Patents Assigned to Ayerst McKenna and Harrison Inc.
  • Patent number: 4431657
    Abstract: Herein is disclosed 2H-benzothieno[3,2-c]pyrazol-3-amine derivatives, therapeutically acceptable acid addition salts thereof, processes for their preparation, methods of using the derivatives and pharmaceutical compositions. The derivatives are useful for producing analgesia in a mammal. In addition, some of the derivatives are useful for inhibiting gastric acid secretion, convulsions, anxiety and aggression, and producing muscle relaxation, hypnosis and sedation in a mammal.
    Type: Grant
    Filed: May 24, 1982
    Date of Patent: February 14, 1984
    Assignee: Ayerst, McKenna & Harrison Inc.
    Inventors: Adolf Philipp, Ivo Jirkovsky, Rene Martel
  • Patent number: 4423060
    Abstract: Disclosed are new methods of using 1-methyl-5-(4-methylbenzoyl)-1H-pyrrole-2-acetic acid or a therapeutically acceptable salt thereof with an organic or inorganic base for the treatment of complications associated with diabetes mellitus. The compound inhibits lens aldose reductase in a diabetic mammal.
    Type: Grant
    Filed: August 17, 1981
    Date of Patent: December 27, 1983
    Assignee: Ayerst, McKenna & Harrison Inc.
    Inventors: Dushan M. Dvornik, Nicole Simard-Duquesne
  • Patent number: 4423074
    Abstract: Disclosed are new methods of using 5-fluoro-2-methyl-1-[[4-(methylthio)phenyl]methylene]-1H-indene-3-acetic acid or a therapeutically acceptable salt thereof with an organic or inorganic base for the treatment of complications associated with diabetes mellitus. The compound inhibits lens aldose reductase in a diabetic mammal.
    Type: Grant
    Filed: December 21, 1981
    Date of Patent: December 27, 1983
    Assignee: Ayerst, McKenna & Harrison Inc.
    Inventors: Dushan M. Dvornik, Nicole Simard-Duquesne
  • Patent number: 4423075
    Abstract: Disclosed are new methods of using 5-fluoro-2-methyl-1-[[4-(methylsulfonyl)phenyl]methylene]-1H-indene-3-acet ic acid or a therapeutically acceptable salt thereof with an organic or inorganic base for the treatment of complications associated with diabetes mellitus. The compound inhibits lens aldose reductase in a diabetic mammal.
    Type: Grant
    Filed: December 21, 1981
    Date of Patent: December 27, 1983
    Assignee: Ayerst, McKenna & Harrison Inc.
    Inventors: Dushan M. Dvornik, Nicole Simard-Duquesne
  • Patent number: 4401653
    Abstract: Described is a method of using a combination of rapamycin and picibanil for the treatment of transplantable carcinogenic tumors.
    Type: Grant
    Filed: March 9, 1981
    Date of Patent: August 30, 1983
    Assignee: Ayerst, McKenna & Harrison Inc.
    Inventor: Chee P. Eng
  • Patent number: 4391825
    Abstract: Aldose reductase inhibitors of the formula ##STR1## wherein R.sup.1 and R.sup.2 each is lower alkyl, or a therapeutically acceptable salt thereof with an organic or inorganic base, are useful for treating diabetic complications.
    Type: Grant
    Filed: November 13, 1981
    Date of Patent: July 5, 1983
    Assignee: Ayerst, McKenna & Harrison Inc.
    Inventors: Francesco Bellini, Kazimir Sestanj, Leslie G. Humber
  • Patent number: 4391816
    Abstract: Herein disclosed are N-(naphthalenylthioxomethyl)aminoacid derivatives having aldose reductase inhibiting activity. The derivatives are useful for treating diabetic complications.
    Type: Grant
    Filed: November 13, 1981
    Date of Patent: July 5, 1983
    Assignee: Ayerst, McKenna & Harrison Inc.
    Inventors: Kazimir Sestanj, Nedumparambil A. Abraham, Francesco Bellini, Adi Treasurywala
  • Patent number: 4382088
    Abstract: Aldose reductase inhibitors of the formula ##STR1## in which R.sup.1 is CH.sub.2 COOR.sup.4 wherein R.sup.4 is hydrogen or lower alkyl; R.sup.2 is COOR.sup.5 wherein R.sup.5 is hydrogen or lower alkyl; and R.sup.3 is lower alkoxy, benzyloxy or CH.sub.2 COOR.sup.6 wherein R.sup.6 is hydrogen or lower alkyl; with the provisos that when R.sup.4 is hydrogen then R.sup.5 and R.sup.6 is hydrogen; and that when R.sup.4 is lower alkyl then R.sup.5 and R.sup.6 are lower alkyl with R.sup.4 and R.sup.6 being the same lower alkyl; are useful for treating diabetic complications.
    Type: Grant
    Filed: August 21, 1981
    Date of Patent: May 3, 1983
    Assignee: Ayerst, McKenna & Harrison, Inc.
    Inventors: Bozidar Palameta, Tibor Bogri, Jehan Bagli
  • Patent number: 4381304
    Abstract: Aldose reductase inhibitors of the formula ##STR1## in which R.sup.1 is COOH and R.sup.2 is hydrogen, 8-halo or 6-hydroxy, or R.sup.1 is CON(R.sup.3)-CH.sub.2 COOH wherein R.sup.3 is lower alkyl and R.sup.2 is hydrogen or 8-halo are useful for treating diabetic complications.
    Type: Grant
    Filed: August 21, 1981
    Date of Patent: April 26, 1983
    Assignee: Ayerst, McKenna & Harrison, Inc.
    Inventors: Bozidar Palameta, Tibor Bogri, Jehan Bagli
  • Patent number: 4375464
    Abstract: Antibiotic AY24,668 is producible by culturing Streptomyces hygroscopicus NRRL 5491 in an aqueous nutrient medium. AY24,668 has antifungal properties. Methods for its preparation and use are disclosed.
    Type: Grant
    Filed: November 19, 1981
    Date of Patent: March 1, 1983
    Assignee: Ayerst, McKenna & Harrison Inc.
    Inventors: Surendra N. Sehgal, Claude Vezina
  • Patent number: 4375463
    Abstract: Ravidomycin is produced by culturing Streptomyces ravidus NRRL 11,300 in an aqueous nutrient medium. Ravidomycin is useful as an antibacterial and antitumor agent. Methods for its preparation and use are disclosed.
    Type: Grant
    Filed: March 13, 1981
    Date of Patent: March 1, 1983
    Assignee: Ayerst, McKenna & Harrison, Inc.
    Inventors: Surendra N. Sehgal, Claude Vezina
  • Patent number: 4369188
    Abstract: Herein are disclosed compounds of the formula ##STR1## in which R.sup.1 is hydrogen, lower alkyl or --(CH.sub.2).sub.m --NR.sup.4 R.sup.5 wherein m is an integer from 2 to 6 and R.sup.4 and R.sup.5 each is hydrogen or lower alkyl; R.sup.2 is hydrogen, bromo or chloro; and R.sup.3 is hydrogen or halo; with the requirement that when R.sup.2 is bromo or chloro, then R.sup.3 is bromo or chloro or a therapeutically acceptable salt thereof. The compounds inhibit lens aldose reductase in a diabetic mammal.
    Type: Grant
    Filed: July 17, 1981
    Date of Patent: January 18, 1983
    Assignee: Ayerst, McKenna & Harrison Inc.
    Inventor: Kazimir Sestanj
  • Patent number: 4361582
    Abstract: Disclosed are new methods of using .gamma.-oxo-8-fluoranthenebutanoic acid, or a therapeutically acceptable salt thereof with an organic or inorganic base for the treatment of complications associated with diabetes mellitus. The compound inhibits lens aldose reductase in a diabetic mammal.
    Type: Grant
    Filed: August 17, 1981
    Date of Patent: November 30, 1982
    Assignee: Ayerst, McKenna & Harrison Inc.
    Inventors: Dushan M. Dvornik, Nicole Simard-Duquesne
  • Patent number: 4337265
    Abstract: Disclosed herein are 1,2-dihydro-2-oxo(or 2-thioxo)cyclohepta[b]-pyrrole-1-acetic acid derivatives having optional substitution at positions 3, on the cycloheptatriene ring and on the acetic acid side chain. The compounds are aldose reductase inhibitors and thus are useful for treating diabetic complications.
    Type: Grant
    Filed: August 21, 1981
    Date of Patent: June 29, 1982
    Assignee: Ayerst, McKenna & Harrison Inc.
    Inventors: Adi Treasurywala, Bozidar Palameta, Tibor Bogri, Jehan Bagli
  • Patent number: 4321260
    Abstract: Herein is described a method of treating benign prostatic hyperlasia without affecting testicular weight in a male mammal by administering an effective amount of gonadorelin.
    Type: Grant
    Filed: May 22, 1980
    Date of Patent: March 23, 1982
    Assignee: Ayerst, McKenna & Harrison Inc.
    Inventor: Claude Auclair
  • Patent number: 4316885
    Abstract: Disclosed are monoacyl and diacyl derivatives of rapamycin, processes for their preparation, methods of using the derivatives and pharmaceutical compositions of the derivatives. The derivatives are useful, inter alia, as antifungal antibiotics.
    Type: Grant
    Filed: August 25, 1980
    Date of Patent: February 23, 1982
    Assignee: Ayerst, McKenna and Harrison, Inc.
    Inventor: Sumanas Rakhit
  • Patent number: 4307092
    Abstract: This invention discloses novel 1-oxo-5H-pyrimidol[2,1-c][1,4]benzoxa(or thia)zinc-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: July 22, 1980
    Date of Patent: December 22, 1981
    Assignee: Ayerst McKenna & Harrison, Inc.
    Inventors: Jean A. Gauthier, Ivo L. Jirkovsky
  • Patent number: 4307114
    Abstract: Disclosed are new methods of using (Z)-5-fluoro-2-methyl-1-[[4-(methylsulfinyl)phenyl]methylene]-1H-indene-3- acetic acid or a therapeutically acceptable salt thereof with an organic or inorganic base for the treatment of complications associated with diabetes mellitus. The compound inhibits lens aldose reductase in a diabetic mammal.
    Type: Grant
    Filed: June 19, 1980
    Date of Patent: December 22, 1981
    Assignee: Ayerst, McKenna & Harrison, Inc.
    Inventors: Dushan M. Dvornik, Nicole Simard-Duquesne
  • Patent number: 4304772
    Abstract: Herein is disclosed ethanocarbazole derivatives, acid addition salts thereof, processes for their preparation, methods of using the derivatives and pharmaceutical compositions of the derivatives. The derivatives are useful for treating depression in a mammal and are represented by the following formula ##STR1## in which R.sup.1 is hydrogen or lower alkyl, R.sup.2 and R.sup.3 each is hydrogen or lower alkyl or R.sup.2 and R.sup.3 together with the nitrogen atom form a 1-pyrrolidinyl, 1-piperidinyl, 1-piperazinyl, 4-morpholinyl or 4-thiomorpholinyl ring, and m is an integer from 0 to 3.
    Type: Grant
    Filed: December 19, 1980
    Date of Patent: December 8, 1981
    Assignee: Ayerst, McKenna & Harrison, Inc.
    Inventors: Andre A. Asselin, Leslie G. Humber
  • Patent number: 4254121
    Abstract: 3-Oxo-5H-pyrimido[2,1-c][1,4]benzoxazine derivatives, optionally substituted with a hydroxymethyl, carboxy or loweer alkoxycarbonyl at position 1 and optionally substituted at positions 8 or 9, with a lowr alkyl or halo are disclosed. The derivatives are antiallergy agents and methods for their preparation and use are given.
    Type: Grant
    Filed: August 13, 1979
    Date of Patent: March 3, 1981
    Assignee: Ayerst, McKenna & Harrison Inc.
    Inventors: Jean A. Gauthier, Ivo L. Jirkovsky