JPWO2021083949A5 - - Google Patents
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- JPWO2021083949A5 JPWO2021083949A5 JP2022525186A JP2022525186A JPWO2021083949A5 JP WO2021083949 A5 JPWO2021083949 A5 JP WO2021083949A5 JP 2022525186 A JP2022525186 A JP 2022525186A JP 2022525186 A JP2022525186 A JP 2022525186A JP WO2021083949 A5 JPWO2021083949 A5 JP WO2021083949A5
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- Prior art keywords
- alkyl
- cancer
- hydrogen
- linker
- iii
- 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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- 229910052739 hydrogen Inorganic materials 0.000 claims description 60
- 239000001257 hydrogen Substances 0.000 claims description 60
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 54
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims description 42
- 150000003839 salts Chemical class 0.000 claims description 38
- 150000001875 compounds Chemical class 0.000 claims description 36
- 125000000623 heterocyclic group Chemical group 0.000 claims description 36
- 239000003446 ligand Substances 0.000 claims description 28
- 230000008685 targeting Effects 0.000 claims description 28
- 229910052736 halogen Inorganic materials 0.000 claims description 18
- 150000002367 halogens Chemical class 0.000 claims description 18
- 125000001424 substituent group Chemical group 0.000 claims description 16
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 14
- 206010028980 Neoplasm Diseases 0.000 claims description 12
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 11
- 208000035475 disorder Diseases 0.000 claims description 11
- 201000011510 cancer Diseases 0.000 claims description 10
- 239000000203 mixture Substances 0.000 claims description 9
- 206010039491 Sarcoma Diseases 0.000 claims description 8
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 8
- 125000006708 (C5-C14) heteroaryl group Chemical group 0.000 claims description 7
- 101000702559 Homo sapiens Probable global transcription activator SNF2L2 Proteins 0.000 claims description 7
- 102100031021 Probable global transcription activator SNF2L2 Human genes 0.000 claims description 7
- 125000001072 heteroaryl group Chemical group 0.000 claims description 7
- 230000001404 mediated effect Effects 0.000 claims description 7
- 206010009944 Colon cancer Diseases 0.000 claims description 6
- 206010060862 Prostate cancer Diseases 0.000 claims description 6
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims description 6
- 125000004432 carbon atom Chemical group C* 0.000 claims description 6
- 150000002431 hydrogen Chemical class 0.000 claims description 6
- 208000032839 leukemia Diseases 0.000 claims description 6
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 6
- 239000003814 drug Substances 0.000 claims description 5
- 206010006187 Breast cancer Diseases 0.000 claims description 4
- 208000026310 Breast neoplasm Diseases 0.000 claims description 4
- 201000009030 Carcinoma Diseases 0.000 claims description 4
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims description 4
- 206010025323 Lymphomas Diseases 0.000 claims description 4
- 201000004253 NUT midline 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
- 206010035226 Plasma cell myeloma Diseases 0.000 claims description 4
- 208000006664 Precursor Cell Lymphoblastic Leukemia-Lymphoma Diseases 0.000 claims description 4
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- 206010041067 Small cell lung cancer Diseases 0.000 claims description 4
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- 206010057644 Testis cancer Diseases 0.000 claims description 4
- 208000009956 adenocarcinoma Diseases 0.000 claims description 4
- 230000001684 chronic effect Effects 0.000 claims description 4
- 210000001072 colon Anatomy 0.000 claims description 4
- 208000029742 colonic neoplasm Diseases 0.000 claims description 4
- 125000001153 fluoro group Chemical group F* 0.000 claims description 4
- 206010073071 hepatocellular carcinoma Diseases 0.000 claims description 4
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims description 4
- 230000003463 hyperproliferative effect Effects 0.000 claims description 4
- 201000007270 liver cancer Diseases 0.000 claims description 4
- 208000014018 liver neoplasm Diseases 0.000 claims description 4
- 201000005202 lung cancer Diseases 0.000 claims description 4
- 208000020816 lung neoplasm Diseases 0.000 claims description 4
- 201000001441 melanoma Diseases 0.000 claims description 4
- 125000000714 pyrimidinyl group Chemical group 0.000 claims description 4
- 208000000587 small cell lung carcinoma Diseases 0.000 claims description 4
- 201000003120 testicular cancer Diseases 0.000 claims description 4
- 229940124597 therapeutic agent Drugs 0.000 claims description 4
- 230000036210 malignancy Effects 0.000 claims description 3
- 206010000830 Acute leukaemia Diseases 0.000 claims description 2
- 208000024893 Acute lymphoblastic leukemia Diseases 0.000 claims description 2
- 208000014697 Acute lymphocytic leukaemia Diseases 0.000 claims description 2
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims description 2
- 201000003076 Angiosarcoma Diseases 0.000 claims description 2
- 206010003571 Astrocytoma Diseases 0.000 claims description 2
- 208000032791 BCR-ABL1 positive chronic myelogenous leukemia Diseases 0.000 claims description 2
- 206010004146 Basal cell carcinoma Diseases 0.000 claims description 2
- 206010005003 Bladder cancer Diseases 0.000 claims description 2
- 208000003174 Brain Neoplasms Diseases 0.000 claims description 2
- 206010008342 Cervix carcinoma Diseases 0.000 claims description 2
- 208000005243 Chondrosarcoma Diseases 0.000 claims description 2
- 201000009047 Chordoma Diseases 0.000 claims description 2
- 208000006332 Choriocarcinoma Diseases 0.000 claims description 2
- 208000010833 Chronic myeloid leukaemia Diseases 0.000 claims description 2
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims description 2
- 208000009798 Craniopharyngioma Diseases 0.000 claims description 2
- 206010014733 Endometrial cancer Diseases 0.000 claims description 2
- 206010014759 Endometrial neoplasm Diseases 0.000 claims description 2
- 206010014967 Ependymoma Diseases 0.000 claims description 2
- 208000031637 Erythroblastic Acute Leukemia Diseases 0.000 claims description 2
- 208000036566 Erythroleukaemia Diseases 0.000 claims description 2
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims description 2
- 208000032027 Essential Thrombocythemia Diseases 0.000 claims description 2
- 208000006168 Ewing Sarcoma Diseases 0.000 claims description 2
- 206010016654 Fibrosis Diseases 0.000 claims description 2
- 208000032612 Glial tumor Diseases 0.000 claims description 2
- 206010018338 Glioma Diseases 0.000 claims description 2
- 208000001258 Hemangiosarcoma Diseases 0.000 claims description 2
- 208000031671 Large B-Cell Diffuse Lymphoma Diseases 0.000 claims description 2
- 208000018142 Leiomyosarcoma Diseases 0.000 claims description 2
- 208000007054 Medullary Carcinoma Diseases 0.000 claims description 2
- 208000000172 Medulloblastoma Diseases 0.000 claims description 2
- 206010027406 Mesothelioma Diseases 0.000 claims description 2
- 206010054949 Metaplasia Diseases 0.000 claims description 2
- 208000003445 Mouth Neoplasms Diseases 0.000 claims description 2
- 208000034578 Multiple myelomas Diseases 0.000 claims description 2
- 208000033761 Myelogenous Chronic BCR-ABL Positive Leukemia Diseases 0.000 claims description 2
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims description 2
- 208000034176 Neoplasms, Germ Cell and Embryonal Diseases 0.000 claims description 2
- 206010029260 Neuroblastoma Diseases 0.000 claims description 2
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims description 2
- 208000035327 Oestrogen receptor positive breast cancer Diseases 0.000 claims description 2
- 201000010133 Oligodendroglioma Diseases 0.000 claims description 2
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims description 2
- 208000007641 Pinealoma Diseases 0.000 claims description 2
- 208000009052 Precursor T-Cell Lymphoblastic Leukemia-Lymphoma Diseases 0.000 claims description 2
- 208000015634 Rectal Neoplasms Diseases 0.000 claims description 2
- 208000006265 Renal cell carcinoma Diseases 0.000 claims description 2
- 201000000582 Retinoblastoma Diseases 0.000 claims description 2
- 201000010208 Seminoma Diseases 0.000 claims description 2
- 208000000453 Skin Neoplasms Diseases 0.000 claims description 2
- 208000005718 Stomach Neoplasms Diseases 0.000 claims description 2
- 208000029052 T-cell acute lymphoblastic leukemia Diseases 0.000 claims description 2
- 210000001744 T-lymphocyte Anatomy 0.000 claims description 2
- 208000024770 Thyroid neoplasm Diseases 0.000 claims description 2
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims description 2
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims description 2
- 208000002495 Uterine Neoplasms Diseases 0.000 claims description 2
- 208000014070 Vestibular schwannoma Diseases 0.000 claims description 2
- 208000033559 Waldenström macroglobulinemia Diseases 0.000 claims description 2
- 208000008383 Wilms tumor Diseases 0.000 claims description 2
- 230000002159 abnormal effect Effects 0.000 claims description 2
- 208000004064 acoustic neuroma Diseases 0.000 claims description 2
- 208000017733 acquired polycythemia vera Diseases 0.000 claims description 2
- 201000011186 acute T cell leukemia Diseases 0.000 claims description 2
- 208000021841 acute erythroid leukemia Diseases 0.000 claims description 2
- 239000002246 antineoplastic agent Substances 0.000 claims description 2
- 210000003719 b-lymphocyte Anatomy 0.000 claims description 2
- 210000000481 breast Anatomy 0.000 claims description 2
- 208000003362 bronchogenic carcinoma Diseases 0.000 claims description 2
- 201000010881 cervical cancer Diseases 0.000 claims description 2
- 208000006990 cholangiocarcinoma Diseases 0.000 claims description 2
- 208000024207 chronic leukemia Diseases 0.000 claims description 2
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 2
- 208000002445 cystadenocarcinoma Diseases 0.000 claims description 2
- 229940127089 cytotoxic agent Drugs 0.000 claims description 2
- 206010012818 diffuse large B-cell lymphoma Diseases 0.000 claims description 2
- 201000002246 embryonal cancer Diseases 0.000 claims description 2
- 201000004101 esophageal cancer Diseases 0.000 claims description 2
- 201000007281 estrogen-receptor positive breast cancer Diseases 0.000 claims description 2
- 230000004761 fibrosis Effects 0.000 claims description 2
- 201000003444 follicular lymphoma Diseases 0.000 claims description 2
- 206010017758 gastric cancer Diseases 0.000 claims description 2
- 210000004602 germ cell Anatomy 0.000 claims description 2
- 208000005017 glioblastoma Diseases 0.000 claims description 2
- 208000002409 gliosarcoma Diseases 0.000 claims description 2
- 208000025750 heavy chain disease Diseases 0.000 claims description 2
- 201000002222 hemangioblastoma Diseases 0.000 claims description 2
- 125000005844 heterocyclyloxy group Chemical group 0.000 claims description 2
- -1 hydroxy, amino Chemical group 0.000 claims description 2
- 208000012987 lip and oral cavity carcinoma Diseases 0.000 claims description 2
- 206010024627 liposarcoma Diseases 0.000 claims description 2
- 210000004072 lung Anatomy 0.000 claims description 2
- 208000012804 lymphangiosarcoma Diseases 0.000 claims description 2
- 208000003747 lymphoid leukemia Diseases 0.000 claims description 2
- 208000030883 malignant astrocytoma Diseases 0.000 claims description 2
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims description 2
- 208000023356 medullary thyroid gland carcinoma Diseases 0.000 claims description 2
- 206010027191 meningioma Diseases 0.000 claims description 2
- 230000015689 metaplastic ossification Effects 0.000 claims description 2
- 208000025113 myeloid leukemia Diseases 0.000 claims description 2
- 201000000050 myeloid neoplasm Diseases 0.000 claims description 2
- 208000001611 myxosarcoma Diseases 0.000 claims description 2
- 201000008026 nephroblastoma Diseases 0.000 claims description 2
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims description 2
- 201000008968 osteosarcoma Diseases 0.000 claims description 2
- 210000001672 ovary Anatomy 0.000 claims description 2
- 210000000496 pancreas Anatomy 0.000 claims description 2
- 201000002528 pancreatic cancer Diseases 0.000 claims description 2
- 208000008443 pancreatic carcinoma Diseases 0.000 claims description 2
- 208000004019 papillary adenocarcinoma Diseases 0.000 claims description 2
- 201000010198 papillary carcinoma Diseases 0.000 claims description 2
- 239000008194 pharmaceutical composition Substances 0.000 claims description 2
- 208000024724 pineal body neoplasm Diseases 0.000 claims description 2
- 201000004123 pineal gland cancer Diseases 0.000 claims description 2
- 208000037244 polycythemia vera Diseases 0.000 claims description 2
- 230000002062 proliferating effect Effects 0.000 claims description 2
- 210000002307 prostate Anatomy 0.000 claims description 2
- 206010038038 rectal cancer Diseases 0.000 claims description 2
- 201000001275 rectum cancer Diseases 0.000 claims description 2
- 201000009410 rhabdomyosarcoma Diseases 0.000 claims description 2
- 201000008407 sebaceous adenocarcinoma Diseases 0.000 claims description 2
- 201000000849 skin cancer Diseases 0.000 claims description 2
- 206010041823 squamous cell carcinoma Diseases 0.000 claims description 2
- 201000011549 stomach cancer Diseases 0.000 claims description 2
- 201000010965 sweat gland carcinoma Diseases 0.000 claims description 2
- 210000001258 synovial membrane Anatomy 0.000 claims description 2
- 201000002510 thyroid cancer Diseases 0.000 claims description 2
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims description 2
- 210000003932 urinary bladder Anatomy 0.000 claims description 2
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- 206010046766 uterine cancer Diseases 0.000 claims description 2
- 210000004291 uterus Anatomy 0.000 claims description 2
- 230000002861 ventricular Effects 0.000 claims description 2
- 125000005647 linker group Chemical group 0.000 claims 29
- 229910052799 carbon Inorganic materials 0.000 claims 3
- 125000000217 alkyl group Chemical group 0.000 description 10
- 125000003118 aryl group Chemical group 0.000 description 5
- 125000000753 cycloalkyl group Chemical group 0.000 description 3
- 238000000034 method Methods 0.000 description 2
- 239000013543 active substance Substances 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201962927340P | 2019-10-29 | 2019-10-29 | |
| US62/927,340 | 2019-10-29 | ||
| EP19209344.1 | 2019-11-15 | ||
| EP19209344 | 2019-11-15 | ||
| PCT/EP2020/080265 WO2021083949A1 (en) | 2019-10-29 | 2020-10-28 | Bifunctional compounds for the treatment of cancer |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2023511472A JP2023511472A (ja) | 2023-03-20 |
| JP2023511472A5 JP2023511472A5 (https=) | 2023-11-01 |
| JPWO2021083949A5 true JPWO2021083949A5 (https=) | 2023-11-01 |
Family
ID=73020226
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022525186A Pending JP2023511472A (ja) | 2019-10-29 | 2020-10-28 | がんの治療のための二官能性化合物 |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US20230024096A1 (https=) |
| EP (1) | EP4051674A1 (https=) |
| JP (1) | JP2023511472A (https=) |
| CN (1) | CN114728936A (https=) |
| WO (1) | WO2021083949A1 (https=) |
Families Citing this family (29)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2019140380A1 (en) | 2018-01-12 | 2019-07-18 | Kymera Therapeutics, Inc. | Protein degraders and uses thereof |
| WO2020010227A1 (en) | 2018-07-06 | 2020-01-09 | Kymera Therapeutics, Inc. | Protein degraders and uses thereof |
| WO2020251972A1 (en) | 2019-06-10 | 2020-12-17 | Kymera Therapeutics, Inc. | Smarca degraders and uses thereof |
| JP2023507590A (ja) * | 2019-12-17 | 2023-02-24 | オリオニス バイオサイエンシズ，インコーポレイテッド | タンパク質の動員および／または分解を調節する化合物 |
| WO2021133917A1 (en) | 2019-12-23 | 2021-07-01 | Kymera Therapeutics, Inc. | Smarca inhibitors and uses thereof |
| BR112022012410A2 (pt) | 2019-12-23 | 2022-08-30 | Kymera Therapeutics Inc | Degradadores smarca e usos dos mesmos |
| US12528785B2 (en) | 2020-03-19 | 2026-01-20 | Kymera Therapeutics, Inc. | MDM2 degraders and uses thereof |
| WO2021207291A1 (en) * | 2020-04-06 | 2021-10-14 | Foghorn Therapeutics Inc. | Compounds and uses thereof |
| EP4192458A4 (en) | 2020-08-05 | 2024-09-04 | C4 Therapeutics, Inc. | COMPOUNDS FOR TARGETED DEGRADATION OF RET |
| EP4259144A4 (en) * | 2020-12-09 | 2025-08-20 | Kymera Therapeutics Inc | SMARCA DEGRADING AGENTS AND THEIR USES |
| JP2024516995A (ja) * | 2021-05-10 | 2024-04-18 | フォグホーン セラピューティクス インコーポレイテッド | 化合物及びその使用 |
| WO2022243333A1 (en) | 2021-05-17 | 2022-11-24 | Universität Zürich | N6-adenosine-methyltransferase inhibitors in cancer treatment |
| WO2022272133A2 (en) * | 2021-06-25 | 2022-12-29 | Stablix, Inc. | Protein stabilizing compounds containing usp7 ligands |
| WO2023283372A1 (en) * | 2021-07-07 | 2023-01-12 | Biogen Ma Inc. | Compounds for targeting degradation of irak4 proteins |
| US11993599B2 (en) | 2021-08-09 | 2024-05-28 | Genentech, Inc. | Therapeutic compounds |
| WO2023039573A1 (en) * | 2021-09-10 | 2023-03-16 | H. Lee Moffitt Cancer Center And Research Institute, Inc. | Compounds for targeted degradation of taf1 |
| CN117384161A (zh) * | 2022-07-04 | 2024-01-12 | 华东理工大学 | 靶向降解cdk蛋白的化合物及其应用 |
| IL318530A (en) * | 2022-07-29 | 2025-03-01 | Abbvie Operations Singapore Pte Ltd | Targeted protein degradation of PARP14 for use in therapy |
| WO2024073507A1 (en) | 2022-09-28 | 2024-04-04 | Theseus Pharmaceuticals, Inc. | Macrocyclic compounds and uses thereof |
| CN116120311B (zh) * | 2022-11-28 | 2025-10-24 | 中国药科大学 | 一种靶向降解atr蛋白的双功能化合物及其制法与用途 |
| CN116284202B (zh) * | 2023-03-28 | 2024-07-02 | 华侨大学 | 白桦脂酸的PROTACs化合物及其制备方法和应用 |
| CN121013852A (zh) * | 2023-04-14 | 2025-11-25 | 南京再明医药有限公司 | Brm选择性降解剂及其应用 |
| KR20260022390A (ko) | 2023-06-08 | 2026-02-19 | 누릭스 테라퓨틱스 인코포레이티드 | Smarca2의 선택적 분해제로서의 이작용성 아진 접합체 및 이의 치료적 용도 |
| 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 |
| CN121368481A (zh) * | 2023-06-29 | 2026-01-20 | 丹娜-法伯癌症研究院 | 用于降解dna甲基转移酶1 (dnmt1)的蛋白水解靶向嵌合体(protacs)的合成和体外表征 |
| CN121909199A (zh) * | 2023-09-19 | 2026-04-21 | 南京再明医药有限公司 | Brm选择性降解剂化合物及其应用 |
| WO2025094065A1 (en) | 2023-11-01 | 2025-05-08 | Aurigene Oncology Limited | Amino-substituted pyridazine compounds as smarca2 and/or smarca4 degraders |
| WO2026061475A1 (zh) * | 2024-09-19 | 2026-03-26 | 标新生物医药科技(上海)有限公司 | 含有芳基取代杂芳基的双功能蛋白降解剂及其应用 |
| CN119798218A (zh) * | 2024-12-31 | 2025-04-11 | 南京优氟医药科技有限公司 | 一种e3酶配体-连接链复合物及其制备方法 |
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| US12371426B2 (en) * | 2018-04-26 | 2025-07-29 | Aurigene Discovery Technologies Limited | Pyridazine derivatives as SMARCA2/4 degraders |
| WO2019213005A1 (en) * | 2018-04-30 | 2019-11-07 | Dana-Farber Cancer Institute, Inc. | Small molecule degraders of polybromo-1 (pbrm1) |
| WO2020010227A1 (en) * | 2018-07-06 | 2020-01-09 | Kymera Therapeutics, Inc. | Protein degraders and uses thereof |
| WO2020251969A1 (en) * | 2019-06-10 | 2020-12-17 | Kymera Therapeutics, Inc. | Smarca degraders and uses thereof |
| US20230072658A1 (en) * | 2019-06-10 | 2023-03-09 | Kymera Therapeutics, Inc. | Smarca degraders and uses thereof |
-
2020
- 2020-10-28 EP EP20797473.4A patent/EP4051674A1/en not_active Withdrawn
- 2020-10-28 WO PCT/EP2020/080265 patent/WO2021083949A1/en not_active Ceased
- 2020-10-28 JP JP2022525186A patent/JP2023511472A/ja active Pending
- 2020-10-28 CN CN202080076232.9A patent/CN114728936A/zh active Pending
- 2020-10-28 US US17/771,204 patent/US20230024096A1/en active Pending
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