专利号:US-6417399-B1 优先权日:1997-01-14 标 题:Amelioration of neurological disorders by the administration of (2R),(3S), and/or (2S),3(S) stereoisomers of valnoctamide 发明人:BIALER MEIR; YAGEN BORIS; SPIEGELSTEIN OFER; ROEDER MICHAEL; SCHURIG VOLKER 权利人:YISSUM RES DEV CO 摘要:The present invention generally relates to the individual stereoisomers of the drug valnoctamide (a mixture of four stereoisomer kinds, VCD-valmethamide or 2-ethyl-3-methyl pentanamide) useful in treatment of neurological and psychotic disorders such as different kinds of epilepsy and affective disorders, and useful as tranquilizers and to treat pain, and to pharmaceutical compositions containing, as an active ingredient, these stereoisomers. The present invention further relates to a method for stereoselective separation and quantification of the four stereoisomers from a racemic mixture of VCD or plasma of patients treated with the racemic drug. The present invention further relates to a unique method for the synthesis of the individual stereoisomers.
专利号:US-2021062179-A1 优先权日:2015-02-26 标题 :Microsomal bioreactor for synthesis of drug metabolites 发明人:KRISHNAN SADAGOPAN; WALGAMA CHARUKSHA THAMEERA; NERIMETLA RAJASEKHARA REDDY 权利人:UNIV OKLAHOMA STATE 摘要:Reusable microsomal biocatalytic systems (bioreactors) constructed on carbon nanostructure modified electrodes are provided. The bioreactors comprise stable, biologically active immobilized enzymes such as human cytochromes P 450 (CYPs) and their redox partner proteins, e.g. CYP-NADPH (reduced nicotinamide adenine dinucleotide phosphate) reductases (CPR), on the carbon nanostructure surface. The immobilized enzymes may be present in liver microsomes, such as human liver microsomes (HLM) or as bactosomes, S9 fractions, etc. The bioreactors are used, for example, for synthesizing metabolites of interest from compounds such as drugs that are catabolized by the enzymes.
专利号:US-2011040105-A1 优先权日:2008-04-16 标题 :Processes useful for the synthesis of (r)-1--2-methyl-pyrrolidine 发明人:HUBER CHRISTIAN H; KHULMAN YOUNG MI; TANDEL SAGUN K; JOHANNSEN STEPHEN R; WANG TINGMIN; ANGELL PAUL 权利人:ARENA PHARM INC 摘要:Processes useful for making a pharmaceutically useful compound according to Formula (I), forms of such a compound, and intermediates useful in such processes are described.
专利号:US-2007059711-A1 优先权日:2004-07-30 标 题:Microarray for evaluation of stress-related genes in skin 发明人:SLOMINSKI ANDRZEJ; PISARCHIK ALEXANDER 权利人:SLOMINSKI ANDRZEJ; PISARCHIK ALEXANDER 摘要:The present invention provides a novel DNA microarray chip that can be used for simultaneous testing of transcriptional responses to cutaneous stressors in the context of neuro-endocrine-immune functions of the skin. The transcriptional responses to ultraviolet radiation in epidermal keratinocytes were tested using such microarray chip containing more than 700 neuro-endocrine-immune related genes. The gene expression pattern was non-random and time dependent; it included increased expression of genes involved in water and salt balance, prostaglandin synthesis, keratinocyte differentiation as well as genes coding for stress effectors, cytokines and metalloproteinases. In contrast, expression was decreased for genes coding for growth factors and their receptors, and for elements of extracellular matrix. This stochastic pattern suggests that transcriptional responses are coordinated and aimed at preservation of epidermal barrier function, prevention of early carcinogenic events and remodeling of extracellular matrix.
专利号:US-6030613-A 优先权日:1995-01-17 标题:Receptor specific transepithelial transport of therapeutics 发明人:BLUMBERG RICHARD S; SIMISTER NEIL E; LENCER WAYNE I 权利人:BRIGHAM & WOMENS HOSPITAL; UNIV BRANDEIS 摘要:The present invention relates in general to methods and products for initiating an immune response against an antigen, and in particular relates to transepithelial delivery of antigens to provoke tolerance and immunity. The present invention further relates to methods and products for the transepithelial delivery of therapeutics. In particular, the invention relates to methods and compositions for the delivery of therapeutics conjugated to a FcRn binding partner to intestinal epithelium, mucosal epithelium and epithelium of the lung. The present invention further relates to the synthesis, preparation and use of the FcRn binding partner conjugates as, or in, pharmaceutical compositions for oral systemic delivery of drugs and vaccines.
专利号:US-8697730-B2 优先权日:2007-10-26 标题 :5-lipoxygenase activating protein (FLAP) inhibitor 发明人:REWOLINSKI MELISSA VIRGINIA; SCHAAB KEVIN MURRAY; KING CHRISTOPHER DAVID; STOCK NICHOLAS SIMON 权利人:REWOLINSKI MELISSA VIRGINIA; SCHAAB KEVIN MURRAY; KING CHRISTOPHER DAVID; STOCK NICHOLAS SIMON; PANMIRA PHARMACEUTICALS LLC 摘要:Described herein are methods for the synthesis of 3-[5-(pyridin-2-ylmethoxy)-3-(2-methyl-2-propylthio)-1-[4-(2-methoxypyridin-5-yl)benzyl]-indol-2-yl]-2,2-dimethyl-propionic acid, pharmaceutically acceptable salts, pharmaceutically acceptable solvates thereof. Also described are pharmaceutical compositions suitable for oral administration to a mammal that include, as well as methods of using such oral pharmaceutical compositions for treating respiratory conditions or diseases, as well as other leukotriene-dependent or leukotriene mediated conditions or diseases.
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