Benzoic acid compound and use thereof as medicine

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 207/09 (2006.01) A61K 31/395 (2006.01) C07D 205/04 (2006.01) C07D 207/08 (2006.01) C07D 207/12 (2006.01) C07D 207/34 (2006.01) C07D 211/26 (2006.01) C07D 211/34 (2006.01) C07D 223/04 (2006.01) C07D 401/02 (2006.01) C07D 401/12 (2006.01) C07D 403/02 (2006.01) C07D 403/06 (2006.01) C07D 403/12 (2006.01) C07D 405/02 (2006.01) C07D 405/12 (2006.01) C07D 409/02 (2006.01) C07D 409/12 (2006.01) C07D 413/02 (2006.01) C07D 413/06 (2006.01) C07D 413/12 (2006.01) C07D 417/02 (2006.01) C07D 419/06 (2006.01) C07D 4

Patent

CA 2186623

Benzoic acid compounds of the formula Image (I) wherein each symbol is as defined in the specification, optical isomers thereof and pharmaceutically acceptable salts thereof; pharmaceutical composition comprising this compound and pharmaceutically acceptable additive; and serotonin 4 receptor agonists, gastrointestinal prokinetic agents and therapeutic agents for various gastrointestinal diseases, which comprise this compound as active ingredient. The compounds of the present invention selectively activate serotonin 4 receptor, and are useful medications for the prophylaxis and treatment of various gastrointestinal diseases (e.g., delayed gastric emptying, indigestion, meteorism, reflux esophagitis, abdominal indefinite complaint, intestinal pseudoileus constipation, acute or chronic gastritis, gastric or duodenal ulcer, Crohn's disease, non-ulcer dyspepsia, ulcerative colitis, postgastrectomy syndrome, postoperative digestive function failure, gastrointestinal injury due to gastric neurosis, gastroptosis, diabetes, etc., and irritable bowel syndrome), central nervous disorders (e.g., schizophrenia, depression, anxiety, disturbance of memory and dementia), cardiac function disorders (e.g., cardiac failure and myocardial ischemia), urinary diseases (e.g., dysuria caused by urinary obstruction, ureterolith or prostatomegaly) and the like.

Composé d'acide benzoïque représenté par la formule générale (I): (dans laquelle chaque symbole est tel que défini dans le descriptif); isomère optique ou sel pharmaceutiquement acceptable de cet isomère; composition médicinale renfermant le composé et les principes actifs pharmaceutiquement acceptable; et agoniste du récepteur 4 de la sérotonine, stimulateur des fonctions digestives et remède des maladie digestives, renfermant le composé comme principe actif. Ce composé exerce une action agoniste contre les récepteurs 4 de la sérotonine et se révèlent utiles comme médicament pour la prévention et le traitement des maladies digestives (comme l'excrésion gastrique retardée, les troubles de la digestion, le tympanisme, l'oesophagite à reflux, les douleurs abdominales diffuses, l'iléus paralytique, la constipation, les gastrites aigues et chroniques, l'ulcère gastro-duodénal, le syndrome de Crohn, la dyspepsie non ulcéreuse, la colite ulcéreuse, le syndrome post gastrectomique, les troubles postanesthésiques du système digestif, la gastroptose, les perturbations gastro intestinales causées par le diabète ou une maladie similaire et la fragilité des intestins), les troubles du système nerveux central (tels que la schizophrénie, la dépression, l'anxiété, les troubles de la mémoire et la démence), les perturbations des fonctions cardiaques (tels que l'insuffisance cardiaque et l'ischémie du myocarde) et des troubles urologiques (tels que l'obstruction urinaire, les calculs de l'urètre et la difficulté à uriner liés à la prostatomégalie).

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