PE20130158A1 - Inhibidores no nucleosidicos de la transcriptasa inversa - Google Patents

Inhibidores no nucleosidicos de la transcriptasa inversa

Info

Publication number
PE20130158A1
PE20130158A1 PE2012001823A PE2012001823A PE20130158A1 PE 20130158 A1 PE20130158 A1 PE 20130158A1 PE 2012001823 A PE2012001823 A PE 2012001823A PE 2012001823 A PE2012001823 A PE 2012001823A PE 20130158 A1 PE20130158 A1 PE 20130158A1
Authority
PE
Peru
Prior art keywords
oxo
methyl
triazol
dihydro
chloro
Prior art date
Application number
PE2012001823A
Other languages
English (en)
Inventor
Jason Burch
Bernard Cote
Natalie Nguyen
Chun Sing Li
Miguel St-Onge
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=PE20130158(A1) "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 PE20130158A1 publication Critical patent/PE20130158A1/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)
  • Molecular Biology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • AIDS & HIV (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Saccharide Compounds (AREA)

Abstract

SE REFIERE A COMPUESTOS DERIVADOS DE 1-[(5-OXO-4,5-DIHIDRO-1H-1,2,4-TRIAZOL-3-IL)METIL]-PIRIDIN-2(1H)-ONA DE FORMULA (I) DONDE R1 ES ALQUILO(C1-C10), CICLOALQUILO(C3-C8) O ARILO; R2 Y R3 SON CADA UNO H, ALQUILO(C1-C6), HALOALQUILO(C1-C6), NO2, CICLOALQUILO(C3-C8), ENTRE OTROS; R4 ES H, ALQUILO(C1-C6), HALOGENO, FLUOROALQUILO(C1-C6), ENTRE OTROS; R5 ES H O ALQUILO(C1-C6). SON COMPUESTOS PREFERIDOS: 3-CLORO-5-({1-[(4-METIL-5-OXO-4,5-DIHIDRO-1H-1,2,4-TRIAZOL-3-IL)METIL]-2-OXO-4-(TRIFLUOROMETIL)-1,2-DIHIDROPIRIDIN-3-IL}OXI)BENZONITRILO; 3-CLORO-5-({4-CLORO-1-[(4-METIL-5-OXO-4,5-DIHIDRO-1H-1,2,4-TRIAZOL-3-IL)METIL]-2-OXO-1,2-DIHIDROPIRIDIN-3-IL}OXI)BENZONITRILO; 3-({5-BROMO-4-CLORO-1-[(4-METIL-5-OXO-4,5-DIHIDRO-1H-1,2,4-TRIAZOL-3-IL)METIL]-2-OXO-1,2-DIHIDROPIRIDIN-3-IL}OXI)-5-CLOROBENZONITRILO; ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE LA TRANSCRIPTASA INVERSA DEL VIH SIENDO UTILES EN EL TRATAMIENTO DE LA INFECCION POR VIH
PE2012001823A 2010-03-30 2011-03-28 Inhibidores no nucleosidicos de la transcriptasa inversa PE20130158A1 (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
PE20130158A1 true PE20130158A1 (es) 2013-02-28

Family

ID=44710363

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2012001823A PE20130158A1 (es) 2010-03-30 2011-03-28 Inhibidores no nucleosidicos 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) ES2536295T3 (es)
FI (1) FIC20190021I1 (es)
GE (1) GEP20156368B (es)
HK (2) HK1175471A1 (es)
HN (1) HN2012002039A (es)
HR (2) HRP20150427T1 (es)
HU (4) HUE031785T2 (es)
IL (2) IL222030A (es)
LT (3) LT2924034T (es)
LU (2) LUC00113I2 (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)
PL (2) PL2552902T3 (es)
PT (2) PT2552902E (es)
RS (2) RS55505B1 (es)
SG (1) SG184347A1 (es)
SI (2) SI2552902T1 (es)
TN (1) TN2012000455A1 (es)
TW (1) TWI458719B (es)
WO (1) WO2011120133A1 (es)

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8486975B2 (en) * 2010-03-30 2013-07-16 Merck Canada Inc. Non-nucleoside reverse transcriptase inhibitors
WO2012048113A2 (en) 2010-10-07 2012-04-12 The General Hospital Corporation Biomarkers of cancer
CN109384765A (zh) * 2012-09-26 2019-02-26 默沙东公司 逆转录酶抑制剂的晶型
JO3470B1 (ar) 2012-10-08 2020-07-05 Merck Sharp & Dohme مشتقات 5- فينوكسي-3h-بيريميدين-4-أون واستخدامها كمثبطات ناسخ عكسي ل hiv
WO2014089140A1 (en) 2012-12-05 2014-06-12 Merck Sharp & Dohme Corp. Process for making reverse transcriptase inhibitors
BR112016011605A8 (pt) * 2013-11-22 2023-04-25 Merck Sharp & Dohme Composição de um inibidor de transcriptase reversa não nucleosídeo
EP3617193B1 (en) 2013-12-04 2024-03-27 Merck Sharp & Dohme LLC 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
ES2895951T3 (es) 2015-12-02 2022-02-23 Merck Sharp & Dohme Composiciones farmacéuticas que contienen doravirina, fumarato de tenofovir disoproxil y lamivudina
WO2018175271A1 (en) * 2017-03-24 2018-09-27 Merck Sharp & Dohme Corp. Formulation for parenteral administration
US11234981B2 (en) 2017-04-18 2022-02-01 Cipla Limited Combination therapy for use in treating retroviral infections
EP4317972A3 (en) 2018-02-06 2024-03-13 The General Hospital Corporation Repeat rna as biomarkers of tumor immune response
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

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
CN100469769C (zh) 2003-03-24 2009-03-18 弗·哈夫曼-拉罗切有限公司 作为逆转录酶抑制剂的苄基-哒嗪酮
TW200505441A (en) * 2003-03-24 2005-02-16 Hoffmann La Roche Non-nucleoside reverse transcriptase inhibitorsⅠ
US7166738B2 (en) 2004-04-23 2007-01-23 Roche Palo Alto Llc Non-nucleoside reverse transcriptase inhibitors
DE602005017604D1 (de) 2004-04-23 2009-12-24 Hoffmann La Roche Inhibitoren der nicht-nukleosid-inhibitoren der reversen transkriptase
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
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
BRPI0820162A2 (pt) 2007-11-20 2019-09-24 Merck Sharp & Dohme composto, composição farmacêutica, método para a profilazia ou tratamento de infecção pela hiv ou para a profilaxia, tratamento ou retardo no início da aids
US8486975B2 (en) * 2010-03-30 2013-07-16 Merck Canada Inc. Non-nucleoside reverse transcriptase inhibitors

Also Published As

Publication number Publication date
ME02181B (me) 2015-10-20
DK2924034T3 (en) 2017-02-06
HRP20161680T1 (hr) 2017-01-27
TN2012000455A1 (en) 2014-01-30
CY2019026I1 (el) 2020-05-29
EP2552902A1 (en) 2013-02-06
CR20120503A (es) 2013-01-09
NO2019019I1 (no) 2019-04-24
HRP20150427T1 (hr) 2015-07-03
SI2924034T1 (sl) 2017-05-31
US20110245296A1 (en) 2011-10-06
AR080859A1 (es) 2012-05-16
BR112012024691A2 (pt) 2019-07-02
DOP2012000256A (es) 2012-12-15
PL2552902T3 (pl) 2015-10-30
PT2924034T (pt) 2017-01-06
LUC00114I2 (es) 2020-07-10
ES2536295T3 (es) 2015-05-22
GEP20156368B (en) 2015-09-25
ES2609636T3 (es) 2017-04-21
FIC20190021I1 (fi) 2019-04-17
KR101421861B1 (ko) 2014-07-22
WO2011120133A1 (en) 2011-10-06
CY2019025I1 (el) 2019-11-27
MX2012011379A (es) 2012-11-30
JP2013209405A (ja) 2013-10-10
HK1209121A1 (en) 2016-03-24
TW201139409A (en) 2011-11-16
CL2012002744A1 (es) 2012-12-14
EP2552902A4 (en) 2013-09-04
JP2013510800A (ja) 2013-03-28
CO6630126A2 (es) 2013-03-01
PT2552902E (pt) 2015-06-02
KR20120128703A (ko) 2012-11-27
NO2019018I1 (no) 2019-04-24
TWI458719B (zh) 2014-11-01
IL233334A0 (en) 2014-09-01
CN102971308B (zh) 2015-02-04
CA2794377A1 (en) 2011-10-06
IL233334A (en) 2015-09-24
CY1118774T1 (el) 2017-07-12
EP2924034A1 (en) 2015-09-30
JP5886790B2 (ja) 2016-03-16
SI2552902T1 (sl) 2015-10-30
MY163979A (en) 2017-11-15
EP2924034B1 (en) 2016-11-02
US20130296382A1 (en) 2013-11-07
CN102971308A (zh) 2013-03-13
HUE025336T2 (en) 2016-03-29
HUS1900022I1 (hu) 2019-05-28
ECSP12012201A (es) 2012-10-30
LTC2924034I2 (lt) 2020-10-12
PL2924034T3 (pl) 2017-07-31
NI201200146A (es) 2013-03-18
HUE031785T2 (en) 2017-08-28
EP2552902B1 (en) 2015-03-11
MA34170B1 (fr) 2013-04-03
EA024804B1 (ru) 2016-10-31
SG184347A1 (en) 2012-11-29
ME02570B (me) 2017-06-20
NL300980I1 (nl) 2019-04-24
IL222030A (en) 2014-07-31
LTPA2019507I1 (lt) 2019-04-25
HUS1900021I1 (hu) 2019-05-28
JP5281718B2 (ja) 2013-09-04
RS54017B1 (en) 2015-10-30
RS55505B1 (sr) 2017-05-31
LTPA2019506I1 (lt) 2019-04-25
EA201290976A1 (ru) 2013-03-29
LUC00114I1 (es) 2019-04-17
CY2019026I2 (el) 2020-05-29
LT2924034T (lt) 2016-12-27
BR112012024691B1 (pt) 2020-11-17
LTC2552902I2 (lt) 2019-12-10
NZ602670A (en) 2014-09-26
HK1175471A1 (en) 2013-07-05
NL300980I2 (nl) 2021-06-17
HN2012002039A (es) 2015-08-24
AU2011235568A1 (en) 2012-11-01
AU2011235568B2 (en) 2013-09-12
LUC00113I2 (es) 2024-05-22
CY2019025I2 (el) 2019-11-27
US8486975B2 (en) 2013-07-16
CA2794377C (en) 2015-06-16
DK2552902T3 (en) 2015-06-15

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