JP2020504711A5 - - Google Patents
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- JP2020504711A5 JP2020504711A5 JP2019526486A JP2019526486A JP2020504711A5 JP 2020504711 A5 JP2020504711 A5 JP 2020504711A5 JP 2019526486 A JP2019526486 A JP 2019526486A JP 2019526486 A JP2019526486 A JP 2019526486A JP 2020504711 A5 JP2020504711 A5 JP 2020504711A5
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- 150000001875 compounds Chemical class 0.000 claims description 136
- 125000000217 alkyl group Chemical group 0.000 claims description 36
- 150000003839 salts Chemical class 0.000 claims description 34
- 125000003118 aryl group Chemical group 0.000 claims description 31
- 125000000623 heterocyclic group Chemical group 0.000 claims description 27
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 24
- 208000017520 skin disease Diseases 0.000 claims description 18
- 229910052760 oxygen Inorganic materials 0.000 claims description 17
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims description 16
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 16
- 239000000203 mixture Substances 0.000 claims description 16
- -1 cyano, nitro, amino Chemical group 0.000 claims description 14
- 229910052736 halogen Inorganic materials 0.000 claims description 14
- 150000002367 halogens Chemical class 0.000 claims description 14
- 125000001072 heteroaryl group Chemical group 0.000 claims description 13
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 12
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims description 10
- XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Natural products NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 claims description 10
- 239000003814 drug Substances 0.000 claims description 10
- 239000008194 pharmaceutical composition Substances 0.000 claims description 9
- 101100516563 Caenorhabditis elegans nhr-6 gene Proteins 0.000 claims description 8
- 201000010099 disease Diseases 0.000 claims description 8
- 208000035475 disorder Diseases 0.000 claims description 8
- 150000002148 esters Chemical class 0.000 claims description 8
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 8
- 239000012453 solvate Substances 0.000 claims description 8
- 208000012641 Pigmentation disease Diseases 0.000 claims description 7
- 229910052799 carbon Inorganic materials 0.000 claims description 7
- 239000011203 carbon fibre reinforced carbon Substances 0.000 claims description 7
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 7
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 7
- 125000006714 (C3-C10) heterocyclyl group Chemical group 0.000 claims description 6
- 102100034357 Casein kinase I isoform alpha Human genes 0.000 claims description 6
- 102000004127 Cytokines Human genes 0.000 claims description 6
- 108090000695 Cytokines Proteins 0.000 claims description 6
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 claims description 6
- 101000994700 Homo sapiens Casein kinase I isoform alpha Proteins 0.000 claims description 6
- 239000004202 carbamide Substances 0.000 claims description 6
- 229910052805 deuterium Inorganic materials 0.000 claims description 6
- 102000004169 proteins and genes Human genes 0.000 claims description 6
- 108090000623 proteins and genes Proteins 0.000 claims description 6
- 102100036816 Eukaryotic peptide chain release factor GTP-binding subunit ERF3A Human genes 0.000 claims description 5
- 101000851788 Homo sapiens Eukaryotic peptide chain release factor GTP-binding subunit ERF3A Proteins 0.000 claims description 5
- 101000599042 Homo sapiens Zinc finger protein Aiolos Proteins 0.000 claims description 5
- 101000599037 Homo sapiens Zinc finger protein Helios Proteins 0.000 claims description 5
- 206010061218 Inflammation Diseases 0.000 claims description 5
- 102100037798 Zinc finger protein Aiolos Human genes 0.000 claims description 5
- 102100037796 Zinc finger protein Helios Human genes 0.000 claims description 5
- 125000006367 bivalent amino carbonyl group Chemical group [H]N([*:1])C([*:2])=O 0.000 claims description 5
- 125000006297 carbonyl amino group Chemical group [H]N([*:2])C([*:1])=O 0.000 claims description 5
- 230000004054 inflammatory process Effects 0.000 claims description 5
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 5
- 150000003672 ureas Chemical class 0.000 claims description 5
- 108010013958 Ikaros Transcription Factor Proteins 0.000 claims description 4
- 102000017182 Ikaros Transcription Factor Human genes 0.000 claims description 4
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims description 4
- 201000001263 Psoriatic Arthritis Diseases 0.000 claims description 4
- 208000036824 Psoriatic arthropathy Diseases 0.000 claims description 4
- 208000000453 Skin Neoplasms Diseases 0.000 claims description 4
- CREMABGTGYGIQB-UHFFFAOYSA-N carbon carbon Chemical group C.C CREMABGTGYGIQB-UHFFFAOYSA-N 0.000 claims description 4
- 229910052739 hydrogen Inorganic materials 0.000 claims description 4
- 201000000849 skin cancer Diseases 0.000 claims description 4
- 229940124530 sulfonamide Drugs 0.000 claims description 4
- 229910052717 sulfur Inorganic materials 0.000 claims description 4
- 208000024827 Alzheimer disease Diseases 0.000 claims description 3
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims description 3
- 206010009900 Colitis ulcerative Diseases 0.000 claims description 3
- 208000011231 Crohn disease Diseases 0.000 claims description 3
- 208000001640 Fibromyalgia Diseases 0.000 claims description 3
- 206010028980 Neoplasm Diseases 0.000 claims description 3
- 206010042496 Sunburn Diseases 0.000 claims description 3
- 201000006704 Ulcerative Colitis Diseases 0.000 claims description 3
- 201000011510 cancer Diseases 0.000 claims description 3
- YQCIWBXEVYWRCW-UHFFFAOYSA-N methane;sulfane Chemical compound C.S YQCIWBXEVYWRCW-UHFFFAOYSA-N 0.000 claims description 3
- 201000008482 osteoarthritis Diseases 0.000 claims description 3
- 206010039073 rheumatoid arthritis Diseases 0.000 claims description 3
- 208000019693 Lung disease Diseases 0.000 claims description 2
- UMGDCJDMYOKAJW-UHFFFAOYSA-N aminothiocarboxamide Natural products NC(N)=S UMGDCJDMYOKAJW-UHFFFAOYSA-N 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 125000001153 fluoro group Chemical group F* 0.000 claims description 2
- 238000001990 intravenous administration Methods 0.000 claims description 2
- 238000007911 parenteral administration Methods 0.000 claims description 2
- 150000003871 sulfonates Chemical class 0.000 claims description 2
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims description 2
- 150000003585 thioureas Chemical class 0.000 claims description 2
- 238000011200 topical administration Methods 0.000 claims description 2
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 2
- 201000004681 Psoriasis Diseases 0.000 claims 2
- 201000002661 Spondylitis Diseases 0.000 claims 2
- 229940079593 drug Drugs 0.000 claims 2
- 230000001256 tonic effect Effects 0.000 claims 2
- GBXQPDCOMJJCMJ-UHFFFAOYSA-M trimethyl-[6-(trimethylazaniumyl)hexyl]azanium;bromide Chemical compound [Br-].C[N+](C)(C)CCCCCC[N+](C)(C)C GBXQPDCOMJJCMJ-UHFFFAOYSA-M 0.000 claims 2
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 1
- 241000219094 Vitaceae Species 0.000 claims 1
- 235000021021 grapes Nutrition 0.000 claims 1
- 230000002757 inflammatory effect Effects 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 238000000034 method Methods 0.000 description 25
- 125000003545 alkoxy group Chemical group 0.000 description 6
- 229940124597 therapeutic agent Drugs 0.000 description 6
- 125000006570 (C5-C6) heteroaryl group Chemical class 0.000 description 4
- 125000000304 alkynyl group Chemical group 0.000 description 4
- 239000002246 antineoplastic agent Substances 0.000 description 4
- 235000013877 carbamide Nutrition 0.000 description 4
- 239000002260 anti-inflammatory agent Substances 0.000 description 2
- 229940121363 anti-inflammatory agent Drugs 0.000 description 2
- 125000003725 azepanyl group Chemical group 0.000 description 2
- 230000000694 effects Effects 0.000 description 2
- 229960001438 immunostimulant agent Drugs 0.000 description 2
- 239000003022 immunostimulating agent Substances 0.000 description 2
- 230000003308 immunostimulating effect Effects 0.000 description 2
- 239000003018 immunosuppressive agent Substances 0.000 description 2
- 229940125721 immunosuppressive agent Drugs 0.000 description 2
- 125000004193 piperazinyl group Chemical group 0.000 description 2
- 125000000719 pyrrolidinyl group Chemical group 0.000 description 2
- 206010002556 Ankylosing Spondylitis Diseases 0.000 description 1
- 102100025064 Cellular tumor antigen p53 Human genes 0.000 description 1
- 102000012199 E3 ubiquitin-protein ligase Mdm2 Human genes 0.000 description 1
- 108050002772 E3 ubiquitin-protein ligase Mdm2 Proteins 0.000 description 1
- 206010047115 Vasculitis Diseases 0.000 description 1
- 125000003342 alkenyl group Chemical group 0.000 description 1
- 125000004438 haloalkoxy group Chemical group 0.000 description 1
- 230000002401 inhibitory effect Effects 0.000 description 1
- 230000004952 protein activity Effects 0.000 description 1
- 230000001568 sexual effect Effects 0.000 description 1
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662437400P | 2016-12-21 | 2016-12-21 | |
| US62/437,400 | 2016-12-21 | ||
| US201762485563P | 2017-04-14 | 2017-04-14 | |
| US62/485,563 | 2017-04-14 | ||
| US201762538203P | 2017-07-28 | 2017-07-28 | |
| US62/538,203 | 2017-07-28 | ||
| PCT/US2017/067353 WO2018118947A1 (en) | 2016-12-21 | 2017-12-19 | Thienopyrrole derivatives for use in targeting proteins, compositions, methods, and uses thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2020504711A JP2020504711A (ja) | 2020-02-13 |
| JP2020504711A5 true JP2020504711A5 (https=) | 2021-02-04 |
Family
ID=60991575
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019526486A Pending JP2020504711A (ja) | 2016-12-21 | 2017-12-19 | タンパク質を標的とすることにおいて使用するための、チエノピロール誘導体、その組成物、方法、および使用 |
Country Status (13)
| Country | Link |
|---|---|
| US (4) | US10040804B2 (https=) |
| EP (1) | EP3559005A1 (https=) |
| JP (1) | JP2020504711A (https=) |
| KR (1) | KR20190093205A (https=) |
| CN (1) | CN110099907A (https=) |
| AU (1) | AU2017382176A1 (https=) |
| CA (1) | CA3043938A1 (https=) |
| IL (1) | IL267323A (https=) |
| MX (1) | MX387646B (https=) |
| RU (1) | RU2771166C2 (https=) |
| TW (2) | TWI756957B (https=) |
| WO (1) | WO2018118947A1 (https=) |
| ZA (1) | ZA201903479B (https=) |
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| CN109790143A (zh) | 2016-05-10 | 2019-05-21 | C4医药公司 | 用于靶蛋白降解的胺连接的c3-戊二酰亚胺降解决定子体 |
| ES2990061T3 (es) | 2016-05-10 | 2024-11-28 | C4 Therapeutics Inc | Degronímeros espirocíclicos para la degradación de proteínas diana |
| CN109641874A (zh) | 2016-05-10 | 2019-04-16 | C4医药公司 | 用于靶蛋白降解的c3-碳连接的戊二酰亚胺降解决定子体 |
| EP3454856B1 (en) | 2016-05-10 | 2024-09-11 | C4 Therapeutics, Inc. | Heterocyclic degronimers for target protein degradation |
| US10040804B2 (en) | 2016-12-21 | 2018-08-07 | Biotheryx, Inc. | Compounds targeting proteins, compositions, methods, and uses thereof |
| CN110769822A (zh) | 2017-06-20 | 2020-02-07 | C4医药公司 | 用于蛋白降解的n/o-连接的降解决定子和降解决定子体 |
| WO2019043217A1 (en) | 2017-09-04 | 2019-03-07 | F. Hoffmann-La Roche Ag | DIHYDROBENZIMIDAZOLONES |
| WO2019043208A1 (en) | 2017-09-04 | 2019-03-07 | F. Hoffmann-La Roche Ag | DIHYDROQUINOLINONES |
| CN118108706A (zh) | 2017-09-04 | 2024-05-31 | C4医药公司 | 戊二酰亚胺 |
| CN111372585A (zh) | 2017-11-16 | 2020-07-03 | C4医药公司 | 用于靶蛋白降解的降解剂和降解决定子 |
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| TW202146412A (zh) | 2020-03-05 | 2021-12-16 | 美商Ｃ４醫藥公司 | 用於標靶降解brd9之化合物 |
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-
2017
- 2017-12-19 US US15/847,628 patent/US10040804B2/en active Active
- 2017-12-19 CA CA3043938A patent/CA3043938A1/en not_active Abandoned
- 2017-12-19 EP EP17829823.8A patent/EP3559005A1/en not_active Withdrawn
- 2017-12-19 JP JP2019526486A patent/JP2020504711A/ja active Pending
- 2017-12-19 WO PCT/US2017/067353 patent/WO2018118947A1/en not_active Ceased
- 2017-12-19 MX MX2019007434A patent/MX387646B/es unknown
- 2017-12-19 RU RU2019115392A patent/RU2771166C2/ru active
- 2017-12-19 CN CN201780079826.3A patent/CN110099907A/zh active Pending
- 2017-12-19 KR KR1020197018882A patent/KR20190093205A/ko not_active Ceased
- 2017-12-19 AU AU2017382176A patent/AU2017382176A1/en not_active Abandoned
- 2017-12-21 TW TW109142439A patent/TWI756957B/zh not_active IP Right Cessation
- 2017-12-21 TW TW106145115A patent/TW201835089A/zh unknown
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2018
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2019
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