发明名称 TRIAZOLO[4,5-D]PYRIMIDINE DERIVATIVES
摘要 Compounds of the formula I;;in which R1 and R2 have the meanings indicated in Claim 1, are inhibitors of GCN2, and can be employed, inter alia, for the treatment of cancer.
申请公布号 US2014378431(A1) 申请公布日期 2014.12.25
申请号 US201214375067 申请日期 2012.12.21
申请人 Merck Patent GmbH 发明人 Dorsch Dieter;Hoelzemann Guenter;Schiemann Kai;Wegener Ansgar
分类号 C07D487/04;A61K31/5377;A61K31/519 主分类号 C07D487/04
代理机构 代理人
主权项 1. Compounds of the formula I in which R1 denotes Ar or Het, R2 denotes furyl, thienyl, pyrrolyl, thiadiazolyl, imidazolyl, pyrazolyl, oxazolyl, isoxazolyl, oxadiazolyl, thiazolyl, triazolyl or tetrazolyl which is unsubstituted or mono- or disubstituted by Hal, A, [C(R3)2]pCyc, [C(R3)2]pOR3, [C(R3)2]pN(R3)2, [C(R3)2]pAr, [C(R3)2]pHet1, NO2, CN, [C(R3)2]pCOOR3, CON(R3)2, NR3COA, NR3SO2A, SO2N(R3)2, S(O)nA, COHet1, O[C(R3)2]mN(R3)2, O[C(R3)2]pHet1, NHCOOA, NHCON(R3)2, NHCOO[C(R3)2]mN(R3)2, NHCOO[C(R3)2]pHet1, NHCONH[C(R3)2]m—N(R3)2, NHCONH[C(R3)2]pHet1, OCONH[C(R3)2]mN(R3)2, OCONH[C(R3)2]pHet1, CHO, COA, ═S, ═NR3 and/or ═O, R3 denotes H or A′, Ar denotes phenyl or naphthyl which is unsubstituted or mono-, di- or trisubstituted by Hal, A, [C(R3)2]pOR3, [C(R3)2]pN(R3)2, [C(R3)2]pHet1, NO2, CN, [C(R6)2]pCOOR3, CON(R3)2, NR3COA, NR3SO2A, SO2N(R3)2, S(O)nA, S(O)nHet1, COHet1, O[C(R3)2]mN(R3)2, O[C(R3)2]pHet1, NHCOOA, NHCON(R3)2, NHCOO[C(R3)2]mN(R3)2, NHCOO[C(R3)2]pHet1, NHCONH[C(R3)2]niN(R3)2, NHCONH[C(R3)2]pHet1, OCONH[C(R3)2]mN(R3)2, OCONH[C(R3)2]p-Het1, CHO and/or COA, Het denotes furyl, thienyl, pyrrolyl, imidazolyl, pyrazolyl, oxazolyl, isoxazolyl, oxadiazolyl, thiazolyl, triazolyl, tetrazolyl, pyridyl, pyrimidyl, pyridazinyl, pyrazinyl, indolyl, isoindolyl, benzimidazolyl, indazolyl, quinolyl, 1,3-benzodioxolyl, benzothiophenyl, benzofuranyl, imidazopyridyl, dihydroindolyl, quinoxalinyl, benzo[1,2,5]thiadiazolyl or furo[3,2-b]pyridyl which is unsubstituted or mono- or disubstituted by Hal, A, [C(R3)2]pOR3, [C(R3)2]pN(R3)2, [C(R3)2]pHet1, NO2, CN, [C(R6)2]pCOOR3, CON(R3)2, NR3COA, NR3SO2A, SO2N(R3)2, S(O)nA, COHet1, O[C(R3)2]mN(R3)2, O[C(R3)2]pHet1, NHCOOA, NHCON(R3)2, NHCOO[C(R3)2]mN(R3)2, NHCOO[C(R3)2]pHet1, NHCONH[C(R3)2]mN(R3)2, NHCONH[C(R3)2]pHet1, OCONH[C(R3)2]mN(R3)2, OCONH[C(R3)2]pHet1, CHO, COA, ═S, ═NR3 and/or ═O, Het1 denotes dihydropyrrolyl, pyrrolidinyl, azetidinyl, oxetanyl, tetrahydro-imidazolyl, dihydropyrazolyl, tetrahydropyrazolyl, tetrahydrofuranyl, dihydropyridyl, tetrahydropyridyl, piperidinyl, morpholinyl, hexa-hydropyridazinyl, hexahydropyrimidinyl, [1,3]dioxolanyl, tetrahydropyranyl, pyrazolyl, pyridyl or piperazinyl, which is unsubstituted or mono- or disubstituted by Hal, CN, OH, OA, COOA, CONH2, S(O)nA, S(O)nAr, COA, A and/or ═O, A denotes unbranched or branched alkyl with 1-10 C-atoms, wherein one or two non-adjacent CH— and/or CH2-groups may be replaced by N—, O- and/or S-atoms and wherein 1-7H-atoms may be replaced by F or Cl, Cyc denotes cyclic alkyl with 3-7 C-atoms, which is unsubstituted or monosubstituted by [C(R3)2]pOH, A′ denotes unbranched or branched alkyl with 1, 2, 3 or 4 C-atoms, Hal denotes F, Cl, Br or I, n denotes 0, 1 or 2, m denotes 1, 2 or 3, p denotes 0, 1, 2, 3 or 4, and pharmaceutically acceptable solvates, salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios.
地址 Darmstadt DE