AU2017379850B2 - Antiviral aliphatic ester prodrugs of tenofovir - Google Patents
Antiviral aliphatic ester prodrugs of tenofovir Download PDFInfo
- Publication number
- AU2017379850B2 AU2017379850B2 AU2017379850A AU2017379850A AU2017379850B2 AU 2017379850 B2 AU2017379850 B2 AU 2017379850B2 AU 2017379850 A AU2017379850 A AU 2017379850A AU 2017379850 A AU2017379850 A AU 2017379850A AU 2017379850 B2 AU2017379850 B2 AU 2017379850B2
- Authority
- AU
- Australia
- Prior art keywords
- hiv
- methyl
- amino
- oxy
- mmol
- 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.)
- Ceased
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
- 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
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- 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
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
- A61K31/52—Purines, e.g. adenine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/66—Phosphorus compounds
- A61K31/675—Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- 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
-
- 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
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Epidemiology (AREA)
- Virology (AREA)
- Molecular Biology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Tropical Medicine & Parasitology (AREA)
- AIDS & HIV (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Biochemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662437753P | 2016-12-22 | 2016-12-22 | |
| US62/437,753 | 2016-12-22 | ||
| US201762574493P | 2017-10-19 | 2017-10-19 | |
| US62/574,493 | 2017-10-19 | ||
| PCT/US2017/067470 WO2018119013A1 (en) | 2016-12-22 | 2017-12-20 | Antiviral aliphatic ester prodrugs of tenofovir |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| AU2017379850A1 AU2017379850A1 (en) | 2019-06-13 |
| AU2017379850B2 true AU2017379850B2 (en) | 2022-03-24 |
Family
ID=60972454
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU2017379850A Ceased AU2017379850B2 (en) | 2016-12-22 | 2017-12-20 | Antiviral aliphatic ester prodrugs of tenofovir |
Country Status (13)
| Country | Link |
|---|---|
| US (1) | US10519159B2 (enExample) |
| EP (1) | EP3559011B1 (enExample) |
| JP (1) | JP6938637B2 (enExample) |
| KR (1) | KR20190100250A (enExample) |
| CN (1) | CN110099912B (enExample) |
| AU (1) | AU2017379850B2 (enExample) |
| BR (1) | BR112019013017A2 (enExample) |
| CA (1) | CA3047573A1 (enExample) |
| MA (1) | MA47094A (enExample) |
| MX (1) | MX388757B (enExample) |
| RU (1) | RU2759902C2 (enExample) |
| TW (1) | TW201829412A (enExample) |
| WO (1) | WO2018119013A1 (enExample) |
Families Citing this family (47)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3386512B1 (en) | 2015-12-10 | 2023-11-22 | Merck Sharp & Dohme LLC | Antiviral phosphodiamide prodrugs of tenofovir |
| WO2017106069A1 (en) | 2015-12-15 | 2017-06-22 | Merck Sharp & Dohme Corp. | Antiviral oxime phosphoramide compounds |
| EP3503895B1 (en) * | 2016-08-25 | 2021-09-15 | Merck Sharp & Dohme Corp. | Antiviral prodrugs of tenofovir |
| MA46535A (fr) | 2016-10-14 | 2019-08-21 | Prec Biosciences Inc | Méganucléases modifiées spécifiques de séquences de reconnaissance dans le génome du virus de l'hépatite b |
| WO2018080903A1 (en) | 2016-10-26 | 2018-05-03 | Merck Sharp & Dohme Corp. | Antiviral aryl-amide phosphodiamide compounds |
| EP3558322B1 (en) | 2016-12-22 | 2021-09-29 | Merck Sharp & Dohme Corp. | Antiviral benzyl-amine phosphodiamide compounds |
| WO2019123339A1 (en) | 2017-12-20 | 2019-06-27 | Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. | 2'3' cyclic dinucleotides with phosphonate bond activating the sting adaptor protein |
| AU2018392213B2 (en) | 2017-12-20 | 2021-03-04 | Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. | 3'3' cyclic dinucleotides with phosphonate bond activating the STING adaptor protein |
| US11447512B2 (en) | 2017-12-21 | 2022-09-20 | Shenzhen Targetrx, Inc. | Antiviral nucleoside reverse transcriptase inhibitor |
| JP7050165B2 (ja) | 2018-02-26 | 2022-04-07 | ギリアード サイエンシーズ， インコーポレイテッド | Ｈｂｖ複製阻害剤としての置換ピロリジン化合物 |
| EP3774883A1 (en) | 2018-04-05 | 2021-02-17 | Gilead Sciences, Inc. | Antibodies and fragments thereof that bind hepatitis b virus protein x |
| TWI818007B (zh) | 2018-04-06 | 2023-10-11 | 捷克科學院有機化學與生物化學研究所 | 2'3'-環二核苷酸 |
| TWI833744B (zh) | 2018-04-06 | 2024-03-01 | 捷克科學院有機化學與生物化學研究所 | 3'3'-環二核苷酸 |
| TW202005654A (zh) | 2018-04-06 | 2020-02-01 | 捷克科學院有機化學與生物化學研究所 | ２，２，─環二核苷酸 |
| CN108586239B (zh) * | 2018-04-11 | 2020-12-29 | 深圳市前海博扬研究院有限公司 | 一种3-羟基丙酸甲酯的制备方法 |
| TW201945388A (zh) | 2018-04-12 | 2019-12-01 | 美商精密生物科學公司 | 對b型肝炎病毒基因體中之識別序列具有特異性之最佳化之經工程化巨核酸酶 |
| TW202014193A (zh) | 2018-05-03 | 2020-04-16 | 捷克科學院有機化學與生物化學研究所 | 包含碳環核苷酸之2’3’－環二核苷酸 |
| WO2020018399A1 (en) | 2018-07-19 | 2020-01-23 | Merck Sharp & Dohme Corp. | Phosphinic amide prodrugs of tenofovir |
| WO2020028097A1 (en) | 2018-08-01 | 2020-02-06 | Gilead Sciences, Inc. | Solid forms of (r)-11-(methoxymethyl)-12-(3-methoxypropoxy)-3,3-dimethyl-8-0x0-2,3,8,13b-tetrahydro-1h-pyrido[2,1-a]pyrrolo[1,2-c] phthalazine-7-c arboxylic acid |
| TWI721624B (zh) | 2018-10-31 | 2021-03-11 | 美商基利科學股份有限公司 | 經取代之6-氮雜苯并咪唑化合物 |
| CA3117556A1 (en) | 2018-10-31 | 2020-05-07 | Gilead Sciences, Inc. | Substituted 6-azabenzimidazole compounds as hpk1 inhibitors |
| CA3125991A1 (en) | 2019-01-25 | 2020-07-30 | Brown University | Compositions and methods for treating, preventing or reversing age-associated inflammation and disorders |
| WO2020178770A1 (en) | 2019-03-07 | 2020-09-10 | Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. | 3'3'-cyclic dinucleotides and prodrugs thereof |
| JP7350871B2 (ja) | 2019-03-07 | 2023-09-26 | インスティチュート オブ オーガニック ケミストリー アンド バイオケミストリー エーエスシーアール，ヴイ．ヴイ．アイ． | ２’３’－環状ジヌクレオチドおよびそのプロドラッグ |
| EP3935065A1 (en) | 2019-03-07 | 2022-01-12 | Institute of Organic Chemistry and Biochemistry ASCR, V.V.I. | 3'3'-cyclic dinucleotide analogue comprising a cyclopentanyl modified nucleotide as sting modulator |
| TW202210480A (zh) | 2019-04-17 | 2022-03-16 | 美商基利科學股份有限公司 | 類鐸受體調節劑之固體形式 |
| TWI751517B (zh) | 2019-04-17 | 2022-01-01 | 美商基利科學股份有限公司 | 類鐸受體調節劑之固體形式 |
| KR102054104B1 (ko) * | 2019-04-30 | 2019-12-09 | 유니셀랩 주식회사 | 신규한 테노포비어 알라펜아미드 염 및 이의 제조방법 |
| EP3972695A1 (en) | 2019-05-23 | 2022-03-30 | Gilead Sciences, Inc. | Substituted exo-methylene-oxindoles which are hpk1/map4k1 inhibitors |
| CN114245807B (zh) | 2019-06-25 | 2025-05-02 | 吉利德科学公司 | Flt3l-fc融合蛋白和使用方法 |
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| MY208114A (en) | 2019-09-30 | 2025-04-16 | Gilead Sciences Inc | Hbv vaccines and methods treating hbv |
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| EP4216963A4 (en) * | 2020-09-23 | 2024-10-23 | Primefour Therapeutics, Inc. | Method for treating cancer with a reverse transcriptase inhibitor |
| TWI815194B (zh) | 2020-10-22 | 2023-09-11 | 美商基利科學股份有限公司 | 介白素2-Fc融合蛋白及使用方法 |
| TW202348237A (zh) | 2021-05-13 | 2023-12-16 | 美商基利科學股份有限公司 | TLR8調節化合物及抗HBV siRNA療法之組合 |
| AU2022298639C1 (en) | 2021-06-23 | 2025-07-17 | Gilead Sciences, Inc. | Diacylglyercol kinase modulating compounds |
| CA3222277A1 (en) | 2021-06-23 | 2022-12-29 | Gilead Sciences, Inc. | Diacylglyercol kinase modulating compounds |
| JP7686091B2 (ja) | 2021-06-23 | 2025-05-30 | ギリアード サイエンシーズ， インコーポレイテッド | ジアシルグリセロールキナーゼ調節化合物 |
| EP4359389A1 (en) | 2021-06-23 | 2024-05-01 | Gilead Sciences, Inc. | Diacylglyercol kinase modulating compounds |
| US20250345389A1 (en) | 2024-05-13 | 2025-11-13 | Gilead Sciences, Inc. | Combination therapies |
| WO2025240244A1 (en) | 2024-05-13 | 2025-11-20 | Gilead Sciences, Inc. | Combination therapies comprising bulevirtide and lonafarnib for use in the treatment of hepatitis d virus infection |
| WO2025240242A1 (en) | 2024-05-13 | 2025-11-20 | Gilead Sciences, Inc. | Combination therapies with ribavirin |
| WO2025240246A1 (en) | 2024-05-13 | 2025-11-20 | Gilead Sciences, Inc. | Combination therapies with ribavirin |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106167504A (zh) * | 2015-11-04 | 2016-11-30 | 洛阳聚慧医药科技有限公司 | 非环核苷磷酰胺d‑氨基酸酯衍生物及其盐的制备以及在抗病毒方面的应用 |
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| AR087546A1 (es) | 2011-08-16 | 2014-04-03 | Gilead Sciences Inc | Hemifumarato de tenofovir alafenamida |
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| PT3194411T (pt) | 2014-09-15 | 2022-06-06 | Univ California | Análogos de nucleótidos |
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| WO2017007701A1 (en) | 2015-07-07 | 2017-01-12 | Merck Sharp & Dohme Corp. | Antiviral phosphodiamide compounds |
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| RU2604068C1 (ru) * | 2015-12-10 | 2016-12-10 | Федеральное государственное бюджетное учреждение науки Институт органического синтеза им. И.Я. Постовского Уральского отделения Российской академии наук | N-(2-аминопурин-6-ил)глицил-(s)-глутаминовая кислота, обладающая противотуберкулёзной активностью |
| EP3386512B1 (en) | 2015-12-10 | 2023-11-22 | Merck Sharp & Dohme LLC | Antiviral phosphodiamide prodrugs of tenofovir |
| WO2017106069A1 (en) | 2015-12-15 | 2017-06-22 | Merck Sharp & Dohme Corp. | Antiviral oxime phosphoramide compounds |
| EP3503895B1 (en) * | 2016-08-25 | 2021-09-15 | Merck Sharp & Dohme Corp. | Antiviral prodrugs of tenofovir |
| WO2018080903A1 (en) | 2016-10-26 | 2018-05-03 | Merck Sharp & Dohme Corp. | Antiviral aryl-amide phosphodiamide compounds |
| EP3558322B1 (en) | 2016-12-22 | 2021-09-29 | Merck Sharp & Dohme Corp. | Antiviral benzyl-amine phosphodiamide compounds |
-
2017
- 2017-12-20 US US15/847,971 patent/US10519159B2/en active Active
- 2017-12-20 CA CA3047573A patent/CA3047573A1/en not_active Abandoned
- 2017-12-20 EP EP17829499.7A patent/EP3559011B1/en active Active
- 2017-12-20 RU RU2019122414A patent/RU2759902C2/ru active
- 2017-12-20 AU AU2017379850A patent/AU2017379850B2/en not_active Ceased
- 2017-12-20 JP JP2019533490A patent/JP6938637B2/ja not_active Expired - Fee Related
- 2017-12-20 MA MA047094A patent/MA47094A/fr unknown
- 2017-12-20 MX MX2019007585A patent/MX388757B/es unknown
- 2017-12-20 BR BR112019013017A patent/BR112019013017A2/pt active Search and Examination
- 2017-12-20 KR KR1020197020682A patent/KR20190100250A/ko not_active Withdrawn
- 2017-12-20 WO PCT/US2017/067470 patent/WO2018119013A1/en not_active Ceased
- 2017-12-20 TW TW106144739A patent/TW201829412A/zh unknown
- 2017-12-20 CN CN201780079454.4A patent/CN110099912B/zh not_active Expired - Fee Related
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106167504A (zh) * | 2015-11-04 | 2016-11-30 | 洛阳聚慧医药科技有限公司 | 非环核苷磷酰胺d‑氨基酸酯衍生物及其盐的制备以及在抗病毒方面的应用 |
Also Published As
| Publication number | Publication date |
|---|---|
| TW201829412A (zh) | 2018-08-16 |
| RU2019122414A (ru) | 2021-01-25 |
| WO2018119013A1 (en) | 2018-06-28 |
| CN110099912A (zh) | 2019-08-06 |
| AU2017379850A1 (en) | 2019-06-13 |
| RU2019122414A3 (enExample) | 2021-04-26 |
| US20180179208A1 (en) | 2018-06-28 |
| JP2020504733A (ja) | 2020-02-13 |
| MX2019007585A (es) | 2019-09-09 |
| MX388757B (es) | 2025-03-20 |
| MA47094A (fr) | 2021-05-26 |
| US10519159B2 (en) | 2019-12-31 |
| CN110099912B (zh) | 2021-10-15 |
| CA3047573A1 (en) | 2018-06-28 |
| RU2759902C2 (ru) | 2021-11-18 |
| EP3559011A1 (en) | 2019-10-30 |
| KR20190100250A (ko) | 2019-08-28 |
| EP3559011B1 (en) | 2022-04-13 |
| JP6938637B2 (ja) | 2021-09-22 |
| BR112019013017A2 (pt) | 2020-01-14 |
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