- Inhibitors to Overcome Secondary Mutations in the Stem Cell Factor Receptor KIT
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In modern cancer therapy, the use of small organic molecules against receptor tyrosine kinases (RTKs) has been shown to be a valuable strategy. The association of cancer cells with dysregulated signaling pathways linked to RTKs represents a key element in
- Kaitsiotou, Helena,Keul, Marina,Hardick, Julia,Mühlenberg, Thomas,Ketzer, Julia,Ehrt, Christiane,Krüll, Jasmin,Medda, Federico,Koch, Oliver,Giordanetto, Fabrizio,Bauer, Sebastian,Rauh, Daniel
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- KINASE INHIBITORS AND USES THEREOF
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This invention described herein relates to compounds of general formula (I) : (I), in which variable groups are as defined herein, and to their preparation and use. Uses for the compounds and for compositions containing them include treatment of cancer and other diseases mediated by protein kinases, such as Bcr-Abl kinase, and mutants thereof, such as the T315I mutant.
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- Benzamide compounds containing acetenyl group
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The invention provides acetenyl group-containing benzamide compounds as shown in a formula (I) and used for treating or preventing diseases related to protein kinase, and medicinal salts or configurational isomers thereof. A connection group L, a ring A and substituents R, R, R, R and R in the formula (I) are as defined in the specification. The invention also discloses a preparation method and a pharmaceutical composition of the compounds as shown in the formula (I), and application of the compounds to preparation or prevention of drugs used for preventing diseases related to protein kinase.
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- 3-ACETYLENYL-PYRAZOLE-PYRIMIDINE DERIVATIVE, AND PREPARATION METHOD THEREFOR AND USES THEREOF
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The present invention relates to the field of chemical and medicine, more particularly, 3-ethynylpyrazolopyrimidine derivatives and their preparation methods and uses. The invention provides a 3-ethynylpyrazolopyrimidine derivative, and the structure is shown in formula I. The present invention also provides preparation methods and use of 3-ethynylpyrazolopyrimidine derivatives, comprising the compounds and derivatives, and their pharmaceutical compositions for the use of the treatment and prevention of tumors.
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Paragraph 0175; 0197
(2017/11/10)
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- PROTEIN KINASE INHIBITORS (VARIANTS), USE THEREOF IN TREATING ONCOLOGICAL DISEASES AND A PHARMACEUTICAL COMPOSITION BASED THEREON
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The present invention relates to the treatment of oncological, chronic inflammatory and similar diseases with the aid of new families of chemical compounds having improved efficiency with regard to the inhibition of Abl kinase and mutant forms thereof, as well as other therapeutically significant kinases. It describes protein kinase inhibitors in the form of compounds of general formula (I) and compounds of general formula (II), or a tautomer, an individual isomer, a mixture of isomers, a pharmaceutically acceptable salt, a solvate or a hydrate thereof.
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Page/Page column
(2014/07/07)
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- SUBSTITUTED PYRIMIDINYL AND PYRIDINYL-PYRROLOPYRIDINONES, PROCESS FOR THEIR PREPARATION AND THEIR USE AS KINASE INHIBITORS
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The present invention relates to substituted pyrimidinyl- and pyridinylpyrrolopyridinone compounds which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity, in particular RET family kinases. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions containing these compounds.
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Page/Page column 53; 60
(2014/05/24)
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