WO2002055079A2 - 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
WO2002055079A2
WO2002055079A2 PCT/US2001/042565 US0142565W WO02055079A2 WO 2002055079 A2 WO2002055079 A2 WO 2002055079A2 US 0142565 W US0142565 W US 0142565W WO 02055079 A2 WO02055079 A2 WO 02055079A2
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WO
WIPO (PCT)
Prior art keywords
alkyl
substituted
sep
fluoroalkyl
ora
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
PCT/US2001/042565
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English (en)
French (fr)
Other versions
WO2002055079A3 (en
Inventor
Neville J Anthony
Robert P Gomez
Jennifer J Bennett
Steven D Young
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
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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
Priority to CA002425625A priority Critical patent/CA2425625A1/en
Priority to DE60124577T priority patent/DE60124577T2/de
Priority to US10/398,988 priority patent/US6841558B2/en
Priority to JP2002555813A priority patent/JP2004517860A/ja
Priority to EP01994068A priority patent/EP1326610B1/en
Priority to AU2002246499A priority patent/AU2002246499B2/en
Publication of WO2002055079A2 publication Critical patent/WO2002055079A2/en
Publication of WO2002055079A3 publication Critical patent/WO2002055079A3/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)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Virology (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • AIDS & HIV (AREA)
  • Engineering & Computer Science (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)
  • Indole Compounds (AREA)
  • Decoration By Transfer Pictures (AREA)
  • Compression Or Coding Systems Of Tv Signals (AREA)
  • Pyrrole Compounds (AREA)
PCT/US2001/042565 2000-10-12 2001-10-09 Aza-and polyaza-naphthalenyl carboxamides useful as hiv integrase inhibitors Ceased WO2002055079A2 (en)

Priority Applications (6)

Application Number Priority Date Filing Date Title
CA002425625A CA2425625A1 (en) 2000-10-12 2001-10-09 Aza-and polyaza-naphthalenyl carboxamides useful as hiv integrase inhibitors
DE60124577T DE60124577T2 (de) 2000-10-12 2001-10-09 Aza- und polyaza-naphthalenylcarbonsäureamide als hiv-integrase-hemmer
US10/398,988 US6841558B2 (en) 2000-10-12 2001-10-09 Aza-and polyaza-naphthalenyl carboxamides useful as HIV intergrase inhibitors
JP2002555813A JP2004517860A (ja) 2000-10-12 2001-10-09 Ｈｉｖインテグラーゼ阻害薬として有用なアザ−およびポリアザ−ナフタレニルカルボキサミド類
EP01994068A EP1326610B1 (en) 2000-10-12 2001-10-09 Aza-and polyaza-naphthalenyl carboxamides useful as hiv integrase inhibitors
AU2002246499A AU2002246499B2 (en) 2000-10-12 2001-10-09 Aza-and polyaza-naphthalenyl carboxamides useful as HIV integrase inhibitors

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US23967900P 2000-10-12 2000-10-12
US60/239,679 2000-10-12

Publications (2)

Publication Number Publication Date
WO2002055079A2 true WO2002055079A2 (en) 2002-07-18
WO2002055079A3 WO2002055079A3 (en) 2002-09-06

Family

ID=22903252

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2001/042565 Ceased WO2002055079A2 (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 (https=)
EP (1) EP1326610B1 (https=)
JP (1) JP2004517860A (https=)
AT (1) ATE345129T1 (https=)
AU (1) AU2002246499B2 (https=)
CA (1) CA2425625A1 (https=)
DE (1) DE60124577T2 (https=)
ES (1) ES2274913T3 (https=)
WO (1) WO2002055079A2 (https=)

Cited By (32)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004096807A3 (en) * 2003-04-28 2005-01-06 Tibotec Pharm Ltd Hiv integrase inhibitors
WO2005028478A1 (en) * 2003-09-19 2005-03-31 Gilead Sciences, Inc. Aza-quinolinol phosphonate integrase inhibitor compounds
WO2005087766A1 (en) 2004-03-09 2005-09-22 Istituto Di Ricerche Di Biologia Molecolare P Angeletti Spa Hiv integrase inhibitors
EP1544199A4 (en) * 2003-08-13 2006-07-26 Japan Tobacco Inc NITROGEN CONDENSED NITROGEN COMPOUND AND ITS USE AS INHIBITOR OF HIV INTEGRASE
US7148237B2 (en) 2001-03-01 2006-12-12 Shionogi & Co., Ltd. Nitrogen-containing heteroaryl compounds having HIV integrase inhibitory activity
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
US7176220B2 (en) 2002-11-20 2007-02-13 Japan Tobacco Inc. 4-oxoquinoline compound and use thereof as pharmaceutical agent
WO2007059229A1 (en) * 2005-11-16 2007-05-24 Bristol-Myers Squibb Company Hiv integrase inhibitors
US7253180B2 (en) 2002-10-16 2007-08-07 Gilead Sciences, Inc. Pre-organized tricyclic integrase inhibitor compounds
US7358249B2 (en) 2002-08-13 2008-04-15 Shionogi & Co., Ltd. Heterocyclic compounds having inhibitory activity against HIV integrase
US7399763B2 (en) 2002-09-11 2008-07-15 Merck & Co., Inc. 8-hydroxy-1-oxo-tetrahydropyrrolopyrazine compounds useful as HIV integrase inhibitors
US7414045B2 (en) 2002-12-27 2008-08-19 Istituto Di Ricerche Di Biologia Molecolare P. Angeletti S.P.A. Substituted pyrimido[1,2-a]azepines useful as HIV integrase inhibitors
US7435735B2 (en) 2003-10-20 2008-10-14 Merck & Co., Inc. Hydroxy pyridopyrrolopyrazine dione compounds useful as HIV integrase inhibitors
US7476666B2 (en) 2004-06-09 2009-01-13 Merck & Co., Inc. HIV integrase inhibitors
US7517532B2 (en) 2002-09-11 2009-04-14 Merck & Co., Inc. Dihydroxypyridopyrazine-1,6-dione compounds useful as HIV integrase inhibitors
US7531554B2 (en) 2004-05-20 2009-05-12 Japan Tobacco Inc. 4-oxoquinoline compound and use thereof as HIV integrase inhibitor
WO2009094190A2 (en) 2008-01-25 2009-07-30 Chimerix, Inc. Methods of treating viral infections
US7598264B2 (en) 2004-03-09 2009-10-06 Merck & Co., Inc. HIV integrase inhibitors
US7619086B2 (en) 2004-03-09 2009-11-17 Merck & Co., Inc. HIV integrase inhibitors
US7635704B2 (en) 2004-05-20 2009-12-22 Japan Tobacco Inc. Stable crystal of 4-oxoquinoline compound
EP2229945A1 (en) 2004-05-21 2010-09-22 Japan Tobacco, Inc. Combinations comprising a 4-isoquinolone derivative and anti-HIV agents
US7820680B2 (en) 2004-03-09 2010-10-26 Merck & Co., Inc. HIV integrase inhibitors
WO2011020822A1 (de) * 2009-08-17 2011-02-24 Aicuris Gmbh & Co. Kg Substituierte (thiazolyl-carbonyl) imidazolidinone und ihre verwendung zur behandlung von retroviralen krankheiten
WO2011045330A1 (en) 2009-10-13 2011-04-21 Tibotec Pharmaceuticals Macrocyclic integrase inhibitors
US8008287B2 (en) 2006-05-16 2011-08-30 Gilead Sciences, Inc. Integrase inhibitors
WO2011121105A1 (en) 2010-04-02 2011-10-06 Tibotec Pharmaceuticals Macrocyclic 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
US8217042B2 (en) 2005-11-11 2012-07-10 Zentaris Gmbh Pyridopyrazines and their use as modulators of kinases
US8383819B2 (en) 2006-03-06 2013-02-26 Japan Tobacco Inc. Method for producing 4-oxoquinoline compound
US8691991B2 (en) 2004-02-11 2014-04-08 Shionogi & Co., Ltd. 2-oxonaphthyridine-3-carboxamides HIV integrase inhibitors
US8937068B2 (en) 2005-11-11 2015-01-20 Zentaris Gmbh Pyridopyrazine derivatives and their use
EP3216789A1 (en) 2010-02-12 2017-09-13 Chimerix, Inc. Methods of treating viral infection

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NZ533057A (en) * 2001-10-26 2005-11-25 Angeletti P Ist Richerche Bio N-substituted hydroxypyrimidinone carboxamide inhibitors of HIV integrase
EP1441734B1 (en) * 2001-10-26 2007-02-28 Istituto di Richerche di Biologia Molecolare P. Angeletti S.p.A. Dihydroxypyrimidine carboxamide inhibitors of 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
ES2529038T3 (es) * 2004-05-07 2015-02-16 Merck Sharp & Dohme Corp. Inhibidores de la integrasa de VIH
CN101146811B (zh) * 2005-03-31 2012-01-11 P.安杰莱蒂分子生物学研究所 Hiv整合酶抑制剂
CA2607151C (en) * 2005-05-10 2012-06-19 Merck & Co., Inc. Hiv integrase inhibitors
CA2622639C (en) * 2005-10-04 2012-01-03 Istituto Di Recerche Di Biologia Molecolare P. Angeletti S.P.A. Hiv integrase inhibitors
JP2009513640A (ja) * 2005-10-27 2009-04-02 メルク エンド カムパニー インコーポレーテッド Ｈｉｖインテグラーゼインヒビター
US20100056516A1 (en) * 2006-07-17 2010-03-04 Williams Peter D 1-hydroxy naphthyridine compounds as anti-hiv agents
KR20090077813A (ko) 2006-09-29 2009-07-15 아이데닉스 파마슈티칼스, 인코포레이티드 Ｈｉｖ 억제제로서의 거울상이성질체적으로 순수한 포스포인돌
WO2008048538A1 (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
US9029391B2 (en) 2011-01-24 2015-05-12 Viiv Healthcare Uk Limited Isoquinoline compounds and methods for treating HIV
JP2016524607A (ja) 2013-05-16 2016-08-18 ザ ユナイテッド ステイツ オブ アメリカ， アズ リプレゼンテッド バイ ザ セクレタリー， デパートメント オブ ヘルス アンド ヒューマン サービシーズ Ｈｉｖ−１インテグラーゼの薬物耐性株を阻害するための化合物

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IL101860A0 (en) * 1991-05-31 1992-12-30 Ici Plc Heterocyclic derivatives
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Cited By (51)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7759372B2 (en) 2001-03-01 2010-07-20 Shionogi & Co., Ltd. Nitrogen-containing heteroaryl compounds having inhibitory activity against HIV integrase
US7148237B2 (en) 2001-03-01 2006-12-12 Shionogi & Co., Ltd. Nitrogen-containing heteroaryl compounds having HIV integrase inhibitory activity
EP2045242A1 (en) 2002-08-13 2009-04-08 Shionogi&Co., Ltd. Heterocyclic compounds having inhibitory activity against HIV integrase
US7358249B2 (en) 2002-08-13 2008-04-15 Shionogi & Co., Ltd. Heterocyclic compounds having inhibitory activity against HIV integrase
US7517532B2 (en) 2002-09-11 2009-04-14 Merck & Co., Inc. Dihydroxypyridopyrazine-1,6-dione compounds useful as HIV integrase inhibitors
US7399763B2 (en) 2002-09-11 2008-07-15 Merck & Co., Inc. 8-hydroxy-1-oxo-tetrahydropyrrolopyrazine compounds useful as HIV integrase inhibitors
US7253180B2 (en) 2002-10-16 2007-08-07 Gilead Sciences, Inc. Pre-organized tricyclic integrase inhibitor compounds
US8232401B2 (en) 2002-11-20 2012-07-31 Japan Tobacco Inc. 4-oxoquinoline compound and use thereof as HIV integrase inhibitor
EP2161258A2 (en) 2002-11-20 2010-03-10 Japan Tabacco Inc. 4-oxoquinoline compound and use thereof as hiv integrase inhibitor
US7176220B2 (en) 2002-11-20 2007-02-13 Japan Tobacco Inc. 4-oxoquinoline compound and use thereof as pharmaceutical agent
EP2272516A2 (en) 2002-11-20 2011-01-12 Japan Tobacco, Inc. 4-Oxoquinoline compound and use thereof as HIV integrase inhibitor
EP3406596A1 (en) 2002-11-20 2018-11-28 Japan Tobacco Inc. 4-oxoquinoline compound and use thereof as hiv integrase inhibitor
EP4059923A1 (en) 2002-11-20 2022-09-21 Japan Tobacco Inc. 4-oxoquinoline compound and use thereof as hiv integrase inhibitor
US7414045B2 (en) 2002-12-27 2008-08-19 Istituto Di Ricerche Di Biologia Molecolare P. Angeletti S.P.A. Substituted pyrimido[1,2-a]azepines useful as HIV integrase inhibitors
US7968553B2 (en) 2002-12-27 2011-06-28 Istituto Di Ricerche Di Biologia Molecolare P. Angeletti S.P.A. Tetrahydro-4H-pyrido[1,2-a] pyrimidines useful as HIV integrase inhibitors
WO2004096807A3 (en) * 2003-04-28 2005-01-06 Tibotec Pharm Ltd Hiv integrase inhibitors
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
US7812016B2 (en) 2003-05-13 2010-10-12 Smithkline Beecham Corporation Naphthyridine integrase inhibitors
US7211572B2 (en) 2003-08-13 2007-05-01 Japan Tobacco Inc. Nitrogen-containing fused ring compound and use thereof as HIV integrase inhibitor
EP2042502A1 (en) 2003-08-13 2009-04-01 Japan Tobacco Inc. Nitrogen-containing fused ring compound and use thereof as HIV integrase inhibitor
EP1544199A4 (en) * 2003-08-13 2006-07-26 Japan Tobacco Inc NITROGEN CONDENSED NITROGEN COMPOUND AND ITS USE AS INHIBITOR OF HIV INTEGRASE
WO2005028478A1 (en) * 2003-09-19 2005-03-31 Gilead Sciences, Inc. Aza-quinolinol phosphonate integrase inhibitor compounds
US7462721B2 (en) 2003-09-19 2008-12-09 Gilead Sciences, Inc. Aza-quinolinol phosphonate integrase inhibitor compounds
US7435735B2 (en) 2003-10-20 2008-10-14 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
US8691991B2 (en) 2004-02-11 2014-04-08 Shionogi & Co., Ltd. 2-oxonaphthyridine-3-carboxamides HIV integrase inhibitors
US7820680B2 (en) 2004-03-09 2010-10-26 Merck & Co., Inc. HIV integrase inhibitors
US7619086B2 (en) 2004-03-09 2009-11-17 Merck & Co., Inc. HIV integrase inhibitors
US7598264B2 (en) 2004-03-09 2009-10-06 Merck & Co., Inc. HIV integrase inhibitors
WO2005087766A1 (en) 2004-03-09 2005-09-22 Istituto Di Ricerche Di Biologia Molecolare P Angeletti Spa Hiv integrase inhibitors
US8981103B2 (en) 2004-05-20 2015-03-17 Japan Tobacco Inc. Stable crystal of 4-oxoquinoline compound
US7635704B2 (en) 2004-05-20 2009-12-22 Japan Tobacco Inc. Stable crystal of 4-oxoquinoline compound
US7531554B2 (en) 2004-05-20 2009-05-12 Japan Tobacco Inc. 4-oxoquinoline compound and use thereof as HIV integrase inhibitor
EP2332538A1 (en) 2004-05-21 2011-06-15 Japan Tobacco, Inc. Combinations comprising a 4-isoquinolone derivative and anti-HIV agents
EP3287130A1 (en) 2004-05-21 2018-02-28 Japan Tobacco Inc. Combinations comprising a 4-isoquinolone derivative and protease inhibitors
US8633219B2 (en) 2004-05-21 2014-01-21 Japan Tobacco Inc. Combination therapy
EP2229945A1 (en) 2004-05-21 2010-09-22 Japan Tobacco, Inc. Combinations comprising a 4-isoquinolone derivative and anti-HIV agents
US7476666B2 (en) 2004-06-09 2009-01-13 Merck & Co., Inc. HIV integrase inhibitors
US8937068B2 (en) 2005-11-11 2015-01-20 Zentaris Gmbh Pyridopyrazine derivatives and their use
US8217042B2 (en) 2005-11-11 2012-07-10 Zentaris Gmbh Pyridopyrazines and their use as modulators of kinases
WO2007059229A1 (en) * 2005-11-16 2007-05-24 Bristol-Myers Squibb Company Hiv integrase inhibitors
US8383819B2 (en) 2006-03-06 2013-02-26 Japan Tobacco Inc. Method for producing 4-oxoquinoline compound
US8008287B2 (en) 2006-05-16 2011-08-30 Gilead Sciences, Inc. Integrase inhibitors
EP3085377A1 (en) 2008-01-25 2016-10-26 Chimerix, Inc. Methods of treating viral infections
WO2009094190A2 (en) 2008-01-25 2009-07-30 Chimerix, Inc. Methods of treating viral infections
US8575357B2 (en) 2009-08-17 2013-11-05 Aicuris Gmbh & Co. Kg Substituted (thiazolyl-carbonyl)imidazolidinones and use thereof
WO2011020822A1 (de) * 2009-08-17 2011-02-24 Aicuris Gmbh & Co. Kg Substituierte (thiazolyl-carbonyl) imidazolidinone und ihre verwendung zur behandlung von retroviralen krankheiten
WO2011045330A1 (en) 2009-10-13 2011-04-21 Tibotec Pharmaceuticals Macrocyclic integrase inhibitors
EP3216789A1 (en) 2010-02-12 2017-09-13 Chimerix, Inc. Methods of treating viral infection
US8716293B2 (en) 2010-04-02 2014-05-06 Janssen R&D Ireland Macrocyclic integrase inhibitors
WO2011121105A1 (en) 2010-04-02 2011-10-06 Tibotec Pharmaceuticals Macrocyclic integrase inhibitors

Also Published As

Publication number Publication date
DE60124577T2 (de) 2007-09-27
ES2274913T3 (es) 2007-06-01
CA2425625A1 (en) 2002-07-18
US20040044207A1 (en) 2004-03-04
JP2004517860A (ja) 2004-06-17
ATE345129T1 (de) 2006-12-15
EP1326610A4 (en) 2004-06-09
AU2002246499B2 (en) 2005-12-22
EP1326610B1 (en) 2006-11-15
WO2002055079A3 (en) 2002-09-06
EP1326610A2 (en) 2003-07-16
US6841558B2 (en) 2005-01-11
DE60124577D1 (en) 2006-12-28

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