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US 2013/0281406 A2Published application
Thiazole derivatives and their use as p2y12 receptor antagonists
AssigneeActelion Pharmaceuticals Ltd.
InventorsEva CAROFF, Kurt HILPERT, Francis HUBLER, David LEHMANN, Emmanuel MEYER, Dorte RENNEBERG
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Abstract
The present invention relates to thiazole derivatives of Formula (I) and their use as P2Y12 receptor antagonists in the treatment and/or prevention of peripheral vascular, of visceral-, hepatic- and renal-vascular, of cardiovascular and of cerebrovascular diseases or conditions associated with platelet aggregation, including thrombosis in humans and other mammals.
Claims15
A compound of formula I
- wherein
- R1 represents (C1-C6)alkoxy;
- Y represents a bond and Z represents hydrogen;
- or
- Y represents (C1-C3)alkandiyl and Z represents hydrogen, hydroxy, —COOH, —COOR5, —P(O)(OH)2, —P(O)(OR6)2, —P(O)(NHR7)2 or phenyl, wherein the phenyl is substituted with —P(O)(OH)2 or —P(O)(OR8)2;
- W represents a group selected from
- R2 represents hydrogen;
- halogen;
- (C1-C4)alkyl which is monosubstituted with (C1-C4)alkoxy, —COOH or —COOR9;
- (C2-C4)alkenyl which is monosubstituted with (C1-C4)alkoxy, —COOH or —COOR9;
- phenyl which is unsubstituted or monosubstituted with halogen;
- (C1-C4)alkyl-amino, wherein the alkyl-group is monosubstituted with hydroxy, (C1-C4)alkoxy, —COOH or —COOR9;
- di-(C1-C4)alkyl-amino;
- heterocyclyl which is unsubstituted or monosubstituted with (C1-C4)alkyl or (C1-C4)alkoxy;
- or 2-methoxymethyl-cycloprop-1-yl;
- R3 represents aryl which is unsubstituted or mono- or di-substituted, wherein the substituents are independently selected from the group consisting of halogen, (C1-C4)alkyl, (C1-C4)alkoxy and phenoxy;
- R4 represents halogen;
- (C1-C4)alkyl which is monosubstituted with (C1-C4)alkoxy, —COOH, or —COOR9;
- (C2-C4)alkenyl which is monosubstituted with (C1-C4)alkoxy or —COOR9;
- phenyl;
- or di-(C1-C6)alkyl-amino;
- R5 represents (C1-C4)alkyl;
- R6 represents (C1-C4)alkyl, (C1-C4)alkyl-C(O)—OCH2— or (C1-C4)alkoxy-C(O)—OCH2—;
- R7 represents (C1-C4)alkoxy-C(O)—(C1-C4)alkyl-;
- R8 represents (C1-C4)alkyl;
- R9 represents (C1-C4)alkyl;
- or a pharmaceutically acceptable salt of such a compound.
24 more elements
Dependencies are inferred from the claim text.