Kappa-opiate agonists for inflammatory bowel disorders
    62.
    发明授权
    Kappa-opiate agonists for inflammatory bowel disorders 失效
    卡帕酸激动剂用于炎症性肠病

    公开(公告)号:US5776972A

    公开(公告)日:1998-07-07

    申请号:US671502

    申请日:1996-06-27

    CPC分类号: A61K31/4025

    摘要: Pharmaceutical preparations which are suitable for the treatment of inflammatory bowel disorders and contain at least one compound of the formula I ##STR1## in which R.sup.1 is Ar, cycloalkyl having 3-7 C atoms or cycloalkylalkyl having 4-8 C atoms, R.sup.2 is Ar, or R.sup.1 and R.sup.2 together are ##STR2## R.sup.3 is H, OH, OA or A, R.sup.4 is A or phenyl which can optionally be mono- or disubstituted by Hal, OH, OA, CF.sub.3, NO.sub.2, NH.sub.2, NHA, NHCOA, NHSO.sub.2 A and/or NA.sub.2, R.sup.5 is OH, CH.sub.2 OH, R.sup.6 and R.sup.7 in each case independently of one another are H, Hal, OH, OA, CF.sub.3, NH.sub.2, NHA, NA.sub.2, NHCOA, NHCONH.sub.2, NO.sub.2 or methylenedioxy, with the oxy groups bonded to adjacent carbons on the ring, A is alkyl having 1-7 C atoms, Ar is a mono- or bicyclic aromatic radical which can optionally contain an N, O or S atom in the ring and can be mono-, di- or trisubstituted by A, Hal, OH, OA, CF.sub.3, NH.sub.2, NHA, NA.sub.2, NHCOA and/or NHCONH.sub.2,D is CH.sub.2, O, S, NH, NA, --CH.sub.2 --CH.sub.2 --,--CH.dbd.CH--,--CH.sub.2 --NH--,--CH.sub.2 --NA-- or a bond and Hal is F, Cl, Br or I; and/or physiologically acceptable salts and/or one of its glycosylated derivatives , and at least one physiologically acceptable excipient or auxiliary.

    摘要翻译: 适用于治疗炎症性肠病并含有至少一种式I g 3-7 C原子的化合物或具有4-8个C原子的环烷基烷基的药物制剂,R 2为Ar或R 1和R 2一起为“ R3是H,OH,OA或A,R4是A或可以被Hal,OH,OA,CF3,NO2,NH2,NHA,NHCOA,NHSO2A和/或NA2单取代或二取代的苯基,R5是OH, CH 2 OH,R 6和R 7各自独立地为H,Hal,OH,OA,CF 3,NH 2,NHA,NA 2,NHCOA,NHCONH 2,NO 2或亚甲二氧基,氧基与环上的相邻碳键合,A 是具有1-7个C原子的烷基,Ar是单环或双环芳族基团,其可以任选地在环中含有N,O或S原子,并且可以被A,Hal,OH,OA单取代,二取代或三取代 ,CF 3,NH 2,NHA,NA 2,NHCOA和/或NHCONH 2,D是CH 2,O,S,NH,NA,-CH 2 -CH 2 - , - CH = CH - , - CH 2 -NH-, - CH 2 - 或键,Hal为F,Cl,Br或I; 和/或生理上可接受的盐和/或其糖基化衍生物之一,和至少一种生理上可接受的赋形剂或辅助剂。

    Use combined 5-HT1A agonists and selective serotonin reuptake inhibitors
    67.
    发明授权
    Use combined 5-HT1A agonists and selective serotonin reuptake inhibitors 有权
    使用组合的5-HT1A激动剂和选择性5-羟色胺再摄取抑制剂

    公开(公告)号:US07479492B2

    公开(公告)日:2009-01-20

    申请号:US10432047

    申请日:2001-11-02

    IPC分类号: A61K31/50 A61K31/4965

    CPC分类号: A61K31/496 A61K31/00

    摘要: The present invention relates to the use of compounds being combined selective serotonin (5-HT) reuptake inhibitors (SSRIs) and 5-HT1A receptor agonists, in particular of 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine or a physiologically acceptable salt thereof or 3-{4-[4-(4-cyano-phenyl)-piperazin-1-yl]-butyl}-1H-indole-5-carbonitrile or a physiologically acceptable salt thereof, for the manufacture of a medicament for the treatment of chronic pain disorders or in treating other conditions where there is hyper-sensitization to painful signals, hyperalgesia, allodynia, enhanced pain perception, and enhanced memory of pain, as well as for the treatment of irritable bowel syndrome (IBS).

    摘要翻译: 本发明涉及化合物是组合的选择性5-羟色胺(5-HT)再摄取抑制剂(SSRI)和5-HT 1A受体激动剂,特别是1- [4-(5-氰基吲哚-3-基)丁基] - 4-(2-氨基甲酰基 - 苯并呋喃-5-基) - 哌嗪或其生理学上可接受的盐或3- {4- [4-(4-氰基 - 苯基) - 哌嗪-1-基] - 丁基} 吲哚-5-腈或其生理上可接受的盐,用于制备用于治疗慢性疼痛障碍或治疗其它对疼痛信号过敏的其他病症,痛觉过敏,异常性疼痛,增强的疼痛感知和增强的药物 记忆疼痛,以及治疗肠易激综合征(IBS)。

    Cleavage system inhibitors as potential antipsychotics
    69.
    发明授权
    Cleavage system inhibitors as potential antipsychotics 失效
    甘氨酸切割系统抑制剂作为潜在的抗精神病药

    公开(公告)号:US06395780B1

    公开(公告)日:2002-05-28

    申请号:US09559831

    申请日:2000-04-28

    IPC分类号: A61K3119

    摘要: The invention relates to inhibitors of the glycine cleavage system and their use as potential antipsychotic agents. The invention relates furthermore to a process for treating humans having psychosis, psychosis associated with an illness, schizophrenia, Alzheimers disease or other related psychotic disorders.

    摘要翻译: 本发明涉及甘氨酸裂解体系的抑制剂及其作为潜在抗精神病药的用途。 本发明还涉及治疗患有精神病,与疾病相关的精神病,精神分裂症,阿尔茨海默病或其它相关精神病的人的方法。