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    • 4. 发明申请
    • NOVEL COMPOUNDS FOR THE TREATMENT OF DISEASES ASSOCIATED WITH AMYLOID OR AMYLOID-LIKE PROTEINS
    • 用于治疗与淀粉样蛋白或类淀粉样蛋白相关的疾病的新型化合物
    • US20100144793A1
    • 2010-06-10
    • US12516167
    • 2007-11-23
    • Wolfgang FroestlNampally SreenivasacharySophie LohmannMaria Pilar Lopez DeberAndreas MuhsMaria Pihlgren Bosch
    • Wolfgang FroestlNampally SreenivasacharySophie LohmannMaria Pilar Lopez DeberAndreas MuhsMaria Pihlgren Bosch
    • A61K31/444C07D403/12C07D401/14A61K31/4155G01N33/53A61P25/28
    • C07D405/14C07D231/38C07D231/40C07D231/56C07D243/02C07D243/12C07D401/14C07D409/14
    • The present invention relates to compounds of the general formula (I) wherein (formula 2) independently represents a single bond or a double bond, represents a linking group A and A′ are each independently a 5- to 7-membered heterocyclic ring, wherein the heterocyclic rings A und A′ are optionally substituted by one or more substituents, selected from C1-6 alkyl, C3-6 cycloalkyl, optionally substituted phenyl, optionally substituted heteroaryl, C1-4 alkylene-(optionally substituted phenyl) and C1-4 alkylene-(optionally substituted heteroaryl), or two substituents may be joined to form an optionally substituted, saturated, unsaturated or aromatic 5- to 7-membered ring which is fused with the heterocyclic ring A or A′, and wherein the heterocyclic rings A und A′ may contain in addition to the units X, X′, Y and Y′ one or more heteroatoms, selected from N, NR, S and Ol wherein R is selected from H and C1-4 alkyl; the units X and X′ are each independently a H-bond acceptor; and the units Y and Y′ are each independently a H-bond donor. The compound of formula (I) can be employed in the treatment of a group of disorders and abnormalities associated with amyloid protein, such as Alzheimer's disease, and of diseases or conditions associated with amyloid-like proteins. The compounds of the present invention can also be used in the treatment of ocular diseases associated with pathological abnormalities/changes in the tissues of the visual system.
    • 本发明涉及通式(I)的化合物,其中(式2)独立地表示单键或双键,表示连接基团A和A'各自独立地为5-至7-元杂环,其中 杂环A和A'任选被一个或多个选自C 1-6烷基,C 3-6环烷基,任选取代的苯基,任选取代的杂芳基,C 1-4亚烷基 - (任选取代的苯基)和C 1-4的取代基取代 亚烷基 - (任选取代的杂芳基)或两个取代基可以连接形成与杂环A或A'稠合的任选取代的,饱和的,不饱和的或芳族的5-至7-元环,并且其中杂环A 除了单元X,X',Y和Y'之外,还可以含有一个或多个选自N,NR,S和O的杂原子,其中R选自H和C 1-4烷基; 单元X和X'各自独立地为H键受体; 单元Y和Y'各自独立地为H键供体。 式(I)化合物可用于治疗与淀粉样蛋白相关的一组疾病和异常,例如阿尔茨海默病,以及与淀粉状蛋白样蛋白相关的疾病或病症。 本发明的化合物还可以用于治疗与视觉系统的组织中的病理学异常/变化相关的眼部疾病。