首页> 外国专利> 2. Pyridine-3-IL-Ac acid derivatives as replication inhibitors of human immunodeficiency virus

2. Pyridine-3-IL-Ac acid derivatives as replication inhibitors of human immunodeficiency virus

机译:2.吡啶-3-IL-Ac酸衍生物作为人免疫缺陷病毒的复制抑制剂

摘要

Propagation formula compound (1),Including pharmaceutically acceptable salts, pharmaceutical compounds including compounds, procedures for the preparation of compounds and their use in the suppression of HIV syndrome and in the treatment of people living with HIV / AIDS. 1. Claim 1: a formula compound (1),O including: R1 is hydrogen, halogen, cyanogen and alkyl c83218331; 8320;a. Halogenated tar c83218d318321; 8320;-C₁₋₁₀-OH alkyl, HO-C₁₋₁₀-O- alkyl,Ar1,-N (R) (R)-C (O) N (R⁷) (R⁸) or (R⁹) (R¹⁰) N-C₁₋₁₀ alkyl;2. The condition is that R 1 and r830808 are non asphalt, R2 is benzodioxillo, naftelenio, fenilo, pirazi Nile, pirizilo, pirimidinilo, quinoline, isoquioli Nile, tetrazinilo or trizinilo, and can be replaced by 1-4 alternatives selected from cyanogen, carbamoyo, carbocilo, halo, hidroxi, c83318321 tar;a. Halogenated tar c83218d318321; 8320;-N (R) (R)C₁₋₁₀-O- alkyl,AR830808,Ar⁴-C₁₋₁₀-O- alkyl,(R⁵) (Ar⁴-C₁₋₁₀ alkyl) N-,a. Ar83088-o-lessor c83221131; ar832008-o (ar830808) (r8309099) n-lessor c83318321; - iv8320;R³ is C₁₋₁₀ alkyl;R⁴ is hydrogen, cyano, halo, haloalkyl C₁₋₁₀,C₁₋₁₀ alkyl,C₁₋₁₀-O- alkyl,alquenilo CNH.8322;e. Hidroxi acquilo c83318321; 8320oh, carbamoyo, azetidini, pirrolidini, piperidinilo, morfolino or piperaznilo; provided that R1 and r830808 are not two kinds of aspha r8309es hydrogen or c83318321; 8320;R8310s is hydrogen, c832131 hydrocarbon; 8320;C₁₋₁₀-O-C₁₋₁₀- alkyl,1. C-832188331-8321; 8320a-o-c (o) -,C₃₋₉ cycloalkyl,(Cicloalquilo C) alquilo C -1 - (rent c83218c83318321); 8320piperidinilo -,Keywords tetrahydropiranil hydrocarbon c83318321; 8320 -;morpholin-C₁₋₁₀- alkyl,(Alquilo C) N-alquilo C -piperidinyl-C₁₋₁₀- alkyl,1 - (c) piperidinil asphalt c832188321; 8320;1- (alquilo C) piperazinil-alquilo C -Arz - lessor c832183.318321; 8320a;Harp.1- (alquilsulfonil C) piperidinilo- o 1- (alquilcarbonil C) piperidinil-R8311811 is hydrogen or c832131; 83218320;R831222 is hydrogen, c8321 aspha 8320;C₃₋₉ cycloalkyl,(Alquilo C) cicloalquilo C --So83223 (rent c832183 31); or - so83222 (rent c8332323);R8313 is hydrogen or c8332131; 8321; 8320;R¹⁰ is hydrogen, C₁₋₁₀ alkyl,(tetrahydropyranyl) C₁₋₁₀ alkyl or C₁₋₁₀-O-C- (O) alkyl;(R⁷) (R⁸) N taken together form an azetidinyl, pyrrolidinyl, piperidinyl, 1,1-dioxidothiomorpholinyl or a morpholinyl ring group; (R⁹) (R¹⁰) N taken together form an azetidinyl, azocanyl, pyrrolidinyl. piperidinyl or an azaspirononanyl ring and are optionally substituted with 1-3 C₁₋₁₀ alkyl substituents;AR1 es imidazollo, pirazolilo, pirid Nile, pirimidinilo, pirrolilo or dihydrocyclopentapirazolilo can be replaced by 1-3 alternatives selected from ammonia, hydrocarbon c833218331a and / or c833238331a;Ar² is imidazolyl, pyrazolyl or pyridinyl and is optionally substituted with 1-3 substituents selected from C₁₋₁₀ alkyl and halo substituents; Ar³ is phenyl, pyridinyl, pyrazolyl, pyridazinyl or pyrimidinyl and is optionally substituted with 1-3 substituents selected from C₁₋₆ alkyl,a. Halo, caboxi and Ciano; and AR 8308088 are phenyl, benzofuran or pyridan, which can be replaced by 1-3 alternatives selected from cyanogen, halo, c8332131 tar and c833183221 tar;Each of the terms "halogenated tar" includes all halogenated isomers from one halogenated to perhalo.
机译:化合物(1)的传播配方,包括药学上可接受的盐,包括化合物在内的药物化合物,化合物的制备程序及其在抑制HIV综合征和治疗HIV / AIDS患者中的用途。 1.根据权利要求1所述的式化合物(1),O,其包括:R 1为氢,卤素,氰和烷基c83218331;和8320; a。卤代焦油c83218d318321; 8320; -C 1 -OH烷基,HO-C 1 -O-烷基,Ar 1 --N(R)(R)-C(O)N(R 4)(R 4)或(R 4)(R 10)N -C 1-4烷基; 2。条件是R 1和r830808为非沥青,R2为苯并二恶英,naftelenio,fenilo,比拉齐尼罗河,pirizilo,piirimidinolo,喹啉,异喹啉尼罗河,四嗪尼罗或trizinilo,并且可以被1-4个选自氰根,氨基甲酸酯的替代物取代,carbocilo,halo,hidroxi,c83318321 tar;卤代焦油c83218d318321; 8320; -N(R)(R)C 1 -O-烷基,AR830808,Ar 1 -C 1 -O-烷基,(R 4)(Ar 1 -C 4烷基)N-,a。 Ar83088-o-lessor c83221131; ar832008-o(ar830808)(r8309099)n出租人c83318321; -iv8320; R 3为C 1-8烷基; R 4为氢,氰基,卤素,卤代烷基C 1,C 6烷基,C 1-0烷基,alquenilo CNH.8322; e。 Hidroxi acquilo c83318321; 8320oh,卡巴莫约,阿齐替尼,吡罗尼迪尼,哌立地诺,morfolino或piperaznilo;前提是R1和r830808不是两种沥青; r8309es氢或c83318321; 8320; R8310s是氢,c832131烃; 8320; C 1 -O-C 4-烷基,1。 C-832188331-8321; 8320a-o-c(o)-,C 6环烷基,(Cicloalquilo C)alquilo C -1-(rent c83218c83318321); 8320piperidinilo-,关键字四氢吡喃基烃c83318321; 8320-;吗啉代-C 1-烷基,(Alquilo C)N-alquilo C-哌啶基-C 8-烷基,1-(c)哌啶基沥青c832188321; 8320; 1-(alquilo C)哌嗪-alquilo C -Arz-出租人c832183.318321; 8320a; Harp.1-(alquilsulfonil C)piperidinilo-1-(alquilcarbonil C)piperidinil-R8311811是氢或c832131; 83218320; R831222是氢,c8321沥青; 8320; C 8环烷基,(Alquilo C)cicloalquilo C --So83223(rent c832183 31);或-so83222(rent c8332323); R8313是氢或c8332131; 8321; 8320; R 17为氢,C 1-8烷基,(四氢吡喃基)C 8烷基或C 8 -OC-(O)烷基;(R 4)(R 4)N一起形成氮杂环丁烷基,吡咯烷基,哌啶基,1,1 -二氧化硫代吗啉基或吗啉基环基; (R 7)(R 15)N一起形成氮杂环丁烷基,偶氮烷基,吡咯烷基。哌啶基或氮杂螺环戊烯基环,并任选被1-3个C 1-4烷基取代基取代; AR1咪唑基,吡唑利洛,吡咯尼罗尔,吡咪唑啉基,吡咯烷酮或二氢环戊哌唑唑基可被1-3个选自氨,烃c833218331a和 / Ar 2是咪唑基,吡唑基或吡啶基,并任选地被1-3个选自C 1-4烷基和卤素取代基的取代基取代;或c833238331a;或c833238331a。 Ar 3是苯基,吡啶基,吡唑基,哒嗪基或嘧啶基,并任选地被1-3个选自C 1-4烷基,a的取代基取代。光晕,卡波西和西亚诺; AR 8308088和AR 8308088是苯基,苯并呋喃或吡喃,它们可以被1-3种选自氰,卤素,c8332131焦油和c833183221焦油的替代物所取代;术语“卤化焦油”包括从一种卤代到全卤代的所有卤代异构体。

著录项

  • 公开/公告号AR110716A1

    专利类型

  • 公开/公告日2019-04-24

    原文格式PDF

  • 申请/专利权人 VIIV HEALTHCARE UK (Nº 5) LIMITED;

    申请/专利号AR2018P100002

  • 发明设计人

    申请日2018-01-02

  • 分类号C07D401/04;A61K31/4439;A61K31/4545;A61P31/18;C07D401/14;C07D405/14;C07D471/04;C07D491/048;

  • 国家 AR

  • 入库时间 2022-08-21 12:03:54

相似文献

  • 专利
  • 外文文献
  • 中文文献
获取专利

客服邮箱:kefu@zhangqiaokeyan.com

京公网安备:11010802029741号 ICP备案号:京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有
  • 客服微信

  • 服务号