Organic compounds -- part of the class 532-570 series – Organic compounds – Carboxylic acids and salts thereof
Patent
1993-01-25
1994-10-11
Dees, Jose G.
Organic compounds -- part of the class 532-570 series
Organic compounds
Carboxylic acids and salts thereof
560 39, 560 41, 562450, C07C22928, C07C22934, A61K 31195
Patent
active
053548922
ABSTRACT:
The invention relates to biaryl substituted 4-amino-butyric acid derivatives of formula I ##STR1## wherein COX and COX' independently represent carboxyl or carboxyl derivatized in form of a pharmaceutically acceptable ester or amide; R.sub.1 represents hydrogen, lower alkyl, C.sub.3 -C.sub.7 -cycloalkyl-lower alkyl, aryl-lower alkyl, biaryl-lower alkyl, lower alkoxy, aryl-lower alkoxy, aryloxy, N-lower alkylamino, N,N-di-lower alkylamino, N-aryl-lower alkylamino, N,N-di-aryl-lower alkylamino, N-arylamino, N,N-diarylamino, lower alkanoylamino, aryl-lower alkanoylamino or aroylamino; R.sub.2 represents hydrogen, hydroxy, lower alkoxy, lower alkyl, aryl-lower alkyl, C.sub.3 -C.sub.7 -cycloalkyl-lower alkyl, amino-lower alkyl, hydroxy-lower alkyl, lower alkylthio-lower alkyl, lower alkoxy-lower alkyl, aryl-lower alkylthio-lower alkyl or aryl-lower alkoxy-lower alkyl; biaryl represents phenyl substituted by carbocyclic or heterocyclic aryl; A represents a direct bond, lower alkylene, phenylene or cyclohexylene; m represents 1 or zero, provided that m represents 1 when A is a direct bond; or pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising said compounds; methods for the preparation of said compounds and for the preparation of intermediates; and methods of treating disorders in mammals which are responsive to the inhibition of neutral endopeptidases by administration of said compounds to mammals in need of such treatment.
REFERENCES:
patent: 2543267 (1951-02-01), Bambas
patent: 4206232 (1980-06-01), Ondetti et al.
patent: 5021430 (1991-06-01), Ksander
patent: 5217996 (1993-06-01), Ksander
Chem. Abstr. 7912p, vol. 112, No. 1, (1990).
McMurry, "Organic Chemistry", 2nd ed., Brooks/Cole Pub. Co. (1988), p. 321.
Ciba-Geigy Corporation
Dees Jos,e G.
Frazier Barbara S.
Gruenfeld Norbert
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