CAS: 178979-85-6; Capravirine

该化合物是主要用于治疗艾滋病毒感染的抗逆转录病毒药物,属于非核反应反转转录酶抑制剂(NNRTIs)类,通过抑制反转发酶酶,防止病毒的复制而发挥作用.卡普瑞因的特点是能够保持活动,防止某些艾滋病毒菌株,这些菌株对其他NRTI有抗药性.复合体展示了一种独特的化学结构,有助于其药理特性,包括它与目标酶的亲近性.它一般是口服的,具有有利的药理基因特征,允许在某些治疗疗法中一次性服用.与其他抗逆转剂一样,潜在的副作用可能包括狂躁症,胃肠扰动和肝酶升高.持续的研究继续评估它在不同病人群体中的效力和安全性,特别是在那些有多种抗药的艾滋病毒菌系的人中.总体而言,卡布拉维因是艾滋病毒治疗环境中一个宝贵的选择.

结构式图片

MSDS等安全信息

    上下游产品

    {5-[(3,5-二氯苯基)硫基]-4-异丙基-1-(4-吡啶基甲基)-1H-咪唑-2-基}甲醇 2-Hydroxymethyl-5-(3,5-Dichlorophenylthio)-4-Isopropyl-1-(Pyridin-4-yl)Methyl-1H-Imidazole 178981-89-0
    2-Carbamoyloxymethyl-4-Isopropyl-1-(Pyridin-4-yl)Methyl-1H-Imidazole 209743-76-0

    合成工艺路线路线简述

      📜2-Carbamoyloxymethyl-4-Isopropyl-1-(Pyridin-4-yl)Methyl-1H-Imidazole,3,5-Dichlorobenzenesulfenyl Chloride置于三乙胺体系中,用 N,N-二甲基甲酰胺 用作溶剂,化学反应 0.5H,以61%的收率获得2-氨基甲酰氧基甲基-5-(3,5-二氯苯基硫代)-4-异丙基-1-(吡啶-4-基)甲基-1H-咪唑
      参考文献:Process For Producing Arylsulfenyl Halide
      标题:Process For Producing Arylsulfenyl Halide
      摘要:一种用于制备化合物的过程,其化学式为(II):其中hal1代表卤素,R1和r2分别独立地代表卤素,烷基,烷氧基,硝基或氰基,包括允许卤化剂与化合物的反应的方法,该化合物的化学式为(I):其中alk代表支链烷基,R1和r2如上定义.

      海关参考信息

      专利信息


      专利号:US-2005124683-A1
      优先权日:2003-09-17
      标 题:HIV protease inhibitors, compositions containing the same, their pharmaceutical uses and materials for their synthesis
      发明人:ALEGRIA LARRY A; CANAN-KOCH STACIE S; DRESS KLAUS R; HUANG BUWEN; KUMPF ROBERT A; LEWIS KATHLEEN K; MATTHEWS JEAN J; SAKATA SYLVIE K; VIRGIL SCOTT C
      权利人:AGOURON PHARMA
      摘要:The present invention relates to a series of chemical compounds useful as Human Immunodeficiency Virus (HIV) protease inhibitors and to the use of such compounds as antiviral agents. The invention further relates to pharmaceutical compositions containing such antiviral agents, and their uses and materials for their synthesis

      专利号:US-2007275953-A1
      优先权日:2003-09-22
      标题:2-Pyridinone Derivatives, Having Hiv Inhibiting Properties
      发明人:LE VAN KIET; GEORGES RENOIT; HEYESI LASZLO; CAUVIN CHRISTINE; BOLAND SANDRA; DURANT FRANCOIS; DEMONTE DOMINIQUE; VAN LINT CHRIS; BURNY ARTHU; BOLLEN ALEX; JACQUET ALAIN; DE WALQUE STEPHAINE
      权利人:UNIV NOTRE DAME DE LA PAIX; UNIV BRUXELLES
      摘要:The present invention relates to 2-Pyridinone derivatives, more specifically 5-ethyl-6-methyl-2-pyridinone derivatives, according to general formula I that inhibit human immunodeficiency virus type 1 (HIV-1) replication and are therefore of interest in the treatment of Acquired Immune Deficiency Syndrome (AIDS). The present invention further relates to the synthesis of said compounds and their use, with or without other pharmaceutical agents, in the treatment of AIDS and viral infections by HIV-1.

      专利号:US-2007099915-A1
      优先权日:2005-10-07
      标题 :Inhibitors of the hiv integrase enzyme
      发明人:DRESS KLAUS R; JOHNSON TED W; PLEWE MICHAEL B; TANIS STEVEN P; ZHU HUICHUN
      权利人:PFIZER
      摘要:The present invention is directed to compounds of formula (I), n nand pharmaceutically acceptable salts and solvates thereof, their synthesis, and their use as modulators or inhibitors of the human immunodeficiency virus (“HIVâ€?) integrase enzyme.

      专利号:US-7468375-B2
      优先权日:2004-04-26
      标题:Inhibitors of the HIV integrase enzyme
      发明人:DRESS KLAUS RUPRECHT; HU QIYUE; JOHNSON TED WILLIAM; PLEWE MICHAEL BRUNO; TANIS STEVEN PAUL; WANG HAI; YANG ANLE; YIN CHUNFENG; ZHANG JUNHU
      权利人:PFIZER
      摘要:The present invention is directed to compounds of formula (I), and pharmaceutically acceptable salts and solvates thereof, their synthesis, and their use as modulators or inhibitors of the human immunodeficiency virus (“HIVâ€?) integrase enzyme.

      专利号:US-2009170846-A1
      优先权日:2005-10-03
      标题 :Inhibitors of the hiv integrase enzyme
      发明人:DRESS KLAUS RUPRECHT; PLEWE MICHAEL BRUNO; JOHNSON TED WILLIAM; TANIS STEVEN PAUL; TRAN KHANH TUAN
      权利人:PFIZER
      摘要:The present invention is directed to compounds of formula (I), and pharmaceutically acceptable salts and solvates thereof, their synthesis, and their use as modulators or inhibitors of the human immunodeficiency virus “HIVâ€? integrase enzyme. Formula (I).

      专利号:EP-1873155-A1
      优先权日:2004-04-26
      标题:Inhibitors of the HIV integrase enzyme
      发明人:DRESS KLAUS RUPRECHT; HU QIYUE; JOHNSON TED WILLIAM; PLEWE MICHAEL BRUNO; TANIS STEVEN PAUL; ZHU HUICHUN; ZHANG JUNHU
      权利人:PFIZER
      摘要:The present invention is directed to compounds of formula (I),n nand pharmaceutically acceptable salts and solvates thereof, their synthesis, and their use as modulators or inhibitors of the human immunodeficiency virus ('HIV') integrase enzyme.

      供应商参考报价(招募中)

      品牌试剂参考报价(招募中)

      📌 第三方产品分析报告

      ✅ COA系统入驻 | 共享模式

      主要参考文献


      1: Li X, Zhan P, De Clercq E, Liu X. The HIV-1 non-nucleoside reverse transcriptase inhibitors (part V): capravirine and its analogues. Curr Med Chem. 2012;19(36):6138-49. Review.

      合成参考文献


      参考文献:10.1124/mol.65.1.244
      摘要:Auwerx J, Esnouf R, De Clercq E, Balzarini J. Susceptibility of feline immunodeficiency virus/human immunodeficiency virus type 1 reverse transcriptase chimeras to non-nucleoside RT inhibitors. Mol Pharmacol. 2004 Jan;65(1):244–51. doi: 10.1124/mol.65.1.244.
      📝 需求与反馈
      尽可能描述清楚需求与问题信息
      ×

      通知