首页> 外国专利> Di (hetero) arilciclohexano Derivatives, Preparation method and Pharmaceutical compositions containing same and Uses of same in Cardiac pathologies.

Di (hetero) arilciclohexano Derivatives, Preparation method and Pharmaceutical compositions containing same and Uses of same in Cardiac pathologies.

机译:二(杂)阿立斯环己酮衍生物,其制备方法和包含其的药物组合物及其在心脏病理学中的用途。

摘要

The compounds of Formula 1 are valuable pharmaceutical compounds that inhibit ATP sensitive potassium channels in the heart, for example, they can be used to treat cardiovascular system disorders, such as arrhythmias or heart failure, such as possible situations, Heart disease, heart disease, or cardiomyopathy. Item 1: a compound of Formula 1, wherein AR1 and ar2 are independent of each other, may be the same or different, be phenyl, naphthalene or isopropyl, and can be replaced with 1, 2, 3 or 4 substitutes that are exactly the same or different from the halogen series,Ciano, C1-5 tar, alquenilo c2-5, cycloquil c3-8-cvh2v, Ar3, c1-5-o -,-5-O---In these substances, all tar, halogenated compounds and cyclopropyl compounds in AR1 and ar2 are replaced by one or more fluorine substitutes; Ar3 and AR5 are independent o f each other and can be the same or different, belonging to phenyl or monocyclic, These alternatives are all optional, consisting of 1, 2 or 3 exactly the same or different halogen, cyanogen, C1-5 tar, c1-5-o --.Oalquil C1-3O alquil C1-5S (O) my R13R14NS (O) 2 en donde todos los grupos alquilo en Ar3 y Ar5 est n opcionalmente sustituidos con uno oms sustituyentes fluor Ar4 es fenilo o heteroarilo que est n todos opcionalmente sustituidos con 1 2 -5-O---C1-3O alkyl, C1-5S alkyl (O) n and R15R16NS (O) 2, wherein all alkyl, alkenyl and cycloalkyl groups in Ar4 are optionally substituted with one or more fluorine substituents; R1 is R3, R4O or R5R6N; R2 is hydrogen, C1-8 alkyl, C2-8 alkenyl, C2-8 alkynyl, C2-8 phenyl-alkenyl, Ar4, R17-O-C1-8 alkyl, R18R19N-C1-8 alkyl, Het-CuH2u or C3 cycloalkyl alkyl -8-CuH2u, wherein the phenyl group in C2-8 phenyl-alkenyl is optionally substituted with 1, 2 or 3 identical or different substituents of the series consisting of halogen, cyano, C1-5 alkyl, C1-5 alkyl- O- and C1-5S alkyl (O) g, and wherein all alkyl groups, alkenyl groups,alkynyl groups and cycloalkyl groups in R2 are optionally substituted with one or more fluorine substituents; R3, R4, R5 and R6, which are all independent of each other and which may be identical or different, are hydrogen, C1-8 alkyl or C3-8-CpH2p cycloalkyl, where all alkyl groups and cycloalkyl groups in R3, R4, R5 and R6 are optionally substituted with one or more fluorine substituents; R11, R12, R13, R14, R15, R16, R17, R18 and R19, which are all independent of each other and can be identical or different, are hydrogen, C1-8 alkyl or C3-8-CqH2q cycloalkyl, where all alkyl groups and cycloalkyl groups in R11, R12, R13, R14, R15, R16, R17,R18 and R19 can be replaced by one or more fluorescent substitutes; het is the residue of a saturated ring composed of four to seven single rings, which contains one or two heterocyclic atoms in a series of nitro, oxygen and sulfur, which are identical or different, and connected together by a cyclic carbon atom, which is optional. 1. 2, 3 or 4 are replaced with the same or different substitutes for C1-5 phenyl and hydrocarbon, wherein the phenyl group in het is replaced with 1, 2 or 3 with the same or different substitutes for halogenated, cyanogen and C1-5 hydrocarbons,C1-5-o - and c1-5-s (o) H tar, in which all tar groups of het and het can be replaced by one or more fluorine substitutes; heteromorphism is the residue of 5 members or 6 single ring aromatic ring systems, or the residue of 1 member in a double ring aromatic ring system composed of 8 members, 9 members or 10 members, 2 or 3 identical or different heterocyclic atoms, consisting of nitro, oxygen and sulfur; F, G, h, K, m and N, independent of each other, may be the same or different, 0, 1 or 2; P, Q, V and W, independent of each other, may be the same or different, 0, 1, 2, 3 or 4; or 0, 1. 2, 3, 4, 5 or 6;In this case, all cyclopropyl compound groups, whether or not there are other substitutes, may choose to use one or more of the same or different C1-4 tar substitutes; in any stereoisomer form or in any way mixed to form an isomer form, Or one of its physiologically acceptable salts; however, if R1 is both hydroxyl and R2 is both hydrogen, AR1 and ar2 should not be substituted for phenyl at the same time.
机译:式1化合物是抑制心脏ATP敏感钾通道的有价值的药物化合物,例如,它们可用于治疗心血管系统疾病,例如心律不齐或心力衰竭,例如可能的情况,心脏病,心脏病,或心肌病。第1项:式1的化合物,其中AR 1和ar 2彼此独立,可以相同或不同,可以是苯基,萘或异丙基,并且可以被1、2、3或4个完全相同的取代基取代。与卤素系列相同或不同的是,Ciano,C1-5焦油,alquenilo c2-5,cycloquil c3-8-cvh2v,Ar3,c1-5-o-,-5-O--在这些物质中,所有焦油, AR1和Ar2中的卤代化合物和环丙基化合物被一种或多种氟代取代物取代; Ar3和AR5彼此独立,可以相同或不同,属于苯基或单环。这些替代物都是可选的,由1、2或3个完全相同或不同的卤素,氰,C1-5焦油,c1组成-5-o-。Oalquil C1-3O alquil C1-5S(O)我的R13R14NS(O)2 en dode todos los grupos alquilo en Ar3 y Ar5 est n opcionalmente sustituidos con uno oms sustituyentes fluor Ar4 es fenilo o heteroarilo que est n个待办事项专用化合物con 1 2 -5-O --- C1-3O烷基,C1-5S烷基(O)n和R15R16NS(O)2,其中Ar4中的所有烷基,烯基和环烷基均可选地被一个或多个更多的氟取代基; R1是R3,R4O或R5R6N; R 2是氢,C 1-8烷基,C 2-8烯基,C 2-8炔基,C 2-8苯基-烯基,Ar 4,​​R 17-O-C 1-8烷基,R 18 R 19 N-C 1-8烷基,Het-CuH 2u或C 3环烷基烷基-8-CuH 2u,其中C 2-8苯基-烯基中的苯基任选地被1、2或3个相同或不同的取代基取代,所述取代基由卤素,氰基,C1-5烷基,C1-5烷基-O组成-和C1-5S烷基(O)g,并且其中R2中的所有烷基,烯基,炔基和环烷基任选地被一个或多个氟取代基取代;彼此独立并且可以相同或不同的R 3,R 4,R 5和R 6是氢,C 1-8烷基或C 3-8 -CpH 2p环烷基,其中R 3,R 4中的所有烷基和环烷基, R5和R6任选地被一个或多个氟取代基取代; R 11,R 12,R 13,R 14,R 15,R 16,R 17,R 18和R 19彼此独立并且可以相同或不同,它们是氢,C 1-8烷基或C 3-8 -C q H 2q环烷基,其中所有烷基R11,R12,R13,R14,R15,R16,R17,R18和R19中的基团和环烷基可以被一个或多个荧光取代基取代; het是由4至7个单环组成的饱和环的残基,该环包含一个或两个在硝基,氧和硫系列中相同或不同的杂环原子,并通过环状碳原子连接在一起,可选的。 1、2、3或4被相同或不同的C1-5苯基和烃取代基取代,其中het中的苯基被1、2或3相同或不同的卤代,氰基和C1-取代基取代5种碳氢化合物,C1-5-o-和c1-5-s(o)H焦油,其中所有het和het焦油基团都可以被一个或多个氟代取代物取代;异质性是5个成员或6个单环芳香族环系统的残基,或在8个成员,9个成员或10个成员,2个或3个相同或不同的杂环原子组成的双环芳香族环系统中1个成员的残基,硝基,氧和硫;彼此独立的F,G,h,K,m和N可以相同或不同,为0、1或2;彼此独立的P,Q,V和W可以相同或不同,0、1、2、3或4;或0、1、2、3、4、5或6;在这种情况下,所有环丙基化合物基团,无论是否有其他取代基,都可以选择使用一种或多种相同或不同的C1-4焦油取代基;或以任何立体异构体形式或以任何方式混合以形成异构体形式,或其生理上可接受的盐之一;但是,如果R1都是羟基,R2都是氢,则AR1和Ar2不能同时被苯基取代。

著录项

  • 公开/公告号AR066833A1

    专利类型

  • 公开/公告日2009-09-16

    原文格式PDF

  • 申请/专利权人 SANOFI - AVENTIS;

    申请/专利号AR2008P102340

  • 发明设计人

    申请日2008-06-03

  • 分类号C07C317/14;C07C321/28;C07C255/50;C07C255/53;C07C61/22;C07D317/12;C07D215/04;C07D217/12;C07D213/46;C07D213/61;C07D213/64;C07D333/22;C07D249/08;C07D277/24;C07D231/12;C07D239/34;C07D487/04;C07D401/08;C07D401/12;C07D405/08;C07D405/12;C07D307/04;A61P9/02;A61P9/04;A61P9/06;A61P9/08;A61P9/10;

  • 国家 AR

  • 入库时间 2022-08-21 19:28:38

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