CN101686972B - 治疗用组合物和方法 - Google Patents

治疗用组合物和方法 Download PDF

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Publication number
CN101686972B
CN101686972B CN2008800228167A CN200880022816A CN101686972B CN 101686972 B CN101686972 B CN 101686972B CN 2008800228167 A CN2008800228167 A CN 2008800228167A CN 200880022816 A CN200880022816 A CN 200880022816A CN 101686972 B CN101686972 B CN 101686972B
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CN
China
Prior art keywords
pharmaceutically acceptable
acceptable salt
oxo
dihydroquinoline
fluorobenzyl
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
Application number
CN2008800228167A
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English (en)
Chinese (zh)
Other versions
CN101686972A (zh
Inventor
B·P·凯尔尼
A·A·麦瑟亚斯
S·拉曼那坦
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Gilead Sciences Inc
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Gilead Sciences Inc
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Publication date
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Publication of CN101686972A publication Critical patent/CN101686972A/zh
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Expired - Fee Related legal-status Critical Current
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Classifications

    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47—Quinolines; Isoquinolines
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/426—1,3-Thiazoles
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4402—Non condensed pyridines; Hydrogenated derivatives thereof only substituted in position 2, e.g. pheniramine, bisacodyl
    • 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
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • 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
    • A61P35/00—Antineoplastic agents
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Virology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • AIDS & HIV (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Quinoline Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN2008800228167A 2007-06-29 2008-06-26 治疗用组合物和方法 Expired - Fee Related CN101686972B (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US94730607P 2007-06-29 2007-06-29
US60/947,306 2007-06-29
US4092008P 2008-03-31 2008-03-31
US61/040,920 2008-03-31
PCT/US2008/068339 WO2009006199A1 (en) 2007-06-29 2008-06-26 Therapeutic compositions and the use thereof

Related Child Applications (1)

Application Number Title Priority Date Filing Date
CN201310302662.XA Division CN103480000A (zh) 2007-06-29 2008-06-26 治疗用组合物和方法

Publications (2)

Publication Number Publication Date
CN101686972A CN101686972A (zh) 2010-03-31
CN101686972B true CN101686972B (zh) 2013-08-14

Family

ID=39831893

Family Applications (2)

Application Number Title Priority Date Filing Date
CN2008800228167A Expired - Fee Related CN101686972B (zh) 2007-06-29 2008-06-26 治疗用组合物和方法
CN201310302662.XA Pending CN103480000A (zh) 2007-06-29 2008-06-26 治疗用组合物和方法

Family Applications After (1)

Application Number Title Priority Date Filing Date
CN201310302662.XA Pending CN103480000A (zh) 2007-06-29 2008-06-26 治疗用组合物和方法

Country Status (19)

Country Link
US (4) US20090093467A1 (enExample)
EP (1) EP2167088A1 (enExample)
JP (3) JP5547066B2 (enExample)
KR (1) KR20100040892A (enExample)
CN (2) CN101686972B (enExample)
AP (1) AP2965A (enExample)
AR (1) AR067183A1 (enExample)
AU (1) AU2008270630B2 (enExample)
BR (1) BRPI0813000A2 (enExample)
CA (1) CA2692101A1 (enExample)
CO (1) CO6251237A2 (enExample)
EA (1) EA200971093A1 (enExample)
EC (1) ECSP109897A (enExample)
IL (1) IL202744A0 (enExample)
MX (1) MX2009013829A (enExample)
NZ (1) NZ582086A (enExample)
SG (1) SG182229A1 (enExample)
TW (1) TW200914011A (enExample)
WO (1) WO2009006199A1 (enExample)

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US20070219243A1 (en) * 2005-12-30 2007-09-20 Kearney Brian P Method for improving the pharmacokinetics of HIV integrase inhibitors
KR101477822B1 (ko) 2006-07-07 2015-01-02 길리애드 사이언시즈, 인코포레이티드 치료제의 약동학 특성의 모듈레이터
ES2536923T3 (es) 2006-09-12 2015-05-29 Gilead Sciences, Inc. Proceso e intermedios para preparar inhibidores de la integrasa del VIH
PT3150586T (pt) * 2007-02-23 2020-03-31 Gilead Sciences Inc Moduladores de propriedades farmacocinéticas de agentes terapêuticos
WO2009006203A1 (en) * 2007-06-29 2009-01-08 Gilead Sciences, Inc. Therapeutic compositions and the use thereof
SG182229A1 (en) * 2007-06-29 2012-07-30 Gilead Sciences Inc Therapeutic compositions and the use thereof
AR068403A1 (es) 2007-09-11 2009-11-18 Gilead Sciences Inc Proceso e intermediarios para la preparacion de inhibidores de integrasa
EA201591353A1 (ru) 2008-05-02 2016-01-29 Джилид Сайэнс, Инк. Применение частиц твердого носителя для улучшения технологических характеристик фармацевтического агента
US20130203759A1 (en) * 2010-04-09 2013-08-08 Faranak Nikfar ATAZANAVIR SULFATE FORMULATIONS WITH IMPROVED pH EFFECT
US20130274254A1 (en) * 2010-12-21 2013-10-17 Gilead Sciences, Inc. Inhibitors of cytochrome p450 (cyp3a4)
US9089574B2 (en) 2011-11-30 2015-07-28 Emory University Antiviral JAK inhibitors useful in treating or preventing retroviral and other viral infections
EP2880017B1 (en) 2012-08-03 2016-10-05 Gilead Sciences, Inc. Process and intermediates for preparing integrase inhibitors
EA030003B1 (ru) 2012-12-21 2018-06-29 Джилид Сайэнс, Инк. Полициклическое карбамоилпиридоновое соединение и его фармацевтическое применение для лечения вич-инфекции
NO2865735T3 (enExample) 2013-07-12 2018-07-21
DK3019503T3 (da) 2013-07-12 2017-11-20 Gilead Sciences Inc Polycykliske-carbamoylpyridon-forbindelser og anvendelse deraf til behandling af hiv-infektioner
US9463194B2 (en) 2014-02-05 2016-10-11 Gilead Sciences, Inc. Methods of treating patients co-infected with HIV and tuberculosis
NO2717902T3 (enExample) 2014-06-20 2018-06-23
TWI744723B (zh) 2014-06-20 2021-11-01 美商基利科學股份有限公司 多環型胺甲醯基吡啶酮化合物之合成
TW201613936A (en) 2014-06-20 2016-04-16 Gilead Sciences Inc Crystalline forms of(2R,5S,13aR)-8-hydroxy-7,9-dioxo-n-(2,4,6-trifluorobenzyl)-2,3,4,5,7,9,13,13a-octahydro-2,5-methanopyrido[1',2':4,5]pyrazino[2,1-b][1,3]oxazepine-10-carboxamide
TWI695003B (zh) 2014-12-23 2020-06-01 美商基利科學股份有限公司 多環胺甲醯基吡啶酮化合物及其醫藥用途
WO2016106050A1 (en) 2014-12-26 2016-06-30 Emory University N4-hydroxycytidine and derivatives and anti-viral uses related thereto
CA2980362C (en) 2015-04-02 2020-02-25 Gilead Sciences, Inc. Polycyclic-carbamoylpyridone compounds and their pharmaceutical use
RU2020116571A (ru) 2017-12-07 2021-11-22 Эмори Юниверсити N4-гидроксицитидин и производные и связанные с этим противовирусные применения

Citations (2)

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WO2006034001A2 (en) * 2004-09-16 2006-03-30 Bristol-Myers Squibb Company Methods of treating hiv infection
CN1956961A (zh) * 2004-05-20 2007-05-02 日本烟草产业株式会社 4－氧代喹啉化合物的稳定晶体

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US20090233964A1 (en) * 2005-12-30 2009-09-17 Gilead Sciences, Inc. Methods for improving the pharmacokinetics of hiv integrase inhibitors
KR101477822B1 (ko) * 2006-07-07 2015-01-02 길리애드 사이언시즈, 인코포레이티드 치료제의 약동학 특성의 모듈레이터
ES2536923T3 (es) * 2006-09-12 2015-05-29 Gilead Sciences, Inc. Proceso e intermedios para preparar inhibidores de la integrasa del VIH
SG182229A1 (en) * 2007-06-29 2012-07-30 Gilead Sciences Inc Therapeutic compositions and the use thereof
WO2009006203A1 (en) * 2007-06-29 2009-01-08 Gilead Sciences, Inc. Therapeutic compositions and the use thereof
AR068403A1 (es) * 2007-09-11 2009-11-18 Gilead Sciences Inc Proceso e intermediarios para la preparacion de inhibidores de integrasa
EA201591353A1 (ru) * 2008-05-02 2016-01-29 Джилид Сайэнс, Инк. Применение частиц твердого носителя для улучшения технологических характеристик фармацевтического агента
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WO2006034001A2 (en) * 2004-09-16 2006-03-30 Bristol-Myers Squibb Company Methods of treating hiv infection

Also Published As

Publication number Publication date
BRPI0813000A2 (pt) 2014-12-23
US20100331331A1 (en) 2010-12-30
US20140343063A1 (en) 2014-11-20
US20090093467A1 (en) 2009-04-09
JP5547066B2 (ja) 2014-07-09
IL202744A0 (en) 2010-06-30
WO2009006199A1 (en) 2009-01-08
AP2965A (en) 2014-09-30
ECSP109897A (es) 2010-03-31
CN103480000A (zh) 2014-01-01
JP5769763B2 (ja) 2015-08-26
CN101686972A (zh) 2010-03-31
JP2013199495A (ja) 2013-10-03
US20170136001A1 (en) 2017-05-18
KR20100040892A (ko) 2010-04-21
MX2009013829A (es) 2010-03-10
AP2009005074A0 (en) 2009-12-31
TW200914011A (en) 2009-04-01
EA200971093A1 (ru) 2010-08-30
AU2008270630B2 (en) 2014-01-16
JP2015143278A (ja) 2015-08-06
AU2008270630A1 (en) 2009-01-08
AR067183A1 (es) 2009-09-30
CO6251237A2 (es) 2011-02-21
EP2167088A1 (en) 2010-03-31
NZ582086A (en) 2012-07-27
JP2010532372A (ja) 2010-10-07
SG182229A1 (en) 2012-07-30
CA2692101A1 (en) 2009-01-08

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