JPWO2021170109A5 - - Google Patents
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- Publication number
- JPWO2021170109A5 JPWO2021170109A5 JP2022551553A JP2022551553A JPWO2021170109A5 JP WO2021170109 A5 JPWO2021170109 A5 JP WO2021170109A5 JP 2022551553 A JP2022551553 A JP 2022551553A JP 2022551553 A JP2022551553 A JP 2022551553A JP WO2021170109 A5 JPWO2021170109 A5 JP WO2021170109A5
- Authority
- JP
- Japan
- Prior art keywords
- amino
- difluorobenzyl
- indazol
- benzamide
- piperazin
- 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
Links
- -1 N-(5-(3,5-difluorobenzyl)-1H-indazol-3-yl)-4-(4-((1-((2-(2,6-dioxopiperidin-3-yl)- 1,3-dioxoisoindolin-5-yl)methyl)azetidin-3-yl)methyl)piperazin-1-yl)-2-((tetrahydro-2H-pyran-4-yl)amino)benzamide Chemical compound 0.000 claims 22
- KXDAEFPNCMNJSK-UHFFFAOYSA-N Benzamide Chemical compound NC(=O)C1=CC=CC=C1 KXDAEFPNCMNJSK-UHFFFAOYSA-N 0.000 claims 18
- 150000003839 salts Chemical class 0.000 claims 13
- 150000001875 compounds Chemical class 0.000 claims 8
- 125000006716 (C1-C6) heteroalkyl group Chemical group 0.000 claims 4
- 201000010099 disease Diseases 0.000 claims 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 4
- 230000001404 mediated effect Effects 0.000 claims 4
- 206010028980 Neoplasm Diseases 0.000 claims 3
- 201000011510 cancer Diseases 0.000 claims 3
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 2
- 125000006714 (C3-C10) heterocyclyl group Chemical group 0.000 claims 2
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims 2
- 208000002193 Pain Diseases 0.000 claims 2
- 125000003545 alkoxy group Chemical group 0.000 claims 2
- 125000000217 alkyl group Chemical group 0.000 claims 2
- 125000004452 carbocyclyl group Chemical group 0.000 claims 2
- QFJRNHWITCOYTM-UHFFFAOYSA-N C(C1=CC=2C(=O)N(C(=O)C=2C=C1)C1C(=O)NC(=O)CC1)N1CCC(CC1)N1CCN(CC1)C1=CC=C(C(=O)NC=2C3=CC(CC4=CC(=CC(=C4)F)F)=CC=C3NN=2)C(NC2CCOCC2)=C1 Chemical compound C(C1=CC=2C(=O)N(C(=O)C=2C=C1)C1C(=O)NC(=O)CC1)N1CCC(CC1)N1CCN(CC1)C1=CC=C(C(=O)NC=2C3=CC(CC4=CC(=CC(=C4)F)F)=CC=C3NN=2)C(NC2CCOCC2)=C1 QFJRNHWITCOYTM-UHFFFAOYSA-N 0.000 claims 1
- 208000000094 Chronic Pain Diseases 0.000 claims 1
- QRPAHVGMUMOIKN-UHFFFAOYSA-N O=C(C(C(NC1CCOCC1)=C1)=CC=C1N(CC1)CCN1C(C1)CC1(CC1)CN1C(C=C1)=CC(C(N2C(CCC(N3)=O)C3=O)=O)=C1C2=O)NC1=NNC2=CC=C(CC3=CC(F)=CC(F)=C3)C=C12 Chemical compound O=C(C(C(NC1CCOCC1)=C1)=CC=C1N(CC1)CCN1C(C1)CC1(CC1)CN1C(C=C1)=CC(C(N2C(CCC(N3)=O)C3=O)=O)=C1C2=O)NC1=NNC2=CC=C(CC3=CC(F)=CC(F)=C3)C=C12 QRPAHVGMUMOIKN-UHFFFAOYSA-N 0.000 claims 1
- KMSVJJXKUAZDSE-UHFFFAOYSA-N O=C(C(C(NC1CCOCC1)=C1)=CC=C1N(CC1)CCN1C(CC1)CCN1C(C=C1)=CC(C(N2C(CCC(N3)=O)C3=O)=O)=C1C2=O)NC1=NNC2=CC=C(CC3=CC(F)=CC(F)=C3)C=C12 Chemical compound O=C(C(C(NC1CCOCC1)=C1)=CC=C1N(CC1)CCN1C(CC1)CCN1C(C=C1)=CC(C(N2C(CCC(N3)=O)C3=O)=O)=C1C2=O)NC1=NNC2=CC=C(CC3=CC(F)=CC(F)=C3)C=C12 KMSVJJXKUAZDSE-UHFFFAOYSA-N 0.000 claims 1
- YCPLUHIVFNQIAA-UHFFFAOYSA-N O=C(C(C(NC1CCOCC1)=C1)=CC=C1N(CC1)CCN1C1CN(CC(C=C2C(N3C(CCC(N4)=O)C4=O)=O)=CC=C2C3=O)CCC1)NC1=NNC2=CC=C(CC3=CC(F)=CC(F)=C3)C=C12 Chemical compound O=C(C(C(NC1CCOCC1)=C1)=CC=C1N(CC1)CCN1C1CN(CC(C=C2C(N3C(CCC(N4)=O)C4=O)=O)=CC=C2C3=O)CCC1)NC1=NNC2=CC=C(CC3=CC(F)=CC(F)=C3)C=C12 YCPLUHIVFNQIAA-UHFFFAOYSA-N 0.000 claims 1
- IOEDKYXHTFGJII-UHFFFAOYSA-N O=C(C(C(NC1CCOCC1)=C1)=CC=C1N1CCN(CC(C2)OCCN2C(C=C2C(N3C(CCC(N4)=O)C4=O)=O)=CC=C2C3=O)CC1)NC1=NNC2=CC=C(CC3=CC(F)=CC(F)=C3)C=C12 Chemical compound O=C(C(C(NC1CCOCC1)=C1)=CC=C1N1CCN(CC(C2)OCCN2C(C=C2C(N3C(CCC(N4)=O)C4=O)=O)=CC=C2C3=O)CC1)NC1=NNC2=CC=C(CC3=CC(F)=CC(F)=C3)C=C12 IOEDKYXHTFGJII-UHFFFAOYSA-N 0.000 claims 1
- WVCMDDNYBQWYHE-UHFFFAOYSA-N O=C(C(C(NCCF)=C1)=CC=C1N1CCN(CC(C2)CN2C(C=C2)=CC(C(N3C(CCC(N4)=O)C4=O)=O)=C2C3=O)CC1)NC1=NNC2=CC=C(CC3=CC(F)=CC(F)=C3)C=C12 Chemical compound O=C(C(C(NCCF)=C1)=CC=C1N1CCN(CC(C2)CN2C(C=C2)=CC(C(N3C(CCC(N4)=O)C4=O)=O)=C2C3=O)CC1)NC1=NNC2=CC=C(CC3=CC(F)=CC(F)=C3)C=C12 WVCMDDNYBQWYHE-UHFFFAOYSA-N 0.000 claims 1
- WWZSCXKSVMAKTD-UHFFFAOYSA-N O=C(C(C=C1)=CC=C1N1CCN(CC(C2)CN2C(C=C2C(N3C(CCC(N4)=O)C4=O)=O)=CC=C2C3=O)CC1)NC1=NNC2=CC=C(CC3=CC(F)=CC(F)=C3)C=C12 Chemical compound O=C(C(C=C1)=CC=C1N1CCN(CC(C2)CN2C(C=C2C(N3C(CCC(N4)=O)C4=O)=O)=CC=C2C3=O)CC1)NC1=NNC2=CC=C(CC3=CC(F)=CC(F)=C3)C=C12 WWZSCXKSVMAKTD-UHFFFAOYSA-N 0.000 claims 1
- CIGKQAWSXVQMGA-UHFFFAOYSA-N O=C(C(C=C1)=CC=C1N1CCN(CCNC(C=C2)=CC(C(N3C(CCC(N4)=O)C4=O)=O)=C2C3=O)CC1)NC1=NNC2=CC=C(CC3=CC(F)=CC(F)=C3)C=C12 Chemical compound O=C(C(C=C1)=CC=C1N1CCN(CCNC(C=C2)=CC(C(N3C(CCC(N4)=O)C4=O)=O)=C2C3=O)CC1)NC1=NNC2=CC=C(CC3=CC(F)=CC(F)=C3)C=C12 CIGKQAWSXVQMGA-UHFFFAOYSA-N 0.000 claims 1
- DGQYLRDJYAWVJG-UHFFFAOYSA-N O=C(CNC(C=C1)=CC(C(N2C(CCC(N3)=O)C3=O)=O)=C1C2=O)N(CC1)CCN1C(C=C1)=CC=C1C(NC1=NNC2=CC=C(CC3=CC(F)=CC(F)=C3)C=C12)=O Chemical compound O=C(CNC(C=C1)=CC(C(N2C(CCC(N3)=O)C3=O)=O)=C1C2=O)N(CC1)CCN1C(C=C1)=CC=C1C(NC1=NNC2=CC=C(CC3=CC(F)=CC(F)=C3)C=C12)=O DGQYLRDJYAWVJG-UHFFFAOYSA-N 0.000 claims 1
- PHJNHVUVPFJGMV-UHFFFAOYSA-N O=C(CNC(C=C1)=CC(C(N2C(CCC(N3)=O)C3=O)=O)=C1C2=O)N(CC1)CCN1C1=CC=C(C(NC2=NNC3=CC=C(CC4=CC(F)=CC(F)=C4)C=C23)=O)C(NCCF)=C1 Chemical compound O=C(CNC(C=C1)=CC(C(N2C(CCC(N3)=O)C3=O)=O)=C1C2=O)N(CC1)CCN1C1=CC=C(C(NC2=NNC3=CC=C(CC4=CC(F)=CC(F)=C4)C=C23)=O)C(NCCF)=C1 PHJNHVUVPFJGMV-UHFFFAOYSA-N 0.000 claims 1
- 208000003251 Pruritus Diseases 0.000 claims 1
- 108091005682 Receptor kinases Proteins 0.000 claims 1
- DHXVGJBLRPWPCS-UHFFFAOYSA-N Tetrahydropyran Chemical compound C1CCOCC1 DHXVGJBLRPWPCS-UHFFFAOYSA-N 0.000 claims 1
- 102000005937 Tropomyosin Human genes 0.000 claims 1
- 108010030743 Tropomyosin Proteins 0.000 claims 1
- 208000005298 acute pain Diseases 0.000 claims 1
- 125000004567 azetidin-3-yl group Chemical group N1CC(C1)* 0.000 claims 1
- 238000002512 chemotherapy Methods 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000004927 fusion Effects 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 150000002367 halogens Chemical class 0.000 claims 1
- 238000001794 hormone therapy Methods 0.000 claims 1
- 238000009169 immunotherapy Methods 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 230000035772 mutation Effects 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
- 238000001959 radiotherapy Methods 0.000 claims 1
- 125000003107 substituted aryl group Chemical group 0.000 claims 1
- 238000011285 therapeutic regimen Methods 0.000 claims 1
- 238000011282 treatment Methods 0.000 claims 1
- 238000011269 treatment regimen Methods 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2020076748 | 2020-02-26 | ||
| CNPCT/CN2020/076748 | 2020-02-26 | ||
| PCT/CN2021/078240 WO2021170109A1 (en) | 2020-02-26 | 2021-02-26 | Tropomyosin receptor kinase (trk) degradation compounds and methods of use |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2023514872A JP2023514872A (ja) | 2023-04-11 |
| JPWO2021170109A5 true JPWO2021170109A5 (ru) | 2024-03-04 |
Family
ID=77490737
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022551553A Pending JP2023514872A (ja) | 2020-02-26 | 2021-02-26 | トロポミオシン受容体キナーゼ（ｔｒｋ）分解化合物とその使用方法 |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US20230257380A1 (ru) |
| EP (1) | EP4110772A4 (ru) |
| JP (1) | JP2023514872A (ru) |
| KR (1) | KR20230010070A (ru) |
| CN (1) | CN115697989A (ru) |
| AU (1) | AU2021225981A1 (ru) |
| BR (1) | BR112022016901A2 (ru) |
| CA (1) | CA3173262A1 (ru) |
| IL (1) | IL295799A (ru) |
| MX (1) | MX2022010465A (ru) |
| WO (1) | WO2021170109A1 (ru) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US11969472B2 (en) | 2018-08-22 | 2024-04-30 | Cullgen (Shanghai), Inc. | Tropomyosin receptor kinase (TRK) degradation compounds and methods of use |
| CA3110267A1 (en) * | 2018-08-22 | 2020-02-27 | Cullgen (Shanghai), Inc. | Tropomyosin receptor kinase (trk) degradation compounds and methods of use |
| WO2022161414A1 (zh) * | 2021-01-26 | 2022-08-04 | 成都茵创园医药科技有限公司 | 芳香化合物、含其的药物组合物及其应用 |
| CN115504963A (zh) * | 2021-06-22 | 2022-12-23 | 苏州开拓药业股份有限公司 | 一种c-Myc蛋白降解剂 |
| WO2023036175A1 (zh) * | 2021-09-08 | 2023-03-16 | 南京明德新药研发有限公司 | 戊二酰亚胺类化合物与其应用 |
| WO2023055952A1 (en) * | 2021-09-29 | 2023-04-06 | C4 Therapeutics, Inc. | Neurotrophic tyrosine receptor kinase (ntrk) degrading compounds |
| WO2023066350A1 (zh) * | 2021-10-22 | 2023-04-27 | 标新生物医药科技(上海)有限公司 | Crbn e3连接酶配体化合物、基于该配体化合物开发的蛋白降解剂及它们的应用 |
| EP4180428A1 (en) | 2021-11-12 | 2023-05-17 | Genzyme Corporation | Crystalline imidazo[4,5-b]pyridine compound, pharmaceutical compositions, and their use in treating medical conditions |
| WO2023116835A1 (zh) * | 2021-12-24 | 2023-06-29 | 苏州开拓药业股份有限公司 | 一种具有酰亚胺骨架的多蛋白降解剂 |
| TW202333670A (zh) * | 2022-01-04 | 2023-09-01 | 大陸商海思科醫藥集團股份有限公司 | 抑制並降解irak4的化合物及其藥物组合物和藥學上的應用 |
| WO2023193760A1 (en) * | 2022-04-06 | 2023-10-12 | Cullgen (Shanghai) , Inc. | Compounds and methods of treating cancers |
| US20230416240A1 (en) * | 2022-06-16 | 2023-12-28 | Prelude Therapeutics Incorporated | Kat6 targeting compounds |
| CN117510504A (zh) * | 2022-08-05 | 2024-02-06 | 深圳市新樾生物科技有限公司 | 蛋白激酶降解剂、药物及应用 |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2015247817C1 (en) * | 2014-04-14 | 2022-02-10 | Arvinas Operations, Inc. | Imide-based modulators of proteolysis and associated methods of use |
| EP3233840B1 (en) * | 2014-12-16 | 2018-11-21 | Eudendron S.r.l. | Heterocyclic derivatives modulating activity of certain protein kinases |
| CA2979070A1 (en) * | 2015-03-18 | 2016-09-22 | Arvinas, Inc. | Compounds and methods for the enhanced degradation of targeted proteins |
| WO2017197046A1 (en) * | 2016-05-10 | 2017-11-16 | C4 Therapeutics, Inc. | C3-carbon linked glutarimide degronimers for target protein degradation |
| WO2017197051A1 (en) * | 2016-05-10 | 2017-11-16 | C4 Therapeutics, Inc. | Amine-linked c3-glutarimide degronimers for target protein degradation |
| WO2017197055A1 (en) * | 2016-05-10 | 2017-11-16 | C4 Therapeutics, Inc. | Heterocyclic degronimers for target protein degradation |
| KR102538307B1 (ko) * | 2017-12-13 | 2023-05-31 | 상하이테크 유니버시티 | Alk 단백질 분해제 및 암 치료에서의 이의 용도 |
| CA3110267A1 (en) * | 2018-08-22 | 2020-02-27 | Cullgen (Shanghai), Inc. | Tropomyosin receptor kinase (trk) degradation compounds and methods of use |
-
2021
- 2021-02-26 JP JP2022551553A patent/JP2023514872A/ja active Pending
- 2021-02-26 BR BR112022016901A patent/BR112022016901A2/pt unknown
- 2021-02-26 MX MX2022010465A patent/MX2022010465A/es unknown
- 2021-02-26 WO PCT/CN2021/078240 patent/WO2021170109A1/en unknown
- 2021-02-26 US US17/904,822 patent/US20230257380A1/en active Pending
- 2021-02-26 IL IL295799A patent/IL295799A/en unknown
- 2021-02-26 EP EP21760113.7A patent/EP4110772A4/en active Pending
- 2021-02-26 AU AU2021225981A patent/AU2021225981A1/en active Pending
- 2021-02-26 KR KR1020227033274A patent/KR20230010070A/ko unknown
- 2021-02-26 CA CA3173262A patent/CA3173262A1/en active Pending
- 2021-02-26 CN CN202180031506.7A patent/CN115697989A/zh active Pending
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