ATE409187T1 - N-(substituierte benzyl)-8-hydroxy-1,6- naphthyridin-7- carbonsäureamide als hiv- integrase-hemmer - Google Patents

N-(substituierte benzyl)-8-hydroxy-1,6- naphthyridin-7- carbonsäureamide als hiv- integrase-hemmer

Info

Publication number
ATE409187T1
ATE409187T1 AT03716466T AT03716466T ATE409187T1 AT E409187 T1 ATE409187 T1 AT E409187T1 AT 03716466 T AT03716466 T AT 03716466T AT 03716466 T AT03716466 T AT 03716466T AT E409187 T1 ATE409187 T1 AT E409187T1
Authority
AT
Austria
Prior art keywords
sup
naphthyridine
hiv
hydroxy
substituted benzyl
Prior art date
Application number
AT03716466T
Other languages
English (en)
Inventor
Melissa Egbertson
H Marie Langford
Jeffrey Melamed
John Wai
Wei Han
Debbie Perlow
Linghang Zhuang
Mark Embrey
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 ATE409187T1 publication Critical patent/ATE409187T1/de

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Virology (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Molecular Biology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
AT03716466T 2002-03-15 2003-03-12 N-(substituierte benzyl)-8-hydroxy-1,6- naphthyridin-7- carbonsäureamide als hiv- integrase-hemmer ATE409187T1 (de)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US36492902P 2002-03-15 2002-03-15

Publications (1)

Publication Number Publication Date
ATE409187T1 true ATE409187T1 (de) 2008-10-15

Family

ID=28041987

Family Applications (1)

Application Number Title Priority Date Filing Date
AT03716466T ATE409187T1 (de) 2002-03-15 2003-03-12 N-(substituierte benzyl)-8-hydroxy-1,6- naphthyridin-7- carbonsäureamide als hiv- integrase-hemmer

Country Status (8)

Country Link
US (1) US7323460B2 (de)
EP (1) EP1496836B1 (de)
JP (1) JP4494020B2 (de)
AT (1) ATE409187T1 (de)
AU (2) AU2003218130A1 (de)
CA (1) CA2478310A1 (de)
DE (1) DE60323743D1 (de)
WO (2) WO2003077857A2 (de)

Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE60323743D1 (en) 2002-03-15 2008-11-06 Merck & Co Inc N-(substituierte benzyl)-8-hydroxy-1,6-naphthyridin-7- carbonsäureamide als hiv-integrase-hemmer
JP3908248B2 (ja) 2002-08-13 2007-04-25 塩野義製薬株式会社 Hivインテグラーゼ阻害活性を有するヘテロ環化合物
PA8586801A1 (es) 2002-10-31 2005-02-04 Pfizer Inhibidores de hiv-integrasa, composiciones farmaceuticas y metodos para su uso
CA2513141A1 (en) 2003-01-27 2004-08-12 Pfizer Inc. Hiv-integrase inhibitors, pharmaceutical compositions, and methods for their use
WO2004080402A2 (en) * 2003-03-12 2004-09-23 Merck & Co. Inc. Potassium salt of an hiv integrase inhibitor
EP1664046B1 (de) 2003-09-19 2009-06-17 Gilead Sciences, Inc. Azachinolinolphosphonatverbindungen als integraseinhibitoren
CN1870896A (zh) 2003-10-20 2006-11-29 默克公司 用作hiv整合酶抑制剂的羟基吡啶并吡咯并吡嗪二酮化合物
EP1714966A4 (de) * 2004-02-04 2008-01-02 Shionogi & Co Naphthylidinderivat mit einer hiv-integrase-hemmenden wirkung
NZ549449A (en) * 2004-03-09 2009-05-31 Merck & Co Inc HIV Integrase inhibitors
DE602005002746T2 (de) 2004-04-26 2008-02-07 Pfizer Inc. Inhibitoren des hiv-integrase-enzyms
BRPI0510319A (pt) 2004-04-26 2007-10-16 Pfizer inibidores da enzima integrase de hiv
EP1942736A2 (de) * 2005-10-27 2008-07-16 Merck & Co., Inc. Hiv-integrasehemmer
CA2662080C (en) 2006-09-07 2012-07-17 F. Hoffmann-La Roche Ag A process for the manufacture of snac (salcaprozate sodium)
CN106117196A (zh) * 2016-06-09 2016-11-16 青岛辰达生物科技有限公司 一种制备抗癌药物达沙替尼的方法
CN107722106A (zh) * 2016-08-11 2018-02-23 重庆大学 Hiv抑制剂
CN112409267A (zh) * 2019-08-22 2021-02-26 江苏阿尔法药业有限公司 一种索菲布韦中间体的制备方法
AR122928A1 (es) * 2020-07-10 2022-10-19 Goldfinch Bio Inc 1,6-naftiridinas sustituidas inhibidoras de cdk5

Family Cites Families (41)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JPS5751837B2 (de) 1973-04-05 1982-11-04
US4416884A (en) * 1978-04-12 1983-11-22 Otsuka Pharmaceutical Co., Ltd. Piperazinylbenzoheterocyclic compounds
FR2632639B1 (fr) * 1988-06-09 1990-10-05 Sanofi Sa Derives d'amino-4 carboxy-3 naphtyridines, leur preparation et compositions pharmaceutiques qui les contiennent
IL101860A0 (en) * 1991-05-31 1992-12-30 Ici Plc Heterocyclic derivatives
TW263498B (de) 1993-11-10 1995-11-21 Takeda Pharm Industry Co Ltd
US5776944A (en) * 1994-06-16 1998-07-07 Lg Chemical Ltd. 7-(4-aminomethyl-3-methyloxyiminopyrroplidin-1-yl)-1-cyclopropyl-6-flu oro-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid and the process for the preparation thereof
DK0688772T3 (da) * 1994-06-16 1999-11-01 Lg Chemical Ltd Quinolincarboxylsyrederivater med 7-(4-aminomethyl-3-oxim)-pyrrolidinsubstituenter og fremgangsmåde til deres fremstilling
US5681832A (en) 1995-02-17 1997-10-28 The United States Of America As Represented By The Department Of Health And Human Services Aroylaniline compounds, pharmaceutical compositions, and methods of using same to inhibit viral activity
JPH11510156A (ja) * 1995-08-02 1999-09-07 カイロサイエンス・リミテッド キノロン類およびその医療上の使用
US5945431A (en) * 1996-03-15 1999-08-31 Biochem Therapeutics Incorporated Cytomegalovirus inhibiting compounds
AU4172197A (en) * 1996-09-10 1998-04-02 Pharmacia & Upjohn Company 8-hydroxy-7-substituted quinolines as anti-viral agents
JP2001500890A (ja) 1996-09-25 2001-01-23 ゼネカ リミテッド Vegfのような成長因子の作用を阻害するキノリン誘導体
US6294547B1 (en) * 1997-06-30 2001-09-25 Nippon Kayaku Kabushiki Kaisha Naphthyridine deratives or salts thereof
EP1007526A1 (de) 1997-08-25 2000-06-14 Neurogen Corporation Substituierte 4-oxo-naphthyridine-3-carbonsaeureamide als gaba-rezeptorliganden des gehirns
GB9720052D0 (en) 1997-09-19 1997-11-19 Smithkline Beecham Plc Novel compounds
IL135180A0 (en) * 1997-09-30 2001-05-20 Daiichi Seiyaku Co Sulfonyl derivatives
WO1999029318A1 (en) * 1997-12-11 1999-06-17 Biochem Pharma Inc. Antiviral compounds
RU2220960C2 (ru) 1997-12-22 2004-01-10 Фармация Энд Апджон Компани 4-гидрокси-3-хинолинкарбоксамиды и гидразиды, фармацевтическая композиция и способ лечения на их основе
US6306891B1 (en) * 1998-06-03 2001-10-23 Merck & Co., Inc. HIV integrase inhibitors
US6380249B1 (en) * 1998-06-03 2002-04-30 Merck & Co., Inc. HIV integrase inhibitors
CA2333707A1 (en) 1998-06-03 1999-12-09 Melissa Egbertson Hiv integrase inhibitors
EP1083897A4 (de) 1998-06-03 2003-01-02 Merck & Co Inc Hiv integrase-inhibitoren
US6262055B1 (en) * 1998-06-03 2001-07-17 Merck & Co., Inc. HIV integrase inhibitors
WO1999062897A1 (en) 1998-06-03 1999-12-09 Merck & Co., Inc. Hiv integrase inhibitors
SE9802550D0 (sv) 1998-07-15 1998-07-15 Active Biotech Ab Quinoline derivatives
NZ509297A (en) 1998-08-11 2003-11-28 Pfizer Prod Inc Substituted 1,8-naphthyridin-4(1H)-ones as phosphodiesterase 4 inhibitors
WO2001000578A1 (en) 1999-06-25 2001-01-04 Merck & Co., Inc. 1-(aromatic- or heteroaromatic-substituted)-3-(heteroaromatic substituted)-1,3-propanediones and uses thereof
US20040039060A1 (en) * 2000-06-14 2004-02-26 Ryuichi Kiyama Inhibitor for enzyme having two divalent metal ions as active centers
US6730682B2 (en) 2000-07-12 2004-05-04 Pharmacia & Upjohn Company Heterocycle carboxamides as antiviral agents
GB0017676D0 (en) 2000-07-19 2000-09-06 Angeletti P Ist Richerche Bio Inhibitors of viral polymerase
WO2002009504A1 (en) * 2000-08-02 2002-02-07 George Robert A Squirrel-proof bird feeding apparatus and method
US20050010048A1 (en) * 2000-10-12 2005-01-13 Linghang Zhuang Aza-and polyaza-naphthalenly ketones useful as hiv integrase inhibitors
ES2287170T3 (es) * 2000-10-12 2007-12-16 MERCK & CO., INC. Aza- y poliaza-naftalenil-carboxamidas utilies como inhibidores de la vih integrasa.
ATE345129T1 (de) * 2000-10-12 2006-12-15 Merck & Co Inc Aza- und polyaza-naphthalenylcarbonsäureamide als hiv-integrase-hemmer
AU1152702A (en) * 2000-10-12 2002-04-22 Merck & Co Inc Aza- and polyaza-naphthalenyl carboxamides useful as hiv integrase inhibitors
JP3616628B2 (ja) * 2001-03-01 2005-02-02 塩野義製薬株式会社 Hivインテグラーゼ阻害活性を有する含窒素芳香族複素環化合物
AR036256A1 (es) * 2001-08-17 2004-08-25 Merck & Co Inc Sal sodica de un inhibidor de integrasa del vih, procesos para su preparacion, composiciones farmaceuticas que lo contienen y su uso para la manufactura de un medicamento
AU2002334205B2 (en) 2001-10-26 2007-07-05 Istituto Di Ricerche Di Biologia Molecolara P. Angeletti Spa Dihydroxypyrimidine carboxamide inhibitors of HIV integrase
US7169780B2 (en) 2001-10-26 2007-01-30 Istitute Di Ricerche Di Biologia Molecolare P. Angeletti S.P.A. N-substituted hydroxypyrimidinone carboxamide inhibitors of HIV integrase
DE60323743D1 (en) * 2002-03-15 2008-11-06 Merck & Co Inc N-(substituierte benzyl)-8-hydroxy-1,6-naphthyridin-7- carbonsäureamide als hiv-integrase-hemmer
AU2003220186A1 (en) * 2002-04-10 2003-10-27 Merck And Co., Inc. Pharmaceutical compositions containing an hiv integrase inhibitor and a nonionic surfactant

Also Published As

Publication number Publication date
WO2003077857A2 (en) 2003-09-25
CA2478310A1 (en) 2003-09-25
AU2003218130A1 (en) 2003-09-29
JP2005527521A (ja) 2005-09-15
EP1496836A2 (de) 2005-01-19
WO2003077850A3 (en) 2004-11-11
WO2003077850A2 (en) 2003-09-25
AU2003218130A8 (en) 2003-09-29
AU2003220170B2 (en) 2008-12-11
JP4494020B2 (ja) 2010-06-30
US7323460B2 (en) 2008-01-29
WO2003077857A3 (en) 2006-06-08
EP1496836B1 (de) 2008-09-24
EP1496836A4 (de) 2006-03-22
US20050176955A1 (en) 2005-08-11
AU2003220170A1 (en) 2003-09-29
DE60323743D1 (en) 2008-11-06

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