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    • 8. 发明专利
    • Antitumoral analog
    • 抗肿瘤模拟
    • JP2011026331A
    • 2011-02-10
    • JP2010209928
    • 2010-09-17
    • Pharma Mar Saファルマ・マール・ソシエダード・アノニマ
    • MARTINEZ VALENTINGALLEGO PILARCUEVAS CARMENMUNT SIMONMANZANARES IGNACIO
    • C07D515/22A61K31/4995A61P35/00
    • C07D515/22
    • PROBLEM TO BE SOLVED: To provide new compounds having most suitable characteristics of cytotoxicity and selectivity to tumor, decreased in systemic toxicity and improved in pharmacokinetic properties. SOLUTION: There are provided derivatives of ecteinascidin 736 of general formula I; [wherein, R 1 , R 2 , R 3 , R 4 and R 5 are each independently selected from the group consisting of H, OH, OR', SH, SR', SOR', SO 2 R', C(=O)R', C(=O)OR', NO 2 , NH 2 , NHR', N(R') 2 , NHC(O)R', CN, halogen, =O and the like; X is independently selected from OR', CN, (=O), or H; each R' is independently selected from the group consisting of H, OH, NO 2 , NH 2 , SH, CN, halogen, =O, C(=O)H, C(=O)CH 3 , CO 2 H and the like; m is 0, 1 or 2; and n is 0, 1, 2, 3 or 4]. COPYRIGHT: (C)2011,JPO&INPIT
    • 要解决的问题:提供具有最适合肿瘤细胞毒性和选择性特征的新化合物,降低全身毒性,提高药代动力学性质。 解决方案:提供通式I的星虫素抗生素736的衍生物; [其中,R SB 1,R SB 2,R SB 3,R SB 4和R SB 5, SB>各自独立地选自H,OH,OR',SH,SR',SOR',SO 2,R',C(= O)R',C(= O )OR',NO 2 ,NH 2,NHR',N(R')2 SBB,NHC(O)R' 卤素,= O等; X独立地选自OR',CN,(= O)或H; 每个R'独立地选自H,OH,NO,SO 2,SO 2,SO,CH,CN,卤素,= O,C(= O)H ,C(= O)CH 3,SO 2,H 2等; m为0,1或2; 和n为0,1,2,3或4]。 版权所有(C)2011,JPO&INPIT