| 摘要 |
Compounds of formula (I) and pharmaceutically acceptable salts thereof: (I) wherein Z1, Z2, Z3 and the carbon atoms to which Z1 and Z3 are attached, form a 5-membered non-aromatic heterocyclic ring; E is absent or is (CH2)n or CH(CH2)n-1 wherein n is 1 to 4; A is -CONH-, -NHCO-, -COO- -S(O)r- wherein r is 0, 1, or 2, or -CH2-; p is 0, 1 or 2; q is 0 or 1; s is 0, 1, 2, 3 or 4; Rz is hydrogen, C1-6 alkyl or, when A is -CH2-, hydroxy; Ra and Rb are independently selected from hydrogen or a substituent; R1 is CH2R9 wherein R9 is optionally substituted aryl or heteroaryl; R2 is CHR10R11 wherein R10 is hydrogen or methyl and R11 is C1-6 alkyl, C3-8 cycloalkyl, optionally substituted aryl or heteroaryl, or R11 is amino, C2-7 alkanoylamino, 2-oxopyrrolidinyl, 2-oxopiperidinyl or C1-6 alkoxycarbonylamino; R3 is CH2R12 wherein R12 is C1-6 alkyl, C3-8 cycloalkyl or phenyl; and R4 is a saturated or unsaturated heterocyclic ring linked through carbon, hydroxy, C1-6 alkoxy, C1-7 alkanoyloxy, amino, C1-7 alkanoylamino, amino substituted by one or two C1-6 alkyl groups, C1-6 alkylsulphonyl, carboxy, C1-6 alkoxycarbonyl, benzyloxycarbonyl, aminocarbonyl or CH(NHR13)CO2R14 wherein R13 is hydrogen or C1-6 alkanoyl and R14 is hydrogen or C1-6 alkyl; or (when s is 2 to 4) R4 is a saturated or unsaturated heterocyclic ring linked through nitrogen; and the dashed line represents an optional bond (when E is present); which are renin inhibitors, a process for their preparation and their use as pharmaceuticals.
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