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=) |
Families Citing this family (54)
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| EP3454862B1 (en) | 2016-05-10 | 2024-09-11 | C4 Therapeutics, Inc. | Spirocyclic degronimers for target protein degradation |
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| 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 |
| 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 |
| CA3043938A1 (en) | 2016-12-21 | 2018-06-28 | Biotheryx, Inc. | Thienopyrrole derivatives for use in targeting proteins, compositions, methods, and uses thereof |
| EP4717317A2 (en) | 2017-06-20 | 2026-04-01 | C4 Therapeutics, Inc. | N/o-linked degrons and degronimers for protein degradation |
| CN111278816B (zh) | 2017-09-04 | 2024-03-15 | C4医药公司 | 二氢喹啉酮 |
| CN118108706A (zh) | 2017-09-04 | 2024-05-31 | C4医药公司 | 戊二酰亚胺 |
| CN118206529A (zh) | 2017-09-04 | 2024-06-18 | C4医药公司 | 二氢苯并咪唑酮 |
| EP3710002A4 (en) | 2017-11-16 | 2021-07-07 | C4 Therapeutics, Inc. | DEGRADER AND DEGRONE FOR TARGETED PROTEIN DEGRADATION |
| JP2021519337A (ja) | 2018-03-26 | 2021-08-10 | シー４ セラピューティクス， インコーポレイテッド | Ｉｋａｒｏｓの分解のためのセレブロン結合剤 |
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| CN119751456A (zh) | 2018-04-16 | 2025-04-04 | C4医药公司 | 螺环化合物 |
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| CN112601751B (zh) * | 2018-06-13 | 2024-04-02 | 拜欧斯瑞克斯公司 | 稠合噻吩化合物 |
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| CN120698983A (zh) | 2018-12-20 | 2025-09-26 | C4医药公司 | 靶向蛋白降解 |
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| FR3092581A1 (fr) * | 2019-02-12 | 2020-08-14 | Impact Biomedicines, Inc | Formes cristallines d'un inhibiteur de jak2 |
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| CN120172958A (zh) | 2019-04-12 | 2025-06-20 | C4医药公司 | Ikaros和aiolos的三环降解物 |
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| WO2021022163A2 (en) | 2019-07-31 | 2021-02-04 | Foghorn Therapeutics Inc. | Compounds and uses thereof |
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| AU2020387392B2 (en) | 2019-11-19 | 2025-09-11 | Bristol-Myers Squibb Company | Compounds useful as inhibitors of Helios protein |
| BR112022011827A2 (pt) | 2019-12-20 | 2022-08-30 | C4 Therapeutics Inc | Composto, composição farmacêutica, uso de um composto, métodos para tratamento ou profilaxia de câncer e para tratar um paciente com um distúrbio mediado por receptor do fator de crescimento epidérmico, e, invenção |
| AU2021214767A1 (en) | 2020-01-29 | 2022-07-28 | Foghorn Therapeutics Inc. | Compounds and uses thereof |
| US12528825B2 (en) | 2020-01-29 | 2026-01-20 | Foghorn Therapeutics Inc. | Compounds and uses thereof |
| WO2023205701A1 (en) | 2022-04-20 | 2023-10-26 | Kumquat Biosciences Inc. | Macrocyclic heterocycles and uses thereof |
| CA3173262A1 (en) | 2020-02-26 | 2021-09-02 | Cullgen (Shanghai), Inc. | Tropomyosin receptor kinase (trk) degradation compounds and methods of use |
| AU2021231898A1 (en) | 2020-03-05 | 2022-10-27 | C4 Therapeutics, Inc. | Compounds for targeted degradation of BRD9 |
| TW202140441A (zh) | 2020-03-23 | 2021-11-01 | 美商必治妥美雅史谷比公司 | 經取代之側氧基異吲哚啉化合物 |
| US11787800B2 (en) | 2020-07-29 | 2023-10-17 | Foghorn Therapeutics Inc. | BRD9 degraders and uses thereof |
| WO2022061348A1 (en) | 2020-09-16 | 2022-03-24 | Biotheryx, Inc. | Sos1 protein degraders, pharmaceutical compositions thereof, and their therapeutic applications |
| WO2022072538A1 (en) * | 2020-09-30 | 2022-04-07 | Biotheryx, Inc. | Antibody-drug conjugates, pharmaceutical compositions thereof, and their therapeutic applications |
| CN116583509A (zh) * | 2020-10-07 | 2023-08-11 | 上海睿跃生物科技有限公司 | 治疗癌症的化合物和方法 |
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| TW202237580A (zh) | 2020-12-14 | 2022-10-01 | 美商拜歐斯瑞克斯公司 | Pde4降解劑、醫藥組合物及治療應用 |
| JP2024504932A (ja) | 2021-01-13 | 2024-02-02 | モンテ ローザ セラピューティクス， インコーポレイテッド | イソインドリノン化合物 |
| BR112023020077A2 (pt) | 2021-04-06 | 2023-11-14 | Bristol Myers Squibb Co | Compostos de oxoisoindolina substituída por piridinila |
| AU2022271290A1 (en) | 2021-05-07 | 2023-11-23 | Kymera Therapeutics, Inc. | Cdk2 degraders and uses thereof |
| WO2022261250A1 (en) | 2021-06-08 | 2022-12-15 | C4 Therapeutics, Inc. | Therapeutics for the degradation of mutant braf |
| WO2023283263A1 (en) | 2021-07-06 | 2023-01-12 | Foghorn Therapeutics Inc. | Citrate salt, pharmaceutical compositions, and methods of making and using the same |
| US12419962B2 (en) | 2022-03-16 | 2025-09-23 | Biotheryx, Inc. | Quinazolines, pharmaceutical compositions, and therapeutic applications |
| JP2025523393A (ja) | 2022-06-06 | 2025-07-23 | シーフォー セラピューティクス， インコーポレイテッド | 二環式置換グルタルイミドセレブロンバインダー |
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| AU2024307234A1 (en) | 2023-06-30 | 2026-01-29 | Kumquat Biosciences Inc. | Substituted condensed tricyclic amine compounds and uses thereof as ras inhibitors |
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-
2017
- 2017-12-19 CA CA3043938A patent/CA3043938A1/en not_active Abandoned
- 2017-12-19 KR KR1020197018882A patent/KR20190093205A/ko not_active Ceased
- 2017-12-19 AU AU2017382176A patent/AU2017382176A1/en not_active Abandoned
- 2017-12-19 JP JP2019526486A patent/JP2020504711A/ja active Pending
- 2017-12-19 CN CN201780079826.3A patent/CN110099907A/zh active Pending
- 2017-12-19 RU RU2019115392A patent/RU2771166C2/ru active
- 2017-12-19 MX MX2019007434A patent/MX387646B/es unknown
- 2017-12-19 WO PCT/US2017/067353 patent/WO2018118947A1/en not_active Ceased
- 2017-12-19 US US15/847,628 patent/US10040804B2/en active Active
- 2017-12-19 EP EP17829823.8A patent/EP3559005A1/en not_active Withdrawn
- 2017-12-21 TW TW109142439A patent/TWI756957B/zh not_active IP Right Cessation
- 2017-12-21 TW TW106145115A patent/TW201835089A/zh unknown
-
2018
- 2018-06-18 US US16/011,090 patent/US10336771B2/en active Active
-
2019
- 2019-05-30 ZA ZA2019/03479A patent/ZA201903479B/en unknown
- 2019-06-13 IL IL267323A patent/IL267323A/en unknown
- 2019-06-28 US US16/457,409 patent/US10889593B2/en active Active
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2021
- 2021-01-11 US US17/146,479 patent/US11345714B2/en active Active
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