发明名称 Compositions including triciribine and bortezomib and derivatives thereof and methods of use thereof
摘要 This application relates to combination therapies including triciribine and related compounds and bortezomib and derivatives thereof analogs and compositions with reduced toxicity for the treatment and prevention of tumors, cancer, and other disorders associated with abnormal cell proliferation.
申请公布号 US9486492(B2) 申请公布日期 2016.11.08
申请号 US201514886882 申请日期 2015.10.19
申请人 University of South Florida 发明人 Cheng Jin Q.;Sebti Said M.
分类号 A61K31/70;A61K31/7052;A61K38/05;A61K31/7076;A61K31/69;A61K31/7064 主分类号 A61K31/70
代理机构 Fanelli Haag PLLC 代理人 Fanelli Haag PLLC
主权项 1. A method of treating a tumor or cancer that overexpresses AKT in a mammal comprising administering to the mammal an effective amount of a composition comprising: (i) a compound of formula I-IV: wherein each R2′, R3′ and R5′ are independently hydrogen, optionally substituted phosphate or phosphonate; acyl; alky; amide, sulfonate ester including alkyl or arylalkyl; sulfonyl, methanesulfonyl; benzylsulfonyl; optionally substituted arylsulfonyl; a lipid, a phospholipid; an amino acid; a carbohydrate; a peptide; or cholesterol; or other pharmaceutically acceptable leaving group that, in vivo, provides a compound wherein R2′, R3′ and R5′ is independently H or mono-, di- or tri-phosphate; wherein Rx and Ry are independently hydrogen, optionally substituted phosphate; acyl; amide, alkyl; aromatic, polyoxyalkylene such as polyethyleneglycol, optionally substituted arylsulfonyl; a lipid, including a phospholipid; an amino acid; a carbohydrate; a peptide; or cholesterol; or other pharmaceutically acceptable leaving group; R1 and R2 each are independently H, optionally substituted straight chained, branched or cyclic alkyl, alkenyl, or alkynyl, CO-alkyl, CO-alkenyl, CO-alkynyl, CO-aryl or heteroaryl, CO-alkoxyalkyl, CO-aryloxyalkyl, CO-substituted aryl, sulfonyl, alkylsulfonyl, arylsulfonyl, aralkylsulfonyl; wherein the compound of formula I-IV is administered to said mammal in an amount of at least 10 mg/m2; (ii) a compound of formula V:wherein R1, R2, R3, R4, and R5 each are independently H, optionally halogenated, substituted straight chained, branched or cyclic alkyl (including lower alkyl), alkoxyl, alkenyl, or alkynyl, aryl, CO-alkyl, CO-alkenyl, CO-alkynyl, CO-aryl or heteroaryl, CO-alkoxyalkyl, CO-aryloxyalkyl, CO-substituted aryl, sulfonyl, alkylsulfonyl, arylsulfonyl, aralkylsulfonyl.
地址 Tampa FL US