Patents Assigned to Ayerst McKenna and Harrison Inc.
  • 1H-Benz[de]isoquinoline-2(3H)-acetic acid derivatives
    Patent number: 4254109
    Abstract: Herein disclosed are 6-substituted derivatives of 1,3-dioxo-1H-benz[de]isoquinoline-2(3H)-acetic acid. The derivatives inhibit lens aldose reductase.
    Type: Grant
    Filed: November 8, 1979
    Date of Patent: March 3, 1981
    Assignee: Ayerst, McKenna & Harrison Inc.
    Inventor: Kazimir Sestanj
  • 1-Oxo-5H-pyrimido[2,1-c][1,4]benzthiazine-2-carboxylic acid esters
    Patent number: 4254118
    Abstract: This invention discloses novel 1-oxo-5H-pyrimido[2,1-c][1,4]benzoxa(or thia)zine-2-carboxylic acid lower alkyl esters, derivatives thereof, process for their preparation, pharmaceutical compositions thereof and methods for using the compounds. The compounds of this invention are useful in the treatment of anaphylactic reactions and allergic conditions in a mammal.
    Type: Grant
    Filed: August 13, 1979
    Date of Patent: March 3, 1981
    Assignee: Ayerst, McKenna & Harrison Inc.
    Inventors: Jean A. Gauthier, Ivo L. Jirkovsky
  • Thioxo-1H-benz[de]isoquinoline-2(3H)-acetic acid derivatives and antidiabetic use thereof
    Patent number: 4254108
    Abstract: Herein disclosed are 1H-benz[de]isoquinoline-2(3H)-acetic acid derivatives. The derivatives are characterized by being derived from 1,3-dioxo-1H-benz[de]-isoquinoline-2H-acetic acid by replacing one of the oxygen atoms with sulfur and by optional substitution at position 6 with a phenylthio group. The derivatives inhibit lens aldose reductase in a diabetic subject.
    Type: Grant
    Filed: November 8, 1979
    Date of Patent: March 3, 1981
    Assignee: Ayerst, McKenna & Harrison Inc.
    Inventor: Kazimir Sestanj
  • N-substituted dimeric cyclopeptide derivatives and preparation thereof
    Patent number: 4252795
    Abstract: The N-substituted dimeric cyclopeptide derivatives of formula ##STR1## in which A is a peptide residue having one to four amino acid residues; R.sup.1 is lower alkyl, phenyl or pheny(lower) alkylene; R.sup.2 is lower alkyl, cyclo(lower)alkyl or lower alkoxycarbonyl(lower)alkylene; R.sup.3 is a neutral amino acid side chain and a method for the preparation of the compounds of formula I are disclosed. The compounds of formula I are useful for treating microbial infections. Pharmaceutical compositions also are disclosed.
    Type: Grant
    Filed: September 11, 1978
    Date of Patent: February 24, 1981
    Assignee: Ayerst McKenna and Harrison Inc.
    Inventors: Amedeo Failli, Hans U. Immer, Manfred K. Gotz
  • Carba decapeptide derivatives of [TYR.sup.6 ]-somatostatin
    Patent number: 4244947
    Abstract: Peptides of formula I ##STR1## in which X is (CH.sub.2).sub.2, S--CH.sub.2 or CH.sub.2 --S or a therapeutically acceptable acid addition salt thereof are disclosed. The peptides of formula I are useful as agents for the treatment of acromegaly and the management of diabetes in a mammal. Compositions and methods for the preparation of the peptides of formula I are also disclosed.
    Type: Grant
    Filed: August 13, 1979
    Date of Patent: January 13, 1981
    Assignee: Ayerst McKenna and Harrison Inc.
    Inventors: Nedumparampil A. Abraham, Francesco Bellini, Hans U. Immer, Marvin M. Kobric
  • Ravidomycin and process of preparation
    Patent number: 4230692
    Abstract: Ravidomycin is produced by culturing Streptomyces ravidus NRRL 11,300 in an aqueous nutrient medium. Ravidomycin is useful as an antibacterial agent. Methods for its preparation and use are disclosed.
    Type: Grant
    Filed: November 3, 1978
    Date of Patent: October 28, 1980
    Assignee: Ayerst McKenna & Harrison, Inc.
    Inventors: Surendra N. Sehgal, Claude Vezina
  • 1,2,3,4-Tetrahydropyrrolo(1,2-A)pyrazines
    Patent number: 4188389
    Abstract: 1,2,3,4-tetrahydropyrrolo(1,2-a)pyrazine derivatives characterized by having a lower alkyl, cyclo(lower)alkyl, phenyl or substituted phenyl at position 1 of the nucleus and optionally further substituted at position 2 of the nucleus with a lower alkyl, cyclo(lower)alkyl, phenyl(lower)alkylene or 2-(indole-3-yl)ethyl are disclosed. The derivatives are useful antidepressant agents. Methods for their preparation also are disclosed.
    Type: Grant
    Filed: November 3, 1978
    Date of Patent: February 12, 1980
    Assignee: Ayerst McKenna & Harrison, Inc.
    Inventor: Ivo L. Jirkovsky