EA201691006A1 - Морфологические формы гексадецилоксипропиловых сложных эфиров фосфоновой кислоты и способы их синтеза - Google Patents
Морфологические формы гексадецилоксипропиловых сложных эфиров фосфоновой кислоты и способы их синтезаInfo
- Publication number
- EA201691006A1 EA201691006A1 EA201691006A EA201691006A EA201691006A1 EA 201691006 A1 EA201691006 A1 EA 201691006A1 EA 201691006 A EA201691006 A EA 201691006A EA 201691006 A EA201691006 A EA 201691006A EA 201691006 A1 EA201691006 A1 EA 201691006A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- synthesis
- methods
- hexadelecylopypropyl
- morphological forms
- complex ethers
- Prior art date
Links
- 238000000034 method Methods 0.000 title abstract 3
- 230000015572 biosynthetic process Effects 0.000 title abstract 2
- 230000000877 morphologic effect Effects 0.000 title abstract 2
- 238000003786 synthesis reaction Methods 0.000 title abstract 2
- 239000002253 acid Substances 0.000 title 1
- 150000002170 ethers Chemical class 0.000 title 1
- ABLZXFCXXLZCGV-UHFFFAOYSA-N Phosphorous acid Chemical class OP(O)=O ABLZXFCXXLZCGV-UHFFFAOYSA-N 0.000 abstract 3
- 238000011031 large-scale manufacturing process Methods 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic 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
- C07D239/28—Heterocyclic 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
- C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
- C07D239/47—One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
-
- 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
- C07F9/645—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having two nitrogen atoms as the only ring hetero atoms
- C07F9/6509—Six-membered rings
- C07F9/6512—Six-membered rings having the nitrogen atoms in positions 1 and 3
-
- 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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic 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
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
-
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
-
- 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
- C07F9/28—Phosphorus compounds with one or more P—C bonds
- C07F9/50—Organo-phosphines
- C07F9/53—Organo-phosphine oxides; Organo-phosphine thioxides
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Molecular Biology (AREA)
- Biochemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Oncology (AREA)
- Virology (AREA)
- Communicable Diseases (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Agricultural Chemicals And Associated Chemicals (AREA)
- Saccharide Compounds (AREA)
Abstract
Изобретение описывает способы синтеза фосфонатных сложных эфиров. Способы в соответствии с изобретением обеспечивают возможность крупномасштабного получения фосфонатных сложных эфиров, имеющих высокую чистоту и высокую стабильность. Также описаны морфологические формы фосфонатных сложных эфиров.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201361904857P | 2013-11-15 | 2013-11-15 | |
PCT/US2014/060185 WO2015073148A1 (en) | 2013-11-15 | 2014-10-10 | Morphic forms of hexadecyloxypropyl-phosphonate esters |
Publications (2)
Publication Number | Publication Date |
---|---|
EA201691006A1 true EA201691006A1 (ru) | 2017-02-28 |
EA031861B1 EA031861B1 (ru) | 2019-03-29 |
Family
ID=52472937
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EA201691006A EA031861B1 (ru) | 2013-11-15 | 2014-10-10 | Морфологические формы гексадецилоксипропиловых сложных эфиров фосфоновой кислоты и способы их синтеза |
Country Status (15)
Country | Link |
---|---|
US (7) | US8962829B1 (ru) |
EP (1) | EP2999476B1 (ru) |
JP (3) | JP6150949B2 (ru) |
KR (3) | KR20170143009A (ru) |
CN (2) | CN111777639A (ru) |
AU (3) | AU2014349103B2 (ru) |
BR (1) | BR112016010862B1 (ru) |
CA (1) | CA2929593C (ru) |
DK (1) | DK2999476T3 (ru) |
EA (1) | EA031861B1 (ru) |
ES (1) | ES2685819T3 (ru) |
IL (3) | IL302520A (ru) |
MX (1) | MX362752B (ru) |
UA (1) | UA116825C2 (ru) |
WO (1) | WO2015073148A1 (ru) |
Families Citing this family (7)
Publication number | Priority date | Publication date | Assignee | Title |
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BR112013004925B1 (pt) * | 2010-08-31 | 2020-09-29 | Chimerix, Inc | Formas mórficas do éster [[(s)-2-(4-amino-2-oxo-1(2h)-pirimidinil) -1-(hidroximetil)etóxi]metil] mono[3-(hexadecilóxi) propílico] do ácido fosfônico, composições farmacêuticas das mesmas, método para síntese e uso de uma forma mórfica b |
SG10201800188SA (en) | 2013-03-15 | 2018-02-27 | Univ California | Acyclic nucleoside phosphonate diesters |
EA031861B1 (ru) * | 2013-11-15 | 2019-03-29 | Чимерикс Инк. | Морфологические формы гексадецилоксипропиловых сложных эфиров фосфоновой кислоты и способы их синтеза |
CN112898345A (zh) | 2014-09-15 | 2021-06-04 | 加利福尼亚大学董事会 | 核苷酸类似物 |
WO2017048956A1 (en) | 2015-09-15 | 2017-03-23 | The Regents Of The University Of California | Nucleotide analogs |
JP6878473B2 (ja) * | 2016-06-28 | 2021-05-26 | キメリックス インコーポレイテッド | ブリンシドフォビルの製剤 |
US20220135653A1 (en) * | 2020-11-05 | 2022-05-05 | Bravado Pharmaceuticals, LLC | Intranasal Antiviral Therapy for Mucosal Protection Against Virus Infections |
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WO1992002511A1 (en) | 1990-08-10 | 1992-02-20 | Bristol-Myers Squibb Company | Novel process for the preparation of nucleotides |
JP2002528461A (ja) * | 1998-10-23 | 2002-09-03 | ダーウィン・ディスカバリー・リミテッド | 公知ペプチドメタロプロテイナーゼインヒビターの単一形態型 |
US6716825B2 (en) | 1999-12-03 | 2004-04-06 | The Regents Of The University Of California | Phosphonate compounds |
US20020022659A1 (en) * | 2000-07-19 | 2002-02-21 | Harris Gregory D. | Crystalline and salt forms of an HIV protease inhibitor |
WO2005030127A2 (en) * | 2003-09-23 | 2005-04-07 | Merck & Co., Inc. | Novel crystalline form of a phosphoric acid salt of a dipeptidyl peptidase-iv inhibitor |
WO2005087788A2 (en) | 2004-03-04 | 2005-09-22 | The Regents Of The University Of California | Methods for preparation of nucleoside phosphonate esters |
WO2006014429A2 (en) * | 2004-07-02 | 2006-02-09 | University Of Southern California (La) | Cidofovir peptide conjugates as prodrugs |
WO2006033848A1 (en) * | 2004-09-15 | 2006-03-30 | Merck & Co., Inc. | Amorphous form of a phosphoric acid salt of a dipeptidyl peptidase-iv inhibitor |
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US20090156545A1 (en) * | 2005-04-01 | 2009-06-18 | Hostetler Karl Y | Substituted Phosphate Esters of Nucleoside Phosphonates |
EP1865967A4 (en) | 2005-04-08 | 2011-02-09 | Chimerix Inc | COMPOUNDS, COMPOSITIONS AND METHODS FOR TREATING VIRAL INFECTIONS AND OTHER DISEASES |
EP1868628B1 (en) | 2005-04-08 | 2014-06-11 | Chimerix, Inc. | Compounds, compositions and methods for the treatment of poxvirus infections |
GB0605344D0 (en) * | 2006-03-17 | 2006-04-26 | Pliva Istrazivanje I Razvoj D | Pharmaceutically acceptable salts and polymorphic forms |
US7749983B2 (en) * | 2006-05-03 | 2010-07-06 | Chimerix, Inc. | Metabolically stable alkoxyalkyl esters of antiviral or antiproliferative phosphonates, nucleoside phosphonates and nucleoside phosphates |
WO2008007392A2 (en) * | 2006-07-12 | 2008-01-17 | Matrix Laboratories Limited | Process for the preparation of tenofovir |
WO2008084494A1 (en) * | 2007-01-08 | 2008-07-17 | Matrix Laboratories Limited | Novel polymorphic forms of carvedilol dihydrogen phosphate and process for preparing the same |
CN101678122A (zh) | 2007-04-27 | 2010-03-24 | 奇默里克斯公司 | 在核苷给药的受体中降低肾中毒性的方法 |
ITMI20071594A1 (it) * | 2007-08-02 | 2009-02-03 | Solmag Spa | Forma cristallina monoidrata di adefovir dipivoxil |
CN101143879A (zh) * | 2007-11-08 | 2008-03-19 | 上海交通大学 | 含硫无环核苷膦酸类似物及其制备方法 |
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WO2011011519A1 (en) * | 2009-07-21 | 2011-01-27 | Chimerix, Inc. | Compounds, compositions and methods for treating ocular conditions |
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AU2011216243B2 (en) * | 2010-02-12 | 2015-07-09 | Chimerix, Inc. | Nucleoside phosphonate salts |
US20110263536A1 (en) | 2010-04-22 | 2011-10-27 | Chimerix, Inc. | Methods of Treating Orthopox Virus Infections and Associated Diseases |
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BR112013004925B1 (pt) * | 2010-08-31 | 2020-09-29 | Chimerix, Inc | Formas mórficas do éster [[(s)-2-(4-amino-2-oxo-1(2h)-pirimidinil) -1-(hidroximetil)etóxi]metil] mono[3-(hexadecilóxi) propílico] do ácido fosfônico, composições farmacêuticas das mesmas, método para síntese e uso de uma forma mórfica b |
WO2013063436A1 (en) * | 2011-10-26 | 2013-05-02 | Chimerix, Inc. | Hexadecyloxypropyl cidofovir for the treatment of double-stranded dna virus infection |
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WO2014008344A1 (en) * | 2012-07-03 | 2014-01-09 | Chimerix, Inc. | Method of treating retroviral infections and related dosage regimes |
EA031861B1 (ru) | 2013-11-15 | 2019-03-29 | Чимерикс Инк. | Морфологические формы гексадецилоксипропиловых сложных эфиров фосфоновой кислоты и способы их синтеза |
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JP6878473B2 (ja) * | 2016-06-28 | 2021-05-26 | キメリックス インコーポレイテッド | ブリンシドフォビルの製剤 |
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2014
- 2014-10-10 EA EA201691006A patent/EA031861B1/ru not_active IP Right Cessation
- 2014-10-10 MX MX2016006241A patent/MX362752B/es active IP Right Grant
- 2014-10-10 WO PCT/US2014/060185 patent/WO2015073148A1/en active Application Filing
- 2014-10-10 KR KR1020177036324A patent/KR20170143009A/ko not_active Application Discontinuation
- 2014-10-10 US US14/512,335 patent/US8962829B1/en active Active
- 2014-10-10 DK DK14861700.4T patent/DK2999476T3/en active
- 2014-10-10 BR BR112016010862-0A patent/BR112016010862B1/pt active IP Right Grant
- 2014-10-10 CN CN202010453121.7A patent/CN111777639A/zh active Pending
- 2014-10-10 CN CN201480071309.8A patent/CN105899215A/zh active Pending
- 2014-10-10 CA CA2929593A patent/CA2929593C/en active Active
- 2014-10-10 EP EP14861700.4A patent/EP2999476B1/en active Active
- 2014-10-10 ES ES14861700.4T patent/ES2685819T3/es active Active
- 2014-10-10 AU AU2014349103A patent/AU2014349103B2/en active Active
- 2014-10-10 UA UAA201606498A patent/UA116825C2/uk unknown
- 2014-10-10 KR KR1020167015513A patent/KR101812433B1/ko active IP Right Grant
- 2014-10-10 KR KR1020177036326A patent/KR20170143010A/ko not_active Application Discontinuation
- 2014-10-10 JP JP2016543558A patent/JP6150949B2/ja active Active
- 2014-10-10 IL IL302520A patent/IL302520A/en unknown
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2015
- 2015-01-23 US US14/604,334 patent/US9371344B2/en active Active
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2016
- 2016-05-10 IL IL245576A patent/IL245576B/en unknown
- 2016-05-20 US US15/160,885 patent/US9862687B2/en active Active
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2017
- 2017-04-11 AU AU2017202386A patent/AU2017202386A1/en not_active Abandoned
- 2017-05-17 AU AU2017203315A patent/AU2017203315A1/en not_active Abandoned
- 2017-05-23 JP JP2017101971A patent/JP2017200920A/ja active Pending
- 2017-05-23 JP JP2017101970A patent/JP6401820B2/ja active Active
- 2017-12-01 US US15/828,935 patent/US10112909B2/en active Active
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2018
- 2018-09-19 US US16/135,171 patent/US10487061B2/en active Active
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2019
- 2019-10-11 US US16/599,392 patent/US11066373B2/en active Active
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2020
- 2020-12-08 IL IL279291A patent/IL279291A/en unknown
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2021
- 2021-06-16 US US17/348,831 patent/US11912667B2/en active Active
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Legal Events
Date | Code | Title | Description |
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MM4A | Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s) |
Designated state(s): KZ |