JPWO2020117635A5 - - Google Patents
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- Publication number
- JPWO2020117635A5 JPWO2020117635A5 JP2021531523A JP2021531523A JPWO2020117635A5 JP WO2020117635 A5 JPWO2020117635 A5 JP WO2020117635A5 JP 2021531523 A JP2021531523 A JP 2021531523A JP 2021531523 A JP2021531523 A JP 2021531523A JP WO2020117635 A5 JPWO2020117635 A5 JP WO2020117635A5
- Authority
- JP
- Japan
- Prior art keywords
- optionally substituted
- alkyl
- solvate
- pharmaceutically acceptable
- 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 description 93
- 150000003839 salts Chemical class 0.000 claims description 91
- 239000012453 solvate Substances 0.000 claims description 91
- 125000000217 alkyl group Chemical group 0.000 claims description 70
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 45
- 229910052739 hydrogen Inorganic materials 0.000 claims description 32
- 239000001257 hydrogen Substances 0.000 claims description 32
- 229910052736 halogen Inorganic materials 0.000 claims description 28
- 150000002367 halogens Chemical class 0.000 claims description 28
- 229910052801 chlorine Inorganic materials 0.000 claims description 25
- 239000000460 chlorine Substances 0.000 claims description 25
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims description 24
- 125000004404 heteroalkyl group Chemical group 0.000 claims description 23
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims description 22
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 22
- 229910052731 fluorine Inorganic materials 0.000 claims description 22
- 239000011737 fluorine Substances 0.000 claims description 22
- 125000003107 substituted aryl group Chemical group 0.000 claims description 20
- 125000001072 heteroaryl group Chemical group 0.000 claims description 18
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 16
- 150000002431 hydrogen Chemical class 0.000 claims description 10
- -1 substituted Chemical class 0.000 claims description 9
- 239000008194 pharmaceutical composition Substances 0.000 claims description 8
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 7
- 102100030013 Endoribonuclease Human genes 0.000 claims description 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 5
- 101001010783 Homo sapiens Endoribonuclease Proteins 0.000 claims description 4
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims description 4
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims description 4
- 201000010099 disease Diseases 0.000 claims description 3
- 230000000694 effects Effects 0.000 claims description 2
- 125000000623 heterocyclic group Chemical group 0.000 claims description 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 2
- NKFLEFWUYAUDJV-UHFFFAOYSA-N pyridine-3-sulfonamide Chemical compound NS(=O)(=O)C1=CC=CN=C1 NKFLEFWUYAUDJV-UHFFFAOYSA-N 0.000 claims description 2
- 230000011664 signaling Effects 0.000 claims description 2
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 10
- 125000006747 (C2-C10) heterocycloalkyl group Chemical group 0.000 claims 6
- 241000255925 Diptera Species 0.000 claims 1
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical compound C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 claims 1
- 150000008331 benzenesulfonamides Chemical class 0.000 claims 1
- 125000001309 chloro group Chemical group Cl* 0.000 claims 1
- 125000003709 fluoroalkyl group Chemical group 0.000 description 24
- 125000000753 cycloalkyl group Chemical group 0.000 description 17
- 206010028980 Neoplasm Diseases 0.000 description 10
- 201000011510 cancer Diseases 0.000 description 10
- 125000000592 heterocycloalkyl group Chemical group 0.000 description 10
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 description 4
- 125000001424 substituent group Chemical group 0.000 description 3
- 206010006187 Breast cancer Diseases 0.000 description 2
- 208000026310 Breast neoplasm Diseases 0.000 description 2
- 101710199605 Endoribonuclease Proteins 0.000 description 2
- 208000003721 Triple Negative Breast Neoplasms Diseases 0.000 description 2
- 230000002062 proliferating effect Effects 0.000 description 2
- 102000004169 proteins and genes Human genes 0.000 description 2
- 108090000623 proteins and genes Proteins 0.000 description 2
- 239000007787 solid Substances 0.000 description 2
- 208000022679 triple-negative breast carcinoma Diseases 0.000 description 2
- KHBQMWCZKVMBLN-UHFFFAOYSA-N Benzenesulfonamide Chemical compound NS(=O)(=O)C1=CC=CC=C1 KHBQMWCZKVMBLN-UHFFFAOYSA-N 0.000 description 1
- 206010005003 Bladder cancer Diseases 0.000 description 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 description 1
- 206010025323 Lymphomas Diseases 0.000 description 1
- 208000034578 Multiple myelomas Diseases 0.000 description 1
- 206010033128 Ovarian cancer Diseases 0.000 description 1
- 206010061535 Ovarian neoplasm Diseases 0.000 description 1
- 108091000080 Phosphotransferase Proteins 0.000 description 1
- 206010035226 Plasma cell myeloma Diseases 0.000 description 1
- 108010083644 Ribonucleases Proteins 0.000 description 1
- 102000006382 Ribonucleases Human genes 0.000 description 1
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 description 1
- 125000003545 alkoxy group Chemical group 0.000 description 1
- 230000004075 alteration Effects 0.000 description 1
- 125000000539 amino acid group Chemical group 0.000 description 1
- 125000004428 fluoroalkoxy group Chemical group 0.000 description 1
- 201000005787 hematologic cancer Diseases 0.000 description 1
- 230000002489 hematologic effect Effects 0.000 description 1
- 208000032839 leukemia Diseases 0.000 description 1
- 201000005202 lung cancer Diseases 0.000 description 1
- 208000020816 lung neoplasm Diseases 0.000 description 1
- 102000020233 phosphotransferase Human genes 0.000 description 1
- 201000005112 urinary bladder cancer Diseases 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862774794P | 2018-12-03 | 2018-12-03 | |
| US62/774,794 | 2018-12-03 | ||
| PCT/US2019/063921 WO2020117635A1 (en) | 2018-12-03 | 2019-12-02 | Ire1 small molecule inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2022511477A JP2022511477A (ja) | 2022-01-31 |
| JPWO2020117635A5 true JPWO2020117635A5 (enExample) | 2022-12-02 |
| JP7546299B2 JP7546299B2 (ja) | 2024-09-06 |
Family
ID=69024615
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021531523A Active JP7546299B2 (ja) | 2018-12-03 | 2019-12-02 | Ｉｒｅ１小分子阻害物質 |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US12071426B2 (enExample) |
| EP (1) | EP3891137B1 (enExample) |
| JP (1) | JP7546299B2 (enExample) |
| AU (1) | AU2019393754A1 (enExample) |
| CA (1) | CA3121755A1 (enExample) |
| IL (1) | IL283433A (enExample) |
| SG (1) | SG11202105690TA (enExample) |
| WO (1) | WO2020117635A1 (enExample) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| SG11202105690TA (en) | 2018-12-03 | 2021-06-29 | Univ Cornell | 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 |
| TWI756636B (zh) * | 2019-02-18 | 2022-03-01 | 美商建南德克公司 | 嘧啶并嘧啶化合物及使用方法 |
| 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 |
| WO2022104148A1 (en) * | 2020-11-13 | 2022-05-19 | The Regents Of The University Of California | Ire1alpha inhibitors and uses thereof |
| EP4247795A1 (en) | 2020-11-18 | 2023-09-27 | Deciphera Pharmaceuticals, LLC | Gcn2 and perk kinase inhibitors and methods of use thereof |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8664230B2 (en) * | 2011-03-17 | 2014-03-04 | The Asan Foundation | Pyridopyrimidine derivatives and use thereof |
| US10934275B2 (en) * | 2016-12-02 | 2021-03-02 | Cornell University | IRE1 small molecule inhibitors |
| CN108239074B (zh) * | 2016-12-26 | 2021-07-06 | 中国医学科学院药物研究所 | 喹唑啉类化合物及其制备方法、用途和药物组合物 |
| 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 |
| AU2018278311B2 (en) * | 2017-06-01 | 2021-10-07 | Cornell University | IRE1 small molecule inhibitors |
| JP7271538B2 (ja) * | 2017-11-10 | 2023-05-11 | コーネル・ユニバーシティー | 低分子ｉｒｅ１阻害剤 |
| SG11202105690TA (en) | 2018-12-03 | 2021-06-29 | Univ Cornell | Ire1 small molecule inhibitors |
-
2019
- 2019-12-02 SG SG11202105690TA patent/SG11202105690TA/en unknown
- 2019-12-02 WO PCT/US2019/063921 patent/WO2020117635A1/en not_active Ceased
- 2019-12-02 CA CA3121755A patent/CA3121755A1/en not_active Abandoned
- 2019-12-02 JP JP2021531523A patent/JP7546299B2/ja active Active
- 2019-12-02 EP EP19828388.9A patent/EP3891137B1/en active Active
- 2019-12-02 US US17/299,684 patent/US12071426B2/en active Active
- 2019-12-02 AU AU2019393754A patent/AU2019393754A1/en not_active Abandoned
-
2021
- 2021-05-25 IL IL283433A patent/IL283433A/en unknown
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