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    • 2. 发明申请
    • SUBSTITUTED 2,3-DIHYDROIMIDAZO[1,2-C]QUINAZOLINE SALTS
    • 取代的2,3-二氢吲哚并[1,2-C]喹唑啉盐
    • WO2012136553A1
    • 2012-10-11
    • PCT/EP2012/055600
    • 2012-03-29
    • Bayer Pharma AktiengesellschaftPETERS, Jan, GeorgMILITZER, Hans-ChristianMÜLLER, Hartwig
    • PETERS, Jan, GeorgMILITZER, Hans-ChristianMÜLLER, Hartwig
    • C07D487/04A61K31/519A61P35/00
    • A61K31/5377A61K45/06C07D487/04
    • The present invention relates : - to 2-amino-N-[7-methoxy-8-(3-morpholin-4-ylpropoxy)-2,3-dihydroimidazo- [1,2-c]quinazolin-5-yl]pyrimidine-5-carboxamide dihydrochloride salt of formula (II) : or a tautomer, solvate or hydrate thereof; - to methods of preparing said dihydrochloride salt; - to said dihydrochloride salt for the treatment and/or prophylaxis of a disease; - to the use of said dihydrochloride salt for the preparation of a medicament for the treatment and/or prophylaxis of a disease, in particular of a hyper- proliferative and/or angiogenesis disorder, more particularly for the treatment or prophylaxis of a cancer, particularly lung cancer, in particular non-small cell lung carcinoma, colorectal cancer, melanoma, pancreatic cancer, hepatocyte carcinoma, pancreatic cancer, hepatocyte carcinoma or breast cancer; - to a pharmaceutical composition comprising said dihydrochloride salt; and - to a pharmaceutical combination comprising said dihydrochloride salt in combination with one or more further pharmaceutical agents.
    • 本发明涉及:2-氨基-N- [7-甲氧基-8-(3-吗啉-4-基丙氧基)-2,3-二氢咪唑并[1,2-c]喹唑啉-5-基]嘧啶 (II)的5-甲酰胺二盐酸盐:或其互变异构体,溶剂合物或水合物; - 制备所述二盐酸盐的方法; - 所述二盐酸盐用于治疗和/或预防疾病; - 使用所述二盐酸盐来制备用于治疗和/或预防疾病,特别是高增殖和/或血管生成障碍的药物,更特别是用于治疗或预防癌症,尤其是 肺癌,特别是非小细胞肺癌,结肠直肠癌,黑素瘤,胰腺癌,肝细胞癌,胰腺癌,肝细胞癌或乳腺癌; - 包含所述二盐酸盐的药物组合物; 以及 - 包含所述二盐酸盐与一种或多种其它药剂组合的药物组合。