JPWO2021086785A5 - - Google Patents
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- JPWO2021086785A5 JPWO2021086785A5 JP2022523943A JP2022523943A JPWO2021086785A5 JP WO2021086785 A5 JPWO2021086785 A5 JP WO2021086785A5 JP 2022523943 A JP2022523943 A JP 2022523943A JP 2022523943 A JP2022523943 A JP 2022523943A JP WO2021086785 A5 JPWO2021086785 A5 JP WO2021086785A5
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- JP
- Japan
- Prior art keywords
- formula
- exist
- alkyldiyl
- iii
- cancer
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- 229910052739 hydrogen Inorganic materials 0.000 claims description 46
- 239000001257 hydrogen Substances 0.000 claims description 46
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 45
- 150000001875 compounds Chemical class 0.000 claims description 40
- 150000003839 salts Chemical class 0.000 claims description 36
- 125000000623 heterocyclic group Chemical group 0.000 claims description 30
- 239000003446 ligand Substances 0.000 claims description 26
- 230000008685 targeting Effects 0.000 claims description 26
- 206010028980 Neoplasm Diseases 0.000 claims description 17
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims description 14
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 14
- 125000001424 substituent group Chemical group 0.000 claims description 14
- 229910052736 halogen Inorganic materials 0.000 claims description 12
- 150000002367 halogens Chemical class 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 9
- 201000009030 Carcinoma Diseases 0.000 claims description 8
- 208000032839 leukemia Diseases 0.000 claims description 8
- 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
- 230000001404 mediated effect Effects 0.000 claims description 7
- 206010060862 Prostate cancer Diseases 0.000 claims description 6
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims description 6
- 206010039491 Sarcoma Diseases 0.000 claims description 6
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- 206010073071 hepatocellular carcinoma Diseases 0.000 claims description 6
- 231100000844 hepatocellular carcinoma Toxicity 0.000 claims description 6
- 230000036210 malignancy Effects 0.000 claims description 6
- 239000000203 mixture Substances 0.000 claims description 6
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 6
- 206010009944 Colon cancer Diseases 0.000 claims description 5
- 239000003814 drug Substances 0.000 claims description 5
- 125000001072 heteroaryl group Chemical group 0.000 claims description 5
- 206010006187 Breast cancer Diseases 0.000 claims description 4
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- 206010058467 Lung neoplasm malignant Diseases 0.000 claims description 4
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- 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
- 208000008938 Rhabdoid tumor Diseases 0.000 claims description 4
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- 230000003463 hyperproliferative effect Effects 0.000 claims description 4
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 4
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- 201000001441 melanoma Diseases 0.000 claims description 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 4
- 239000008194 pharmaceutical composition Substances 0.000 claims description 4
- 208000000587 small cell lung carcinoma Diseases 0.000 claims description 4
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims description 4
- 229940124597 therapeutic agent Drugs 0.000 claims description 4
- 210000001072 colon Anatomy 0.000 claims description 3
- 208000029742 colonic neoplasm Diseases 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
- 206010004593 Bile duct cancer 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
- 206010058314 Dysplasia Diseases 0.000 claims description 2
- 201000009051 Embryonal Carcinoma 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
- 201000008808 Fibrosarcoma 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
- 206010025323 Lymphomas 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
- 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
- 206010041067 Small cell lung cancer 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
- 208000024313 Testicular Neoplasms Diseases 0.000 claims description 2
- 201000000331 Testicular germ cell cancer Diseases 0.000 claims description 2
- 206010057644 Testis cancer Diseases 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
- 125000003118 aryl group Chemical group 0.000 claims description 2
- 210000003719 b-lymphocyte Anatomy 0.000 claims description 2
- 201000007180 bile duct carcinoma Diseases 0.000 claims description 2
- 210000001185 bone marrow 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
- 208000024207 chronic leukemia Diseases 0.000 claims description 2
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 2
- 125000000753 cycloalkyl group Chemical group 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
- 208000037828 epithelial carcinoma 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
- 201000003444 follicular lymphoma Diseases 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
- 208000012987 lip and oral cavity carcinoma Diseases 0.000 claims description 2
- 206010024627 liposarcoma Diseases 0.000 claims description 2
- 201000007270 liver cancer Diseases 0.000 claims description 2
- 208000014018 liver neoplasm 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
- 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
- 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
- 201000010198 papillary carcinoma Diseases 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
- 206010041823 squamous cell carcinoma Diseases 0.000 claims description 2
- 206010042863 synovial sarcoma Diseases 0.000 claims description 2
- 201000003120 testicular 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
- 201000005112 urinary bladder cancer Diseases 0.000 claims description 2
- 206010046766 uterine cancer Diseases 0.000 claims description 2
- 210000004291 uterus Anatomy 0.000 claims description 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 description 26
- 238000000034 method Methods 0.000 description 3
- 125000006708 (C5-C14) heteroaryl group Chemical group 0.000 description 2
- 239000013543 active substance Substances 0.000 description 1
- 125000003545 alkoxy group Chemical group 0.000 description 1
- 230000000112 colonic effect Effects 0.000 description 1
- 238000004519 manufacturing process Methods 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP19205545 | 2019-10-28 | ||
| EP19205545.7 | 2019-10-28 | ||
| PCT/US2020/057356 WO2021086785A1 (en) | 2019-10-28 | 2020-10-26 | Bifunctional compounds |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2023511471A JP2023511471A (ja) | 2023-03-20 |
| JP2023511471A5 JP2023511471A5 (https=) | 2023-10-31 |
| JPWO2021086785A5 true JPWO2021086785A5 (https=) | 2023-10-31 |
Family
ID=68382246
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022523943A Pending JP2023511471A (ja) | 2019-10-28 | 2020-10-26 | 二官能性化合物 |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US20230002367A1 (https=) |
| EP (1) | EP4054724A4 (https=) |
| JP (1) | JP2023511471A (https=) |
| CN (1) | CN114599428A (https=) |
| WO (1) | WO2021086785A1 (https=) |
Families Citing this family (19)
| 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 |
| 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 |
| 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 |
| US11993599B2 (en) | 2021-08-09 | 2024-05-28 | Genentech, Inc. | Therapeutic compounds |
| WO2023129506A1 (en) * | 2021-12-28 | 2023-07-06 | Board Of Regents, The University Of Texas System | Potent and selective smarca2 degrading chimeric molecules as cancer therapeutics |
| EP4476225A4 (en) * | 2022-02-09 | 2026-01-14 | Aurigene Oncology Ltd | PYRIDAZINE 3-SUBSTITUTED COMPOUNDS USED AS SMARCA2 AND/OR SMARCA4 DEGRADING AGENTS |
| KR20250023362A (ko) * | 2022-06-15 | 2025-02-18 | 씨4 테라퓨틱스, 인코포레이티드 | Smarca2의 표적화된 분해를 위한 화합물 |
| CN119384414A (zh) * | 2022-06-30 | 2025-01-28 | 甘李药业股份有限公司 | 一种用作smarca2/4抑制剂的化合物及其应用 |
| WO2024064316A1 (en) | 2022-09-23 | 2024-03-28 | Regents Of The University Of Michigan | Compounds and compositions as smarca2/4 inhibitors and uses thereof |
| WO2024064328A1 (en) | 2022-09-23 | 2024-03-28 | Regents Of The University Of Michigan | Compounds and compositions as smarca2/4 degraders and uses thereof |
| WO2024073507A1 (en) | 2022-09-28 | 2024-04-04 | Theseus Pharmaceuticals, Inc. | Macrocyclic compounds and uses thereof |
| WO2024137742A1 (en) | 2022-12-20 | 2024-06-27 | Blueprint Medicines Corporation | Compounds and compositions as fgfr3 degraders and uses thereof |
| WO2025096976A1 (en) * | 2023-11-01 | 2025-05-08 | Cornell University | Arid1a is a prognostic marker for aggressive lymphoma transformation and presents a vulnerability to pharmacological inhibition of smarca4/2 |
| WO2025129116A1 (en) * | 2023-12-14 | 2025-06-19 | C4 Therapeutics, Inc. | Compounds for the targeted degradation of smarca2 |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20190300521A1 (en) * | 2018-04-01 | 2019-10-03 | Arvinas Operations, Inc. | Brm targeting compounds and associated methods of use |
| 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) |
| PH12022550578A1 (en) * | 2019-09-12 | 2024-02-19 | Aurigene Discovery Tech Ltd | Method for identifying responders to smarca2/4 degraders |
-
2020
- 2020-10-26 JP JP2022523943A patent/JP2023511471A/ja active Pending
- 2020-10-26 EP EP20880820.4A patent/EP4054724A4/en not_active Withdrawn
- 2020-10-26 WO PCT/US2020/057356 patent/WO2021086785A1/en not_active Ceased
- 2020-10-26 US US17/771,127 patent/US20230002367A1/en not_active Abandoned
- 2020-10-26 CN CN202080074772.3A patent/CN114599428A/zh active Pending
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