JPWO2022077010A5 - - Google Patents
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- Publication number
- JPWO2022077010A5 JPWO2022077010A5 JP2023521335A JP2023521335A JPWO2022077010A5 JP WO2022077010 A5 JPWO2022077010 A5 JP WO2022077010A5 JP 2023521335 A JP2023521335 A JP 2023521335A JP 2023521335 A JP2023521335 A JP 2023521335A JP WO2022077010 A5 JPWO2022077010 A5 JP WO2022077010A5
- Authority
- JP
- Japan
- Prior art keywords
- nitrogen
- sulfur
- oxygen
- independently selected
- heteroatoms independently
- 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
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 94
- 229910052757 nitrogen Inorganic materials 0.000 claims description 86
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims description 78
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 78
- 125000005842 heteroatom Chemical group 0.000 claims description 78
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 78
- 229910052760 oxygen Inorganic materials 0.000 claims description 78
- 239000001301 oxygen Chemical group 0.000 claims description 78
- 229910052717 sulfur Chemical group 0.000 claims description 78
- 239000011593 sulfur Chemical group 0.000 claims description 78
- 229920006395 saturated elastomer Polymers 0.000 claims description 66
- 229910052739 hydrogen Inorganic materials 0.000 claims description 42
- 239000001257 hydrogen Substances 0.000 claims description 42
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims description 40
- 150000001875 compounds Chemical class 0.000 claims description 39
- 125000002619 bicyclic group Chemical group 0.000 claims description 28
- 125000000623 heterocyclic group Chemical group 0.000 claims description 24
- 229910052736 halogen Inorganic materials 0.000 claims description 20
- 150000002367 halogens Chemical class 0.000 claims description 20
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims description 18
- 150000003839 salts Chemical class 0.000 claims description 17
- 125000001931 aliphatic group Chemical group 0.000 claims description 16
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 16
- -1 or spirocyclic Chemical group 0.000 claims description 16
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 14
- 125000004452 carbocyclyl group Chemical group 0.000 claims description 12
- 229910052799 carbon Inorganic materials 0.000 claims description 12
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 12
- 238000000034 method Methods 0.000 claims description 10
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims description 10
- 239000008194 pharmaceutical composition Substances 0.000 claims description 10
- 201000010099 disease Diseases 0.000 claims description 9
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 8
- 125000002837 carbocyclic group Chemical group 0.000 claims description 8
- 125000001183 hydrocarbyl group Chemical group 0.000 claims description 8
- UUEVFMOUBSLVJW-UHFFFAOYSA-N oxo-[[1-[2-[2-[2-[4-(oxoazaniumylmethylidene)pyridin-1-yl]ethoxy]ethoxy]ethyl]pyridin-4-ylidene]methyl]azanium;dibromide Chemical compound [Br-].[Br-].C1=CC(=C[NH+]=O)C=CN1CCOCCOCCN1C=CC(=C[NH+]=O)C=C1 UUEVFMOUBSLVJW-UHFFFAOYSA-N 0.000 claims description 8
- 102000004495 STAT3 Transcription Factor Human genes 0.000 claims description 6
- 108010017324 STAT3 Transcription Factor Proteins 0.000 claims description 6
- 125000005605 benzo group Chemical group 0.000 claims description 6
- 208000035475 disorder Diseases 0.000 claims description 6
- 206010073478 Anaplastic large-cell lymphoma Diseases 0.000 claims description 4
- 208000023275 Autoimmune disease Diseases 0.000 claims description 4
- 206010066476 Haematological malignancy Diseases 0.000 claims description 4
- 208000002250 Hematologic Neoplasms Diseases 0.000 claims description 4
- 208000031671 Large B-Cell Diffuse Lymphoma Diseases 0.000 claims description 4
- 208000032004 Large-Cell Anaplastic Lymphoma Diseases 0.000 claims description 4
- 206010028980 Neoplasm Diseases 0.000 claims description 4
- 208000027190 Peripheral T-cell lymphomas Diseases 0.000 claims description 4
- 208000031839 Peripheral nerve sheath tumour malignant Diseases 0.000 claims description 4
- 206010035226 Plasma cell myeloma Diseases 0.000 claims description 4
- XUIMIQQOPSSXEZ-UHFFFAOYSA-N Silicon Chemical group [Si] XUIMIQQOPSSXEZ-UHFFFAOYSA-N 0.000 claims description 4
- 208000031673 T-Cell Cutaneous Lymphoma Diseases 0.000 claims description 4
- 208000031672 T-Cell Peripheral Lymphoma Diseases 0.000 claims description 4
- 125000004429 atom Chemical group 0.000 claims description 4
- 239000012472 biological sample Substances 0.000 claims description 4
- 201000011510 cancer Diseases 0.000 claims description 4
- 150000001721 carbon Chemical group 0.000 claims description 4
- 201000007241 cutaneous T cell lymphoma Diseases 0.000 claims description 4
- 206010012818 diffuse large B-cell lymphoma Diseases 0.000 claims description 4
- 239000003814 drug Substances 0.000 claims description 4
- 208000032839 leukemia Diseases 0.000 claims description 4
- 201000009020 malignant peripheral nerve sheath tumor Diseases 0.000 claims description 4
- 208000020968 mature T-cell and NK-cell non-Hodgkin lymphoma Diseases 0.000 claims description 4
- 230000001404 mediated effect Effects 0.000 claims description 4
- 125000002950 monocyclic group Chemical group 0.000 claims description 4
- 201000005962 mycosis fungoides Diseases 0.000 claims description 4
- 125000001624 naphthyl group Chemical group 0.000 claims description 4
- 208000029974 neurofibrosarcoma Diseases 0.000 claims description 4
- 208000025638 primary cutaneous T-cell non-Hodgkin lymphoma Diseases 0.000 claims description 4
- 229910052710 silicon Chemical group 0.000 claims description 4
- 229940124597 therapeutic agent Drugs 0.000 claims description 4
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims description 3
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims description 2
- 206010004593 Bile duct cancer Diseases 0.000 claims description 2
- 208000020084 Bone disease Diseases 0.000 claims description 2
- 206010006187 Breast cancer Diseases 0.000 claims description 2
- 208000026310 Breast neoplasm Diseases 0.000 claims description 2
- 208000024172 Cardiovascular disease Diseases 0.000 claims description 2
- 206010009944 Colon cancer Diseases 0.000 claims description 2
- 208000035473 Communicable disease Diseases 0.000 claims description 2
- 206010012438 Dermatitis atopic Diseases 0.000 claims description 2
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims description 2
- 206010051066 Gastrointestinal stromal tumour Diseases 0.000 claims description 2
- 208000032612 Glial tumor Diseases 0.000 claims description 2
- 206010018338 Glioma Diseases 0.000 claims description 2
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 2
- 201000009794 Idiopathic Pulmonary Fibrosis Diseases 0.000 claims description 2
- 208000029462 Immunodeficiency disease Diseases 0.000 claims description 2
- 208000026350 Inborn Genetic disease Diseases 0.000 claims description 2
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims description 2
- 208000008839 Kidney Neoplasms Diseases 0.000 claims description 2
- 206010025323 Lymphomas Diseases 0.000 claims description 2
- 208000034578 Multiple myelomas Diseases 0.000 claims description 2
- 201000003793 Myelodysplastic syndrome Diseases 0.000 claims description 2
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims description 2
- 201000007224 Myeloproliferative neoplasm Diseases 0.000 claims description 2
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims description 2
- 206010033128 Ovarian cancer Diseases 0.000 claims description 2
- 206010061535 Ovarian neoplasm Diseases 0.000 claims description 2
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims description 2
- 206010060862 Prostate cancer Diseases 0.000 claims description 2
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims description 2
- 206010038389 Renal cancer Diseases 0.000 claims description 2
- 208000000102 Squamous Cell Carcinoma of Head and Neck Diseases 0.000 claims description 2
- 208000005718 Stomach Neoplasms Diseases 0.000 claims description 2
- 201000009594 Systemic Scleroderma Diseases 0.000 claims description 2
- 206010042953 Systemic sclerosis Diseases 0.000 claims description 2
- 230000006044 T cell activation Effects 0.000 claims description 2
- 210000001744 T-lymphocyte Anatomy 0.000 claims description 2
- 108090000190 Thrombin Proteins 0.000 claims description 2
- 208000024340 acute graft versus host disease Diseases 0.000 claims description 2
- 239000002671 adjuvant Substances 0.000 claims description 2
- 125000003118 aryl group Chemical group 0.000 claims description 2
- 201000008937 atopic dermatitis Diseases 0.000 claims description 2
- 208000026900 bile duct neoplasm Diseases 0.000 claims description 2
- 230000030833 cell death Effects 0.000 claims description 2
- 208000015114 central nervous system disease Diseases 0.000 claims description 2
- 208000006990 cholangiocarcinoma Diseases 0.000 claims description 2
- 208000017760 chronic graft versus host disease Diseases 0.000 claims description 2
- 208000029742 colonic neoplasm Diseases 0.000 claims description 2
- 208000030381 cutaneous melanoma Diseases 0.000 claims description 2
- 230000000593 degrading effect Effects 0.000 claims description 2
- 230000001066 destructive effect Effects 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 201000004101 esophageal cancer Diseases 0.000 claims description 2
- 206010017758 gastric cancer Diseases 0.000 claims description 2
- 201000011243 gastrointestinal stromal tumor Diseases 0.000 claims description 2
- 208000016361 genetic disease Diseases 0.000 claims description 2
- 201000000459 head and neck squamous cell carcinoma Diseases 0.000 claims description 2
- 239000005556 hormone Substances 0.000 claims description 2
- 229940088597 hormone Drugs 0.000 claims description 2
- 208000015181 infectious disease Diseases 0.000 claims description 2
- 208000027866 inflammatory disease Diseases 0.000 claims description 2
- 208000036971 interstitial lung disease 2 Diseases 0.000 claims description 2
- 201000010982 kidney cancer Diseases 0.000 claims description 2
- 201000007270 liver cancer Diseases 0.000 claims description 2
- 208000019423 liver disease Diseases 0.000 claims description 2
- 208000014018 liver neoplasm Diseases 0.000 claims description 2
- 230000000527 lymphocytic effect Effects 0.000 claims description 2
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims description 2
- 208000030159 metabolic disease Diseases 0.000 claims description 2
- 206010028537 myelofibrosis Diseases 0.000 claims description 2
- 201000000050 myeloid neoplasm Diseases 0.000 claims description 2
- 210000000822 natural killer cell Anatomy 0.000 claims description 2
- 230000004770 neurodegeneration Effects 0.000 claims description 2
- 208000015122 neurodegenerative disease Diseases 0.000 claims description 2
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims description 2
- 210000000056 organ Anatomy 0.000 claims description 2
- 201000002528 pancreatic cancer Diseases 0.000 claims description 2
- 208000008443 pancreatic carcinoma Diseases 0.000 claims description 2
- 230000001575 pathological effect Effects 0.000 claims description 2
- 239000013610 patient sample Substances 0.000 claims description 2
- 230000002062 proliferating effect Effects 0.000 claims description 2
- 206010039073 rheumatoid arthritis Diseases 0.000 claims description 2
- 201000003708 skin melanoma Diseases 0.000 claims description 2
- 208000010110 spontaneous platelet aggregation Diseases 0.000 claims description 2
- 201000011549 stomach cancer Diseases 0.000 claims description 2
- 229960004072 thrombin Drugs 0.000 claims description 2
- 210000001519 tissue Anatomy 0.000 claims description 2
- 206010044412 transitional cell carcinoma Diseases 0.000 claims description 2
- 238000002054 transplantation Methods 0.000 claims description 2
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims description 2
- 239000003981 vehicle Substances 0.000 claims description 2
- 230000003612 virological effect Effects 0.000 claims description 2
- 239000000203 mixture Substances 0.000 claims 6
- 206010016654 Fibrosis Diseases 0.000 claims 1
- 230000004761 fibrosis Effects 0.000 claims 1
- 125000001072 heteroaryl group Chemical group 0.000 claims 1
- 230000003176 fibrotic effect Effects 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US202063088787P | 2020-10-07 | 2020-10-07 | |
| US63/088,787 | 2020-10-07 | ||
| US202063123337P | 2020-12-09 | 2020-12-09 | |
| US63/123,337 | 2020-12-09 | ||
| PCT/US2021/071762 WO2022077010A1 (en) | 2020-10-07 | 2021-10-07 | Stat degraders and uses thereof |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2023545730A JP2023545730A (ja) | 2023-10-31 |
| JPWO2022077010A5 true JPWO2022077010A5 (https=) | 2024-10-15 |
| JP2023545730A5 JP2023545730A5 (https=) | 2024-10-15 |
Family
ID=81126142
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2023521335A Pending JP2023545730A (ja) | 2020-10-07 | 2021-10-07 | Ｓｔａｔ分解剤およびそれらの使用 |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US20240293423A1 (https=) |
| EP (1) | EP4225303A4 (https=) |
| JP (1) | JP2023545730A (https=) |
| AU (1) | AU2021358130A1 (https=) |
| CA (1) | CA3194492A1 (https=) |
| IL (1) | IL301830A (https=) |
| MX (1) | MX2023003973A (https=) |
| WO (1) | WO2022077010A1 (https=) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| CN115677831B (zh) * | 2021-07-22 | 2026-03-17 | 杭州和正医药有限公司 | 拟肽类stat降解药物、组合物及应用 |
| EP4499656A1 (en) * | 2022-03-31 | 2025-02-05 | Recludix Pharma, Inc. | Stat modulators and uses thereof |
| WO2024064080A1 (en) * | 2022-09-19 | 2024-03-28 | Kymera Therapeutics, Inc. | Stat6 degraders and uses thereof |
| EP4709370A2 (en) * | 2023-05-09 | 2026-03-18 | Recludix Pharma, Inc. | Stat degraders and uses thereof |
| EP4712974A2 (en) * | 2023-05-15 | 2026-03-25 | Recludix Pharma, Inc. | Stat degraders and uses thereof |
| AU2024334386A1 (en) * | 2023-08-30 | 2026-02-19 | Kymera Therapeutics, Inc. | Stat6 degraders and uses thereof |
| WO2025217647A1 (en) * | 2024-04-12 | 2025-10-16 | Kymera Therapeutics, Inc. | Stat6 degraders and uses thereof |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2010077589A2 (en) * | 2008-12-08 | 2010-07-08 | The Regents Of The University Of Michigan Office Of Technology Transfer | Stat3 inhibitors and therapeutic methods using the same |
| MX2020003190A (es) * | 2017-09-22 | 2020-11-11 | Kymera Therapeutics Inc | Degradadores de proteinas y usos de los mismos. |
| CN114269763A (zh) * | 2019-03-26 | 2022-04-01 | 美国密歇根州立大学试剂中心 | Stat3的小分子降解剂 |
-
2021
- 2021-10-07 JP JP2023521335A patent/JP2023545730A/ja active Pending
- 2021-10-07 IL IL301830A patent/IL301830A/en unknown
- 2021-10-07 AU AU2021358130A patent/AU2021358130A1/en not_active Abandoned
- 2021-10-07 MX MX2023003973A patent/MX2023003973A/es unknown
- 2021-10-07 CA CA3194492A patent/CA3194492A1/en active Pending
- 2021-10-07 WO PCT/US2021/071762 patent/WO2022077010A1/en not_active Ceased
- 2021-10-07 EP EP21878728.1A patent/EP4225303A4/en not_active Withdrawn
- 2021-10-07 US US18/030,865 patent/US20240293423A1/en active Pending
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