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NOVEDOSOS DERIVADOS HETEROCICLICOS
专利权人:
NOVARTIS AG
发明人:
RADETICH, BRANKO,YU, BING,ZHU, YANYI
申请号:
PE0017142013
公开号:
PE02932014A1
申请日:
2012.01.30
申请国别(地区):
PE
年份:
2014
代理人:
摘要:
Purine derivatives relates to compounds of formula (i) where X is n or CH r1 is a compound of formula (i), (ii), among others R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15 R16 and R17 are each H or Methyl and is, or chr25 or cr26r27 where R25 is hydroxyl or alkoxyl (C1 - C3) R26, R27 are each H or Halogen.Preferred compounds are: 3 - (2,4 - dimorfolino - 7h pyrrolo [2,3-d] pyrimidine 6 - il) phenol 2,6-bis - ((S) - 3 - methyl - 4 - (IL) - 6 - (1h pyrrolo [2,3-b] pyridine - 4-yl) - 9h purine {2-fluoro-5 - [6 - ((S) - 3 - methyl - 4 - (IL) - 2 - (4 - il - 9h purin - il - 8}] - phenyl Methanol among others. It also relates to a Pharmaceutical composition.These compounds have Inhibitory activity of phosphatidylinositol 3-kinase (PI3K) and mTOR being useful in the treatment of cancer or a neurodegenerative disorder.SE REFIERE A COMPUESTOS DERIVADOS DE PURINA DE FORMULA (I) DONDE X ES N O CH R1 ES UN COMPUESTO DE FORMULA (i), (ii), ENTRE OTROS R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16 Y R17 SON CADA UNO H O METILO Y ES O, CHR25 O CR26R27, EN DONDE R25 ES HIDROXILO O ALCOXILO(C1-C3) R26 Y R27 SON CADA UNO H O HALOGENO. SON COMPUESTOS PREFERIDOS: 3-(2,4-DIMORFOLINO-7H-PIRROLO[2,3-d]PIRIMIDIN-6-IL)FENOL 2,6-BIS-((S)-3-METIL-MORFOLIN-4-IL)-8-(1H-PIRROLO[2,3-b]PIRIDINA-4-IL)-9H-PURINA {2-FLUORO-5-[6-((S)-3-METIL-MORFOLIN-4-IL)-2-MORFOLIN-4-IL-9H-PURIN-8-IL]-FENIL}-METANOL ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS TIENEN ACTIVIDAD INHIBITORIA DE LA FOSFATIDILINOSITOL-3-QUINASA (PI3K) Y mTOR SIENDO UTILES EN EL TRATAMIENTO DE CANCER O UN TRASTORNO NEURODEGENERATIVO
来源网站:
中国工程科技知识中心
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http://www.ckcest.cn/home/

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