Abstract: The masking N-formyl group of an N-formyl-amino acid ester or N-formyl-peptide ester is removed without major side reactions when the ester is reacted in an inert liquid medium with hydroxylamine of which at least 70% is present in the form of a salt with a strong acid, the remainder, if any, being present as the free base or the salt of a weak acid.

Abstract: Two eosinophilotactic tetrapeptides of amino acid sequence Val-Gly-Ser-Glu and Ala-Gly-Ser-Glu have been isolated from extracts of human lung fragments. These tetrapeptides have been synthesized by solid phase peptide synthesis procedures and the synthetic and natural materials behaved similarly in analytical assays and bioassays. Novel N-terminal analogs have been prepared and have shown eosinophilotactic activity. Thus, the tetrapeptides disclosed herein have utility as therapeutic agents in the prophylaxis and/or treatment of parasitic diseases, anaphylaxis and bronchial asthma.

Abstract: Compounds of the formula 1 or 1a ##STR1##HSCH.sub.2 CH(R)CO--Lys--Asn--Phe--Phe--Trp--Lys--Thr--Phe--Thr--Ser--NHCH.sub.2 CH.sub.2 SH (1a)In which R is hydrogen or NHR.sup.1 in which R.sup.1 is lower aliphatic acyl containing from 1 - 6 carbon atoms or benzoyl, and pharmaceutically acceptable salts thereof are disclosed. The compounds of formulae 1 and 1a are useful for the management of diabetes and the treatment of acromegaly in mammals. Methods for their use also are disclosed.

Abstract: The tripeptide derivatives of formula 1H--L--Pro--N(R.sup.1)CH(R.sup.2)CO--Y--R.sup.3 (1)in which R.sup.1 is hydrogen, lower alkyl or NR.sup.4 R.sup.5 wherein R.sup.4 and R.sup.5 each are lower alkyl, R.sup.2 is hydrogen or lower alkyl, R.sup.3 is amino, lower alkylamino, di(lower)alkylamino or amino(lower)alkylamino and Y is one of the amino acid residues Gly or D-Ala with the proviso that when R.sup.1 is NR.sup.4 R.sup.5 wherein R.sup.4 and R.sup.5 are as defined herein and R.sup.2 and Y are as defined herein, R.sup.3 is lower alkylamino, di(lower)alkylamino or amino(lower)alkylamino, and a method for their preparation are disclosed. The tripeptide derivatives of formula 1 possess central nervous system activity and methods for their use are given.

Abstract: A polypeptide of the formula:X.sub.1 --Tyr--Ser--X.sub.2 --X.sub.3 --His--Phe--Arg--Trp--Gly--Lys--Pro--Val--Gly--(Lys).sub.n --Ywherein X.sub.1 is .alpha.-aminoisobutyric acid, .beta.-alanine, L-serine, D-serine, glycine, D-alanine, .gamma.-aminobutyric acid or sarcosine residue; X.sub.2 is L-methionine, L-norleucine, L-isoleucine or L-norvaline residue; X.sub.3 is L-glutamic acid or L-glutamine residue; n is an integer of 5-10; and Y is --R.sub.1, ##STR1## wherein R.sub.1 is hydroxy or lower alkoxy having 1-5 carbon atoms; R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are each hydrogen or lower alkyl having 1-5 carbon atoms; m is an integer of 1-10 and Y is a group bound to the carbonyl group of the C-terminal lysine residue; non-toxic acid addition salts thereof; and complexes thereof; being useful as a medicament owing to their strong adrenal-stimulating activity with protracted action and little side effects.

Abstract: The decapeptide [D-Phe.sup.6 ]-LH-RH, salts thereof, and intermediates used for the synthesis thereof are disclosed. The decapeptide has potent LH- and FSH-releasing hormone properties.

Abstract: A polypeptide of the formula:X.sub.1 -Tyr-Ser-X.sub.2 -X.sub.3 -His-Phe-Arg-Trp-Gly-Lys-Pro-Val-Gly-(Lys).sub.n -Ywherein X.sub.1 is .alpha.-aminoisobutyric acid, .beta.-alanine, L-serine, glycine, D-serine, D-alanine, .gamma.-aminobutyric acid or sarcosine residue; X.sub.2 is L-methionine, L-norleucine, L-isoleucine or L-norvaline residue; X.sub.3 is L-glutamic acid or L-glutamine residue; n is an integer of 1-4 and Y is a group of ##STR1## which is linked to the carbonyl group of the C-terminal lysine residue, wherein R.sub.1 and R.sub.2 are each hydrogen or the same or different lower alkyl having 1-5 carbon atoms, and R.sub.1 and R.sub.2, when taken together with or without another hetero atom, form a substituted or unsubstituted nitrogen containing heterocyclic ring, with the proviso that a peptide when X.sub.1 is a .alpha.-aminoisobutyric acid or D-serine, R.sub.1 and R.sub.

Abstract: The isolation of certain dipeptide esters, known to be potent sweetening agents, is achieved by selectively extracting, with a suitable alkanol in a heterogeneous system, an aqueous solution containing the dipeptide ester together with a variety of impurities.

Abstract: Antigenic phenethylamine conjugates are produced by blocking the amine of the phenethylamine hapten with a group, coupling of the phenethylamine to a carrier, and removal of the blocking group. Specific phenethylamines useful in this invention are amphetamine, epinephrine, and norepinephrine. The antigens thus produced can be used to raise antibodies in animal bodies, the antibodies being specific to the phenethylamine compound employed. In particular, this disclosure is directed to blocked phenethylamines for production of antigens and to a process for preparing the antigens.

Abstract: Polypeptides containing at least four amino acids are useful as mammalian contraceptives.

Abstract: A polypeptide having important biological activity including systemic vasodilation, hypotension, increased cardiac output and bronchodilation is isolated from intestines of chickens. The isolation procedure for purification includes extraction, ion-exchange chromatography, gel chromatography and countercurrent distribution separation. The polypeptide has the general amino acid structure:His-Ser-Asp-Ala-Val-Phe-Thr-Asp-Asn-Tyr-Ser-Arg-Phe-Arg-Lys-Gln-Met-Ala-Val -Lys-Lys-Tyr-Leu-Asn-Ser-Val-Leu-Thr-NH.sub.2. Therapeutic biological actions may be produced in animals and humans by administration of 0.02-10 .mu.g of the peptide per kg of body weight.

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.

Abstract: A process for the manufacture of insulin and derivatives thereof by treating an insulin derivative, wherein the A-chain is cross-linked with the B-chain by means of a sulfonyl diethyl-bisoxycarbonyl bridge and the B-chain may contain an acyl group in the 1-position, with alkali metal hydroxides or quaternary organic bases having a pH value of more than 13.

Abstract: The dodecapeptide H-Cys-Lys-Asn-Phe-Phe-Trp-Lys-Thr-Met-Thr-Ser-Cys-OH, its oxidized form, D-Trp.sup.6 analogue and intermediates obtained in their synthesis are described. These dodecapeptides inhibit the secretion of the hormone somatotropin (growth hormone).

Abstract: This invention encompasses novel tetrapeptide amides and their intermediates containing an L-aspartic acid residue. These peptides are inhibitors of gastric acid secretion and therefore useful in the treatment of ulcers.

Abstract: Cyclic undecapeptide analogs of somatostatin without cysteine amino acid residues and intermediates obtained in the synthesis of such compounds are described. These cyclic undecapeptides inhibit the secretion of the hormone somatotropin (growth hormone) without materially affecting glucagon levels.

Abstract: The undecapeptide H-Cys-Asn-Phe-Phe-Trp-Lys-Thr-Phe-Thr-Ser-Cys-OH, its D-Trp.sup.8 analogue, their oxidized forms and intermediates obtained in their synthesis are described. These undecapeptides inhibit the secretion of the hormone somatotropin (growth hormone).

Abstract: Peptides having the formulaN-Acetyl-N-methylglycyl-L-histidyl-L-tryptophyl-L-seryl-L-tyrosyl-Y-L-leucy l-L-arginyl-L-prolyl-Zwherein Y is a D-.alpha.-alkylglycine residue of the formula ##STR1## in which n is an integer of 0 through 3 inclusive and Z is ethylamino group or an ethylamino group which is substituted with 1 to 3 fluorine atoms at the 2-position and pharmaceutically acceptable salts thereof. They show luteinizing hormone-releasing hormone like activities and are prepared by reactingL-histidyl-L-tryptophyl-L-seryl(or L-seryl having a protected hydroxyl group)-L-tyrosyl(or L-tyrosyl having a protected hydroxyl group)-Y-L-leucyl-L-arginyl(or L-arginyl having a protected guanidyl group)-L-prolyl-Zwherein Y and Z are as defined above witha reactive derivative of N-Acetyl-N-methylglycineAnd, if a protective group is attached, then removing the protective group, and, if necessary, converting further the resultant into an acid addition salt thereof in the usual manner.

Abstract: A highly purified extract of the mammalian thymus gland and a process for its preparation is described. This extract is a hormonally active proteinaceous material which is involved in the regulation of cell-mediated immunity. The hormone has been named thymosin.

Abstract: The decapeptide [D-Trp.sup.6 ]-LH-RH, salts thereof, and intermediates used for the synthesis thereof are disclosed. The decapeptide has potent LH- and FSH-releasing hormone properties.