JP2020522520A5 - - Google Patents
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- Publication number
- JP2020522520A5 JP2020522520A5 JP2019566754A JP2019566754A JP2020522520A5 JP 2020522520 A5 JP2020522520 A5 JP 2020522520A5 JP 2019566754 A JP2019566754 A JP 2019566754A JP 2019566754 A JP2019566754 A JP 2019566754A JP 2020522520 A5 JP2020522520 A5 JP 2020522520A5
- Authority
- JP
- Japan
- Prior art keywords
- optionally substituted
- amino
- aminocyclohexyl
- solvate
- compound
- 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
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- 150000001875 compounds Chemical class 0.000 claims 31
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 22
- 150000003839 salts Chemical class 0.000 claims 19
- 239000012453 solvate Substances 0.000 claims 19
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 10
- 125000001072 heteroaryl group Chemical group 0.000 claims 10
- 125000006747 (C2-C10) heterocycloalkyl group Chemical group 0.000 claims 9
- 125000003107 substituted aryl group Chemical group 0.000 claims 9
- 102100030013 Endoribonuclease Human genes 0.000 claims 6
- 239000008194 pharmaceutical composition Substances 0.000 claims 5
- 101710199605 Endoribonuclease Proteins 0.000 claims 4
- 229910052736 halogen Inorganic materials 0.000 claims 4
- 150000002367 halogens Chemical class 0.000 claims 4
- -1 quinazoline-6-yl Chemical group 0.000 claims 4
- 125000003118 aryl group Chemical group 0.000 claims 3
- 101001010783 Homo sapiens Endoribonuclease Proteins 0.000 claims 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 125000000623 heterocyclic group Chemical group 0.000 claims 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 2
- KHBQMWCZKVMBLN-UHFFFAOYSA-N Benzenesulfonamide Chemical compound NS(=O)(=O)C1=CC=CC=C1 KHBQMWCZKVMBLN-UHFFFAOYSA-N 0.000 claims 1
- 108091000080 Phosphotransferase Proteins 0.000 claims 1
- 108010083644 Ribonucleases Proteins 0.000 claims 1
- 102000006382 Ribonucleases Human genes 0.000 claims 1
- 125000000539 amino acid group Chemical group 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 125000001620 monocyclic carbocycle group Chemical group 0.000 claims 1
- 125000002911 monocyclic heterocycle group Chemical group 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 102000020233 phosphotransferase Human genes 0.000 claims 1
- 230000002062 proliferating effect Effects 0.000 claims 1
- 102000004169 proteins and genes Human genes 0.000 claims 1
- 108090000623 proteins and genes Proteins 0.000 claims 1
- 230000011664 signaling Effects 0.000 claims 1
- 0 CC(NC1CCCCCCCCCCCC1)=NC=C(C(C)=C(C(*)=C1*)C2=CC=CC(N)=CC(NS(C3=C(*)C=C*(*)C=C3)(=O)=O)=CC=CC=C2)C1=* Chemical compound CC(NC1CCCCCCCCCCCC1)=NC=C(C(C)=C(C(*)=C1*)C2=CC=CC(N)=CC(NS(C3=C(*)C=C*(*)C=C3)(=O)=O)=CC=CC=C2)C1=* 0.000 description 2
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762513929P | 2017-06-01 | 2017-06-01 | |
| US62/513,929 | 2017-06-01 | ||
| PCT/US2018/035465 WO2018222918A1 (en) | 2017-06-01 | 2018-05-31 | Ire1 small molecule inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2020522520A JP2020522520A (ja) | 2020-07-30 |
| JP2020522520A5 true JP2020522520A5 (enExample) | 2021-02-12 |
| JP7126084B2 JP7126084B2 (ja) | 2022-08-26 |
Family
ID=64455585
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019566754A Active JP7126084B2 (ja) | 2017-06-01 | 2018-05-31 | Ｉｒｅ１小分子阻害薬 |
Country Status (6)
| Country | Link |
|---|---|
| US (3) | US20180346446A1 (enExample) |
| EP (1) | EP3630748B1 (enExample) |
| JP (1) | JP7126084B2 (enExample) |
| AU (1) | AU2018278311B2 (enExample) |
| CA (1) | CA3064837A1 (enExample) |
| WO (1) | WO2018222918A1 (enExample) |
Families Citing this family (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2018102751A1 (en) | 2016-12-02 | 2018-06-07 | Quentis Therapeutics, Inc. | Ire1 small molecule inhibitors |
| EP3630748B1 (en) | 2017-06-01 | 2023-04-19 | Cornell University | Ire1 small molecule inhibitors |
| CN111566089B (zh) | 2017-11-10 | 2023-11-17 | 康奈尔大学 | Ire1小分子抑制剂 |
| TWI831829B (zh) | 2018-09-12 | 2024-02-11 | 美商建南德克公司 | 苯氧基-吡啶基-嘧啶化合物及使用方法 |
| US12071426B2 (en) | 2018-12-03 | 2024-08-27 | Cornell University | IRE1 small molecule inhibitors |
| WO2020142612A1 (en) * | 2019-01-03 | 2020-07-09 | Genentech, Inc. | Pyrido-pyrimidinone and pteridinone compounds as inhibitors of endoribonuclease inositol requiring enzyme i (ire i alpha) for the treatment of cancer diseases. |
| CN113795307A (zh) * | 2019-02-18 | 2021-12-14 | 基因泰克公司 | 吡啶并嘧啶基化合物及其使用方法 |
| SG11202109194UA (en) * | 2019-02-27 | 2021-09-29 | Optikira Llc | Pyrazolopyridine compounds for ire1 inhibition |
| WO2020176761A1 (en) * | 2019-02-27 | 2020-09-03 | Optikira, LLC | Imidazolopyrazine compounds for ire1 inhibition |
| WO2020232401A1 (en) * | 2019-05-15 | 2020-11-19 | Cornell University | Combination therapies with ire1 small molecule inhibitors |
| US12479818B2 (en) | 2019-05-15 | 2025-11-25 | Cornell University | Treatment of fibrosis with IRE1 small molecule inhibitors |
| CN114302877A (zh) * | 2019-06-11 | 2022-04-08 | 基因泰克公司 | 喹唑啉基化合物及使用方法 |
| BR112022007981A2 (pt) * | 2019-11-01 | 2022-07-05 | Janssen Biotech Inc | Quinolina fluorada e derivados de quinoxalina como inibidores da di-hidro-orotato desidrogenase (dhodh) para o tratamento de câncer, doenças autoimunes e inflamatórias |
| WO2021158516A1 (en) * | 2020-02-03 | 2021-08-12 | Nimbus Iaso, Inc. | IRE1α MODULATORS AND USES THEREOF |
| BR112022016072A2 (pt) * | 2020-02-17 | 2022-10-04 | Alesta Therapeutics BV | Compostos moduladores de gcn2, sal farmaceuticamente aceitável, seus usos, e composição farmacêutica |
| EP4192462A4 (en) * | 2020-08-07 | 2024-09-04 | Optikira LLC | PYRAZOLOPYRIDINE COMPOUNDS AND METHODS OF INHIBITING IRE1 USING THEM |
| CN116710429A (zh) * | 2020-11-13 | 2023-09-05 | 加利福尼亚大学董事会 | IRE1α抑制剂及其用途 |
| JP2023549540A (ja) | 2020-11-18 | 2023-11-27 | デシフェラ・ファーマシューティカルズ，エルエルシー | Ｇｃｎ２およびｐｅｒｋキナーゼ阻害剤およびその使用方法 |
| WO2024131893A1 (en) * | 2022-12-22 | 2024-06-27 | Shanghai Yi Zhong Xing Biotechnology Co., Ltd. | IRE1α SMALL MOLECULE INHIBITORS |
Family Cites Families (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6632608B2 (en) | 1999-12-30 | 2003-10-14 | President And Fellows Of Harvard College | Methods and compositions relating to modulation of hepatocyte growth, plasma cell differentiation or T cell subset activity by modulation of XBP-1 activity |
| US20070054916A1 (en) | 2004-10-01 | 2007-03-08 | Amgen Inc. | Aryl nitrogen-containing bicyclic compounds and methods of use |
| EP1878727A4 (en) | 2005-04-28 | 2013-11-13 | Kyowa Hakko Kirin Co Ltd | 2-AMINOQUINAZOLINE DERIVATIVES |
| US8017331B2 (en) * | 2005-11-04 | 2011-09-13 | Mannkind Corporation | IRE-1α substrates |
| US20090291857A1 (en) | 2006-02-27 | 2009-11-26 | The Board Of Trustees Of The Leland Stanford Junior University | Methods to identify inhibitors of the unfolded protein response |
| US8227184B2 (en) | 2008-01-14 | 2012-07-24 | President And Fellows Of Harvard College | Methods for modulating de novo hepatic lipogenesis by modulating XBP-1 activity |
| US8980899B2 (en) | 2009-10-16 | 2015-03-17 | The Regents Of The University Of California | Methods of inhibiting Ire1 |
| SA111320200B1 (ar) | 2010-02-17 | 2014-02-16 | ديبيوفارم اس ايه | مركبات ثنائية الحلقة واستخداماتها كمثبطات c-src/jak مزدوجة |
| EP3799870A1 (en) * | 2010-04-05 | 2021-04-07 | Fosun Orinove Pharmatech, Inc. | Ire-1a inhibitors |
| WO2012109238A2 (en) | 2011-02-07 | 2012-08-16 | President And Fellows Of Harvard College | Methods for increasing immune responses using agents that directly bind to and activate ire-1 |
| US9422298B2 (en) * | 2011-03-17 | 2016-08-23 | Cmg Pharmaceutical Co., Ltd. | Pyridopyrimidine derivatives and use thereof |
| US20150018406A1 (en) | 2012-03-09 | 2015-01-15 | Cornell University | Modulation of breast cancer growth by modulation of xbp1 activity |
| MX2015003874A (es) * | 2012-09-26 | 2015-12-16 | Univ California | Modulacion de ire1. |
| WO2014176348A1 (en) | 2013-04-23 | 2014-10-30 | H. Lee Moffitt Cancer Center And Research Institute, Inc. | Inhibitors of the ire-1/xbp-1 pathway and methods of using thereof |
| WO2015048331A1 (en) | 2013-09-25 | 2015-04-02 | Cornell University | Compounds for inducing anti-tumor immunity and methods thereof |
| US9682123B2 (en) | 2013-12-20 | 2017-06-20 | The Trustees Of Columbia University In The City Of New York | Methods of treating metabolic disease |
| AU2017228405A1 (en) | 2016-03-03 | 2018-10-18 | Cornell University | Small molecule IRE1-alpha inhibitors |
| WO2018102751A1 (en) | 2016-12-02 | 2018-06-07 | Quentis Therapeutics, Inc. | Ire1 small molecule inhibitors |
| WO2018161033A1 (en) | 2017-03-02 | 2018-09-07 | Wright, Adrian | Small molecule ire1-alpha inhibitors |
| AR111281A1 (es) | 2017-03-17 | 2019-06-26 | Genentech Inc | Compuestos de pirimidinil-piridiloxi-naftil y métodos para tratar enfermedades y trastornos relacionados con ire1 |
| EP3630748B1 (en) | 2017-06-01 | 2023-04-19 | Cornell University | Ire1 small molecule inhibitors |
| CN111566089B (zh) * | 2017-11-10 | 2023-11-17 | 康奈尔大学 | Ire1小分子抑制剂 |
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2018
- 2018-05-31 EP EP18809060.9A patent/EP3630748B1/en active Active
- 2018-05-31 US US15/994,901 patent/US20180346446A1/en not_active Abandoned
- 2018-05-31 WO PCT/US2018/035465 patent/WO2018222918A1/en not_active Ceased
- 2018-05-31 CA CA3064837A patent/CA3064837A1/en active Pending
- 2018-05-31 AU AU2018278311A patent/AU2018278311B2/en not_active Ceased
- 2018-05-31 JP JP2019566754A patent/JP7126084B2/ja active Active
-
2019
- 2019-08-16 US US16/543,188 patent/US11021466B2/en active Active
-
2021
- 2021-05-06 US US17/313,688 patent/US11649224B2/en active Active