JPWO2022069520A5 - - Google Patents
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- JPWO2022069520A5 JPWO2022069520A5 JP2023519522A JP2023519522A JPWO2022069520A5 JP WO2022069520 A5 JPWO2022069520 A5 JP WO2022069520A5 JP 2023519522 A JP2023519522 A JP 2023519522A JP 2023519522 A JP2023519522 A JP 2023519522A JP WO2022069520 A5 JPWO2022069520 A5 JP WO2022069520A5
- Authority
- JP
- Japan
- Prior art keywords
- pharma
- formula
- acceptable salt
- compound
- ceutically acceptable
- 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 description 97
- 150000003839 salts Chemical class 0.000 claims description 95
- 241001465754 Metazoa Species 0.000 claims description 33
- 238000011865 proteolysis targeting chimera technique Methods 0.000 claims description 32
- 229940124823 proteolysis targeting chimeric molecule Drugs 0.000 claims description 32
- 108010026668 snake venom protein C activator Proteins 0.000 claims description 32
- 206010028980 Neoplasm Diseases 0.000 claims description 30
- 102000006275 Ubiquitin-Protein Ligases Human genes 0.000 claims description 28
- 108010083111 Ubiquitin-Protein Ligases Proteins 0.000 claims description 28
- 238000011282 treatment Methods 0.000 claims description 26
- 125000004432 carbon atom Chemical group C* 0.000 claims description 22
- 239000003814 drug Substances 0.000 claims description 17
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 14
- 125000000217 alkyl group Chemical group 0.000 claims description 13
- -1 6-fluoro-2,4-dioxohexahydropyrimidin-1-yl Chemical group 0.000 claims description 12
- 108091005625 BRD4 Proteins 0.000 claims description 11
- 102100029895 Bromodomain-containing protein 4 Human genes 0.000 claims description 11
- 239000008194 pharmaceutical composition Substances 0.000 claims description 11
- 201000011510 cancer Diseases 0.000 claims description 10
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims description 9
- 125000005842 heteroatom Chemical group 0.000 claims description 8
- 125000001424 substituent group Chemical group 0.000 claims description 8
- SIKJAQJRHWYJAI-UHFFFAOYSA-N Indole Chemical compound C1=CC=C2NC=CC2=C1 SIKJAQJRHWYJAI-UHFFFAOYSA-N 0.000 claims description 6
- 230000015556 catabolic process Effects 0.000 claims description 6
- 238000006731 degradation reaction Methods 0.000 claims description 6
- 125000000623 heterocyclic group Chemical group 0.000 claims description 6
- 230000002797 proteolythic effect Effects 0.000 claims description 5
- UWYZHKAOTLEWKK-UHFFFAOYSA-N 1,2,3,4-tetrahydroisoquinoline Chemical compound C1=CC=C2CNCCC2=C1 UWYZHKAOTLEWKK-UHFFFAOYSA-N 0.000 claims description 4
- LBUJPTNKIBCYBY-UHFFFAOYSA-N 1,2,3,4-tetrahydroquinoline Chemical compound C1=CC=C2CCCNC2=C1 LBUJPTNKIBCYBY-UHFFFAOYSA-N 0.000 claims description 4
- FCEHBMOGCRZNNI-UHFFFAOYSA-N 1-benzothiophene Chemical compound C1=CC=C2SC=CC2=C1 FCEHBMOGCRZNNI-UHFFFAOYSA-N 0.000 claims description 4
- BAXOFTOLAUCFNW-UHFFFAOYSA-N 1H-indazole Chemical compound C1=CC=C2C=NNC2=C1 BAXOFTOLAUCFNW-UHFFFAOYSA-N 0.000 claims description 4
- MVXVYAKCVDQRLW-UHFFFAOYSA-N 1h-pyrrolo[2,3-b]pyridine Chemical compound C1=CN=C2NC=CC2=C1 MVXVYAKCVDQRLW-UHFFFAOYSA-N 0.000 claims description 4
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical compound C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims description 4
- 125000004429 atom Chemical group 0.000 claims description 4
- IOJUPLGTWVMSFF-UHFFFAOYSA-N benzothiazole Chemical compound C1=CC=C2SC=NC2=C1 IOJUPLGTWVMSFF-UHFFFAOYSA-N 0.000 claims description 4
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 4
- 230000005764 inhibitory process Effects 0.000 claims description 4
- 229920006395 saturated elastomer Polymers 0.000 claims description 4
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 3
- 230000002265 prevention Effects 0.000 claims description 3
- 238000002560 therapeutic procedure Methods 0.000 claims description 3
- KTZQTRPPVKQPFO-UHFFFAOYSA-N 1,2-benzoxazole Chemical compound C1=CC=C2C=NOC2=C1 KTZQTRPPVKQPFO-UHFFFAOYSA-N 0.000 claims description 2
- BCMCBBGGLRIHSE-UHFFFAOYSA-N 1,3-benzoxazole Chemical compound C1=CC=C2OC=NC2=C1 BCMCBBGGLRIHSE-UHFFFAOYSA-N 0.000 claims description 2
- HYZJCKYKOHLVJF-UHFFFAOYSA-N 1H-benzimidazole Chemical compound C1=CC=C2NC=NC2=C1 HYZJCKYKOHLVJF-UHFFFAOYSA-N 0.000 claims description 2
- XLKDJOPOOHHZAN-UHFFFAOYSA-N 1h-pyrrolo[2,3-c]pyridine Chemical compound C1=NC=C2NC=CC2=C1 XLKDJOPOOHHZAN-UHFFFAOYSA-N 0.000 claims description 2
- XWIYUCRMWCHYJR-UHFFFAOYSA-N 1h-pyrrolo[3,2-b]pyridine Chemical compound C1=CC=C2NC=CC2=N1 XWIYUCRMWCHYJR-UHFFFAOYSA-N 0.000 claims description 2
- ASSKVPFEZFQQNQ-UHFFFAOYSA-N 2-benzoxazolinone Chemical compound C1=CC=C2OC(O)=NC2=C1 ASSKVPFEZFQQNQ-UHFFFAOYSA-N 0.000 claims description 2
- KWYHDKDOAIKMQN-UHFFFAOYSA-N N,N,N',N'-tetramethylethylenediamine Chemical compound CN(C)CCN(C)C KWYHDKDOAIKMQN-UHFFFAOYSA-N 0.000 claims description 2
- WNSGNWDQCZVCIF-UHFFFAOYSA-N OC(CCN(C(C=CC(N(CCC(N1)=O)C1=O)=C1)=C1O1)C1=O)=O Chemical compound OC(CCN(C(C=CC(N(CCC(N1)=O)C1=O)=C1)=C1O1)C1=O)=O WNSGNWDQCZVCIF-UHFFFAOYSA-N 0.000 claims description 2
- 125000003342 alkenyl group Chemical group 0.000 claims description 2
- 125000000304 alkynyl group Chemical group 0.000 claims description 2
- RFRXIWQYSOIBDI-UHFFFAOYSA-N benzarone Chemical compound CCC=1OC2=CC=CC=C2C=1C(=O)C1=CC=C(O)C=C1 RFRXIWQYSOIBDI-UHFFFAOYSA-N 0.000 claims description 2
- QRUDEWIWKLJBPS-UHFFFAOYSA-N benzotriazole Chemical compound C1=CC=C2N[N][N]C2=C1 QRUDEWIWKLJBPS-UHFFFAOYSA-N 0.000 claims description 2
- 239000012964 benzotriazole Substances 0.000 claims description 2
- 125000004452 carbocyclyl group Chemical group 0.000 claims description 2
- YRTCKZIKGWZNCU-UHFFFAOYSA-N furo[3,2-b]pyridine Chemical compound C1=CC=C2OC=CC2=N1 YRTCKZIKGWZNCU-UHFFFAOYSA-N 0.000 claims description 2
- 125000001183 hydrocarbyl group Chemical group 0.000 claims description 2
- UTCSSFWDNNEEBH-UHFFFAOYSA-N imidazo[1,2-a]pyridine Chemical compound C1=CC=CC2=NC=CN21 UTCSSFWDNNEEBH-UHFFFAOYSA-N 0.000 claims description 2
- PZOUSPYUWWUPPK-UHFFFAOYSA-N indole Natural products CC1=CC=CC2=C1C=CN2 PZOUSPYUWWUPPK-UHFFFAOYSA-N 0.000 claims description 2
- RKJUIXBNRJVNHR-UHFFFAOYSA-N indolenine Natural products C1=CC=C2CC=NC2=C1 RKJUIXBNRJVNHR-UHFFFAOYSA-N 0.000 claims description 2
- PXZQEOJJUGGUIB-UHFFFAOYSA-N isoindolin-1-one Chemical compound C1=CC=C2C(=O)NCC2=C1 PXZQEOJJUGGUIB-UHFFFAOYSA-N 0.000 claims description 2
- GWVMLCQWXVFZCN-UHFFFAOYSA-N isoindoline Chemical compound C1=CC=C2CNCC2=C1 GWVMLCQWXVFZCN-UHFFFAOYSA-N 0.000 claims description 2
- 102000004169 proteins and genes Human genes 0.000 claims description 2
- 108090000623 proteins and genes Proteins 0.000 claims description 2
- DVUBDHRTVYLIPA-UHFFFAOYSA-N pyrazolo[1,5-a]pyridine Chemical compound C1=CC=CN2N=CC=C21 DVUBDHRTVYLIPA-UHFFFAOYSA-N 0.000 claims description 2
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 claims description 2
- 125000005931 tert-butyloxycarbonyl group Chemical group [H]C([H])([H])C(OC(*)=O)(C([H])([H])[H])C([H])([H])[H] 0.000 claims description 2
- 125000003545 alkoxy group Chemical group 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 description 14
- 238000000034 method Methods 0.000 description 12
- 230000000694 effects Effects 0.000 description 9
- 238000011321 prophylaxis Methods 0.000 description 8
- 230000001740 anti-invasion Effects 0.000 description 6
- 230000001028 anti-proliverative effect Effects 0.000 description 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 6
- 230000002401 inhibitory effect Effects 0.000 description 6
- 239000003795 chemical substances by application Substances 0.000 description 4
- 102100037799 DNA-binding protein Ikaros Human genes 0.000 description 3
- 101000599038 Homo sapiens DNA-binding protein Ikaros Proteins 0.000 description 3
- 230000003413 degradative effect Effects 0.000 description 2
- 230000000593 degrading effect Effects 0.000 description 2
- 230000001225 therapeutic effect Effects 0.000 description 2
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 description 1
- 238000000354 decomposition reaction Methods 0.000 description 1
- GOTYRUGSSMKFNF-UHFFFAOYSA-N lenalidomide Chemical compound C1C=2C(N)=CC=CC=2C(=O)N1C1CCC(=O)NC1=O GOTYRUGSSMKFNF-UHFFFAOYSA-N 0.000 description 1
- 229960004942 lenalidomide Drugs 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US202063085384P | 2020-09-30 | 2020-09-30 | |
| US63/085,384 | 2020-09-30 | ||
| PCT/EP2021/076752 WO2022069520A1 (en) | 2020-09-30 | 2021-09-29 | Compounds and their use in treating cancer |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2023543299A JP2023543299A (ja) | 2023-10-13 |
| JPWO2022069520A5 true JPWO2022069520A5 (https=) | 2024-10-07 |
| JP2023543299A5 JP2023543299A5 (https=) | 2024-10-07 |
Family
ID=78085628
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2023519522A Pending JP2023543299A (ja) | 2020-09-30 | 2021-09-29 | 化合物及び癌の治療におけるそれらの使用 |
Country Status (17)
| Country | Link |
|---|---|
| US (1) | US20230374007A1 (https=) |
| EP (1) | EP4221756A1 (https=) |
| JP (1) | JP2023543299A (https=) |
| KR (1) | KR20230079408A (https=) |
| CN (1) | CN116249554A (https=) |
| AU (2) | AU2021353968B2 (https=) |
| BR (1) | BR112023005708A2 (https=) |
| CA (1) | CA3195695A1 (https=) |
| CL (1) | CL2023000881A1 (https=) |
| CO (1) | CO2023005188A2 (https=) |
| CR (1) | CR20230185A (https=) |
| DO (1) | DOP2023000062A (https=) |
| EC (1) | ECSP23030959A (https=) |
| IL (1) | IL301626A (https=) |
| MX (1) | MX2023003564A (https=) |
| PE (1) | PE20230782A1 (https=) |
| WO (1) | WO2022069520A1 (https=) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN115141179B (zh) * | 2021-03-31 | 2024-09-13 | 江苏恒瑞医药股份有限公司 | 一种新型苯并杂环基类衍生物、其制备方法及其在医药上的应用 |
| CN119301111A (zh) | 2022-03-24 | 2025-01-10 | 葛兰素史密斯克莱知识产权发展有限公司 | 作为protac中的降解决定子的2,4-二氧代四氢嘧啶基衍生物 |
| USD1018676S1 (en) * | 2022-04-15 | 2024-03-19 | Puttshack LTD | Miniature golf hole |
| USD1018746S1 (en) * | 2022-04-15 | 2024-03-19 | Puttshack LTD | Miniature golf hole |
| USD1020957S1 (en) * | 2022-04-15 | 2024-04-02 | Puttshack LTD | Miniature golf hole |
| USD1018747S1 (en) * | 2022-04-15 | 2024-03-19 | Puttshack LTD | Miniature golf hole |
| CN119855812A (zh) * | 2022-09-14 | 2025-04-18 | 海南先声再明医药股份有限公司 | 多并环类化合物及其用途 |
| US20240374588A1 (en) | 2023-04-07 | 2024-11-14 | Astrazeneca Ab | Irak4 protacs |
| TW202515566A (zh) | 2023-06-14 | 2025-04-16 | 瑞典商阿斯特捷利康公司 | Ｓｍａｒｃａ２降解劑及其用途 |
| MX2025015084A (es) * | 2023-06-14 | 2026-02-03 | Astrazeneca Ab | Degradadores de smarca2 y usos de estos |
| WO2025036489A1 (zh) * | 2023-08-17 | 2025-02-20 | 海思科医药集团股份有限公司 | 一种氰基芳香环衍生物及其在医药上的应用 |
| IL326555A (en) | 2023-09-22 | 2026-04-01 | Glaxosmithkline Ip Dev Ltd | Androgen receptor protax |
| CN117430605A (zh) * | 2023-10-26 | 2024-01-23 | 广西天铭药业有限公司 | 一种kras g12c抑制剂amg-510中间体的合成方法 |
| US20250177539A1 (en) * | 2023-12-01 | 2025-06-05 | Astrazeneca Ab | Er degraders and uses thereof |
| WO2025125575A1 (en) | 2023-12-14 | 2025-06-19 | Astrazeneca Ab | Irak4 protacs |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0422263D0 (en) | 2004-10-07 | 2004-11-10 | Glaxo Group Ltd | Novel compounds |
| PH12012502079A1 (en) | 2010-04-16 | 2013-02-11 | Ac Immune Sa | Novel compounds for the treatment of diseases associated with amyloid or amyloid-like proteins |
| JP6509838B2 (ja) | 2013-06-26 | 2019-05-08 | アッヴィ・インコーポレイテッド | Ｂｔｋ阻害薬としての一級カルボキサミド類 |
| ES2826443T3 (es) | 2014-09-25 | 2021-05-18 | Araxes Pharma Llc | Inhibidores de proteínas mutantes KRAS G12C |
| JP6815318B2 (ja) * | 2014-12-23 | 2021-01-20 | ダナ−ファーバー キャンサー インスティテュート，インコーポレイテッド | 二官能性分子によって標的化タンパク質分解を誘導する方法 |
| BR112019015484A2 (pt) * | 2017-01-31 | 2020-04-28 | Arvinas Operations Inc | ligantes de cereblon e compostos bifuncionais compreendendo os mesmos |
| WO2019057757A1 (en) * | 2017-09-20 | 2019-03-28 | Astrazeneca Ab | 1,3-DIHYDROIMIDAZO [4,5-C] CINNOLIN-2-ONE COMPOUNDS AND THEIR USE IN THE TREATMENT OF CANCER |
| WO2019140387A1 (en) * | 2018-01-12 | 2019-07-18 | Kymera Therapeutics, Inc. | Crbn ligands and uses thereof |
| CN120698983A (zh) * | 2018-12-20 | 2025-09-26 | C4医药公司 | 靶向蛋白降解 |
-
2021
- 2021-09-29 EP EP21787317.3A patent/EP4221756A1/en active Pending
- 2021-09-29 BR BR112023005708A patent/BR112023005708A2/pt unknown
- 2021-09-29 KR KR1020237014514A patent/KR20230079408A/ko active Pending
- 2021-09-29 IL IL301626A patent/IL301626A/en unknown
- 2021-09-29 CR CR20230185A patent/CR20230185A/es unknown
- 2021-09-29 WO PCT/EP2021/076752 patent/WO2022069520A1/en not_active Ceased
- 2021-09-29 CN CN202180065971.2A patent/CN116249554A/zh active Pending
- 2021-09-29 US US18/247,014 patent/US20230374007A1/en active Pending
- 2021-09-29 CA CA3195695A patent/CA3195695A1/en active Pending
- 2021-09-29 AU AU2021353968A patent/AU2021353968B2/en active Active
- 2021-09-29 MX MX2023003564A patent/MX2023003564A/es unknown
- 2021-09-29 PE PE2023001220A patent/PE20230782A1/es unknown
- 2021-09-29 JP JP2023519522A patent/JP2023543299A/ja active Pending
-
2023
- 2023-03-24 DO DO2023000062A patent/DOP2023000062A/es unknown
- 2023-03-27 CL CL2023000881A patent/CL2023000881A1/es unknown
- 2023-04-24 CO CONC2023/0005188A patent/CO2023005188A2/es unknown
- 2023-04-27 EC ECSENADI202330959A patent/ECSP23030959A/es unknown
-
2025
- 2025-01-09 AU AU2025200137A patent/AU2025200137A1/en active Pending
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