Abstract: A peptide having an amino acid sequence of Arg-Arg-Glu-Ala-Glu-Asp-Leu-Gln-Val-Gly-Gln-Val-Glu-Leu-Gly-Gly-Gly-Pro-Gl y-Ala-Gly-Ser-Leu-Gln-Pro-Leu-Ala-Leu-Glu-Gly-Ser-Leu-Gln-Lys-Arg; Tyr-Arg-Arg-Glu-Ala-Glu-Asp-Leu-Gln-Val-Gly-Gln-Val-Glu-Leu-Gly-Gly-Gly-Pr o-Gly-Ala-Gly-Ser-Leu-Gln-Pro-Leu-Ala-Leu-Glu-Gly-Ser-Leu-Gln-Lys-Arg; or Tyr-Arg-Arg-Glu-Ala-Glu-Asp-Leu-Gln-Val-Gly-Gly-Gln-Val-Glu-Leu-Gly-Gly-Gl y-Pro-Gly-Ala-Gly-Ser-Leu-Gln-Pro-Leu-Ala-Leu-Glu-Gly-Ser-Leu-Gln-Lys-Arg; and the N.sup..epsilon. formyl-Lys derivative thereof.
Abstract: The invention relates to the preparation of biologically active polypeptides containing the aspartyl group, particularly an aspartyl-glycine moiety, using the active-ester technique.According to the method of the invention, human adrenocorticotropic hormone and its fragments characteristic to the individual species, as well as the blocked derivatives of such compounds are prepared by the pentafluorophenol method, i.e., the carboxy group of the acylating component is activated by converting it into pentafluorophenyl ester in the coupling reaction carried out with blocked peptides containing the aspartyl group or an aspartylglycine moiety. The acylation is carried out preferably using equimolar quantities of the respective reactants. The free peptides obtained after removing the blocking groups can be converted into their acid addition salts or pharmaceutically acceptable complexes or condensates.Human adrenocorticotropic hormone and its derivatives are valuable substances of therapeutical activity.
Type:
Grant
Filed:
May 14, 1973
Date of Patent:
April 27, 1976
Assignee:
Richter Gedeon Vegyeszeti Gyar Rt
Inventors:
Lajos Kisfaludy, Miklos Low, Istvan Schon, Tamas Szirtes, Maria Sz. Sarkozi, Sandor Bajusz, Andrae Turan, Rosa Beks, Attila Juhasz, Laszlo Graf, Kalman Medzihradszky, Laszlo Szporny
Abstract: Modified trypsin-callicrein inhibitor wherein the five carboxyl groups present in the unmodified material are amidated by--(R)(R).sub.X W groups,Wherein R is prolyl or ##EQU1## X is an integer from 1 to 10, Y is hydrogen, alkyl, or substituted alkyl and W is --OH, --NH.sub.2, --NHC.sub.2 H.sub.5, --OCH.sub.3, or --OC.sub.2 H.sub.5. Method for making trypsin-callicrein inhibitor so modified by amidation.
Type:
Grant
Filed:
September 4, 1974
Date of Patent:
April 27, 1976
Assignee:
Hoechst Aktiengesellschaft
Inventors:
Wolfgang Konig, Oswald Zwisler, Gerhard Guthorlein
Abstract: A nuclease-resistant hydrophilic complex of polyriboinosinic-polyribocytidylic acid, poly-1-lysine and carboxymethylcellulose, and injectable preparations thereof in a pharmaceutically acceptable aqueous carrier such as saline solution. When administered to a non-human primate host, the complex is effective in inducing the synthesis in such host of antiviral levels of interferon.
Type:
Grant
Filed:
September 27, 1974
Date of Patent:
April 20, 1976
Assignee:
The United States of America as represented by the Department of Health, Education and Welfare
Abstract: Method and apparatus are provided for preparing polypeptides by conjugating arginine as an end group to a polyethyleneimine water soluble polymer, stepwise addition of amino acids as their N-carboxyanhydrides to prepare the desired polypeptide, enzymatic cleavage of the polypeptide with the arginine group from the polyethyleneimine and enzymatic cleavage of the arginine to provide the desired polypeptide. An automated apparatus is provided for performing the above process.
Type:
Grant
Filed:
July 3, 1974
Date of Patent:
April 20, 1976
Inventors:
Peter Pfaender, Helmut Pratzel, Hartmut Blecher
Abstract: The present invention relates to polypeptides, to a process for isolating them from sea-anemones (Actinaria), preferably from Anemonia Sulcata, and their use as polyvalent isoinhibitors for proteases, peptidases and esterases such as trypsin, chymotrypsin, plasmin and Kallicrein.
Type:
Grant
Filed:
July 8, 1974
Date of Patent:
April 20, 1976
Assignee:
Behringwerke Aktiengesellschaft
Inventors:
Hans Fritz, Laszlo Beress, Rosemarie Beress, Brunhilde Forg-Brey
Abstract: A method for augmenting hard or soft connective tissue, such as skin, tendon, cartilage, bone or interstitium, in a living mammal comprising implanting a proteolytic enzyme-solubilized, purified, native, in situ polymerizable collagen solution into the mammal at the augmentation site. The solution polymerizes at the site into a stable, non-reactive fibrous mass of tissue which is rapidly colonized by host cells and vascularized.
Type:
Grant
Filed:
November 18, 1974
Date of Patent:
April 6, 1976
Assignee:
The Board of Trustees of Leland Stanford Junior University
Abstract: Peptides of the calcitonin type when obtained by synthesis can be purified in a simple manner by forming inner salts, which precipitate from aqueous solutions of salts of the peptides with acids or bases when these solutions are adjusted to the isoelectric range. Impurities remain in solution, while the inner salts separate practically quantitatively. The precipitation is completed after several hours. The peptides can then be recuperated by treatment with an acid, especially a therapeutically suitable acid. The process affords products which are superior to those obtained by purification methods hitherto known and gives higher yields. Other long-chain peptides such as ACTH, insulin or glucagon cannot be purified in this manner.
Type:
Grant
Filed:
December 3, 1974
Date of Patent:
April 6, 1976
Assignee:
Ciba-Geigy Corporation
Inventors:
Werner Rittel, Max Brugger, Bernhard Riniker
Abstract: A process for preparing the LH- and FSH-releasing hormone of the formula Ih--pyr--His--Trp--Ser--Tyr--Gly--Leu--Arg--Pro--Gly--NH.sub.2which is isolated as the hydrochloride salt and optionally converted to other pharmaceutically acceptable salts or to pharmaceutically acceptable metal complexes.
Type:
Grant
Filed:
March 14, 1974
Date of Patent:
March 30, 1976
Assignee:
American Home Products Corporation
Inventors:
Hans U. Immer, Verner R. Nelson, Manfred K. Gotz
Abstract: A method for isolating insulin from the cultured seeds or fruit of Memordica charantia Linn in which the starting material is extracted with ethanol, water and sulfuric acid, adjusting the pH of the extract to 1.5 to 2.0 and then precipitating the insulin by adding cold ethanol and diethyl ether. Zinc traces are added to precipitate the insulin as white crude crystals which are then purified to white needle-like crystals. Comparison of this product with standard insulin by chromatography showed that the present product is substantially the same as the standard insulin.
Type:
Grant
Filed:
July 16, 1974
Date of Patent:
March 23, 1976
Inventors:
Pushpa Khann, Tej Narain Nag, Satish Chandrajain, Suchendra Mohan
Abstract: In situ process for synthesizing peptides not linked to polymers. The peptide derivatives remain in the same reaction vessel throughout the chain-lengthening procedure. Preferred apparatus for performing the process comprises means for mixing, evaporation and centrifugation.
Abstract: Tuberculin active simple proteins and peptides which have the following peptide linkage--Asn--Gly--Ser--Gln--Met--as a tuberculin active functional group, and a process for preparing the same from the cells of tubercle bacilli.
Abstract: The synthesis of the decapeptide pGlu-D-Met-Trp-Ser-Tyr-D-Ala-Leu-Arg-Pro-Gly-NH.sub.2 by solid-phase techniques is described. The decapeptide inhibits LH release.
Abstract: Antibiotic EM-49, an antimicrobially active material obtained from the microorganism Bacillus circulans ATCC 21656, is chemically treated to acylate the hydroxyl group, thereby obtaining O-acyl derivatives which are effective against a variety of bacteria and fungi.
Abstract: D-Phe.sup.2 -2-Me.Ala.sup. 6 -LRF, is described as well as its synthesis by solid phase techniques and novel intermediates formed by such synthesis. The novel decapeptide possess anti-ovulatory activity in mammals.
Abstract: The invention relates to a new and useful antibacterial substance which is of the formula ##EQU1## and to processes for its production and recovery. The invention embraces this antibacterial agent and its salts as crude concentrates, as purifed solids and in pure crystaline forms. This antibiotic of the Formula I is effective in inhibiting the growth of gram positive bacteria. The compound of the Formula I is prepared by cultivating a strain of Streptomyces sp. X-1092 in an aqueous carbohydrate solution containing a nitrogenous nutrient under submerged aerobic conditions until substantial activity versus Gram-positive bacteria is imparted to said solution and then recovering said compound of the Formula I from said solution.
Abstract: A process for the recovery of bacitracin in the form of a zinc complex wherein the pH is raised to precipitate the zinc bacitracin complex. The zinc bacitracin complex is precipitated in the presence of ammonium ion which complexes the excess zinc and maintains it in solution, thereby preventing coprecipitation of zinc hydroxide.
Type:
Grant
Filed:
April 12, 1974
Date of Patent:
February 10, 1976
Assignee:
Phylaxia Oltoanyag- es Tapszertermelo Vallalat
Inventors:
Judit Bathory, Marta Ery nee Nagy, Lajos Gerei, Ferenc Lakatos, Magdolna Stiller nee Kisteleki, Tamas Vaghy
Abstract: The present invention provides new salts and complexes of lysozyme and of basic derivatives of lysozyme with bile acids, processes for the preparation thereof and the pharmaceutical use thereof.
Abstract: A stable composition of the sulfated octapeptide, ##EQU1## having cholecystokinin activity, is obtained by lyophilizing an aqueous solution of the octapeptide and NaCl.
Type:
Grant
Filed:
July 22, 1974
Date of Patent:
February 10, 1976
Assignee:
E. R. Squibb & Sons, Inc.
Inventors:
Miguel Angel Ondetti, Charles Riffkin, Bernard Rubin, Aaron L. Weiss
Abstract: A novel insulin composition of improved stability and compatibility comprising in an aqueous suspension crystallized insulin and amorphous des-phenyl-alanine.sup.B1 insulin of the same species, and a method for its manufacture.
Type:
Grant
Filed:
November 14, 1973
Date of Patent:
February 10, 1976
Assignee:
Hoechst Aktiengesellschaft
Inventors:
Adolf Mager, Hans-Hermann Schone, Rolf Geiger, Franz Enzmann