Patents Represented by Attorney Richard K. Jackson
  • Patent number: 5530025
    Abstract: The compounds of formula I: ##STR1## wherein R.sub.1 and R.sub.2 are hydrogen, alkyl or cyclic or bicyclic alkyl; R.sub.3 is formyl, alkanoyl, alkenoyl, alkylsulfonyl, aroyl, arylalkenoyl, arylsulfonyl arylalkanoyl or arylalkylsulfonyl; A is a substituted phenyl group of the following formula: ##STR2## wherein R.sub.5 is cyano and R.sub.6 is alkyl, chloro, bromo, fluoro or iodo and pharmaceutically acceptable salts thereof, are smooth muscle relaxants.
    Type: Grant
    Filed: June 2, 1995
    Date of Patent: June 25, 1996
    Assignee: American Home Products Corporation
    Inventors: Madelene M. Antane, John A. Butera, Bradford H. Hirth, Schuyler A. Antane
  • Patent number: 5527794
    Abstract: The compound of the formula: ##STR1## where R.sub.1 and R.sub.5 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.6 and R.sub.7 are independently H, C.sub.1 -C.sub.10 alkyl, C.sub.2 -C.sub.10 alkenyl, C.sub.3 -C.sub.
    Type: Grant
    Filed: May 23, 1995
    Date of Patent: June 18, 1996
    Assignee: American Home Products Corporation
    Inventors: Thomas J. Commons, Christa M. LaClair, Susan Christman
  • Patent number: 5523427
    Abstract: The solvate 3.beta.,5.alpha.,6.beta.-trihydroxy-6.alpha.,17.alpha.-dimethylpregnan-20- one monomethanolate, a crystalline intermediate in the manufacture of medrogestone, and a method for its production by displacing the solvent in a solution of 3.beta.,5.alpha.,6.beta.-trihydroxy-6.alpha.,17.alpha.-dimethylpregnan-20- one with methanol are disclosed.
    Type: Grant
    Filed: March 14, 1995
    Date of Patent: June 4, 1996
    Assignee: American Home Products Corporation
    Inventor: Michael W. Winkley
  • Patent number: 5519025
    Abstract: This invention provides anxiolytic/antidepressant agents of the formula: ##STR1## in which R.sup.1 is alkyl;R.sup.2 and R.sup.3 are alkyl or taken together they are polymethylene;R.sup.4 is hydrogen or alkyl;R.sup.5 is phenyl, benzyl, substituted phenyl, or substituted benzyl in which the substituents are hydroxy, halo, alkoxy, trifluoromethyl, nitro, cyano, alkoxycarbonyl, amino or dialkylamino;or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: April 10, 1995
    Date of Patent: May 21, 1996
    Assignee: American Home Products Corporation
    Inventors: John P. Yardley, Horace Fletcher, III
  • Patent number: 5519153
    Abstract: A process for the production of 6,17.alpha.-dimethylpregna-4,6-diene-3,20-dione which comprises isolating 3.beta.,5.alpha., 6.beta.-trihydroxy- 6.alpha.,17.alpha.- dimethylpregnan-20-one monomethanolate from the solution of a Grignard reaction product of 3.beta.,5.alpha.-dihydroxy -17.alpha.-methyl-17.beta.-carbomethoxyandrostane-6-one and a methylmagnesium halide by solvent displacement with methanol; oxidizing the monomethanolate to the 3,20-dione; dehydrating the said 3,20-dione to the 4-ene-3,20-dione; dehydrating the 4-ene-3,20 dione; removing a 6-methylene-4-ene-3,20-dione byproduct and isolating the desired product.
    Type: Grant
    Filed: March 14, 1995
    Date of Patent: May 21, 1996
    Assignee: American Home Products Corporation
    Inventor: Michael W. Winkley
  • Patent number: 5512574
    Abstract: The compound of the formula: ##STR1## in which Y is oxygen or sulfur; A is oxygen, sulfur or --NR.sub.2, where R.sub.2 is hydrogen or alkyl; R is --CH.sub.2 CH.sub.3, --CH.sub.2 CH.sub.2 CH.sub.3, --CH(CH.sub.3).sub.2, --CH.sub.2 CH(CH.sub.3).sub.2, --CH.sub.2 CF.sub.3, --CH.sub.2 CH.sub.2 CF.sub.3, --CH(CF.sub.3).sub.2, --CH.sub.2 CH(CF.sub.3).sub.2, --C.sub.3 H.sub.5, --CH.sub.2 C.sub.3 H.sub.5, --CH.sub.2 CH.sub.2 C.sub.3 H.sub.5, --C.sub.4 H.sub.7, --CH.sub.2 C.sub.4 H.sub.7, --C.sub.5 H.sub.9, --CH.sub.2 C.sub.9, --C.sub.6 H.sub.10, --CH.sub.2 C.sub.6 H.sub.10, --C.sub.4 H.sub.3 S, --CH.sub.2 C.sub.4 H.sub.3 S, --C.sub.6 H.sub.5 or --CH.sub.2 C.sub.6 H.sub.5 ; and n is one of the integers 1 or 2; or a pharmaceutically acceptable salt thereof are centrally active muscarinic agents.
    Type: Grant
    Filed: March 31, 1995
    Date of Patent: April 30, 1996
    Assignee: American Home Products Corporation
    Inventors: George E. M. Husbands, Joseph Tokolics
  • Patent number: 5512585
    Abstract: The compound of the formula: ##STR1## wherein: R.sub.1 and R.sub.2 are, independent from each other, hydrogen, C.sub.1-10 straight chain alkyl, C.sub.1-10 branched alkyl, or C.sub.3-10 cyclic or bicyclic alkyl;R.sub.3 is an acyl substituent selected from the group consisting of formyl, alkanoyl of 2 to 7 carbon atoms, alkenoyl of 3 to 7 carbon atoms, alkylsulfonyl of 1 to 7 carbon atoms, aroyl of 7 to 12 carbon atoms, arylalkenoyl of 9 to 20 carbon atoms, arylsulfonyl of 6 to 12 carbon atoms, arylalkanoyl of 8 to 12 carbon atoms or arylalkylsulfonyl of 7 to 12 carbon atoms;A is selected from the group consisting of: ##STR2## wherein: R.sub.4 is hydrogen, C.sub.1-6 alkyl, C.sub.1-6 perfluoroalkyl, C.sub.1-6 alkoxy, C.sub.1-6 perfluoroalkoxy, amino, C.sub.1-6 alkylamino, C.sub.2-12 dialkylamino, C.sub.1-6 alkylsulfonamido, alkylcarboxamido containing 2 to 7 carbon atoms, nitro, cyano or carboxyl;or a pharmaceutically acceptable salt thereof, are smooth muscle relaxants.
    Type: Grant
    Filed: June 2, 1995
    Date of Patent: April 30, 1996
    Assignee: American Home Products Corporation
    Inventors: Madelene M. Antane, John A. Butera, Bradford H. Hirth, Schuyler A. Antane
  • Patent number: 5512565
    Abstract: The compounds of the formula: ##STR1## in which ##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: March 30, 1995
    Date of Patent: April 30, 1996
    Assignee: American Home Products Corporation
    Inventors: Richard E. Mewshaw, Thomas J. Commons, Donald P. Strike
  • Patent number: 5510478
    Abstract: The compound of the formula: ##STR1## where R.sub.1, R.sub.2 and R.sub.3 are, independently, H, alkyl, halo, perhaloalkyl, hydroxy, alkoxy, aryl or arylalkyl; n is an integer from 0-5; R is azabicyclo 2.2.2!octyl or azabicyclo 2.2.1!heptyl when n.sub.1 is zero, or R is NR.sub.4 R.sub.5 when n.sub.1 is 1, 2, 3, 4, or 5, in which R.sub.4 and R.sub.5 are alkyl or R.sub.4 and R.sub.5, taken with the nitrogen atom to which they are attached, are N-(substituted aryl)piperazinyl in which said substituent is alkoxy, halo, or perhaloalkyl; N-(pyridyl)piperazinyl; N-(pyrimidinyl)piperazinyl; or 3-azabicyclo- 3.2.2!non-3-yl; X is oxygen or NH; n and n.sub.1 are, independently, one of the integers 0, 1, 2, 3, 4 or 5; or a pharmaceutically acceptable salt thereof are centrally active muscarinic agents.
    Type: Grant
    Filed: November 30, 1994
    Date of Patent: April 23, 1996
    Assignee: American Home Products Corporation
    Inventor: Annmarie L. Sabb
  • Patent number: 5508401
    Abstract: This invention involves novel neuroprotectant agents of the formula: ##STR1## in which R.sup.1 and R.sup.3 are, independently, hydrogen, cyano, nitro, halo or perhaloalkyl, with the proviso that one of R.sup.1 and R.sup.3 is other than hydrogen; R.sub.2 is alkyl; or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: February 20, 1991
    Date of Patent: April 16, 1996
    Assignee: American Home Products Corporation
    Inventors: Wayne E. Childers, Jr., Magid A. Abou-Gharbia, Edward J. Podlesny
  • Patent number: 5506252
    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 cyano substituent and one substituent selected from cyano, nitro, alkyl, perfluoroalkyl, alkoxy, perfluoroalkoxy, amino, alkylamino, dialkylamino, sulfamyl, alkylsulfonamido, arylsulfonamido, alkylcarboxamido, arylcarboxamido, alkylsulfonyl, perfluoroalkylsulfonyl, arylsulfonyl, chloro, bromo, fluoro, iodo, 1-imidazolyl or carboxyl; or a pharmaceutically acceptable salt thereof, are smooth muscle relaxants.
    Type: Grant
    Filed: October 2, 1994
    Date of Patent: April 9, 1996
    Assignee: American Home Products Corporation
    Inventors: John A. Butera, Schuyler A. Antane
  • Patent number: 5486518
    Abstract: This invention provides anxiolytic/antidepressant agents of the formula:A compound of the formula: ##STR1## in which R.sup.1 is alkyl, cycloalkyl, aryl or arylalkyl;R.sup.2 is hydrogen or alkyl;R.sup.3 is phenyl, benzyl, substituted phenyl, or substituted benzyl in which the substituents are hydroxy, halo, alkoxy, trifluoromethyl, nitro, cyano, alkoxycarbonyl, amino or dialkylamino;or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: April 10, 1995
    Date of Patent: January 23, 1996
    Assignee: American Home Products Corporation
    Inventors: John P. Yardley, Horace Fletcher, III, Michael G. Kelly, Alan C. White
  • Patent number: 5482935
    Abstract: A method for the treatment of atherosclerosis by administering to a patient in need of anti-atherosclerotic treatment, an effective amount of 17 alpha-dihydroequilin, a C.sub.2 -C.sub.6 alkanoyloxy ester thereof or a pharmaceutically acceptable salt of it's sulfate or phosphate ester, in the absence of naturally occurring estrogenic sreroids. A pharmaceutical composition containing 17 alpha-dihydroequilin, a C.sub.2 -C.sub.6 alkanoyloxy ester thereof or a pharmaceutically acceptable salt of it's sulfate or phosphate ester, in the absence of naturally occurring estrogenic sreroids, and a pharmaceutically acceptable carrier therefor.
    Type: Grant
    Filed: December 1, 1993
    Date of Patent: January 9, 1996
    Assignee: American Home Product Corporation
    Inventors: Steven J. Adelman, Kurt E. Steiner
  • Patent number: 5478939
    Abstract: Compounds of the Formulae I or II ##STR1## wherein Z and R.sub.1, are as described herein which compounds are muscarinic agonists useful in treating central cholinergic disfunction and pharmaceutical compositions containing the compounds.
    Type: Grant
    Filed: July 20, 1994
    Date of Patent: December 26, 1995
    Assignee: American Cyanamid Company
    Inventors: Eugene Trybulski, Jing Zhang
  • Patent number: 5468875
    Abstract: The compound 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 centrally active muscarinic agents.
    Type: Grant
    Filed: December 22, 1994
    Date of Patent: November 21, 1995
    Assignee: American Home Products Corporation
    Inventors: Annmarie L. Sabb, Reinhardt P. Stein
  • Patent number: 5466688
    Abstract: The compound of the formula: ##STR1## where R.sub.1 and R.sub.5 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.6 and R.sub.7 are independently H, C.sub.1 -C.sub.10 alkyl, C.sub.2 -C.sub.10 alkenyl, C.sub.3 -C.sub.
    Type: Grant
    Filed: October 20, 1994
    Date of Patent: November 14, 1995
    Assignee: American Home Products Corporation
    Inventors: Thomas J. Commons, Christa M. LaClair, Susan Christman
  • Patent number: 5466712
    Abstract: The compound of the formula (I) or a pharmaceutically acceptable salt thereof, are smooth muscle relaxants ##STR1##
    Type: Grant
    Filed: November 4, 1994
    Date of Patent: November 14, 1995
    Assignee: American Home Products Corporation
    Inventors: John A. Butera, Schuyler A. Antane, Bradford H. Hirth
  • Patent number: 5464867
    Abstract: The compound of the formula (I) or a pharmaceutically acceptable salt thereof, are smooth muscle relaxants.
    Type: Grant
    Filed: November 16, 1994
    Date of Patent: November 7, 1995
    Assignee: American Home Products Corporation
    Inventors: Madelene M. Antane, John A. Butera, Bradford H. Hirth, Schuyler A. Antane
  • Patent number: 5459131
    Abstract: Renin inhibiting compounds of the formula: ##STR1## wherein A is a moiety selected from those of the formula: ##STR2## where Z is O, S, SO, or SO.sub.2, P is 1 or 2 and X is --O-- or --S--; and analogs thereof which inhibit the substrate-cleaving acting of renin, pharmaceutical compositions containing these compounds, processes for producing the compounds and methods of treating hypertension which employ the novel renin inhibitors.
    Type: Grant
    Filed: March 15, 1991
    Date of Patent: October 17, 1995
    Assignee: American Cyanamid Company
    Inventors: Jay D. Albright, Charles F. Howell
  • Patent number: 5451685
    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: July 13, 1994
    Date of Patent: September 19, 1995
    Assignee: American Cyanamid Company
    Inventors: Eugene J. Trybulski, Richard H. Kramss, Herbert Brabander