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    • 7. 发明申请
    • SULFONAMIDE DERIVATIVES WITH ACTIVITY ON PROTEIN KINASE A AND B
    • 蛋白激酶A和B具有活性的磺酰胺衍生物
    • WO2005011697A3
    • 2005-04-21
    • PCT/GB2004003196
    • 2004-07-23
    • ASTEX TECHNOLOGY LTDCANCER REC TECH LTDCANCER RES INST ROYALMCDONALD EDWARDDE FONSECA TATIANA FARIABAVETSIAS VASSILIOSCALDWELL JOHNWYATT PAUL GRAHAMBERDINI VALERIO
    • MCDONALD EDWARDDE FONSECA TATIANA FARIABAVETSIAS VASSILIOSCALDWELL JOHNWYATT PAUL GRAHAMBERDINI VALERIO
    • A61K31/472C07D217/02C07D401/12
    • C04B35/632A61K31/472C07D217/02C07D401/12
    • The invention provides compounds for the prophylaxis or treatment of a disease state or condition mediated by protein kinase A or protein kinase B, the compounds having the formula (I°), or being salts or solvates thereof. In formula (I°), n is 0 or 1; A and E are alkylene 2-3 carbon atoms in length optionally substituted by R and -X-CH(R )(R ); G is hydrogen when n is 0 and, when n is 1, G is hydrogen or -X-CH(R )(R ); R is an aryl or heteroaryl group having 5-12 ring members; R and R are selected from hydrogen, R , R and CH(R )(R ); R , R and R are selected from hydrogen, R and -X-CH(R )(R ); or any one pair or any two non-overlapping pairs selected from R and R ; R and R ; R and R ; R and R ; R and R ; R and R ; and R and R are linked together in a ring and together form an alkylene chain of 1-5 carbon atoms in length which may be optionally substituted by R and -X-CH(R )(R ); or the pair R and R are linked together in a ring and together form an alkylene chain of 2-5 carbon atoms in length which may be optionally substituted by R and -X-CH(R )(R ); and optionally R and R may be linked together in a ring and together form an alkylene chain of 1-6 carbon atoms in length which may be optionally substituted by R and -X-CH(R )(R ); or R and R together with the carbon atom to which they are attached form a cyclic group having 5-12 ring members; X, R , R , R , R , R and R are each as defined in claim 1; and wherein the definitions of, A, E, G, X, n and R to R are subject to the provisos set ou in claim 1.
    • 本发明提供了用于预防或治疗由蛋白激酶A或蛋白激酶B,具有式(I°)的化合物或其盐或溶剂合物介导的疾病状态或病症的化合物。 在式(I°)中,n为0或1; A和E是长度任选被R 11和-X-CH(R 6)(R 7)取代的2-3个碳原子的亚烷基; 当n为0时,G为氢,当n为1时,G为氢或-X-CH(R 6)(R 7); R 1是具有5-12个环成员的芳基或杂芳基; R 2和R 4选自氢,R 7,R 7和CH(R 6)(R 7); R 3,R 3a和R 5选自氢,R 11和-X-CH(R 6)(R 7); 或选自R 2和R 3中的任何一对或任何两个非重叠对; R 3和R 4; R 2和R 5; R 3和R 5; R 4和R 5; R 3和R 8; 并且R 4和R 8以环连接在一起并且一起形成长度为1-5个碳原子的亚烷基链,其可任选地被R 11和-X-CH(R 6)取代, )(R <7>); 或者R 2和R 4在环中连接在一起并且一起形成长度为2-5个碳原子的亚烷基链,其可以任选地被R 11和-X-CH(R' 6>)(R <7>); 并且任选地R 3和R 3a可以以环连接在一起并且一起形成长度为1-6个碳原子的亚烷基链,其可任选地被R 11和-X-CH(R' 6>)(R <7>); 或R 6和R 7与它们所连接的碳原子一起形成具有5-12个环成员的环状基团; X,R 6,R 7,R 8,R 9,R 10和R 11各自如权利要求1所定义; 并且其中A,E,G,X,n和R 1至R 11的定义符合权利要求1所述的限制条件。