175075-24-8Relevant academic research and scientific papers
Hexahydro-cyclohepta-pyrrole oxindole as potent kinase inhibitors
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Page/Page column 21, (2010/02/08)
The present invention is directed to a class indolinone compounds, hexahydro-cyclohepta-pyrrole oxindoles, which are useful as protein kinase inhibitors.
5-sulfonamido-substituted indolinone compounds as protein kinase inhibitors
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Page/Page column 28, (2010/02/08)
The present invention relates to 5-sulfonamido substituted indolinones that modulate the activity of protein kinases (“PKs”). The compounds of this invention are therefore useful in treating disorders related to abnormal PK activity. Pharmaceutical compositions comprising these compounds, methods of treating diseases utilizing pharmaceutical compositions comprising these compounds and methods of preparing them are also disclosed.
Sulfonamide substituted indolinones as inhibitors of DNA dependent protein kinase (DNA-PK)
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Page 24, (2010/02/10)
The present invention relates generally to the field of radiosensitizing agents which are capable of enhancing radiotherapy by inhibiting DNA-PK (DNA-protein kinase). In particular, it relates to sulfonamide substituted indolinones which inhibit DNA-PK.
Design and synthesis of aminopropyl tetrahydroindole-based indolin-2-ones as selective and potent inhibitors of Src and Yes tyrosine kinase
Guan, Huiping,Laird, A. Douglas,Blake, Robert A.,Tang, Cho,Liang, Chris
, p. 187 - 190 (2007/10/03)
A novel series of substituted 3-[3-(aminopropyl)-4,5,6,7-tetrahydro-1H- indol-2-ylmethylene]-1,3-dihydro-indole-2-ones was discovered as potent inhibitors of the non-receptor tyrosine kinase Src and Yes. A structure-activity relationship was developed in order to optimize their potency and selectivity. Syntheses of these compounds are also described herein.
Prodrugs of a 3-(pyrrol-2-ylmethylidene)-2-indolinone derivatives
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, (2008/06/13)
The present invention relates to pyrrole substituted 2-indolinone compounds and their pharmaceutically acceptable salts which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related cellular disorders such as cancer.
Combination therapy for the treatment of cancer
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, (2008/06/13)
The present invention relates to methods for treatment or prevention of neoplasia disorders using protein tyrosine kinase inhibitors in combination with cyclooxygenase inhibitors, in particular cyclooxygenase-2 selective inhibitors.
Potent small molecule inhibitors of spleen tyrosine kinase (Syk)
Lai, Justine Y. Q.,Cox, Paul J.,Patel, Rajesh,Sadiq, Shazia,Aldous, David J.,Thurairatnam, Sukanthini,Smith, Keith,Wheeler, Darren,Jagpal, Savita,Parveen, Sofia,Fenton, Gary,Harrison, Trevor K. P.,McCarthy, Clive,Bamborough, Paul
, p. 3111 - 3114 (2007/10/03)
A series of oxindoles demonstrating inhibition of the phosphorylation of biotinylated substrates of Syk and IgE/FcεRI triggered basophil cell degranulation has been identified. A study of the SAR around sulfonamide 31 (IC50=5 nM, EC50=1400 nM) is discussed. The modest cellular activity representative of the sulfonamide series was overcome when the Polar Surface Area was lowered to 2, leading to the identification of amide 32 (IC50=145 nM, EC50=100 nM).
Methods of modulating protein tyrosine kinase function with substituted indolinone compounds
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, (2008/06/13)
The invention relates to certain indolinone compounds, their method of synthesis, and a combinatorial library consisting of the indolinone compounds. The invention also relates to methods of modulating the function of protein kinases using indolinone compounds and methods of treating diseases by modulating the function of protein kinases and related signal transduction pathways.
