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 |
|---|---|---|---|---|
| SG11201704764PA (en) | 2014-12-11 | 2017-07-28 | Harvard College | Inhibitors of cellular necrosis and related methods |
| WO2016101885A1 (en) * | 2014-12-24 | 2016-06-30 | National Institute Of Biological Sciences, Beijing | Necrosis inhibitors |
| IL287136B2 (en) | 2016-02-05 | 2023-09-01 | Denali Therapeutics Inc | Receptor inhibitors - interacting with protein kinase 1 |
| JP7208137B2 (ja) | 2016-12-09 | 2023-01-18 | デナリ セラピューティクス インコーポレイテッド | 化合物、組成物および方法 |
| US12065407B2 (en) | 2017-08-21 | 2024-08-20 | Plex Pharmaceuticals, Inc. | Dual acting FKBP12 and FKBP52 inhibitors |
| CN113272272B (zh) * | 2018-11-20 | 2023-04-07 | 圣瑞诺有限公司 | Rip1抑制剂 |
| 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 |
| EP4085059B1 (en) * | 2020-01-02 | 2024-03-20 | Accro Bioscience (HK) Limited | Heteroaryl compounds as inhibitors of programmed necrosis pathway, composition and method using the same |
| JP7774579B2 (ja) | 2020-05-20 | 2025-11-21 | シロナックス リミテッド． | ピペラジン複素環アミド尿素類を含む受容体共役タンパク質１阻害剤 |
| IL298188A (en) | 2020-05-20 | 2023-01-01 | Sironax Ltd | Circular structures of piperazine |
| CN117500795A (zh) * | 2021-03-18 | 2024-02-02 | 维泰瑞隆有限公司 | 受体相互作用蛋白1抑制剂、其制备及用途 |
| IL308348A (en) | 2021-05-20 | 2024-01-01 | Sironax Ltd | RIP1 modulators including cyclic ureas aztidine, their preparation and uses |
| CN117460722A (zh) | 2021-08-10 | 2024-01-26 | 艾伯维公司 | 烟酰胺ripk1抑制剂 |
| US20240409501A1 (en) * | 2021-10-22 | 2024-12-12 | Sironax Ltd. | Cyrstalline forms of rip1 inhibitor |
| JP2024540522A (ja) | 2021-11-19 | 2024-10-31 | ザ・ブロード・インスティテュート・インコーポレイテッド | キナーゼを標的結合部分で標識するための二官能性キメラ分子及びその使用方法 |
| TW202334164A (zh) | 2022-01-12 | 2023-09-01 | 美商戴納立製藥公司 | （Ｓ）－５－苄基－Ｎ－（５－甲基－４－側氧基－２，３，４，５－四氫吡啶並［３，２－ｂ］［１，４］氧氮呯－３－基）－４Ｈ－１，２，４－三唑－３－甲醯胺的晶型 |
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 |
| EP2384753B1 (en) | 2003-08-29 | 2016-01-06 | The Brigham and Women's Hospital, Inc. | Hydantoin derivatives as inhibitors of cellular necrosis |
| RU2367661C2 (ru) | 2004-03-05 | 2009-09-20 | Тайсо Фармасьютикал Ко., Лтд. | Производные тиазола |
| CN100584842C (zh) * | 2004-03-05 | 2010-01-27 | 大正制药株式会社 | 噻唑衍生物 |
| TWI407960B (zh) * | 2007-03-23 | 2013-09-11 | Jerini Ag | 小分子緩激肽ｂ２受體調節劑 |
| EP2192838A4 (en) | 2007-08-15 | 2011-07-27 | Harvard College | HETEROCYCLIC NEKROPTOSIS HEMMER |
| WO2010075290A1 (en) | 2008-12-22 | 2010-07-01 | President And Fellows Of Harvard College | Unsaturated heterocyclic inhibitors of necroptosis |
| JP2012513481A (ja) | 2008-12-23 | 2012-06-14 | プレジデント アンド フェロウズ オブ ハーバード カレッジ | ネクロトーシスの小分子阻害剤 |
| CA2789457A1 (en) * | 2010-02-26 | 2011-09-01 | Susumu Miyazaki | 1,3,4,8-tetrahydro-2h-pyrido[1,2-a]pyrazine derivative and use of same as hiv integrase inhibitor |
| 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 |
| US9643977B2 (en) * | 2011-03-11 | 2017-05-09 | 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 |
| US20160024098A1 (en) * | 2013-03-15 | 2016-01-28 | 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 |
| WO2016101885A1 (en) * | 2014-12-24 | 2016-06-30 | National Institute Of Biological Sciences, Beijing | Necrosis inhibitors |
-
2015
- 2015-12-23 WO PCT/CN2015/098367 patent/WO2016101885A1/en not_active Ceased
- 2015-12-23 JP JP2017534534A patent/JP6772141B2/ja active Active
- 2015-12-23 AU AU2015371822A patent/AU2015371822B2/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 EP EP15871953.4A patent/EP3224237B1/en active Active
- 2015-12-23 KR KR1020177020381A patent/KR102606064B1/ko active Active
- 2015-12-23 CA CA2972366A patent/CA2972366C/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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