Abstract: Compounds of the formula 1 or 1a ##STR1## IN WHICH R is hydrogen or CONHCH.sub.2 CONHCH.sub.2 CH.sub.3 are disclosed. The compounds are obtained by a process which comprises the following step: preparing peptide fragments II, III, V and VII see below, by a series of condensations involving the reaction of an appropriately protected peptide having an activated ester group with an appropriately protected peptide having a free amino group; condensing ##STR2## by means of the azide method with ##STR3## followed by hydrogenolysis of the reaction product to obtain ##STR4## condensing the latter by means of the azide method with ##STR5## followed by treating the resulting compound with hydrazine hydrate to obtain ##STR6## condensing the latter by means of the azide method with ##STR7## in which R is hydrogen or CONHCH.sub.2 CONHCH.sub.2 CH.sub.
Type:
Grant
Filed:
July 28, 1975
Date of Patent:
March 1, 1977
Assignee:
Ayerst McKenna & Harrison Ltd.
Inventors:
Hans U. Immer, Nedumparambil A. Abraham, Verner R. Nelson
Abstract: A complex of a polysaccharide or its derivative with reduced glutathione having in its infrared absorption spectrum no absorption peak at about 2500 cm.sup.-.sup.1 which appears in the infrared absorption spectrum of the reduced glutathione. The complex is prepared by reacting the polysaccharide or its derivative activated with an activating agent selected from cyanogen halides, organic cyanic acid esters and alkyl esters of halogenocarbonic acids, with the reduced glutathione at a pH of less than 7. The complex is especially useful for stabilizing thiol groups.
Abstract: The novel nonapeptide amide derivatives of the formula(Pyr)Glu-His-Trp-Ser-R.sub.1 -R.sub.2 -R.sub.3 -Arg-Pro-NH-R.sub.4wherein R.sub.1 is Tyr or Phe; R.sub.2 is D-Leu, D-Ile, D-Nle, D-Val, D-NVa, D-Abu, .alpha.-Aibu, D-Phe, D-Phg, D-Ser, D-Thr or D-Met; R.sub.3 is Leu, Ile or Nle and R.sub.4 is alkyl of 1 to 3 carbon atoms which may be substituted with hydroxyl group have a strong ovulation inducing activity.
Abstract: Pharmaceutical compositions comprising an .alpha..sub.1 glycoproteic complex, a lipoprotic complex, a kalikrein-inhibitor polypeptide, thiaminediphosphate and L-tryptophan are disclosed. The compositions may be administered to afflicted man and animals to treat radiation disease without prior and exact determination of the time of exposure to the radiation.
Abstract: An unnatural nonapeptide with improved biological activities surpassing those of the natural follicle-stimulating lutenizing hormone-releasing hormone (Gn--RH) is described. The new peptide induces ovulation in warm-blooded animals at an oral dose of 5-100 .mu.g./kg.
Type:
Grant
Filed:
May 15, 1975
Date of Patent:
January 25, 1977
Assignee:
Abbott Laboratories
Inventors:
Ronald Lee Gendrich, Riemond Henry Rippel, John Hunter Seely
Abstract: This invention relates to chemical conjugates of acid polysaccharides and biochemically active complex organic molecules and particularly to such conjugates which are capable of forming soluble sodium salts and insoluble calcium salts.
Type:
Grant
Filed:
August 8, 1972
Date of Patent:
January 18, 1977
Assignee:
Miles Laboratories, Inc.
Inventors:
Patrick James Mill, Michael Alan Cresswell, Joseph George Feinberg
Abstract: There is disclosed a tridecapeptide of the following sequence:H.sub.2 N--Gly--Glu--Gln--Arg--Lys--Asp--Val--Tyr--Val--Gln--Leu--Tyr--Leu--COOHthis tridecapeptide has the capability of including the differentiation of T lymphocytes but not of complement receptor (CR.sup.+) B lymphocytes and thus is useful in a number of therapeutic areas. Also provided are novel intermediate polypeptides and methods of manufacture of the peptides.
Abstract: There is disclosed a new Ubiquitous Immunopoietic Polypeptide (UBIP) which has been isolated in fluffy white powder form from bovine thymus but which has been found to be present in living cellular tissue of all animals and plants tested including various guinea pig tissues, cells in tissue cultures and tissues from birds, fish, squid, plants, fungi and bacteria, the polypeptide being characterized by its ability to induce in vitro, in nanogram concentrations, the differentiation of both T cell and B cell immunocytes from precursors present in bone marrow or spleen and thus the polypeptide is useful in therapeutic areas involving thymic or immunity deficiencies and the like. The polypeptide also exhibits hypotensive properties. The polypeptide is isolated from living source materials by a combination of sizing techniques and ion-exchange chromatography and may be described by the following amino acid structural sequence:H.sub.
Abstract: This invention concerns polymerized, cross-linked, stromal-free hemoglobin useful as a blood substitute for carrying oxygen to tissues and organs, as a blood plasma expander and for supplying oxygen to oxygen-requiring environments.
Type:
Grant
Filed:
February 27, 1975
Date of Patent:
January 4, 1977
Assignee:
Alza Corporation
Inventors:
Pieter Bonsen, Myron B. Laver, Kent C. Morris
Abstract: Novel polypeptides of the formulaR.sub.1 --Arg--R.sub.2 --Phe--Phe--R.sub.3wherein R.sub.1 is hydrogen, or a basic or neutral amino acid residue, R.sub.2 is a neutral amino acid residue and R.sub.3 is NH.sub.2, Tyr--NH.sub.2, a residue of tyrosyl peptides consisting of 1 to 5 amino acid residues or amides of the tyrosyl peptides, provided that when R.sub.1 is hydrogen, R.sub.2 is Pro, are effectively used for treatment of insufficiency of carbohydrate metabolism and of lipid metabolism, especially for the treatment of diabetes by not only parenteral administration but also oral administration.
Abstract: Cyclic dodecapeptide analogs of somatostatin without cysteine amino acid residues and intermediates obtained in the synthesis of such compounds are described. These cyclic dodecapeptides inhibit the secretion of glucagon and hence have application in the treatment of diabetes mellitus.
Abstract: .alpha.-Hydrazinocarboxamide and .alpha.-(.alpha.'-acylhydrazino)-carboxamide derivatives of formula I ##STR1## in which R.sup.1 and R.sup.2 each are lower alkyl or R.sup.1 and R.sup.2 together with the nitrogen atom to which they are joined form a piperidino or morpholino radical; R.sup.3 is hydrogen, lower alkanoyl, benzoyl, p-nitrobenzoyl, p-aminobenzoyl, p-chlorobenzoyl, isocyanoacetyl, or protected amino acyl radicals, for example, N-formylglycyl or ##STR2## (N-carbobenzoxyglycylglycyl); R.sup.4 is lower alkyl, CHR.sup.7 COOR.sup.8 or CH.sub.2 CH.sub.2 COOR.sup.8 wherein R.sup.7 is hydrogen or phenyl and R.sup.8 is hydrogen or lower alkyl; R.sup.5 is hydrogen or lower alkyl; or R.sup.4 and R.sup.5 together with the carbon atom to which they are joined form a cyclohexylidene radical; and R.sup.6 is a cyclohexyl or CHR.sup.9 COY wherein R.sup.9 is hydrogen or benzyl and Y is hydroxyl, lower alkoxy or amine, with the provisos that when Y is hydroxyl then R.sup.
Type:
Grant
Filed:
April 7, 1975
Date of Patent:
December 28, 1976
Assignee:
American Home Products Corporation
Inventors:
Amedeo Failli, Verner R. Nelson, Hans U. Immer, Manfred K. Gotz
Abstract: There is provided, novel, transient pro-drug forms of L-DOPA (3,4-dihydroxy-L-phenylalanine), having the formula: ##STR1## wherein n represents an integer of from 2 to 50 with respect to formula (V-A), and wherein n represents an integer of from 1 to 50 with respect to formula (V-B);R represents a hydrogen atom, an acyl group, ##STR2## --CO-pyridyl, or --CO--R.sub.3, wherein R.sub.3 is the residue of any N,N-C.sub.1 -C.sub.2 dialkylamino acid or a C.sub.4 -C.sub.6 cycloalkylamino acid; R.sub.1 represents --OH, --O-lower alkyl, --O-benzyl, or a naturally occurring protein amino acid; and R.sub.2 represents ##STR3## --CO-pyridyl, a naturally occurring protein amino acid, 3',4'-L-diacyloxy phenylalanine, or --CO-R.sub.3.These compounds are all useful in the treatment of Parkinson's Disease.
Type:
Grant
Filed:
April 17, 1975
Date of Patent:
December 21, 1976
Assignee:
Interx Research Corporation
Inventors:
Nicolae S. Bodor, Kenneth B. Sloan, Anwar A. Hussain
Abstract: The growth hormone release inhibiting compound ##STR1## in which Y represents an .alpha.-amino acid of the D-series and A is alkyl of 1 to 17 carbon atoms or phenyl; the protamine zinc, protamine aluminum and non-toxic acid addition salts thereof, as well as the corresponding linear octadecapeptide and intermediates therefore are herein described.
Abstract: A guanidino group in an amino acid or a peptide can be protected with a specific protective group, i.e. lower alkoxybenzenesulfonyl group or tri-lower alkylbenzenesulfonyl group, and the protective group may easily be removed without affecting the amino acid or the peptide to be derived from the protected amino acid or peptide. Thus, the method is useful in the related chemical industries, especially in the peptide synthesis.
Abstract: Cyclized somatostatin analogues containing the Cys-Cys disulfide linkage, their pharmaceutically acceptable acid addition salts as well as their cyclic disulfhydryl precursors and intermediates therefor are disclosed. The cyclized analogues of somatostatin selectively reduce blood serum concentrations of growth hormone without materially affecting the concentrations of glucagon or insulin.
Abstract: Process for the manufacture of peptides which contain more than one disulphide bond characterized in that in one or two aminoacid sequences containing cysteine, in which disulphide bonds are to be produced, two cysteine radicals which are to be linked are protected by a mercapto-protective group R.sub.1 of the aralkyl type, two further cysteine radicals are protected by an acylaminomethyl group R.sub.2, the protective groups R.sub.1 are removed by treatment with iodine in the presence of a polyhalogenated lower aliphatic hydroxy compound or oxo compound, or a corresponding lower alkanoic acid lower alkyl ester, at the same time forming the disulphide bond between these cysteine radicals, which are protected by R.sub.1, and at any desired point after removal of the polyhalogenated compound the second disulphide bridge is formed in the usual manner.
Type:
Grant
Filed:
May 20, 1974
Date of Patent:
November 30, 1976
Assignee:
Ciba-Geigy Corporation
Inventors:
Bruno Kamber, Peter Sieber, Bernhard Riniker, Albert Hartmann, Werner Rittel