发明名称 (AZA-)ISOQUINOLINONE DERIVATIVES
摘要 Compounds of the formula I;;in which R1, X, Y and n have the meanings indicated in Claim 1, are inhibitors of Tankyrase, and can be employed, inter alia, for the treatment of diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation.
申请公布号 US2015210686(A1) 申请公布日期 2015.07.30
申请号 US201314420578 申请日期 2013.07.12
申请人 MERCK PATENT GMBH 发明人 Dorsch Dieter;Buchstaller Hans-Peter
分类号 C07D471/04;C07D217/24;C07D405/10;C07D401/10;A61K31/4725;A61K31/4375;A61K31/472 主分类号 C07D471/04
代理机构 代理人
主权项 1. A Compound of the formula Iin which R1 denotes F, Cl, CH3, OCH3, CF3, CHF2 or CH2F, R2 denotes H or unbranched or branched alkyl with 1-6 C-atoms, X denotes C or N, with the proviso that only one X denotes N, Y denotes A, Cyc, [C(R2)2]qOA, [C(R2)2]qN(R2)2, [C(R2)2]pHet1, [C(R2)2]pCOOR2, [C(R2)2]pCON(R2)2 or [C(R2)2]pSO2N(R2)2, Ar denotes phenyl, which is unsubstituted, or mono- or disubstituted by Hal, A, [C(R2)2]pOR, [C(R2)2]pN(R2)2, [C(R2)2]pHet2, NO2, CN, [C(R2)2]pCOOR, [C(R2)2]pN(R2)2, N(R2)2COA, NR2SO2A, [C(R2)2]pSO2N(R2)2, S(O)nA, COHet2, O[C(R2)2]mN(R2)2, O[C(R2)2]pHet2, NHCOOA, NHCON(R2)2 or COA, Het1 denotes pyrrolidinyl, azetidinyl, tetrahydroimidazolyl, tetrahydrofuranyl, oxetanyl, tetrahydropyrazolyl, tetrahydropyranyl, piperidinyl, morpholinyl, hexahydropyridazinyl, hexahydropyrimidinyl, [1,3]dioxolanyl, piperazinyl, furyl, thienyl, pyrrolyl, imidazolyl, pyrazolyl, oxazolyl, isoxazolyl, oxadiazolyl, thiazolyl, triazolyl, tetrazolyl, pyridyl, pyrimidyl, pyridazinyl, indolyl, isoindolyl, benzimidazolyl, indazolyl, quinolyl, 1,3-benzodioxolyl, benzothiophenyl, benzofuranyl, imidazopyridyl or furo[3,2-b]pyridyl, each of which is unsubstituted or mono- or disubstituted by Hal, A, [C(R2)2]pOR2, [C(R2)2]pN(R2)2, [C(R2)2]pHet2, [C(R2)2]pOHet2, [C(R2)2]pAr, NO2, CN, [C(R2)2]pCOOR2, [C(R2)2]pCON(R2)2, NR2COA, NR2SO2A, [C(R2)2]pSO2N(R2)2, S(O)nA, COHet2, O[C(R2)2]mN(R2)2, O[C(R2)2]pAr, O[C(R2)2]pHet2, NHCOOA, NHCON(R2)2, CHO, COA, ═S, ═NR and/or ═O, Het2 denotes dihydropyrrolyl, pyrrolidinyl, azetidinyl, oxetanyl, tetrahydroimidazolyl, dihydropyrazolyl, tetrahydropyrazolyl, tetrahydrofuranyl, dihydropyridyl, tetrahydropyridyl, piperidinyl, morpholinyl, hexahydro-pyridazinyl, hexahydropyrimidinyl, [1,3]dioxolanyl, tetrahydropyranyl or piperazinyl, each of which is unsubstituted or mono- or disubstituted by Hal, CN, OR2, COOR2, CON(R2)2, S(O)nA, S(O)nAr, COA, A and/or ═O, A denotes unbranched or branched alkyl with 1-10 C-atoms, wherein two adjacent carbon atoms may form a double bond and/or one or two non-adjacent CH— and/or CH2-groups may be replaced by N—, O— and/or S-atoms and wherein 1-7 H-atoms may be replaced by F or Cl, Cyc denotes cycloalkyl with 3-7 C-atoms, which is unsubstituted or monosubstituted by OH, Hal or A, 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, q denotes 1, 2, 3 or 4, with the proviso that, if R1 is absent or methyl or methoxy, then Y is not methyl, trifluoromethyl, piperidinomethyl, butyl, 3-methoxy-1-propyl or 4-morpholinyl, and pharmaceutically acceptable solvates, salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios.
地址 Darmstadt DE