Peripheral localized GABA positive allosteric modulators for the treatment of irritable bowel syndrome and other diseases in the peripheral nervous system
A novel allosteric modulator of GABA-A receptor that selectively targets the peripheral nervous system and organs of the body, and provides compounds and compositions that do not pass through the blood-brain barrier.Compound 1 or 2 compound. The compounds and compositions of the present invention may also be, for example, visceral pain, bowel movement, irritable bowel syndrome, functional abdominal pain, functional idiopathic diarrhea, inflammatory bowel disease, drug induced pain, bile salt absorption deficiency, lactase or other carbohydrate intolerance, as well as diseases mediated by GABA-A neuronal activity Is useful for treatment of disorders.Diagram【課題】身体の末梢神経系および器官を選択的に標的とするGABA-A受容体のポジティブアロステリックモジュレーターであって、血液脳関門を通過しない化合物および組成物の提供。【解決手段】式1または2の化合物。本発明の化合物および組成物は、例えば、内臓痛、腸運動、過敏性腸症候群、機能性腹痛、機能性特発性下痢、炎症性腸疾患、薬物誘導性疼痛、胆汁酸塩吸収不良、ラクターゼまたは他の炭水化物不耐症などの、GABA-Aニューロン活性により媒介される疾患または障害の治療に有用である。【選択図】図2