EA201490753A1 - Способы получения обладающих противовирусным действием аналогов нуклеотидов - Google Patents
Способы получения обладающих противовирусным действием аналогов нуклеотидовInfo
- Publication number
- EA201490753A1 EA201490753A1 EA201490753A EA201490753A EA201490753A1 EA 201490753 A1 EA201490753 A1 EA 201490753A1 EA 201490753 A EA201490753 A EA 201490753A EA 201490753 A EA201490753 A EA 201490753A EA 201490753 A1 EA201490753 A1 EA 201490753A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- owners
- obtaining
- methods
- viral action
- nucleotides analogues
- Prior art date
Links
- 230000000840 anti-viral effect Effects 0.000 title abstract 2
- 238000000034 method Methods 0.000 title abstract 2
- 239000002773 nucleotide Substances 0.000 title 1
- 239000000543 intermediate Substances 0.000 abstract 2
- 238000004519 manufacturing process Methods 0.000 abstract 2
- ONBQEOIKXPHGMB-VBSBHUPXSA-N 1-[2-[(2s,3r,4s,5r)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]oxy-4,6-dihydroxyphenyl]-3-(4-hydroxyphenyl)propan-1-one Chemical compound O[C@@H]1[C@H](O)[C@@H](CO)O[C@H]1OC1=CC(O)=CC(O)=C1C(=O)CCC1=CC=C(O)C=C1 ONBQEOIKXPHGMB-VBSBHUPXSA-N 0.000 abstract 1
- 229940126142 compound 16 Drugs 0.000 abstract 1
- LDEKQSIMHVQZJK-CAQYMETFSA-N tenofovir alafenamide Chemical compound O([P@@](=O)(CO[C@H](C)CN1C2=NC=NC(N)=C2N=C1)N[C@@H](C)C(=O)OC(C)C)C1=CC=CC=C1 LDEKQSIMHVQZJK-CAQYMETFSA-N 0.000 abstract 1
Classifications
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- 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
- A61P35/00—Antineoplastic agents
-
- 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
- C07F9/645—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having two nitrogen atoms as the only ring hetero atoms
- C07F9/6509—Six-membered rings
- C07F9/6512—Six-membered rings having the nitrogen atoms in positions 1 and 3
-
- 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
- C07F9/6558—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system
- C07F9/65583—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom containing at least two different or differently substituted hetero rings neither condensed among themselves nor condensed with a common carbocyclic ring or ring system each of the hetero rings containing nitrogen as ring hetero atom
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Molecular Biology (AREA)
- Biochemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Virology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Saccharide Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
В изобретении предложены способы выделения 9-{(R)-2-[((S)-{[(S)-1-(изопропоксикарбонил)этил]амино}феноксифосфинил)метокси]пропил}аденина (соединения 16)способ получения промежуточных соединений 13 и 15 с высокой диастереомерной чистотойи способ получения промежуточного соединения 129-{(R)-2-[((S)-{[(S)-1-(изопропоксикарбонил)этил]амино}феноксифосфинил)метокси]пропил}аденина, обладающего противовирусными свойствами.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161544950P | 2011-10-07 | 2011-10-07 | |
| PCT/US2012/000441 WO2013052094A2 (en) | 2011-10-07 | 2012-10-03 | Methods for preparing anti-viral nucleotide analogs |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| EA201490753A1 true EA201490753A1 (ru) | 2014-09-30 |
| EA027086B1 EA027086B1 (ru) | 2017-06-30 |
Family
ID=47297386
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| EA201490753A EA027086B1 (ru) | 2011-10-07 | 2012-10-03 | Способы получения обладающих противовирусным действием аналогов нуклеотидов |
Country Status (25)
| Country | Link |
|---|---|
| US (4) | US8664386B2 (ru) |
| EP (2) | EP3333173B1 (ru) |
| JP (2) | JP6190372B2 (ru) |
| KR (3) | KR102033802B1 (ru) |
| CN (4) | CN103842366B (ru) |
| AR (1) | AR088109A1 (ru) |
| AU (1) | AU2012319172B2 (ru) |
| BR (1) | BR112014011340A2 (ru) |
| CA (2) | CA3042169C (ru) |
| CL (1) | CL2014000827A1 (ru) |
| CO (1) | CO6940431A2 (ru) |
| CR (1) | CR20140204A (ru) |
| EA (1) | EA027086B1 (ru) |
| EC (1) | ECSP14000074A (ru) |
| ES (2) | ES2746859T3 (ru) |
| HK (3) | HK1200834A1 (ru) |
| IL (1) | IL231879B (ru) |
| MX (1) | MX353064B (ru) |
| PE (1) | PE20141160A1 (ru) |
| PL (1) | PL3333173T3 (ru) |
| PT (2) | PT2764002T (ru) |
| SI (1) | SI3333173T1 (ru) |
| TW (4) | TWI613211B (ru) |
| UY (1) | UY34361A (ru) |
| WO (1) | WO2013052094A2 (ru) |
Families Citing this family (50)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103732594A (zh) | 2011-08-16 | 2014-04-16 | 吉联亚科学公司 | 替诺福韦艾拉酚胺(tenofovir alafenamide)半反丁烯二酸盐 |
| CN103842366B (zh) | 2011-10-07 | 2017-06-16 | 吉利德科学公司 | 制备抗病毒核苷酸类似物的方法 |
| CN107312039B (zh) | 2012-08-30 | 2019-06-25 | 江苏豪森药业集团有限公司 | 一种替诺福韦前药的制备方法 |
| ZA201404147B (en) | 2013-06-07 | 2016-01-27 | Cipla Ltd | An efficient process for separation of diastereomers of 9-[(r)-2-[[(r,s)-[[(s)-1-(isopropoxycarbonyl)ethyl]amino]-phenoxyphosphinyl] methoxy]propyl]adenine |
| CN104628773B (zh) * | 2013-11-06 | 2018-10-23 | 杭州和泽医药科技有限公司 | (r)-9-[2-(磷酰苯酚基甲氧基)丙基]腺嘌呤的制备方法 |
| WO2015079455A2 (en) * | 2013-11-27 | 2015-06-04 | Laurus Labs Private Limited | A recycling process for preparing tenofovir alafenamide diastereomers |
| IN2014MU00118A (ru) * | 2014-01-14 | 2015-08-28 | Mylan Lab Ltd | |
| TWI660965B (zh) | 2014-01-15 | 2019-06-01 | 美商基利科學股份有限公司 | 泰諾福韋之固體形式 |
| WO2015161785A1 (zh) * | 2014-04-21 | 2015-10-29 | 四川海思科制药有限公司 | 氨基磷酸酯类衍生物制备方法及其中间体和中间体的制备方法 |
| WO2015197006A1 (zh) * | 2014-06-25 | 2015-12-30 | 四川海思科制药有限公司 | 一种取代的氨基酸硫酯类化合物、其组合物及应用 |
| CN105399771B (zh) * | 2014-07-21 | 2020-11-24 | 江苏豪森药业集团有限公司 | 替诺福韦前药晶型及其制备方法和用途 |
| CN108191913A (zh) * | 2014-11-12 | 2018-06-22 | 四川海思科制药有限公司 | 一种替诺福韦艾拉酚胺晶型a及其制备方法 |
| CN104817593B (zh) * | 2015-04-27 | 2016-11-16 | 广州同隽医药科技有限公司 | 半富马酸替诺福韦艾拉酚胺关键中间体的合成工艺 |
| MX2018001557A (es) | 2015-08-05 | 2018-05-02 | Eisai R&D Man Co Ltd | Reactivos quirales para la preparacion de oligomeros homogeneos. |
| TWI616452B (zh) * | 2015-08-26 | 2018-03-01 | Preparation method of nucleoside analog and intermediate thereof | |
| CN105330700A (zh) * | 2015-12-17 | 2016-02-17 | 中国药科大学 | 富马酸替诺福韦艾拉酚胺杂质的制备方法 |
| WO2017118928A1 (en) | 2016-01-06 | 2017-07-13 | Lupin Limited | Process for the separation of diastereomers of tenofovir alafenamide |
| CZ2016156A3 (cs) * | 2016-03-17 | 2017-09-27 | Zentiva, K.S. | Způsob přípravy diastereomerně čistého Tenofoviru Alafenamidu nebo jeho solí |
| CN107286190A (zh) * | 2016-04-13 | 2017-10-24 | 刘沛 | 核苷之烃氧基苄基氨基磷酸/膦酸酯衍生物的制备及其医药用途 |
| EP3455218A4 (en) | 2016-05-10 | 2019-12-18 | C4 Therapeutics, Inc. | C3 CARBON-BASED GLUTARIMIDE DEGRONIMERS FOR TARGET PROTEIN REDUCTION |
| WO2017197055A1 (en) | 2016-05-10 | 2017-11-16 | C4 Therapeutics, Inc. | Heterocyclic degronimers for target protein degradation |
| CN109562113A (zh) | 2016-05-10 | 2019-04-02 | C4医药公司 | 用于靶蛋白降解的螺环降解决定子体 |
| CN106565785B (zh) * | 2016-11-09 | 2019-11-12 | 周雨恬 | 一种具有抗hbv/hiv活性的核苷氨基磷酸酯类化合物及其盐和用途 |
| CN106946935B (zh) * | 2017-04-28 | 2020-01-07 | 福建广生堂药业股份有限公司 | 一种非对映异构体核苷衍生物的制备方法 |
| CN111417634A (zh) * | 2017-10-04 | 2020-07-14 | 细胞基因公司 | 用于制备顺式-4-[2-{[(3s,4r)-3-氟噁烷-4-基]氨基}-8-(2,4,6-三氯苯胺基)-9h-嘌呤-9-基]-1-甲基环己烷-1-甲酰胺的方法 |
| CN109942632B (zh) * | 2017-12-20 | 2021-08-31 | 上海博志研新药物研究有限公司 | 替诺福韦艾拉酚胺中间体的制备方法 |
| CN109942633B (zh) * | 2017-12-20 | 2021-08-31 | 上海新礼泰药业有限公司 | 替诺福韦艾拉酚胺中间体的制备方法 |
| CN110092803A (zh) * | 2018-01-31 | 2019-08-06 | 北京睿创康泰医药研究院有限公司 | 替诺福韦艾拉酚胺富马酸盐工艺杂质的制备及其应用 |
| CN108409788B (zh) * | 2018-03-12 | 2020-05-08 | 科兴生物制药股份有限公司 | 一种富马酸替诺福韦艾拉酚胺的制备方法 |
| CN110305163A (zh) * | 2018-03-27 | 2019-10-08 | 北京济美堂医药研究有限公司 | 替诺福韦艾拉酚胺半富马酸盐的制备方法 |
| CN108467410B (zh) * | 2018-04-09 | 2021-04-09 | 重庆三圣实业股份有限公司 | 一种taf中间体的制备方法及产品和应用 |
| CN108484672A (zh) * | 2018-05-23 | 2018-09-04 | 中国药科大学制药有限公司 | 磷丙替诺福韦的手性拆分方法 |
| CN108822149B (zh) * | 2018-06-01 | 2020-08-11 | 成都苑东生物制药股份有限公司 | 一种富马酸替诺福韦艾拉酚胺关键中间体的制备方法 |
| CN110283208B (zh) * | 2018-06-22 | 2022-07-08 | 南京济群医药科技股份有限公司 | 一种替诺福韦艾拉酚胺的手性拆分方法 |
| CN109081853A (zh) * | 2018-09-03 | 2018-12-25 | 南京正大天晴制药有限公司 | 一种磷丙替诺福韦有关物质的制备方法 |
| CN111484527A (zh) * | 2019-01-25 | 2020-08-04 | 上海清松制药有限公司 | 一种替诺福韦艾拉酚胺中间体的制备方法 |
| CN111943981A (zh) * | 2019-05-14 | 2020-11-17 | 博瑞生物医药泰兴市有限公司 | 一种磷丙替诺福韦的制备方法 |
| CN112175003B (zh) * | 2019-07-01 | 2022-02-15 | 上海医药工业研究院 | 一种苯基氢膦酸酯及其中间体的制备方法 |
| US20220257619A1 (en) | 2019-07-18 | 2022-08-18 | Gilead Sciences, Inc. | Long-acting formulations of tenofovir alafenamide |
| CN112390824B (zh) * | 2019-08-19 | 2022-07-05 | 鲁南制药集团股份有限公司 | 一种替诺福韦艾拉酚胺中间体的制备方法 |
| CN110981911A (zh) * | 2019-10-08 | 2020-04-10 | 浙江车头制药股份有限公司 | 一种替诺福韦艾拉酚胺的制备方法 |
| CN111171076A (zh) * | 2019-12-26 | 2020-05-19 | 合肥启旸生物科技有限公司 | 一种替诺福韦二聚体的制备方法 |
| CN115605493A (zh) | 2020-03-20 | 2023-01-13 | 吉利德科学公司（Us） | 4′-c-取代的-2-卤代-2′-脱氧腺苷核苷的前药及其制备和使用方法 |
| KR20210125298A (ko) | 2020-04-08 | 2021-10-18 | 주식회사 파마코스텍 | 테노포비어 알라펜아미드 헤미타르트레이트의 신규한 제조방법 |
| AU2021377614A1 (en) | 2020-11-11 | 2023-06-22 | Gilead Sciences, Inc. | METHODS OF IDENTIFYING HIV PATIENTS SENSITIVE TO THERAPY WITH gp120 CD4 BINDING SITE-DIRECTED ANTIBODIES |
| KR20220141457A (ko) | 2021-04-13 | 2022-10-20 | 경동제약 주식회사 | 신규 결정형의 테노포비어 알라펜아미드 말레산염 및 이를 포함하는 약제학적 조성물 |
| TW202400172A (zh) | 2022-04-06 | 2024-01-01 | 美商基利科學股份有限公司 | 橋聯三環胺甲醯基吡啶酮化合物及其用途 |
| WO2024006982A1 (en) | 2022-07-01 | 2024-01-04 | Gilead Sciences, Inc. | Therapeutic compounds useful for the prophylactic or therapeutic treatment of an hiv virus infection |
| WO2024044477A1 (en) | 2022-08-26 | 2024-02-29 | Gilead Sciences, Inc. | Dosing and scheduling regimen for broadly neutralizing antibodies |
| WO2024076915A1 (en) | 2022-10-04 | 2024-04-11 | Gilead Sciences, Inc. | 4'-thionucleoside analogues and their pharmaceutical use |
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| PT1301519E (pt) * | 2000-07-21 | 2015-06-11 | Gilead Sciences Inc | Profármacos de análogos de nucleótidos de fosfonato e métodos para selecionar e preparar os mesmos |
| US20050239054A1 (en) | 2002-04-26 | 2005-10-27 | Arimilli Murty N | Method and compositions for identifying anti-HIV therapeutic compounds |
| PT2258376T (pt) | 2004-07-27 | 2019-05-31 | Gilead Sciences Inc | Análogos fosfonatados de compostos inibidores do vih |
| MX2008012398A (es) | 2006-03-29 | 2008-12-17 | Gilead Sciences Inc | Proceso para la preparacion de inhibidores de proteasa de vih. |
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| JP5372751B2 (ja) * | 2006-07-21 | 2013-12-18 | ギリアード サイエンシーズ， インコーポレイテッド | Ａｚａ−ペプチドプロテアーゼ阻害剤 |
| US8106064B2 (en) * | 2006-07-24 | 2012-01-31 | Korea Research Institute Of Chemical Technology | Pyrimidine-2,4-dione HIV reverse transcriptase inhibitors |
| WO2009005693A1 (en) * | 2007-06-29 | 2009-01-08 | Gilead Sciences, Inc. | Novel hiv reverse transcriptase inhibitors |
| CN103732594A (zh) | 2011-08-16 | 2014-04-16 | 吉联亚科学公司 | 替诺福韦艾拉酚胺(tenofovir alafenamide)半反丁烯二酸盐 |
| CN103842366B (zh) | 2011-10-07 | 2017-06-16 | 吉利德科学公司 | 制备抗病毒核苷酸类似物的方法 |
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2012
- 2012-10-03 CN CN201280048965.7A patent/CN103842366B/zh active Active
- 2012-10-03 EP EP18153951.1A patent/EP3333173B1/en active Active
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- 2012-10-03 ES ES18153951T patent/ES2746859T3/es active Active
- 2012-10-03 CN CN201710365515.5A patent/CN107266498B/zh active Active
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- 2012-10-03 KR KR1020147011619A patent/KR102033802B1/ko active IP Right Grant
- 2012-10-03 BR BR112014011340A patent/BR112014011340A2/pt unknown
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- 2014-05-05 CR CR20140204A patent/CR20140204A/es unknown
- 2014-05-05 EC ECIEPI201474A patent/ECSP14000074A/es unknown
-
2015
- 2015-02-06 HK HK15101331.9A patent/HK1200834A1/xx unknown
- 2015-02-06 HK HK18114351.4A patent/HK1255222B/zh unknown
- 2015-04-08 US US14/681,955 patent/US9346841B2/en active Active
-
2016
- 2016-04-21 US US15/135,357 patent/US9676804B2/en active Active
-
2017
- 2017-04-19 JP JP2017083047A patent/JP2017160228A/ja not_active Withdrawn
-
2018
- 2018-04-17 HK HK18104995.7A patent/HK1245798A1/zh unknown
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