Patents Examined by Reginald J. Suyat
  • Patent number: 4010260
    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
  • Patent number: 4010261
    Abstract: With the administration of 2 - 200 .mu.g./kg. of a nonapeptide, reproduction is prevented in warm-blooded animals of the reproductive age.
    Type: Grant
    Filed: November 25, 1974
    Date of Patent: March 1, 1977
    Assignee: Abbott Laboratories
    Inventors: Edwin Samuel Johnson, Riemond Henry Rippel, Jr.
  • Patent number: 4009264
    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.
    Type: Grant
    Filed: April 1, 1975
    Date of Patent: February 22, 1977
    Assignee: Meito Sangyo Kabushiki Kaisha
    Inventor: Akihiro Mizutani
  • Patent number: 4008209
    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.
    Type: Grant
    Filed: July 11, 1975
    Date of Patent: February 15, 1977
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Masahiko Fujino, Tsunehiko Fukuda, Susumu Shinagawa
  • Patent number: 4006223
    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.
    Type: Grant
    Filed: December 16, 1974
    Date of Patent: February 1, 1977
    Assignee: Spitalul Clinic Filantropia Bucuresti
    Inventors: Irina Chitulescu, Octav Costachel
  • Patent number: 4005063
    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
  • Patent number: 4003792
    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
  • Patent number: 4003884
    Abstract: Peptides having LH-RH/FSH-RH activity useful for treatment of male and female sterility.
    Type: Grant
    Filed: May 16, 1975
    Date of Patent: January 18, 1977
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Wolfgang Konig, Rolf Geiger, Jurgen K. Sandow
  • Patent number: 4002739
    Abstract: A soluble lyophilized collagen preparation is disclosed which is capable of reproducible aggregating platelets.
    Type: Grant
    Filed: February 18, 1975
    Date of Patent: January 11, 1977
    Assignee: Warner-Lambert Company
    Inventors: James E. Turner, James R. Butler
  • Patent number: 4002740
    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.
    Type: Grant
    Filed: August 21, 1975
    Date of Patent: January 11, 1977
    Inventors: Gideon Goldstein, David H. Schlesinger
  • Patent number: 4002602
    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.
    Type: Grant
    Filed: August 22, 1975
    Date of Patent: January 11, 1977
    Inventor: Gideon Goldstein
  • Patent number: 4001200
    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
  • Patent number: 4001199
    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.
    Type: Grant
    Filed: March 19, 1975
    Date of Patent: January 4, 1977
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Masahiko Fujino, Mitsuhiro Wakimasu, Shigehisa Taketomi, Eiichiro Ishikawa
  • Patent number: 4000259
    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.
    Type: Grant
    Filed: June 16, 1975
    Date of Patent: December 28, 1976
    Assignee: American Home Products Corporation
    Inventor: Victor M. Garsky
  • Patent number: 4000122
    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
  • Patent number: 3998799
    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
  • Patent number: 3998795
    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.
    Type: Grant
    Filed: June 23, 1975
    Date of Patent: December 21, 1976
    Assignee: American Home Products Corporation
    Inventor: Dimitrios Sarantakis
  • Patent number: 3997516
    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.
    Type: Grant
    Filed: June 27, 1975
    Date of Patent: December 14, 1976
    Assignee: Takeda Chemical Industries, Ltd.
    Inventor: Osamu Nishimura
  • Patent number: 3997517
    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.
    Type: Grant
    Filed: January 30, 1976
    Date of Patent: December 14, 1976
    Assignee: American Home Products Corporation
    Inventor: Dimitrios Sarantakis
  • Patent number: 3994871
    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