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PE20120617A1 - Procesos para preparar cobicistat y sus productos intermedios - Google Patents

Procesos para preparar cobicistat y sus productos intermedios

Info

Publication number
PE20120617A1
PE20120617A1 PE2011001737A PE2011001737A PE20120617A1 PE 20120617 A1 PE20120617 A1 PE 20120617A1 PE 2011001737 A PE2011001737 A PE 2011001737A PE 2011001737 A PE2011001737 A PE 2011001737A PE 20120617 A1 PE20120617 A1 PE 20120617A1
Authority
PE
Peru
Prior art keywords
compound
formula
prepare
cobicistat
processes
Prior art date
Application number
PE2011001737A
Other languages
English (en)
Inventor
Richard Polniaszek
Steven Pfeiffer
Richard Yu
Aaron Cullen
Eric Dowdy
Duong Tran
Kenneth Kent
Doug Cordeau
Leah Easton
Zhongxin Zhou
Original Assignee
Gilead Sciences Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=42634770&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=PE20120617(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Gilead Sciences Inc filed Critical Gilead Sciences Inc
Publication of PE20120617A1 publication Critical patent/PE20120617A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/22—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D277/30—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C209/00—Preparation of compounds containing amino groups bound to a carbon skeleton
    • C07C209/62—Preparation of compounds containing amino groups bound to a carbon skeleton by cleaving carbon-to-nitrogen, sulfur-to-nitrogen, or phosphorus-to-nitrogen bonds, e.g. hydrolysis of amides, N-dealkylation of amines or quaternary ammonium compounds
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C209/00—Preparation of compounds containing amino groups bound to a carbon skeleton
    • C07C209/68—Preparation of compounds containing amino groups bound to a carbon skeleton from amines, by reactions not involving amino groups, e.g. reduction of unsaturated amines, aromatisation, or substitution of the carbon skeleton
    • C07C209/70—Preparation of compounds containing amino groups bound to a carbon skeleton from amines, by reactions not involving amino groups, e.g. reduction of unsaturated amines, aromatisation, or substitution of the carbon skeleton by reduction of unsaturated amines
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C303/00—Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides
    • C07C303/34—Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides of amides of sulfuric acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C307/00—Amides of sulfuric acids, i.e. compounds having singly-bound oxygen atoms of sulfate groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C307/02—Monoamides of sulfuric acids or esters thereof, e.g. sulfamic acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C307/00—Amides of sulfuric acids, i.e. compounds having singly-bound oxygen atoms of sulfate groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C307/04—Diamides of sulfuric acids
    • C07C307/06—Diamides of sulfuric acids having nitrogen atoms of the sulfamide groups bound to acyclic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/22—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D277/28—Radicals substituted by nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Engineering & Computer Science (AREA)
  • Virology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

REFERIDA A UN METODO PARA PREPARAR UN COMPUESTO DE FORMULA (I) QUE COMPRENDE a) DIMERIZAR UN COMPUESTO DE FORMULA (II) PARA PROPORCIONAR UN COMPUESTO DE FORMULA (V), b) DESPROTEGER EL COMPUESTO (V) PROPORCIONANDO UN COMPUESTO (VI), c) REDUCIR EL COMPUESTO (VI) A UN COMPUESTO (VII), d) CONVERTIR EL COMPUESTO (VII) A LA SAL CORRESPONDIENTE MEDIANTE TRATAMIENTO CON UN ACIDO Y UN SOLVENTE ORGANICO, e) CONVERTIR LA SAL DE d) EN UN COMPUESTO DE FORMULA (IX) Y f) ACOPLAR EL COMPUESTO (IX) CON UN ACIDO DE FORMULA (Xa) PROPORCIONANDO EL COMPUESTO DE FORMULA (I), DONDE R1 ES -S(=O)2NRaRb; Ra Y Rb SON ALQUILO C1-C8 O JUNTOS Ra Y Rb FORMAN CON EL NITROGENO AL CUAL ESTAN UNIDOS UN ANILLO SATURADO DE 3 O 4 MIEMBROS O UN ANILLO SATURADO O PARCIALMENTE INSATURADO DE 5, 6 O 7 MIEMBROS QUE COMPRENDE 1 O 2 HETEROATOMOS
PE2011001737A 2009-04-03 2010-04-01 Procesos para preparar cobicistat y sus productos intermedios PE20120617A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US16649809P 2009-04-03 2009-04-03

Publications (1)

Publication Number Publication Date
PE20120617A1 true PE20120617A1 (es) 2012-05-26

Family

ID=42634770

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2011001737A PE20120617A1 (es) 2009-04-03 2010-04-01 Procesos para preparar cobicistat y sus productos intermedios

Country Status (27)

Country Link
US (4) US8497396B2 (es)
EP (2) EP2414325B1 (es)
JP (8) JP5612662B2 (es)
KR (3) KR101874557B1 (es)
CN (4) CN111217808A (es)
AP (1) AP2887A (es)
AR (1) AR076027A1 (es)
AU (1) AU2010232559B2 (es)
BR (1) BRPI1012638B8 (es)
CA (4) CA2754698C (es)
CL (1) CL2011002370A1 (es)
CO (1) CO6400216A2 (es)
EA (2) EA201590979A1 (es)
EC (1) ECSP11011391A (es)
ES (1) ES2548252T3 (es)
HK (1) HK1223912A1 (es)
IL (4) IL215399A (es)
MX (2) MX2011010397A (es)
NZ (4) NZ726536A (es)
PE (1) PE20120617A1 (es)
PT (1) PT2414325E (es)
SG (2) SG174585A1 (es)
TW (2) TWI464165B (es)
UA (1) UA108738C2 (es)
UY (1) UY32535A (es)
WO (1) WO2010115000A2 (es)
ZA (1) ZA201107430B (es)

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UA108738C2 (uk) 2009-04-03 2015-06-10 Спосіб одержання інгібітора цитохром р450 монооксигенази та залучені проміжні сполуки
JP2012140390A (ja) * 2011-01-06 2012-07-26 Sumitomo Chemical Co Ltd α−アミノ−γ−ブチロラクトンの製造方法
WO2012151165A1 (en) * 2011-05-02 2012-11-08 Gilead Sciences, Inc. Amorphous solid salts
CN104093702A (zh) 2012-02-03 2014-10-08 吉里德科学公司 用于制备药物试剂的方法和中间体
WO2014047849A1 (zh) * 2012-09-27 2014-04-03 上海迪赛诺化学制药有限公司 细胞色素p450单加氧酶抑制剂中间体及其制法和用途
CN103694196A (zh) * 2012-09-27 2014-04-02 上海迪赛诺化学制药有限公司 细胞色素p450单加氧酶抑制剂中间体及其制法和用途
WO2014057498A2 (en) 2012-10-08 2014-04-17 Mylan Laboratories Ltd. Process for the preparation of cobicistat intermediates
JP2016504364A (ja) * 2012-12-26 2016-02-12 アッシア・ケミカル・インダストリーズ・リミテッド コビシスタット塩
CN104370777A (zh) * 2013-08-13 2015-02-25 上海迪赛诺化学制药有限公司 合成(2r,5r)-1,6-二苯基己烷-2,5-二胺及其盐的中间体及所述中间体的制备方法和应用
AU2014356067A1 (en) * 2013-11-29 2016-06-16 Mylan Laboratories Ltd. Amorphous cobicistat solid dispersion
EP3077373B1 (en) 2013-12-03 2018-09-12 Mylan Laboratories Ltd. Preparation of cobicistat intermediates
CN104193643B (zh) * 2014-09-12 2016-02-10 宁波九胜创新医药科技有限公司 用于合成抗艾滋病药物增强剂cobicistat的中间体
CN104447472A (zh) * 2014-11-06 2015-03-25 江苏森萱医药化工股份有限公司 D)-2-苄基-n,n-二甲基氮杂环丙烷基-1-磺酰胺合成方法
CN104557565B (zh) * 2015-01-08 2016-07-06 浙江工业大学 抗艾滋病药物增强剂Cobicistat关键中间体盐酸盐的制备方法
WO2016128885A1 (en) * 2015-02-09 2016-08-18 Laurus Labs Private Limited A process for preparation of cobicistat
EP3259267A4 (en) * 2015-02-18 2019-01-23 MSN Laboratories Private Limited A NOVEL PROCESS FOR THE PREPARATION OF 1,3-THIAZOL-5-YLMETHYL [(2R, 5R) -5 - {[(2S) -2 - [(METHYL {[2- (PROPAN-2-YL) -1) CARBAMATE 3-thiazol-4-yl] methyl} carbamoyl) amino] -4- (morpholin-4-yl) butanoyl] amino} -1,6-DIPHÉNYLHEXAN-2-YL]
CN107674039A (zh) * 2016-08-01 2018-02-09 上海朴颐化学科技有限公司 一种可比西他中间体的制备方法
WO2018064071A1 (en) 2016-09-27 2018-04-05 Gilead Sciences, Inc. Therapeutic compositions for treatment of human immunodeficiency virus
CN109912530A (zh) * 2017-12-13 2019-06-21 上海奥博生物医药技术有限公司 一种可比司他原料杂质的制备方法
CN109232301B (zh) * 2018-10-15 2021-01-01 天津希恩思生化科技有限公司 一种四异丙基肼的制备方法
CN110642721B (zh) * 2018-12-21 2022-09-30 安徽贝克生物制药有限公司 盐酸司来吉兰的制备方法
CN110878071A (zh) * 2019-11-21 2020-03-13 华南农业大学 一种α-氨基-γ-丁内酯及其盐的制备方法

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Also Published As

Publication number Publication date
AP2887A (en) 2014-05-31
HK1223912A1 (en) 2017-08-11
IL215399A0 (en) 2011-12-29
CN102438982A (zh) 2012-05-02
JP6491706B2 (ja) 2019-03-27
CN104876888B (zh) 2018-06-15
JP2017122107A (ja) 2017-07-13
JP2020189861A (ja) 2020-11-26
IL215399A (en) 2015-11-30
TWI464165B (zh) 2014-12-11
KR101728375B1 (ko) 2017-04-19
PT2414325E (pt) 2015-10-29
KR20120006035A (ko) 2012-01-17
NZ726536A (en) 2018-04-27
IL237643A0 (en) 2015-04-30
HK1166976A1 (zh) 2012-11-16
JP2016128476A (ja) 2016-07-14
JP2018162274A (ja) 2018-10-18
CA2754698A1 (en) 2010-10-07
CA2754698C (en) 2016-06-07
US9115100B2 (en) 2015-08-25
CN107382997B (zh) 2021-02-26
US20150005493A1 (en) 2015-01-01
CA3083433C (en) 2022-08-09
ZA201107430B (en) 2012-12-27
NZ594864A (en) 2014-03-28
JP2018008983A (ja) 2018-01-18
IL250068A0 (en) 2017-03-30
US8497396B2 (en) 2013-07-30
IL237642A (en) 2017-01-31
JP5986599B2 (ja) 2016-09-06
EA201190179A1 (ru) 2013-01-30
CA2925137A1 (en) 2010-10-07
CL2011002370A1 (es) 2012-05-25
US20140088304A1 (en) 2014-03-27
CN104876888A (zh) 2015-09-02
CO6400216A2 (es) 2012-03-15
AU2010232559B2 (en) 2015-06-18
CA3008903C (en) 2021-06-08
AR076027A1 (es) 2011-05-11
UY32535A (es) 2010-10-29
WO2010115000A3 (en) 2011-09-22
KR20180077324A (ko) 2018-07-06
CN111217808A (zh) 2020-06-02
SG10201404926UA (en) 2015-02-27
CN102438982B (zh) 2015-05-06
US9428473B2 (en) 2016-08-30
EA022739B1 (ru) 2016-02-29
EP3009434A1 (en) 2016-04-20
JP2023002679A (ja) 2023-01-10
US8853210B2 (en) 2014-10-07
SG174585A1 (en) 2011-10-28
JP2014193897A (ja) 2014-10-09
JP5612662B2 (ja) 2014-10-22
EP2414325B1 (en) 2015-08-26
TW201518283A (zh) 2015-05-16
ECSP11011391A (es) 2012-03-30
US20160002186A1 (en) 2016-01-07
MX338731B (es) 2016-04-28
JP2012522797A (ja) 2012-09-27
HK1214265A1 (zh) 2016-07-22
WO2010115000A2 (en) 2010-10-07
KR101874557B1 (ko) 2018-07-04
BRPI1012638A2 (pt) 2016-04-05
JP6336161B2 (ja) 2018-06-06
EP2414325A2 (en) 2012-02-08
BRPI1012638B8 (pt) 2021-05-25
CA2925137C (en) 2018-07-31
AP2011005864A0 (en) 2011-10-31
NZ708978A (en) 2017-01-27
CN107382997A (zh) 2017-11-24
JP6180561B2 (ja) 2017-08-16
ES2548252T3 (es) 2015-10-15
IL237642A0 (en) 2015-04-30
IL237643A (en) 2017-01-31
AU2010232559A1 (en) 2011-10-06
CA3008903A1 (en) 2010-10-07
HK1245785A1 (zh) 2018-08-31
EA201590979A1 (ru) 2016-02-29
TW201100412A (en) 2011-01-01
KR20170043672A (ko) 2017-04-21
NZ617773A (en) 2016-02-26
CA3083433A1 (en) 2010-10-07
UA108738C2 (uk) 2015-06-10
US20100256366A1 (en) 2010-10-07
MX2011010397A (es) 2011-10-24
AU2010232559A8 (en) 2011-11-10
BRPI1012638B1 (pt) 2021-04-20

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