JPWO2021188696A5 - - Google Patents
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- Publication number
- JPWO2021188696A5 JPWO2021188696A5 JP2022556046A JP2022556046A JPWO2021188696A5 JP WO2021188696 A5 JPWO2021188696 A5 JP WO2021188696A5 JP 2022556046 A JP2022556046 A JP 2022556046A JP 2022556046 A JP2022556046 A JP 2022556046A JP WO2021188696 A5 JPWO2021188696 A5 JP WO2021188696A5
- Authority
- JP
- Japan
- Prior art keywords
- nitrogen
- sulfur
- oxygen
- partially unsaturated
- membered
- 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 Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 98
- 229910052757 nitrogen Inorganic materials 0.000 claims description 66
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims description 58
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 58
- 125000005842 heteroatom Chemical group 0.000 claims description 58
- 229910052760 oxygen Inorganic materials 0.000 claims description 58
- 239000001301 oxygen Substances 0.000 claims description 58
- 229910052717 sulfur Inorganic materials 0.000 claims description 58
- 239000011593 sulfur Substances 0.000 claims description 58
- 229920006395 saturated elastomer Polymers 0.000 claims description 56
- 150000001875 compounds Chemical class 0.000 claims description 37
- 229910052739 hydrogen Inorganic materials 0.000 claims description 36
- 239000001257 hydrogen Substances 0.000 claims description 36
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 34
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 32
- 125000002619 bicyclic group Chemical group 0.000 claims description 30
- 150000002431 hydrogen Chemical class 0.000 claims description 26
- 150000003839 salts Chemical class 0.000 claims description 23
- 125000000623 heterocyclic group Chemical group 0.000 claims description 18
- -1 R A Chemical class 0.000 claims description 17
- 201000010099 disease Diseases 0.000 claims description 16
- 208000035475 disorder Diseases 0.000 claims description 16
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 14
- 229910052736 halogen Inorganic materials 0.000 claims description 14
- 150000002367 halogens Chemical class 0.000 claims description 14
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims description 12
- 125000001931 aliphatic group Chemical group 0.000 claims description 12
- 238000000034 method Methods 0.000 claims description 11
- 239000008194 pharmaceutical composition Substances 0.000 claims description 11
- 102000004495 STAT3 Transcription Factor Human genes 0.000 claims description 10
- 108010017324 STAT3 Transcription Factor Proteins 0.000 claims description 10
- 125000002837 carbocyclic group Chemical group 0.000 claims description 10
- 229910052799 carbon Inorganic materials 0.000 claims description 10
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 10
- 206010006187 Breast cancer Diseases 0.000 claims description 8
- 208000026310 Breast neoplasm Diseases 0.000 claims description 8
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 8
- 206010028980 Neoplasm Diseases 0.000 claims description 8
- 208000031839 Peripheral nerve sheath tumour malignant Diseases 0.000 claims description 8
- 125000004429 atom Chemical group 0.000 claims description 8
- 201000011510 cancer Diseases 0.000 claims description 8
- 239000003814 drug Substances 0.000 claims description 8
- 125000001183 hydrocarbyl group Chemical group 0.000 claims description 8
- 201000009020 malignant peripheral nerve sheath tumor Diseases 0.000 claims description 8
- 230000001404 mediated effect Effects 0.000 claims description 8
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims description 8
- 208000029974 neurofibrosarcoma Diseases 0.000 claims description 8
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 6
- 125000002950 monocyclic group Chemical group 0.000 claims description 6
- 229940124597 therapeutic agent Drugs 0.000 claims description 6
- 125000005330 8 membered heterocyclic group Chemical group 0.000 claims description 4
- 208000023275 Autoimmune disease Diseases 0.000 claims description 4
- 208000020084 Bone disease Diseases 0.000 claims description 4
- 208000024172 Cardiovascular disease Diseases 0.000 claims description 4
- 208000035473 Communicable disease Diseases 0.000 claims description 4
- 208000032612 Glial tumor Diseases 0.000 claims description 4
- 206010018338 Glioma Diseases 0.000 claims description 4
- 206010061598 Immunodeficiency Diseases 0.000 claims description 4
- 208000029462 Immunodeficiency disease Diseases 0.000 claims description 4
- 208000026350 Inborn Genetic disease Diseases 0.000 claims description 4
- 206010033128 Ovarian cancer Diseases 0.000 claims description 4
- 206010061535 Ovarian neoplasm Diseases 0.000 claims description 4
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims description 4
- 206010060862 Prostate cancer Diseases 0.000 claims description 4
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims description 4
- 208000000102 Squamous Cell Carcinoma of Head and Neck Diseases 0.000 claims description 4
- 230000006044 T cell activation Effects 0.000 claims description 4
- 108090000190 Thrombin Proteins 0.000 claims description 4
- 208000003721 Triple Negative Breast Neoplasms Diseases 0.000 claims description 4
- 230000030833 cell death Effects 0.000 claims description 4
- 208000015114 central nervous system disease Diseases 0.000 claims description 4
- 208000030381 cutaneous melanoma Diseases 0.000 claims description 4
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 4
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims description 4
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 4
- 230000001066 destructive effect Effects 0.000 claims description 4
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 4
- 208000016361 genetic disease Diseases 0.000 claims description 4
- 201000000459 head and neck squamous cell carcinoma Diseases 0.000 claims description 4
- 239000005556 hormone Substances 0.000 claims description 4
- 229940088597 hormone Drugs 0.000 claims description 4
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 4
- 230000007813 immunodeficiency Effects 0.000 claims description 4
- 208000027866 inflammatory disease Diseases 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
- 208000019423 liver disease Diseases 0.000 claims description 4
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims description 4
- 208000030159 metabolic disease Diseases 0.000 claims description 4
- 230000004770 neurodegeneration Effects 0.000 claims description 4
- 208000015122 neurodegenerative disease Diseases 0.000 claims description 4
- 210000000056 organ Anatomy 0.000 claims description 4
- 201000002528 pancreatic cancer Diseases 0.000 claims description 4
- 208000008443 pancreatic carcinoma Diseases 0.000 claims description 4
- 230000001575 pathological effect Effects 0.000 claims description 4
- 230000002062 proliferating effect Effects 0.000 claims description 4
- 201000003708 skin melanoma Diseases 0.000 claims description 4
- 208000010110 spontaneous platelet aggregation 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
- 229960004072 thrombin Drugs 0.000 claims description 4
- 238000002054 transplantation Methods 0.000 claims description 4
- 208000022679 triple-negative breast carcinoma Diseases 0.000 claims description 4
- 230000003612 virological effect Effects 0.000 claims description 4
- 239000012472 biological sample Substances 0.000 claims description 3
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims description 3
- XUIMIQQOPSSXEZ-UHFFFAOYSA-N Silicon Chemical group [Si] XUIMIQQOPSSXEZ-UHFFFAOYSA-N 0.000 claims description 2
- 239000002671 adjuvant Substances 0.000 claims description 2
- 125000005605 benzo group Chemical group 0.000 claims description 2
- 125000004452 carbocyclyl group Chemical group 0.000 claims description 2
- 150000001721 carbon Chemical group 0.000 claims description 2
- 230000000593 degrading effect Effects 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 238000004519 manufacturing process Methods 0.000 claims description 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 2
- 239000013610 patient sample Substances 0.000 claims description 2
- 229910052710 silicon Inorganic materials 0.000 claims description 2
- 239000003981 vehicle Substances 0.000 claims description 2
- 239000000203 mixture Substances 0.000 claims 5
- 239000000523 sample Substances 0.000 description 1
Applications Claiming Priority (9)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US202062990555P | 2020-03-17 | 2020-03-17 | |
| US62/990,555 | 2020-03-17 | ||
| US202063088945P | 2020-10-07 | 2020-10-07 | |
| US63/088,945 | 2020-10-07 | ||
| US202063123335P | 2020-12-09 | 2020-12-09 | |
| US63/123,335 | 2020-12-09 | ||
| US202163159102P | 2021-03-10 | 2021-03-10 | |
| US63/159,102 | 2021-03-10 | ||
| PCT/US2021/022794 WO2021188696A1 (en) | 2020-03-17 | 2021-03-17 | Stat degraders and uses thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2023518422A JP2023518422A (ja) | 2023-05-01 |
| JPWO2021188696A5 true JPWO2021188696A5 (de) | 2024-03-29 |
Family
ID=77771311
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022556046A Pending JP2023518422A (ja) | 2020-03-17 | 2021-03-17 | Ｓｔａｔ分解剤およびそれらの使用 |
Country Status (9)
| Country | Link |
|---|---|
| US (1) | US20240016942A1 (de) |
| EP (1) | EP4121055A4 (de) |
| JP (1) | JP2023518422A (de) |
| CN (1) | CN115776891A (de) |
| AU (1) | AU2021238333A1 (de) |
| CA (1) | CA3170503A1 (de) |
| IL (1) | IL296334A (de) |
| MX (1) | MX2022011437A (de) |
| WO (1) | WO2021188696A1 (de) |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2023192960A1 (en) * | 2022-03-31 | 2023-10-05 | Recludix Pharma, Inc. | Stat modulators and uses thereof |
| WO2024030628A1 (en) * | 2022-08-05 | 2024-02-08 | Kymera Therapeutics, Inc. | Deuterated stat3 degraders and uses thereof |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MX2020003190A (es) * | 2017-09-22 | 2020-11-11 | Kymera Therapeutics Inc | Degradadores de proteinas y usos de los mismos. |
| SG11202110449YA (en) * | 2019-03-26 | 2021-10-28 | Univ Michigan Regents | Small molecule degraders of stat3 |
| WO2020205467A1 (en) * | 2019-03-29 | 2020-10-08 | The Regents Of The University Of Michigan | Stat3 protein degraders |
| TW202106676A (zh) * | 2019-04-05 | 2021-02-16 | 美商凱麥拉醫療公司 | Stat降解劑及其用途 |
-
2021
- 2021-03-17 MX MX2022011437A patent/MX2022011437A/es unknown
- 2021-03-17 US US17/912,388 patent/US20240016942A1/en active Pending
- 2021-03-17 WO PCT/US2021/022794 patent/WO2021188696A1/en unknown
- 2021-03-17 CA CA3170503A patent/CA3170503A1/en active Pending
- 2021-03-17 EP EP21771947.5A patent/EP4121055A4/de active Pending
- 2021-03-17 CN CN202180032886.6A patent/CN115776891A/zh active Pending
- 2021-03-17 IL IL296334A patent/IL296334A/en unknown
- 2021-03-17 JP JP2022556046A patent/JP2023518422A/ja active Pending
- 2021-03-17 AU AU2021238333A patent/AU2021238333A1/en active Pending
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