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) DK2552902T3 (es)
DO (1) DOP2012000256A (es)
EA (1) EA024804B1 (es)
EC (1) ECSP12012201A (es)
ES (2) ES2609636T3 (es)
FI (1) FIC20190021I1 (es)
GE (1) GEP20156368B (es)
HN (1) HN2012002039A (es)
HR (2) HRP20150427T1 (es)
HU (4) HUE025336T2 (es)
IL (2) IL222030A (es)
LT (3) LT2924034T (es)
LU (2) LUC00114I2 (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) PL2552902T3 (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
CN102971308B (zh) * 2010-03-30 2015-02-04 默克加拿大有限公司 非核苷类逆转录酶抑制剂
US20140031250A1 (en) 2010-10-07 2014-01-30 David Tsai Ting 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
MX355439B (es) * 2012-12-05 2018-04-18 Merck Sharp & Dohme Proceso para preparar inhibidores de la transcriptasa inversa.
MX375870B (es) * 2013-11-22 2025-03-07 Merck Sharp & Dohme Llc Composicion de un inhibidor de la transcriptasa inversa sin nucleosido.
CA2930585A1 (en) 2013-12-04 2015-06-11 Merck Sharp & Dohme Corp. Process for making reverse transcriptase inhibitors
RU2693622C2 (ru) 2014-04-01 2019-07-03 Мерк Шарп И Доум Корп. Пролекарственные средства ингибиторов обратной транскриптазы вич
EP3760208B1 (en) 2014-06-25 2024-05-29 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
JP2020517633A (ja) 2017-04-18 2020-06-18 シプラ・リミテッド レトロウイルス感染の治療に用いる併用療法
US20210213041A1 (en) 2018-02-06 2021-07-15 The General Hospital Corporation Repeat rna as biomarkers of tumor immune response
US12005072B2 (en) 2018-07-17 2024-06-11 Merck Sharp & Dohme Llc HIV drug combination for increasing barrier against resistance
MA54549A (fr) 2018-12-18 2022-03-30 Merck Sharp & Dohme Dérivés de pyrimidone en tant qu'agents cytotoxiques sélectifs contre des cellules infectées par le 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
EP1608629A1 (en) 2003-03-24 2005-12-28 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
DK1742908T3 (da) 2004-04-23 2010-01-18 Hoffmann La Roche Ikke nukleosid revers transkriptase inhibitorer
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
BRPI0617720A2 (pt) 2005-10-19 2011-08-02 Hoffmann La Roche compostos inibidores de nnrt de fenil-acetamida, usos dos referidos compostos e composição farmacêutica que os contém
ES2320042T3 (es) 2005-10-19 2009-05-18 F. Hoffmann-La Roche Ag Inhibidores de transcriptasa reversa con nucleosidos de n-fenil fenilacetamida.
TW200831085A (en) 2006-12-13 2008-08-01 Merck & Co Inc Non-nucleoside reverse transcriptase inhibitors
AU2008326784B2 (en) 2007-11-20 2014-04-24 Merck Sharp & Dohme Corp. Non-nucleoside reverse transcriptase inhibitors
CN102971308B (zh) * 2010-03-30 2015-02-04 默克加拿大有限公司 非核苷类逆转录酶抑制剂

Also Published As

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

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