公开(公告)号：US06706734B2

公开(公告)日：2004-03-16

申请号：US10196362

申请日：2002-07-17

申请人： Hirokazu Annoura ,  Kyoko Nakanishi ,  Shigeki Tamura

发明人： Hirokazu Annoura ,  Kyoko Nakanishi ,  Shigeki Tamura

IPC分类号： A61K314465

CPC分类号： C07D211/44 ,  C07D211/12 ,  C07D211/14 ,  C07D211/18 ,  C07D211/52 ,  C07D211/70

摘要： A pharmaceutical composition, especially a pharmaceutical composition for the alleviation or treatment of symptoms due to ischemic diseases and symptoms derived from seizures, epilepsy, and migraine, and a Ca2+ overload suppressant, containing an arylpiperidinol or arylpiperidine derivative having the formula (I): wherein, R is H, an optionally substituted phenyl, an optionally substituted phenoxy, or an optionally substituted benzoyl, A is a connecting bond, a cycloalkylene, or an alkenylene optionally substituted with a lower alkyl, B is an alkylene optionally substituted with OH or an alkoxy or —NHCO(CH2)n— where n is an integer of 1 to 5, E is a connecting bond, O, or a methylene, X is OH or H provided that when E is O or a methylene, X is not H, and Y and Z are independently H, a halogen, an alkoxy, or an alkyl optionally substituted with a halogen.

摘要翻译： 一种药物组合物，特别是用于缓解或治疗由缺血性疾病引起的症状和由癫痫发作，癫痫和偏头痛引起的症状的药物组合物，以及包含具有下式的芳基哌啶醇或芳基哌啶衍生物的Ca 2+过量抑制剂 I）：其中R为H，任选取代的苯基，任选取代的苯氧基或任选取代的苯甲酰基，A为任选被低级烷基取代的连接键，亚环烷基或亚烯基，B为任选取代的亚烷基 与OH或烷氧基或-NHCO（CH 2）n - ，其中n为1至5的整数，E为连接键，O或亚甲基，X为OH或H，条件是当E为O或亚甲基时， X不为H，Y和Z独立地为H，卤素，烷氧基或任选被卤素取代的烷基。

公开(公告)号：US06525070B2

公开(公告)日：2003-02-25

申请号：US09827488

申请日：2001-04-06

申请人： Aaron Rigby ,  Hitesh Sanganee ,  Brian Springthorpe ,  Louise Lawrence

发明人： Aaron Rigby ,  Hitesh Sanganee ,  Brian Springthorpe ,  Louise Lawrence

IPC分类号： A61K314465

CPC分类号： C07D401/14 ,  C07D211/58 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D473/08 ,  C07D495/04 ,  C07D513/04

摘要： The present invention provides a compound of a formula (I): wherein the variables are defined herein; to a process for preparing such a compound; and to the use of such a compound in the treatment of a chemokine (such as CCR3) or H1 mediated disease state.

摘要翻译： 本发明提供式（I）的化合物：其中变量在本文中定义; 涉及制备这种化合物的方法; 以及这种化合物在治疗趋化因子（例如CCR3）或H1介导的疾病状态中的用途。

公开(公告)号：US06518284B2

公开(公告)日：2003-02-11

申请号：US09824189

申请日：2001-04-02

申请人： Aurello Orjales Venero ,  Antonio Toledo Avello ,  Carmen Pumar Duran

发明人： Aurello Orjales Venero ,  Antonio Toledo Avello ,  Carmen Pumar Duran

IPC分类号： A61K314465

CPC分类号： C07D211/22

摘要： New 4-substituted piperidines of the following general formula (I) are disclosed in which R1 and R2 are substituted in unsubstituted aryl radicals, which compounds are obtained as racemic mixtures and as pure enantiomers. The compounds, and their pharmaceutically acceptable salts, inhibit the serotonin and/or noradrenaline reuptake, and are useful as medicaments in disorders in which an increase of levels of those neurotransmitters is necessary.

摘要翻译： 公开了以下通式（I）的新的4-取代的哌啶，其中R 1和R 2在未取代的芳基中被取代，该化合物作为外消旋混合物和纯对映体获得。化合物及其药学上可接受的盐抑制 5-羟色胺和/或去甲肾上腺素再摄取，并且可用作需要增加这些神经递质水平的疾病中的药物。