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)
  • Tropical Medicine & Parasitology (AREA)
  • Molecular Biology (AREA)
  • AIDS & HIV (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Bioinformatics & Cheminformatics (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 (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)

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
US7517532B2 (en) * 2002-09-11 2009-04-14 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
US20070161639A1 (en) * 2004-03-09 2007-07-12 Philip Jones 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
WO2005087768A1 (en) * 2004-03-09 2005-09-22 Merck & Co., Inc. Hiv integrase inhibitors
EP3187225B1 (en) 2005-04-28 2022-01-05 VIIV Healthcare Company Polycyclic carbamoylpyridone derivative having hiv integrase inhibitory activity
US8338622B2 (en) 2008-05-30 2012-12-25 Takeda Pharmaceutical Company Limited Heterocyclic compound
KR101700267B1 (ko) 2008-07-25 2017-01-26 비이브 헬쓰케어 컴퍼니 화합물
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
PT3617194T (pt) 2008-12-11 2023-11-27 Shionogi & Co Processos e intermediários para inibidores carbamoilpiridona da integrase do vih
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
PT2444400T (pt) 2009-06-15 2018-06-06 Shionogi & Co Derivado de carbamoilpiridona policíclico substituído
US8283366B2 (en) 2010-01-22 2012-10-09 Ambrilia Biopharma, Inc. Derivatives of pyridoxine for inhibiting HIV integrase
EP2540720B1 (en) 2010-02-26 2015-04-15 Japan Tobacco, Inc. 1,3,4,8-tetrahydro-2h-pyrido[1,2-a]pyrazine derivative and use of same as hiv integrase 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
MX2013003139A (es) 2010-09-24 2013-06-18 Shionogi & Co Profarmaco de derivado de carbamoilpiridona policiclica substituida.
ES2602794T3 (es) 2011-03-31 2017-02-22 Pfizer Inc Piridinonas bicíclicas novedosas
CA2856722C (en) 2011-11-30 2022-11-22 Emory University Antiviral jak inhibitors useful in treating or preventing retroviral and other viral infections
UA110688C2 (uk) 2012-09-21 2016-01-25 Пфайзер Інк. Біциклічні піридинони
EP3330272B1 (en) 2013-05-17 2021-02-17 Merck Sharp & Dohme Corp. Fused tricyclic heterocyclic compounds as hiv integrase inhibitors
WO2016125048A1 (en) 2015-02-03 2016-08-11 Pfizer Inc. Novel cyclopropabenzofuranyl pyridopyrazinediones
WO2017072341A1 (en) * 2015-10-30 2017-05-04 F. Hoffmann-La Roche Ag Pyrimidone derivatives and their use in the treatment, amelioration or prevention of a viral disease

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
US6380249B1 (en) 1998-06-03 2002-04-30 Merck & Co., Inc. HIV integrase inhibitors
US6262055B1 (en) 1998-06-03 2001-07-17 Merck & Co., Inc. HIV integrase inhibitors
US6187000B1 (en) * 1998-08-20 2001-02-13 Endius Incorporated Cannula for receiving surgical instruments
WO2001000578A1 (en) 1999-06-25 2001-01-04 Merck & Co., Inc. 1-(aromatic- or heteroaromatic-substituted)-3-(heteroaromatic substituted)-1,3-propanediones and uses thereof
IL155089A0 (en) 2000-10-12 2003-10-31 Merck & Co Inc Aza and polyaza-naphthalenyl carboxamides useful as hiv integrase inhibitors
EP1326611B1 (en) 2000-10-12 2007-06-13 Merck & Co., Inc. Aza- and polyaza-naphthalenyl-carboxamides useful as hiv integrase inhibitors
US20050010048A1 (en) 2000-10-12 2005-01-13 Linghang Zhuang Aza-and polyaza-naphthalenly ketones useful as hiv integrase inhibitors
CA2425625A1 (en) 2000-10-12 2002-07-18 Merck & Co., Inc. Aza-and polyaza-naphthalenyl carboxamides useful as hiv integrase inhibitors
CN101513402B (zh) 2001-08-10 2012-03-21 盐野义制药株式会社 抗病毒药
AU2002334205B2 (en) 2001-10-26 2007-07-05 Istituto Di Ricerche Di Biologia Molecolara P. Angeletti Spa Dihydroxypyrimidine carboxamide inhibitors of HIV integrase
DK1441735T3 (da) 2001-10-26 2006-06-12 Angeletti P Ist Richerche Bio N-substituerede hydroxypyrimidinon-carboxamid-inhibitorer af HIV-integrase
ATE370948T1 (de) 2002-01-17 2007-09-15 Merck & Co Inc Hydroxynaphthyridinoncarbonsäureamide, die sich als inhibitoren der hiv-integrase eignen
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
WO2005087768A1 (en) 2004-03-09 2005-09-22 Merck & Co., Inc. Hiv integrase inhibitors
US20070161639A1 (en) 2004-03-09 2007-07-12 Philip Jones 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
LT1729810T (lt) * 2004-04-02 2018-11-26 Swedish Orphan Biovitrum Ab (Publ) Il-1ra agregacijos sumažinimo būdas
EP1881825B1 (en) 2005-05-10 2013-07-24 Merck Sharp & Dohme Corp. 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
EP1725102A4 (en) 2009-04-29
JP2007528394A (ja) 2007-10-11
US20080009490A1 (en) 2008-01-10
EP1725102A1 (en) 2006-11-29
CA2557785A1 (en) 2005-10-06
US7820680B2 (en) 2010-10-26
AU2005227258A1 (en) 2005-10-06
WO2005092099A1 (en) 2005-10-06

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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