Di-isopropyl-phosphinoyl-alkanes as topical agents for the treatment of sensory discomfort
申请人:Wei Edward T.
公开号:US20150164924A1
公开(公告)日:2015-06-18
The present discovery pertains generally to the field of therapeutic compounds. More specifically the present discovery pertains to certain di-isopropyl-phosphinoyl-alkanes as described herein, DIPA-1-5, DIPA-1-6, DIPA-1-7, DIPA-1-8, and DIPA-1-9, collectively referred to herein as “DIPA compounds”, that are useful, for example, in the treatment of disorders (e.g., diseases) including: sensory discomfort (e.g., caused by irritation, itch, or pain); a skin dysesthesia; dermatitis; ocular pain and discomfort; heat discomfort; heat stress; flushing and/or night sweats (vasomotor symptoms); post-operative hypothermia; post-anaesthetic shivering; fatigue; tiredness; depression; cognitive dysfunction; and to enhance cognitive function. The applicant has found that localized delivery of DIPA compounds to the upper eyelid and/or facial skin has an alerting and enhancement effect on behavior and can be used to give a cosmetic refreshing look, to mental alertness, to reduce fatigue, and to improve work output. The present discovery also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, for example, in therapy, in diagnosis of neuropathic pain, and in study of TRPM8 function.
本发现通常涉及治疗化合物领域。更具体地,本发现涉及如下所述的某些二异丙基磷酰基烷烃,即DIPA-1-5、DIPA-1-6、DIPA-1-7、DIPA-1-8和DIPA-1-9,以下统称为“DIPA化合物”,这些化合物在治疗包括但不限于感觉不适(例如由刺激、瘙痒或疼痛引起)、皮肤感觉异常、皮炎、眼部疼痛和不适、热感不适、热应激、潮红和/或盗汗(血管运动症状)、术后低体温、麻醉后颤抖、疲劳、疲倦、抑郁、认知功能障碍以及增强认知功能等疾病(例如疾病)的治疗中具有用途。申请人发现将DIPA化合物局部传递至上眼睑和/或面部皮肤对行为具有警觉和增强效果,并可用于给予一种化妆上的焕然一新的外观,提高精神警觉度,减轻疲劳,并提高工作产出。本发现还涉及包含此类化合物的药物组合物,以及此类化合物和组合物的用途,例如在治疗、神经病痛诊断和TRPM8功能研究中的应用。