Abstract: The invention relates to novel pyrazole derivatives with an ergoline skeleton of the general formula I, ##STR1## wherein x . . . y stands for a ##STR2## R is a hydrogen atom or methyl group, R.sub.1 stands for a hydrogen atom, C.sub.1-4 alkyl, carbethoxy or pyridyl-group,R.sub.2 stands for a hydrogen atom, C.sub.1-4 alkyl, allyl, C.sub.2-4 oxoalkyl-, C.sub.2-4 hydroxyalkyl or C.sub.2-4 hydroxyiminoalkyl group,R.sub.3 stands for a hydrogen atom, C.sub.1-4 alkyl, hydroxy or pyridyl group, furthermoreR.sub.2 and R.sub.3 may stand together for a group of general formula (II), ##STR3## wherein Z stands for a methylene, carbonyl, hydroxymethylene or hydroxyiminomethylene group,R.sub.4 stands for a hydrogen atom or one or two C.sub.1-4 alkyl group(s), andn is 1 or 2,and pharmaceutically acceptable salts thereof.Furthermore the invention relates to a process for the preparation of these compounds.The novel compounds are potent PGF.sub.2.alpha. receptor antagonists.

Abstract: Analgesic compounds having the formula (I):Tyr-A-Gly-Phe-B-X-YwhereinA is a D-aminoacid group having a lower alkyl group or a lower thioalkyl group as a side chain,B is an aminoacid or a cyclic iminoacid group, either of which has a lower alkyl group as a side chain,X is an oxygen atom or an NH group, andY is a hydrogen atom or a lower alkyl group,or a pharmaceutically effective amide, ester or salt thereof.

Abstract: The invention relates to new enkephalin analogues of the general formula (I),Tyr-X-Gly-Phe-Y (I)whereinTyr, Gly and Phe represent L-tyrosyl, glycyl and L-phenylalanyl residue, respectively,X is glycyl residue or a D-.alpha.-aminocarboxylic acid residue with a lower alkyl, lower thioalkyl or phenyl-(lower)-alkyl side chain, andY is the residue of an L, D or DL-.alpha.-aminophosphonic acid or L, D or DL-.alpha.-aminosulfonic acid, each having a lower alkyl side chain,and salts thereof. These compounds are prepared according to the invention so that an L-, D- or DL-.alpha.-aminophosphonic acid or an L-, D- or DL-.alpha.-aminosulfonic acid, each bearing a lower alkyl side chain, is coupled in the proper order, as defined by formula (I), with the amino acids and/or peptide fragments each having a removable protecting group on the terminal amino group, the protecting group is split off from the terminal amino group, and the free peptide is isolated as such or in the form of its salt.