公开(公告)号：US3935266A

公开(公告)日：1976-01-27

申请号：US192557

申请日：1971-10-26

申请人： Sadao Hashimoto ,  Ryuji Sakakibara ,  Yasushi Kurashige ,  Katsuo Takikawa ,  Yoko Osame ,  Hiroshi Minami ,  Takashi Suzue

发明人： Sadao Hashimoto ,  Ryuji Sakakibara ,  Yasushi Kurashige ,  Katsuo Takikawa ,  Yoko Osame ,  Hiroshi Minami ,  Takashi Suzue

IPC分类号： A61K31/16 ,  A61K31/165 ,  C07C67/00 ,  C07C239/00 ,  C07C279/14 ,  C07C103/30

CPC分类号： C07C279/14

摘要： An N-substituted guanidino acid derivatives having the following formula of ##EQU1## wherein R is an alkyl having 6 to 15 carbon atoms,. a cycloalkyl having 6 to 15 carbon atoms or an aryl(C.sub.6 to C.sub.8)alkyl(C.sub.1 to C.sub.9); A represents R.sup.1 or R.sub.2 CO--, R.sup.1 being an alkyl having 1 to 4 carbon atoms, an alkenyl having 2 to 4 carbon atoms, cyclohexyl, a phenyl containing or not containing a substitute of a lower alkyl, a halogenated lower alkyl, a lower alkoxy, hydroxy or a halogen, or a benzyl containing or not containing a substitute of a lower alkyl, a halogenated lower alkyl, a lower alkoxy, hydroxy or a halogen, and R.sup.2 being an alkyl of 1 to 3 carbon atoms, an alkenyl of 2 to 3 carbon atoms, an aryl of 6 to 8 carbon atoms or an aryl(C.sub.6 to C.sub.8)alkyl(C.sub.1 to C.sub.2); and n is an integer of 4 to 10. The present compounds are excellent in pharmacological activities, particularly in antagonism to bradykinin and histamine, and useful as anti-inflammatory agent.

摘要翻译： 具有下式的ANH ANGLE CNH（CH 2）n CONHR NH的N-取代胍基衍生物，其中R是具有6至15个碳原子的烷基。 具有6至15个碳原子的环烷基或芳基（C 6至C 8）烷基（C 1至C 9）; A表示R 1或R 2 CO-，R 1为具有1至4个碳原子的烷基，具有2至4个碳原子的烯基，环己基，含有或不含有低级烷基，卤代低级烷基，低级烷氧基 ，羟基或卤素，或含有或不含低级烷基，卤代低级烷基，低级烷氧基，羟基或卤素的取代基的苄基，R 2为1至3个碳原子的烷基，烯基为2 至3个碳原子，6至8个碳原子的芳基或芳基（C6至C8）烷基（C1至C2）; n为4〜10的整数。本发明化合物的药理活性特别优选缓激肽和组胺的拮抗作用，作为抗炎剂有用。