Patents Represented by Attorney Richard K. Jackson
  • Patent number: 4985560
    Abstract: The compound of the formula: ##STR1## in which R.sup.1 is hydrogen, alkoxy, cyano, halo, nitro, amino, or mono- or dialkylamino; R.sup.2 is hydrogen, alkyl, phenyl, benzyl, 2-thienyl, 3-thienyl or 2-,3- or 4-pyridinyl; R.sup.3 is hydrogen, alkyl or phenyl; R.sup.4 is N-methyl-pyrrolidin-2yl, 2-, 3- or 4-pyridinyl, 3-quinuclidinyl or ##STR2## where n is 1 to 5; m is 0 to 3; and R.sup.8 is hydrogen or alkyl of 1 to 6 carbon atoms; or R.sup.4 is ##STR3## wherein: (a) n is 2, R.sup.5 taken with R.sup.3 is ethylene and R.sup.6 is --CHO, alkyl, unsubstituted or substituted phenyl, pyrimidinyl, pyridinyl, or pyrazinyl, where the substituents are alkyl, alkoxyl, halo, cyano, nitro or trifluoromethyl; (b) n is 1 to 5, and R.sup.5 and R.sup.6 taken together are polymethylene which may be alkyl substituted or R.sup.5 nd R.sup.6 are morpholino, 3-azabicyclo[3.2.
    Type: Grant
    Filed: January 12, 1990
    Date of Patent: January 15, 1991
    Assignee: American Home Products Corporation
    Inventors: Annmarie L. Sabb, Magid A. Abou-Gharbia, Gervais Dionne
  • Patent number: 4966905
    Abstract: A compound of the formula: ##STR1## in which R is alkyl, phenyl or halophenyl; R.sup.2 is substituted phenyl having from 1 to 3 substituents selected from halo, alkyl, alkylthio, alkylsulfonyl, cyano, trifluoromethyl, or R.sup.2 is pyridinyl, pyrazinyl, quinolinyl, N-alkylpyrrolyl, thienyl, benzothienyl, or furyl; and n is 1 or 2, are cytoprotective anti-ulcer agents.
    Type: Grant
    Filed: December 12, 1989
    Date of Patent: October 30, 1990
    Assignee: American Home Products Corporation
    Inventors: Steven W. Felman, Ivo L. Jirkovsky, Kevin A. Memoli
  • Patent number: 4959051
    Abstract: A dual chambered container for delivery of a liquid medicament comprising a teat sealed to a hollow, bottom compartment by a retaining ring, the teat forming one chamber for diluent or medicament and the bottom forming the other chamber for medicament or diluent, respectively, said chambers being separated by a stopper adapted to seal either the bottom chamber or the teat chamber.
    Type: Grant
    Filed: October 13, 1989
    Date of Patent: September 25, 1990
    Assignee: American Home Products Corporation
    Inventors: Richard A. Glass, Robert F. Ryer, II, Deborah T. Tomcanin
  • Patent number: 4957909
    Abstract: The use of the compounds: ##STR1## where R is hydrogen, alkyl, alkoxy, hydroxy, alkanoyloxy, phenylalkoxy, halo or trifluoromethyl; R.sup.1 is alkyl, alkenyl or phenylalkyl; R.sup.2 is hydrogen, alkyl, phenylalkyl, alkenyl, alkynyl, thienylalkyl or furylalkyl; n is one of the integers 2, 3, 4, 5 or 6; or a pharmaceutically acceptable salt thereof, as NMDA antagonists in the treatment of convulsions and neurodegenerative disease states. The compounds in which R.sup.2 are heterocyclylalkylamines are novel and useful NMDA antagonists.
    Type: Grant
    Filed: January 2, 1990
    Date of Patent: September 18, 1990
    Assignee: American Home Products Corporation
    Inventors: Magid A. Abou-Gharbia, Ronald R. Notvest
  • Patent number: 4957913
    Abstract: Hypertension in the mammal is controlable by administration of a compound of the formula: ##STR1## wherein R is ##STR2## in which X is methylene, ethylene or ethylidene and Q is alkylene, alkylidene, or Q is a ##STR3## in which the dotted line represents optional unsaturation; n is one of the integers 2,3 or 4;Ar is phenyl or phenyl substituted with halo. trifluoromethyl or alkoxy, or Ar is 2-pyrimidinyl or halopyrimidin-2-yl, 2-pyrazinyl or halo-pyrazin-2-yl, 2-pyridinyl, cyanopyridin-2-yl or halopyridin-2-yl;or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: November 22, 1989
    Date of Patent: September 18, 1990
    Assignee: American Home Products Corp.
    Inventors: Magid A. Abou-Gharbia, Gary P. Stack, Rodney W. Lappe
  • Patent number: 4940789
    Abstract: This invention involves novel neuroprotectant agents of the formula: ##STR1## in which R.sup.1 and R.sup.3 are, independently, hydrogen, alkyl, alkoxy, hydroxy, cyano, nitro, halo, trifluoromethyl, amino, alkylamino or dialkylamino; R.sup.2 is alkyl; R.sup.4 is alkyl, phenyl or benzyl; n is 0 or 1; m is one of the integers 0,1,2,3,4,5 or 6; and X is alkyl, alkylamino, dialkylamino, alkanoyl or substituted or unsubstituted phenyl, pyridinyl, pyrimidinyl, pyrazinyl, quinolyl, morpholinyl, furyl thienyl, pyrrolyl, tetrahydrofuryl, tetrahydrothienyl, pyrrolidinyl, piperidinyl, piperazinyl or perhydropyridminyl, in which the subsitutent is alkyl, alkoxy, halo, trifluoromethyl, cyano, nitro or hydroxy; or a pharmaceutically acceptable salt thereof; and their use in control of degenerative CNS disease states.
    Type: Grant
    Filed: October 10, 1989
    Date of Patent: July 10, 1990
    Assignee: American Home Products Corporation
    Inventors: Wayne E. Childers, Jr., Magid A. Abou-Gharbia
  • Patent number: 4923991
    Abstract: The invention provides a compound of formula III ##STR1## or an acid addition salt thereof, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and R.sup.7 are the same or different and represent hydrogen or lower alkyl, cycloalkyl, lower aralkyl or phenyl radicals any of which radicals may be substituted by lower alkyl, lower alkoxy or trifluoromethyl or R.sup.2 and R.sup.3 taken together, form a 5, 6 or 7 membered saturated ring, R.sup.4 and R.sup.5 may also represent lower alkoxy or cycloalkoxy, n is 1, 2 or 3 and, if more than one R.sup.4 radical is present the R.sup.4 radicals may be the same or different and esters of carboxylic acids with the hydroxy group shown, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and n are as defined above, with the provisos that (1) R.sup.6 and R.sup.7 are other than hydrogen when R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are all hydrogen and (2) R.sup.6 and R.sup.7 are not both methyl when R.sup.4 is methyl.
    Type: Grant
    Filed: December 16, 1988
    Date of Patent: May 8, 1990
    Assignee: John Weyth & Brother Limited
    Inventors: Roger Crossley, Kenneth Heatherington
  • Patent number: 4924008
    Abstract: The use of the compounds: ##STR1## where R is hydrogen, alkyl, alkoxy, hydroxy, alkanoyloxy, phenylalkoxy, halo or trifluoromethyl; R.sup.1 is alkyl, alkenyl or phenylalkyl; R.sup.2 is hydrogen, alkyl, phenylalkyl, alkenyl, alkynyl, thienylalkyl or furylalkyl; n is one of the integers 2, 3, 4, 5 or 6; or a pharmaceutically acceptable salt thereof, as NMDA antagonists in the treatment of convulsions and neurodegenerative disease states. The compounds in which R.sup.2 are heterocyclylalkylamines are novel and useful NMDA antagonists.
    Type: Grant
    Filed: May 4, 1989
    Date of Patent: May 8, 1990
    Assignee: American Home Products Corporation
    Inventors: Magid A. Abou-Gharbia, Ronald R. Notvest
  • Patent number: 4920121
    Abstract: N-(2-Methoxyphenyl)piperazine as a useful anxiolytic agent.
    Type: Grant
    Filed: September 22, 1989
    Date of Patent: April 24, 1990
    Assignee: American Home Products Corporation
    Inventor: John A. Moyer
  • Patent number: 4916071
    Abstract: Hybrid, third generation, plasminogen activators containing plural, heterologous polypeptide kringles prepared by recombinant DNA techniques as well as the genes coding for the activators, Vectors containing those genes and a method for using the plasminogen activators as thrombolytic agents, are disclosed.
    Type: Grant
    Filed: July 11, 1986
    Date of Patent: April 10, 1990
    Assignee: American Home Products Corporation
    Inventors: Paul P. Hung, Narender K. Kalyan, Shaw-guang L. Lee
  • Patent number: 4910302
    Abstract: Compounds of the formula: ##STR1## in which Z is ##STR2## wherein X is alkylene, ethanylene or alkylidene; Q is alkylene, alkylidene, ##STR3## or Q, taken together with the carbon atoms to which it is attached forms a benzene ring or a substituted benzene ring, in which said substituents are --OH, --OCH.sub.3, alkyl, halo, --CF.sub.3, --NH.sub.2, monoalkylamino, dialkylamino or alkanoylamino; R.sup.1 is hydrogen or alkyl; R.sup.2 and R.sup.3 are, independently, hydrogen or alkyl or taken together with the carbon atoms to which they are attached, they form a cycloalkane or cycloalkene ring; m is one of the integers 2-5; R.sup.4 is hydrogen, hydroxy, cyano, alkyl, alkoxy, halo, amino, alkylamino, phenylamino, tolylamino, xylylamino, mesitylamino, methoxyphenylamino, or halophenylamino; and the dotted lines represent optional unsaturation; or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: December 19, 1988
    Date of Patent: March 20, 1990
    Assignee: American Home Products Corporation
    Inventors: Magid A. Abou-Gharbia, Gary P. Stack
  • Patent number: 4910019
    Abstract: The compounds: ##STR1## in which the dotted line represents optional unsaturation; R.sup.1 is hydrogen, halo or alkoxy; R.sup.2 is hydrogen or alkoxy and X is methylene, ethylene, ethylidene, 1,2-propylene or propylene; or a biologically acceptable salt thereof are growth promoting agents which rapidly lead to increased lean body mass in domestic animals and humans.
    Type: Grant
    Filed: June 7, 1989
    Date of Patent: March 20, 1990
    Assignee: American Home Products Corporation
    Inventor: Michael L. McCaleb
  • Patent number: 4900835
    Abstract: p is one of the integers 2, 3, 4 or 5;q is one of the integers 1, 2 or 3;and ##STR2## where R.sup.4 is hydrogen, alkyl, alkoxy or halo; or a pharmaceutically acceptable salt thereof are antipsychotic and anxiolytic agents.
    Type: Grant
    Filed: April 7, 1989
    Date of Patent: February 13, 1990
    Assignee: American Home Products Corporation
    Inventor: Magid A. Abou-Gharbia
  • Patent number: 4883875
    Abstract: The compounds: ##STR1## in which R.sup.1 and R.sup.2 are hydrogen or alkyl and R.sup.6 and R.sup.7, taken together, are tetramethylene, pentamethylene or hexamethylene;p is one of the integers 2, 3, 4 or 5;and ##STR2## where R.sup.4 is hydrogen, alkyl, alkoxy or halo;or a pharmaceutically acceptable salt thereof are antipsychotic and anxiolytic agents.
    Type: Grant
    Filed: April 7, 1989
    Date of Patent: November 28, 1989
    Assignee: American Home Products Corporation
    Inventor: Magid A. Abou-Gharbia
  • Patent number: 4882432
    Abstract: The compounds of the formula: ##STR1## wherein Ad is 1-adamantyl, 2-adamantyl or 3-noradamantyl; X is --O-- or ##STR2## n is 1,2,3 or 4; R.sup.1 and R.sup.2 are, independently, hydrogen, alkyl, phenyl, benzyl, or substituted phenyl or benzyl in which the substituent is alkyl, alkoxy, halo, cyano, nitro or trifluoromethyl; and R.sup.3 is phenyl, benzyl or substituted phenyl or benzyl in which the substituent is alkyl, alkoxy, halo, nitro, cyano or perhalomethyl, 2-, 3-, or 4-pyridinyl, 2-, 4-or 5-pyrimidiny; or 2- or 3-pyrazinyl; R.sup.4 and R.sup.5 are independently, hydrogen, methyl, phenyl or benzyl; or a pharmaceutically acceptable salt thereof, are useful anxiolytic/antidepressant agents, with elements of antipsychotic activity.
    Type: Grant
    Filed: January 9, 1989
    Date of Patent: November 21, 1989
    Assignee: American Home Products Corporation
    Inventors: Magid A. Abou-Gharbia, John P. Yardley, Wayne E. Childers, Jr.
  • Patent number: 4873331
    Abstract: The compounds of the following structural formula posses useful anxiolytic, antidepressant, antipsychotic and learning and memory enhancement properties: ##STR1## in which R.sup.1 is 3-noradamantyl;n is 0 or 1;X is --CO.sub.2 --, --O.sub.2 C-- or --OCO.sub.2 --;m is 1, 2, 3, 4, or 5;andR.sup.2 is phenyl, benzyl, pyridinyl, pyrimidinyl, pyrazinyl or substituted phenyl or benzyl in which the substituent is alkyl, alkoxy, halo, cyano, nitro or trifluoromethyl;or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: December 9, 1988
    Date of Patent: October 10, 1989
    Assignee: American Home Products Corporation
    Inventors: Wayne E. Childers, Jr., Magid A. Abou-Gharbia
  • Patent number: 4851533
    Abstract: The compounds: ##STR1## in which n is one of the integers 0 or 1; andwhen n is 1, R.sup.1 and R.sup.2 are hydrogen or alkyl of 1 to 3 carbon atoms, and R.sup.6 and R.sup.7, taken together, are tetramethylene, pentamethylene or hexamethylene; andwhen n is 0, R.sup.1 and R.sup.2, taken together, are ##STR2## where the dotted line represents optional unsaturation; p is one of the integers 2, 3, 4 or 5;q is one of the integers 1, 2 or 3; andR.sup.3 is ##STR3## where R.sup.4 is hydrogen, alkyl of 1 to 6 carbon atoms; alkoxy of 1 to 6 carbon atoms or halo; and R.sup.5 is hydrogen or halo;or a pharmaceutically acceptable salt thereof are antipsychotic and anxiolytic agents.
    Type: Grant
    Filed: March 5, 1987
    Date of Patent: July 25, 1989
    Assignee: American Home Products Corporation
    Inventor: Magid A. Abou-Gharbia
  • Patent number: 4845221
    Abstract: The compounds ##STR1## in which R.sub.1 is hydroxy, alkoxy of 1 to 6 carbon atoms, amino, alkylamino of 1 to 6 carbon atoms, dialkylamino where each alkyl substituent contains 1 to 6 carbon atoms, or alkanoylamino of 2 to 6 carbon atoms;R.sub.2 is 3-trifluoromethylphenyl, 3-halophenyl, 2-pyrimidinyl, halopyrimidin-2-yl, 2-pyrazinyl or halopyrazin-2-yl; andn is one of the integers 1 or 2;or a pharmaceutically acceptable salt thereof, are selective serotonergic agents useful in the treatment of depression and/or anxiety, as well as related sexual dysfunctions and appetite disorders.
    Type: Grant
    Filed: April 15, 1988
    Date of Patent: July 4, 1989
    Assignee: American Home Products Corporation
    Inventors: Gary P. Stack, Edward J. Podlesny
  • Patent number: 4845231
    Abstract: Compounds of the formula: ##STR1## in which R is a substituted or unsubstituted monocyclic or bicyclic alkyl group containing from 3 to 8 ring carbon atoms, wherein any substituent is alkyl of 1 to 3 carbon atoms, oxo, hydroxy, carboxy or when the hydroxy and carboxy substituents taken together they form a 1,3-carbonyloxy lactone ring closed structure;n is one of the integers 0, 1, 2 or 3;X is --O--, ##STR2## or --SO.sub.2 NH--; and Z is .dbd.CH-- or --N.dbd.;or a pharmaceutically acceptable salt thereof, are anti-hyperglycemic agents.
    Type: Grant
    Filed: February 12, 1988
    Date of Patent: July 4, 1989
    Assignee: American Home Products Corporation
    Inventor: Kenneth L. Kees
  • Patent number: 4837325
    Abstract: The compounds ##STR1## in which R is halo or trifluoromethyl;n is one of the integers 2, 3 or 4;or a pharmaceutically acceptable salt thereof are useful as histamine H.sub.1 -receptor antagonists.
    Type: Grant
    Filed: April 8, 1988
    Date of Patent: June 6, 1989
    Assignee: American Home Products Corporation
    Inventor: Magid A. Abou-Gharbia