KR101097623B1 - Ｈｉｖ 인테그라제 억제제로서의 비시클릭 헤테로사이클 - Google Patents

Ｈｉｖ 인테그라제 억제제로서의 비시클릭 헤테로사이클 Download PDF

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Publication number
KR101097623B1
KR101097623B1 KR1020067027455A KR20067027455A KR101097623B1 KR 101097623 B1 KR101097623 B1 KR 101097623B1 KR 1020067027455 A KR1020067027455 A KR 1020067027455A KR 20067027455 A KR20067027455 A KR 20067027455A KR 101097623 B1 KR101097623 B1 KR 101097623B1
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KR
South Korea
Prior art keywords
oxo
methyl
oxazine
dimethyl
hydroxy
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Expired - Fee Related
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KR1020067027455A
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English (en)
Korean (ko)
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KR20070039502A (ko
Inventor
비. 나라시물루 나이두
자크. 방빌
프란시스 베를류
티모시 피. 콘놀리
마크 알. 크리스탈
존 디. 마티스켈라
칼 월렛
서지 플라몬돈
로저 레밀라드
마가렛 이. 소렌손
야스쯔구 우에다
마이클 에이. 워커
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브리스톨-마이어스 스큅 컴퍼니
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Publication of KR20070039502A publication Critical patent/KR20070039502A/ko
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—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
    • A61K31/535—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
    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/538—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic ring 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
    • 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
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Virology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • AIDS & HIV (AREA)
  • Molecular Biology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
KR1020067027455A 2004-05-28 2006-12-27 Ｈｉｖ 인테그라제 억제제로서의 비시클릭 헤테로사이클 Expired - Fee Related KR101097623B1 (ko)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US57551304P 2004-05-28 2004-05-28
US60/575,513 2004-05-28
US60337104P 2004-08-20 2004-08-20
US60/603,371 2004-08-20
US11/126,891 US7176196B2 (en) 2004-05-28 2005-05-11 Bicyclic heterocycles as HIV integrase inhibitors
US11/126,891 2005-05-11
PCT/US2005/016473 WO2005118593A1 (en) 2004-05-28 2005-05-12 Bicyclic heterocycles as hiv integrase inhibitors

Publications (2)

Publication Number Publication Date
KR20070039502A KR20070039502A (ko) 2007-04-12
KR101097623B1 true KR101097623B1 (ko) 2011-12-22

Family

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KR1020067027455A Expired - Fee Related KR101097623B1 (ko) 2004-05-28 2006-12-27 Ｈｉｖ 인테그라제 억제제로서의 비시클릭 헤테로사이클

Country Status (26)

Country Link
US (2) US7176196B2 (https=)
EP (1) EP1749011B1 (https=)
JP (1) JP4874959B2 (https=)
KR (1) KR101097623B1 (https=)
AR (1) AR049124A1 (https=)
AT (1) ATE412656T1 (https=)
AU (1) AU2005250356C1 (https=)
BR (1) BRPI0511623A (https=)
CA (1) CA2568356C (https=)
CY (1) CY1110266T1 (https=)
DE (1) DE602005010690D1 (https=)
DK (1) DK1749011T3 (https=)
ES (1) ES2315875T3 (https=)
HR (1) HRP20090005T3 (https=)
IL (1) IL179455A (https=)
MX (1) MXPA06013835A (https=)
NO (1) NO20065879L (https=)
NZ (1) NZ551282A (https=)
PE (1) PE20060242A1 (https=)
PL (1) PL1749011T3 (https=)
PT (1) PT1749011E (https=)
RS (1) RS50700B (https=)
RU (1) RU2381228C2 (https=)
SI (1) SI1749011T1 (https=)
TW (1) TWI366567B (https=)
WO (1) WO2005118593A1 (https=)

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US7115601B2 (en) 2004-05-18 2006-10-03 Bristol-Myers Squibb Company HIV integrase inhibitors
CN101146811B (zh) * 2005-03-31 2012-01-11 P.安杰莱蒂分子生物学研究所 Hiv整合酶抑制剂
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
US7902182B2 (en) * 2005-11-16 2011-03-08 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
WO2007064502A1 (en) * 2005-12-01 2007-06-07 Bristol-Myers Squibb Company Forms of n-[(4-fluorophenyl)methyl]-4,6,7,9-tetrahydro-3-hydroxy-9,9-dimethyl-4-oxo-pyrimido[2,1-c][1,4]oxazine-2-carboxamide
US20070129379A1 (en) * 2005-12-01 2007-06-07 Bristol-Myers Squibb Company Hiv integrase inhibitors
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
EP2046328A4 (en) * 2006-07-19 2009-10-28 Univ Georgia Res Found PYRIDINONE DIKETOIC ACIDS: INHIBITORS OF HIV REPLICATION IN COMBINATION THERAPY
US7763630B2 (en) * 2007-06-06 2010-07-27 Bristol-Myers Squibb Company HIV integrase inhibitors
US8129398B2 (en) * 2008-03-19 2012-03-06 Bristol-Myers Squibb Company HIV integrase inhibitors
AU2009228254A1 (en) * 2008-03-27 2009-10-01 Bristol-Myers Squibb Company Crystalline form of N-[[4-fluoro-2- (5-methyl-1H-1,2,4-triazol-1-yl) phenyl]methyl]-4,6,7,9-tetrahydro-3- hydroxy-9,9-dimethyl-4-oxo-pyrimido [2,1-c][1,4]oxazine-2-carboxamide, sodium salt monohydrate
WO2010042392A2 (en) * 2008-10-06 2010-04-15 Merck & Co., Inc. Hiv integrase inhibitors
US8143244B2 (en) * 2009-02-26 2012-03-27 Bristol-Myers Squibb Company Cyclopropyl fused indolobenzazepine HCV NS5B inhibitors
WO2011045330A1 (en) 2009-10-13 2011-04-21 Tibotec Pharmaceuticals Macrocyclic integrase inhibitors
US8383639B2 (en) 2009-10-15 2013-02-26 Bristol-Myers Squibb Company HIV integrase inhibitors
WO2011071849A2 (en) 2009-12-07 2011-06-16 University Of Georgia Research Foundation, Inc. Pyridinone hydroxycyclopentyl carboxamides: hiv integrase inhibitors with therapeutic applications
PE20121524A1 (es) 2010-01-27 2012-12-03 Viiv Healthcare Co Combinaciones de compuestos que comprenden inhibidores de la integrasa de vih y otros agentes terapeuticos
RU2567385C2 (ru) 2010-04-02 2015-11-10 ЯНССЕН Ар ЭНД Ди АЙРЛЭНД Макроциклические ингибиторы интегразы
WO2012007500A2 (de) 2010-07-15 2012-01-19 Bayer Cropscience Ag Neue heterocyclische verbindungen als schädlingsbekämpfungsmittel
US8791108B2 (en) 2011-08-18 2014-07-29 Bristol-Myers Squibb Company Inhibitors of human immunodeficiency virus replication
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
EP2807149A2 (en) * 2012-01-26 2014-12-03 CRO Consulting Limited Agents for treating neurodegenerative disorders
EP2931730B1 (en) 2012-12-17 2019-08-07 Merck Sharp & Dohme Corp. 4-pyridinonetriazine derivatives as hiv integrase inhibitors
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)
WO2018140368A1 (en) 2017-01-26 2018-08-02 Merck Sharp & Dohme Corp. Substituted quinolizine derivatives useful as hiv integrase inhibitors
WO2021050555A1 (en) * 2019-09-10 2021-03-18 X-Chem, Inc. Compositions and uses thereof
CN113912622B (zh) * 2020-07-10 2023-12-01 上海纽思克生物科技有限公司 三环嘧啶酮类化合物、其制备方法、其组合物和用途

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EP1539762A2 (en) 2002-06-26 2005-06-15 Bristol-Myers Squibb Company Bicyclic pyrimidinones as coagulation cascade inhibitors
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AR046938A1 (es) 2003-12-12 2006-01-04 Merck & Co Inc Procedimiento para preparar hexahidropirimido[1,2-a]azepin-2-carboxilatos y compuetos similares
TW200526635A (en) 2003-12-22 2005-08-16 Shionogi & Co Hydroxypyrimidinone derivative having HIV integrase inhibitory activity
RU2403066C2 (ru) 2004-12-03 2010-11-10 Мерк Шарп Энд Домэ Корп Применение атазанавира для улучшения фармакокинетики лекарственных средств, метаболизируемых ugt1a1
CN101146811B (zh) 2005-03-31 2012-01-11 P.安杰莱蒂分子生物学研究所 Hiv整合酶抑制剂

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Also Published As

Publication number Publication date
EP1749011B1 (en) 2008-10-29
WO2005118593A1 (en) 2005-12-15
JP2008501018A (ja) 2008-01-17
ATE412656T1 (de) 2008-11-15
ES2315875T3 (es) 2009-04-01
RS50700B (sr) 2010-06-30
AU2005250356A1 (en) 2005-12-15
US7176196B2 (en) 2007-02-13
AR049124A1 (es) 2006-06-28
JP4874959B2 (ja) 2012-02-15
CA2568356C (en) 2012-07-03
CA2568356A1 (en) 2005-12-15
AU2005250356B2 (en) 2011-03-17
US7511037B2 (en) 2009-03-31
PE20060242A1 (es) 2006-03-31
KR20070039502A (ko) 2007-04-12
SI1749011T1 (sl) 2009-08-31
US20050267105A1 (en) 2005-12-01
RU2381228C2 (ru) 2010-02-10
TWI366567B (en) 2012-06-21
MXPA06013835A (es) 2007-02-02
BRPI0511623A (pt) 2008-03-11
DK1749011T3 (da) 2009-02-16
CY1110266T1 (el) 2015-01-14
PT1749011E (pt) 2008-11-27
DE602005010690D1 (de) 2008-12-11
NZ551282A (en) 2009-05-31
PL1749011T3 (pl) 2009-04-30
TW200600503A (en) 2006-01-01
EP1749011A1 (en) 2007-02-07
US20060276466A1 (en) 2006-12-07
NO20065879L (no) 2007-02-20
HRP20090005T3 (hr) 2009-02-28
IL179455A (en) 2011-10-31
IL179455A0 (en) 2007-05-15
RU2006146970A (ru) 2008-07-10
HK1107343A1 (en) 2008-04-03
AU2005250356C1 (en) 2011-10-06

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