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
    • 3. 发明授权
    • Substituted 1,4-benzodiazepines and uses thereof
    • 取代的1,4-苯并二氮杂及其用途
    • US07067512B2
    • 2006-06-27
    • US10292876
    • 2002-11-13
    • Tianbao LuLouis V Lafrance, IIIDaniel J ParksKaren L MilkiewiczRaul R CalvoMaxwell D CummingsAlexander J KimBruce L GrasbergerTheodore E Carver, Jr.
    • Tianbao LuLouis V Lafrance, IIIDaniel J ParksKaren L MilkiewiczRaul R CalvoMaxwell D CummingsAlexander J KimBruce L GrasbergerTheodore E Carver, Jr.
    • C07D243/12C07D243/18C07D243/24A61K31/55
    • C07D401/04C07D243/14C07D403/10C07D405/04C07D409/04
    • The present invention is directed to novel 1,4-benzodiazepines, pharmaceutical compositions thereof, and the use thereof as inhibitors of HDM2-p53 interactions. Compounds have Formula I: or a solvate, hydrate or pharmaceutically acceptable salt thereof; wherein: X and Y are independently —C(O)—, —CH2— or —C(S)—; R1, R2, R3, R4, R7, R8, Rb, Rc, Rd and M are defined herein; R5 is hydrogen, alkyl, cycloalkyl, optionally substituted aryl, optionally substituted heteroaryl, optionally substituted aralkyl, optionally substituted heteroaralkyl, carboxyalkyl, alkoxycarbonyl, alkoxycarbonylalkyl, aminocarbonyl, aminocarbonylalkyl, alkylaminocarbonyl or alkylaminocarbonylalkyl; R6 is cycloalkyl, aryl, heteroaryl, cycloalkylalkyl, aralkyl, heteroarylalkyl, or a saturated or partially unsaturated heterocycle, each of which is optionally substituted; R9 is cycloalkyl, aryl, heteroaryl, a saturated or partially unsaturated heterocycle, cycloalkyl(alkyl), aralkyl or heteroarylalkyl, each of which is optionally substituted; and R10 is —(CH2)n—CO2Rb, —(CH2)m—CO2M, —(CH2)i—OH or —(CH2)j—CONRcRd n is 0–8, m is 0–8, i is 1–8 and j is 0–8.
    • 本发明涉及新的1,4-苯二氮卓类药物,其药物组合物及其作为HDM2-p53相互作用抑制剂的用途。 化合物具有式I:或其溶剂合物,水合物或其药学上可接受的盐; 其中:X和Y独立地为-C(O) - , - CH 2 - 或-C(S) - ; R 1,R 2,R 3,R 4,R 7, R 8,R b,R c,R d和M在本文中定义; R 5是氢,烷基,环烷基,任选取代的芳基,任选取代的杂芳基,任选取代的芳烷基,任选取代的杂芳烷基,羧基烷基,烷氧基羰基,烷氧基羰基烷基,氨基羰基,氨基羰基烷基,烷基氨基羰基或烷基氨基羰基烷基; R 6是环烷基,芳基,杂芳基,环烷基烷基,芳烷基,杂芳基烷基或饱和或部分不饱和的杂环,其各自任选被取代; R 9是环烷基,芳基,杂芳基,饱和或部分不饱和的杂环,环烷基(烷基),芳烷基或杂芳基烷基,其各自任选被取代; 和R 10是 - (CH 2)n - - - - - - (CH 2)n - , - (CH 2)2 - , - M 2 - , - (CH 2) -OH或 - (CH 2 CH 2)n -CONR C n R n为0-8 ,m为0-8,i为1-8,j为0-8。