JP2018504393A5 - - Google Patents
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- Publication number
- JP2018504393A5 JP2018504393A5 JP2017534556A JP2017534556A JP2018504393A5 JP 2018504393 A5 JP2018504393 A5 JP 2018504393A5 JP 2017534556 A JP2017534556 A JP 2017534556A JP 2017534556 A JP2017534556 A JP 2017534556A JP 2018504393 A5 JP2018504393 A5 JP 2018504393A5
- Authority
- JP
- Japan
- Prior art keywords
- compound
- corresponding sulfonamide
- unsubstituted
- substituted
- pharmaceutically acceptable
- 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 21
- 229940124530 sulfonamide Drugs 0.000 claims 16
- 150000003456 sulfonamides Chemical class 0.000 claims 16
- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical compound C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims 12
- -1 amide compound Chemical class 0.000 claims 12
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 claims 8
- 150000003839 salts Chemical class 0.000 claims 8
- KAESVJOAVNADME-UHFFFAOYSA-N 1H-pyrrole Natural products C=1C=CNC=1 KAESVJOAVNADME-UHFFFAOYSA-N 0.000 claims 7
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical class C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims 5
- 230000017074 necrotic cell death Effects 0.000 claims 5
- WYNCHZVNFNFDNH-UHFFFAOYSA-N Oxazolidine Chemical compound C1COCN1 WYNCHZVNFNFDNH-UHFFFAOYSA-N 0.000 claims 4
- 201000010099 disease Diseases 0.000 claims 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 4
- YNGDWRXWKFWCJY-UHFFFAOYSA-N 1,4-Dihydropyridine Chemical compound C1C=CNC=C1 YNGDWRXWKFWCJY-UHFFFAOYSA-N 0.000 claims 2
- VSWICNJIUPRZIK-UHFFFAOYSA-N 2-piperideine Chemical compound C1CNC=CC1 VSWICNJIUPRZIK-UHFFFAOYSA-N 0.000 claims 2
- RSEBUVRVKCANEP-UHFFFAOYSA-N 2-pyrroline Chemical compound C1CC=CN1 RSEBUVRVKCANEP-UHFFFAOYSA-N 0.000 claims 2
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-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
- HONIICLYMWZJFZ-UHFFFAOYSA-N azetidine Chemical compound C1CNC1 HONIICLYMWZJFZ-UHFFFAOYSA-N 0.000 claims 2
- 150000001539 azetidines Chemical class 0.000 claims 2
- 150000001541 aziridines Chemical class 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
- LPIQUOYDBNQMRZ-UHFFFAOYSA-N cyclopentene Chemical compound C1CC=CC1 LPIQUOYDBNQMRZ-UHFFFAOYSA-N 0.000 claims 2
- 125000005842 heteroatom Chemical group 0.000 claims 2
- 239000000203 mixture Substances 0.000 claims 2
- OZQGLZFAWYKKLQ-UHFFFAOYSA-N oxazinane Chemical compound C1CCONC1 OZQGLZFAWYKKLQ-UHFFFAOYSA-N 0.000 claims 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims 2
- USPWKWBDZOARPV-UHFFFAOYSA-N pyrazolidine Chemical compound C1CNNC1 USPWKWBDZOARPV-UHFFFAOYSA-N 0.000 claims 2
- JYEUMXHLPRZUAT-UHFFFAOYSA-N 1,2,3-triazine Chemical compound C1=CN=NN=C1 JYEUMXHLPRZUAT-UHFFFAOYSA-N 0.000 claims 1
- OGYGFUAIIOPWQD-UHFFFAOYSA-N 1,3-thiazolidine Chemical compound C1CSCN1 OGYGFUAIIOPWQD-UHFFFAOYSA-N 0.000 claims 1
- BCHZICNRHXRCHY-UHFFFAOYSA-N 2h-oxazine Chemical compound N1OC=CC=C1 BCHZICNRHXRCHY-UHFFFAOYSA-N 0.000 claims 1
- AGIJRRREJXSQJR-UHFFFAOYSA-N 2h-thiazine Chemical compound N1SC=CC=C1 AGIJRRREJXSQJR-UHFFFAOYSA-N 0.000 claims 1
- 101001109145 Homo sapiens Receptor-interacting serine/threonine-protein kinase 1 Proteins 0.000 claims 1
- OAICVXFJPJFONN-UHFFFAOYSA-N Phosphorus Chemical compound [P] OAICVXFJPJFONN-UHFFFAOYSA-N 0.000 claims 1
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical compound C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 claims 1
- 102100022501 Receptor-interacting serine/threonine-protein kinase 1 Human genes 0.000 claims 1
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 1
- JZFICWYCTCCINF-UHFFFAOYSA-N Thiadiazin Chemical compound S=C1SC(C)NC(C)N1CCN1C(=S)SC(C)NC1C JZFICWYCTCCINF-UHFFFAOYSA-N 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 claims 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 1
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- YRTMEEURRDTMST-UHFFFAOYSA-N diazetidine Chemical compound C1CNN1 YRTMEEURRDTMST-UHFFFAOYSA-N 0.000 claims 1
- DIXBSCZRIZDQGC-UHFFFAOYSA-N diaziridine Chemical compound C1NN1 DIXBSCZRIZDQGC-UHFFFAOYSA-N 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 125000001153 fluoro group Chemical group F* 0.000 claims 1
- 102000057669 human RIPK1 Human genes 0.000 claims 1
- 230000005764 inhibitory process Effects 0.000 claims 1
- 125000001624 naphthyl group Chemical group 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- XHWNEBDUPVMPKI-UHFFFAOYSA-N oxazetidine Chemical compound C1CON1 XHWNEBDUPVMPKI-UHFFFAOYSA-N 0.000 claims 1
- SJGALSBBFTYSBA-UHFFFAOYSA-N oxaziridine Chemical compound C1NO1 SJGALSBBFTYSBA-UHFFFAOYSA-N 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- 239000001301 oxygen Substances 0.000 claims 1
- RGSFGYAAUTVSQA-UHFFFAOYSA-N pentamethylene Natural products C1CCCC1 RGSFGYAAUTVSQA-UHFFFAOYSA-N 0.000 claims 1
- 229910052698 phosphorus Inorganic materials 0.000 claims 1
- 239000011574 phosphorus Substances 0.000 claims 1
- UBRJWPDONDYLLX-UHFFFAOYSA-N pyrazolidine Chemical compound C1CNNC1.C1CNNC1 UBRJWPDONDYLLX-UHFFFAOYSA-N 0.000 claims 1
- UMJSCPRVCHMLSP-UHFFFAOYSA-N pyridine Natural products COC1=CC=CN=C1 UMJSCPRVCHMLSP-UHFFFAOYSA-N 0.000 claims 1
- 150000003233 pyrroles Chemical class 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
- 239000011593 sulfur Substances 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
- MNFSSEUNEZGWRS-UHFFFAOYSA-N thiazetidine Chemical compound C1CSN1 MNFSSEUNEZGWRS-UHFFFAOYSA-N 0.000 claims 1
- AJZGFFKDLABHDD-UHFFFAOYSA-N thiazinane Chemical compound C1CCSNC1 AJZGFFKDLABHDD-UHFFFAOYSA-N 0.000 claims 1
- DSXQWLYNLIETTE-UHFFFAOYSA-N thiaziridine Chemical compound C1NS1 DSXQWLYNLIETTE-UHFFFAOYSA-N 0.000 claims 1
- 229930192474 thiophene Natural products 0.000 claims 1
- LWRSWPKQBXMPAI-UHFFFAOYSA-N CCC(C)(C)C(N1C(c2cc(F)ccc2)NCC1)=O Chemical compound CCC(C)(C)C(N1C(c2cc(F)ccc2)NCC1)=O LWRSWPKQBXMPAI-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNPCT/CN2014/094734 | 2014-12-24 | ||
| CNPCT/CN2014/094734 | 2014-12-24 | ||
| PCT/CN2015/098385 WO2016101887A1 (en) | 2014-12-24 | 2015-12-23 | Necrosis inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018504393A JP2018504393A (ja) | 2018-02-15 |
| JP2018504393A5 true JP2018504393A5 (enExample) | 2019-01-31 |
| JP6683712B2 JP6683712B2 (ja) | 2020-04-22 |
Family
ID=56149285
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017534556A Active JP6683712B2 (ja) | 2014-12-24 | 2015-12-23 | ネクローシス阻害薬 |
Country Status (9)
| Country | Link |
|---|---|
| US (3) | US10092529B2 (enExample) |
| EP (1) | EP3224245B1 (enExample) |
| JP (1) | JP6683712B2 (enExample) |
| KR (1) | KR102596723B1 (enExample) |
| CN (1) | CN107108492B (enExample) |
| AU (1) | AU2015371824B2 (enExample) |
| CA (1) | CA2972294C (enExample) |
| HK (1) | HK1244792B (enExample) |
| WO (1) | WO2016101887A1 (enExample) |
Families Citing this family (28)
| 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 |
| TWI730959B (zh) | 2015-05-19 | 2021-06-21 | 英商葛蘭素史克智慧財產發展有限公司 | 作為激酶抑制劑之雜環醯胺 |
| IL287136B2 (en) | 2016-02-05 | 2023-09-01 | Denali Therapeutics Inc | Receptor inhibitors - interacting with protein kinase 1 |
| CN105968068B (zh) * | 2016-05-12 | 2018-08-03 | 太原理工大学 | 一种芳香亚硝基化合物与氮杂环丙烷化合物成环的方法 |
| CN105949144B (zh) * | 2016-05-12 | 2018-02-02 | 太原理工大学 | 芳香亚硝基化合物与氮杂环丙烷化合物成环的方法 |
| TW201831464A (zh) * | 2016-11-18 | 2018-09-01 | 英商葛蘭素史克智慧財產發展有限公司 | 作為激酶抑制劑之雜環醯胺 |
| 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 |
| US20200062735A1 (en) | 2017-02-27 | 2020-02-27 | Glaxosmithkline Intellectual Property Development Limited | Heterocyclic amides as kinase inhibitors |
| WO2018192416A1 (en) * | 2017-04-17 | 2018-10-25 | National Institute Of Biological Sciences, Beijing | Treating Male Senescence |
| JP7140781B2 (ja) | 2017-05-17 | 2022-09-21 | 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 |
| US12048703B2 (en) * | 2018-04-13 | 2024-07-30 | University Of North Dakota | Use of small molecule FAK activators to promote mucosal healing |
| WO2019204740A1 (en) * | 2018-04-19 | 2019-10-24 | University Of Virginia Patent Foundation | Compositions and methods for preparing and using azetidines |
| WO2020044206A1 (en) | 2018-08-29 | 2020-03-05 | Glaxosmithkline Intellectual Property Development Limited | Heterocyclic amides as kinase inhibitors for use in the treatment cancer |
| SG11202105250TA (en) * | 2018-11-20 | 2021-06-29 | Sironax Ltd | Cyclic Ureas |
| CN113272272B (zh) | 2018-11-20 | 2023-04-07 | 圣瑞诺有限公司 | Rip1抑制剂 |
| CN111978311B (zh) * | 2019-05-21 | 2024-05-31 | 中国科学院上海有机化学研究所 | 一类细胞程序性坏死抑制剂及其制备方法和用途 |
| WO2021046515A1 (en) | 2019-09-06 | 2021-03-11 | Board Of Regents, The University Of Texas System | Inhibitors of receptor interacting protein kinase i for the treatment of disease |
| IL291665B2 (en) | 2019-09-27 | 2025-07-01 | Univ Texas | Inhibitors of receptor interacting protein kinase i for the treatment of disease |
| BR112022010082A2 (pt) | 2019-11-26 | 2022-08-30 | Univ Texas | Composto de fórmula estrutural i ou sal do mesmo, composição farmacêutica, uso do composto e uso da composição farmacêutica |
| IL298188A (en) | 2020-05-20 | 2023-01-01 | Sironax Ltd | Circular structures of piperazine |
| 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 |
| KR20230012582A (ko) * | 2020-05-20 | 2023-01-26 | 시로낙스 엘티디 | 아제티딘 환형 우레아 |
| TW202214617A (zh) | 2020-06-02 | 2022-04-16 | 法商賽諾菲公司 | 作為ｒｉｐｋ１抑制劑之異㗁唑啶及其用途 |
| WO2021257849A1 (en) | 2020-06-18 | 2021-12-23 | The Regents Of The University Of California | Nitrosation reagents and methods |
| 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 |
| JP2024544533A (ja) | 2021-11-11 | 2024-12-03 | ジェンザイム・コーポレーション | Ｒｉｐｋ１阻害剤としてのイソオキサゾリジン及びその使用 |
| 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 (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| EP2384753B1 (en) | 2003-08-29 | 2016-01-06 | The Brigham and Women's Hospital, Inc. | Hydantoin derivatives as inhibitors of cellular necrosis |
| HUP0500921A2 (en) * | 2005-10-05 | 2007-07-30 | Richter Gedeon Nyrt | Tetrazole derivatives, process for their preparation and their use |
| EP1968583A4 (en) * | 2005-12-20 | 2010-09-15 | Harvard College | COMPOUNDS, SCREENING AND TREATMENT PROCEDURES |
| EP2192838A4 (en) | 2007-08-15 | 2011-07-27 | Harvard College | HETEROCYCLIC NEKROPTOSIS HEMMER |
| BRPI0820400A2 (pt) * | 2007-11-20 | 2015-05-19 | Sumitomo Chemical Co | Composto de piridina, composição pesticida e método de controle de pragas. |
| JP2010100611A (ja) * | 2008-09-26 | 2010-05-06 | Sumitomo Chemical Co Ltd | ピリジン化合物及びその有害生物の防除用途 |
| 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 |
| JP2012041325A (ja) * | 2010-08-23 | 2012-03-01 | Bayer Cropscience Ag | オキサジアゾリノン誘導体およびその有害生物の防除用途 |
| US9643977B2 (en) | 2011-03-11 | 2017-05-09 | President And Fellows Of Harvard College | Necroptosis inhibitors and methods of use therefor |
| US8889730B2 (en) * | 2012-04-10 | 2014-11-18 | Pfizer Inc. | Indole and indazole compounds that activate AMPK |
| JP5532078B2 (ja) | 2012-05-23 | 2014-06-25 | 株式会社デンソー | 乗員保護装置 |
| TWI730959B (zh) | 2015-05-19 | 2021-06-21 | 英商葛蘭素史克智慧財產發展有限公司 | 作為激酶抑制劑之雜環醯胺 |
-
2015
- 2015-12-23 EP EP15871955.9A patent/EP3224245B1/en active Active
- 2015-12-23 HK HK18104020.6A patent/HK1244792B/en unknown
- 2015-12-23 CA CA2972294A patent/CA2972294C/en active Active
- 2015-12-23 JP JP2017534556A patent/JP6683712B2/ja active Active
- 2015-12-23 AU AU2015371824A patent/AU2015371824B2/en active Active
- 2015-12-23 KR KR1020177020383A patent/KR102596723B1/ko active Active
- 2015-12-23 CN CN201580071229.7A patent/CN107108492B/zh active Active
- 2015-12-23 WO PCT/CN2015/098385 patent/WO2016101887A1/en not_active Ceased
-
2017
- 2017-06-26 US US15/632,422 patent/US10092529B2/en active Active
-
2018
- 2018-10-06 US US16/153,706 patent/US10555920B2/en active Active
-
2020
- 2020-02-11 US US16/787,052 patent/US11478438B2/en active Active
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