主权项 |
1. A compound of Formula (I): and stereoisomers, geometric isomers, tautomers, or pharmaceutically acceptable salts thereof, wherein: R1 is —NR—C1-C12-hydroxyalkyl, —NR—(C1-C12-alkylenyl)n-C3-C6-cycloalkyl, —NR—(C1-C12-alkylenyl)n-heterocyclyl, —NR—(C1-C12-alkylenyl)n-C6-C20-aryl, —NR—(C1-C12-alkylenyl)n-heteroaryl, —NR—(C1-C12-alkylenyl)n-C6-C20-aryloxy, C6-C20-aryl, pyridine, N-linked piperidine, N-linked pyrrolidine, N-linked piperazine, N-linked morpholine, 1H-pyrazol-4-yl, C6-C20-aryloxy or heteroaryloxy, each of which can be unsubstituted or substituted by one or more substituent(s) selected from the group consisting of:
CN;oxo;OH;NH2;halo;C1-C12-alkyl;(C1-C12-alkylenyl)n-C1-C12-alkoxy, unsubstituted or substituted by one or more substituent(s) selected from the group consisting of C3-C6-cycloalkyl, heterocyclyl, aryl and heteroaryl;C1-C12-hydroxyalkyl;C1-C12-haloalkyl;C1-C12-haloalkoxy;(C1-C12-alkylenyl)n-C(O)O—C1-C12-alkyl;—C(O)—C1-C12-alkyl;O—R′, wherein R′ is C3-C6-cycloalkyl, heterocycloalkyl, aryl or heteroaryl, each of which are unsubstituted or substituted by one or more Rg;(C1-C12-alkylenyl)n-cycloalkyl or (C1-C12-alkylenyl)n-heterocyclyl unsubstituted or substituted by one or more substituent(s) selected from the group consisting of:
halo, oxo, OH, NH2, C1-C12-alkyl, C1-C12-hydroxyalkyl, C1-C12-haloalkyl, (C1-C12-alkylenyl)n-C1-C12-alkoxy, —NH(C1-C12-alkyl), —N(C1-C12-alkyl)2, —N(C1-C12-alkyl)-C(O)—C1-C12-alkyl, —C(O)—C1-C12-alkyl, —C(O)O—C1-C12-alkyl, (C1-C12-alkylenyl)n-C(O)—NH2, (C1-C12-alkylenyl)n-C(O)—NH(C1-C12-alkyl), —C(O)—NH(C1-C12-hydroxyalkyl), (C1-C12-alkylenyl)n-C(O)—N(C1-C12-alkyl)2, —C(O)—NH(C1-C12-haloalkyl), —C(O)—NH-heterocyclyl, —S(O)2—C1-C12-alkyl, —S(O)2—N(C1-C12-alkyl)2, —C(O)OH, —C(O)-heterocyclyl, (C1-C12-alkylenyl)n-heterocyclyl and (C1-C12-alkylenyl)n-heteroaryl, which heterocyclyl and heteroaryl group(s) can be unsubstituted or substituted by one or more substituent(s) selected from the group consisting of:
OH, NH2, halo, C1-C12-alkyl, C1-C12-alkoxy, C1-C12-haloalkyl and C1-C12-hydroxyalkyl;(C1-C12-alkylenyl)n-aryl or (C1-C12-alkylenyl)n-heteroaryl, wherein the aryl or heteroaryl is unsubstituted or substituted by one or more substituent(s) selected from the group consisting of:
halo, OH, NH2, C1-C12-alkyl, C1-C12-hydroxyalkyl, C1-C12-haloalkyl, (C1-C12-alkylenyl)n-C1-C12-alkoxy, —NH(C1-C12-alkyl), —N(C1-C12-alkyl)2, —N(C1-C12-alkyl)C(O)—C1-C12-alkyl, —C(O)—C1-C12-alkyl, —C(O)—NH2, —C(O)—NH(C1-C12-alkyl), —C(O)—NH(C1-C12-hydroxyalkyl), —C(O)—N(C1-C12-alkyl)2, —C(O)—NH(C1-C12-haloalkyl), —C(O)—NH-heterocyclyl, —S(O)2—C1-C12-alkyl, —S(O)2—N(C1-C12-alkyl)2, C1-C12-alkylenyl-C(O)N(C1-C12-alkyl)2, —C(O)OH, —C(O)-heterocyclyl and heterocyclyl, which heterocyclyl group(s) can be unsubstituted or substituted by one or more substituent(s) selected from the group consisting of:
OH, NH2, halo, C1-C12-alkyl, C1-C12-alkoxy, C1-C12-haloalkyl, and C1-C12-hydroxyalkyl;(C1-C12-alkylenyl)n-NRaRb, wherein Ra and Rb are independently selected from:
H,C1-C12-alkyl,C1-C12-hydroxyalkyl,C1-C12-haloalkyl,(C1-C12-alkylenyl)n-C1-C12-alkoxy,—S(O)2—(C1-C12-alkylenyl)n-heterocyclyl unsubstituted or substituted by one or more Rg,(C1-C12-alkylenyl)n-C6-C20-aryl, which aryl is unsubstituted or substituted by one or more Rg,(C1-C12-alkylenyl)n-C3-C6-cycloalkyl unsubstituted or substituted by one or more Rg,(C1-C12-alkylenyl)n-heterocyclyl unsubstituted or substituted by one or more oxo, —C(O)—C1-C12-alkyl, —C(O)O—C1-C12-alkyl or Rg,C1-C12-alkylenyl-C(O)-heteroaryl unsubstituted or substituted by one or more Rg,C1-C12-alkylenyl-NH2,C1-C12-alkylenyl-NH(C1-C12-alkyl),C1-C12-alkylenyl-N(C1-C12-alkyl)2,C1-C12-alkylenyl-C(O)NH2,C1-C12-alkylenyl-C(O)NH(C1-C12-alkyl), or,C1-C12-alkylenyl-C(O)N(C1-C12-alkyl)2,(C1-C12-alkylenyl)n-C(O)NRcRd, wherein Rc and Rd are independently selected from:
H,C1-C12-alkyl,C1-C12-hydroxyalkyl,C1-C12-haloalkyl,(C1-C12-alkylenyl)n-C1-C12-alkoxy,C1-C12-alkylenyl-NH(C1-C12-alkyl),C1-C12-alkylenyl-N(C1-C12-alkyl)2,(C1-C12-alkylenyl)n-heterocyclyl, unsubstituted or substituted by one or more substituent(s) selected from the group consisting of oxo, —C(O)—C1-C12-alkyl and Rg,(C1-C12-alkylenyl)n-C3-C6-cycloalkyl unsubstituted or substituted by one or more Rg,(C1-C12-alkylenyl)n-C6-C20-aryl unsubstituted or substituted by one or more Rg,—NH—C3-C6-cycloalkyl; oror Rc and Rd together with the nitrogen atom to which they are attached, form a 5 or 6 membered heterocyclyl which can or cannot comprise 1 or 2 additional heteroatom selected from N, O or S; and,(C1-C12-alkylenyl)n-NReC(O)Rf, wherein Re is H or C1-C12-alkyl, Rf is halo, CN, OH, C1-C12-alkyl, C1-C12-haloalkyl, (C1-C12-alkylenyl)n-C1-C12-alkoxy, C1-C12-hydroxyalkyl, C1-C12-cyanoalkyl, (C1-C12-alkylenyl)n-NH2, (C1-C12-alkylenyl)n-NH(C1-C12-alkyl), (C1-C12-alkylenyl)n-N(C1-C12-alkyl)2, (C1-C12-alkylenyl)n-C3-C6-cycloalkyl, (C1-C12-alkylenyl)n-heterocyclyl, or (C1-C12-alkylenyl)n-NH—C3-C6-cycloalkyl, wherein said cycloalkyl, heterocyclyl or heteroaryl are unsubstituted or substituted by oxo, —C(O)—C1-C12-alkyl or one or more Rg; R2 is H, CN, —C(O)—NH(C1-C12-alkyl)-NH—C(O)—C1-C12-alkyl, —C(O)—N(C1-C12-alkyl)(C1-C12-alkoxy), —C(O)—N(C1-C12-alkyl)(C1-C12-alkylalkoxy), —C(O)—NH(heterocyclyl), —C(O)—NH(C1-C12-alkyl-heterocyclyl), —C(O)—N(C1-C12-alkyl)(heterocyclyl), or —C(O)— heterocyclyl, which heterocyclyl groups are unsubstituted or substituted by one or more Rg, —N(C1-C12-alkyl)-C(O)—C1-C12-alkyl, or —N(C1-C12-alkyl)2; R3 is H, i-butyl, C1-C12-haloalkyl, cyclobutyl, —C(O)—C1-C12-alkyl-C3-C6-cycloalkyl, —C(O)—C1-C12-alkyl-heterocyclyl —C(O)—C1-C12-alkyl-C6-C20-aryl, —C(O)—C1-C12-alkyl-heteroaryl or pyridinyl; R is H or C1-C12-alkyl; Rg is H, OH, halo, NH2, C1-C12-alkyl, (C1-C12-alkylenyl)n-C1-C12-alkoxy, C1-C12-haloalkyl, C1-C12-haloalkoxy, C1-C12-hydroxyalkyl, or C1-C12-cyanoalkyl; n is 0 or 1; wherein in the preceeding heteroaryl groups are 5 or 6 membered heteroaryls comprising 1, 2 or 3 heteroatom(s) selected from N, O or S and heterocyclyl groups are 5 to 10 membered heterocyclyls comprising 1, 2 or 3 heteroatom(s) selected from N, O or S; with the proviso that the compounds of Formula I is not: 6-(3-(trifluoromethyl)phenyl)pyrido[3,2-d]pyrimidin-4-amine 6-(3-(trifluoromethoxy)phenyl)pyrido[3,2-d]pyrimidin-4-amine 6-phenylpyrido[3,2-d]pyrimidin-4-amine 6-(4-fluorophenyl)pyrido[3,2-d]pyrimidin-4-amine |