C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 495/10 (2006.01) A61K 31/381 (2006.01) A61K 31/403 (2006.01) A61K 31/538 (2006.01) A61P 1/00 (2006.01) A61P 25/06 (2006.01) C07D 209/88 (2006.01) C07D 265/38 (2006.01) C07D 333/78 (2006.01)
Patent
CA 2617473
It is intended to provide a compound which can be used for preventing and/or treating a disease associated with 5HT2B receptor and 5HT7 receptor, particularly for treating irritable bowel syndrome (IBS) and/or preventing migraine. It was found that an acylguanidine derivative characterized by having a tricyclic structure or a pharmaceutically acceptable salt thereof has a strong antagonism to 5HT2B receptor and 5HT7 receptor. In addition, the compound of the invention having the antagonism to both receptors showed a better pharmacological action compared to the case where an antagonist selective to one of the receptors was solely used. From the above results, the compound of the invention is useful for preventing and/or treating a disease associated with 5HT2B receptor and 5HT7 receptor, particularly for treating irritable bowel syndrome (IBS) and/or preventing migraine.
L~invention entend proposer un composé pouvant s~utiliser pour la prévention et/ou le traitement d~une maladie associée au récepteur 5HT2B et au récepteur 5HT7, notamment pour traiter un syndrome d~intestin irritable (IBS) et/ou prévenir la migraine. Il est apparu qu~un dérivé d~acylguanidine caractérisé en ce qu~il possède une structure tricyclique ou bien sel de celui-ci acceptable pharmaceutiquement, avec un fort antagonisme au récepteur 5HT2B et au récepteur 5HT7. En outre, le composé de l~invention ayant l~antagonisme face aux deux récepteurs présentait une meilleure action pharmacologique comparée au cas de figure utilisant un seul antagoniste sélectif pour l~un des récepteurs. Il ressort des résultats ci-dessus que le composé de l~invention servait à la prévention et/ou au traitement d~une maladie associée au récepteur 5HT2B et au récepteur 5HT7, notamment pour traiter un syndrome d~intestin irritable (IBS) et/ou pour prévenir la migraine.
Akuzawa Shinobu
Harada Koichiro
Itahana Hirotsune
Matsuzawa Takaho
Moritomo Ayako
Astellas Pharma Inc.
Dennison Associates
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