DERIVATIVES OF 1H-INDOLE-3-CARBOXAMIDE AND THEIR USE AS P2Y12 ANTAGONISTS

摘要

1H-Indole-3-carboxamide derivatives (I), are new. 1H-Indole-3-carboxamide derivatives of formula (I) in the form of base or salt addition with an acid or base or their enantiomers and diastereoisomers including their racemic mixtures, are new. A : bivalent group of formula (Ia) or (Ib); R1 : 1-4C alkyl; R2 : 1-3C alkyl; R3 : -NR7R8, where R7 and R8 are combined together with nitrogen atom to obtain saturated 4-6 membered heterocycle ring containing another nitrogen atom, and the heterocycle ring is substituted with 1-3C alkyl (optionally substituted by two or three halogen atoms or 1-3C alkoxy (optionally substituted by two or three halogen atoms)); and R4 : halo. Independent claims are included for: (1) preparing the 1H-indole-3-carboxamide derivative; (2) a o-tolyl-vinyl-amine compound of formula (IIA); and (3) o-tolyl-vinyl-amine compound of formula (IIB). [Image] [Image] [Image] ACTIVITY : Antianginal; Cardiant; Vasotropic; Anticoagulant; Thrombolytic; Antiarteriosclerotic; Antiinflammatory; Muscular-Gen.; Hemostatic; Gynecological; Antianemic; Antisickling; Nephrotropic; Gastrointestinal-Gen.; Antimigraine; Antiasthmatic. MECHANISM OF ACTION : Purinergic (P2Y12) receptor antagonist.