CA3064837A1 - Ire1 small molecule inhibitors - Google Patents
Ire1 small molecule inhibitors Download PDFInfo
- Publication number
- CA3064837A1 CA3064837A1 CA3064837A CA3064837A CA3064837A1 CA 3064837 A1 CA3064837 A1 CA 3064837A1 CA 3064837 A CA3064837 A CA 3064837A CA 3064837 A CA3064837 A CA 3064837A CA 3064837 A1 CA3064837 A1 CA 3064837A1
- Authority
- CA
- Canada
- Prior art keywords
- optionally substituted
- compound
- solvate
- pharmaceutically acceptable
- acceptable salt
- 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
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
- C07D217/22—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the nitrogen-containing ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
- C07D239/72—Quinazolines; Hydrogenated quinazolines
- C07D239/78—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 2
- C07D239/84—Nitrogen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
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 (1)
| Publication Number | Publication Date |
|---|---|
| CA3064837A1 true CA3064837A1 (en) | 2018-12-06 |
Family
ID=64455585
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA3064837A Pending CA3064837A1 (en) | 2017-06-01 | 2018-05-31 | Ire1 small molecule inhibitors |
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 |
-
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
Also Published As
| Publication number | Publication date |
|---|---|
| US20210284628A1 (en) | 2021-09-16 |
| JP7126084B2 (ja) | 2022-08-26 |
| EP3630748A4 (en) | 2021-01-27 |
| US20180346446A1 (en) | 2018-12-06 |
| US11649224B2 (en) | 2023-05-16 |
| US11021466B2 (en) | 2021-06-01 |
| EP3630748A1 (en) | 2020-04-08 |
| WO2018222918A1 (en) | 2018-12-06 |
| AU2018278311B2 (en) | 2021-10-07 |
| EP3630748B1 (en) | 2023-04-19 |
| JP2020522520A (ja) | 2020-07-30 |
| AU2018278311A1 (en) | 2019-12-12 |
| US20200157079A1 (en) | 2020-05-21 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| EEER | Examination request |
Effective date: 20220926 |
|
| EEER | Examination request |
Effective date: 20220926 |
|
| EEER | Examination request |
Effective date: 20220926 |
|
| EEER | Examination request |
Effective date: 20220926 |
|
| EEER | Examination request |
Effective date: 20220926 |
|
| EEER | Examination request |
Effective date: 20220926 |