JP2018150302A5 - - Google Patents
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- Publication number
- JP2018150302A5 JP2018150302A5 JP2018072831A JP2018072831A JP2018150302A5 JP 2018150302 A5 JP2018150302 A5 JP 2018150302A5 JP 2018072831 A JP2018072831 A JP 2018072831A JP 2018072831 A JP2018072831 A JP 2018072831A JP 2018150302 A5 JP2018150302 A5 JP 2018150302A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- optionally substituted
- ring
- compound
- aryl
- 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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- 125000000217 alkyl group Chemical group 0.000 claims 65
- 125000000623 heterocyclic group Chemical group 0.000 claims 34
- 150000001875 compounds Chemical class 0.000 claims 26
- 150000003839 salts Chemical class 0.000 claims 25
- 125000004452 carbocyclyl group Chemical group 0.000 claims 19
- 125000003118 aryl group Chemical group 0.000 claims 17
- 125000001072 heteroaryl group Chemical group 0.000 claims 16
- 229910052739 hydrogen Inorganic materials 0.000 claims 14
- 239000001257 hydrogen Substances 0.000 claims 14
- 125000000304 alkynyl group Chemical group 0.000 claims 13
- 102000001267 GSK3 Human genes 0.000 claims 11
- 108060006662 GSK3 Proteins 0.000 claims 11
- 125000004093 cyano group Chemical group *C#N 0.000 claims 11
- 150000002431 hydrogen Chemical class 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
- 125000001931 aliphatic group Chemical group 0.000 claims 9
- 125000003342 alkenyl group Chemical group 0.000 claims 9
- 125000004429 atom Chemical group 0.000 claims 9
- 125000006708 (C5-C14) heteroaryl group Chemical group 0.000 claims 8
- 125000002837 carbocyclic group Chemical group 0.000 claims 7
- 125000005843 halogen group Chemical group 0.000 claims 6
- 125000005842 heteroatom Chemical group 0.000 claims 6
- 238000000034 method Methods 0.000 claims 6
- 125000004432 carbon atom Chemical group C* 0.000 claims 5
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 5
- 208000035475 disorder Diseases 0.000 claims 5
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 4
- -1 C 1-6 perhaloalkyl Chemical group 0.000 claims 4
- 125000006374 C2-C10 alkenyl group Chemical group 0.000 claims 4
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 4
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 4
- 229910052799 carbon Inorganic materials 0.000 claims 4
- 239000003814 drug Substances 0.000 claims 4
- 238000004519 manufacturing process Methods 0.000 claims 4
- 230000001404 mediated effect Effects 0.000 claims 4
- 125000003107 substituted aryl group Chemical group 0.000 claims 4
- 125000006714 (C3-C10) heterocyclyl group Chemical group 0.000 claims 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 3
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 3
- 229910052736 halogen Inorganic materials 0.000 claims 3
- 150000002367 halogens Chemical class 0.000 claims 3
- 230000002401 inhibitory effect Effects 0.000 claims 3
- 229910052757 nitrogen Inorganic materials 0.000 claims 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 3
- 229920006395 saturated elastomer Polymers 0.000 claims 3
- 229910052717 sulfur Inorganic materials 0.000 claims 3
- 239000011593 sulfur Substances 0.000 claims 3
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims 2
- 102100034184 Macrophage scavenger receptor types I and II Human genes 0.000 claims 2
- 101710134306 Macrophage scavenger receptor types I and II Proteins 0.000 claims 2
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims 2
- 125000003710 aryl alkyl group Chemical group 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 2
- 125000001424 substituent 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
- 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
- 208000012902 Nervous system disease Diseases 0.000 claims 1
- 208000025966 Neurological disease 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
- 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
- 125000001153 fluoro group Chemical group F* 0.000 claims 1
- 125000004435 hydrogen atom Chemical group [H]* 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
- 125000001971 neopentyl group Chemical group [H]C([*])([H])C(C([H])([H])[H])(C([H])([H])[H])C([H])([H])[H] 0.000 claims 1
- 230000004770 neurodegeneration Effects 0.000 claims 1
- 208000015122 neurodegenerative disease Diseases 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 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
- 208000020016 psychiatric disease Diseases 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 (4)
| 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 |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015536972A Division JP6321662B2 (ja) | 2012-10-12 | 2013-10-11 | Ｇｓｋ３阻害剤およびその使用の方法 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018150302A JP2018150302A (ja) | 2018-09-27 |
| JP2018150302A5 true JP2018150302A5 (cg-RX-API-DMAC7.html) | 2019-01-10 |
| JP6606691B2 JP6606691B2 (ja) | 2019-11-20 |
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 Before (1)
| 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 |
Country Status (16)
| Country | Link |
|---|---|
| US (4) | US9096594B2 (cg-RX-API-DMAC7.html) |
| EP (1) | EP2909204B1 (cg-RX-API-DMAC7.html) |
| JP (2) | JP6321662B2 (cg-RX-API-DMAC7.html) |
| CA (1) | CA2887701C (cg-RX-API-DMAC7.html) |
| CY (1) | CY1122601T1 (cg-RX-API-DMAC7.html) |
| DK (1) | DK2909204T3 (cg-RX-API-DMAC7.html) |
| ES (1) | ES2719776T3 (cg-RX-API-DMAC7.html) |
| HR (1) | HRP20190406T1 (cg-RX-API-DMAC7.html) |
| HU (1) | HUE043853T2 (cg-RX-API-DMAC7.html) |
| LT (1) | LT2909204T (cg-RX-API-DMAC7.html) |
| PL (1) | PL2909204T3 (cg-RX-API-DMAC7.html) |
| PT (1) | PT2909204T (cg-RX-API-DMAC7.html) |
| RS (1) | RS58700B1 (cg-RX-API-DMAC7.html) |
| SI (1) | SI2909204T1 (cg-RX-API-DMAC7.html) |
| SM (1) | SMT201900136T1 (cg-RX-API-DMAC7.html) |
| WO (1) | WO2014059383A1 (cg-RX-API-DMAC7.html) |
Families Citing this family (28)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2887701C (en) | 2012-10-12 | 2020-12-15 | The Broad Institute, Inc. | Gsk3 inhibitors and methods of use thereof |
| BR112015023261A2 (pt) | 2013-03-14 | 2017-07-18 | Massachusetts Inst Technology | composições e métodos para expansão e cultura de células-tronco epiteliais |
| EP3166637B1 (en) | 2014-07-10 | 2020-01-29 | The J. David Gladstone Institutes | Compositions and methods for treating dengue virus infection |
| JP6773645B2 (ja) | 2014-09-03 | 2020-10-21 | ザ ブリガム アンド ウィミンズ ホスピタル，インコーポレイテッド | 聴覚障害の治療のための内耳毛細胞を生成するための組成物、システムおよび方法 |
| WO2016061344A1 (en) * | 2014-10-15 | 2016-04-21 | Mirx Pharmaceuticals Llc | Gsk3 inhibitors and their uses |
| WO2017120543A1 (en) | 2016-01-08 | 2017-07-13 | Massachusetts Institute Of Technology | 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 |
| AU2017386417B2 (en) | 2016-12-30 | 2022-07-14 | Frequency Therapeutics, Inc. | 1H-pyrrole-2,5-dione compounds and methods of using them to induce self-renewal of stem/progenitor supporting cells |
| EP3606528B1 (en) | 2017-04-05 | 2023-10-18 | The Broad Institute, Inc. | Tricyclic compounds as glycogen synthase kinase 3 (gsk3) inhibitors and uses thereof |
| US11331313B2 (en) | 2017-05-22 | 2022-05-17 | 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 |
| BR112020024931A2 (pt) | 2018-06-05 | 2021-03-09 | Actuate Therapeutics, Inc. | Uso de um inibidor de gsk-3ss |
| US20210299233A1 (en) * | 2018-07-12 | 2021-09-30 | The Children's Medical Center Corporation | Method for treating cancer |
| JP2021533788A (ja) | 2018-08-17 | 2021-12-09 | フリークエンシー セラピューティクス インコーポレイテッド | Ｊａｇ−１を上方制御することにより有毛細胞を生成するための組成物及び方法 |
| US11617745B2 (en) | 2018-08-17 | 2023-04-04 | Frequency Therapeutics, Inc. | Compositions and methods for generating hair cells by downregulating FOXO |
| WO2020163812A1 (en) | 2019-02-08 | 2020-08-13 | Frequency Therapeutics, Inc. | Valproic acid compounds and wnt agonists for treating ear disorders |
| US20230014430A1 (en) * | 2019-11-20 | 2023-01-19 | 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 |
| WO2024081939A2 (en) * | 2022-10-13 | 2024-04-18 | 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 |
| WO2025080946A2 (en) | 2023-10-12 | 2025-04-17 | 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 |
| WO2025255438A1 (en) | 2024-06-07 | 2025-12-11 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
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-
2013
- 2013-10-11 CA CA2887701A patent/CA2887701C/en active Active
- 2013-10-11 WO PCT/US2013/064716 patent/WO2014059383A1/en not_active Ceased
- 2013-10-11 PT PT13780300T patent/PT2909204T/pt unknown
- 2013-10-11 JP JP2015536972A patent/JP6321662B2/ja active Active
- 2013-10-11 SM SM20190136T patent/SMT201900136T1/it unknown
- 2013-10-11 HU HUE13780300A patent/HUE043853T2/hu unknown
- 2013-10-11 US US14/052,661 patent/US9096594B2/en active Active
- 2013-10-11 PL PL13780300T patent/PL2909204T3/pl unknown
- 2013-10-11 ES ES13780300T patent/ES2719776T3/es active Active
- 2013-10-11 RS RS20190292A patent/RS58700B1/sr unknown
- 2013-10-11 LT LTEP13780300.3T patent/LT2909204T/lt unknown
- 2013-10-11 EP EP13780300.3A patent/EP2909204B1/en active Active
- 2013-10-11 SI SI201331368T patent/SI2909204T1/sl unknown
- 2013-10-11 HR HRP20190406TT patent/HRP20190406T1/hr unknown
- 2013-10-11 DK DK13780300.3T patent/DK2909204T3/en active
-
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