JP2013545817A5 - - Google Patents
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- JP2013545817A5 JP2013545817A5 JP2013544809A JP2013544809A JP2013545817A5 JP 2013545817 A5 JP2013545817 A5 JP 2013545817A5 JP 2013544809 A JP2013544809 A JP 2013544809A JP 2013544809 A JP2013544809 A JP 2013544809A JP 2013545817 A5 JP2013545817 A5 JP 2013545817A5
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- JP
- Japan
- Prior art keywords
- alkyl
- group
- independently
- optionally
- substituted
- 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 description 237
- 150000001875 compounds Chemical class 0.000 claims description 137
- 229910052736 halogen Inorganic materials 0.000 claims description 80
- 150000002367 halogens Chemical class 0.000 claims description 79
- -1 cyano, hydroxy Chemical group 0.000 claims description 60
- 125000004043 oxo group Chemical group O=* 0.000 claims description 44
- 125000001424 substituent group Chemical group 0.000 claims description 43
- 125000002837 carbocyclic group Chemical group 0.000 claims description 41
- 229910052799 carbon Inorganic materials 0.000 claims description 25
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 25
- 125000001188 haloalkyl group Chemical group 0.000 claims description 23
- 229910052757 nitrogen Inorganic materials 0.000 claims description 22
- 238000000034 method Methods 0.000 claims description 21
- 229910052739 hydrogen Inorganic materials 0.000 claims description 20
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims description 18
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 16
- 150000003839 salts Chemical class 0.000 claims description 16
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 14
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 14
- 125000005330 8 membered heterocyclic group Chemical group 0.000 claims description 13
- 125000002221 trityl group Chemical group [H]C1=C([H])C([H])=C([H])C([H])=C1C([*])(C1=C(C(=C(C(=C1[H])[H])[H])[H])[H])C1=C([H])C([H])=C([H])C([H])=C1[H] 0.000 claims description 13
- 125000000623 heterocyclic group Chemical group 0.000 claims description 12
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims description 10
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 8
- 125000000041 C6-C10 aryl group Chemical group 0.000 claims description 7
- 125000004429 atom Chemical group 0.000 claims description 6
- 239000012472 biological sample Substances 0.000 claims description 6
- 125000003118 aryl group Chemical group 0.000 claims description 5
- 125000001072 heteroaryl group Chemical group 0.000 claims description 5
- 125000004432 carbon atom Chemical group C* 0.000 claims description 4
- 239000003814 drug Substances 0.000 claims description 4
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 4
- 229940124597 therapeutic agent Drugs 0.000 claims description 4
- 241000712461 unidentified influenza virus Species 0.000 claims description 4
- 229940126062 Compound A Drugs 0.000 claims description 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 description 2
- 239000002671 adjuvant Substances 0.000 claims description 2
- 239000003443 antiviral agent Substances 0.000 claims description 2
- 125000006367 bivalent amino carbonyl group Chemical group [H]N([*:1])C([*:2])=O 0.000 claims description 2
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 206010022000 influenza Diseases 0.000 claims description 2
- 229960003971 influenza vaccine Drugs 0.000 claims description 2
- 230000002401 inhibitory effect Effects 0.000 claims description 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 2
- 125000002950 monocyclic group Chemical group 0.000 claims description 2
- 125000006574 non-aromatic ring group Chemical group 0.000 claims description 2
- 239000008194 pharmaceutical composition Substances 0.000 claims description 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 2
- 125000004765 (C1-C4) haloalkyl group Chemical group 0.000 claims 14
- 239000000203 mixture Substances 0.000 claims 6
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 5
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 5
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 1
- 125000006164 6-membered heteroaryl group Chemical group 0.000 claims 1
- 125000003341 7 membered heterocyclic group Chemical group 0.000 claims 1
- 125000005843 halogen group Chemical group 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- 230000010076 replication Effects 0.000 claims 1
- 125000001931 aliphatic group Chemical group 0.000 description 15
- 125000003545 alkoxy group Chemical group 0.000 description 2
- 230000029812 viral genome replication Effects 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US42392510P | 2010-12-16 | 2010-12-16 | |
| US61/423,925 | 2010-12-16 | ||
| US201161527276P | 2011-08-25 | 2011-08-25 | |
| US61/527,276 | 2011-08-25 | ||
| PCT/US2011/065388 WO2012083121A1 (en) | 2010-12-16 | 2011-12-16 | Inhibitors of influenza viruses replication |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2013545817A JP2013545817A (ja) | 2013-12-26 |
| JP2013545817A5 true JP2013545817A5 (enExample) | 2015-02-12 |
Family
ID=45478532
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013544809A Pending JP2013545817A (ja) | 2010-12-16 | 2011-12-16 | インフルエンザウイルス複製阻害物質 |
Country Status (10)
| Country | Link |
|---|---|
| US (1) | US20140005197A1 (enExample) |
| EP (1) | EP2651941A1 (enExample) |
| JP (1) | JP2013545817A (enExample) |
| KR (1) | KR20130128436A (enExample) |
| CN (1) | CN103492382A (enExample) |
| AU (1) | AU2011343646A1 (enExample) |
| CA (1) | CA2822059A1 (enExample) |
| MX (1) | MX2013006846A (enExample) |
| RU (1) | RU2013132717A (enExample) |
| WO (1) | WO2012083121A1 (enExample) |
Families Citing this family (36)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GEP20207129B (en) | 2009-06-17 | 2020-07-10 | Vertex Pharma | Inhibitors of influenza viruses replication |
| RU2013132681A (ru) | 2010-12-16 | 2015-01-27 | Вертекс Фармасьютикалз Инкорпорейтед | Ингибиторы репликации вирусов гриппа |
| UA118010C2 (uk) | 2011-08-01 | 2018-11-12 | Вертекс Фармасьютікалз Інкорпорейтед | Інгібітори реплікації вірусів грипу |
| PT3068776T (pt) | 2013-11-13 | 2019-08-26 | Vertex Pharma | Inibidores da replicação de vírus da gripe |
| HUE038820T2 (hu) | 2013-11-13 | 2018-11-28 | Vertex Pharma | Eljárás influenzavírusok replikációjának inhibitorai elõállítására |
| EP3929293A3 (en) | 2015-04-03 | 2022-03-16 | University Of Massachusetts | Fully stabilized asymmetric sirna |
| WO2016183120A1 (en) | 2015-05-13 | 2016-11-17 | Vertex Pharmaceuticals Incorporated | Inhibitors of influenza viruses replication |
| EP3294717B1 (en) | 2015-05-13 | 2020-07-29 | Vertex Pharmaceuticals Inc. | Methods of preparing inhibitors of influenza viruses replication |
| WO2017030973A1 (en) | 2015-08-14 | 2017-02-23 | University Of Massachusetts | Bioactive conjugates for oligonucleotide delivery |
| EP3362451B1 (en) | 2015-12-09 | 2023-04-12 | Sunshine Lake Pharma Co., Ltd. | Inhibitors of influenza virus replication, application methods and uses thereof |
| WO2017132669A1 (en) | 2016-01-31 | 2017-08-03 | University Of Massachusetts | Branched oligonucleotides |
| WO2017133664A1 (en) * | 2016-02-05 | 2017-08-10 | Savira Pharmaceuticals Gmbh | Bicyclic pyridine and pyrimidine derivatives and their use in the treatment， amelioration or prevention of influenza |
| WO2017133670A1 (en) * | 2016-02-05 | 2017-08-10 | Savira Pharmaceuticals Gmbh | Pyridine and pyrimidine derivatives and their use in treatment, amelioration or prevention of influenza |
| WO2017133657A1 (en) * | 2016-02-05 | 2017-08-10 | Savira Pharmaceuticals Gmbh | Pyridine and pyrimidine derivatives and their use in treatment, amelioration or prevention of influenza |
| WO2017133665A1 (en) * | 2016-02-05 | 2017-08-10 | Savira Pharmaceuticals Gmbh | 6,7-diazaindazole and 6,7-diazaindole derivatives and use in treatment, amelioration or prevention of influenza thereof |
| WO2017133667A1 (en) * | 2016-02-05 | 2017-08-10 | Savira Pharmaceuticals Gmbh | Pyrimidine and pyridine derivatives and use in treatment, amelioration or prevention of influenza thereof |
| WO2017133658A1 (en) * | 2016-02-05 | 2017-08-10 | Savira Pharmaceuticals Gmbh | 4, 7-diazaindole and 4, 7-diazaindazole derivatives and their use in the treatment, amelioration or prevention of influenza |
| CN107759571B (zh) | 2016-08-16 | 2021-03-02 | 广东东阳光药业有限公司 | 流感病毒复制抑制剂及其使用方法和用途 |
| US10647693B2 (en) | 2016-08-30 | 2020-05-12 | North & South Brother Pharmacy Investment Company Limited | Inhibitors of influenza virus replication, application methods and uses thereof |
| CA3045371C (en) | 2016-12-15 | 2024-05-14 | Sunshine Lake Pharma Co., Ltd. | Inhibitors of influenza virus replication and uses thereof |
| WO2018127096A1 (en) * | 2017-01-05 | 2018-07-12 | Sunshine Lake Pharma Co., Ltd. | Inhibitors of influenza virus replication and uses thereof |
| US10927118B2 (en) | 2017-03-02 | 2021-02-23 | Sunshine Lake Pharma Co., Ltd. | Inhibitors of influenza virus replication and uses thereof |
| CN108727369B (zh) * | 2017-04-25 | 2023-06-09 | 广东东阳光药业有限公司 | 流感病毒复制抑制剂及其用途 |
| WO2018237245A1 (en) | 2017-06-23 | 2018-12-27 | University Of Massachusetts | TWO TAIL SELF-ADMINISTRATION SIRNA AND ASSOCIATED METHODS |
| WO2019089734A1 (en) * | 2017-10-31 | 2019-05-09 | Arizona Board Of Regents On Behalf Of The University Of Arizona | Methods and compositions for the treatment of influenza |
| BR112021002440A2 (pt) | 2018-08-10 | 2021-05-04 | University Of Massachusetts | oligonucleotídeos modificados visando snps |
| WO2020041769A1 (en) | 2018-08-23 | 2020-02-27 | University Of Massachusetts | O-methyl rich fully stabilized oligonucleotides |
| CN113614232A (zh) | 2019-01-18 | 2021-11-05 | 马萨诸塞大学 | 动态药代动力学修饰锚 |
| EP3946369A4 (en) | 2019-03-26 | 2023-10-18 | University Of Massachusetts | MODIFIED OLIGONUCLEOTIDES WITH INCREASED STABILITY |
| KR20220047989A (ko) | 2019-08-09 | 2022-04-19 | 유니버시티 오브 매사추세츠 | Snp를 표적화하는 화학적으로 변형된 올리고뉴클레오타이드 |
| US12365894B2 (en) | 2019-09-16 | 2025-07-22 | University Of Massachusetts | Branched lipid conjugates of siRNA for specific tissue delivery |
| CN110787170B (zh) * | 2019-12-19 | 2022-06-28 | 浙江立恩生物科技有限公司 | 一种治疗流感病毒感染的药物 |
| AU2021244600A1 (en) | 2020-03-26 | 2022-11-03 | University Of Massachusetts | Synthesis of modified oligonucleotides with increased stability |
| CA3174079A1 (en) | 2020-05-26 | 2021-12-02 | Anastasia Khvorova | Synthetic oligonucleotides having regions of block and cluster modifications |
| TW202329937A (zh) | 2021-12-03 | 2023-08-01 | 美商英塞特公司 | 雙環胺ｃｋ１２抑制劑 |
| US12084453B2 (en) | 2021-12-10 | 2024-09-10 | Incyte Corporation | Bicyclic amines as CDK12 inhibitors |
Family Cites Families (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2004509897A (ja) | 2000-09-22 | 2004-04-02 | イーライ・リリー・アンド・カンパニー | シクロヘキシルアミン誘導体の立体選択的製造方法 |
| CA2450769A1 (en) * | 2001-06-15 | 2002-12-27 | Vertex Pharmaceuticals Incorporated | 5-(2-aminopyrimidin-4-yl) benzisoxazoles as protein kinase inhibitors |
| CA2456292A1 (en) | 2001-08-14 | 2003-02-27 | Toyama Chemical Co., Ltd. | Novel virus growth inhibitor and/or virucidal method, and novel pyrazine nucleotide or pirazine nucleoside analog |
| ES2364340T3 (es) * | 2004-03-30 | 2011-08-31 | Vertex Pharmaceuticals Incorporated | Azaindoles útiles como inhibidores de jak y otras proteína quinasas. |
| UA87494C2 (en) * | 2004-03-30 | 2009-07-27 | Вертекс Фармасьютикалс Инкорпорейтед | Azaindoles useful as inhibitors of jak and other protein kinases |
| WO2006050076A1 (en) * | 2004-10-29 | 2006-05-11 | Janssen Pharmaceutica, N.V. | Pyrimidinyl substituted fused-pyrrolyl compounds useful in treating kinase disorders |
| AU2006247322A1 (en) * | 2005-05-16 | 2006-11-23 | Irm Llc | Pyrrolopyridine derivatives as protein kinase inhibitors |
| NZ592968A (en) | 2006-01-17 | 2012-08-31 | Vertex Pharma | Azaindoles substituted with either triazine or pyrimidine useful as inhibitors of janus kinases consisting of JAK1, JAK2, JAK3, and TYK2 |
| US8173635B2 (en) | 2007-11-02 | 2012-05-08 | Vertex Pharmaceuticals Incorporated | Kinase inhibitors |
| NZ590784A (en) | 2008-07-23 | 2012-12-21 | Vertex Pharma | Pyrazolopyridine kinase inhibitors |
| CA2731432A1 (en) | 2008-07-23 | 2010-01-28 | Vertex Pharmaceuticals Incorporated | Tri-cyclic pyrazolopyridine kinase inhibitors |
| MX2011000837A (es) | 2008-07-23 | 2011-04-05 | Vertex Pharma | Inhibidores de pirazolpiridina cinasa triciclica. |
| US20100038988A1 (en) | 2008-08-12 | 2010-02-18 | Gannon Ramy | Stator and Method of Making the Same |
| GEP20207129B (en) * | 2009-06-17 | 2020-07-10 | Vertex Pharma | Inhibitors of influenza viruses replication |
-
2011
- 2011-12-16 JP JP2013544809A patent/JP2013545817A/ja active Pending
- 2011-12-16 CN CN201180066553.1A patent/CN103492382A/zh active Pending
- 2011-12-16 RU RU2013132717/04A patent/RU2013132717A/ru not_active Application Discontinuation
- 2011-12-16 WO PCT/US2011/065388 patent/WO2012083121A1/en not_active Ceased
- 2011-12-16 EP EP11808476.3A patent/EP2651941A1/en not_active Withdrawn
- 2011-12-16 CA CA2822059A patent/CA2822059A1/en not_active Abandoned
- 2011-12-16 AU AU2011343646A patent/AU2011343646A1/en not_active Abandoned
- 2011-12-16 KR KR1020137018528A patent/KR20130128436A/ko not_active Withdrawn
- 2011-12-16 MX MX2013006846A patent/MX2013006846A/es not_active Application Discontinuation
-
2013
- 2013-06-14 US US13/918,110 patent/US20140005197A1/en not_active Abandoned
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