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    • 3. 发明申请
    • METHOD OF TREATING A SOLID TUMOR DISEASE COMPRISING ADMINISTERING A COMBINATION COMPRISING IMATINIB AND AN INHIBITOR OF AN EFFLUX PUMP ACTIVE AT THE BLOOD BRAIN BARRIER OR DEMETHYL IMATINIB
    • 治疗包括包含IMATINIB的组合和在血脑屏障或DEMETHYL IMATINIB上活化的血液泵的抑制剂的固体肿瘤疾病的方法
    • WO2006136391A2
    • 2006-12-28
    • PCT/EP2006005960
    • 2006-06-21
    • NOVARTIS AGNOVARTIS PHARMA GMBHBIHOREL SEBASTIENGROSS GERHARDLEMAIRE MICHELCAMENISCH GIAN P
    • BIHOREL SEBASTIENGROSS GERHARDLEMAIRE MICHELCAMENISCH GIAN P
    • F16H7/20F16C1/00
    • A61K45/06A61K31/506A61K2300/00
    • The invention relates to a method of treating a warm-blooded animal having a solid tumor disease comprising administering a combination which comprises: a) a N-phenyl-2- pyrimidine-amine derivative, especially N-{5-[4-(4-methyl-piperazino-methyl)-benzoylamido]- 2-methylphenyl}-4-(3-pyridyl)-2-pyrimidine-amine, b) at least one compound inhibiting the efflux pump active at the blood brain barrier selected from MDR1 and MRP2, c) optionally an antineoplastic agent, especially as defined herein, d) optionally an alkylating agent and e) optionally, hydroxyurea; to the use of such a combination for the preparation of a medicament for the treatment of a solid tumor disease; and to a commercial package or product comprising such a combination together with instructions for the treatment of a solid tumor disease. In a further aspect, the present invention pertains to a combination which comprises: a) optionally a N-phenyl-2-pyrimidine-amine derivative, especially N-{5-[4-(4- methyl-piperazino-methyl)-benzoylamido]-2-methylphenyl}-4-(3-pyridyl)-2-pyrimidine-amine (STI571 ), b) N-{5-[4-(piperazino-methyl)-benzoylamido]-2-methylphenyl}-4-(3-pyridyl)-2- pyrimidine-amine (CGP74588), c) optionally an antineoplastic agent, d) optionally an alkylating agent and e) optionally, hydroxyurea; to the use of such a combination for the preparation of a medicament for the treatment of a solid tumor disease; and to a commercial package or product comprising such a combination together with instructions for the treatment of a solid tumor disease.
    • 本发明涉及一种治疗具有实体肿瘤疾病的温血动物的方法,包括施用组合,其包含:a)N-苯基-2-嘧啶胺衍生物,特别是N- {5- [4-(4 - 甲基 - 哌嗪子基 - 甲基) - 苯甲酰氨基] -2-甲基苯基} -4-(3-吡啶基)-2-嘧啶胺,b)至少一种抑制血液屏障的外排泵活性的化合物,其选自MDR1和 MRP2,c)任选的抗肿瘤剂,特别是如本文定义的d)任选的烷化剂和e)任选的羟基脲; 涉及使用这种组合来制备用于治疗实体瘤疾病的药物; 以及包含这种组合的商业包装或产品以及治疗实体瘤疾病的说明书。 在另一方面,本发明涉及一种组合,其包括:a)任选地N-苯基-2-嘧啶胺衍生物,特别是N- {5- [4-(4-甲基 - 哌嗪子基 - 甲基) - 苯甲酰氨基 ] -2-甲基苯基} -4-(3-吡啶基)-2-嘧啶胺(STI571),b)N- {5- [4-(哌嗪基 - 甲基) - 苯甲酰氨基] -2-甲基苯基} -4- (3-吡啶基)-2-嘧啶胺(CGP74588),c)任选的抗肿瘤剂,d)任选的烷化剂和e)任选的羟基脲; 涉及使用这种组合来制备用于治疗实体瘤疾病的药物; 以及包含这种组合的商业包装或产品以及治疗实体瘤疾病的说明书。