PE20181016A1 - Compuestos antivirales de fosfodiamida de ester de beta aminoacido - Google Patents
Compuestos antivirales de fosfodiamida de ester de beta aminoacidoInfo
- Publication number
- PE20181016A1 PE20181016A1 PE2018000216A PE2018000216A PE20181016A1 PE 20181016 A1 PE20181016 A1 PE 20181016A1 PE 2018000216 A PE2018000216 A PE 2018000216A PE 2018000216 A PE2018000216 A PE 2018000216A PE 20181016 A1 PE20181016 A1 PE 20181016A1
- Authority
- PE
- Peru
- Prior art keywords
- amino
- acid ester
- amino acid
- methylethoxy
- methyl
- Prior art date
Links
Classifications
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
- C07F9/06—Phosphorus compounds without P—C bonds
- C07F9/16—Esters of thiophosphoric acids or thiophosphorous acids
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Molecular Biology (AREA)
- Epidemiology (AREA)
- Biochemistry (AREA)
- Virology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- AIDS & HIV (AREA)
- Tropical Medicine & Parasitology (AREA)
- Communicable Diseases (AREA)
- Oncology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
La presente invencion refiere un compuesto de formula I, en la que R1 y R2 se seleccionan cada uno independientemente entre H, -alquilo C1-C4, -CH2-fenilo, entre otros; R3 es -alquilo C1-C10 no sustituido, -CH2-fenilo no sustituido, arilo no sustituido, entre otros; RA es un resto de ester de L-aminoacido de formula i, un resto de ester de D-aminoacido de formula ii, entre otros; R4 es -alquilo C1-C4, -CH2-fenol, arilo; R9 es -alquilo C1-C10, -CH2-fenilo, arilo no sustituido, entre otros. Son compuestos favoritos: N-[(S)-{[(1R)-2-(6-amino-9H-purin-9-il)-1-metiletoxi]metil}{[(2S)-2-metil-3-(1-metiletoxi)-3-oxopropil]amino}fosforil]-L-alaninato 1-metiletilico; N-[(R)-{[(1R)-2-(6-amino-9H-purin-9-il)-1-metiletoxi]metil}{[(2S)-2-metil-3-(1-metiletoxi)-3-oxopropil]amino}fosforil]-L-alaninato 1-metiletilico, entre otros. La presente invencion tambien refiere a una composicion farmaceutica que comprende una cantidad eficaz de uno o mas agente antivirales del VIH como el abacavir, efavirenz, entre otros y un vehiculo farmaceuticamente aceptable. Es util para la inhibicion de la transcriptasa inversa del VIH tanto para su prevencion, tratamiento y la profilaxis y/o el retraso de la aparicion o de la progresion del SIDA y/o del ARC.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562203265P | 2015-08-10 | 2015-08-10 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20181016A1 true PE20181016A1 (es) | 2018-06-26 |
Family
ID=56852398
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2018000216A PE20181016A1 (es) | 2015-08-10 | 2016-08-08 | Compuestos antivirales de fosfodiamida de ester de beta aminoacido |
Country Status (26)
| Country | Link |
|---|---|
| US (2) | US9822138B2 (es) |
| EP (1) | EP3334743B1 (es) |
| JP (2) | JP6563585B2 (es) |
| KR (1) | KR102163611B1 (es) |
| CN (1) | CN107849071B (es) |
| AR (1) | AR105643A1 (es) |
| AU (1) | AU2016305941B2 (es) |
| CA (1) | CA2994720C (es) |
| CL (1) | CL2018000351A1 (es) |
| CO (1) | CO2018001296A2 (es) |
| CR (1) | CR20180092A (es) |
| EA (1) | EA035028B1 (es) |
| EC (1) | ECSP18018823A (es) |
| HK (1) | HK1249107A1 (es) |
| IL (1) | IL257156A (es) |
| MA (1) | MA42615A (es) |
| MX (1) | MX386992B (es) |
| MY (1) | MY192607A (es) |
| NI (1) | NI201800023A (es) |
| PE (1) | PE20181016A1 (es) |
| PH (1) | PH12018500292A1 (es) |
| SV (1) | SV2018005629A (es) |
| TN (1) | TN2018000048A1 (es) |
| TW (1) | TWI639598B (es) |
| WO (1) | WO2017027434A1 (es) |
| ZA (1) | ZA201800514B (es) |
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| WO2017100108A1 (en) * | 2015-12-10 | 2017-06-15 | Merck Sharp & Dohme Corp. | Antiviral phosphodiamide prodrugs of tenofovir |
| WO2017106069A1 (en) | 2015-12-15 | 2017-06-22 | Merck Sharp & Dohme Corp. | Antiviral oxime phosphoramide compounds |
| JP2017182110A (ja) * | 2016-03-28 | 2017-10-05 | セイコーエプソン株式会社 | 表示システム、表示装置、情報処理装置及び情報処理方法 |
| WO2018039157A1 (en) | 2016-08-25 | 2018-03-01 | Merck Sharp & Dohme Corp. | Antiviral prodrugs of tenofovir |
| AU2017342536A1 (en) | 2016-10-14 | 2019-05-02 | Precision Biosciences, Inc. | Engineered meganucleases specific for recognition sequences in the Hepatitis B virus genome |
| WO2018080903A1 (en) | 2016-10-26 | 2018-05-03 | Merck Sharp & Dohme Corp. | Antiviral aryl-amide phosphodiamide compounds |
| CA3046029A1 (en) | 2016-12-22 | 2018-06-28 | Merck Sharp & Dohme Corp. | Antiviral benzyl-amine phosphodiamide compounds |
| RU2759902C2 (ru) | 2016-12-22 | 2021-11-18 | Мерк Шарп И Доум Корп. | Антивирусные алифатические сложноэфирные пролекарства тенофовира |
| CA3084569A1 (en) | 2017-12-20 | 2019-06-27 | Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. | 3'3' cyclic dinucleotides with phosphonate bond activating the sting adaptor protein |
| EP3728282B1 (en) | 2017-12-20 | 2023-11-22 | Institute of Organic Chemistry and Biochemistry ASCR, V.V.I. | 2'3' cyclic dinucleotides with phosphonate bond activating the sting adaptor protein |
| PL3759109T3 (pl) | 2018-02-26 | 2024-03-04 | Gilead Sciences, Inc. | Podstawione związki pirolizyny jako inhibitory replikacji hbv |
| US10870691B2 (en) | 2018-04-05 | 2020-12-22 | Gilead Sciences, Inc. | Antibodies and fragments thereof that bind hepatitis B virus protein X |
| 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 |
| 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 |
| 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 |
| 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 |
| US20190359645A1 (en) | 2018-05-03 | 2019-11-28 | Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. | 2'3'-cyclic dinucleotides comprising carbocyclic nucleotide |
| 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 |
| KR20210044806A (ko) * | 2018-08-09 | 2021-04-23 | 글락소스미스클라인 인털렉츄얼 프로퍼티 (넘버 2) 리미티드 | Hiv 요법에 유용한 화합물 |
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| JP7273172B2 (ja) | 2018-10-31 | 2023-05-12 | ギリアード サイエンシーズ， インコーポレイテッド | Ｈｐｋ１阻害活性を有する置換６－アザベンゾイミダゾール化合物 |
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| WO2011140640A1 (en) | 2010-05-11 | 2011-11-17 | Simon Fraser University | Selective glycosidase inhibitors and uses thereof |
| WO2012154321A1 (en) | 2011-03-31 | 2012-11-15 | Idenix Pharmaceuticals, Inc. | Compounds and pharmaceutical compositions for the treatment of viral infections |
| HRP20161696T4 (hr) | 2011-08-16 | 2023-10-13 | Gilead Sciences, Inc. | Tenofovir alafenamid hemifumarat |
| EP3578563B1 (en) | 2011-12-22 | 2021-04-14 | Geron Corporation | Guanine analogs as telomerase substrates and telomere length affectors |
| 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 |
| WO2017007701A1 (en) | 2015-07-07 | 2017-01-12 | Merck Sharp & Dohme Corp. | Antiviral phosphodiamide compounds |
-
2016
- 2016-08-08 KR KR1020187006590A patent/KR102163611B1/ko not_active Expired - Fee Related
- 2016-08-08 MA MA042615A patent/MA42615A/fr unknown
- 2016-08-08 HK HK18108839.8A patent/HK1249107A1/zh unknown
- 2016-08-08 JP JP2018506607A patent/JP6563585B2/ja not_active Expired - Fee Related
- 2016-08-08 EA EA201890425A patent/EA035028B1/ru not_active IP Right Cessation
- 2016-08-08 AU AU2016305941A patent/AU2016305941B2/en not_active Ceased
- 2016-08-08 AR ARP160102427A patent/AR105643A1/es unknown
- 2016-08-08 MY MYPI2018000176A patent/MY192607A/en unknown
- 2016-08-08 WO PCT/US2016/045946 patent/WO2017027434A1/en not_active Ceased
- 2016-08-08 CN CN201680046470.9A patent/CN107849071B/zh not_active Expired - Fee Related
- 2016-08-08 EP EP16759910.9A patent/EP3334743B1/en active Active
- 2016-08-08 TN TNP/2018/000048A patent/TN2018000048A1/en unknown
- 2016-08-08 CA CA2994720A patent/CA2994720C/en active Active
- 2016-08-08 PE PE2018000216A patent/PE20181016A1/es unknown
- 2016-08-08 US US15/231,365 patent/US9822138B2/en active Active
- 2016-08-08 MX MX2018001729A patent/MX386992B/es unknown
- 2016-08-08 CR CR20180092A patent/CR20180092A/es unknown
- 2016-08-08 TW TW105125206A patent/TWI639598B/zh not_active IP Right Cessation
-
2017
- 2017-09-25 US US15/714,786 patent/US20180065999A1/en not_active Abandoned
-
2018
- 2018-01-24 ZA ZA2018/00514A patent/ZA201800514B/en unknown
- 2018-01-25 IL IL257156A patent/IL257156A/en unknown
- 2018-02-07 NI NI201800023A patent/NI201800023A/es unknown
- 2018-02-07 CL CL2018000351A patent/CL2018000351A1/es unknown
- 2018-02-08 CO CONC2018/0001296A patent/CO2018001296A2/es unknown
- 2018-02-08 PH PH12018500292A patent/PH12018500292A1/en unknown
- 2018-02-09 SV SV2018005629A patent/SV2018005629A/es unknown
- 2018-03-09 EC ECIEPI201818823A patent/ECSP18018823A/es unknown
-
2019
- 2019-06-10 JP JP2019107685A patent/JP2019194200A/ja not_active Withdrawn
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