EA201600241A1 - Замещенные (2r,3r,5r)-3-гидрокси-(5-пиримидин-1-ил)тетрагидрофуран-2-илметил арил фосфорамидаты - Google Patents
Замещенные (2r,3r,5r)-3-гидрокси-(5-пиримидин-1-ил)тетрагидрофуран-2-илметил арил фосфорамидатыInfo
- Publication number
- EA201600241A1 EA201600241A1 EA201600241A EA201600241A EA201600241A1 EA 201600241 A1 EA201600241 A1 EA 201600241A1 EA 201600241 A EA201600241 A EA 201600241A EA 201600241 A EA201600241 A EA 201600241A EA 201600241 A1 EA201600241 A1 EA 201600241A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- ylcarbonyl
- alkyl
- optionally substituted
- pyrimidin
- piperidin
- Prior art date
Links
- 150000008298 phosphoramidates Chemical class 0.000 title 1
- -1 aryl phosphoramidate Chemical compound 0.000 abstract 7
- 229910052739 hydrogen Inorganic materials 0.000 abstract 4
- 239000001257 hydrogen Substances 0.000 abstract 4
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 3
- 241000711549 Hepacivirus C Species 0.000 abstract 2
- 125000001624 naphthyl group Chemical group 0.000 abstract 2
- 125000004076 pyridyl group Chemical group 0.000 abstract 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 1
- 101800001554 RNA-directed RNA polymerase Proteins 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 125000003277 amino group Chemical group 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 150000002148 esters Chemical class 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 1
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 1
- PTMHPRAIXMAOOB-UHFFFAOYSA-N phosphoramidic acid Chemical compound NP(O)(O)=O PTMHPRAIXMAOOB-UHFFFAOYSA-N 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/6558—Heterocyclic 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
- C07F9/65586—Heterocyclic 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 at least one of the hetero rings does not contain nitrogen as ring hetero atom
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/66—Phosphorus compounds
- A61K31/665—Phosphorus compounds having oxygen as a ring hetero atom, e.g. fosfomycin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/66—Phosphorus compounds
- A61K31/675—Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/695—Silicon compounds
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
- A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
- A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
- A61K31/7068—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
- A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
- A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
- A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
- A61K31/7068—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
- A61K31/7072—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid having two oxo groups directly attached to the pyrimidine ring, e.g. uridine, uridylic acid, thymidine, zidovudine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
- C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
- C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
- C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
- C07H19/06—Pyrimidine radicals
- C07H19/067—Pyrimidine radicals with ribosyl as the saccharide radical
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
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- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
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- Pharmacology & Pharmacy (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Organic Chemistry (AREA)
- Molecular Biology (AREA)
- Biochemistry (AREA)
- Virology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Genetics & Genomics (AREA)
- Oncology (AREA)
- Biotechnology (AREA)
- Communicable Diseases (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Данное изобретение относится к новым замещенным эфирам амидофосфорной кислоты - (2R,3R,5R)-3-гидрокси-(5-пиримидин-1-ил)тетрагидрофуран-2-илметил арил фосфорамидату общей формулы 1, или его стереоизомеру, или фармацевтически приемлемой солигде Rпредставляет собой водород, (СН)[(СН)С]Si, C-C-ацил, необязательно замещенный NRRгруппой, в которой Rи Rпредставляют собой независимо водород или C-C-алкил; 1-пиррол-2-илкарбонил, пиперидин-3-илкарбонил или пиперидин-4-илкарбонил; Rи Rпредставляют собой F или Rпредставляет собой F или ОН и Rпредставляет собой СН; Rпредставляет собой водород или метил; Ar представляет собой фенил, пиридил или нафтил, где фенил, пиридил или нафтил являются необязательно замещенными по крайней мере одним из следующего: C-алкил, C-алкенил, С-алкинил, С-алкокси, F, Cl, Br, I, нитро, циано, -N(Cалкил); Pm представляет собой 2,4-диоксо-3,4-дигидро-2Н-пиримидин-1-ил или 4-амино-2-оксо-2Н-пиримидин-1-ил, в котором аминогруппа является необязательно замещенной радикалом C(O)R, где Rпредставляет собой (1) C-С-алкил, необязательно замещенный NRRгруппой, где Rи Rпредставляют собой независимо водород или C-C-алкил; C-алкокси, необязательно замещенную фенилом; (2) 1-пиррол-2-илкарбонил, пиперидин-3-илкарбонил, пиперидин-4-илкарбонил; X представляет собой О или N-R, где Rпредставляет собой C-C-алкил, необязательно замещенный ОН или ОСН; n=1, 2 или 3. Новое соединение может быть использовано в качестве ингибитора полимеразы NS5B вируса гепатита С и для лечения заболевания, обусловленного вирусом гепатита С.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US14/051,464 US8889701B1 (en) | 2013-10-11 | 2013-10-11 | Substituted (S)-(2R,3R,5R)-3-hydroxy-(5-pyrimidin-1-yl)tetrahydrofuran-2-ylmethyl aryl phosphoramidate |
PCT/RU2014/000742 WO2015053662A1 (ru) | 2013-10-11 | 2014-10-06 | Замещенные (2r, 3r, 5r)-3-гидрокси-(5-пиримидин-1-ил) тетрагидрофуран-2-илметил арил фосфорамидаты |
Publications (2)
Publication Number | Publication Date |
---|---|
EA201600241A1 true EA201600241A1 (ru) | 2016-07-29 |
EA027990B1 EA027990B1 (ru) | 2017-09-29 |
Family
ID=51870103
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EA201600241A EA027990B1 (ru) | 2013-10-11 | 2014-10-06 | Замещенные (2r,3r,5r)-3-гидрокси(5-пиримидин-1-ил)тетрагидрофуран-2-илметил арил фосфорамидаты |
Country Status (7)
Country | Link |
---|---|
US (1) | US8889701B1 (ru) |
EP (2) | EP3078669A4 (ru) |
JP (1) | JP2016538252A (ru) |
KR (1) | KR20160070758A (ru) |
AU (1) | AU2014331682A1 (ru) |
EA (1) | EA027990B1 (ru) |
WO (2) | WO2015053662A1 (ru) |
Families Citing this family (12)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US8889701B1 (en) * | 2013-10-11 | 2014-11-18 | Alla Chem, Llc | Substituted (S)-(2R,3R,5R)-3-hydroxy-(5-pyrimidin-1-yl)tetrahydrofuran-2-ylmethyl aryl phosphoramidate |
RU2553996C1 (ru) * | 2013-11-27 | 2015-06-20 | Андрей Александрович Иващенко | Замещенные (2r,3r,5r)-3-гидрокси-(5-пиримидин-1-ил)тетрагидрофуран-2-илметил арил фосфорамидаты |
EP3265102A4 (en) | 2015-03-06 | 2018-12-05 | ATEA Pharmaceuticals, Inc. | Beta-d-2'-deoxy-2'alpha-fluoro-2'-beta-c-substituted-2-modified-n6-substituted purine nucleotides for hcv treatment |
WO2018013937A1 (en) | 2016-07-14 | 2018-01-18 | Atea Pharmaceuticals, Inc. | Beta-d-2'-deoxy-2'-alpha-fluoro-2'-beta-c-substituted-4'-fluoro-n6-substituted-6-amino-2-substituted purine nucleotides for the treatment of hepatitis c virus infection |
WO2018048937A1 (en) | 2016-09-07 | 2018-03-15 | Atea Pharmaceuticals, Inc. | 2'-substituted-n6-substituted purine nucleotides for rna virus treatment |
US10266558B2 (en) * | 2016-10-07 | 2019-04-23 | Alexandre Vasilievich Ivachtchenko | Macroheterocyclic nucleoside derivatives and their analogues, production and use thereof |
SG10202012214WA (en) | 2017-02-01 | 2021-01-28 | Atea Pharmaceuticals Inc | Nucleotide hemi-sulfate salt for the treatment of hepatitis c virus |
EP3592430B1 (en) * | 2017-03-10 | 2024-06-26 | Lakewood Amedex, Inc. | Antimicrobial compounds, compositions, and uses thereof |
US12030908B2 (en) | 2017-03-10 | 2024-07-09 | Lakewood Amedex, Inc. | Antimicrobial compounds, compositions, and uses thereof |
WO2019027905A1 (en) * | 2017-07-31 | 2019-02-07 | January Therapeutics, Inc. | ORGANOPHOSPHATE DERIVATIVES |
TW202012001A (zh) | 2018-04-10 | 2020-04-01 | 美商亞堤製藥公司 | C型肝炎病毒(hcv)感染硬化之患者的治療 |
US10874687B1 (en) | 2020-02-27 | 2020-12-29 | Atea Pharmaceuticals, Inc. | Highly active compounds against COVID-19 |
Family Cites Families (5)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
WO2008079206A1 (en) * | 2006-12-20 | 2008-07-03 | Merck & Co., Inc. | Nucleoside cyclic phosphoramidates for the treatment of rna-dependent rna viral infection |
US7964580B2 (en) | 2007-03-30 | 2011-06-21 | Pharmasset, Inc. | Nucleoside phosphoramidate prodrugs |
TWI598358B (zh) * | 2009-05-20 | 2017-09-11 | 基利法瑪席特有限責任公司 | 核苷磷醯胺 |
EP2697242B1 (en) * | 2011-04-13 | 2018-10-03 | Merck Sharp & Dohme Corp. | 2'-azido substituted nucleoside derivatives and methods of use thereof for the treatment of viral diseases |
US8889701B1 (en) * | 2013-10-11 | 2014-11-18 | Alla Chem, Llc | Substituted (S)-(2R,3R,5R)-3-hydroxy-(5-pyrimidin-1-yl)tetrahydrofuran-2-ylmethyl aryl phosphoramidate |
-
2013
- 2013-10-11 US US14/051,464 patent/US8889701B1/en not_active Expired - Fee Related
-
2014
- 2014-10-06 EP EP14852462.2A patent/EP3078669A4/en not_active Withdrawn
- 2014-10-06 EA EA201600241A patent/EA027990B1/ru not_active IP Right Cessation
- 2014-10-06 WO PCT/RU2014/000742 patent/WO2015053662A1/ru active Application Filing
- 2014-12-10 EP EP14852129.7A patent/EP3055316A1/en not_active Withdrawn
- 2014-12-10 JP JP2016521976A patent/JP2016538252A/ja active Pending
- 2014-12-10 AU AU2014331682A patent/AU2014331682A1/en not_active Abandoned
- 2014-12-10 KR KR1020167009904A patent/KR20160070758A/ko not_active Application Discontinuation
- 2014-12-10 WO PCT/US2014/069489 patent/WO2015054706A1/en active Application Filing
Also Published As
Publication number | Publication date |
---|---|
US8889701B1 (en) | 2014-11-18 |
AU2014331682A1 (en) | 2016-04-07 |
KR20160070758A (ko) | 2016-06-20 |
EP3078669A1 (en) | 2016-10-12 |
WO2015054706A1 (en) | 2015-04-16 |
WO2015053662A1 (ru) | 2015-04-16 |
EP3055316A1 (en) | 2016-08-17 |
EP3078669A4 (en) | 2017-06-21 |
EA027990B1 (ru) | 2017-09-29 |
JP2016538252A (ja) | 2016-12-08 |
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