Amino acid derivative

A - Human Necessities – 61 – K

Patent

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Details

A61K 38/05 (2006.01) A61K 31/40 (2006.01) A61K 31/42 (2006.01) A61K 31/44 (2006.01) A61K 31/55 (2006.01) C07D 209/48 (2006.01) C07D 223/16 (2006.01) C07D 243/12 (2006.01) C07D 267/14 (2006.01) C07D 281/10 (2006.01) C07D 401/06 (2006.01) C07D 409/06 (2006.01) C07D 471/04 (2006.01) C07D 487/04 (2006.01) C07D 495/14 (2006.01) C07D 498/04 (2006.01) C07D 513/04 (2006.01) C07K 5/078 (2006.01)

Patent

CA 2140553

The present invention relates to an amino acid derivative having an angiotensin I-converting enzyme inhibition activity, a vasopressin antagonism and an atrial natriuretic peptide hydrolase inhibition activity. This amino acid derivative is represented by the following general formula (I): Image (I) wherein R1 represents a hydrogen atom or an acyl group; R2 represents a hydrogen atom, a lower alkyl group, a cycloalkyl group, an ary group which may have a substituent, a heteroaryl group which may have a substituent, an arylalkyl group which may have a substituent or a heteroarylalkyl group which may have a substituent; m and n represent each independently an integer of 0, 1 or 2 and J represents a cyclic group having an angiotensin I-converting enzyme inhibition activity.

L'invention concerne un dérivé aminoacide présentant une activité inhibitrice de l'enzyme convertissant l'angiotensine I, une activité antagoniste vis-à-vis de la vasopressine, et une activité inhibitrice de l'hydrolase peptidique natriurétique auriculaire. Ledit dérivé est représenté par la formule générale (I), dans laquelle R<1> représente hydrogène ou acyle; R<2> représente hydrogène, alkyle inférieur, cycloalkyle, aryle éventuellement substitué, hétéroaryle éventuellement substitué, arylalkyle éventuellement substitué ou hétéroaryle éventuellement substitué; m et n représentent chacun, indépendamment, un nombre entier valant 0,1 ou 2; et J représente un groupe cyclique ayant une activité inhibitrice de l'enzyme convertissant l'angiotensine I.

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