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MX2016012915A - Profarmacos de inhibidores de la transcriptasa inversa del virus de la inmunodeficiencia humana (vih). - Google Patents

Profarmacos de inhibidores de la transcriptasa inversa del virus de la inmunodeficiencia humana (vih).

Info

Publication number
MX2016012915A
MX2016012915A MX2016012915A MX2016012915A MX2016012915A MX 2016012915 A MX2016012915 A MX 2016012915A MX 2016012915 A MX2016012915 A MX 2016012915A MX 2016012915 A MX2016012915 A MX 2016012915A MX 2016012915 A MX2016012915 A MX 2016012915A
Authority
MX
Mexico
Prior art keywords
reverse transcriptase
prodrugs
hiv reverse
transcriptase inhibitors
compounds
Prior art date
Application number
MX2016012915A
Other languages
English (en)
Inventor
Christopher S Burgey
Patel Mehul
BALSELLS Jaume
F Fritzen Jeffrey
Original Assignee
Merck Sharp & Dohme
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
Application filed by Merck Sharp & Dohme filed Critical Merck Sharp & Dohme
Publication of MX2016012915A publication Critical patent/MX2016012915A/es

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6558Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
    • 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
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/50Pyridazines; Hydrogenated pyridazines
    • A61K31/501Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
    • 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
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/513Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/66Phosphorus compounds
    • A61K31/662Phosphorus acids or esters thereof having P—C bonds, e.g. foscarnet, trichlorfon
    • 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
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D237/00Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings
    • C07D237/02Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
    • C07D237/06Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D237/10Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D237/22Nitrogen and oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/47One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Virology (AREA)
  • Molecular Biology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • AIDS & HIV (AREA)
  • Biochemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Micro-Organisms Or Cultivation Processes Thereof (AREA)

Abstract

Se describen compuestos de fórmula I, (ver Fórmula]) en donde R1 y R2 se definen en la presente; los compuestos de fórmula I son útiles en la inhibición de la transcriptasa inversa del VIH, la profilaxis y el tratamiento de la infección por el VIH, y la profilaxis, la demora en el inicio o la progresión y el tratamiento del SIDA; los compuestos pueden usarse como ingredientes en composiciones farmacéuticas, opcionalmente en combinación con otros antivirales, inmunomoduladores, antibióticos o vacunas.
MX2016012915A 2014-04-01 2015-03-27 Profarmacos de inhibidores de la transcriptasa inversa del virus de la inmunodeficiencia humana (vih). MX2016012915A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201461973689P 2014-04-01 2014-04-01
PCT/US2015/022868 WO2015153304A1 (en) 2014-04-01 2015-03-27 Prodrugs of hiv reverse transcriptase inhibitors

Publications (1)

Publication Number Publication Date
MX2016012915A true MX2016012915A (es) 2016-12-07

Family

ID=54241131

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2016012915A MX2016012915A (es) 2014-04-01 2015-03-27 Profarmacos de inhibidores de la transcriptasa inversa del virus de la inmunodeficiencia humana (vih).

Country Status (21)

Country Link
US (1) US10004740B2 (es)
EP (2) EP3125894B1 (es)
JP (1) JP6342011B2 (es)
KR (1) KR102440843B1 (es)
CN (1) CN106456639B (es)
AU (1) AU2015241247B2 (es)
BR (1) BR112016022722B8 (es)
CA (1) CA2944187C (es)
CY (1) CY1123582T1 (es)
DK (1) DK3125894T3 (es)
ES (1) ES2828951T3 (es)
HR (1) HRP20201780T1 (es)
HU (1) HUE051848T2 (es)
LT (1) LT3125894T (es)
MX (1) MX2016012915A (es)
PL (1) PL3125894T3 (es)
PT (1) PT3125894T (es)
RS (1) RS61016B1 (es)
RU (1) RU2693622C2 (es)
SI (1) SI3125894T1 (es)
WO (1) WO2015153304A1 (es)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JO3470B1 (ar) 2012-10-08 2020-07-05 Merck Sharp & Dohme مشتقات 5- فينوكسي-3h-بيريميدين-4-أون واستخدامها كمثبطات ناسخ عكسي ل hiv
RS61016B1 (sr) 2014-04-01 2020-12-31 Merck Sharp & Dohme Prolekovi inhibitora hiv reverzne transkriptaze
CN106008362B (zh) * 2016-05-24 2018-08-10 杰达维(上海)医药科技发展有限公司 一种嘧啶衍生物的制备方法
EP3730494B1 (en) 2017-12-22 2023-11-08 Sumitomo Chemical Company, Limited Heterocyclic compound and harmful arthropod controlling agent containing same
EP3898595B1 (en) 2018-12-18 2024-05-01 Merck Sharp & Dohme LLC Pyrimidone derivatives as selective cytotoxic agents against hiv infected cells
BR112021016488A2 (pt) 2019-02-20 2021-10-26 Sumitomo Chemical Company, Limited Composto de éter e composição de controle de artrópode nocivo contendo o mesmo
CA3141143A1 (en) * 2019-05-22 2020-11-26 Merck Sharp & Dohme Corp. Pyridinone derivatives as selective cytotoxic agents against hiv infected cells
JP7618642B2 (ja) * 2019-07-16 2025-01-21 ブリストル-マイヤーズ スクイブ カンパニー インターロイキンの調節におけるプロドラッグ
TW202304919A (zh) 2021-03-31 2023-02-01 印度商皮埃企業有限公司 稠合雜環化合物及其作為害蟲控制劑之用途

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SE9904045D0 (sv) 1999-11-09 1999-11-09 Astra Ab Compounds
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TW200505441A (en) 2003-03-24 2005-02-16 Hoffmann La Roche Non-nucleoside reverse transcriptase inhibitorsⅠ
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RS61016B1 (sr) 2014-04-01 2020-12-31 Merck Sharp & Dohme Prolekovi inhibitora hiv reverzne transkriptaze

Also Published As

Publication number Publication date
KR102440843B1 (ko) 2022-09-29
LT3125894T (lt) 2020-12-10
HRP20201780T1 (hr) 2021-06-25
EP3125894A1 (en) 2017-02-08
US20170173015A1 (en) 2017-06-22
PL3125894T3 (pl) 2021-02-08
SI3125894T1 (sl) 2020-12-31
CN106456639A (zh) 2017-02-22
BR112016022722B1 (pt) 2023-03-07
KR20160133000A (ko) 2016-11-21
US10004740B2 (en) 2018-06-26
JP2017512802A (ja) 2017-05-25
WO2015153304A1 (en) 2015-10-08
BR112016022722A2 (pt) 2017-10-31
RS61016B1 (sr) 2020-12-31
CA2944187A1 (en) 2015-10-08
CY1123582T1 (el) 2022-03-24
CA2944187C (en) 2018-06-19
HUE051848T2 (hu) 2021-03-29
RU2016142611A (ru) 2018-05-03
JP6342011B2 (ja) 2018-06-13
EP3125894B1 (en) 2020-09-09
EP3785714A1 (en) 2021-03-03
BR112016022722B8 (pt) 2023-11-21
ES2828951T3 (es) 2021-05-28
AU2015241247A1 (en) 2016-10-06
PT3125894T (pt) 2020-11-05
EP3125894A4 (en) 2017-12-13
CN106456639B (zh) 2019-05-10
AU2015241247B2 (en) 2017-09-14
RU2016142611A3 (es) 2018-12-26
DK3125894T3 (da) 2020-11-16
RU2693622C2 (ru) 2019-07-03

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