JP2019510798A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2019510798A5 JP2019510798A5 JP2018552846A JP2018552846A JP2019510798A5 JP 2019510798 A5 JP2019510798 A5 JP 2019510798A5 JP 2018552846 A JP2018552846 A JP 2018552846A JP 2018552846 A JP2018552846 A JP 2018552846A JP 2019510798 A5 JP2019510798 A5 JP 2019510798A5
- Authority
- JP
- Japan
- Prior art keywords
- group
- pharmaceutically acceptable
- solvate
- acceptable salt
- optionally substituted
- 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
Links
- 150000003839 salts Chemical class 0.000 claims description 123
- 239000012453 solvate Substances 0.000 claims description 121
- 150000001875 compounds Chemical class 0.000 claims description 104
- 229910052739 hydrogen Inorganic materials 0.000 claims description 50
- 239000001257 hydrogen Substances 0.000 claims description 50
- 206010028980 Neoplasm Diseases 0.000 claims description 37
- 125000000217 alkyl group Chemical group 0.000 claims description 33
- 201000011510 cancer Diseases 0.000 claims description 27
- 125000005843 halogen group Chemical group 0.000 claims description 27
- 150000002431 hydrogen Chemical class 0.000 claims description 27
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 23
- 125000003545 alkoxy group Chemical group 0.000 claims description 11
- 125000004438 haloalkoxy group Chemical group 0.000 claims description 11
- 125000001188 haloalkyl group Chemical group 0.000 claims description 11
- 229910052799 carbon Inorganic materials 0.000 claims description 10
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims description 10
- 125000001072 heteroaryl group Chemical group 0.000 claims description 9
- 239000008194 pharmaceutical composition Substances 0.000 claims description 9
- 125000005466 alkylenyl group Chemical group 0.000 claims description 8
- 125000004432 carbon atom Chemical group C* 0.000 claims description 8
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 8
- 125000003107 substituted aryl group Chemical group 0.000 claims description 8
- 125000000623 heterocyclic group Chemical group 0.000 claims description 7
- 208000023275 Autoimmune disease Diseases 0.000 claims description 6
- 206010040047 Sepsis Diseases 0.000 claims description 6
- 208000036142 Viral infection Diseases 0.000 claims description 6
- 230000001684 chronic effect Effects 0.000 claims description 6
- 208000035475 disorder Diseases 0.000 claims description 6
- 230000004968 inflammatory condition Effects 0.000 claims description 6
- 230000002062 proliferating effect Effects 0.000 claims description 6
- 230000009385 viral infection Effects 0.000 claims description 6
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 4
- 125000001153 fluoro group Chemical group F* 0.000 claims description 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 3
- 201000010099 disease Diseases 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 125000004404 heteroalkyl group Chemical group 0.000 claims description 2
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 2
- 125000004076 pyridyl group Chemical group 0.000 claims description 2
- 125000000714 pyrimidinyl group Chemical group 0.000 claims description 2
- 125000001544 thienyl group Chemical group 0.000 claims description 2
- -1 alkylenyl compound Chemical class 0.000 claims 3
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 1
- XDTMQSROBMDMFD-UHFFFAOYSA-N Cyclohexane Chemical compound C1CCCCC1 XDTMQSROBMDMFD-UHFFFAOYSA-N 0.000 claims 1
- 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 1
- 206010041067 Small cell lung cancer Diseases 0.000 description 10
- 208000000587 small cell lung carcinoma Diseases 0.000 description 10
- 238000000034 method Methods 0.000 description 6
- 206010000871 Acute monocytic leukaemia Diseases 0.000 description 5
- 208000031261 Acute myeloid leukaemia Diseases 0.000 description 5
- 208000010839 B-cell chronic lymphocytic leukemia Diseases 0.000 description 5
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 description 5
- 206010006187 Breast cancer Diseases 0.000 description 5
- 208000026310 Breast neoplasm Diseases 0.000 description 5
- 208000011691 Burkitt lymphomas Diseases 0.000 description 5
- 206010008342 Cervix carcinoma Diseases 0.000 description 5
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 description 5
- 206010009944 Colon cancer Diseases 0.000 description 5
- 208000001333 Colorectal Neoplasms Diseases 0.000 description 5
- 208000000461 Esophageal Neoplasms Diseases 0.000 description 5
- 208000031422 Lymphocytic Chronic B-Cell Leukemia Diseases 0.000 description 5
- 208000035489 Monocytic Acute Leukemia Diseases 0.000 description 5
- 208000034578 Multiple myelomas Diseases 0.000 description 5
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 description 5
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 description 5
- 206010030155 Oesophageal carcinoma Diseases 0.000 description 5
- 206010033128 Ovarian cancer Diseases 0.000 description 5
- 206010061535 Ovarian neoplasm Diseases 0.000 description 5
- 206010035226 Plasma cell myeloma Diseases 0.000 description 5
- 206010060862 Prostate cancer Diseases 0.000 description 5
- 208000000236 Prostatic Neoplasms Diseases 0.000 description 5
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 description 5
- 210000004027 cell Anatomy 0.000 description 5
- 201000010881 cervical cancer Diseases 0.000 description 5
- 208000032852 chronic lymphocytic leukemia Diseases 0.000 description 5
- 201000004101 esophageal cancer Diseases 0.000 description 5
- 208000032839 leukemia Diseases 0.000 description 5
- 210000003757 neuroblast Anatomy 0.000 description 5
- 0 C[C@@]([C@](C(*)N*)N(**)[C@@]1(*)**)[C@@]11c(cccc2)c2NC1=* Chemical compound C[C@@]([C@](C(*)N*)N(**)[C@@]1(*)**)[C@@]11c(cccc2)c2NC1=* 0.000 description 3
- 239000003814 drug Substances 0.000 description 3
- 229910052757 nitrogen Inorganic materials 0.000 description 3
- 229940124597 therapeutic agent Drugs 0.000 description 2
- JLQHICJMQYMTDQ-RKUZKHJWSA-N O=C([C@@H]([C@@H]1c(cccc2Cl)c2F)NC2(CCCCC2)[C@@]1(c(c(N1)c2)ccc2Cl)C1=O)Nc(cc1)ccc1C(NCCCCOc1cccc2c1CN(C(CCC(N1)=O)C1=O)C2=O)=O Chemical compound O=C([C@@H]([C@@H]1c(cccc2Cl)c2F)NC2(CCCCC2)[C@@]1(c(c(N1)c2)ccc2Cl)C1=O)Nc(cc1)ccc1C(NCCCCOc1cccc2c1CN(C(CCC(N1)=O)C1=O)C2=O)=O JLQHICJMQYMTDQ-RKUZKHJWSA-N 0.000 description 1
- 125000003118 aryl group Chemical group 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2022033173A JP2022078201A (ja) | 2016-04-06 | 2022-03-04 | Mdm2タンパク質分解剤 |
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662318974P | 2016-04-06 | 2016-04-06 | |
| US62/318,974 | 2016-04-06 | ||
| US201662393874P | 2016-09-13 | 2016-09-13 | |
| US62/393,874 | 2016-09-13 | ||
| US201662409571P | 2016-10-18 | 2016-10-18 | |
| US62/409,571 | 2016-10-18 | ||
| PCT/US2017/026274 WO2017176957A1 (en) | 2016-04-06 | 2017-04-06 | Mdm2 protein degraders |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022033173A Division JP2022078201A (ja) | 2016-04-06 | 2022-03-04 | Mdm2タンパク質分解剤 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019510798A JP2019510798A (ja) | 2019-04-18 |
| JP2019510798A5 true JP2019510798A5 (enExample) | 2020-03-19 |
| JP7037500B2 JP7037500B2 (ja) | 2022-03-16 |
Family
ID=58549316
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018552846A Active JP7037500B2 (ja) | 2016-04-06 | 2017-04-06 | Mdm2タンパク質分解剤 |
| JP2022033173A Pending JP2022078201A (ja) | 2016-04-06 | 2022-03-04 | Mdm2タンパク質分解剤 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022033173A Pending JP2022078201A (ja) | 2016-04-06 | 2022-03-04 | Mdm2タンパク質分解剤 |
Country Status (13)
| Country | Link |
|---|---|
| US (2) | US11192898B2 (enExample) |
| EP (1) | EP3440066B1 (enExample) |
| JP (2) | JP7037500B2 (enExample) |
| KR (1) | KR102387316B1 (enExample) |
| CN (2) | CN113788818A (enExample) |
| AU (1) | AU2017246452C1 (enExample) |
| IL (1) | IL262103B (enExample) |
| MX (1) | MX2018012174A (enExample) |
| RU (2) | RU2021102253A (enExample) |
| SG (1) | SG11201808728QA (enExample) |
| UA (1) | UA123786C2 (enExample) |
| WO (1) | WO2017176957A1 (enExample) |
| ZA (1) | ZA201806968B (enExample) |
Families Citing this family (106)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP3440066B1 (en) * | 2016-04-06 | 2022-11-30 | The Regents of The University of Michigan | Mdm2 protein degraders |
| WO2017185036A1 (en) | 2016-04-22 | 2017-10-26 | Dana Farber Cancer Institute, Inc. | Bifunctional molecules for degradation of egfr and methods of use |
| 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 |
| 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 |
| WO2017197036A1 (en) | 2016-05-10 | 2017-11-16 | C4 Therapeutics, Inc. | Spirocyclic degronimers for target protein degradation |
| ES2989988T3 (es) | 2016-05-10 | 2024-11-28 | C4 Therapeutics Inc | Degronímeros heterorocíclicos para la degradación de proteínas diana |
| JP6957620B2 (ja) | 2016-12-01 | 2021-11-02 | アルビナス・オペレーションズ・インコーポレイテッドArvinas Operations, Inc. | エストロゲン受容体分解物質としてのテトラヒドロナフタレン誘導体およびテトラヒドロイソキノリン誘導体 |
| US11173211B2 (en) | 2016-12-23 | 2021-11-16 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of rapidly accelerated Fibrosarcoma polypeptides |
| EP3577109A4 (en) | 2017-01-31 | 2020-11-18 | Arvinas Operations, Inc. | CEREMONY LIGANDS AND BIFUNCTIONAL COMPOUNDS CONTAINING THEM |
| CN118440096A (zh) | 2017-06-20 | 2024-08-06 | 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 |
| ES2992913T3 (en) | 2017-07-10 | 2024-12-19 | Celgene Corp | 4-(4-(4-(((2-(2,6-dioxopiperidin-3-yl)-l-oxoisoindolin-4-yl)oxy)methyl)benzyl)piperazin-l-yl)-3-fluorobenzonitrile as antiproliferative compound |
| WO2019043217A1 (en) | 2017-09-04 | 2019-03-07 | F. Hoffmann-La Roche Ag | DIHYDROBENZIMIDAZOLONES |
| EP3679028A1 (en) | 2017-09-04 | 2020-07-15 | C4 Therapeutics, Inc. | Dihydroquinolinones |
| EP3679026A1 (en) | 2017-09-04 | 2020-07-15 | C4 Therapeutics, Inc. | Glutarimide |
| CA3076613A1 (en) | 2017-09-22 | 2019-03-28 | Kymera Therapeutics, Inc. | Protein degraders and uses thereof |
| US11358948B2 (en) | 2017-09-22 | 2022-06-14 | Kymera Therapeutics, Inc. | CRBN ligands and uses thereof |
| 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 |
| IL315310A (en) | 2017-12-26 | 2024-10-01 | Kymera Therapeutics Inc | Irak degraders and uses thereof |
| EP3737675A4 (en) | 2018-01-12 | 2022-01-05 | Kymera Therapeutics, Inc. | Crbn ligands and uses thereof |
| US11485743B2 (en) | 2018-01-12 | 2022-11-01 | Kymera Therapeutics, Inc. | Protein degraders and uses thereof |
| CN111902141A (zh) | 2018-03-26 | 2020-11-06 | C4医药公司 | 用于ikaros降解的羟脑苷脂结合剂 |
| CN110357889B (zh) | 2018-04-09 | 2022-03-15 | 上海科技大学 | 蛋白降解靶向化合物、其抗肿瘤应用、其中间体及中间体应用 |
| EP3781156A4 (en) | 2018-04-16 | 2022-05-18 | C4 Therapeutics, Inc. | SPIROCYCLIC COMPOUNDS |
| CN111989322B (zh) | 2018-04-23 | 2024-04-02 | 细胞基因公司 | 取代的4-氨基异吲哚啉-1,3-二酮化合物以及它们用于治疗淋巴瘤的用途 |
| EP3787747A4 (en) * | 2018-04-30 | 2022-01-12 | Dana-Farber Cancer Institute, Inc. | POLYBROMO-1 (PBRM1) SMALL MOLECULE DEGRADATION PRODUCTS |
| EP3578561A1 (en) | 2018-06-04 | 2019-12-11 | F. Hoffmann-La Roche AG | Spiro compounds |
| WO2020010177A1 (en) | 2018-07-06 | 2020-01-09 | Kymera Therapeutics, Inc. | Tricyclic crbn ligands and uses thereof |
| WO2020010227A1 (en) | 2018-07-06 | 2020-01-09 | Kymera Therapeutics, Inc. | Protein degraders and uses thereof |
| CN108864113B (zh) * | 2018-08-03 | 2021-08-13 | 南方科技大学 | 一种mdm2-hdac双靶点抑制剂、药物组合物及其制备和用途 |
| US12268665B2 (en) * | 2018-08-08 | 2025-04-08 | Ascentage Pharma (Suzhou) Co., Ltd | Combination of immunotherapies with MDM2 inhibitors |
| CN112912376A (zh) | 2018-08-20 | 2021-06-04 | 阿尔维纳斯运营股份有限公司 | 用于治疗神经变性疾病的具有E3泛素连接酶结合活性并靶向α-突触核蛋白的蛋白水解靶向嵌合(PROTAC)化合物 |
| BR112021003098A2 (pt) | 2018-08-22 | 2021-05-11 | Cullgen (Shanghai), Inc. | compostos de degradação de receptor de tropomiosina quinase (trk) e métodos de uso |
| US11969472B2 (en) | 2018-08-22 | 2024-04-30 | Cullgen (Shanghai), Inc. | Tropomyosin receptor kinase (TRK) degradation compounds and methods of use |
| EP3846800A4 (en) | 2018-09-04 | 2022-08-24 | C4 Therapeutics, Inc. | Compounds for the degradation of brd9 or mth1 |
| CN110963958B (zh) * | 2018-09-30 | 2025-10-10 | 上海长森药业有限公司 | 一种mdm2抑制剂,及其制备方法、药物组合物和应用 |
| CA3112591A1 (en) | 2018-10-08 | 2020-04-16 | The Regents Of The University Of Michigan | Small molecule mdm2 protein degraders |
| CN111018857B (zh) * | 2018-10-09 | 2023-06-02 | 嘉兴优博生物技术有限公司 | 靶向蛋白酶降解平台(ted) |
| US10844039B2 (en) | 2018-11-13 | 2020-11-24 | Biotheryx, Inc. | Substituted isoindolinones |
| TWI750539B (zh) * | 2018-11-23 | 2021-12-21 | 大陸商蘇州亞盛藥業有限公司 | 新穎藥物組成物及其用途 |
| AU2019387370A1 (en) | 2018-11-30 | 2021-06-10 | Nuvation Bio Inc. | Pyrrole and pyrazole compounds and methods of use thereof |
| KR20250167680A (ko) | 2018-11-30 | 2025-12-01 | 카이메라 쎄라퓨틱스 인코포레이티드 | Irak 분해제 및 이의 용도 |
| AU2019399772B2 (en) | 2018-12-14 | 2021-11-04 | Ascentage Pharma (Suzhou) Co., Ltd. | A compound for treating osteoarthritis |
| CN113453679B (zh) | 2018-12-20 | 2025-07-08 | C4医药公司 | 靶向蛋白降解 |
| WO2020160295A1 (en) | 2019-01-30 | 2020-08-06 | Montelino Therapeutics, Llc | Bi-functional compounds and methods for targeted ubiquitination of androgen receptor |
| US11547759B2 (en) | 2019-01-30 | 2023-01-10 | Montelino Therapeutics, Inc. | Bi-functional compounds and methods for targeted ubiquitination of androgen receptor |
| TWI875749B (zh) | 2019-04-05 | 2025-03-11 | 美商凱麥拉醫療公司 | Stat降解劑及其用途 |
| WO2020232115A1 (en) * | 2019-05-14 | 2020-11-19 | Wisconsin Alumni Research Foundation | Bifunctional nutlin-lenalidomide derivatives ((4,5-dihydro-1h-imidazole-1-carbonyl)piperazin-1-yl-[linker]-1-oxoisoindolin-2-yl)piperidine-2,6-dione derivatives) as mdm2 degraders and mdm2-p53 inhibitors for use in cancer therapy |
| WO2020251972A1 (en) | 2019-06-10 | 2020-12-17 | Kymera Therapeutics, Inc. | Smarca degraders and uses thereof |
| CA3144805A1 (en) | 2019-06-28 | 2020-12-30 | Kymera Therapeutics, Inc. | Irak degraders and uses thereof |
| EP3814358B1 (en) * | 2019-07-11 | 2025-09-03 | Ascentage Pharma (Suzhou) Co., Ltd. | Method for preparing 2-indolinospirone compounds and intermediates thereof |
| CN119954801A (zh) | 2019-07-17 | 2025-05-09 | 阿尔维纳斯运营股份有限公司 | Tau蛋白靶向化合物及相关使用方法 |
| IL290789B2 (en) | 2019-08-26 | 2025-09-01 | Arvinas Operations Inc | Methods for treating breast cancer with a history of tetrahydronaphthalene as estrogen receptor-disrupting agents |
| NZ787624A (en) | 2019-10-17 | 2025-07-25 | Arvinas Operations Inc | Bifunctional molecules containing an e3 ubiquitine ligase binding moiety linked to a bcl6 targeting moiety |
| CN112745298B (zh) * | 2019-10-30 | 2024-04-09 | 中国科学院上海药物研究所 | 多取代异吲哚啉类化合物、其制备方法、药物组合物及用途 |
| US11548870B2 (en) | 2019-11-19 | 2023-01-10 | Bristol-Myers Squibb Company | Compounds useful as inhibitors of helios protein |
| AU2020407200A1 (en) | 2019-12-17 | 2022-07-21 | Kymera Therapeutics, Inc. | Irak degraders and uses thereof |
| WO2021127283A2 (en) | 2019-12-17 | 2021-06-24 | Kymera Therapeutics, Inc. | Irak degraders and uses thereof |
| AU2020405129A1 (en) | 2019-12-19 | 2022-06-23 | Arvinas Operations, Inc. | Compounds and methods for the targeted degradation of androgen receptor |
| US11850239B2 (en) | 2019-12-19 | 2023-12-26 | Ascentage Pharma (Suzhou) Co., Ltd. | MDM2 inhibitor and a platinum compound for cancer treatment |
| KR20220151160A (ko) | 2019-12-23 | 2022-11-14 | 카이메라 쎄라퓨틱스 인코포레이티드 | Smarca 분해제 및 이의 용도 |
| GB201919219D0 (en) | 2019-12-23 | 2020-02-05 | Otsuka Pharma Co Ltd | Cancer biomarkers |
| TWI777380B (zh) * | 2020-01-23 | 2022-09-11 | 大陸商蘇州亞盛藥業有限公司 | 2-吲哚啉螺環酮類化合物之結晶形式 |
| US12410171B2 (en) | 2020-02-26 | 2025-09-09 | 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 |
| CN115380026B (zh) * | 2020-03-17 | 2023-11-07 | 南京明德新药研发有限公司 | 蛋白降解调节剂与其使用方法 |
| EP4121043A4 (en) * | 2020-03-19 | 2024-07-24 | Kymera Therapeutics, Inc. | Mdm2 degraders and uses thereof |
| CN113509557A (zh) * | 2020-04-09 | 2021-10-19 | 嘉兴优博生物技术有限公司 | 靶向蛋白酶降解平台(ted) |
| TW202210483A (zh) | 2020-06-03 | 2022-03-16 | 美商凱麥拉醫療公司 | Irak降解劑之結晶型 |
| JP2023534528A (ja) * | 2020-07-20 | 2023-08-09 | 江蘇恒瑞医薬股▲ふん▼有限公司 | 硫黄含有イソインドリン系誘導体、その調製方法及びその医薬的応用 |
| EP4192458A4 (en) | 2020-08-05 | 2024-09-04 | C4 Therapeutics, Inc. | COMPOUNDS FOR TARGETED DEGRADATION OF RET |
| CA3181715A1 (en) | 2020-08-27 | 2022-03-03 | Otsuka Pharmaceutical Co., Ltd. | Biomarkers for cancer therapy using mdm2 antagonists |
| US12180193B2 (en) | 2020-08-28 | 2024-12-31 | Arvinas Operations, Inc. | Accelerating fibrosarcoma protein degrading compounds and associated methods of use |
| US20240024494A1 (en) * | 2020-09-11 | 2024-01-25 | Shanghai Mewsgen Biotechnology Co., Ltd | Small-molecule conjugate and use thereof |
| WO2022120355A1 (en) | 2020-12-02 | 2022-06-09 | Ikena Oncology, Inc. | Tead degraders and uses thereof |
| PH12023500015A1 (en) | 2020-12-30 | 2024-03-11 | Kymera Therapeutics Inc | Irak degraders and uses thereof |
| CN114853731A (zh) * | 2021-02-04 | 2022-08-05 | 上海长森药业有限公司 | 一种双功能mdm2蛋白降解剂,及其制备方法、药物组合物和应用 |
| TW202245788A (zh) | 2021-02-15 | 2022-12-01 | 美商凱麥拉醫療公司 | Irak4降解劑及其用途 |
| GB202103080D0 (en) | 2021-03-04 | 2021-04-21 | Otsuka Pharma Co Ltd | Cancer biomarkers |
| HRP20250796T1 (hr) | 2021-04-06 | 2025-08-29 | Bristol-Myers Squibb Company | Piridinil supstituirani oksoizoindolinski spojevi |
| PE20240639A1 (es) | 2021-04-16 | 2024-04-04 | Arvinas Operations Inc | Moduladores de la proteolisis bcl6 y metodos de uso asociados |
| CN117580592A (zh) | 2021-05-05 | 2024-02-20 | 渤健马萨诸塞州股份有限公司 | 用于靶向布鲁顿酪氨酸激酶降解的化合物 |
| KR20240020735A (ko) | 2021-05-07 | 2024-02-15 | 카이메라 쎄라퓨틱스 인코포레이티드 | Cdk2 분해제 및 그 용도 |
| US20240343733A1 (en) | 2021-07-07 | 2024-10-17 | Biogen Ma Inc. | Compounds for targeting degradation of irak4 proteins |
| EP4366834A1 (en) | 2021-07-07 | 2024-05-15 | Biogen MA Inc. | Compounds for targeting degradation of irak4 proteins |
| IL309666A (en) | 2021-07-09 | 2024-02-01 | Plexium Inc | Aryl compounds and pharmaceutical compositions that modulate ikzf2 |
| US11981672B2 (en) | 2021-09-13 | 2024-05-14 | Montelino Therapeutics Inc. | Bi-functional compounds and methods for targeted ubiquitination of androgen receptor |
| EP4402143A1 (en) | 2021-09-13 | 2024-07-24 | Astrazeneca AB | Spirocyclic compounds |
| WO2023049790A2 (en) * | 2021-09-22 | 2023-03-30 | Kymera Therapeutics, Inc. | Mdm2 degraders and uses thereof |
| JP2024539280A (ja) | 2021-10-25 | 2024-10-28 | カイメラ セラピューティクス, インコーポレイテッド | Tyk2分解剤およびそれらの使用 |
| AR127505A1 (es) | 2021-10-29 | 2024-01-31 | Kymera Therapeutics Inc | Degradadores irak-4 y síntesis de los mismos |
| US20230233546A1 (en) * | 2021-12-15 | 2023-07-27 | Kymera Therapeutics, Inc. | Methods of treating cancer |
| CN113979999B (zh) * | 2021-12-23 | 2022-05-20 | 北京鑫开元医药科技有限公司 | 靶向泛素化降解bcr-abl激酶的化合物及其制备方法、组合物和用途 |
| CA3243560A1 (en) | 2022-01-31 | 2023-08-03 | Kymera Therapeutics, Inc. | Iraqi Degradation Agents and Their Uses |
| WO2023230059A1 (en) * | 2022-05-24 | 2023-11-30 | Newave Pharmaceutical Inc. | Mdm2 degrader |
| WO2024006776A1 (en) | 2022-06-27 | 2024-01-04 | Relay Therapeutics, Inc. | Estrogen receptor alpha degraders and medical use thereof |
| KR20250041622A (ko) | 2022-06-27 | 2025-03-25 | 릴레이 테라퓨틱스, 인크. | 에스트로겐 수용체 알파 분해제 및 그의 용도 |
| WO2024050016A1 (en) | 2022-08-31 | 2024-03-07 | Oerth Bio Llc | Compositions and methods for targeted inhibition and degradation of proteins in an insect cell |
| EP4584258A1 (en) | 2022-09-07 | 2025-07-16 | Arvinas Operations, Inc. | Rapidly accelerated fibrosarcoma (raf) degrading compounds and associated methods of use |
| WO2024064358A1 (en) | 2022-09-23 | 2024-03-28 | Ifm Due, Inc. | Compounds and compositions for treating conditions associated with sting activity |
| WO2024078370A1 (zh) * | 2022-10-13 | 2024-04-18 | 中国科学院上海药物研究所 | 具有取代苯基螺[吲哚啉-3,3'-吡咯烷]结构的小分子化合物 |
| WO2024097948A1 (en) | 2022-11-04 | 2024-05-10 | Roivant Discovery, Inc. | Degraders of mdm2 and uses thereof |
| WO2024148257A1 (en) * | 2023-01-05 | 2024-07-11 | The Wistar Institute Of Anatomy And Biology | Mdm2 targeting protacs |
| WO2024187066A1 (en) * | 2023-03-08 | 2024-09-12 | Regents Of The University Of Michigan | Compounds and compositions as cbp/p300 degraders and uses thereof |
| WO2024197219A1 (en) * | 2023-03-22 | 2024-09-26 | Kymera Therapeutics, Inc. | Mdm2 degraders and uses thereof |
| KR20240166948A (ko) * | 2023-05-18 | 2024-11-26 | 아주대학교산학협력단 | 골 분화 유도 가능한 신규 화합물 |
| WO2025049555A1 (en) | 2023-08-31 | 2025-03-06 | Oerth Bio Llc | Compositions and methods for targeted inhibition and degradation of proteins in an insect cell |
Family Cites Families (92)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5093330A (en) | 1987-06-15 | 1992-03-03 | Ciba-Geigy Corporation | Staurosporine derivatives substituted at methylamino nitrogen |
| US7083983B2 (en) | 1996-07-05 | 2006-08-01 | Cancer Research Campaign Technology Limited | Inhibitors of the interaction between P53 and MDM2 |
| AU716490B2 (en) | 1996-09-13 | 2000-02-24 | Mitsubishi Tanabe Pharma Corporation | Thienotriazolodiazepine compounds and pharmaceutical use thereof |
| US6831155B2 (en) | 1999-12-08 | 2004-12-14 | President And Fellows Of Harvard College | Inhibition of p53 degradation |
| US7091353B2 (en) * | 2000-12-27 | 2006-08-15 | Celgene Corporation | Isoindole-imide compounds, compositions, and uses thereof |
| US20030045552A1 (en) * | 2000-12-27 | 2003-03-06 | Robarge Michael J. | Isoindole-imide compounds, compositions, and uses thereof |
| PL370909A1 (en) | 2001-12-18 | 2005-05-30 | F.Hoffmann-La Roche Ag | Cis-imidazolines as mdm2 inhibitors |
| ES2301717T3 (es) | 2001-12-18 | 2008-07-01 | F. Hoffmann-La Roche Ag | Cis-2,4,5-trifenil-imidazolinas y su utilizacion para el tratamiento de tumores. |
| US8146941B2 (en) * | 2002-05-17 | 2012-04-03 | Steins Karl M | Collapsible trailer |
| WO2003106384A2 (en) | 2002-06-01 | 2003-12-24 | Johns Hopkins University | Novel boronic chalcone derivatives and uses thereof |
| US20040171035A1 (en) | 2002-11-08 | 2004-09-02 | Irm Llc | Methods and compositions for modulating P53 transcription factor |
| US20050227932A1 (en) | 2002-11-13 | 2005-10-13 | Tianbao Lu | Combinational therapy involving a small molecule inhibitor of the MDM2: p53 interaction |
| CA2514374A1 (en) | 2003-02-13 | 2004-09-02 | Government Of The United States Of America, As Represented By The Secret Ary, Department Of Health And Human Services | Deazaflavin compounds and methods of use thereof |
| US6916833B2 (en) | 2003-03-13 | 2005-07-12 | Hoffmann-La Roche Inc. | Substituted piperidines |
| US7425638B2 (en) | 2003-06-17 | 2008-09-16 | Hoffmann-La Roche Inc. | Cis-imidazolines |
| US7132421B2 (en) | 2003-06-17 | 2006-11-07 | Hoffmann-La Roche Inc. | CIS-imidazoles |
| US7829742B2 (en) | 2003-12-22 | 2010-11-09 | Johns Hopkins University | Boronic acid aryl analogs |
| WO2005097820A1 (en) | 2004-04-06 | 2005-10-20 | Korea Research Institute Of Bioscience And Biotechnology | Peptides for inhibiting mdm2 function |
| JP4814228B2 (ja) | 2004-05-18 | 2011-11-16 | エフ.ホフマン−ラ ロシュ アーゲー | 新規cis−イミダゾリン |
| GB0419481D0 (en) | 2004-09-02 | 2004-10-06 | Cancer Rec Tech Ltd | Isoindolin-1-one derivatives |
| CN101023074B (zh) | 2004-09-22 | 2012-10-10 | 詹森药业有限公司 | Mdm2及p53间相互作用的抑制剂 |
| WO2006091646A2 (en) | 2005-02-22 | 2006-08-31 | The Regents Of The University Of Michigan | Small molecule inhibitors of mdm2 and uses thereof |
| US7759383B2 (en) | 2005-02-22 | 2010-07-20 | The Regents Of The University Of Michigan | Small molecule inhibitors of MDM2 and the uses thereof |
| JP4955646B2 (ja) | 2005-03-16 | 2012-06-20 | エフ.ホフマン−ラ ロシュ アーゲー | シス−2,4,5−トリアリール−イミダゾリン及びそれらの抗癌薬としての使用 |
| TWI447120B (zh) | 2005-05-30 | 2014-08-01 | Mitsubishi Tanabe Pharma Corp | 噻吩并三唑并苯二氮呯化合物、其醫藥上之用途 |
| US7576082B2 (en) | 2005-06-24 | 2009-08-18 | Hoffman-La Roche Inc. | Oxindole derivatives |
| US7495007B2 (en) | 2006-03-13 | 2009-02-24 | Hoffmann-La Roche Inc. | Spiroindolinone derivatives |
| WO2007107543A1 (en) | 2006-03-22 | 2007-09-27 | Janssen Pharmaceutica N.V. | Inhibitors of the interaction between mdm2 and p53 |
| CN101528223B (zh) * | 2006-08-30 | 2013-05-01 | 密执安州立大学董事会 | Mdm2的新型小分子抑制剂和其用途 |
| US7737174B2 (en) | 2006-08-30 | 2010-06-15 | The Regents Of The University Of Michigan | Indole inhibitors of MDM2 and the uses thereof |
| US7638548B2 (en) | 2006-11-09 | 2009-12-29 | Hoffmann-La Roche Inc. | Spiroindolinone derivatives |
| AU2007332493A1 (en) | 2006-12-14 | 2008-06-19 | Daiichi Sankyo Company, Limited | Imidazothiazole derivatives |
| KR101444489B1 (ko) | 2007-02-01 | 2014-09-24 | 리스버로직스 코퍼레이션 | 심혈관 질환을 예방 및 치료하기 위한 화합물 |
| WO2008106507A2 (en) | 2007-02-27 | 2008-09-04 | University Of South Florida | Mdm2/mdmx inhibitor peptide |
| KR20090122403A (ko) | 2007-03-29 | 2009-11-27 | 노파르티스 아게 | 증식성 질환의 치료를 위한 3-이미다졸릴-인돌 |
| US7625895B2 (en) | 2007-04-12 | 2009-12-01 | Hoffmann-Le Roche Inc. | Diphenyl-dihydro-imidazopyridinones |
| WO2008130614A2 (en) | 2007-04-20 | 2008-10-30 | University Of Pittsburg-Of The Commonwealth System Of Higher Education | Selective and dual-action p53/mdm2/mdm4 antagonists |
| US7553833B2 (en) | 2007-05-17 | 2009-06-30 | Hoffmann-La Roche Inc. | 3,3-spiroindolinone derivatives |
| CA2694646C (en) * | 2007-07-30 | 2017-09-05 | Ardea Biosciences, Inc. | Combinations of mek inhibitors and raf kinase inhibitors and uses thereof |
| CA2699707C (en) | 2007-09-21 | 2016-05-17 | Janssen Pharmaceutica Nv | Inhibitors of the interaction between mdm2 and p53 |
| JP5478262B2 (ja) | 2007-12-28 | 2014-04-23 | 田辺三菱製薬株式会社 | 抗癌剤 |
| WO2009151069A1 (ja) | 2008-06-12 | 2009-12-17 | 第一三共株式会社 | 4,7-ジアザスピロ[2.5]オクタン環構造を有するイミダゾチアゾール誘導体 |
| GB0811643D0 (en) | 2008-06-25 | 2008-07-30 | Cancer Rec Tech Ltd | New therapeutic agents |
| PT2346837E (pt) | 2008-06-26 | 2015-04-02 | Resverlogix Corp | Métodos de preparação de derivados de quinazolinona |
| EP2421533B1 (en) | 2009-04-22 | 2018-10-17 | Resverlogix Corp. | Novel anti-inflammatory agents |
| DE102009051823A1 (de) | 2009-11-04 | 2011-05-05 | Fraunhofer-Gesellschaft zur Förderung der angewandten Forschung e.V. | Einkristallines Schweißen von direktional verfestigten Werkstoffen |
| GB0919434D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
| GB0919426D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
| GB0919432D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Use |
| GB0919423D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
| US9102677B2 (en) | 2009-11-05 | 2015-08-11 | Glaxosmithkline Llc | Benzodiazepine bromodomain inhibitor |
| JP2013510860A (ja) | 2009-11-12 | 2013-03-28 | ザ、リージェンツ、オブ、ザ、ユニバーシティ、オブ、ミシガン | スピロ−オキシインドールmdm2アンタゴニスト |
| US20110118283A1 (en) | 2009-11-17 | 2011-05-19 | Qingjie Ding | Substituted Pyrrolidine-2-Carboxamides |
| US8088815B2 (en) * | 2009-12-02 | 2012-01-03 | Hoffman-La Roche Inc. | Spiroindolinone pyrrolidines |
| CN104311562B (zh) | 2010-05-14 | 2017-07-04 | 达那-法伯癌症研究所 | 用于治疗瘤形成、炎性疾病和其他失调的组合物和方法 |
| US20130252331A1 (en) | 2010-05-14 | 2013-09-26 | James Elliott Bradner | Compositions and methods for modulating metabolism |
| EP2569434B1 (en) | 2010-05-14 | 2019-09-04 | Dana-Farber Cancer Institute, Inc. | Compositions and methods for treating leukemia and related disorders |
| JO2998B1 (ar) * | 2010-06-04 | 2016-09-05 | Amgen Inc | مشتقات بيبيريدينون كمثبطات mdm2 لعلاج السرطان |
| EP2585465B1 (en) | 2010-06-22 | 2014-11-12 | GlaxoSmithKline LLC | Benzotriazolodiazepine compounds inhibitors of bromodomains |
| UY33725A (es) | 2010-11-12 | 2012-06-29 | Sanofi Sa | Antagonistas de mdm2 de espiro-oxindol |
| US9249161B2 (en) | 2010-12-02 | 2016-02-02 | Constellation Pharmaceuticals, Inc. | Bromodomain inhibitors and uses thereof |
| AR084070A1 (es) | 2010-12-02 | 2013-04-17 | Constellation Pharmaceuticals Inc | Inhibidores del bromodominio y usos de los mismos |
| EP2677865A4 (en) | 2011-02-23 | 2015-04-22 | Icahn School Med Mount Sinai | BROMODOMAIN INHIBITORS AS MODULATORS OF GENE EXPRESSION |
| RU2612534C2 (ru) * | 2011-03-10 | 2017-03-09 | Дайити Санкио Компани, Лимитед | Диспиропирролидиновые производные |
| US9422292B2 (en) | 2011-05-04 | 2016-08-23 | Constellation Pharmaceuticals, Inc. | Bromodomain inhibitors and uses thereof |
| MX346375B (es) * | 2011-05-11 | 2017-03-16 | Univ Michigan Regents | Antagonistas de espiro-oxindol de mdm2. |
| WO2012174487A2 (en) | 2011-06-17 | 2012-12-20 | Constellation Pharmaceuticals, Inc. | Bromodomain inhibitors and uses thereof |
| GB201114103D0 (en) | 2011-08-17 | 2011-09-28 | Glaxosmithkline Llc | Novel compounds |
| WO2013027168A1 (en) | 2011-08-22 | 2013-02-28 | Pfizer Inc. | Novel heterocyclic compounds as bromodomain inhibitors |
| WO2013033268A2 (en) | 2011-08-29 | 2013-03-07 | Coferon, Inc. | Bivalent bromodomain ligands, and methods of using same |
| DE102011082013A1 (de) | 2011-09-01 | 2013-03-07 | Bayer Pharma AG | 6H-Thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine |
| WO2013097052A1 (en) | 2011-12-30 | 2013-07-04 | Abbott Laboratories | Bromodomain inhibitors |
| US20130245089A1 (en) | 2012-03-19 | 2013-09-19 | Hoffmann-La Roche Inc. | Method for administration |
| US20140079636A1 (en) * | 2012-04-16 | 2014-03-20 | Dinesh U. Chimmanamada | Targeted therapeutics |
| US20130281399A1 (en) | 2012-04-19 | 2013-10-24 | Rvx Therapeutics Inc. | Treatment of diseases by epigenetic regulation |
| WO2013155695A1 (en) | 2012-04-20 | 2013-10-24 | Abbott Laboratories | Isoindolone derivatives |
| CN104718201A (zh) | 2012-06-12 | 2015-06-17 | 艾伯维公司 | 吡啶酮和哒嗪酮衍生物 |
| MX368703B (es) * | 2013-02-28 | 2019-10-11 | Amgen Inc | Un inhibidor de mdm2 derivado de acido benzoico para el tratamiento del cancer. |
| AU2014249192B2 (en) * | 2013-03-11 | 2017-12-21 | The Regents Of The University Of Michigan | BET bromodomain inhibitors and therapeutic methods using the same |
| CN107074861A (zh) * | 2014-02-28 | 2017-08-18 | 密执安大学评议会 | 作为bet溴结构域抑制剂的9h嘧啶并[4,5‑b]吲哚和相关类似物 |
| EP3129380B1 (en) | 2014-04-11 | 2018-11-28 | Boehringer Ingelheim International Gmbh | Spiro[3h-indole-3,2'-pyrrolidin]-2(1h)-one derivatives and their use as mdm2-p53 inhibitors |
| US20150291562A1 (en) | 2014-04-14 | 2015-10-15 | Arvinas, Inc. | Imide-based modulators of proteolysis and associated methods of use |
| US20160058872A1 (en) * | 2014-04-14 | 2016-03-03 | Arvinas, Inc. | Imide-based modulators of proteolysis and associated methods of use |
| JP6694827B2 (ja) * | 2014-04-17 | 2020-05-20 | ザ リージェンツ オブ ザ ユニバーシティー オブ ミシガン | Mdm2阻害剤及びそれを使用する治療方法 |
| JP6503386B2 (ja) | 2014-07-03 | 2019-04-17 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | MDM2−p53阻害剤としての新しいスピロ[3H−インドール−3,2’−ピロリジン]−2(1H)−オン化合物および誘導体 |
| WO2016028391A2 (en) * | 2014-08-18 | 2016-02-25 | Hudson Biopharma Inc. | Spiropyrrolidines as mdm2 inhibitors |
| CN107001385B (zh) | 2014-08-21 | 2020-03-13 | 勃林格殷格翰国际有限公司 | 作为mdm2-p53抑制剂的螺-[3h-吲哚-3,2’-吡咯烷]-2(1h)-酮化合物及其衍生物 |
| WO2016138332A1 (en) * | 2015-02-27 | 2016-09-01 | The Regents Of The University Of Michigan | 9h-pyrimido [4,5-b] indoles as bet bromodomain inhibitors |
| EP3337476A4 (en) * | 2015-08-19 | 2019-09-04 | Arvinas, Inc. | Compounds and methods for the targeted degradation of bromodomain-containing proteins |
| EP3440066B1 (en) * | 2016-04-06 | 2022-11-30 | The Regents of The University of Michigan | Mdm2 protein degraders |
| EP3440082A1 (en) * | 2016-04-06 | 2019-02-13 | The Regents of The University of Michigan | Monofunctional intermediates for ligand-dependent target protein degradation |
| CA3112591A1 (en) * | 2018-10-08 | 2020-04-16 | The Regents Of The University Of Michigan | Small molecule mdm2 protein degraders |
-
2017
- 2017-04-06 EP EP17718290.4A patent/EP3440066B1/en active Active
- 2017-04-06 RU RU2021102253A patent/RU2021102253A/ru unknown
- 2017-04-06 CN CN202111145294.3A patent/CN113788818A/zh active Pending
- 2017-04-06 KR KR1020187032122A patent/KR102387316B1/ko active Active
- 2017-04-06 AU AU2017246452A patent/AU2017246452C1/en active Active
- 2017-04-06 SG SG11201808728QA patent/SG11201808728QA/en unknown
- 2017-04-06 CN CN201780034689.1A patent/CN109415336B/zh active Active
- 2017-04-06 MX MX2018012174A patent/MX2018012174A/es unknown
- 2017-04-06 UA UAA201810884A patent/UA123786C2/uk unknown
- 2017-04-06 US US16/091,541 patent/US11192898B2/en active Active
- 2017-04-06 WO PCT/US2017/026274 patent/WO2017176957A1/en not_active Ceased
- 2017-04-06 RU RU2018138735A patent/RU2743432C2/ru active
- 2017-04-06 JP JP2018552846A patent/JP7037500B2/ja active Active
-
2018
- 2018-10-03 IL IL262103A patent/IL262103B/en active IP Right Grant
- 2018-10-18 ZA ZA2018/06968A patent/ZA201806968B/en unknown
-
2021
- 2021-08-31 US US17/462,355 patent/US20220411432A1/en active Pending
-
2022
- 2022-03-04 JP JP2022033173A patent/JP2022078201A/ja active Pending
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2019510798A5 (enExample) | ||
| RU2021102253A (ru) | Деструкторы белка mdm2 | |
| JP2019526615A5 (enExample) | ||
| IL274936B2 (en) | Transmuted heterocyclic bicyclic compounds as prmt5 inhibitors | |
| JP2020007311A5 (enExample) | ||
| JP2019526616A5 (enExample) | ||
| JP2016538313A5 (enExample) | ||
| JP2016505512A5 (enExample) | ||
| JP2006524660A5 (enExample) | ||
| JP2016525135A5 (enExample) | ||
| ME02838B (me) | 3,4-dihidroizokinolin-2(1h)-ilni spojevi | |
| JP2019512505A5 (enExample) | ||
| JP2016523974A5 (enExample) | ||
| JP2016506962A5 (enExample) | ||
| JP2019511528A5 (enExample) | ||
| JP2015514808A5 (enExample) | ||
| FI3436461T3 (fi) | Pyrrolotriatsiiniyhdisteitä tam-inhibiittoreina | |
| JP2017508789A5 (enExample) | ||
| JP2013542996A5 (enExample) | ||
| RU2014105624A (ru) | Соединения индазола, способ их применения и фармацевтическая композиция | |
| JP2017528487A5 (enExample) | ||
| EA031030B1 (ru) | Ингибиторы фактора в комплемента на основе производных пиперидинилиндола и их применение | |
| RU2012117398A (ru) | Бензоксазепиновые ингибиторы pi3 и способы применения | |
| WO2016161361A4 (en) | Compositions and methods of targeting mutant k-ras | |
| RU2018138828A (ru) | Уменьшение массы опухоли путем введения ccr1 антагонистов в комбинации с pd-1 ингибиторами или pd-l1 ингибиторами |