CAS: 632-11-1; (R)-3-Amino-2-Hydroxypropanoic Acid

相似化合物

565-71-9 632-13-3 52558-24-4

上下游产品

(11S)-cycl°Cinamide A R)-3-benzoyl-oxazolidine-5-carboxylic acid(R)-3-benzoyl-oxazolidine-5-carboxylic acid -N-(diphenylmethyl)-3-hydroxy-2-oxo-1-azedineacetamide(3R)-α-(p-benzyloxy)phenyl-N-(diphenylmethyl)-3-hydroxy-2-oxo-1-azedineacetamide -N-(diphenylmethyl)-3-hydroxy-2-oxo-1-azedineacetamide(3S)-α-(p-benzyloxy)phenyl-N-(diphenylmethyl)-3-hydroxy-2-oxo-1-azedineacetamide N-(Diphenelmethyl)-3-hydroxy-2-oxo-α-phenyl-1-azetidineacetamide

📜(R)-3-Benzyloxycarbonylamino-2-Hydroxypropionic Acid置于palladium 10% On Activated Carbon,氢气体系中,用 乙醇 作为反应溶剂,20.0 °C,101.33 Kpa 条件下,反应 17.0H,以92%的收率获得产物(R)-异丝氨酸
参考文献:Novel Glucagon Receptor Antagonists With Improved Selectivity Over The Glucose-Dependent Insulinotropic Polypeptide Receptor
标题:Novel Glucagon Receptor Antagonists With Improved Selectivity Over The Glucose-Dependent Insulinotropic Polypeptide Receptor
摘要:Optimization Of A New Series Of Small Molecule Human Glucagon Receptor (Hglur) Antagonists Is Described. In The Process Of Optimizing Glucagon Receptor Antagonists,We Counter-Screened Against The Closeli Related Human Gastric Inhibitory Polypeptide Receptor (Hgipr),And Through Structure Activity Analysis,We Obtained Compounds With Low Nanomolar Affinities Toward The Hglur,Which Were Selective Against The Hgipr And The Human Glucagon-Like Peptide-1 Receptor (Hglp-1R). In The Best Cases,We Obtained A >50 Fold Selectivity For The Hglur Over The Hgipr And A > 1000 Fold Selectivity Over The Hglp-1R. A Potent And Selective Glucagon Receptor Antagonist Was Demonstrated To Inhibit Glucagon-Induced Glycogenolysis In Primary Rat Hepatocytes As Well As To Lower Glucagon-Induced Hyperolycemia In Sprague-Dawley Rats. Furthermore. The Compound Was Shown To Lower Blood Glucose In The Ob/ob Mouse After Oral Dosing.
DOI:10.1021/jm7015599

专利信息

专利号:WO-9746543-A1
优先权日:1996-05-31
标题:Acetyl derivatives of thiazoles and analogues
发明人：PYNE STEPHEN GEOFFREY; UNG ALISON THAVARY
权利人:UNIV WOLLONGONG; PYNE STEPHEN GEOFFREY; UNG ALISON THAVARY
摘要:The present invention is directed to compounds useful in the treatment of autoimmune diseases and inflammatory diseases of general formula (I) wherein R1 is alkyl, alkenyl or alkynyl having from 1 to 6 carbons, phenyl, benzyl or phenethyl; R2 is H, C1 to C5 alkyl which can optionally be partially hydroxylated or the group (a) wherein n is from 0 to 4; and X, Y and Z are independently CH, N, NH, O or S, or a pharmaceutically acceptable ester or acid addition salt thereof, or a stereoisomer or a geometric isomer thereof, with the proviso that at least one of X, Y or Z is CH, that one and only one of X, Y and Z is NH, O or S and further that when Y is N or NH then Z is not N or NH. The present invention is also concerned with processes for the synthesis of the compounds and with methods of use of the compounds.