42873-96-1Relevant academic research and scientific papers
SUBSTITUTED DIHYDRO AND TETRAHYDRO OXAZOLOPYRIMIDINONES, PREPARATION AND USE THEREOF
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Page/Page column 29, (2010/04/23)
The present invention relates to a series of substituted dihydro and tetrahydro oxazolopyrimidinones, specifically, to a series of 2-substituted-2,3-dihydro-oxazolo[3,2-a]pyrimidin-7-ones and 2-substituted-2,3,5,6-tetra-hydro-oxazolo[3,2-a]pyrimidin-7-ones of formula (I): Wherein p, n, X, Y, R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein. This invention also relates to methods of making these compounds including novel intermediates. The compounds of this invention are modulators of metabotropic glutamate receptors (mGluR), particularly, mGluR2 receptor. Therefore, the compounds of this invention are useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of central nervous system disorders (CNS), including but not limited to acute and chronic neurodegenerative conditions, psychoses, convulsions, anxiety, depression, migraine, pain, sleep disorders and emesis.
Reduction of CYP450 inhibition in the 4-[(1H-imidazol-4-yl)methyl] piperidine series of histamine H3 receptor antagonists
Berlin, Michael,Ting, Pauline C.,Vaccaro, Wayne D.,Aslanian, Robert,McCormick, Kevin D.,Lee, Joe F.,Albanese, Margaret M.,Mutahi, Mwangi W.,Piwinski, John J.,Shih, Neng-Yang,Duguma, Luli,Solomon, Daniel M.,Zhou, Wei,Sher, Rosy,Favreau, Leonard,Bryant, Matthew,Korfmacher, Walter A.,Nardo, Cymbelene,West Jr., Robert E.,Anthes, John C.,Williams, Shirley M.,Wu, Ren-Long,Susan She,Rivelli, Maria A.,Corboz, Michel R.,Hey, John A.
, p. 989 - 994 (2007/10/03)
A novel series of histamine H3 receptor antagonists based on the 4-[(1H-imidazol-4-yl)methyl]piperidine template displaying low CYP2D6 and CYP3A4 inhibitory profiles has been identified. Structural features responsible for the reduction of P450 activity, a typical liability of 4-substituted imidazoles, have been established.
Synthesis and Copolymerization of a Mesogenic Acrylate Having 4-(2,2,6,6-Tetramethylpiperidyl-4-oxy)phenyl Benzoate as a Precursor for Nitroxide-Containing Liquid-Crystalline Side-Chain Polymers
Morishima, Yotaro,Fujita, Junko,Ikeda, Takahiro,Kamachi, Mikiharu
, p. 557 - 560 (2007/10/02)
A mesogenic acrylate monomer 4-(2,2,6,6-tetramethylpiperidyl-4-oxy)phenyl 4'-(6-acryloyloxyhexyl)benzoate was synthesized and copolymerized with 4-cyclohexyloxyphenyl 4'-(6-acryloyloxyhexyloxy)benzoate.Oxidation of the copolymer yielded a nitroxide-containing liquid-crystalline side-chain polymer.
