114343-31-6Relevant articles and documents
N-HETEROCYCLIC ALCOHOL DERIVATIVES
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, (2008/06/13)
Compounds of the formula STR1 wherein R 1 is an N-heterocyclic group as defined herein, are disclosed. These compounds are inhibitors of renin and therefore useful as cardiovascular agents.
Peptidyl difluorodiol renin inhibitors
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, (2008/06/13)
A renin inhibiting compound of the formula: wherein A is a functional group; W is (1)-C(O)-,(2)-CH(OH)-or(3)-N(R?)-wherein R? is hydrogen or loweralkyl; U is (1)-C(O)-,(2)-CH?-or(3)-N(R?)-wherein R? is hydrogen or lower alkyl, with the proviso that when W is-CH(OH)-then U is-CH?-and with the proviso that U is-C(O)-or-CH?-when W is-N(R?)-; V is (1)-CH-,(2)-C(OH)-or(3)-C(halogen)-with the proviso that v is-CH--when U is-N(R?)-; Q is-CH(R?)-or-C(=CHR1a)-wherein R? is (1) loweralkyl,(2) cycloalkylalkyl,(3) arylalkyl,(4) (heterocyclic) alkyl,(5) 1-benzyloxyethyl,(6) phenoxy,(7) thiophenoxy or(8) anilino, provided that B is-CH?-or-CH(OH)-or A is hydrogen when R? is phenoxy, thiophenoxy or anilino and R1a is aryl or heterocyclic; R? is a functional group; R? is (1) loweralkyl,(2) cycloalkylmethyl or(3) benzyl; R? is-CH(OH)-or-C(O)-; R? is-CH(OH)-or-C(O)-; and Z is (1) lower alkyl,(2) aryl,(3) arylalkyl,(4) cycloalkyl,(5) cycloalkylalkyl,(6) heterocyclic or(7) (heterocyclic)alkyl; or a pharmaceutically acceptable salt, ester or prodrug thereof.
Novel amino acid derivatives possessing renin-inhibitory activities
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, (2008/06/13)
An amino acid derivative of the general formula: wherein, R1? is a lower alkyl group and R11 is (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 R1? and R11 are combinedly together with the adjacent nitrogen atom; R12 is a hydrogen atom, CnH2n+ 1-O-CO-(n is as defined above) or R13 is a lower alkyl group which may be substituted by substituent(s) selected from HOOC-(H?C)n-O-, R12-NH-(n and R12 are as defined above) and pyridyl group; X is-CH?-,-O-or-NH-and Y is-O-or-NH-; wherein (wherein Z is-O-,-S-,-S(O)-,-S(O)?-,-CH?-,-CH(OH)-,---,-NH-or 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; R? 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.