Amino acid derivatives possessing renin-inhibitory activities

Details Amino acid derivatives possessing renin-inhibitory activities Amino acid derivatives possessing renin-inhibitory activities

C - Chemistry, Metallurgy

07

D

167/208, 260/305

C07D 413/12 (2006.01) A61K 31/415 (2006.01) A61K 31/535 (2006.01) A61K 38/05 (2006.01) C07D 233/54 (2006.01) C07D 233/64 (2006.01) C07K 5/02 (2006.01) C07K 5/06 (2006.01) C07K 5/065 (2006.01) C07K 5/083 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2015827

ABSTRACT An amino acid derivative of the general formula: Image wherein R1 is Image , R12-NH-, R13-CO-Y-, R13-SO2-CH2-, Image , HO- or Image wherein, R10 is a lower alkyl group and R11 is Image (wherein R111 is a lower alkyl group and n is an integer of 1 to 5) or a lower alkyl group which may be substituted by hydroxy group or methoxyethoxymethoxy group, or R10 and R11 are Image combinedly together with the adjacent nitrogen atom; R12 is a hydrogen atom, CnH2n+1-O-CO- (n is as defined above) or Image ; R13 is a lower alkyl group which may be substituted by substituent(s) selected from HOOC-(H2C)n-O-, R12-NH- (n and R12 are as defined above) and pyridyl group; X is -CH2-, -O- or -NH- and Y is -O- or -NH-; wherein Image is Image (wherein Z is -O-, -S-, -S(O)-, -S(O)2-, -CH2-, -CH(OH)-, Image , -NH- or Image and a and b are independently an integer of 1 to 4 and the total of a and b is not more than 5) ; R2 is an aralkyl group which may be substituted by lower alkyl group(s); R3 is a hydrogen atom or a lower alkyl group; R4 is a lower alkyl group; and A is hydroxy group and B is a hydrogen atom, or A and B are carbonyl group combinedly together with the adjacent carbon atom, a pharmaceutically acceptable acid addition salt or an ester thereof is described. The compounds of the invention possess inhibitory activities against renin and are useful as an antihypertensive agent.

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