Renin inhibiting polyhydroxymonoamides

Details Renin inhibiting polyhydroxymonoamides Renin inhibiting polyhydroxymonoamides

C - Chemistry, Metallurgy

07

C

C07C 235/34 (2006.01) A61K 31/165 (2006.01) A61K 31/38 (2006.01) A61K 31/41 (2006.01) C07C 235/08 (2006.01) C07C 235/26 (2006.01) C07D 233/54 (2006.01) C07D 233/61 (2006.01) C07D 233/88 (2006.01) C07D 277/30 (2006.01) C07D 277/36 (2006.01) C07D 277/40 (2006.01) C07D 307/58 (2006.01) C07D 333/24 (2006.01)

Patent

CA 2058603

Disclosed herein are compounds of the formula: R1CH2CH(X)CH(Y)CH(Z)CHR2C(O)NHCHR3CH(OH)CH(OH)R4 wherein R1 is a terminal unit, for example lower cycloalkyl or phenyl; R2 is, for example, an optionally substituted alkyl, cycloalkylmethyl, benzyl, 4-imidazolylmethyl, 2-thienylmethyl or 4- thiazolylmethyl; R3 is alkyl, cycloalkylmethyl or an optionally substituted benzyl; R4 is alkyl or cycloalkyl; and X and Y each is hydroxy and Z is hydrogen, or X and Z each is hydroxy and Y is hydrogen; with the provisos that (a) the carbon atom bearing R2 has the "R" configuration except when R2 is 2-thienylmethyl or 2-thiazolylmethyl, X and Y each is hydroxy and Z is hydrogen, then the carbon atom bearing R2 has the "S" configuration; (b) the carbon atoms bearing R3 and R4 each has the "S" configuration; and (c) the carbon atom located between the last-said two carbon atoms has the "R" configuration. The compounds inhibit renin activity and are indicated for the treatment of hypertension and congestive heart failure.

Composés de formule R1CH2CH(X)CH(Y)CH(Z)CHR2C(O)NHCHR3CH(OH)CH(OH)R4, où R1 est un groupe terminal, par exemple un cycloalkyle inf. ou un phényle; R2 est, par exemple, un groupe alkyle avec substitution facultative, cycloalkylméthyle, benzyle, 4-imidazolylméthyle, 2-thiénylméthyle ou 4- thiazolylméthyle; R3 est un groupe alkyle, cycloalkylméthyle ou un benzyle avec substitution facultative; R4 est un alkyle ou un cycloalkyle; X et Y sont chacun un hydroxy et Z est de l'hydrogène, ou X et Z sont chacun un hydroxy et Y est de l'hydrogène; à la condition que (a) l'atome de carbone portant R2 ait la configuration "R", sauf si R2 est le 2-thiénylméthyle ou le 2-thiazolylméthyle, X et Y étant chacun un hydroxy et Z un hydrogène, alors l'atome de carbone portant R2 a la configuration "S", (b) les atomes de carbone portant R3 et R4 aient chacun la configuration "S", (c) l'atome de carbone situé entre ces deux derniers atomes de carbone ait la configuration "R". Les composés sont des inhibiteurs de l'activité de la rénine et sont indiqués pour le traitement de l'hypertension et de l'insuffisance cardiaque globale.

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