135948-75-3Relevant academic research and scientific papers
BMS-933043, a Selective α7 nAChR Partial Agonist for the Treatment of Cognitive Deficits Associated with Schizophrenia
King, Dalton,Iwuagwu, Christiana,Cook, Jim,McDonald, Ivar M.,Mate, Robert,Zusi, F. Christopher,Hill, Matthew D.,Fang, Haiquan,Zhao, Rulin,Wang, Bei,Easton, Amy E.,Miller, Regina,Post-Munson, Debra,Knox, Ronald J.,Gallagher, Lizbeth,Westphal, Ryan,Molski, Thaddeus,Fan, Jingsong,Clarke, Wendy,Benitex, Yulia,Lentz, Kimberley A.,Denton, Rex,Morgan, Daniel,Zaczek, Robert,Lodge, Nicholas J.,Bristow, Linda J.,Macor, John E.,Olson, Richard E.
supporting information, p. 366 - 371 (2017/03/17)
The therapeutic treatment of negative symptoms and cognitive dysfunction associated with schizophrenia is a significant unmet medical need. Preclinical literature indicates that α7 neuronal nicotinic acetylcholine (nACh) receptor agonists may provide an effective approach to treating cognitive dysfunction in schizophrenia. We report herein the discovery and evaluation of 1c (BMS-933043), a novel and potent α7 nACh receptor partial agonist with high selectivity against other nicotinic acetylcholine receptor subtypes (>100-fold) and the 5-HT3A receptor (>300-fold). In vivo activity was demonstrated in a preclinical model of cognitive impairment, mouse novel object recognition. BMS-933043 has completed Phase I clinical trials.
Α 7 as intranuclear hydroxynicotinic acetylcholine receptor quinuclidines compd.
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Paragraph 0742; 0743, (2018/10/03)
PROBLEM TO BE SOLVED: To provide ligands for the nicotinic α-7 receptor used for the treatment of various disorders of the central nervous system, especially affective and neurodegenerative disorders.SOLUTION: The disclosure provides compounds of the specified formula I, including their salts, and compositions and methods using the compounds.
CSF-1R INHIBITORS, COMPOSITIONS, AND METHODS OF USE
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Page/Page column 85-86, (2009/01/20)
Benzoxazole and benzothiazole compounds and their oxides, esters, prodrugs, solvates, and pharmaceutically acceptable salts thereof are disclosed. Compositions of the compounds, either alone or in combination with at least one additional therapeutic agent, with a pharmaceutically acceptable carrier, and uses of the compounds, either alone or in combination with at least one additional therapeutic agent are also disclosed. The embodiments are useful for inhibiting cellular proliferation, inhibiting the growth and/or metathesis of tumors, treating or preventing cancer, treating or preventing degenerating bone diseases such as rheumatoid arthritis, and/or inhibiting molecules such as CSF 1R.
NOVEL SUBSTITUTED PYRIMIDINYLOXY UREAS USEFUL AS INHIBITORS OF PROTEIN KINASES
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Page/Page column 31, (2010/11/27)
The present invention relates to compounds and methods useful as inhibitors of protein kinases, including B-Raf and several receptor tyrosine and cytoplasmic tyrosine kinases. The present invention is directed to new substituted pyrimidinyloxy urea compounds of Formulas II, III and IV and compositions and their application as pharmaceuticals for the treatment of disease. Methods of modulating of protein kinase activity in a human or animal subject are also provided for the treatment diseases such as cancers.
