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
- -1 BETA AMINO ACID ESTER Chemical class 0.000 title abstract 3
- 150000001875 compounds Chemical class 0.000 title abstract 3
- 230000000840 anti-viral effect Effects 0.000 title 1
- 125000003118 aryl group Chemical group 0.000 abstract 3
- 125000000848 adenin-9-yl group Chemical group [H]N([H])C1=C2N=C([H])N(*)C2=NC([H])=N1 0.000 abstract 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 2
- 208000030507 AIDS Diseases 0.000 abstract 1
- XPOQHMRABVBWPR-UHFFFAOYSA-N Efavirenz Natural products O1C(=O)NC2=CC=C(Cl)C=C2C1(C(F)(F)F)C#CC1CC1 XPOQHMRABVBWPR-UHFFFAOYSA-N 0.000 abstract 1
- 108010078851 HIV Reverse Transcriptase Proteins 0.000 abstract 1
- MCGSCOLBFJQGHM-SCZZXKLOSA-N abacavir Chemical compound C=12N=CN([C@H]3C=C[C@@H](CO)C3)C2=NC(N)=NC=1NC1CC1 MCGSCOLBFJQGHM-SCZZXKLOSA-N 0.000 abstract 1
- 229960004748 abacavir Drugs 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 239000003443 antiviral agent Substances 0.000 abstract 1
- XPOQHMRABVBWPR-ZDUSSCGKSA-N efavirenz Chemical compound C([C@]1(C2=CC(Cl)=CC=C2NC(=O)O1)C(F)(F)F)#CC1CC1 XPOQHMRABVBWPR-ZDUSSCGKSA-N 0.000 abstract 1
- 229960003804 efavirenz Drugs 0.000 abstract 1
- 230000005764 inhibitory process Effects 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 1
- 238000011321 prophylaxis Methods 0.000 abstract 1
- 238000011282 treatment Methods 0.000 abstract 1
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)
- Veterinary Medicine (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Molecular Biology (AREA)
- Epidemiology (AREA)
- Biochemistry (AREA)
- Virology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (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) | MX2018001729A (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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EP3285582B1 (en) * | 2015-03-26 | 2020-11-11 | Merck Sharp & Dohme Corp. | Phosphate-substituted quinolizine derivatives useful as hiv integrase inhibitors |
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US10450335B2 (en) | 2015-12-15 | 2019-10-22 | 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 |
US10449208B2 (en) | 2016-08-25 | 2019-10-22 | Merck Sharp & Dohme Corp. | Antiviral prodrugs of tenofovir |
CN110023495A (zh) | 2016-10-14 | 2019-07-16 | 精密生物科学公司 | 对乙肝病毒基因组中的识别序列特异性的工程化大范围核酸酶 |
US10736908B2 (en) | 2016-10-26 | 2020-08-11 | Merck Sharp & Dohme Corp. | Antiviral aryl-amide phosphodiamide compounds |
RU2759902C2 (ru) | 2016-12-22 | 2021-11-18 | Мерк Шарп И Доум Корп. | Антивирусные алифатические сложноэфирные пролекарства тенофовира |
AU2017378893A1 (en) | 2016-12-22 | 2019-05-16 | Idenix Pharmaceuticals Llc | Antiviral benzyl-amine phosphodiamide compounds |
EP3728283B1 (en) | 2017-12-20 | 2023-11-22 | Institute of Organic Chemistry and Biochemistry ASCR, V.V.I. | 3'3' cyclic dinucleotides with phosphonate bond activating the sting adaptor protein |
JP7098748B2 (ja) | 2017-12-20 | 2022-07-11 | 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2’3’環状ジヌクレオチド |
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 |
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 |
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 |
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 |
EP3823629A4 (en) | 2018-07-19 | 2022-05-04 | Merck Sharp & Dohme Corp. | PHOSPHINAMIDE 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 |
BR112021002169A2 (pt) * | 2018-08-09 | 2021-05-04 | Glaxosmithkline Intellectual Property (No.2) Limited | compostos úteis na terapia do hiv |
CN108623632A (zh) * | 2018-08-17 | 2018-10-09 | 上海麦步医药科技有限公司 | 一种替诺福韦艾拉酚胺的制备方法 |
WO2020092528A1 (en) | 2018-10-31 | 2020-05-07 | Gilead Sciences, Inc. | Substituted 6-azabenzimidazole compounds having hpk1 inhibitory activity |
PE20211655A1 (es) | 2018-10-31 | 2021-08-24 | Gilead Sciences Inc | Compuestos de 6-azabencimidazol sustituidos como inhibidores de hpk1 |
KR20210137434A (ko) | 2019-01-25 | 2021-11-17 | 브라운 유니버시티 | 연령 관련 염증 및 장애를 치료, 예방 또는 역전시키기 위한 조성물 및 방법 |
CA3129022C (en) | 2019-03-07 | 2023-08-01 | Institute Of Organic Chemistry And Biochemistry Ascr, V.V.I. | 2'3'-cyclic dinucleotides and prodrugs thereof |
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 |
KR20210137518A (ko) | 2019-03-07 | 2021-11-17 | 인스티튜트 오브 오가닉 케미스트리 앤드 바이오케미스트리 에이에스 씨알 브이.브이.아이. | 3'3'-사이클릭 다이뉴클레오티드 및 이의 프로드럭 |
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CN117843811A (zh) | 2019-09-30 | 2024-04-09 | 吉利德科学公司 | Hbv疫苗和治疗hbv的方法 |
WO2021113765A1 (en) | 2019-12-06 | 2021-06-10 | Precision Biosciences, Inc. | Optimized engineered meganucleases having specificity for a recognition sequence in the hepatitis b virus genome |
WO2021188959A1 (en) | 2020-03-20 | 2021-09-23 | Gilead Sciences, Inc. | Prodrugs of 4'-c-substituted-2-halo-2'-deoxyadenosine nucleosides and methods of making and using the same |
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TW202406932A (zh) | 2020-10-22 | 2024-02-16 | 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 |
KR20240006683A (ko) | 2021-05-13 | 2024-01-15 | 길리애드 사이언시즈, 인코포레이티드 | TLR8 조절 화합물과 항-HBV siRNA 치료제의 조합물 |
CA3222439A1 (en) | 2021-06-23 | 2022-12-29 | Gilead Sciences, Inc. | Diacylglyercol kinase modulating compounds |
EP4359389A1 (en) | 2021-06-23 | 2024-05-01 | Gilead Sciences, Inc. | Diacylglyercol kinase modulating compounds |
US11976072B2 (en) | 2021-06-23 | 2024-05-07 | Gilead Sciences, Inc. | Diacylglycerol kinase modulating compounds |
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PL2038290T3 (pl) * | 2006-07-07 | 2014-03-31 | Gilead Sciences Inc | Modulatory receptora Toll-podobnego 7 |
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ES2874774T3 (es) | 2011-12-22 | 2021-11-05 | Geron Corp | Análogos de guanina como sustratos de telomerasa y afectores de la longitud de los telómeros |
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 |
WO2017007701A1 (en) | 2015-07-07 | 2017-01-12 | Merck Sharp & Dohme Corp. | Antiviral phosphodiamide compounds |
-
2016
- 2016-08-08 TW TW105125206A patent/TWI639598B/zh not_active IP Right Cessation
- 2016-08-08 CR CR20180092A patent/CR20180092A/es unknown
- 2016-08-08 PE PE2018000216A patent/PE20181016A1/es unknown
- 2016-08-08 WO PCT/US2016/045946 patent/WO2017027434A1/en active Application Filing
- 2016-08-08 MX MX2018001729A patent/MX2018001729A/es unknown
- 2016-08-08 AR ARP160102427A patent/AR105643A1/es unknown
- 2016-08-08 EA EA201890425A patent/EA035028B1/ru not_active IP Right Cessation
- 2016-08-08 EP EP16759910.9A patent/EP3334743B1/en active Active
- 2016-08-08 MY MYPI2018000176A patent/MY192607A/en unknown
- 2016-08-08 JP JP2018506607A patent/JP6563585B2/ja not_active Expired - Fee Related
- 2016-08-08 CN CN201680046470.9A patent/CN107849071B/zh active Active
- 2016-08-08 AU AU2016305941A patent/AU2016305941B2/en not_active Ceased
- 2016-08-08 MA MA042615A patent/MA42615A/fr unknown
- 2016-08-08 KR KR1020187006590A patent/KR102163611B1/ko active IP Right Grant
- 2016-08-08 CA CA2994720A patent/CA2994720C/en active Active
- 2016-08-08 TN TNP/2018/000048A patent/TN2018000048A1/en unknown
- 2016-08-08 US US15/231,365 patent/US9822138B2/en active Active
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2017
- 2017-09-25 US US15/714,786 patent/US20180065999A1/en not_active Abandoned
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2018
- 2018-01-24 ZA ZA2018/00514A patent/ZA201800514B/en unknown
- 2018-01-25 IL IL257156A patent/IL257156A/en unknown
- 2018-02-07 CL CL2018000351A patent/CL2018000351A1/es unknown
- 2018-02-07 NI NI201800023A patent/NI201800023A/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
- 2018-07-09 HK HK18108839.8A patent/HK1249107A1/zh unknown
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2019
- 2019-06-10 JP JP2019107685A patent/JP2019194200A/ja not_active Withdrawn
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