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    • 7. 发明授权
    • Pyrimidin-4-yl-3, 4-dihydro-2H-pyrrolo [1,2A] pyrazin-1-one compounds
    • 嘧啶-4-基-3,4-二氢-2H-吡咯并[1,2A]吡嗪-1-酮化合物
    • US08404692B2
    • 2013-03-26
    • US12083534
    • 2006-10-09
    • Stuart JonesRobert WestwoodMark ThomasJanice McLachlanKenneth DuncanFred ScaerouDaniella I. Zheleva
    • Stuart JonesRobert WestwoodMark ThomasJanice McLachlanKenneth DuncanFred ScaerouDaniella I. Zheleva
    • A61K31/4965
    • C07D487/04
    • The present invention relates to compounds of formula (I), or pharmaceutically acceptable salts thereof, wherein Z is NR11, NHCO, NHSO2, NHCH2, CH2, CH2CH2, or CH═CH; X is a hydrocarbyl group optionally substituted by one or more R12 groups; R10 and R11 are each independently II or alkyl; R1-R4 are each independently II or (CII2)mR12, where m is O, 1, 2, or 3; each R12 is independently (CH2)aR16, where each R16 is independently selected from O(CH2)bR13, R13, COR13, COOR13, CN, CONR13R14, NR13R14, NR13COR14, SR13, SOR13, SO2R13, NR13SO2R14, SO2OR13, SO2NR13R14, halogen, CF3, and NO2, and wherein each a is 0, 1, 2, or 3 and b is 0, 1, 2, or 3; R13 and R14 are each independently H or (CH2)aR15, where n is 0, 1, 2, or 3; and each R15 is independently selected from alkyl, cycloalkyl, heteroaryl, aralkyl, aryl and heterocycloalkyl, each of which may be optionally substituted by one or more substituents selected from halogen, OH, CN, COO-alkyl, aralkyl, SO2-alkyl, SO2-aryl, COOH, CO-alkyl, CO-aryl, NH2, NH-alkyl, N(alkyl)2, CF3, alkyl and alkoxy, wherein said alkyl and alkoxy groups may be further substituted by one or more OH groups. Further aspects of the invention relate to pharmaceutical compositions comprising compounds of formula I, and the use of compounds of formula (I) in the preparation of a medicament for treating a variety of disorders, including proliferative disorders, viral disorders, stroke, etc.
    • 本发明涉及式(I)化合物或其药学上可接受的盐,其中Z为NR11,NHCO,NHSO2,NHCH2,CH2,CH2CH2或CH = CH; X是任选被一个或多个R 12基团取代的烃基; R 10和R 11各自独立地为II或烷基; R1-R4各自独立地为II或(CII2)mR12,其中m为0,1,2或3; 每个R 12独立地为(CH 2)a R 16,其中每个R 16独立地选自O(CH 2)b R 13,R 13,COR 13,COOR 13,CN,CONR 13 R 14,NR 13 R 14,NR 13 COR 14,SR 13,SOR 13,SO 2 R 13,NR 13 SO 2 R 14,SO 2 R 13,SO 2 NR 13 R 14, CF 3和NO 2,并且其中每个a是0,1,2或3,b是0,1,2或3; R 13和R 14各自独立地为H或(CH 2)a R 15,其中n为0,1,2或3; 并且每个R 15独立地选自烷基,环烷基,杂芳基,芳烷基,芳基和杂环烷基,其各自可以任选被一个或多个选自卤素,OH,CN,COO-烷基,芳烷基,SO 2 - 烷基,SO 2 - 芳基,COOH,CO-烷基,CO-芳基,NH 2,NH-烷基,N(烷基)2,CF 3,烷基和烷氧基,其中所述烷基和烷氧基可进一步被一个或多个OH基取代。 本发明的其它方面涉及包含式I化合物的药物组合物,以及式(I)化合物在制备用于治疗多种病症(包括增殖性病症,病毒性疾病,中风等)的药物中的用途。