Cyclic amine-1-carboxylic acid ester derivative and pharmaceutical composition containing the same
    6.
    发明授权
    Cyclic amine-1-carboxylic acid ester derivative and pharmaceutical composition containing the same 有权
    环状胺-1-羧酸酯衍生物和含有它的药物组合物

    公开(公告)号:US08367835B2

    公开(公告)日:2013-02-05

    申请号:US12991224

    申请日:2009-05-07

    IPC分类号: A61K31/445 C07D211/26

    CPC分类号: C07D205/04

    摘要: Provided is a compound useful as a therapeutic drug for pain and inflammation caused by various pathological conditions such as neuropathic pain and rheumatoid arthritis. The compound of the formula (I) or a salt thereof [wherein R1 is a methyl group or a hydrogen atom, R2 represents a hydrogen atom, an alkyl group, an alkylcarbonyl group or an aryl carbonyl group, A represents a cycloalkyl group, a cycloalkenyl group, an aryl group or a heteroaryl group (each group may be substituted with a substituent selected from the group consisting of alkyl, alkenyl, cycloalkyl and halogen), n and m each represent an integer of 1, 2 or 3, and p represents an integer of 0, 1, 2 or 3].

    摘要翻译: 提供作为用于由各种病理状况如神经性疼痛和类风湿性关节炎引起的疼痛和炎症的治疗药物的化合物。 式(I)化合物或其盐[其中R 1是甲基或氢原子,R 2表示氢原子,烷基,烷基羰基或芳基羰基,A表示环烷基, 环烯基,芳基或杂芳基(各基团可以被选自烷基,烯基,环烷基和卤素的取代基取代),n和m各自表示1,2或3的整数,p 表示0,1,2或3的整数]。

    6-methoxy-1H-benzotriazole-5-carboxamide derivatives and pharmaceutical
compositions containing them
    9.
    发明授权
    6-methoxy-1H-benzotriazole-5-carboxamide derivatives and pharmaceutical compositions containing them 失效
    6-甲氧基-1H-苯并三唑-5-甲酰胺衍生物和含有它们的药物组合物

    公开(公告)号:US5932568A

    公开(公告)日:1999-08-03

    申请号:US849415

    申请日:1997-05-21

    CPC分类号: C07D403/12

    摘要: 6-Methoxy-1H-benzotriazole-5-carboxamide derivatives which are represented by the formula (I) below: ##STR1## �in which R.sup.1 stands for ethyl or cyclopropylmethyl group, R.sup.2 stands for hydrogen atom, methyl or ethyl group,n is 1, 2 or 3, andthe wavy line () signifies that configuration of the substituents on the carbon atom bound to the N-atom in the amide moiety is racemic (RS) or optically active (R or S)!or their pharmaceutically acceptable acid addition salts; processes for their preparation; pharmaceutical compositions containing a compound of formula (I) or its pharmaceutically acceptable acid addition salt; and novel intermediates. The compounds of the present invention possess concurrently excellent antiemetic activity and gastrointestinal motility enhancing activity. They furthermore exhibit less central nervous system (CNS) depressant activity and, therefore, are used for treatments and prophylaxis of functional disorders of gastrointestinal tract associated with various diseases and therapeutical treatments, as gastrointestinal motility enhancing agent.

    摘要翻译: PCT No.PCT / JP95 / 02310 Sec。 371日期1997年5月21日 102(e)日期1997年5月21日PCT提交1995年11月13日PCT公布。 公开号WO96 / 16059 日期:1991年5月30日 - 由以下式(I)表示的甲氧基-1H-苯并三唑-5-甲酰胺衍生物:其中R1代表乙基或环丙基甲基,R2代表氢原子,甲基或乙基,n 是1,2或3,波浪线(+ Z)表示与酰胺部分中的N-原子结合的碳原子上的取代基的构型是外消旋(RS)或光学活性(R或S)]或 其药学上可接受的酸加成盐; 其准备过程; 含有式(I)化合物或其药学上可接受的酸加成盐的药物组合物; 和新型中间体。 本发明的化合物具有优异的止吐活性和胃肠蠕动增强活性。 它们还表现出较少的中枢神经系统(CNS)抑制活性,因此用作治疗和预防与各种疾病和治疗治疗相关的胃肠道功能障碍作为胃肠蠕动增强剂。

    Indazole-3-carboxylic acid derivatives
    10.
    发明授权
    Indazole-3-carboxylic acid derivatives 失效
    吲唑-3-羧酸衍生物

    公开(公告)号:US5017573A

    公开(公告)日:1991-05-21

    申请号:US384766

    申请日:1989-07-25

    摘要: An indazole-3-carboxylic acid derivative represented by the following general formula (I) or its physiologically acceptable acid addition salt or quaternary ammonium salt, ##STR1## wherein Y represents --NH-- or --O--; R.sub.1 and R.sub.2 are identical or different and each represents a hydrogen atom, a lower alkyl group, a substituted lower alkyl group, a cycloalkyl group, a lower alkenyl group, a cycloalkenyl group, a lower alkynyl group, an unsubstituted or substituted aryl-lower alkyl group, a lower alkoxycarbonyl group, an unsubstituted or substituted aralkyloxycarbonyl group or an acyl group, or R.sub.1 and R.sub.2, taken together, form a lower alkylene group; R.sub.3 represents a hydrogen atom, a lower alkyl group, or a phenyl group; R.sub.4 represents a hydrogen atom, a lower alkyl group, a substituted lower alkyl group, a cycloalkyl group, a lower alkenyl group, a cycloalkenyl group, a lower alkynyl group, an unsubstituted or substituted aryl-lower alkyl group, a lower alkoxycarbonyl group, an unsubstituted or substituted aralkyloxycarbonyl group or an acyl group; R.sub.5 represents a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group, a hydroxyl group, a trifluoromethyl group, a nitro group, an amino group or an acylamino group; m represents a number of 1, 2, 3 or 4; n represents a number of 1, 2 or 3; and p represents a number of 1, 2, 3 or 4.This compound is useful as a potent and selective antagonist of serotonin 3 (5--HT.sub.3) receptor.