JP2015535261A5 - - Google Patents
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- JP2015535261A5 JP2015535261A5 JP2015539919A JP2015539919A JP2015535261A5 JP 2015535261 A5 JP2015535261 A5 JP 2015535261A5 JP 2015539919 A JP2015539919 A JP 2015539919A JP 2015539919 A JP2015539919 A JP 2015539919A JP 2015535261 A5 JP2015535261 A5 JP 2015535261A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- substituted
- cycloalkyl
- aryl
- group
- 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.)
- Pending
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- 125000000217 alkyl group Chemical group 0.000 claims 124
- XCUAIINAJCDIPM-XVFCMESISA-N N(4)-hydroxycytidine Chemical compound O[C@@H]1[C@H](O)[C@@H](CO)O[C@H]1N1C(=O)NC(=NO)C=C1 XCUAIINAJCDIPM-XVFCMESISA-N 0.000 claims 60
- 125000003118 aryl group Chemical group 0.000 claims 33
- 125000001072 heteroaryl group Chemical group 0.000 claims 32
- 229910052739 hydrogen Inorganic materials 0.000 claims 32
- 125000000753 cycloalkyl group Chemical group 0.000 claims 30
- 229910052799 carbon Inorganic materials 0.000 claims 29
- -1 C 1 -C 6 alkoxy Chemical group 0.000 claims 27
- 125000001424 substituent group Chemical group 0.000 claims 27
- 125000003545 alkoxy group Chemical group 0.000 claims 25
- 125000001153 fluoro group Chemical group F* 0.000 claims 24
- 125000003342 alkenyl group Chemical group 0.000 claims 22
- SNOOUWRIMMFWNE-UHFFFAOYSA-M sodium;6-[(3,4,5-trimethoxybenzoyl)amino]hexanoate Chemical compound [Na+].COC1=CC(C(=O)NCCCCCC([O-])=O)=CC(OC)=C1OC SNOOUWRIMMFWNE-UHFFFAOYSA-M 0.000 claims 22
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims 21
- 125000002877 alkyl aryl group Chemical group 0.000 claims 14
- 150000001875 compounds Chemical class 0.000 claims 14
- 229910052760 oxygen Inorganic materials 0.000 claims 14
- 229910052717 sulfur Inorganic materials 0.000 claims 14
- 125000000304 alkynyl group Chemical group 0.000 claims 13
- 125000003710 aryl alkyl group Chemical group 0.000 claims 13
- 235000000346 sugar Nutrition 0.000 claims 13
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 12
- 125000003107 substituted aryl group Chemical group 0.000 claims 12
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 9
- 239000003814 drug Substances 0.000 claims 9
- 229910052736 halogen Inorganic materials 0.000 claims 9
- 150000002367 halogens Chemical class 0.000 claims 9
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 8
- 229910052731 fluorine Inorganic materials 0.000 claims 8
- 125000002252 acyl group Chemical group 0.000 claims 7
- 229910052794 bromium Inorganic materials 0.000 claims 7
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 7
- 229910052801 chlorine Inorganic materials 0.000 claims 7
- 229910052740 iodine Inorganic materials 0.000 claims 7
- DNIAPMSPPWPWGF-GSVOUGTGSA-N (R)-(-)-Propylene glycol Chemical compound C[C@@H](O)CO DNIAPMSPPWPWGF-GSVOUGTGSA-N 0.000 claims 6
- 239000003795 chemical substances by application Substances 0.000 claims 6
- 125000005842 heteroatom Chemical group 0.000 claims 6
- 208000015181 infectious disease Diseases 0.000 claims 6
- 229910052757 nitrogen Inorganic materials 0.000 claims 6
- 150000003290 ribose derivatives Chemical class 0.000 claims 6
- 208000031886 HIV Infections Diseases 0.000 claims 5
- 230000004071 biological effect Effects 0.000 claims 4
- 239000001177 diphosphate Substances 0.000 claims 4
- 235000011180 diphosphates Nutrition 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 3
- HMFHBZSHGGEWLO-SOOFDHNKSA-N D-ribofuranose Chemical compound OC[C@H]1OC(O)[C@H](O)[C@@H]1O HMFHBZSHGGEWLO-SOOFDHNKSA-N 0.000 claims 3
- 241000710831 Flavivirus Species 0.000 claims 3
- 241000700588 Human alphaherpesvirus 1 Species 0.000 claims 3
- 241000701074 Human alphaherpesvirus 2 Species 0.000 claims 3
- 241000713772 Human immunodeficiency virus 1 Species 0.000 claims 3
- 241001263478 Norovirus Species 0.000 claims 3
- PYMYPHUHKUWMLA-LMVFSUKVSA-N Ribose Natural products OC[C@@H](O)[C@@H](O)[C@@H](O)C=O PYMYPHUHKUWMLA-LMVFSUKVSA-N 0.000 claims 3
- HMFHBZSHGGEWLO-UHFFFAOYSA-N alpha-D-Furanose-Ribose Natural products OCC1OC(O)C(O)C1O HMFHBZSHGGEWLO-UHFFFAOYSA-N 0.000 claims 3
- 125000004432 carbon atom Chemical group C* 0.000 claims 3
- 125000004093 cyano group Chemical group *C#N 0.000 claims 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 3
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 3
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 3
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 3
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 3
- 125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 3
- 239000001226 triphosphate Substances 0.000 claims 3
- 235000011178 triphosphate Nutrition 0.000 claims 3
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 2
- WNXJIVFYUVYPPR-UHFFFAOYSA-N 1,3-dioxolane Chemical compound C1COCO1 WNXJIVFYUVYPPR-UHFFFAOYSA-N 0.000 claims 2
- IMLSAISZLJGWPP-UHFFFAOYSA-N 1,3-dithiolane Chemical compound C1CSCS1 IMLSAISZLJGWPP-UHFFFAOYSA-N 0.000 claims 2
- 125000004442 acylamino group Chemical group 0.000 claims 2
- HVYWMOMLDIMFJA-DPAQBDIFSA-N cholesterol Chemical compound C1C=C2C[C@@H](O)CC[C@]2(C)[C@@H]2[C@@H]1[C@@H]1CC[C@H]([C@H](C)CCCC(C)C)[C@@]1(C)CC2 HVYWMOMLDIMFJA-DPAQBDIFSA-N 0.000 claims 2
- 125000001188 haloalkyl group Chemical group 0.000 claims 2
- 125000006302 indol-3-yl methyl group Chemical group [H]N1C([H])=C(C2=C([H])C([H])=C([H])C([H])=C12)C([H])([H])* 0.000 claims 2
- OOFGXDQWDNJDIS-UHFFFAOYSA-N oxathiolane Chemical compound C1COSC1 OOFGXDQWDNJDIS-UHFFFAOYSA-N 0.000 claims 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 2
- 229940002612 prodrug Drugs 0.000 claims 2
- 239000000651 prodrug Substances 0.000 claims 2
- 125000004076 pyridyl group Chemical group 0.000 claims 2
- 150000008163 sugars Chemical class 0.000 claims 2
- 241000713340 Human immunodeficiency virus 2 Species 0.000 claims 1
- 150000008575 L-amino acids Chemical class 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 239000002259 anti human immunodeficiency virus agent Substances 0.000 claims 1
- 230000003441 anti-flavivirus Effects 0.000 claims 1
- 229940124411 anti-hiv antiviral agent Drugs 0.000 claims 1
- 239000002246 antineoplastic agent Substances 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 125000001309 chloro group Chemical group Cl* 0.000 claims 1
- 235000012000 cholesterol Nutrition 0.000 claims 1
- 125000002944 cyanoaryl group Chemical group 0.000 claims 1
- 235000014113 dietary fatty acids Nutrition 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000000194 fatty acid Substances 0.000 claims 1
- 229930195729 fatty acid Natural products 0.000 claims 1
- 150000004665 fatty acids Chemical class 0.000 claims 1
- 150000002191 fatty alcohols Chemical class 0.000 claims 1
- 239000001257 hydrogen Substances 0.000 claims 1
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 1
- 150000002632 lipids Chemical class 0.000 claims 1
- 125000002950 monocyclic group Chemical group 0.000 claims 1
- 150000003904 phospholipids Chemical class 0.000 claims 1
- 229940068065 phytosterols Drugs 0.000 claims 1
- 102000004196 processed proteins & peptides Human genes 0.000 claims 1
- 108090000765 processed proteins & peptides Proteins 0.000 claims 1
- 229910052711 selenium Inorganic materials 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261719696P | 2012-10-29 | 2012-10-29 | |
| US61/719,696 | 2012-10-29 | ||
| US201361763534P | 2013-02-12 | 2013-02-12 | |
| US61/763,534 | 2013-02-12 | ||
| PCT/US2013/067309 WO2014070771A1 (en) | 2012-10-29 | 2013-10-29 | Pyrimidine nucleotides and their monophosphate prodrugs for treatment of viral infections and cancer |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2015535261A JP2015535261A (ja) | 2015-12-10 |
| JP2015535261A5 true JP2015535261A5 (OSRAM) | 2016-12-15 |
Family
ID=50627997
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015539919A Pending JP2015535261A (ja) | 2012-10-29 | 2013-10-29 | ウイルス感染及び癌の治療のためのピリミジンヌクレオチド及びその一リン酸プロドラッグ |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US9809616B2 (OSRAM) |
| EP (1) | EP2912050A4 (OSRAM) |
| JP (1) | JP2015535261A (OSRAM) |
| KR (1) | KR20150090894A (OSRAM) |
| CN (1) | CN104884462A (OSRAM) |
| BR (1) | BR112015009636A8 (OSRAM) |
| CA (1) | CA2889717A1 (OSRAM) |
| HK (1) | HK1214270A1 (OSRAM) |
| MX (1) | MX2015005500A (OSRAM) |
| RU (1) | RU2015119999A (OSRAM) |
| WO (1) | WO2014070771A1 (OSRAM) |
Families Citing this family (53)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SG171914A1 (en) | 2008-12-02 | 2011-07-28 | Chiralgen Ltd | Method for the synthesis of phosphorus atom modified nucleic acids |
| IN2012DN00720A (OSRAM) | 2009-07-06 | 2015-06-19 | Ontorii Inc | |
| WO2012039448A1 (ja) | 2010-09-24 | 2012-03-29 | 株式会社キラルジェン | 不斉補助基 |
| MX347361B (es) | 2011-07-19 | 2017-04-12 | Wave Life Sciences Ltd | Metodos para la sintesis de acidos nucleicos funcionalizados. |
| EP2794627B1 (en) | 2011-12-22 | 2018-09-26 | Alios Biopharma, Inc. | Substituted nucleosides, nucleotides and analogs thereof |
| US9441007B2 (en) | 2012-03-21 | 2016-09-13 | Alios Biopharma, Inc. | Substituted nucleosides, nucleotides and analogs thereof |
| USRE48171E1 (en) | 2012-03-21 | 2020-08-25 | Janssen Biopharma, Inc. | Substituted nucleosides, nucleotides and analogs thereof |
| HUE029038T2 (en) | 2012-05-25 | 2017-01-30 | Janssen Sciences Ireland Uc | Uracil spirooxetan nucleosides |
| EP2872485B1 (en) | 2012-07-13 | 2020-12-16 | Wave Life Sciences Ltd. | Asymmetric auxiliary group |
| 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 |
| EP2935303B1 (en) | 2012-12-21 | 2021-02-17 | Janssen BioPharma, Inc. | 4'-fluoro-nucleosides, 4'-fluoro-nucleotides and analogs thereof for the treatment of hcv |
| AU2014331863C1 (en) | 2013-10-11 | 2019-05-16 | Alios Biopharma, Inc. | Substituted nucleosides, nucleotides and analogs thereof |
| CN106068325B (zh) | 2014-01-16 | 2021-07-09 | 波涛生命科学有限公司 | 手性设计 |
| US9828409B2 (en) * | 2014-03-19 | 2017-11-28 | Minghong Zhong | Bridged-cyclo-ProTides as prodrugs of therapeutic nucleosides and nucleotides |
| US10358458B2 (en) * | 2014-09-26 | 2019-07-23 | Riboscience Llc | 4′-vinyl substituted nucleoside derivatives as inhibitors of respiratory syncytial virus RNA replication |
| WO2016099982A2 (en) | 2014-12-15 | 2016-06-23 | Emory University | Phosphoramidates for the treatment of hepatitis b virus |
| CN118286245A (zh) * | 2014-12-26 | 2024-07-05 | 埃莫里大学 | N4-羟基胞苷和衍生物及与其相关的抗病毒用途 |
| HK1247829A1 (zh) | 2015-03-06 | 2018-10-05 | Atea Pharmaceuticals, Inc. | 用於治疗HCV的β-D-2'-脱氧-2'Α-氟-2'-β-C-取代-2-改性N6-取代的嘌呤核苷酸 |
| MX382566B (es) | 2015-05-01 | 2025-03-13 | Univ Emory | Analogos de nucleosidos para el tratamiento de la familia de virus flaviviridae y cancer |
| WO2017156380A1 (en) * | 2016-03-10 | 2017-09-14 | Emory University | N4-hydroxycytidine and derivatives and anti-viral uses related thereto |
| US11963972B2 (en) | 2016-03-23 | 2024-04-23 | Emory University | Antiviral agents and nucleoside analogs for treatment of Zika virus |
| CA3029315A1 (en) * | 2016-06-24 | 2017-12-28 | Emory University | Phosphoramidates for the treatment of hepatitis b virus |
| US10202412B2 (en) | 2016-07-08 | 2019-02-12 | Atea Pharmaceuticals, Inc. | β-D-2′-deoxy-2′-substituted-4′-substituted-2-substituted-N6-substituted-6-aminopurinenucleotides for the treatment of paramyxovirus and orthomyxovirus infections |
| LU100724B1 (en) | 2016-07-14 | 2018-07-31 | Atea Pharmaceuticals Inc | Beta-d-2'-deoxy-2'-alpha-fluoro-2'-beta-c-substituted-4'-fluoro-n6-substituted-6-amino-2-substituted purine nucleotides for the treatment of hepatitis c virus infection |
| EP3512863B1 (en) | 2016-09-07 | 2021-12-08 | ATEA Pharmaceuticals, Inc. | 2'-substituted-n6-substituted purine nucleotides for rna virus treatment |
| EP4450129A3 (en) | 2017-02-01 | 2025-03-19 | ATEA Pharmaceuticals, Inc. | Nucleotide hemi-sulfate salt for the treatment of hepatitis c virus |
| US12030908B2 (en) | 2017-03-10 | 2024-07-09 | Lakewood Amedex, Inc. | Antimicrobial compounds, compositions, and uses thereof |
| CN110612143B (zh) * | 2017-03-10 | 2021-07-02 | 莱克伍德阿美达克斯股份有限公司 | 抗微生物化合物、组合物及其用途 |
| US11331331B2 (en) | 2017-12-07 | 2022-05-17 | Emory University | N4-hydroxycytidine and derivatives and anti-viral uses related thereto |
| TW202012001A (zh) | 2018-04-10 | 2020-04-01 | 美商亞堤製藥公司 | C型肝炎病毒(hcv)感染硬化之患者的治療 |
| KR20210018806A (ko) * | 2018-05-09 | 2021-02-18 | 코크리스탈 파마, 아이엔씨. | Hcv의 치료를 위한 병용 요법 |
| CN110075291B (zh) * | 2019-02-01 | 2023-01-06 | 广州中医药大学(广州中医药研究院) | 一种单磷酸类酯A缀合Tn抗肿瘤疫苗及其应用 |
| MX2021011606A (es) | 2019-04-02 | 2021-12-10 | Aligos Therapeutics Inc | Compuestos dirigidos a prmt5. |
| BR112021024310A2 (pt) | 2019-06-05 | 2022-02-15 | Univ Emory | Peptidomiméticos para o tratamento de infecções por coronavírus e picornavírus |
| US10874687B1 (en) | 2020-02-27 | 2020-12-29 | Atea Pharmaceuticals, Inc. | Highly active compounds against COVID-19 |
| WO2022008025A1 (en) * | 2020-07-05 | 2022-01-13 | Since & Technology Development Fund Authority | 2-hydroxyiminopyrimidine nucleosides and derivitives and antiviral uses thereto |
| JP7774836B2 (ja) * | 2021-01-29 | 2025-11-25 | 国立大学法人東海国立大学機構 | プロドラッグ化合物 |
| WO2022218274A1 (zh) * | 2021-04-15 | 2022-10-20 | 中国科学院上海药物研究所 | 核苷类似物及其用途 |
| CA3219218A1 (en) * | 2021-05-06 | 2022-11-10 | Council Of Scientific And Industrial Research | A process for the preparation of n4-hydroxycytidine and its derivatives |
| CN117500494A (zh) | 2021-06-17 | 2024-02-02 | 阿堤亚制药公司 | 有利的抗hcv联合疗法 |
| CN113321694A (zh) * | 2021-06-22 | 2021-08-31 | 药康众拓(江苏)医药科技有限公司 | N4-羟基胞苷衍生物及其制备方法和用途 |
| CN113278041B (zh) * | 2021-07-16 | 2021-10-19 | 南京颐媛生物医学研究院有限公司 | 一种核苷磷酸酯及其合成方法与抗肝炎病毒的制药应用 |
| CN117886870A (zh) * | 2021-08-27 | 2024-04-16 | 南京知和医药科技有限公司 | 一种新型的胞苷衍生物及其药物组合物和用途 |
| CN115819483A (zh) * | 2021-09-17 | 2023-03-21 | 南京知和医药科技有限公司 | 用于治疗癌症的核苷类衍生物及其用途 |
| CN113735928A (zh) * | 2021-10-21 | 2021-12-03 | 药康众拓(江苏)医药科技有限公司 | 一种n4-羟基胞苷衍生物及其制备方法和用途 |
| US11541071B1 (en) | 2021-12-16 | 2023-01-03 | Ascletis BioScience Co., Ltd | Nucleoside derivatives and methods of use thereof |
| AU2023236711A1 (en) | 2022-03-15 | 2024-10-03 | Rome Therapeutics, Inc. | Compounds and methods for treating disease |
| CN114437159B (zh) * | 2022-04-11 | 2022-06-28 | 佛山市晨康生物科技有限公司 | 一种环状碳酸酯核苷类化合物及其应用 |
| CN117285566A (zh) * | 2022-06-24 | 2023-12-26 | 润佳（苏州）医药科技有限公司 | 一种膦酸酯类化合物及其医药用途 |
| WO2024123207A1 (ru) * | 2022-12-08 | 2024-06-13 | федеральное государственное бюджетное учреждение "Национальный исследовательский центр эпидемиологии и микробиологии имени почетного академика Н.Ф. Гамалеи" Министерства здравоохранения Российской Федерации | 5'-о-(3-фенилпропионил)-n4-гидроксицитидин и его применение |
| WO2024123206A1 (ru) * | 2022-12-08 | 2024-06-13 | федеральное государственное бюджетное учреждение "Национальный исследовательский центр эпидемиологии и микробиологии имени почетного академика Н.Ф. Гамалеи" Министерства здравоохранения Российской Федерации | Способ получения 5',-о-(3-фенилпропионил)-n4-гидроксицитидина |
| WO2024249234A1 (en) * | 2023-05-26 | 2024-12-05 | Altesa BioSciences, Inc. | Method of treating hepatitis c virus in patients |
| WO2025024346A2 (en) * | 2023-07-27 | 2025-01-30 | Merck Sharp & Dohme Llc | Solid dosage form of a small molecule antiviral and uses thereof |
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| CN102558263A (zh) * | 2010-12-28 | 2012-07-11 | 上海瑞广生化科技开发有限公司 | 去氧氟尿苷类衍生物,其制备方法及其制药用途 |
-
2013
- 2013-10-29 EP EP13851564.8A patent/EP2912050A4/en not_active Withdrawn
- 2013-10-29 KR KR1020157014128A patent/KR20150090894A/ko not_active Ceased
- 2013-10-29 CA CA2889717A patent/CA2889717A1/en not_active Abandoned
- 2013-10-29 JP JP2015539919A patent/JP2015535261A/ja active Pending
- 2013-10-29 HK HK16102408.4A patent/HK1214270A1/zh unknown
- 2013-10-29 BR BR112015009636A patent/BR112015009636A8/pt not_active Application Discontinuation
- 2013-10-29 CN CN201380068925.3A patent/CN104884462A/zh active Pending
- 2013-10-29 WO PCT/US2013/067309 patent/WO2014070771A1/en not_active Ceased
- 2013-10-29 MX MX2015005500A patent/MX2015005500A/es unknown
- 2013-10-29 RU RU2015119999A patent/RU2015119999A/ru not_active Application Discontinuation
- 2013-10-29 US US14/066,461 patent/US9809616B2/en active Active
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