85302-07-4Relevant academic research and scientific papers
NEW THERAPEUTIC AGENTS FOR THE TREATMENT OF HAEMATOLOGICAL PATHOLOGIES
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Page/Page column 26-27, (2021/03/05)
The present invention relates to compounds having a tetracyclic system and the use thereof as new therapeutic agents in the treatment of acute myeloid leukemia (AML), preferably in FLT3/ITD hemizygote patients resistant to conventional therapies. The invention also relates to 5,7-dihydro-4H-[1,3]thiazolo[4,5-e]isoindol-2-amine compounds useful as intermediates for the synthesis of tetracyclic imidazo[2',1':2,3][1,3]thiazolo[4,5-e]isoindole compounds.
Design, synthesis and biological evaluation of selective histone deacetylase 6 (HDAC6) inhibitors bearing benzoindazole or pyrazoloindazole scaffold as surface recognition motif
Xu, Qihao,Mou, Yanhua,Wang, Siyuan,Gao, Xiaoxiao,Zhang, Yulong,Wang, Zhi,Xu, Xiangwei,Han, Yu,Jia, Wenlong,Zhang, Meihui,Zhao, Linxiang,Liu, Dan
, (2021/04/27)
A series of compounds were designed and synthesized based on the compound 11i bearing phenylpyrazole scaffold with histone deacetylase 6 (HDAC6) inhibitory activity. Most of the compounds showed considerable inhibitory activity against HDAC6 and compound
Inhibition studies on carbonic anhydrase isoforms I, II, IV and IX with N-arylsubstituted secondary sulfonamides featuring a bicyclic tetrahydroindazole scaffold
Salerno, Silvia,Amendola, Giorgio,Angeli, Andrea,Baglini, Emma,Barresi, Elisabetta,Marini, Anna Maria,Ravichandran, Rahul,Viviano, Monica,Castellano, Sabrina,Novellino, Ettore,Da Settimo, Federico,Supuran, Claudiu T.,Cosconati, Sandro,Taliani, Sabrina
, (2021/06/07)
Carbonic Anhydrases (CAs) are pharmaceutically relevant targets for the treatment of several disease conditions. The ubiquitous localization of these enzymes and the high homology shared by the different isoforms represent substantial impediments for the
Tetrahydroquinazole-based secondary sulphonamides as carbonic anhydrase inhibitors: synthesis, biological evaluation against isoforms I, II, IV, and IX, and computational studies
Baglini, Emma,Barresi, Elisabetta,Berrino, Emanuela,Castellano, Sabrina,Cosconati, Sandro,Da Settimo, Federico,Marini, Anna Maria,Ravichandran, Rahul,Salerno, Silvia,Supuran, Claudiu T.,Taliani, Sabrina,Viviano, Monica
, p. 1874 - 1883 (2021/08/10)
A library of variously decorated N-phenyl secondary sulphonamides featuring the bicyclic tetrahydroquinazole scaffold was synthesised and biologically evaluated for their inhibitory activity against human carbonic anhydrase (hCA) I, II, IV, and IX. Of not
GPR52 MODULATOR COMPOUNDS
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Page/Page column 45; 48; 58-59, (2021/05/15)
The disclosures herein relate to novel compounds of Formula (1): (1) and salts thereof, wherein R1, Q, X, Y and Z are defined herein, and their use in treating, preventing, ameliorating, controlling or reducing the risk of disorders associated with GPR52 receptors.
Discovery and Optimization of 2 H-1λ2-Pyridin-2-one Inhibitors of Mutant Isocitrate Dehydrogenase 1 for the Treatment of Cancer
Rohde, Jason M.,Karavadhi, Surendra,Pragani, Rajan,Liu, Li,Fang, Yuhong,Zhang, Weihe,McIver, Andrew,Zheng, Hongchao,Liu, Qingyang,Davis, Mindy I.,Urban, Daniel J.,Lee, Tobie D.,Cheff, Dorian M.,Hollingshead, Melinda,Henderson, Mark J.,Martinez, Natalia J.,Brimacombe, Kyle R.,Yasgar, Adam,Zhao, Wei,Klumpp-Thomas, Carleen,Michael, Sam,Covey, Joseph,Moore, William J.,Stott, Gordon M.,Li, Zhuyin,Simeonov, Anton,Jadhav, Ajit,Frye, Stephen,Hall, Matthew D.,Shen, Min,Wang, Xiaodong,Patnaik, Samarjit,Boxer, Matthew B.
, p. 4913 - 4946 (2021/05/07)
Neomorphic mutations in isocitrate dehydrogenase 1 (IDH1) are oncogenic for a number of malignancies, primarily low-grade gliomas and acute myeloid leukemia. We report a medicinal chemistry campaign around a 7,7-dimethyl-7,8-dihydro-2H-1λ2-quinoline-2,5(6H)-dione screening hit against the R132H and R132C mutant forms of isocitrate dehydrogenase (IDH1). Systematic SAR efforts produced a series of potent pyrid-2-one mIDH1 inhibitors, including the atropisomer (+)-119 (NCATS-SM5637, NSC 791985). In an engineered mIDH1-U87-xenograft mouse model, after a single oral dose of 30 mg/kg, 16 h post dose, between 16 and 48 h, (+)-119 showed higher tumoral concentrations that corresponded to lower 2-HG concentrations, when compared with the approved drug AG-120 (ivosidenib).
INHIBITORS OF GLUCOSE-6-PHOSPHATE DEHYDROGENASE AND USES THEREOF
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Paragraph 00293, (2021/07/24)
Provided herein are compounds having the following structural formula, wherein values for the variables are as described herein. Also provided are pharmaceutical compositions of the compounds, as well as methods of using the compounds to inhibit the oxida
1,5,6,7-Tetrahydro-4H-indazol-4-ones as human neutrophil elastase (HNE) inhibitors
Bartolucci, Gianluca,Cantini, Niccolo,Crocetti, Letizia,Giovannoni, Maria Paola,Guerrini, Gabriella,Pallecchi, Marco,Quinn, Mark T.,Schepetkin, Igor A.,Teodori, Elisabetta,Vergelli, Claudia
, (2021/10/04)
Human neutrophil elastase (HNE) is a serine protease that is expressed in polymorphonuclear neutrophils. It has been recognized as an important therapeutic target for treating inflammatory diseases, especially related to the respiratory system, but also f
Tetrahydroquinazoline derivatives and pharmaceutical composition for preventing or treating psoriasis comprising the same
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Paragraph 0238-0241, (2020/11/06)
The present invention relates to a tetrahydroquinazoline derivative and a pharmaceutical composition for preventing or treating psoriasis containing the same as an active ingredient. The compound provided in one aspect of the present invention has an effe
Mercaptan compound having HDAC6 (histone deacetylase 6) inhibitory activity and application thereof
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Paragraph 0148; 0149; 0150; 0151, (2019/03/10)
The invention belongs to the technical field of medicines and relates to a mercaptan compound having an anti-tumor activity, in particular to a mercaptan compound containing a 6(7)-substituted-N-(6-decylhexyl)-pyrazolo[3,4-e] indazole-3-formamide fragment
