Homocyclostatine and cyclostatine containing polypeptides as...

C - Chemistry – Metallurgy – 07 – K

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167/103.05, 530/

C07K 5/06 (2006.01) C07K 5/02 (2006.01)

Patent

CA 1321676

72222-88 HOMOCYCLOSTATINE AND CYCLOSTATINE CONTAINING POLYPEPTIDES AS ANTIHYPERTENSIVE AGENTS Abstract Polypeptides and derivatives thereof containing homocyclostatine and cyclostatine of the formula Image (I) (wherein X is hydrogen, methoxy or hydroxy; R is alkyl having one to six carbon atoms or methylthiomethyl; n is an integer of 0 or 1; R1 is amino, alkylamino having from one to five carbon atoms, alkoxy having from one to three carbon atoms or 2-alkoxycarbonylpyrrolidin-1-yl in which the alkoxy has from one to three carbon atoms; and R2 is -CH2CH(Cl)=CH2, C3-4alkyl, -CH2CH=CH-CH2N3, -(CH2)4NH2, -CH2CH(Br)=CH2, -CH2CH=CHCl, -CH2CH=C(CH3)2, -CH2CH=CHCH3 or -CH2CH?CH, with the proviso that n is 0, only when R is methylthiomethyl and R1 is amino, the alkylamino, the alkoxy or the 2-alkoxycarbonylpyrrolidin-1-yl) are useful for inhibiting the angiotensinogen-cleaving action of the enzyme resin.

570669

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