DK3125894T3 - Prodrugs af hiv-reverstranscriptasehæmmere - Google Patents

Prodrugs af hiv-reverstranscriptasehæmmere Download PDF

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Publication number
DK3125894T3
DK3125894T3 DK15774282.6T DK15774282T DK3125894T3 DK 3125894 T3 DK3125894 T3 DK 3125894T3 DK 15774282 T DK15774282 T DK 15774282T DK 3125894 T3 DK3125894 T3 DK 3125894T3
Authority
DK
Denmark
Prior art keywords
reverstranscriptase
hiv
inhibitors
products
reverstranscriptase inhibitors
Prior art date
Application number
DK15774282.6T
Other languages
English (en)
Inventor
Christopher S Burgey
Jeffrey F Fritzen
Jaume Balsells
Mehul Patel
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
Application granted granted Critical
Publication of DK3125894T3 publication Critical patent/DK3125894T3/da

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Classifications

    • 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
    • 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
    • A61K31/506Pyrimidines; 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
    • A61K31/505Pyrimidines; 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
    • 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 System
    • 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
DK15774282.6T 2014-04-01 2015-03-27 Prodrugs af hiv-reverstranscriptasehæmmere DK3125894T3 (da)

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
DK3125894T3 true DK3125894T3 (da) 2020-11-16

Family

ID=54241131

Family Applications (1)

Application Number Title Priority Date Filing Date
DK15774282.6T DK3125894T3 (da) 2014-04-01 2015-03-27 Prodrugs af hiv-reverstranscriptasehæmmere

Country Status (21)

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

Families Citing this family (8)

* 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
JP6342011B2 (ja) 2014-04-01 2018-06-13 メルク・シャープ・アンド・ドーム・コーポレーションMerck Sharp & Dohme Corp. Hiv逆転写酵素阻害剤のプロドラッグ
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
MX2020006527A (es) 2017-12-22 2020-09-17 Sumitomo Chemical Co Compuesto heterociclico y agente para controlar artropodos perjudiciales que contienen el mismo.
AU2019402998B2 (en) * 2018-12-18 2022-12-15 Merck Sharp & Dohme Llc Pyrimidone derivatives as selective cytotoxic agents against HIV infected cells
US20220135537A1 (en) 2019-02-20 2022-05-05 Sumitomo Chemical Company, Limited Ether compound and harmful arthropod-controlling composition containing same
JP2022533681A (ja) * 2019-05-22 2022-07-25 メルク・シャープ・アンド・ドーム・コーポレーション Hivに感染した細胞に対する選択的細胞毒性薬としてのピリジノン誘導体
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

Family Cites Families (28)

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Publication number Priority date Publication date Assignee Title
US5665720A (en) 1992-08-07 1997-09-09 Merck & Co., Inc. Benzoxazinones as inhibitors of HIV reverse transcriptase
IT1305313B1 (it) 1998-07-17 2001-05-04 Colla Paolo 3,4 - diidro- 6- benzil-4-oxopirimidine sostituite e relativo processodi produzione e impiego nella terapia delle infezioni da hiv-1.
SE9904045D0 (sv) 1999-11-09 1999-11-09 Astra Ab Compounds
EP1597237B1 (en) 2003-02-07 2016-07-27 Janssen Pharmaceutica NV Pyrimidine derivatives for the prevention of HIV infection
TW200423930A (en) 2003-02-18 2004-11-16 Hoffmann La Roche Non-nucleoside reverse transcriptase inhibitors
EP1608629A1 (en) 2003-03-24 2005-12-28 F. Hoffmann-La Roche Ag Benzyl-pyridazinons as reverse transcriptase inhibitors
TW200505441A (en) 2003-03-24 2005-02-16 Hoffmann La Roche Non-nucleoside reverse transcriptase inhibitorsⅠ
WO2005026148A1 (en) * 2003-09-08 2005-03-24 Takeda San Diego, Inc. Dipeptidyl peptidase inhibitors
US7288942B2 (en) * 2003-10-02 2007-10-30 Naoyuki Sato Plasma potential measuring method and apparatus, and plasma potential measuring probe
EP1711476A2 (en) 2004-01-12 2006-10-18 Gilead Sciences, Inc. Pyrimidyl phosphonate antiviral compounds and methods of use
CA2559552A1 (en) * 2004-03-23 2005-09-29 F. Hoffmann-La Roche Ag Benzyl-pyridazinone derivatives as non-nucleoside reverse transcriptase inhibitors
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
CA2592092A1 (en) 2004-12-22 2006-06-29 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
ATE425138T1 (de) 2005-10-19 2009-03-15 Hoffmann La Roche N-phenyl-phenylacetamid-nichtnukleosidinhibitor n reverser transkriptase
US7803940B2 (en) 2006-11-24 2010-09-28 Takeda Pharmaceutical Company Limited Heteromonocyclic compound or a salt thereof having strong antihypertensive action, insulin sensitizing activity and the like production thereof and use thereof for prophylaxis or treatment of cardiovascular diseases, metabolic diseases and/or central nervous system diseases
MX2009005449A (es) 2006-11-24 2009-06-02 Takeda Pharmaceutical Compuesto heteromonociclico y uso del mismo.
TW200831085A (en) 2006-12-13 2008-08-01 Merck & Co Inc Non-nucleoside reverse transcriptase inhibitors
US8404253B2 (en) 2006-12-28 2013-03-26 Newport Laboratories, Inc. Modified live (JMSO strain) Haemophilus parasuis vaccine
DE102007032507A1 (de) * 2007-07-12 2009-04-02 Merck Patent Gmbh Pyridazinonderivate
CN101952274A (zh) * 2007-11-20 2011-01-19 默沙东公司 非核苷逆转录酶抑制剂
EP2231621B1 (en) * 2008-01-08 2016-11-02 Merck Sharp & Dohme Corp. Process for preparing n-substituted hydroxypyrimidinone carboxamides
AU2011235568B2 (en) * 2010-03-30 2013-09-12 Merck Canada Inc. Non-nucleoside reverse transcriptase inhibitors
WO2011126969A1 (en) 2010-04-08 2011-10-13 Merck Sharp & Dohme Corp. Prodrugs of an hiv 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
JP6342011B2 (ja) 2014-04-01 2018-06-13 メルク・シャープ・アンド・ドーム・コーポレーションMerck Sharp & Dohme Corp. Hiv逆転写酵素阻害剤のプロドラッグ

Also Published As

Publication number Publication date
RU2693622C2 (ru) 2019-07-03
PL3125894T3 (pl) 2021-02-08
PT3125894T (pt) 2020-11-05
LT3125894T (lt) 2020-12-10
BR112016022722B8 (pt) 2023-11-21
CA2944187A1 (en) 2015-10-08
SI3125894T1 (sl) 2020-12-31
JP2017512802A (ja) 2017-05-25
US20170173015A1 (en) 2017-06-22
AU2015241247A1 (en) 2016-10-06
ES2828951T3 (es) 2021-05-28
BR112016022722A2 (pt) 2017-10-31
EP3125894A4 (en) 2017-12-13
RU2016142611A (ru) 2018-05-03
HRP20201780T1 (hr) 2021-06-25
HUE051848T2 (hu) 2021-03-29
CN106456639A (zh) 2017-02-22
RU2016142611A3 (da) 2018-12-26
AU2015241247B2 (en) 2017-09-14
CN106456639B (zh) 2019-05-10
EP3125894A1 (en) 2017-02-08
CY1123582T1 (el) 2022-03-24
EP3785714A1 (en) 2021-03-03
KR102440843B1 (ko) 2022-09-29
KR20160133000A (ko) 2016-11-21
JP6342011B2 (ja) 2018-06-13
RS61016B1 (sr) 2020-12-31
CA2944187C (en) 2018-06-19
MX2016012915A (es) 2016-12-07
WO2015153304A1 (en) 2015-10-08
BR112016022722B1 (pt) 2023-03-07
US10004740B2 (en) 2018-06-26
EP3125894B1 (en) 2020-09-09

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