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-9700543-B2 优先权日:2011-05-31 标题 :GLP-1 receptor stabilizers and modulators 发明人:BOEHM MARCUS F; MARTINBOROUGH ESTHER; MOORJANI MANISHA; TAMIYA JUNKO; HUANG LIMING; FOWLER THOMAS; NOVAK ANDREW; MEGHANI PREMJI; BRAHMACHARY ENUGURTHI; YEAGER ADAM RICHARD 权利人:CELGENE INT II SÀRL 摘要:Compounds that bind the glucagon-like peptide 1 (GLP-1) receptor, methods of their synthesis, methods of their therapeutic and/or prophylactic use, and methods of their use in stabilizing GLP-1 receptor in vitro for crystallization of the GLP-1 receptor are provided. Certain compounds may have activity as modulators or potentiators with respect to glucagon receptor, GIP receptor, GLP-1 and GLP-2 receptors, and PTH receptor on their own or in the presence of receptor ligands such as GIP(1-42), PTH(1-34), Glucagon(1-29), GLP-2(1-33), GLP-1(7-36), GLP-1(9-36), oxyntomodulin and exendin variants.
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合成参考文献
参考文献:10.1007/s002109900124 摘要:Knapp J, Bokník P, Deng MC, Huke S, Lüss I, Klein-Wiele O, Linck B, Lüss H, Müller FU, Nacke P, Scheld HH, Schmitz W, Vahlensieck U, Neumann J. On the contractile function of protein phosphatases in isolated human coronary arteries. Naunyn Schmiedebergs Arch Pharmacol. 1999 Oct;360(4):464–72. doi: 10.1007/s002109900124.