4-AMINO-3-HYDROXY-4-SUBSTITUTED BUTANOIC ACIDS AND 5-AMINO-2,5-DISUBSTITUTED-4-HYDROXYPENTANOIC ACIDS AND PHARMACEUTICAL COMPOSITIONS

摘要

4-Amino-5-cyclohexyl-3-hydroxypentanoic or 5-amino-6-cyclohexyl-4-hydroxyhexanoic acid derivs. of formula (I) and their salts are new, where A = indolyl, 2,3-dihydroindolyl, benzofuranyl, 2,3-dihydrobenzo(b)pyranyl, 2-oxobenzo(b)pyranyl, 2-benzimidazolyl, benzo(1,4)dioxan-2-yl; benzo(1,3)dioxanyl or 1,2,3,4-tetrahydroisoquinolinyl; n = 0 or 1; B = Me, n-Pr or 1H-imidazol-5-ylmethyl; D = 2-carboxy-1-pyrrolidinyl, OR or NHR; R = 1-6C alkyl or phenyl, both opt. substd. by NH2, OH, COOH or 2-7C alkoxycarbonyl, provided that R is not CH2NH2 or CH2OH; Y = i-Bu or allyl. - Intermediates of formula (II) and (III) are also new (see 'Preparation'). - (I) may be prepd. by conventional peptide synthesis methods, e.g. via intermediates of formula (II) and/or (III). In (II) and (III) D1 = 1-6C alkoxy, benzyloxy or OH.