公开(公告)号：US07435744B2

公开(公告)日：2008-10-14

申请号：US10761940

申请日：2004-01-21

申请人： Gyorgy Domány ,  Csilla Horváth ,  Gizella Bartáné Szalai ,  József Nagy ,  Sándor Kolok ,  Éva Kovácsné Bozó ,  István Borza ,  István Vágó ,  Attila Bielik ,  Györgyi Ignáczné Szendrei ,  György Keserü ,  Sándor Farkas

发明人： Gyorgy Domány ,  Csilla Horváth ,  Gizella Bartáné Szalai ,  József Nagy ,  Sándor Kolok ,  Éva Kovácsné Bozó ,  István Borza ,  István Vágó ,  Attila Bielik ,  Györgyi Ignáczné Szendrei ,  György Keserü ,  Sándor Farkas

IPC分类号： A61K31/445 ,  C07D401/12

CPC分类号： C07D211/14 ,  C07D211/16 ,  C07D401/12 ,  C07D413/12 ,  C07D417/12

摘要： The present invention relates to a compound of formula (I): wherein: V and U are hydrogen, halogen, C1-C4 alkylamino, or together form a group that contains one or more heteroatoms, and that taken together with one or more: (a) hydrogen atoms; (b) carbon atoms; (c) —CH═ groups; (d) —CH2— groups; or (e) additional heteroatoms of the same or different type; or any combination thereof, form a 4-7 membered homocyclic or heterocyclic ring, wherein the homocyclic or heterocyclic ring may combine with the phenyl group to form a bicyclic ring, and wherein the homocyclic or heterocyclic ring or the bicyclic ring may contain one or more oxo, thioxo, amino, mercapto, trifluoromethyl, C1-C4 alkyl, ═S or —SH groups; W: is —CO—, —CH2— or —CH2—(C1-C4 alkyl)-; X: is —CO—; Y: is —O—, C1-C4 alkylene, C1-C4 alkynylene, cycloalkylene, aminocarbonyl, —NH—, —N(C1-C4 alkyl)-, -C1-C4 alkylene-N(C1-C4 alkyl)-, —CH2O—, —CH(OH)— or —OCH2—; Z: is hydrogen, halogen, nitro, amino, C1-C4 alkyl, C1-C4 alkoxy, cyano, trifluoromethyl, hydroxyl or carboxyl; R1 and R2: are hydrogen, or together form a C1-C3 bridge; and n and m: independently are 0-3, wherein n and m cannot each be 0; or an optical antipode, racemate or pharmaceutically-acceptable salt thereof. The carboxylic acid amide derivatives of formula (I) are highly effective and selective antagonists of the NMDA receptor.

公开(公告)号：US20130217702A1

公开(公告)日：2013-08-22

申请号：US13823221

申请日：2011-11-04

申请人： Gyula Beke ,  Gyula Attila Bényei ,  István Borza ,  Éva Bozó ,  Sándor Farkas ,  Katalin Hornok ,  Andrea Papp ,  István Vágó ,  Mónika Vastag

发明人： Gyula Beke ,  Gyula Attila Bényei ,  István Borza ,  Éva Bozó ,  Sándor Farkas ,  Katalin Hornok ,  Andrea Papp ,  István Vágó ,  Mónika Vastag

IPC分类号： C07D413/14 ,  C07D209/42 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14

CPC分类号： C07D413/14 ,  C07D209/42 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D413/12

摘要： The present invention relates to the indole derivatives of formula (I), wherein R1-R6 and X are defined in the claims and optical antipodes or racemates and/or salts thereof which are selective antagonists of bradykinin B1 to process for producing these compounds, pharmacological compositions containing them and to their use in therapy or prevention of painful and inflammatory conditions.

摘要翻译： 本发明涉及式（I）的吲哚衍生物，其中R1-R6和X在权利要求书中定义，光学对映体或外消旋体和/或其盐是缓激肽B1的选择性拮抗剂，用于制备这些化合物，药理学 含有它们的组合物及其在治疗中的用途或预防疼痛和炎症状况。