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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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)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Virology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Molecular Biology (AREA)
  • AIDS & HIV (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 2005-05-11
US11/126,891 US7176196B2 (en) 2004-05-28 2005-05-11 Bicyclic heterocycles as HIV integrase inhibitors
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

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

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US7115601B2 (en) 2004-05-18 2006-10-03 Bristol-Myers Squibb Company HIV integrase inhibitors
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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
JP5094725B2 (ja) 2005-10-04 2012-12-12 イステイチユート・デイ・リチエルケ・デイ・ビオロジア・モレコラーレ・ピ・アンジエレツテイ・エツセ・エルレ・エルレ Ｈｉｖインテグラーゼ阻害剤
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
AU2007275805A1 (en) * 2006-07-19 2008-01-24 University Of Georgia Research Foundation, Inc. Pyridinone diketo 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
WO2009120841A1 (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
EP2349276B1 (en) * 2008-10-06 2019-11-27 Merck Sharp & Dohme Corp. Hiv integrase inhibitors
US8143244B2 (en) * 2009-02-26 2012-03-27 Bristol-Myers Squibb Company Cyclopropyl fused indolobenzazepine HCV NS5B inhibitors
ES2446720T3 (es) 2009-10-13 2014-03-10 Elanco Animal Health Ireland Limited Inhibidores de la integrasa macrocíclica
US8383639B2 (en) * 2009-10-15 2013-02-26 Bristol-Myers Squibb Company HIV integrase inhibitors
KR20120094098A (ko) 2009-12-07 2012-08-23 유니버시티 오브 조지아 리서치 파운데이션, 인코포레이티드 피리디논 하이드록시사이클로펜틸 카복사미드: 치료 용도의 ｈｉｖ 인테그라제 억제제
EA032868B1 (ru) 2010-01-27 2019-07-31 Вайв Хелткер Компани Комбинация для лечения вич-инфекции
RU2567385C2 (ru) 2010-04-02 2015-11-10 ЯНССЕН Ар ЭНД Ди АЙРЛЭНД Макроциклические ингибиторы интегразы
JP5996532B2 (ja) 2010-07-15 2016-09-21 バイエル・インテレクチュアル・プロパティ・ゲゼルシャフト・ミット・ベシュレンクテル・ハフツングＢａｙｅｒ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ ＧｍｂＨ 有害生物防除剤としての新規複素環式化合物
US8791108B2 (en) 2011-08-18 2014-07-29 Bristol-Myers Squibb Company Inhibitors of human immunodeficiency virus replication
US9089574B2 (en) 2011-11-30 2015-07-28 Emory University Antiviral JAK inhibitors useful in treating or preventing retroviral and other viral infections
EP2807149A2 (en) * 2012-01-26 2014-12-03 CRO Consulting Limited Agents for treating neurodegenerative disorders
WO2014099586A1 (en) 2012-12-17 2014-06-26 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
ES2656696T3 (es) 2013-05-17 2018-02-28 Merck Sharp & Dohme Corp. Compuestos heterocíclicos tricíclicos condensados como inhibidores de la integrasa del VIH
US9951079B2 (en) 2013-06-13 2018-04-24 Merck Sharp & Dohme Corp. Fused tricyclic heterocyclic compounds as HIV integrase inhibitors
MX367057B (es) 2013-09-27 2019-08-02 Merck Sharp & Dohme Derivados de quinolizina sustituidos utiles como inhibidores de integrasa del vih.
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
US10544155B2 (en) 2015-12-15 2020-01-28 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
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)
AU2017367714B2 (en) 2016-12-02 2020-11-12 Merck Sharp & Dohme Corp. Tricyclic heterocycle compounds useful as HIV integrase inhibitors
EP3573984A4 (en) 2017-01-26 2020-07-29 Merck Sharp & Dohme Corp. USEFUL SUBSTITUTE QUINOLIZINE DERIVATIVES 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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MXPA06013835A (es) 2007-02-02
IL179455A0 (en) 2007-05-15
SI1749011T1 (sl) 2009-08-31
PE20060242A1 (es) 2006-03-31
RU2006146970A (ru) 2008-07-10
WO2005118593A1 (en) 2005-12-15
US20050267105A1 (en) 2005-12-01
TW200600503A (en) 2006-01-01
RS50700B (sr) 2010-06-30
JP2008501018A (ja) 2008-01-17
RU2381228C2 (ru) 2010-02-10
TWI366567B (en) 2012-06-21
AR049124A1 (es) 2006-06-28
AU2005250356A1 (en) 2005-12-15
KR20070039502A (ko) 2007-04-12
PT1749011E (pt) 2008-11-27
NZ551282A (en) 2009-05-31
CA2568356A1 (en) 2005-12-15
CA2568356C (en) 2012-07-03
DK1749011T3 (da) 2009-02-16
AU2005250356C1 (en) 2011-10-06
CY1110266T1 (el) 2015-01-14
US20060276466A1 (en) 2006-12-07
EP1749011B1 (en) 2008-10-29
PL1749011T3 (pl) 2009-04-30
ES2315875T3 (es) 2009-04-01
NO20065879L (no) 2007-02-20
HK1107343A1 (en) 2008-04-03
JP4874959B2 (ja) 2012-02-15
ATE412656T1 (de) 2008-11-15
EP1749011A1 (en) 2007-02-07
DE602005010690D1 (de) 2008-12-11
US7511037B2 (en) 2009-03-31
IL179455A (en) 2011-10-31
US7176196B2 (en) 2007-02-13
HRP20090005T3 (hr) 2009-02-28
AU2005250356B2 (en) 2011-03-17
BRPI0511623A (pt) 2008-03-11

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