AP2757A - Process for preparation of HIV protease inhibitors - Google Patents

Process for preparation of HIV protease inhibitors

Info

Publication number
AP2757A
AP2757A AP2008004641A AP2008004641A AP2757A AP 2757 A AP2757 A AP 2757A AP 2008004641 A AP2008004641 A AP 2008004641A AP 2008004641 A AP2008004641 A AP 2008004641A AP 2757 A AP2757 A AP 2757A
Authority
AP
ARIPO
Prior art keywords
preparation
protease inhibitors
hiv protease
hiv
inhibitors
Prior art date
Application number
AP2008004641A
Other languages
English (en)
Other versions
AP2008004641A0 (en
Inventor
Kenneth R Crawford
Eric D Dowdy
Arnold Gutierrez
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
Application filed by Gilead Sciences Inc filed Critical Gilead Sciences Inc
Publication of AP2008004641A0 publication Critical patent/AP2008004641A0/xx
Application granted granted Critical
Publication of AP2757A publication Critical patent/AP2757A/xx

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C327/00—Thiocarboxylic acids
    • C07C327/38—Amides of thiocarboxylic acids
    • C07C327/40—Amides of thiocarboxylic acids having carbon atoms of thiocarboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C327/42—Amides of thiocarboxylic acids having carbon atoms of thiocarboxamide groups bound to hydrogen atoms or to acyclic carbon atoms to hydrogen atoms or to carbon atoms of a saturated carbon skeleton
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/66—Phosphorus compounds
    • A61K31/665—Phosphorus compounds having oxygen as a ring hetero atom, e.g. fosfomycin
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • 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
    • C07C253/00—Preparation of carboxylic acid nitriles
    • C07C253/30—Preparation of carboxylic acid nitriles by reactions not involving the formation of cyano groups
    • 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
    • C07C303/36—Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides of amides of sulfonic acids
    • C07C303/38—Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides of amides of sulfonic acids by reaction of ammonia or amines with sulfonic acids, or with esters, anhydrides, or halides thereof
    • 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
    • C07C303/36—Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides of amides of sulfonic acids
    • C07C303/40—Preparation of esters or amides of sulfuric acids; Preparation of sulfonic acids or of their esters, halides, anhydrides or amides of amides of sulfonic acids by reactions not involving the formation of sulfonamide groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/22—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound oxygen atoms
    • C07C311/29—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound oxygen atoms having the sulfur atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C51/00—Preparation of carboxylic acids or their salts, halides or anhydrides
    • C07C51/41—Preparation of salts of carboxylic acids
    • C07C51/412—Preparation of salts of carboxylic acids by conversion of the acids, their salts, esters or anhydrides with the same carboxylic acid part
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/28—Phosphorus compounds with one or more P—C bonds
    • C07F9/38—Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)]
    • C07F9/40—Esters thereof
    • C07F9/4003—Esters thereof the acid moiety containing a substituent or a structure which is considered as characteristic
    • C07F9/4006—Esters of acyclic acids which can have further substituents on alkyl
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/28—Phosphorus compounds with one or more P—C bonds
    • C07F9/38—Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)]
    • C07F9/40—Esters thereof
    • C07F9/4071—Esters thereof the ester moiety containing a substituent or a structure which is considered as characteristic
    • C07F9/4075—Esters with hydroxyalkyl compounds
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/28—Phosphorus compounds with one or more P—C bonds
    • C07F9/38—Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)]
    • C07F9/40—Esters thereof
    • C07F9/4071—Esters thereof the ester moiety containing a substituent or a structure which is considered as characteristic
    • C07F9/4084—Esters with hydroxyaryl compounds

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Virology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Epidemiology (AREA)
  • Oil, Petroleum & Natural Gas (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Medicinal Preparation (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Plural Heterocyclic Compounds (AREA)
AP2008004641A 2006-03-29 2007-03-29 Process for preparation of HIV protease inhibitors AP2757A (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US78712606P 2006-03-29 2006-03-29
PCT/US2007/007564 WO2007126812A2 (en) 2006-03-29 2007-03-29 Process for preparation of hiv protease inhibitors

Publications (2)

Publication Number Publication Date
AP2008004641A0 AP2008004641A0 (en) 2008-10-31
AP2757A true AP2757A (en) 2013-09-30

Family

ID=38323963

Family Applications (2)

Application Number Title Priority Date Filing Date
AP2008004641A AP2757A (en) 2006-03-29 2007-03-29 Process for preparation of HIV protease inhibitors
AP2013006690A AP2013006690A0 (en) 2006-03-29 2007-03-29 Process for preparation of HIV protease inhibitors

Family Applications After (1)

Application Number Title Priority Date Filing Date
AP2013006690A AP2013006690A0 (en) 2006-03-29 2007-03-29 Process for preparation of HIV protease inhibitors

Country Status (25)

Country Link
US (4) US8173623B2 (zh)
EP (2) EP1999133B1 (zh)
JP (2) JP5430395B2 (zh)
KR (2) KR101395377B1 (zh)
CN (2) CN102516259B (zh)
AP (2) AP2757A (zh)
AU (1) AU2007245194B2 (zh)
BR (1) BRPI0710199A2 (zh)
CA (1) CA2647316C (zh)
DK (1) DK1999133T3 (zh)
EA (2) EA016140B1 (zh)
ES (2) ES2572001T3 (zh)
HK (2) HK1126756A1 (zh)
HR (2) HRP20080554B1 (zh)
IL (2) IL194122A (zh)
MX (1) MX2008012398A (zh)
NO (2) NO342102B1 (zh)
NZ (2) NZ571302A (zh)
PL (1) PL1999133T3 (zh)
PT (1) PT1999133E (zh)
SG (1) SG170794A1 (zh)
SI (1) SI1999133T1 (zh)
UA (1) UA97241C2 (zh)
WO (1) WO2007126812A2 (zh)
ZA (1) ZA200808046B (zh)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8921415B2 (en) 2009-01-29 2014-12-30 Mapi Pharma Ltd. Polymorphs of darunavir
AU2011210349A1 (en) 2010-01-28 2012-07-05 Mapi Pharma Limited Process for the preparation of darunavir and darunavir intermediates
CN102190638A (zh) * 2010-03-16 2011-09-21 中国科学院上海药物研究所 联芳基醇二胺类化合物、其药物组合物、制备方法及应用
CN102584748B (zh) * 2011-01-13 2015-02-11 浙江九洲药业股份有限公司 夫沙那韦中间体的制备方法
PT2702045T (pt) * 2011-04-26 2018-01-11 Mylan Laboratories Ltd Método inovador para a preparação de etravirina
KR20200090975A (ko) 2011-10-07 2020-07-29 길리애드 사이언시즈, 인코포레이티드 항-바이러스 뉴클레오티드 유사체의 제조 방법
EP2634180A1 (en) 2012-03-01 2013-09-04 Lonza Ltd. Enzymatic process for the preparation of butyrolactones
CN103664976B (zh) * 2013-12-12 2015-11-04 惠州市莱佛士制药技术有限公司 一种顺式六氢呋喃并[2,3-b]呋喃-3-醇的制备方法
EP3104712B1 (en) * 2014-02-12 2020-05-06 Firmenich Incorporated Improved process for the synthesis of substituted 1-benzyl-3-(1-(isoxazol-4-ylmethyl)-1h-pyrazol-4-yl)imidazolidine-2,4-diones
HUE056470T2 (hu) 2014-12-26 2022-02-28 Univ Emory Vírusellenes N4-Hidroxicitidin származékok
JP6435907B2 (ja) * 2015-02-16 2018-12-12 住友化学株式会社 ヘキサヒドロフロフラノール誘導体の製造方法
CN108610227B (zh) * 2016-12-10 2021-02-09 中国科学院大连化学物理研究所 一种制备双环芳香化合物的方法
GB2590198B (en) 2017-12-07 2022-02-23 Univ Emory N4-hydroxycytidine derivatives and anti-viral uses related thereto
SG11202107145SA (en) 2019-01-25 2021-08-30 Univ Brown Compositions and methods for treating, preventing or reversing age-associated inflammation and disorders

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1994026749A1 (en) * 1993-05-14 1994-11-24 Merck & Co., Inc. Hiv protease inhibitors
WO2002067239A2 (en) * 2000-10-24 2002-08-29 Glaxo Group Limited Process for preparing intermediates of hiv protease inhibitors
WO2005042772A1 (en) * 2003-10-24 2005-05-12 Gilead Sciences, Inc. Methods and compositions for identifying therapeutic compounds

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU1369001A (en) * 1995-12-13 2001-03-22 Abbott Laboratories Retroviral protease inhibiting compounds
DE60039533D1 (de) 1999-12-23 2008-08-28 Ampac Fine Chemicals Llc Verbessertes verfahren zur herstellung von 2s,3s-n-isobutyl-n-(2-hydroxy-3-amino-4-phenylbutyl)-p-nitrobenzenesulfonylamid hydrochlorid und anderen derivaten von 2-hydroxy-1,3-diamin
WO2003009690A2 (en) 2001-07-20 2003-02-06 Koninklijke Philips Electronics N.V. Oscillating circuit, converter with such oscillating circuit, and preconditioner with such converter
US20050239054A1 (en) * 2002-04-26 2005-10-27 Arimilli Murty N Method and compositions for identifying anti-HIV therapeutic compounds
AU2003231766A1 (en) 2002-04-26 2003-11-10 Gilead Sciences, Inc. Non nucleoside reverse transcriptase inhibitors

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1994026749A1 (en) * 1993-05-14 1994-11-24 Merck & Co., Inc. Hiv protease inhibitors
WO2002067239A2 (en) * 2000-10-24 2002-08-29 Glaxo Group Limited Process for preparing intermediates of hiv protease inhibitors
WO2005042772A1 (en) * 2003-10-24 2005-05-12 Gilead Sciences, Inc. Methods and compositions for identifying therapeutic compounds

Also Published As

Publication number Publication date
AP2013006690A0 (en) 2013-01-31
MX2008012398A (es) 2008-12-17
HRP20080554A2 (en) 2009-02-28
NO20084547L (no) 2008-12-22
CA2647316C (en) 2013-05-28
WO2007126812A3 (en) 2007-12-21
CA2647316A1 (en) 2007-11-08
NO342965B1 (no) 2018-09-10
PT1999133E (pt) 2013-10-16
US20110065631A1 (en) 2011-03-17
EP1999133A2 (en) 2008-12-10
EP1999133B1 (en) 2013-08-21
US8431745B2 (en) 2013-04-30
UA97241C2 (uk) 2012-01-25
KR101395377B1 (ko) 2014-05-14
KR101429300B1 (ko) 2014-08-11
AU2007245194A1 (en) 2007-11-08
HRP20140626A2 (hr) 2014-11-07
SI1999133T1 (sl) 2013-10-30
DK1999133T3 (da) 2013-11-25
HK1180311A1 (zh) 2013-10-18
HRP20080554B1 (hr) 2014-11-21
EA020088B1 (ru) 2014-08-29
EA201100994A1 (ru) 2012-03-30
ES2572001T3 (es) 2016-05-27
ES2430557T3 (es) 2013-11-21
CN102516259B (zh) 2014-12-10
NO342102B1 (no) 2018-03-26
CN102516259A (zh) 2012-06-27
CN101448838B (zh) 2012-07-04
US20120258935A1 (en) 2012-10-11
SG170794A1 (en) 2011-05-30
EP2570416A1 (en) 2013-03-20
KR20080108322A (ko) 2008-12-12
KR20140021047A (ko) 2014-02-19
WO2007126812A2 (en) 2007-11-08
JP2013082717A (ja) 2013-05-09
US20080004242A1 (en) 2008-01-03
IL225167A (en) 2016-03-31
US20130172295A1 (en) 2013-07-04
EA016140B1 (ru) 2012-02-28
ZA200808046B (en) 2009-06-24
US8173623B2 (en) 2012-05-08
NZ571302A (en) 2011-11-25
PL1999133T3 (pl) 2014-01-31
AU2007245194B2 (en) 2013-03-14
HK1126756A1 (en) 2009-09-11
JP5430395B2 (ja) 2014-02-26
BRPI0710199A2 (pt) 2012-03-06
NO20180086A1 (no) 2008-12-22
AP2008004641A0 (en) 2008-10-31
NZ596074A (en) 2013-03-28
IL194122A (en) 2016-08-31
JP2009531441A (ja) 2009-09-03
EP2570416B1 (en) 2016-03-16
EA200802074A1 (ru) 2009-02-27
CN101448838A (zh) 2009-06-03

Similar Documents

Publication Publication Date Title
AP2757A (en) Process for preparation of HIV protease inhibitors
HK1223370A1 (zh) 製備整合酶抑制劑的方法和中間體
EP2224920A4 (en) PROCESS FOR THE PREPARATION OF MACROCYCLIC OXIMYL HEPATITIS C PROTEASE INHIBITORS
EP2051707A4 (en) Plasma kallikrein INHIBITORS
HK1166308A1 (zh) 激活酶抑制劑
HK1132754A1 (en) 4-amino-4-oxobutanoyl peptides as inhibitors of viral replication
IL200611A0 (en) Inhibitors of serine proteases
ZA200900551B (en) Process for the preparation of 2-substituted-5-(1-alkylthio)alkylpyridines
EP2099789A4 (en) INHIBITORS OF HIV REPLICATION
HK1127345A1 (en) Azapeptide derivatives as hiv protease inhibitors
EP2139883A4 (en) INHIBITORS OF HIV-1 PROTEASE
EP2304043A4 (en) HIV PROTEASE INHIBITORS AND METHOD FOR THEIR USE
EP2088136A4 (en) PROCESS FOR PRODUCING HYDROXYADAMANTANE-AMINE
EP2244571A4 (en) SMALL INHIBITORY MOLECULES OF HIV PROTEASES
EP2134336A4 (en) HIV PROTEASE INHIBITORS DERIVED FROM BENZOFURAN
EP2096103A4 (en) PROCESS FOR THE PRODUCTION OF BETAINE
EP2057151A4 (en) PROCESS FOR PURIFYING APREPITANT
EP2291077A4 (en) METHOD OF MANUFACTURING RHO-KINASE INHIBITOR COMPOUNDS
EP2144871A4 (en) AMIDATION METHOD FOR THE PREPARATION OF CATHEPSIN K INHIBITORS
GB0621669D0 (en) Process for preparation of l-gluconic acid
ZA201201740B (en) Process for the preparation of cathepsin s inhibitors
EP1984525A4 (en) METHODS FOR DETERMINING HIV RESISTANCE TO TREATMENTS WITH PROTEASE INHIBITOR
EP1985611A4 (en) PROCESS FOR THE PREPARATION OF O-METHYL-N-NITROISOHARNSTOFF
IL198836A0 (en) Processes for preparation of 9-haloacetamidomidominocyclines
IL193470A0 (en) Process for preparing of 2-alkyl-3-aryl-prop-2- ene-1-ols