Abstract: Disclosed are monocyclic compounds containing four bifunctional residues linked together via peptide or pseudopeptide bonds of the general formula (I): having tachykinin receptor antagonist activity. In particular, compounds of formula I are shown to be neurokinin-2 (NK-2) antagonists useful in the treatment or prevention of disorders of the central nervous system, inflammatory diseases, asthma, or pain.

Abstract: A process for the preparation of polymorph A of zofenopril calcium salt in substantially pure form, which comprises: a) reaction of S(−)-3-benzoylthio-2-methylpropanoic acid chloride with cis-4-phenylthio-L-proline in water at pH ranging from 9.0 to 9.5 and recovery of zofenopril in the acidic form; b) salification of acid zofenopril with a potassium salt in alcoholic solution, and recovery of the resulting potassium salt; c) conversion of the potassium salt to the calcium salt by addition of a zofenopril potassium salt aqueous solution to a CaCl2 aqueous solution at a temperature of 70-90° C. with simultaneous seeding to promote the precipitation of polymorph A.

Abstract: A process for the preparation of polymorph A of zofenopril calcium salt in substantially pure form, which comprises: 1) reaction of S(−)-3-benzoylthio-2-methylpropanoic acid chloride with cis-4-phenylthio-L-proline in water at pH ranging from 9.0 to 9.5 and recovery of zofenopril in the acidic form; b) salification of acid zofenopril with a poyassium salt in alcoholic solution, and recovery of the resulting potassium salt; c) conversion of the potassium salt to the calcium salt by addition of zofenopril potassium salt aqueous solution to a CaCl2 aqueous solution at a temperature of 70-90° C. with simultaneous seeding to promote the precipitation of polymorph A.

Abstract: A process for the preparation of polymorph A of zofenopril calcium salt in substantially pure form, which comprises: 1) reaction of S(-)-3-benzoylthio-2-methylpropanoic acid chloride with cis-4-phenylthio-L-proline in water at pH ranging from 9.0 to 9.5 and recovery of zofenopril in the acidic form; b) salification of acid zofenopril with a potassium salt in alcoholic solution, and recovery of the resulting potassium salt; c) conversion of the potassium salt to the calcium salt by addition of zofenopril potassium salt aqueous solution to a CaCl2 aqueous solution at a temperature of 70-90° C. with simultaneous seeding to promote the precipitation of polymorph A.

Abstract: A process is provided for producing delphinidin which comprises reacting a compound of formula ##STR1## wherein each Pg represents a hydroxyl protecting group, and Lg represents a leaving group with a compound of formula ##STR2## wherein Pg' represents a hydroxyl protecting group characterized in that the compound of formula VII is produced from an intermediate of formula ##STR3## wherein each Pg" represents a hydroxyl protecting group and each Alk represents lower alkyl, by(i) subjecting the intermediate of formula IX to hydrolysis and decarboxylation to form 3,4,5-trihydroxyacetophenone of formula ##STR4## (ii) converting the 3,4,5-trihydroxyacetophenone to the compound of formula VII by introduction of the protecting groups Pg" and converting the group of formula --COCH.sub.3 to a group of formula --COCH.sub.2 Lg.

Abstract: Novel water-soluble derivatives of silybin of enhanced activity are provided as well as methods of preparing the derivatives and pharmaceutical compositions containing them. The novel derivatives according to the invention have the following general formula (I); ##STR1## where: R=H or PO(OH).sub.2 and R'=PO(OH).sub.2 The compounds of the invention are useful inter alia in therapy of liver disorders and other applications where an anti-radical effect is required. They have the advantages of high hydrophilicity and are soluble at approximately pH 4, compared to prior art compounds which are water-soluble only at higher pH and enhanced stability.

Abstract: Benzoyoxyacetic acid derivatives of formula (I) ##STR1## wherein M denotes hydrogen or one equivalent of a pharmaceutically acceptable inorganic or organic cation are useful as analgesics and anti-inflammatory agents. A novel process for their preparation is also disclosed along with novel intermediates.