申请人:Mitsui Toatsu Chemicals, Inc.
公开号:US04839376A1
公开(公告)日:1989-06-13
2-Pyrazoline derivatives of the formula (A): ##STR1## where R.sup.1 is a pyridyl, a pyrazyl or an alkoxy group; and R.sup.2 is a hydrogen atom, an alkyl, a pyridyl, a furyl, phenyl or a substituted phenyl group, and to a process for producing the same. Therapeutic agents for treating cerebrovascular diseases containing, as the active ingredient, a 2-pyrazoline derivative represented by the formula (G): ##STR2## where R.sup.3 is a hydrogen atom, an alkyl, acetyl, an alkoxycarbonyl, an amino, benzoyl, a substituted benzoyl, a pyridylcarbonyl, a furylcarbonyl, a thienylcarbonyl, a pyrazylcarbonyl, an N-substituted carbamoyl, an N-substituted thiocarbamoyl, or carboxy group; and R.sup.4 is a hydrogen atom, an alkyl, a pyridyl, a thienyl, a furyl, cyclohexyl, phenyl or a substituted phenyl group or a pharmaceutically acceptable salt thereof. These therapeutic agents cope with cerebral edemas in the acute stage of cerebral apoplexy and regulates the whole-body and intracranial body circulation, thereby protecting ischemic lesions and minimizing the spread to affected parts.
式(A)的2-
吡唑啉衍
生物:##STR1##
其中R1是
吡啶基,
吡唑基或烷氧基;R2是氢原子,烷基,
吡啶基,
呋喃基,苯基或取代苯基,以及制备它们的方法。治疗脑血管疾病的药物,其活性成分是由式(G)表示的2-
吡唑啉衍
生物:##STR2##
其中R3是氢原子,烷基,乙酰基,烷氧羰基,
氨基,苯甲酰基,取代苯甲酰基,
吡啶基羰基,
呋喃基羰基,
噻吩基羰基,
吡唑基羰基,N-取代
氨基甲酰基,N-取代
硫代
氨基甲酰基或羧基;R4是氢原子,烷基,
吡啶基,
噻吩基,
呋喃基,环己基,苯基或取代苯基,或其药学上可接受的盐。这些治疗剂能够应对急性脑卒中的脑
水肿,并调节全身和颅内循环,从而保护缺血损伤并将其扩散到受影响的部位最小化。