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 (enExample) | 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 (enExample) |
| EP (2) | EP2192838A4 (enExample) |
| JP (1) | JP5645663B2 (enExample) |
| CA (1) | CA2696349A1 (enExample) |
| WO (1) | WO2009023272A1 (enExample) |
Families Citing this family (30)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2384753B1 (en) * | 2003-08-29 | 2016-01-06 | The Brigham and Women's Hospital, Inc. | Hydantoin derivatives as inhibitors of cellular necrosis |
| EP1968583A4 (en) * | 2005-12-20 | 2010-09-15 | Harvard College | COMPOUNDS, SCREENING AND TREATMENT PROCEDURES |
| 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 |
| WO2011133964A2 (en) | 2010-04-23 | 2011-10-27 | Massachusetts Eye And Ear Infirmary | Methods and compositions for preserving photoreceptor and retinal pigment epithelial cells |
| EP2580201B1 (en) | 2010-06-11 | 2017-08-02 | Rhodes Technologies | Transition metal-catalyzed processes for the preparation of n-allyl compounds and use thereof |
| CA2802294C (en) | 2010-06-11 | 2016-05-10 | Rhodes Technologies | Process for n-dealkylation of tertiary amines |
| WO2012061045A2 (en) | 2010-11-01 | 2012-05-10 | Massachusetts Eye And Ear Infirmary | Methods and compositions for preserving retinal ganglion cells |
| US9643977B2 (en) | 2011-03-11 | 2017-05-09 | 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 |
| TWI637951B (zh) | 2013-02-15 | 2018-10-11 | 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 |
| US20160024098A1 (en) | 2013-03-15 | 2016-01-28 | President And Fellows Of Harvard College | Hybrid necroptosis 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 |
| SG11201704764PA (en) | 2014-12-11 | 2017-07-28 | Harvard College | Inhibitors of cellular necrosis and related methods |
| EP3224245B1 (en) | 2014-12-24 | 2018-09-12 | National Institute Of Biological Sciences, Beijing | Necrosis inhibitors |
| WO2016101885A1 (en) | 2014-12-24 | 2016-06-30 | National Institute Of Biological Sciences, Beijing | Necrosis inhibitors |
| IL247368A0 (en) | 2016-08-18 | 2016-11-30 | Yeda Res & Dev | Diagnostic and therapeutic uses of exosomes |
| MD3788045T2 (ro) | 2018-05-03 | 2023-09-30 | Rigel Pharmaceuticals Inc | Compuși inhibitori ai RIP1 și procedee de obţinere și utilizare a acestora |
| HRP20231381T1 (hr) | 2018-05-03 | 2024-03-01 | Rigel Pharmaceuticals, Inc. | Spojevi inhibitori rip1 i postupci za njihovo dobivanje i upotrebu |
| 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 |
| CA3149926A1 (en) | 2019-09-06 | 2021-03-11 | Yan Chen | Rip1 inhibitory compounds and methods for making and using the same |
| JP7493586B2 (ja) | 2019-09-06 | 2024-05-31 | ライジェル ファーマシューティカルズ， インコーポレイテッド | Ｒｉｐ１阻害化合物ならびにそれを作製および使用するための方法 |
| SI4055021T1 (sl) | 2019-11-07 | 2026-02-27 | Rigel Pharmaceuticals, Inc. | Heterociklične spojine, ki inhibirajo rip1 |
| AR121717A1 (es) | 2020-04-02 | 2022-06-29 | Rigel Pharmaceuticals Inc | Inhibidores de rip1k |
| 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 |
| TWI840311B (zh) | 2020-07-01 | 2024-04-21 | 美商雷傑製藥公司 | Rip1k抑制劑 |
| CA3198930A1 (en) * | 2020-11-19 | 2022-05-27 | Acousia Therapeutics Gmbh | Non-aqueous gel composition |
| AR125587A1 (es) | 2021-03-11 | 2023-08-02 | Rigel Pharmaceuticals Inc | Inhibidores heterocíclicos de la quinasa de rip1 |
| IL308348A (en) | 2021-05-20 | 2024-01-01 | Sironax Ltd | RIP1 modulators including cyclic ureas aztidine, their preparation and uses |
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 |
| EP0930305B1 (en) | 1996-09-30 | 2003-05-14 | 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 |
| DE69903992T2 (de) * | 1998-04-15 | 2003-08-21 | Pfizer Products Inc., Groton | Heterocyclische Carboxamide |
| ATE238661T1 (de) * | 1998-07-30 | 2003-05-15 | Nihon Nohyaku Co Ltd | Fungizide zusammensetzung enthaltend ein 1,2,3- thiadiazolderivat sowie deren verwendung |
| 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 |
| 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 |
| EP1386913B1 (en) * | 2001-04-19 | 2008-07-16 | Dainippon Sumitomo Pharma Co., Ltd. | Pyrrole derivative |
| DE10132686A1 (de) * | 2001-07-05 | 2003-01-16 | Boehringer Ingelheim Pharma | Heteroarylcarbonsäureamide, ihre Herstellung und ihre Verwendung als Arzneimittel |
| WO2003030937A1 (en) * | 2001-10-05 | 2003-04-17 | Ono Pharmaceutical Co., Ltd. | Remedies for stress diseases comprising mitochondrial benzodiazepine receptor antagonists |
| ATE375980T1 (de) | 2002-02-12 | 2007-11-15 | Smithkline Beecham Corp | Nicotinamide und deren verwendung als p38 inhibitoren |
| 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 |
| WO2005000821A1 (en) * | 2003-06-12 | 2005-01-06 | Eli Lilly And Company | Tachykinin receptor antagonists |
| EP2384753B1 (en) | 2003-08-29 | 2016-01-06 | The Brigham and Women's Hospital, Inc. | Hydantoin derivatives as inhibitors of cellular necrosis |
| US7462612B2 (en) * | 2004-03-26 | 2008-12-09 | Vertex Pharmaceuticals Incorporated | Pyridine inhibitors of ERK2 and uses thereof |
| CA2573426C (en) * | 2004-07-30 | 2015-11-17 | 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 |
| ZA200707353B (en) * | 2005-02-24 | 2009-03-25 | Nihon Nohyaku Co Ltd | 4-cyclopropyl-1,2,3-thiadiazole compound, agrohorticultural plant disease controlling agent and method of using the same |
| 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 |
| US8455658B2 (en) | 2006-01-25 | 2013-06-04 | 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 |
| AU2007227210A1 (en) * | 2006-03-20 | 2007-09-27 | Synta Pharmaceuticals Corp. | Benzoimidazolyl-parazine compounds for inflammation and immune-related uses |
| AU2007230911A1 (en) * | 2006-03-23 | 2007-10-04 | 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 |
| EP1995241B1 (en) * | 2007-03-23 | 2010-03-17 | ICAgen, Inc. | Inhibitors of ion channels |
| 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 |
-
2008
- 2008-08-15 EP EP20080795375 patent/EP2192838A4/en not_active Withdrawn
- 2008-08-15 WO PCT/US2008/009793 patent/WO2009023272A1/en not_active Ceased
- 2008-08-15 CA CA2696349A patent/CA2696349A1/en not_active Abandoned
- 2008-08-15 US US12/228,750 patent/US20090099242A1/en not_active Abandoned
- 2008-08-15 EP EP15002668.0A patent/EP3034494A1/en not_active Withdrawn
- 2008-08-15 JP JP2010521050A patent/JP5645663B2/ja active Active
-
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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