31/535; A61K31/5377; A61K31/54; A61K31/541; A61K31/55; A61K31/551; A61P1/00; A61P5/00; C07D487/08; A61P5/02; A61P5/06; A61P5/24; A61P13/00; A61P13/02; A61P15/00; A61P35/00; A61P43/00; C07D209/14; C07D209/16; C07D401/04; C07D401/06; C07D401/12; C07D403/04; C07D403/06; C07D403/12; C07D405/12; C07D405/14; C07D413/04; C07D413/12; C07D417/04; C07D417/12; C07D471/10; (IPC1-7): C07D209/16; A61K31/4045; A61K31/407; A61K31/41; A61K31/4155; A61K31/4178; A61K31/4184; A61K31/422; A61K31/423; A61K31/427; A61K31/4439; A61K31/454; A61K31/496; A61K31/506; A61K31/5377; A61K31/541; A61K31/551; A61P1/00; A61P5/06; A61P5/24; A61P13/00; A61P15/00; A61P35/00; A61P43/00; C07D401/12; C07D403/04; C07D403/06; C07D403/12; C07D405/12; C07D405/14; C07D413/12; C07D417/04; C07D417/12; C07D471/10; C07D487/08
Attorney, Agent or Firm:
Yoshio Kawaguchi (1 person outside)