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6, 9-disubstituted 2-trans-(4-aminocyclohexyl)amino purines

机译:6,9-二取代的2-反-(4-氨基环己基)氨基嘌呤

摘要

The present invention provides novel compounds of the formula (I) embedded image;wherein;R is selected from the group consisting of R2, R2NH, or R3R4NR5- wherein;R2 is selected from the group consisting of C9-C12 alkyl, embedded image;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, and;wherein 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, embedded image;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; embedded image;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; and;R1 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 group embedded image;wherein 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 of embedded image;In 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:本发明提供了式(I)的新型化合物。<化学名称=” CHEM-US-00001“> <图像alt =”嵌入式图像“ file =” US06479487-20021112-C00001.GIF“ he =” 74.9007“ imgContent = “未定义” imgFormat =“ GIF” wi =“ 187.4502” /> ;其中; R选自R2,R2NH或R3R4NR5-,其中; R2被选择从C 9 -C 12 烷基组成的组中,<化学id =“ CHEM-US-00002”> “嵌入式图像” ; Z选自苯基,杂环,环烷基和萘烷; M选自氢,C 1 -C 4 烷基,和;其中每个C 9 -C 12 烷基或Z任选地被1-3个取代基取代,这些取代基可以相同或不同,并且选自D,E, “嵌入式图像” < ;其中每个D独立地选自三氟甲基,三氟甲氧基和C 1 -C 4 烷氧基;每个E独立地选自Hal,OH和C 1 -C 8 烷基; <图像alt =“嵌入式图像” file =“ US06479487-20021112-C00004.GIF” he =“ 39.123” imgContent =“ undefined” imgFormat =“ GIF” wi =“ 49.4424 “ /> ; R3和R4选自氢,C 1 -C 4 烷基和( CH 2 y -苯基,其中y是0-8的整数,条件是R3和R4都不都是氢;; R5是C 1 -C 8 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为基团时 <图像alt =”嵌入式图像“ file =” US06479487-20021112-C00005.GIF“ he =” 37.1952“ imgContent =” undefined“ imgFormat =” GIF“ wi =” 38.41425“ /> ;其中n为1或更大; R1是异丙基或环戊基; R6是氢,C 1 -C 4 烷基或(CH 2 m -苯基;并且Z为苯基,杂环或环烷基,其中Z被1-3个取代基取代,所述取代基可以相同或不同,并且选自 <图片alt =“嵌入的图片”文件=“ US06479487-20021112-C00006.GIF” he =“ 113.0598” imgContent =“未定义” imgFormat =“ GIF” wi =“ 168.99435” />

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