AU2002246499B2 - Aza-and polyaza-naphthalenyl carboxamides useful as HIV integrase inhibitors - Google Patents

Aza-and polyaza-naphthalenyl carboxamides useful as HIV integrase inhibitors Download PDF

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Publication number
AU2002246499B2
AU2002246499B2 AU2002246499A AU2002246499A AU2002246499B2 AU 2002246499 B2 AU2002246499 B2 AU 2002246499B2 AU 2002246499 A AU2002246499 A AU 2002246499A AU 2002246499 A AU2002246499 A AU 2002246499A AU 2002246499 B2 AU2002246499 B2 AU 2002246499B2
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AU
Australia
Prior art keywords
alkyl
substituted
fluoroalkyl
ora
halogen
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Ceased
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AU2002246499A
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AU2002246499A1 (en
Inventor
Neville J. Anthony
Jennifer J. Bennett
Robert P. Gomez
Steven D. Young
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Merck and Co Inc
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Merck and Co Inc
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Publication of AU2002246499A1 publication Critical patent/AU2002246499A1/en
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Publication of AU2002246499B2 publication Critical patent/AU2002246499B2/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/04—Ortho-condensed systems
    • 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
    • A61P43/00—Drugs 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)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Virology (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Communicable Diseases (AREA)
  • Molecular Biology (AREA)
  • AIDS & HIV (AREA)
  • Engineering & Computer Science (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Compression Or Coding Systems Of Tv Signals (AREA)
  • Pyrrole Compounds (AREA)
  • Decoration By Transfer Pictures (AREA)
  • Indole Compounds (AREA)
AU2002246499A 2000-10-12 2001-10-09 Aza-and polyaza-naphthalenyl carboxamides useful as HIV integrase inhibitors Ceased AU2002246499B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US23967900P 2000-10-12 2000-10-12
US60/239,679 2000-10-12
PCT/US2001/042565 WO2002055079A2 (en) 2000-10-12 2001-10-09 Aza-and polyaza-naphthalenyl carboxamides useful as hiv integrase inhibitors

Publications (2)

Publication Number Publication Date
AU2002246499A1 AU2002246499A1 (en) 2003-02-06
AU2002246499B2 true AU2002246499B2 (en) 2005-12-22

Family

ID=22903252

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2002246499A Ceased AU2002246499B2 (en) 2000-10-12 2001-10-09 Aza-and polyaza-naphthalenyl carboxamides useful as HIV integrase inhibitors

Country Status (9)

Country Link
US (1) US6841558B2 (enExample)
EP (1) EP1326610B1 (enExample)
JP (1) JP2004517860A (enExample)
AT (1) ATE345129T1 (enExample)
AU (1) AU2002246499B2 (enExample)
CA (1) CA2425625A1 (enExample)
DE (1) DE60124577T2 (enExample)
ES (1) ES2274913T3 (enExample)
WO (1) WO2002055079A2 (enExample)

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CA2463975A1 (en) * 2001-10-26 2003-05-01 Maria Emilia Di Francesco Dihydroxypyrimidine carboxamide inhibitors of hiv integrase
DE122009000048I1 (de) * 2001-10-26 2010-04-08 Angeletti P Ist Richerche Bio N-substituierte hydroxypyrimidinoncarboxamid-hemmer der hiv-integrase
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
ATE404537T1 (de) 2002-08-13 2008-08-15 Shionogi & Co Heterocyclische verbindungen mit hiv-integrase- hemmender wirkung
EP1539714B1 (en) * 2002-09-11 2008-08-13 Merck & Co., Inc. 8-hydroxy-1-oxo-tetrahydropyrrolopyrazine compounds useful as hiv integrase inhibitors
WO2004024078A2 (en) 2002-09-11 2004-03-25 Merck & Co., Inc. Dihydroxypyridopyrazine-1,6-dione compounds useful as hiv integrase inhibitors
AU2003301439A1 (en) 2002-10-16 2004-05-04 Gilead Sciences, Inc. Pre-organized tricyclic integrase inhibitor compounds
US7176220B2 (en) 2002-11-20 2007-02-13 Japan Tobacco Inc. 4-oxoquinoline compound and use thereof as pharmaceutical agent
WO2004058756A1 (en) 2002-12-27 2004-07-15 Istituto Di Ricerche Di Biologia Molecolare P. Angeletti Spa Tetrahydro-4h-pyrido[1,2-a]pyrimidines and related compounds useful as hiv integrase inhibitors
CN1812992A (zh) * 2003-04-28 2006-08-02 泰博特克药品有限公司 Hiv整合酶抑制剂
JP2006528694A (ja) * 2003-05-13 2006-12-21 スミスクライン ビーチャム コーポレーション ナフチリジンインテグラーゼインヒビター
TW200510425A (en) * 2003-08-13 2005-03-16 Japan Tobacco Inc Nitrogen-containing fused ring compound and use thereof as HIV integrase inhibitor
ATE433974T1 (de) 2003-09-19 2009-07-15 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
US7919623B2 (en) * 2004-02-04 2011-04-05 Shionogi & Co., Ltd. Naphthyridine derivatives having inhibitory activity against HIV integrase
CN1976915A (zh) 2004-02-11 2007-06-06 史密丝克莱恩比彻姆公司 Hiv整合酶抑制剂
WO2005087768A1 (en) 2004-03-09 2005-09-22 Merck & Co., Inc. Hiv integrase inhibitors
US7820680B2 (en) 2004-03-09 2010-10-26 Merck & Co., Inc. HIV integrase inhibitors
AU2005221864A1 (en) 2004-03-09 2005-09-22 Istituto Di Ricerche Di Biologia Molecolare P Angeletti Spa HIV integrase inhibitors
EP1725535A4 (en) 2004-03-09 2009-11-25 Merck & Co Inc HIV integrase
ES2529038T3 (es) * 2004-05-07 2015-02-16 Merck Sharp & Dohme Corp. Inhibidores de la integrasa de VIH
US7531554B2 (en) 2004-05-20 2009-05-12 Japan Tobacco Inc. 4-oxoquinoline compound and use thereof as HIV integrase inhibitor
MY134672A (en) 2004-05-20 2007-12-31 Japan Tobacco Inc Stable crystal of 4-oxoquinoline compound
US8633219B2 (en) 2004-05-21 2014-01-21 Japan Tobacco Inc. Combination therapy
US7476666B2 (en) 2004-06-09 2009-01-13 Merck & Co., Inc. HIV integrase inhibitors
WO2006103399A1 (en) * 2005-03-31 2006-10-05 Istituto Di Ricerche Di Biologia Molecolare P Angeletti Spa Hiv integrase inhibitors
WO2006121831A2 (en) * 2005-05-10 2006-11-16 Merck & Co., Inc. Hiv integrase inhibitors
JP5094725B2 (ja) * 2005-10-04 2012-12-12 イステイチユート・デイ・リチエルケ・デイ・ビオロジア・モレコラーレ・ピ・アンジエレツテイ・エツセ・エルレ・エルレ Ｈｉｖインテグラーゼ阻害剤
AU2006306355A1 (en) * 2005-10-27 2007-05-03 Merck & Co., Inc. HIV integrase inhibitors
US8217042B2 (en) 2005-11-11 2012-07-10 Zentaris Gmbh Pyridopyrazines and their use as modulators of kinases
EP1790342A1 (de) 2005-11-11 2007-05-30 Zentaris GmbH Pyridopyrazin-Derivate und deren Verwendung als Modulatoren der Signaltransduktionswege
US7902182B2 (en) * 2005-11-16 2011-03-08 Bristol-Myers Squibb Company HIV integrase inhibitors
JP4669040B2 (ja) 2006-03-06 2011-04-13 日本たばこ産業株式会社 ４−オキソキノリン化合物の製造方法
WO2007136714A2 (en) 2006-05-16 2007-11-29 Gilead Sciences, Inc. Integrase inhibitors
WO2008010964A1 (en) * 2006-07-17 2008-01-24 Merck & Co., Inc. 1-hydroxy naphthyridine compounds as anti-hiv agents
ES2488922T3 (es) 2006-09-29 2014-09-01 Idenix Pharmaceuticals, Inc. Fosfoindoles enantiómeramente puros como inhibidores del HIV
CA2665538A1 (en) * 2006-10-18 2008-04-24 Merck & Co., Inc. Hiv integrase inhibitors
US8513420B2 (en) * 2007-03-19 2013-08-20 Monika Mazik Amino-naphthyridine derivatives
EP1972627A1 (en) * 2007-03-19 2008-09-24 Technische Universität Carolo-Wilhelmina zu Braunschweig Amino-napthyridine derivatives
CN105055432A (zh) 2008-01-25 2015-11-18 奇默里克斯公司 治疗病毒感染的方法
DE102009038123A1 (de) 2009-08-17 2011-02-24 Aicuris Gmbh & Co. Kg Substituierte (Thiazolyl-carbonyl)imidazolidinone und ihre Verwendung
WO2011045330A1 (en) 2009-10-13 2011-04-21 Tibotec Pharmaceuticals Macrocyclic integrase inhibitors
CA2789443C (en) 2010-02-12 2016-09-13 Chimerix, Inc. Nucleoside phosphonate salts
WO2011121105A1 (en) 2010-04-02 2011-10-06 Tibotec Pharmaceuticals Macrocyclic integrase inhibitors
US9029391B2 (en) 2011-01-24 2015-05-12 Viiv Healthcare Uk Limited Isoquinoline compounds and methods for treating HIV
CN105611927A (zh) 2013-05-16 2016-05-25 美国政府(由卫生和人类服务部的部长所代表) 用于抑制耐药性hiv-1整合酶耐药株的化合物

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Publication number Priority date Publication date Assignee Title
US3945995A (en) * 1973-04-05 1976-03-23 Sumitomo Chemical Company, Limited D-α-(4-hydroxypyridine-3-carbonamido)-p-hydroxyphenylacetamidopenicillanic acid
US4416884A (en) * 1978-04-12 1983-11-22 Otsuka Pharmaceutical Co., Ltd. Piperazinylbenzoheterocyclic compounds
WO1998011073A1 (en) * 1996-09-10 1998-03-19 Pharmacia & Upjohn Company 8-hydroxy-7-substituted quinolines as anti-viral agents
WO1999016747A1 (en) * 1997-09-30 1999-04-08 Daiichi Pharmaceutical Co., Ltd. Sulfonyl derivatives

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AU1625192A (en) * 1991-05-31 1992-12-03 Zeneca Limited Heterocyclic derivatives
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
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HUP0003258A3 (en) 1997-08-25 2001-05-28 Neurogen Corp Branford Substituted 4-oxo-napthyridine-3-carboxamides as gaba brain receptor ligands
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GB9720052D0 (en) * 1997-09-19 1997-11-19 Smithkline Beecham Plc Novel compounds
EP1042295B1 (en) 1997-12-22 2005-09-07 Pharmacia & Upjohn Company LLC 4-hydroxyquinoline-3-carboxamides and hydrazides as antiviral agents
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GB0017676D0 (en) 2000-07-19 2000-09-06 Angeletti P Ist Richerche Bio Inhibitors of viral polymerase
CA2463975A1 (en) 2001-10-26 2003-05-01 Maria Emilia Di Francesco Dihydroxypyrimidine carboxamide inhibitors of hiv integrase
DE122009000048I1 (de) 2001-10-26 2010-04-08 Angeletti P Ist Richerche Bio N-substituierte hydroxypyrimidinoncarboxamid-hemmer der hiv-integrase

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3945995A (en) * 1973-04-05 1976-03-23 Sumitomo Chemical Company, Limited D-α-(4-hydroxypyridine-3-carbonamido)-p-hydroxyphenylacetamidopenicillanic acid
US4416884A (en) * 1978-04-12 1983-11-22 Otsuka Pharmaceutical Co., Ltd. Piperazinylbenzoheterocyclic compounds
WO1998011073A1 (en) * 1996-09-10 1998-03-19 Pharmacia & Upjohn Company 8-hydroxy-7-substituted quinolines as anti-viral agents
WO1999016747A1 (en) * 1997-09-30 1999-04-08 Daiichi Pharmaceutical Co., Ltd. Sulfonyl derivatives

Also Published As

Publication number Publication date
CA2425625A1 (en) 2002-07-18
ATE345129T1 (de) 2006-12-15
WO2002055079A2 (en) 2002-07-18
WO2002055079A3 (en) 2002-09-06
US20040044207A1 (en) 2004-03-04
DE60124577D1 (en) 2006-12-28
JP2004517860A (ja) 2004-06-17
DE60124577T2 (de) 2007-09-27
ES2274913T3 (es) 2007-06-01
EP1326610A2 (en) 2003-07-16
EP1326610A4 (en) 2004-06-09
EP1326610B1 (en) 2006-11-15
US6841558B2 (en) 2005-01-11

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Legal Events

Date Code Title Description
FGA Letters patent sealed or granted (standard patent)
MK14 Patent ceased section 143(a) (annual fees not paid) or expired