专利号:US-10005720-B2 优先权日:2013-04-05 标题:Compounds useful for the treatment of metabolic disorders and synthesis of the same 发明人:SEXTON JONATHAN Z; BRENMAN JAY E; MUSSO DAVID L 权利人:NORTH CAROLINA CENTRAL UNIV; UNIV NORTH CAROLINA CHAPEL HILL 摘要:The present invention provides compounds of Formula (I): wherein variables X, Y, Z and R1 are as described herein. Some of the compounds described herein are glutamate dehydrogenase activators. The invention is also directed to pharmaceutical compositions comprising these compounds, uses of these compounds and compositions in the treatment of metabolic disorders as well as synthesis of the compounds.
专利号:WO-03055857-A8 优先权日:2001-12-28 标题 :A process for synthesis of heterocyclic aminoalkyl benzamides 发明人:STANKOVIC SLOBODAN; MITOV SLOBODAN; STANOJEVIC CASLAV; PESIC LJILJANA 权利人:FARMACEUTSKO HEMIJSKA IND ZDRA; STANKOVIC SLOBODAN; MITOV SLOBODAN; STANOJEVIC CASLAV; PESIC LJILJANA 摘要:The simple, new, original and convenient for use, procedure for obtaining of compounds, belonging to the group of $i(heterocyclic aminoalkyl benzamides) of general formula 1, is developed, and/or salts and/or hydrates and/or optical isomers thereof, wherein R1 and R2 denote C1-C4 $i(alkyl) group, R3 denotes an $i(aminosulphonyl) group, denotes a $i(hydrogen) atom or an $i(amino) group, R5 denotes a $i(hydrogen) or a $i(halogen) atom, and and the coefficients $i(m )and $i(n) have value of 1 and/or 2. Of a particular interest in clinical practice are: $i(sulpiride )(RS, R+ or S-)-(5-$i(aminosulphonyl))-N-/(1-$i(ethyl)-2-$i(pyrrolidinyl))$i(methyl)/-2-$i(methoxybenzamide)) and sulmepride (RS, R+ or S-)-(5-($i(aminosulphonyl))-2-$i(methoxy)-N-/-(1-$i(methyl-)2-$i(pyrrolidinyl)methyl/benzamide)). The compounds belonging to this group are used in therapy as: antipsychotics, anti depressives and anti emetics, fungicides, for contraceptive mixtures, in treatment of sterility, as radiopharmaceutical compositions in nuclear medicine, in treatment of migraine of various origins, as well as in treatment of parkinsonism. The advantage of the present invention is in its completely new and simple way to carry out the synthesis of $i(heterocyclic aminoalkyl benzamides )and/or salts and/or hydrates thereof, through reaction of $i(2-alcoxy-5-suiphamoyl-alkyl benzoate )with the corresponding (RS R+ or S-) heterocyclic amine. )Lower temperature of rection and work at atmospheric pressure without catalysts, performing the reaction in cheaper and safer organic solvents, i obtaining the final product which does not require any additional purification, achieving of I good yield and high quality of the final product, cheaper procedure for industrial use and obtaining of the product of high pharmacopeic purity.
专利号:US-5468876-A 优先权日:1986-05-22 标题:Intermediates for the stereoconservative synthesis of 1-substituted (S)-and (R)-2-aminomethylpyrrolidines 发明人:FEDERSEL HANS-JUEGEN; HOE THOMAS; RAEMSBY STEN I; STROEM PETER H E 权利人:ASTRA AB 摘要:Disclosed are (R)- and (S)-isomers of the compounds of the Formulas II and III with at least 95% optical purity ##STR1## wherein R 1 and R 2 are the same or different and represent a hydrogen atom, a lower alkyl, lower alkenyl or lower alkynyl group, a cycloalkyl group or a group (CH 2 ) m Ph, wherein m is 0-3 and Ph is a substituted or unsubstituted phenyl group. n These compounds are intermediates in the stereoconservative synthesis of 1-substituted (S)- and (R)-2-aminomethylpyrrolidines.
专利号:US-7576211-B2 优先权日:2004-09-30 标题 :Synthesis of thienopyridinone compounds and related intermediates 发明人:DHANOA DALE S; BECKER OREN; NOIMAN SILVIA; CHEN DONGLI; MARANTZ YAEL; SHACHAM SHARON; HEIFETZ ALEXANDER; INBAL BOAZ; BAR-HAIM SHAY; MOHANTY PRADYUMNA; LOBERA MERCEDES; WU LAURENCE 权利人:EPIX DELAWARE INC 摘要:The invention relates to 5-HT receptor agonists and partial agonists. Novel thienopyridinone compounds represented by Formula I, and synthesis and uses thereof for treating diseases mediated directly or indirectly by 5-HT receptors, are disclosed. Such conditions include Alzheimer's disease, cognition disorders, irritable bowel syndrome, nausea, emesis, vomiting, prokinesia, gastroesophageal reflux disease, nonulcer dyspepsia, depression, anxiety, urinary incontinence, migraine, arrhythmia, atrial fibrillation, ischemic stroke, gastritis, gastric emptying disorders, feeding disorders, gastrointestinal disorders, constipation, erectile dysfunction, and respiratory depression. Methods of preparation and novel intermediates and pharmaceutical salts thereof are also included.
专利号:WO-2016123658-A1 优先权日:2015-02-08 标题:Solid state synthesis of polyaromatic hydrocarbons and their hydrides 发明人:WHITE BRUCE WILLIAM 权利人:NOVELCHEM AUSTRALIA PTY LTD 摘要:A process of dehydrogenation of hydrocarbons in a closed reactor by the action of oxidants under beat and pressure and time and presents as a solid-state process is disclosed. The reactor contains absorbents in situ to remove any unwanted products as the dehydrogenation proceeds. The process could be employed as a useful step in relevant organic synthesis work in future. In a specific example, a process of synthesising fullerene hydrides is described.
专利号:US-8278296-B2 优先权日:2006-08-10 标题:Manipulation of brain CDP-diacylglycerol and uses thereof 发明人:UNDIEH ASHIWEL S 权利人:UNDIEH ASHIWEL S 摘要:Provided herein methods of screening for potential antidepressant compounds effective to increase production of cellular CDP-diacylglycerol and synthesis of inositol phospholipid in depression-related areas of the brain. Also, provided are methods of diagnosing and treating depressive or mood disorders in a subject by administering these screened antidepressant compounds. Further provided is a method of determining the therapeutic efficacy of an antidepressant drug regimen by comparing the ratio of CDP-diacylglycerol/inositol phosphate after treatment to a basal ratio in a subject.
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