申请人:Astellas Pharma Inc.
公开号:EP1955697A1
公开(公告)日:2008-08-13
To provide a novel and excellent agent for treating or preventing nociceptive pain, neuropathic pain, cancer pain, headache, bladder function disorder and the like, based on the inhibitory action on the capsaicin receptor VR1 activation.
The present invention was accomplished by confirming that a benzamide derivative characterized by the possession of a benzene ring in which a single ring is condensed on the nitrogen atom of amido group and possession of a lower alkylamino or an amino group substituted with a ring group at the neighboring position of said amido group has a strong inhibitory action on VR1 activation and excellent pharmacological actions based on this and by finding that it can become an excellent agent for treating or preventing VR1-involved diseases such as nociceptive pain, neuropathic pain, cancer pain, headache, bladder function disorder and the like.
提供一种基于对辣椒素受体 VR1 激活的抑制作用,用于治疗或预防痛觉痛、神经病 理痛、癌痛、头痛、膀胱功能紊乱等的新型优良制剂。
本发明是通过确认一种苯甲酰胺衍生物,其特征在于该衍生物具有一个苯环,在该苯环中,一个单环缩合在氨基基团的氮原子上,并且在所述氨基基团的邻近位置上具有一个被环基取代的低级烷基氨基或氨基,该衍生物对 VR1 的活化具有很强的抑制作用,并在此基础上具有很好的药理作用,并发现该衍生物可以成为治疗或预防 VR1 相关疾病(如痛觉疼痛)的一种很好的药物、神经性疼痛、癌痛、头痛、膀胱功能紊乱等。