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FATTY ACID DERIVATIVES FOR ORAL ADMINISTRATION ENDOWED WITH HIGH PALATABILITY
专利权人:
ROBERTO BERNI CANANI;ANTONIO CALIGNANO;ANNA CORUZZO;ORIETTA (EREDI) MAZZONI
发明人:
CORUZZO, ANNA,CALIGNANO ANTONIO,BERNI CANANI, ROBERTO,MAZZONI, ORIETTA (EREDI
申请号:
NZ58937209
公开号:
NZ589372A
申请日:
2009.04.21
申请国别(地区):
NZ
年份:
2013
代理人:
摘要:
589372 Disclosed are N-(1-carbamoyl-2-phenyl-ethyl)butyramide derivatives selected from N-(1-carbamoyl-2-phenyl-ethyl)butyramide; N-(1-butyroyl-carbamoyl-2-phenyl-ethyl)butyramide; 5-benzyl-2-propyl-1H-imidazol-4(5H)-one; N-(1-oxo-3-phenyl-1-(piperidin-1-yl)propan-2-yl)butyramide; N-(1-oxo-3-phenyl-1-(pyrrolidin-1-yl)propan-2-yl)butyramide; N-(1-(methylcarbamoyl)-2-phenylethyl)butyramide; N-(1-(ethylcarbamoyl)-2-phenylethyl)butyramide; N-(1-(propylcarbamoyl)-2-phenylethyl)butyramide; N-(1-(butylcarbamoyl)-2-phenylethyl)butyramide; N-(1-(pentylcarbamoyl)-2-phenylethyl)butyramide; N-(1-carbamoyl-2-phenylethyl)-N-methylbutyramide; N-(1-carbamoyl-2-phenylethyl)-N-ethylbutyramide; and N-(1-carbamoyl-2-phenylethyl)-N-propylbutyramide; and corresponding mixtures and salts of pharmaceutically acceptable bases or acids, pure diastereoisomeric forms and enantiomeric forms or mixtures thereof. Also disclosed is a process for the preparation of the above compounds and their mixtures comprising the stages of reacting a phenylalanine derivative and a butyroyl derivative, in substantially equimolecular amounts, in an aprotic polar or inert organic solvent at room temperature, separating, and purifying the product obtained. Further disclosed is the use of one or more compounds having the general formula (I) wherein: A represents a straight or branched alkyl chain, possibly substituted with phenyl; X represents nitrogen; R and R1 independently represent hydrogen or an alkyl group or a acyl group and W is nil; or W represents a 1,2-alkylene chain with 2 to 6 carbon atoms and R and R1 are methylene groups; R2 represents hydrogen or an alkyl group or an acyl group; R3 is selected from the group consisting of H, alkyl, alkoxyl, halogen, oxidryl, cyano, nitro, amino, mono- or di-alkylamino, acylamino, formyl, hydroxyiminomethyl, alkoxyiminomethyl and carbamoyl; corresponding salts with pharmaceutically acceptable bases or acids thereof, pure diastereoisomeric forms and enantiomeric forms
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