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    • 4. 发明公开
    • COLCHICINE DERIVATIVES
    • 醋酸衍生物
    • EP3207929A2
    • 2017-08-23
    • EP16198280.6
    • 2004-04-14
    • California Pacific Medical CenterCatholic Healthcare West, d.b.a. St. Mary's Medical Center
    • YANG, Li-Xi
    • A61K31/4439A61K31/433A61K31/403A61K31/155A61K31/175C07C323/41C07C323/42C07C323/60C07H5/06C07D295/15
    • C07C323/41C07C323/42C07C323/60C07C2603/18C07C2603/24C07C2603/34C07D295/15C07H5/06
    • Certain N-deacetylcolchicine and N-deacetylthiocolchine derivatives are described wherein the 7-N position on the B ring is substituted with the group - C(O)-(CHR 4 ) m -AR, wherein m is an integer of 0-10, A is S, O, N or a covalent bond; R 1 is substituted phenyl or substituted benzoyl; optionally substituted cycloalkyl of 3-7 carbons; optionally substituted naphtyl; an optionally substituted imide ring; an optionally substituted 5 or 6 member heterocycle with at least one N, S, or O in the ring; or an optionally substituted fused heterocyclic or fused carboxyclic ring system; R 2 (at the 2-position of the A ring) is methoxy, hydroxy, or methylenedioxy when taken together with R 3 ; R 3 (at the 3-position of the A ring) is methoxy, hydroxy, a monosaccharide radical, or is methylenedioxy when taken together with R 2 ; and R 4 is H or is H or methyl when m is 1. Also dimers of such compounds are disclosed. When combined with suitable pharmaceutical excipients, these compounds are useful for treating various types of cancer.
    • 描述了某些N-去乙酰基秋水仙碱和N-脱乙酰硫代秋水仙碱衍生物,其中B环上的7-N位被基团-C(O) - (CHR4)m-AR取代,其中m是0-10的整数,A 是S,O,N或共价键; R1是取代的苯基或取代的苯甲酰基; 任选取代的3-7个碳的环烷基; 任选取代的萘基; 任选取代的酰亚胺环; 在环中具有至少一个N,S或O的任选取代的5或6元杂环; 或任选取代的稠合杂环或稠合羧基环体系; R2(在A环的2-位)与R3结合时为甲氧基,羟基或亚甲二氧基; R3(在A环的3-位)是甲氧基,羟基,单糖基团,或当与R2一起时是亚甲二氧基; 当m是1时,R4是H或是H或甲基。还公开了这些化合物的二聚体。 当与合适的药物赋形剂组合时,这些化合物可用于治疗各种类型的癌症。