CN102971308B - 非核苷类逆转录酶抑制剂 - Google Patents

非核苷类逆转录酶抑制剂 Download PDF

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Publication number
CN102971308B
CN102971308B CN201180018074.2A CN201180018074A CN102971308B CN 102971308 B CN102971308 B CN 102971308B CN 201180018074 A CN201180018074 A CN 201180018074A CN 102971308 B CN102971308 B CN 102971308B
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CN
China
Prior art keywords
hiv
pharmaceutically acceptable
compound
alkyl
acceptable salt
Prior art date
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Active
Application number
CN201180018074.2A
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English (en)
Chinese (zh)
Other versions
CN102971308A (zh
Inventor
J.伯奇
B.科特
N.阮
C.S.李
M.圣-翁奇
D.戈夫罗
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 Canada Inc
Original Assignee
Merck Frosst Canada Ltd
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Publication date
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=44710363&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CN102971308(B) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Merck Frosst Canada Ltd filed Critical Merck Frosst Canada Ltd
Publication of CN102971308A publication Critical patent/CN102971308A/zh
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (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)
  • Epidemiology (AREA)
  • Communicable Diseases (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Virology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Molecular Biology (AREA)
  • AIDS & HIV (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
CN201180018074.2A 2010-03-30 2011-03-28 非核苷类逆转录酶抑制剂 Active CN102971308B (zh)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US31882410P 2010-03-30 2010-03-30
US61/318,824 2010-03-30
US61/318824 2010-03-30
US32157310P 2010-04-07 2010-04-07
US61/321573 2010-04-07
US61/321,573 2010-04-07
PCT/CA2011/000320 WO2011120133A1 (en) 2010-03-30 2011-03-28 Non-nucleoside reverse transcriptase inhibitors

Publications (2)

Publication Number Publication Date
CN102971308A CN102971308A (zh) 2013-03-13
CN102971308B true CN102971308B (zh) 2015-02-04

Family

ID=44710363

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201180018074.2A Active CN102971308B (zh) 2010-03-30 2011-03-28 非核苷类逆转录酶抑制剂

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US (2) US8486975B2 (enExample)
EP (2) EP2924034B1 (enExample)
JP (2) JP5281718B2 (enExample)
KR (1) KR101421861B1 (enExample)
CN (1) CN102971308B (enExample)
AR (1) AR080859A1 (enExample)
AU (1) AU2011235568B2 (enExample)
BR (1) BR112012024691B1 (enExample)
CA (1) CA2794377C (enExample)
CL (1) CL2012002744A1 (enExample)
CO (1) CO6630126A2 (enExample)
CR (1) CR20120503A (enExample)
CY (3) CY1118774T1 (enExample)
DK (2) DK2924034T3 (enExample)
DO (1) DOP2012000256A (enExample)
EA (1) EA024804B1 (enExample)
EC (1) ECSP12012201A (enExample)
ES (2) ES2609636T3 (enExample)
FI (1) FIC20190021I1 (enExample)
GE (1) GEP20156368B (enExample)
HN (1) HN2012002039A (enExample)
HR (2) HRP20150427T1 (enExample)
HU (4) HUE025336T2 (enExample)
IL (2) IL222030A (enExample)
LT (3) LT2924034T (enExample)
LU (2) LUC00114I2 (enExample)
MA (1) MA34170B1 (enExample)
ME (2) ME02570B (enExample)
MX (1) MX2012011379A (enExample)
MY (1) MY163979A (enExample)
NI (1) NI201200146A (enExample)
NL (1) NL300980I2 (enExample)
NO (2) NO2019019I1 (enExample)
NZ (1) NZ602670A (enExample)
PE (1) PE20130158A1 (enExample)
PH (1) PH12012501923A1 (enExample)
PL (2) PL2924034T3 (enExample)
PT (2) PT2924034T (enExample)
RS (2) RS55505B1 (enExample)
SG (1) SG184347A1 (enExample)
SI (2) SI2924034T1 (enExample)
TN (1) TN2012000455A1 (enExample)
TW (1) TWI458719B (enExample)
WO (1) WO2011120133A1 (enExample)

Families Citing this family (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX2012011379A (es) * 2010-03-30 2012-11-30 Merck Canada Inc Inhibidores no nucleosidicos de la transcriptasa inversa.
WO2012048113A2 (en) 2010-10-07 2012-04-12 The General Hospital Corporation Biomarkers of cancer
EP2900240B1 (en) * 2012-09-26 2020-01-08 Merck Sharp & Dohme Corp. Crystalline form of a reverse transcriptase inhibitor
JO3470B1 (ar) 2012-10-08 2020-07-05 Merck Sharp & Dohme مشتقات 5- فينوكسي-3h-بيريميدين-4-أون واستخدامها كمثبطات ناسخ عكسي ل hiv
CN104994855B (zh) * 2012-12-05 2018-06-05 默沙东公司 制备逆转录酶抑制剂的方法
EP3071037A4 (en) * 2013-11-22 2017-08-02 Merck Sharp & Dohme Corp. Composition of a non-nucleoside reverse transcriptase inhibitor
KR101803671B1 (ko) * 2013-12-04 2017-11-30 머크 샤프 앤드 돔 코포레이션 역전사효소 억제제의 제조 방법
SI3125894T1 (sl) 2014-04-01 2020-12-31 Merck Sharp & Dohme Corp. Predzdravila inhibitorjev reverzne transkriptaze HIV
EP3161159B1 (en) 2014-06-25 2020-08-05 The General Hospital Corporation Targeting human satellite ii (hsatii)
RU2736941C2 (ru) 2015-12-02 2020-11-23 Мерк Шарп энд Доум Корп. Фармацевтические композиции, содержащие доравирин, тенофовира дизопроксила фумарат и ламивудин
WO2018175271A1 (en) * 2017-03-24 2018-09-27 Merck Sharp & Dohme Corp. Formulation for parenteral administration
RU2019136678A (ru) 2017-04-18 2021-05-18 Сипла Лимитед Комбинированная терапия для применения в лечении ретровирусных инфекций
EP4317972A3 (en) 2018-02-06 2024-03-13 The General Hospital Corporation Repeat rna as biomarkers of tumor immune response
WO2020018352A1 (en) 2018-07-17 2020-01-23 Merck Sharp & Dohme Corp. Hiv drug combination for increasing barrier against resistance
MX2021007382A (es) 2018-12-18 2021-07-15 Merck Sharp & Dohme Llc Derivados de pirimidona como agentes citotoxicos selectivos contra celulas infectadas por vih.
CN110801455B (zh) * 2019-11-12 2020-06-02 河北医科大学第二医院 用于治疗mrsa的药物组合物及其应用
CN114163309B (zh) * 2021-12-27 2023-04-25 甘肃皓天医药科技有限责任公司 一种多拉韦林中间体的制备方法
CN114349690B (zh) * 2022-02-15 2023-04-25 甘肃皓天医药科技有限责任公司 一种多拉韦林中间体合成方法
CN116903590A (zh) * 2023-06-06 2023-10-20 延边大学 一种含杂环结构的吡啶酮类化合物及其制备方法和用途
CN120157613A (zh) * 2023-12-15 2025-06-17 山东诚创蓝海医药科技有限公司 多拉韦林中间体及其应用和合成方法

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SE9904045D0 (sv) 1999-11-09 1999-11-09 Astra Ab Compounds
TW200423930A (en) * 2003-02-18 2004-11-16 Hoffmann La Roche Non-nucleoside reverse transcriptase inhibitors
TW200505441A (en) * 2003-03-24 2005-02-16 Hoffmann La Roche Non-nucleoside reverse transcriptase inhibitorsⅠ
WO2004085406A1 (en) 2003-03-24 2004-10-07 F. Hoffmann-La Roche Ag Benzyl-pyridazinons as reverse transcriptase inhibitors
US7166738B2 (en) 2004-04-23 2007-01-23 Roche Palo Alto Llc Non-nucleoside reverse transcriptase inhibitors
AU2005235692B2 (en) 2004-04-23 2011-11-10 F. Hoffmann-La Roche Ag Non-nucleoside reverse transcriptase inhibitors
JP2008525419A (ja) 2004-12-22 2008-07-17 ファイザー・リミテッド Hiv−1逆転写酵素の非ヌクレオシド阻害剤
AR057455A1 (es) 2005-07-22 2007-12-05 Merck & Co Inc Inhibidores de la transcriptasa reversa de vih y composicion farmaceutica
ES2320042T3 (es) 2005-10-19 2009-05-18 F. Hoffmann-La Roche Ag Inhibidores de transcriptasa reversa con nucleosidos de n-fenil fenilacetamida.
EP1940781A1 (en) 2005-10-19 2008-07-09 F.Hoffmann-La Roche Ag Phenyl-acetamide nnrt inhibitors
TW200831085A (en) 2006-12-13 2008-08-01 Merck & Co Inc Non-nucleoside reverse transcriptase inhibitors
CN101952274A (zh) 2007-11-20 2011-01-19 默沙东公司 非核苷逆转录酶抑制剂
MX2012011379A (es) * 2010-03-30 2012-11-30 Merck Canada Inc Inhibidores no nucleosidicos de la transcriptasa inversa.

Also Published As

Publication number Publication date
EA024804B1 (ru) 2016-10-31
LUC00113I9 (enExample) 2024-06-07
EP2552902A1 (en) 2013-02-06
AR080859A1 (es) 2012-05-16
CY2019026I1 (el) 2020-05-29
CR20120503A (es) 2013-01-09
KR20120128703A (ko) 2012-11-27
NL300980I2 (nl) 2021-06-17
CY2019025I2 (el) 2019-11-27
IL222030A (en) 2014-07-31
US20110245296A1 (en) 2011-10-06
HUS1900022I1 (hu) 2019-05-28
KR101421861B1 (ko) 2014-07-22
CY2019025I1 (el) 2019-11-27
EA201290976A1 (ru) 2013-03-29
IL233334A (en) 2015-09-24
CO6630126A2 (es) 2013-03-01
EP2552902B1 (en) 2015-03-11
TN2012000455A1 (en) 2014-01-30
EP2924034A1 (en) 2015-09-30
NO2019018I1 (no) 2019-04-24
BR112012024691B1 (pt) 2020-11-17
GEP20156368B (en) 2015-09-25
PL2552902T3 (pl) 2015-10-30
PT2924034T (pt) 2017-01-06
LT2924034T (lt) 2016-12-27
PT2552902E (pt) 2015-06-02
HK1175471A1 (en) 2013-07-05
JP2013209405A (ja) 2013-10-10
DK2924034T3 (en) 2017-02-06
ECSP12012201A (es) 2012-10-30
HRP20161680T1 (hr) 2017-01-27
HN2012002039A (es) 2015-08-24
SI2924034T1 (sl) 2017-05-31
LTC2552902I2 (lt) 2019-12-10
SI2552902T1 (sl) 2015-10-30
MX2012011379A (es) 2012-11-30
AU2011235568A1 (en) 2012-11-01
SG184347A1 (en) 2012-11-29
NO2019019I1 (no) 2019-04-24
JP2013510800A (ja) 2013-03-28
HUE025336T2 (en) 2016-03-29
AU2011235568B2 (en) 2013-09-12
ES2536295T3 (es) 2015-05-22
MY163979A (en) 2017-11-15
CN102971308A (zh) 2013-03-13
LTC2924034I2 (lt) 2020-10-12
TWI458719B (zh) 2014-11-01
TW201139409A (en) 2011-11-16
PH12012501923A1 (en) 2013-02-04
BR112012024691A2 (pt) 2019-07-02
CA2794377A1 (en) 2011-10-06
HUS1900021I1 (hu) 2019-05-28
LTPA2019506I1 (lt) 2019-04-25
EP2924034B1 (en) 2016-11-02
HUE031785T2 (en) 2017-08-28
HK1209121A1 (en) 2016-03-24
CA2794377C (en) 2015-06-16
PL2924034T3 (pl) 2017-07-31
LTPA2019507I1 (lt) 2019-04-25
US8486975B2 (en) 2013-07-16
JP5886790B2 (ja) 2016-03-16
NL300980I1 (nl) 2019-04-24
ME02181B (me) 2015-10-20
HRP20150427T1 (hr) 2015-07-03
RS55505B1 (sr) 2017-05-31
ES2609636T3 (es) 2017-04-21
CY1118774T1 (el) 2017-07-12
LUC00114I1 (enExample) 2019-04-17
EP2552902A4 (en) 2013-09-04
ME02570B (me) 2017-06-20
DOP2012000256A (es) 2012-12-15
NZ602670A (en) 2014-09-26
FIC20190021I1 (fi) 2019-04-17
LUC00113I2 (enExample) 2024-05-22
LUC00114I2 (enExample) 2020-07-10
CY2019026I2 (el) 2020-05-29
PE20130158A1 (es) 2013-02-28
JP5281718B2 (ja) 2013-09-04
WO2011120133A1 (en) 2011-10-06
IL233334A0 (en) 2014-09-01
CL2012002744A1 (es) 2012-12-14
DK2552902T3 (en) 2015-06-15
MA34170B1 (fr) 2013-04-03
NI201200146A (es) 2013-03-18
RS54017B1 (sr) 2015-10-30
US20130296382A1 (en) 2013-11-07

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