会员体验
专利管家(专利管理)
工作空间(专利管理)
风险监控(情报监控)
数据分析(专利分析)
侵权分析(诉讼无效)
联系我们
交流群
官方交流:
QQ群: 891211   
微信请扫码    >>>
现在联系顾问~
热词
    • 4. 发明申请
    • BISPHOSPHONATE COMPOUNDS AND METHODS WITH ENHANCED POTENCY FOR MULTIPLE TARGETS INCLUDING FPPS, GGPPS, AND DPPS
    • 双膦酸盐化合物和具有增强靶点的方法,包括FPPS,GGPPS和DPPS
    • WO2008128056A1
    • 2008-10-23
    • PCT/US2008/060051
    • 2008-04-11
    • THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOISOLDFIELD, EricZHANG, Yonghui
    • OLDFIELD, EricZHANG, Yonghui
    • C07F9/576C07F9/6503
    • C07F9/3865C07F9/386C07F9/3873C07F9/5414C07F9/581C07F9/587C07F9/65061C07F9/65517C07F9/655345C07F9/65583C07F9/6561C07F9/723G01N33/5011
    • The disclosure provides, inter alia, novel bisphosphonate compounds and methods of making and using such compounds. In certain embodiments, compounds of the invention include bisphosphonates that are capable of selectively inhibiting one or more of farnesyl diphosphate synthase (FPPS), geranylgeranyl diphosphate synthase (GGPPS), and decaprenyl pyrophosphate synthase (DPPS). In preferred embodiments, compounds of the invention are capable of selectively inhibiting two or more of FPPS, GGPPS, and DPPS. In embodiments, compounds and methods of the invention demonstrate superior activity levels, such as in the anti-cancer context, immunostimulation context, and other contexts, which in several cases exceed the activity levels of previous generation bisphosphonate drugs by orders of magnitude. In embodiments, the invention provides compounds and methods in connection with research and therapeutic applications, e.g., for tumor or cancer cell growth inhibition, activation of gammadelta T cells, inhibition of certain enzymes related to the mevalonate metabolic pathway, bone resorption diseases, cancer, immune disorders, immunotherapy, and infectious diseases.
    • 本公开尤其提供了新的双膦酸盐化合物以及制备和使用这些化合物的方法。 在某些实施方案中,本发明的化合物包括能够选择性抑制法呢基二磷酸合成酶(FPPS),香叶基香叶基二磷酸合成酶(GGPPS)和癸酰焦磷酸合酶(DPPS)中的一种或多种的双膦酸盐。 在优选的实施方案中,本发明的化合物能够选择性地抑制FPPS,GGPPS和DPPS中的两种或更多种。 在实施方案中,本发明的化合物和方法表现出优异的活性水平,例如在抗癌情境,免疫刺激背景和其他情况下,其在若干情况下超过前一代二膦酸药物的活性水平达数量级。 在实施方案中,本发明提供了与研究和治疗应用相关的化合物和方法,例如用于肿瘤或癌细胞生长抑制,Gammadelta T细胞的活化,与甲羟戊酸代谢途径相关的某些酶的抑制,骨吸收疾病,癌症, 免疫疾病,免疫治疗和传染病。