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Title:
PEPTIDIC QUINUCLIDINE
Document Type and Number:
Japanese Patent JPH05320162
Kind Code:
A
Abstract:

PURPOSE: To provide a new compound having excellent P-substance antagonistic activity, thus useful as a medicine for gastrointestinal injuries, central nervous system disorders, inflammatory diseases, asthma, pain, or migraine.

CONSTITUTION: The compound of formula I { X1 is 1-5C (halogensubstituted) alkoxy; X2 is H, halogen, 1-5C alkyl, 2-5C alkenyl, etc.; Ar1 and Ar2 are each thienyl, (fluoro)phenyl, chlorophenyl, etc.; A is of formula II [R1 is H, 1-5C alkyl, benzyl, etc.; R2 is H, 1-5C (substituted) alkyl, benzyl, etc.; Y is CN, CH2Z (Z is OH, amino, 1-5C alkoxy, etc.), etc.]}, e.g. (3R, 4S, 5S, 6S)-N- carbamoylmethyl-5-(5-isopropyl-2-methoxybenzylamino)-6-diphenylmethyl-1- azabicyclo[2,2,2]octane-3-carboxamide. The compound of the formula I can be obtained by reaction of a compound of formula III with an amino acid protected with e.g. amino group in the presence of triethylamine to form a compound of formula IV, which is, in turn, made to react with a compound of formula V.


Inventors:
SATAKE KUNIO
WAKABAYASHI HIROAKI
NAKANE MASAMI
Application Number:
JP1992000307179
Publication Date:
December 03, 1993
Filing Date:
November 17, 1992
Export Citation:
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Assignee:
PFIZER PHARMA
International Classes:
A61K31/435; A61P1/00; A61P11/00; A61P25/00; A61P25/04; A61P25/06; A61P29/00; C07D453/02; (IPC1-7): C07D453/02; A61K31/435
Attorney, Agent or Firm:
Yoshio Kawaguchi (2 outside)



 
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