230615-53-9Relevant academic research and scientific papers
PYRIMIDINE DERIVATIVES FOR THE TREATMENT OF ABNORMAL CELL GROWTH
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Page/Page column 81-82, (2010/11/27)
The present invention relates to a compound of the formula (I), or a pharmaceutically acceptable salt thereof, wherein Ar is a group of formula (III), and R1, R2, R13, A, K, M, L1, L2, X, Y1, Y2, Q, salt thereof, wherein R1, R2, R13, A, K, L1, L2, W, X, Z1, Z2, Y1, Y2, Z1, Z2, M, Q, W, X, m, p and q are as defined herein. Such novel pyrimidine derivatives are useful in the treatment of abnormal cell growth, such as cancer, in mammals. This invention also relates to a method of using such compounds in the treatment of abnormal cell growth in mammals, especially humans, and to pharmaceutical compositions containing such compounds.
VARENICLINE STANDARDS AND IMPURITY CONTROLS
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Page/Page column 10-11, (2008/06/13)
The subject invention provides a varenicline composition that comprises varenicline, or a pharmaceutically acceptable salt thereof, and an amount of a compound selected from one or more of several mononitro, monoamine mixed aminonitro, diamino or dinitro intermediates, and the concentration of said compound is greater than O ppm and not greater than about 500 ppm, not greater than about 100 ppm or not greater than about 10 ppm. Methods for synthesizing and using such varenicline compositions are also provided.
3,5-Bicyclic aryl piperidines: A novel class of α4β2 neuronal nicotinic receptor partial agonists for smoking cessation
Coe, Jotham W.,Brooks, Paige R.,Wirtz, Michael C.,Bashore, Crystal G.,Bianco, Krista E.,Vetelino, Michael G.,Arnold, Eric P.,Lebel, Lorraine A.,Fox, Carol B.,Tingley III, F. David,Schulz, David W.,Davis, Thomas I.,Sands, Steven B.,Mansbach, Robert S.,Rollema, Hans,O'Neill, Brian T.
, p. 4889 - 4897 (2008/12/23)
3,5-Bicyclic aryl piperidines are a new class of high-affinity α4β2 nicotinic receptor agents. We have sought nicotinic receptor partial agonists of the α4β2 nicotinic acetylcholine receptor for smoking cessation, and a number of compounds fulfill potency, selectivity, and efficacy requirements in vitro. In vivo, selected agents demonstrate potent partial agonist efficacy on the mesolimbic dopamine system, a key measure of therapeutic potential for smoking cessation.
Process for the preparation of 1,3-substituted indenes and aryl-fused azapolycyclic componunds
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, (2008/06/13)
The present invention relates to processes for the preparation of any of the intermediate 1,3-substituted indenes of the formulae (Ia), (Ib) and (Ic) or a mixture thereof: wherein R1, R2, R3, R4, and R5 are defined herein. Compounds of formulae (Ia), (Ib) and (IC) or mixtures thereof are useful in the preparation of compounds of formula (II): wherein R2, R3 and R6 are also defined herein.
