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
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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.)
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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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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)

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HUE025528T2 (en) 2008-04-23 2016-05-30 Gilead Sciences Inc 1'-substituted carba-nucleoside analogs for antiviral treatment
MX2012003126A (es) 2009-09-21 2012-06-19 Gilead Sciences Inc Procesos e intermedios para la preparacion de analogos de 1'-carbonucleosidos sustituidos.
AU2011282241B2 (en) 2010-07-19 2015-07-30 Gilead Sciences, Inc. Methods for the preparation of diasteromerically pure phosphoramidate prodrugs
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
TWI687432B (zh) 2014-10-29 2020-03-11 美商基利科學股份有限公司 絲狀病毒科病毒感染之治療
DK3785717T3 (da) 2015-09-16 2022-03-21 Gilead Sciences Inc Fremgangsmåder til behandling af coronaviridae-infektioner
US10682368B2 (en) 2017-03-14 2020-06-16 Gilead Sciences, Inc. Methods of treating feline coronavirus infections
CA3059777C (en) 2017-05-01 2023-02-21 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
WO2019014247A1 (en) 2017-07-11 2019-01-17 Gilead Sciences, Inc. COMPOSITIONS COMPRISING POLYMERASE RNA INHIBITOR AND CYCLODEXTRIN FOR THE TREATMENT OF VIRAL INFECTIONS
JP2023512656A (ja) 2020-01-27 2023-03-28 ギリアード サイエンシーズ， インコーポレイテッド ＳＡＲＳ ＣｏＶ－２感染を治療するための方法
KR20220153619A (ko) 2020-03-12 2022-11-18 길리애드 사이언시즈, 인코포레이티드 1'-시아노 뉴클레오사이드의 제조 방법
CA3172483A1 (en) 2020-04-06 2021-10-14 Scott Ellis Inhalation formulations of 1'-cyano substituted carbanucleoside analogs
TW202203941A (zh) 2020-05-29 2022-02-01 美商基利科學股份有限公司 瑞德西韋之治療方法
PE20230618A1 (es) 2020-06-24 2023-04-14 Gilead Sciences Inc Analogos de nucleosido de 1'-ciano y usos de los mismos
IL300453A (en) 2020-08-27 2023-04-01 Gilead Sciences Inc COMPOSITIONS AND METHODS FOR THE 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
KR20240154647A (ko) 2022-03-02 2024-10-25 길리애드 사이언시즈, 인코포레이티드 바이러스성 감염 치료를 위한 화합물 및 방법
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

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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
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Also Published As

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

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