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)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Virology (AREA)
- Molecular Biology (AREA)
- Tropical Medicine & Parasitology (AREA)
- AIDS & HIV (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Chemical Kinetics & Catalysis (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 |
|---|---|---|---|---|
| WO2017100108A1 (en) | 2015-12-10 | 2017-06-15 | Merck Sharp & Dohme Corp. | Antiviral phosphodiamide prodrugs of tenofovir |
| US10450335B2 (en) | 2015-12-15 | 2019-10-22 | Merck Sharp & Dohme Corp. | Antiviral oxime phosphoramide compounds |
| WO2018039157A1 (en) * | 2016-08-25 | 2018-03-01 | Merck Sharp & Dohme Corp. | Antiviral prodrugs of tenofovir |
| KR20230010826A (ko) | 2016-10-14 | 2023-01-19 | 프리시젼 바이오사이언시스 인코포레이티드 | B형 간염 바이러스 게놈 내의 인식 서열에 대해 특이적인 조작된 메가뉴클레아제 |
| 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 |
| US11203610B2 (en) | 2017-12-20 | 2021-12-21 | Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. | 2′3′ cyclic dinucleotides with phosphonate bond activating the sting adaptor protein |
| JP7037667B2 (ja) | 2017-12-20 | 2022-03-16 | 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． | Ｓｔｉｎｇアダプタータンパク質を活性化するホスホン酸結合を有する３’３’環状ジヌクレオチド |
| EP3730503B8 (en) * | 2017-12-21 | 2026-03-18 | Shenzhen TargetRx Co., Ltd. | 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 |
| WO2019195181A1 (en) | 2018-04-05 | 2019-10-10 | Gilead Sciences, Inc. | Antibodies and fragments thereof that bind hepatitis b virus protein x |
| 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 |
| 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 |
| 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 |
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| EP3823629B1 (en) | 2018-07-19 | 2024-12-25 | Merck Sharp & Dohme LLC | 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 |
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| EP4371987B9 (en) | 2018-10-31 | 2025-11-26 | Gilead Sciences, Inc. | Substituted 6-azabenzimidazole compounds as hpk1 inhibitors |
| MX2021008751A (es) | 2019-01-25 | 2021-11-12 | Univ Brown | Composiciones y metodos para tratar, prevenir o revertir la inflamacion y los trastornos asociados a la edad. |
| WO2020178768A1 (en) | 2019-03-07 | 2020-09-10 | Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. | 3'3'-cyclic dinucleotide analogue comprising a cyclopentanyl modified nucleotide as sting modulator |
| WO2020178769A1 (en) | 2019-03-07 | 2020-09-10 | Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. | 2'3'-cyclic dinucleotides and prodrugs thereof |
| CN113574063B (zh) | 2019-03-07 | 2025-03-18 | 捷克共和国有机化学与生物化学研究所 | 3’3’-环二核苷酸及其前药 |
| 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 |
| 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 |
| KR102054104B1 (ko) * | 2019-04-30 | 2019-12-09 | 유니셀랩 주식회사 | 신규한 테노포비어 알라펜아미드 염 및 이의 제조방법 |
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| 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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| LT4192474T (lt) | 2020-08-07 | 2025-11-25 | Fosfonamidų nukleotidų analogų provaistai ir jų farmacinis panaudojimas | |
| IL301560A (en) * | 2020-09-23 | 2023-05-01 | 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 |
| US20240269142A1 (en) | 2021-05-13 | 2024-08-15 | Gilead Sciences, Inc. | COMBINATION OF A TLR8 MODULATING COMPOUND AND ANTI-HBV siRNA THERAPEUTICS |
| MX2023014762A (es) | 2021-06-23 | 2024-01-15 | Gilead Sciences Inc | Compuestos moduladores de diacilglicerol quinasa. |
| EP4359413A1 (en) | 2021-06-23 | 2024-05-01 | Gilead Sciences, Inc. | Diacylglyercol kinase modulating compounds |
| CN117355531A (zh) | 2021-06-23 | 2024-01-05 | 吉利德科学公司 | 二酰基甘油激酶调节化合物 |
| JP7651018B2 (ja) | 2021-06-23 | 2025-03-25 | 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 |
| WO2025240246A1 (en) | 2024-05-13 | 2025-11-20 | Gilead Sciences, Inc. | Combination therapies with ribavirin |
| TW202608468A (zh) | 2024-05-13 | 2026-03-01 | 美商基利科學股份有限公司 | 組合療法 |
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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 |
| US10450335B2 (en) | 2015-12-15 | 2019-10-22 | Merck Sharp & Dohme Corp. | Antiviral oxime phosphoramide compounds |
| WO2018039157A1 (en) * | 2016-08-25 | 2018-03-01 | 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 KR KR1020197020682A patent/KR20190100250A/ko not_active Withdrawn
- 2017-12-20 AU AU2017379850A patent/AU2017379850B2/en not_active Ceased
- 2017-12-20 CN CN201780079454.4A patent/CN110099912B/zh not_active Expired - Fee Related
- 2017-12-20 EP EP17829499.7A patent/EP3559011B1/en active Active
- 2017-12-20 US US15/847,971 patent/US10519159B2/en active Active
- 2017-12-20 JP JP2019533490A patent/JP6938637B2/ja not_active Expired - Fee Related
- 2017-12-20 BR BR112019013017A patent/BR112019013017A2/pt active Search and Examination
- 2017-12-20 WO PCT/US2017/067470 patent/WO2018119013A1/en not_active Ceased
- 2017-12-20 CA CA3047573A patent/CA3047573A1/en not_active Abandoned
- 2017-12-20 MX MX2019007585A patent/MX388757B/es unknown
- 2017-12-20 RU RU2019122414A patent/RU2759902C2/ru active
- 2017-12-20 MA MA047094A patent/MA47094A/fr unknown
- 2017-12-20 TW TW106144739A patent/TW201829412A/zh unknown
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 |
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| JP6938637B2 (ja) | 2021-09-22 |
| MX388757B (es) | 2025-03-20 |
| KR20190100250A (ko) | 2019-08-28 |
| MA47094A (fr) | 2021-05-26 |
| WO2018119013A1 (en) | 2018-06-28 |
| EP3559011B1 (en) | 2022-04-13 |
| CN110099912B (zh) | 2021-10-15 |
| RU2759902C2 (ru) | 2021-11-18 |
| CN110099912A (zh) | 2019-08-06 |
| US10519159B2 (en) | 2019-12-31 |
| AU2017379850A1 (en) | 2019-06-13 |
| TW201829412A (zh) | 2018-08-16 |
| US20180179208A1 (en) | 2018-06-28 |
| MX2019007585A (es) | 2019-09-09 |
| BR112019013017A2 (pt) | 2020-01-14 |
| CA3047573A1 (en) | 2018-06-28 |
| RU2019122414A (ru) | 2021-01-25 |
| EP3559011A1 (en) | 2019-10-30 |
| JP2020504733A (ja) | 2020-02-13 |
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