Abstract: Certain peptides which exhibit high selectivity for the kappa opioid receptor (KOR) versus the mu opioid receptor and little or no CYP3A4 inhibitory activity including tetrapeptides of four D-isomer amino acid residues having a C-terminus which is an N-oxide-substituted amide such, as H-D-Phe-D-Phe-D-Nle-D-Arg-NH-4-picolyl-N-oxide.

Abstract: Heptapeptide analogues or pharmaceutically acceptable salts thereof consist of a hexapeptide moiety S and a C-terminal .beta.-aminoalcohol residue Z bound to the moiety S by an amide bond, wherein the .beta.-aminoalcohol Z is --NR--CH(Q)--CH.sub.2 OH, Q is (CH.sub.2).sub.n --NH--A is H or --C(.dbd.NH)NH.sub.2, and R is CH.sub.3 or C.sub.2 H.sub.5, and the moiety S wherein H is a D-aromatic .alpha.-aminoacid and Y is an aliphatic .alpha.-aminoacid and have oxytocin antagonist activity. Also disclosed is: a method of their synthesis; pharmaceutical compositions containing these analogues; the synthesis of such compositions; a method of control of uterine contractions.

Abstract: An artificial peptide having an amino acid sequence which corresponds to a naturally occurring amino acid sequence of a HIV comprising an epitope and which further has two cysteine residues located on each side of said epitope, and further having a sulphur bridge between said two cysteine residues, which has been formed by a chemical oxidation step, is described.Furthermore, an artificial antigen which reacts with antibodies induced by a HIV is described. Said antigen mainly consists of an artificial peptide according to the invention.Additionally, a method of detecting antibodies induced by a HIV in a sample of body fluid, wherein said sample is subjected to an immunoassay, especially ELISA, and wherein an artificial antigen according to the invention is used as a diagnostic antigen, is described. A diagnostic immunoassay kit for said method is also described.Finally, a vaccine composition comprising, as an immunizing component, at least one antigen according to the invention, is described.

Abstract: Peptides which exhibit high selectivity for the kappa opioid receptor (KOR) and long duration of peripheral action without significant entry into the brain are created which are sequences of four D-isomer amino acid residues having a C-terminus which is a mono or di-substituted amide. Representative compounds, which have an affinity for the KOR at least 1,000 times their affinity for the mu opioid receptor and an ED.sub.50 of not greater than about 0.5 mg/kg, includeH-D-Phe-D-Phe-D-Nle-D-Arg-NHEt,H-D-Phe-D-Phe-D-Nle-D-Arg-morpholinyl,H-D-Phe-D-Phe-D-Nle-D-Arg-NH-4-picolyl,H-D-Phe-D-Phe-D-Nle-D-Arg-NHPr,H-D-Phe-D-Phe-D-Nle-D-Arg-thiomorpholinyl,H-D-Phe-D-Phe-D-Nle-D-Arg-NEt.sub.2,H-D-Phe-D-Phe-D-Nle-D-Arg-NHMe,H-D-Phe-D-Phe-D-Leu-D-Orn-morpholinyl,H-D-Phe-D-Phe-D-Nle-D-Arg-NHhEt,H-D-Phe-D-Phe-D-Nle-D-Arg-NH-cyclopropyl,H-D-Ala(2Thi)-D-4Cpa-D-Leu-D-Arg-morpholinyl,H-D-Phe-D-Phe-D-Nle-D-Arg-piperidinyl,H-D-Phe-D-Phe-D-Leu-D-Orn-NHEt,H-D-Phe-D-Phe-D-Leu-D-Lys-morpholinyl,andH-D-Phe-D-Phe-D-Nle-D-Arg-piperazinyl.

Abstract: A peptide of the formula (SEQ ID NO:1) Met Ser Thr Ash Pro Lys Pro Cys Arg Lys Thr Lys Arg Asn Thr Asn Arg Arg Pro Cys Asp Val Lys Phe Pro Gly Gly, Gly wherein there is a disulfide bridge between the two cysteine residues, is described. Further, a diagnostic antigen in carrier-bound form comprising said peptide is disclosed. Said peptide may be used in a method of in vitro diagnosing an active infection caused by hepatitis C virus.

Abstract: Vasopressin analogues of formula (I) ##STR1## wherein X is (S)-2-amino-2-methyl-butanoic acid (CaMeAbu) or Valine (Val), Y is Thienylalanine (Thi) or Methionine (Met), Z is D-Phenylalanine (D-Phe) or D-Thienylalanine (Thi) or D-Tyrosine (D-Tyr), are disclosed. Pharmaceutical preparations comprising a vasopressin analogue of the invention as active ingredient are disclosed and exemplified by oral preparations, nasal preparations, and intravenous preparations. The vasopressin analogues of the invention are intended for use as a medicament, specially an antidiuretic agent. The antidiuretic agent is preferably used for the treatment of diabetes insipidus or enuresis.

Abstract: The present invention relates to new vasotocin derivatives with prolonged activity compared to previous vasotocin derivatives. In particular, the vasotocin derivatives of the present invention are of the formula (I) ##STR1## wherein Hmp is a 2-hydroxy-3-mercaptopropionic acid residue, ##STR2## Z is Phe or Tyr, Y is Hgn or Hci, X is a residue of the formula ##STR3## wherein Q is H, alanyl or L-2-aminobutyryl and n is 1, 2 or 3. The present invention also relates to pharmaceutical compositions containing these vasotocin derivatives.

Abstract: New compounds which are cysteine proteinase inhibitors of the formulaB - A - CwhereinB=Pro-Arg-Leu-Val-Gly-, Arg-Leu-Val-Gly-, Leu-Val-Gly-, or Val-Gly-, or zero; the N-terminal amino acid optionally having a protective group,A=a reactive group capable of specifically reacting with free-SH groups,C=-Gly-Pro-Met-Asp-Ala; -Gly-Pro-Met-Asp; -Gly-Pro-Met; or -Gly-Pro, or zero;with the proviso that B and C are not both zero.

Abstract: Novel vasotocin derivatives having an inhibitory effect on uterine contractions, pharmaceutical compositions containing these derivatives, and the use thereof in the therapeutical treatment of excessive muscle contractions in the uterus and described. The derivatives differ from vasotocin in that the structure of the original hormone has been modified at positions 1, 2 and, optionally, 4 and/or 8. The vasotocin derivatives thus have the formula ##STR1## wherein Mpa is a 3-mercaptopropionoyl residue (--S--CH.sub.2 --CH.sub.2 --CO--);A is the peptide residue of L- or D-tyrosine-O-ethyl ether (in other words, 4-ethoxy-L or D-phenyl alanine, i.e.

Abstract: The invention relates to a method of preparation of 2-aminobutanol from readily available raw materials. The method of this invention is based on the reaction between 1.2-epoxybutane or isomeric butylene halogenehydrines with ammonia. The product, isomeric aminobutanols, are, subsequently transformed into 2-ethylaziridine by means of esterification with sulphuric acid followed by treatment with alkali. 2-Ethylaziridine is then submitted to a reaction with aromatic carboxylic acid or with aromatic orthobicarboxylic acid anhydride which produces the corresponding monomeric or polymeric amide, which is transformed into 2-aminobutanol by hydrolysis.The method of this invention is a multistage one but is quite simple and employs aqueous solutions and organic solvents, such as chloroform or benzene, which may be easily recovered.