JP2006506352A - Ｈｉｖインテグラーゼ阻害剤として有用なジヒドロキシピリドピラジン−１，６−ジオン化合物 - Google Patents

Ｈｉｖインテグラーゼ阻害剤として有用なジヒドロキシピリドピラジン−１，６−ジオン化合物 Download PDF

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Publication number
JP2006506352A
JP2006506352A JP2004536438A JP2004536438A JP2006506352A JP 2006506352 A JP2006506352 A JP 2006506352A JP 2004536438 A JP2004536438 A JP 2004536438A JP 2004536438 A JP2004536438 A JP 2004536438A JP 2006506352 A JP2006506352 A JP 2006506352A
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Japan
Prior art keywords
alkyl
haloalkyl
dione
pyrido
dihydroxy
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Withdrawn
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JP2004536438A
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English (en)
Japanese (ja)
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JP2006506352A5 (OSRAM
Inventor
ワイ，ジヨン・エス
キム，ボヤン
フイツシヤー，ソーステン・イー
チユワン，リンハン
ウイリアムズ，ピーター・デイー
ライル，テリー・エイ
ラングフオード，エイチ・マリー
ロビンソン，カイル・エイ
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Merck and Co Inc
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Merck and Co Inc
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Application filed by Merck and Co Inc filed Critical Merck and Co Inc
Publication of JP2006506352A publication Critical patent/JP2006506352A/ja
Publication of JP2006506352A5 publication Critical patent/JP2006506352A5/ja
Withdrawn legal-status Critical Current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
    • C07D471/12—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 three hetero rings
    • C07D471/14—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
    • 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

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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)
  • 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)
JP2004536438A 2002-09-11 2003-09-10 Ｈｉｖインテグラーゼ阻害剤として有用なジヒドロキシピリドピラジン−１，６−ジオン化合物 Withdrawn JP2006506352A (ja)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US40974102P 2002-09-11 2002-09-11
PCT/US2003/028366 WO2004024078A2 (en) 2002-09-11 2003-09-10 Dihydroxypyridopyrazine-1,6-dione compounds useful as hiv integrase inhibitors

Publications (2)

Publication Number Publication Date
JP2006506352A true JP2006506352A (ja) 2006-02-23
JP2006506352A5 JP2006506352A5 (OSRAM) 2006-10-26

Family

ID=31993997

Family Applications (1)

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JP2004536438A Withdrawn JP2006506352A (ja) 2002-09-11 2003-09-10 Ｈｉｖインテグラーゼ阻害剤として有用なジヒドロキシピリドピラジン−１，６−ジオン化合物

Country Status (6)

Country Link
US (1) US7517532B2 (OSRAM)
EP (1) EP1549315A4 (OSRAM)
JP (1) JP2006506352A (OSRAM)
AU (1) AU2003267098B2 (OSRAM)
CA (1) CA2498111A1 (OSRAM)
WO (1) WO2004024078A2 (OSRAM)

Cited By (6)

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JP2005232103A (ja) * 2004-02-20 2005-09-02 Nagase & Co Ltd 光学活性なビシナルジアミンおよびその製造方法
WO2010147068A1 (ja) * 2009-06-15 2010-12-23 塩野義製薬株式会社 置換された多環性カルバモイルピリドン誘導体
JP2014510747A (ja) * 2011-03-31 2014-05-01 ファイザー・インク 新規二環式ピリジノン
JP2015517517A (ja) * 2012-05-16 2015-06-22 ヤンセン ファーマシューティカルズ，インコーポレーテッド （特に）アルツハイマー病の治療に有用な置換３，４−ジヒドロ−２Ｈ−ピリド［１，２−ａ］ピラジン−１，６−ジオン誘導体
JP2016531863A (ja) * 2013-09-27 2016-10-13 メルク・シャープ・アンド・ドーム・コーポレーションＭｅｒｃｋ Ｓｈａｒｐ ＆ Ｄｏｈｍｅ Ｃｏｒｐ． Ｈｉｖインテグラーゼ阻害薬として有用な置換されたキノリジン誘導体
JP2022500406A (ja) * 2018-09-12 2022-01-04 ノバルティス アーゲー 抗ウイルス性ピリドピラジンジオン化合物

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ATE404563T1 (de) * 2002-09-11 2008-08-15 Merck & Co Inc 8-hydroxy-1- oxotetrahydropyrrolopyrazinverbindungen, die sich als inhibitoren von hiv-integrase eignen
TW200510425A (en) 2003-08-13 2005-03-16 Japan Tobacco Inc Nitrogen-containing fused ring compound and use thereof as HIV integrase inhibitor
EP1758585A4 (en) 2004-06-09 2009-07-22 Merck & Co Inc HIV integrase
US7745459B2 (en) 2004-09-21 2010-06-29 Japan Tobacco Inc. Quinolizinone compound and use thereof as HIV integrase inhibitor
WO2006066414A1 (en) * 2004-12-23 2006-06-29 Virochem Pharma Inc. Hydroxydihydropyridopy razine-1,8-diones and methods for inhibiting hiv integrase
ATE516026T1 (de) * 2005-02-21 2011-07-15 Shionogi & Co Bicyclisches carbamoylpyridonderivat mit hiv- integrase-hemmender wirkung
US8008066B2 (en) 2005-03-10 2011-08-30 Gen-Probe Incorporated System for performing multi-formatted assays
EP3187225B1 (en) * 2005-04-28 2022-01-05 VIIV Healthcare Company Polycyclic carbamoylpyridone derivative having hiv integrase inhibitory activity
PH12012502411A1 (en) 2005-05-10 2019-07-17 Intermune Inc Method of modulating stress-activated protein kinase system
CA2625673A1 (en) * 2005-10-27 2007-05-03 Merck & Co., Inc. Hiv integrase inhibitors
KR20080064182A (ko) 2005-10-27 2008-07-08 시오노기세야쿠 가부시키가이샤 Ｈｉｖ 인테그라아제 억제활성을 가지는 다환성카르바모일피리돈 유도체
US8304413B2 (en) 2008-06-03 2012-11-06 Intermune, Inc. Compounds and methods for treating inflammatory and fibrotic disorders
KR101700267B1 (ko) 2008-07-25 2017-01-26 비이브 헬쓰케어 컴퍼니 화합물
PT3617194T (pt) 2008-12-11 2023-11-27 Shionogi & Co Processos e intermediários para inibidores carbamoilpiridona da integrase do vih
CA2744019C (en) 2008-12-11 2017-03-14 Shionogi & Co., Ltd. Synthesis of carbamoylpyridone hiv integrase inhibitors and intermediates
TWI518084B (zh) 2009-03-26 2016-01-21 鹽野義製藥股份有限公司 哌喃酮與吡啶酮衍生物之製造方法
EP2540720B1 (en) * 2010-02-26 2015-04-15 Japan Tobacco, Inc. 1,3,4,8-tetrahydro-2h-pyrido[1,2-a]pyrazine derivative and use of same as hiv integrase inhibitor
TWI582097B (zh) 2010-03-23 2017-05-11 Ｖｉｉｖ醫療保健公司 製備胺甲醯吡啶酮衍生物及中間體之方法
MX2013003139A (es) 2010-09-24 2013-06-18 Shionogi & Co Profarmaco de derivado de carbamoilpiridona policiclica substituida.
US9359300B2 (en) 2010-12-06 2016-06-07 Confluence Life Sciences, Inc. Methyl/difluorophenyl-methoxy substituted pyridinone-pyridinyl compounds, methyl-pyridinyl-methoxy substituted pyridinone-pyridinyl compounds, and methyl-pyrimidinyl-methoxy substituted pyridinone-pyridinyl compounds
EP3469907B1 (en) 2010-12-06 2021-03-03 Aclaris Therapeutics, Inc. Substituted pyridinone-pyridinyl compounds
WO2012104866A1 (en) * 2011-01-31 2012-08-09 Council Of Scientific & Industrial Research Chiral 1-(4-methylphenylmethyl)-5-oxo-{n-[(3-t-butoxycarbonyl- aminomethyl)]-piperidin-1-yl}-pyrrolidine-2-carboxamides as inhibitors of collagen induced platelet activation and adhesion
UA110688C2 (uk) 2012-09-21 2016-01-25 Пфайзер Інк. Біциклічні піридинони
AR092742A1 (es) 2012-10-02 2015-04-29 Intermune Inc Piridinonas antifibroticas
JP6275161B2 (ja) 2012-12-20 2018-02-07 ヤンセン ファーマシューティカ エヌ．ベー． γセクレターゼ調節剤としての新規な三環式３，４−ジヒドロ−２Ｈ−ピリド［１，２−ａ］ピラジン−１，６−ジオン誘導体
AU2013361401C1 (en) 2012-12-21 2018-08-09 Gilead Sciences, Inc. Polycyclic-carbamoylpyridone compounds and their pharmaceutical use
WO2014111457A1 (en) 2013-01-17 2014-07-24 Janssen Pharmaceutica Nv Novel substituted pyrido-piperazinone derivatives as gamma secretase modulators
WO2014172188A2 (en) * 2013-04-16 2014-10-23 Merck Sharp & Dohme Corp. 4-pyridone derivative compounds and uses thereof as hiv integrase inhibitors
US9115089B2 (en) 2013-06-07 2015-08-25 Confluence Life Sciences, Inc. Methyl/fluoro-pyridinyl-methoxy substituted pyridinone-pyridinyl compounds and fluoro-pyrimidinyl-methoxy substituted pyridinone-pyridinyl compounds
PL3019503T3 (pl) 2013-07-12 2018-01-31 Gilead Sciences Inc Policykliczne związki karbamoilopirydonowe i ich zastosowanie do leczenia infekcji hiv
NO2865735T3 (OSRAM) 2013-07-12 2018-07-21
US10562897B2 (en) 2014-01-16 2020-02-18 Janssen Pharmaceutica Nv Substituted 3,4-dihydro-2H-pyrido[1,2-a]pyrazine-1,6-diones as gamma secretase modulators
RU2692485C2 (ru) 2014-04-02 2019-06-25 Интермьюн, Инк. Противофиброзные пиридиноны
TWI677489B (zh) 2014-06-20 2019-11-21 美商基利科學股份有限公司 多環型胺甲醯基吡啶酮化合物之合成
NO2717902T3 (OSRAM) 2014-06-20 2018-06-23
TW201613936A (en) 2014-06-20 2016-04-16 Gilead Sciences Inc Crystalline forms of(2R,5S,13aR)-8-hydroxy-7,9-dioxo-n-(2,4,6-trifluorobenzyl)-2,3,4,5,7,9,13,13a-octahydro-2,5-methanopyrido[1',2':4,5]pyrazino[2,1-b][1,3]oxazepine-10-carboxamide
CN107074880A (zh) * 2014-07-07 2017-08-18 萨维拉制药有限公司 二氢吡啶并吡嗪‑1,8‑二酮和它们在治疗、改善或预防病毒疾病中的用途
TWI738321B (zh) 2014-12-23 2021-09-01 美商基利科學股份有限公司 多環胺甲醯基吡啶酮化合物及其醫藥用途
WO2016125048A1 (en) 2015-02-03 2016-08-11 Pfizer Inc. Novel cyclopropabenzofuranyl pyridopyrazinediones
CN110790773A (zh) 2015-04-02 2020-02-14 吉利德科学公司 多环氨甲酰基吡啶酮化合物及其药物用途
CA2948021C (en) 2015-11-09 2024-06-18 Gilead Sciences, Inc. Pharmaceutical formulations of (2r,5s,13 ar)-8hydroxy-7,9-dioxo-n-(2,4,6-trifluorobenzy1)-2,3,4,5,7,9,13,13a-octahydro-2,5-methanopyrido[1'2':4,5]pyrazino [2,1-b][1,3] oxazepine-10-carboxamide
JP7353707B2 (ja) 2018-05-31 2023-10-02 塩野義製薬株式会社 多環性ピリドン誘導体
MX2020012176A (es) 2018-05-31 2021-01-29 Shionogi & Co Derivado policiclico de carbamoilpiridona.
US20230089442A1 (en) * 2019-03-20 2023-03-23 Pachamuthu Kandasamy Technologies useful for oligonucleotide preparation
CN115666566A (zh) 2020-03-27 2023-01-31 阿克拉瑞斯治疗股份有限公司 用于免疫病况的治疗的mk2途径抑制剂的口服组合物

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WO2000000478A1 (en) 1998-06-26 2000-01-06 Bristol-Myers Squibb Pharma Company Substituted quinoxalin-2(1h)-ones useful as hiv reverse transcriptase inhibitors
IL155089A0 (en) * 2000-10-12 2003-10-31 Merck & Co Inc Aza and polyaza-naphthalenyl carboxamides 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
US20050010048A1 (en) * 2000-10-12 2005-01-13 Linghang Zhuang Aza-and polyaza-naphthalenly ketones useful as hiv integrase inhibitors
CA2425625A1 (en) * 2000-10-12 2002-07-18 Merck & Co., Inc. Aza-and polyaza-naphthalenyl carboxamides useful as hiv integrase inhibitors
DK1441735T3 (da) * 2001-10-26 2006-06-12 Angeletti P Ist Richerche Bio N-substituerede hydroxypyrimidinon-carboxamid-inhibitorer af HIV-integrase
AU2002334205B2 (en) 2001-10-26 2007-07-05 Istituto Di Ricerche Di Biologia Molecolara P. Angeletti Spa Dihydroxypyrimidine carboxamide inhibitors of HIV integrase
ATE404563T1 (de) * 2002-09-11 2008-08-15 Merck & Co Inc 8-hydroxy-1- oxotetrahydropyrrolopyrazinverbindungen, die sich als inhibitoren von hiv-integrase eignen
EP1725102A4 (en) * 2004-03-09 2009-04-29 Merck & Co Inc HIV integrase

Cited By (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2005232103A (ja) * 2004-02-20 2005-09-02 Nagase & Co Ltd 光学活性なビシナルジアミンおよびその製造方法
WO2010147068A1 (ja) * 2009-06-15 2010-12-23 塩野義製薬株式会社 置換された多環性カルバモイルピリドン誘導体
JPWO2010147068A1 (ja) * 2009-06-15 2012-12-06 塩野義製薬株式会社 置換された多環性カルバモイルピリドン誘導体
JP2014510747A (ja) * 2011-03-31 2014-05-01 ファイザー・インク 新規二環式ピリジノン
JP2015517517A (ja) * 2012-05-16 2015-06-22 ヤンセン ファーマシューティカルズ，インコーポレーテッド （特に）アルツハイマー病の治療に有用な置換３，４−ジヒドロ−２Ｈ−ピリド［１，２−ａ］ピラジン−１，６−ジオン誘導体
JP2016531863A (ja) * 2013-09-27 2016-10-13 メルク・シャープ・アンド・ドーム・コーポレーションＭｅｒｃｋ Ｓｈａｒｐ ＆ Ｄｏｈｍｅ Ｃｏｒｐ． Ｈｉｖインテグラーゼ阻害薬として有用な置換されたキノリジン誘導体
JP2017105793A (ja) * 2013-09-27 2017-06-15 メルク・シャープ・アンド・ドーム・コーポレーションＭｅｒｃｋ Ｓｈａｒｐ ＆ Ｄｏｈｍｅ Ｃｏｒｐ． Ｈｉｖインテグラーゼ阻害薬として有用な置換されたキノリジン誘導体
JP2022500406A (ja) * 2018-09-12 2022-01-04 ノバルティス アーゲー 抗ウイルス性ピリドピラジンジオン化合物
JP7273951B2 (ja) 2018-09-12 2023-05-15 ノバルティス アーゲー 抗ウイルス性ピリドピラジンジオン化合物

Also Published As

Publication number Publication date
US7517532B2 (en) 2009-04-14
AU2003267098A1 (en) 2004-04-30
EP1549315A4 (en) 2007-05-23
US20060024330A1 (en) 2006-02-02
AU2003267098B2 (en) 2008-11-20
WO2004024078A2 (en) 2004-03-25
EP1549315A2 (en) 2005-07-06
CA2498111A1 (en) 2004-03-25
WO2004024078A3 (en) 2004-05-13

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