Dipeptide derivatives

C - Chemistry – Metallurgy – 07 – K

Patent

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Details

C07K 5/065 (2006.01) C07D 213/56 (2006.01) C07D 233/54 (2006.01) C07D 233/64 (2006.01) C07D 263/06 (2006.01) C07D 277/30 (2006.01) C07D 277/46 (2006.01) C07D 295/26 (2006.01) C07D 401/12 (2006.01) C07D 405/06 (2006.01) C07D 405/12 (2006.01) C07D 409/00 (2006.01) C07D 413/00 (2006.01) C07D 413/06 (2006.01) C07D 417/06 (2006.01) C07D 417/12 (2006.01) C07D 417/14 (2006.01) C07K 5/02 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2045008

- 141 - Abstract of the Disclosure. A novel dipeptide derivative of the following formula (I), which compound is capable of inhibiting the enzymatic activity of renin and thereby depressing the renin-angiotensin system and lowering the blood pressure, is provided. Image (I) wherein: R1 is C1-C12 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, C3-C10 cycloalkyl, aryl, or heterocyclic radical; R2 is carbamoyl, aryl, 5- or 6-membered heterocyclic radical, C1-C12 alkyl-S-, C1-C12 alkyl-S-CH2-, or C3-C10 cycloalkyl-S-; R3 is aryl or 5- or 6-membered heterocyclic radical; R4 is R4'-SO2 or R4'-CO; R4' is aryl, C1-C12 alkyl, C2-C6 alkenyl, C2-C6 alkynyl; C3-C10 cycloaklyl, or heterocyclic radical; X is CH2, NH, O, or S; and Y is CO or NHSO2, wherein R1, R2, R3 and R4' each may be substituted with one to three substituents selected independently from a group consisting of hydroxy; halogen; - 142 - trifluoromethyl; -CN; heterocyclic radical; C1-C6 alkyl; C3-C10 cycloalkyl; -O-C1-C6 alkyl; C1-C6 alkylenedioxy; -CO-O-C1-C6 alkyl; -NHCO-C1-C6 alkyl; -S-C1-C6 alkyl; -SO-C1-C6 alkyl; -SO2-C1-C6 alkyl; -NHSO2-C1-C6 alkyl; -NR5R6; -O-CO-NR5R6; -CO-NR5R6; -O-C1-C6 alkyl NR5R6; R5 and R6 are independently hydrogen, formyl or C1-C6 alkyl, or R5 and R6, when taken together with the nitrogen to which they are attached, form a cyclic amino group, or an acid addition salt thereof.

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