CN1929737A - Hiv整合酶抑制剂 - Google Patents

Hiv整合酶抑制剂 Download PDF

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Publication number
CN1929737A
CN1929737A CNA2005800074682A CN200580007468A CN1929737A CN 1929737 A CN1929737 A CN 1929737A CN A2005800074682 A CNA2005800074682 A CN A2005800074682A CN 200580007468 A CN200580007468 A CN 200580007468A CN 1929737 A CN1929737 A CN 1929737A
Authority
CN
China
Prior art keywords
alkyl
independently
pyrimidine
dihydro
optional
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.)
Pending
Application number
CNA2005800074682A
Other languages
English (en)
Chinese (zh)
Inventor
P·D·威廉斯
J·S·维
M·W·恩布里
D·D·斯塔斯
庄凌航
H·M·朗福德
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 CN1929737A publication Critical patent/CN1929737A/zh
Pending legal-status Critical Current

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/50Pyridazines; Hydrogenated pyridazines
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/54Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P43/00Drugs 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)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Virology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (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)
CNA2005800074682A 2004-03-09 2005-03-04 Hiv整合酶抑制剂 Pending CN1929737A (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US55160204P 2004-03-09 2004-03-09
US60/551,602 2004-03-09

Publications (1)

Publication Number Publication Date
CN1929737A true CN1929737A (zh) 2007-03-14

Family

ID=35055916

Family Applications (1)

Application Number Title Priority Date Filing Date
CNA2005800074682A Pending CN1929737A (zh) 2004-03-09 2005-03-04 Hiv整合酶抑制剂

Country Status (7)

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

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102775371A (zh) * 2012-07-26 2012-11-14 山东大学 一种取代噻二嗪类衍生物及其制备方法与应用

Families Citing this family (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2498111A1 (en) * 2002-09-11 2004-03-25 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
EP1725556A1 (en) * 2004-03-09 2006-11-29 Merck & Co., Inc. Hiv integrase inhibitors
WO2005087766A1 (en) * 2004-03-09 2005-09-22 Istituto Di Ricerche Di Biologia Molecolare P Angeletti Spa Hiv integrase inhibitors
JP2007528396A (ja) * 2004-03-09 2007-10-11 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
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
KR20110022620A (ko) 2008-05-30 2011-03-07 다케다 야쿠힌 고교 가부시키가이샤 복소환 화합물
EP2320909B8 (en) 2008-07-25 2016-03-30 VIIV Healthcare Company Chemical compounds
WO2010011819A1 (en) * 2008-07-25 2010-01-28 Smithkline Beecham Corporation Chemical compounds
CA2744019C (en) 2008-12-11 2017-03-14 Shionogi & Co., Ltd. Synthesis of carbamoylpyridone hiv integrase inhibitors and intermediates
KR101682058B1 (ko) 2008-12-11 2016-12-02 비이브 헬쓰케어 컴퍼니 카르바모일피리돈 hiv 인테그라제 억제제를 위한 제조방법 및 중간체
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
LT2444400T (lt) 2009-06-15 2018-06-11 Shionogi & Co., Ltd. Pakeistasis policiklinis karbamoilpiridono darinys
US8283366B2 (en) 2010-01-22 2012-10-09 Ambrilia Biopharma, Inc. Derivatives of pyridoxine for inhibiting HIV integrase
PE20130010A1 (es) 2010-02-26 2013-02-05 Japan Tobacco Inc Derivado de 1,3,4,8-tetrahidro-2h-pirido[1,2-a]pirazina como inhibidor de la integrasa del vih
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
MX2013003139A (es) 2010-09-24 2013-06-18 Shionogi & Co Profarmaco de derivado de carbamoilpiridona policiclica substituida.
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
AU2014267951A1 (en) 2013-05-17 2015-11-19 Merck Sharp & Dohme Corp. Fused Tricyclic Heterocyclic compounds as HIV integrase inhibitors
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
US6306891B1 (en) * 1998-06-03 2001-10-23 Merck & Co., Inc. HIV integrase inhibitors
US6262055B1 (en) * 1998-06-03 2001-07-17 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
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
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
CA2425440C (en) * 2000-10-12 2010-04-13 Merck & Co., Inc. Aza- and polyaza-naphthalenyl carboxamides useful as hiv integrase inhibitors
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
US6919351B2 (en) * 2000-10-12 2005-07-19 Merck & Co., Inc. Aza-and polyaza-naphthalenyl-carboxamides useful as HIV integrase inhibitors
BR0211750A (pt) 2001-08-10 2004-10-13 Shionogi & Co Agente antiviral
NZ533057A (en) * 2001-10-26 2005-11-25 Angeletti P Ist Richerche Bio N-substituted hydroxypyrimidinone carboxamide inhibitors of HIV integrase
EP1441734B1 (en) 2001-10-26 2007-02-28 Istituto di Richerche di Biologia Molecolare P. Angeletti S.p.A. Dihydroxypyrimidine carboxamide inhibitors of hiv integrase
EP1467970B1 (en) * 2002-01-17 2007-08-22 Merck & Co., Inc. Hydroxynaphthyridinone carboxamides useful as hiv integrase inhibitors
US7109186B2 (en) * 2002-07-09 2006-09-19 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
JP2007528396A (ja) * 2004-03-09 2007-10-11 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
WO2005087766A1 (en) * 2004-03-09 2005-09-22 Istituto Di Ricerche Di Biologia Molecolare P Angeletti Spa Hiv integrase inhibitors
EP1725556A1 (en) * 2004-03-09 2006-11-29 Merck & Co., Inc. Hiv integrase inhibitors
PT1729810T (pt) * 2004-04-02 2018-11-22 Swedish Orphan Biovitrum Ab Publ Métodos de redução da agregação de il-ira
CA2607151C (en) * 2005-05-10 2012-06-19 Merck & Co., Inc. Hiv integrase inhibitors

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102775371A (zh) * 2012-07-26 2012-11-14 山东大学 一种取代噻二嗪类衍生物及其制备方法与应用

Also Published As

Publication number Publication date
US7820680B2 (en) 2010-10-26
AU2005227258A1 (en) 2005-10-06
US20080009490A1 (en) 2008-01-10
EP1725102A4 (en) 2009-04-29
CA2557785A1 (en) 2005-10-06
EP1725102A1 (en) 2006-11-29
JP2007528394A (ja) 2007-10-11
WO2005092099A1 (en) 2005-10-06

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PB01 Publication
C10 Entry into substantive examination
SE01 Entry into force of request for substantive examination
C02 Deemed withdrawal of patent application after publication (patent law 2001)
WD01 Invention patent application deemed withdrawn after publication

Open date: 20070314