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Focal adhesion kinase inhibitors

机译:黏着斑激酶抑制剂

摘要

Compound of formula (I): in which: n1 and R2 are each independently a monocyclic, bicyclic or polycyclic, aromatic or partially aromatic 5-12 membered ring system in which each ring system independently comprises 0-3 heteroatoms selected from the group consisting of N, 0, S, S (0) and S (0) 2, and each ring system is substituted with 0-5 substituents independently selected from Y; in which Y comprises halo, hydroxy, cyano, thio, nitro, trifluoromethyl, oxo, (C1-C6) alkyl, (C2-C6) alkenyl, (C2-C6) alkynyl, alkoxy, methylenedioxy, ethylenedioxy, NH (R) , N (R) 2, SR, C (0) NH (R), C (0) N (R) 2, RC (0) N (R), C (0) C (0) NR2, C (0 ) C (0) 0R, RC (0) 0, ROC (0), ROC (0) 0, RC (0), RS02, RS02-alkyl (C1-C3), SO2N (R) 2, N (R) S02R, urea carrying 0-3 R, aryl (C3-C10), heteroaryl (C2-C10), dihydroheteroaryl (C2-C10), tetrahydroheteroaryl (C2-C10), hexahydroheteroaryl (C2-C10), mono or bicyclic cycloalkyl ( C3-C10), or mono- or bicyclo-heterocyclyl (C2-C10), in which each R independently comprises hydrogen or substituted or unsubstituted aryl or substituted or unsubstituted (C1-C6) alkyl, or in which two groups R taken together with a nitrogen atom to which they are attached together with the nitrogen atom form a heterocyclic ring comprising 0-2 additional heteroatoms selected from the group consisting of N, 0, S, S (0) and S (0) 2, and substituted with 0-3 alkyl groups (C1-C3), hydroxyl, hydroxyalkyl (Ci-C3) or (C-C3) alkoxy (ci-c3) alkyl; in which any alkyl, alkenyl, alkynyl, alkoxy, aryl, heteroaryl, dihydroheteroaryl, tetrahydroheteroaryl, hexahydroheteroaryl, cycloalkyl or heterocyclyl of Y or R, or both, may be further substituted with 1-3 substituents selected from halo, hydroxyl, cyano, thio, nitro, trifluoromethyl, oxo, (C1-C6) alkyl, (C2-C6) alkenyl, (C2-C6) alkynyl, alkoxy, methylenedioxy, ethylenedioxy, NH (R), N (R) 2, SR, C ( 0) NH (R), C (0) N (R) 2, RC (0) N (R), C (0) C (0) NR2, C (0) C (0) 0R, RC (0) 0, ROC (0), ROC (0) 0, RC (0), RS02, RS02-alkyl (C1-C3), SO2N (R) 2, N (R) S02R, urea carrying 0-3 R, or with an aryl (C6-C10), heteroaryl (C2-C10), dihydroheteroaryl (C2-C10), tetrahydroheteroaryl (C2-C10), hexahydroheteroaryl (C2-C10), mono or bicyclic cycloalkyl (C3-C10), or mono or substituted or unsubstituted bicyclo-heterocyclyl (C2-C10); X is a bond or (C1-C3) alkyl comprising 0-1 heteroatoms selected from the group consisting of NR, 0, S, S (0) and S (0) 2, and in which the (C1-C3) alkyl ) is substituted with 0-1 hydroxyl, halo, (C1-C3) alkoxy, (C1-C3) alkylamino or dialkylamino (C1-C3) 2 groups; R3 is trifluoromethyl, halo, nitro or cyano; or a salt, tautomer, solvate or hydrate thereof for use in the treatment of cancer.
机译:式(I)的化合物:其中:n 1和R 2各自独立地是单环,双环或多环,芳族或部分芳族的5-12元环系统,其中每个环系统独立地包含0-3个选自以下的杂原子: N,0,S,S(0)和S(0)2,并且每个环系统被0-5个独立地选自Y的取代基取代;其中Y包括卤素,羟基,氰基,硫代,硝基,三氟甲基,氧代,(C1-C6)烷基,(C2-C6)烯基,(C2-C6)炔基,烷氧基,亚甲二氧基,乙二氧基,NH(R), N(R)2,SR,C(0)NH(R),C(0)N(R)2,RC(0)N(R),C(0)C(0)NR2,C(0) C(0)0R,RC(0)0,ROC(0),ROC(0)0,RC(0),RS02,RS02-烷基(C1-C3),SO2N(R)2,N(R)S02R ,带有0-3 R的尿素,芳基(C3-C10),杂芳基(C2-C10),二氢杂芳基(C2-C10),四氢杂芳基(C2-C10),六氢杂芳基(C2-C10),单环或双环环烷基(C3- (C10),或单或双环杂环基(C2-C10),其中每个R独立地包含氢或取代或未取代的芳基或取代或未取代的(C1-C6)烷基,或其中两个基团R与氮一起它们与氮原子连接的原子形成杂环,该杂环包含0-2个额外的杂原子,该杂原子选自N,0,S,S(0)和S(0)2,并被0-3取代烷基(C1-C3),羟基,羟烷基(C1-C3)或(C-C3)烷氧基(C1-C3)烷基;其中任何烷基,烯基,炔基,烷氧基,芳基,杂芳基,二氢杂芳基,Y或R或两者的四氢杂芳基,六氢杂芳基,环烷基或杂环基可进一步被1-3个选自卤素,羟基,氰基,硫代的取代基取代,硝基,三氟甲基,羰基,(C1-C6)烷基,(C2-C6)烯基,(C2-C6)炔基,烷氧基,亚甲二氧基,乙二氧基,NH(R),N(R)2,SR,C(0 )NH(R),C(0)N(R)2,RC(0)N(R),C(0)C(0)NR2,C(0)C(0)0R,RC(0)0 ,ROC(0),ROC(0)0,RC(0),RS02,RS02-烷基(C1-C3),SO2N(R)2,N(R)SO2R,带有0-3 R的尿素或带有芳基(C6-C10),杂芳基(C2-C10),二氢杂芳基(C2-C10),四氢杂芳基(C2-C10),六氢杂芳基(C2-C10),单或双环环烷基(C3-C10)或单或取代或未取代的双环杂环基(C 2 -C 10); X是包含0-1个选自NR,0,S,S(0)和S(0)2的杂原子的键或(C1-C3)烷基,其中(C1-C3)烷基被0-1个羟基,卤素,(C1-C3)烷氧基,(C1-C3)烷基氨基或二烷基氨基(C1-C3)2个基团取代; R 3是三氟甲基,卤素,硝基或氰基;或其盐,互变异构体,溶剂化物或水合物用于癌症的治疗。

著录项

  • 公开/公告号ES2485040T3

    专利类型

  • 公开/公告日2014-08-12

    原文格式PDF

  • 申请/专利权人 THE SCRIPPS RESEARCH INSTITUTE;

    申请/专利号ES20080726698T

  • 申请日2008-03-10

  • 分类号C07D213/74;A61K31/47;A61P35;C07D401/12;C07D401/14;C07D405/12;C07D413/12;C07D417/12;C07D417/14;

  • 国家 ES

  • 入库时间 2022-08-21 15:55:03

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