专利号:US-6936600-B2 优先权日:1999-04-01 标题:Sorbitol dehrydrogenase inhibitors 发明人:CHU-MOYER MARGARET Y; MYLARI BANAVARA L; ZEMBROWSKI WILLIAM J 权利人:PFIZER 摘要:This invention is directed to sorbitol dehydrogenase inhibitory compounds of the formula I, n n nwherein R 1 , R 2 and R 3 are as defined in the specification. This invention is also directed to pharmaceutical compositions containing those compounds and methods of treating or preventing diabetic complications, particularly diabetic neuropathy, diabetic nephropathy, diabetic microangiopathy, diabetic macroangiopathy and diabetic cardiomyopathy by administering such compounds to a mammal suffering from diabetes and therefore at risk for developing such complications. This invention is also directed to pharmaceutical compositions comprising a combination of a compound of formula I of this invention with an aldose reductase inhibitor and to methods of treating or preventing diabetic complications therewith. This invention is also directed to pharmaceutical compositions comprising a combination of a compound of formula I of this invention with an NHE-1 inhibitor and to methods of treating cardiomyopathy and other heart-related problems therewith. This invention is also directed to certain intermediates used in the synthesis of the compounds of formula I and to processes for preparing those intermediates.
专利号:US-2009137557-A1 优先权日:2005-11-22 标题 :Calcilytic Compounds 发明人:KU THOMAS WEN FU; LIN HONG; LUENGO JUAN I; MARQUIS JR ROBERT W; RAMANJULU JOSHI M; TROUT ROBERT; YAMASHITA DENNIS S 权利人:KU THOMAS WEN FU; LIN HONG; LUENGO JUAN I; MARQUIS JR ROBERT W; RAMANJULU JOSHI M; TROUT ROBERT; YAMASHITA DENNIS S 摘要:Novel calcilytic compounds, pharmaceutical compositions, methods of synthesis and methods of using them are provided.
参考标题:Water-Based Conditions For The Microscale Parallel Synthesis Of Bicyclic Lactams 作者:Sandra Malaquin,Mouhamad Jida,Justin Courtin,Guillaume Laconde,Nicolas Willand,Benoit Deprez,Rebecca Deprez-Poulain |发布日期:2013.2 摘要:A Mixture Of Ethanol And Water Yields The Expected Lactams, We Exemplified The Reaction And Procedure With The Preparation Of A Library Of 80 Members. Our Synthesis Scheme Is Validated For Synthesis Scales From 1 To 100 Mg. Therefore, It Can Be Used Both To Produce Rapidly Test Samples For Hts As Well As To Prepare Intermediates For The Synthesis Of More Elaborated Nature-Inspired Compounds.
合成参考文献
参考文献:10.1023/a:1023438511753 摘要:Vafina GF, Yakhina GR, Khakimova TV, Spirikhin LV, Galin FZ, Yunusov MS. Synthesis and Stereochemistry of Some 3-Azabicyclo[3.3.1]nonane Derivatives. Russian Journal of Organic Chemistry. 2003 Jan;39(1):49–56. doi: 10.1023/a:1023438511753.