JPWO2022029138A5 - - Google Patents
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- JPWO2022029138A5 JPWO2022029138A5 JP2023507550A JP2023507550A JPWO2022029138A5 JP WO2022029138 A5 JPWO2022029138 A5 JP WO2022029138A5 JP 2023507550 A JP2023507550 A JP 2023507550A JP 2023507550 A JP2023507550 A JP 2023507550A JP WO2022029138 A5 JPWO2022029138 A5 JP WO2022029138A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- compound
- unsubstituted
- membered
- pharmaceutical composition
- 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.)
- Pending
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- 150000001875 compounds Chemical class 0.000 claims 69
- 239000008194 pharmaceutical composition Substances 0.000 claims 39
- 125000000217 alkyl group Chemical group 0.000 claims 31
- 125000000623 heterocyclic group Chemical group 0.000 claims 30
- 125000003118 aryl group Chemical group 0.000 claims 29
- 229910052739 hydrogen Inorganic materials 0.000 claims 29
- SIKJAQJRHWYJAI-UHFFFAOYSA-N Indole Chemical compound C1=CC=C2NC=CC2=C1 SIKJAQJRHWYJAI-UHFFFAOYSA-N 0.000 claims 20
- 125000001072 heteroaryl group Chemical group 0.000 claims 18
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 claims 17
- 229910052805 deuterium Inorganic materials 0.000 claims 17
- 229910052799 carbon Inorganic materials 0.000 claims 16
- 125000001424 substituent group Chemical group 0.000 claims 16
- 239000001257 hydrogen Substances 0.000 claims 15
- 125000006163 5-membered heteroaryl group Chemical group 0.000 claims 11
- PZOUSPYUWWUPPK-UHFFFAOYSA-N indole Natural products CC1=CC=CC2=C1C=CN2 PZOUSPYUWWUPPK-UHFFFAOYSA-N 0.000 claims 11
- RKJUIXBNRJVNHR-UHFFFAOYSA-N indolenine Natural products C1=CC=C2CC=NC2=C1 RKJUIXBNRJVNHR-UHFFFAOYSA-N 0.000 claims 11
- 206010028980 Neoplasm Diseases 0.000 claims 10
- 201000011510 cancer Diseases 0.000 claims 10
- 150000002431 hydrogen Chemical class 0.000 claims 10
- 150000001413 amino acids Chemical class 0.000 claims 9
- 150000002148 esters Chemical class 0.000 claims 9
- 229940002612 prodrug Drugs 0.000 claims 9
- 239000000651 prodrug Substances 0.000 claims 9
- 150000003839 salts Chemical class 0.000 claims 9
- 239000012453 solvate Substances 0.000 claims 9
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 8
- 125000003342 alkenyl group Chemical group 0.000 claims 7
- -1 dioxolyl Chemical group 0.000 claims 7
- 125000002373 5 membered heterocyclic group Chemical group 0.000 claims 6
- 125000004070 6 membered heterocyclic group Chemical group 0.000 claims 6
- 125000004432 carbon atom Chemical group C* 0.000 claims 6
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 6
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 6
- 238000000034 method Methods 0.000 claims 6
- 229910052757 nitrogen Inorganic materials 0.000 claims 6
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 6
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 5
- 125000000262 haloalkenyl group Chemical group 0.000 claims 4
- 125000001188 haloalkyl group Chemical group 0.000 claims 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 4
- 206010029260 Neuroblastoma Diseases 0.000 claims 3
- 208000003837 Second Primary Neoplasms Diseases 0.000 claims 3
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 3
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 3
- 125000000753 cycloalkyl group Chemical group 0.000 claims 3
- 125000005059 halophenyl group Chemical group 0.000 claims 3
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims 3
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims 3
- 208000032839 leukemia Diseases 0.000 claims 3
- 238000011275 oncology therapy Methods 0.000 claims 3
- 108090000623 proteins and genes Proteins 0.000 claims 3
- 102000004169 proteins and genes Human genes 0.000 claims 3
- 208000036762 Acute promyelocytic leukaemia Diseases 0.000 claims 2
- 206010006187 Breast cancer Diseases 0.000 claims 2
- 208000026310 Breast neoplasm Diseases 0.000 claims 2
- 102100036816 Eukaryotic peptide chain release factor GTP-binding subunit ERF3A Human genes 0.000 claims 2
- 101000851788 Homo sapiens Eukaryotic peptide chain release factor GTP-binding subunit ERF3A Proteins 0.000 claims 2
- 208000034578 Multiple myelomas Diseases 0.000 claims 2
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 2
- 208000033826 Promyelocytic Acute Leukemia Diseases 0.000 claims 2
- 206010060862 Prostate cancer Diseases 0.000 claims 2
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 2
- 239000003795 chemical substances by application Substances 0.000 claims 2
- 125000001041 indolyl group Chemical group 0.000 claims 2
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 1
- 206010005003 Bladder cancer Diseases 0.000 claims 1
- 206010005949 Bone cancer Diseases 0.000 claims 1
- 208000018084 Bone neoplasm Diseases 0.000 claims 1
- 206010008342 Cervix carcinoma Diseases 0.000 claims 1
- 208000006332 Choriocarcinoma Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 108090000695 Cytokines Proteins 0.000 claims 1
- 102000004127 Cytokines Human genes 0.000 claims 1
- 102100037799 DNA-binding protein Ikaros Human genes 0.000 claims 1
- 206010014733 Endometrial cancer Diseases 0.000 claims 1
- 206010014759 Endometrial neoplasm Diseases 0.000 claims 1
- 101000599038 Homo sapiens DNA-binding protein Ikaros Proteins 0.000 claims 1
- 101000740178 Homo sapiens Sal-like protein 4 Proteins 0.000 claims 1
- 101000599042 Homo sapiens Zinc finger protein Aiolos Proteins 0.000 claims 1
- 108010002386 Interleukin-3 Proteins 0.000 claims 1
- 102100039064 Interleukin-3 Human genes 0.000 claims 1
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 208000002231 Muscle Neoplasms Diseases 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 206010038389 Renal cancer Diseases 0.000 claims 1
- 102100037192 Sal-like protein 4 Human genes 0.000 claims 1
- 208000000453 Skin Neoplasms Diseases 0.000 claims 1
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 1
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 1
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 1
- 208000002495 Uterine Neoplasms Diseases 0.000 claims 1
- 102100037798 Zinc finger protein Aiolos Human genes 0.000 claims 1
- 239000003242 anti bacterial agent Substances 0.000 claims 1
- 239000000427 antigen Substances 0.000 claims 1
- 102000036639 antigens Human genes 0.000 claims 1
- 108091007433 antigens Proteins 0.000 claims 1
- 239000002246 antineoplastic agent Substances 0.000 claims 1
- 229940041181 antineoplastic drug Drugs 0.000 claims 1
- 230000003115 biocidal effect Effects 0.000 claims 1
- 201000010881 cervical cancer Diseases 0.000 claims 1
- 238000002512 chemotherapy Methods 0.000 claims 1
- 208000029742 colonic neoplasm Diseases 0.000 claims 1
- 201000010918 connective tissue cancer Diseases 0.000 claims 1
- 239000003246 corticosteroid Substances 0.000 claims 1
- 229940111134 coxibs Drugs 0.000 claims 1
- 239000003255 cyclooxygenase 2 inhibitor Substances 0.000 claims 1
- 206010017758 gastric cancer Diseases 0.000 claims 1
- 201000005787 hematologic cancer Diseases 0.000 claims 1
- 208000024200 hematopoietic and lymphoid system neoplasm Diseases 0.000 claims 1
- 230000002519 immonomodulatory effect Effects 0.000 claims 1
- 229960003444 immunosuppressant agent Drugs 0.000 claims 1
- 230000001861 immunosuppressant effect Effects 0.000 claims 1
- 239000003018 immunosuppressive agent Substances 0.000 claims 1
- 238000009169 immunotherapy Methods 0.000 claims 1
- 201000010982 kidney cancer Diseases 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 201000002077 muscle cancer Diseases 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 201000008814 placenta cancer Diseases 0.000 claims 1
- 238000001959 radiotherapy Methods 0.000 claims 1
- 201000000849 skin cancer Diseases 0.000 claims 1
- 201000011549 stomach cancer Diseases 0.000 claims 1
- 230000001225 therapeutic effect Effects 0.000 claims 1
- 201000005112 urinary bladder cancer Diseases 0.000 claims 1
- 206010046766 uterine cancer Diseases 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| PL2020000066 | 2020-08-03 | ||
| PLPCT/PL2020/000066 | 2020-08-03 | ||
| PCT/EP2021/071694 WO2022029138A1 (en) | 2020-08-03 | 2021-08-03 | Low molecular weight protein degraders and their applications |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2023541522A JP2023541522A (ja) | 2023-10-03 |
| JPWO2022029138A5 true JPWO2022029138A5 (pt) | 2024-07-25 |
Family
ID=72193535
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2023507550A Pending JP2023541522A (ja) | 2020-08-03 | 2021-08-03 | 低分子量タンパク質分解物質及びその適用 |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US20240294489A1 (pt) |
| EP (1) | EP4188373A1 (pt) |
| JP (1) | JP2023541522A (pt) |
| KR (1) | KR20230048373A (pt) |
| CN (1) | CN116457344A (pt) |
| AU (1) | AU2021319847A1 (pt) |
| BR (1) | BR112023001956A2 (pt) |
| CA (1) | CA3186919A1 (pt) |
| IL (1) | IL300308A (pt) |
| MX (1) | MX2023001401A (pt) |
| WO (1) | WO2022029138A1 (pt) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2023274246A1 (zh) * | 2021-06-28 | 2023-01-05 | 成都分迪药业有限公司 | 酰胺类化合物及其用途 |
| CN116082301A (zh) * | 2021-11-05 | 2023-05-09 | 上海美志医药科技有限公司 | 具有降解gspt1活性的化合物及其应用 |
| EP4452415A1 (en) | 2021-12-22 | 2024-10-30 | Gilead Sciences, Inc. | Ikaros zinc finger family degraders and uses thereof |
| CN118488946A (zh) * | 2021-12-22 | 2024-08-13 | 吉利德科学公司 | Ikaros锌指家族降解剂及其用途 |
| IL315083A (en) | 2022-03-17 | 2024-10-01 | Gilead Sciences Inc | The IKAROS family of zinc fingers degrades and uses them |
| CN114835680A (zh) * | 2022-04-29 | 2022-08-02 | 成都分迪药业有限公司 | 卤素取代异吲哚啉化合物及其应用 |
| CN115636811A (zh) * | 2022-08-17 | 2023-01-24 | 成都分迪药业有限公司 | 异吲哚啉苄胺衍生物的合成方法 |
| WO2024054832A1 (en) | 2022-09-09 | 2024-03-14 | Innovo Therapeutics, Inc. | CK1α AND DUAL CK1α / GSPT1 DEGRADING COMPOUNDS |
| WO2024096753A1 (en) | 2022-11-02 | 2024-05-10 | Captor Therapeutics S.A. | Nek7 degraders and methods of use thereof |
Family Cites Families (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5635517B1 (en) | 1996-07-24 | 1999-06-29 | Celgene Corp | Method of reducing TNFalpha levels with amino substituted 2-(2,6-dioxopiperidin-3-YL)-1-oxo-and 1,3-dioxoisoindolines |
| US6306663B1 (en) | 1999-02-12 | 2001-10-23 | Proteinex, Inc. | Controlling protein levels in eucaryotic organisms |
| US7323479B2 (en) | 2002-05-17 | 2008-01-29 | Celgene Corporation | Methods for treatment and management of brain cancer using 1-oxo-2-(2,6-dioxopiperidin-3-yl)-4-methylisoindoline |
| CL2007002513A1 (es) | 2006-08-30 | 2008-04-04 | Celgene Corp Soc Organizada Ba | Compuestos derivados de isoindolina sustituidos, compuestos intermediarios; composicion farmaceutica; y uso en el tratamiento y prevencion de enfermedades tales como cancer, dolor, degeneracion macular, entre otras. |
| US8877780B2 (en) * | 2006-08-30 | 2014-11-04 | Celgene Corporation | 5-substituted isoindoline compounds |
| KR101414786B1 (ko) | 2006-09-26 | 2014-07-03 | 셀진 코포레이션 | 항암제로서의 5-치환 퀴나졸린온 유도체 |
| CN104693193B (zh) | 2010-02-11 | 2018-09-18 | 细胞基因公司 | 芳基甲氧基异吲哚啉衍生物和包括其的组合物及它们的使用方法 |
| US9499514B2 (en) * | 2014-07-11 | 2016-11-22 | Celgene Corporation | Antiproliferative compounds and methods of use thereof |
| 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 |
| WO2017197056A1 (en) * | 2016-05-10 | 2017-11-16 | C4 Therapeutics, Inc. | Bromodomain targeting degronimers for target protein degradation |
| CN109562107A (zh) * | 2016-05-10 | 2019-04-02 | C4医药公司 | 用于靶蛋白降解的杂环降解决定子体 |
| EP3577109A4 (en) * | 2017-01-31 | 2020-11-18 | Arvinas Operations, Inc. | CEREBLON LIGANDS AND BIFUNCTIONAL CONNECTIONS THEREOF |
| WO2018169777A1 (en) * | 2017-03-14 | 2018-09-20 | Biotheryx, Inc. | Compounds targeting proteins, compositions, methods, and uses thereof |
| EP3641762A4 (en) | 2017-06-20 | 2021-03-10 | C4 Therapeutics, Inc. | N / O BONDED DEGRONS AND DEGRONIMERS FOR PROTEIN DEGRADATION |
| WO2019014100A1 (en) | 2017-07-10 | 2019-01-17 | Celgene Corporation | ANTIPROLIFERATIVE COMPOUNDS AND METHODS OF USE THEREOF |
| US10905684B2 (en) * | 2018-06-13 | 2021-02-02 | Biotheryx, Inc. | Aminoamide compounds |
| CA3125189A1 (en) * | 2018-12-31 | 2020-07-09 | Celgene Corporation | Compositions and methods of use of 2-(4-chlorophenyl)-n-((2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-5yl) methyl)-2,2-difluoroacetamide |
-
2021
- 2021-08-03 EP EP21758624.7A patent/EP4188373A1/en active Pending
- 2021-08-03 IL IL300308A patent/IL300308A/en unknown
- 2021-08-03 BR BR112023001956A patent/BR112023001956A2/pt unknown
- 2021-08-03 CN CN202180067832.3A patent/CN116457344A/zh active Pending
- 2021-08-03 WO PCT/EP2021/071694 patent/WO2022029138A1/en active Application Filing
- 2021-08-03 CA CA3186919A patent/CA3186919A1/en active Pending
- 2021-08-03 JP JP2023507550A patent/JP2023541522A/ja active Pending
- 2021-08-03 MX MX2023001401A patent/MX2023001401A/es unknown
- 2021-08-03 KR KR1020237007785A patent/KR20230048373A/ko active Search and Examination
- 2021-08-03 AU AU2021319847A patent/AU2021319847A1/en active Pending
- 2021-08-03 US US18/040,383 patent/US20240294489A1/en active Pending
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