JPWO2021163629A5 - - Google Patents
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- JPWO2021163629A5 JPWO2021163629A5 JP2022549145A JP2022549145A JPWO2021163629A5 JP WO2021163629 A5 JPWO2021163629 A5 JP WO2021163629A5 JP 2022549145 A JP2022549145 A JP 2022549145A JP 2022549145 A JP2022549145 A JP 2022549145A JP WO2021163629 A5 JPWO2021163629 A5 JP WO2021163629A5
- Authority
- JP
- Japan
- Prior art keywords
- substituted
- unsubstituted
- alkyl
- cycloalkyl
- compound according
- Prior art date
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- 150000001875 compounds Chemical class 0.000 claims description 183
- 125000000217 alkyl group Chemical group 0.000 claims description 145
- 229910052736 halogen Inorganic materials 0.000 claims description 84
- 150000002367 halogens Chemical class 0.000 claims description 84
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 82
- 125000003118 aryl group Chemical group 0.000 claims description 66
- 125000001072 heteroaryl group Chemical group 0.000 claims description 63
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 63
- 229910052739 hydrogen Inorganic materials 0.000 claims description 25
- 150000003839 salts Chemical class 0.000 claims description 22
- 125000001188 haloalkyl group Chemical group 0.000 claims description 15
- 229910052799 carbon Inorganic materials 0.000 claims description 12
- 239000001257 hydrogen Substances 0.000 claims description 12
- 229910052757 nitrogen Inorganic materials 0.000 claims description 12
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 12
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 10
- 239000008194 pharmaceutical composition Substances 0.000 claims description 10
- 125000004429 atom Chemical group 0.000 claims description 9
- 201000010099 disease Diseases 0.000 claims description 9
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 9
- 125000004404 heteroalkyl group Chemical group 0.000 claims description 9
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 8
- 239000003814 drug Substances 0.000 claims description 7
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims description 7
- 108010014380 Autophagy-Related Protein-1 Homolog Proteins 0.000 claims description 6
- 102000016956 Autophagy-Related Protein-1 Homolog Human genes 0.000 claims description 6
- 230000001404 mediated effect Effects 0.000 claims description 6
- 125000005842 heteroatom Chemical group 0.000 claims description 5
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 5
- 229940124597 therapeutic agent Drugs 0.000 claims description 5
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 4
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 4
- 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
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 4
- 150000002825 nitriles Chemical class 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
- 230000004900 autophagic degradation Effects 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
- 229940124647 MEK inhibitor Drugs 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
- 230000002159 abnormal effect Effects 0.000 claims description 2
- 125000003545 alkoxy group Chemical group 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
- 125000004432 carbon atom Chemical group C* 0.000 claims description 2
- 229960004562 carboplatin Drugs 0.000 claims description 2
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 2
- 125000004122 cyclic group Chemical group 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 125000000623 heterocyclic group Chemical group 0.000 claims description 2
- 125000002887 hydroxy group Chemical group [H]O* 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
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims description 2
- 239000002829 mitogen activated protein kinase inhibitor Substances 0.000 claims description 2
- 125000004043 oxo group Chemical group O=* 0.000 claims description 2
- 229910052760 oxygen Inorganic materials 0.000 claims description 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 2
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 2
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 2
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 1
- 125000006577 C1-C6 hydroxyalkyl group Chemical group 0.000 claims 1
- 102220632799 Immunoglobulin heavy variable 1-69_R11A_mutation Human genes 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 1
- 238000000034 method Methods 0.000 description 13
- 150000002431 hydrogen Chemical class 0.000 description 6
- 229910052731 fluorine Inorganic materials 0.000 description 5
- 238000006467 substitution reaction Methods 0.000 description 4
- 229910052794 bromium Inorganic materials 0.000 description 3
- 229910052801 chlorine Inorganic materials 0.000 description 3
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 description 2
- 239000011737 fluorine Substances 0.000 description 2
- 150000004820 halides Chemical class 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
- 230000001594 aberrant effect Effects 0.000 description 1
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 description 1
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 description 1
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 208000002154 non-small cell lung carcinoma Diseases 0.000 description 1
- 201000008129 pancreatic ductal adenocarcinoma Diseases 0.000 description 1
- 125000004076 pyridyl group Chemical group 0.000 description 1
- 125000000714 pyrimidinyl group Chemical group 0.000 description 1
- 210000002784 stomach Anatomy 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 |
|---|---|---|---|
| US202062977040P | 2020-02-14 | 2020-02-14 | |
| US62/977,040 | 2020-02-14 | ||
| PCT/US2021/018040 WO2021163629A1 (en) | 2020-02-14 | 2021-02-12 | Inhibitors of ulk1/2 and methods of using same |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2023513794A JP2023513794A (ja) | 2023-04-03 |
| JPWO2021163629A5 true JPWO2021163629A5 (https=) | 2024-02-20 |
| JP2023513794A5 JP2023513794A5 (https=) | 2024-02-20 |
Family
ID=77292760
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022549145A Pending JP2023513794A (ja) | 2020-02-14 | 2021-02-12 | Ｕｌｋ１／２の阻害剤およびその使用方法 |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US20230135635A1 (https=) |
| EP (1) | EP4103182A4 (https=) |
| JP (1) | JP2023513794A (https=) |
| KR (1) | KR20220153581A (https=) |
| CN (1) | CN115515589A (https=) |
| AU (1) | AU2021218739A1 (https=) |
| CA (1) | CA3171187A1 (https=) |
| WO (1) | WO2021163629A1 (https=) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20220153582A (ko) | 2020-02-14 | 2022-11-18 | 솔크 인스티튜트 포 바이올로지칼 스터디즈 | 마크로시클릭 ulk1/2 억제제 |
| WO2022072668A1 (en) * | 2020-09-30 | 2022-04-07 | Salk Institute For Biological Studies | Patient selection biomarkers for treatment with ulk inhibitors |
| WO2023134582A1 (zh) * | 2022-01-14 | 2023-07-20 | 上海立森印迹医药技术有限公司 | 一种嘧啶-2,4-二胺衍生物及其制备方法和用途 |
| WO2024140401A1 (zh) * | 2022-12-30 | 2024-07-04 | 捷思英达控股有限公司 | 作为激酶抑制剂的杂环化合物以及包括其的组合物 |
| CN116768885B (zh) * | 2023-03-14 | 2026-03-24 | 浙江大学 | N2-取代双环-2-氨基嘧啶类衍生物、其制备方法及医药用途 |
| WO2024233766A1 (en) * | 2023-05-10 | 2024-11-14 | Erasca, Inc. | Macrocyclic ulk1/2 inhibitors and their use thereof |
| WO2025045182A1 (zh) * | 2023-09-01 | 2025-03-06 | 深圳众格生物科技有限公司 | Ulk1抑制剂及其制备方法和用途 |
Family Cites Families (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6939874B2 (en) * | 2001-08-22 | 2005-09-06 | Amgen Inc. | Substituted pyrimidinyl derivatives and methods of use |
| WO2006129100A1 (en) * | 2005-06-03 | 2006-12-07 | Glaxo Group Limited | Novel compounds |
| WO2007028445A1 (en) * | 2005-07-15 | 2007-03-15 | Glaxo Group Limited | 6-indolyl-4-yl-amino-5-halogeno-2-pyrimidinyl-amino derivatives |
| EP2089369B1 (en) * | 2006-10-19 | 2011-02-02 | Rigel Pharmaceuticals, Inc. | 2,4 -pyrimidinediamine derivatives as inhibitors of jak kinases for the treatment of autoimmune diseases |
| BRPI0810641A2 (pt) * | 2007-04-12 | 2019-09-24 | Hoffmann La Roche | "compostos farmacêuticos". |
| CA2693594A1 (en) * | 2007-07-17 | 2009-01-22 | Rigel Pharmaceuticals, Inc. | Cyclic amine substituted pyrimidinediamines as pkc inhibitors |
| EA201100078A1 (ru) * | 2008-06-25 | 2011-08-30 | Айрм Ллк | Производные пиримидина в качестве ингибиторов киназы |
| WO2014197680A1 (en) * | 2013-06-05 | 2014-12-11 | Salk Institute For Biological Studies | Vitamin d receptor agonists to treat diseases involving cxcl12 activity |
| US10300058B2 (en) * | 2014-04-18 | 2019-05-28 | Xuanzhu Pharma Co., Ltd. | Tyrosine kinase inhibitor and uses thereof |
| CA2952787A1 (en) * | 2014-06-17 | 2015-12-23 | Korea Research Institute Of Chemical Technology | Pyrimidine-2,4-diamine derivative and anticancer pharmaceutical composition comprising same as effective ingredient |
| DK3185868T3 (da) * | 2014-08-25 | 2022-05-23 | Salk Inst For Biological Studi | Hidtil ukendte ULK1-inhibitorer og fremgangsmåder til anvendelse af samme |
| KR20250081944A (ko) * | 2014-09-24 | 2025-06-05 | 솔크 인스티튜트 포 바이올로지칼 스터디즈 | 종양 살상 바이러스 및 이의 사용방법 |
| CN105524045B (zh) * | 2014-10-22 | 2020-04-10 | 山东轩竹医药科技有限公司 | 四环类间变性淋巴瘤激酶抑制剂 |
| WO2016090079A1 (en) * | 2014-12-05 | 2016-06-09 | Celgene Avilomics Research, Inc. | Heteroaryl compounds and uses thereof |
| CN106188029B (zh) * | 2015-05-05 | 2018-09-18 | 山东轩竹医药科技有限公司 | 二并环类间变性淋巴瘤激酶抑制剂 |
| EP3528814B1 (en) * | 2016-10-18 | 2024-08-14 | Dana-Farber Cancer Institute, Inc. | Pyrimido-diazepinone kinase scaffold compounds and methods of treating dclk1/2-mediated disorders |
| US11180482B2 (en) * | 2016-11-30 | 2021-11-23 | Ariad Pharmaceuticals, Inc. | Anilinopyrimidines as haematopoietic progenitor kinase 1 (HPK1) inhibitors |
| EP3620457A4 (en) * | 2017-05-02 | 2021-01-06 | Korea Research Institute of Chemical Technology | PYRIMIDE-DERIVATIVE COMPOUND, OPTICAL ISOMER THEREOF, OR PHARMACEUTICAL SALT THEREOF AND COMPOSITION FOR THE PREVENTION OR TREATMENT OF TYRO-3 RELATED DISEASES THEREOF AS ACTIVE SUBSTANCE |
-
2021
- 2021-02-12 CN CN202180027810.4A patent/CN115515589A/zh active Pending
- 2021-02-12 CA CA3171187A patent/CA3171187A1/en active Pending
- 2021-02-12 US US17/799,639 patent/US20230135635A1/en active Pending
- 2021-02-12 WO PCT/US2021/018040 patent/WO2021163629A1/en not_active Ceased
- 2021-02-12 EP EP21753740.6A patent/EP4103182A4/en active Pending
- 2021-02-12 AU AU2021218739A patent/AU2021218739A1/en active Pending
- 2021-02-12 KR KR1020227028925A patent/KR20220153581A/ko active Pending
- 2021-02-12 JP JP2022549145A patent/JP2023513794A/ja active Pending
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