JP2017525699A5 - - Google Patents
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- Publication number
- JP2017525699A5 JP2017525699A5 JP2017508531A JP2017508531A JP2017525699A5 JP 2017525699 A5 JP2017525699 A5 JP 2017525699A5 JP 2017508531 A JP2017508531 A JP 2017508531A JP 2017508531 A JP2017508531 A JP 2017508531A JP 2017525699 A5 JP2017525699 A5 JP 2017525699A5
- Authority
- JP
- Japan
- Prior art keywords
- pharmaceutically acceptable
- alkyl
- acceptable salt
- formula
- cycloalkyl
- 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.)
- Granted
Links
- 150000003839 salts Chemical class 0.000 claims description 101
- 150000001875 compounds Chemical class 0.000 claims description 96
- 125000000217 alkyl group Chemical group 0.000 claims description 66
- 229910052739 hydrogen Inorganic materials 0.000 claims description 51
- 229910052799 carbon Inorganic materials 0.000 claims description 48
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims description 28
- 208000030925 respiratory syncytial virus infectious disease Diseases 0.000 claims description 26
- 238000000034 method Methods 0.000 claims description 21
- 150000002148 esters Chemical class 0.000 claims description 20
- 125000003003 spiro group Chemical group 0.000 claims description 20
- 239000012453 solvate Substances 0.000 claims description 19
- 125000006413 ring segment Chemical group 0.000 claims description 18
- 239000001257 hydrogen Substances 0.000 claims description 17
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims description 16
- 229910052731 fluorine Inorganic materials 0.000 claims description 15
- 150000001721 carbon Chemical group 0.000 claims description 14
- 241000282412 Homo Species 0.000 claims description 13
- 229910052757 nitrogen Inorganic materials 0.000 claims description 13
- 229910052760 oxygen Inorganic materials 0.000 claims description 13
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 12
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 12
- 239000003814 drug Substances 0.000 claims description 12
- 229910052717 sulfur Inorganic materials 0.000 claims description 12
- 230000009385 viral infection Effects 0.000 claims description 11
- 241000711904 Pneumoviridae Species 0.000 claims description 10
- 125000001424 substituent group Chemical group 0.000 claims description 10
- HSFWRNGVRCDJHI-UHFFFAOYSA-N alpha-acetylene Natural products C#C HSFWRNGVRCDJHI-UHFFFAOYSA-N 0.000 claims description 8
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 8
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 8
- 125000002534 ethynyl group Chemical group [H]C#C* 0.000 claims description 8
- 125000000623 heterocyclic group Chemical group 0.000 claims description 8
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 8
- 125000004368 propenyl group Chemical group C(=CC)* 0.000 claims description 8
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims description 8
- 229940124597 therapeutic agent Drugs 0.000 claims description 8
- 125000000391 vinyl group Chemical group [H]C([*])=C([H])[H] 0.000 claims description 8
- 229920002554 vinyl polymer Polymers 0.000 claims description 8
- 125000004209 (C1-C8) alkyl group Chemical group 0.000 claims description 6
- 125000004648 C2-C8 alkenyl group Chemical group 0.000 claims description 6
- 125000004649 C2-C8 alkynyl group Chemical group 0.000 claims description 6
- 125000003118 aryl group Chemical group 0.000 claims description 6
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 6
- 125000001072 heteroaryl group Chemical group 0.000 claims description 6
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 6
- 150000002431 hydrogen Chemical class 0.000 claims description 5
- 125000001637 1-naphthyl group Chemical group [H]C1=C([H])C([H])=C2C(*)=C([H])C([H])=C([H])C2=C1[H] 0.000 claims description 4
- 125000001622 2-naphthyl group Chemical group [H]C1=C([H])C([H])=C2C([H])=C(*)C([H])=C([H])C2=C1[H] 0.000 claims description 4
- 206010061603 Respiratory syncytial virus infection Diseases 0.000 claims description 4
- 125000003710 aryl alkyl group Chemical group 0.000 claims description 4
- 229910052736 halogen Inorganic materials 0.000 claims description 4
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims description 4
- 238000002360 preparation method Methods 0.000 claims description 4
- 125000003107 substituted aryl group Chemical group 0.000 claims description 4
- 229910052801 chlorine Inorganic materials 0.000 claims description 3
- 125000005843 halogen group Chemical group 0.000 claims description 3
- 150000002367 halogens Chemical group 0.000 claims description 3
- 230000000241 respiratory effect Effects 0.000 claims description 3
- 125000006650 (C2-C4) alkynyl group Chemical group 0.000 claims description 2
- 206010006448 Bronchiolitis Diseases 0.000 claims description 2
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims description 2
- 206010035664 Pneumonia Diseases 0.000 claims description 2
- 229910019946 S-S Inorganic materials 0.000 claims description 2
- 229910019939 S—S Inorganic materials 0.000 claims description 2
- 230000002730 additional effect Effects 0.000 claims description 2
- 239000000654 additive Substances 0.000 claims description 2
- 230000000996 additive effect Effects 0.000 claims description 2
- 125000003342 alkenyl group Chemical group 0.000 claims description 2
- 229910052794 bromium Inorganic materials 0.000 claims description 2
- 125000002837 carbocyclic group Chemical group 0.000 claims description 2
- 125000004432 carbon atom Chemical group C* 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 125000004415 heterocyclylalkyl group Chemical group 0.000 claims description 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 2
- 229910052740 iodine Inorganic materials 0.000 claims description 2
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 2
- 238000004519 manufacturing process Methods 0.000 claims description 2
- 125000001624 naphthyl group Chemical group 0.000 claims description 2
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 2
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 2
- 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 description 2
- 125000005017 substituted alkenyl group Chemical group 0.000 claims description 2
- 125000000547 substituted alkyl group Chemical group 0.000 claims description 2
- 125000004426 substituted alkynyl group Chemical group 0.000 claims description 2
- 208000024891 symptom Diseases 0.000 claims description 2
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims description 2
- 239000000203 mixture Substances 0.000 claims 17
- 229940126062 Compound A Drugs 0.000 claims 2
- NLDMNSXOCDLTTB-UHFFFAOYSA-N Heterophylliin A Natural products O1C2COC(=O)C3=CC(O)=C(O)C(O)=C3C3=C(O)C(O)=C(O)C=C3C(=O)OC2C(OC(=O)C=2C=C(O)C(O)=C(O)C=2)C(O)C1OC(=O)C1=CC(O)=C(O)C(O)=C1 NLDMNSXOCDLTTB-UHFFFAOYSA-N 0.000 claims 2
- 208000036142 Viral infection Diseases 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 125000006656 (C2-C4) alkenyl group Chemical group 0.000 description 1
- 125000001963 4 membered heterocyclic group Chemical group 0.000 description 1
- 125000002373 5 membered heterocyclic group Chemical group 0.000 description 1
- 125000004070 6 membered heterocyclic group Chemical group 0.000 description 1
- 241000725643 Respiratory syncytial virus Species 0.000 description 1
- 125000000304 alkynyl group Chemical group 0.000 description 1
- 125000005842 heteroatom Chemical group 0.000 description 1
- 208000015181 infectious disease Diseases 0.000 description 1
- 239000002904 solvent Substances 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462040349P | 2014-08-21 | 2014-08-21 | |
| US62/040,349 | 2014-08-21 | ||
| PCT/US2015/045849 WO2016028866A1 (en) | 2014-08-21 | 2015-08-19 | 2'-chloro aminopyrimidinone and pyrimidine dione nucleosides |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020070958A Division JP2020111608A (ja) | 2014-08-21 | 2020-04-10 | ２’−クロロアミノピリミジノンおよびピリミジンジオンヌクレオシド |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017525699A JP2017525699A (ja) | 2017-09-07 |
| JP2017525699A5 true JP2017525699A5 (en:Method) | 2018-09-06 |
| JP6765364B2 JP6765364B2 (ja) | 2020-10-07 |
Family
ID=54066190
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017508531A Active JP6765364B2 (ja) | 2014-08-21 | 2015-08-19 | ２’−クロロアミノピリミジノンおよびピリミジンジオンヌクレオシド |
| JP2020070958A Withdrawn JP2020111608A (ja) | 2014-08-21 | 2020-04-10 | ２’−クロロアミノピリミジノンおよびピリミジンジオンヌクレオシド |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020070958A Withdrawn JP2020111608A (ja) | 2014-08-21 | 2020-04-10 | ２’−クロロアミノピリミジノンおよびピリミジンジオンヌクレオシド |
Country Status (17)
| Country | Link |
|---|---|
| US (6) | US9617295B2 (en:Method) |
| EP (2) | EP3183261B1 (en:Method) |
| JP (2) | JP6765364B2 (en:Method) |
| KR (1) | KR102528928B1 (en:Method) |
| CN (1) | CN106573954A (en:Method) |
| AR (1) | AR101561A1 (en:Method) |
| AU (1) | AU2015305593C1 (en:Method) |
| BR (1) | BR112017003242A2 (en:Method) |
| CA (1) | CA2958546C (en:Method) |
| EA (1) | EA201790234A1 (en:Method) |
| ES (1) | ES2808868T3 (en:Method) |
| IL (1) | IL250426A0 (en:Method) |
| MX (1) | MX2017002288A (en:Method) |
| NZ (1) | NZ728707A (en:Method) |
| SG (1) | SG11201700810SA (en:Method) |
| TW (1) | TWI673283B (en:Method) |
| WO (1) | WO2016028866A1 (en:Method) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| UA117095C2 (uk) | 2011-12-22 | 2018-06-25 | Аліос Біофарма, Інк. | Нуклеозидна сполука або її фармацевтично прийнятна сіль |
| USRE48171E1 (en) | 2012-03-21 | 2020-08-25 | Janssen 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 |
| TWI673283B (zh) * | 2014-08-21 | 2019-10-01 | 美商基利科學股份有限公司 | ２’－氯胺基嘧啶酮及嘧啶二酮核苷類 |
| AU2015320511B2 (en) * | 2014-09-26 | 2020-11-12 | Riboscience Llc | 4'-vinyl substituted nucleoside derivatives as inhibitors of Respiratory Syncytial Virus RNA replication |
| CA2972259A1 (en) | 2014-12-26 | 2016-06-30 | Emory University | N4-hydroxycytidine and derivatives and anti-viral uses related thereto |
| WO2018009623A1 (en) * | 2016-07-08 | 2018-01-11 | Atea Pharmaceuticals, Inc. | β-D-2'-DEOXY-2'-SUBSTITUTED-4'-SUBSTITUTED-2-SUBSTITUTED-N6-SUBSTITUTED-6-AMINOPURINE NUCLEOTIDES FOR THE TREATMENT OF PARAMYXOVIRUS AND ORTHOMYXOVIRUS INFECTIONS |
| MX2020005392A (es) | 2017-12-07 | 2020-12-07 | Univ Emory | N4-hidroxicitidina y derivados y usos antivirales relacionados con los mismos. |
| US20250009777A1 (en) * | 2021-11-12 | 2025-01-09 | National University Corporation Hokkaido University | Antiviral agent |
| AU2023236711A1 (en) | 2022-03-15 | 2024-10-03 | Rome Therapeutics, Inc. | Compounds and methods for treating disease |
| WO2024016639A1 (zh) * | 2022-07-21 | 2024-01-25 | 华创合成制药股份有限公司 | 一种抗病毒感染的化合物及其制备方法和用途 |
Family Cites Families (40)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3361306A (en) | 1966-03-31 | 1968-01-02 | Merck & Co Inc | Aerosol unit dispensing uniform amounts of a medically active ingredient |
| US3565070A (en) | 1969-02-28 | 1971-02-23 | Riker Laboratories Inc | Inhalation actuable aerosol dispenser |
| FR2224175B1 (en:Method) | 1973-04-04 | 1978-04-14 | Isf Spa | |
| US4069819A (en) | 1973-04-13 | 1978-01-24 | Societa Farmaceutici S.P.A. | Inhalation device |
| IT1017153B (it) | 1974-07-15 | 1977-07-20 | Isf Spa | Apparecchio per inalazioni |
| SE438261B (sv) | 1981-07-08 | 1985-04-15 | Draco Ab | Anvendning i dosinhalator av ett perforerat membran |
| US4805811A (en) | 1985-03-29 | 1989-02-21 | Aktiebolaget Draco | Dosage device |
| SE448277B (sv) | 1985-04-12 | 1987-02-09 | Draco Ab | Indikeringsanordning vid en doseringsanordning for lekemedel |
| IT1228459B (it) | 1989-02-23 | 1991-06-19 | Phidea S R L | Inalatore con svuotamento regolare e completo della capsula. |
| US4955371A (en) | 1989-05-08 | 1990-09-11 | Transtech Scientific, Inc. | Disposable inhalation activated, aerosol device for pulmonary medicine |
| CA2112674C (en) | 1991-07-02 | 2005-10-04 | John S. Patton | Method and device for delivering aerosolized medicaments |
| US5261538A (en) | 1992-04-21 | 1993-11-16 | Glaxo Inc. | Aerosol testing method |
| US5785049A (en) | 1994-09-21 | 1998-07-28 | Inhale Therapeutic Systems | Method and apparatus for dispersion of dry powder medicaments |
| US5388572A (en) | 1993-10-26 | 1995-02-14 | Tenax Corporation (A Connecticut Corp.) | Dry powder medicament inhalator having an inhalation-activated piston to aerosolize dose and deliver same |
| US5522385A (en) | 1994-09-27 | 1996-06-04 | Aradigm Corporation | Dynamic particle size control for aerosolized drug delivery |
| US5544647A (en) | 1994-11-29 | 1996-08-13 | Iep Group, Inc. | Metered dose inhalator |
| US5622163A (en) | 1994-11-29 | 1997-04-22 | Iep Group, Inc. | Counter for fluid dispensers |
| US6116234A (en) | 1999-02-01 | 2000-09-12 | Iep Pharmaceutical Devices Inc. | Metered dose inhaler agitator |
| US20030087873A1 (en) | 2000-10-18 | 2003-05-08 | Lieven Stuyver | Modified nucleosides for the treatment of viral infections and abnormal cellular proliferation |
| WO2008089105A2 (en) | 2007-01-12 | 2008-07-24 | Biocryst Pharmaceuticals, Inc. | Antiviral nucleoside analogs |
| PL2155758T3 (pl) | 2007-05-10 | 2013-06-28 | Biocryst Pharm Inc | Pochodne tetrahydrofuro[3,4-d]dioksolanu przeznaczone do stosowania w leczeniu infekcji wirusowych i raka |
| SI2268642T1 (sl) | 2008-04-23 | 2015-05-29 | Gilead Sciences, Inc. | 1'-substituirani karba-nukleozidni analogi za antivirusno zdravljenje |
| WO2010002877A2 (en) | 2008-07-03 | 2010-01-07 | Biota Scientific Management | Bycyclic nucleosides and nucleotides as therapeutic agents |
| ME02656B (me) | 2009-09-21 | 2017-06-20 | Gilead Sciences Inc | 2' -fluoro supstituisani karba-nukleozidni analozi za antiviralno lečenje |
| US8455451B2 (en) | 2009-09-21 | 2013-06-04 | Gilead Sciences, Inc. | 2'-fluoro substituted carba-nucleoside analogs for antiviral treatment |
| WO2011035250A1 (en) | 2009-09-21 | 2011-03-24 | Gilead Sciences, Inc. | Processes and intermediates for the preparation of 1'-substituted carba-nucleoside analogs |
| TW201201815A (en) | 2010-05-28 | 2012-01-16 | Gilead Sciences Inc | 1'-substituted-carba-nucleoside prodrugs for antiviral treatment |
| US9090642B2 (en) | 2010-07-19 | 2015-07-28 | Gilead Sciences, Inc. | Methods for the preparation of diasteromerically pure phosphoramidate prodrugs |
| JP5969471B2 (ja) | 2010-07-22 | 2016-08-17 | ギリード・サイエンシズ・インコーポレーテッド | パラミクソウイルス科ウイルス感染症を治療するための方法及び化合物 |
| TW201305185A (zh) | 2010-09-13 | 2013-02-01 | Gilead Sciences Inc | 用於抗病毒治療之２’－氟取代之碳－核苷類似物 |
| ES2701020T3 (es) * | 2010-09-22 | 2019-02-20 | Alios Biopharma Inc | Nucleósidos azido y análogos nucleotídicos |
| US20130273005A1 (en) | 2010-12-20 | 2013-10-17 | Gilead Sciences, Inc. | Methods for treating hcv |
| WO2012142075A1 (en) | 2011-04-13 | 2012-10-18 | Merck Sharp & Dohme Corp. | 2'-azido substituted nucleoside derivatives and methods of use thereof for the treatment of viral diseases |
| UA117095C2 (uk) * | 2011-12-22 | 2018-06-25 | Аліос Біофарма, Інк. | Нуклеозидна сполука або її фармацевтично прийнятна сіль |
| KR102172040B1 (ko) * | 2012-03-21 | 2020-10-30 | 얀센 바이오파마, 인코퍼레이트. | 치환된 뉴클레오사이드, 뉴클레오타이드 및 그의 유사체 |
| GB201220843D0 (en) * | 2012-11-20 | 2013-01-02 | Univ College Cork Nat Univ Ie | Compound |
| US10034893B2 (en) * | 2013-02-01 | 2018-07-31 | Enanta Pharmaceuticals, Inc. | 5, 6-D2 uridine nucleoside/tide derivatives |
| HK1224229A1 (zh) * | 2013-06-26 | 2017-08-18 | Alios Biopharma, Inc. | 取代的核苷，核苷酸及其类似物 |
| KR102314960B1 (ko) * | 2013-10-11 | 2021-10-19 | 얀센 바이오파마, 인코퍼레이트. | 치환된 뉴클레오사이드, 뉴클레오타이드 및 이의 유사체 |
| TWI673283B (zh) * | 2014-08-21 | 2019-10-01 | 美商基利科學股份有限公司 | ２’－氯胺基嘧啶酮及嘧啶二酮核苷類 |
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2015
- 2015-08-07 TW TW104125796A patent/TWI673283B/zh active
- 2015-08-14 AR ARP150102625A patent/AR101561A1/es unknown
- 2015-08-19 EP EP15760544.5A patent/EP3183261B1/en active Active
- 2015-08-19 CA CA2958546A patent/CA2958546C/en active Active
- 2015-08-19 EA EA201790234A patent/EA201790234A1/ru unknown
- 2015-08-19 WO PCT/US2015/045849 patent/WO2016028866A1/en not_active Ceased
- 2015-08-19 ES ES15760544T patent/ES2808868T3/es active Active
- 2015-08-19 CN CN201580044979.5A patent/CN106573954A/zh active Pending
- 2015-08-19 AU AU2015305593A patent/AU2015305593C1/en active Active
- 2015-08-19 EP EP20180058.8A patent/EP3738969A1/en active Pending
- 2015-08-19 MX MX2017002288A patent/MX2017002288A/es unknown
- 2015-08-19 US US14/830,121 patent/US9617295B2/en active Active
- 2015-08-19 KR KR1020177006312A patent/KR102528928B1/ko active Active
- 2015-08-19 SG SG11201700810SA patent/SG11201700810SA/en unknown
- 2015-08-19 NZ NZ728707A patent/NZ728707A/en unknown
- 2015-08-19 BR BR112017003242A patent/BR112017003242A2/pt not_active Application Discontinuation
- 2015-08-19 JP JP2017508531A patent/JP6765364B2/ja active Active
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2017
- 2017-02-02 IL IL250426A patent/IL250426A0/en unknown
- 2017-02-24 US US15/441,561 patent/US9982006B2/en active Active
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2018
- 2018-04-11 US US15/950,442 patent/US20180340004A1/en not_active Abandoned
- 2018-12-06 US US16/212,374 patent/US20190202852A1/en not_active Abandoned
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2019
- 2019-06-27 US US16/454,536 patent/US20200157137A1/en not_active Abandoned
- 2019-09-10 US US16/565,888 patent/US20200087337A1/en not_active Abandoned
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2020
- 2020-04-10 JP JP2020070958A patent/JP2020111608A/ja not_active Withdrawn