专利号:US-2006069260-A1 优先权日:2004-09-28 标 题:Preparation of N-aryl pyridones 发明人:ZHANG HUIPING; CHEN BANG-CHI; ZHAO RULIN 权利人:ZHANG HUIPING; CHEN BANG-CHI; ZHAO RULIN 摘要:A novel process and intermediates thereof for making N-aryl pyridones of the type shown below from appropriate pyridinolates is described. n nThese compounds are useful as intermediates for the synthesis of clinical candidates.
专利号:WO-2013046211-A1 优先权日:2011-09-27 标 题 :Processes for the preparation of 5-chloro-n-({(5s)-2-oxo-3-[4-(3-oxo-4-morpholinyl) phenyl]-1,3-oxazolidin-5-yl}methyl)-2-thiophene-carboxamide and intermediates thereof 发明人:MOHAN RAO DODDA; KRISHNA REDDY PINGILI; VENKAT REDDY BUTHUKURI 权利人:SYMED LABS LTD; MOHAN RAO DODDA; KRISHNA REDDY PINGILI; VENKAT REDDY BUTHUKURI 摘要:TThe present invention provides processes for the preparation of 5-chloro-N-({(5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)phenyl]-1,3-oxazolidin-5-yl}methyl)-2-thiophene-carboxamide (I) and intermediates thereof. Also provides novel intermediates and their use in the synthesis of oxazolidine derivatives.
专利号:WO-2015198259-A1 优先权日:2014-06-26 标 题:Process for the synthesis of rivaroxaban and intermediate for the production thereof 发明人:FERRARI MASSIMO; GHEZZI EMANUELE; GHEZZI MARCELLO 权利人:ERREGIERRE SPA 摘要:A process is described for the production of Rivaroxaban, a compound having the following structural formula: (I) by means of obtaining a novel intermediate of said process.
专利号:US-2005192265-A1 优先权日:2003-03-20 标 题:Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting beta-amyloid peptide release and/or its synthesis by use of such compounds 发明人:THOMPSON RICHARD C; WILKIE STEPHEN; STACK DOUGLAS R; VANMETER ELDON E; SHI QING; BRITTON THOMAS C; AUDIA JAMES E; REEL JON K; MABRY THOMAS E; DRESSMAN BRUCE A; CWI CYNTHIA L; HENRY STEVEN S; MCDANIEL STACEY L; STUCKY RUSSELL D; PORTER WARREN J 摘要:Disclosed are compounds which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions that include a compound which inhibits β-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
专利号:US-6906056-B2 优先权日:1998-06-22 标 题:Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds 发明人:THOMPSON RICHARD C; WILKIE STEPHEN; STACK DOUGLAS R; VANMETER ELDON E; SHI QING; BRITTON THOMAS C; AUDIA JAMES E; REEL JON K; MABRY THOMAS E; DRESSMAN BRUCE A; CWI CYNTHIA L; HENRY STEVEN S; MCDANIEL STACEY L; STUCKY RUSSELL D; PORTER WARREN J 权利人:LILLY CO ELI 摘要:Disclosed are compounds which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions that include a compound which inhibits β-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
专利号:US-9763953-B2 优先权日:2005-09-22 标题:Cholinergic enhancers with improved blood-brain barrier permeability for the treatment of diseases accompanied by cognitive impairment 发明人:MAELICKE ALFRED 权利人:GALANTOS PHARMA GMBH; NEURODYN LIFE SCIENCES INC 摘要:The present invention refers to compounds that, in addition to enhancing the sensitivity to acetylcholine and choline, and their exogenous agonists, of neuronal cholinergic receptors and/or acting as cholinesterase inhibitors and/or neuroprotective agents, have enhanced blood-brain barrier permeability in comparison to their parent compounds. The compounds are derived (either formally by their chemical structure or directly by chemical synthesis) from natural compounds belonging to the class of amaryllidaceae alkaloids e.g., galantamine, narwedine and lycoramine, or from metabolites of said compounds. The compounds of the present invention can either interact as such with their target molecules, or they can act as “pro-drugsâ€?, in the sense that after reaching their target regions in the body they are converted by hydrolysis or enzymatic attack to the original parent compound and react as such with their target molecules, or both. The compounds of this invention may be used as medicaments.