PE20011025A1 - Gamma-hidroxi-2-(fluoroalquilaminocarbonil)-1-piperazinapentanamidas como inhibidores de proteasa del vih - Google Patents

Gamma-hidroxi-2-(fluoroalquilaminocarbonil)-1-piperazinapentanamidas como inhibidores de proteasa del vih

Info

Publication number
PE20011025A1
PE20011025A1 PE2000001259A PE0012592000A PE20011025A1 PE 20011025 A1 PE20011025 A1 PE 20011025A1 PE 2000001259 A PE2000001259 A PE 2000001259A PE 0012592000 A PE0012592000 A PE 0012592000A PE 20011025 A1 PE20011025 A1 PE 20011025A1
Authority
PE
Peru
Prior art keywords
alkyl
hydroxy
cycloalkyl
hiv protease
piperazineapentanamides
Prior art date
Application number
PE2000001259A
Other languages
English (en)
Inventor
Kevin T Chapman
Yuan Cheng
Joseph Leslie Duffy
Tracy Huening
Nancy J Kevin
Fengqi Zhang
Zhijian Lu
Subharekha Raghavan
Thomas A Rano
James R Tata
Brian Anthony Kirk
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
Publication of PE20011025A1 publication Critical patent/PE20011025A1/es

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)
  • 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)
  • 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)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

SE REFIERE A PIPERAZINA 2 CARBOXAMIDO SUSTITUIDAS DE FORMULA I DONDE R1 ES ALQUILO C1-C6, ALQUENILO C2-C6, ALQUINILO C2-C6, CICLOALQUILO C3-C6, ENTRE OTROS; R2 Y R3 SON H, ALQUILO C1-C4 O JUNTO A C FORMAN CICLOALQUILO C3-C6; R4 ES ALQUILO C1-C6, CICLOALQUILO, ARILO, HETEROARILO, ENTRE OTROS; R5 ES CARBOCICLICO, HETEROCICLO, ENTRE OTROS; R6 ES ALQUILO C1-C6 FLUORADO; Ra Y Rb SON ALQUILO C1-C4 O JUNTO A N FORMAN AZACICLOALQUILO C3-C6. UN COMPUESTO PREFERIDO ES (OR,þS,2S)-N-((3S,4S)-3,4-DIHIDRO-3-HIDROXI-2H-1-BENZOPIRAN-4-IL)-4-(1-FLUORO[3,2-c]-PIRIDIN-2-IL-1-METILETIL)-þ-HIDROXI-O-(FENILMETIL)-2-[[(2,2,2-TRIFLUOROETIL)AMINO]CARBONIL]-1-PIPERAZINAPENTANAMIDA, ENTRE OTROS. TAMBIEN SE REFIERE A COMPOSICIONES QUE COMPRENDEN ADEMAS AGENTES ANTIVIRALES DE VIH/SIDA, INMUNOMODULADORES, AGENTES ANTIINFECCIOSOS, INHIBIDORES DE TRANSCRIPTASA INVERSA NUCLEOSIDO Y NO NUCLESIDO, INDINAVIR, RITONAVIR. EL COMPUESTO I ES UN INHIBIDOR DE PROTEASA DEL VIH
PE2000001259A 1999-11-24 2000-11-24 Gamma-hidroxi-2-(fluoroalquilaminocarbonil)-1-piperazinapentanamidas como inhibidores de proteasa del vih PE20011025A1 (es)

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
PE20011025A1 true PE20011025A1 (es) 2001-10-12

Family

ID=26863215

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2000001259A PE20011025A1 (es) 1999-11-24 2000-11-24 Gamma-hidroxi-2-(fluoroalquilaminocarbonil)-1-piperazinapentanamidas como inhibidores de proteasa del vih

Country Status (11)

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

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
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
US8030336B2 (en) * 2002-12-13 2011-10-04 Ym Biosciences Australia Pty Ltd Nicotinamide-based kinase inhibitors
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
KR101835893B1 (ko) 2009-10-26 2018-04-19 머크 샤프 앤드 돔 코포레이션 인테그라제 억제제를 함유하는 고형 제약 조성물
EP3235818A3 (en) 2010-04-01 2018-03-14 Critical Outcome Technologies, Inc. Compounds for the treatment of hiv
EP2630133A1 (de) 2010-10-22 2013-08-28 Bayer Intellectual Property GmbH Neue heterocylische verbindungen als schädlingsbekämpfungsmittel
WO2012055031A1 (en) 2010-10-28 2012-05-03 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
US9133157B2 (en) 2011-10-26 2015-09-15 Merck Canada Inc. HIV protease inhibitors
CN104755475B (zh) 2012-09-11 2016-12-28 默沙东公司 Hiv蛋白酶抑制剂
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
US9834526B2 (en) 2013-12-19 2017-12-05 Merck Sharp & Dohme Corp. HIV protease inhibitors
US9994587B2 (en) 2014-03-06 2018-06-12 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
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)
AR114422A1 (es) 2018-03-30 2020-09-02 Syngenta Participations Ag Compuestos herbicidas
CA3118623A1 (en) 2018-11-12 2020-05-22 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

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
EP0541168B1 (en) 1991-11-08 1998-03-11 Merck & Co. Inc. HIV protease inhibitors useful for the treatment of 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
CZ288312B6 (en) 1993-12-15 2001-05-16 Merck & Co Inc HIV-protease inhibitors and pharmaceutical preparations in which they are comprised
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
ATE377011T1 (de) 2007-11-15
CO5261497A1 (es) 2003-03-31
AU777824B2 (en) 2004-11-04
CA2391643C (en) 2010-01-12
US6642237B1 (en) 2003-11-04
DE60036961D1 (de) 2007-12-13
EP1242426A1 (en) 2002-09-25
DE60036961T2 (de) 2008-08-28
ES2295068T3 (es) 2008-04-16
EP1242426B1 (en) 2007-10-31
AU1790901A (en) 2001-06-04
JP2003514910A (ja) 2003-04-22
WO2001038332A1 (en) 2001-05-31
CA2391643A1 (en) 2001-05-31

Similar Documents

Publication Publication Date Title
PE20011025A1 (es) Gamma-hidroxi-2-(fluoroalquilaminocarbonil)-1-piperazinapentanamidas como inhibidores de proteasa del vih
PE20040241A1 (es) Inhibidores proteasa hiv, composiciones que los contienen y materiales para sus sintesis
AR048055A1 (es) Derivados de pirimidina como inhibidores de dipeptidil peptidasa
EA200400986A1 (ru) Гетероциклические трипептиды в качестве ингибиторов вируса гепатита c
PE20080072A1 (es) Compuestos heterociclicos como inhibidores de proteasas serinas
TW200615275A (en) Hepatitis C inhibitor dipeptide analogs
HK1143579A1 (en) Hiv protease inhibiting sulfonamides
ECSP088150A (es) Inhibidores macrociclicos del virus de la hepatitis c
PE20070138A1 (es) Compuestos heterociclicos como inhibidores de aspartil proteasas
DK0810209T3 (da) Alpha - and beta-aminosyre-hydroxyethylaminosulfonamider til anvendelse som inhibitorer af retrovirale proteaser
CO6190525A2 (es) Fosfoindoles enantiomericamente puros como inhibidores de vih
ATE512971T1 (de) Peptidanaloga als hepatitis c-hemmer
PE20020786A1 (es) Derivados de azaindol antiviral
AR047076A1 (es) Compuestos de pirrolotriazina como inhibidores de tirosina quinasas, composiciones farmaceuticas
DE60234028D1 (de) Hydantion-derivate als hemmer von matrix-metalloproteinasen
AR055360A1 (es) Inhibidores macrociclicos del virus de la hepatitis c
AP2001002205A0 (en) Cyclopentyl-substituted glutaramide derivatives as inhibitors of neutral endopeptidase.
HK1100659A1 (en) Hiv protease inhibiting compounds hiv
NO20005261L (no) Nye heterocyklisk substituerte amider med cystein-protease- inhiberende virkning
AR051392A1 (es) Antagonistas no peptidicos de bradiquinina y composiciones farmaceuticas de los mismos
DE69902754D1 (de) Heteroaryl-amidinen,-methylamidinen und -guanidinen als protease inhibitoren, insbesondere als urokinase inhibitoren
PE20090548A1 (es) Compuestos aza-biciclohexano como inhibidores de trombina
MXPA03010258A (es) 2-amino-benzoxazol sulfonamidas, inhibidores de amplio espectro de la vih proteasa.
AR050718A1 (es) Co-cristales entre polietilenglicolesy 5-fenilpirazolil-1-bencensulfonamidas. procesos de obtencion y composiciones farmaceuticas.
AR039937A1 (es) Derivados de azetidina como inhibidores de tripsina proteasas

Legal Events

Date Code Title Description
FD Application declared void or lapsed