NO2006018I2 - Entekavir - Google Patents

Entekavir

Info

Publication number
NO2006018I2
NO2006018I2 NO2006018C NO2006018C NO2006018I2 NO 2006018 I2 NO2006018 I2 NO 2006018I2 NO 2006018 C NO2006018 C NO 2006018C NO 2006018 C NO2006018 C NO 2006018C NO 2006018 I2 NO2006018 I2 NO 2006018I2
Authority
NO
Norway
Prior art keywords
entecavir
chem
exhibited
compounds
formula
Prior art date
Application number
NO2006018C
Other languages
English (en)
Other versions
NO2006018I1 (no
Original Assignee
E R Squibb & Sons Llc
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=24400159&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=NO2006018(I2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by E R Squibb & Sons Llc filed Critical E R Squibb & Sons Llc
Publication of NO2006018I1 publication Critical patent/NO2006018I1/no
Publication of NO2006018I2 publication Critical patent/NO2006018I2/no

Links

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
    • 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
    • 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
    • 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
    • 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
    • C07D239/52—Two oxygen atoms
    • C07D239/54—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
    • 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
    • C07D239/52—Two oxygen atoms
    • C07D239/54—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
    • C07D239/545—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals with other 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
    • C07D239/553—Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals with other 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 with halogen atoms or nitro radicals directly attached to ring carbon atoms, e.g. fluorouracil
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Oncology (AREA)
  • Animal Behavior & Ethology (AREA)
  • Communicable Diseases (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Virology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Transition And Organic Metals Composition Catalysts For Addition Polymerization (AREA)
  • Tires In General (AREA)
  • Other Investigation Or Analysis Of Materials By Electrical Means (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Steroid Compounds (AREA)
NO2006018C 1990-10-18 2006-12-05 Entekavir NO2006018I2 (no)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US59956890A 1990-10-18 1990-10-18

Publications (2)

Publication Number Publication Date
NO2006018I1 NO2006018I1 (no) 2006-12-27
NO2006018I2 true NO2006018I2 (no) 2008-10-20

Family

ID=24400159

Family Applications (2)

Application Number Title Priority Date Filing Date
NO914089A NO179906C (no) 1990-10-18 1991-10-17 Fremgangsmåte for fremstilling av hydroksymetyl(metylencyklopentyl) puriner og -pyrimidiner
NO2006018C NO2006018I2 (no) 1990-10-18 2006-12-05 Entekavir

Family Applications Before (1)

Application Number Title Priority Date Filing Date
NO914089A NO179906C (no) 1990-10-18 1991-10-17 Fremgangsmåte for fremstilling av hydroksymetyl(metylencyklopentyl) puriner og -pyrimidiner

Country Status (28)

Country Link
US (1) US5206244A (no)
EP (1) EP0481754B1 (no)
JP (1) JP2994117B2 (no)
KR (1) KR0160523B1 (no)
CN (1) CN1030916C (no)
AT (1) ATE157095T1 (no)
AU (1) AU634423B2 (no)
BR (1) BR1100846A (no)
CA (1) CA2053339C (no)
CY (2) CY2063B1 (no)
DE (3) DE69127336T2 (no)
DK (1) DK0481754T3 (no)
ES (1) ES2104673T3 (no)
FI (1) FI109905B (no)
GR (1) GR3025395T3 (no)
HK (1) HK1001343A1 (no)
HU (1) HU213207B (no)
IE (1) IE913451A1 (no)
IL (1) IL99755A (no)
LU (1) LU91275I2 (no)
NL (1) NL300241I1 (no)
NO (2) NO179906C (no)
NZ (1) NZ240053A (no)
PL (1) PL169403B1 (no)
PT (1) PT99281B (no)
RU (1) RU2037496C1 (no)
SG (1) SG70958A1 (no)
ZA (1) ZA917894B (no)

Families Citing this family (62)

* Cited by examiner, † Cited by third party
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EP0630897A3 (en) * 1993-06-25 1995-03-01 Bristol Myers Squibb Co 3-hydroxy-4-hydroxymethyl-2-methylene-cyclopentyl purines and pyrimidines.
US5811408A (en) * 1994-07-12 1998-09-22 Yamasa Corporation 2'-deoxy-2'-(substituted or unsubstituted)methylidene-4'-thionucleosides
AU4303996A (en) * 1994-12-19 1996-07-10 Novartis Ag 6'-substituted carbocyclic nucleosides
GB9520363D0 (en) * 1995-10-05 1995-12-06 Chiroscience Ltd Compounds
AU4090697A (en) * 1996-09-03 1998-03-26 Bristol-Myers Squibb Company Improved process for preparing the antiviral agent {1s-(1alpha, 3alpha, 4beta)}-2-amino-1,9-dihydro-9-{4-hydroxy-3-(hydroxymethyl)-2 -methylenecyclopentyl}-6h-purin-6-one
US6444652B1 (en) * 1998-08-10 2002-09-03 Novirio Pharmaceuticals Limited β-L-2'-deoxy-nucleosides for the treatment of hepatitis B
DK1431304T3 (en) * 1998-08-10 2015-03-02 Novartis Ag Beta - L-2'-deoxynucleosides for the treatment of hepatitis B
US6432966B2 (en) 1999-10-29 2002-08-13 Smithkline Beecham Corporation Antiviral combinations
EP1642582A1 (en) 2000-02-29 2006-04-05 Bristol-Myers Squibb Company Low dose entecavir formulation and use
CN101385732A (zh) * 2000-02-29 2009-03-18 布里斯托尔-迈尔斯斯奎布公司 低剂量艾替开韦制剂及其应用
US20020056123A1 (en) * 2000-03-09 2002-05-09 Gad Liwerant Sharing a streaming video
MY131488A (en) * 2002-04-08 2007-08-30 Bristol Myers Squibb Co Low dose liquid entecavir formulations and use
US7153691B2 (en) * 2002-11-13 2006-12-26 G6 Science Corp. Method of identifying and assessing DNA euchromatin in biological cells for detecting disease, monitoring wellness, assessing bio-activity, and screening pharmacological agents
EP1644384B1 (en) * 2002-12-11 2012-10-31 Bristol-Myers Squibb Company Process and intermediates for the synthesis of entecavir
US7511139B2 (en) * 2004-06-04 2009-03-31 Bristol-Myers Squibb Company Process for the preparation of entecavir and novel intermediates thereof via carbon-silicon oxidation
TW200540175A (en) * 2004-06-04 2005-12-16 Bristol Myers Squibb Co Process for the preparation of entecavir and novel intermediates thereof via carbon-silicon oxidation
CN100379736C (zh) * 2005-05-13 2008-04-09 上海仲夏化学有限公司 恩替卡韦的制备方法
CN1699366A (zh) * 2005-06-03 2005-11-23 北京市典范科技有限责任公司 嘌呤衍生物
CN1907987B (zh) * 2005-08-03 2010-05-05 江苏正大天晴药业股份有限公司 恩地卡韦酸加成盐及其制备方法和用途
US20070060599A1 (en) * 2005-09-09 2007-03-15 Dimarco John D Crystalline forms of [1S-(1alpha, 3alpha, 4beta)]-2-amino-1,9-dihydro-9-[4-hydroxy-3-(hydroxymethyl)-2-methylenecyclopentyl]-6H-purin-6-one
CN101016299B (zh) * 2006-02-09 2010-05-12 北京典范科技有限责任公司 制备嘌呤衍生物的新方法
CN101130542B (zh) * 2006-08-24 2010-08-04 江苏正大天晴药业股份有限公司 抗病毒核苷类似物的合成方法
CN101210015B (zh) * 2006-12-26 2010-09-22 上海国创医药有限公司 一种乙肝治疗药物恩替卡韦的制备方法
CN101245068A (zh) * 2007-02-14 2008-08-20 浙江医药股份有限公司新昌制药厂 结晶型态的恩替卡韦及其制备方法和其药物组合物及用途
CN101074217B (zh) * 2007-04-04 2010-11-24 北京精华耀邦医药科技有限公司 通过制备色谱分离得到高纯度恩替卡韦关键中间体的方法
PT2514750E (pt) 2007-06-18 2014-01-23 Sunshine Lake Pharma Co Ltd Tiazolil dihidropirimidinas substituídas com bromo-fenilo
US20090076038A1 (en) * 2007-09-14 2009-03-19 Protia, Llc Deuterium-enriched entecavir
US8173621B2 (en) 2008-06-11 2012-05-08 Gilead Pharmasset Llc Nucleoside cyclicphosphates
TW201010692A (en) 2008-06-19 2010-03-16 Public Univ Corp Nagoya City Univ Pharmaceutical composition for treatment or prevention of hbv infection
WO2010075517A2 (en) * 2008-12-23 2010-07-01 Pharmasset, Inc. Nucleoside analogs
PA8855801A1 (es) 2008-12-23 2010-07-27 Sintesis de nucleosidos de purina
NZ593648A (en) * 2008-12-23 2013-09-27 Gilead Pharmasset Llc Nucleoside phosphoramidates
KR101150254B1 (ko) * 2008-12-26 2012-06-12 한미사이언스 주식회사 신규 중간체 및 이를 활용한 엔테카비르 제조방법
CN101531660B (zh) * 2009-04-14 2012-07-04 安徽贝克联合制药有限公司 一种恩替卡韦一水合物的工业化生产工艺
WO2011046303A2 (en) 2009-10-12 2011-04-21 Hanmi Holdings Co., Ltd. Novel method for preparing entecavir and intermediate used therein
US9700560B2 (en) * 2009-11-16 2017-07-11 University Of Georgia Research Foundation, Inc. 2′-fluoro-6′-methylene carbocyclic nucleosides and methods of treating viral infections
CN101759698B (zh) * 2009-12-15 2012-01-18 上海医药集团股份有限公司 一种恩替卡韦的制备方法
US8481728B2 (en) * 2010-02-16 2013-07-09 Scinopharm Taiwan, Ltd. Process for preparing entecavir and its intermediates
ES2551944T3 (es) 2010-03-31 2015-11-24 Gilead Pharmasset Llc (S)-2-(((S)-(((2R,3R,4R,5R)-5-(2,4-dioxo-3,4-dihidropirimidin-1-(2H)-il)-4-fluoro-3-hidroxi-4-metiltetrahidrofuran-2-il)metoxi)(fenoxi)fosforil)amino)propanoato de isopropilo cristalino
CA2705953C (en) 2010-05-31 2018-05-01 Alphora Research Inc. Carbanucleoside synthesis and intermediate compounds useful therein
EP2474548A1 (en) * 2010-12-23 2012-07-11 Esteve Química, S.A. Preparation process of an antiviral drug and intermediates thereof
EP2508172A1 (en) 2011-04-06 2012-10-10 Zentiva, a.s. Stable and uniform formulations of entecavir and preparation method thereof
CN102491960A (zh) * 2011-11-16 2012-06-13 福建广生堂药业股份有限公司 一种合成恩替卡韦的中间体及其制备方法和应用
EP2597096A1 (en) 2011-11-24 2013-05-29 Esteve Química, S.A. Process for preparing entecavir and intermediates thereof
CN103304375B (zh) * 2012-03-12 2017-04-12 浙江奥翔药业股份有限公司 恩替卡韦的合成中间体及其制备方法
JP2015520144A (ja) 2012-05-11 2015-07-16 アクロン・モレキュールズ・アクチェンゲゼルシャフトＡｋｒｏｎ Ｍｏｌｅｃｕｌｅｓ Ａｇ 疼痛の治療のための化合物の使用
KR102186030B1 (ko) 2012-10-29 2020-12-03 시플라 리미티드 항 바이러스성 포스포네이트 유사체 및 이의 제조를 위한 방법
WO2015014737A1 (en) 2013-07-29 2015-02-05 Sanovel Ilac Sanayi Ve Ticaret A.S. Multilayer tablet formulations comprising tenofovir and entecavir
WO2015051900A1 (en) 2013-10-08 2015-04-16 Pharmathen S.A. Process for the preparation of entecavir through novel intermediates
KR101640503B1 (ko) * 2015-04-15 2016-07-18 동방에프티엘(주) 엔테카비르 일수화물의 개선된 제조방법
KR101640504B1 (ko) * 2015-04-15 2016-07-18 동방에프티엘(주) 엔테카비르 일수화물의 제조방법
US10933067B2 (en) 2016-11-16 2021-03-02 National Center For Global Health And Medicine Nucleoside derivative having physiological activity such as antiviral activity
CN108203435B (zh) * 2016-12-16 2020-09-04 正大天晴药业集团股份有限公司 一种利用Boc保护基的恩替卡韦的制备方法
CN106749251A (zh) * 2017-01-17 2017-05-31 博瑞生物医药泰兴市有限公司 一种恩替卡韦中间体的合成与提纯方法
KR102197257B1 (ko) * 2017-10-19 2020-12-31 단국대학교 천안캠퍼스 산학협력단 엔테카비어 지방산 에스테르 유도체 수성현탁액의 안정화 조성물
CN109956975B (zh) * 2017-12-22 2020-11-06 浙江柏拉阿图医药科技有限公司 肝递送恩替卡韦前体药物核苷环磷酸酯化合物及应用
JP2022512397A (ja) * 2018-12-12 2022-02-03 ヤンセン バイオファーマ インク． 抗ウイルス薬としてのシクロペンチルヌクレオシド類似体
CN113024574B (zh) * 2019-12-25 2024-03-29 南通诺泰生物医药技术有限公司 一种氧杂二环己烷类化合物的制备方法
CN111732589B (zh) * 2020-06-08 2021-07-30 王乔 一种改进的恩替卡韦中间体合成工艺以及改进的恩替卡韦合成工艺
CN112625041A (zh) * 2020-12-25 2021-04-09 常州博海威医药科技股份有限公司 恩替卡韦的新制备方法以及中间体
CN115433188A (zh) * 2022-09-29 2022-12-06 苏州东瑞制药有限公司 一种恩替卡韦的制备方法
CN115819422A (zh) * 2022-12-13 2023-03-21 淄博矿业集团有限责任公司 恩替卡韦中间体制备新工艺方法及分析方法

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Also Published As

Publication number Publication date
CN1030916C (zh) 1996-02-07
DE122006000069I1 (de) 2007-05-24
DE69127336T2 (de) 1998-01-02
ES2104673T3 (es) 1997-10-16
DE122006000069I2 (de) 2012-04-19
PT99281A (pt) 1992-08-31
PL169403B1 (pl) 1996-07-31
PL292101A1 (en) 1992-08-10
ATE157095T1 (de) 1997-09-15
RU2037496C1 (ru) 1995-06-19
EP0481754A3 (en) 1992-09-16
HU213207B (en) 1997-03-28
NO179906B (no) 1996-09-30
JPH04282373A (ja) 1992-10-07
DK0481754T3 (da) 1997-09-15
HUT59109A (en) 1992-04-28
BR1100846A (pt) 2000-04-18
GR3025395T3 (en) 1998-02-27
ZA917894B (en) 1993-03-31
NO179906C (no) 1997-01-08
FI109905B (fi) 2002-10-31
IL99755A0 (en) 1992-08-18
FI914928A (fi) 1992-04-19
AU8559891A (en) 1992-04-30
JP2994117B2 (ja) 1999-12-27
CN1061972A (zh) 1992-06-17
PT99281B (pt) 1999-04-30
US5206244A (en) 1993-04-27
CY2006008I1 (el) 2009-11-04
NZ240053A (en) 1993-05-26
IE913451A1 (en) 1992-04-22
LU91275I2 (fr) 2007-06-16
SG70958A1 (en) 2000-03-21
EP0481754B1 (en) 1997-08-20
KR0160523B1 (ko) 1998-12-01
NO914089L (no) 1992-04-21
HU913283D0 (en) 1992-01-28
KR920008043A (ko) 1992-05-27
CA2053339A1 (en) 1992-04-19
CY2006008I2 (el) 2016-10-05
EP0481754A2 (en) 1992-04-22
DE69127336D1 (de) 1997-09-25
CA2053339C (en) 2001-05-29
IL99755A (en) 1996-08-04
AU634423B2 (en) 1993-02-18
CY2063B1 (en) 1998-06-12
NO914089D0 (no) 1991-10-17
FI914928A0 (fi) 1991-10-18
NL300241I1 (nl) 2006-12-01
NO2006018I1 (no) 2006-12-27
HK1001343A1 (en) 1998-06-12

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