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公开(公告)号：EP2001486A2
公开(公告)日：2008-12-17
申请号：EP07758756.6
申请日：2007-03-16
IPC分类号： A61K31/663
CPC分类号： C07F9/4037 , C07F9/3843 , C07F9/3856 , C07F9/3865 , C07F9/3869 , C07F9/3873 , C07F9/4028 , C07F9/404 , C07F9/4046 , C07F9/5414 , C07F9/5728 , C07F9/581 , C07F9/65061 , C07F9/655345 , C07F9/655363 , C07F9/723
摘要： The invention provides, inter alia, novel bisphosphonate compounds and methods of making and using. In embodiments, the invention provides compounds and methods in connection with research and therapeutic applications, e.g., for tumor cell growth inhibition, activation of gammadelta T cells, inhibition of farnesyldiphosphate (FPPS) and/or undecaprenyldiphosphate synthase enzymes, bone resorption diseases, cancer, immune disorders, immunotherapy, and infectious diseases. In regards to certain embodiments, a surprising advance has been the recognition that certain structural features can significantly enhance the activity of the compounds. For example, the presence of particular cationic species e.g., phosphonium, sulfonium, and arsonium moieties can contribute to desirable functional activity when positioned near a bisphosphonate moiety. In other embodiments of non-nitrogen containing bisphosphonates, terphenyl and benzyl bisphosphonate compounds and methods are provided. Further variations are also provided.
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2.发明公开BISPHOSPHONATE COMPOUNDS AND METHODS FOR BONE RESORPTION DISEASES, CANCER, BONE PAIN, IMMUNE DISORDERS, AND INFECTIOUS DISEASES 有权双膦酸酯和骨收缩疾病，癌症，骨痛，免疫系统疾病与感染性疾病程序
公开(公告)号：EP1802641A2
公开(公告)日：2007-07-04
申请号：EP05824408.8
申请日：2005-10-07
CPC分类号： C07F9/3873 , C07F9/581 , C07F9/582 , C07F9/60 , C07F9/62 , C07F9/65061 , C07F9/65583
摘要： Bishosphonate compounds and related methods of making and using are disclosed, including pyridinium-1-yl, quinolinium-1-yl, and related compounds. The activity of compounds is disclosed in the context of functional assays such as Leishmania major farnesyl diphosphate synthase (FPPS) inhibition, Dictyostelium discoideum growth inhibition, human gamma delta T cell activation, and bone resorption. The applicability of bisphosphonate compounds in the context of parasitic infections, for example against trypanosomes, is disclosed. Further potential applications of the invention are disclosed regarding the treatment of one or more conditions such as bone resorption disorders, cancer, bone pain, infectious diseases, and in immunotherapy.
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3.发明授权BISPHOSPHONATE COMPOUNDS AND METHODS FOR BONE RESORPTION DISEASES, CANCER, BONE PAIN, IMMUNE DISORDERS, AND INFECTIOUS DISEASES 有权双膦酸酯和骨收缩疾病，癌症，骨痛，免疫系统疾病与感染性疾病程序
公开(公告)号：EP1802641B8
公开(公告)日：2012-03-07
申请号：EP05824408.8
申请日：2005-10-07
CPC分类号： C07F9/3873 , C07F9/581 , C07F9/582 , C07F9/60 , C07F9/62 , C07F9/65061 , C07F9/65583
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4.发明公开BISPHOSPHONATE COMPOUNDS AND METHODS WITH ENHANCED POTENCY FOR MULTIPLE TARGETS INCLUDING FPPS, GGPPS, AND DPPS 审中-公开双膦酸盐化合物及其具有多重目标，包括FPPS，DPPS和GGPPS增加的效力方法
公开(公告)号：EP2203460A1
公开(公告)日：2010-07-07
申请号：EP08780519.8
申请日：2008-04-11
发明人： OLDFIELD, Eric , ZHANG, Yonghui , YIN, Fenglin
IPC分类号： C07F9/576 , C07F9/6503
CPC分类号： C07F9/3878 , C07F9/3839 , C07F9/3865 , C07F9/3873 , C07F9/5532 , C07F9/581 , C07F9/582 , C07F9/591 , C07F9/65061 , C07F9/65062 , C07F9/6539 , C07F9/65517 , C07F9/655345 , C07F9/65583 , C07F9/6561 , C07F9/723 , C12Q1/48 , G01N2333/91171
摘要： 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.
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5.发明授权BISPHOSPHONATE COMPOUNDS AND METHODS FOR BONE RESORPTION DISEASES, CANCER, BONE PAIN, IMMUNE DISORDERS, AND INFECTIOUS DISEASES 有权双膦酸酯和骨收缩疾病，癌症，骨痛，免疫系统疾病与感染性疾病程序
公开(公告)号：EP1802641B1
公开(公告)日：2011-08-10
申请号：EP05824408.8
申请日：2005-10-07
CPC分类号： C07F9/3873 , C07F9/581 , C07F9/582 , C07F9/60 , C07F9/62 , C07F9/65061 , C07F9/65583
摘要： Bishosphonate compounds and related methods of making and using are disclosed, including pyridinium-1-yl, quinolinium-1-yl, and related compounds. The activity of compounds is disclosed in the context of functional assays such as Leishmania major farnesyl diphosphate synthase (FPPS) inhibition, Dictyostelium discoideum growth inhibition, human gamma delta T cell activation, and bone resorption. The applicability of bisphosphonate compounds in the context of parasitic infections, for example against trypanosomes, is disclosed. Further potential applications of the invention are disclosed regarding the treatment of one or more conditions such as bone resorption disorders, cancer, bone pain, infectious diseases, and in immunotherapy.
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