首页> 外国专利> Composite pharmaceutical composition process to treat patients suffering from systemic disorders such as anorexia nausea vomiting feeling abdominal discomfort superior abdominal pain and heartburn caused by gastrointestinal dysfunction use of a compound and process to prepare a compound

Composite pharmaceutical composition process to treat patients suffering from systemic disorders such as anorexia nausea vomiting feeling abdominal discomfort superior abdominal pain and heartburn caused by gastrointestinal dysfunction use of a compound and process to prepare a compound

机译:用于治疗患有全身性疾病如食欲不振,恶心呕吐,腹部不适,上腹部疼痛和胃肠道功能障碍引起的胃灼热的复合药物组合物的方法和化合物的制备方法

摘要

6-Methoxy-1H-benzotriazole-5-carboxamide derivatives which are represented by the formula (I) below: CHEM Äin which R1 stands for ethyl or cyclopropylmethyl group, R2 stands for hydrogen atom, methyl or ethyl group, n is 1, 2 or 3, and the 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)Ü 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 sa 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.
机译:由下式(I)表示的6-甲氧基-1H-苯并三唑-5-羧酰胺衍生物:<化学式>其中R 1代表乙基或环丙基甲基,R 2代表氢原子,甲基或甲基。乙基,n为1、2或3,波浪线(@)表示酰胺部分中与N原子键合的碳原子上的取代基构型为外消旋(RS)或旋光性(R或S )Ü或其药学上可接受的酸加成盐;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。本发明的化合物同时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,作为胃肠动力增强剂,被用于治疗和预防与各种疾病和治疗方法有关的胃肠道功能性疾病。

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