633283-64-4Relevant academic research and scientific papers
SUBSTITUTED PYRIDINE-PIPERAZINYL ANALOGUES AS RSV ANTIVIRAL COMPOUNDS
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Page/Page column 15, (2015/02/25)
The invention concerns novel substituted pyridine-piperazinyl analogues of formula (I) having antiviral activity, in particular, having an inhibitory activity on the replication of the respiratory syncytial virus (RSV). The invention further concerns the preparation of such novel compounds, compositions comprising these compounds, and the compounds for use in the treatment of respiratory syncytial virus infection.
Discovery of a novel series of potent and orally bioavailable phosphoinositide 3-kinase γ inhibitors
Leahy, James W.,Buhr, Chris A.,Johnson, Henry W. B.,Kim, Byung Gyu,Baik, Taegon,Cannoy, Jonah,Forsyth, Timothy P.,Jeong, Joon Won,Lee, Matthew S.,Ma, Sunghoon,Noson, Kevin,Wang, Longcheng,Williams, Matthew,Nuss, John M.,Brooks, Eric,Foster, Paul,Goon, Leanne,Heald, Nathan,Holst, Charles,Jaeger, Christopher,Lam, Scott,Lougheed, Julie,Nguyen, Lam,Plonowski, Arthur,Song, Joanne,Stout, Thomas,Wu, Xiang,Yakes, Michael F.,Yu, Peiwen,Zhang, Wentao,Lamb, Peter,Raeber, Olivia
experimental part, p. 5467 - 5482 (2012/09/25)
The phosphoinositide 3-kinases (PI3Ks) have been linked to an extraordinarily diversified group of cellular functions making these enzymes compelling targets for the treatment of disease. A large body of evidence has linked PI3Kγ to the modulation of autoimmune and inflammatory processes making it an intriguing target for drug discovery. Our high-throughput screening (HTS) campaign revealed two hits that were nominated for further optimization studies. The in vitro activity of the first HTS hit, designated as the sulfonylpiperazine scaffold, was optimized utilizing structure-based design. However, nonoptimal pharmacokinetic properties precluded this series from further studies. An overlay of the X-ray structures of the sulfonylpiperazine scaffold and the second HTS hit within their complexes with PI3Kγ revealed a high degree of overlap. This feature was utilized to design a series of hybrid analogues including advanced leads such as 31 with desirable potency, selectivity, and oral bioavailability.
5-HT7 RECEPTOR ANTAGONISTS
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Page/Page column 10; 11, (2009/05/28)
The present invention provides selective 5-HT7 receptor antagonist compounds of Formula I and their use in the treatment of migraine: where A is C(H)= or -N= and R1-7 are as defined herein.
SUBSTITUTED PIPERAZINYL PYRAZINES AND PYRIDINES AS 5-HT7 RECEPTOR ANTAGONISTS
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Page/Page column 22, (2009/04/25)
The present invention provides selective 5-HT7 receptor antagonist compounds of Formula (I) and their use in the treatment of migraine: where A is C(H)= or N=; m is 0, 1 or 2; R1 is optionally substituted phenyl, optionally substituted pyrazol-4-yl; optionally substituted imidazolyl, optionally substituted pyridyl, or thienyl; R2 is hydrogen or methyl; and R3 and R4 are as defined herein.
Selective Amination of Polyhalopyridines Catalyzed by a Palladium-Xantphos Complex
Ji, Jianguo,Li, Tao,Bunnelle, William H.
, p. 4611 - 4614 (2007/10/03)
(Matrix presented) Amination of 5-bromo-2-chloropyridine (1a) catalyzed by a palladium-Xantphos complex predominately gives 5-amino-2-chloropyridine product 3a in 96% isolated yield and excellent chemoselectivity (3a/4a = 97:3). Amination of 2,5-dibromopyridine (11) under the same conditions exclusively affords 2-amino-5-bromopyridine 4a.
