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
Links
- 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 (https=) | 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 (https=) |
| EP (1) | EP3630748B1 (https=) |
| JP (1) | JP7126084B2 (https=) |
| AU (1) | AU2018278311B2 (https=) |
| CA (1) | CA3064837A1 (https=) |
| WO (1) | WO2018222918A1 (https=) |
Families Citing this family (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3548476A4 (en) | 2016-12-02 | 2020-05-20 | Quentis Therapeutics, Inc. | SMALL MOLECULAR IRE1 INHIBITORS |
| CA3064837A1 (en) | 2017-06-01 | 2018-12-06 | Quentis Therapeutics, Inc. | Ire1 small molecule inhibitors |
| US10745379B2 (en) | 2017-11-10 | 2020-08-18 | Cornell University | IRE1 small molecule inhibitors |
| 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 |
| EP3891137B1 (en) | 2018-12-03 | 2024-10-09 | Cornell University | Ire1 small molecule inhibitors |
| JP7539892B2 (ja) * | 2019-01-03 | 2024-08-26 | ジェネンテック， インコーポレイテッド | 癌疾患の処置のためのエンドリボヌクレアーゼのイノシトール要求酵素ｉ（ｉｒｅｉアルファ）の阻害剤としてのピリド－ピリミジノン化合物及びプテリジノン化合物 |
| 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 |
| CN113795254B (zh) * | 2019-02-27 | 2024-08-09 | 奥普提卡拉公司 | 用于ire1抑制的吡唑并吡啶化合物 |
| US20220194945A1 (en) * | 2019-02-27 | 2022-06-23 | Optikira, LLC | Imidazolopyridine Compounds For IRE1 Inhibition |
| WO2020232401A1 (en) * | 2019-05-15 | 2020-11-19 | Cornell University | Combination therapies with ire1 small molecule inhibitors |
| WO2020232403A1 (en) * | 2019-05-15 | 2020-11-19 | Cornell University | Treatment of fibrosis with ire1 small molecule inhibitors |
| WO2020252165A1 (en) * | 2019-06-11 | 2020-12-17 | Genentech, Inc. | Quinazolinyl compounds and methods of use |
| JP2023500252A (ja) * | 2019-11-01 | 2023-01-05 | ヤンセン バイオテツク，インコーポレーテツド | 癌、自己免疫疾患及び炎症性疾患の治療用のジヒドロオロト酸デヒドロゲナーゼ（ｄｈｏｄｈ）阻害剤としてのフッ素化キノリン及びキノキサリン誘導体 |
| US20240262830A1 (en) * | 2020-02-03 | 2024-08-08 | Nimbus Iaso, Inc. | Ire1a 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 |
| CA3188602A1 (en) * | 2020-08-07 | 2022-02-10 | Richard Keenan | Pyrazolopyridine compounds and methods of inhibiting ire1 using same |
| US11840523B2 (en) * | 2020-11-13 | 2023-12-12 | The Regents Of The University Of California | IRE1α inhibitors and uses thereof |
| MX2023005747A (es) | 2020-11-18 | 2023-07-28 | Deciphera Pharmaceuticals Llc | Inhibidores de gcn2 y perk quinasas y metodos de uso de los mismos. |
| KR20240113496A (ko) | 2021-12-03 | 2024-07-22 | 데시페라 파마슈티칼스, 엘엘씨. | Gcn2 및 perk 키나아제 억제제로서의 헤테로고리 화합물 |
| 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 |
|---|---|---|---|---|
| JP2003518942A (ja) | 1999-12-30 | 2003-06-17 | プレジデント・アンド・フェローズ・オブ・ハーバード・カレッジ | 肝細胞成長、形質細胞分化、又はｔ細胞サブセットの活性を、ｘｂｐ−１活性の変調により変調することに関する方法及び組成物 |
| US20070054916A1 (en) * | 2004-10-01 | 2007-03-08 | Amgen Inc. | Aryl nitrogen-containing bicyclic compounds and methods of use |
| JP5079500B2 (ja) | 2005-04-28 | 2012-11-21 | 協和発酵キリン株式会社 | ２−アミノキナゾリン誘導体 |
| US8017331B2 (en) * | 2005-11-04 | 2011-09-13 | Mannkind Corporation | IRE-1α substrates |
| AU2007220039A1 (en) | 2006-02-27 | 2007-09-07 | The Board Of Trustees Of The Leland Stanford Junior University | Inhibitors of the unfolded protein response and methods for their use |
| WO2009091815A2 (en) | 2008-01-14 | 2009-07-23 | 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 |
| EP2555768B1 (en) * | 2010-04-05 | 2018-08-29 | Fosun Orinove Pharmatech, Inc. | Ire-1 inhibitors |
| US9956236B2 (en) | 2011-02-07 | 2018-05-01 | Cornell University | 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. |
| US10323013B2 (en) | 2013-04-23 | 2019-06-18 | H. Lee Moffitt Cancer Center And Research Institute, Inc. | Inhibitors of the IRE-1/XBP-1 pathway and methods of using thereof |
| DK3049521T3 (en) | 2013-09-25 | 2019-04-23 | Univ Cornell | Compounds for inducing antitumor 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 |
| CA3016161A1 (en) | 2016-03-03 | 2017-09-08 | Cornell University | Small molecule ire1-alpha inhibitors |
| EP3548476A4 (en) | 2016-12-02 | 2020-05-20 | Quentis Therapeutics, Inc. | SMALL MOLECULAR IRE1 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 |
| CA3064837A1 (en) | 2017-06-01 | 2018-12-06 | Quentis Therapeutics, Inc. | Ire1 small molecule inhibitors |
| US10745379B2 (en) * | 2017-11-10 | 2020-08-18 | Cornell University | IRE1 small molecule inhibitors |
-
2018
- 2018-05-31 CA CA3064837A patent/CA3064837A1/en active Pending
- 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 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
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