Evaluation of WO2013125543, WO2013146963 and EP2634185: the first Tyk2 inhibitors from Takeda and Sareum [0.03%]
Takeda和Sareum的首个Tyk2抑制剂WO2013125543,WO2013146963和EP2634185的评估报告摘要
Peter Norman
Peter Norman
Three patent applications, from two different companies, claim structurally novel Tyk2 inhibitors and their uses for the treatment of autoimmune diseases. In EP-2634185 Sareum claims 5-anilino-2-(2-halophenyl)-oxazole-4-carboxamide derivati...
Michael Risch
Michael Risch
The patent troll debate has reached a fevered pitch in the USA. This editorial seeks to frame the debate by pointing out the lack of clarity in defining patent trolls and their allegedly harmful actions. It then frames the debate by asking ...
Yi-Min Liu,Hsiao-Ling Chen,Hsueh-Yun Lee et al.
Yi-Min Liu et al.
Introduction: Microtubules play an important role in several cellular processes, particularly in the formation of the mitotic spindle during the process of mitosis. These highly dynamic mitotic-spindle microtubules have b...
Liming Shao,Wei Li,Qiong Xie et al.
Liming Shao et al.
Introduction: The dysfunctions of three very important monoamine neurotransmitters, serotonin (5-HT), norepinephrine (NE) and dopamine (DA), are associated with some of important CNS diseases such as depression; developin...
Yangbo Feng,Philip V LoGrasso
Yangbo Feng
Introduction: The Rho kinase/ROCK is critical in vital signal transduction pathways central to many essential cellular activities. Since ROCK possess multiple substrates, modulation of ROCK activity is useful for treatmen...
Evaluation of WO2013136076: two crystalline forms of the phosphatidylinositol 3-kinase-δ inhibitor RV-1729 [0.03%]
WO2013136076评价:PI3K-d抑制剂RV-1729的两种晶体形式的评估
Peter Norman
Peter Norman
This application claims two crystalline forms and inhaled formulations of a the selective phosphatidylinositol 3-kinase-δ inhibitor (PI3Kδ) inhibitor 6-(2-((4-amino-3-(3-hydroxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)methyl)-3-(2-chlorob...
Kongkai Zhu,Xiangqian Kong,Dan Zhao et al.
Kongkai Zhu et al.
Introduction: The receptor tyrosine kinase c-MET displays aberrant activation in the malignant phenotype of various tumors, and thus, has drawn considerable attention as drug target for cancer therapy. Many c-MET inhibito...
Evaluation of WO-2013040863, WO-2013041042 and WO-2013043962. Selective JAK1 inhibitors based on a 3-aminopyrazole-4-carboxamide scaffold [0.03%]
WO2013040863、WO2013041042及WO2013043962的评价:一类基于3-氨基吡唑-4-甲酰胺的Janus激酶1(JAK1)选择性抑制剂
Peter Norman
Peter Norman
1-alkyl-3-arylaminopyrazole-4-carboxamide derivatives have previously been described as JAK2 selective inhibitors. Modification of the 1-substituent to incorporate a 2-cyanoethyl moiety modulates the selectivity for JAK kinases providing JA...
Jean-Marc Garnier,Phillip P Sharp,Christopher J Burns
Jean-Marc Garnier
Introduction: The bromodomain (BRD) and extra-C terminal domain (BET) protein family consists of four members (BRD2, BRD3, BRD4 and BRDT). These "epigenetic readers" bind to acetyllysine (KAc) residues on the tails of his...
An overview of patented small molecule stearoyl coenzyme-A desaturase inhibitors (2009 - 2013) [0.03%]
专利小分子硬脂酰辅酶A脱氢酶抑制剂概览(2009-2013)
David A Powell
David A Powell
Introduction: Stearoyl coenzyme-A desaturase (SCD) is a critical lipogenic enzyme that converts a range of unsaturated lipids to their corresponding monounsaturated fatty acids. Genetic and enzyme-knockdown experiments ha...