JP2013545818A5 - - Google Patents
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- JP2013545818A5 JP2013545818A5 JP2013544810A JP2013544810A JP2013545818A5 JP 2013545818 A5 JP2013545818 A5 JP 2013545818A5 JP 2013544810 A JP2013544810 A JP 2013544810A JP 2013544810 A JP2013544810 A JP 2013544810A JP 2013545818 A5 JP2013545818 A5 JP 2013545818A5
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- JP
- Japan
- Prior art keywords
- alkyl
- independently
- group
- 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.)
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- 125000000217 alkyl group Chemical group 0.000 claims description 236
- 150000001875 compounds Chemical class 0.000 claims description 139
- 229910052736 halogen Inorganic materials 0.000 claims description 79
- 150000002367 halogens Chemical class 0.000 claims description 78
- -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 39
- 229910052799 carbon Inorganic materials 0.000 claims description 26
- 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 24
- 150000003839 salts Chemical class 0.000 claims description 24
- 229910052757 nitrogen Inorganic materials 0.000 claims description 22
- 229910052739 hydrogen Inorganic materials 0.000 claims description 20
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims description 17
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 16
- 238000000034 method Methods 0.000 claims description 15
- 125000002088 tosyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1C([H])([H])[H])S(*)(=O)=O 0.000 claims description 15
- 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 12
- 125000000623 heterocyclic group Chemical group 0.000 claims description 12
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims description 10
- 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 9
- 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
- 125000001072 heteroaryl group Chemical group 0.000 claims description 6
- 125000003118 aryl group Chemical group 0.000 claims description 5
- 229910052794 bromium Inorganic materials 0.000 claims description 4
- 125000004432 carbon atom Chemical group C* 0.000 claims description 4
- 229910052801 chlorine Inorganic materials 0.000 claims description 4
- 239000003814 drug Substances 0.000 claims description 4
- 229910052731 fluorine Inorganic materials 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
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 5
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 5
- 239000000203 mixture Substances 0.000 claims 5
- 125000003341 7 membered heterocyclic group Chemical group 0.000 claims 2
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 1
- 125000006164 6-membered heteroaryl 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 |
|---|---|---|---|
| US42393310P | 2010-12-16 | 2010-12-16 | |
| US61/423,933 | 2010-12-16 | ||
| US201161527277P | 2011-08-25 | 2011-08-25 | |
| US61/527,277 | 2011-08-25 | ||
| PCT/US2011/065389 WO2012083122A1 (en) | 2010-12-16 | 2011-12-16 | Inhibitors of influenza viruses replication |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2013545818A JP2013545818A (ja) | 2013-12-26 |
| JP2013545818A5 true JP2013545818A5 (cg-RX-API-DMAC7.html) | 2015-02-12 |
Family
ID=45464909
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013544810A Pending JP2013545818A (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) | US20130345218A1 (cg-RX-API-DMAC7.html) |
| EP (1) | EP2651938A1 (cg-RX-API-DMAC7.html) |
| JP (1) | JP2013545818A (cg-RX-API-DMAC7.html) |
| KR (1) | KR20130128435A (cg-RX-API-DMAC7.html) |
| CN (1) | CN103562205A (cg-RX-API-DMAC7.html) |
| AU (1) | AU2011343647A1 (cg-RX-API-DMAC7.html) |
| CA (1) | CA2822062A1 (cg-RX-API-DMAC7.html) |
| MX (1) | MX2013006840A (cg-RX-API-DMAC7.html) |
| RU (1) | RU2013132683A (cg-RX-API-DMAC7.html) |
| WO (1) | WO2012083122A1 (cg-RX-API-DMAC7.html) |
Families Citing this family (41)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2006127587A1 (en) * | 2005-05-20 | 2006-11-30 | Vertex Pharmaceuticals Incorporated | Pyrrolopyridines useful as inhibitors of protein kinase |
| PL2442809T3 (pl) | 2009-06-17 | 2017-02-28 | Vertex Pharmaceuticals Incorporated | Inhibitory replikacji wirusów grypy |
| AU2011343642A1 (en) | 2010-12-16 | 2013-05-02 | Vertex Pharmaceuticals Incorporated | Inhibitors of influenza viruses replication |
| UA118010C2 (uk) | 2011-08-01 | 2018-11-12 | Вертекс Фармасьютікалз Інкорпорейтед | Інгібітори реплікації вірусів грипу |
| EP3421468B1 (en) | 2013-11-13 | 2020-11-04 | Vertex Pharmaceuticals Incorporated | Methods of preparing inhibitors of influenza viruses replication |
| LT3068776T (lt) * | 2013-11-13 | 2019-08-12 | Vertex Pharmaceuticals Incorporated | Gripo virusų replikacijos inhibitoriai |
| RU2016129380A (ru) | 2013-12-20 | 2018-01-25 | СИГНАЛ ФАРМАСЬЮТИКАЛЗ, ЭлЭлСи | Замещенные диаминопиримидильные соединения, их композиции и способы лечения с их участием |
| SG11201700956VA (en) * | 2014-08-08 | 2017-03-30 | Janssen Sciences Ireland Uc | Indoles for use in influenza virus infection |
| DK3191489T3 (da) * | 2014-09-08 | 2021-03-29 | Janssen Sciences Ireland Unlimited Co | Pyrrolopyrimidiner til anvendelse ved influenzavirusinfektion |
| JP6892433B2 (ja) | 2015-04-03 | 2021-06-23 | ユニバーシティ・オブ・マサチューセッツＵｎｉｖｅｒｓｉｔｙ Ｏｆ Ｍａｓｓａｃｈｕｓｅｔｔｓ | 十分に安定化された非対称ｓｉｒｎａ |
| WO2016183120A1 (en) | 2015-05-13 | 2016-11-17 | Vertex Pharmaceuticals Incorporated | Inhibitors of influenza viruses replication |
| JP6704416B2 (ja) | 2015-05-13 | 2020-06-03 | バーテックス ファーマシューティカルズ インコーポレイテッドＶｅｒｔｅｘ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃｏｒｐｏｒａｔｅｄ | インフルエンザウイルスの複製の阻害剤を調製する方法 |
| US10633653B2 (en) | 2015-08-14 | 2020-04-28 | University Of Massachusetts | Bioactive conjugates for oligonucleotide delivery |
| WO2017089518A1 (en) * | 2015-11-27 | 2017-06-01 | Janssen Sciences Ireland Uc | Heterocyclic indoles for use in influenza virus infection |
| US10717732B2 (en) | 2015-12-09 | 2020-07-21 | Sunshine Lake Pharma Co., Ltd. | Inhibitors of influenza virus replication, application methods and uses thereof |
| CA3010327A1 (en) * | 2016-01-20 | 2017-07-27 | Janssen Sciences Ireland Uc | Aryl substituted pyrimidines for use in influenza virus infection |
| US10478503B2 (en) | 2016-01-31 | 2019-11-19 | University Of Massachusetts | Branched oligonucleotides |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| WO2018041091A1 (en) * | 2016-08-30 | 2018-03-08 | Sunshine Lake Pharma Co., Ltd. | Inhibitors of influenza virus replication, application methods and uses thereof |
| KR102554019B1 (ko) | 2016-12-15 | 2023-07-11 | 선샤인 레이크 파르마 컴퍼니 리미티드 | 인플루엔자 바이러스 복제의 억제제 및 이의 용도 |
| CN108276401B (zh) | 2017-01-05 | 2020-12-22 | 广东东阳光药业有限公司 | 流感病毒复制抑制剂及其用途 |
| WO2018157830A1 (en) | 2017-03-02 | 2018-09-07 | 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 |
| CN110799647A (zh) | 2017-06-23 | 2020-02-14 | 马萨诸塞大学 | 双尾自递送sirna及相关的方法 |
| TWI821343B (zh) * | 2018-07-27 | 2023-11-11 | 美商共結晶製藥公司 | 流感病毒複製之抑制劑 |
| WO2020041769A1 (en) | 2018-08-23 | 2020-02-27 | University Of Massachusetts | O-methyl rich fully stabilized oligonucleotides |
| CN109678738B (zh) * | 2018-12-26 | 2021-11-30 | 深圳市华先医药科技有限公司 | 一种合成(2s,3s)-3-氨基-二环[2.2.2]辛烷-2-甲酸酯的方法 |
| CN113614232A (zh) | 2019-01-18 | 2021-11-05 | 马萨诸塞大学 | 动态药代动力学修饰锚 |
| US11820985B2 (en) | 2019-03-26 | 2023-11-21 | University Of Massachusetts | Modified oligonucleotides with increased stability |
| AU2020329155A1 (en) | 2019-08-09 | 2022-03-10 | University Of Massachusetts | Chemically modified oligonucleotides targeting SNPs |
| US12365894B2 (en) | 2019-09-16 | 2025-07-22 | University Of Massachusetts | Branched lipid conjugates of siRNA for specific tissue delivery |
| CA3172168A1 (en) | 2020-03-26 | 2021-09-30 | Anastasia Khvorova | Synthesis of modified oligonucleotides with increased stability |
| IL297069A (en) * | 2020-04-10 | 2022-12-01 | Cocrystal Pharma Inc | Replication inhibitors of norovirus and corona virus |
| CN112063726A (zh) * | 2020-09-21 | 2020-12-11 | 杭州市疾病预防控制中心 | 一种用于检测奥司他韦耐药突变的引物、探针及检测方法 |
| WO2023107705A1 (en) | 2021-12-10 | 2023-06-15 | Incyte Corporation | Bicyclic amines as cdk12 inhibitors |
Family Cites Families (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1322652A1 (en) | 2000-09-22 | 2003-07-02 | Eli Lilly And Company | Stereoselective process for preparing cyclohexyl amine derivatives |
| 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 |
| AR045595A1 (es) * | 2003-09-04 | 2005-11-02 | Vertex Pharma | Composiciones utiles como inhibidores de proteinas quinasas |
| PL2332940T3 (pl) | 2004-03-30 | 2013-03-29 | Vertex Pharma | Azaindole użyteczne jako inhibitory JAK i innych kinaz białkowych |
| UA87494C2 (en) * | 2004-03-30 | 2009-07-27 | Вертекс Фармасьютикалс Инкорпорейтед | Azaindoles useful as inhibitors of jak and other protein kinases |
| US20060161001A1 (en) * | 2004-12-20 | 2006-07-20 | Amgen Inc. | Substituted heterocyclic compounds and methods of use |
| CN101218241B (zh) * | 2005-05-16 | 2011-02-16 | Irm责任有限公司 | 用作蛋白激酶抑制剂的吡咯并吡啶衍生物 |
| KR20080063809A (ko) * | 2005-09-30 | 2008-07-07 | 버텍스 파마슈티칼스 인코포레이티드 | 야누스 키나아제의 억제제로서 유용한 데아자퓨린 |
| TWI424999B (zh) * | 2006-01-17 | 2014-02-01 | Vertex Pharma | 適合作為傑納斯激酶（ｊａｎｕｓ ｋｉｎａｓｅ）抑制劑之氮雜吲哚 |
| WO2008079346A1 (en) | 2006-12-21 | 2008-07-03 | Vertex Pharmaceuticals Incorporated | 5-cyan0-4- (pyrrolo [2, 3b] pyridine-3-yl) -pyrimidine derivatives useful as protein kinase inhibitors |
| WO2009073300A1 (en) | 2007-11-02 | 2009-06-11 | Vertex Pharmaceuticals Incorporated | [1h- pyrazolo [3, 4-b] pyridine-4-yl] -phenyle or -pyridin-2-yle derivatives as protein kinase c-theta |
| WO2010011768A1 (en) | 2008-07-23 | 2010-01-28 | Vertex Pharmaceuticals Incorporated | Tri-cyclic pyrazolopyridine kinase inhibitors |
| MX2011000843A (es) | 2008-07-23 | 2011-04-11 | Vertex Pharma | Inhibidores de pirazolopiridin cinasa triciclicos. |
| WO2010011756A1 (en) | 2008-07-23 | 2010-01-28 | Vertex Pharmaceuticals Incorporated | Pyrazolopyridine kinase inhibitors |
| US20100038988A1 (en) | 2008-08-12 | 2010-02-18 | Gannon Ramy | Stator and Method of Making the Same |
| PL2442809T3 (pl) * | 2009-06-17 | 2017-02-28 | Vertex Pharmaceuticals Incorporated | Inhibitory replikacji wirusów grypy |
| CN102471339A (zh) * | 2009-07-15 | 2012-05-23 | 雅培制药有限公司 | 激酶的吡咯并吡啶抑制剂 |
-
2011
- 2011-12-16 KR KR1020137018522A patent/KR20130128435A/ko not_active Withdrawn
- 2011-12-16 JP JP2013544810A patent/JP2013545818A/ja active Pending
- 2011-12-16 RU RU2013132683/04A patent/RU2013132683A/ru not_active Application Discontinuation
- 2011-12-16 MX MX2013006840A patent/MX2013006840A/es not_active Application Discontinuation
- 2011-12-16 EP EP11806096.1A patent/EP2651938A1/en not_active Withdrawn
- 2011-12-16 CA CA2822062A patent/CA2822062A1/en not_active Abandoned
- 2011-12-16 WO PCT/US2011/065389 patent/WO2012083122A1/en not_active Ceased
- 2011-12-16 CN CN201180066551.2A patent/CN103562205A/zh active Pending
- 2011-12-16 AU AU2011343647A patent/AU2011343647A1/en not_active Abandoned
-
2013
- 2013-06-14 US US13/918,115 patent/US20130345218A1/en not_active Abandoned