Abstract: Analogs of rCRF and oCRF are disclosed that can be administered to achieve a substantial elevation of ACTH, .beta.-endorphin, .beta.-lipotropin, other products of the pro-opiomelanocortin gene and corticosterone levels and/or a lowering of blood pressure over an extended period of time. One analog which has been found to be particularly potent is: H-Ser-Gln-Glu-Pro-Pro-Ile-Ser-Leu-Asp-Leu-Thr-Phe-His-Leu-Leu-Arg-Glu-Met- Leu-Glu-Met-Ala-Lys-Ala-Glu-Gln-Glu-Ala-Glu-Gln-Ala-Ala-Leu-Asn-Arg-Leu-Leu -Leu-Glu-Glu-Ala-NH.sub.2. In the analogs, one or more of the first five N-terminal residues may be deleted or may be substituted by a peptide up to 10 amino acids long and/or by an acylating agent containing up to 7 carbon atoms. A number of other substitutions may also be made throughout the chain. These analogs or pharmaceutically or veterinarily acceptable salts thereof, dispersed in a pharmaceutically or veterinarily acceptable liquid or solid carrier, can be administered to mammals, including humans.

Abstract: Peptides of the formula Tyr.sup.1 -X-A-Pro-B-Pro-C-Pro-D, in which Tyr.sup.1 is equal to the amino acid tyrosine and Pro is equal to the amino acid proline; A, B, C, D is any desired amino acid in the L-form and X any amino acid in the D-form, except D-proline, D-alanine, D-threonine and D-valine, preferably D-serine, D-arginine or D-methionine; they act opiate-like and may be used as medicaments and animal medicaments.

Abstract: Pharmaceutical compositions for sustained release of pharmaceutical compounds comprising a reaction product of a water soluble salt of a pharmaceutically active compound containing a primary, secondary or tertiary amino group, and an alkali or ammonium salt of a synthetic copolymer containing an acid group, and selected from the group consisting of methacrylic acid/methacrylic acid methyl ester, methacrylic acid/acrylic acid methyl ester and methacrylic acid/acrylic acid methyl ester/methacrylic acid methyl ester copolymers and a pharmaceutically acceptable excipient. The water soluble salt of a pharmaceutically active compound containing a primary, secondary or tertiary amino group is reacted in aqueous medium with an alkali or ammonium salt of a copolymer selected from the group consisting of the above mentioned copolymers, and the resulting product is converted into a pharmaceutical composition.

Abstract: Pharmaceutical compositions of sulfonamide and sulfonamide-potentiator are disclosed. These compositions, which are suitable for injection administration, comprise an aldehyde in addition to the sulfonamide and its potentiator.

Abstract: Heat-stable composition, destined to emit insecticidal vapors by being heated, which contains at least one insecticidal substance of the family of pyrethrinoids, a stabilizer chosen from among the compounds defined by the chemical formula ##STR1## in which R represents one or two optional alkyl radicals containing one to twelve carbon atoms, R' and R", alike or different, represent each an alkyl radical containing one to eighteen carbon atoms, R' and R" together can represent a divalent saturated hydrocarbon group containing two to seven carbon atoms, and R'" represents a hydrogen atom or an alkyl radical containing one to seven carbon atoms; and, optionally, an adjuvant inert to the insecticide and chosen from among diluents, thickening agents, perfumes, synergists, colorants, repellants, solid supports and comburants.

Abstract: A method of releasing a functional group present in an amino acid or amino acyl residue from a resin or protecting residue which is bonded to the functional group by a linkage having proton affinity, which comprises: reacting the functional group bonded to the organic residue, with a mixture of HF and a base for a time and under conditions effective to produce the release; wherein the amounts of HF and base in the mixture are adjusted so that said release occurs substantially by an S.sub.N 2 mechanism.

Abstract: Novel cyclic pentapeptide somatostatin antagonists and method for increasing the release of growth hormone, insulin, and glucagon in mammals are described.

Abstract: This invention relates to novel peptides, of pharmacological activity, of the formula: ##STR1## wherein R.sup.1 is heptanoyl, stearoyl, 2-hydroxypropionyl or 2-acetoxypropionyl,R.sup.2 is hydrogen or methyl,R.sup.3 is carboxy, benzyloxycarbonyl or hydroxymethyl,R.sup.4 is hydrogen or methyl,R.sup.5 is carboxy or hydroxymethyl,R.sup.6 is carboxy, methoxycarbonyl, 3-t-butoxycarbonylcarbazoyl or hydroxymethyl,R.sup.7 is hydrogen, 3-t-butoxycarbonyl or benzyloxycarbonyl, andn is an integer 0 or 1, with the proviso that when each of R.sup.3 and R.sup.6 is not simultaneously hydroxymethyl, then R.sup.5 is hydroxymethyl.

Abstract: A rodenticide is disclosed comprising an encapsulated zinc phosphide toxicant, a bait, and a binder for adhering the encapsulated zinc phosphide to the bait, said binder comprising a polyol or a sugar-containing fluid. The encapsulant is a thermoplastic polyamide, preferably nylon, present in an amount of from about 2% to about 10% by weight of zinc phosphide. When the bait is a grain or a processed grain, a zinc salt is preferably added to the rodenticide to inhibit the generation of phosphine. Histamine, a histamine salt or a histamine-producing substance, such as red pepper, can also be added to the rodenticide to stimulate acid secretion in the stomach of the rodent.A particulate encapsulated product is also disclosed comprising a core of zinc phosphide having a coating of a thermoplastic polyamide present in the range of from about 2% to about 10% by weight. The encapsualted product is a small particle capable of passing through a 40 mesh size screen.

Abstract: A process for recovering a dipeptide derivative comprises admixing an aqueous mixture of a solid dipeptide ester derivative of the formula ##STR1## wherein R.sub.1 is a lower alkyl group, R.sub.2 is a side chain group of an amino acid, n is 1 or 2, X is a benzyloxycarbonyl group which can have a nuclear substituent and Y is a hydrogen ion or an ammonium derivative ion of the formula ##STR2## wherein R.sub.3 is a side chain group of an amino acid and R.sub.4 is a lower alkyl group with an organic solvent capable of forming a binary phase system with water; said solvent being present in an amount effective to obtain the transfer of said peptide in the form of a solid from the aqueous phase to the organic solvent phase, settling the resulting admixture to form(1) an organic solvent phase containing in a solid state a substantial amount of dipeptide derivative of the formula ##STR3## wherein R.sub.1, R.sub.

Abstract: The invention relates to novel peptides and their pharmaceutically acceptable salts, particularly useful for pharmaceutical purposes such as in the therapeutic treatment of infectious diseases caused by pathogenic microorganisms. The compounds have the structure ##STR1## wherein R.sup.1 is hydrogen or acyl;R.sup.2 is carboxy or protected carboxy or a group of the formula: --COHN--R.sub.a.sup.2 wherein R.sub.a.sup.2 is carboxy (lower) alkyl or protected carboxy (lower) alkyl;R.sup.3 is carboxy, protected carboxy, lower alkyl, hydroxyphenyl, carbamoyl or a group of the formula: ##STR2## wherein R.sub.a.sup.3 is hydrogen, amino, protected amino or acylamino, R.sub.b.sup.3 is carboxy or protected carboxy,R.sup. is carboxy, protected carboxy, carbamoyl, carboxy (lower) alkyl or protected carboxy (lower) alkyl;l is an integer 2,m is an integer 0 to 2 andn is an integer 1, provided that, whenR.sup.1 is hydrogen or acyl,R.sup.2 is carboxy, protected carboxy or a group of the formula: --CONHR.sub.a.sup.2 wherein R.

Abstract: Compounds of the formula: ##STR1## wherein R.sup.1 and R.sup.2 stand for alk-2-enyl radicals of not more than 6 carbon atoms, A stands for Gly or Azgly, B stands for Leu or Met, J stands for --(CH.sub.2).sub.n --, wherein n stands for an integer from 1 to 10, or a phenylene radical, and pharmaceutically-acceptable acid-addition salts thereof. Processes for the manufacture of the compounds. Pharmaceutical compositions comprising one of the compounds and a pharmaceutical diluent or carrier. The compounds are selective .delta.-opiate-receptor antagonists.

Abstract: Disclosed herein are nasal spray compositions and methods for enhancing polypeptide absorption across nasal membranes comprising a chelating agent and a polypeptide in a pharmaceutically acceptable excipient.

Abstract: A method for improving the intestinal absorption of a cephalosporin derivative by bonding an oligopeptide having the general formula (I): ##STR1## wherein X is a hydrogen atom, C.sub.1-15 alkyl group, R.sub.3 CO-- group wherein R.sub.3 is a hydrogen atom or straight or branched chain C.sub.1-15 alkyl group or a protective group easily removable by acid hydrolysis, hydrogenolysis or enzyme existing in a living body;R.sub.1 and R.sub.2 each independently is a side chain of an amino acid constituting the oligopeptide; andn is integer of 1 to 3,to any side chain at the 3-, 4- or 7-position of a 7-aminocephalosporanic acid derivative having antibacterial activity.

Abstract: A process for the removal of the formyl group in N-formylated peptides or their esters is described. The N-formyl compound is reacted with hydrazine or a substituted hydrazine of formula I: ##STR1## at a pH between 1 and 3.5, keeping the pH constant during the reaction. The process is particularly useful for the preparation of aspartam.