首页> 外国专利> diasendatud - 6.9 - trans - 2 - (4-aminocyclohexyl) amino puriinid, containing them and their use in pharmaceutical kompositsioonid

diasendatud - 6.9 - trans - 2 - (4-aminocyclohexyl) amino puriinid, containing them and their use in pharmaceutical kompositsioonid

机译:diasendatud-6.9-反式-[2-(4-氨基环己基)氨基]嘌呤类化合物,及其在药物中的用途

摘要

The present invention provides novel compounds of the formula (I)whereinR is selected from the group consisting of R2, R2NH-, or R3R4N-R5- whereinR2 is selected from the group consisting of C9-C12 alkyl,Z is selected from the group consisting of phenyl, heterocycle, cycloalkyl, and naphthanlene; and M is selected from the group consisting of hydrogen, C1-C4 alkyl, andwherein each C9-C12 alkyl or Z is optionally substituted with 1 to 3 substituents, which may be the same or different, and which are selected from the group consisting of D, E,wherein each D is independently selected from the group consisting of trifluoromethyl, trifluoromethoxy, and C1-C4 alkoxy; each E is independently selected from the group consisting of Hal, OH, and C1-C8 alkyl;R3 and R4 are selected from the group consisting of hydrogen, C1-C4 alkyl and (CH2)y-phenyl, wherein y is an integer 0-8, with the proviso that R3 and R4 not both be hydrogen;R5 is C1-C8 alkylene; andR1 is selected from the group consisting of cyclopentyl, cyclopentenyl and isopropyl,and the pharmaceutically acceptable salts, optical isomers, and hydrates thereof,with the proviso that when R2 is the groupwherein n is 1 or greater; R1 is isopropyl or cyclopentyl; R6 is hydrogen, C1-C4 alkyl, or (CH2)m-phenyl; and Z is phenyl, heterocycle, or cycloalkyl, that Z is substituted with 1 to 3 substituents, which may be the same or different, and which are selected from the group consisting ofIn addition, the present invention provides a method of inhibiting cyclin dependent kinases, particularly cdk-2.The present invention also provides a method of preventing apoptosis in neuronal cells and a method of inhibiting the development of neoplasms.
机译:本发明提供式(I)的新型化合物,其中R 2选自R 2,R 2 NH-或R 3 R 4 N-R 5-,其中R 2选自C 9 -C 12烷基,Z选自苯基,杂环,环烷基和萘烯; M选自氢,C 1 -C 4烷基,其中每个C 9 -C 12烷基或Z任选地被1-3个相同或不同的取代基取代,所述取代基选自下组: D,E,其中每个D独立地选自三氟甲基,三氟甲氧基和C1-C4烷氧基;每个E独立地选自Hal,OH和C1-C8烷基; R3和R4选自氢,C1-C4烷基和(CH2)y-苯基,其中y是整数0 -8,条件是R3和R4不都是氢; R5是C1-C8亚烷基; R1选自环戊基,环戊烯基和异丙基,以及它们的药学上可接受的盐,旋光异构体和水合物,条件是当R2是其中n为1或更大的基团时; R1是异丙基或环戊基; R6是氢,C1-C4烷基或(CH2)间苯基; Z为苯基,杂环或环烷基,Z被1至3个取代基取代,该取代基可以相同或不同,并且选自由以下组成的组:此外,本发明提供了抑制细胞周期蛋白依赖性激酶的方法本发明还提供了防止神经元细胞凋亡的方法和抑制肿瘤发展的方法。

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