JP2007528394A - Ｈｉｖインテグラーゼ阻害薬 - Google Patents

Ｈｉｖインテグラーゼ阻害薬 Download PDF

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Publication number
JP2007528394A
JP2007528394A JP2007502860A JP2007502860A JP2007528394A JP 2007528394 A JP2007528394 A JP 2007528394A JP 2007502860 A JP2007502860 A JP 2007502860A JP 2007502860 A JP2007502860 A JP 2007502860A JP 2007528394 A JP2007528394 A JP 2007528394A
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JP
Japan
Prior art keywords
alkyl
independently
pyrazino
fluorobenzyl
hydroxy
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.)
Withdrawn
Application number
JP2007502860A
Other languages
English (en)
Japanese (ja)
Other versions
JP2007528394A5 (enExample
Inventor
ウイリアムズ，ピーター・デイー
ワイ，ジヨン・エス
エンブリー，マーク・ダブリユ
スタース，ドネツト・デイー
チユワン，リンハン
ラングフオード，エイチ・マリー
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
Original Assignee
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
Publication of JP2007528394A publication Critical patent/JP2007528394A/ja
Publication of JP2007528394A5 publication Critical patent/JP2007528394A5/ja
Withdrawn legal-status Critical Current

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Virology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Molecular Biology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • AIDS & HIV (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
JP2007502860A 2004-03-09 2005-03-04 Ｈｉｖインテグラーゼ阻害薬 Withdrawn JP2007528394A (ja)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US55160204P 2004-03-09 2004-03-09
PCT/US2005/006916 WO2005092099A1 (en) 2004-03-09 2005-03-04 Hiv integrase inhibitors

Publications (2)

Publication Number Publication Date
JP2007528394A true JP2007528394A (ja) 2007-10-11
JP2007528394A5 JP2007528394A5 (enExample) 2008-04-17

Family

ID=35055916

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2007502860A Withdrawn JP2007528394A (ja) 2004-03-09 2005-03-04 Ｈｉｖインテグラーゼ阻害薬

Country Status (7)

Country Link
US (1) US7820680B2 (enExample)
EP (1) EP1725102A4 (enExample)
JP (1) JP2007528394A (enExample)
CN (1) CN1929737A (enExample)
AU (1) AU2005227258A1 (enExample)
CA (1) CA2557785A1 (enExample)
WO (1) WO2005092099A1 (enExample)

Families Citing this family (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2003267098B2 (en) * 2002-09-11 2008-11-20 Merck & Co., Inc. Dihydroxypyridopyrazine-1,6-dione compounds 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
EP1725535A4 (en) * 2004-03-09 2009-11-25 Merck & Co Inc HIV integrase
CA2557926A1 (en) * 2004-03-09 2005-09-22 Monica Donghi Hiv integrase inhibitors
KR20070026414A (ko) * 2004-03-09 2007-03-08 머크 앤드 캄파니 인코포레이티드 Ｈｉｖ 인테그라제 억제제
US8129385B2 (en) 2005-04-28 2012-03-06 Shionogi & Co., Ltd. Substituted 5-hydroxy-3,4,6,9,9a, 10-hexanhydro-2h-1-oxa04a,8a-diaza-anthracene-6,10-dioness
CA2725680A1 (en) 2008-05-30 2009-12-03 Takeda Pharmaceutical Company Limited Heterocyclic compound
SG192550A1 (en) 2008-07-25 2013-08-30 Viiv Healthcare Co Chemical compounds
WO2010011819A1 (en) * 2008-07-25 2010-01-28 Smithkline Beecham Corporation Chemical compounds
EP2376453B1 (en) 2008-12-11 2019-11-20 VIIV Healthcare Company Intermediates for carbamoylpyridone hiv integrase inhibitors
EP2376080B1 (en) 2008-12-11 2017-09-13 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
RS57244B1 (sr) 2009-06-15 2018-07-31 Shionogi & Co Supstituisani policiklički derivati karbamoilpiridona
US8283366B2 (en) 2010-01-22 2012-10-09 Ambrilia Biopharma, Inc. Derivatives of pyridoxine for inhibiting HIV integrase
PH12012501689A1 (en) 2010-02-26 2012-11-05 Japan Tobacco Inc 1,3,4,8-tetrahydro-2h-pyrido[1,2-a]pyrazine derivative and use of same as hiv intergrase 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
JP5903718B2 (ja) * 2010-08-09 2016-04-13 アンスティチュ ナショナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシュ メディカル Ｈｉｖ−１感染の処置のための方法及び医薬的組成物
CN103228653B (zh) 2010-09-24 2016-03-16 盐野义制药株式会社 被取代的多环性氨基甲酰基吡啶酮衍生物的前药
ES2602794T3 (es) 2011-03-31 2017-02-22 Pfizer Inc Piridinonas bicíclicas novedosas
US9089574B2 (en) 2011-11-30 2015-07-28 Emory University Antiviral JAK inhibitors useful in treating or preventing retroviral and other viral infections
CN102775371B (zh) * 2012-07-26 2015-01-21 山东大学 一种取代噻二嗪类衍生物及其制备方法与应用
UA110688C2 (uk) 2012-09-21 2016-01-25 Пфайзер Інк. Біциклічні піридинони
ES2656696T3 (es) 2013-05-17 2018-02-28 Merck Sharp & Dohme Corp. Compuestos heterocíclicos tricíclicos condensados como inhibidores de la integrasa del VIH
MX368391B (es) 2015-02-03 2019-09-30 Pfizer Ciclopropabenzofuranil-piridopirazindionas novedosas.
TW201726678A (zh) 2015-10-30 2017-08-01 赫孚孟拉羅股份公司 嘧啶酮衍生物及其於治療、改善或預防病毒性疾病之用途

Family Cites Families (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6262055B1 (en) 1998-06-03 2001-07-17 Merck & Co., Inc. HIV integrase inhibitors
US6306891B1 (en) 1998-06-03 2001-10-23 Merck & Co., Inc. HIV integrase inhibitors
US6380249B1 (en) 1998-06-03 2002-04-30 Merck & Co., Inc. HIV integrase inhibitors
US6187000B1 (en) * 1998-08-20 2001-02-13 Endius Incorporated Cannula for receiving surgical instruments
AU5880600A (en) 1999-06-25 2001-01-31 Merck & Co., Inc. 1-(aromatic- or heteroaromatic-substituted)-3-(heteroaromatic substituted)-1,3-propanediones and uses thereof
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
NZ525088A (en) 2000-10-12 2004-11-26 Merck & Co Inc Aza- and polyaza-naphthalenyl carboxamides useful as HIV integrase inhibitors
DE60128936T2 (de) 2000-10-12 2008-04-10 Merck & Co, Inc. Aza- und polyaza-naphthalenylcarbonsäureamide als hiv-integrase-hemmer
AU2002230392A1 (en) 2000-10-12 2002-05-15 Merck & Co., Inc. AZA-and polyaza-naphthalenyl ketones useful as HIV integrase inhibitors
WO2003016275A1 (fr) 2001-08-10 2003-02-27 Shionogi & Co., Ltd. Agent antiviral
DE60218511T2 (de) 2001-10-26 2007-10-25 Istituto Di Richerche Di Biologia Molecolare P. Angeletti S.P.A. Dihydroxypyrimidin-carbonsäueramid-hemmer der hiv-integrase
EP1441735B1 (en) 2001-10-26 2006-02-22 Istituto Di Ricerche Di Biologia Molecolare P. Angeletti S.P.A. N-substituted hydroxypyrimidinone carboxamide inhibitors of hiv integrase
DE60315796T2 (de) 2002-01-17 2008-06-05 Merck & Co., Inc. Hydroxynaphthyridinoncarbonsäureamide, die sich als inhibitoren der hiv-integrase eignen
WO2004004657A2 (en) 2002-07-09 2004-01-15 Bristol-Myers Squibb Company Hiv integrase inhibitors
US7169497B2 (en) * 2003-05-15 2007-01-30 The Gillette Company Electrochemical cells
TW200510425A (en) 2003-08-13 2005-03-16 Japan Tobacco Inc Nitrogen-containing fused ring compound and use thereof as HIV integrase inhibitor
CA2557926A1 (en) 2004-03-09 2005-09-22 Monica Donghi Hiv integrase inhibitors
EP1725535A4 (en) 2004-03-09 2009-11-25 Merck & Co Inc HIV integrase
KR20070026414A (ko) 2004-03-09 2007-03-08 머크 앤드 캄파니 인코포레이티드 Ｈｉｖ 인테그라제 억제제
JP2007531738A (ja) * 2004-04-02 2007-11-08 アムジエン・インコーポレーテツド ＩＬ−１ｒａの凝集を低下させる方法
WO2006121831A2 (en) 2005-05-10 2006-11-16 Merck & Co., Inc. Hiv integrase inhibitors

Also Published As

Publication number Publication date
AU2005227258A1 (en) 2005-10-06
EP1725102A1 (en) 2006-11-29
US20080009490A1 (en) 2008-01-10
EP1725102A4 (en) 2009-04-29
US7820680B2 (en) 2010-10-26
CA2557785A1 (en) 2005-10-06
CN1929737A (zh) 2007-03-14
WO2005092099A1 (en) 2005-10-06

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