JPWO2019241271A5 - - Google Patents
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- JPWO2019241271A5 JPWO2019241271A5 JP2020569169A JP2020569169A JPWO2019241271A5 JP WO2019241271 A5 JPWO2019241271 A5 JP WO2019241271A5 JP 2020569169 A JP2020569169 A JP 2020569169A JP 2020569169 A JP2020569169 A JP 2020569169A JP WO2019241271 A5 JPWO2019241271 A5 JP WO2019241271A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- substituted
- optionally substituted
- cancer
- alkoxy
- 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.)
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- 210000004027 cell Anatomy 0.000 claims description 56
- 125000000217 alkyl group Chemical group 0.000 claims description 50
- 150000001875 compounds Chemical class 0.000 claims description 50
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 24
- 125000000623 heterocyclic group Chemical group 0.000 claims description 24
- 229910052736 halogen Inorganic materials 0.000 claims description 20
- 150000002367 halogens Chemical class 0.000 claims description 20
- 125000001424 substituent group Chemical group 0.000 claims description 18
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 17
- 150000003839 salts Chemical class 0.000 claims description 16
- 125000003118 aryl group Chemical group 0.000 claims description 13
- 201000010099 disease Diseases 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
- 208000035475 disorder Diseases 0.000 claims description 11
- 125000001188 haloalkyl group Chemical group 0.000 claims description 11
- 229910052739 hydrogen Inorganic materials 0.000 claims description 11
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 claims description 10
- 208000034578 Multiple myelomas Diseases 0.000 claims description 10
- 206010035226 Plasma cell myeloma Diseases 0.000 claims description 10
- 229910052805 deuterium Inorganic materials 0.000 claims description 10
- 102000004169 proteins and genes Human genes 0.000 claims description 10
- 108090000623 proteins and genes Proteins 0.000 claims description 10
- 108010002350 Interleukin-2 Proteins 0.000 claims description 9
- 239000001257 hydrogen Substances 0.000 claims description 9
- -1 chloro, methyl Chemical group 0.000 claims description 8
- 102100034357 Casein kinase I isoform alpha Human genes 0.000 claims description 7
- 102100036816 Eukaryotic peptide chain release factor GTP-binding subunit ERF3A Human genes 0.000 claims description 7
- 101000994700 Homo sapiens Casein kinase I isoform alpha Proteins 0.000 claims description 7
- 101000851788 Homo sapiens Eukaryotic peptide chain release factor GTP-binding subunit ERF3A Proteins 0.000 claims description 7
- 102000000588 Interleukin-2 Human genes 0.000 claims description 7
- 108090001005 Interleukin-6 Proteins 0.000 claims description 7
- 102000004889 Interleukin-6 Human genes 0.000 claims description 7
- 206010028980 Neoplasm Diseases 0.000 claims description 7
- 108060008682 Tumor Necrosis Factor Proteins 0.000 claims description 7
- 102000000852 Tumor Necrosis Factor-alpha Human genes 0.000 claims description 7
- 208000002250 Hematologic Neoplasms Diseases 0.000 claims description 6
- 206010025323 Lymphomas Diseases 0.000 claims description 6
- 201000004681 Psoriasis Diseases 0.000 claims description 6
- 239000012472 biological sample Substances 0.000 claims description 6
- 125000004452 carbocyclyl group Chemical group 0.000 claims description 6
- 125000001153 fluoro group Chemical group F* 0.000 claims description 6
- 125000001072 heteroaryl group Chemical group 0.000 claims description 6
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 6
- 208000032839 leukemia Diseases 0.000 claims description 6
- 239000008194 pharmaceutical composition Substances 0.000 claims description 6
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 6
- 208000011231 Crohn disease Diseases 0.000 claims description 5
- 208000001640 Fibromyalgia Diseases 0.000 claims description 5
- 206010016654 Fibrosis Diseases 0.000 claims description 5
- 101000599042 Homo sapiens Zinc finger protein Aiolos Proteins 0.000 claims description 5
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 5
- 108010013958 Ikaros Transcription Factor Proteins 0.000 claims description 5
- 102000017182 Ikaros Transcription Factor Human genes 0.000 claims description 5
- 201000002661 Spondylitis Diseases 0.000 claims description 5
- 102100037798 Zinc finger protein Aiolos Human genes 0.000 claims description 5
- 125000003282 alkyl amino group Chemical group 0.000 claims description 5
- 230000004761 fibrosis Effects 0.000 claims description 5
- 125000004438 haloalkoxy group Chemical group 0.000 claims description 5
- 206010025135 lupus erythematosus Diseases 0.000 claims description 5
- 229910052757 nitrogen Inorganic materials 0.000 claims description 5
- 201000008482 osteoarthritis Diseases 0.000 claims description 5
- 206010039073 rheumatoid arthritis Diseases 0.000 claims description 5
- 230000001256 tonic effect Effects 0.000 claims description 5
- 208000003174 Brain Neoplasms Diseases 0.000 claims description 4
- 206010006187 Breast cancer Diseases 0.000 claims description 4
- 208000026310 Breast neoplasm Diseases 0.000 claims description 4
- 206010009900 Colitis ulcerative Diseases 0.000 claims description 4
- 206010009944 Colon cancer Diseases 0.000 claims description 4
- 206010014733 Endometrial cancer Diseases 0.000 claims description 4
- 206010014759 Endometrial neoplasm Diseases 0.000 claims description 4
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims description 4
- 206010018341 Gliosis Diseases 0.000 claims description 4
- 101000599037 Homo sapiens Zinc finger protein Helios Proteins 0.000 claims description 4
- 208000008839 Kidney Neoplasms Diseases 0.000 claims description 4
- 206010029260 Neuroblastoma Diseases 0.000 claims description 4
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims description 4
- 206010033128 Ovarian cancer Diseases 0.000 claims description 4
- 206010061535 Ovarian neoplasm Diseases 0.000 claims description 4
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims description 4
- 201000001263 Psoriatic Arthritis Diseases 0.000 claims description 4
- 208000036824 Psoriatic arthropathy Diseases 0.000 claims description 4
- 208000015634 Rectal Neoplasms Diseases 0.000 claims description 4
- 206010038389 Renal cancer Diseases 0.000 claims description 4
- 208000000453 Skin Neoplasms Diseases 0.000 claims description 4
- 206010041067 Small cell lung cancer Diseases 0.000 claims description 4
- 208000005718 Stomach Neoplasms Diseases 0.000 claims description 4
- 208000024313 Testicular Neoplasms Diseases 0.000 claims description 4
- 206010057644 Testis cancer Diseases 0.000 claims description 4
- 201000006704 Ulcerative Colitis Diseases 0.000 claims description 4
- 102100037796 Zinc finger protein Helios Human genes 0.000 claims description 4
- 208000037875 astrocytosis Diseases 0.000 claims description 4
- 230000007341 astrogliosis Effects 0.000 claims description 4
- 201000000053 blastoma Diseases 0.000 claims description 4
- 239000011203 carbon fibre reinforced carbon Substances 0.000 claims description 4
- 208000029742 colonic neoplasm Diseases 0.000 claims description 4
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 4
- 201000008184 embryoma Diseases 0.000 claims description 4
- 201000004101 esophageal cancer Diseases 0.000 claims description 4
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 4
- 206010017758 gastric cancer Diseases 0.000 claims description 4
- 201000010536 head and neck cancer Diseases 0.000 claims description 4
- 208000014829 head and neck neoplasm Diseases 0.000 claims description 4
- 125000004051 hexyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims description 4
- 150000002431 hydrogen Chemical class 0.000 claims description 4
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 4
- 201000010982 kidney cancer Diseases 0.000 claims description 4
- 206010024627 liposarcoma Diseases 0.000 claims description 4
- 201000007270 liver cancer Diseases 0.000 claims description 4
- 208000014018 liver neoplasm Diseases 0.000 claims description 4
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims description 4
- 201000001441 melanoma Diseases 0.000 claims description 4
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 4
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims description 4
- 229910052760 oxygen Inorganic materials 0.000 claims description 4
- 201000002528 pancreatic cancer Diseases 0.000 claims description 4
- 208000008443 pancreatic carcinoma Diseases 0.000 claims description 4
- 125000004076 pyridyl group Chemical group 0.000 claims description 4
- 206010038038 rectal cancer Diseases 0.000 claims description 4
- 201000001275 rectum cancer Diseases 0.000 claims description 4
- 230000002207 retinal effect Effects 0.000 claims description 4
- 201000000849 skin cancer Diseases 0.000 claims description 4
- 208000000587 small cell lung carcinoma Diseases 0.000 claims description 4
- 206010041823 squamous cell carcinoma Diseases 0.000 claims description 4
- 201000011549 stomach cancer Diseases 0.000 claims description 4
- 229910052717 sulfur Inorganic materials 0.000 claims description 4
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims description 4
- 201000003120 testicular cancer Diseases 0.000 claims description 4
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 4
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims description 4
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims description 3
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims description 3
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims description 3
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims description 3
- 206010060862 Prostate cancer Diseases 0.000 claims description 3
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims description 3
- 206010046914 Vaginal infection Diseases 0.000 claims description 3
- 201000008100 Vaginitis Diseases 0.000 claims description 3
- 201000011510 cancer Diseases 0.000 claims description 3
- 230000000694 effects Effects 0.000 claims description 3
- 230000036244 malformation Effects 0.000 claims description 3
- 230000004770 neurodegeneration Effects 0.000 claims description 3
- 208000015122 neurodegenerative disease Diseases 0.000 claims description 3
- 208000024827 Alzheimer disease Diseases 0.000 claims description 2
- 208000018737 Parkinson disease Diseases 0.000 claims description 2
- 239000000654 additive Substances 0.000 claims description 2
- 230000000996 additive effect Effects 0.000 claims description 2
- 229910052799 carbon Inorganic materials 0.000 claims description 2
- CREMABGTGYGIQB-UHFFFAOYSA-N carbon carbon Chemical compound C.C CREMABGTGYGIQB-UHFFFAOYSA-N 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 230000002489 hematologic effect Effects 0.000 claims description 2
- YQCIWBXEVYWRCW-UHFFFAOYSA-N methane;sulfane Chemical compound C.S YQCIWBXEVYWRCW-UHFFFAOYSA-N 0.000 claims description 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 2
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 2
- 210000004881 tumor cell Anatomy 0.000 claims description 2
- 239000000203 mixture Substances 0.000 claims 6
- 125000004123 n-propyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 2
- 208000025865 Ulcer Diseases 0.000 claims 1
- 206010003246 arthritis Diseases 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 230000004952 protein activity Effects 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 description 16
- 125000000033 alkoxyamino group Chemical group 0.000 description 2
- 125000003342 alkenyl group Chemical group 0.000 description 1
- 125000000304 alkynyl group Chemical group 0.000 description 1
- 239000003814 drug Substances 0.000 description 1
- 229940124597 therapeutic agent Drugs 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862684495P | 2018-06-13 | 2018-06-13 | |
| US62/684,495 | 2018-06-13 | ||
| PCT/US2019/036581 WO2019241271A1 (en) | 2018-06-13 | 2019-06-11 | Fused thiophene compounds |
Publications (4)
| Publication Number | Publication Date |
|---|---|
| JP2021527098A JP2021527098A (ja) | 2021-10-11 |
| JPWO2019241271A5 true JPWO2019241271A5 (https=) | 2022-06-10 |
| JP2021527098A5 JP2021527098A5 (https=) | 2022-06-10 |
| JP7365059B2 JP7365059B2 (ja) | 2023-10-19 |
Family
ID=67263033
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020569169A Active JP7365059B2 (ja) | 2018-06-13 | 2019-06-11 | 縮合チオフェン化合物 |
Country Status (8)
| Country | Link |
|---|---|
| US (2) | US11191769B2 (https=) |
| EP (1) | EP3807283A1 (https=) |
| JP (1) | JP7365059B2 (https=) |
| CN (1) | CN112601751B (https=) |
| AU (1) | AU2019284605A1 (https=) |
| CA (1) | CA3101335C (https=) |
| TW (1) | TWI826463B (https=) |
| WO (1) | WO2019241271A1 (https=) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10513515B2 (en) * | 2017-08-25 | 2019-12-24 | Biotheryx, Inc. | Ether compounds and uses thereof |
| AU2020387392B2 (en) | 2019-11-19 | 2025-09-11 | Bristol-Myers Squibb Company | Compounds useful as inhibitors of Helios protein |
| WO2021155050A1 (en) * | 2020-01-29 | 2021-08-05 | Biotheryx, Inc. | Kinase modulators, pharmaceutical compositions, and therapeutic applications |
| 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 |
| WO2022061348A1 (en) | 2020-09-16 | 2022-03-24 | Biotheryx, Inc. | Sos1 protein degraders, 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 |
| WO2022087335A1 (en) | 2020-10-23 | 2022-04-28 | Biotheryx, Inc. | Kras protein degraders, pharmaceutical compositions thereof, and their therapeutic applications |
| 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 |
| WO2023069731A1 (en) * | 2021-10-22 | 2023-04-27 | Monte Rosa Therapeutics, Inc. | Compounds that mediate protein degradation and methods of use thereof |
| US12419962B2 (en) | 2022-03-16 | 2025-09-23 | Biotheryx, Inc. | Quinazolines, pharmaceutical compositions, and therapeutic applications |
| WO2024015855A1 (en) | 2022-07-13 | 2024-01-18 | Monte Rosa Therapeutics, Inc. | COMBINATION THERAPY COMPRISING GSPT1-DIRECTED MOLECULAR GLUE DEGRADERS AND PI3K/AKT/mTOR PATHWAY INHIBITORS |
| CN120303264A (zh) | 2022-09-09 | 2025-07-11 | 医诺康治疗公司 | CK1α和双重CK1α/GSPT1降解化合物 |
| WO2024222918A1 (zh) * | 2023-04-28 | 2024-10-31 | 中国药科大学 | 一种苯并六元杂环类gspt1蛋白降解剂及其应用 |
| CN119371398A (zh) * | 2023-07-25 | 2025-01-28 | 安道麦阿甘有限公司 | 用于制备噻吩酮的新路线 |
| WO2025179161A1 (en) | 2024-02-21 | 2025-08-28 | Innovo Therapeutics, Inc. | Protein degrading compounds |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1939922B (zh) * | 2005-09-27 | 2010-10-13 | 天津和美生物技术有限公司 | 可抑制细胞释放肿瘤坏死因子的5H-噻吩[3，4-c]吡咯-4，6-二酮衍生物 |
| CN101186611B (zh) * | 2006-11-15 | 2011-05-18 | 天津和美生物技术有限公司 | 可抑制细胞释放肿瘤坏死因子的吡咯啉-2-酮衍生物及其制备和应用 |
| KR20170042598A (ko) | 2014-08-22 | 2017-04-19 | 셀진 코포레이션 | 항체와 조합된 면역조절 화합물을 이용하여 다발성 골수종을 치료하는 방법 |
| AU2016266942B2 (en) * | 2015-05-22 | 2018-10-18 | Biotheryx, Inc. | Compounds targeting proteins, compositions, methods, and uses thereof |
| CA3043938A1 (en) * | 2016-12-21 | 2018-06-28 | Biotheryx, Inc. | Thienopyrrole derivatives for use in targeting proteins, compositions, methods, and uses thereof |
-
2019
- 2019-06-11 CN CN201980039027.2A patent/CN112601751B/zh active Active
- 2019-06-11 CA CA3101335A patent/CA3101335C/en active Active
- 2019-06-11 AU AU2019284605A patent/AU2019284605A1/en not_active Abandoned
- 2019-06-11 US US16/438,244 patent/US11191769B2/en active Active
- 2019-06-11 WO PCT/US2019/036581 patent/WO2019241271A1/en not_active Ceased
- 2019-06-11 EP EP19739747.4A patent/EP3807283A1/en not_active Withdrawn
- 2019-06-11 JP JP2020569169A patent/JP7365059B2/ja active Active
- 2019-06-13 TW TW108120511A patent/TWI826463B/zh not_active IP Right Cessation
-
2021
- 2021-12-06 US US17/457,733 patent/US20220088025A1/en not_active Abandoned
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