Patents Represented by Attorney Richard K. Jackson
  • Patent number: 5451584
    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 alkynyl of 2 to 8 carbon atoms or 1-alkynylcycloalkyl in which the alkynyl group contains 2 to 6 carbon atoms and the cycloalkyl group contains 3 to 10 carbon atoms;or a pharmaceutically acceptable salt thereof, are useful anxiolytic/antidepressant agents.
    Type: Grant
    Filed: November 10, 1994
    Date of Patent: September 19, 1995
    Assignee: American Home Products Corporation
    Inventors: Reinhardt B. Baudy, Scott C. Berta
  • Patent number: 5439915
    Abstract: The compound of the formula: ##STR1## where R.sub.1 and R.sub.7 are independently hydrogen, fluorine, chlorine, bromine, iodine, trifluoromethyl, cyano, nitro, CO.sub.2 H, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.10 alkenyl, C.sub.1 -C.sub.6 alkoxy, C.sub.3 -C.sub.8 cycloalkyl, cycloalkylalkyl, C.sub.3 -C.sub.8 cycloalkyloxy, C.sub.2 -C.sub.7 alkylcarbonyl, C.sub.2 -C.sub.7 alkylcarbonyloxy, C.sub.2 -C.sub.7 alkoxycarbonyl, mono or di-alkylaminocarbonyl, tetrazolyl,-OH,-(CH.sub.2).sub.1-6 OH, -SH, -NH.sub.2 or-(CH.sub.2).sub.1-6 NR.sub.8 R.sub.9 where R.sub.8 is hydrogen, C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.7 alkylcarbonyl, C.sub.2 -C.sub.7 alkoxycarbonyl and R.sub.9 is hydrogen or C.sub.1 -C.sub.6 alkyl; R.sub.2 is hydrogen or C.sub.1 -C.sub.6 alkyl; R.sub.3 and R.sub.4 are hydrogen or taken together with the carbon atoms to which they are attached form a double bond; R.sub.5 is hydrogen or C.sub.1 -C.sub.6 alkyl; R.sub.6 is C.sub. 1 -C.sub.12 alkyl, C.sub.3 to C.sub.8 cycloalkyl, cycloalkylalkyl, or C.sub.
    Type: Grant
    Filed: October 20, 1994
    Date of Patent: August 8, 1995
    Assignee: American Home Products Corporation
    Inventors: Thomas J. Commons, Christa M. LaClair, Susan Christman
  • Patent number: 5437797
    Abstract: Method for removal of organic and inorganic mercury contaminants from a biological vaccine production facility.
    Type: Grant
    Filed: June 14, 1994
    Date of Patent: August 1, 1995
    Assignee: American Home Products Corporation
    Inventor: Edward G. Helmig
  • Patent number: 5428151
    Abstract: A process for the production of medrogestone, in which, in an intermediate step, the solvate 3.beta.,5.alpha.,6.beta.-trihydroxy-6.alpha.,17.alpha.-dimethylpregnan-20- one monomethanolate is obtained as a solid, stable compound by displacing the organic solvent from a solution of of 3.beta.,5.alpha.,6.beta.-trihydroxy-6.alpha.,17.alpha.-dimethylpregnan-20- one with a lower alkanol, and a Diels-Alder adduct of 6-methylene-17.alpha.-methylpregn-4-ene-3,20-dione with maleic anhydride is used as an intermediate for production of the corresponding dicarboxylic acid salt for removal of 6-methylene-17.alpha.-methylpregn-4-ene-3,20-dione contamination of the desired product. Another intermediate, 6.beta.-hydroxy-6.alpha.,17.alpha.-dimethylpregn-4-ene-3,20-dione, has been found to prevent smooth muscle proliferation and is useful in the treatment of atherosclerosis and restinosis.
    Type: Grant
    Filed: May 5, 1994
    Date of Patent: June 27, 1995
    Assignee: American Home Products Corporation
    Inventors: Michael W. Winkley, Robert D. Mitchell
  • Patent number: 5403853
    Abstract: The compounds of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are, independently, hydrogen, straight or branched chain alkyl or mono- or bi-cyclic alkyl;A is a substituted phenyl group containing one or two substituents selected from cyano, nitro, alkyl, perfluoroalkyl, alkoxy, perfluoroalkoxy, amino, alkylamino, dialkylamino, sulfamyl, alkylsulfonamido, arylsulfonamido, alkylcarboxamido, arylcarboxamido, alkylsulfone, perfluoroalkylsulfone, arylsulfone, chloro, bromo, fluoro, iodo, 1-imidazolyl or carboxyl; or a pharmaceutically acceptable salt thereof, are smooth muscle relaxants.
    Type: Grant
    Filed: June 13, 1994
    Date of Patent: April 4, 1995
    Assignee: American Home Products Corporation
    Inventors: John A. Butera, Schuyler A. Antane
  • Patent number: 5403854
    Abstract: The compounds of the formula: ##STR1## wherein: R.sub.1 and R.sub.2 are, independently, hydrogen, straight or branched chain alkyl or mono- or bi-cyclic alkyl;A is a benzodiazole of the formula: ##STR2## wherein: R.sub.3 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: June 13, 1994
    Date of Patent: April 4, 1995
    Assignee: American Home Products Corporation
    Inventors: John A. Butera, Schuyler A. Antane
  • Patent number: 5401769
    Abstract: A compound of formula A: ##STR1## wherein R.sup.1 and R.sup.2 are, independently, hydrogen, fluorine, chlorine, bromine, iodine, trifluoromethyl, cyano, nitro, alkyl, alkoxy, --CO.sub.2 H, alkylcarbonyl, alkylcarbonyloxy, alkoxycarbonyl, alkoxycarbonyloxy, mono or dialkylaminocarbonyl, or mono or dialkylaminocarbonyloxy; R.sup.3 is hydrogen or alkyl; R.sup.4 is alkyl, cycloalkylalkyl or phenylalkyl or substituted phenylalkyl, and the substituent on the benzene ring is alkyl, alkoxy, halo, nitro, cyano, trifluoromethyl or phenyl, are anti-cholesterolemic agents.
    Type: Grant
    Filed: February 2, 1994
    Date of Patent: March 28, 1995
    Assignee: American Home Products Corporation
    Inventors: Thomas J. Commons, Richard E. Mewshaw, Donald P. Strike
  • Patent number: 5401753
    Abstract: The compounds of the formula: ##STR1## wherein: R.sub.1 and R.sub.2 are, independently, hydrogen, straight or branched chain alkyl or mono- or bi-cyclic alkyl;A is quinoline group which may be substituted by 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: June 13, 1994
    Date of Patent: March 28, 1995
    Assignee: American Home Products Corporation
    Inventors: John A. Butera, Schuyler A. Antane
  • Patent number: 5399697
    Abstract: The compounds of the formula: ##STR1## in which X, Y and Z are, independently, hydrogen, halogen, hydroxy, nitro, cyano, carboxyl, trifluoromethyl, phenyl, amino, alkylamino, dialkylamino, alkyl, alkoxy or phenylalkyloxy; R.sub.1 is thienyl, imidazolyl, thiazolyl, pyridinyl, quinolinyl, pyrimidinyl, pyrazinyl, benzamidazolyl, phenylalkylpiperidinyl or morpholino or athaae analogous hetercyclic groups with from one to three substituents selected from halogen, hydroxy, nitro, cyano, carboxyl, trifluoromethyl, phenyl, amino, alkylamino of 1 to 6 carbon atoms, dialkylamino in which each alkyl group has 1 to 6 carbon atoms, alkyl of 1 to 6 carbon atoms, or alkoxy of 1 to 6 carbon atoms; R.sub.2 is hydrogen, alkyl, cycloalkyl, phenyl, benzyl or substituted phenyl or benzyl in which said substituent is alkyl, alkoxy, halogen, cyano, trifluoromethyl amino, nitro, alkylamino or dialkylamino; and a pharmaceutically acceptable salt thereof; are ACAT inhibitors, some of which possess antioxidant properties.
    Type: Grant
    Filed: November 15, 1993
    Date of Patent: March 21, 1995
    Assignee: American Home Products Corporation
    Inventors: William F. Fobare, Donald P. Strike
  • Patent number: 5397790
    Abstract: The compounds of the formula: ##STR1## wherein: R.sub.1 and R.sub.2 are, independently, hydrogen, straight or branched chain alkyl or mono- or bi-cyclic alkyl; andA is an isoquinoline group which may be substituted by 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: June 13, 1994
    Date of Patent: March 14, 1995
    Assignee: American Home Products Corporation
    Inventors: John A. Butera, Schuyler A. Antane
  • Patent number: 5391571
    Abstract: The compounds of the formula: ##STR1## in which R.sup.1 is alkyl of 4 or more carbon atoms, cycloalkyl, 1-adamantyl, 2-adamantyl, 3-noradamantyl, 3-methyl-1-adamantyl, 1-fluorenyl, 9-fluorenyl, cycloalkylalkyl, phenyl, substituted phenyl, alkyl, alkoxy, halo, nitro, cyano or trifluoromethyl, phenylalkyl or substituted phenylalkyl, where the substituent on the benzene ring is alkyl, alkoxy, halo, nitro, cyano, trifluoromethyl or phenyl; R.sup.2 is hydrogen, alkyl or R.sup.1 taken with R.sup.2 and the nitrogen atom to which they are attached form a heterocyclic moiety of the formula: ##STR2## wherein ##STR3## in which 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.
    Type: Grant
    Filed: May 13, 1993
    Date of Patent: February 21, 1995
    Assignee: American Home Products Corporation
    Inventors: Richard E. Mewshaw, Thomas J. Commons, Donald P. Strike
  • Patent number: 5389672
    Abstract: The present invention relates to novel 4- or 5-(substituted sulfonyl) methyl-3(2H)-furanones having the formula (I) ##STR1## wherein R.sup.1 and R.sup.2 are independently alkyl containing 1 to 6 branched or straight chain carbon atoms, phenyl, or halogen substituted phenyl; or R.sup.1 and R.sup.2 are joined by 5 to 7 carbon atoms;R.sup.3 and R.sup.4 are independently hydrogen, alkyl containing 1 to 6 branched or straight chain carbon atoms or R.sup.3 and R.sup.4 are joined by 4 to 6 carbon atoms;R.sup.
    Type: Grant
    Filed: February 16, 1994
    Date of Patent: February 14, 1995
    Assignee: American Home Products Corporation
    Inventors: Steven W. Felman, Ivo L. Jirkovsky, Kevin A. Memoli
  • Patent number: 5389671
    Abstract: The present invention relates to novel 4- or 5-(substituted sulfonyl) methyl-3(2H)-furanones having the formula (I) ##STR1## wherein R.sup.1 and R.sup.2 are independently alkyl containing 1 to 6 branched or straight chain carbon atoms, phenyl, or halogen substituted phenyl; or R.sup.1 and R.sup.2 are joined by 5 to 7 carbon atoms;R.sup.3 and R.sup.4 are independently hydrogen, alkyl containing 1 to 6 branched or straight chain carbon atoms or R.sup.3 and R.sup.4 are joined by 4 to 6 carbon atoms;R.sup.
    Type: Grant
    Filed: February 16, 1994
    Date of Patent: February 14, 1995
    Assignee: American Home Products Corporation
    Inventors: Steven W. Felman, Ivo L. Jirkovsky, Kevin A. Memoli
  • Patent number: 5389673
    Abstract: The present invention relates to novel 4- or 5-(substituted sulfonyl) methyl-3(2H)-furanones having the formula (I) ##STR1## wherein R.sup.1 and R.sup.2 are independently alkyl containing 1 to 6 branched or straight chain carbon atoms, phenyl, or halogen substituted phenyl; or R.sup.1 and R.sup.2 are joined by 5 to 7 carbon atoms;R.sup.3 and R.sup.4 are independently hydrogen, alkyl containing 1 to 6 branched or straight chain carbon atoms or R.sup.3 and R.sup.4 are joined by 4 to 6 carbon atoms;R.sup.
    Type: Grant
    Filed: February 16, 1994
    Date of Patent: February 14, 1995
    Assignee: American Home Products Corporation
    Inventors: Steven W. Felman, Ivo L. Jirkovsky, Kevin A. Memoli
  • Patent number: 5380853
    Abstract: The compounds of the formula: ##STR1## in which X, Y and Z are, independently, hydrogen, halogen, hydroxy, nitro, cyano, carboxyl, trifluoromethyl, phenyl, amino, alkylamino, dialkylamino, alkyl, alkoxy or phenylalkyloxy; R.sub.1 is thienyl, imidazolyl, thiazolyl, pyridinyl, quinolinyl, pyrimidinyl, pyrazinyl, benzamidazolyl, phenylalkylpiperidinyl or morpholino or athaae analogous hetercyclic groups with from one to tahree substituents selected from halogen, hydroxy, nitro, cyano, carboxyl, trifluoromethyl, phenyl, amino, alkylamino of 1 to 6 carbon atoms, dialkylamino in which each alkyl group has 1 to 6 carbon atoms, alkyl of 1 to 6 carbon atoms, or alkoxy of 1 to 6 carbon atoms; R.sub.2 is hydrogen, alkyl, cycloalkyl, phenyl, benzyl or substituted phenyl or benzyl in which said substituent is alkyl, alkoxy, halogen, cyano, trifluoromethyl amino, nitro, alkylamino or dialkylamino; and a pharmaceutically acceptable salt thereof; are ACAT inhibitors, some of which possess antioxidant properties.
    Type: Grant
    Filed: November 15, 1993
    Date of Patent: January 10, 1995
    Assignee: American Home Products Corporation
    Inventors: William F. Fobare, Donald P. Strike
  • Patent number: 5376547
    Abstract: Des-epidermal growth factor homologous--plasminogen activators with greatly diminished affinity for liver membranes.
    Type: Grant
    Filed: January 29, 1988
    Date of Patent: December 27, 1994
    Assignee: American Home Products Corporation
    Inventors: Narender K. Kalyan, Shawguang L. Lee, Paul P. Hung
  • Patent number: 5373009
    Abstract: A compound of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are, independently, halo, trifluoromethyl, cyano, nitro, alkyl, alkoxy, --CO.sub.2 H, alkylcarbonyl, alkylcarbonyloxy, alkoxycarbonyl, mono- or di-alkylaminocarbonyl, or mono- or di-alkylaminocarbonyloxy;m is 0, 1 or 2 andR.sup.3 is alkyl;n and p are, independently, 0, 1 or 2;X is O, S or CR.sup.4 R.sup.5,where R.sup.4 and R.sup.5 are, independently, H or alkyl or R.sup.4 and R.sup.5 together with the interposed carbon atom form a 3 to 8 membered carbocyclic ring, are anti-cholesterolemic agents.
    Type: Grant
    Filed: February 2, 1994
    Date of Patent: December 13, 1994
    Assignee: American Home Products Corporation
    Inventors: Thomas J. Commons, Donald P. Strike
  • Patent number: 5354763
    Abstract: The compounds of the formula: ##STR1## wherein: R.sub.1 and R.sub.2 are, independently, hydrogen, straight or branched chain alkyl or mono- or bi-cyclic alkyl;A is an N-heterocycle which may be substituted by alkyl, perfluoroalkyl, alkoxy, perfluoroalkoxy, amino, alkylamino, dialkylamino, alkylsulfonamido, alkylcarboxamido, nitro, cyano or carboxyl;or, A is a substituted phenyl group containing one or two substituents selected from cyano, nitro, alkyl, perfluoroalkyl, alkoxy, perfluoroalkoxy, amino, alkylamino, dialkylamino, sulfamyl, alkylsulfonamido, arylsulfonamido, alkylcarboxamido, arylcarboxamido, alkylsulfone, perfluoroalkylsulfone, arylsulfone, chloro, bromo, fluoro, iodo, 1-imidazolyl or carboxyl;or a pharmaceutically acceptable salt thereof, are smooth muscle relaxants.
    Type: Grant
    Filed: November 17, 1993
    Date of Patent: October 11, 1994
    Assignee: American Home Products Corporation
    Inventors: John A. Butera, Schuyler A. Antane
  • Patent number: 5288717
    Abstract: This invention presents alkali metal salts of 8,9-dehydroestrone, its sulfate ester, and stable compositions thereof, as well as processes for their production. The sulfate ester salts are useful in estrogen replacement therapy.
    Type: Grant
    Filed: December 3, 1992
    Date of Patent: February 22, 1994
    Assignee: American Home Products Corporation
    Inventors: Panolil C. Raveendranath, John A. Wichtowski
  • Patent number: 5281714
    Abstract: The compounds of the formula: ##STR1## in which X, Y and Z are, independently, hydrogen, halogen, hydroxy, nitro, cyano, carboxyl, trifluoromethyl, phenyl, amino, alkylamino, dialkylamino, alkyl, alkoxy or phenylalkyloxy; R.sub.1 is thienyl, imidazolyl, thiazolyl, pyridinyl, quinolinyl, pyrimidinyl, pyrazinyl, benzamidazolyl, phenylalkylpiperidinyl or morpholino or athaae analogous hetercyclic groups with from one to tahree substituents selected from halogen, hydroxy, nitro, cyano, carboxyl, trifluoromethyl, phenyl, amino, alkylamino of 1 to 6 carbon atoms, dialkylamino in which each alkyl group has 1 to 6 carbon atoms, alkyl of 1 to 6 carbon atoms, or alkoxy of 1 to 6 carbon atoms; R.sub.2 is hydrogen, alkyl, cycloalkyl, phenyl, benzyl or substituted phenyl or benzyl in which said substituent is alkyl, alkoxy, halogen, cyano, trifluoromethyl amino, nitro, alkylamino or dialkylamino; and a pharmaceutically acceptable salt thereof; are ACAT inhibitors, some of which possess antioxidant properties.
    Type: Grant
    Filed: December 30, 1992
    Date of Patent: January 25, 1994
    Assignee: American Home Products Corporation
    Inventors: William F. Fobare, Donald P. Strike