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CAS号31891-06-2 2-氨基噻吩-3-羧酸乙酯 | CAS号31891-06-2 2-氨基噻吩-3-羧酸乙酯 | CAS号65076-02-0 2-((噻吩-3-基氨基)亚甲... | CAS号79242-76-5 2-(1H-吡咯-1-基)噻吩-3-羧酸2-氨基噻吩-3-甲酸乙酯置于sodium Hydroxide体系中,用 甲醇 作为反应溶剂,化学反应生成 2-氨基噻吩-3-甲酸
参考文献:Design,Synthesis And Structure-activity-Relationship Of 1,5-Tetrahydronaphthyridines As Cetp Inhibitors
标题:Design,Synthesis And Structure-activity-Relationship Of 1,5-Tetrahydronaphthyridines As Cetp Inhibitors
摘要:This Letter Describes The Discovery And Sar Optimization Of 1,5-Tetrahydronaphthyridines,A New Class Of Potent Cetp Inhibitors. The Effort Led To The Identification Of 21B And 21D With In Vitro Human Plasma Cetp Inhibitory Activity In The Nanomolar Range (Ic50 = 23 And 22 Nm,Respectively). Both 21B And 21D Exhibited Robust Hdl-C Increase In Hcetp/hapoa1 Dual Heterozygous Mice Model. (C) 2012 Elsevier Ltd. All Rights Reserved.
DOI:10.1016/j.Bmcl.2012.03.075
专利信息
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:US-4701528-A
优先权日:1985-12-23
标 题 :Intermediates useful in the preparation of 3,4-dihydro-4-oxothieno[2,3-d]pyrimidine-2-carboxylates and process for preparing same
发明人:THOMPSON MICHAEL D; MADDING GARY D
权利人:BRISTOL MYERS CO
摘要:There are disclosed compounds of Formulas I and II: ##STR1## wherein R 1 and R 2 may be hydrogen, lower alkyl having from 1 to 8 carbon atoms, lower alkenyl having from 3 to 6 carbon atoms, lower alkoxy having from 1 to 6 carbon atoms, hydroxy, nitro, amino, halo including chlorine, bromine, iodine, and fluorine, phenyl, alkanoyl having from 2 to 6 carbon atoms or they are bonded to one another to form a cycloalkene ring fused to the thiophene ring and having a total of from 5 to 7 annular ring carbon atoms, and R 3 is an aliphatic or an aromatic group such as lower alkyl, e.g., methyl or ethyl. Such compounds are useful as intermediates in the production of tiprinast and related compounds. n There is also disclosed a process for the regioselective synthesis of a compound of Formula I wherein R 1 is CH 3 and R 2 is (CH 3 ) 2 CHCH 2 which comprises reacting a mixture of compounds of the following formulas: ##STR2## and ##STR3## with trichloroacetonitrile under acidic conditions.
专利号:US-2006084805-A1
优先权日:2004-09-30
标题:Synthesis of thienopyridinone compounds and related intermediates
专利号:US-7982040-B2
优先权日:2004-05-17
标题 :Thienopyridinone compounds and methods of treatment
发明人:DHANOA DALE S; BECKER OREN; NOIMAN SILVIA; MOHANTY PRADYUMNA; CHEN DONGLI; LOBERA MERCEDES; WU LAURENCE; MARANTZ YAEL; INBAL BOAZ; HEIFETZ ALEXANDER; BAR-HAIM SHAY; SHACHAM SHARON
权利人:NANOTHERAPEUTICS 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-2005073265-A1
优先权日:2004-02-04
标题 :Conjugated thiophenes having conducting properties and synthesis of same
专利号:NO-327896-B1
优先权日:1999-01-19
标 题 :Tricyclic benzodiazepines, pharmaceutical composition, use of the compounds and intermediates useful in the synthesis of the compounds