CN100343253C - 用作HIV整合酶抑制剂的四氢－4H－吡啶并[1,2－а]嘧啶和相关化合物 - Google Patents

用作HIV整合酶抑制剂的四氢－4H－吡啶并[1,2－а]嘧啶和相关化合物 Download PDF

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Publication number
CN100343253C
CN100343253C CNB2003801099211A CN200380109921A CN100343253C CN 100343253 C CN100343253 C CN 100343253C CN B2003801099211 A CNB2003801099211 A CN B2003801099211A CN 200380109921 A CN200380109921 A CN 200380109921A CN 100343253 C CN100343253 C CN 100343253C
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CN
China
Prior art keywords
oxo
hydroxy
amino
fluorobenzyl
pyrido
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.)
Expired - Fee Related
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CNB2003801099211A
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English (en)
Chinese (zh)
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CN1753892A (zh
Inventor
B·克雷申齐
O·金策尔
E·穆拉利亚
F·奥尔维托
G·佩斯卡托雷
M·劳利
V·苏马
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Istituto di Ricerche di Biologia Molecolare P Angeletti SpA
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Istituto di Ricerche di Biologia Molecolare P Angeletti SpA
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Publication of CN1753892A publication Critical patent/CN1753892A/zh
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Publication of CN100343253C publication Critical patent/CN100343253C/zh
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    • 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/04—Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Virology (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Molecular Biology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • AIDS & HIV (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
CNB2003801099211A 2002-12-27 2003-12-18 用作HIV整合酶抑制剂的四氢－4H－吡啶并[1,2－а]嘧啶和相关化合物 Expired - Fee Related CN100343253C (zh)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US43683002P 2002-12-27 2002-12-27
US60/436,830 2002-12-27
US52877603P 2003-12-12 2003-12-12
US60/528,776 2003-12-12

Publications (2)

Publication Number Publication Date
CN1753892A CN1753892A (zh) 2006-03-29
CN100343253C true CN100343253C (zh) 2007-10-17

Family

ID=32685467

Family Applications (1)

Application Number Title Priority Date Filing Date
CNB2003801099211A Expired - Fee Related CN100343253C (zh) 2002-12-27 2003-12-18 用作HIV整合酶抑制剂的四氢－4H－吡啶并[1,2－а]嘧啶和相关化合物

Country Status (20)

Country Link
US (2) US7414045B2 (https=)
EP (1) EP1578748B1 (https=)
JP (1) JP4733986B2 (https=)
KR (1) KR20050087865A (https=)
CN (1) CN100343253C (https=)
AT (1) ATE481401T1 (https=)
AU (2) AU2003292437A1 (https=)
BR (1) BR0317749A (https=)
CA (1) CA2509554C (https=)
DE (1) DE60334248D1 (https=)
EC (1) ECSP055890A (https=)
HR (1) HRP20050593A2 (https=)
IS (1) IS7892A (https=)
MA (1) MA27583A1 (https=)
MX (1) MXPA05007010A (https=)
NO (1) NO20053624L (https=)
NZ (1) NZ540729A (https=)
PL (1) PL377354A1 (https=)
RU (1) RU2329265C2 (https=)
WO (2) WO2004058757A1 (https=)

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TW200526635A (en) * 2003-12-22 2005-08-16 Shionogi & Co Hydroxypyrimidinone derivative having HIV integrase inhibitory activity
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US7157447B2 (en) 2004-05-28 2007-01-02 Bristol-Myers Squibb Company Bicyclic heterocycles as HIV integrase inhibitors
US7176196B2 (en) 2004-05-28 2007-02-13 Bristol-Myers Squibb Company Bicyclic heterocycles as HIV integrase inhibitors
US7173022B2 (en) 2004-05-28 2007-02-06 Bristol-Myers Squibb Company Bicyclic heterocycles as HIV integrase inhibitors
US7192948B2 (en) * 2004-05-28 2007-03-20 Bristol-Myers Squibb Company Bicyclic heterocycles as HIV integrase inhibitors
WO2006060225A2 (en) * 2004-11-23 2006-06-08 Merck & Co., Inc. Process for asymmetric synthesis of hexahydropyrimido[1,2-a] azepine-2-carboxamides and related compounds
MX2007006635A (es) * 2004-12-03 2007-06-19 Merck & Co Inc Formulacion farmaceutica de inhibidores dela carboxamida vih integrasa que contienen una composicion que controla la velocidad de liberacion.
EP1819323B2 (en) * 2004-12-03 2023-03-22 Merck Sharp & Dohme Corp. Pharmaceutical composition containing an anti-nucleating agent
UA87884C2 (uk) * 2004-12-03 2009-08-25 Мерк Энд Ко., Инк. Безводна кристалічна калієва сіль інгібітора віл-інтегрази
RU2403066C2 (ru) * 2004-12-03 2010-11-10 Мерк Шарп Энд Домэ Корп Применение атазанавира для улучшения фармакокинетики лекарственных средств, метаболизируемых ugt1a1
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US7494984B2 (en) * 2005-08-31 2009-02-24 Bristol-Myers Squibb Company Substituted imidazo[1,2-a]pyrimidines as HIV viral DNA integrase inhibitors
CA2622639C (en) * 2005-10-04 2012-01-03 Istituto Di Recerche Di Biologia Molecolare P. Angeletti S.P.A. Hiv integrase inhibitors
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EA200801144A1 (ru) 2005-10-27 2008-10-30 Сионоги Энд Ко., Лтд. Полициклическое карбамоилпиридоновое производное, обладающее ингибиторной активностью в отношении интегразы вич
US7897592B2 (en) * 2005-11-15 2011-03-01 Bristol-Myers Squibb Company HIV integrase inhibitors
WO2007058646A1 (en) * 2005-11-15 2007-05-24 Bristol-Myers Squibb Company Hiv integrase inhibitors: cyclic pyrimidinone compounds
US7902182B2 (en) * 2005-11-16 2011-03-08 Bristol-Myers Squibb Company HIV integrase inhibitors
US8039458B2 (en) * 2005-11-17 2011-10-18 Bristol-Myers Squibb Company HIV integrase inhibitors
WO2007064316A1 (en) * 2005-11-30 2007-06-07 Bristol-Myers Squibb Company Bicyclic heterocycles as hiv integrase inhibitors
US20070129379A1 (en) * 2005-12-01 2007-06-07 Bristol-Myers Squibb Company Hiv integrase inhibitors
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US7897593B2 (en) 2006-05-30 2011-03-01 Bristol-Myers Squibb Company HIV integrase inhibitors
US7893055B2 (en) * 2006-06-28 2011-02-22 Bristol-Myers Squibb Company HIV integrase inhibitors
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WO2010042392A2 (en) * 2008-10-06 2010-04-15 Merck & Co., Inc. Hiv integrase inhibitors
CA2744019C (en) * 2008-12-11 2017-03-14 Shionogi & Co., Ltd. Synthesis of carbamoylpyridone hiv integrase inhibitors and intermediates
US8143244B2 (en) * 2009-02-26 2012-03-27 Bristol-Myers Squibb Company Cyclopropyl fused indolobenzazepine HCV NS5B inhibitors
BRPI1015943A8 (pt) * 2009-07-02 2018-01-09 Sanofi Sa derivados de 1,2,3,4-tetra - hidro - pirimido {1,2-a} pirimidin-6-ona, o respectivo preparo e a respectiva utilização farmacêutica.
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IN2012DN03377A (https=) 2009-10-26 2015-10-23 Merck Sharp & Dohme
RU2567385C2 (ru) 2010-04-02 2015-11-10 ЯНССЕН Ар ЭНД Ди АЙРЛЭНД Макроциклические ингибиторы интегразы
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EP2986291B1 (en) 2013-04-16 2020-05-27 Merck Sharp & Dohme Corp. 4-pyridone derivative compounds and uses thereof as hiv integrase inhibitors
AU2014267951A1 (en) 2013-05-17 2015-11-19 Merck Sharp & Dohme Corp. Fused Tricyclic Heterocyclic compounds as HIV integrase inhibitors
US9951079B2 (en) 2013-06-13 2018-04-24 Merck Sharp & Dohme Corp. Fused tricyclic heterocyclic compounds as HIV integrase inhibitors
MD4794B1 (ro) 2013-09-27 2022-02-28 Merck Sharp & Dohme Corp Derivaţi de chinolizină substituiţi utili ca inhibitori de integrază HIV
WO2016187788A1 (en) 2015-05-25 2016-12-01 Merck Sharp & Dohme Corp. Fused tricyclic heterocyclic compounds useful for treating hiv infection
US10548910B2 (en) 2015-11-17 2020-02-04 Merck Sharp & Dohme Corp. Amido-substituted pyridotriazine derivatives useful as HIV integrase inhibitors
WO2017106071A1 (en) 2015-12-15 2017-06-22 Merck Sharp & Dohme Corp. Spirocyclic quinolizine derivatives useful as hiv integrase inhibitors
WO2017113288A1 (en) 2015-12-31 2017-07-06 Merck Sharp & Dohme Corp. Fused tricyclic heterocyclic compounds as hiv integrase inhibitors
US10934312B2 (en) 2016-12-02 2021-03-02 Merck Sharp & Dohme Corp. Tricyclic heterocycle compounds useful as HIV integrase inhibitors
JOP20190130A1 (ar) 2016-12-02 2019-06-02 Merck Sharp & Dohme مركبات حلقية غير متجانسة رباعية الحلقات مفيدة كمثبطات إنزيم مدمج لفيروس نقص المناعة البشرية (hiv)
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Citations (2)

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Also Published As

Publication number Publication date
CA2509554C (en) 2011-02-01
EP1578748B1 (en) 2010-09-15
US20080176869A1 (en) 2008-07-24
PL377354A1 (pl) 2006-01-23
NO20053624D0 (no) 2005-07-26
MXPA05007010A (es) 2005-08-18
CA2509554A1 (en) 2004-07-15
AU2003292436A1 (en) 2004-07-22
AU2003292437A1 (en) 2004-07-22
NO20053624L (no) 2005-09-26
ATE481401T1 (de) 2010-10-15
US7414045B2 (en) 2008-08-19
IS7892A (is) 2005-06-13
EP1578748A1 (en) 2005-09-28
JP4733986B2 (ja) 2011-07-27
HRP20050593A2 (en) 2006-03-31
KR20050087865A (ko) 2005-08-31
US20060046985A1 (en) 2006-03-02
ECSP055890A (es) 2005-09-20
AU2003292436B2 (en) 2009-07-30
DE60334248D1 (de) 2010-10-28
US7968553B2 (en) 2011-06-28
CN1753892A (zh) 2006-03-29
RU2329265C2 (ru) 2008-07-20
BR0317749A (pt) 2005-11-22
JP2006513200A (ja) 2006-04-20
MA27583A1 (fr) 2005-10-03
RU2005123807A (ru) 2006-01-20
WO2004058757A1 (en) 2004-07-15
NZ540729A (en) 2008-03-28
WO2004058756A1 (en) 2004-07-15

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