Patents Represented by Attorney Arthur E. Wilfond

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  • Tricyclic isoindole derivatives
    Patent number: 4423232
    Abstract: Tricyclic isoindole derivatives characterized by having a 1,2,3,4,6,10b-hexahydropyrazino]2,1-a]isoindole or 1,3,4,10b-tetrahydropyrimido[6,1-a]isoindol-6(2H)-one nucleus are disclosed. The foregoing compounds are useful antihypertensive agents.Claimed compounds include those of the formula ##STR1## in which R.sup.3 and R.sup.4 each is hydrogen, lower alkoxy, lower alkyl, trifluoromethyl, halo or hydroxy, or R.sup.3 and R.sup.4 together form an OCH.sub.2 O chain; and R.sup.14 and R.sup.15 each is hydrogen or lower alkyl.
    Type: Grant
    Filed: February 19, 1981
    Date of Patent: December 27, 1983
    Assignee: American Home Products Corporation
    Inventors: Christopher A. Demerson, Leslie G. Humber, Jean-Marie Ferland
  • Benzofuro[3,2-c]pyrazol-3-amine derivatives
    Patent number: 4420476
    Abstract: Herein is disclosed benzofuro[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: December 13, 1983
    Assignee: Averst McKenna & Harrison, Inc.
    Inventors: Adolf Philipp, Ivo Jirkovsky, Rene Martel
  • Pyrimido[1,6-a]indole derivatives
    Patent number: 4409224
    Abstract: Pyrimido[1,6-a]indole derivatives characterized by having a substituted ethyl group at position 5 and optionally being further substituted at various positions on the pyrimido[1,6-a]indole nucleus are disclosed. The foregoing compounds are useful as antihypertensive agents in a mammal. Methods for their preparation also are disclosed.
    Type: Grant
    Filed: July 13, 1981
    Date of Patent: October 11, 1983
    Assignee: American Home Products Corp.
    Inventor: Ivo L. Jirkovsky
  • 6-(Lower alkoxy)-5-(trifluoromethyl)-1-naphthalenecarboxaldehydes
    Patent number: 4408077
    Abstract: A process and intermediates for preparing 6-(lower alkoxy)-5-(trifluoromethyl)-1-naphthalenecarboxylic acid derivatives are disclosed. The derivatives are useful for preparing aldose reductase inhibitors. With reference to the process, 1,1,1-trifluoro-5-(2-methylphenyl)-2,3-pentadione 3-oxime is cyclized to give a key intermediate 3,4-dihydro-1-hydroxy-5-methyl-1-(trifluoromethyl)-2(1H)-naphthalenone oxime; and 3,4-dihydro-1-hydroxy-5-methyl-1-(trifluoromethyl)-2(1H)-naphthalenone is aromatized to 5-methyl-1-(trifluoromethyl)-2-naphthalenol with a dehydrating agent.
    Type: Grant
    Filed: November 13, 1981
    Date of Patent: October 4, 1983
    Assignee: Ayerst, McKeena & Harrison, Inc.
    Inventors: Kazimir Sestanj, Steven Fung, Nedumparambil A. Abraham, Francesco Bellini
  • N-Substituted dimeric cyclopeptide derivatives
    Patent number: 4401656
    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 phenyl(lower)alkylene; R.sup.2 is lower alkyl, cyclo(lower)alkyl or lower alkoxycarbonyl(lower)alkylene; and 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 22, 1980
    Date of Patent: August 30, 1983
    Assignee: Ayerst, McKenna & Harrison, Ltd.
    Inventors: Amedeo Failli, Hans U. Immer, Manfred K. Gotz
  • Combination of rapamycin and picibanil for the treatment of tumors
    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
  • N-(Naphthalenylthioxomethyl)aminoacid derivatives
    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
  • 4,7-Dihydro-4,7-dioxi-1H-cyclohepta[b]pyridine derivatives
    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
  • 4,9-Dihydro-4,9-dioxo-1H-cyclohepta[b]pyridine derivatives
    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
  • 17 .alpha.-Dihydroequilin hapten and assay method
    Patent number: 4379780
    Abstract: A hapten is obtained by replacing the 3-hydroxy group of 17 .alpha.-dihydroequilin with HO--CO--A--O-- wherein A is an alkylene of one to six carbon atoms. The hapten is conjugated with an immunological carrier to provide an immunogen, which in turn produces a specific antiserum to 17 .alpha.-dihydroequilin. The antiserum is used in a radioimmunoassay for 17 .alpha.-dihydroequilin.
    Type: Grant
    Filed: September 29, 1980
    Date of Patent: April 12, 1983
    Assignee: American Home Products Corporation
    Inventor: Pemmaraju N. Rao
  • Equilin hapten and assay method
    Patent number: 4379779
    Abstract: A hapten is obtained by replacing the 3-hydroxy group of equilin with HO--CO--A--O-- wherein A is an alkylene of one to six carbon atoms. The hapten is conjugated with an immunological carrier to provide an immunogen, which in turn produces a specific antiserum to equilin. The antiserum is used in a radioimmunoassay for equilin.
    Type: Grant
    Filed: September 29, 1980
    Date of Patent: April 12, 1983
    Assignee: American Home Products Corporation
    Inventors: Pemmaraju N. Rao, Robert H. Purdy, Perry H. Moore, Jr.
  • 1,4,5,6-Tetrahydropyrimidine derivatives
    Patent number: 4379926
    Abstract: 1,4,5,6-Tetrahydropyrimidine derivatives characterized by having a phenyl or substituted phenyl at positions 1 and 6 in addition being further substituted at position 2. The foregoing compounds are useful as diuretic agents in a mammal. Methods for the preparation and use of the compounds are disclosed.
    Type: Grant
    Filed: May 8, 1978
    Date of Patent: April 12, 1983
    Assignee: Ayerst, McKenna & Harrison Ltd.
    Inventors: Jean A. Gauthier, Ivo Jirkovsky
  • 2(1-Piperazinyl)-cycloheptimidazole antihypertensive composition and methods
    Patent number: 4375470
    Abstract: 2-(1-Piperazinyl)-cycloheptimidazole derivatives are disclosed. The foregoing compounds are useful antihypertensive agents.
    Type: Grant
    Filed: October 17, 1980
    Date of Patent: March 1, 1983
    Assignee: American Home Products Corporation
    Inventors: Jehan F. Bagli, Tibor Bogri
  • Antibiotic AY24,668 and process of preparation
    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
  • Ravidomycin and process for preparation
    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
  • Articles for carrying chemicals
    Patent number: 4371516
    Abstract: The invention relates to shaped articles carrying chemicals, particular to pharmaceutical dosage forms carrying pharmaceuticals, which disintegrate rapidly in water. The shaped articles comprise an open matrix network of carrier material carrying the chemical. The articles may be prepared by subliming solvent from a composition comprising the chemical and a solution of the carrier material in a solvent, the composition being in the solid state in a mould.
    Type: Grant
    Filed: July 17, 1981
    Date of Patent: February 1, 1983
    Assignee: John Wyeth & Brother Limited
    Inventors: George K. E. Gregory, James M. Peach, James D. Du Mayne
  • 6,7,8,9-Tetrahydro-3H-benz[E]indol-8-amine derivatives
    Patent number: 4370341
    Abstract: Herein is disclosed compounds of the formula ##STR1## in which R.sup.1,R.sup.2,R.sup.3,R.sup.4 and R.sup.5 each is hydrogen or lower alkyl, therapeutically acceptable acid addition salts thereof, processes for their preparation, methods of using the compounds and pharmaceutical compositions. The compounds exhibit dopamine-receptor stimulating activity in a mammal and are useful for treating hyperprolactinemia, galactorrhea, amenorrhea, impotence, Parkinsonism, diabetes, acromegaly, hypertension and other central nervous system disorders.
    Type: Grant
    Filed: December 11, 1980
    Date of Patent: January 25, 1983
    Assignee: Ayerst, McKenna & Harrison, Ltd.
    Inventors: Andre A. Asselin, Leslie G. Humber
  • 2-Thioxobenz[cd]indole-1(2H)-acetic acid derivatives
    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
  • N-Substituted 2-(8-halo and trifluoromethyl 4-quinolylamino)benzamides and analgesic use thereof
    Patent number: 4357333
    Abstract: The disclosure describes new 4-aminoquinoline derivatives of general formula ##STR1## and their pharmaceutically acceptable acid addition salts, where X is trifluoromethyl or halogen, Z is hydrogen or a defined substituent and R is a group having one of the formulae ##STR2## where R.sup.1 is hydrogen or lower alkyl, R.sup.2 is lower alkyl, R.sup.3 is lower alkyl and A is lower alkylene. The new 4-aminoquinoline derivatives show analgesic activity and, in some cases, anti-inflammatory activity.
    Type: Grant
    Filed: August 11, 1980
    Date of Patent: November 2, 1982
    Assignee: John Wyeth & Brother Limited
    Inventors: John L. Archibald, John T. A. Boyle
  • 2,3-Dihydro-3-[4-(substituted)-1-piperazinyl]-1H-isoindol-1-ones
    Patent number: 4355031
    Abstract: Pyrazinoisoindolone derivatives of the formula ##STR1## wherein R.sup.1 is lower alkyl, phenyl, diphenylmethyl, pyridinyl, pyrimidinyl, pyrazinyl or pyrazinyl substituted with a lower alkyl, lower alkoxy or halo; and R.sup.2 is hydrogen, lower alkyl or di(lower)alkylamino(lower)alkyl are useful as antihypertensive agents.
    Type: Grant
    Filed: May 11, 1981
    Date of Patent: October 19, 1982
    Assignee: American Home Products Corp.
    Inventors: Christopher A. Demerson, Ivo L. Jirkovsky