A - Human Necessities – 61 – K
Patent
A - Human Necessities
61
K
A61K 38/00 (2006.01)
Patent
CA 2621262
The present invention is directed to a thio-containing compound inhibiting aminopeptidase P (mAPP or APP), whose natural substrate is bradykinin. The compound allows bradykinin to exert its beneficial effects on the cardiovascular system, to improve renal function, and to improve glucose tolerance and insulin-sensitivity. The present invention is also directed to a pharmaceutical composition comprising the mAPP inhibitor of the present invention and a pharmaceutically acceptable carrier. In another aspect, the present invention is directed to a method of inhibiting bradykinin degradation in a mammalian patient, preferably human, in need of treatment comprising administering to the patient a therapeutically effective amount of an a thio- containing compound of the present invention. The method of the present invention also contemplates the further step of administering to the mammalian patient in need of treatment a therapeutically effective amount of an inhibitor of angiotensin converting enzyme (ACE).
L'invention concerne un composé contenant thio capable d'inhiber l'enzyme, la membrane aminopeptidase P (mAPP, ou APP), dont le substrat naturel est la bradykinine. Le composé est utilisé en tant qu'agent pharmaceutique grâce à l'inhibition de la dégradation de la bradykinine, le composé permettant à la bradykinine d'exercer ses effets bénéfiques sur le système cardiovasculaire, d'améliorer les fonctions rénales et d'améliorer la tolérance au glucose et la sensibilité à l'insuline. L'invention concerne également une composition pharmaceutique comprenant un inhibiteur de mAPP et une porteuse pharmaceutiquement acceptable. Selon un autre aspect de l'invention, un procédé permet d'inhiber la dégradation de la bradykinine chez un patient mammifère, de préférence un humain, nécessitant un traitement comprenant l'administration d'une quantité thérapeutique efficace d'un composé comprenant thio. Le procédé comprend également l'administration au patient d'une quantité efficace d'un inhibiteur de l'enzyme de conversion de l'angiotensine (ACE).
Marks & Clerk
Simmons William H.
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