公开(公告)号：US5294439A

公开(公告)日：1994-03-15

申请号：US379256

申请日：1989-07-13

申请人： Heinojo Yamasaka ,  Hiroyasu Uchiyama ,  Hirotaka Masuda ,  Yoshiomi Sakamoto ,  Yoshimi Nakamigawa ,  Mitsuko Yoshioka ,  Terumasa Moriga

发明人： Heinojo Yamasaka ,  Hiroyasu Uchiyama ,  Hirotaka Masuda ,  Yoshiomi Sakamoto ,  Yoshimi Nakamigawa ,  Mitsuko Yoshioka ,  Terumasa Moriga

IPC分类号： C07D235/28 ,  A61K31/41 ,  A61K31/415 ,  A61K31/74

CPC分类号： C07D235/28

摘要： A stabilized physiologically active benzimidazole derivative having the formula (I): ##STR1## wherein R.sup.1 is hydrogen atom, an alkyl group having 1 to 8 carbon atoms, a fluoroalkyl group having 1 to 6 carbon atoms, a cycloalkyl group, phenyl group or an aralkyl group, R.sup.2 is hydrogen atom or a lower alkyl group, or R.sup.1 and R.sup.2 together with the adjacent nitrogen atom form a ring, and each of R.sup.3a, R.sup.3b, R.sup.4a, R.sup.4b and R.sup.4c independently is hydrogen atom, a halogen atom, a fluoroalkyl group having 1 to 6 carbon atoms, a lower alkyl group, a lower alkoxy group, a lower alkoxycarbonyl group or an amino group. The stabilized benzimidazole derivative is in amorphous form or present in contact with a basic material.

摘要翻译： 具有式（I）的稳定的生理活性苯并咪唑衍生物：其中R 1是氢原子，具有1至8个碳原子的烷基，具有1至6个碳原子的氟代烷基，环烷基，苯基 基团或芳烷基，R 2是氢原子或低级烷基，或者R 1和R 2与相邻的氮原子一起形成环，R3a，R3b，R4a，R4b和R4c各自独立地是氢原子，卤素原子 ，碳原子数1〜6的氟代烷基，低级烷基，低级烷氧基，低级烷氧基羰基或氨基。 稳定的苯并咪唑衍生物是无定形形式或与碱性材料接触。