JP2018502101A5 - - Google Patents
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- Publication number
- JP2018502101A5 JP2018502101A5 JP2017534534A JP2017534534A JP2018502101A5 JP 2018502101 A5 JP2018502101 A5 JP 2018502101A5 JP 2017534534 A JP2017534534 A JP 2017534534A JP 2017534534 A JP2017534534 A JP 2017534534A JP 2018502101 A5 JP2018502101 A5 JP 2018502101A5
- Authority
- JP
- Japan
- Prior art keywords
- substituted
- unsubstituted
- compound
- heteroatom
- alkyl
- 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.)
- Granted
Links
- 150000001875 compounds Chemical class 0.000 claims 54
- 125000005842 heteroatom Chemical group 0.000 claims 16
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 15
- 150000003839 salts Chemical class 0.000 claims 13
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 claims 12
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 10
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 10
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical class C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims 8
- -1 amide compound Chemical class 0.000 claims 8
- 230000017074 necrotic cell death Effects 0.000 claims 6
- OAICVXFJPJFONN-UHFFFAOYSA-N Phosphorus Chemical compound [P] OAICVXFJPJFONN-UHFFFAOYSA-N 0.000 claims 5
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 5
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 5
- 201000010099 disease Diseases 0.000 claims 5
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 5
- 229910052757 nitrogen Inorganic materials 0.000 claims 5
- 229910052760 oxygen Inorganic materials 0.000 claims 5
- 239000001301 oxygen Substances 0.000 claims 5
- 229910052698 phosphorus Inorganic materials 0.000 claims 5
- 239000011574 phosphorus Substances 0.000 claims 5
- 229910052717 sulfur Inorganic materials 0.000 claims 5
- 239000011593 sulfur Substances 0.000 claims 5
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 4
- LPIQUOYDBNQMRZ-UHFFFAOYSA-N cyclopentene Chemical compound C1CC=CC1 LPIQUOYDBNQMRZ-UHFFFAOYSA-N 0.000 claims 4
- 125000001624 naphthyl group Chemical group 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- 125000004051 hexyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 3
- 239000000203 mixture Substances 0.000 claims 3
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 2
- XKTYXVDYIKIYJP-UHFFFAOYSA-N 3h-dioxole Chemical compound C1OOC=C1 XKTYXVDYIKIYJP-UHFFFAOYSA-N 0.000 claims 2
- YLQBMQCUIZJEEH-UHFFFAOYSA-N Furan Chemical compound C=1C=COC=1 YLQBMQCUIZJEEH-UHFFFAOYSA-N 0.000 claims 2
- YTPLMLYBLZKORZ-UHFFFAOYSA-N Thiophene Chemical compound C=1C=CSC=1 YTPLMLYBLZKORZ-UHFFFAOYSA-N 0.000 claims 2
- 125000003545 alkoxy group Chemical group 0.000 claims 2
- 125000000217 alkyl group Chemical group 0.000 claims 2
- 125000003118 aryl group Chemical group 0.000 claims 2
- 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 2
- ZSWFCLXCOIISFI-UHFFFAOYSA-N cyclopentadiene Chemical compound C1C=CC=C1 ZSWFCLXCOIISFI-UHFFFAOYSA-N 0.000 claims 2
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 2
- RGSFGYAAUTVSQA-UHFFFAOYSA-N pentamethylene Natural products C1CCCC1 RGSFGYAAUTVSQA-UHFFFAOYSA-N 0.000 claims 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims 2
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 1
- KAESVJOAVNADME-UHFFFAOYSA-N 1H-pyrrole Natural products C=1C=CNC=1 KAESVJOAVNADME-UHFFFAOYSA-N 0.000 claims 1
- 101001109145 Homo sapiens Receptor-interacting serine/threonine-protein kinase 1 Proteins 0.000 claims 1
- 241000023320 Luma <angiosperm> Species 0.000 claims 1
- 102100022501 Receptor-interacting serine/threonine-protein kinase 1 Human genes 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 claims 1
- 125000003342 alkenyl group Chemical group 0.000 claims 1
- 125000000304 alkynyl group Chemical group 0.000 claims 1
- 125000004122 cyclic group Chemical group 0.000 claims 1
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 1
- SINKOGOPEQSHQD-UHFFFAOYSA-N cyclopentadienide Chemical compound C=1C=C[CH-]C=1 SINKOGOPEQSHQD-UHFFFAOYSA-N 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 125000000623 heterocyclic group Chemical group 0.000 claims 1
- 102000057669 human RIPK1 Human genes 0.000 claims 1
- 150000004677 hydrates Chemical class 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 230000005764 inhibitory process Effects 0.000 claims 1
- 125000001973 tert-pentyl group Chemical group [H]C([H])([H])C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 1
- 229940124597 therapeutic agent Drugs 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNPCT/CN2014/094735 | 2014-12-24 | ||
| CNPCT/CN2014/094735 | 2014-12-24 | ||
| PCT/CN2015/098367 WO2016101885A1 (en) | 2014-12-24 | 2015-12-23 | Necrosis inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018502101A JP2018502101A (ja) | 2018-01-25 |
| JP2018502101A5 true JP2018502101A5 (enExample) | 2019-01-31 |
| JP6772141B2 JP6772141B2 (ja) | 2020-10-21 |
Family
ID=56149283
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017534534A Active JP6772141B2 (ja) | 2014-12-24 | 2015-12-23 | ネクローシス阻害薬 |
Country Status (8)
| Country | Link |
|---|---|
| US (2) | US9974762B2 (enExample) |
| EP (1) | EP3224237B1 (enExample) |
| JP (1) | JP6772141B2 (enExample) |
| KR (1) | KR102606064B1 (enExample) |
| CN (2) | CN115197098B (enExample) |
| AU (1) | AU2015371822B2 (enExample) |
| CA (1) | CA2972366C (enExample) |
| WO (1) | WO2016101885A1 (enExample) |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2016094846A1 (en) | 2014-12-11 | 2016-06-16 | President And Fellows Of Harvard College | Inhibitors of cellular necrosis and related methods |
| JP6772141B2 (ja) * | 2014-12-24 | 2020-10-21 | ナショナル・インスティチュート・オブ・バイオロジカル・サイエンシズ，ベイジン | ネクローシス阻害薬 |
| SG10201913587WA (en) | 2016-02-05 | 2020-02-27 | Denali Therapeutics Inc | Inhibitors of receptor-interacting protein kinase 1 |
| DK3552017T3 (da) | 2016-12-09 | 2022-05-16 | Denali Therapeutics Inc | Forbindelser, der er anvendelige som ripk1-inhibitorer |
| US12065407B2 (en) | 2017-08-21 | 2024-08-20 | Plex Pharmaceuticals, Inc. | Dual acting FKBP12 and FKBP52 inhibitors |
| CA3120726C (en) * | 2018-11-20 | 2023-05-09 | Sironax Ltd | Rip1 inhibitors |
| EP3811937A1 (en) * | 2019-10-24 | 2021-04-28 | Sorbonne Universite | Compounds for use in the prevention and/or treatment of non-alcoholic fatty liver disease |
| WO2021138694A1 (en) * | 2020-01-02 | 2021-07-08 | Accro Bioscience Inc. | Heteroaryl compounds as inhibitors of programmed necrosis pathway, composition and method using the same |
| US12612388B2 (en) | 2020-05-20 | 2026-04-28 | Sironax Ltd. | Receptor-interacting protein 1 inhibitors including piperazine heterocyclic amide ureas |
| JP7760530B2 (ja) | 2020-05-20 | 2025-10-27 | シロナックス リミテッド． | ピペラジン環状尿素類 |
| JP2024512931A (ja) * | 2021-03-18 | 2024-03-21 | シロナックス リミテッド． | 受容体相互作用タンパク質１阻害剤、その調製、及び使用 |
| US20240294508A1 (en) | 2021-05-20 | 2024-09-05 | Sironax Ltd. | Rip1 modulators including azetidine cyclic ureas, preparations, and uses thereof |
| EP4301744A1 (en) | 2021-08-10 | 2024-01-10 | AbbVie Inc. | Nicotinamide ripk1 inhibitors |
| CN118139841A (zh) * | 2021-10-22 | 2024-06-04 | 维泰瑞隆有限公司 | Rip1抑制剂的结晶形式 |
| US12404348B2 (en) | 2021-11-19 | 2025-09-02 | The Brigham And Women's Hospital, Inc. | Bifunctional chimeric molecules for labeling of kinases with target binding moieties and methods of use thereof |
| WO2023137035A1 (en) | 2022-01-12 | 2023-07-20 | Denali Therapeutics Inc. | Crystalline forms of (s)-5-benzyl-n-(5-methyl-4-oxo-2, 3,4,5- tetrahydropyrido [3,2-b] [l,4]oxazepin-3-yl)-4h-l,2,4-triazole-3-carboxamide |
Family Cites Families (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3498792A (en) * | 1965-08-07 | 1970-03-03 | Fuji Photo Film Co Ltd | Silver halide photographic compositions containing a sulfinamide as a fog inhibitor |
| US4405357A (en) * | 1980-06-02 | 1983-09-20 | Fmc Corporation | Herbicidal 3-isoxazolidinones and hydroxamic acids |
| US4337332A (en) * | 1981-04-09 | 1982-06-29 | Minnesota Mining And Manufacturing Company | Latently curable organosilicone compositions |
| GB8531839D0 (en) * | 1985-12-30 | 1986-02-05 | Wellcome Found | Aryl derivatives |
| US4957533A (en) * | 1987-10-26 | 1990-09-18 | Eli Lilly And Company | N-phenylalkylbenzamide fungicides |
| US5189180A (en) * | 1989-09-28 | 1993-02-23 | E. R. Squibb & Sons, Inc. | Seco-mevinic acid derivatives useful as antihypercholesterolemic agents and new intermediates |
| US6756394B1 (en) | 1999-10-15 | 2004-06-29 | President And Fellow Of Harvard College | Small molecule inhibitors of necrosis |
| US6706766B2 (en) | 1999-12-13 | 2004-03-16 | President And Fellows Of Harvard College | Small molecules used to increase cell death |
| GB0011838D0 (en) * | 2000-05-17 | 2000-07-05 | Astrazeneca Ab | Chemical compounds |
| DK2384753T3 (en) | 2003-08-29 | 2016-04-11 | Brigham & Womens Hospital | Hydantoin derivatives as inhibitors of cell necrosis |
| CN100584842C (zh) * | 2004-03-05 | 2010-01-27 | 大正制药株式会社 | 噻唑衍生物 |
| US7678810B2 (en) * | 2004-03-05 | 2010-03-16 | Taisho Pharmaceutical Co., Ltd | Thiazole derivative |
| TWI407960B (zh) * | 2007-03-23 | 2013-09-11 | Jerini Ag | 小分子緩激肽ｂ２受體調節劑 |
| CA2696349A1 (en) | 2007-08-15 | 2009-02-19 | President And Fellows Of Harvard College | Heterocyclic inhibitors of necroptosis |
| WO2010075290A1 (en) | 2008-12-22 | 2010-07-01 | President And Fellows Of Harvard College | Unsaturated heterocyclic inhibitors of necroptosis |
| BRPI0923126A2 (pt) * | 2008-12-23 | 2021-09-08 | President And Fellows Of Harvard College | Compostos inibidores de molécula pequena de necroptose, uso e composição compreendendo os mesmos e método de diminuir necroptose |
| MX2012009869A (es) * | 2010-02-26 | 2012-09-12 | Japan Tobacco Inc | Derivado de 1, 3,4, 8-tetrahidro-2h-pirido[1, 2-a]pirazina y sus uso como inhibidor de la integrasa del vih. |
| AR084174A1 (es) * | 2010-12-21 | 2013-04-24 | Lilly Co Eli | Compuestos de imidazol-2-benzamida utiles para el tratamiento de osteoartritis y una composicion farmaceutica |
| WO2012125544A2 (en) * | 2011-03-11 | 2012-09-20 | President And Fellows Of Harvard College | Necroptosis inhibitors and methods of use therefor |
| CN102503860A (zh) * | 2011-11-14 | 2012-06-20 | 武汉大学 | 一种1，3-二取代脲和氨基甲酸酯的合成方法 |
| CN102617259B (zh) * | 2012-03-09 | 2014-12-24 | 温州大学 | 一种醇与胺脱水合成胺类化合物的方法 |
| WO2014160185A2 (en) * | 2013-03-14 | 2014-10-02 | The Board Of Trustees Of The Leland Stanford Junior University | Mitochondrial aldehyde dehydrogenase-2 modulators and methods of use thereof |
| EP2968276A4 (en) * | 2013-03-15 | 2017-02-15 | President and Fellows of Harvard College | Hybrid necroptosis inhibitors |
| TWI651310B (zh) * | 2014-02-20 | 2019-02-21 | 日商日本煙草產業股份有限公司 | 三化合物及其醫藥用途 |
| JP6772141B2 (ja) * | 2014-12-24 | 2020-10-21 | ナショナル・インスティチュート・オブ・バイオロジカル・サイエンシズ，ベイジン | ネクローシス阻害薬 |
-
2015
- 2015-12-23 JP JP2017534534A patent/JP6772141B2/ja active Active
- 2015-12-23 CA CA2972366A patent/CA2972366C/en active Active
- 2015-12-23 CN CN202210717817.5A patent/CN115197098B/zh active Active
- 2015-12-23 CN CN201580071413.1A patent/CN107108467B/zh active Active
- 2015-12-23 WO PCT/CN2015/098367 patent/WO2016101885A1/en not_active Ceased
- 2015-12-23 EP EP15871953.4A patent/EP3224237B1/en active Active
- 2015-12-23 KR KR1020177020381A patent/KR102606064B1/ko active Active
- 2015-12-23 AU AU2015371822A patent/AU2015371822B2/en active Active
-
2017
- 2017-06-26 US US15/632,412 patent/US9974762B2/en active Active
-
2018
- 2018-05-22 US US15/985,698 patent/US10682319B2/en active Active
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