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Isolated compounds of formula I: and stereoisomers, enantiomers, diastereomers, and pharmaceutically acceptable salts thereof are described, as well as processes for production, and methods of use of these compounds and compositions thereof for the treatment of diseases associated with abnormal protein kinase activities and/or abnormal histone deacetylase activities including, for example, inflammatory diseases, autoimmune diseases, cancer, neurological and neurodegenerative diseases, cardiovascular diseases, metabolic disease, allergies and asthma and/or hormone-related diseases.


Yang Q.-J.,Shenzhen Chipscreen Biosciences Ltd. | Yu J.-D.,Shenzhen Chipscreen Biosciences Ltd. | Pan D.-S.,Shenzhen Chipscreen Biosciences Ltd. | Shan S.,Shenzhen Chipscreen Biosciences Ltd. | And 3 more authors.
Chinese Journal of New Drugs | Year: 2015

The Janus kinases (JAKs) are a family of intracellular non-receptor tyrosine kinases that play an essential role in the cytokine receptor signaling pathways by interacting with signal transducers and activators of transcription (STAT) proteins. The JAK/STAT pathways have been implicated in the pathogenesis of inflammatory diseases, such as rheumatoid arthritis. In recent years, JAK inhibitors, especially subtype selective inhibitors for the treatment of this indication have drawn significant attention from the pharmaceutical industry. This paper provides a review of novel therapeutic strategies for rheumatoid arthritis, JAK kinases and cytokine receptors, and the role of the JAK/STAT signaling pathway in rheumatoid arthritis. Meanwhile, the latest development of selective JAK inhibitors is also mainly described. ©, 2014, Chinese Journal of New Drugs Co. Ltd. All right reserved.


Pan D.-S.,Shenzhen Chipscreen Biosciences Ltd. | Yang Q.-J.,Shenzhen Chipscreen Biosciences Ltd. | Fu X.,Shenzhen Chipscreen Biosciences Ltd. | Shan S.,Shenzhen Chipscreen Biosciences Ltd. | And 5 more authors.
MedChemComm | Year: 2014

Tumorigenesis is maintained through a complex interplay of multiple cellular biological processes and is regulated to some extent by epigenetic control of gene expression. Targeting one signaling pathway or biological function in cancer treatment often results in compensatory modulation of others, such as off-target drivers of cell survival. As a result, overall survival of cancer patients is still far from satisfactory. Epigenetic-modulating agents can concurrently target multiple aberrant or compensatory signaling pathways found in cancer cells. However, existing epigenetic-modulating agents in cancer treatment have not yet fully translated into survival benefits beyond hematological tumors. In this article, we present a historical rationale for use of chidamide (CS055/Epidaza), an orally active and subtype-selective histone deacetylase (HDAC) inhibitor of the benzamide chemical class. This compound was discovered and successfully developed as mono-therapy for relapsed and refractory peripheral T cell lymphoma (PTCL) in China. We discuss the evidence supporting chidamide as a durable epigenetic modulator that allows cellular reprogramming with little cytotoxicity in cancer treatments. This journal is © The Royal Society of Chemistry 2014.


Patent
Shenzhen Chipscreen Biosciences Ltd. | Date: 2012-12-18

The present invention belongs to the field of pharmaceutical chemistry, and disclosed are two crystal forms of Childamide, that is, Chidamide crystal form A and Chidamide crystal form B, and the method for preparing the new crystal forms of Chidamide. The Chidamide crystal form A and Chidamide crystal form B of the present invention can be used for preparing drugs for treating diseases related to cell differentiation and proliferation.

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