,;EFFECT: technical result is new activity of compounds of formula (I) or (II), which can be used in medicine for treating inflammatory conditions, immunological conditions, neurodegenerative diseases.;50 cl, 1 tbl, 20 ex"/> MTOR KINASE INHIBITORS FOR ONCOLOGIC INDICATIONS AND DISEASES ASSOCIATED WITH MTOR/PI3K/AKT BY METABOLISM
首页> 外国专利> MTOR KINASE INHIBITORS FOR ONCOLOGIC INDICATIONS AND DISEASES ASSOCIATED WITH MTOR/PI3K/AKT BY METABOLISM

MTOR KINASE INHIBITORS FOR ONCOLOGIC INDICATIONS AND DISEASES ASSOCIATED WITH MTOR/PI3K/AKT BY METABOLISM

机译:MTOR激酶抑制剂与代谢引起的MTOR / PI3K / AKT相关的肿瘤迹象和疾病

摘要

FIELD: chemistry.;SUBSTANCE: invention relates to use of compounds of formula (I) or (II), where R1 is a substituted phenyl, substituted or unsubstituted heterocyclyl which is an aromatic cycloalkyl containing 6 to 10 atoms in a ring and in which one to two carbon atoms in the cycle are independently substituted on N, where said substitutes are selected from C1-8alkyl, triazolyl, halogen, aminocarbonyl, cyano or hydroxyalkyl; R2 is H, substituted or unsubstituted C1-8alkyl substituted with C3-6cycloalkyl, unsubstituted heterocyclyl, which is a non-aromatic cycloalkyl containing from 5 to 6 atoms in a cycle and in which one to two carbon atoms in the cycle are independently substituted with N or O; unsubstituted heterocyclylalkyl, where heterocyclyl is a non-aromatic cycloalkyl containing 5 to 6 atoms in a ring and in which one to two carbon atoms in the cycle are independently substituted with N and O; substituted or unsubstituted phenylalkyl or substituted or unsubstituted C3-6cycloalkylalkyl, where said substitutes are selected from C1-4alkyl, CF3, OR and NR2, where R is H or C1-4alkyl; R3 and R4, each independently represent H, unsubstituted C1-8alkyl or R3 and R4 together with atom, to which they are attached form C3-6cycloalkyl; or R2 and one of R3 and R4 together with atoms to which they are bonded, form a substituted or unsubstituted heterocyclyl containing from 5 to 6 ring atoms and which may contain an additional heteroatom selected from O; where the substitutes are selected from -C(O)CH2OCN3, -CH2CH2OCN3, OCH3 or CH3; provided that the compound is not 6-(4-hydroxyphenyl)-4-(3-methoxybenzyl)-3,4-dihydropyrazino[2,3-b]pyrazine-2(1H)-one, 6-(4-(1H-1,2,4-triazol-5-yl)phenyl)-3-(cyclohexylmethyl)-3,4-dihydropyrazino[2,3-b]pyrazine-2(1H)-one or (R)-6-(4-(1H-1,2,4-triazol-5-yl)phenyl)-3-(cyclohexylmethyl)-3,4-dihydropyrazino[2,3-b]pyrazin-2(1H)-one, to obtain a pharmaceutical composition for treating conditions mediated by mTOR kinase, selected from inflammatory conditions, neurodegenerative diseases and cardiovascular conditions.; ,;EFFECT: technical result is new activity of compounds of formula (I) or (II), which can be used in medicine for treating inflammatory conditions, immunological conditions, neurodegenerative diseases.;50 cl, 1 tbl, 20 ex
机译:发明领域本发明涉及式(I)或(II)的化合物的用途,其中R Sup 1是取代的苯基,取代的或未取代的杂环基,其为含有6至3的芳族环烷基。环中有10个原子,且循环中有1至2个碳原子独立地在N上取代,其中所述取代基选自C 1-8 烷基,三唑基,卤素,氨基羰基,氰基或羟烷基; R 2 是H,被C 3-6 环烷基取代或未被取代的C 1-8 烷基,未被取代的杂环基,在一个环中含有5至6个原子并且该环中的1-2个碳原子独立地被N或O取代的芳族环烷基;未取代的杂环基烷基,其中杂环基是在环中包含5至6个原子并且其中环中的1-2个碳原子独立地被N和O取代的非芳族环烷基;取代或未取代的苯基烷基或取代或未取代的C 3-6 环烷基烷基,其中所述取代基选自C 1-4 烷基,CF 3 , OR和NR 2 ,其中R为H或C 1-4 烷基; R 3 和R 4 各自独立地代表H,未取代的C 1-8 烷基或R 3 和R 4 与原子一起形成C 3-6 环烷基;或R 2 和R 3 和R 4 之一与它们所键合的原子一起形成取代基或未取代的杂环基,其含有5至6个环原子,并且可包含选自O的额外杂原子;从-C(O)CH 2 OCN 3 ,-CH 2 CH 2 OCN中选择替代物的地方 3 ,OCH 3 或CH 3 ;前提是该化合物不是6-(4-羟基苯基)-4-(3-甲氧基苄基)-3,4-二氢吡嗪并[2,3-b]吡嗪-2(1H)-一,6-(4-(1H) -1,2,4-三唑-5-基)苯基)-3-(环己基甲基)-3,4-二氢吡嗪并[2,3-b]吡嗪-2(1H)-one或(R)-6-( 4-(1H-1,2,4-三唑-5-基)苯基)-3-(环己基甲基)-3,4-二氢吡嗪并[2,3-b]吡嗪-2(1H)-一用于治疗由mTOR激酶介导的疾病的药物组合物,所述mTOR激酶选自炎性疾病,神经退行性疾病和心血管疾病。

著录项

相似文献

  • 专利
  • 外文文献
  • 中文文献
获取专利

客服邮箱:kefu@zhangqiaokeyan.com

京公网安备:11010802029741号 ICP备案号:京ICP备15016152号-6 六维联合信息科技 (北京) 有限公司©版权所有
  • 客服微信

  • 服务号