[go: up one dir, main page]

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

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/06Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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
    • C07D405/06Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic 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
    • C07D491/02Heterocyclic 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
    • C07D491/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic 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
    • C07D495/04Ortho-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)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Virology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Molecular Biology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • AIDS & HIV (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)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (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)

Families Citing this family (42)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
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
US20040131504A1 (en) * 2002-09-17 2004-07-08 Landers James P. 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
WO2010138338A1 (en) 2009-05-27 2010-12-02 Merck Sharp & Dohme Corp. Hiv protease inhibitors
EP2493312B1 (de) 2009-10-26 2021-10-20 Merck Sharp & Dohme Corp. Feste pharmazeutische zusammensetzungen mit einem integrasehemmer
US8987272B2 (en) 2010-04-01 2015-03-24 Critical Outcome Technologies Inc. Compounds and method for treatment of HIV
WO2012052412A1 (de) 2010-10-22 2012-04-26 Bayer Cropscience Ag Neue heterocylische verbindungen als schädlingsbekämpfungsmittel
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
GB201101140D0 (en) 2011-01-21 2011-03-09 Eisai Ltd Fused aminodihydrothiazine derivatives
GB201101139D0 (en) 2011-01-21 2011-03-09 Eisai Ltd Fused aminodihydrothiazine derivatives
AR087971A1 (es) 2011-09-23 2014-04-30 Bayer Ip Gmbh Uso de derivados del acido 1-fenil-pirazol-3-carboxilico 4-sustituidos como principios activos contra estres abiotico de plantas
US9133157B2 (en) 2011-10-26 2015-09-15 Merck Canada Inc. HIV protease inhibitors
AU2013315833A1 (en) 2012-09-11 2015-03-05 Merck Canada Inc. HIV protease inhibitors
WO2015013835A1 (en) 2013-07-31 2015-02-05 Merck Sharp & Dohme Corp. Piperazine derivatives as hiv protease inhibitors
EP3052132B1 (de) 2013-09-30 2020-07-29 Beth Israel Deaconess Medical Center, Inc. Antikörpertherapien für den humanen immundefizienzvirus (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
US9994587B2 (en) 2014-03-06 2018-06-12 Merck Sharp & Dohme Corp. HIV protease inhibitors
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
BR112016030604B8 (pt) * 2014-07-08 2022-08-23 Dow Agrosciences Llc Processo para preparação 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)
AR114422A1 (es) 2018-03-30 2020-09-02 Syngenta Participations Ag Compuestos herbicidas
AU2019377986A1 (en) 2018-11-12 2021-05-27 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
US12083099B2 (en) 2020-10-28 2024-09-10 Accencio LLC Methods of treating symptoms of coronavirus infection with viral protease inhibitors

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB8927913D0 (en) 1989-12-11 1990-02-14 Hoffmann La Roche Amino acid derivatives
ATE163926T1 (de) 1991-11-08 1998-03-15 Merck & Co Inc Hiv-protease-inhibitoren verwendbar in der aids- behandlung
US5413999A (en) 1991-11-08 1995-05-09 Merck & Co., Inc. HIV protease inhibitors useful for the treatment of AIDS
US5484926A (en) 1993-10-07 1996-01-16 Agouron Pharmaceuticals, Inc. HIV protease inhibitors
IL110255A (en) 1993-07-16 1998-12-06 Merck & Co Inc Formation and resolution of 2-tert-butylcarboxamido-piperazine
US5455351A (en) * 1993-12-13 1995-10-03 Abbott Laboratories Retroviral protease inhibiting piperazine compounds
PL314984A1 (en) * 1993-12-15 1996-09-30 Merck & Co Inc Hiv protease inhibitors
IL111991A (en) 1994-01-28 2000-07-26 Abbott Lab Liquid pharmaceutical composition of HIV protease inhibitors in organic solvent
TW438799B (en) 1997-05-29 2001-06-07 Merck & Co Inc HIV protease inhibitor
AU2012199A (en) * 1997-12-24 1999-07-19 Vertex Pharmaceuticals Incorporated Prodrugs of aspartyl protease inhibitors

Also Published As

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

Similar Documents

Publication Publication Date Title
DE60036961D1 (de) Gamma-hydroxy-2-(fluoralkylaminocarbonyl)-1-piperazinpentanamide als hiv-proteasehemmer
DE69228106D1 (de) HIV-Protease-Inhibitoren
EA200300449A1 (ru) Аза- и полиаза-нафталинилкарбоксамиды, полезные в качестве ингибиторов вич-интегразы
DE60128936D1 (en) Aza- und polyaza-naphthalenylcarbonsäureamide als hiv-integrase-hemmer
DE60124577D1 (en) Aza- und polyaza-naphthalenylcarbonsäureamide als hiv-integrase-hemmer
LU91428I2 (fr) ISENTRESS- raltégravir
MY109834A (en) Benzoxazinones as inhibitors of hiv reverse transcriptase
ATE252081T1 (de) Neue hiv-protease-inhibitoren
ATE215952T1 (de) Hiv-proteaseinhibitoren
PT617968E (pt) Inibidores de protease de hiv em combinacao farmaceutica para tratamento de sida
WO1996000068A3 (en) Combination therapy for hiv infection
DK0774969T3 (da) HIV-proteaseinhibitor kombination
WO2002096359A3 (en) Piperazine pentanamide hiv protease inhibitors
FI970565A0 (fi) HIV-proteaasia inhiboiva yhdistelmä

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