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    • 9. 发明授权
    • Guanidine derivatives quinazoline and quinoline for use in the treatment of autoimmune diseases
    • 胍衍生物喹唑啉和喹啉用于治疗自身免疫性疾病
    • US07001904B1
    • 2006-02-21
    • US10311587
    • 2001-06-19
    • Jeffrey Philip Poyser
    • Jeffrey Philip Poyser
    • C07D403/12C07D413/12A61K31/505
    • C07D401/12C07D239/94C07D401/14C07D403/12C07D405/12C07D405/14C07D409/12C07D409/14
    • The invention concerns quinazoline and quinoline derivatives of Formula (I) wherein Q1 includes a quinazoline or quinoline ring optionally substituted with a group such as halogeno, trifluoromethyl and cyano, or a group of the formula: Q3—X1— wherein X1 includes a direct bond and O and Q3 includes aryl, aryl-(1-6C)alkyl, heterocyclyl and heterocyclyl-(1-6C)alkyl; each of R2, R3 and R5 is hydrogen or (1-6C)alkyl, provides that one of the parts of groups R2 and R4 together, R3 and R4 together and R5 and R4 together forms a bond; R6 is an optionally substituted group selected from (2-6C) alkenyl, (2-6C) alkynyl, (3-7C)cycloalkyl and (3-7C) cycloalkenyl, or R6 is a substituted (1-6C) alkyl group; and Q2 includes aryl and aryl-(1-3C)alkyl or a pharmaceutically-acceptable salt thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the prevention or treatment of T cell mediated diseases or medical conditions in a warm-blooded animal.
    • 本发明涉及式(I)的喹唑啉和喹啉衍生物,其中Q 1包括任选被诸如卤代,三氟甲基和氰基的基团取代的喹唑啉或喹啉,或下式的基团: 其中X 1包括直接键,O和Q 3包括芳基,芳基 - ( 1-6C)烷基,杂环基和杂环基 - (1-6C)烷基; R 2,R 3和R 5各自为氢或(1-6C)烷基,提供基团R的一部分 R 2和R 4一起,R 3和R 4一起和R 5, 和R 4一起形成键; R 6是选自(2-6C)烯基,(2-6C)炔基,(3-7C)环烷基和(3-7C)环烯基中的任选取代的基团,或R 6 取代的(1-6C)烷基; 并且Q 2包括芳基和芳基 - (1-3C)烷基或其药学上可接受的盐; 其制备方法,含有它们的药物组合物及其在制备用于预防或治疗温血动物中的T细胞介导的疾病或医学病症的药物中的用途。