公开(公告)号：WO2012054996A1

公开(公告)日：2012-05-03

申请号：PCT/BR2011/000389

申请日：2011-10-25

申请人： UNIVERSIDADE FEDERAL DO RIO DE JANEIRO ,  MOREIRA LIMA, Lídia ,  DE LACERDA BARREIRO ELIEZER, Jesus ,  FREITAS DE LIMA CLEVERTON, Kleiton ,  DE OLIVEIRA LOPES, Raquel ,  PALHARES DE MIRANDA, Ana, Luisa ,  SARNO, Euzenir, Nunes ,  PINHEIRO, Roberta, Olmo ,  FUNDAÇÂO OSWALDO CRUZ / FIOCRUZ

发明人： MOREIRA LIMA, Lídia ,  DE LACERDA BARREIRO ELIEZER, Jesus ,  FREITAS DE LIMA CLEVERTON, Kleiton ,  DE OLIVEIRA LOPES, Raquel ,  PALHARES DE MIRANDA, Ana, Luisa ,  SARNO, Euzenir, Nunes ,  PINHEIRO, Roberta, Olmo

IPC分类号： C07D317/68 ,  C07D213/80 ,  C07D233/64 ,  C07C275/26 ,  A61K31/357 ,  A61K31/44 ,  A61K31/17 ,  A61P29/00 ,  A61P19/02 ,  A61P17/06 ,  A61P11/06

CPC分类号： C07D317/68 ,  C07D213/80

摘要： A presente invenção refere-se a compostos aril e/ou heteroaril uréias funcionalizados de fórmula geral (I) e (II), assim como seus sais e/ou solvatos e polimorfos capazes de atuar na inibição de proteínas quinases da família MAPK e, ainda, na modulação das citocinas como TNF e IL1β. Além disso, a invenção descreve um processo sintético para tais compostos, o preparo de uma composição farmacêutica que será utilizada na produção de medicamentos para o tratamento ou prevenção de distúrbios associados à dor aguda ou crónica, bem como no tratamento de doenças de natureza inflamatórias, sendo esta inflamação aguda ou crónica.

摘要翻译： 本发明涉及通式（I）和（II）的官能化芳基和/或杂芳基脲化合物，以及其可以抑制来自MAPK家族的蛋白激酶的盐和/或溶剂化物和多晶型物，并且还调节细胞因子如TNF 和IL1β。 此外，本发明涉及合成这些化合物的方法，制备药物组合物的方法，该药物组合物将用于制备用于治疗或预防与急性或慢性疼痛有关的疾病的药物，以及用于治疗炎性疾病，所述方法 炎症是急性或慢性的。

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：WO2006039767A1

公开(公告)日：2006-04-20

申请号：PCT/BR2004/000202

申请日：2004-10-15

申请人： UNIVERSIDADE FEDERAL DO RIO DE JANEIRO-UFRJ ,  UNIVERSIDADE ESTADUAL PAULISTA-UNESP ,  VIEGAS, Claudio, Jr. ,  BOLZANI, Vanderlan da Silva ,  DE LACERDA BARREIRO, Eliezer, Jesus ,  CASTRO, Newton, G. ,  YOUNG, Maria, Cláudia, Marx ,  SANTOS, Rocha, Mônica

发明人： VIEGAS, Claudio, Jr. ,  BOLZANI, Vanderlan da Silva ,  DE LACERDA BARREIRO, Eliezer, Jesus ,  CASTRO, Newton, G. ,  YOUNG, Maria, Cláudia, Marx ,  SANTOS, Rocha, Mônica

IPC分类号： C07D211/22

CPC分类号： C07D211/40 ,  C07D211/42

摘要： The present invention provides pharmaceutical compositions containing new molecules capable of inhibiting acetylcholinesterase, thus being useful in the treatment of pathologies associated to cholinergic transmission, such as memory related disorders, neurodegenerative disorders such as Alzheimer's Disease, Miastenia Gravis or in the treatment of intoxications induced by chemical agents of central action; the production processes of those compositions are also described here.

摘要翻译： 本发明提供含有能够抑制乙酰胆碱酯酶的新分子的药物组合物，因此可用于治疗与胆碱能传递相关的病症，例如记忆相关病症，神经退行性疾病如阿尔茨海默病，三叠纪糜烂或治疗由 化学药剂的中枢作用; 这里也描述了这些组合物的生产方法。

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。