254751-09-2Relevant academic research and scientific papers
CASPASE INHIBITOR AND PHARMACEUTICAL COMPOSITION, USE AND THERAPEUTIC METHOD THEREOF
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Paragraph 0073; 0079, (2019/04/05)
Disclosed are a class of compounds as a caspase inhibitor, and in particular the compound as shown in formula (I) or a pharmaceutically acceptable salt thereof, and the use of the compound in treating caspase-related diseases.
Caspase inhibitor and pharmaceutical composition, application and treatment method thereof
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Paragraph 0037-0038; 0041-0042, (2019/05/28)
The invention provides a compound serving as a caspase inhibitor and particularly relates to a novel compound with caspase inhibition activity or a pharmaceutically acceptable salt of the novel compound, a preparation method of the novel compound and a ph
LINKED CYCLIC COMPOUND AS CASPASE INHIBITOR
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Paragraph 0057; 0059, (2019/12/05)
A compound represented by formula (I), a pharmaceutically acceptable salt or tautomer thereof, and an application of the compound as a caspase inhibitor.
Structure-activity relationship study of a series of caspase inhibitors containing γ-amino acid moiety for treatment of cholestatic liver disease
Mou, Jianfeng,Wu, Songliang,Luo, Zhi,Guo, Fengying,He, Haiying,Wang, Jianhua,Lin, Fusen,Guo, Fengxun,Sun, Jianping,Shen, Liang,Zeng, Minggao,Wang, Chuan,Xu, Deming,Gu, Zhengxian,Tian, Xin,Zhang, Aiming,Xu, Hongjiang,Yang, Ling,Zhang, Xiquan,Li, Jian,Chen, Shuhui
supporting information, p. 1874 - 1878 (2018/04/12)
A series of caspase inhibitors containing γ-amino acid moiety have been synthesized. A systemic study on their structure-activity relationship of anti-apoptotic cellular activity is presented. These efforts led to the discovery of compound 20o as a potent caspase inhibitor, which demonstrated preclinical ameliorating total bilirubin efficacy with a significantly improved pharmacokinetic profile.
Synthesis and evaluation of indole aspartyl ketones as novel caspase-3 inhibitors
Sengupta,Rao, G.Venkateshwar,Dubey
, p. 5517 - 5520 (2012/07/27)
Synthesis, biological evaluation and structure-activity relationships for a series of novel nonpeptide small molecule inhibitors of caspase-3 are described. Among the synthesized compounds, 2,3,5,6-tetrafluorophenoxymethyl ketone derivatives of indole-N-a
CASPASE INHIBITORS BASED ON PYRIDAZINONE SCAFFOLD
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Page/Page column 8, (2010/03/04)
The present invention relates to a pyridazinone derivative which can be used as a caspase inhibitor, process for the preparation thereof, and pharmaceutical composition for inhibiting caspase comprising the same.
CASPASE INHIBITORS BASED ON PYRIDAZINONE SCAFFOLD
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Page/Page column 16-17, (2008/12/05)
The present invention relates to a pyridazinone derivative which can be used as a caspase inhibitor, process for the preparation thereof, and pharmaceutical composition for inhibiting caspase comprising the same.
CASPASE INHIBITORS CONTAINING DICARBONYLAMINO-ISOXAZOLINE
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Page/Page column 23, (2010/10/20)
The present invention relates to a dicarbonylamino-isoxazoline derivative as an inhibitor against various caspases and a therapeutic composition for preventing inflammation and apoptosis comprising the same.
Oxamyl dipeptide caspase inhibitors developed for the treatment of stroke
Linton, Steven D.,Aja, Teresa,Allegrini, Peter R.,Deckwerth, Thomas L.,Diaz, Jose-Luis,Hengerer, Bastian,Herrmann, Julia,Jahangiri, Kathy G.,Kallen, Joerg,Karanewsky, Donald S.,Meduna, Steven P.,Nalley, Kip,Robinson, Edward D.,Roggo, Silvio,Rovelli, Giorgio,Sauter, Andre,Sayers, Robert O.,Schmitz, Albert,Smidt, Robert,Ternansky, Robert J.,Tomaselli, Kevin J.,Ullman, Brett R.,Wiessner, Christoph,Wu, Joe C.
, p. 2685 - 2691 (2007/10/03)
Structural modifications were made to a previously described acyl dipeptide caspase inhibitor, leading to the oxamyl dipeptide series. Subsequent SAR studies directed toward the warhead, P2, and P4 regions of this novel peptidomimetic are described herein.
4-OXO-3-(1-OXO-1H-ISOQUINOLIN-2-YLACETYLAMINO)-PENTANOIC ACID ESTER AND AMIDE DERIVATIVES AND THEIR USE AS CASPASE INHIBITORS
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Page 55, (2008/06/13)
The present invention provides a compound of formula (I):, wherein: X i s -OR1 or -N (R5) 2 , Y is halo, trifluorophenoxy, or tetrafluorophenoxy; R1 is: C1-6 straight chained or branched alkyl, alkeny
