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 (https=) | 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 (https=) |
| EP (1) | EP2651941A1 (https=) |
| JP (1) | JP2013545817A (https=) |
| KR (1) | KR20130128436A (https=) |
| CN (1) | CN103492382A (https=) |
| AU (1) | AU2011343646A1 (https=) |
| CA (1) | CA2822059A1 (https=) |
| MX (1) | MX2013006846A (https=) |
| RU (1) | RU2013132717A (https=) |
| WO (1) | WO2012083121A1 (https=) |
Families Citing this family (34)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RS57869B1 (sr) | 2009-06-17 | 2018-12-31 | Vertex Pharma | Inhibitori replikacije virusa gripa |
| 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 |
| HRP20181272T1 (hr) | 2013-11-13 | 2018-10-05 | Vertex Pharmaceuticals Incorporated | Postupci priprave inhibitora replikacije virusa influence |
| RS59144B1 (sr) | 2013-11-13 | 2019-09-30 | Vertex Pharma | Inhibitori replikacije virusa influence |
| EP3277811B1 (en) | 2015-04-03 | 2020-12-23 | University of Massachusetts | Fully stabilized asymmetric sirna |
| JP6857617B2 (ja) | 2015-05-13 | 2021-04-14 | 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 |
| 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 |
| CN109748915B (zh) | 2015-12-09 | 2021-03-26 | 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 |
| WO2017132669A1 (en) | 2016-01-31 | 2017-08-03 | University Of Massachusetts | Branched oligonucleotides |
| 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 |
| 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 |
| 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 |
| 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 |
| 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 |
| CN109641868B (zh) * | 2016-08-30 | 2021-12-03 | 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 |
| US10987354B2 (en) | 2016-12-15 | 2021-04-27 | 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 |
| JP7406793B2 (ja) | 2017-06-23 | 2023-12-28 | ユニバーシティー オブ マサチューセッツ | ２テイル自己デリバリー型ｓｉＲＮＡおよび関連方法 |
| 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 |
| JP7627042B2 (ja) | 2018-08-23 | 2025-02-05 | ユニバーシティー オブ マサチューセッツ | Ｏ－メチルリッチ完全安定化オリゴヌクレオチド |
| 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 |
| MX2022001710A (es) | 2019-08-09 | 2022-05-10 | Univ Massachusetts | Oligonucleótidos modificados químicamente dirigidos a los snp. |
| 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 |
| JP7837560B2 (ja) | 2020-03-26 | 2026-03-31 | ユニバーシティー オブ マサチューセッツ | 安定性の向上を有する修飾オリゴヌクレオチドの合成 |
| WO2021242883A1 (en) | 2020-05-26 | 2021-12-02 | University Of Massachusetts | Synthetic oligonucleotides having regions of block and cluster modifications |
| WO2023107705A1 (en) | 2021-12-10 | 2023-06-15 | Incyte Corporation | Bicyclic amines as cdk12 inhibitors |
Family Cites Families (14)
| 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 |
| US6825190B2 (en) * | 2001-06-15 | 2004-11-30 | Vertex Pharmaceuticals Incorporated | Protein kinase inhibitors and uses thereof |
| BR0211900A (pt) | 2001-08-14 | 2004-08-24 | Toyama Chemical Co Ltd | Método para inibição do desenvolvimento de vìrus e/ou virucida, análogos de nucleotìdeo de pirazina e de nucleosìdeo de pirazina, precursor do inibidor da polimerase de rna, inibidor da polimerase de rna, método para tratar pacientes infectados por vìrus, e, usos de um análogo de nucleotìdeo de pirazina ou um sal deste e de um análogo de nucleosìdeo de pirazina ou um sal deste |
| TWI372624B (en) * | 2004-03-30 | 2012-09-21 | Vertex Pharma | Azaindoles useful as inhibitors of jak and other protein kinases |
| UA87494C2 (en) * | 2004-03-30 | 2009-07-27 | Вертекс Фармасьютикалс Инкорпорейтед | Azaindoles useful as inhibitors of jak and other protein kinases |
| US7855205B2 (en) * | 2004-10-29 | 2010-12-21 | Janssen Pharmaceutica Nv | Pyrimidinyl substituted fused-pyrrolyl compounds useful in treating kinase disorders |
| DE602006014540D1 (en) * | 2005-05-16 | 2010-07-08 | Irm Llc | Pyrrolopyridinderivate als proteinkinaseinhibitoren |
| CN102532133A (zh) | 2006-01-17 | 2012-07-04 | 沃泰克斯药物股份有限公司 | 适用作詹纳斯激酶抑制剂的吖吲哚类 |
| CA2704266A1 (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 |
| CN102159574A (zh) | 2008-07-23 | 2011-08-17 | 沃泰克斯药物股份有限公司 | 三-环吡唑并吡啶激酶抑制剂 |
| ES2402087T3 (es) | 2008-07-23 | 2013-04-26 | Vertex Pharmaceuticals Incorporated | Inhibidores de la pirazolopiridina quinasa |
| AU2009274023A1 (en) | 2008-07-23 | 2010-01-28 | Vertex Pharmaceuticals Incorporated | Tri-cyclic pyrazolopyridine kinase inhibitors |
| US20100038988A1 (en) | 2008-08-12 | 2010-02-18 | Gannon Ramy | Stator and Method of Making the Same |
| RS57869B1 (sr) * | 2009-06-17 | 2018-12-31 | Vertex Pharma | Inhibitori replikacije virusa gripa |
-
2011
- 2011-12-16 CN CN201180066553.1A patent/CN103492382A/zh active Pending
- 2011-12-16 AU AU2011343646A patent/AU2011343646A1/en not_active Abandoned
- 2011-12-16 CA CA2822059A patent/CA2822059A1/en not_active Abandoned
- 2011-12-16 EP EP11808476.3A patent/EP2651941A1/en not_active Withdrawn
- 2011-12-16 KR KR1020137018528A patent/KR20130128436A/ko not_active Withdrawn
- 2011-12-16 MX MX2013006846A patent/MX2013006846A/es not_active Application Discontinuation
- 2011-12-16 JP JP2013544809A patent/JP2013545817A/ja 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
-
2013
- 2013-06-14 US US13/918,110 patent/US20140005197A1/en not_active Abandoned
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