Patents Represented by Attorney Richard K. Jackson
  • Patent number: 5684039
    Abstract: Compounds of the formula: ##STR1## in which R is a straight or branched chain alkyl group of 1 to 6 carbon atoms, hydroxyalkyl of 1 to 6 carbon atoms or a cycloalkyl group of 3 to 8 carbon atoms; or a pharmaceutically acceptable salt thereof are inhibitors of dopamine synthesis and release, useful in the treatment of schizophrenia, Parkinson's Disease, Tourette's Syndrome, alcohol addiction, cocaine addiction, and addiction to analagous drugs.
    Type: Grant
    Filed: July 19, 1996
    Date of Patent: November 4, 1997
    Assignee: American Home Products Corporation
    Inventor: Richard E. Mewshaw
  • Patent number: 5684030
    Abstract: Disclosed herein are compounds of the formula: ##STR1## where R.sub.1 is substituted phenyl in which the substituents are one or two halogens, alkyl groups, carboxyl groups or alkoxycarbonyl groups;R.sub.2 is H or alkyl;R.sub.3 and R.sub.4 are, independently, H, alkyl, halogen or nitro;and n is 1, 2 or 3;or a pharmaceutically acceptable salt thereof, which are useful as inhibitors of smooth muscle cell proliferation.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: November 4, 1997
    Assignee: American Home Products Corporation
    Inventors: Hassan M. Elokdah, Sie-Yearl Chai, Theodore S. Sulkowski
  • Patent number: 5670667
    Abstract: Compounds of the formula: ##STR1## in which Z is hydrogen or a halogen; n is one of the integers 1, 2, 3, or 4; m is one of the integers 0 or 1; R is a substituted or unsubstituted aryl group in which the substituents are, independently, one or two members selected from the group consisting of alkyl, hydroxy, halo or amino groups; R.sup.2 is hydrogen or alkyl; or a pharmaceutically acceptable salt thereof, are inhibitors of dopamine synthesis and release, useful in the treatment of schizophrenia, Parkinson's Disease, Tourette's Syndrome, alcohol addiction, cocaine addiction, and addiction to analagous drugs.
    Type: Grant
    Filed: April 10, 1996
    Date of Patent: September 23, 1997
    Assignee: American Home Products Corporation
    Inventor: Richard E. Mewshaw
  • Patent number: 5668144
    Abstract: The compounds of the formula: ##STR1## where R is H, alkyl, haloalkyl, cycloalkyl, alkenyl or alkynyl; Y is oxygen, sulfur or NR.sub.2 where R.sub.2 is H or alkyl; or a pharmaceutically acceptable salt thereof, are useful centrally active muscarinic agents.
    Type: Grant
    Filed: October 30, 1996
    Date of Patent: September 16, 1997
    Assignee: American Home Products Corporation
    Inventors: Annmarie L. Sabb, Reinhardt P. Stein
  • Patent number: 5663363
    Abstract: The compound of formula I ##STR1## in which R is alkynyl; and X and Y are, independently, alkyl, halo, perfluoralkyl, perfluoralkoxy, or, taken together, X and Y are ortho substituted trimethylene or tetramethylene are useful for increasing blood serum HDL levels.
    Type: Grant
    Filed: November 21, 1996
    Date of Patent: September 2, 1997
    Assignee: American Home Products Corporation
    Inventors: Hassan M. Elokdah, Sie-Yearl Chai, Theodore S. Sulkowski, Donald P. Strike
  • Patent number: 5663194
    Abstract: Described herein are compounds of the formula: ##STR1## in which n is 1, 2 or 3; m is 0 or 1; and R is a substituted or unsubstituted phenyl group in which the substitutents are, independently, one or two members selected from the group consisting of alkyl, hydroxy, halo or amino groups or R is alkyl of 1 to 6 carbon atoms or hydroxyalkyl of 1 to 6 carbon atoms; or a pharmaceutically acceptable salt thereof, which are inhibitors of dopamine synthesis and release, and are useful in the treatment of schizophrenia, Parkinson's Disease, Tourette's Syndrome, alcohol addiction, cocaine addiction, and addiction to analagous drugs.
    Type: Grant
    Filed: July 19, 1996
    Date of Patent: September 2, 1997
    Inventor: Richard E. Mewshaw
  • Patent number: 5637731
    Abstract: This disclosure describes novel substituted oxotremorine derivatives of formula I having nitrogen, oxygen or sulfur groups and the prodrug forms of these derivatives. The compounds have cholinergic activity. Also disclosed are methods for treating diseases of the central nervous system in mammals employing the compounds, pharmaceutical preparations containing the compounds and the processes for the production of the compounds.
    Type: Grant
    Filed: April 30, 1996
    Date of Patent: June 10, 1997
    Assignee: American Home Products Corporation
    Inventors: Eugene J. Trybulski, Richard H. Kramss, Herbert J. Brabander
  • Patent number: 5605909
    Abstract: The compounds of formula I are smooth muscle relaxants: ##STR1## wherein R.sub.1 is hydrogen, alkyl, cycloalkyl, alkanoyl, alkylsulfonyl, aroyl, arylalkenoyl, arylsulfonyl, arylalkanoyl or arylalkylsulfonyl; R.sub.
    Type: Grant
    Filed: February 14, 1996
    Date of Patent: February 25, 1997
    Assignee: American Home Products Corporation
    Inventors: John A. Butera, Schuyler A. Antane, Bradford H. Hirth
  • Patent number: 5602151
    Abstract: The compounds of the formula: ##STR1## in which X is ##STR2## where R.sup.7 is hydrogen, alkyl, hydroxy, alkanoyloxy, hydroxyalkyl, hydroxycarbonyl, alkoxycarbonyl, phenyl or substituted phenyl, in which the substituent is alkyl, alkoxy, halo, nitro, cyano, haloalkyl, perhaloalkyl or dialkylaminoalkyl; R.sup.8 is hydrogen or alkyl or R.sup.7 and R.sup.8 taken together are polymethylene; R.sup.9 is hydrogen, alkyl, phenyl or substituted phenyl, in which the substituent is alkyl, alkoxy, halo, nitro, cyano or perhaloalkyl; R.sup.10 is hydrogen, alkyl or gemdialkyl; n is one of the integers 0, 1 or 2; and R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are, independently, hydrogen, alkyl, alkoxy, halo, nitro, cyano or perhaloalkyl, alkoxycarbonyl or hydroxycarbonyl; and when X is --NR.sup.9 -- or R.sup.7 is an amino alkyl group, a pharmaceutically acceptable salt thereof; are useful as inhibitors of cholesterol ester hydrolase.
    Type: Grant
    Filed: December 15, 1995
    Date of Patent: February 11, 1997
    Assignee: American Home Products Corporation
    Inventors: Richard E. Mewshaw, Thomas J. Commons, Donald P. Strike
  • Patent number: 5602128
    Abstract: The compounds ##STR1## where R and R.sup.6 are members independently selected from the group consisting of H, CN, OR.sup.2, NO.sub.2, NR.sup.2 R.sup.3, NR.sup.2 COR.sup.3, NR.sup.2 COOR.sup.3, COR.sup.2, COOR.sup.2, CONR.sup.2 R.sup.3, SR.sup.2, SOR.sup.2, SO.sub.2 R.sup.2, SO.sub.2 NR.sup.2 R.sup.3, alkyl, alkenyl, alkynyl, perhaloalkyl, and a halogen; in which R.sup.2 and R.sup.3 are alkyl, alkenyl, alkynyl, phenyl, or benzyl; R.sup.4 is a member selected from the group consisting of H, alkyl, heteroalkyl, in which the hetero atom is oxygen, sulfur or nitrogen, alkenyl and alkynyl; R.sup.5 is ##STR2## where X is O, S or NR.sup.7 and R.sup.7 is H or alkyl and n is 1, 2, 3, 4, 5, or 6; or a pharmaceutically acceptable salt thereof, are useful anxiolytic/antidepressant agents.
    Type: Grant
    Filed: December 2, 1994
    Date of Patent: February 11, 1997
    Assignee: American Home Products Corporation
    Inventors: Reinhardt B. Baudy, Scott C. Berta
  • Patent number: 5599829
    Abstract: A method for increasing blood serum HDL cholesterol levels in a mammal in need of increased HDL cholesterol blood serum levels, which comprises administering to said mammal, an effective amount of a compound of formula I: ##STR1## wherein R is phenyl or phenyl optionally substituted with one or more groups selected from halogen, alkyl, perfluoroalkyl, alkoxy, perfluoroalkoxy, hydroxy, alkanoyloxy, aroyloxy or arylalkanoyloxy; R.sup.3 is alkyl, aryl or arylalkyl; or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: November 28, 1995
    Date of Patent: February 4, 1997
    Assignee: American Home Products Corporation
    Inventors: Hassan M. Elokdah, Theodore S. Sulkowski, Donald P. Strike
  • Patent number: 5591823
    Abstract: Chimeric DNA fragments are provided which include a nucleotide sequence substantially the same as that which codes for the HA surface protein of an influenza A virus having five immunodominant antigenic sites, wherein a nucleotide sequence substantially the same as that which codes for a foreign epitope is inserted into the nucleotide sequence of an antigenic site. Corresponding chimeric peptides, expression vectors, and transformed hosts are provided as well. These peptides are useful in providing vaccines against the respective antigens and in test kits to detect the exposure to such antigens. Additionally, these peptides or their corresponding antibodies are useful in methods of treatment and prevention of the manifestations of exposure to these antigens, including immunotherapy.
    Type: Grant
    Filed: December 17, 1993
    Date of Patent: January 7, 1997
    Assignee: American Home Products Corporation
    Inventors: Paul P. Hung, Shaw-Guang L. Lee, Narender K. Kalyan
  • Patent number: 5554607
    Abstract: A method for increasing the HDL cholesterol concentration in the blood of a mammal in need of increased HDL cholesterol blood concentration, which comprises administering to said mammal, orally or parenterally, a compound of formula I: ##STR1## wherein R is alkyl; a substituted or unsubstituted aromatic N, O or S heterocycle; substituted or unsubstituted aryl, arylalkyl, benzhydryl or indanyl, in which the substituents are one to three members independently selected from the group consisting of alkyl, alkoxy, alkylthio, alkenyl, alkynyl, halo, perfluoroalkyl, perfluoroalkyl or hydroxy; and R.sup.1 is aryl, alkyl, alkenyl, alkynyl or substituted aryl where the substituents are one to three members independently selected from the group consisting of alkyl, alkoxy, alkylthio, alkenyl, alkynyl, halo, perfluoroalkyl, perfluoroalkoxy or hydroxy.
    Type: Grant
    Filed: November 28, 1995
    Date of Patent: September 10, 1996
    Assignee: American Home Products Corporation
    Inventors: Hassan M. Elokdah, Sie-Yearl Chai, Theodore S. Sulkowski, Donald P. Strike
  • Patent number: 5550257
    Abstract: This disclosure describes novel substituted oxotremorine derivatives of formula I having nitrogen, oxygen or sulfur groups and the prodrug forms of these derivatives. The compounds have cholinergic activity. Also disclosed are methods for treating diseases of the central nervous system in mammals employing the compounds, pharmaceutical preparations containing the compounds and the processes for the production of the compounds.
    Type: Grant
    Filed: February 22, 1995
    Date of Patent: August 27, 1996
    Assignee: American Cyanamid Company
    Inventors: Eugene J. Trybulski, Richard H. Kramss, Herbert J. Brabander
  • Patent number: 5547948
    Abstract: A sugar coating composition for application to a compressed medicinal tablet comprising a sugar, a dose of a hormonal steroid and a steroid release rate controlling amount of microcrystalline cellulose.
    Type: Grant
    Filed: January 17, 1995
    Date of Patent: August 20, 1996
    Assignee: American Home Products Corporation
    Inventor: Reginald J. Barcomb
  • Patent number: 5541199
    Abstract: Compounds of the formula: ##STR1## in which n is one of the integers 1, 2, 3,or 4; m is one of the integers 0 or 1; R is ##STR2## or a pharmaceutically acceptable salt thereof, are inhibitors of dopamine synthesis and release, useful in the treatment of schizophrenia, Parkinson's Disease, Tourette's Syndrome, alcohol addiction, cocaine addiction, and addiction to analagous drugs.
    Type: Grant
    Filed: June 2, 1995
    Date of Patent: July 30, 1996
    Assignee: American Home Products Corporation
    Inventor: Richard E. Mewshaw
  • Patent number: 5538977
    Abstract: Disclosed are 3-substituted-7-[3-(imidazol-1-yl)phenyl]-pyrazolo[1,5-a]pyrimidines of the formula: ##STR1## wherein R.sup.1, R.sup.3 and R.sup.4 are defined in the specification which compounds have anxiolytic, anti-convulsant, sedative-hypnotic and skeletal muscle relaxant activity.
    Type: Grant
    Filed: March 17, 1995
    Date of Patent: July 23, 1996
    Assignee: American Cyanamid Company
    Inventors: John P. Dusza, Jay D. Albright, Andrew S. Tomcufcik
  • Patent number: 5536741
    Abstract: The compound of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are, independent from each other, hydrogen, alkyl or cyclic or bicyclic alkyl; R.sub.3 is an acyl substituent selected from the group consisting of formyl, alkanoyl, alkenoyl, alkylsulfonyl, aroyl, arylalkenoyl, arylsulfonyl, arylalkanoyl or arylalkylsulfonyl; A is selected from the group consisting of: ##STR2## wherein R.sub.4 is hydrogen, alkyl, perfluoroalkyl, alkoxy, perfluoroalkoxy, amino, alkylamino, dialkylamino, alkylsulfonamido, alkylcarboxamido, nitro, cyano or carboxyl; or a pharmaceutically acceptable salt thereof, are smooth muscle relaxants.
    Type: Grant
    Filed: May 31, 1995
    Date of Patent: July 16, 1996
    Assignee: American Home Products Corporation
    Inventors: Madelene M. Antane, John A. Butera, Bradford H. Hirth, Schuyler A. Antane
  • Patent number: 5536731
    Abstract: The compounds of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are, independent from each other, hydrogen, alkyl, or cyclic or bicyclic alkyl; R.sub.3 is an acyl substituent selected from the group consisting of formyl, alkanoyl, alkenoyl, alkylsulfonyl, aroyl, arylalkenoyl, arylsulfonyl, arylalkanoyl or arylalkylsulfonyl; A is selected from the group consisting of: ##STR2## wherein R.sub.4 is hydrogen, alkyl, perfluoroalkyl, alkoxy, perfluoroalkoxy, amino, alkylamino, dialkylamino, alkylsulfonamido, alkylcarboxamido, nitro, cyano or carboxyl; or a pharmaceutically acceptable salt thereof, are smooth muscle relaxants.
    Type: Grant
    Filed: May 31, 1995
    Date of Patent: July 16, 1996
    Assignee: American Home Products Corporation
    Inventors: Madelene M. Antane, John A. Butera, Bradford H. Hirth, Schuyler A. Antane
  • Patent number: 5532245
    Abstract: The compounds of the formula: ##STR1## wherein R.sub.1 is hydrogen, straight or branched chain alkyl, cyclic or bicyclic alkyl, alkanoyl, alkylsulfonyl, aroyl, arylalkenoyl, arylsulfonyl, arylalkanoyl or arylalkylsulfonyl; R.sub.2 is hydrogen, straight or branched chain alkyl or cyclic or bicyclic alkyl; A is selected from the following: ##STR2## wherein R.sub.9 is hydrogen, alkyl, perfluoroalkyl, alkoxy, perfluoroalkoxy, amino, mono- or dialkylamino, alkylsulfonamido, alkylcarboxamido, nitro, cyano, carboxyl, chloro, bromo, fluoro or iodo; n is an integer from 0 to 6; R.sub.3 and R.sub.4, independent from each other, are hydrogen, straight or branched chain alkyl, cyclic or bicyclic alkyl, perfluoroalkyl, hydroxyalkyl, alkoxyalkyl, fluoro, or, when taken together, form a spirocyclic ring; R.sub.5 and R.sub.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: July 2, 1996
    Assignee: American Home Products Corporation
    Inventors: John A. Butera, Schuyler A. Antane, Bradford H. Hirth