CAS: 718630-59-2; N-(6,6-Dimethyl-5-(1-Methylpiperidine-4-Carbonyl)-1,4,5,6-Tetrahydropyrrolo[3,4-C]Pyrazol-3-yl)-3-Methylbutanamide

📜在 甲醇,三乙胺体系中,化学反应生成 3-甲基-N-[1,4,5,6-四氢-6,6-二甲基-5-[(1-甲基-4-哌啶基)甲酰基]吡咯并[3,4-C]吡唑-3-基]丁酰胺
参考文献:Optimization Of 6,6-Dimethyl Pyrrolo[3,4-C]Pyrazoles: Identification Of Pha-793887,A Potent Cdk Inhibitor Suitable For Intravenous Dosing
标题:Optimization Of 6,6-Dimethyl Pyrrolo[3,4-C]Pyrazoles: Identification Of Pha-793887,A Potent Cdk Inhibitor Suitable For Intravenous Dosing
摘要:We Have Recently Reported Cdk Inhibitors Based On The 6-Substituted Pyrrolo[3,4-C]Pyrazole Core Structure. Improvement Of Inhibitory Potency Against Multiple Cdks,Antiproliferative Activity Against Cancer Cell Lines And Optimization Of The Physico-Chemical Properties Led To The Identification Of Highly Potent Compounds. Compound 31 (Pha-793887) Showed Good Efficacy In The Human Ovarian A2780,Colon Hct-116 And Pancreatic Bx-Pc3 Carcinoma Xenograft Models And Was Well Tolerated Upon Daily Treatments By Iv Administration. It Was Identified As A Drug Candidate For Clinical Evaluation In Patients With Solid Tumors.
DOI:10.1016/j.Bmc.2010.01.042

专利信息

专利号:US-11285169-B2
优先权日:2013-03-13
标题 :Methods for modulating chemotherapeutic cytotoxicity
发明人：ROBERTS DAVID D; SOTO PANTOJA DAVID R
权利人:US HEALTH
摘要:Methods of reducing cytotoxicity of a chemotherapeutic agent to non-cancer cells by administering to a subject with cancer an effective amount of an agent that inhibits CD47 signaling and a DNA damaging agent, such as an anthracycline, topoisomerase inhibitor, or nucleotide synthesis inhibitor, are provided. Example disclosed methods reduce cardiotoxicity. In one example, the methods include administering to a subject with cancer an effective amount of a CD47 antisense morpholino oligonucleotide and an anthracycline such as doxorubicin. Methods of increasing cytotoxicity of a chemotherapeutic agent in cancer cells by administering to a subject with a tumor an effective amount of an agent that inhibits CD47 signaling and a DNA damaging agent such as an anthracycline, topoisomerase inhibitor, or nucleotide synthesis inhibitor, are also provided. In some embodiments, the inhibitor of CD47 signaling is administered to the subject before, during, or after the administration of the DNA damaging agent.