公开(公告)号：WO2009130735A1

公开(公告)日：2009-10-29

申请号：PCT/IT2009/000179

申请日：2009-04-21

Applicant: BERNI CANANI, Roberto ,  CALIGNANO Antonio ,  MAZZONI, Orietta (EREDI) ,  CORUZZO, Anna

Inventor： BERNI CANANI, Roberto ,  CALIGNANO Antonio ,  MAZZONI, Orietta (EREDI) ,  CORUZZO, Anna

IPC: C07C231/02 ,  C07C233/31 ,  C07C233/91 ,  C07D295/185 ,  C07D233/86 ,  A61K31/165 ,  A61K31/395 ,  A61P1/12

CPC classification number: C07C231/02 ,  C07C233/31 ,  C07C233/91

Abstract: The invention relates to novel derivatives of short-chain fatty acids, in particular derivatives of butyric acid, useful for all the known clinical applications of the latter, which show physicochemical characteristics suitable for an easy oral administration, being devoid of the unpleasant organoleptic properties that characterise butyrate. The new compounds are amide derivatives which can be synthesised by reaction of the corresponding fatty acid halide with a naturally occurring amino acid, phenylalanine or a suitable derivative thereof, and which are in a poorly hygroscopic, easily weighable form, stable to acids and alkalis and able to release the acid at the small and large bowel level in a constant manner over time. They do not have disagreeable odours and are practically tasteless, thus allowing the manufacture of preparations for oral administration also suitable for the therapy of chronic diseases and in the paediatric field.

Abstract translation: 本发明涉及短链脂肪酸的新衍生物，特别是丁酸的衍生物，其可用于后者的所有已知临床应用，其显示适合于容易口服给药的物理化学特性，没有令人不愉快的感官特性， 表征丁酸盐。 新化合物是酰胺衍生物，其可以通过相应的脂肪酰卤与天然存在的氨基酸，苯丙氨酸或其合适的衍生物的反应合成，并且它们的吸水性差，易于称重的形式，对酸和碱稳定，并且 能够以恒定的方式随着时间的推移在小肠和大肠排出酸。 它们没有不愉快的气味，几乎没有味道，因此允许口服制剂的制备也适用于治疗慢性疾病和儿科领域。