DE60036961D1 - Gamma-hydroxy-2-(fluoralkylaminocarbonyl)-1-piperazinpentanamide als hiv-proteasehemmer - Google Patents

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

Info

Publication number
DE60036961D1
DE60036961D1 DE60036961T DE60036961T DE60036961D1 DE 60036961 D1 DE60036961 D1 DE 60036961D1 DE 60036961 T DE60036961 T DE 60036961T DE 60036961 T DE60036961 T DE 60036961T DE 60036961 D1 DE60036961 D1 DE 60036961D1
Authority
DE
Germany
Prior art keywords
hiv
compounds
gamma
hydroxy
hiv protease
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
Other languages
English (en)
Other versions
DE60036961T2 (de
Inventor
James R Tata
Kevin T Chapman
Joseph Leslie Duffy
Nancy J Kevin
Yuan Cheng
Thomas A Rano
Fengqi Zhang
Tracy Huening
Brian Anthony Kirk
Zhijian Lu
Subharekha Raghavan
Fred J Fleitz
Daniel E Petrillo
Joseph D Armstrong
Richard J Varsolona
David Askin
R Scott Hoerrner
Robert Purick
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 DE60036961D1 publication Critical patent/DE60036961D1/de
Application granted granted Critical
Publication of DE60036961T2 publication Critical patent/DE60036961T2/de
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

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)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Engineering & Computer Science (AREA)
  • Virology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Hydrogenated Pyridines (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 true DE60036961D1 (de) 2007-12-13
DE60036961T2 DE60036961T2 (de) 2008-08-28

Family

ID=26863215

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 (de)
EP (1) EP1242426B1 (de)
JP (1) JP2003514910A (de)
AT (1) ATE377011T1 (de)
AU (1) AU777824B2 (de)
CA (1) CA2391643C (de)
CO (1) CO5261497A1 (de)
DE (1) DE60036961T2 (de)
ES (1) ES2295068T3 (de)
PE (1) PE20011025A1 (de)
WO (1) WO2001038332A1 (de)

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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
US7049146B2 (en) 2000-11-14 2006-05-23 Facet Analytical Services And Technology, Llc Calibration standards, methods, and kits for water determination
US7122376B2 (en) * 2001-11-01 2006-10-17 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
US8497383B2 (en) 2009-05-27 2013-07-30 Merck Sharp & Dohme Corp. HIV protease inhibitors
CA2777937C (en) 2009-10-26 2017-08-29 Merck Sharp & Dohme Corp. 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
CN103270029B (zh) 2010-10-22 2016-01-20 拜耳知识产权有限责任公司 作为农药的杂环化合物
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
WO2013059928A1 (en) 2011-10-26 2013-05-02 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)
US9834526B2 (en) 2013-12-19 2017-12-05 Merck Sharp & Dohme Corp. HIV protease inhibitors
US9737545B2 (en) 2013-12-19 2017-08-22 Merck Sharp & Dohme Corp. HIV protease inhibitors
EP3113780B1 (de) 2014-03-06 2019-08-14 Merck Sharp & Dohme Corp. Hiv-proteasehemmer
EP3116862B1 (de) 2014-03-10 2019-04-17 Merck Sharp & Dohme Corp. Piperazinderivate als hiv-proteasehemmer
EP2944955A1 (de) * 2014-05-13 2015-11-18 Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V. Bezugspunkt für LC-MS-Systeme
ES2726927T3 (es) * 2014-07-08 2019-10-10 Dow Agrosciences Llc Proceso para la preparación de ácidos 3-hidroxipicolínicos
CN104311479B (zh) * 2014-09-15 2016-06-15 西华大学 3,5-二碘-4-羟基吡啶的合成
US9938265B2 (en) * 2015-11-30 2018-04-10 Astrazeneca Ab 1,3,4-thiadiazole compounds and their use in treating cancer
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
WO2019175464A1 (en) 2018-03-14 2019-09-19 Orion Corporation Compounds useful as inhibitors of sodium-calcium exchanger (ncx)
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US20210403435A1 (en) 2018-11-12 2021-12-30 Syngenta Crop Protection Ag Herbicidal compounds
CN112824417A (zh) * 2019-11-21 2021-05-21 上海天慈国际药业有限公司 一种劳拉替尼的制备方法

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Also Published As

Publication number Publication date
CO5261497A1 (es) 2003-03-31
ATE377011T1 (de) 2007-11-15
EP1242426A1 (de) 2002-09-25
CA2391643C (en) 2010-01-12
AU777824B2 (en) 2004-11-04
DE60036961T2 (de) 2008-08-28
EP1242426B1 (de) 2007-10-31
AU1790901A (en) 2001-06-04
WO2001038332A1 (en) 2001-05-31
CA2391643A1 (en) 2001-05-31
ES2295068T3 (es) 2008-04-16
PE20011025A1 (es) 2001-10-12
US6642237B1 (en) 2003-11-04
JP2003514910A (ja) 2003-04-22

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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