263257-15-4Relevant articles and documents
OXYSTEROLS AND METHODS OF USE THEREOF
-
Paragraph 00272, (2018/05/16)
Compounds are provided according to Formula (A): and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein R1, R2, R3, R4, R5, R6, and RG are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of conditions.
BROMODOMAIN INHIBITORS AND USES THEREOF
-
Page/Page column 112, (2012/06/16)
The present invention relates to compounds useful as inhibitors of bromodomain-containing proteins. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using said compositions in the treatment of various disorders.
3-PHENOXYMETHYLPYRROLIDINE COMPOUNDS
-
Page/Page column 27-28, (2011/02/18)
In one aspect, the invention relates to compounds of formula I: where R1-6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin and norepinephrine reuptake inhibitors. In a
Practical synthesis of chiral 2-morpholine: (4-Benzylmorpholin-2-(s)-yl)- (tetrahydropyran-4-yl) Methanone mesylate, a useful pharmaceutical intermediate
Kopach, Michael E.,Singh, Utpal K.,Kobierski, Michael E.,Trankle, William G.,Murray, Michael M.,Pietz, Mark A.,Forst, Mindy B.,Stephenson, Gregory A.,Mancuso, Vincent,Giard, Thierry,Vanmarsenille, Michel,De France, Thierry
experimental part, p. 209 - 224 (2010/04/22)
A commercial synthesis was developed for the production of (4-benzylmorpholin-2-(S)-yl)-(tetrahydropyran-4-yl) methanone mesylate, la, a key starting material for a phase 2, new investigational drug candidate at Eli Lilly and Company. The target compound was produced in the clinical pilot plant by the combination of two key steps: resolution of a morpholine amide intermediate to install the S-morpholino stereocenter in 35% yield and a high-yielding (89%) Grignard reaction to generate the title compound la, isolated as a mesylate salt. The Grignard reaction was found to proceed optimally when using a combination of I2 and DIBAL-H for the initiation. In addition, the Grignard reagent formation was monitored by ReactMax calorimetry, and proof-of-concept studies were completed, demonstrating that the Grignard step could potentially be run as a continuous process with magnesium recycling.
Dibenzyl Amine Compounds and Derivatives
-
Page/Page column 48, (2010/11/28)
Dibenzyl amine compounds and derivatives, pharmaceutical compositions containing such compounds and the use of such compounds to elevate certain plasma lipid levels, including high density lipoprotein-cholesterol and to lower certain other plasma lipid levels, such as LDL-cholesterol and triglycerides and accordingly to treat diseases which are exacerbated by low levels of HDL cholesterol and/or high levels of LDL-cholesterol and triglycerides, such as atherosclerosis and cardiovascular diseases in some mammals, including humans.
FLUORENE DERIVATIVE
-
Page/Page column 18, (2010/11/24)
This invention relates to a novel fluorene derivative having a characteristic structure in which guanidino group or the like functional group is linked to the fluorene structure via carbonyl group, or a salt thereof. The compound of the invention has an a
MORPHOLINE DERIVATIVES AS NOREPINEPHRINE REUPTAKE INHIBITORS
-
Page/Page column 56, (2010/02/11)
Compounds of the general formula (I) are inhibitors of the reuptake of norepinephrine. As such, they may be useful for the treatment of disorders of the central and/or peripheral nervous system.