JP3616628B2 - 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 - Google Patents

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 Download PDF

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JP3616628B2
JP3616628B2 JP2002569806A JP2002569806A JP3616628B2 JP 3616628 B2 JP3616628 B2 JP 3616628B2 JP 2002569806 A JP2002569806 A JP 2002569806A JP 2002569806 A JP2002569806 A JP 2002569806A JP 3616628 B2 JP3616628 B2 JP 3616628B2
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JPWO2002070486A1 (ja
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雅弘 冨士
秀勲 三神山
均 村井
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Shionogi and Co Ltd
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    • A61K31/4353Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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  • AIDS & HIV (AREA)
  • Molecular Biology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Quinoline Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
JP2002569806A 2001-03-01 2002-02-27 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 Expired - Fee Related JP3616628B2 (ja)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
JP2001057037 2001-03-01
JP2001057037 2001-03-01
JP2001243530 2001-08-10
JP2001243530 2001-08-10
JP2001395022 2001-12-26
JP2001395022 2001-12-26
PCT/JP2002/001778 WO2002070486A1 (en) 2001-03-01 2002-02-27 Nitrogen-containing heteroaryl compounds having hiv integrase inhibitory activity

Related Child Applications (1)

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JP2004027473A Division JP4367762B2 (ja) 2001-03-01 2004-02-04 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

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JPWO2002070486A1 JPWO2002070486A1 (ja) 2004-07-02
JP3616628B2 true JP3616628B2 (ja) 2005-02-02

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JP2004027473A Expired - Fee Related JP4367762B2 (ja) 2001-03-01 2004-02-04 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

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US (2) US7148237B2 (enExample)
EP (2) EP2033952B1 (enExample)
JP (2) JP3616628B2 (enExample)
KR (1) KR20030078958A (enExample)
CN (1) CN1659143A (enExample)
AT (1) ATE411292T1 (enExample)
BR (1) BR0207809A (enExample)
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Families Citing this family (72)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NZ511255A (en) * 2001-04-20 2003-12-19 Deep Video Imaging Ltd Multi-focal plane display having an optical retarder and a diffuser interposed between its screens
DK3042894T1 (da) 2001-08-10 2016-11-07 Shionogi & Co Antiviralt middel
DE10145457A1 (de) * 2001-09-14 2003-04-03 Basf Ag Substituierte Imidazo[1,2-a]-5,6,7,8-tetrahydropyridin-8-one, Verfahren zu ihrer Herstellung, sowie deren Verwendung zur Herstellung von Imidazo[1,2,-a]pyridinen
DE60209381T2 (de) * 2001-10-26 2006-10-05 Istituto Di Ricerche Di Biologia Molecolare P. Angeletti S.P.A. N-substituierte hydroxypyrimidinoncarboxamid-hemmer der hiv-integrase
SI1441734T1 (sl) * 2001-10-26 2007-08-31 Angeletti P Ist Richerche Bio Dihidropirimidin karboksamidni inhibitorji HIV-integraze
AU2003218130A1 (en) * 2002-03-15 2003-09-29 Merck And Co., Inc. N-(substituted benzyl)-8-hydroxy-1,6-naphthyridine-7- carboxamides useful as hiv integrase inhibitors
DE60322920D1 (de) * 2002-08-13 2008-09-25 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
WO2004046115A1 (ja) 2002-11-20 2004-06-03 Japan Tobacco Inc. 4−オキソキノリン化合物及びそのhivインテグラーゼ阻害剤としての利用
BRPI0407052A (pt) 2003-01-27 2006-01-17 Pfizer Inibidores da hiv-integrase, composições farmacêuticas, e métodos para sua utilização
WO2004101512A2 (en) * 2003-05-13 2004-11-25 Smithkline Beecham Corporation Naphthyridine integrase inhibitors
CN1240700C (zh) * 2003-06-18 2006-02-08 复旦大学 芳杂环羧酸衍生物,制备方法及在药学上的应用
EP1720856B1 (en) 2004-02-11 2013-08-14 GlaxoSmithKline LLC Hiv integrase inhibitors
EP1725556A1 (en) * 2004-03-09 2006-11-29 Merck & Co., Inc. Hiv integrase inhibitors
MXPA06012449A (es) 2004-04-26 2007-01-17 Pfizer Inhibidores de la enzima integrasa de vih.
WO2005103051A1 (en) 2004-04-26 2005-11-03 Pfizer Inc. Inhibitors of the hiv integrase enzyme
WO2005113509A1 (en) * 2004-05-20 2005-12-01 Japan Tobacco Inc. Novel 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
EP2229945A1 (en) 2004-05-21 2010-09-22 Japan Tobacco, Inc. Combinations comprising a 4-isoquinolone derivative and anti-HIV agents
WO2005121132A1 (ja) * 2004-06-11 2005-12-22 Shionogi & Co., Ltd. 抗hcv作用を有する縮合ヘテロ環化合物
RU2007115522A (ru) 2004-10-12 2008-10-27 Декод Дженетикс Ехф (Is) Пери-замещенные бициклические карбоновые кислоты для лечения окклюзионного заболевания артерий
US7674822B2 (en) 2004-11-24 2010-03-09 Wyeth PTP1b inhibitors
WO2006129134A1 (en) * 2005-06-01 2006-12-07 Bioalliance Pharma Synergic combinations comprising a styrylquinoline compound and other hiv infection therapeutic agents
DK1928457T3 (da) * 2005-09-30 2013-02-04 Pulmagen Therapeutics Asthma Ltd Quinoliner og deres terapeutiske anvendelse
CA2622639C (en) * 2005-10-04 2012-01-03 Istituto Di Recerche Di Biologia Molecolare P. Angeletti S.P.A. Hiv integrase inhibitors
JP2009525261A (ja) * 2006-02-01 2009-07-09 日本たばこ産業株式会社 レトロウイルス感染症の治療のための、6−(3−クロロ−2−フルオロベンジル)−1−[(2s)−1−ヒドロキシ−3−メチルブタン−2−イル]−7−メトキシ−4−オキソ−1,4−ジヒドロキノリン−3−カルボン酸またはその塩の使用
AU2007215247B2 (en) * 2006-02-10 2012-12-13 Transtech Pharma, Llc Benzazole derivatives, compositions, and methods of use as Aurora kinase inhibitors
KR101023635B1 (ko) 2006-03-06 2011-03-22 니뽄 다바코 산교 가부시키가이샤 4-옥소퀴놀린 화합물 제조 방법
EP2463283B1 (en) * 2006-04-20 2014-06-11 Pfizer Products Inc. Fused phenyl Amido heterocyclic compounds for the prevention and treatment of glucokinase-mediated diseases
CA2658793A1 (en) * 2006-07-25 2008-02-07 Daniel Dumas Quinoline derivatives
JP5523107B2 (ja) * 2006-11-30 2014-06-18 プロビオドルグ エージー グルタミニルシクラーゼの新規阻害剤
WO2009021083A1 (en) * 2007-08-09 2009-02-12 Smithkline Beecham Corporation Quinoxaline derivatives as pi3 kinase inhibitors
CN102271511A (zh) * 2008-10-29 2011-12-07 默沙东公司 可用作抗糖尿病剂的新颖的环状苯并咪唑衍生物
FR2938538B1 (fr) * 2008-11-17 2011-08-05 Univ Nice Sophia Antipolis Procede de preparation d'acides et d'esters boroniques en presence de magnesium metallique
GB0908394D0 (en) 2009-05-15 2009-06-24 Univ Leuven Kath Novel viral replication inhibitors
EP2845856A1 (en) 2009-06-29 2015-03-11 Incyte Corporation Pyrimidinones as PI3K inhibitors
GB0913636D0 (en) 2009-08-05 2009-09-16 Univ Leuven Kath Novel viral replication inhibitors
US8759359B2 (en) * 2009-12-18 2014-06-24 Incyte Corporation Substituted heteroaryl fused derivatives as PI3K inhibitors
WO2011075630A1 (en) * 2009-12-18 2011-06-23 Incyte Corporation Substituted fused aryl and heteroaryl derivatives as pi3k inhibitors
KR101483834B1 (ko) * 2009-12-23 2015-01-16 카트호리이케 유니버시타이트 로이펜 항바이러스 화합물
EP2345641A1 (en) 2009-12-29 2011-07-20 Polichem S.A. New secondary 8-hydroxyquinoline-7-carboxamide derivatives
EP2345643A1 (en) 2009-12-29 2011-07-20 Polichem S.A. New tertiary 8-hydroxyquinoline-7-carboxamide derivatives and uses thereof
EP2345642A1 (en) * 2009-12-29 2011-07-20 Polichem S.A. Secondary 8-hydroxyquinoline-7-carboxamide derivatives for use as antifungal agents
JP6026284B2 (ja) * 2010-03-03 2016-11-16 プロビオドルグ エージー グルタミニルシクラーゼの阻害剤
EP2558463A1 (en) 2010-04-14 2013-02-20 Incyte Corporation Fused derivatives as i3 inhibitors
WO2011163195A1 (en) 2010-06-21 2011-12-29 Incyte Corporation Fused pyrrole derivatives as pi3k inhibitors
KR101789129B1 (ko) 2010-06-30 2017-11-20 후지필름 가부시키가이샤 신규 니코틴아미드 유도체 또는 그 염
US8633200B2 (en) * 2010-09-08 2014-01-21 Bristol-Myers Squibb Company Inhibitors of human immunodeficiency virus replication
BR112013011737A2 (pt) 2010-11-15 2016-08-09 Univ Leuven Kath composto, uso de um composto composição farmacêutica, e, método de tratamento ou prevenção de uma infecção por hiv
TW201249844A (en) 2010-12-20 2012-12-16 Incyte Corp N-(1-(substituted-phenyl)ethyl)-9H-purin-6-amines as PI3K inhibitors
WO2012125629A1 (en) 2011-03-14 2012-09-20 Incyte Corporation Substituted diamino-pyrimidine and diamino-pyridine derivatives as pi3k inhibitors
US9126948B2 (en) 2011-03-25 2015-09-08 Incyte Holdings Corporation Pyrimidine-4,6-diamine derivatives as PI3K inhibitors
UA121539C2 (uk) 2011-09-02 2020-06-25 Інсайт Холдинґс Корпорейшн Гетероцикліламіни як інгібітори рі3к
CA3131037A1 (en) 2011-11-30 2013-06-06 Emory University Antiviral jak inhibitors useful in treating or preventing retroviral and other viral infections
AR090548A1 (es) 2012-04-02 2014-11-19 Incyte Corp Azaheterociclobencilaminas biciclicas como inhibidores de pi3k
WO2015004533A2 (en) 2013-06-21 2015-01-15 Zenith Epigenetics Corp. Novel substituted bicyclic compounds as bromodomain inhibitors
SG11201510409QA (en) * 2013-06-21 2016-01-28 Zenith Epigenetics Corp Novel bicyclic bromodomain inhibitors
AU2014298051B2 (en) 2013-07-31 2018-11-15 Zenith Epigenetics Ltd. Novel quinazolinones as bromodomain inhibitors
CN103554019B (zh) * 2013-09-30 2015-08-05 浙江工业大学 一种甲溴羟喹的合成方法
CN104140402B (zh) * 2014-05-27 2016-01-20 天津市斯芬克司药物研发有限公司 一种苯并噻唑类化合物及其制备方法
US10077277B2 (en) 2014-06-11 2018-09-18 Incyte Corporation Bicyclic heteroarylaminoalkyl phenyl derivatives as PI3K inhibitors
CN104447547B (zh) * 2014-11-10 2017-04-19 苏州康润医药有限公司 4‑氨基异喹啉‑8‑甲酸甲酯的合成方法
CN104447543B (zh) * 2014-11-10 2016-08-24 苏州康润医药有限公司 3-氨基-7,8-二氟喹啉及其中间体的合成方法
WO2016087936A1 (en) 2014-12-01 2016-06-09 Zenith Epigenetics Corp. Substituted pyridinones as bromodomain inhibitors
CN107207474B (zh) 2014-12-11 2021-05-07 恒翼生物医药科技(上海)有限公司 被取代的杂环作为溴结构域抑制剂
CA2966450A1 (en) 2014-12-17 2016-06-23 Olesya KHARENKO Inhibitors of bromodomains
UA122332C2 (uk) 2015-02-27 2020-10-26 Інсайт Корпорейшн Солі інгібітора pi3k і способи їх отримання
WO2016183060A1 (en) 2015-05-11 2016-11-17 Incyte Corporation Process for the synthesis of a phosphoinositide 3-kinase inhibitor
WO2016183063A1 (en) 2015-05-11 2016-11-17 Incyte Corporation Crystalline forms of a pi3k inhibitor
MX2020012826A (es) 2018-06-01 2021-03-09 Incyte Corp Regimen de dosificacion para el tratamiento de trastornos relacionados con fosfatidilinositol 3-cinasas (pi3k).
WO2020061103A1 (en) 2018-09-18 2020-03-26 Nikang Therapeutics, Inc. Fused tricyclic ring derivatives as src homology-2 phosphatase inhibitors
WO2025264844A1 (en) * 2024-06-20 2025-12-26 Lieber Institute, Inc. Heterocyclic gpr52 modulators and methods of use thereof

Family Cites Families (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CH370082A (de) * 1958-12-06 1963-06-30 Geigy Ag J R Verfahren zur Herstellung von neuen N-heterocyclischen Verbindungen
CH385846A (de) 1960-03-31 1964-12-31 Geigy Ag J R Verfahren zur Herstellung von neuen 7-Acyl-8-hydroxy-chinolinen und ihre Verwendung als Fungizide und Bakterizide im Pflanzen- und Materialschutz
JPS5417754B2 (enExample) * 1972-12-15 1979-07-02
JPS587637B2 (ja) * 1973-12-27 1983-02-10 住友化学工業株式会社 シンキペニシリンノ セイホウ
JPS5227794A (en) 1975-08-29 1977-03-02 Sumitomo Chem Co Ltd Preparation of synthesis of nnacylaminoo arylacetamido cephalosporin s
JPS5268193A (en) 1975-11-28 1977-06-06 Sumitomo Chem Co Ltd Synthesis of novel cephalosporin derivatives
JPS5293790A (en) 1976-02-02 1977-08-06 Sumitomo Chem Co Ltd 7-(n-acylamino-alpha-arylacetamide) cephalosporins
JPH0527385A (ja) 1991-07-24 1993-02-05 Fuji Photo Film Co Ltd ハロゲン化銀カラー写真感光材料
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
US6310211B1 (en) * 1996-09-10 2001-10-30 Pharmacia & Upjohn Company 8-hydroxy-7-substituted quinolines as anti-viral agents
FR2761687B1 (fr) 1997-04-08 2000-09-15 Centre Nat Rech Scient Derives de quinoleines, possedant notamment des proprietes antivirales, leurs preparations et leurs applications biologiques
EP1069111A4 (en) 1998-03-26 2001-06-06 Shionogi & Co INDOLE DERIVATIVES EXER ANT ANTIVIRAL ACTIVITY
AU757409B2 (en) 1998-06-03 2003-02-20 Merck & Co., Inc. Hiv integrase inhibitors
CA2329134A1 (en) 1998-06-03 1999-12-09 David L. Clark Hiv integrase inhibitors
WO1999062520A1 (en) 1998-06-03 1999-12-09 Merck & Co., Inc. Hiv integrase inhibitors
JP2003503386A (ja) 1999-06-25 2003-01-28 メルク エンド カムパニー インコーポレーテッド 1−(芳香族またはヘテロ芳香族置換)−3−(ヘテロ芳香族置換)−1,3−プロパンジオン類およびそれの使用
US6730682B2 (en) 2000-07-12 2004-05-04 Pharmacia & Upjohn Company Heterocycle carboxamides as antiviral agents
WO2002036734A2 (en) 2000-10-12 2002-05-10 Merck & Co., Inc. Aza-and polyaza-naphthalenyl ketones useful as hiv integrase inhibitors
AU1532802A (en) * 2000-10-12 2002-04-22 Merck & Co Inc Aza- and polyaza-naphthalenyl-carboxamides useful as hiv integrase inhibitors
ATE430745T1 (de) 2000-10-12 2009-05-15 Merck & Co Inc Aza- und polyaza naphthalenyl karboxamide als inhibitoren der hiv-integrase
DE60124577T2 (de) 2000-10-12 2007-09-27 Merck & Co., Inc. Aza- und polyaza-naphthalenylcarbonsäureamide als hiv-integrase-hemmer

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CA2439666A1 (en) 2002-09-12
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