公开(公告)号：US20110212904A1

公开(公告)日：2011-09-01

申请号：US13015980

申请日：2011-01-28

申请人： Maria Grazia RIMOLI ,  Antonio CALIGNANO ,  Rosario CUOMO ,  Gianpiero BOATTO ,  Enrico ABIGNENTE ,  Daniela MELISI ,  Annalisa CURCIO ,  Elvira LUONGO ,  Giovanna LA RANA ,  Oscar SASSO ,  Giovanni SARNELLI ,  Roberto RUSSO ,  Maria NIEDDU ,  Carla CIRILLO ,  Salvatore DE LUCIA

发明人： Maria Grazia RIMOLI ,  Antonio CALIGNANO ,  Rosario CUOMO ,  Gianpiero BOATTO ,  Enrico ABIGNENTE ,  Daniela MELISI ,  Annalisa CURCIO ,  Elvira LUONGO ,  Giovanna LA RANA ,  Oscar SASSO ,  Giovanni SARNELLI ,  Roberto RUSSO ,  Maria NIEDDU ,  Carla CIRILLO ,  Salvatore DE LUCIA

IPC分类号： A61K31/7056 ,  C07H13/00 ,  A61K31/7024 ,  A61P25/04

CPC分类号： A61K31/7024 ,  A61K47/549 ,  C07H13/02 ,  C07H13/04 ,  C07H13/08 ,  C07H13/10

摘要： Pro-drugs of all non-steroidal anti-inflammatories with free acid function derivatized with an ester group, which have the general structural formula given below (I) where A is: aspirin, diflunisal, benorylate, ibufenac, diclofenac, indomethacin, sulindac, ketorolac, ibuprofen, naproxen, ketoprofen, fenoprofen, flurbiprofen, mefenamic acid, meclof enamic acid, flufenamic acid, niflumic acid, and where in the ester group R can be a sugar (amongst which aldose, or ketose pentose, or esose selected from a group of D- and L-enantioiuers of ribose, glucose, galactose, mannose, arabinose, xilose, allose, altrose, gulose, idose and talose and substituted derivatives thereof, such as glucosamine, galactosamine, N-acetyl glucosamine, N-acetyl galactosamine, N-acetyl ribosamine), a disaccharide, a trisaccharide or an oligosaccharide.

摘要翻译： 所有具有由酯基衍生的游离酸功能的所有非甾体抗炎药的前药具有下面给出的一般结构式（I），其中A是：阿司匹林，二氟尼柳，苯磺酸盐，异丙酸，双氯芬酸，吲哚美辛，舒林酸， 酮咯酸，布洛芬，萘普生，酮洛芬，非诺洛芬，氟比洛芬，甲芬那酸，甲酰胺酸，氟芬那酸，尼氟酸，其中酯基R中的糖可以是糖（其中醛糖或酮糖戊糖或选自 核糖，葡萄糖，半乳糖，甘露糖，阿拉伯糖，半乳糖，阿洛糖，阿卓糖，古洛糖，阿糖和托洛糖及其取代衍生物的D-和L-对映体组如葡萄糖胺，半乳糖胺，N-乙酰葡糖胺，N-乙酰半乳糖胺 ，N-乙酰基核糖胺），二糖，三糖或寡糖。