Patents Represented by Attorney Richard K. Jackson

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  • Nitriles
    Patent number: 4760158
    Abstract: Novel 3-halo-2,2-disubstituted propanenitriles of formula ##STR1## wherein Z represents bromo or chloro and A, together with the carbon atom to which it is attached, represents a 5,6 or 7 membered saturated carbocyclic or heterocyclic ring, are useful as intermediates for preparing substituted pyrimido[1,2-a]indoles. The intermediates can be prepared by a novel process which comprises condensing a 2,2-disubstituted ethanenitrile with a dihalomethane in the presence of a non-nucleophilic strong base.
    Type: Grant
    Filed: March 9, 1987
    Date of Patent: July 26, 1988
    Assignee: John Wyeth & Brother Limited
    Inventors: Ian A. Cliffe, Richard S. Todd
  • Hypodermic syringe tray
    Patent number: 4753345
    Abstract: A hypodermic syringe tray adapted to hold at least one hypodermic syringe, comprising a barrel, plunger, cannula and cannula cover, in such manner as to secure said cannula cover and said plunger during thermal sterilization of the syringe and its contents.
    Type: Grant
    Filed: June 14, 1984
    Date of Patent: June 28, 1988
    Assignee: American Home Products Corporation
    Inventors: Stephen W. Goodsir, Dominic A. Ventura
  • Carboline histamine H.sub.1 antagonists
    Patent number: 4754038
    Abstract: Histaminic H.sub.1 -receptor antagonists of the formula: ##STR1## in which R.sup.1 is ##STR2## where R.sup.2 is hydrogen, alkyl of 1 to 3 carbon atoms, alkoxy of 1 to 3 carbon atoms, halo, nitro, cyano or trifluoromethyl; and R.sup.3 is hydrogen, alkyl of 1 to 3 carbon atoms, alkoxy of 1 to 3 carbon atoms, halo, nitro, cyano or trifluoromethyl;X is hydrogen, alkyl of 1 to 3 carbon atoms, alkoxy of 1 to 3 carbon atoms or halo;Z is ##STR3## where R.sup.4 is pyridinyl, quinolinyl or benzoyl, any of which may be substituted by alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 3 carbon atoms, halo or trifluoromethyl; and m is one of the integers 2, 3 or 4; andn is one of the integers 1, 2, 3 or 4;or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: February 26, 1987
    Date of Patent: June 28, 1988
    Assignee: American Home Products Corporation
    Inventor: Magid A. Abou-Gharbia
  • 2-[4-[4-(2-Pyrimidinyl)-1-piperazinyl]alkyl]alkyl]pyrido- and pyrazino-indole-1,3-dione derivatives as histamine H.sub.1 antagonists
    Patent number: 4748247
    Abstract: Histamine H.sub.1 receptor antagonists of the formula: ##STR1## in which R.sup.1 and R.sup.2 taken together represent an ortho-fused 1,2-indolo or 2,3-indolo moiety of the formulas: ##STR2## where R.sup.4 is hydrogen, alkyl of 1 to 6 carbon atoms, alkoxy of 1 to 6 carbon atoms or halo; andR.sup.5 is hydrogen, alkyl of 1 to 6 carbon atoms, benzyl, phenyl or substituted phenyl or benzyl where the substituent is taken from the group alkyl of 1 to 6 carbon atoms, alkoxy of 1 to 6 carbon atoms, halo or trifluoromethyl;R.sup.3 is ##STR3## where one X is --N.dbd. and the other is --CH.dbd.;Y is --N.dbd. or --CH.dbd.;and R.sup.6 and R.sup.7 are alkyl of 1 to 6 carbon atoms, alkoxy of 1 to 6 carbon atoms or halo;n is one of the integers 0 or 1;m is one of the integers 0, 1, 2 or 3; ando is one of the integers 1 or 2;or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: October 21, 1986
    Date of Patent: May 31, 1988
    Assignee: American Home Products Corporation
    Inventor: Magid A. Abou-Gharbia
  • Psychotropic bicyclic imides
    Patent number: 4748240
    Abstract: Substituted imides of the following formula are antipsychotic, anxiolytic agents with very little extrapyramidal side effects: ##STR1## in which X is --O--, --S--, --SO--, --SO.sub.2 --, --CR.sub.3 R.sub.4 --where R.sub.3 and R.sub.4, independently, are hydrogen, alkyl of 1 to 4 carbon atoms or, taken together with the carbon atom to which they are attached, R.sub.3 and R.sub.4 form a cycloalkyl group of 3 to 5 carbon atoms; Y is alkylene of 1 to 3 carbon atoms or alkenylene of 2 to 3 carbon atoms; n is one of the integers 0 to 1; m is one of the integers 2, 3, 4 or 5; R is phenyl, halophenyl, trifluoromethylphenyl, alkoxyphenyl in which the alkoxy substituent contains 1 to 3 carbon atoms, 2-pyrimidinyl, halopyrimidin-2-yl, 2-pyrazinyl, halopyrazin-2-yl, 2-pyridinyl, cyanopyridin-2-yl, halopyridin-2-yl, quinolyl, or haloquinolyl; or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: April 3, 1987
    Date of Patent: May 31, 1988
    Assignee: American Home Products Corporation
    Inventors: Gary P. Stack, Magid A. Abou-Gharbia, Edward J. Podlesny
  • 1-((A-substituted phenyl-.omega.-substituted piperazinyl)alkenyl) cyclohexanol
    Patent number: 4745191
    Abstract: The compounds ##STR1## in which R.sup.1 is 3-hydroxy, 4-hydroxy, 3-methoxy, 4-methoxy or 3,4-methylenedioxy; n is 1 or 2; and R.sup.2 is ##STR2## where R.sup.3 is hydrogen, alkoxy of 1 to 6 carbon atoms, halo or trifluoromethyl; or a pharmaceutically acceptable salt thereof possess anxiolytic and antidepressant activity and are useful in treating psychiatric disorders involving anxiety and/or depression.
    Type: Grant
    Filed: September 30, 1987
    Date of Patent: May 17, 1988
    Assignee: American Home Products Corporation
    Inventor: G. E. Morris Husbands
  • N-(pyridinylalkyl)-thieno-or benzo-isothiazol-3-amine derivatives
    Patent number: 4743692
    Abstract: A compound of the formula: ##STR1## in which A is a 3,4-; 3,2-; or 2,3-fused thieno- moiety or a benzo- moiety;X is alkylene of 2 to 5 carbon atoms;R.sup.1 is hydrogen, bromo or methyl;R.sup.2 is methoxy when R.sup.1 is hydrogen, methyl when R.sup.1 is bromo, and bromo when R.sup.1 is methyl;R.sup.3 is hydrogen or alkyl of 1 to 6 carbon atoms;R.sup.4 is hydrogen or alkyl of 1 to 6 carbon atoms;R.sup.3 and R.sup.4, taken together, are ethylene when X is ethylene;R.sup.5 is hydrogen when A is thieno, and when A is benzo, R.sup.5 is hydrogen, alkyl of 1 to 6 carbon atoms, halo or alkoxy of 1 to 6 carbon atoms;R.sup.6 is hydrogen when A is thieno, and when A is benzo, R.sup.
    Type: Grant
    Filed: September 30, 1986
    Date of Patent: May 10, 1988
    Assignee: American Home Products Corporation
    Inventors: Daniel M. Teller, Donald P. Strike, Arthur A. Santilli, Guy A. Schiehser
  • Pyschotropic polycyclic imides
    Patent number: 4732983
    Abstract: Substituted imides of the following formulae are antipsychotic, anxiolytic agents with very little extrapyramidal side effects: ##STR1## in which n is one of the integers 2, 3, 4 or 5; R is phenyl, halophenyl, trifluoromethylphenyl, alkoxyphenyl in which the alkoxy substituent contains 1 to 3 carbon atoms, 2-pyrimidinyl halopyrimidin-2-yl, 2-pyrazinyl, halopyrazin-2-yl, 2-pyridinyl, halopyridin-2-yl, cyanopyridin-2-yl, quinolyl, or haloquinolyl; and the dotted lines represent optional unsaturation; or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: April 3, 1987
    Date of Patent: March 22, 1988
    Assignee: American Home Products Corporation
    Inventors: Gary P. Stack, Guy A. Schiehser, Magid A. Abou-Gharbia
  • Hypoglycemic thiazolidinediones
    Patent number: 4728739
    Abstract: The compounds: ##STR1## in which R is hydrogen, lower alkyl, phenyl or benzyl, and R.sup.2 is hydrogen or lower alkyl, or a pharmaceutically acceptable salt thereof, are useful hypoglycemic and hypoinsulinemic agents for the treatment of diabetes mellitus and cardiovascular disease states involved in elevated insulin levels such as atherosclerosis.
    Type: Grant
    Filed: June 15, 1987
    Date of Patent: March 1, 1988
    Assignee: American Home Products Corporation
    Inventors: Kenneth L. Kees, Robert S. Cheeseman
  • Alkylsulfonamido or perfluoroalkylsulfonamido benzenesulfonamides
    Patent number: 4721809
    Abstract: This invention provides Class III anti-arrhythmic agents of the formula: ##STR1## in which R.sup.1 is alkylsulfonamido, arylsulfonamido, perfluoroalkylsulfonamido, R.sup.2 and R.sup.3 are hydrogen or alkyl, R.sup.4 is alkyl, and n is 2 to 4, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: September 18, 1986
    Date of Patent: January 26, 1988
    Assignee: American Home Products Corporation
    Inventors: George C. Buzby, Jr., Thomas J. Colatsky
  • N-(aminoalkylene)benzenesulfonamides
    Patent number: 4720580
    Abstract: This invention provides a group of anti-arrhythmic agents of the formula: ##STR1## in which R.sup.1 is hydrogen, hydroxy, alkoxy or halo;R.sup.2 is hydrogen, alkoxy, halo or trifluoromethyl, with the proviso that R.sup.2 is not hydrogen when R.sup.1 is hydrogen;R.sup.3 is alkyl or, when R.sup.2 is trifluoromethyl and R.sup.1 is hydrogen, R.sup.3 may be hydrogen;R.sup.4 is alkyl, cycloalkyl or cycloalkylmethyl;R.sup.5 is hydrogen or alkyl;n is 2-4;or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: April 11, 1986
    Date of Patent: January 19, 1988
    Assignee: American Home Products Corporation
    Inventor: George C. Buzby, Jr.
  • Histamine H.sub.1 antagonists
    Patent number: 4716165
    Abstract: Histamine H.sub.1 antagonists of the formula: ##STR1## in which R.sup.1 is hydrogen or alkyl of 1 to 6 carbon atoms; ##STR2## and the other is hydrogen or alkyl of 1 to 6 carbon atoms, where ##STR3## in which X is hydrogen, alkyl of 1 to 6 carbon atoms, alkoxy of 1 to 6 carbon atoms, halo, cyano or a nitro substituent on one of the available carbon atoms; andn is one of the integers 2, 3 or 4;or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: September 24, 1986
    Date of Patent: December 29, 1987
    Assignee: American Home Products Corporation
    Inventors: Magid A. Abou-Gharbia, Susan T. Nielsen
  • Histamine H1 antagonists
    Patent number: 4716166
    Abstract: Histamine H.sub.1 -receptor antagonists of the formula: ##STR1## where R.sup.1 is hydrogen or alkyl; one of R.sub.2 and R.sup.3 is alkyl and the other is ##STR2## where R.sup.4 is pyridin-2-yl, pyridin-4-yl, thienyl, or phenyl, any of which is optionally substituted by a halo, alkyl of 1 to 6 carbon atoms, nitro, trifluoromethyl, hydroxy or alkoxy of 1 to 6 carbon atoms substituent; and R.sup.5 is pyridin-2-yl, pyridin-4-yl or phenyl, any of which is optionally substituted by a halo, alkyl of 1 to 6 carbon atoms, alkoxy of 1 to 6 carbon atoms, nitro or trifluoromethyl substituent.
    Type: Grant
    Filed: October 21, 1986
    Date of Patent: December 29, 1987
    Assignee: American Home Products Corporation
    Inventors: Magid A. Abou-Gharbia, Susan T. Nielsen, Michael B. Webb
  • Histamine H.sub.1 antagonists
    Patent number: 4710572
    Abstract: N-Theophyllin-7-ylalkylene-N.sup.1 -(bis-p-fluorophenyl)methyl-piperazine derivatives as histamine H.sub.1 -antagonists.
    Type: Grant
    Filed: July 30, 1986
    Date of Patent: December 1, 1987
    Assignee: American Home Products Corporation
    Inventors: Magid A. Abou-Gharbia, Susan T. Nielsen
  • Beta-lactams substituted at C-4 with substituted aminooxymethyl
    Patent number: 4709025
    Abstract: This invention provides novel antibacterial beta-lactams of the formula: ##STR1## in which R is alkyl of 1 to 6 carbon atoms, carboxyalkyl of 2 to 6 carbon atoms or alkoxycarbonylalkyl wherein the alkyl and alkoxy moieties contain, independently, 1 to 6 carbon atoms;R.sup.1 is alkylideneamino of 2 to 6 carbon atoms, alkanoylamino of 2 to 6 carbon atoms, carboxyalkylideneamino of 2 to 6 carbon atoms, alkylsulfonylamino of 1 to 6 carbon atoms, alkoxycarbonylalkylsulfonylamino of 3 to 13 carbon atoms, or N,N-cyclodialkanoylamino of 4 to 6 carbon atoms;or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: January 20, 1987
    Date of Patent: November 24, 1987
    Assignee: American Home Products Corporation
    Inventors: Richard E. Mewshaw, Thomas J. Commons
  • 4-amino benzenesulfonamides
    Patent number: 4698445
    Abstract: N-Aminoalkyl(aminophenyl)sulfonic acid amides of the formula: ##STR1## in which R.sup.1 is --NH.sub.2, alkylamino of 1 to 3 carbon atoms or alkanoylamino of 2 to 4 carbon atoms, in 3- or 4-position of the benzene ring;R.sup.2 is hydrogen or alkyl of 1 to 4 carbon atoms;R.sup.3 is hydrogen or straight or branched chain alkyl of 1 to 4 carbon atoms;R.sup.4 is straight or branched chain alkyl of 1 to 4 carbon atoms; with the proviso that R.sup.3 and R.sup.4 are branched chain alkyl when R.sup.2 is hydrogen;and n is one of the integers 2, 3 or 4;or a pharmaceutically acceptable salt thereof, an anti-arrhythmic agents useful in the treatment of cardiac arrhythmias and conditions characterized by coronary arteries vasospasm.
    Type: Grant
    Filed: June 18, 1986
    Date of Patent: October 6, 1987
    Assignee: American Home Products Corporation
    Inventors: George C. Buzby, Jr., Thomas J. Colatsky
  • Antipsychotic gamma-carbolines
    Patent number: 4672117
    Abstract: The compounds: ##STR1## in which R.sup.1 is hydrogen, halogen, hydroxy, or alkyl;R.sup.2 is substituted or unsubstituted pyridinyl, pyrazinyl, quinolinyl or quinoxalinyl and said substituents are alkyl, alkoxy, alkoxycarbonyl, halogen, cyano or nitro;R.sup.5 and R.sup.6 are, independently, hydrogen, alkyl, phenyl, halophenyl, methylphenyl, trifluoromethylphenyl, cyanophenyl or nitrophenyl; with the proviso that one of R.sup.5 and R.sup.6 is other than hydrogen;and n is an integer from 1 to 7;or a pharmaceutically acceptable salt thereof, are antipsychotic and anxiolytic agents.
    Type: Grant
    Filed: September 16, 1985
    Date of Patent: June 9, 1987
    Assignee: American Home Products Corporation
    Inventors: Magid A. Abou-Gharbia, Usha R. Patel, Reinhardt P. Stein
  • N-substituted-4(3)-nitrobenzene sulphonamides
    Patent number: 4665227
    Abstract: Compounds presenting the following structural formula: ##STR1## in which the nitro substituent is in 3 or 4 position of the phenyl ring; R.sup.1 is hydrogen or alkyl;R.sup.2 is alkyl;R.sup.3 is hydrogen or alkyl;and n is one of the integers 0, 1 or 2;or a pharmaceutically acceptable salt thereof, are Class III anti-arrhythmic agents.
    Type: Grant
    Filed: May 23, 1986
    Date of Patent: May 12, 1987
    Assignee: American Home Products Corporation
    Inventors: Thomas J. Colatsky, George C. Buzby, Jr.
  • 2-(substituted piperazinylalkyl).beta.-carbolines useful in treatment of psychological disorders
    Patent number: 4663456
    Abstract: The .beta.-carbolines N-substituted in 2-position with a piperidinyl alkyl group are antipsychotic agents and anxiolytic agents with minimal extrapyramidal side effects, useful in the treatment of psychological disorders such as paranoia and schizophrania as well as general states of anxiety.
    Type: Grant
    Filed: September 16, 1985
    Date of Patent: May 5, 1987
    Assignee: American Home Products Corporation
    Inventor: Magid A. Abou-Gharbia
  • Hydroxy substituted 4,5-diphenyl-2-oxazole propanoic acid
    Patent number: 4659728
    Abstract: This invention discloses 5-(4-hydroxyphenyl)-4-phenyl-2-oxazolepropanoic acid, 4-(4-hydroxyphenyl-5-phenyl-2-oxazolepropanoic acid and pharmaceutically acceptable salts thereof as antiinflammatory agents, pharmaceutical compositions thereof and methods for their use.
    Type: Grant
    Filed: February 25, 1985
    Date of Patent: April 21, 1987
    Assignee: American Home Products Corporation
    Inventors: Alan J. Lewis, Richard P. Carlson, Horace Fletcher, 3rd