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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Prior art keywords
alkyl
haloalkyl
dione
pyrido
dihydroxy
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JP2004536438A
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Japanese (ja)
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JP2006506352A5 (enExample
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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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Withdrawn legal-status Critical Current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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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Virology (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Molecular Biology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (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)
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 (enExample) 2006-10-26

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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 (enExample)
EP (1) EP1549315A4 (enExample)
JP (1) JP2006506352A (enExample)
AU (1) AU2003267098B2 (enExample)
CA (1) CA2498111A1 (enExample)
WO (1) WO2004024078A2 (enExample)

Cited By (6)

* Cited by examiner, † Cited by third party
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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
CN101146540A (zh) 2004-06-09 2008-03-19 默克公司 Hiv整合酶抑制剂
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
EP1852434B1 (en) * 2005-02-21 2011-07-13 Shionogi Co., Ltd. Bicyclic carbamoylpyridone derivative having hiv integrase inhibiting activity
US7932081B2 (en) 2005-03-10 2011-04-26 Gen-Probe Incorporated Signal measuring system for conducting real-time amplification assays
KR101580310B1 (ko) 2005-04-28 2016-01-04 비이브 헬쓰케어 컴퍼니 Ｈｉｖ 통합효소 억제 활성을 가지는 다환식 카르바모일피리돈 유도체
BRPI0608907A2 (pt) 2005-05-10 2010-02-17 Itermune Inc método de modulação de sistema de proteìna cinase ativada por estresse
EP1942736A2 (en) * 2005-10-27 2008-07-16 Merck & Co., Inc. Hiv integrase inhibitors
CA2626956A1 (en) 2005-10-27 2007-05-03 Shionogi & Co., Ltd. Polycyclic carbamoylpyridone derivative having hiv integrase inhibitory activity
EP2296653B1 (en) 2008-06-03 2016-01-27 Intermune, Inc. Compounds and methods for treating inflammatory and fibrotic disorders
KR101700267B1 (ko) 2008-07-25 2017-01-26 비이브 헬쓰케어 컴퍼니 화합물
CN102245182B (zh) 2008-12-11 2014-07-23 盐野义制药株式会社 氨基甲酰基吡啶酮hiv整合酶抑制剂和中间体的合成
CN107011260A (zh) 2008-12-11 2017-08-04 盐野义制药株式会社 氨甲酰基吡啶酮hiv整合酶抑制剂的方法和中间体
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
AR080314A1 (es) * 2010-02-26 2012-03-28 Japan Tobacco Inc Derivado de 1,3,4,8-tetrahidro-2h-pirido (1,2-a) pirazina y su uso como inhibidor de la hiv integrasa
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
RS57490B1 (sr) 2010-09-24 2018-10-31 Shionogi & Co Supstituisani prolek derivata policikličnog karbamoil piridona
CA2819889C (en) 2010-12-06 2020-12-15 Confluence Life Sciences, Inc. Substituted pyridinone-pyridinyl compounds
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
EP2670722B1 (en) * 2011-01-31 2016-10-12 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
CA2889249C (en) 2012-12-20 2021-02-16 Francois Paul Bischoff Tricyclic 3,4-dihydro-2h-pyrido[1,2-a]pyrazine-1,6-dione derivatives as gamma secretase modulators
NZ709260A (en) 2012-12-21 2016-07-29 Gilead Sciences Inc Polycyclic-carbamoylpyridone compounds and their pharmaceutical use
AU2014206834B2 (en) 2013-01-17 2017-06-22 Janssen Pharmaceutica Nv Novel substituted pyrido-piperazinone derivatives as gamma secretase modulators
EP2986291B1 (en) 2013-04-16 2020-05-27 Merck Sharp & Dohme Corp. 4-pyridone derivative compounds and uses thereof as hiv integrase inhibitors
PT3003039T (pt) 2013-06-07 2021-03-04 Aclaris Therapeutics Inc Compostos piridinona-piridinilo substituídos com metil/fluoro-piridinil-metoxilo e compostos piridinona-pirimidinilo substituídos com fluoro-pirimidinil-metoxilo
NO2865735T3 (enExample) 2013-07-12 2018-07-21
ES2859102T3 (es) 2013-07-12 2021-10-01 Gilead Sciences Inc Compuestos de carbamoilpiridona policíclica y su uso para el tratamiento de infecciones por VIH
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
NO2717902T3 (enExample) 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
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
CA2953862A1 (en) * 2014-07-07 2016-01-14 F. Hoffmann-La Roche Ag Dihydropyridopyrazine-1,8-diones and their use in the treatment, amelioration or prevention of viral diseases
TWI695003B (zh) 2014-12-23 2020-06-01 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
DK3253755T3 (da) 2015-02-03 2020-09-28 Pfizer Hidtil ukendte cyclopropabenzofuranyl-pyridopyrazindioner
SI3466490T1 (sl) 2015-04-02 2020-12-31 Gilead Sciences, Inc. Policiklične spojine karbamoilpiridona in njihova farmacevtska uporaba
CN113546052A (zh) 2015-11-09 2021-10-26 吉利德科学公司 治疗人免疫缺陷病毒的治疗组合物
IL313474A (en) 2018-05-31 2024-08-01 Shionogi & Co Polycyclic carbamoylpyridone derivative
SG11202011386QA (en) 2018-05-31 2020-12-30 Shionogi & Co Polycyclic pyridone derivative
CA3134036A1 (en) * 2019-03-20 2020-09-24 Wave Life Sciences Ltd. 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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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
US7820680B2 (en) * 2004-03-09 2010-10-26 Merck & Co., Inc. HIV integrase inhibitors

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

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