Catechol derivatives, and preventive and remedial preparations for regressive disorders in the central nervous system
申请人:MITSUI TOATSU CHEMICALS, Inc.
公开号:EP0261977A2
公开(公告)日:1988-03-30
Catechol derivatives which relate to the production of group. nerve growth factor in particular tissues of the brain are disclosed, as are methods for their synthesis, data on their physiological activity, and data on the toxicity of these derivatives. Examples of preparation for their administration are also disclosed.
The disclosed derivatives provide preventive and remedial effects for regressive disorders in the central nervous system including senile dementia of Alzheimer type: a preparation for this purpose includes a catechol derivative having the formula:
wherein R is two hydrogen atoms, two acyl groups, a -CO-group. -CO•CO- group, or -C(CH3)2- group, and wherein R1 and R2 are each independently a hydrogen atom or lower alkyl
公开了与在大脑特定组织中产生神经生长因子有关的儿茶酚衍生物,以及它们的合成方法、有关其生理活性的数据和有关这些衍生物毒性的数据。 还公开了用于给药的制剂实例。 公开的衍生物对包括阿尔茨海默型老年痴呆症在内的中枢神经系统退行性疾病具有预防和治疗作用:用于此目的的制剂包括具有以下式子的儿茶酚衍生物: 其中R为两个氢原子、两个酰基、一个-CO-基团、-CO-CO-基团或-C(CH3)2-基团,且R1和R2各自独立地为氢原子或低级烷基。