Certain macrocyclic lactam derivatives

Details Certain macrocyclic lactam derivatives Certain macrocyclic lactam derivatives

C - Chemistry, Metallurgy

07

D

C07D 225/02 (2006.01) A61K 31/395 (2006.01) C07D 267/00 (2006.01) C07D 281/00 (2006.01) C07D 401/00 (2006.01) C07D 401/12 (2006.01) C07D 403/06 (2006.01) C07D 405/12 (2006.01) C07D 409/12 (2006.01) C07D 413/06 (2006.01) C07D 417/06 (2006.01) C07K 5/078 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2083622

4-18867/A/CGC 1583 CERTAIN MACROCYCLIC LACTAM DERIVATIVES Abstract of the Invention The invention relates to macrocyclic lactam derivatives of formula I Image (I) wherein R is hydrogen or acyl; m is an integer from 4 to 9 inclusive; n is 1 or 2; p is zero, 1 or 2; X is -CONH- or -NHCO-; Y is S, O or CH2; R1 is -COOH; or R1 is Image in which R2 is hydrogen, lower alkyl, aryl-lower alkyl, amino-lower alkyl, hydroxy-lower alkyl, acyloxy-lower alkyl, lower alkoxy-lower alkyl, mercapto-lower alkyl, lower alkyl-(thio, sulfinyl or sulfonyl)-lower alkyl, or carboxy-lower alkyl, R3 is hydrogen or lower alkyl, and q is zero or an integer from 1 to 5 inclusive; or R1 is Image in which R4 is hydrogen, lower alkyl, lower alkoxy, hydroxy or acyloxy, and r is 1 or 2; or R1 is Image in which s is 1 or 2; or R1 is Image . in which R5 and R6 independently represent hydrogen, lower alkyl, C5- or C6-cycloalkyl, (hydroxy-, acyloxy or lower alkoxy-) lower alkyl, carbocyclic or heterocyclic monocyclic aryl, or (hydroxy-, acyloxy- or alkoxy-) lower alkyloxy-lower alkyl; or R5 and R6 together with the nitrogen to which they are attached represent pyrrolidino, piperidino, molpholino, piperazino or N-alkylpiperazino; and macrocyclic sulfur and oxygen containing lactam ring isomers in which a CH2 group of (CH2)m in formula I is replaced by O or S, and Y represents CH2; and pharmaceutically acceptable prodrug esters of any above saidcompound with a free carboxyl group; and pharmaceutically acceptable salts of any said compounds with a free acid or basic salt forming group; 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 saidcompounds to mammals in need of such treatment.

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