专利号:US-9598418-B2 优先权日:2012-12-31 标 题:Substituted phthalazin-1 (2H)-one derivatives as selective inhibitors of poly (ADP-ribose) polymerase-1 发明人:SRIVASTAVA BRIJESH K; DESAI RANJIT C; PATEL PANKAJ R 权利人:CADILA HEALTHCARE LTD 摘要:The present invention relates to novel compounds of general formula (I), their stereoisomers, regioisomers, tautomeric forms and novel intermediates involved in their synthesis, their pharmaceutically acceptable salts, pharmaceutically acceptable solvates and pharmaceutical compositions containing them. The present invention also relates to a process of preparing novel compounds of general formula (I), their stereoisomers, regioisomers, their tautomeric forms, their pharmaceutically acceptable salts, pharmaceutically acceptable solvates, pharmaceutical compositions containing them, and novel intermediates involved in their synthesis.
专利号:US-8871765-B2 优先权日:2010-07-27 标 题 :Substituted 4-(4-fluoro-3-(piperazine-1-carbonyl)benzyl)phthalazin-1(2H)-one derivatives as poly (ADP-ribose) polymerase-1 inhibitors 发明人:SHRIVASTAVA BRIJESH KUMAR 权利人:SHRIVASTAVA BRIJESH KUMAR; CADILA HEALTHCARE LTD 摘要:Disclosed are compounds of general formula (I), their stereoisomers, regioisomers, tautomeric forms and novel intermediates involved in their synthesis, their pharmaceutically acceptable salts. These compounds are suitable as Poly(ADP-ribose)polymerase-1 inhibitors (PARP-1 inhibitors).
1: Koosha F, Neshasteh-Riz A, Takavar A, Eyvazzadeh N, Mazaheri Z, Eynali S, Mousavi M. The combination of A-966492 and Topotecan for effective radiosensitization on glioblastoma spheroids. Biochem Biophys Res Commun. 2017 Sep 30;491(4):1092-1097. doi: 10.1016/j.bbrc.2017.08.018. Epub 2017 Aug 7. 177:109904. doi: 10.1016/j.apradiso.2021.109904. Epub 2021 Aug 24. 53(8):3142-53. doi: 10.1021/jm901775y. 12(1):736. doi: 10.1038/s41467-021-20998-8.
合成参考文献
参考文献:10.1021/jm901775y 摘要:Penning TD, Zhu GD, Gong J, Thomas S, Gandhi VB, Liu X, Shi Y, Klinghofer V, Johnson EF, Park CH, Fry EH, Donawho CK, Frost DJ, Buchanan FG, Bukofzer GT, Rodriguez LE, Bontcheva-Diaz V, Bouska JJ, Osterling DJ, Olson AM, Marsh KC, Luo Y, Giranda VL. Optimization of phenyl-substituted benzimidazole carboxamide poly(ADP-ribose) polymerase inhibitors: identification of (S)-2-(2-fluoro-4-(pyrrolidin-2-yl)phenyl)-1H-benzimidazole-4-carboxamide (A-966492), a highly potent and efficacious inhibitor. J Med Chem. 2010 Apr 22;53(8):3142–53. doi: 10.1021/jm901775y.