首页> 外国专利> FUSED pyrrole Derivatives, Pharmaceutical compositions containing them and their use in the preparation of a Medicament for the treatment of diseases mediated by inhibition of the Kinase.

FUSED pyrrole Derivatives, Pharmaceutical compositions containing them and their use in the preparation of a Medicament for the treatment of diseases mediated by inhibition of the Kinase.

机译:FUSED吡咯衍生物,包含它们的药物组合物及其在制备药物中的用途,该药物用于治疗通过抑制激酶介导的疾病。

摘要

These compounds inhibit quinase and can be used as drugs. Requirement 1: formula compound (1), wherein a is a benzene ring or a heterocyclic ring, which is a single ring aromatic ring composed of 5 or 6 atoms, among the selected rings between N or s, there are 1, 2 or 3 heteroatoms, and the other atoms are C; AR is nataleni or heterocyclic, which is an excited aromatic ring There are 8 to 10 atoms on the ring, at least one aromatic ring, which contains 1, 2 or 3 heteromorphic atoms, selected from n to s, and the other atoms of the ring are C,One to three substitutes can be selected from C1-6, cycloquilo c3-7 (cyclopropene c3-7) - C1-6, c2-6, alquenilo c2-6, tar c2-6, hydroxy, alcox C1-6, halogenated, ISO tar, ISO propoxy, nitro, Cano and other oils to replace the above mentioned Nagorno Nagorno and non-n-propane. Ammonia water and mono or sulfur dioxide in C1-6 tar; R1 is h, halogen, C1-6 tar, alcoxi C1-6, carboxyl, nitro, cyanogen, ammonia water, mono or with C1-6 tar, ISO tar, isopropoxide, cyclo-c3-7 (epoxidation c3-7) - C1-6 tar, alquenio c2-6, c2-6, c1xi, C16, Alternative to C1-6 non circulating oiloptionally substituted heterocyclylcarbonyl-C1-6 alkyl, optionally substituted phenyl-C1-6 alkyl, optionally substituted phenylcarbonyl-C1-6 alkyl optionally substituted, optionally substituted heteroarylcarbonyl-C1-6 alkyl or heteroalkoxy-C1- alkyl 6, or R1 is N (R ') (Rö),N (R ') (Rö) -C 1-6 alkyl- or N (R') (Rö) -carbonyl-C 1-6 alkyl-,in which R 'and Rö independently from each other are selected from the group consisting of H, C1-6 alkyl, C3-7 cycloalkyl, (C3-7 cycloalkyl) -C1-6 alkyl, C2-6 alkenyl, C2- alkynyl 6, heteroalkyl, optionally substituted phenyl-C 1-6 alkyl, optionally substituted heteroaryl-C 1-6 alkyl, optionally substituted heterocyclyl-C 1-6 alkyl, optionally substituted phenylcarbonyl, optionally substituted heteroarylcarbonyl and optionally substituted heterocyclylcarbonyl; or R1 is R'-CO-N (Rö) -C 1-6 alkyl-,R -O-CO-N (R) -alquilo C1-6-R'-SO2-N (Rö) -C1-6 alkyl- or (R ') (Rö) N-SO2-N (R'ö) -C1-6 alkyl-,Members on the blacklistRö and R'ö independently from each other are selected from the group consisting of H, C1-6 alkyl, C3-7 cycloalkyl, (C3-7 cycloalkyl) -C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, heteroalkyl, optionally substituted phenyl, optionally substituted heteroaryl, optionally substituted heterocyclyl, optionally substituted phenyl-C 1-6 alkyl, optionally substituted heteroaryl-C 1-6 alkyl and optionally substituted heterocyclyl-C 1-6 alkyl; R2, R2 ',and R2ö independently of each other are H, halogen, cyano, nitro, amino, mono- or disubstituted amino with C 1-6 alkyl, C 1-6 alkyl, C 3-7 cycloalkyl, (C 3-7 cycloalkyl) -C 1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, heteroalkyl, hydroxy, C1-6 alkoxy or heteroalkoxy; n is an integer from 0 to 4; and pharmaceutically acceptable prodrugs and salts thereof; wherein, unless otherwise defined, the term "heteroalkyl" means C1-6 alkyl substituted with one or more substituents independently selected from the group consisting of nitro, hydroxy, halogen, cyano, C1-6 alkoxy, formyl, (C1-6 alkyl) -carbonyl, carboxyl, C1-6 alkylthio, C1-6 alkylsulfinyl,The term isopropoxy refers to ISO tar-o -;Heterocyclic ring is a single aromatic ring with 5 to 8 atoms in the ring shape, including 1, 2 or 3 heteroatoms in the ring selected from n to s, and other atoms in the ring are C; heterocyclic ring is a non aromatic single ring matrix with 3 to 8 atoms in the ring shape, including 1 to 2 atoms. A ring is a heteromorphic atom selected from n, O and s, n (or) n, where n is an integer between 0 and 2.The other atom on the ring is C, and the optional aryl word replaces do,Optional heterogeneous substitutes, i.e. substitutes independently selected among halogen, nitro, cyanogen, ammonia, C1-6 tar, dichlorodiene-6, acrylonitrile-c2-6, acrylonitrile-c2-6, and propylene-c2-6 groups, respectively representing phenyl, isopropene, and isopropene, Hydroxy group, alcoxi C1-6, monoamine or cluster containing C1-6 tar, isotar and isoalcoxi; the term "bicyclic aromatic hydrocarbon" refers to the radical substance containing two aromatic rings, which are fused.
机译:这些化合物抑制奎纳酶,可用作药物。要求1:通式化合物(1),其中a为苯环或杂环,为5或6个原子组成的单环芳香环,在N或s之间选择的环中有1、2或3杂原子,其他原子为C; AR是纳那替尼或杂环,它是一个激发的芳香环。该环上有8至10个原子,至少一个芳香环包含1,2或3个选自n至s的杂多态原子,并且其他原子环是C,C 1-6,环quilo c3-7(环丙烯c3-7)-C1-6,c2-6,alquenilo c2-6,焦油c2-6,羟基,醇类C1-可以选择1-3个取代基6,卤代,ISO焦油,ISO丙氧基,硝基,卡诺等油替代上述Nagorno Nagorno和非正丙烷。 C1-6焦油中的氨水和一氧化硫或二氧化硫; R1为h,卤素,C1-6焦油,醇C1-6,羧基,硝基,氰,氨水,一元或含C1-6焦油,ISO焦油,异丙醇,环c3-7(环氧化c3-7)- C1-6焦油,烷基c2-6,c2-6,c1xi,C16,C1-6非循环油的替代品任选取代的杂环基羰基-C1-6烷基,任选取代的苯基-C1-6烷基,任选取代的苯基羰基-C1-6任选取代的烷基,任选取代的杂芳基羰基-C 1-6烷基或杂烷氧基-C 1-烷基6,或R 1为N(R')(Rö),N(R')(Rö)-C 1-6烷基-或N( R')(Rö)-羰基-C 1-6烷基-,其中R'和Rö彼此独立地选自H,C1-6烷基,C3-7环烷基,(C3-7环烷基)-C 1-6烷基,C 2-6烯基,C 2-炔基6,杂烷基,任选取代的苯基-C 1-6烷基,任选取代的杂芳基-C 1-6烷基,任选取代的杂环基-C 1-6烷基,取代的苯基羰基,任选取代的杂芳基羰基和d。任选取代的杂环羰基;或R1是R'-CO-N(Rö)-C 1-6烷基-,R -O-CO-N(R)-alquilo C1-6-R'-SO2-N(Rö)-C1-6烷基-或(R')(Rö)N-SO2-N(R'ö)-C1-6烷基-,黑名单上的成员Rö和R'ö彼此独立地选自H,C1-6烷基,C 3-7环烷基,(C 3-7环烷基)-C 1-6烷基,C 2-6烯基,C 2-6炔基,杂烷基,任选取代的苯基,任选取代的杂芳基,任选取代的杂环基,任选取代的苯基-C 1- 6个烷基,任选取代的杂芳基-C 1-6烷基和任选取代的杂环基-C 1-6烷基; R 2,R 2'和R2ö彼此独立地是H,卤素,氰基,硝基,氨基,具有C 1-6烷基,C 1-6烷基,C 3-7环烷基的单或双取代氨基,(C 3- 7个环烷基)-C 1-6烷基,C 2-6烯基,C 2-6炔基,杂烷基,羟基,C 1-6烷氧基或杂烷氧基; n是0至4的整数;及其药学上可接受的前药及其盐;其中,除非另有定义,否则术语“杂烷基”是指被一个或多个独立地选自硝基,羟基,卤素,氰基,C1-6烷氧基,甲酰基,(C1-6烷基)的取代基取代的C 1-6烷基-羰基,羧基,C 1-6烷硫基,C 1-6烷基亚磺酰基,术语异丙氧基是指ISO tar-o-杂环是指一个具有5至8个原子的环状芳香环,包括1、2或3个杂原子在选自n至s的环中,环中的其他原子为C;杂环是具有3至8个原子的环状的非芳香族单环基质,包括1至2个原子。环是选自n,O和s,n(或)n的异构原子,其中n是0到2之间的整数。环上的另一个原子是C,可选的芳基词取代do,可选的异构替代物,即分别独立地选自代表苯基,异丙基和异丙基,羟基,醇C1-6,含有C1-6焦油,异戊醇和异醇的单胺或簇;术语“双环芳族烃”是指含有两个稠合的芳环的自由基物质。

著录项

  • 公开/公告号AR058338A1

    专利类型

  • 公开/公告日2008-01-30

    原文格式PDF

  • 申请/专利权人 F. HOFFMANN-LA ROCHE AG;

    申请/专利号AR2006P105492

  • 发明设计人

    申请日2006-12-13

  • 分类号C07D209/42;C07D401/06;C07D403/06;C07D405/06;C07D409/06;C07D471/04;C07D491/04;C07D495/04;A61K31/404;A61K31/407;A61K31/496;A61K31/4045;A61K31/4453;A61K31/5377;A61P9/10;A61P11/06;A61P19/02;A61P37/08;

  • 国家 AR

  • 入库时间 2022-08-21 20:09:00

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