Novel Heterocyclic Carboxamides as Modulators of Kinase Activity

摘要

The invention provides novel heterocyclic carboxamide compounds compounds according to Formula (I) their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.

主权项

1. A compound of Formula (I), or its stereoisomers or tautomers, or pharmaceutically acceptable salts of each of the foregoing, including mixtures thereof in all ratios, wherein X is N, or C—R4; Y is N—R5, O, or absent; R1 is L1-R6, or L1-R6-L2-R7; R2 is H, Hal, OH, OA, CN, NH2, or NHA; R3 is H, CH3, or C(Hal)3; R4 is H, Hal, OH, COOH, NH2, or CN; R5 is H, LA or monocyclic alkyl having 3, 4, 5, 6, or 7 ring atoms, wherein one or two CH2 groups may be replaced by a —NH— group, or R5, R1 together form a monocyclic alkyl ring having 3, 4, 5, 6, or 7 ring atoms, wherein one or two CH2 groups may be replaced by an O atom and/or an —NH—, —NA-, —N(L1-R6)—, —CHA-, —CA2-, CH(L1-R6)— or —CO— group, and wherein the monocyclic alkyl ring may be substituted by NH2; L1, L2 are each independently a single bond, or unbranched or branched alkyl having 1, 2, 3, 4 or 5 C atoms, which may be unsubstituted, or mono- or disubstituted with Hal, OH, NH2, NH(LA), N(LA)2, and wherein one or two CH2 groups may be replaced by an O atom or by a —CO—, —NH—, —N(LA)-, —CONH—, —N(LA)COO— or —NHCO— group; R6, R7 are each independently Ar or a monocyclic alkyl ring having 3, 4, 5, 6, or 7 ring atoms, wherein one or two CH2 groups may be replaced by an O atom and/or an —NH—, —NA-, —CHA-, —CO— or —CONHA- group; each Ar is independently a mono- or bicyclic aromatic homo- or heterocycle having 0, 1, 2, 3 or 4N, O and/or S atoms and 5, 6, 8, 9, or 10 skeleton atoms, which may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by Hal, A, OA, OH, NH2, or NHA; each A is independently an unbranched or branched linear or cyclic alkyl having 1, 2, 3, 4, 5 or 6 C atoms, wherein one or two CH2 groups may be replaced by an O atom and/or an —NH—, —NHCOAr or —CONHAr group wherein 1-3H atoms may be replaced by Hal, and wherein one or two CH3 groups may be replaced by NH2, OH, NH(LA) or N(LA)2 group; each LA is independently an unbranched or branched, linear alkyl having 1, 2, 3, or 4 C atoms wherein 1, 2 or 3H atoms may be replaced by Hal; and each Hal is independently F, Cl, Br or I.