Abstract: The invention relates to peptides of the formula IR.sup.4 -A.sup.5 -A.sup.6 -A.sup.7 (I)in which R.sup.4 denotes an acyl group, R.sup.5 denotes D-Lys or Lys, A.sup.6 denotes the radical of phenylalanine, N-methylphenylalanine, 4-alkoxyphenylalanine or 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid, and R.sup.7 denotes a basic radical, processes for their preparation and their use.

Abstract: The invention relates to a process for resolving racemic mixtures of bicyclic imino-.alpha.-carboxylic esters into the components by crystallization of diastereomeric salts, which comprises preparing the salts of the racemic esters with optically active N-acylated R- or S-aminocarboxylic acid which contain a phenyl nucleus, recrystallizing them from an organic solvent, decomposing the precipitated, optically homogeneous diastereomeric salts in a manner known per se, and isolating the enantiomers and, where appropriate, converting the latter into the free acids by hydrolysis in a manner known per se. The invention also relates to optically pure compounds of the formula ##STR1## and to diastereomeric salts of these compounds, in which two of the radicals A, B.sup.1, B.sup.2 and C form a carbon chain and the others denote hydrogen, and R is an esterifying group.

Abstract: The invention relates to a process for the preparation of peptides of the general formulaArg--Lys--S--Val--Yin which S denotes glutamic acid or .alpha.-aminoadipic acid and Y denotes tyrosine or tryptophan or esters or amides thereof, which comprises subjecting tetrapeptides of the formulaZ--Arg(Z'.sub.2)--Lys(Z')--S--(Bzl)--Val--OHin which Z' represents a protective group of the benzyl type, to a condensation reaction with corresponding tyrosine esters or amides or tryptophan esters or amides and removing the protective groups by hydrogenation. The invention furthermore relates to tetrapeptides as intermediate products of this process.

Abstract: The invention relates to a process for the preparation of insulins from analogs of preproinsulins, which comprises reacting preproinsulin analogs, at a pH below the isoelectric point of the insulins in the presence of trypsin or a trypsin-like endopeptidase, with an ester of natural amino acids or their derivatives and then cleaving off the ester group and other protective groups which may optionally be present.

Abstract: Compounds of the formula I ##STR1## in which n denotes 0-3,R.sup.1 and R.sup.1' are the same or different and denote hydrogen, alkyl or alkenyl, phenyl or benzyl, each substituted as desired;R.sup.2 denotes hydrogen, alkyl or alkenyl;R.sup.3 denotes hydrogen, alkyl, hydroxyalkyl, alkoxyalkyl or aminoalkyl, alkanoylaminoalkyl, guanidinoalkyl, imidazolylalkyl, indolylalkyl, mercaptoalkyl or alkylthioalkyl, phenylalkyl, hydroxphenylalkyl, phenoxyalkyl or phenylthioalkyl, or R.sup.2 and R.sup.3, together with the C and N atoms carrying them, denote a saturated or unsaturated 4- to 8-membered monocyclic or 8- to 10-membered bicyclic isocycle or heterocycle, optionally monosubstituted or disubstituted by hydroxyl, alkoxy having 1 to 3 C atoms or alkyl,R.sup.4 denotes hydrogen, alkyl, alkenyl, alkadienyl, alkinyl, alkeninyl or alkadiinyl, cycloalkyl, phenyl, benzyl, phenethyl or phenylpropyl, each of which can be optionally monosubstituted or disubstituted;R.sup.5 denotes hydrogen or alkyl, hydroxyl or alkoxy andR.

Abstract: The invention relates to peptides of the formula IR.sup.4 --A.sup.5 --A.sup.6 --A.sup.7 (I)in which R.sup.4 denotes an acyl group, R.sup.5 denotes D-Lys or Lys, A.sup.6 denotes the radical of phenylalanine, N-methylphenylalanine, 4- alkoxyphenylalanine or 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid, and R.sup.7 denotes a basic radical, processes for their preparation and their use.

Abstract: The invention relates to cyclic hexapeptides of the general formula III ##STR1## in which X represents the radical of an L-aminoacid of the general formula IIIa ##STR2## in which A and B are identical or different and denote alkyl having 1 to 3 carbon atoms, or A and B together represent a saturated, unsaturated or aromatic monocyclic or bicyclic structure having 3 to 6 carbon atoms, n denotes 0 or 1, and Y represents an aliphatic or aromatic L-aminoacid the side chain of which can be hydroxylated, and their salts with physiologically tolerated acids, and to a process for their preparation and their use and their intermediates.

Abstract: What are disclosed are indole, quinoline and isoquinoline compounds of the formula ##STR1## in which n denotes 0 or 1, m denotes 1 or 2, but (n+m).ltoreq.2, A together with the bridgehead carbon atoms denotes a benzene or a cyclohexane ring, Y.sub.1 denotes hydrogen, lower alkanoyl or lower cycloalkanoyl, benzoyl nicotinoyl or a radical of the formula II, and Y.sub.2 denotes methyl, amino, lower alkanoylamino, lower cycloalkanoylamino, benzoylamino or nicotinoylamino, and salts thereof, useful as hypotensive agents, and methods for making the same.

Abstract: Compounds of the formula I ##STR1## in which n denotes 0-3,R.sup.1 and R.sup.1' are the same or different and denote hydrogen, alkyl or alkenyl, phenyl or benzyl, each substituted as desired;R.sup.2 denotes hydrogen, alkyl or alkenyl;R.sup.3 denotes hydrogen, alkyl, hydroxyalkyl, alkoxyalkyl or aminoalkyl, alkanoylaminoalkyl, guanidinoalkyl, imidazolylalkyl, indolylalkyl, mercaptoalkyl or alkylthioalkyl, phenylalkyl, hydroxyphenylalkyl, phenoxyalkyl or phenylthioalkyl, or R.sup.2 and R.sup.3, together with the C and N atoms carrying them, denote a saturated or unsaturated 4- to 8-membered monocyclic or 8- to 10-membered bicyclic isocycle or heterocycle, optionally monosubstituted or disubstituted by hydroxyl, alkoxy having 1 to 3 C atoms or alkyl,R.sup.4 denotes hydrogen, alkyl, alkenyl, alkadienyl, alkinyl, alkeninyl or alkadiinyl, cycloalkyl, phenyl, benzyl, phenethyl or phenylpropyl, each of which can be optionally monosubstituted or disubstituted;R.sup.5 denotes hydrogen or alkyl, hydroxyl or alkoxy andR.

Abstract: A peptide of the formulaB.sub.1 --B.sub.2 --A.sub.1 --A.sub.2 --Xin whichB.sub.1 denotes a basic aminoacid,B.sub.2 denotes a basic aminoacid,A.sub.1 denotes an aromatic aminoacid,A.sub.2 denotes an aromatic aminoacid andX denotes an aminoacid in which the carboxyl group can be esterified, a process for the preparation thereof and the use thereof.

Abstract: The invention provides a nonapeptide of the formula IGlu-Asp-Ser-Ser-Ser-Thr-Gly-Trp-Asn-OH (I)a process for the preparation thereof and its use, furthermore intermediates for preparing a compound of the formula I.

Abstract: New peptide amides of the formula IH--Tyr--D--Lys(For)--Gly--X (I)whereinFor is formyl,X is alkylamino, dehydro-Phe or Phe-alkylamido having up to 6 carbon atoms in the alkyl moiety, which moiety may be substituted by hydroxy and/or phenyl, Phe-cycloalkylamide or Phe-cycloalkylene amide having up to 8 carbon atoms in the cycloalkyl or cyclalkylene moiety, 1 to 2 CH.sub.2 groups being optionally replaced by --NH--, --O--, --S-- or --CO--, Phe-alkylene-cycloalkylamide having from 5 to 6 ring carbon atoms, which amide may be substituted by carbonamido,N-alkylcarbonamido or alkyl and 1 carbon atom whereof may be replaced by nitrogen, Phe-endo- or exo-norbornylamide or Phe-thiazolamide or Phe-thiazolidine-carboxylic acid amide, which may be substituted by 1 to 4 methyl groups each,and process for their manufacture are disclosed. These peptide amides are distinguished by an analgetic activity and suppress the motility of the ileum of the guinea pig.

Abstract: What are disclosed are chromogenic peptides useful as substrates for the detection and determination of enzymes having a hydrolytic action and methods for detecting and determining enzymes with such peptides.

Abstract: What are disclosed are pentapeptides, useful for influencing the maturing of T-lymphocytes, of the formulaG--K--Q--X--MwhereinG is arginine, lysine, ornithine, or homoarginine, or is an unsubstituted or substituted .omega.-aminoalkanoyl, .omega.-guanidinoalkanoyl, or .omega.-dimethylaminoalkanoyl;K is a basic amino acid such as lysine, arginine, homoarginine, or ornithine;Q is L- or D-glutamic acid, d-aspartic acid, or D-.alpha.-aminoadipic acid;X is L-valine or L-isoleucine; andM is an L- or D-aminoacid having a hydrophobic side chain, or an ester or amide of such an acid.

Abstract: What are disclosed are a nonapeptide of the formula ##STR1## wherein D-Aad (OBu.sup.t) represents D-.alpha.-aminoadipic acid .delta.-tert. butyl ester, methods for making this peptide, pharmaceutical preparations containing this peptide, and methods for its use in increasing fertility or for contraception.

Abstract: What are disclosed are secretin preparations with an intensified and protracted action, especially subcutaneously and rectally administrable preparations containing phenolic depot bodies. A process for the manufacture of the preparations and their use as well as phenolic depot bodies and the manufacture thereof are described.

Abstract: What is disclosed is a method for the manufacture of LH-RH and LH-RH analogs, which comprises reacting Glu-His(DnP)-OH with the corresponding peptide having a free amino group and protected carboxy groups in a solvent as used in peptide chemistry and with the addition of 3-hydroxy-4-oxo-3,4-dihydro-1,2,3-benzotriazine (HOObt) and a carbodiimide and then splitting off the Dnp-(2,4-dinitrophenyl) group. The new method greatly reduces the degree of histidine racemization. The invention also provides a new dipeptide, i.e. Glu-His(Dnp)-OH.

Abstract: A peptide with LH-RH-activity which is a LH-RH-peptide wherein Gly in 6-position is replaced by D-glutaminic-acid which may be N-substituted at the CO-NH.sub.2 moiety, wherein in 10-position Gly-NH.sub.2 may be replaced by a NH-alkyl or NH-cycloalkyl group and/or wherein the amino acids in 4-, 5-, 7- and/or 8-position may be replaced by other amino acids and a process for its manufacture.

Abstract: A process for the purification of secretin by chromatography on an alkylated dextran gel is disclosed, as is a method of its manufacture appropriate for preparing larger amounts of secretin.

Abstract: A process for manufacture of insulin, analogs and derivatives thereof by treating an insulin compound wherein the A- and B-chains are linked by a bis-methionyl-carbonyl-bridge, with cyano bromide.