公开(公告)号：US5356916A

公开(公告)日：1994-10-18

申请号：US830298

申请日：1992-01-31

申请人： Hatsunori Toyofuku ,  Jun Matsumoto ,  Toshie Takahashi ,  Masakazu Ebie ,  Naomi Sasada ,  Mitsuzi Agata ,  Shohei Sawaki ,  Masayoshi Goto

发明人： Hatsunori Toyofuku ,  Jun Matsumoto ,  Toshie Takahashi ,  Masakazu Ebie ,  Naomi Sasada ,  Mitsuzi Agata ,  Shohei Sawaki ,  Masayoshi Goto

IPC分类号： A61K31/41 ,  A61K31/4245 ,  A61K31/44 ,  A61K31/445 ,  A61K31/495 ,  A61K31/496 ,  A61K31/535 ,  A61K31/5377 ,  A61P25/00 ,  C07D271/06 ,  C07D413/12 ,  C07D521/00 ,  C12N9/99

CPC分类号： C07D271/06 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D413/10

摘要： A 1,2,4-oxadiazole derivative is represented by the following general formula (I): ##STR1## wherein R.sup.1 represents a lower alkyl or cycloalkyl group, a lower alkyl group substituted with a halogen atom, a lower alkylamino group or a phenyl group; R.sup.2 represents a hydrogen atom, a lower dialkylamino group, a cyclic alkylamino group, a cyclic amino group having an oxygen or nitrogen atom in the ring, a phenyl group which may be substituted with a halogen atom, a pyridyl group, an imidazolyl group, an alkylimidazolyl group, a benzimidazolyl group or a 2-oxopyrrolidinyl group; and n is 1, 2 or 3. The derivative has excellent monoamine oxidase-inhibitory activity and is effective as a medicine for treating Parkinson's disease.

摘要翻译： 1,2,4-恶二唑衍生物由以下通式（I）表示：其中R 1表示低级烷基或环烷基，被卤素原子取代的低级烷基，低级烷基氨基 或苯基; R2表示氢原子，低级二烷基氨基，环状烷基氨基，环中具有氧或氮原子的环状氨基，可被卤素原子取代的苯基，吡啶基，咪唑基， 烷基咪唑基，苯并咪唑基或2-氧代吡咯烷基; 并且n为1,2或3.该衍生物具有优异的单胺氧化酶抑制活性，作为治疗帕金森病的药物是有效的。