EA201190205A1 - ПОЛЕЗНЫЕ ФАРМАЦЕВТИЧЕСКИЕ СОЛИ 7-[(3R,4R)-3-ГИДРОКСИ-4-ГИДРОКСИМЕТИЛПИРРОЛИДИН-1-ИЛМЕТИЛ]-3,5-ДИГИДРОПИРРОЛО[3,2-d]ПИРИМИДИН-4-ОНА - Google Patents

ПОЛЕЗНЫЕ ФАРМАЦЕВТИЧЕСКИЕ СОЛИ 7-[(3R,4R)-3-ГИДРОКСИ-4-ГИДРОКСИМЕТИЛПИРРОЛИДИН-1-ИЛМЕТИЛ]-3,5-ДИГИДРОПИРРОЛО[3,2-d]ПИРИМИДИН-4-ОНА

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Publication number
EA201190205A1
EA201190205A1 EA201190205A EA201190205A EA201190205A1 EA 201190205 A1 EA201190205 A1 EA 201190205A1 EA 201190205 A EA201190205 A EA 201190205A EA 201190205 A EA201190205 A EA 201190205A EA 201190205 A1 EA201190205 A1 EA 201190205A1
Authority
EA
Eurasian Patent Office
Prior art keywords
dihydropyrrolo
pyrimidin
hydroxy
acids
hydroximetilpyrrolidin
Prior art date
Application number
EA201190205A
Other languages
English (en)
Other versions
EA020931B1 (ru
Inventor
Гэри Бэртли
Томас Клиэри
Джон Ф. Лэнг
Original Assignee
Байокрист Фармасьютикалз, Инк.
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 Байокрист Фармасьютикалз, Инк. filed Critical Байокрист Фармасьютикалз, Инк.
Publication of EA201190205A1 publication Critical patent/EA201190205A1/ru
Publication of EA020931B1 publication Critical patent/EA020931B1/ru

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • 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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A61K31/525—Isoalloxazines, e.g. riboflavins, vitamin B2
    • 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
    • C07D239/48—Two nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • C07D403/06—Heterocyclic 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

В настоящем изобретении предложены новые геми- и моносоли 7-[(3R,4R)-3-гидрокси-4-гидроксиметилпирролидин-1-илметил]-3,5-дигидропирроло[3,2-d]пиримидин-4-она (соединение 1) с различными органическими и неорганическими кислотами. В одном из воплощений органическая кислота представляет собой Сорганические двухосновные кислоты. В настоящем изобретении дополнительно предложены новые способы получения этих солей. Новые моногидраты гемисоли Сорганических двухосновных кислот являются изоструктурными и могут быть получены с различными свойствами. Множество кислот может быть использовано одновременно, и доля кислот может варьировать, обеспечивая возможность выбора гемисолей соединения 1 с желаемыми свойствами.
EA201190205A 2009-03-24 2010-03-24 ПОЛЕЗНЫЕ ФАРМАЦЕВТИЧЕСКИЕ СОЛИ 7-[(3R,4R)-3-ГИДРОКСИ-4-ГИДРОКСИМЕТИЛПИРРОЛИДИН-1-ИЛМЕТИЛ]-3,5-ДИГИДРОПИРРОЛО[3,2-d]ПИРИМИДИН-4-ОНА EA020931B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US16280509P 2009-03-24 2009-03-24
PCT/US2010/028490 WO2010111381A2 (en) 2009-03-24 2010-03-24 Useful pharmaceutical salts of 7-[(3r, 4r)-3-hydroxy-4-hydroxymethyl-pyrrolidin-1-ylmethyl]-3,5-dihydro-pyrrolo[3,2-d]pyrimidin-4-one

Publications (2)

Publication Number Publication Date
EA201190205A1 true EA201190205A1 (ru) 2012-06-29
EA020931B1 EA020931B1 (ru) 2015-02-27

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
EA201190205A EA020931B1 (ru) 2009-03-24 2010-03-24 ПОЛЕЗНЫЕ ФАРМАЦЕВТИЧЕСКИЕ СОЛИ 7-[(3R,4R)-3-ГИДРОКСИ-4-ГИДРОКСИМЕТИЛПИРРОЛИДИН-1-ИЛМЕТИЛ]-3,5-ДИГИДРОПИРРОЛО[3,2-d]ПИРИМИДИН-4-ОНА

Country Status (17)

Country Link
US (1) US8501753B2 (ru)
EP (1) EP2411394B1 (ru)
JP (1) JP5766687B2 (ru)
KR (1) KR101763672B1 (ru)
CN (1) CN102448963B (ru)
AU (1) AU2010230008B2 (ru)
BR (1) BRPI1006534B1 (ru)
CA (1) CA2755950C (ru)
EA (1) EA020931B1 (ru)
ES (1) ES2519568T3 (ru)
IL (1) IL215298A (ru)
MX (1) MX2011009928A (ru)
NZ (1) NZ595590A (ru)
PL (1) PL2411394T3 (ru)
RU (1) RU2489435C2 (ru)
SG (1) SG174517A1 (ru)
WO (1) WO2010111381A2 (ru)

Families Citing this family (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
HRP20130048T1 (hr) 2008-04-23 2013-02-28 Gilead Sciences, Inc. Karba-nukleozidni analozi za antivirusnu terapiju
WO2011035250A1 (en) 2009-09-21 2011-03-24 Gilead Sciences, Inc. Processes and intermediates for the preparation of 1'-substituted carba-nucleoside analogs
EA025311B1 (ru) 2010-07-19 2016-12-30 Гайлид Сайэнсиз, Инк. Способы получения диастереомерно чистых фосфорамидатных пролекарств
ES2524356T3 (es) 2010-07-22 2014-12-05 Gilead Sciences, Inc. Métodos y compuestos para tratar infecciones provocadas por virus Paramyxoviridae
AR090699A1 (es) * 2012-04-18 2014-12-03 Biocryst Pharm Inc Compuestos inhibidores de la actividad de la arn polimerasa viral
TWI740546B (zh) 2014-10-29 2021-09-21 美商基利科學股份有限公司 製備核糖苷的方法
HRP20220355T1 (hr) 2015-09-16 2022-05-13 Gilead Sciences, Inc. Postupci za liječenje infekcija coronaviridae
CN116036112A (zh) 2017-03-14 2023-05-02 吉利德科学公司 治疗猫冠状病毒感染的方法
WO2018204198A1 (en) 2017-05-01 2018-11-08 Gilead Sciences, Inc. Crystalline forms of (s) 2 ethylbutyl 2 (((s) (((2r,3s,4r,5r) 5 (4 aminopyrrolo[2,1-f] [1,2,4]triazin-7-yl)-5-cyano-3,4-dihydroxytetrahydrofuran-2 yl)methoxy)(phenoxy) phosphoryl)amino)propanoate
EP4512475A3 (en) 2017-07-11 2025-05-14 Gilead Sciences, Inc. Compositions comprising an rna polymerase inhibitor and cyclodextrin for treating viral infections
AU2021214911A1 (en) 2020-01-27 2022-07-21 Gilead Sciences, Inc. Methods for treating SARS CoV-2 infections
CN118994170A (zh) 2020-03-12 2024-11-22 吉利德科学公司 制备1'-氰基核苷的方法
EP4132651B1 (en) 2020-04-06 2026-03-18 Gilead Sciences, Inc. Inhalation formulations of 1'-cyano substituted carbanucleoside analogs
ES3041698T3 (en) 2020-05-29 2025-11-13 Gilead Sciences Inc Remdesivir for the treatment of viral infections
CA3187821A1 (en) 2020-06-24 2021-12-30 Gilead Sciences, Inc. 1'-cyano nucleoside analogs and uses thereof
WO2022047065A2 (en) 2020-08-27 2022-03-03 Gilead Sciences, Inc. Compounds and methods for treatment of viral infections
KR102580079B1 (ko) * 2020-10-29 2023-09-19 한양대학교 산학협력단 기생 인덕턴스 감소를 위한 적층형 회로 구조체
GB202110403D0 (en) * 2021-07-20 2021-09-01 Laevoroc Immunology Ulodesine Salt
TW202525810A (zh) 2022-03-02 2025-07-01 美商基利科學股份有限公司 用於治療病毒感染的化合物及方法
US12357577B1 (en) 2024-02-02 2025-07-15 Gilead Sciences, Inc. Pharmaceutical formulations and uses thereof
GB202218782D0 (en) 2022-12-13 2023-01-25 Mehrling Thomas Purine nucleoside phosphorylase inhibitor for metabolic syndrome

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3870732A (en) 1973-08-21 1975-03-11 Velsicol Chemical Corp Mixed salts of aluminum
US5386031A (en) * 1993-12-15 1995-01-31 Warner-Lambert Company Process for the synthesis of 2-amino-3,5-dihydro-7-substituted-4H-pyrrolo[3,]pyrimidin-4-ones
CN1107068C (zh) * 1997-05-29 2003-04-30 诺瓦提斯公司 2－氨基－7－(1－取代的－2－羟乙基)－3,5－二氢－吡咯并[3,2－d]嘧啶－4－酮
ES2363766T3 (es) * 2002-08-21 2011-08-16 Albert Einstein College Of Medicine Of Yeshiva University Inhibidores de nucleosidasas y fosforilasas de nucleosidos.
NZ523970A (en) * 2003-02-04 2005-02-25 Ind Res Ltd Process for preparing inhibitors of nucleoside phoshorylases and nucleosidases
NZ544187A (en) * 2005-12-15 2008-07-31 Ind Res Ltd Deazapurine analogs of 1'-aza-l-nucleosides

Also Published As

Publication number Publication date
CN102448963B (zh) 2015-06-17
CA2755950C (en) 2017-04-25
WO2010111381A2 (en) 2010-09-30
RU2489435C2 (ru) 2013-08-10
SG174517A1 (en) 2011-10-28
MX2011009928A (es) 2012-03-16
KR101763672B1 (ko) 2017-08-01
EA020931B1 (ru) 2015-02-27
PL2411394T3 (pl) 2015-01-30
BRPI1006534B1 (pt) 2021-05-25
IL215298A0 (en) 2011-12-29
NZ595590A (en) 2013-11-29
JP5766687B2 (ja) 2015-08-19
EP2411394A2 (en) 2012-02-01
CA2755950A1 (en) 2010-09-30
KR20120005466A (ko) 2012-01-16
AU2010230008A1 (en) 2011-10-06
EP2411394A4 (en) 2012-08-15
US8501753B2 (en) 2013-08-06
CN102448963A (zh) 2012-05-09
US20120165526A1 (en) 2012-06-28
EP2411394B1 (en) 2014-08-06
AU2010230008B2 (en) 2015-06-04
BRPI1006534A2 (pt) 2016-08-02
HK1170486A1 (en) 2013-03-01
WO2010111381A3 (en) 2011-03-31
RU2011141212A (ru) 2013-04-27
JP2012521992A (ja) 2012-09-20
ES2519568T3 (es) 2014-11-07
IL215298A (en) 2017-04-30

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