Patents Represented by Attorney Arthur E. Wilfond

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  • N-Substituted cyclopeptide derivatives
    Patent number: 4351828
    Abstract: The N-substituted cyclopeptide derivatives of formula I ##STR1## in which R.sup.1 is lower alkyl, R.sup.2 is lower alkyl or cyclo(lower)alkyl, R.sup.3 is a neutral amino acid side chain and Y is a peptide residue having three to nine amino acid residues and a method for the preparation of the compounds of formula I are disclosed. The compounds of formula I are useful antibacterial and antifungal agents. Pharmaceutical compositions also are disclosed.
    Type: Grant
    Filed: June 30, 1980
    Date of Patent: September 28, 1982
    Assignee: American Home Products Corporation
    Inventors: Amedeo Failli, Hans U. Immer, Manfred K. Gotz
  • 2-(Piperazinyl)-4-pyrimidinamines
    Patent number: 4351832
    Abstract: Herein is disclosed 2-(1-piperazinyl)-4-pyrimidinamine derivatives, acid addition salts thereof, processes for their preparation, methods of using the derivatives and pharmaceutical compositions of the derivatives. The derivatives are distinguished most readily by having novel substituents at position 4 of the piperazinyl radical, the substituents being selected from the group consisting of 2-thiazoylyl, oxazolo(4,5-b)pyridin-2-yl and optionally substituted 1-(lower alkyl)-1H-benzimidazol-2-yl. The derivatives are useful for treating hypertension in a mammal.
    Type: Grant
    Filed: March 20, 1981
    Date of Patent: September 28, 1982
    Assignee: American Home Products Corporation
    Inventors: Sumanas Rakhit, Jehan F. Bagli
  • Isochromans
    Patent number: 4351942
    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: January 7, 1980
    Date of Patent: September 28, 1982
    Assignee: American Home Products Corp.
    Inventors: Thomas A. Dobson, Leslie G. Humber, Christopher A. Demerson, Ivo L. Jirkovsky
  • Cyclohepta[b]pyrrole derivatives
    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
  • 2-(Piperazinyl)-4-pyrimioinamines
    Patent number: 4333937
    Abstract: Herein is disclosed 2-(1-piperazinyl)-4-pyrimidinamine derivatives, acid addition salts thereof, processes for their preparation, methods of using the derivatives and pharmaceutical compositions of the derivatives. The derivatives are distinguished most readily by having novel substituents at position 4 of the piperazinyl radical, the substituents being selected from the group consisting of optionally substituted 2-cycloheptimidazolyl, 1,4,5,6,7,8-hexahydrocycloheptimidazol-2-yl, 2-benzoxazolyl, benzthiazol-2-yl, 1H-2-benzimidazolyl and 1-oxo-2,4,6-cycloheptarien-2-yl. The derivatives are useful for treating hypertension in a mammal.
    Type: Grant
    Filed: April 18, 1980
    Date of Patent: June 8, 1982
    Assignee: American Home Products Corp.
    Inventors: Sumanas Rakhit, Jehan F. Bagli
  • Antihypertensive tricyclic isoindole derivatives
    Patent number: 4323572
    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.
    Type: Grant
    Filed: February 6, 1981
    Date of Patent: April 6, 1982
    Assignee: American Home Products Corporation
    Inventors: Christopher A. Demerson, Leslie G. Humber, Jean-Marie Ferland
  • Hydroxyalkanamide tetrahydrocarbazoles
    Patent number: 4319029
    Abstract: Indole derivatives characterized by having a 1,2,3,4-tetrahydrocarbazole or 1,2,3,4-tetrahydrocyclopent[b]indole nucleus with a hydroxyalkanamine substituent are disclosed. The nucleus is optionally further substituted at various positions. The derivatives are useful diuretic agents, and methods for the preparation and use are also disclosed.
    Type: Grant
    Filed: June 9, 1980
    Date of Patent: March 9, 1982
    Assignee: American Home Products Corporation
    Inventors: Gervais Dionne, Andre A. Asselin, Leslie G. Humber
  • Acyl derivatives of rapamycin
    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
  • Tricyclic indole derivatives
    Patent number: 4309348
    Abstract: Indole derivatives characterized by having a 1,3,4,9-tetrahydropyrano[3,4-b]indole or 1,3,4,9-tetrahydrothiopyrano[3,4-b]indole nucleus with a hydroxyalkanamine or lower alkoxyalkanamine substituent and a lower alkyl group at position 1 are disclosed. The nucelus is optionally further substituted at position 9 and on the aromatic ring. The derivatives are useful diuretic agents, and methods for their preparation and use are also disclosed.
    Type: Grant
    Filed: June 13, 1980
    Date of Patent: January 5, 1982
    Assignee: American Home Products Corporation
    Inventors: Andre A. Asselin, Leslie G. Humber, Gervais Dionne, Clara Revesz, Amedeo Failli
  • Pyrimido[1,6-a]indole derivatives
    Patent number: 4307234
    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: September 11, 1978
    Date of Patent: December 22, 1981
    Assignee: American Home Products Corp.
    Inventor: Ivo L. Jirkovsky
  • 1-Oxo-5H-pyrimido[2,1-C]benzoxazine-2-carboxylic acid esters
    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
  • Pharmaceutical dosage form packges
    Patent number: 4305502
    Abstract: The invention relates to packages containing shaped articles carrying chemicals, particularly to pharmaceutical dosage forms carrying pharmaceuticals. The shaped articles, which disintegrate rapidly in water are contained in depressions in sheets of filmic material and are enclosed by a covering sheet adhering to the filmic material. The shaped articles may be formed in the depressions by a sublimation process.
    Type: Grant
    Filed: July 14, 1978
    Date of Patent: December 15, 1981
    Assignee: John Wyeth & Brother Limited
    Inventors: George K. E. Gregory, David S. S. Ho
  • Ethanocarbazole derivatives and antidepressant compositions
    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
  • Preparation of (D-Trp .sup.6)-LH-RH via the heptapeptide H-Ser-Tyr-D-Trp-Leu-Arg-Pro-Gly-NH.sub.2
    Patent number: 4301066
    Abstract: Herein is described a process for preparing the decapeptide Pry-His-Trp-Ser-Tyr-D-Trp-Leu-Arg-Pro-Gly-NH.sub.2 ([D-Trp.sup.6 ]-LH-RH) by coupling Pyr-His-Trp-NHNH.sub.2 with H-Ser-Tyr-D-Trp-Leu-Arg-Pro-Gly-NH.sub.2. [D-Trp.sup.6 ]-LH-RH had been established to be an efficient agent for causing release of lutenizing hormone and follicle-stimulating hormone in mammals.
    Type: Grant
    Filed: May 8, 1980
    Date of Patent: November 17, 1981
    Assignee: American Home Products Corp.
    Inventors: Francesco Bellini, Hans U. Immer
  • Piperidino ureas and thioureas
    Patent number: 4281132
    Abstract: Compounds of formula ##STR1## in which X represents oxygen or sulphur;Y represents --CHOH-- or ##STR2## Z represent ##STR3## or a direct bond; R represents cycloalkyl group having 5 to 7 carbon atoms or an optionally substituted aryl or heteroaryl radical, or when --Z-- is a direct bond R also represents hydrogen;R.sup.1 represents hydrogen or lower alkyl;R.sup.2 represents hydrogen, halogen, lower alkyl or lower alkoxy; andR.sup.3 represents hydrogen or lower alkyl, and a pharmaceutically acceptable acid addition or quarternary ammonium salts thereof, are disclosed which possess hypotensive activity.
    Type: Grant
    Filed: October 24, 1978
    Date of Patent: July 28, 1981
    Assignee: John Wyeth & Brother Limited
    Inventor: Terence J. Ward
  • Amide derivatives
    Patent number: 4278685
    Abstract: Novel amides of formula ##STR1## wherein R.sup.1 and R.sup.2 are each halogen, R.sup.3 and R.sup.4 are each hydrogen or lower alkyl, R.sup.5 and R.sup.6 are each hydrogen or lower alkyl and n is an integer of from 1 to 3 inclusive, are anti-ulcer agents which possess anti-secretory activity.
    Type: Grant
    Filed: November 8, 1978
    Date of Patent: July 14, 1981
    Assignee: John Wyeth & Brother Limited
    Inventor: Terence J. Ward
  • Antihypertensive tricyclic isoindole derivatives
    Patent number: 4273773
    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.
    Type: Grant
    Filed: September 24, 1979
    Date of Patent: June 16, 1981
    Assignee: American Home Products Corporation
    Inventors: Christopher A. Demerson, Leslie G. Humber, Jean-Marie Ferland
  • Novel pyridine derivatives
    Patent number: 4272628
    Abstract: New 4-pyridinamine derivatives having the formula ##STR1## and their pharmaceutically acceptable acid addition salts, [wherein one of R.sup.1 and R.sup.2 is aryl or heteroaryl, the other of R.sup.1 and R.sup.2 is lower alkyl, R.sup.3 and R.sup.4 are independently hydrogen or lower alkyl, and n is 0 or 1] are described. They show CNS activity and may used as antidepressant drugs. N-([.alpha.-Phenyl]-n-propyl)-4-pyridinamine also shows anti-ulcer activity.
    Type: Grant
    Filed: June 22, 1979
    Date of Patent: June 9, 1981
    Assignee: John Wyeth & Brother Limited
    Inventors: Edwin T. Edington, Alan C. White
  • Pyridine derivatives
    Patent number: 4271304
    Abstract: Pyridine derivatives having the formula ##STR1## and their N-oxides and pharmaceutically acceptable acid addition salts, wherein R.sup.1 and R.sup.2 are independently aryl, R.sup.3 is hydrogen or lower alkyl and n is 0, 1 or 2, have CNS activity and may be used as antidepressants.
    Type: Grant
    Filed: May 9, 1979
    Date of Patent: June 2, 1981
    Assignee: John Wyeth & Brother, Ltd.
    Inventors: Edwin T. Edington, Alan C. White
  • Method of use and composition for 1,3-dihydro-3-(2-hydroxy-2-methylpropyl)-2H-isoindol-1-one
    Patent number: 4267189
    Abstract: Disclosed is pharmaceutical compositions and methods of using 1,3-dihydro-3-(2-hydroxy-2-methylpropyl)-2H-isoindol-1-one for treating ulcers in a mammal and for preventing or decreasing the secretion or availability of excessive amounts of gastric acid in a mammal suffering from hyperchlorhydria and/or associated conditions.
    Type: Grant
    Filed: September 24, 1979
    Date of Patent: May 12, 1981
    Assignee: American Home Products Corporation
    Inventor: Wilbur Lippmann