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首页> 外国专利> Isoindolina or Isoquinoline Compounds, a process for their preparation, Pharmaceutical compositions containing them and their use in the manufacture of a Medicament for different types of cancer

Isoindolina or Isoquinoline Compounds, a process for their preparation, Pharmaceutical compositions containing them and their use in the manufacture of a Medicament for different types of cancer

机译：异吲哚啉或异喹啉化合物，其制备方法，包含它们的药物组合物及其在制备用于不同类型癌症的药物中的用途

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摘要

Anticancer drugs. Claim 1: consists of formula (1),wherein: Het represents a heteroaryl group; T represents a hydrogen atom, a linear or branched C₁₋₆ alkyl group optionally substituted with one to three halogen atoms, a C₁₋₄-NR¹R² alkyl group,O c83318324-r8310a, rental group c8332121;R¹ and R² independently represent each other a hydrogen atom or a linear or branched C₁₋₆ alkyl group, or R¹ and R² form with the nitrogen atom to which a heterocycloalkyl group is attached; R³ represents a linear or branched C₁₋₆ alkyl group, a linear or branched C₂₋₆ alkenyl group, a linear or branched C₂₋₆ alkynyl group, a cycloalkyl group, a C₃₋₁₀-C₁₋₆ cycloalkyl group in which the alkyl group may be linear or branched, a heterocycloalkyl group, an aryl group or a heteroaryl group, it being understood that one or more carbon atoms of the groups defined hereinbefore,Or the carbon atoms in its possible substitutes may be heavy;R83088 is an arilo, heteromorphic, epoxidated or tar c8321s 83318326 linear or separable group, on the understanding that heavy matter may have occurred to one or more carbon atoms in the group defined above or to the carbon atoms of their possible substitutes;R⁵ represents a hydrogen atom or a halogen atom, a linear or branched C₁₋₆ alkyl group, or a linear or branched C₁₋₆ alkoxy group; R⁶ represents a hydrogen atom or a linear or branched C₁₋₆ alkyl group; R⁷ represents a selected group of R⁷,R8311-CO-,-O-CO--No. 8311; No. 8311 - co -,R⁷-SO₂-,R⁷NR⁷-SO₂- in which R⁷ and R⁷ independently represent each other a hydrogen atom, a linear or branched C₁₋₆ alkyl group, a linear or branched C₂₋₆ alkenyl group or a linear or branched C₂₋₆ alkynyl group , a cycloalkyl, a heterocycloalkyl, an aryl group or a heteroaryl; R⁸ and R⁹ independently represent each other, an oxo group or a halogen atom; p and p are, independently of each other, integers equal to 0, 1, 2, 3 or 4; q and q are, independently of each other, integers equal to 1, 2 or 3; it being understood that when the compound of formula (1) contains a hydroxy group,The latter can be replaced by the following: Po (OM) (OM),-PO (OM) (O M)-PO (O M) (O M)-PO (O) (O) M-PO (OM) (O CH CH O CH)o -PO (O M) (O CH CH O CH)wherein M and M independently represent each other a hydrogen atom, a linear or branched C₁₋₆ alkyl group, a linear or branched C₂₋₆ alkenyl group, a linear or branched C₂₋₆ alkynyl group, a cycloalkyl or a heterocycloalkyl, the two compounds being 5 to 6 ring members, while M₁⁺ and M₂⁺ independently represent each other a pharmaceutically acceptable monovalent cation, M₃²⁺ represents a pharmaceutically acceptable divalent cation and n is an integer comprised between 1 and 5; it is also understood that: aryl means a phenyl, naphthyl, biphenyl or indenyl group;Heteromorphic refers to any single cycle or double cycle group consisting of 5 to 10 members in the ring, with at least one aromatic part and 1 to 4 selected non biological oxygen, sulfur and nitrogen atoms (including four generations of nitrogen);Cyclopentadienyl ring refers to any non monocyclic or bicyclic aromatic carbon group with 3 to 10 members in the ring, which may include a fusion ring with a bridge or a helix; isocyclic propyl group refers to any non monocyclic or bicyclic aromatic carbon group composed of 3 to 10 members in the ring, It contains one or three heteroatoms selected from oxygen, sulfur, So, So832222 and nitrogen; however, it is understood that the double cycle atom group can be polymorph or spiral type, which may be Arilo, heteromorph, cyclopropene and heterocyclopropene, tar, Alquenilo, asphalt and Alcoxi,be substituted with 1 to 3 groups selected from: linear or branched C₁₋₆ alkyl optionally substituted; linear or branched C al alkenyl group optionally substituted; optionally substituted linear or branched C₂₋₆ alkynyl group; spiro C₃₋₆;C o linear or branched alkoxy optionally substituted; C₁₋₆-S- alkyl;a. Hydroxyl; oxo (or positive oxidation at appropriate time);nitro ciano -COOR -OCOR -NRR RCONR-NRCO-;C₁₋₆ linear or branched polyhaloalkyl; trifluoromethoxy; C₁₋₆sulfonyl alkyl; halogen; optionally substituted aryl; optionally substituted heteroaryl; optionally substituted aryloxy; optionally substituted arylthio; optionally substituted cycloalkyl or optionally substituted heterocycloalkyl, it being understood that R and R represent, independently of each other, a hydrogen atom, an optionally substituted linear or branched C₁₋₆ alkyl group or an aryl group; their enantiomers and diastereoisomers, and addition salts thereof with a pharmaceutically acceptable acid or base.
机译：抗癌药。权利要求1：由式（1）组成，其中：Het表示杂芳基; T代表氢原子，可被1-3个卤素原子取代的直链或支链C 1-4烷基，C 1-4 -NR 1 R 2烷基，O c83318324-r8310a，租用基团c8332121; R 1和R 2彼此独立地表示。氢原子或直链或支链的C 1-4烷基，或R 1和R 2与连接杂环烷基的氮原子形成; R 3代表直链或支链的C 1-8烷基，直链或支链的C 20烯基，直链或支链的C 20炔基，环烷基，C 1 -C 4环烷基，其中烷基基团可以是直链或支链的，杂环烷基，芳基或杂芳基，应理解为上文所定义的基团中的一个或多个碳原子，或在其可能的取代基中的碳原子可以是重的; R83088为芳基，杂多，环氧化或焦油酸c8321s 83318326线性或可分离基团，但应理解为上面定义的基团中的一个或多个碳原子或它们的可能取代基的碳原子可能已发生重质反应; R 5表示氢原子或卤原子，直链或支链的C 1-4烷基或直链或支链的C 1-4烷氧基; R 5代表氢原子或直链或支链的C 1-4烷基; R 7代表R 3的选定基团，R8311-CO-，-O-CO-No。 8311; No.8311-共-，R 4 -SO 2-，R 3 NR 4 -SO 2-，其中R 5和R 4彼此独立地表示氢原子，直链或支链的C 1-4烷基，直链或支链的C 20烯基或线性或支化的C 20炔基，环烷基，杂环烷基，芳基或杂芳基; R 5和R 6彼此独立地表示氧代基团或卤素原子。 p和p彼此独立地是等于0、1、2、3或4的整数; q和q彼此独立地是等于1、2或3的整数;应当理解，当式（1）的化合物包含羟基时，后者可以被以下取代：Po（OM）（OM），-PO（OM）（OM）-PO（OM）（OM） -PO（O）（O）M-PO（OM）（O CH CH O CH）o -PO（OM）（O CH CH O CH）其中M和M彼此独立地表示氢原子，直链或支链C 6烷基，直链或支链的C 20烯基，直链或支链的C 20炔基，环烷基或杂环烷基，两个化合物为5至6个环成员，而M 5和M 20独立地表示彼此为药学上可接受的单价阳离子，M 1 -C 6代表药学上可接受的二价阳离子，n为1至5之间的整数。还应理解：芳基是指苯基，萘基，联苯或茚基;亚同型是指在环中由5至10个成员组成的任何单环或双环基团，其中至少有一个芳族部分和1至4个选择的非生物氧，硫和氮原子（包括四代氮）;环戊二烯基环是指环中具有3-10个成员的任何非单环或双环芳族碳基团，其中可包括带有桥或螺旋的稠合环;杂环丙基是指由环中的3至10个成员组成的任何非单环或双环芳族碳基，它含有一个或三个选自氧，硫，So，So832222和氮的杂原子;然而，应理解的是，双环原子基团可以是多晶型或螺旋型的，其可以是被选自以下的1-3个基团取代的芳基，杂晶型，环丙烯和杂环丙烯，焦油，Alquenilo，沥青和Alcoxi。任选取代的C 1-8烷基;直链或支链的C 1-8烯基，任选地被取代;任选取代的直链或支链C 20炔基;螺C 5; C o任选被取代的直链或支链烷氧基; C 1 -S-烷基; a。羟;氧代（或在适当的时候进行正氧化）;硝基钢琴-COOR -OCOR -NRR RCONR-NRCO-; C 1线性或支化的多卤代烷基三氟甲氧基C₁₋₆磺酰基烷基;卤素;任选取代的芳基;任选取代的杂芳基;任选取代的芳氧基;任选取代的芳硫基;任选取代的环烷基或任选取代的杂环烷基，应理解，R 1和R 2彼此独立地代表氢原子，任选取代的直链或支链C 1-4烷基或芳基;它们的对映异构体和非对映异构体，以及它们与药学上可接受的酸或碱的加成盐。

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