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    • 6. 发明申请
    • USE OF C-SRC INHIBITORS IN COMBINATION WITH A PYRIMIDYLAMINOBENZAMIDE COMPOUND FOR THE TREATMENT OF LEUKEMIA
    • C-SRC抑制剂与吡嗪酰胺苯甲酸化合物联合用于治疗白血病的用途
    • WO2007116025A3
    • 2007-12-13
    • PCT/EP2007053399
    • 2007-04-05
    • NOVARTIS AGNOVARTIS PHARMA GMBHMANLEY PAUL W
    • MANLEY PAUL W
    • A61K31/506A61K31/4709A61K31/519A61P35/02
    • A61K31/4709A61K31/506A61K31/519
    • The invention relates to a combination which comprises (a) at least one compound decreasing the c-Src activity and (b) a pyrimidylaminobenzamide compound; to pharmaceutical compositions comprising said combinations; and to a method of treating a warm-blooded animal having leukemia, especially chronic myelogenous leukemia, comprising administering to the animal at least one compound inhibiting the activity of a member of the Src kinase family, the Btk kinase family, the Tec kinase family or a Raf kinase inhibitor, in particular inhibiting the c-Src protein tyrosine kinase activity or inhibiting simultaneously the c-Src protein tyrosine kinase activity and the Bcr-Abl tyrosine kinase activity, in combination with a pyrimidylaminobenzamide compound, in particular 4-Methyl-3-[[4-(3-pyridinyl)-2-pyrimidinyl]amino]-N-[5-(4-methyl-1H-imidazol-1-yl)-3- (trifluoromethyl)phenyl] benzamide.
    • 本发明涉及一种组合,其包含(a)至少一种降低c-Src活性的化合物和(b)嘧啶基氨基苯甲酰胺化合物; 包含所述组合的药物组合物; 以及治疗具有白血病,特别是慢性骨髓性白血病的温血动物的方法,包括向所述动物施用至少一种抑制Src激酶家族成员,Btk激酶家族,Tec激酶家族的活性的化合物或 Raf激酶抑制剂,特别是抑制c-Src蛋白酪氨酸激酶活性或同时抑制c-Src蛋白酪氨酸激酶活性和Bcr-Abl酪氨酸激酶活性,与嘧啶氨基苯甲酰胺化合物,特别是4-甲基-3 - [[4-(3-吡啶基)-2-嘧啶基]氨基] -N- [5-(4-甲基-1H-咪唑-1-基)-3-(三氟甲基)苯基]苯甲酰胺。
    • 8. 发明申请
    • SULPHONAMIDOANILINE DERIVATIVES BEING JANUS KINASES INHIBITORS
    • 磺胺类药物抑制剂磺酰胺衍生物
    • WO2007071393A3
    • 2007-07-26
    • PCT/EP2006012311
    • 2006-12-20
    • NOVARTIS AGNOVARTIS PHARMA GMBHCAPRARO HANS-GEORGCOUPEZ BERNARDFURET PASCALMANLEY PAUL WPISSOT SOLDERMANN CAROLE
    • CAPRARO HANS-GEORGCOUPEZ BERNARDFURET PASCALMANLEY PAUL WPISSOT SOLDERMANN CAROLE
    • C07D473/16A61K31/52A61K31/5377A61P35/00C07D473/18C07D487/04C07D519/00
    • C07D473/16C07D473/18C07D487/04C07D519/00
    • The invention relates to sulphonamidoanilines of formula (I) wherein A is N or CH, W, X, Y and Z are N or CH under the proviso that at least one of the three symbols W, X and Y represent CH, R 1 represents NR 4 R 5 or OR 4 , wherein R 4 represents optionally substituted alkyl, optionally substituted cycloalkyl optionally comprising one or two nitrogen or oxygen atoms, or substituted aryl, and R 5 represents hydrogen or unsubstituted or substituted alkyl, or R 4 and R 5 together with the nitrogen to which they are attached represent an optionally substituted five- or six-membered nitrogen containing monocyclic ring, an optionally substituted nitrogen containing fully saturated bicyclic ring, or an spirocyclic fully saturated ring system containing one or two nitrogen atoms, R 2 is hydrogen, lower alkenyl or alkyl, R 3 is alkyl which is unsubstituted or mono-, di- or trisubstituted by halogen; alkenyl or aryl, and their salts; processes for their preparation, their application in the treatment of the human or animal body, the use thereof - alone or in combination with one or more other pharmaceutically active compounds - for the treatment of diseases, a method for the treatment of such a disease and the use of such a compound - alone or in combination with one or more other pharmaceutically active compounds - for the manufacture of a pharmaceutical preparation for the treatment of a proliferative disease.
    • 本发明涉及式(I)的磺酰氨基苯胺,其中A为N或CH,W,X,Y和Z为N或CH,条件是三个符号W,X和Y中的至少一个表示CH,R < > 1表示NR 4 R 5或OR 4,其中R 4表示任选取代的烷基 任选包含一个或两个氮原子或氧原子的任选取代的环烷基或取代的芳基,R 5表示氢或未取代或取代的烷基,或R 4和R 3 > 5个与它们所连接的氮一起代表任选取代的五元或六元含氮单环,任选取代的含氮完全饱和双环,或含有一个或多个 两个氮原子,R 2是氢,低级烯基或烷基,R 3是未被取代的或被卤代基单 - ,二 - 或三取代的烷基 N; 烯基或芳基,及其盐; 其制备方法,它们在人体或动物体内的治疗中的应用,其单独或与一种或多种其它药物活性化合物组合用于治疗疾病的用途,治疗这种疾病的方法和 使用这种化合物 - 单独或与一种或多种其它药学活性化合物组合用于制备用于治疗增殖性疾病的药物制剂。