Pharmaceuticals

Details Pharmaceuticals Pharmaceuticals

C - Chemistry, Metallurgy

07

K

530/5.06, 530/5.

C07K 5/087 (2006.01) A61K 38/05 (2006.01) A61K 38/06 (2006.01) C07K 5/02 (2006.01) C07K 5/065 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2031684

-1- Abstract Compounds of formula (I), and pharmaceutically acceptable salts thereof: Image (I) wherein the Ar ring is of sub-formula (a) or (b): Image (a) Image (b) one or two of W1, W2, W3 and W4 is CH, N or NO (such that if two are NO then these are are W1 and W4), and the others are CH, CRa or CRb; -2- 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; 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 or C3-8 cycloalkyl or phenyl; R4 is C1-6 alkyl, C3-8 cycloalkyl, C3-8 cycloalkyl-C1-4 alkyl or a group of structure c), d), e) or f): c) Image d) Image -3- e) Image f) Image wherein Rp, Rq, Rs, Rt, Ru, Rv and Rw are selected from hydrogen or C1-6 alkyl; or NRvRw is 1-imidazolyl; and the dashed line represents an optional bond (when E is present); having renin inhibitor activity, a process for their preparation and their use as pharmaceuticals.

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