CA2822059A1 - Inhibitors of influenza viruses replication - Google Patents
Inhibitors of influenza viruses replication Download PDFInfo
- Publication number
- CA2822059A1 CA2822059A1 CA2822059A CA2822059A CA2822059A1 CA 2822059 A1 CA2822059 A1 CA 2822059A1 CA 2822059 A CA2822059 A CA 2822059A CA 2822059 A CA2822059 A CA 2822059A CA 2822059 A1 CA2822059 A1 CA 2822059A1
- Authority
- CA
- Canada
- Prior art keywords
- alkyl
- independently
- group
- compound
- 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.)
- Abandoned
Links
- 241000712461 unidentified influenza virus Species 0.000 title claims abstract description 45
- 230000010076 replication Effects 0.000 title claims abstract description 16
- 239000003112 inhibitor Substances 0.000 title description 6
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- 238000000034 method Methods 0.000 claims abstract description 83
- 150000003839 salts Chemical class 0.000 claims abstract description 77
- 206010022000 influenza Diseases 0.000 claims abstract description 65
- 239000012472 biological sample Substances 0.000 claims abstract description 21
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract description 21
- 239000003937 drug carrier Substances 0.000 claims abstract description 16
- 239000003981 vehicle Substances 0.000 claims abstract description 11
- 230000002401 inhibitory effect Effects 0.000 claims abstract description 10
- 239000002671 adjuvant Substances 0.000 claims abstract description 8
- -1 cyano, hydroxy Chemical group 0.000 claims description 198
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims description 167
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- 125000001424 substituent group Chemical group 0.000 claims description 90
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- 229910052757 nitrogen Inorganic materials 0.000 claims description 77
- 125000004043 oxo group Chemical group O=* 0.000 claims description 71
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- 125000001931 aliphatic group Chemical group 0.000 claims description 61
- 125000002837 carbocyclic group Chemical group 0.000 claims description 61
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 50
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- AWUCVROLDVIAJX-GSVOUGTGSA-N sn-glycerol 3-phosphate Chemical compound OC[C@@H](O)COP(O)(O)=O AWUCVROLDVIAJX-GSVOUGTGSA-N 0.000 description 1
- URGAHOPLAPQHLN-UHFFFAOYSA-N sodium aluminosilicate Chemical compound [Na+].[Al+3].[O-][Si]([O-])=O.[O-][Si]([O-])=O URGAHOPLAPQHLN-UHFFFAOYSA-N 0.000 description 1
- 229910000029 sodium carbonate Inorganic materials 0.000 description 1
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- 239000001509 sodium citrate Substances 0.000 description 1
- NLJMYIDDQXHKNR-UHFFFAOYSA-K sodium citrate Chemical compound O.O.[Na+].[Na+].[Na+].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O NLJMYIDDQXHKNR-UHFFFAOYSA-K 0.000 description 1
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- IOGXOCVLYRDXLW-UHFFFAOYSA-N tert-butyl nitrite Chemical compound CC(C)(C)ON=O IOGXOCVLYRDXLW-UHFFFAOYSA-N 0.000 description 1
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- QEMXHQIAXOOASZ-UHFFFAOYSA-N tetramethylammonium Chemical compound C[N+](C)(C)C QEMXHQIAXOOASZ-UHFFFAOYSA-N 0.000 description 1
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- JOXIMZWYDAKGHI-UHFFFAOYSA-N toluene-4-sulfonic acid Chemical compound CC1=CC=C(S(O)(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-N 0.000 description 1
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- 229910052722 tritium Inorganic materials 0.000 description 1
- ZDPHROOEEOARMN-UHFFFAOYSA-N undecanoic acid Chemical compound CCCCCCCCCCC(O)=O ZDPHROOEEOARMN-UHFFFAOYSA-N 0.000 description 1
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- NQPDZGIKBAWPEJ-UHFFFAOYSA-N valeric acid Chemical class CCCCC(O)=O NQPDZGIKBAWPEJ-UHFFFAOYSA-N 0.000 description 1
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/16—Antivirals for RNA viruses for influenza or rhinoviruses
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Virology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Oncology (AREA)
- Communicable Diseases (AREA)
- Pulmonology (AREA)
- Molecular Biology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
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 (1)
| Publication Number | Publication Date |
|---|---|
| CA2822059A1 true CA2822059A1 (en) | 2012-06-21 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA2822059A Abandoned CA2822059A1 (en) | 2010-12-16 | 2011-12-16 | Inhibitors of influenza viruses replication |
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=) |
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| 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 |
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| 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
Also Published As
| Publication number | Publication date |
|---|---|
| JP2013545817A (ja) | 2013-12-26 |
| WO2012083121A1 (en) | 2012-06-21 |
| MX2013006846A (es) | 2013-12-16 |
| US20140005197A1 (en) | 2014-01-02 |
| RU2013132717A (ru) | 2015-01-27 |
| EP2651941A1 (en) | 2013-10-23 |
| AU2011343646A1 (en) | 2013-05-02 |
| KR20130128436A (ko) | 2013-11-26 |
| CN103492382A (zh) | 2014-01-01 |
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| FZDE | Discontinued |
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