ATE377011T1 - Gamma-hydroxy-2-(fluoralkylaminocarbonyl)-1- piperazinpentanamide als hiv-proteasehemmer - Google Patents

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

Info

Publication number
ATE377011T1
ATE377011T1 AT00980679T AT00980679T ATE377011T1 AT E377011 T1 ATE377011 T1 AT E377011T1 AT 00980679 T AT00980679 T AT 00980679T AT 00980679 T AT00980679 T AT 00980679T AT E377011 T1 ATE377011 T1 AT E377011T1
Authority
AT
Austria
Prior art keywords
hiv
compounds
gamma
hydroxy
hiv protease
Prior art date
Application number
AT00980679T
Other languages
English (en)
Inventor
James Tata
Kevin Chapman
Joseph Duffy
Nancy Kevin
Yuan Cheng
Thomas Rano
Fengqi Zhang
Tracy Huening
Brian Kirk
Zhijian Lu
Subharekha Raghavan
Fred Fleitz
Daniel Petrillo
Joseph Armstrong
Richard Varsolona
David Askin
R Hoerrner
Robert Purick
Original Assignee
Merck & 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 & Co Inc filed Critical Merck & Co Inc
Application granted granted Critical
Publication of ATE377011T1 publication Critical patent/ATE377011T1/de

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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
AT00980679T 1999-11-24 2000-11-21 Gamma-hydroxy-2-(fluoralkylaminocarbonyl)-1- piperazinpentanamide als hiv-proteasehemmer ATE377011T1 (de)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US16747899P 1999-11-24 1999-11-24
US17705300P 2000-01-20 2000-01-20

Publications (1)

Publication Number Publication Date
ATE377011T1 true ATE377011T1 (de) 2007-11-15

Family

ID=26863215

Family Applications (1)

Application Number Title Priority Date Filing Date
AT00980679T ATE377011T1 (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 (41)

* 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
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
WO2010138338A1 (en) 2009-05-27 2010-12-02 Merck Sharp & Dohme Corp. Hiv protease inhibitors
KR101835893B1 (ko) 2009-10-26 2018-04-19 머크 샤프 앤드 돔 코포레이션 인테그라제 억제제를 함유하는 고형 제약 조성물
US8987272B2 (en) 2010-04-01 2015-03-24 Critical Outcome Technologies Inc. Compounds and method for treatment of HIV
JP5953308B2 (ja) 2010-10-22 2016-07-20 バイエル・インテレクチュアル・プロパティ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツングBayer Intellectual Property GmbH 殺害虫剤としての新規ヘテロ環式化合物
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
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
US9226505B2 (en) 2011-09-23 2016-01-05 Bayer Intellectual Property Gmbh 4-substituted 1-phenylpyrazole-3-carboxylic acid derivatives as agents against abiotic plant stress
EP2771332B1 (de) 2011-10-26 2016-06-29 Merck Canada Inc. Thiophen- und Thiazol-Sulfonamid-Derivate als HIV Protease Inhibitoren zur Behandlung von AIDS
WO2014043019A1 (en) 2012-09-11 2014-03-20 Merck Sharp & Dohme Corp. 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)
WO2015095265A1 (en) 2013-12-19 2015-06-25 Merck Sharp & Dohme Corp. Hiv protease inhibitors
EP3082822B1 (de) 2013-12-19 2020-01-15 Merck Sharp & Dohme Corp. Hiv-proteasehemmer
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
EP3166928B1 (de) * 2014-07-08 2019-04-03 Dow AgroSciences LLC Verfahren zur herstellung von 3-hydroxypicolinsäure
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
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
BR112021009046A2 (pt) 2018-11-12 2021-08-10 Syngenta Crop Protection Ag compostos herbicidas
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

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
DK0541168T3 (da) 1991-11-08 1998-05-11 Merck & Co Inc HIV-proteaseinhibitorer, som er egnede til behandling af AIDS
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 Creation and resolution of 2 tert-butylcarboxamidopiprazine
US5455351A (en) * 1993-12-13 1995-10-03 Abbott Laboratories Retroviral protease inhibiting piperazine compounds
HUT74681A (en) 1993-12-15 1997-01-28 Merck & Co Inc N-(2-hydroxy-1-indenyl)-2-phenylmethyl-4-hydroxy-5-(2-carboxamido-piperazinyl)-pentaneamide derivatives of hiv protease inhibitor activity and phrmaceutical compositions contining them
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
WO1999033795A1 (en) * 1997-12-24 1999-07-08 Vertex Pharmaceuticals Incorporated Prodrugs of aspartyl protease inhibitors

Also Published As

Publication number Publication date
CO5261497A1 (es) 2003-03-31
DE60036961T2 (de) 2008-08-28
AU1790901A (en) 2001-06-04
PE20011025A1 (es) 2001-10-12
DE60036961D1 (de) 2007-12-13
ES2295068T3 (es) 2008-04-16
US6642237B1 (en) 2003-11-04
EP1242426B1 (de) 2007-10-31
WO2001038332A1 (en) 2001-05-31
AU777824B2 (en) 2004-11-04
EP1242426A1 (de) 2002-09-25
CA2391643C (en) 2010-01-12
CA2391643A1 (en) 2001-05-31
JP2003514910A (ja) 2003-04-22

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