A compound comprising a monovalent active site mTOR inhibitor covalently linked to a monovalent rapamycin or a monovalent rapamycin analog. SOLUTION: The following compounds and the like. Compound as a therapeutic agent for cancer, autoimmune disease, inflammatory disease, metabolic disease, neurodegenerative disease, fungal infection, transplant rejection, aging, stenosis, neointimal hyperplasia, cardiovascular disease or polycystic disease Use of. [Selection diagram] Fig. 11【課題】一価のラパマイシンまたは一価のラパマイシン類似体に共有結合した一価の活性部位ｍＴＯＲ阻害剤を含む、化合物の提供。【解決手段】下記化合物など。癌、自己免疫疾患、炎症性疾患、代謝疾患、神経変性疾患、真菌感染症、移植拒絶反応、加齢、狭窄症、新生内膜増殖、心血管疾患または多発生嚢胞疾患の治療薬としての化合物の使用。【選択図】図１１
