C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
260/284, 260/317
C07D 209/42 (2006.01) C07D 215/54 (2006.01) C07K 5/02 (2006.01) C07K 5/062 (2006.01) A61K 38/00 (2006.01)
Patent
CA 1341206
Carboxyalkyl dipeptides, processes for their production and pharmaceutical compositions containing them. Disclosed are novel carboxyalkyl dipeptides which are useful as inhibitors of angiotensinconverting enzyme and as antihypertensive agents, having the formula (see formula I) and the pharmaceutically acceptable salts thereof, wherein R and R6 are for example hydroxy, lower alkoxy or aryllower-alkoxy; R1 is for example hydrogen, alkyl, lower alkoxy or aryloxy; R2 and R7 are the same or different and are hydrogen or lower alkyl; R3 is for example lower alkyl or phenyl lower alkyl; R4 and R5 are selected from hydrogen, lower alkyl and 2, or R4 and R5 taken together form a group represented by Q, U, V, Y, D or E wherein Z is Image wherein X1 and X2 independent of each other are O, S or CH2, R8 and R9 independent of each other are lower alkyl, lower alkenyl, lower alkynyl, cycloalkyl having 3 to 8 carbon atoms, hydroxy lower alkyl or -(CH2)n Ar, wherein n is 0, 1, 2 or 3 or R8 and R9 taken together form a bridge W, wherein W is a single bond or a methylene bridge or a substituted methylene bridge when at least one of X1 and X2 is methylene, or W is an alkylene or substituted alkylene bridge having 2 or 3 carbon atoms; with the proviso that at least one of R4 and R5 is Z; Q is Image V is Image U is Image wherein X1, X2 and W are as defined above; Y is Image wherein G is oxygen, sulfur or CH2; D is Image wherein F is O or S; E is Image wherein L is O or S. The compounds can be prepared according to known methods such as for example by condensation of an aminoacid XXI with an aminoacid XVII Image
388336
Gold Elijah H.
Neustadt Bernard R.
Smith Elizabeth M.
Gold Elijah H.
Gowling Lafleur Henderson Llp
Neustadt Bernard R.
Schering Corporation
Smith Elizabeth M.
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