公开(公告)号：WO2006128268A1

公开(公告)日：2006-12-07

申请号：PCT/BR2006/000107

申请日：2006-06-01

申请人： UNIVERSIDADE FEDERAL DO RIO DE JANEIRO - UFRJ ,  LACERDA BARREIRO, Eliezer Jesus de ,  MANSSOUR FRAGA, Carlos Alberto ,  SPERÃNDIO DA SILVA, Gilberto Marcelo ,  MOREIRA LIMA, Lidia ,  MEDEIROS DE CARVALHO, Fátima ,  MENEZES QUINTAS, Luis Eduardo ,  LÉGORA MACHADO, Alexandre ,  GONCALVES KOATZ, Vera Lúcia

发明人： LACERDA BARREIRO, Eliezer Jesus de ,  MANSSOUR FRAGA, Carlos Alberto ,  SPERÃNDIO DA SILVA, Gilberto Marcelo ,  MOREIRA LIMA, Lidia ,  MEDEIROS DE CARVALHO, Fátima ,  MENEZES QUINTAS, Luis Eduardo ,  LÉGORA MACHADO, Alexandre ,  GONCALVES KOATZ, Vera Lúcia

IPC分类号： C07D491/14 ,  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。

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。

公开(公告)号：WO2009073940A3

公开(公告)日：2009-11-12

申请号：PCT/BR2008000386

申请日：2008-12-12

申请人： UNICAMP ,  UNIV RIO DE JANEIRO ,  UNIV ESTADUAL PAULISTA JULIO D ,  DOS SANTOS JEAN LEANDRO ,  CHUNG MAN CHIN ,  MOREIRA LIMA LIDIA ,  FERREIRA COSTA FERNANDO ,  LANARO CAROLINA

发明人： DOS SANTOS JEAN LEANDRO ,  CHUNG MAN CHIN ,  MOREIRA LIMA LIDIA ,  FERREIRA COSTA FERNANDO ,  LANARO CAROLINA

IPC分类号： A61K31/4035 ,  C07D209/48

CPC分类号： A61K31/4196 ,  A61K9/0019

摘要： The present invention refers to the use of phthalimide and/or sulphonamide derivatives with nitric oxide donor properties, which have important activities in increasing the gamma-globin gene expression and anti-inflammatory and analgesic activities, effective in the treatment of hematologic diseases which require reducing the TNF-a levels and an exogenous source of nitric oxide. More particularly, the present invention describes the use of such phthalimide and/or sulphonamide derivatives for the treatment of sickle-cell diseases. The invention also has as a novel characteristic the disclosure of new functionalized phthalimide derivatives designed from the prototypes thalidomide and hydroxyurea, and designed rationally through the strategy of molecular hybridization for the treatment of said diseases. The invention still discloses a new method for obtaining a specific sulphonamide derivative which can be used in the preparation of a drug for the treatment of diseases which require reducing the levels of the TNF-a factor and an exogenous source of nitric oxide.

摘要翻译： 本发明涉及具有一氧化氮供体性质的邻苯二甲酰亚胺和/或磺酰胺衍生物的用途，其具有增加γ珠蛋白基因表达和抗炎和止痛活性的重要活性，其有效治疗需要减少的血液学疾病 TNF-α水平和一氧化氮的外源性来源。 更具体地，本发明描述了这种邻苯二甲酰亚胺和/或磺酰胺衍生物在治疗镰状细胞疾病中的用途。 本发明还具有从原型沙利度胺和羟基脲设计的新的官能化邻苯二甲酰亚胺衍生物的新颖特征，并通过分子杂交策略合理设计用于治疗所述疾病。 本发明还公开了一种获得特异性磺酰胺衍生物的新方法，其可用于制备用于治疗需要降低TNF-α因子和外源性一氧化氮水平的疾病的药物。