494772-07-5Relevant articles and documents
Discovery of a Series of 7-Azaindoles as Potent and Highly Selective CDK9 Inhibitors for Transient Target Engagement
Barlaam, Bernard,De Savi, Chris,Dishington, Allan,Drew, Lisa,Ferguson, Andrew D.,Ferguson, Douglas,Gu, Chungang,Hande, Sudhir,Hassall, Lorraine,Hawkins, Janet,Hird, Alexander W.,Holmes, Jane,Lamb, Michelle L.,Lister, Andrew S.,McGuire, Thomas M.,Moore, Jane E.,O'Connell, Nichole,Patel, Anil,Pike, Kurt G.,Sarkar, Ujjal,Shao, Wenlin,Stead, Darren,Varnes, Jeffrey G.,Vasbinder, Melissa M.,Wang, Lei,Wu, Liangwei,Xue, Lin,Yang, Bin,Yao, Tieguang
supporting information, p. 15189 - 15213 (2021/11/01)
Optimization of a series of azabenzimidazoles identified from screening hit 2 and the information gained from a co-crystal structure of the azabenzimidazole-based lead 6 bound to CDK9 led to the discovery of azaindoles as highly potent and selective CDK9 inhibitors. With the goal of discovering a highly selective and potent CDK9 inhibitor administrated intravenously that would enable transient target engagement of CDK9 for the treatment of hematological malignancies, further optimization focusing on physicochemical and pharmacokinetic properties led to azaindoles 38 and 39. These compounds are highly potent and selective CDK9 inhibitors having short half-lives in rodents, suitable physical properties for intravenous administration, and the potential to achieve profound but transient inhibition of CDK9 in vivo.
NOVEL PHENYL PROPIONIC ACID DERIVATIVES AND USES THEREOF
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Paragraph 211-212; 213-215, (2018/07/05)
The present invention relates to the compounds according to Formula (I), the racemates, enantiomers, diastereomers thereof or pharmaceutical acceptable salts thereof, or pharmaceutical compositions comprising these, for the treatment or prevention of meta
New Positive allosteric modulators of nicotinic acetylcholine receptor
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Paragraph 0184, (2013/03/26)
The present invention relates to compounds useful in therapy, to compositions comprising said compounds, and to methods of treating diseases comprising administration of said compounds. The compounds referred to are positive allosteric modulators (PAMs) of the nicotinic acetylcholine α7 receptor.