PT99281A - Processo para a preparacao de hidroximetil (metilenociclopentil) purinas e de hidroximetil (metilenociclopentil) pirimidinas - Google Patents

Processo para a preparacao de hidroximetil (metilenociclopentil) purinas e de hidroximetil (metilenociclopentil) pirimidinas

Info

Publication number
PT99281A
PT99281A PT99281A PT9928191A PT99281A PT 99281 A PT99281 A PT 99281A PT 99281 A PT99281 A PT 99281A PT 9928191 A PT9928191 A PT 9928191A PT 99281 A PT99281 A PT 99281A
Authority
PT
Portugal
Prior art keywords
methylenocycyclopentil
methylenocyclopentil
purins
hydroximethyl
pyrimidines
Prior art date
Application number
PT99281A
Other languages
English (en)
Other versions
PT99281B (pt
Inventor
Robert Zahler
William A Slusarchyk
Original Assignee
Squibb & Sons Inc
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=PT99281(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Squibb & Sons Inc filed Critical Squibb & Sons Inc
Publication of PT99281A publication Critical patent/PT99281A/pt
Publication of PT99281B publication Critical patent/PT99281B/pt

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic 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
    • C07D239/28Heterocyclic 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
    • C07D239/46Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/47One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic 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
    • C07D239/28Heterocyclic 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
    • C07D239/46Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/52Two oxygen atoms
    • C07D239/54Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic 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
    • C07D239/28Heterocyclic 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
    • C07D239/46Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/52Two oxygen atoms
    • C07D239/54Two oxygen atoms as doubly bound oxygen atoms or as unsubstituted hydroxy radicals
    • C07D239/545Two 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
    • C07D239/553Two 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D473/00Heterocyclic 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)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Other Investigation Or Analysis Of Materials By Electrical Means (AREA)
  • Transition And Organic Metals Composition Catalysts For Addition Polymerization (AREA)
  • Tires In General (AREA)
  • Steroid Compounds (AREA)
PT99281A 1990-10-18 1991-10-18 Processo para a preparacao de hidroximetil (metilenociclopentil) purinas e de hidroximetil (metilenociclopentil) pirimidinas PT99281B (pt)

Applications Claiming Priority (1)

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

Publications (2)

Publication Number Publication Date
PT99281A true PT99281A (pt) 1992-08-31
PT99281B PT99281B (pt) 1999-04-30

Family

ID=24400159

Family Applications (1)

Application Number Title Priority Date Filing Date
PT99281A PT99281B (pt) 1990-10-18 1991-10-18 Processo para a preparacao de hidroximetil (metilenociclopentil) purinas e de hidroximetil (metilenociclopentil) pirimidinas

Country Status (28)

Country Link
US (1) US5206244A (pt)
EP (1) EP0481754B1 (pt)
JP (1) JP2994117B2 (pt)
KR (1) KR0160523B1 (pt)
CN (1) CN1030916C (pt)
AT (1) ATE157095T1 (pt)
AU (1) AU634423B2 (pt)
BR (1) BR1100846A (pt)
CA (1) CA2053339C (pt)
CY (2) CY2063B1 (pt)
DE (3) DE122006000069I1 (pt)
DK (1) DK0481754T3 (pt)
ES (1) ES2104673T3 (pt)
FI (1) FI109905B (pt)
GR (1) GR3025395T3 (pt)
HK (1) HK1001343A1 (pt)
HU (1) HU213207B (pt)
IE (1) IE913451A1 (pt)
IL (1) IL99755A (pt)
LU (1) LU91275I2 (pt)
NL (1) NL300241I1 (pt)
NO (2) NO179906C (pt)
NZ (1) NZ240053A (pt)
PL (1) PL169403B1 (pt)
PT (1) PT99281B (pt)
RU (1) RU2037496C1 (pt)
SG (1) SG70958A1 (pt)
ZA (1) ZA917894B (pt)

Families Citing this family (62)

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WO1996001834A1 (fr) * 1994-07-12 1996-01-25 Yamasa Corporation 2'-desoxy-2'-(methylidene substitue ou non substitue)-4'-thionucleoside
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WO1998009964A1 (en) * 1996-09-03 1998-03-12 Bristol-Myers Squibb Company IMPROVED PROCESS FOR PREPARING THE ANTIVIRAL AGENT [1S-(1α, 3α, 4β)]-2-AMINO-1,9-DIHYDRO-9-[4-HYDROXY-3-(HYDROXYMETHYL)-2-METHYLENECYCLOPENTYL]-6H-PURIN-6-ONE
AU5475799A (en) * 1998-08-10 2000-03-06 Centre National De La Recherche Scientifique Beta-l-2'-deoxy-nucleosides for the treatment of hepatitis
US6444652B1 (en) * 1998-08-10 2002-09-03 Novirio Pharmaceuticals Limited β-L-2'-deoxy-nucleosides for the treatment of hepatitis B
US6432966B2 (en) 1999-10-29 2002-08-13 Smithkline Beecham Corporation Antiviral combinations
ATE312613T1 (de) * 2000-02-29 2005-12-15 Bristol Myers Squibb Co Niedrig dosierte entecavir formulierung und deren verwendung
CN101444511B (zh) * 2000-02-29 2013-01-02 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
WO2001067772A2 (en) * 2000-03-09 2001-09-13 Videoshare, Inc. 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
CN101130543B (zh) * 2002-12-11 2011-06-08 布里斯托尔-迈尔斯斯奎布公司 制备抗病毒药[1S-(1α,3α,4β)]-2-氨基-1,9-二氢-9-[4-羟基-3-(羟甲基)-2-亚甲环戊基]-6H-嘌呤-6-酮的方法
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
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US20090076038A1 (en) * 2007-09-14 2009-03-19 Protia, Llc Deuterium-enriched entecavir
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EP2671888A1 (en) 2008-12-23 2013-12-11 Gilead Pharmasset LLC 3',5'-cyclic nucleoside phosphate analogues
MX2011006891A (es) 2008-12-23 2011-10-06 Pharmasset Inc Fosforamidatos de nucleosidos.
EA201100851A1 (ru) * 2008-12-23 2012-04-30 Фармассет, Инк. Аналоги нуклеозидов
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
US8569491B2 (en) * 2009-10-12 2013-10-29 Hanmi Science Co., Ltd 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
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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
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KR101640503B1 (ko) * 2015-04-15 2016-07-18 동방에프티엘(주) 엔테카비르 일수화물의 개선된 제조방법
JP6912100B2 (ja) * 2016-11-16 2021-07-28 国立研究開発法人国立国際医療研究センター 抗ウイルス活性等の生理活性を有するヌクレオシド誘導体
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
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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
EP0481754B1 (en) 1997-08-20
GR3025395T3 (en) 1998-02-27
LU91275I2 (fr) 2007-06-16
IL99755A0 (en) 1992-08-18
CY2063B1 (en) 1998-06-12
US5206244A (en) 1993-04-27
NO2006018I2 (no) 2008-10-20
PL169403B1 (pl) 1996-07-31
KR0160523B1 (ko) 1998-12-01
DE69127336D1 (de) 1997-09-25
PT99281B (pt) 1999-04-30
EP0481754A3 (en) 1992-09-16
AU8559891A (en) 1992-04-30
NL300241I1 (nl) 2006-12-01
KR920008043A (ko) 1992-05-27
CN1061972A (zh) 1992-06-17
HUT59109A (en) 1992-04-28
IE913451A1 (en) 1992-04-22
FI914928A (fi) 1992-04-19
ZA917894B (en) 1993-03-31
NO179906C (no) 1997-01-08
NO2006018I1 (no) 2006-12-27
NZ240053A (en) 1993-05-26
HU213207B (en) 1997-03-28
DE122006000069I2 (de) 2012-04-19
SG70958A1 (en) 2000-03-21
DK0481754T3 (da) 1997-09-15
NO179906B (no) 1996-09-30
IL99755A (en) 1996-08-04
CN1030916C (zh) 1996-02-07
CA2053339C (en) 2001-05-29
BR1100846A (pt) 2000-04-18
FI914928A0 (fi) 1991-10-18
HU913283D0 (en) 1992-01-28
JP2994117B2 (ja) 1999-12-27
AU634423B2 (en) 1993-02-18
HK1001343A1 (en) 1998-06-12
PL292101A1 (en) 1992-08-10
NO914089D0 (no) 1991-10-17
EP0481754A2 (en) 1992-04-22
DE122006000069I1 (de) 2007-05-24
CA2053339A1 (en) 1992-04-19
ES2104673T3 (es) 1997-10-16
ATE157095T1 (de) 1997-09-15
CY2006008I2 (el) 2016-10-05
NO914089L (no) 1992-04-21
RU2037496C1 (ru) 1995-06-19
DE69127336T2 (de) 1998-01-02
CY2006008I1 (el) 2009-11-04
FI109905B (fi) 2002-10-31
JPH04282373A (ja) 1992-10-07

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