Proline ester and preparation containing the same for...

C - Chemistry – Metallurgy – 07 – K

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C07K 5/062 (2006.01) A61K 9/70 (2006.01) A61K 38/05 (2006.01) A61K 47/14 (2006.01) A61K 47/16 (2006.01) A61P 9/04 (2006.01) A61P 9/12 (2006.01) A61P 43/00 (2006.01) C07K 5/02 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2498757

A proline ester represented by the general formula (I): (I) (wherein R1 represents lower hydroxyalkyl, lower alkyl substituted by lower alkoxy, or lower alkyl substituted by lower alkoxy substituted by lower alkoxy) or a pharmaceutically acceptable salt of the ester. The proline ester (I) and pharmaceutically acceptable salt thereof are useful as a prodrug for enalaprilate, which is a medicine useful in the prevention of and treatments for, e.g., circulatory diseases such as hypertension, cardiac diseases (cardiac hypertrophy, cardiac failure, myocardial infarct, etc.), nephritis, and apoplexy. A medicine containing either of these is suitable for use as a preparation for percutaneous administration, especially an adhesive patch, from the standpoints of medicinal activity and use.

L'invention concerne un ester de proline de formule (I). Dans cette formule, R?1¿ désigne un hydroxyalkyle inférieur, ou un alkyle inférieur substitué par un alcoxy inférieur. L'invention concerne également un sel pharmaceutiquement acceptable de cet ester. L'ester de proline (I) et un sel pharmaceutiquement acceptable de celui-ci sont utiles en tant que promédicament pour l'énalaprilate, qui est un médicament utile pour la prévention et pour les traitements, par exemple, des maladies circulatoires comme l'hypertension, les maladies cardiaques (hypertrophie cardiaque, insuffisance cardiaque, infarctus du myocarde etc.), la néphrite et l'apoplexie. L'invention concerne un médicament contenant l'ester ou le sel de l'invention, lequel médicament étant approprié à une utilisation en tant que préparation pour une administration percutanée, en particulier un patch adhésif destiné à une activité et à une utilisation médicale.

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