15861-30-0Relevant articles and documents
Cyclin-dependent kinase inhibitors and application thereof
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Paragraph 0369; 0371; 0372; 0373, (2018/07/30)
The invention relates to compounds used as cyclin-dependent kinase inhibitors and application thereof, belonging to the field of medical chemistry. Specifically, the invention provides the compound asshown in a formula I which is described in the specification, or isomers, pharmaceutically acceptable salts, solvates, crystals or prodrugs thereof, preparation methods thereof, pharmaceutical compositions containing the compounds, and application of the compounds or the compositions to treatment of cancer, tissue hyperplasia diseases or inflammatory diseases. The compounds of the invention havegood inhibitory activity to CDK7 and are highly expected to be developed into a therapeutic agent for cancer, tissue hyperplasia diseases and inflammatory diseases.
Discovery of N-[(3R)-1-azabicyclo[2.2.2]oct-3-yl]furo[2,3-c]pyridine-5- carboxamide, an agonist of the α7 nicotinic acetylcholine receptor, for the potential treatment of cognitive deficits in schizophrenia: Synthesis and structure-activity relationship
Wishka, Donn G.,Walker, Daniel P.,Yates, Karen M.,Reitz, Steven C.,Jia, Shaojuan,Myers, Jason K.,Olson, Kirk L.,Jacobsen, E. Jon,Wolfe, Mark L.,Groppi, Vincent E.,Hanchar, Alexander J.,Thornburgh, Bruce A.,Cortes-Burgos, Luz A.,Wong, Erik H. F.,Staton, Brian A.,Raub, Thomas J.,Higdon, Nicole R.,Wall, Theron M.,Hurst, Raymond S.,Walters, Rodney R.,Hoffmann, William E.,Hajos, Mihaly,Franklin, Stanley,Carey, Galen,Gold, Lisa H.,Cook, Karen K.,Sands, Steven B.,Zhao, Sabrina X.,Soglia, John R.,Kalgutkar, Amit S.,Arneric, Stephen P.,Rogers, Bruce N.
, p. 4425 - 4436 (2007/10/03)
N-[(3R)-1-Azabicyclo[2.2.2]oct-3-yl]furo[2,3-c]pyridine-5-carboxamide (14, PHA-543,613), a novel agonist of the α7 neuronal nicotinic acetylcholine receptor (α7 nAChR), has been identified as a potential treatment of cognitive deficits in schizophrenia. Compound 14 is a potent and selective a7 nAChR agonist with an excellent in vitro profile. The compound is characterized by rapid brain penetration and high oral bioavailability in rat and demonstrates in vivo efficacy in auditory sensory gating and, in an in vivo model to assess cognitive performance, novel object recognition.
A new photolabile linker for the photoactivation of carboxyl groups
Nicolaou,Safina,Winssinger
, p. 900 - 903 (2007/10/03)
A new photolabile linker enabling nucleophilic cleavage of a carboxyl functionality upon irradiation with UV light (>290 nm) was developed. When the photocleavage is carried out in the presence of primary or secondary amines, amides are obtained in high yields and purifies, while the intramolecular version of this reaction leads to heterocycles via a cyclorelease mechanism.