AU2013204727A1 - Therapeutic compounds - Google Patents
Therapeutic compounds Download PDFInfo
- Publication number
- AU2013204727A1 AU2013204727A1 AU2013204727A AU2013204727A AU2013204727A1 AU 2013204727 A1 AU2013204727 A1 AU 2013204727A1 AU 2013204727 A AU2013204727 A AU 2013204727A AU 2013204727 A AU2013204727 A AU 2013204727A AU 2013204727 A1 AU2013204727 A1 AU 2013204727A1
- Authority
- AU
- Australia
- Prior art keywords
- cobicistat
- tenofovir alafenamide
- pharmaceutically acceptable
- acceptable salt
- alafenamide hemifumarate
- 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.)
- Abandoned
Links
- 230000001225 therapeutic effect Effects 0.000 title claims description 64
- 150000001875 compounds Chemical class 0.000 title description 55
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- 229960002402 cobicistat Drugs 0.000 claims abstract description 471
- 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 claims abstract description 378
- 229960004946 tenofovir alafenamide Drugs 0.000 claims abstract description 355
- SVUJNSGGPUCLQZ-FQQAACOVSA-N tenofovir alafenamide fumarate Chemical compound OC(=O)\C=C\C(O)=O.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.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 SVUJNSGGPUCLQZ-FQQAACOVSA-N 0.000 claims abstract description 325
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Classifications
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- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
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| PCT/US2013/024451 WO2013116730A1 (en) | 2012-02-03 | 2013-02-01 | Combination therapy comprising tenofovir alafenamide hemifumarate and cobicistat for use in the treatment of viral infections |
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| RS53347B (sr) | 2008-12-09 | 2014-10-31 | Gilead Sciences, Inc. | Modulatori toll-sličnih receptora |
| ES2608871T5 (es) | 2011-08-16 | 2024-04-04 | Gilead Sciences Inc | Alafenamide hemifumarate de tenofovir |
| 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 |
| HK1220390A1 (zh) * | 2013-08-29 | 2017-05-05 | Teva Pharmaceutical Industries Ltd. | 包括恩曲他滨，替诺福韦，达芦那韦和利托那韦的单位剂型以及包含达芦那韦和利托那韦的单体片剂 |
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| CA2942877A1 (en) * | 2014-04-08 | 2015-10-15 | Nitzan SHAHAR | Unit dosage form comprising emtricitabine, tenofovir, darunavir and ritonavir |
| CN105518011B (zh) * | 2014-04-21 | 2018-07-27 | 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 |
| US10076512B2 (en) | 2014-05-01 | 2018-09-18 | Eiger Biopharmaceuticals, Inc. | Treatment of hepatitis delta virus infection |
| US11311519B2 (en) | 2014-05-01 | 2022-04-26 | Eiger Biopharmaceuticals, Inc. | Treatment of hepatitis delta virus infection |
| JP6522732B2 (ja) * | 2014-07-11 | 2019-05-29 | ギリアード サイエンシーズ， インコーポレイテッド | Ｈｉｖを治療するためのトール様受容体の調節因子 |
| SG11201701520TA (en) | 2014-09-16 | 2017-04-27 | Gilead Sciences Inc | Solid forms of a toll-like receptor modulator |
| CN105237571B (zh) * | 2014-11-28 | 2018-03-09 | 成都苑东生物制药股份有限公司 | 9‑[(r)‑2‑[[(s)‑[[(s)‑1‑(异丙氧基羰基)乙基]氨基]苯氧基氧膦基]甲氧基]丙基]腺嘌呤的盐 |
| US20180338993A1 (en) * | 2014-12-04 | 2018-11-29 | Eiger Biopharmaceuticals, Inc. | Treatment of hepatitis delta virus infection |
| JP7381190B2 (ja) | 2014-12-26 | 2023-11-15 | エモリー・ユニバーシテイ | Ｎ４－ヒドロキシシチジン及び誘導体並びにそれに関連する抗ウイルス用途 |
| AU2015373104B2 (en) * | 2015-01-03 | 2020-07-09 | Mylan Laboratories Limited | Processes for the preparation of amorphous tenofovir alafenamide hemifumarate and a premix thereof |
| WO2016172342A1 (en) | 2015-04-21 | 2016-10-27 | Eiger Biopharmaceuticals, Inc. | Pharmaceutical compositions comprising lonafarnib and ritonavir |
| 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 |
| CA2921336A1 (en) * | 2015-06-30 | 2016-12-30 | Gilead Sciences, Inc. | Pharmaceutical formulations |
| PT4070788T (pt) * | 2015-06-30 | 2023-06-06 | Gilead Sciences Inc | Formulações farmacêuticas |
| US9598459B2 (en) | 2015-08-03 | 2017-03-21 | Pop Test Oncology Llc | Pharmaceutical compositions and methods |
| CN105153231A (zh) * | 2015-08-28 | 2015-12-16 | 浙江车头制药股份有限公司 | 一种一苯基pmpa的制备方法 |
| WO2017083304A1 (en) * | 2015-11-09 | 2017-05-18 | Gilead Sciences, Inc. | Therapeutic compositions for treatment of human immunodeficiency virus |
| US20170232020A1 (en) * | 2016-02-12 | 2017-08-17 | Cipla Limited | Pharmaceutical compositions |
| CN107179355B (zh) * | 2016-03-11 | 2021-08-10 | 广东东阳光药业有限公司 | 一种分离检测替诺福韦艾拉酚胺及其有关物质的方法 |
| EP3503895B1 (en) * | 2016-08-25 | 2021-09-15 | Merck Sharp & Dohme Corp. | Antiviral prodrugs of tenofovir |
| CN108070003A (zh) * | 2016-12-02 | 2018-05-25 | 上海博志研新药物技术有限公司 | 替诺福韦艾拉酚胺半反丁烯二酸盐晶型及制备方法和应用 |
| RU2659388C1 (ru) | 2017-02-28 | 2018-07-02 | Васильевич Иващенко Александр | Нуклеотиды, включающие N-[(S)-1-циклобутоксикарбонил]фосфорамидатный фрагмент, их аналоги и их применение |
| RU2647576C1 (ru) * | 2017-02-28 | 2018-03-16 | Васильевич Иващенко Александр | Циклобутил (S)-2-[[[(R)-2-(6-аминопурин-9-ил)-1-метил-этокси]метил-фенокси-фосфорил]амино]-пропаноаты, способ их получения и применения |
| CN106928277A (zh) * | 2017-03-16 | 2017-07-07 | 江苏诚信药业有限公司 | 一种替诺福韦艾拉酚胺合成的工艺方法 |
| AU2018239257B2 (en) | 2017-03-20 | 2023-09-28 | The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | HIV post-exposure prophylaxis |
| CN110769856A (zh) * | 2017-04-18 | 2020-02-07 | 希普拉有限公司 | 用于治疗逆转录病毒感染的组合疗法 |
| RU2659693C1 (ru) * | 2017-06-30 | 2018-07-03 | Общество с ограниченной ответственностью "Изварино Фарма" | Фармацевтическая композиция, обладающая активностью против ВИЧ-инфекции |
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| PT3706762T (pt) | 2017-12-07 | 2024-12-05 | Univ Emory | N4-hidroxicitidina e derivados e utilizações antivirais relacionadas com os mesmos |
| 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 |
| 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 |
| 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 |
| TWI810456B (zh) | 2019-05-22 | 2023-08-01 | 美商基利科學股份有限公司 | Tlr7調節化合物及hiv疫苗之組合 |
| EP3989956A1 (en) * | 2019-06-28 | 2022-05-04 | Anhui Ronghang Biotech Development Co., Ltd. | Compositions and methods for treatment of hepatitis b virus infection |
| AU2020318808A1 (en) | 2019-07-19 | 2022-02-03 | The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | HIV pre-exposure prophylaxis |
| CN111606949A (zh) * | 2020-03-13 | 2020-09-01 | 浙江车头制药股份有限公司 | 一种磷丙替诺福韦杂质的制备方法 |
| CN111303209A (zh) * | 2020-03-21 | 2020-06-19 | 石家庄龙泽制药股份有限公司 | 一种丙酚替诺福韦降解杂质的制备方法 |
| WO2022118020A1 (en) * | 2020-12-02 | 2022-06-09 | Cipla Limited | Method of treating viral infection |
| WO2024196814A1 (en) | 2023-03-17 | 2024-09-26 | The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | Methods for treatment of age-related macular degeneration |
| EP4640214A1 (en) * | 2024-03-28 | 2025-10-29 | Sanovel Ilac Sanayi Ve Ticaret Anonim Sirketi | A tablet comprising tenofovir alafenamide monofumarate |
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| US5922695A (en) | 1996-07-26 | 1999-07-13 | Gilead Sciences, Inc. | Antiviral phosphonomethyoxy nucleotide analogs having increased oral bioavarilability |
| US20020119443A1 (en) | 2000-07-21 | 2002-08-29 | Gilead Sciences, Inc. | Prodrugs of phosphonate nucleotide analogues and methods for selecting and making same |
| DE10153078A1 (de) | 2001-10-30 | 2003-05-22 | Degussa | Verwendung von Granulaten auf Basis von pyrogen hergestelltem Siliciumdioxid in pharmazeutischen Zusammensetzungen |
| DK1583542T3 (da) | 2003-01-14 | 2008-09-22 | Gilead Sciences Inc | Sammensætninger og fremgangsmåder til antiviral kombinationsterapi |
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| WO2009005693A1 (en) | 2007-06-29 | 2009-01-08 | Gilead Sciences, Inc. | Novel hiv reverse transcriptase inhibitors |
| EP2393485B1 (en) * | 2009-02-06 | 2015-07-29 | Gilead Sciences, Inc. | Bilayer tablets comprising elvitegravir, cobicistat, emtricitabine and tenofovir |
| ES2608871T5 (es) * | 2011-08-16 | 2024-04-04 | Gilead Sciences Inc | Alafenamide hemifumarate de tenofovir |
-
2013
- 2013-02-01 AU AU2013204727A patent/AU2013204727A1/en not_active Abandoned
- 2013-02-01 JP JP2014555783A patent/JP6059255B2/ja active Active
- 2013-02-01 EP EP13704863.3A patent/EP2809323A1/en not_active Withdrawn
- 2013-02-01 AU AU2013204731A patent/AU2013204731C1/en active Active
- 2013-02-01 BR BR112014018918A patent/BR112014018918A8/pt not_active IP Right Cessation
- 2013-02-01 HK HK15103394.9A patent/HK1202801A1/xx unknown
- 2013-02-01 HK HK15105031.3A patent/HK1204914A1/xx unknown
- 2013-02-01 CN CN201380007670.XA patent/CN104105484A/zh active Pending
- 2013-02-01 WO PCT/US2013/024451 patent/WO2013116730A1/en not_active Ceased
- 2013-02-01 EA EA201491287A patent/EA026138B1/ru unknown
- 2013-02-01 KR KR20147024291A patent/KR20140119177A/ko not_active Withdrawn
- 2013-02-01 WO PCT/US2013/024438 patent/WO2013116720A1/en not_active Ceased
- 2013-02-01 CA CA 2863662 patent/CA2863662A1/en not_active Abandoned
- 2013-02-01 MD MDA20140091A patent/MD20140091A2/ro not_active Application Discontinuation
- 2013-02-01 MX MX2014009172A patent/MX2014009172A/es unknown
- 2013-02-01 US US14/376,116 patent/US20150105350A1/en not_active Abandoned
- 2013-02-01 NZ NZ629896A patent/NZ629896A/en unknown
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2014
- 2014-07-30 IL IL233874A patent/IL233874A0/en unknown
-
2016
- 2016-06-02 AU AU2016203666A patent/AU2016203666A1/en not_active Abandoned
- 2016-10-03 US US15/284,105 patent/US20170056423A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| AU2013204731A1 (en) | 2013-08-22 |
| EA026138B1 (ru) | 2017-03-31 |
| NZ629896A (en) | 2016-03-31 |
| EA201491287A1 (ru) | 2015-04-30 |
| BR112014018918A2 (https=) | 2017-06-20 |
| BR112014018918A8 (pt) | 2017-07-11 |
| WO2013116720A1 (en) | 2013-08-08 |
| MX2014009172A (es) | 2014-08-27 |
| MD20140091A2 (ro) | 2015-01-31 |
| WO2013116730A1 (en) | 2013-08-08 |
| JP6059255B2 (ja) | 2017-01-11 |
| HK1202801A1 (en) | 2015-10-09 |
| HK1204914A1 (en) | 2015-12-11 |
| AU2013204731C1 (en) | 2017-08-31 |
| US20170056423A1 (en) | 2017-03-02 |
| JP2015505565A (ja) | 2015-02-23 |
| IL233874A0 (en) | 2014-09-30 |
| CA2863662A1 (en) | 2013-08-08 |
| KR20140119177A (ko) | 2014-10-08 |
| US20150105350A1 (en) | 2015-04-16 |
| AU2016203666A1 (en) | 2016-06-23 |
| EP2809323A1 (en) | 2014-12-10 |
| AU2013204731B2 (en) | 2016-03-03 |
| CN104105484A (zh) | 2014-10-15 |
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