CAS: 755038-02-9; (R)-4-((8-Cyclopentyl-7-Ethyl-5-Methyl-6-Oxo-5,6,7,8-Tetrahydropteridin-2-yl)Amino)-3-Methoxy-N-(1-Methylpiperidin-4-yl)Benzamide

上下游产品

CAS号41838-46-4 4-氨基-1-甲基哌啶 | CAS号755039-55-5 (7R)-2-氯-8-环戊基-... | CAS号876126-60-2 4-amino-3-metho... | CAS号755039-56-6 (R)-4-(8-cyclop... | CAS号755039-53-3 (2R)-2-[(2-氯-5-... | CAS号755039-54-4 (7R)-2-氯-8-环戊烷基... | CAS号755039-52-2 (2R)-2-(环戊氨基)-丁酸甲酯

4-氨基-1-甲基哌啶置于o-(Benzotriazol-1-yl)-N,N,N',N'-Tetramethyluronium Tetrafluoroborate,N,N-二异丙基乙胺体系中,用 二氯甲烷 作为反应溶剂,化学反应 3.0H,反应生成 4-[[(7R)-8-环戊基-7-乙基-5,6,7,8-四氢-5-甲基-6-氧代-2-喋啶基]氨基]-3-甲氧基-N-(1-甲基-4-哌啶基)苯甲酰胺
参考文献:Storage Stable Perfusion Solution For Dihydropteridinones
标题:Storage Stable Perfusion Solution For Dihydropteridinones
摘要:公开了含有一种一般式(i)的活性物质的储存稳定的水性不可注射或可注射溶液,其中组l,R1,R2,R3,R4和r5具有声明中给出的含义和说明书中的含义,以及足以溶解活性物质并起稳定剂作用的生理可接受酸或酸混合物的量,可选地与适用于肌肉注射的其他配方辅料一起,并根据本发明制备不可注射或可注射溶液的方法.

专利信息

专利号:US-10905769-B2
优先权日:2015-11-13
标 题:Peptide and peptide mimetic binding antagonists of polo-like kinase 1 polo box domain and methods of use
发明人：BURKE JR TERRENCE R; HYMEL DAVID T; TSUJI KOHEI
权利人:THE US SECRETARY DEPARTMENT OF HEALTH & HUMAN SERVICES
摘要:The description provides novel compounds that may serve as anticancer therapeutics. The compounds of the description bind to polo-like kinases through the polo-box domain. The peptide derivatives of the description have achieved improved efficacy in biochemical assays against Plk1. Exemplary compounds of the description include macrocyclic peptidomimetics with high affinity and selectivity for polo-like kinases, which may provide the basis for a new genre of anticancer therapeutics. Other exemplary compounds of the description include bi-valent compounds with that bind to polo-like kinases through both kinase domain and polo-box domain simultaneously by incorporating additional moieties that target Plk1 kinase domain, which significantly enhances affinitity relative and may provide the basis for a new genre of anticancer therapeutics. The description also provides methods of use, methods of preparation, compositions, and kits thereof. Further, the description provides a novel method of design and/or synthesis of phosphoryl-derived peptide derivatives useful as therapeutic agents.