AU777824B2 - Gamma-hydroxy-2-(fluoroalkylaminocarbonyl)-1- piperazinepentanamides as HIV protease inhibitors - Google Patents

Gamma-hydroxy-2-(fluoroalkylaminocarbonyl)-1- piperazinepentanamides as HIV protease inhibitors Download PDF

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Publication number
AU777824B2
AU777824B2 AU17909/01A AU1790901A AU777824B2 AU 777824 B2 AU777824 B2 AU 777824B2 AU 17909/01 A AU17909/01 A AU 17909/01A AU 1790901 A AU1790901 A AU 1790901A AU 777824 B2 AU777824 B2 AU 777824B2
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AU
Australia
Prior art keywords
hydroxy
dihydro
alkyl
piperazinepentanamide
benzopyran
Prior art date
Legal status (The legal status 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 status listed.)
Ceased
Application number
AU17909/01A
Other languages
English (en)
Other versions
AU1790901A (en
Inventor
Joseph D. Armstrong Iii
David Askin
Kevin T Chapman
Yuan Cheng
Joseph Leslie Duffy
Fred J. Fleitz
R. Scott Hoerrner
Tracy Huening
Nancy J Kevin
Brian Anthony Kirk
Zhijian Lu
Daniel E. Petrillo
Robert Purick
Subharekha Raghavan
Thomas A Rano
James R. Tata
Richard J. Varsolona
Fengqi Zhang
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Merck Sharp and Dohme LLC
Original Assignee
Merck and Co 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 Merck and Co Inc filed Critical Merck and Co Inc
Publication of AU1790901A publication Critical patent/AU1790901A/en
Application granted granted Critical
Publication of AU777824B2 publication Critical patent/AU777824B2/en
Assigned to MERCK SHARP & DOHME CORP. reassignment MERCK SHARP & DOHME CORP. Request to Amend Deed and Register Assignors: MERCK & CO., INC.
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • 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
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • 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
    • C07D417/14—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Oncology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Immunology (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Molecular Biology (AREA)
  • AIDS & HIV (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Hydrogenated Pyridines (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
AU17909/01A 1999-11-24 2000-11-21 Gamma-hydroxy-2-(fluoroalkylaminocarbonyl)-1- piperazinepentanamides as HIV protease inhibitors Ceased AU777824B2 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US16747899P 1999-11-24 1999-11-24
US60/167478 1999-11-24
US17705300P 2000-01-20 2000-01-20
US60/177053 2000-01-20
PCT/US2000/032089 WO2001038332A1 (en) 1999-11-24 2000-11-21 Gamma-hydroxy-2-(fluoroalkylaminocarbonyl)-1-piperazinepentanamides as hiv protease inhibitors

Publications (2)

Publication Number Publication Date
AU1790901A AU1790901A (en) 2001-06-04
AU777824B2 true AU777824B2 (en) 2004-11-04

Family

ID=26863215

Family Applications (1)

Application Number Title Priority Date Filing Date
AU17909/01A Ceased AU777824B2 (en) 1999-11-24 2000-11-21 Gamma-hydroxy-2-(fluoroalkylaminocarbonyl)-1- piperazinepentanamides as HIV protease inhibitors

Country Status (11)

Country Link
US (1) US6642237B1 (cg-RX-API-DMAC7.html)
EP (1) EP1242426B1 (cg-RX-API-DMAC7.html)
JP (1) JP2003514910A (cg-RX-API-DMAC7.html)
AT (1) ATE377011T1 (cg-RX-API-DMAC7.html)
AU (1) AU777824B2 (cg-RX-API-DMAC7.html)
CA (1) CA2391643C (cg-RX-API-DMAC7.html)
CO (1) CO5261497A1 (cg-RX-API-DMAC7.html)
DE (1) DE60036961T2 (cg-RX-API-DMAC7.html)
ES (1) ES2295068T3 (cg-RX-API-DMAC7.html)
PE (1) PE20011025A1 (cg-RX-API-DMAC7.html)
WO (1) WO2001038332A1 (cg-RX-API-DMAC7.html)

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GB9815567D0 (en) * 1998-07-18 1998-09-16 Glaxo Group Ltd Antiviral compound
WO2001055326A2 (en) * 2000-01-31 2001-08-02 Human Genome Sciences, Inc. Nucleic acids, proteins, and antibodies
US7122376B2 (en) * 2001-11-01 2006-10-17 Facet Analytical Services And Technology, Llc Calibration standards, methods, and kits for water determination
US7049146B2 (en) 2000-11-14 2006-05-23 Facet Analytical Services And Technology, Llc Calibration standards, methods, and kits for water determination
AU2002305720A1 (en) * 2001-05-30 2002-12-09 Huening, Tracy, T. Piperazine pentanamide hiv protease inhibitors
US6649761B2 (en) 2001-05-30 2003-11-18 Merck & Co., Inc. Process for preparing piperazinepentaneamide HIV protease inhibitors
US6835860B2 (en) 2002-02-01 2004-12-28 Merck & Co., Inc. Iodohydroxylation of olefins
US20040067216A1 (en) * 2002-02-22 2004-04-08 Karki Shyam B. Hiv protease inhibitors supported on cation exchange resins for oral administration
GB0218876D0 (en) * 2002-08-13 2002-09-25 Merck Sharp & Dohme Therapeutic agents
WO2004027361A1 (en) * 2002-09-17 2004-04-01 University Of Virginia Patent Foundation Remote temperature sensing of small volume and related apparatus thereof
US7199240B2 (en) 2002-12-11 2007-04-03 Merck & Co., Inc. Reductive alkylation of saturated cyclic amines
ES2571779T3 (es) * 2002-12-13 2016-05-26 Ym Biosciences Australia Pty Inhibidores de cinasa a base de nicotinamida
TW574132B (en) * 2003-04-14 2004-02-01 Univ Nat Cheng Kung Integrated microfluidic electro-spray chip system and the analysis method thereof
US7161015B1 (en) * 2005-09-08 2007-01-09 The United States Of America As Represented By The Secretary Of The Navy Method of making 2-furylalkylketones
JP2006316049A (ja) * 2006-04-11 2006-11-24 Tanabe Seiyaku Co Ltd ２，２−ジアルコキシエチルアミン化合物およびその製造方法
CA2762582A1 (en) 2009-05-27 2010-12-02 Merck Sharp & Dohme Corp. Hiv protease inhibitors
JP6122639B2 (ja) 2009-10-26 2017-04-26 メルク・シャープ・エンド・ドーム・コーポレイション インテグラーゼ阻害剤を含有する固形医薬組成物
US8987272B2 (en) 2010-04-01 2015-03-24 Critical Outcome Technologies Inc. Compounds and method for treatment of HIV
US9173396B2 (en) 2010-10-22 2015-11-03 Bayer Intellectual Property Gmbh Heterocyclic compounds as pesticides
EP2632895B1 (en) 2010-10-28 2018-10-03 Merck Canada Inc. Hiv protease inhibitors
GB201100181D0 (en) 2011-01-06 2011-02-23 Eisai Ltd Fused aminodihydrothiazine derivatives
GB201101139D0 (en) 2011-01-21 2011-03-09 Eisai Ltd Fused aminodihydrothiazine derivatives
GB201101140D0 (en) 2011-01-21 2011-03-09 Eisai Ltd Fused aminodihydrothiazine derivatives
CN103929964A (zh) 2011-09-23 2014-07-16 拜耳知识产权有限责任公司 4-取代的1-苯基吡唑-3-甲酸衍生物作为对抗非生物植物胁迫的活性物质的用途
US9133157B2 (en) 2011-10-26 2015-09-15 Merck Canada Inc. HIV protease inhibitors
RU2015113091A (ru) 2012-09-11 2016-11-10 Мерк Шарп И Доум Корп. Ингибиторы протеазы вич
WO2015013835A1 (en) 2013-07-31 2015-02-05 Merck Sharp & Dohme Corp. Piperazine derivatives as hiv protease inhibitors
US10376583B2 (en) 2013-09-30 2019-08-13 Beth Israel Deaconess Medical Center, Inc. Human immunodeficiency virus therapies utilizing N332-glycan-dependent antibodies and a reservoir activator
US9737545B2 (en) 2013-12-19 2017-08-22 Merck Sharp & Dohme Corp. HIV protease inhibitors
WO2015095276A1 (en) 2013-12-19 2015-06-25 Merck Sharp & Dohme Corp. Hiv protease inhibitors
WO2015134366A1 (en) 2014-03-06 2015-09-11 Merck Sharp & Dohme Corp. Hiv protease inhibitors
EP3116862B1 (en) 2014-03-10 2019-04-17 Merck Sharp & Dohme Corp. Piperazine derivatives as hiv protease inhibitors
EP2944955A1 (en) * 2014-05-13 2015-11-18 Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V. Benchmark for LC-MS systems
WO2016007532A1 (en) * 2014-07-08 2016-01-14 Dow Agrosciences Llc Process for the preparation of 3-hydroxypicolinic acids
CN104311479B (zh) * 2014-09-15 2016-06-15 西华大学 3,5-二碘-4-羟基吡啶的合成
TW201730188A (zh) * 2015-11-30 2017-09-01 阿斯特捷利康公司 1,3,4-噻二唑化合物及其在治療癌症中之用途
TW201822637A (zh) 2016-11-07 2018-07-01 德商拜耳廠股份有限公司 用於控制動物害蟲的經取代磺醯胺類
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WO1994026717A1 (en) * 1993-05-07 1994-11-24 Merck & Co., Inc. Hiv protease inhibitors useful for the treatment of aids
US5455351A (en) * 1993-12-13 1995-10-03 Abbott Laboratories Retroviral protease inhibiting piperazine compounds
WO1995016688A1 (en) * 1993-12-15 1995-06-22 Merck & Co., Inc. Hiv protease inhibitors

Also Published As

Publication number Publication date
CA2391643A1 (en) 2001-05-31
ATE377011T1 (de) 2007-11-15
CA2391643C (en) 2010-01-12
US6642237B1 (en) 2003-11-04
JP2003514910A (ja) 2003-04-22
EP1242426A1 (en) 2002-09-25
EP1242426B1 (en) 2007-10-31
WO2001038332A1 (en) 2001-05-31
PE20011025A1 (es) 2001-10-12
CO5261497A1 (es) 2003-03-31
DE60036961D1 (de) 2007-12-13
ES2295068T3 (es) 2008-04-16
AU1790901A (en) 2001-06-04
DE60036961T2 (de) 2008-08-28

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