公开(公告)号：US07763751B2

公开(公告)日：2010-07-27

申请号：US10582141

申请日：2004-12-10

申请人： Carla Caccia ,  Laura Girola ,  Petra Karin Kaltofen ,  Daniele Losi ,  Patricia Salvati ,  Enrico Selva ,  Florian Thaler

发明人： Carla Caccia ,  Laura Girola ,  Petra Karin Kaltofen ,  Daniele Losi ,  Patricia Salvati ,  Enrico Selva ,  Florian Thaler

IPC分类号： C07C239/00 ,  A61K31/13

CPC分类号： C07C239/20 ,  A61K31/13 ,  C07C239/12 ,  C07C2602/10

摘要： This invention is related to hydroxylamino derivatives of the general formula (I) wherein n is 0, 1 or 2; R1 and R2, independently of each other, are H, OH or OCH3; R3 is H or CH3; R4 is H, C1-C3 straight or branched alkyl or, together with R3, forms a five to seven-membered carbocyclic ring; and R5 and R6, independently of each other, are H or C1-C5 straight or branched alkyl and the pharmaceutically acceptable salts or prodrug thereof, for the preparation of medicaments useful for the prevention, treatment and diagnosis of CNS degenerative disorders related to protein misfolding and/or misaggregation. The invention also relates to novel compounds included in formula (I), to a method for preparing said compounds and to pharmaceutical compositions containing them.

摘要翻译： 本发明涉及通式（I）的羟基氨基衍生物，其中n为0,1或2; R 1和R 2彼此独立地是H，OH或OCH 3; R3是H或CH3; R4是H，C1-C3直链或支链烷基，或与R3一起形成五至七元碳环; 和R5和R6彼此独立地是H或C 1 -C 5直链或支链烷基及其药学上可接受的盐或前药，用于制备用于预防，治疗和诊断与蛋白质错折叠有关的CNS退行性病症的药物 和/或散乱。 本发明还涉及式（I）中包括的新化合物，涉及制备所述化合物的方法和含有它们的药物组合物。

公开(公告)号：US20100197799A1

公开(公告)日：2010-08-05

申请号：US12760007

申请日：2010-04-14

申请人： Carla CACCIA ,  Laura Girola ,  Petra Karin Kaltofen ,  Daniele Losi ,  Patricia Salvati ,  Enrico Selva ,  Florian Thaler

发明人： Carla CACCIA ,  Laura Girola ,  Petra Karin Kaltofen ,  Daniele Losi ,  Patricia Salvati ,  Enrico Selva ,  Florian Thaler

IPC分类号： A61K31/13 ,  C07C239/20 ,  A61P25/16 ,  A61P25/28

CPC分类号： C07C239/20 ,  A61K31/13 ,  C07C239/12 ,  C07C2602/10

摘要： This invention is related to hydroxylamino derivatives of the following general formula (I) wherein n is 0, 1 or 2; R1 and R2, independently of each other, are H, OH or OCH3; R3 is H or CH3; R4 is H, C1-C3 straight or branched alkyl or, together with R3, forms a five to seven-membered carbocyclic ring; and R5 and R6, independently of each other, are H or C1-C5 straight or branched alkyl and the pharmaceutically acceptable salts or prodrug thereof, for the preparation of medicaments useful for the prevention, treatment and diagnosis of CNS degenerative disorders related to protein misfolding and/or misaggregation. The invention also relates to novel compounds included in formula (I), to a method for preparing the compounds and to pharmaceutical compositions containing them.

摘要翻译： 本发明涉及以下通式（I）的羟基氨基衍生物，其中n为0,1或2; R 1和R 2彼此独立地是H，OH或OCH 3; R3是H或CH3; R4是H，C1-C3直链或支链烷基，或与R3一起形成五至七元碳环; 和R5和R6彼此独立地是H或C 1 -C 5直链或支链烷基及其药学上可接受的盐或前药，用于制备用于预防，治疗和诊断与蛋白质错折叠相关的CNS退行性病症的药物 和/或散乱。 本发明还涉及式（I）中包括的新化合物，涉及制备该化合物的方法和含有该化合物的药物组合物。