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    • 7. 发明公开
    • 아미노 치환기를 갖는 알파-아릴메톡시아크릴레이트 유도체및 이를 함유하는 대사성 골 질환의 예방 및 치료용 약학조성물
    • 具有氨基取代基和药物组合物的ALPHA-ARYLMETHOXYACRYLATE衍生物用于预防和治疗含有其的代谢性骨髓疾病
    • KR1020060134303A
    • 2006-12-28
    • KR1020050053883
    • 2005-06-22
    • 한국화학연구원주식회사 오스코텍
    • 김범태민용기이연수허정녕이혁박노균김정근김세원고선일
    • A61K31/44A61K31/496A61K31/535
    • A61K31/5375A61K31/136A61K31/4439A61K31/451
    • A pharmaceutical composition comprising an alpha-arylmethoxyacrylate derivative is provided to be able to excellently inhibit osteoclast formation and absorption activity thereof, thereby being effectively utilized for preventing metabolic bone diseases such as osteoporosis and ossification at a growth period. The pharmaceutical composition for preventing and treating metabolic bone disease comprises an alpha-arylmethoxyacrylate derivative represented by the formula(1), a physiologically acceptable salt thereof or a solvate thereof as an effective ingredient. In the formula(1), A is N or CH, X is H or halogen, Y is H, halogen or CF3, Z is substituted or unsubstituted N-containing heteroaryl or (CH2)n-NR^1R^2(where n is 0, 1 or 2 and each R^1 and R^2 is independently H, C1-8 alkyl, C1-8 haloalkyl, hydroxy, C2-8 alkenyl, C2-4 alkynyl, C3-8 cycloalkyl, C3-8 cycloalkyl C1-4 alkyl, C1-4 alkoxy C1-4 alkyl, C3-8 cycloalkoxy C1-4 alkyl, C1-8 alkylsulfonyl, C2-7 heterocyclyl C1-4 alkyl containing at least one N, O or S, or substituted or unsubstituted aryl, or forms a heterocycle with adjacent N).
    • 提供包含α-芳基甲氧基丙烯酸酯衍生物的药物组合物,以能够极好地抑制破骨细胞形成和吸收活性,从而有效地用于预防生长期骨质疏松和骨化等代谢骨疾病。 用于预防和治疗代谢性骨病的药物组合物包含由式(1)表示的α-芳基甲氧基丙烯酸酯衍生物,其生理学上可接受的盐或其溶剂合物作为有效成分。 在式(1)中,A是N或CH,X是H或卤素,Y是H,卤素或CF 3,Z是取代或未取代的含N杂芳基或(CH 2)n -NR 4 R 12(其中n 每个R 1和R 2独立地为H,C 1-8烷基,C 1-8卤代烷基,羟基,C 2-8烯基,C 2-4炔基,C 3-8环烷基,C 3-8环烷基 C 1-4烷基,C 1-4烷氧基C 1-4烷基,C 3-8环烷氧基C 1-4烷基,C 1-8烷基磺酰基,含有至少一个N,O或S的C 2-7杂环基C 1-4烷基,或取代或未取代的 芳基,或与相邻的N形成杂环)。