公开(公告)号：US07176199B2

公开(公告)日：2007-02-13

申请号：US10472236

申请日：2002-03-14

申请人： Toshiya Morie ,  Seiji Iwama ,  Mitsue Notake ,  Tomoko Kitano

发明人： Toshiya Morie ,  Seiji Iwama ,  Mitsue Notake ,  Tomoko Kitano

IPC分类号： C07D239/14 ,  C07D233/50 ,  C07D401/14 ,  A61K31/506 ,  C07D413/14

CPC分类号： C07D401/12 ,  A61K31/445 ,  A61K31/4545 ,  A61K31/497 ,  A61K31/506 ,  A61K31/551 ,  C07D211/62 ,  C07D239/14 ,  C07D239/16 ,  C07D239/42 ,  C07D295/185 ,  C07D401/04 ,  C07D401/14 ,  C07D413/14

摘要： An aryl-substituted alicyclic compound of the formula (I): wherein U is 1,4,5,6-tetrahydropyrimidin-2-yl, etc., A is phenylene, etc., B is piperidine-1,4-diyl, etc., Z is —CONH—, etc., R3 is hydrogen, etc., R5 is hydrogen, aryl, etc., R6 is a mono-substituted amino (e,g., benzyloxycarbonylamino), R7 is hydrogen, etc., and a process for preparation thereof, and a pharmaceutical composition containing the same. The compound of the present invention has a high selectivity for αvβ3 integrin, and exhibits a potent inhibitory activity thereto, and hence, it is useful as a preventive or/and a therapeutic agent for a disease in which αvβ3 integrin is involved.

摘要翻译： 式（I）的芳基取代的脂环族化合物：其中U是1,4,5,6-四氢嘧啶-2-基等，A是亚苯基等，B是哌啶-1,4-二基， 等等，Z是-CONH-等，R 3是氢等，R 5是氢，芳基等，R 6， / SUP>是单取代的氨基（例如，苄氧羰基氨基），R 7是氢等，及其制备方法和含有它们的药物组合物。 本发明的化合物对于alphavbeta3整联蛋白具有高选择性，并且对其表现出有效的抑制活性，因此可用作涉及α-角蛋白3整联蛋白的疾病的预防和/或治疗剂。

公开(公告)号：US20110224304A1

公开(公告)日：2011-09-15

申请号：US13129394

申请日：2009-11-13

申请人： Seiji Iwama ,  Tomoyuki Tanaka ,  Nana Najima

发明人： Seiji Iwama ,  Tomoyuki Tanaka ,  Nana Najima

IPC分类号： A61K31/165 ,  C07C233/05 ,  A61P25/08 ,  A61P25/00

CPC分类号： C07C235/34 ,  C07C233/11 ,  C07C255/57 ,  C07C317/44 ,  C07C323/62 ,  C07C2601/02

摘要： The present invention provides a compound of formula (I) or a salt thereof, wherein R1, R2 and R3 are independently selected from the group consisting of hydrogen atom, fluorine atom, chlorine atom, bromine atom, C1-6 alkyl, C1-6 alkoxy substituted with fluorine atom, and others; R4 and R5 are independently selected from the group consisting of hydrogen atom, fluorine atom, chlorine atom, C1-6 alkyl, C1-6 alkoxy substituted with fluorine atom, and others; R6 and R7 are independently selected from the group consisting of hydrogen atom, fluorine atom, methyl, ethyl, hydroxy group, and others; and R8 and R9 are independently selected from the group consisting of hydrogen atom, C1-6 alkyl, and others, which is useful as an agent for treating or preventing various types of epilepsy including partial seizures and/or generalized seizures.

摘要翻译： 本发明提供式（I）化合物或其盐，其中R 1，R 2和R 3独立地选自氢原子，氟原子，氯原子，溴原子，C 1-6烷基，C 1-6 氟原子取代的烷氧基等; R4和R5独立地选自氢原子，氟原子，氯原子，C1-6烷基，被氟原子取代的C1-6烷氧基等; R6和R7独立地选自氢原子，氟原子，甲基，乙基，羟基等; R8和R9独立地选自氢原子，C1-6烷基等，其可用作治疗或预防各种类型癫痫的药物，包括部分发作和/或全身性发作。