申请人:Otsuka Pharmaceutical Co., Ltd.
公开号:EP3318557A2
公开(公告)日:2018-05-09
The present invention provides a compound represented by the formula (I)
wherein X is a hydrogen atom or a fluorine atom; R is a hydrogen atom or alkyl; R1 is (1) cyclopropyl optionally substituted by 1 to 3 halogen atoms or (2) phenyl optionally substituted by 1 to 3 halogen atoms; R2 is alkyl, alkoxy, haloalkoxy, a halogen atom, cyano, etc.; and R3 is 7-oxo-7,8-dihydro-1,8-naphthyridinyl, 3-pyridyl, etc., or a salt thereof. The compound of the present invention has excellent antimicrobial activity against Clostridium difficile and is useful for the prevention or treatment of intestinal infection such as Clostridium difficile-associated diarrhea.
本发明提供了一种由式 (I) 表示的化合物
其中 X 是氢原子或氟原子;R 是氢原子或烷基;R1 是(1)任选被 1 至 3 个卤素原子取代的环丙基或(2)任选被 1 至 3 个卤素原子取代的苯基;R2 是烷基、烷氧基、卤代烷氧基、卤素原子、氰基等;R3 是 7-氧代-7,8-二氢-1,8-萘啶基、3-吡啶基等或其盐。本发明的化合物对艰难梭菌具有优异的抗菌活性,可用于预防或治疗艰难梭菌相关性腹泻等肠道感染。