JP2009537546A - インテグラーゼ阻害剤 - Google Patents

インテグラーゼ阻害剤 Download PDF

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Publication number
JP2009537546A
JP2009537546A JP2009511069A JP2009511069A JP2009537546A JP 2009537546 A JP2009537546 A JP 2009537546A JP 2009511069 A JP2009511069 A JP 2009511069A JP 2009511069 A JP2009511069 A JP 2009511069A JP 2009537546 A JP2009537546 A JP 2009537546A
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JP
Japan
Prior art keywords
alkyl
compound
mmol
optionally substituted
substituted
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JP2009511069A
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English (en)
Japanese (ja)
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JP2009537546A5 (https=
Inventor
チェンホン アール. カイ,
サルマン ワイ. ジャブリ,
ハオルン チン,
レイチェル エー. ランズダウン,
サミュエル イー. メトボ,
マイケル エル. ミッシュ,
リチャード パストール,
Original Assignee
ギリアード サイエンシーズ, インコーポレイテッド
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Application filed by ギリアード サイエンシーズ, インコーポレイテッド filed Critical ギリアード サイエンシーズ, インコーポレイテッド
Publication of JP2009537546A publication Critical patent/JP2009537546A/ja
Publication of JP2009537546A5 publication Critical patent/JP2009537546A5/ja
Pending legal-status Critical Current

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic 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
    • C07D471/02Heterocyclic 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
    • C07D471/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/04Immunostimulants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

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  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Virology (AREA)
  • Immunology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Molecular Biology (AREA)
  • AIDS & HIV (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
JP2009511069A 2006-05-16 2007-05-16 インテグラーゼ阻害剤 Pending JP2009537546A (ja)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US80102006P 2006-05-16 2006-05-16
PCT/US2007/011851 WO2007136714A2 (en) 2006-05-16 2007-05-16 Integrase inhibitors

Publications (2)

Publication Number Publication Date
JP2009537546A true JP2009537546A (ja) 2009-10-29
JP2009537546A5 JP2009537546A5 (https=) 2011-06-16

Family

ID=38573219

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2009511069A Pending JP2009537546A (ja) 2006-05-16 2007-05-16 インテグラーゼ阻害剤

Country Status (7)

Country Link
US (2) US20090306054A1 (https=)
EP (1) EP2066670A2 (https=)
JP (1) JP2009537546A (https=)
AU (1) AU2007254190A1 (https=)
CA (1) CA2651579A1 (https=)
NZ (1) NZ572367A (https=)
WO (1) WO2007136714A2 (https=)

Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20090291921A1 (en) * 2007-11-20 2009-11-26 Gilead Sciences, Inc. Integrase inhibitors
US20100233270A1 (en) 2009-01-08 2010-09-16 Northwestern University Delivery of Oligonucleotide-Functionalized Nanoparticles
US9018227B2 (en) 2010-03-19 2015-04-28 Indiana State University Nicotinic acetylcholine receptor agonists
EP2691393B1 (en) 2011-03-31 2016-09-14 Pfizer Inc Novel bicyclic pyridinones
EP4556010A3 (en) 2011-11-30 2025-07-23 Emory University Jak inhibitors for use in the prevention or treatment of a viral disease caused by a coronaviridae
UA110688C2 (uk) 2012-09-21 2016-01-25 Пфайзер Інк. Біциклічні піридинони
MX368391B (es) 2015-02-03 2019-09-30 Pfizer Ciclopropabenzofuranil-piridopirazindionas novedosas.
CN106632397B (zh) * 2016-12-01 2019-03-22 齐鲁天和惠世制药有限公司 一种6α-溴青霉烷-3α-羧酸二苯甲酯-1β-氧化物的制备方法
ES2747768T3 (es) 2017-03-20 2020-03-11 Forma Therapeutics Inc Composiciones de pirrolopirrol como activadores de quinasa de piruvato (PKR)
ES2989438T3 (es) 2018-09-19 2024-11-26 Novo Nordisk Healthcare Ag Activación de la piruvato cinasa R
US12053458B2 (en) 2018-09-19 2024-08-06 Novo Nordisk Health Care Ag Treating sickle cell disease with a pyruvate kinase R activating compound
CN112142714A (zh) * 2019-06-27 2020-12-29 山东润博生物科技有限公司 一种灭草烟的合成方法
CN112142713A (zh) * 2019-06-27 2020-12-29 山东润博生物科技有限公司 一种咪草烟的合成方法
CN112142712A (zh) * 2019-06-27 2020-12-29 山东润博生物科技有限公司 一种甲基咪草烟的合成方法
US20220378756A1 (en) 2019-09-19 2022-12-01 Forma Therapeutics, Inc. Activating pyruvate kinase r
US12128035B2 (en) 2021-03-19 2024-10-29 Novo Nordisk Health Care Ag Activating pyruvate kinase R
CN116675684B (zh) * 2023-08-02 2023-11-07 上海翰森生物医药科技有限公司 含炔基稠环类衍生物拮抗剂、其制备方法和应用

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004024693A1 (ja) * 2002-08-13 2004-03-25 Shionogi & Co., Ltd. Hivインテグラーゼ阻害活性を有するヘテロ環化合物
WO2004096807A2 (en) * 2003-04-28 2004-11-11 Tibotec Pharmaceuticals Ltd. Hiv integrase inhibitors
WO2005117904A2 (en) * 2004-04-14 2005-12-15 Gilead Sciences, Inc. Phosphonate analogs of hiv integrase inhibitor compounds
JP2006514099A (ja) * 2002-10-16 2006-04-27 ギリアード サイエンシーズ, インコーポレイテッド 組織化前の三環系インテグラーゼインヒビター化合物

Family Cites Families (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4816570A (en) * 1982-11-30 1989-03-28 The Board Of Regents Of The University Of Texas System Biologically reversible phosphate and phosphonate protective groups
US4968788A (en) 1986-04-04 1990-11-06 Board Of Regents, The University Of Texas System Biologically reversible phosphate and phosphonate protective gruops
ATE131825T1 (de) 1990-06-13 1996-01-15 Arnold Glazier Phosphorylierte prodrugs
EP0481214B1 (en) 1990-09-14 1998-06-24 Institute Of Organic Chemistry And Biochemistry Of The Academy Of Sciences Of The Czech Republic Prodrugs of phosphonates
US5543523A (en) 1994-11-15 1996-08-06 Regents Of The University Of Minnesota Method and intermediates for the synthesis of korupensamines
US5683999A (en) * 1995-03-17 1997-11-04 The Dupont Merck Pharmaceutical Company Cyclic urea HIV protease inhibitors
US6312662B1 (en) * 1998-03-06 2001-11-06 Metabasis Therapeutics, Inc. Prodrugs phosphorus-containing compounds
WO1999062513A1 (en) 1998-06-03 1999-12-09 Merck & Co., Inc. Hiv integrase inhibitors
WO1999062520A1 (en) 1998-06-03 1999-12-09 Merck & Co., Inc. Hiv integrase inhibitors
AU3118200A (en) 1998-12-14 2000-07-03 Merck & Co., Inc. Hiv integrase inhibitors
JP3929244B2 (ja) 1998-12-25 2007-06-13 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芳香族ヘテロ環誘導体
KR100423781B1 (ko) 1999-06-02 2004-03-22 시오노기세이야쿠가부시키가이샤 신규 치환 프로페논 유도체의 제조방법
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
US6245806B1 (en) 1999-08-03 2001-06-12 Merck & Co., Inc. HIV integrase inhibitors
WO2001027309A1 (en) * 1999-10-13 2001-04-19 Merck & Co., Inc. Hiv integrase inhibitors
US6919351B2 (en) 2000-10-12 2005-07-19 Merck & Co., Inc. Aza-and polyaza-naphthalenyl-carboxamides useful as HIV integrase inhibitors
JP2004513134A (ja) 2000-10-12 2004-04-30 メルク エンド カムパニー インコーポレーテッド Hivインテグラーゼ阻害薬として有用なアザ−およびポリアザ−ナフタレニルケトン類
JP2004517860A (ja) 2000-10-12 2004-06-17 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
CA2425440C (en) 2000-10-12 2010-04-13 Merck & Co., Inc. Aza- and polyaza-naphthalenyl carboxamides useful as hiv integrase inhibitors
TW200510425A (en) * 2003-08-13 2005-03-16 Japan Tobacco Inc Nitrogen-containing fused ring compound and use thereof as HIV integrase inhibitor
WO2005075475A1 (ja) 2004-02-04 2005-08-18 Shionogi & Co., Ltd. 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
TW200716632A (en) * 2005-05-16 2007-05-01 Gilead Sciences Inc Integrase inhibitor compounds
WO2007076005A2 (en) 2005-12-21 2007-07-05 Gilead Sciences, Inc. Processes and intermediates useful for preparing integrase inhibitor compounds

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004024693A1 (ja) * 2002-08-13 2004-03-25 Shionogi & Co., Ltd. Hivインテグラーゼ阻害活性を有するヘテロ環化合物
JP2006514099A (ja) * 2002-10-16 2006-04-27 ギリアード サイエンシーズ, インコーポレイテッド 組織化前の三環系インテグラーゼインヒビター化合物
WO2004096807A2 (en) * 2003-04-28 2004-11-11 Tibotec Pharmaceuticals Ltd. Hiv integrase inhibitors
WO2005117904A2 (en) * 2004-04-14 2005-12-15 Gilead Sciences, Inc. Phosphonate analogs of hiv integrase inhibitor compounds

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
JPN5009006589; VERSCHUEREN, WIM G.: JOURNAL OF MEDICINAL CHEMISTRY V48 N6, 2005, P1930-1940 *

Also Published As

Publication number Publication date
EP2066670A2 (en) 2009-06-10
AU2007254190A1 (en) 2007-11-29
WO2007136714A2 (en) 2007-11-29
WO2007136714A3 (en) 2008-12-18
CA2651579A1 (en) 2007-11-29
US20090306054A1 (en) 2009-12-10
NZ572367A (en) 2011-09-30
US20080058315A1 (en) 2008-03-06
US8008287B2 (en) 2011-08-30

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