公开(公告)号：WO2006128268A8

公开(公告)日：2007-04-26

申请号：PCT/BR2006000107

申请日：2006-06-01

申请人： UNIV RIO DE JANEIRO ,  LACERDA BARREIRO ELIEZER JESUS ,  MANSSOUR FRAGA CARLOS ALBERTO ,  SPERANDIO DA SILVA GILBERTO MA ,  MOREIRA LIMA LIDIA ,  MEDEIROS DE CARVALHO FATIMA ,  MENEZES QUINTAS LUIS EDUARDO ,  LEGORA MACHADO ALEXANDRE ,  GONCALVES KOATZ VERA LUCIA

发明人： LACERDA BARREIRO ELIEZER JESUS ,  MANSSOUR FRAGA CARLOS ALBERTO ,  SPERANDIO DA SILVA GILBERTO MA ,  MOREIRA LIMA LIDIA ,  MEDEIROS DE CARVALHO FATIMA ,  MENEZES QUINTAS LUIS EDUARDO ,  LEGORA MACHADO ALEXANDRE ,  GONCALVES KOATZ VERA LUCIA

IPC分类号： C07D491/056 ,  C07D491/14 ,  A61K31/4741 ,  A61P29/00 ,  C07C275/38

CPC分类号： C07D491/048

摘要： The present invention describes functionalizeds derivatives of ethyl 6-N- alkyl and/or 6-N-aryl ureas [1 ,3]dioxolo[5,4-g]quinolin-7-carboxylate (3a-z, 4a-z) and similar types (5a-z), of general formula (I, II, III and IV), useful in the treatment and/or prevention of inflammatory diseases, such as acute or chronic inflammatory conditions, different types of arthritis, asthma, Crohn's Disease and diabetes mellitus Type I, among others. These derivatives have the ability of modulate the inflammatory process, acting in mitogen activated protein kinase p-38 (MAPK-p38). Moreover, the derivatives of the present invention present expressive anti-inflammatory properties evaluated in in vivo models. The present invention also discloses processes for the production of such derivatives and harmaceutical com ositions containin the same.

摘要翻译： 本发明描述了6-N-烷基和/或6-N-芳基脲[1,3]二氧杂环戊烯并[5,4-g]喹啉-7-羧酸乙酯（3a-z，4a-z）的官能化衍生物和 可用于治疗和/或预防炎性疾病如急性或慢性炎症性疾病，不同类型的关节炎，哮喘，克罗恩病的通式（I，II，III和IV）的类似类型（5a-z） 和I型糖尿病等。 这些衍生物具有调节炎症过程的能力，作用于丝裂原活化蛋白激酶p38（MAPK-p38）。 此外，本发明的衍生物表现出在体内模型中评估的表现的抗炎特性。 本发明还公开了生产这种衍生物的方法和含有其的药物组合物。