JP2010536761A5 - - Google Patents
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- Publication number
- JP2010536761A5 JP2010536761A5 JP2010521050A JP2010521050A JP2010536761A5 JP 2010536761 A5 JP2010536761 A5 JP 2010536761A5 JP 2010521050 A JP2010521050 A JP 2010521050A JP 2010521050 A JP2010521050 A JP 2010521050A JP 2010536761 A5 JP2010536761 A5 JP 2010536761A5
- Authority
- JP
- Japan
- Prior art keywords
- pharmaceutically acceptable
- solvate
- stereoisomer
- acceptable salt
- compound
- 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
- 150000003839 salts Chemical class 0.000 claims 28
- 239000012453 solvate Substances 0.000 claims 28
- 125000000217 alkyl group Chemical group 0.000 claims 20
- 150000001875 compounds Chemical class 0.000 claims 18
- 229910052736 halogen Inorganic materials 0.000 claims 14
- 150000002367 halogens Chemical class 0.000 claims 14
- 229910052739 hydrogen Inorganic materials 0.000 claims 12
- 239000001257 hydrogen Substances 0.000 claims 12
- 125000004093 cyano group Chemical group *C#N 0.000 claims 6
- 150000002431 hydrogen Chemical group 0.000 claims 6
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 6
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 5
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 5
- 229910052799 carbon Inorganic materials 0.000 claims 5
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims 4
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 4
- 125000003545 alkoxy group Chemical group 0.000 claims 4
- 229910052801 chlorine Inorganic materials 0.000 claims 4
- 239000000460 chlorine Substances 0.000 claims 4
- 125000000753 cycloalkyl group Chemical group 0.000 claims 4
- 229910052731 fluorine Inorganic materials 0.000 claims 4
- 239000011737 fluorine Substances 0.000 claims 4
- 125000003107 substituted aryl group Chemical group 0.000 claims 4
- 150000003857 carboxamides Chemical class 0.000 claims 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 3
- 208000024891 symptom Diseases 0.000 claims 3
- XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Chemical compound NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 claims 2
- 229910052717 sulfur Inorganic materials 0.000 claims 2
- KXDHJXZQYSOELW-UHFFFAOYSA-M Carbamate Chemical compound NC([O-])=O KXDHJXZQYSOELW-UHFFFAOYSA-M 0.000 claims 1
- KXDHJXZQYSOELW-UHFFFAOYSA-N Carbamic acid Chemical group NC(O)=O KXDHJXZQYSOELW-UHFFFAOYSA-N 0.000 claims 1
- BVKZGUZCCUSVTD-UHFFFAOYSA-L Carbonate Chemical compound [O-]C([O-])=O BVKZGUZCCUSVTD-UHFFFAOYSA-L 0.000 claims 1
- 206010019196 Head injury Diseases 0.000 claims 1
- OAKJQQAXSVQMHS-UHFFFAOYSA-N Hydrazine Chemical compound NN OAKJQQAXSVQMHS-UHFFFAOYSA-N 0.000 claims 1
- 208000012902 Nervous system disease Diseases 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 claims 1
- 125000004104 aryloxy group Chemical group 0.000 claims 1
- 150000001540 azides Chemical group 0.000 claims 1
- 210000004556 brain Anatomy 0.000 claims 1
- 230000030833 cell death Effects 0.000 claims 1
- 230000024245 cell differentiation Effects 0.000 claims 1
- 230000004663 cell proliferation Effects 0.000 claims 1
- 208000029078 coronary artery disease Diseases 0.000 claims 1
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
- 150000002148 esters Chemical class 0.000 claims 1
- 125000001207 fluorophenyl group Chemical group 0.000 claims 1
- -1 hydrogen compound Chemical class 0.000 claims 1
- 230000004068 intracellular signaling Effects 0.000 claims 1
- 208000037906 ischaemic injury Diseases 0.000 claims 1
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 1
- 150000002576 ketones Chemical class 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 230000002107 myocardial effect Effects 0.000 claims 1
- 230000021597 necroptosis Effects 0.000 claims 1
- 230000004770 neurodegeneration Effects 0.000 claims 1
- 208000015122 neurodegenerative disease Diseases 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 230000002207 retinal effect Effects 0.000 claims 1
- 0 *c1c(*N*c2c(C3CC3)nn[s]2)c(F)ccc1 Chemical compound *c1c(*N*c2c(C3CC3)nn[s]2)c(F)ccc1 0.000 description 16
- NFGOUMMGMGHCJJ-MRVPVSSYSA-N CC(C)[C@@H](C)c(c(N)ccc1)c1N Chemical compound CC(C)[C@@H](C)c(c(N)ccc1)c1N NFGOUMMGMGHCJJ-MRVPVSSYSA-N 0.000 description 1
- RYPGXQXLHDFTQD-UHFFFAOYSA-N CC(C)c1c(C=C)cccc1N Chemical compound CC(C)c1c(C=C)cccc1N RYPGXQXLHDFTQD-UHFFFAOYSA-N 0.000 description 1
- HDNVDXJTQZMBCR-UHFFFAOYSA-N Cc1c(C(NCc(c(F)ccc2)c2Cl)=O)[s]nn1 Chemical compound Cc1c(C(NCc(c(F)ccc2)c2Cl)=O)[s]nn1 HDNVDXJTQZMBCR-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US95596607P | 2007-08-15 | 2007-08-15 | |
| US60/955,966 | 2007-08-15 | ||
| US3817508P | 2008-03-20 | 2008-03-20 | |
| US61/038,175 | 2008-03-20 | ||
| PCT/US2008/009793 WO2009023272A1 (en) | 2007-08-15 | 2008-08-15 | Heterocyclic inhibitors of necroptosis |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2010536761A JP2010536761A (ja) | 2010-12-02 |
| JP2010536761A5 true JP2010536761A5 (https=) | 2011-09-29 |
| JP5645663B2 JP5645663B2 (ja) | 2014-12-24 |
Family
ID=40351022
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010521050A Active JP5645663B2 (ja) | 2007-08-15 | 2008-08-15 | ネクロトーシスのヘテロ環式抑制剤 |
Country Status (5)
| Country | Link |
|---|---|
| US (5) | US20090099242A1 (https=) |
| EP (2) | EP2192838A4 (https=) |
| JP (1) | JP5645663B2 (https=) |
| CA (1) | CA2696349A1 (https=) |
| WO (1) | WO2009023272A1 (https=) |
Families Citing this family (29)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| SI2384753T1 (sl) * | 2003-08-29 | 2016-06-30 | The Brigham And Women's Hospital, Inc. | Hidantoinski derivati kot inhibitorji celične nekroze |
| EP1968583A4 (en) * | 2005-12-20 | 2010-09-15 | Harvard College | COMPOUNDS, SCREENING AND TREATMENT PROCEDURES |
| CA2772760A1 (en) | 2008-12-23 | 2010-07-01 | President And Fellows Of Harvard College | Small molecule inhibitors of necroptosis |
| US20130137642A1 (en) | 2010-04-23 | 2013-05-30 | Demetrios Vavvas | Methods and compositions for preserving photoreceptor and retinal pigment epithelial cells |
| AU2011263416B2 (en) | 2010-06-11 | 2014-04-10 | Rhodes Technologies | Process for N-dealkylation of tertiary amines |
| CA2802295C (en) | 2010-06-11 | 2016-09-20 | Rhodes Technologies | Transition metal-catalyzed processes for the preparation of n-allyl compounds and use thereof |
| US20140024598A1 (en) | 2010-11-01 | 2014-01-23 | Demetrios Vavvas | Methods and compositions for preserving retinal ganglion cells |
| WO2012125544A2 (en) | 2011-03-11 | 2012-09-20 | President And Fellows Of Harvard College | Necroptosis inhibitors and methods of use therefor |
| EP2773341A2 (en) * | 2011-10-21 | 2014-09-10 | Massachusetts Eye & Ear Infirmary | Compositions comprising necrosis inhibitors, such as necrostatins, alone or in combination, for promoting axon regeneration and nerve function, thereby treating cns disorders |
| TWI648274B (zh) | 2013-02-15 | 2019-01-21 | 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類 （二） |
| US9725452B2 (en) | 2013-03-15 | 2017-08-08 | Presidents And Fellows Of Harvard College | Substituted indoles and pyrroles as RIP kinase inhibitors |
| CN103535358B (zh) * | 2013-10-18 | 2015-04-15 | 孙家隆 | 一组邻位取代苯甲酰化合物的杀菌剂用途 |
| EP3229807A4 (en) | 2014-12-11 | 2018-10-17 | President and Fellows of Harvard College | Inhibitors of cellular necrosis and related methods |
| AU2015371822B2 (en) * | 2014-12-24 | 2020-04-09 | National Institute Of Biological Sciences, Beijing | Necrosis inhibitors |
| HK1244792B (en) | 2014-12-24 | 2019-07-12 | 北京生命科学研究所 | Necrosis inhibitors |
| IL247368A0 (en) | 2016-08-18 | 2016-11-30 | Yeda Res & Dev | Diagnostic and therapeutic uses of exosomes |
| EA202092580A1 (ru) | 2018-05-03 | 2021-04-07 | Ригел Фармасьютикалз, Инк. | Соединения, ингибирующие rip1, а также способы их получения и применения |
| UA128160C2 (uk) | 2018-05-03 | 2024-04-24 | Райджел Фармасутікалс, Інк. | Сполуки, що інгібують rip1, а також способи їх одержання та застосування |
| EP3883918B1 (en) | 2018-11-20 | 2023-07-19 | Sironax Ltd | Rip1 inhibitors |
| 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 |
| CA3149926A1 (en) | 2019-09-06 | 2021-03-11 | Yan Chen | Rip1 inhibitory compounds and methods for making and using the same |
| KR102793185B1 (ko) | 2019-09-06 | 2025-04-09 | 리겔 파마슈티칼스, 인크. | Rip1 억제 화합물 및 그를 제조 및 사용하는 방법 |
| AU2020378407B2 (en) | 2019-11-07 | 2024-02-01 | Rigel Pharmaceuticals, Inc. | Heterocyclic RIP1 inhibitory compounds |
| AR121717A1 (es) | 2020-04-02 | 2022-06-29 | Rigel Pharmaceuticals Inc | Inhibidores de rip1k |
| CN115697991B (zh) | 2020-05-20 | 2024-11-22 | 维泰瑞隆有限公司 | 哌嗪环状脲 |
| TWI840311B (zh) | 2020-07-01 | 2024-04-21 | 美商雷傑製藥公司 | Rip1k抑制劑 |
| CN116600787A (zh) * | 2020-11-19 | 2023-08-15 | 阿库西亚医疗有限责任公司 | 非水性凝胶组合物 |
| AR125587A1 (es) | 2021-03-11 | 2023-08-02 | Rigel Pharmaceuticals Inc | Inhibidores heterocíclicos de la quinasa de rip1 |
| CA3218159A1 (en) | 2021-05-20 | 2022-11-24 | Zhaolan ZHANG | Rip1 modulators including azetidine cyclic ureas, preparations, and uses thereof |
Family Cites Families (31)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE2728523C2 (de) * | 1977-06-23 | 1986-02-27 | Schering AG, 1000 Berlin und 4709 Bergkamen | 4-Methyl-1,2,3-thiadiazol-5-carbonsäure-(cyclohexylmethyl)-amid, Mittel mit herbizider und wachstumsregulatorischer Wirkung enthaltend diese Verbindung sowie Verfahren zu seiner Herstellung |
| US4356787A (en) | 1977-12-30 | 1982-11-02 | Harley Richard C | Float construction |
| AU725138B2 (en) * | 1996-09-30 | 2000-10-05 | Nihon Nohyaku Co., Ltd. | 1,2,3-thiadiazole derivatives and salts thereof, disease controlling agents for agricultural and horticultural use, and method for the use thereof |
| JPH10152482A (ja) * | 1996-09-30 | 1998-06-09 | Nippon Nohyaku Co Ltd | １，２，３−チアジアゾール誘導体又はその塩類及び農園芸用病害防除剤ならびにその使用方法 |
| ATE228119T1 (de) * | 1998-04-15 | 2002-12-15 | Pfizer Prod Inc | Heterocyclische carboxamide |
| JP2000103710A (ja) * | 1998-07-30 | 2000-04-11 | Nippon Nohyaku Co Ltd | 殺菌剤組成物及びその使用方法 |
| EP0976326B1 (en) | 1998-07-30 | 2003-05-02 | Nihon Nohyaku Co., Ltd. | Fungicidal composition containing a 1,2,3-tiadiazole derivative and its use |
| US6756394B1 (en) * | 1999-10-15 | 2004-06-29 | President And Fellow Of Harvard College | Small molecule inhibitors of necrosis |
| US6420400B1 (en) * | 2000-04-07 | 2002-07-16 | Kinetek Pharmaceuticals, Inc. | Antiproliferative 1,2,3-thiadiazole compounds |
| DE60227655D1 (de) * | 2001-04-19 | 2008-08-28 | Dainippon Sumitomo Pharma Co | Pyrrolderivat |
| DE10132686A1 (de) * | 2001-07-05 | 2003-01-16 | Boehringer Ingelheim Pharma | Heteroarylcarbonsäureamide, ihre Herstellung und ihre Verwendung als Arzneimittel |
| JPWO2003030937A1 (ja) | 2001-10-05 | 2005-01-20 | 小野薬品工業株式会社 | ミトコンドリアルベンゾジアゼピン受容体アンタゴニストからなるストレス疾患の治療剤 |
| EP2258687B1 (en) | 2002-02-12 | 2012-12-26 | Glaxosmithkline LLC | Nicotinamide derivates useful as P38 inhibitors |
| DE10261131A1 (de) * | 2002-12-20 | 2004-07-01 | Grünenthal GmbH | Substituierte 5-Aminomethyl-1H-pyrrol-2-carbonsäureamide |
| GB0302671D0 (en) * | 2003-02-06 | 2003-03-12 | Astrazeneca Ab | Pharmaceutical formulations |
| EP1638944A1 (en) * | 2003-06-12 | 2006-03-29 | Eli Lilly And Company | Tachykinin receptor antagonists |
| SI2384753T1 (sl) * | 2003-08-29 | 2016-06-30 | The Brigham And Women's Hospital, Inc. | Hidantoinski derivati kot inhibitorji celične nekroze |
| EP1730134A1 (en) * | 2004-03-26 | 2006-12-13 | Vertex Pharmaceuticals Incorporated | Pyridine inhibitors of erk2 and uses thereof |
| SG155188A1 (en) * | 2004-07-30 | 2009-09-30 | Exelixis Inc | Pyrrole derivatives as pharmaceutical agents |
| PL1848435T3 (pl) * | 2005-01-25 | 2016-08-31 | Synta Pharmaceuticals Corp | Związki przeciwko zapaleniom i zastosowania związane z odpornością |
| CN101128445B (zh) * | 2005-02-24 | 2012-01-18 | 日本农药株式会社 | 4-环丙基-1,2,3-噻二唑化合物，用于农业和园艺用途的植物病害控制剂和其使用方法 |
| EP1968583A4 (en) | 2005-12-20 | 2010-09-15 | Harvard College | COMPOUNDS, SCREENING AND TREATMENT PROCEDURES |
| JP2007186435A (ja) * | 2006-01-12 | 2007-07-26 | Astellas Pharma Inc | ニコチンアミド誘導体 |
| CA2639910A1 (en) | 2006-01-25 | 2007-08-02 | Synta Pharmaceuticals Corp. | Thiazole and thiadiazole compounds for inflammation and immune-related uses |
| US20070254926A1 (en) * | 2006-01-31 | 2007-11-01 | Jun Jiang | Pyridylphenyl compounds for inflammation and immune-related uses |
| US8119643B2 (en) * | 2006-03-20 | 2012-02-21 | Synta Pharmaceuticals Corp. | Benzoimidazolyl-pyrazine compounds for inflammation and immune-related uses |
| US8163777B2 (en) * | 2006-03-23 | 2012-04-24 | Synta Pharmaceuticals Corp. | Benzimidazolyl-pyridine compounds for inflammation and immune-related uses |
| US20100087453A1 (en) | 2006-10-10 | 2010-04-08 | President And Fellows Of Harvard College | Compounds, screens, and methods of treatment |
| JP5361857B2 (ja) | 2007-03-23 | 2013-12-04 | ファイザー・リミテッド | イオンチャネルの阻害剤 |
| WO2010075290A1 (en) | 2008-12-22 | 2010-07-01 | President And Fellows Of Harvard College | Unsaturated heterocyclic inhibitors of necroptosis |
| CA2772760A1 (en) | 2008-12-23 | 2010-07-01 | President And Fellows Of Harvard College | Small molecule inhibitors of necroptosis |
-
2008
- 2008-08-15 US US12/228,750 patent/US20090099242A1/en not_active Abandoned
- 2008-08-15 CA CA2696349A patent/CA2696349A1/en not_active Abandoned
- 2008-08-15 JP JP2010521050A patent/JP5645663B2/ja active Active
- 2008-08-15 EP EP20080795375 patent/EP2192838A4/en not_active Withdrawn
- 2008-08-15 EP EP15002668.0A patent/EP3034494A1/en not_active Withdrawn
- 2008-08-15 WO PCT/US2008/009793 patent/WO2009023272A1/en not_active Ceased
-
2010
- 2010-08-20 US US12/859,997 patent/US8278344B2/en active Active
-
2012
- 2012-08-20 US US13/589,867 patent/US8658689B2/en active Active
-
2014
- 2014-01-10 US US14/152,703 patent/US9108955B2/en active Active
-
2015
- 2015-07-10 US US14/796,378 patent/US20160102053A1/en not_active Abandoned
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