CAS: 1004316-88-4; Thiazol-5-Ylmethyl ((2R,5R)-5-((S)-2-(3-((2-Isopropylthiazol-4-yl)Methyl)-3-Methylureido)-4-Morpholinobutanamido)-1,6-Diphenylhexan-2-yl)Carbamate

该化合物是细胞色素P450 3A(CYP3A)酶的选择性,基于机制的抑制剂,主要用作抗逆转录病毒疗法的药代动力增强剂,其主要优势在于能够促进CYP3A代谢的共同管理药物(如蛋白抑制剂)的系统性接触,从而提高其治疗效果.与Ritonavir不同的是,Cobicistat缺乏内在抗病毒活动,从而最大限度地减少非目标效应.它具有可预测的药代动力,并由于它具有特定的CYP3A抑制作用,减少了药物-药物相互作用的潜力.此外, Cobicistat被作为独立的制剂或固定剂量组合体来制定,从而提高患者的合规性.它与其他抗逆转录病毒药物的兼容性,其稳定性和兼容性使它成为艾滋病毒治疗方案的一个宝贵组成部分.

结构式图片

上下游产品

2,7,10,12-Tetraazatridecanoic Acid, 9-(2-Aminoethyl)-12-Methyl-13-[2-(1-Methylethyl)-4-Thiazolyl]-8,11-Dioxo-3,6-Bis(Phenylmethyl)-, 5-Thiazolylmethyl Ester, (3R,6R,9S)- 1004316-87-3
2-[3-(2-异丙基-噻唑-4-基甲基)-3-甲基-脲基]-4-吗啉-4-基丁酸 2-[3-(2-Isopropyl-Thiazol-4-Ylmethyl)-3-Methyl-Ureido]-4-Morpholin-4-Ylbutyric Acid 1051463-80-9
3-Methyl-1-[(3S)-2-Oxooxolan-3-Yl]-3-{[2-(Propan-2-yl)-1,3-Thiazol-4-Yl]Methyl}Urea 1004316-93-1

合成工艺路线路线简述

    N-[(1R,4R)-4-氨基-5-苯基-1-(苄基)戊基]氨基甲酸 5-噻唑基甲基酯置于盐酸,碳酸氢钠,Sodium Carbonate,1-羟基苯并三唑,盐酸-N-乙基-N'-(3-二甲氨基丙基)碳二亚胺,N,N-二异丙基乙胺体系中,用 四氢呋喃,1,4-二氧六环,水,N,N-二甲基甲酰胺 用作溶剂,化学反应 29.0H,反应生成可比司他
    参考文献: Methods And Intermediates For Preparing Pharmaceutical Agents[fr] Procédés Et Intermédiaires Pour La Préparation D'Agents Pharmaceutiques
    标题: Methods And Intermediates For Preparing Pharmaceutical Agents[fr] Procédés Et Intermédiaires Pour La Préparation D'Agents Pharmaceutiques
    摘要:用于制备式i化合物及其盐的方法和中间体.

    专利信息


    专利号:WO-2024028893-A1
    优先权日:2022-08-01
    标 题:Substituted benzimidazoles for treating viral diseases
    发明人:CHAUDHARI VINOD DINKAR; THAKUR KRISHAN GOPAL; RINGE RAJESH PRAKASH; SINGH DESHKANWAR; KAUR SIMRAN; CHAWLA RAVNEET SINGH; JOSHI AKSHAY
    权利人:COUNCIL OF SCIENT AND INDUSTRIAL RESEARCH AN INDIAN REGISTERED BODY INCORPORATED UNDER THE REGN OF S
    摘要:The invention relates to benzimidazole compounds, pharmaceutically acceptable salts thereof and its pharmaceutical compositions for reducing/treating viral infections. The present invention also relates to synthesis of such benzimidazole compounds. The present invention further relates to compositions which comprise such benzimidazole compounds or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, optionally in combination. The compounds of the invention are useful in reducing/treating viral infections particularly coronavirus infections caused by SARS-CoV, MERS-CoV and SARS-CoV-2.

    专利号:US-5935946-A
    优先权日:1997-07-25
    标 题 :Nucleotide analog composition and synthesis method
    发明人:MUNGER JR JOHN D; ROHLOFF JOHN C; SCHULTZE LISA M
    权利人:GILEAD SCIENCES INC
    摘要:The invention provides a composition comprising bis(POC)PMPA and fumaric acid (1:1). The composition is useful as an intermediate for the preparation of antiviral compounds, or is useful for administration to patients for antiviral therapy or prophylaxis. The composition is particularly useful when administered orally. The invention also provides methods to make PMPA and intermediates in PMPA synthesis. Embodiments include lithium t-butoxide, 9-(2-hydroxypropyl) adenine and diethyl p-toluenesulfonylmethoxyphosphonate in an organic solvent such as DMF. The reaction results in diethyl PMPA preparations containing an improved by-product profile compared to diethyl PMPA made by prior methods.

    专利号:US-2014051888-A1
    优先权日:2012-08-20
    标题 :Novel stereoisomeric mixtures, synthesis and uses thereof
    发明人:DUBAY WILLIAM; BUTLER JEFFREY D; LIOTTA CHARLES L
    权利人:AMPAC FINE CHEMICALS LLC
    摘要:A novel stereochemical mixture of 1,6-diaryl-2,5-diaminohexanes, such as a mixture of stereoisomers of 1,6-diphenylhexane-2,5-diamine, is described. Also described are methods of preparing stereochemically pure 1,6-diaryl-2,5-diaminohexanes, and particularly stereochemically pure 1,6-diphenyl-2,5-diaminohexane. Also described is the use of both the mixture of stereoisomers and the individual stereoisomers.

    专利号:CN-104193643-B
    优先权日:2014-09-12
    标 题:For the synthesis of the intermediate of anti-AIDS drug toughener cobicistat

    专利号:CN-104193643-A
    优先权日:2014-09-12
    标 题 :A new intermediate for the synthesis of cobicistat, an anti-AIDS drug enhancer

    专利号:CN-109912426-B
    优先权日:2017-12-13
    标题:Intermediate for the synthesis of anti-AIDS drug enhancer cobicistant
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    ✅ COA系统入驻 | 共享模式

    主要参考文献


    1: Cattaneo D, Cossu MV, Rizzardini G. Pharmacokinetic drug evaluation of ritonavir (versus cobicistat) as adjunctive therapy in the treatment of HIV. Expert Opin Drug Metab Toxicol. 2019 Nov;15(11):927-935. doi: 10.1080/17425255.2019.1685495. Epub 2019 Nov 3. Review. Available from http://www.ncbi.nlm.nih.gov/books/NBK540525/ No abstract available. Available from http://www.ncbi.nlm.nih.gov/books/NBK540287/ doi: 10.1080/14656566.2018.1559299. Epub 2018 Dec 26. Review. doi: 10.2147/DDDT.S147493. eCollection 2018. Review.
    6: Deeks ED. Darunavir/Cobicistat/Emtricitabine/Tenofovir Alafenamide: A Review in HIV-1 Infection. Drugs. 2018 Jul;78(10):1013-1024. doi: 10.1007/s40265-018-0934-2. Review. doi: 10.1097/COH.0000000000000465. Review. Available from http://www.ncbi.nlm.nih.gov/books/NBK458451/ Available from http://www.ncbi.nlm.nih.gov/books/NBK458440/ doi: 10.1177/1060028017717018. Epub 2017 Jun 19. Review.
    11: Angione SA, Cherian SM, Özdener AE. A Review of the Efficacy and Safety of Genvoya® (Elvitegravir, Cobicistat, Emtricitabine, and Tenofovir Alafenamide) in the Management of HIV-1 Infection. J Pharm Pract. 2018 Apr;31(2):216-221. doi: 10.1177/0897190017710519. Epub 2017 May 30. Review. doi: 10.1080/14787210.2017.1323634. Epub 2017 May 9. Review. Available from http://www.ncbi.nlm.nih.gov/books/NBK409851/ doi: 10.1016/S0213-005X(17)30006-X. Review. Spanish. eCollection 2016. Review.

    合成参考文献


    摘要:S76 | LUXPHARMA | Pharmaceuticals Marketed in Luxembourg | Pharmaceuticals marketed in Luxembourg, as published by d'Gesondheetskeess (CNS, la caisse nationale de sante, www.cns.lu), mapped by name to structures using CompTox by R. Singh et al. (2021) DOI:10.1021/acsenvironau.1c00008. List downloaded from
    参考文献:10.1358/dot.2012.48.12.1895682
    摘要:Temesgen Z. Cobicistat-boosted elvitegravir-based fixed-dose combination antiretroviral therapy for HIV infection. Drugs Today (Barc). 2012 Dec;48(12):765–71. doi: 10.1358/dot.2012.48.12.1895682.
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