AU2003220170B2 - N-(Substituted benzyl)-8-hydroxy-1,6-naphthyridine-7- carboxamides useful as HIV integrase inhibitors - Google Patents

N-(Substituted benzyl)-8-hydroxy-1,6-naphthyridine-7- carboxamides useful as HIV integrase inhibitors Download PDF

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Publication number
AU2003220170B2
AU2003220170B2 AU2003220170A AU2003220170A AU2003220170B2 AU 2003220170 B2 AU2003220170 B2 AU 2003220170B2 AU 2003220170 A AU2003220170 A AU 2003220170A AU 2003220170 A AU2003220170 A AU 2003220170A AU 2003220170 B2 AU2003220170 B2 AU 2003220170B2
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AU
Australia
Prior art keywords
alkyl
naphthyridine
hydroxy
dioxido
pharmaceutically acceptable
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.)
Ceased
Application number
AU2003220170A
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English (en)
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AU2003220170A1 (en
Inventor
Melissa Egbertson
Mark Embrey
Wei Han
H. Marie Langford
Jeffrey Y. Melamed
Debbie S. Perlow
John S. Wai
Linghang Zhuang
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 Sharp and Dohme Ltd
Merck Sharp and Dohme LLC
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Publication of AU2003220170A1 publication Critical patent/AU2003220170A1/en
Application granted granted Critical
Publication of AU2003220170B2 publication Critical patent/AU2003220170B2/en
Assigned to MERCK SHARP & DOHME CORP. reassignment MERCK SHARP & DOHME CORP. Request to Amend Deed and Register Assignors: MERCK & CO., INC.
Assigned to MERCK SHARP & DOHME CORP. reassignment MERCK SHARP & DOHME CORP. Request to Amend Deed and Register Assignors: MERCK & CO., INC.
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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    • 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

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Virology (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Molecular Biology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • AIDS & HIV (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
AU2003220170A 2002-03-15 2003-03-12 N-(Substituted benzyl)-8-hydroxy-1,6-naphthyridine-7- carboxamides useful as HIV integrase inhibitors Ceased AU2003220170B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US36492902P 2002-03-15 2002-03-15
US60/364,929 2002-03-15
PCT/US2003/007448 WO2003077850A2 (en) 2002-03-15 2003-03-12 N-(substituted benzyl)-8-hydroxy-1,6-naphthyridine-7- carboxamides useful as hiv integrase inhibitors

Publications (2)

Publication Number Publication Date
AU2003220170A1 AU2003220170A1 (en) 2003-09-29
AU2003220170B2 true AU2003220170B2 (en) 2008-12-11

Family

ID=28041987

Family Applications (2)

Application Number Title Priority Date Filing Date
AU2003220170A Ceased AU2003220170B2 (en) 2002-03-15 2003-03-12 N-(Substituted benzyl)-8-hydroxy-1,6-naphthyridine-7- carboxamides useful as HIV integrase inhibitors
AU2003218130A Abandoned AU2003218130A1 (en) 2002-03-15 2003-03-12 N-(substituted benzyl)-8-hydroxy-1,6-naphthyridine-7- carboxamides useful as hiv integrase inhibitors

Family Applications After (1)

Application Number Title Priority Date Filing Date
AU2003218130A Abandoned AU2003218130A1 (en) 2002-03-15 2003-03-12 N-(substituted benzyl)-8-hydroxy-1,6-naphthyridine-7- carboxamides useful as hiv integrase inhibitors

Country Status (8)

Country Link
US (1) US7323460B2 (https=)
EP (1) EP1496836B1 (https=)
JP (1) JP4494020B2 (https=)
AT (1) ATE409187T1 (https=)
AU (2) AU2003220170B2 (https=)
CA (1) CA2478310A1 (https=)
DE (1) DE60323743D1 (https=)
WO (2) WO2003077857A2 (https=)

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ATE409187T1 (de) * 2002-03-15 2008-10-15 Merck & Co Inc N-(substituierte benzyl)-8-hydroxy-1,6- naphthyridin-7- carbonsäureamide als hiv- integrase-hemmer
ATE404537T1 (de) 2002-08-13 2008-08-15 Shionogi & Co Heterocyclische verbindungen mit hiv-integrase- hemmender wirkung
PA8586801A1 (es) 2002-10-31 2005-02-04 Pfizer Inhibidores de hiv-integrasa, composiciones farmaceuticas y metodos para su uso
WO2004067531A1 (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
CA2537325A1 (en) * 2003-09-19 2005-03-31 Gilead Sciences, Inc. Aza-quinolinol phosphonate integrase inhibitor compounds
AU2004285449A1 (en) 2003-10-20 2005-05-12 Merck & Co., Inc. Hydroxy pyridopyrrolopyrazine dione compounds useful as HIV integrase inhibitors
JP4789144B2 (ja) * 2004-02-04 2011-10-12 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ナフチリジン誘導体
JP4625838B2 (ja) * 2004-03-09 2011-02-02 メルク・シャープ・エンド・ドーム・コーポレイション Hivインテグラーゼ阻害薬
CA2564356A1 (en) 2004-04-26 2005-11-03 Pfizer Inc. Pyrrolopyridine derivatives and their use as hiv-integrase inhibitors
DE602005002746T2 (de) 2004-04-26 2008-02-07 Pfizer Inc. Inhibitoren des hiv-integrase-enzyms
AU2006306355A1 (en) * 2005-10-27 2007-05-03 Merck & Co., Inc. HIV integrase inhibitors
BRPI0716539A2 (pt) 2006-09-07 2016-11-01 Emisphere Tech Inc métodos para sintetização de ácido n-(8-[2-hidroxibenzoil]amino) caprílico e de sal de sódio deste
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

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WO2002009504A1 (en) * 2000-08-02 2002-02-07 George Robert A Squirrel-proof bird feeding apparatus and method
WO2002030931A2 (en) * 2000-10-12 2002-04-18 Merck & Co., Inc. Aza- and polyaza-naphthalenyl carboxamides useful as hiv integrase inhibitors
WO2003077857A2 (en) * 2002-03-15 2003-09-25 Merck & Co., Inc. N-(substituted benzyl)-8-hydroxy-1,6-naphthyridine-7- carboxamides useful as hiv integrase inhibitors
WO2003086319A2 (en) * 2002-04-10 2003-10-23 Merck & Co., Inc. Pharmaceutical compositions containing an hiv integrase inhibitor and a nonionic surfactant

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DE69828284T2 (de) * 1997-06-30 2005-12-08 Nippon Kayaku K.K. Naphthyridinderivate oder salze davon
KR20010023313A (ko) 1997-08-25 2001-03-26 해피 페너 ; 해리 에이치. 페너 2세 Gaba 뇌 수용체 리간드로서의 치환된4-옥소-나프티리딘-3-카르복스아미드
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JP2002517390A (ja) 1998-06-03 2002-06-18 メルク エンド カムパニー インコーポレーテッド Hivインテグラーゼ阻害薬
US6306891B1 (en) * 1998-06-03 2001-10-23 Merck & Co., Inc. HIV integrase inhibitors
US6262055B1 (en) * 1998-06-03 2001-07-17 Merck & Co., Inc. HIV integrase inhibitors
CA2329134A1 (en) 1998-06-03 1999-12-09 David L. Clark Hiv integrase inhibitors
US6380249B1 (en) * 1998-06-03 2002-04-30 Merck & Co., Inc. HIV integrase inhibitors
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ID27843A (id) * 1998-08-11 2001-04-26 Pfizer Prod Inc Substitusi 1, 8-naftiridin-4(ih)-on sebagai penghambat fosfodiesterase 4
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US20040039060A1 (en) * 2000-06-14 2004-02-26 Ryuichi Kiyama Inhibitor for enzyme having two divalent metal ions as active centers
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GB0017676D0 (en) * 2000-07-19 2000-09-06 Angeletti P Ist Richerche Bio Inhibitors of viral polymerase
ATE345129T1 (de) * 2000-10-12 2006-12-15 Merck & Co Inc Aza- und polyaza-naphthalenylcarbonsäureamide als hiv-integrase-hemmer
WO2002036734A2 (en) * 2000-10-12 2002-05-10 Merck & Co., Inc. Aza-and polyaza-naphthalenyl ketones useful as hiv integrase inhibitors
EP1326611B1 (en) * 2000-10-12 2007-06-13 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
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ATE355064T1 (de) 2001-10-26 2006-03-15 Angeletti P Ist Richerche Bio Dihydroxypyrimidin-carbonsäueramid-hemmer der hiv-integrase

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2002009504A1 (en) * 2000-08-02 2002-02-07 George Robert A Squirrel-proof bird feeding apparatus and method
WO2002030931A2 (en) * 2000-10-12 2002-04-18 Merck & Co., Inc. Aza- and polyaza-naphthalenyl carboxamides useful as hiv integrase inhibitors
WO2002030930A2 (en) * 2000-10-12 2002-04-18 Merck & Co., Inc. Aza- and polyaza-naphthalenyl carboxamides useful as hiv integrase inhibitors
WO2003077857A2 (en) * 2002-03-15 2003-09-25 Merck & Co., Inc. N-(substituted benzyl)-8-hydroxy-1,6-naphthyridine-7- carboxamides useful as hiv integrase inhibitors
WO2003086319A2 (en) * 2002-04-10 2003-10-23 Merck & Co., Inc. Pharmaceutical compositions containing an hiv integrase inhibitor and a nonionic surfactant

Also Published As

Publication number Publication date
EP1496836A4 (en) 2006-03-22
US7323460B2 (en) 2008-01-29
JP2005527521A (ja) 2005-09-15
CA2478310A1 (en) 2003-09-25
WO2003077857A2 (en) 2003-09-25
WO2003077857A3 (en) 2006-06-08
JP4494020B2 (ja) 2010-06-30
US20050176955A1 (en) 2005-08-11
AU2003218130A1 (en) 2003-09-29
WO2003077850A3 (en) 2004-11-11
EP1496836B1 (en) 2008-09-24
DE60323743D1 (en) 2008-11-06
WO2003077850A2 (en) 2003-09-25
AU2003220170A1 (en) 2003-09-29
EP1496836A2 (en) 2005-01-19
AU2003218130A8 (en) 2003-09-29
ATE409187T1 (de) 2008-10-15

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Legal Events

Date Code Title Description
FGA Letters patent sealed or granted (standard patent)
DA3 Amendments made section 104

Free format text: THE NATURE OF THE AMENDMENT IS: AMEND THE PATENTEE NAME FROM MERCK & CO., INC. TO MERCK SHARP & DOHME CORP.

MK14 Patent ceased section 143(a) (annual fees not paid) or expired