JPWO2021163627A5 - - Google Patents
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- JPWO2021163627A5 JPWO2021163627A5 JP2022549144A JP2022549144A JPWO2021163627A5 JP WO2021163627 A5 JPWO2021163627 A5 JP WO2021163627A5 JP 2022549144 A JP2022549144 A JP 2022549144A JP 2022549144 A JP2022549144 A JP 2022549144A JP WO2021163627 A5 JPWO2021163627 A5 JP WO2021163627A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- independently
- heteroaryl
- aryl
- heterocycloalkyl
- 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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- 125000000217 alkyl group Chemical group 0.000 claims description 84
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 83
- 125000003118 aryl group Chemical group 0.000 claims description 79
- 125000001072 heteroaryl group Chemical group 0.000 claims description 73
- 150000001875 compounds Chemical class 0.000 claims description 71
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 71
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 61
- 229910052736 halogen Chemical group 0.000 claims description 59
- 150000002367 halogens Chemical group 0.000 claims description 59
- 229910052739 hydrogen Inorganic materials 0.000 claims description 39
- 239000001257 hydrogen Substances 0.000 claims description 39
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 28
- 125000006577 C1-C6 hydroxyalkyl group Chemical group 0.000 claims description 23
- 150000002431 hydrogen Chemical group 0.000 claims description 23
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims description 18
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 16
- 229910052799 carbon Inorganic materials 0.000 claims description 14
- 125000004429 atom Chemical group 0.000 claims description 12
- 201000010099 disease Diseases 0.000 claims description 9
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 9
- 239000008194 pharmaceutical composition Substances 0.000 claims description 9
- 239000003814 drug Substances 0.000 claims description 8
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 8
- 229910052757 nitrogen Inorganic materials 0.000 claims description 7
- 150000003839 salts Chemical class 0.000 claims description 7
- 230000001404 mediated effect Effects 0.000 claims description 6
- 125000001424 substituent group Chemical group 0.000 claims description 6
- 229940124597 therapeutic agent Drugs 0.000 claims description 6
- 125000002947 alkylene group Chemical group 0.000 claims description 5
- 125000001188 haloalkyl group Chemical group 0.000 claims description 5
- 206010049459 Lymphangioleiomyomatosis Diseases 0.000 claims description 4
- 206010028980 Neoplasm Diseases 0.000 claims description 4
- 208000026911 Tuberous sclerosis complex Diseases 0.000 claims description 4
- 201000011510 cancer Diseases 0.000 claims description 4
- 208000009999 tuberous sclerosis Diseases 0.000 claims description 4
- 206010006187 Breast cancer Diseases 0.000 claims description 3
- 208000026310 Breast neoplasm Diseases 0.000 claims description 3
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims description 3
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims description 3
- 230000002159 abnormal effect Effects 0.000 claims description 3
- 230000004900 autophagic degradation Effects 0.000 claims description 3
- 125000004474 heteroalkylene group Chemical group 0.000 claims description 3
- 201000005202 lung cancer Diseases 0.000 claims description 3
- 208000020816 lung neoplasm Diseases 0.000 claims description 3
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims description 3
- 201000002528 pancreatic cancer Diseases 0.000 claims description 3
- 208000008443 pancreatic carcinoma Diseases 0.000 claims description 3
- 125000004076 pyridyl group Chemical group 0.000 claims description 3
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 2
- 239000012661 PARP inhibitor Substances 0.000 claims description 2
- 229940121906 Poly ADP ribose polymerase inhibitor Drugs 0.000 claims description 2
- VSRXQHXAPYXROS-UHFFFAOYSA-N azanide;cyclobutane-1,1-dicarboxylic acid;platinum(2+) Chemical compound [NH2-].[NH2-].[Pt+2].OC(=O)C1(C(O)=O)CCC1 VSRXQHXAPYXROS-UHFFFAOYSA-N 0.000 claims description 2
- 229960004562 carboplatin Drugs 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 125000000623 heterocyclic group Chemical group 0.000 claims description 2
- 229940124302 mTOR inhibitor Drugs 0.000 claims description 2
- 239000003628 mammalian target of rapamycin inhibitor Substances 0.000 claims description 2
- 239000002829 mitogen activated protein kinase inhibitor Substances 0.000 claims description 2
- 239000012453 solvate Substances 0.000 claims description 2
- 125000005842 heteroatom Chemical group 0.000 claims 1
- 238000000034 method Methods 0.000 description 14
- 125000004965 chloroalkyl group Chemical group 0.000 description 12
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 description 4
- 125000004367 cycloalkylaryl group Chemical group 0.000 description 4
- 229910052731 fluorine Inorganic materials 0.000 description 4
- 239000011737 fluorine Substances 0.000 description 4
- 229910052794 bromium Inorganic materials 0.000 description 3
- 229910052801 chlorine Inorganic materials 0.000 description 3
- 239000000460 chlorine Substances 0.000 description 3
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical compound [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 description 2
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 description 2
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Substances BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 description 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 description 2
- 102100020689 Autophagy-related protein 13 Human genes 0.000 description 1
- 101000785138 Homo sapiens Autophagy-related protein 13 Proteins 0.000 description 1
- 208000003721 Triple Negative Breast Neoplasms Diseases 0.000 description 1
- 239000000203 mixture Substances 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 208000002154 non-small cell lung carcinoma Diseases 0.000 description 1
- 125000004043 oxo group Chemical group O=* 0.000 description 1
- 201000008129 pancreatic ductal adenocarcinoma Diseases 0.000 description 1
- 125000005346 substituted cycloalkyl group Chemical group 0.000 description 1
- 238000006467 substitution reaction Methods 0.000 description 1
- 229910052717 sulfur Inorganic materials 0.000 description 1
- 208000022679 triple-negative breast carcinoma Diseases 0.000 description 1
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US202062977039P | 2020-02-14 | 2020-02-14 | |
| US62/977,039 | 2020-02-14 | ||
| PCT/US2021/018038 WO2021163627A1 (en) | 2020-02-14 | 2021-02-12 | Macrocyclic ulk1/2 inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2023513793A JP2023513793A (ja) | 2023-04-03 |
| JPWO2021163627A5 true JPWO2021163627A5 (https=) | 2024-02-20 |
| JP2023513793A5 JP2023513793A5 (https=) | 2024-02-20 |
Family
ID=77292762
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022549144A Pending JP2023513793A (ja) | 2020-02-14 | 2021-02-12 | 大環状ulk1/2阻害剤 |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US12594277B2 (https=) |
| EP (1) | EP4103183A4 (https=) |
| JP (1) | JP2023513793A (https=) |
| KR (1) | KR20220153582A (https=) |
| CN (1) | CN115515588A (https=) |
| AU (1) | AU2021221162A1 (https=) |
| CA (1) | CA3171185A1 (https=) |
| WO (1) | WO2021163627A1 (https=) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2021216440A1 (en) * | 2020-04-20 | 2021-10-28 | Tenova Pharmaceuticals Inc. | Novel protein kinase inhibitors |
| WO2022072668A1 (en) * | 2020-09-30 | 2022-04-07 | Salk Institute For Biological Studies | Patient selection biomarkers for treatment with ulk inhibitors |
| TW202404979A (zh) * | 2022-07-18 | 2024-02-01 | 大陸商江蘇恆瑞醫藥股份有限公司 | 抑制並誘導egfr降解的大環類化合物、其製備方法及其在醫藥上的應用 |
| WO2024017258A1 (zh) * | 2022-07-19 | 2024-01-25 | 百极弘烨(南通)医药科技有限公司 | Egfr小分子抑制剂、含其的药物组合物及其用途 |
| WO2024233766A1 (en) * | 2023-05-10 | 2024-11-14 | Erasca, Inc. | Macrocyclic ulk1/2 inhibitors and their use thereof |
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| IL325201A (en) | 2019-06-17 | 2026-02-01 | Deciphera Pharmaceuticals Llc | Aminopyrimidine amide autophagy inhibitors and methods of using them |
| CN115515589A (zh) | 2020-02-14 | 2022-12-23 | 萨克生物研究学院 | Ulk1/2抑制剂及其使用方法 |
| JP2023513797A (ja) | 2020-02-14 | 2023-04-03 | ソーク インスティテュート フォー バイオロジカル スタディーズ | Ulk1/2阻害剤による単剤療法および併用療法 |
| WO2021216440A1 (en) | 2020-04-20 | 2021-10-28 | Tenova Pharmaceuticals Inc. | Novel protein kinase inhibitors |
| WO2022072668A1 (en) | 2020-09-30 | 2022-04-07 | Salk Institute For Biological Studies | Patient selection biomarkers for treatment with ulk inhibitors |
-
2021
- 2021-02-12 KR KR1020227028938A patent/KR20220153582A/ko active Pending
- 2021-02-12 JP JP2022549144A patent/JP2023513793A/ja active Pending
- 2021-02-12 CN CN202180027809.1A patent/CN115515588A/zh active Pending
- 2021-02-12 WO PCT/US2021/018038 patent/WO2021163627A1/en not_active Ceased
- 2021-02-12 AU AU2021221162A patent/AU2021221162A1/en active Pending
- 2021-02-12 US US17/799,634 patent/US12594277B2/en active Active
- 2021-02-12 CA CA3171185A patent/CA3171185A1/en active Pending
- 2021-02-12 EP EP21753844.6A patent/EP4103183A4/en active Pending
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