EA201170780A1 - Урацильные циклопропилнуклеотиды - Google Patents

Урацильные циклопропилнуклеотиды

Info

Publication number
EA201170780A1
EA201170780A1 EA201170780A EA201170780A EA201170780A1 EA 201170780 A1 EA201170780 A1 EA 201170780A1 EA 201170780 A EA201170780 A EA 201170780A EA 201170780 A EA201170780 A EA 201170780A EA 201170780 A1 EA201170780 A1 EA 201170780A1
Authority
EA
Eurasian Patent Office
Prior art keywords
benzyl
hydrogen
cycloalkyl
alkyl
compounds
Prior art date
Application number
EA201170780A
Other languages
English (en)
Other versions
EA020244B1 (ru
Inventor
Тим Хьюго Мария Йонкерс
Пьер Жан-Мари Бернар Рабуассон
Стивен Морис Паула Ван Хоф
Лен Анна Мария Вандекеркхове
Коэн Вандик
Original Assignee
СЕНТОКОР ОРТО БАЙОТЕК ПРОДАКТС Эл.Пи.
Медивир Аб
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 СЕНТОКОР ОРТО БАЙОТЕК ПРОДАКТС Эл.Пи., Медивир Аб filed Critical СЕНТОКОР ОРТО БАЙОТЕК ПРОДАКТС Эл.Пи.
Publication of EA201170780A1 publication Critical patent/EA201170780A1/ru
Publication of EA020244B1 publication Critical patent/EA020244B1/ru

Links

Classifications

    • 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
    • C07H19/10—Pyrimidine radicals with the saccharide radical esterified by phosphoric or polyphosphoric acids
    • 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
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Virology (AREA)
  • Molecular Biology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Engineering & Computer Science (AREA)
  • Biochemistry (AREA)
  • Genetics & Genomics (AREA)
  • Biotechnology (AREA)
  • AIDS & HIV (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Pulmonology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Описаны соединения формулы I, включающие любые их возможные стереоизомеры, где Rпредставляет собой водород или галоген; Rпредставляет собой монофосфатный, дифосфатный или трифосфатный сложный эфир; или Rпредставляет собой группу формулы (II), Rпредставляет собой необязательно замещенный фенил; нафтил; индолил или N-C-Салкилоксикарбонилиндолил; Rпредставляет собой водород, C-Салкил, бензил; Rпредставляет собой водород, C-Салкил, бензил; или Rи Rвместе с атомом углерода, к которому они присоединены, образуют С-Сциклоалкил; Rпредставляет собой C-Салкил, С-Сциклоалкил, С-Салкенил, бензил или необязательно замещенный фенил, или их фармацевтически приемлемая соль или сольват, а также фармацевтические составы и применение соединений I в качестве ингибиторов HCV.
EA201170780A 2008-12-08 2009-12-08 Урацильные циклопропилнуклеотиды EA020244B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP08171006 2008-12-08
PCT/EP2009/066562 WO2010066699A1 (en) 2008-12-08 2009-12-08 Uracyl cyclopropyl nucleotides

Publications (2)

Publication Number Publication Date
EA201170780A1 true EA201170780A1 (ru) 2011-12-30
EA020244B1 EA020244B1 (ru) 2014-09-30

Family

ID=40852521

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201170780A EA020244B1 (ru) 2008-12-08 2009-12-08 Урацильные циклопропилнуклеотиды

Country Status (21)

Country Link
US (1) US8399429B2 (ru)
EP (1) EP2373671B1 (ru)
JP (1) JP5683480B2 (ru)
KR (1) KR20110104000A (ru)
CN (1) CN102256991B (ru)
AP (1) AP2011005717A0 (ru)
AR (1) AR074504A1 (ru)
AU (1) AU2009326125B2 (ru)
BR (1) BRPI0922681A2 (ru)
CA (1) CA2745523C (ru)
CL (1) CL2011001364A1 (ru)
EA (1) EA020244B1 (ru)
ES (1) ES2525007T3 (ru)
IL (1) IL212897A (ru)
MX (1) MX2011006023A (ru)
PA (1) PA8852101A1 (ru)
SG (1) SG171973A1 (ru)
TW (1) TW201036989A (ru)
UY (1) UY32308A (ru)
WO (1) WO2010066699A1 (ru)
ZA (1) ZA201104231B (ru)

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* Cited by examiner, † Cited by third party
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JO3027B1 (ar) * 2009-05-14 2016-09-05 Janssen Products Lp نيوكليوسيدات يوراسيل سبيرواوكسيتان
US9676797B2 (en) 2015-09-02 2017-06-13 Abbvie Inc. Anti-viral compounds
SG11201407336PA (en) 2012-05-25 2015-03-30 Janssen Sciences Ireland Uc Uracyl spirooxetane nucleosides
MY176133A (en) * 2012-11-16 2020-07-24 Nucana Biomed Ltd Process for preparing nucleoside prodrugs
BR112015020472B1 (pt) * 2013-03-08 2021-01-19 Nanjing Sanhome Pharmaceutical Co., Ltd. composto de fosforamidato de nucleosídeo, composição farmacêutica e uso do mesmo
CN103848876B (zh) * 2013-03-25 2016-05-11 安徽贝克联合制药有限公司 一种核苷磷酰胺前药及其制备方法和其应用
CN105705511A (zh) 2013-04-12 2016-06-22 艾其林医药公司 用于治疗hcv的氘化核苷前药
CN105348342B (zh) * 2014-09-30 2018-09-21 南京正大天晴制药有限公司 核苷氨基磷酸酯化合物及药物组合物和用途
WO2016073756A1 (en) * 2014-11-06 2016-05-12 Enanta Pharmaceuticals, Inc. Deuterated nucleoside/tide derivatives
CN105801646B (zh) * 2014-12-31 2019-08-16 浙江大德药业集团有限公司 炔基取代的核苷氨基磷酸酯
WO2016134053A1 (en) * 2015-02-18 2016-08-25 Abbvie Inc. Anti-viral compounds
KR102363946B1 (ko) 2015-03-06 2022-02-17 아테아 파마슈티컬즈, 인크. HCV 치료를 위한 β-D-2'-데옥시-2'-α-플루오로-2'-β-C-치환된-2-변형된-N6-치환된 퓨린 뉴클레오티드
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
KR20190043602A (ko) 2016-09-07 2019-04-26 아테아 파마슈티컬즈, 인크. Rna 바이러스 치료를 위한 2'-치환된-n6-치환된 퓨린 뉴클레오티드
GEP20237457B (en) 2017-02-01 2023-01-10 Atea Pharmaceuticals Inc Nucleotide hemi-sulfate salt for treatment of hepatitis c virus
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 (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4916122A (en) * 1987-01-28 1990-04-10 University Of Georgia Research Foundation, Inc. 3'-Azido-2',3'-dideoxyuridine anti-retroviral composition
DE69334250D1 (de) 1992-12-29 2009-01-29 Abbott Lab Verfahren und Intermediate zur Herstellung von retroviralen Proteasehemmern
US20010021509A1 (en) * 1997-10-23 2001-09-13 Sathe Ganesh Madhusudan cDNA clone HNEAA81 that encodes a human 7-transmembrane receptor
EP2799442A1 (en) * 2002-06-28 2014-11-05 IDENIX Pharmaceuticals, Inc. Modified 2' and 3' -nucleoside prodrugs for treating flaviridae infections
BRPI0407374A (pt) * 2003-02-19 2006-01-10 Univ Yale Análogos de nucleosìdeo antiviral e métodos para tratar infecções virais, especialmente infecções de hiv
ATE490788T1 (de) * 2003-04-25 2010-12-15 Gilead Sciences Inc Antivirale phosphonate analoge
AU2006222563A1 (en) * 2005-03-08 2006-09-14 Biota Scientific Management Pty Ltd. Bicyclic nucleosides and nucleotides as therapeutic agents
EP2361922B1 (en) 2006-10-10 2012-08-22 Janssen Products, L.P. Intermediate to HCV-Nucleoside Inhibitors

Also Published As

Publication number Publication date
MX2011006023A (es) 2011-06-28
JP2012510980A (ja) 2012-05-17
PA8852101A1 (es) 2010-07-27
WO2010066699A1 (en) 2010-06-17
AU2009326125A1 (en) 2010-06-17
SG171973A1 (en) 2011-07-28
IL212897A (en) 2013-12-31
CA2745523A1 (en) 2010-06-17
JP5683480B2 (ja) 2015-03-11
KR20110104000A (ko) 2011-09-21
TW201036989A (en) 2010-10-16
AP2011005717A0 (en) 2011-06-30
CL2011001364A1 (es) 2011-09-23
EP2373671B1 (en) 2014-09-10
CA2745523C (en) 2017-07-04
EA020244B1 (ru) 2014-09-30
UY32308A (es) 2010-06-30
EP2373671A1 (en) 2011-10-12
AR074504A1 (es) 2011-01-19
US8399429B2 (en) 2013-03-19
IL212897A0 (en) 2011-07-31
ZA201104231B (en) 2012-11-28
US20110230436A1 (en) 2011-09-22
BRPI0922681A2 (pt) 2016-01-05
CN102256991A (zh) 2011-11-23
AU2009326125B2 (en) 2015-03-12
ES2525007T3 (es) 2014-12-17
CN102256991B (zh) 2015-08-12

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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): AM AZ BY KG MD TJ TM

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 RU