Patents Examined by Reginald J. Suyat
  • Patent number: 3992530
    Abstract: Compounds of the formula: ##EQU1## in which R.sup.4 and R.sup. 5 are methyl or R.sup. 4 is hydrogen and R.sup.5 is alkyl of 1 to 5 carbon atoms or phenethyl, or a non-toxic acid addition salt thereof, are claudogenic-interceptive agents useful in preventing or terminating pregnancy in mammals.
    Type: Grant
    Filed: December 8, 1975
    Date of Patent: November 16, 1976
    Assignee: American Home Products Corporation
    Inventors: Theodore J. Foell, Richard W. A. Rees
  • Patent number: 3992365
    Abstract: Novel peptide compounds of the formulaGlu-His-X.sup.3 -X.sup.4 -X.sup.5 -X.sup.6 -X.sup.7 -X.sup.8 -Pro-Ware provided together with their acid addition salts and their complexes with pharmaceutically acceptable metals. The compounds are LH-RH analogues and together with their salts and complexes exhibit LH-RH agonist activity. In the formulaX.sup.3 and X.sup.5 are the same or different and each is phenylalanyl optionally substituted in the benzene ring;X.sup.4 and X.sup.6 are the same or different and each is selected from glycyl, alanyl (D- or L-) and asparaginyl;X.sup.7 is a radical of a neutral hydrophobic nonsulphur containing non-heterocyclic amino acid;X.sup.8 is a radical of a basic amino acid or is glycyl or phenylalanyl optionally substituted in the benzene ring; andW is selected from glycine amide and a group --NR.sup.1 R.sup.2.All references are to the L-amino acids and their radicals except in the case of glycine and unless otherwise stated.
    Type: Grant
    Filed: October 31, 1974
    Date of Patent: November 16, 1976
    Assignee: Burroughs Wellcome Co.
    Inventors: Christopher Raymond Beddell, Lawrence Alfred Lowe, Samuel Wilkinson
  • Patent number: 3992528
    Abstract: Antimicrobial agent particularly effective as an antiviral agent but also exhibiting antifungal and antibacterial activity characterized as a triad containing peptide, fatty acid and carbohydrate moieties.
    Type: Grant
    Filed: February 18, 1975
    Date of Patent: November 16, 1976
    Assignee: Research Corporation
    Inventors: Shirl O. Graham, Sarangamat Gurusiddaiah
  • Patent number: 3992529
    Abstract: Method of treating excessive fibrinolysis with a 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.
    Type: Grant
    Filed: December 1, 1975
    Date of Patent: November 16, 1976
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Wolfgang Konig, Oswald Zwisler, Gerhard Guthorlein
  • Patent number: 3991041
    Abstract: The growth hormone release inhibiting compound: ##EQU1## the corresponding linear heptadecapeptide, non-toxic acid addition salts and intermediates therefore are herein described, in which Trp is D-tryptophyl or L-tryptophyl and each of the other optically active amino acid moieties are of the L-configuration and A represents --OH, --NH.sub.2, dimethylamino, alkylamino of 1-5 carbon atoms or phenethylamino.
    Type: Grant
    Filed: December 18, 1975
    Date of Patent: November 9, 1976
    Assignee: American Home Products Corporation
    Inventor: Victor M. Garsky
  • Patent number: 3989812
    Abstract: Novel folic acid derivatives useful for radio-assaying folic acid and its metabolites in biological liquids are prepared from pteroyl-.gamma.-glutamyl-tyrosines by iodination with I.sup.125 or I.sup.131.
    Type: Grant
    Filed: August 9, 1974
    Date of Patent: November 2, 1976
    Assignee: SmithKline Instruments, Inc.
    Inventors: M. James Barrett, Joseph I. De Graw
  • Patent number: 3988304
    Abstract: Compounds of the formula: ##EQU1## in which m and n are independently one of the integers from 1 to 5, inclusive, and pharmaceutically acceptable salts thereof, inhibit the release of growth hormone and are useful in the treatment of diabetes mellitus and acromegaly.
    Type: Grant
    Filed: August 25, 1975
    Date of Patent: October 26, 1976
    Assignee: American Home Products Corporation
    Inventor: Victor M. Garsky
  • Patent number: 3988308
    Abstract: The tetradecapeptide Ala-Gly-Tyr-Lys-Asn-Phe-Phe-Trp-Lys-Thr-Phe-Thr-Ser-Tyr-OH is described as well as novel intermediates used in the synthesis of such tetradecapeptide. This tetradecapeptide inhibits the release of growth hormone.
    Type: Grant
    Filed: November 4, 1974
    Date of Patent: October 26, 1976
    Assignee: American Home Products Corporation
    Inventor: Dimitrios Sarantakis
  • Patent number: 3988307
    Abstract: The method of utilizing .alpha.,.beta.-unsaturated amino acids, acyl, and N-acyl derivatives as linking agents in the solid phase synthesis of peptides with the corresponding production of carboxyl terminal amides. Preferred unsaturated amino acids are dehydroalanine and dehydrobutyrine which are constituents in naturally occurring amides such as nisin and subtilin. The synthesis follows conventional lines of R. B. Merrifield et al including blocking of the amino nitrogen, with the exception that the release agent contains an amount of water equimolar to the reactant .alpha.,.beta.-unsaturated amino acid.
    Type: Grant
    Filed: September 6, 1974
    Date of Patent: October 26, 1976
    Assignee: The United States of America as represented by the Secretary of the Department of Health, Education and Welfare
    Inventor: Erhard Gross
  • Patent number: 3987014
    Abstract: [6-TYR] Secretin is biologically active and can be radio-iodinated for use in the radioimmunoassay of secretin. The peptide can be produced by solid phase synthesis using benzhydrylamine resin as the support.
    Type: Grant
    Filed: January 10, 1974
    Date of Patent: October 19, 1976
    Assignee: Becton, Dickinson and Company
    Inventors: Mariano Guiducci, Roger Piasio
  • Patent number: 3985723
    Abstract: A process for N-trifluoroacetylating an amino compound, such as an amino acid or a peptide, comprising reacting the amino compound with sym-trichlorotrifluoroacetone in a dimethyl sulfoxide solvent under substantially neutral conditions.
    Type: Grant
    Filed: September 7, 1971
    Date of Patent: October 12, 1976
    Assignee: The University of Mississippi
    Inventors: Charles A. Panetta, Travis G. Casanova
  • Patent number: 3985722
    Abstract: A mixed acid anhydride consisting of higher fatty acid having 6 to 22 carbon atoms and sulfuric anhydride is reacted with amino acids, peptides or proteins in the presence of a base to form N-higher aliphatic acyl derivatives of amino acids, peptides or proteins respectively in good yield. The reaction mixture comprises N-acylated-amino acids, peptides or -proteins and sulfate salts and may be directly used as detergent.
    Type: Grant
    Filed: December 9, 1974
    Date of Patent: October 12, 1976
    Assignee: Ajinomoto Co., Inc.
    Inventors: Ryonosuke Yoshida, Takashi Shishido
  • Patent number: 3983099
    Abstract: The present invention is concerned with the production of novel derivatives of thyroid hormones which are useful in the radioimmunoassay (RIA) of such hormones. The invention is particularly concerned with derivatives of thyroxine and triiodothyronine which contain an additional phenol group which is readily iodinatable so that the phenol conjugate can be readily tagged with a radioactive iodine isotope, such as .sup.125 I or .sup.131 I, without detrimentally interfering with the ability of the tagged conjugate so competitively bind with the naturally occurring thyroid hormone in the biological liquid to be analyzed by RIA technique. The invention is also concerned with the iodine-tagged derivatives or conjugates.
    Type: Grant
    Filed: March 19, 1975
    Date of Patent: September 28, 1976
    Assignee: Micromedic Diagonistics, Inc.
    Inventor: Gordon Dean Niswender
  • Patent number: 3980631
    Abstract: Stepwise synthesis in solution and cyclization by means of active esters or another method suitable for peptide bond formation were used to prepare analogues of deamino-vasopressin with the disulphide bridge altered to the thioether group. In sequence position 8 of the peptide chain the analogs differed by the nature of basic amino acid. Typical vasopressin-like activities, mainly antidiuretic, were very high in these analogs; of particular importance will be their haemodynamic activity.
    Type: Grant
    Filed: October 7, 1974
    Date of Patent: September 14, 1976
    Assignee: Ceskoslovenska akademie ved
    Inventors: Zdenko Prochazka, Tomislav Barth, Joseph Henry Cort, Karel Jost, Frantisek Sorm
  • Patent number: 3978035
    Abstract: The specification describes the total synthesis of L-norleucine-13-motilin ased on the replacement of the L-methionine radical located in the 13-position by an L-norleucine radical. In accordance with the present day development of peptide synthesis the central arginyl-methionyl-bond (amino acids 12 and 13 of motilin) can in practice hardly be synthesised, while on the other hand the norleucine-13-docosapeptide corresponding to motilin can be more readily produced synthetically, and this provides for a comparatively rapid determination of structure and can give important information as regards the biological effect specificity of methionine.
    Type: Grant
    Filed: March 27, 1974
    Date of Patent: August 31, 1976
    Assignee: Max-Planck-Gesellschaft zur Forderung der Wissenschaften e.V.
    Inventors: Erich Wunsch, Gerhard Wendlberger, Ernst Jaeger, Regine Scharf, Karl-Heinz Deimer, Hans Stocker
  • Patent number: 3978034
    Abstract: Dipeptides of the formula: ##EQU1## wherein n is an integer from 0 to 5, R.sub.1 is an alkyl, alkylaryl or alicyclic radical, and R.sub.2 is a cycloalkenyl radical, and, in addition, may be phenyl when n is 0. The carbon marked with an asterisk is always of the L-configuration. These compounds have a sweet taste and are useful as sweetening agents.
    Type: Grant
    Filed: November 12, 1969
    Date of Patent: August 31, 1976
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: John T. Sheehan, Miguel A. Ondetti
  • Patent number: 3976770
    Abstract: A new octapeptide having profound angiotensin antagonist properties has been found. The new compound resembles angiotensin II except for the two terminal amino acids, carrying unnatural amino acids at the N-terminus, and at the C-terminus.
    Type: Grant
    Filed: February 10, 1975
    Date of Patent: August 24, 1976
    Inventors: Francis Merlin Bumpus, Mahesh Chandra Khosla, Robert Rudolph Smeby
  • Patent number: 3975365
    Abstract: Octapeptide derivatives characterized by an oxygen or sulfur-containing moiety in the C-terminal position are potent inhibitors of the pharmacological effects of Angiotensin and possess the additional advantage of a favorable antagonist/agonist ratio.
    Type: Grant
    Filed: January 27, 1975
    Date of Patent: August 17, 1976
    Assignee: G. D. Searle & Co.
    Inventor: Robert H. Mazur
  • Patent number: 3975366
    Abstract: A process for producing new pepstatins having anti-pepsin activity by cultivating a pepstatin producing strain in a nutrient medium containing assimilable carbon sources and nitrogen sources, and extracting the new pepstatins from the cultivated broth or medium.
    Type: Grant
    Filed: February 4, 1975
    Date of Patent: August 17, 1976
    Assignee: Zaidan Hojin Biseibutsu Kagaku Kenkyu Kai
    Inventors: Hamao Umezawa, Tetsuji Miyano, Kohtaro Funaishi, Tomio Takeuchi, Takaaki Aoyagi
  • Patent number: 3972859
    Abstract: The novel decapeptide amide derivatives of the formula(Pyr)Glu-His-Trp-Ser-R.sub.1 -R.sub.2 -R.sub.3 -Arg-Pro-Gly-NH.sub.2wherein R.sub.1 is Tyr or Phe; R.sub.2 is D-Nle, D-Nva, D-Abu, D-Phe, D-Ser, D-Thr or D-Met and R.sub.3 is Leu, Ile or Nle have a strong ovulation inducing activity.
    Type: Grant
    Filed: March 4, 1975
    Date of Patent: August 3, 1976
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Masahiko Fujino, Susumu Shinagawa, Tsunehiko Fukuda