Compounds

Details Compounds Compounds

C - Chemistry, Metallurgy

07

K

530/5, 167/103.0

C07K 5/065 (2006.01) A61K 38/05 (2006.01) A61K 38/06 (2006.01) C07K 5/02 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2022816

Abstract Compounds of formula (I), and pharmaceutically acceptable salts thereof: Image (I) wherein the Het ring is of sub-formula (a) or (b): Image (a) (b) wherein one or two of W1, W2, W3 and W4 is N or NO (such that if two are NO then these are are W1 and W4), and the others are CH, CRa or CRb; one of Q1, Q2 and Q3 is S and the other two are CH and CRC; either Z1 and Z2 are absent and Z3, Z4 and Z5 and the carbon atoms to which Z3 and Z5 are attached, form a 5-membered non-aromatic heterocyclic ring; or Z1 is absent and Z2, Z3, Z4, Z5 and the carbon atoms to which Z2 and Z5 are attached, form a 6-membered non-aromatic heterocyclic ring; or Z1, Z2, Z3, Z4 and Z5 and the carbon atoms to which Z1 and Z5 are attached, form a 7-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; s is 0, 1, 2, 3 or 4; q is 0 or 1; 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, C3-8cycloalkyl or phenyl; R4 is C1-6 alkyl, C3-8 cycloalkyl, 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, or 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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