JPWO2022174253A5 - - Google Patents
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- JPWO2022174253A5 JPWO2022174253A5 JP2023548686A JP2023548686A JPWO2022174253A5 JP WO2022174253 A5 JPWO2022174253 A5 JP WO2022174253A5 JP 2023548686 A JP2023548686 A JP 2023548686A JP 2023548686 A JP2023548686 A JP 2023548686A JP WO2022174253 A5 JPWO2022174253 A5 JP WO2022174253A5
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- JP
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- Prior art keywords
- nitrogen
- compound
- sulfur
- oxygen
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- 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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- 150000001875 compounds Chemical class 0.000 claims description 94
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 89
- 229910052757 nitrogen Inorganic materials 0.000 claims description 82
- 125000005842 heteroatom Chemical group 0.000 claims description 78
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims description 76
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims description 76
- 229910052760 oxygen Inorganic materials 0.000 claims description 76
- 239000001301 oxygen Chemical group 0.000 claims description 76
- 229920006395 saturated elastomer Polymers 0.000 claims description 76
- 239000011593 sulfur Chemical group 0.000 claims description 76
- 229910052717 sulfur Chemical group 0.000 claims description 76
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims description 75
- 150000003839 salts Chemical class 0.000 claims description 47
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 26
- 125000001931 aliphatic group Chemical group 0.000 claims description 24
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 24
- 125000002950 monocyclic group Chemical group 0.000 claims description 24
- 125000000623 heterocyclic group Chemical group 0.000 claims description 22
- 229910052736 halogen Inorganic materials 0.000 claims description 18
- 150000002367 halogens Chemical class 0.000 claims description 18
- 125000002619 bicyclic group Chemical group 0.000 claims description 14
- -1 2H-pyrrolyl Chemical group 0.000 claims description 12
- 101001059991 Homo sapiens Mitogen-activated protein kinase kinase kinase kinase 1 Proteins 0.000 claims description 12
- 102100028199 Mitogen-activated protein kinase kinase kinase kinase 1 Human genes 0.000 claims description 12
- OAICVXFJPJFONN-UHFFFAOYSA-N Phosphorus Chemical group [P] OAICVXFJPJFONN-UHFFFAOYSA-N 0.000 claims description 10
- XUIMIQQOPSSXEZ-UHFFFAOYSA-N Silicon Chemical group [Si] XUIMIQQOPSSXEZ-UHFFFAOYSA-N 0.000 claims description 10
- 239000008194 pharmaceutical composition Substances 0.000 claims description 10
- 229910052698 phosphorus Inorganic materials 0.000 claims description 10
- 239000011574 phosphorus Chemical group 0.000 claims description 10
- 229910052710 silicon Inorganic materials 0.000 claims description 10
- 239000010703 silicon Chemical group 0.000 claims description 10
- 125000002618 bicyclic heterocycle group Chemical group 0.000 claims description 8
- 125000000160 oxazolidinyl group Chemical group 0.000 claims description 8
- 125000003566 oxetanyl group Chemical group 0.000 claims description 8
- 230000002062 proliferating effect Effects 0.000 claims description 8
- 125000004076 pyridyl group Chemical group 0.000 claims description 8
- 125000000714 pyrimidinyl group Chemical group 0.000 claims description 8
- 229910052739 hydrogen Inorganic materials 0.000 claims description 6
- 238000000034 method Methods 0.000 claims description 6
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims description 6
- 125000004502 1,2,3-oxadiazolyl group Chemical group 0.000 claims description 4
- 125000001399 1,2,3-triazolyl group Chemical group N1N=NC(=C1)* 0.000 claims description 4
- 125000004504 1,2,4-oxadiazolyl group Chemical group 0.000 claims description 4
- 125000001376 1,2,4-triazolyl group Chemical group N1N=C(N=C1)* 0.000 claims description 4
- 125000001781 1,3,4-oxadiazolyl group Chemical group 0.000 claims description 4
- 206010028980 Neoplasm Diseases 0.000 claims description 4
- 230000003213 activating effect Effects 0.000 claims description 4
- 125000002393 azetidinyl group Chemical group 0.000 claims description 4
- 201000011510 cancer Diseases 0.000 claims description 4
- 229910052799 carbon Inorganic materials 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
- 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 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
- 201000010099 disease Diseases 0.000 claims description 4
- 208000035475 disorder Diseases 0.000 claims description 4
- 239000003814 drug Substances 0.000 claims description 4
- 125000003838 furazanyl group Chemical group 0.000 claims description 4
- 125000002541 furyl group Chemical group 0.000 claims description 4
- 125000002632 imidazolidinyl group Chemical group 0.000 claims description 4
- 125000002636 imidazolinyl group Chemical group 0.000 claims description 4
- 125000002883 imidazolyl group Chemical group 0.000 claims description 4
- 125000001786 isothiazolyl group Chemical group 0.000 claims description 4
- 125000000842 isoxazolyl group Chemical group 0.000 claims description 4
- 230000001404 mediated effect Effects 0.000 claims description 4
- 230000035772 mutation Effects 0.000 claims description 4
- 125000001624 naphthyl group Chemical group 0.000 claims description 4
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 4
- 125000001715 oxadiazolyl group Chemical group 0.000 claims description 4
- 125000002971 oxazolyl group Chemical group 0.000 claims description 4
- 125000004193 piperazinyl group Chemical group 0.000 claims description 4
- 125000003386 piperidinyl group Chemical group 0.000 claims description 4
- 125000004309 pyranyl group Chemical group O1C(C=CC=C1)* 0.000 claims description 4
- 125000003373 pyrazinyl group Chemical group 0.000 claims description 4
- 125000003072 pyrazolidinyl group Chemical group 0.000 claims description 4
- 125000002755 pyrazolinyl group Chemical group 0.000 claims description 4
- 125000003226 pyrazolyl group Chemical group 0.000 claims description 4
- 125000002098 pyridazinyl group Chemical group 0.000 claims description 4
- 125000001422 pyrrolinyl group Chemical group 0.000 claims description 4
- 125000000168 pyrrolyl group Chemical group 0.000 claims description 4
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims description 4
- 125000000335 thiazolyl group Chemical group 0.000 claims description 4
- 125000001544 thienyl group Chemical group 0.000 claims description 4
- 125000004306 triazinyl group Chemical group 0.000 claims description 4
- 239000002671 adjuvant Substances 0.000 claims description 2
- 125000003118 aryl group Chemical group 0.000 claims description 2
- 125000004429 atom Chemical group 0.000 claims description 2
- 239000012472 biological sample Substances 0.000 claims description 2
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 125000001072 heteroaryl group Chemical group 0.000 claims description 2
- 125000001183 hydrocarbyl group Chemical group 0.000 claims description 2
- 239000001257 hydrogen Substances 0.000 claims description 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 2
- 230000002401 inhibitory effect Effects 0.000 claims description 2
- 238000004519 manufacturing process Methods 0.000 claims description 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims description 2
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims description 2
- 125000002757 morpholinyl group Chemical group 0.000 claims description 2
- 125000001147 pentyl group Chemical group C(CCCC)* 0.000 claims description 2
- 239000000523 sample Substances 0.000 claims description 2
- 125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims description 2
- 125000003003 spiro group Chemical group 0.000 claims description 2
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims description 2
- 239000003981 vehicle Substances 0.000 claims description 2
- 125000001834 xanthenyl group Chemical group C1=CC=CC=2OC3=CC=CC=C3C(C12)* 0.000 claims description 2
- 239000000203 mixture Substances 0.000 claims 5
- LMBFAGIMSUYTBN-MPZNNTNKSA-N teixobactin Chemical compound C([C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H](CCC(N)=O)C(=O)N[C@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H]1C(N[C@@H](C)C(=O)N[C@@H](C[C@@H]2NC(=N)NC2)C(=O)N[C@H](C(=O)O[C@H]1C)[C@@H](C)CC)=O)NC)C1=CC=CC=C1 LMBFAGIMSUYTBN-MPZNNTNKSA-N 0.000 claims 1
- 102000004127 Cytokines Human genes 0.000 description 1
- 108090000695 Cytokines Proteins 0.000 description 1
- 102000001253 Protein Kinase Human genes 0.000 description 1
- 238000010835 comparative analysis Methods 0.000 description 1
- 238000000338 in vitro Methods 0.000 description 1
- 238000001727 in vivo Methods 0.000 description 1
- 239000003112 inhibitor Substances 0.000 description 1
- 230000031146 intracellular signal transduction Effects 0.000 description 1
- 230000001575 pathological effect Effects 0.000 description 1
- 108060006633 protein kinase Proteins 0.000 description 1
- 230000019491 signal transduction Effects 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US202163148857P | 2021-02-12 | 2021-02-12 | |
| US63/148,857 | 2021-02-12 | ||
| PCT/US2022/070627 WO2022174253A1 (en) | 2021-02-12 | 2022-02-11 | Hpk1 antagonists and uses thereof |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2024506909A JP2024506909A (ja) | 2024-02-15 |
| JPWO2022174253A5 true JPWO2022174253A5 (https=) | 2025-02-18 |
| JP2024506909A5 JP2024506909A5 (https=) | 2025-02-18 |
Family
ID=82837982
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2023548686A Pending JP2024506909A (ja) | 2021-02-12 | 2022-02-11 | Ｈｐｋ１アンタゴニスト及びその使用 |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US12252488B2 (https=) |
| EP (1) | EP4291235A4 (https=) |
| JP (1) | JP2024506909A (https=) |
| CN (1) | CN117120090A (https=) |
| WO (1) | WO2022174253A1 (https=) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI721623B (zh) | 2018-10-31 | 2021-03-11 | 美商基利科學股份有限公司 | 經取代之6-氮雜苯并咪唑化合物 |
| TW202136261A (zh) | 2018-10-31 | 2021-10-01 | 美商基利科學股份有限公司 | 經取代之6-氮雜苯并咪唑化合物 |
| US11453681B2 (en) | 2019-05-23 | 2022-09-27 | Gilead Sciences, Inc. | Substituted eneoxindoles and uses thereof |
| CN116063329A (zh) * | 2021-10-29 | 2023-05-05 | 北京望实智慧科技有限公司 | Hpk1抑制剂、制备方法及其用途 |
| WO2023193759A1 (en) * | 2022-04-07 | 2023-10-12 | Insilico Medicine Ip Limited | Hpk1 antagonists and uses thereof |
| GB202216324D0 (en) * | 2022-11-02 | 2022-12-14 | Cerevance Ltd | Novel compounds |
| WO2024140679A1 (en) * | 2022-12-26 | 2024-07-04 | Insilico Medicine Ip Limited | Spirocyclic hpk1 antagonists and uses thereof |
| US11932649B1 (en) | 2023-08-17 | 2024-03-19 | King Faisal University | 5-(3-substituted phenyl)-pyrimido[4,5-d]pyrimidine-2,4,7(1H,3H,8H)-trione derivatives as anticancer agents |
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| WO2016101119A1 (en) | 2014-12-23 | 2016-06-30 | Merck Sharp & Dohme Corp. | Fused heteroaryl derivatives as orexin receptor antagonists |
| RS61919B1 (sr) | 2015-06-25 | 2021-06-30 | Univ Health Network | Inhibitori hpk1 i postupci za njihovo korišćenje |
| CN108699077B (zh) | 2016-01-15 | 2021-03-02 | 英安塔制药有限公司 | 作为rsv抑制剂的杂环化合物 |
| EP3523289A1 (en) | 2016-10-07 | 2019-08-14 | Araxes Pharma LLC | Heterocyclic compounds as inhibitors of ras and methods of use thereof |
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| MX2019011511A (es) | 2017-03-30 | 2019-11-18 | Hoffmann La Roche | Naftiridinas como inhibidores de cinasa 1 progenitora hematopoyetica (hpk1). |
| WO2019070742A1 (en) * | 2017-10-03 | 2019-04-11 | Sidecar Therapeutics, Inc. | APOPTOSIS SIGNAL REGULATION KINASE 1 (ASK 1) INHIBITORS COMPOUNDS |
| WO2019164847A1 (en) | 2018-02-20 | 2019-08-29 | Incyte Corporation | Indazole compounds and uses thereof |
| US12539292B2 (en) | 2018-04-01 | 2026-02-03 | Arvinas Operations, Inc. | BRM targeting compounds and associated methods of use |
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| WO2020106307A1 (en) * | 2018-11-20 | 2020-05-28 | Nflection Therapeutics, Inc. | Aryl-aniline and heteroaryl-aniline compounds for treatment of birthmarks |
| WO2020111087A1 (ja) * | 2018-11-28 | 2020-06-04 | 武田薬品工業株式会社 | 複素環化合物 |
| CN111961035B (zh) * | 2019-05-20 | 2022-11-01 | 南京科技职业学院 | 一类含有羟基异喹啉类结构的化合物、药物组合物以及其应用 |
| IL289612B2 (en) * | 2019-07-04 | 2026-02-01 | Qilu Regor Therapeutics Inc | HPK1 inhibitors and their uses |
| CN114945366B (zh) * | 2019-09-13 | 2025-01-07 | 林伯士萨顿公司 | Hpk1拮抗剂和其用途 |
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2022
- 2022-02-11 CN CN202280027804.3A patent/CN117120090A/zh active Pending
- 2022-02-11 US US17/650,732 patent/US12252488B2/en active Active
- 2022-02-11 WO PCT/US2022/070627 patent/WO2022174253A1/en not_active Ceased
- 2022-02-11 JP JP2023548686A patent/JP2024506909A/ja active Pending
- 2022-02-11 EP EP22753561.4A patent/EP4291235A4/en active Pending
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