174767-44-3Relevant academic research and scientific papers
DERIVATIVES OF PHOSPHINIC ACID USEFUL AS ENDOTHELIN CONVERTING ENZYME INHIBITORS
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, (2008/06/13)
Phosphinic acid derivatives of the structural formula STR1 or a pharmaceutically acceptable salt thereof, wherein R is H, alkyl or alkanoyloxymethylene;R 1, R 2, R 3 and R. sub.4 are H, alkyl, alkenyl, alkenylalkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, hydroxyalkyl, carboxyalkyl, thioalkyl, alkoxythioalkyl, aminoalkyl, alkylaminoalkyl, cycloalkyl-substituted alkyl or heterocycloalkyl; or R 1 and R 2 form a cycloalkyl ring of 3-8 members and R 3 and R 4 are as defined; or R 3 and R 4 form a cycloalkyl ring of 3-7 members and R 1 and R 2 are as defined; or R 1 and R 2 together, and R 3 and R 4 together, each form a cycloalkyl ring;R 5 is--OR. sub.9 or--NHR 9, wherein R. sub.9 is hydrogen or alkyl;n is 0 or 1;A. sub.1 is p-aminobenzoyl or p-aminobenzenesulfonyl, or A 1 and R 5 together form a radical of an α-aminoacyl derivative; andR. sub.6 is phenylmethoxycarbonyl, arylcarbonyl, heteroarylcarbonyl or--A 2--R. sub.7, wherein A 2 is a divalent α-aminoacyl radical, and R 7 is a substituent on the α-amino atom selected from H, R 8 OCO--, R. sub.8 SO 2--and R 8 NHCO--, wherein R 8 is aryl, arylmethyl or (C. sub.1-C 8)alkyl;are disclosed for use as endothelin converting enzyme inhibitors; also disclosed are a genus of novel compounds wherein R 3 and R 4 form a cycloalkyl ring, and pharmaceutical compositions comprising said novel compounds.
