ES2187989T3 - Composicion de analogos de nucleotido y procedimiento de sintesis. - Google Patents

Composicion de analogos de nucleotido y procedimiento de sintesis.

Info

Publication number
ES2187989T3
ES2187989T3 ES98937022T ES98937022T ES2187989T3 ES 2187989 T3 ES2187989 T3 ES 2187989T3 ES 98937022 T ES98937022 T ES 98937022T ES 98937022 T ES98937022 T ES 98937022T ES 2187989 T3 ES2187989 T3 ES 2187989T3
Authority
ES
Spain
Prior art keywords
pmpa
composition
diethyl
useful
nucleotide analogs
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Lifetime
Application number
ES98937022T
Other languages
English (en)
Inventor
John D Munger Jr
John C Rohloff
Lisa M Schultze
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Gilead Sciences Inc
Original Assignee
Gilead Sciences 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=26732232&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=ES2187989(T3) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Priority claimed from US08/900,752 external-priority patent/US5935946A/en
Application filed by Gilead Sciences Inc filed Critical Gilead Sciences Inc
Application granted granted Critical
Publication of ES2187989T3 publication Critical patent/ES2187989T3/es
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6561—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings
    • C07F9/65616—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing systems of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring or ring system, with or without other non-condensed hetero rings containing the ring system having three or more than three double bonds between ring members or between ring members and non-ring members, e.g. purine or analogs
    • 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
    • A61P31/18—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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/20—Antivirals for DNA viruses
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D473/00—Heterocyclic compounds containing purine ring systems
    • C07D473/26—Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
    • C07D473/32—Nitrogen atom
    • C07D473/34—Nitrogen atom attached in position 6, e.g. adenine

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Virology (AREA)
  • General Health & Medical Sciences (AREA)
  • Molecular Biology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Oncology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Communicable Diseases (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Biochemistry (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Engineering & Computer Science (AREA)
  • Biotechnology (AREA)
  • AIDS & HIV (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Saccharide Compounds (AREA)
  • Medicinal Preparation (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Steroid Compounds (AREA)

Abstract

La invención se refiere a una composición que comprende la 9-{[}2-(R)-{[}{[}Bis{[}{[}isopropoxicarbonil{oxi{]}metoxi{]}fosfinoil{]}metoxi{]}propil{]}adenina ("bis(POC)PMPA") y ácido fumárico (1: 1). Esta composición es útil como intermedio en la elaboración de compuestos antivirales, o bien para la administración a pacientes en guisa de terapia o de profilaxis antiviral. La invención es particularmente útil en la administración oral. La invención se refiere también a los procedimientos relativos a la elaboración de la (R)-9-{[}2-{(}fosfonometoxi{ propil{]}adenina ("PMPA") y los intermedio para la síntesis de la PMPA. Entre las variantes figuran el t-butoxido de litio, la 9-{(}2-hidroxipropil{ adenina y el dietil p-toluenosulfonilmetoxi-fosfonato en un solvente orgánico como el dimetilformamido. La reacción da preparaciones de dietil PMPA que tienen un perfil de subproducto mejorado respecto de los procedimientos utilizados anteriormente para la elaboración de dietil PMPA.
ES98937022T 1997-07-25 1998-07-23 Composicion de analogos de nucleotido y procedimiento de sintesis. Expired - Lifetime ES2187989T3 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US5377797P 1997-07-25 1997-07-25
US08/900,752 US5935946A (en) 1997-07-25 1997-07-25 Nucleotide analog composition and synthesis method

Publications (1)

Publication Number Publication Date
ES2187989T3 true ES2187989T3 (es) 2003-06-16

Family

ID=26732232

Family Applications (3)

Application Number Title Priority Date Filing Date
ES98937022T Expired - Lifetime ES2187989T3 (es) 1997-07-25 1998-07-23 Composicion de analogos de nucleotido y procedimiento de sintesis.
ES02010677T Expired - Lifetime ES2249511T3 (es) 1997-07-25 1998-07-23 Composiciones de analogos de nucleotido y procedimiento de sintesis.
ES02010678T Expired - Lifetime ES2236389T3 (es) 1997-07-25 1998-07-23 Composicion de analogos de nucleotidos y procedimiento de sintesis.

Family Applications After (2)

Application Number Title Priority Date Filing Date
ES02010677T Expired - Lifetime ES2249511T3 (es) 1997-07-25 1998-07-23 Composiciones de analogos de nucleotido y procedimiento de sintesis.
ES02010678T Expired - Lifetime ES2236389T3 (es) 1997-07-25 1998-07-23 Composicion de analogos de nucleotidos y procedimiento de sintesis.

Country Status (19)

Country Link
EP (1) EP0998480B1 (es)
JP (7) JP4173202B2 (es)
KR (3) KR100707505B1 (es)
CN (2) CN1251679C (es)
AT (3) ATE305009T1 (es)
AU (1) AU756793B2 (es)
BR (1) BR9811045A (es)
CA (1) CA2298059C (es)
DE (3) DE69831694T2 (es)
DK (2) DK0998480T3 (es)
ES (3) ES2187989T3 (es)
HK (2) HK1051360B (es)
ID (1) ID24701A (es)
IN (1) IN190780B (es)
NZ (1) NZ501287A (es)
PT (2) PT1243590E (es)
SG (2) SG106657A1 (es)
TW (2) TWI224103B (es)
WO (1) WO1999005150A1 (es)

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ATE305009T1 (de) * 1997-07-25 2005-10-15 Gilead Sciences Inc Nukleotid-analog zusamensetzung und synthese verfahren
GB0013407D0 (en) * 2000-06-02 2000-07-26 Astrazeneca Ab Forms of a chemical compound
US20020119443A1 (en) * 2000-07-21 2002-08-29 Gilead Sciences, Inc. Prodrugs of phosphonate nucleotide analogues and methods for selecting and making same
UA93354C2 (ru) * 2004-07-09 2011-02-10 Гилиад Сайенсиз, Инк. Местный противовирусный препарат
TWI471145B (zh) 2005-06-13 2015-02-01 Bristol Myers Squibb & Gilead Sciences Llc 單一式藥學劑量型
CN100352823C (zh) * 2005-08-19 2007-12-05 浙江车头制药有限公司 一种腺嘌呤衍生物的制备方法
CN100396689C (zh) * 2006-03-07 2008-06-25 中国医学科学院医药生物技术研究所 一组具有抑制hiv-1/hbv病毒复制活性的替诺福韦单酯化合物
ES2532502T3 (es) 2006-07-12 2015-03-27 Mylan Laboratories Limited Proceso para la preparación de tenofovir
AU2008253803A1 (en) * 2007-05-22 2008-11-27 Ultimorphix Technolgies B.V. Tenofovir disoproxil hemi-fumaric acid Co-crystal
WO2010026603A2 (en) * 2008-09-05 2010-03-11 Matrix Laboratories Limited Novel amine salts of tenofovir, process for producing the same and use thereof in production of tenofovir dioproxil
CN101906119B (zh) * 2009-06-03 2012-12-26 中国人民解放军军事医学科学院毒物药物研究所 制备替诺福韦的新方法
EP2389929A1 (en) 2010-05-30 2011-11-30 Abdi Ibrahim Ilac Sanayi ve Ticaret Anonim Sirketi Pharmaceutical formulations of tenofovir
WO2012137227A2 (en) 2011-04-08 2012-10-11 Laurus Labs Private Limited Solid forms of antiretroviral compounds, process for the preparation and their pharmaceutical composition thereof
CN102295660A (zh) * 2011-07-04 2011-12-28 常州大学 泰诺福韦的合成工艺
ES2608871T5 (es) 2011-08-16 2024-04-04 Gilead Sciences Inc Alafenamide hemifumarate de tenofovir
CN103626803B (zh) * 2012-08-23 2017-12-15 四川海思科制药有限公司 替诺福韦二吡呋酯的固体及其制备方法和用途
CN103665043B (zh) 2012-08-30 2017-11-10 江苏豪森药业集团有限公司 一种替诺福韦前药及其在医药上的应用
CN103230404A (zh) * 2013-05-14 2013-08-07 福建广生堂药业股份有限公司 替诺福韦二吡呋酯或其药用盐的新用途
PT2860184T (pt) 2013-10-09 2018-11-20 Zentiva Ks Sal de di-hidrogenofosfato de tenofovir disoproxil
EP2860185A1 (en) 2013-10-09 2015-04-15 Zentiva, k.s. An improved process for the preparation of Tenofovir disoproxil and pharmaceutically acceptable salts thereof
CN103483385B (zh) * 2013-10-11 2015-11-18 福建广生堂药业股份有限公司 替诺福韦单酯富马酸盐的新晶型及其制备方法
CN104688747B (zh) * 2013-12-04 2019-04-12 重庆药友制药有限责任公司 包含富马酸替诺福韦二吡呋酯的药物组合物
CN104725423A (zh) * 2013-12-18 2015-06-24 山东新时代药业有限公司 一种富马酸替诺福韦二吡呋酯的合成方法
CN103705478B (zh) * 2013-12-23 2020-02-07 浙江华海药业股份有限公司 含有富马酸替诺福韦二吡呋酯的口服片剂
CN104744512B (zh) * 2013-12-26 2017-01-11 成都伊诺达博医药科技有限公司 一种“一锅法”制备泰诺福韦的新工艺
KR20160003532A (ko) 2014-07-01 2016-01-11 한미약품 주식회사 테노포비어 디소프록실 인산염과, 비금속염 붕해제 및 비금속염 활택제를 포함하는 약학 조성물
CN104288118A (zh) * 2014-07-08 2015-01-21 南京卡文迪许生物工程技术有限公司 富马酸替诺福韦二吡呋酯片剂及其制备方法
JP2017535520A (ja) * 2014-09-30 2017-11-30 ハンミ・ファイン・ケミカル・カンパニー・リミテッドＨａｎｍｉ Ｆｉｎｅ Ｃｈｅｍｉｃａｌ Ｃｏ．， Ｌｔｄ． 高純度の（ｒ）−９−［２−（ホスホノメトキシ）プロピル］アデニンの製造方法
CN106046055A (zh) * 2016-05-27 2016-10-26 湖北丽益医药科技有限公司 R‑9‑(2‑膦酰甲氧基丙基)‑腺嘌呤一水合物晶体及制备、富马酸替诺福韦二吡呋酯制备
KR101909570B1 (ko) 2016-12-05 2018-10-19 (주) 성운파마코피아 고순도 테노포비어 디소프록실 제조방법
CN108358968B (zh) * 2018-04-03 2020-09-15 科兴生物制药股份有限公司 一种替诺福韦的制备方法
CN109942634A (zh) * 2019-01-24 2019-06-28 深圳科兴药业有限公司 一种富马酸替诺福韦二吡呋酯的晶型i及制备方法和应用
CN110507625A (zh) * 2019-09-19 2019-11-29 苏州东瑞制药有限公司 一种新型富马酸替诺福韦酯片及其制备方法
CN111939134B (zh) * 2020-08-24 2023-02-17 山东罗欣药业集团股份有限公司 一种抗病毒药物组合物
KR20220141457A (ko) 2021-04-13 2022-10-20 경동제약 주식회사 신규 결정형의 테노포비어 알라펜아미드 말레산염 및 이를 포함하는 약제학적 조성물

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US6057305A (en) * 1992-08-05 2000-05-02 Institute Of Organic Chemistry And Biochemistry Of The Academy Of Sciences Of The Czech Republic Antiretroviral enantiomeric nucleotide analogs
ATE199906T1 (de) * 1993-06-29 2001-04-15 Mitsubishi Chem Corp Phosphonat-nukleotid ester-derivate
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ATE305009T1 (de) * 1997-07-25 2005-10-15 Gilead Sciences Inc Nukleotid-analog zusamensetzung und synthese verfahren

Also Published As

Publication number Publication date
AU8582798A (en) 1999-02-16
HK1051360B (en) 2005-10-14
SG106657A1 (en) 2004-10-29
KR100617608B1 (ko) 2006-09-01
JP2015199773A (ja) 2015-11-12
JP2013213071A (ja) 2013-10-17
JP5398662B2 (ja) 2014-01-29
DK0998480T3 (da) 2003-03-24
HK1051360A1 (en) 2003-08-01
KR100661153B1 (ko) 2006-12-26
IN190780B (es) 2003-08-23
TWI224103B (en) 2004-11-21
JP2018016645A (ja) 2018-02-01
CA2298059C (en) 2008-12-30
KR20060038452A (ko) 2006-05-03
SG106656A1 (en) 2004-10-29
KR100707505B1 (ko) 2007-04-16
TWI242561B (en) 2005-11-01
JP2017057233A (ja) 2017-03-23
KR20060038451A (ko) 2006-05-03
JP4173202B2 (ja) 2008-10-29
HK1051373B (en) 2006-04-07
JP4628437B2 (ja) 2011-02-09
CN1264387A (zh) 2000-08-23
JP2008208126A (ja) 2008-09-11
DE69829010D1 (de) 2005-03-17
ATE228526T1 (de) 2002-12-15
HK1029793A1 (en) 2001-04-12
AU756793B2 (en) 2003-01-23
CN100383148C (zh) 2008-04-23
DE69809750D1 (de) 2003-01-09
DK1243593T3 (da) 2005-11-14
EP0998480B1 (en) 2002-11-27
PT998480E (pt) 2003-03-31
CA2298059A1 (en) 1999-02-04
HK1051373A1 (en) 2003-08-01
ATE288914T1 (de) 2005-02-15
DE69809750T2 (de) 2003-08-21
PT1243590E (pt) 2005-05-31
JP2010280694A (ja) 2010-12-16
JP2002511098A (ja) 2002-04-09
BR9811045A (pt) 2000-08-22
DE69831694T2 (de) 2006-07-13
TW200510438A (en) 2005-03-16
ATE305009T1 (de) 2005-10-15
WO1999005150A1 (en) 1999-02-04
DE69829010T2 (de) 2006-04-13
ID24701A (id) 2000-08-03
DE69831694D1 (de) 2005-10-27
ES2236389T3 (es) 2005-07-16
CN1554350A (zh) 2004-12-15
NZ501287A (en) 2001-09-28
ES2249511T3 (es) 2006-04-01
EP0998480A1 (en) 2000-05-10
KR20010022067A (ko) 2001-03-15
CN1251679C (zh) 2006-04-19

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