DE60036961T2 - Gamma-hydroxy-2-(fluoralkylaminocarbonyl)-1-piperazinpentanamide als hiv-proteasehemmer - Google Patents

Gamma-hydroxy-2-(fluoralkylaminocarbonyl)-1-piperazinpentanamide als hiv-proteasehemmer Download PDF

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Publication number
DE60036961T2
DE60036961T2 DE60036961T DE60036961T DE60036961T2 DE 60036961 T2 DE60036961 T2 DE 60036961T2 DE 60036961 T DE60036961 T DE 60036961T DE 60036961 T DE60036961 T DE 60036961T DE 60036961 T2 DE60036961 T2 DE 60036961T2
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Germany
Prior art keywords
hydroxy
alkyl
dihydro
amino
carbonyl
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.)
Expired - Lifetime
Application number
DE60036961T
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German (de)
English (en)
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DE60036961D1 (de
Inventor
James R. Rahway TATA
Kevin T. Rahway CHAPMAN
Joseph Leslie Rahway DUFFY
Nancy J. Rahway KEVIN
Yuan Rahway CHENG
Thomas A. Rahway RANO
Fengqi Rahway ZHANG
Tracy Rahway HUENING
Brian Anthony Rahway KIRK
Zhijian Rahway LU
Subharekha Rahway RAGHAVAN
Fred J. Rahway FLEITZ
Daniel E. Rahway PETRILLO
Joseph D. Rahway ARMSTRONG
Richard J. Rahway VARSOLONA
David Rahway ASKIN
R. Scott Rahway HOERRNER
Robert Rahway PURICK
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Merck Sharp & Dohme LLC
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Merck and Co Inc
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Publication of DE60036961D1 publication Critical patent/DE60036961D1/de
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Expired - Lifetime legal-status Critical Current

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    • 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

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  • 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)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Hydrogenated Pyridines (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)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
DE60036961T 1999-11-24 2000-11-21 Gamma-hydroxy-2-(fluoralkylaminocarbonyl)-1-piperazinpentanamide als hiv-proteasehemmer Expired - Lifetime DE60036961T2 (de)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US16747899P 1999-11-24 1999-11-24
US167478P 1999-11-24
US17705300P 2000-01-20 2000-01-20
US177053P 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
DE60036961D1 DE60036961D1 (de) 2007-12-13
DE60036961T2 true DE60036961T2 (de) 2008-08-28

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
DE60036961T Expired - Lifetime DE60036961T2 (de) 1999-11-24 2000-11-21 Gamma-hydroxy-2-(fluoralkylaminocarbonyl)-1-piperazinpentanamide als hiv-proteasehemmer

Country Status (11)

Country Link
US (1) US6642237B1 (enExample)
EP (1) EP1242426B1 (enExample)
JP (1) JP2003514910A (enExample)
AT (1) ATE377011T1 (enExample)
AU (1) AU777824B2 (enExample)
CA (1) CA2391643C (enExample)
CO (1) CO5261497A1 (enExample)
DE (1) DE60036961T2 (enExample)
ES (1) ES2295068T3 (enExample)
PE (1) PE20011025A1 (enExample)
WO (1) WO2001038332A1 (enExample)

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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
US6649761B2 (en) 2001-05-30 2003-11-18 Merck & Co., Inc. Process for preparing piperazinepentaneamide HIV protease inhibitors
WO2002096359A2 (en) * 2001-05-30 2002-12-05 Merck & Co., Inc. Piperazine pentanamide 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
AU2003270727A1 (en) * 2002-09-17 2004-04-08 Luna Innovations, Inc. 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
JP4896518B2 (ja) * 2002-12-13 2012-03-14 ワイエム・バイオサイエンシズ・オーストラリア・ピーティーワイ・リミテッド ニコチンアミド系キナーゼ阻害薬
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
AU2010313571B2 (en) 2009-10-26 2014-07-31 Merck Sharp & Dohme Llc Solid pharmaceutical compositions containing an integrase inhibitor
WO2011120153A1 (en) 2010-04-01 2011-10-06 Critical Outcome Technologies Inc. Compounds and method for treatment of hiv
BR112013009823A2 (pt) 2010-10-22 2016-07-05 Bayer Ip Gmbh novos compostos heterocíclicos como pesticidas
US9079834B2 (en) 2010-10-28 2015-07-14 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
EP2757886A1 (de) 2011-09-23 2014-07-30 Bayer Intellectual Property GmbH Verwendung 4-substituierter 1-phenyl-pyrazol-3-carbonsäurederivate als wirkstoffe gegen abiotischen pflanzenstress
US9133157B2 (en) 2011-10-26 2015-09-15 Merck Canada Inc. HIV protease inhibitors
JP2015527403A (ja) 2012-09-11 2015-09-17 メルク・シャープ・アンド・ドーム・コーポレーションＭｅｒｃｋ Ｓｈａｒｐ ＆ Ｄｏｈｍｅ Ｃｏｒｐ． Ｈｉｖプロテアーゼ阻害剤
WO2015013835A1 (en) 2013-07-31 2015-02-05 Merck Sharp & Dohme Corp. Piperazine derivatives as hiv protease inhibitors
WO2015048770A2 (en) 2013-09-30 2015-04-02 Beth Israel Deaconess Medical Center, Inc. Antibody therapies for human immunodeficiency virus (hiv)
WO2015095265A1 (en) 2013-12-19 2015-06-25 Merck Sharp & Dohme Corp. Hiv protease inhibitors
WO2015095276A1 (en) 2013-12-19 2015-06-25 Merck Sharp & Dohme Corp. Hiv protease inhibitors
US9994587B2 (en) 2014-03-06 2018-06-12 Merck Sharp & Dohme Corp. HIV protease inhibitors
WO2015138220A1 (en) 2014-03-10 2015-09-17 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
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Also Published As

Publication number Publication date
DE60036961D1 (de) 2007-12-13
EP1242426B1 (en) 2007-10-31
ATE377011T1 (de) 2007-11-15
AU1790901A (en) 2001-06-04
CO5261497A1 (es) 2003-03-31
CA2391643C (en) 2010-01-12
PE20011025A1 (es) 2001-10-12
ES2295068T3 (es) 2008-04-16
AU777824B2 (en) 2004-11-04
WO2001038332A1 (en) 2001-05-31
CA2391643A1 (en) 2001-05-31
JP2003514910A (ja) 2003-04-22
EP1242426A1 (en) 2002-09-25
US6642237B1 (en) 2003-11-04

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Legal Events

Date Code Title Description
8364 No opposition during term of opposition
8327 Change in the person/name/address of the patent owner

Owner name: MERCK SHARP & DOHME CORP., RAHWAY, N.J., US

8328 Change in the person/name/address of the agent

Representative=s name: MARKS & CLERK (LUXEMBOURG) LLP, LUXEMBOURG, LU