247085-22-9Relevant academic research and scientific papers
Exploiting the 4-Phenylquinazoline Scaffold for the Development of High Affinity Fluorescent Probes for the Translocator Protein (TSPO)
Milite, Ciro,Barresi, Elisabetta,Da Pozzo, Eleonora,Costa, Barbara,Viviano, Monica,Porta, Amalia,Messere, Anna,Sbardella, Gianluca,Da Settimo, Federico,Novellino, Ettore,Cosconati, Sandro,Castellano, Sabrina,Taliani, Sabrina,Martini, Claudia
, p. 7897 - 7909 (2017/10/06)
The quinazoline class was exploited to search for a new translocator protein (TSPO) fluorescent probe endowed with improved affinity and residence time (RT). Computational studies on an "in-house" collection of quinazoline derivatives, featuring highly st
Design, synthesis, and evaluation of indolinones as inhibitors of the transforming growth factor β receptor i (TGFβRI)
Roth, Gerald J.,Heckel, Armin,Brandl, Trixi,Grauert, Matthias,Hoerer, Stefan,Kley, Joerg T.,Schnapp, Gisela,Baum, Patrick,Mennerich, Detlev,Schnapp, Andreas,Park, John E.
supporting information; experimental part, p. 7287 - 7295 (2011/02/23)
Inhibition of transforming growth factor β (TGFβ) type I receptor (Alk5) offers a novel approach for the treatment of fibrotic diseases and cancer. Indolinones substituted in position 6 were identified as a new chemotype inhibiting TGFβRI concomitant with
8-HETEROARYLPURINE MNK2 INHIBITORS FOR TREATING METABOLIC DISORDERS
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Page/Page column 50, (2010/11/28)
This invention relates to 8-Heteroarylpurine Mnk2 Inhibitors which are useful for the treatment and prevention of metabolic disorders such as obesity and diabetes.
Substituted indolines which inhibit receptor tyrosine kinases
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Page column 47, (2008/06/13)
Indolinones of the formula having an inhibitory effect on receptor tyrosine kinases and cyclin/CDK complexes, as well as on the proliferation of endothelial cells and various tumor cells. Exemplary are: (a) 3-Z-[1-(4-(piperidin-1-yl-methyl)-anilino)-1-phenyl-methylene]-6-ethoxycarbonyl-2-indolinone, (b) 3-Z-[(1-(4-(piperidin-1-yl-methyl)-anilino)-1-phenyl-methylene]-6-carbamoyl-2-indolinone, and (c) 3-Z-[1-(4-(piperidin-1-yl-methyl)-anilino)-1-phenyl-methylene]-6-metboxycarbonyl-2-indolinone.
Substituted indolinones, preparation thereof and their use as pharmaceutical compositions
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, (2008/06/13)
Indolinones of general formula I which are inhibitors of cell proliferation, particularly of tumour cells, and inhibitors of protein kinases. The following compounds are exemplary: (Z)-3-{1-[4-(N-(2-aminoethyl)-N-methylsulphonyl-amino)-phenylamino]-1-phenyl-methylidene}-5-phenylsulphonylamino-2-indolinone, (Z)-3-{1 -[4-(N-(2-dimethylaminoethyl)-N-phenylsulphonyl-amino)-phenylamino]-1-phenyl-methylidene}-5-phenylsulphonylamino-2-indolinone, and (Z)-3-{1-[4-(4-methylpiperazinomethyl)-phenylamino]-1-phenyl-methylidene}-5-phenylsulphonylamino-2-indolinone.
Indolinones having kinase inhibitory activity
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, (2008/06/13)
The present invention relates to substituted indolinones of general formula [Figure] wherein R1 to R5, and X are defined as in claim 1, the isomers thereof and the salts thereof, particularly the physiologically acceptable salts thereof which have valuable pharmacological properties, particularly an inhibitory effect on various kinases and cycline/CDK complexes and on the proliferation of various tumour cells, pharmaceutical compositions containing these (compounds, their use and processes for preparing them.
