BR112013004925B1 - 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 - Google Patents

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 Download PDF

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BR112013004925B1
BR112013004925B1 BR112013004925-1A BR112013004925A BR112013004925B1 BR 112013004925 B1 BR112013004925 B1 BR 112013004925B1 BR 112013004925 A BR112013004925 A BR 112013004925A BR 112013004925 B1 BR112013004925 B1 BR 112013004925B1
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Brazil
Prior art keywords
hexadecyloxy
methyl
propyl
amino
ester
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BR112013004925-1A
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English (en)
Portuguese (pt)
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BR112013004925A2 (pt
Inventor
Roy W. Ware
Merrick R. Almond
Bernhard M. Lampert
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Chimerix, Inc
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Publication date
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Publication of BR112013004925A2 publication Critical patent/BR112013004925A2/pt
Publication of BR112013004925B1 publication Critical patent/BR112013004925B1/pt

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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
    • C07F9/28—Phosphorus compounds with one or more P—C bonds
    • C07F9/38—Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)]
    • C07F9/40—Esters thereof
    • C07F9/4003—Esters thereof the acid moiety containing a substituent or a structure which is considered as characteristic
    • C07F9/4021—Esters of aromatic acids (P-C aromatic linkage)
    • 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
    • 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
    • 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
    • A61P31/16—Antivirals for RNA viruses for influenza or rhinoviruses
    • 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
    • A61P31/18—Antivirals for RNA viruses for HIV
    • 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
    • A61P31/20—Antivirals for DNA viruses
    • 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
    • A61P31/20—Antivirals for DNA viruses
    • A61P31/22—Antivirals for DNA viruses for herpes viruses
    • 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
    • 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
    • C07F9/38—Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)]
    • C07F9/40—Esters thereof
    • C07F9/4003—Esters thereof the acid moiety containing a substituent or a structure which is considered as characteristic
    • C07F9/4006—Esters of acyclic acids which can have further substituents on alkyl
    • 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
    • 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
    • C07F9/6564—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms
    • C07F9/6571—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and oxygen atoms as the only ring hetero atoms
    • C07F9/657163—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and oxygen atoms as the only ring hetero atoms the ring phosphorus atom being bound to at least one carbon atom
    • C07F9/657181—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having phosphorus atoms, with or without nitrogen, oxygen, sulfur, selenium or tellurium atoms, as ring hetero atoms having phosphorus and oxygen atoms as the only ring hetero atoms the ring phosphorus atom being bound to at least one carbon atom the ring phosphorus atom and, at least, one ring oxygen atom being part of a (thio)phosphonic acid derivative
    • 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
    • C07F9/38—Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)]
    • C07F9/3804—Phosphonic acids [RP(=O)(OH)2]; Thiophosphonic acids ; [RP(=X1)(X2H)2(X1, X2 are each independently O, S or Se)] not used, see subgroups
    • C07F9/3808—Acyclic saturated acids which can have further substituents on alkyl
    • C07F9/65121—
    • 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
    • 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
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

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  • Health & Medical Sciences (AREA)
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  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Molecular Biology (AREA)
  • Virology (AREA)
  • Biochemistry (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Biotechnology (AREA)
  • Pulmonology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
BR112013004925-1A 2010-08-31 2011-08-31 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 BR112013004925B1 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US37874310P 2010-08-31 2010-08-31
US61/378,743 2010-08-31
PCT/US2011/050099 WO2012031045A2 (en) 2010-08-31 2011-08-31 Phosphonate ester derivatives and methods of synthesis thereof

Publications (2)

Publication Number Publication Date
BR112013004925A2 BR112013004925A2 (pt) 2016-04-26
BR112013004925B1 true BR112013004925B1 (pt) 2020-09-29

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BR112013004925-1A BR112013004925B1 (pt) 2010-08-31 2011-08-31 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

Country Status (11)

Country Link
US (3) US8569321B2 (https=)
EP (2) EP3020720B1 (https=)
JP (3) JP2013536865A (https=)
CN (3) CN105218580A (https=)
AU (1) AU2011295937B2 (https=)
BR (1) BR112013004925B1 (https=)
CA (1) CA2809679C (https=)
ES (2) ES2604137T3 (https=)
IL (4) IL224955A (https=)
RU (2) RU2015141024A (https=)
WO (1) WO2012031045A2 (https=)

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ES2604137T3 (es) * 2010-08-31 2017-03-03 Chimerix, Inc. Derivados de éster de fosfonato y métodos de síntesis de los mismos
EA201892769A3 (ru) 2013-03-15 2019-08-30 Дзе Риджентс Оф Дзе Юниверсити Оф Калифорния Сложные диэфиры ациклических нуклеозидфосфонатов
DK2999476T3 (en) 2013-11-15 2018-09-03 Chimerix Inc MORPHIC FORMS OF HEXADECYLOXYPROPYL PHOSPHONATE TESTERS
WO2015085256A1 (en) * 2013-12-05 2015-06-11 Chimerix, Inc. Branched chain acyclic nucleoside phosphonate esters and methods of synthesis and uses thereof
CN103951703A (zh) * 2014-04-28 2014-07-30 中国人民解放军军事医学科学院微生物流行病研究所 制备膦酯衍生物的方法
BR112017005111B1 (pt) 2014-09-15 2023-02-14 The Regents Of The University Of California Compostos análogos de nucleotídeo acíclico, composição farmacêutica contendo tais compostos, e usos da composição no tratamento de uma infecção por papilomavírus
EP3212656B1 (en) 2014-10-27 2019-06-05 Concert Pharmaceuticals Inc. Pyrimidine phosphonic acid esters bearing at least one deuterium atom
WO2017048956A1 (en) 2015-09-15 2017-03-23 The Regents Of The University Of California Nucleotide analogs
EP4295853A3 (en) 2016-06-28 2024-03-06 Emergent BioDefense Operations Lansing LLC Formulations of brincidofovir
CA3105038A1 (en) 2018-06-26 2020-01-02 Tsrl, Inc. Metabolically stable prodrugs
CN109021011A (zh) * 2018-08-14 2018-12-18 山东沾化永浩医药科技有限公司 一种合成对甲苯磺酰氧甲基膦酸二乙酯的方法
IL318465A (en) 2022-07-21 2025-03-01 Antiva Biosciences Inc Compositions and dosage forms for the treatment of HPV infection and HPV-induced neoplasia

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FI930552A7 (fi) * 1990-08-10 1993-02-22 Rega Stichting Uusi menetelmä nukleotidien valmistamiseksi
EP1123308A1 (en) * 1998-10-23 2001-08-16 Darwin Discovery Limited Single morphic forms of known peptide metalloproteinase inhibitors
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DK2999476T3 (en) * 2013-11-15 2018-09-03 Chimerix Inc MORPHIC FORMS OF HEXADECYLOXYPROPYL PHOSPHONATE TESTERS

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IL244076A0 (en) 2016-04-21
JP2016094388A (ja) 2016-05-26
CA2809679A1 (en) 2012-03-08
CN105218580A (zh) 2016-01-06
ES2700117T3 (es) 2019-02-14
AU2011295937B2 (en) 2015-04-16
IL224955A (en) 2016-02-29
WO2012031045A3 (en) 2012-06-21
JP2017214378A (ja) 2017-12-07
US20140046085A1 (en) 2014-02-13
AU2011295937A1 (en) 2013-03-14
EP2611818A4 (en) 2014-02-12
RU2015141024A (ru) 2018-12-26
US8569321B2 (en) 2013-10-29
WO2012031045A2 (en) 2012-03-08
CN103209985A (zh) 2013-07-17
CN103209985B (zh) 2016-08-24
EP3020720A1 (en) 2016-05-18
BR112013004925A2 (pt) 2016-04-26
CN105998039A (zh) 2016-10-12
IL240574A0 (en) 2015-09-24
RU2015141024A3 (https=) 2018-12-26
RU2581045C2 (ru) 2016-04-10
US20150329575A1 (en) 2015-11-19
RU2013114370A (ru) 2014-10-10
IL238217A (en) 2017-07-31
US20120058976A1 (en) 2012-03-08
CA2809679C (en) 2018-03-20
ES2604137T3 (es) 2017-03-03
EP2611818B1 (en) 2016-08-24
EP2611818A2 (en) 2013-07-10
US9303051B2 (en) 2016-04-05
JP2013536865A (ja) 2013-09-26
EP3020720B1 (en) 2018-09-19

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B07D Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette]
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