JP2015536307A5 - - Google Patents
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- Publication number
- JP2015536307A5 JP2015536307A5 JP2015536972A JP2015536972A JP2015536307A5 JP 2015536307 A5 JP2015536307 A5 JP 2015536307A5 JP 2015536972 A JP2015536972 A JP 2015536972A JP 2015536972 A JP2015536972 A JP 2015536972A JP 2015536307 A5 JP2015536307 A5 JP 2015536307A5
- Authority
- JP
- Japan
- Prior art keywords
- optionally substituted
- compound
- acceptable salt
- salt
- gsk3
- 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 29
- 150000003839 salts Chemical class 0.000 claims 25
- 125000000623 heterocyclic group Chemical group 0.000 claims 17
- 125000001931 aliphatic group Chemical group 0.000 claims 13
- 239000000203 mixture Substances 0.000 claims 12
- 102000001267 GSK3 Human genes 0.000 claims 11
- 108060006662 GSK3 Proteins 0.000 claims 11
- 125000004429 atom Chemical group 0.000 claims 11
- NFVJNJQRWPQVOA-UHFFFAOYSA-N n-[2-chloro-5-(trifluoromethyl)phenyl]-2-[3-(4-ethyl-5-ethylsulfanyl-1,2,4-triazol-3-yl)piperidin-1-yl]acetamide Chemical compound CCN1C(SCC)=NN=C1C1CN(CC(=O)NC=2C(=CC=C(C=2)C(F)(F)F)Cl)CCC1 NFVJNJQRWPQVOA-UHFFFAOYSA-N 0.000 claims 11
- 125000002837 carbocyclic group Chemical group 0.000 claims 9
- 125000001072 heteroaryl group Chemical group 0.000 claims 9
- 229910052739 hydrogen Inorganic materials 0.000 claims 9
- 239000001257 hydrogen Substances 0.000 claims 9
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 8
- 125000004093 cyano group Chemical group *C#N 0.000 claims 6
- 125000005843 halogen group Chemical group 0.000 claims 6
- 230000001404 mediated effect Effects 0.000 claims 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 5
- 208000035475 disorder Diseases 0.000 claims 5
- 238000000034 method Methods 0.000 claims 5
- 125000003107 substituted aryl group Chemical group 0.000 claims 5
- 239000003814 drug Substances 0.000 claims 4
- 238000004519 manufacturing process Methods 0.000 claims 4
- 102100034356 Casein kinase I isoform alpha-like Human genes 0.000 claims 3
- 125000004452 carbocyclyl group Chemical group 0.000 claims 3
- 230000002401 inhibitory effect Effects 0.000 claims 3
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 3
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims 2
- 125000003118 aryl group Chemical group 0.000 claims 2
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 1
- 208000024893 Acute lymphoblastic leukemia Diseases 0.000 claims 1
- 208000014697 Acute lymphocytic leukaemia Diseases 0.000 claims 1
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 1
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 206010003805 Autism Diseases 0.000 claims 1
- 208000020706 Autistic disease Diseases 0.000 claims 1
- 208000010839 B-cell chronic lymphocytic leukemia Diseases 0.000 claims 1
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims 1
- 208000020925 Bipolar disease Diseases 0.000 claims 1
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims 1
- 208000001914 Fragile X syndrome Diseases 0.000 claims 1
- 201000011240 Frontotemporal dementia Diseases 0.000 claims 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 1
- WHXSMMKQMYFTQS-UHFFFAOYSA-N Lithium Chemical compound [Li] WHXSMMKQMYFTQS-UHFFFAOYSA-N 0.000 claims 1
- 208000031422 Lymphocytic Chronic B-Cell Leukemia Diseases 0.000 claims 1
- 208000034578 Multiple myelomas Diseases 0.000 claims 1
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims 1
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 1
- 208000006664 Precursor Cell Lymphoblastic Leukemia-Lymphoma Diseases 0.000 claims 1
- 239000000654 additive Substances 0.000 claims 1
- 230000000996 additive effect Effects 0.000 claims 1
- 210000004227 basal ganglia Anatomy 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 208000032852 chronic lymphocytic leukemia Diseases 0.000 claims 1
- 230000001054 cortical effect Effects 0.000 claims 1
- 125000004122 cyclic group Chemical group 0.000 claims 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
- 230000007850 degeneration Effects 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- -1 difluorocyclobutyl Chemical group 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 125000001153 fluoro group Chemical group F* 0.000 claims 1
- 238000000338 in vitro Methods 0.000 claims 1
- 125000000959 isobutyl group Chemical group [H]C([H])([H])C([H])(C([H])([H])[H])C([H])([H])* 0.000 claims 1
- 208000032839 leukemia Diseases 0.000 claims 1
- 229910052744 lithium Inorganic materials 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 208000030159 metabolic disease Diseases 0.000 claims 1
- 230000000626 neurodegenerative effect Effects 0.000 claims 1
- 230000000926 neurological effect Effects 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 201000002212 progressive supranuclear palsy Diseases 0.000 claims 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 208000020016 psychiatric disease Diseases 0.000 claims 1
- 229920006395 saturated elastomer Polymers 0.000 claims 1
- 201000000980 schizophrenia Diseases 0.000 claims 1
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261713314P | 2012-10-12 | 2012-10-12 | |
| US61/713,314 | 2012-10-12 | ||
| US201361779394P | 2013-03-13 | 2013-03-13 | |
| US61/779,394 | 2013-03-13 | ||
| PCT/US2013/064716 WO2014059383A1 (en) | 2012-10-12 | 2013-10-11 | Gsk3 inhibitors and methods of use thereof |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018072831A Division JP6606691B2 (ja) | 2012-10-12 | 2018-04-05 | Ｇｓｋ３阻害剤およびその使用の方法 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2015536307A JP2015536307A (ja) | 2015-12-21 |
| JP2015536307A5 true JP2015536307A5 (enExample) | 2016-12-22 |
| JP6321662B2 JP6321662B2 (ja) | 2018-05-09 |
Family
ID=49474737
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015536972A Active JP6321662B2 (ja) | 2012-10-12 | 2013-10-11 | Ｇｓｋ３阻害剤およびその使用の方法 |
| JP2018072831A Active JP6606691B2 (ja) | 2012-10-12 | 2018-04-05 | Ｇｓｋ３阻害剤およびその使用の方法 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018072831A Active JP6606691B2 (ja) | 2012-10-12 | 2018-04-05 | Ｇｓｋ３阻害剤およびその使用の方法 |
Country Status (16)
| Country | Link |
|---|---|
| US (4) | US9096594B2 (enExample) |
| EP (1) | EP2909204B1 (enExample) |
| JP (2) | JP6321662B2 (enExample) |
| CA (1) | CA2887701C (enExample) |
| CY (1) | CY1122601T1 (enExample) |
| DK (1) | DK2909204T3 (enExample) |
| ES (1) | ES2719776T3 (enExample) |
| HR (1) | HRP20190406T1 (enExample) |
| HU (1) | HUE043853T2 (enExample) |
| LT (1) | LT2909204T (enExample) |
| PL (1) | PL2909204T3 (enExample) |
| PT (1) | PT2909204T (enExample) |
| RS (1) | RS58700B1 (enExample) |
| SI (1) | SI2909204T1 (enExample) |
| SM (1) | SMT201900136T1 (enExample) |
| WO (1) | WO2014059383A1 (enExample) |
Families Citing this family (30)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PL2909204T3 (pl) | 2012-10-12 | 2019-07-31 | The Broad Institute, Inc. | Inhibitory GSK3 i sposoby ich stosowania |
| PT3702443T (pt) | 2013-03-14 | 2022-02-17 | Massachusetts Inst Technology | Composições e métodos para expansão e cultura de células estaminais epiteliais |
| WO2016007540A2 (en) | 2014-07-10 | 2016-01-14 | The J. David Gladstone Institutes | Compositions and methods for treating dengue virus infection |
| EP3189134A1 (en) | 2014-09-03 | 2017-07-12 | The Brigham and Women's Hospital, Inc. | Compositions, systems, and methods for generating inner ear hair cells for treatment of hearing loss |
| WO2016061344A1 (en) * | 2014-10-15 | 2016-04-21 | Mirx Pharmaceuticals Llc | Gsk3 inhibitors and their uses |
| US11021687B2 (en) | 2016-01-08 | 2021-06-01 | The Brigham And Women's Hospital, Inc. | Production of differentiated enteroendocrine cells and insulin producing cells |
| US10213511B2 (en) | 2016-03-02 | 2019-02-26 | Frequency Therapeutics, Inc. | Thermoreversible compositions for administration of therapeutic agents |
| US11260130B2 (en) | 2016-03-02 | 2022-03-01 | Frequency Therapeutics, Inc. | Solubilized compositions for controlled proliferation of stem cells / generating inner ear hair cells using a GSK3 inhibitor: IV |
| US10201540B2 (en) | 2016-03-02 | 2019-02-12 | Frequency Therapeutics, Inc. | Solubilized compositions for controlled proliferation of stem cells / generating inner ear hair cells using GSK3 inhibitors: I |
| SG10201910821XA (en) | 2016-12-30 | 2020-01-30 | Frequency Therapeutics Inc | 1h-pyrrole-2,5-dione compounds and methods of using them to induce self-renewal of stem/progenitor supporting cells |
| CN110958882B (zh) * | 2017-04-05 | 2023-08-29 | 布罗德研究所股份有限公司 | 作为糖原合酶激酶3(gsk3)抑制剂的三环化合物及其用途 |
| WO2018217766A1 (en) | 2017-05-22 | 2018-11-29 | Whitehead Institute For Biomedical Research | Kcc2 expression enhancing compounds and uses thereof |
| CN110407769B (zh) * | 2018-04-27 | 2022-11-08 | 复旦大学 | 3,4-二氢-苯并[f][1,4]硫氮杂䓬-5(2H)-酮类化合物及其药物用途 |
| KR20210045364A (ko) | 2018-06-05 | 2021-04-26 | 액투에이트 테라퓨틱스 인크. | 악성 림프증식성 장애를 치료하는 방법 |
| US20210299233A1 (en) * | 2018-07-12 | 2021-09-30 | The Children's Medical Center Corporation | Method for treating cancer |
| EP3837351A1 (en) | 2018-08-17 | 2021-06-23 | Frequency Therapeutics, Inc. | Compositions and methods for generating hair cells by downregulating foxo |
| US11162071B2 (en) | 2018-08-17 | 2021-11-02 | Frequency Therapeutics, Inc. | Compositions and methods for generating hair cells by upregulating JAG-1 |
| EP3920885A1 (en) | 2019-02-08 | 2021-12-15 | Frequency Therapeutics, Inc. | Valproic acid compounds and wnt agonists for treating ear disorders |
| WO2021102305A1 (en) * | 2019-11-20 | 2021-05-27 | Washington University | Methods and compositions for generating functionally mature beta cells and uses thereof |
| WO2023056463A1 (en) * | 2021-09-30 | 2023-04-06 | Trustees Of Tufts College | Glycogen synthase kinase 3 (gsk3) inhibitors for treating ctnnb1 syndrome |
| EP4601637A2 (en) * | 2022-10-13 | 2025-08-20 | The Broad Institute Inc. | Glycogen synthase kinase 3 inhibitors and uses thereof |
| AU2024265078A1 (en) | 2023-05-04 | 2025-12-11 | Revolution Medicines, Inc. | Combination therapy for a ras related disease or disorder |
| WO2024259178A1 (en) | 2023-06-14 | 2024-12-19 | The Broad Institute, Inc. | Glycogen synthase kinase 3 inhibitors and uses thereof |
| US20250049810A1 (en) | 2023-08-07 | 2025-02-13 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| US20250154171A1 (en) | 2023-10-12 | 2025-05-15 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025171296A1 (en) | 2024-02-09 | 2025-08-14 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025240847A1 (en) | 2024-05-17 | 2025-11-20 | Revolution Medicines, Inc. | Ras inhibitors |
| US20250375445A1 (en) | 2024-06-07 | 2025-12-11 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| WO2025265060A1 (en) | 2024-06-21 | 2025-12-26 | Revolution Medicines, Inc. | Therapeutic compositions and methods for managing treatment-related effects |
| WO2026006747A1 (en) | 2024-06-28 | 2026-01-02 | Revolution Medicines, Inc. | Ras inhibitors |
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| DE2722416A1 (de) | 1977-05-18 | 1978-11-30 | Thomae Gmbh Dr K | Neue thiazolo-pyridine |
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2013
- 2013-10-11 PL PL13780300T patent/PL2909204T3/pl unknown
- 2013-10-11 HR HRP20190406TT patent/HRP20190406T1/hr unknown
- 2013-10-11 HU HUE13780300A patent/HUE043853T2/hu unknown
- 2013-10-11 SM SM20190136T patent/SMT201900136T1/it unknown
- 2013-10-11 LT LTEP13780300.3T patent/LT2909204T/lt unknown
- 2013-10-11 ES ES13780300T patent/ES2719776T3/es active Active
- 2013-10-11 WO PCT/US2013/064716 patent/WO2014059383A1/en not_active Ceased
- 2013-10-11 EP EP13780300.3A patent/EP2909204B1/en active Active
- 2013-10-11 PT PT13780300T patent/PT2909204T/pt unknown
- 2013-10-11 SI SI201331368T patent/SI2909204T1/sl unknown
- 2013-10-11 RS RS20190292A patent/RS58700B1/sr unknown
- 2013-10-11 US US14/052,661 patent/US9096594B2/en active Active
- 2013-10-11 JP JP2015536972A patent/JP6321662B2/ja active Active
- 2013-10-11 DK DK13780300.3T patent/DK2909204T3/en active
- 2013-10-11 CA CA2887701A patent/CA2887701C/en active Active
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2015
- 2015-07-14 US US14/799,281 patent/US10137122B2/en active Active
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2018
- 2018-04-05 JP JP2018072831A patent/JP6606691B2/ja active Active
- 2018-11-21 US US16/198,589 patent/US11052080B2/en active Active
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2019
- 2019-03-05 CY CY20191100268T patent/CY1122601T1/el unknown
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2021
- 2021-06-10 US US17/344,830 patent/US12419885B2/en active Active