Patents Represented by Attorney Arthur E. Wilfond

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  • 1-Hydroxyimidazole-5-methanamine derivatives
    Patent number: 4232029
    Abstract: 1-Hydroxyimidazole-5-methanamine derivatives characterized by having a lower alkyl group at positions N, N and 5 of the latter derivatives as well as having various substituents at position 2 of the imidazole ring are disclosed. These derivatives are useful as antihypertensive agents in a mammal. Methods for their preparation, use and pharmaceutical compositions also are disclosed.
    Type: Grant
    Filed: November 3, 1978
    Date of Patent: November 4, 1980
    Assignee: American Home Products Corporation
    Inventors: Adolf H. Philipp, Ivo L. Jirkovsky
  • 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
  • Spiroindolones
    Patent number: 4226860
    Abstract: Herein is disclosed spiroindolone derivatives of the formula ##STR1## in which R.sup.1 is lower alkyl or carboxy(lower)alkyl, R.sup.2 is lower alkyl, R.sup.3 is lower alkyl or phenyl(lower)alkyl, and X is oxygen or CH.sub.2, or a therapeutically acceptable base addition salt thereof when R.sup.1 is carboxy(lower)alkyl, a process for their preparation, methods of using the derivatives and pharmaceutical compositions of the derivatives. The derivatives are useful for treating hypertension in a mammal.
    Type: Grant
    Filed: August 6, 1979
    Date of Patent: October 7, 1980
    Assignee: American Home Products Corporation
    Inventors: Christopher A. Demerson, Leslie G. Humber
  • 1H-Pyrrole-1-acetamide compounds and their pharmaceutical compositions
    Patent number: 4225613
    Abstract: Pyrrole derivatives of general formula (II) ##STR1## wherein R.sup.7 and R.sup.8 are the same or different and each represent hydrogen or lower alkyl, R.sup.13 and R.sup.14 are each hydrogen, lower alkyl or halogen with the proviso that at least one or R.sup.13 and R.sup.14 is halogen or (lower)alkyl, R.sup.15 and R.sup.16 are each hydrogen or lower alkyl and R.sup.17 is aryl or aryl(lower)alkyl are useful as hypotensive or antihypertensive agents.
    Type: Grant
    Filed: April 30, 1979
    Date of Patent: September 30, 1980
    Assignee: John Wyeth & Brother Limited
    Inventor: Terence J. Ward
  • Somatostatin analogs having a substituted tryptophyl residue in position eight
    Patent number: 4224199
    Abstract: Tetradecapeptides of the formula ##STR1## in which A represents L, D or DL 5- or 6- fluoro-, bromo-,chloro- or iodotryptophyl, or a therapeutically acceptable acid addition salt thereof, their preparation and intermediates for their preparation are disclosed. The tetradecapeptides are useful for inhibiting the release of growth hormone. Compositions and methods for their use also are disclosed.
    Type: Grant
    Filed: April 9, 1979
    Date of Patent: September 23, 1980
    Inventors: Chester A. Meyers, David H. Coy, Andrew V. Schally
  • Process for preparing polycyclic heterocycles having a pyran ring
    Patent number: 4223151
    Abstract: A process applicable to the preparation of a wide variety of novel polycyclic heterocycles having a newly-formed pyran ring is disclosed. According to the process an aromatic nucleus bearing an ethanol group, for example, 3,4-dimethoxyphenethyl alcohol, is condensed with an aldehyde or ketone or a protected aldehyde or ketone, for example, aminoactaldehyde diethyl acetal, in the presence of an acid catalyst to afford the polycyclic heterocycle, for example, 6,7-dimethoxy-1-isochromanmethylamine. The new heterocycles so formed are useful for preparing derivatives having antiinflammatory, antibacterial or antifungal activities.
    Type: Grant
    Filed: February 3, 1977
    Date of Patent: September 16, 1980
    Assignee: American Home Products Corporation
    Inventors: Thomas A. Dobson, Leslie G. Humber, Christopher A. Demerson, Ivo L. Jirkovsky
  • Slow release pharmaceutical compositions containing 3-[2-(4-benzamido-1-piperidyl)ethyl]indole, embonate
    Patent number: 4223008
    Abstract: The invention provides a pharmaceutical composition in tablet form having an enteric coating and comprising 3-[2-(4-benzamido-1-piperidyl)ethyl]indole, embonate and a pharmaceutically acceptable carrier useful as a prolonged release antihypertensive formulation.
    Type: Grant
    Filed: May 14, 1979
    Date of Patent: September 16, 1980
    Assignee: John Wyeth & Brother Limited
    Inventor: George K. E. Gregory
  • Tripeptide angiotensin converting enzyme inhibitors
    Patent number: 4216209
    Abstract: Compounds of the formula HSCH.sub.2 CHR.sup.1 CO--Pro--R.sup.2 --R.sup.3 --OH in which R.sup.1 is hydrogen or lower alkyl, R.sup.2 is an amino acid residue exclusive of prolyl and R.sup.3 is an amino acid residue exclusive of glutamyl are useful for alleviating angiotensin related hypertension.
    Type: Grant
    Filed: March 19, 1979
    Date of Patent: August 5, 1980
    Assignee: American Home Products Corporation
    Inventors: Francesco Bellini, Hans U. Immer
  • Anti-depressant indole derivatives
    Patent number: 4209521
    Abstract: The invention concerns a compound of formula II ##STR1## or a pharmaceutically acceptable acid addition or quaternary ammonium salt thereof wherein R.sup.5 represents hydrogen, hydroxy, lower alkoxy or lower alkyl, R.sup.6 represents hydrogen or lower alkyl, and R.sup.7 represents phenyl, lower alkoxy phenyl, halophenyl, or thenyl and X represents oxygen or sulphur. These indole derivatives exhibit psychotropic activity. The invention includes a method of alleviating depression in a warm blooded animal afflicted with depression which method comprises administering to said animal an effective amount of a compound of formula II or a pharmaceutically acceptable acid addition salt thereof.
    Type: Grant
    Filed: November 8, 1978
    Date of Patent: June 24, 1980
    Assignee: John Wyeth & Brother Limited
    Inventors: John L. Archibald, Terence J. Ward
  • Piperidino ureas and thioureas
    Patent number: 4199590
    Abstract: Compounds of formula ##STR1## in which hal represents halogen;R represents hydrogen or lower alkyl having 1 to 6 carbon atoms;R.sup.2 represents a subsituted or unsubstituted monocyclic heterocyclic group;and X represents oxygen or sulphur; or a pharmaceutically acceptable acid addition or quaternary ammonium salt thereof, are disclosed which have hypotensive and/or antihypertensive activity.
    Type: Grant
    Filed: August 24, 1978
    Date of Patent: April 22, 1980
    Assignee: John Wyeth & Brother Limited
    Inventor: Terence J. Ward
  • 2-Substituted-3-methyl-.gamma.-pyrone tricyclic derivatives
    Patent number: 4198426
    Abstract: Compounds of formula I ##STR1## in which R.sup.1 is hydrogen, halogen, nitro, trifluoromethyl, lower alkyl or lower alkoxy; R.sup.2 is hydrogen or lower alkyl; R.sup.3 is hydroxy, 1H-tetrazol-5-yl or COOR.sup.4 wherein R.sup.4 is hydrogen or lower alkyl, and X is O, S, SO or SO.sub.2, are disclosed. The compounds of formula I are useful for treating allergic conditions. Methods for the preparation and use of the compounds are disclosed.
    Type: Grant
    Filed: January 29, 1979
    Date of Patent: April 15, 1980
    Assignee: Ayerst McKenna & Harrison Ltd.
    Inventors: Adolf H. Philipp, Ivo L. Jirkovsky
  • Hexahydroazepine, piperidine and pyrrolidine derivatives
    Patent number: 4197239
    Abstract: The invention concerns novel 2-oxo-hexahydroazepine, -piperidine and -pyrrolidine of formula I ##STR1## where n is 2,3 or 4, R is hydrogen, lower alkyl or aryl(lower)alkyl and R.sup.1 is lower alkyl. The compounds may be aromatized and the aromatized compounds converted to 3,3-disubstituted-hexahydroazepine, -piperidine and -pyrrolidine compounds having pharmacological activity, particularly analgesic activity.
    Type: Grant
    Filed: November 15, 1978
    Date of Patent: April 8, 1980
    Assignee: John Wyeth & Brother Limited
    Inventors: John F. Cavalla, Alan C. White, Robin G. Shepherd
  • Hexahydroazepine, piperidine and pyrrolidine derivatives
    Patent number: 4197241
    Abstract: The invention concerns novel 2-oxo-hexahydroazepine, -piperidine and -pyrrolidine derivatives of formula (I) and their aromatized derivatives of formula (II) ##STR1## where n is 2, 3 or 4, R is hydrogen, lower alkyl or aryl(lower)alkyl, R.sup.2 is hydrogen, lower alkyl or aryl(lower)alkyl and R.sup.3 is hydrogen, lower alkyl, aryl(lower)alkyl, lower alkenyl or lower alkynyl. The compounds are useful as intermediates for preparing 3,3-disubstituted -hexahydroazepine, -piperidine and -pyrrolidine compounds having pharmacological activity, particularly analgesic activity.
    Type: Grant
    Filed: November 15, 1978
    Date of Patent: April 8, 1980
    Assignee: John Wyeth & Brother Limited
    Inventors: John F. Cavalla, Alan C. White
  • Copper complexes of tetrahydroquinoline derivatives having anti-ulcer activity
    Patent number: 4191761
    Abstract: The invention relates to copper complexes of 5,6,7,8-tetrahydroquinoline-8-thiocarboxamides. The copper complexes are of value in the treatment of ulcers and hypersecretion in mammals.
    Type: Grant
    Filed: December 8, 1977
    Date of Patent: March 4, 1980
    Assignee: John Wyeth & Brother Ltd.
    Inventor: Roger Crossley
  • Process for preparing oxazoles
    Patent number: 4190584
    Abstract: (4,5-Diaryloxazol-2-yl)propionic and butyric acids having anti-inflammatory activity had previously been prepared by esterification of aroylarylcarbinols with a reactive derivative of butanedioic and pentanedioic acids, for instance, succinic or glutaric anhydride, isolation of the keto ester so formed and cyclization of the keto ester with a nitrogen-donating cyclizing agent, for instance, ammonium acetate in acetic acid. It has now been found that the omission of the isolation of the keto ester intermediate improves the purity of the oxazole product.
    Type: Grant
    Filed: July 17, 1978
    Date of Patent: February 26, 1980
    Assignee: John Wyeth & Brother Limited
    Inventor: George O. Weston
  • 2-Substituted-3-methyl-.gamma.-pyrone tricyclic derivatives
    Patent number: 4189490
    Abstract: Compounds of formula I ##STR1## in which R.sup.1 is hydrogen, halogen, nitro, trifluoromethyl, lower alkyl or lower alkoxy; R.sup.2 is hydrogen or lower alkyl; R.sup.3 is hydroxy, 1H-tetrazol-5-yl or COOR.sup.4 wherein R.sup.4 is hydrogen or lower alkyl, and X is O, S, SO or SO.sub.2, are disclosed. The compounds of formula I are useful for treating allergic conditions. Methods for the preparation and use of the compounds are disclosed.
    Type: Grant
    Filed: January 29, 1979
    Date of Patent: February 19, 1980
    Assignee: Ayerst McKenna & Harrison Limited
    Inventors: Adolf H. Philipp, Ivo L. Jirkovsky
  • 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
  • Blood pressure lowering benzoquinolizines
    Patent number: 4183937
    Abstract: The invention concerns novel benzoquinolizines of formula (I) ##STR1## and their pharmaceutically acceptable acid addition salts. In formula (I) R.sup.1 and R.sup.2 which may be the same or different, each represent hydrogen, lower alkyl, lower alkoxy or halogen, R.sup.3 and R.sup.4 which may be the same or different each represent hydrogen, lower alkyl, aryl or aryl(lower)alkyl or R.sup.3 and R.sup.4 together represent a tetra- or penta-methylene chain.The novel compounds of the invention lower blood pressure in warm-blooded animals.
    Type: Grant
    Filed: November 22, 1978
    Date of Patent: January 15, 1980
    Assignee: John Wyeth & Brother Limited
    Inventor: Terence J. Ward
  • Thiazole compound
    Patent number: 4183854
    Abstract: The invention relates to pharmaceutical compositions for use in treating ulcers or hypersecretion in mammals comprising a compound of formula Ia ##STR1## where Hal is a halogen atom, R.sup.1 is hydrogen or alkyl of 1-6 carbon atoms, R is hydrogen, alkyl of 1-5 carbon atoms (which may be substituted by two or more chlorine or bromine atoms), alkenyl of 2 to 5 carbon atoms, perfluoroalkyl of 1-5 carbon atoms, cycloalkyl of 3 to 5 carbon atoms, R.sup.3 is hydrogen, alkyl of 1-6 carbon atoms, or COR.sup.4 where R.sup.4 is as defined for R and R and R.sup.4 may be the same or different, and a pharmaceutically acceptable carrier.Methods of treatment of affected mammals and some novel compounds are also described.
    Type: Grant
    Filed: July 28, 1978
    Date of Patent: January 15, 1980
    Assignee: John Wyeth & Brother Limited
    Inventor: Roger Crossley
  • Troponyl-oxamic acid derivatives for treating allergic conditions
    Patent number: 4183955
    Abstract: Tropone derivatives characterized by having a derivative of oxamic acid at positions 2 and or 5 are disclosed. In addition, the tropone nucleus can be optionally further substituted. The foregoing compounds are useful for preventing or treating allergic conditions in a mammal. Methods for the preparation and use of said compounds are disclosed.
    Type: Grant
    Filed: August 31, 1978
    Date of Patent: January 15, 1980
    Assignee: Ayerst. McKenna & Harrison Limited
    Inventors: Jehan F. Bagli, Tibor Bogri