ES2295068T3 - Gamma-hidroxi-2-(fluoroalquilaminocarbonil)-1-piperazinpentanamidas como inhibidores de la proteasa del vih. - Google Patents

Gamma-hidroxi-2-(fluoroalquilaminocarbonil)-1-piperazinpentanamidas como inhibidores de la proteasa del vih. Download PDF

Info

Publication number
ES2295068T3
ES2295068T3 ES00980679T ES00980679T ES2295068T3 ES 2295068 T3 ES2295068 T3 ES 2295068T3 ES 00980679 T ES00980679 T ES 00980679T ES 00980679 T ES00980679 T ES 00980679T ES 2295068 T3 ES2295068 T3 ES 2295068T3
Authority
ES
Spain
Prior art keywords
hydroxy
dihydro
amino
alkyl
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
ES00980679T
Other languages
English (en)
Spanish (es)
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, Iii
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 and Co Inc
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
Application granted granted Critical
Publication of ES2295068T3 publication Critical patent/ES2295068T3/es
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)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Oncology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Immunology (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • AIDS & HIV (AREA)
  • Molecular Biology (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Hydrogenated Pyridines (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)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
ES00980679T 1999-11-24 2000-11-21 Gamma-hidroxi-2-(fluoroalquilaminocarbonil)-1-piperazinpentanamidas como inhibidores de la proteasa del vih. Expired - Lifetime ES2295068T3 (es)

Applications Claiming Priority (4)

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

Publications (1)

Publication Number Publication Date
ES2295068T3 true ES2295068T3 (es) 2008-04-16

Family

ID=26863215

Family Applications (1)

Application Number Title Priority Date Filing Date
ES00980679T Expired - Lifetime ES2295068T3 (es) 1999-11-24 2000-11-21 Gamma-hidroxi-2-(fluoroalquilaminocarbonil)-1-piperazinpentanamidas como inhibidores de la proteasa del vih.

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)

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
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
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
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
JP2012528160A (ja) 2009-05-27 2012-11-12 メルク・シャープ・エンド・ドーム・コーポレイション Hivプロテアーゼ阻害薬
EP3970702A1 (en) 2009-10-26 2022-03-23 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
EP2630133A1 (de) 2010-10-22 2013-08-28 Bayer Intellectual Property GmbH Neue heterocylische verbindungen als schädlingsbekämpfungsmittel
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
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
JP2014527973A (ja) 2011-09-23 2014-10-23 バイエル・インテレクチユアル・プロパテイー・ゲー・エム・ベー・ハー 非生物的な植物ストレスに対する作用剤としての4−置換1−フェニルピラゾール−3−カルボン酸誘導体の使用
EP2771332B1 (en) 2011-10-26 2016-06-29 Merck Canada Inc. Thiophen and thiazol sulfonamid derivatives as HIV protease inhibitors for the treatment of AIDS
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
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
EP3083609B1 (en) 2013-12-19 2018-08-15 Merck Sharp & Dohme Corp. Hiv protease inhibitors
EP3113780B1 (en) 2014-03-06 2019-08-14 Merck Sharp & Dohme Corp. Hiv protease inhibitors
US10138255B2 (en) 2014-03-10 2018-11-27 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
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
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
JP2022507262A (ja) 2018-11-12 2022-01-18 シンジェンタ クロップ プロテクション アクチェンゲゼルシャフト 除草化合物
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
US5413999A (en) 1991-11-08 1995-05-09 Merck & Co., Inc. HIV protease inhibitors useful for the treatment of AIDS
IL103613A (en) 1991-11-08 1999-05-09 Merck & Co Inc Hiv protease inhibitors process and intermediats for their preparation and pharmaceutical compositions containing them
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
WO1995016688A1 (en) 1993-12-15 1995-06-22 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
WO1999033795A1 (en) 1997-12-24 1999-07-08 Vertex Pharmaceuticals Incorporated Prodrugs of aspartyl protease inhibitors

Also Published As

Publication number Publication date
AU1790901A (en) 2001-06-04
EP1242426A1 (en) 2002-09-25
CA2391643C (en) 2010-01-12
EP1242426B1 (en) 2007-10-31
JP2003514910A (ja) 2003-04-22
PE20011025A1 (es) 2001-10-12
DE60036961T2 (de) 2008-08-28
AU777824B2 (en) 2004-11-04
ATE377011T1 (de) 2007-11-15
CO5261497A1 (es) 2003-03-31
US6642237B1 (en) 2003-11-04
WO2001038332A1 (en) 2001-05-31
DE60036961D1 (de) 2007-12-13
CA2391643A1 (en) 2001-05-31

Similar Documents

Publication Publication Date Title
ES2295068T3 (es) Gamma-hidroxi-2-(fluoroalquilaminocarbonil)-1-piperazinpentanamidas como inhibidores de la proteasa del vih.
CN104892582B (zh) 作为用于治疗增生性疾病的mek抑制剂的吖丁啶
JP6349360B2 (ja) Cb2アゴニストとして有用なピリジン−2−アミド
KR102616762B1 (ko) 타겟화된 단백질들의 향상된 분해를 위한 화합물들 및 방법들
US11098010B2 (en) Substituted dihydroindene-4-carboxamides and analogs thereof, and methods using same
US11807644B2 (en) Methods and compounds for restoring mutant p53 function
KR101877187B1 (ko) 치환된 다이하이드로이소퀴놀린온 화합물
ES2914677T3 (es) Compuestos farmacéuticos
CN119019369A (zh) 含有与bcl6靶向部分连接的e3泛素连接酶结合部分的双官能分子
CN108137507A (zh) 基于mdm2的蛋白水解调节剂和相关的使用方法
IL293558A (en) Functional heterocyclic compounds as modulators of the stimulator of interferon genes (sting)
TW202204338A (zh) 半胱胺酸蛋白酶抑制劑及其使用方法
KR20030019423A (ko) 프로페논 유도체를 함유하는 의약 조성물
HK1193594B (en) Pyridin- 2 -amides useful as cb2 agonists
HK1193594A (en) Pyridin- 2 -amides useful as cb2 agonists