C - Chemistry – Metallurgy – 07 – C
Patent
C - Chemistry, Metallurgy
07
C
C07C 237/22 (2006.01) A61K 31/16 (2006.01) A61K 31/33 (2006.01) C07D 207/27 (2006.01) C07D 213/40 (2006.01) C07D 233/64 (2006.01) C07D 277/20 (2006.01) C07D 295/185 (2006.01) C07D 295/215 (2006.01) C07D 333/24 (2006.01) C07D 409/12 (2006.01) C07D 413/12 (2006.01) C07D 417/00 (2006.01)
Patent
CA 2143300
Disclosed herein are compounds of the formula: A-N(R1)C(O)CH2CHR2C(O)-B, wherein A is R3R4NC(O)CH2 wherein, for example, R3 is hydrogen or alkyl and R4 is hydrogen, alkyl or a substituted alkyl such as 2-(2-pyridinyl)ethyl, or R3 and R4 together with the nitrogen atom to which they are attached form a pyrrolidino, piperidino, morpholino or thiomorpholino; R1 is, for example, benzyl, alkyl or a substituted alkyl such as cyclohexylmethyl; R2 is, for example, alkyl, cycloalkylmethyl, 1H-imidazol-4-ylmethyl, 4-thiazolylmethyl or (2-amino-4-thiazolyl)methyl; and B is a renin substrate transition state analog, for example, [1(S)-(cyclohexylmethyl)-2(R),3(S)-dihydroxy-5-methylhexyl]amino. The compounds inhibit renin activity and are indicated for the treatment of hypertension and congestive heart failure.
L'invention porte sur des composés de formule A-N(R1)C(O)CH2CHR2C(O)-B, où A est R3R4NC(O)CH2; R3 est un hydrogène ou un alkyle; R4 est un hydrogène, un alkyle ou un alkyle avec substitution, comme le 2-(2-pyridinyl)éthyle; ou R3 et R4 forment, avec l'atome d'azote auquel ils sont liés, un groupe pyrrolidino, pipéridino, morpholino ou thiomorpholino; R1 est un benzyle, un alkyle ou un alkyle avec substitution, comme le cyclohexylméthyle; R2 est un groupe alkyle, cycloalkylméthyle, 1H-imidazol-4-ylméthyle, 4-thiazolylméthyle ou (2-amino-4-thiazolyl)méthyle; B est un analogue à l'état de transition d'un substrat de la rénine, comme [1(S)-(cyclohexylméthyl)-2(R),3(S)-dihydroxy-5-méthylhexyl]amino. Ces composés sont des inhibiteurs de l'activité de la rénine et ils sont utiles pour le traitement de l'hypertension et de l'insuffisance cardiaque globale.
Lavalee Pierre
Simoneau Bruno
Boehringer Ingelheim (canada) Ltd. Boehringer Ingelheim (canada)
Norton Rose Or S.e.n.c.r.l. S.r.l./llp
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