ECSP12012201A - Inhibidores no nucleosídicos de la transcriptasa inversa - Google Patents

Inhibidores no nucleosídicos de la transcriptasa inversa

Info

Publication number
ECSP12012201A
ECSP12012201A ECSP12012201A ECSP12012201A EC SP12012201 A ECSP12012201 A EC SP12012201A EC SP12012201 A ECSP12012201 A EC SP12012201A EC SP12012201 A ECSP12012201 A EC SP12012201A
Authority
EC
Ecuador
Prior art keywords
inhibitors
nucleosid
compounds
reverse transcript
prophylaxis
Prior art date
Application number
Other languages
English (en)
Inventor
Chu-Sing Li
Bernard Cote
Jason Burch
Natalie Nguyen
Onge Miguel St
Danny Gauvreau
Original Assignee
Merck Canada Inc
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Family has litigation
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=ECSP12012201(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Merck Canada Inc filed Critical Merck Canada Inc
Publication of ECSP12012201A publication Critical patent/ECSP12012201A/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/06Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439Non 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV

Landscapes

  • 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)

Abstract

Los compuestos heteroaromáticos de Fórmula I:Son inhibidores de la transcriptasa inversa del vih, en la que r1, r2, r3, r4 y r5 se definen en este documento. Los compuestos de fórmula i y sus sales farmacéuticamente aceptables son útiles en la inhibición de la transcriptasa inversa del vih, la profilaxis y el tratamiento de la infección por vih y en la profilaxis, retraso en la aparición o progresión, y tratamiento del sida. Los compuestos y sus sales pueden emplearse como ingredientes en composiciones farmacéuticamente, opcionalmente junto con otros antivirales, inmunomoduladores, antibióticos o vacunas.
ECSP12012201 2010-03-30 2012-10-01 Inhibidores no nucleosídicos de la transcriptasa inversa ECSP12012201A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US31882410P 2010-03-30 2010-03-30
US32157310P 2010-04-07 2010-04-07

Publications (1)

Publication Number Publication Date
ECSP12012201A true ECSP12012201A (es) 2012-10-30

Family

ID=44710363

Family Applications (1)

Application Number Title Priority Date Filing Date
ECSP12012201 ECSP12012201A (es) 2010-03-30 2012-10-01 Inhibidores no nucleosídicos de la transcriptasa inversa

Country Status (44)

Country Link
US (2) US8486975B2 (es)
EP (2) EP2552902B1 (es)
JP (2) JP5281718B2 (es)
KR (1) KR101421861B1 (es)
CN (1) CN102971308B (es)
AR (1) AR080859A1 (es)
AU (1) AU2011235568B2 (es)
BR (1) BR112012024691B1 (es)
CA (1) CA2794377C (es)
CL (1) CL2012002744A1 (es)
CO (1) CO6630126A2 (es)
CR (1) CR20120503A (es)
CY (3) CY1118774T1 (es)
DK (2) DK2924034T3 (es)
DO (1) DOP2012000256A (es)
EA (1) EA024804B1 (es)
EC (1) ECSP12012201A (es)
ES (2) ES2536295T3 (es)
FI (1) FIC20190021I1 (es)
GE (1) GEP20156368B (es)
HN (1) HN2012002039A (es)
HR (2) HRP20150427T1 (es)
HU (4) HUE031785T2 (es)
IL (2) IL222030A (es)
LT (3) LT2924034T (es)
LU (2) LUC00113I9 (es)
MA (1) MA34170B1 (es)
ME (2) ME02570B (es)
MX (1) MX2012011379A (es)
MY (1) MY163979A (es)
NI (1) NI201200146A (es)
NL (1) NL300980I2 (es)
NO (2) NO2019019I1 (es)
NZ (1) NZ602670A (es)
PE (1) PE20130158A1 (es)
PH (1) PH12012501923A1 (es)
PL (2) PL2924034T3 (es)
PT (2) PT2552902E (es)
RS (2) RS55505B1 (es)
SG (1) SG184347A1 (es)
SI (2) SI2924034T1 (es)
TN (1) TN2012000455A1 (es)
TW (1) TWI458719B (es)
WO (1) WO2011120133A1 (es)

Families Citing this family (20)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PL2924034T3 (pl) * 2010-03-30 2017-07-31 Merck Canada Inc. Kompozycja farmaceutyczna zawierająca nienukleozydowy inhibitor odwrotnej transkryptazy
CN103517990A (zh) 2010-10-07 2014-01-15 通用医疗公司 癌症生物标志物
WO2014052171A1 (en) * 2012-09-26 2014-04-03 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
CA2892919A1 (en) * 2012-12-05 2014-06-12 Merck Sharp & Dohme Corp. Process for making reverse transcriptase inhibitors
RU2661399C1 (ru) * 2013-11-22 2018-07-16 Мерк Шарп И Доум Корп. Композиция ненуклеозидного ингибитора обратной транскриптазы
EP3077376B1 (en) * 2013-12-04 2019-10-16 Merck Sharp & Dohme Corp. Process for making reverse transcriptase inhibitors
EP3785714A1 (en) * 2014-04-01 2021-03-03 Merck Sharp & Dohme Corp. Prodrugs of hiv reverse transcriptase inhibitors
EP3760208B1 (en) 2014-06-25 2024-05-29 The General Hospital Corporation Targeting human satellite ii (hsatii)
RS62466B1 (sr) 2015-12-02 2021-11-30 Merck Sharp & Dohme Farmaceutske kompozicije koje sadrže doravirin, tenofovir dizoproksil fumarat i lamivudin
US11077050B2 (en) 2017-03-24 2021-08-03 Merck Sharp & Dohme Corp. Formulation for parenteral administration
AU2018255954B2 (en) 2017-04-18 2024-04-04 Cipla Limited Combination therapy for use in treating retroviral infections
US20210213041A1 (en) 2018-02-06 2021-07-15 The General Hospital Corporation Repeat rna as biomarkers of tumor immune response
EP3823632B1 (en) * 2018-07-17 2025-10-29 Merck Sharp & Dohme LLC Efda in combination with doravirine for use in treating f227c mutated hiv infections
EP3898595B1 (en) 2018-12-18 2024-05-01 Merck Sharp & Dohme LLC Pyrimidone derivatives as selective cytotoxic agents against hiv infected cells
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
KR20050119652A (ko) 2003-03-24 2005-12-21 에프. 호프만-라 로슈 아게 역전사 효소 저해제로서의 벤질-피리다진온
CN1946680B (zh) 2004-04-23 2011-04-06 弗·哈夫曼-拉罗切有限公司 非核苷逆转录酶抑制剂
US7166738B2 (en) 2004-04-23 2007-01-23 Roche Palo Alto Llc Non-nucleoside reverse transcriptase inhibitors
EP1831157A2 (en) 2004-12-22 2007-09-12 Pfizer Limited Nonnucleoside inhibitors of hiv-1 reverse transcriptase
AR057455A1 (es) 2005-07-22 2007-12-05 Merck & Co Inc Inhibidores de la transcriptasa reversa de vih y composicion farmaceutica
EP1940781A1 (en) 2005-10-19 2008-07-09 F.Hoffmann-La Roche Ag Phenyl-acetamide nnrt inhibitors
CN101287702A (zh) 2005-10-19 2008-10-15 弗·哈夫曼-拉罗切有限公司 N-苯基苯乙酰胺非核苷逆转录酶抑制剂
TW200831085A (en) 2006-12-13 2008-08-01 Merck & Co Inc Non-nucleoside reverse transcriptase inhibitors
KR20100088142A (ko) * 2007-11-20 2010-08-06 머크 샤프 앤드 돔 코포레이션 비-뉴클레오사이드 역전사효소 억제제
PL2924034T3 (pl) * 2010-03-30 2017-07-31 Merck Canada Inc. Kompozycja farmaceutyczna zawierająca nienukleozydowy inhibitor odwrotnej transkryptazy

Also Published As

Publication number Publication date
BR112012024691B1 (pt) 2020-11-17
SG184347A1 (en) 2012-11-29
PE20130158A1 (es) 2013-02-28
CO6630126A2 (es) 2013-03-01
AU2011235568A1 (en) 2012-11-01
PH12012501923A1 (en) 2013-02-04
NO2019018I1 (no) 2019-04-24
GEP20156368B (en) 2015-09-25
HUS1900022I1 (hu) 2019-05-28
LTPA2019507I1 (lt) 2019-04-25
SI2552902T1 (sl) 2015-10-30
EP2924034A1 (en) 2015-09-30
CR20120503A (es) 2013-01-09
KR20120128703A (ko) 2012-11-27
CY2019026I2 (el) 2020-05-29
CA2794377A1 (en) 2011-10-06
JP5886790B2 (ja) 2016-03-16
DK2924034T3 (en) 2017-02-06
NL300980I1 (nl) 2019-04-24
EP2552902A1 (en) 2013-02-06
US20110245296A1 (en) 2011-10-06
CY2019026I1 (el) 2020-05-29
ME02181B (me) 2015-10-20
SI2924034T1 (sl) 2017-05-31
PT2552902E (pt) 2015-06-02
CY1118774T1 (el) 2017-07-12
LTC2552902I2 (lt) 2019-12-10
TN2012000455A1 (en) 2014-01-30
DK2552902T3 (en) 2015-06-15
MA34170B1 (fr) 2013-04-03
BR112012024691A2 (pt) 2019-07-02
LUC00114I1 (es) 2019-04-17
CN102971308A (zh) 2013-03-13
LTC2924034I2 (lt) 2020-10-12
RS54017B1 (sr) 2015-10-30
AR080859A1 (es) 2012-05-16
JP2013209405A (ja) 2013-10-10
PL2552902T3 (pl) 2015-10-30
US20130296382A1 (en) 2013-11-07
DOP2012000256A (es) 2012-12-15
IL233334A0 (en) 2014-09-01
LUC00113I2 (es) 2024-05-22
MX2012011379A (es) 2012-11-30
CN102971308B (zh) 2015-02-04
EA024804B1 (ru) 2016-10-31
HUE031785T2 (en) 2017-08-28
HUS1900021I1 (hu) 2019-05-28
EP2552902B1 (en) 2015-03-11
HRP20161680T1 (hr) 2017-01-27
EP2552902A4 (en) 2013-09-04
HRP20150427T1 (hr) 2015-07-03
JP5281718B2 (ja) 2013-09-04
LT2924034T (lt) 2016-12-27
NI201200146A (es) 2013-03-18
KR101421861B1 (ko) 2014-07-22
HUE025336T2 (en) 2016-03-29
HK1175471A1 (en) 2013-07-05
NZ602670A (en) 2014-09-26
NL300980I2 (nl) 2021-06-17
MY163979A (en) 2017-11-15
CA2794377C (en) 2015-06-16
FIC20190021I1 (fi) 2019-04-17
AU2011235568B2 (en) 2013-09-12
TWI458719B (zh) 2014-11-01
LUC00114I2 (es) 2020-07-10
ES2536295T3 (es) 2015-05-22
CY2019025I2 (el) 2019-11-27
PT2924034T (pt) 2017-01-06
IL233334A (en) 2015-09-24
WO2011120133A1 (en) 2011-10-06
EA201290976A1 (ru) 2013-03-29
IL222030A (en) 2014-07-31
CY2019025I1 (el) 2019-11-27
JP2013510800A (ja) 2013-03-28
EP2924034B1 (en) 2016-11-02
ME02570B (me) 2017-06-20
US8486975B2 (en) 2013-07-16
TW201139409A (en) 2011-11-16
HK1209121A1 (en) 2016-03-24
HN2012002039A (es) 2015-08-24
RS55505B1 (sr) 2017-05-31
LUC00113I9 (es) 2024-06-07
NO2019019I1 (no) 2019-04-24
CL2012002744A1 (es) 2012-12-14
LTPA2019506I1 (lt) 2019-04-25
PL2924034T3 (pl) 2017-07-31
ES2609636T3 (es) 2017-04-21

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