Patents Represented by Attorney Richard K. Jackson
  • Patent number: 4837329
    Abstract: A process for preparing dihydro compounds of formula I, by rearranging compounds of formula II, e.g. in the presence of acids or noble metal catalysts, is described. The compounds II may be prepared from intermediates of formula III. ##STR1## In these formulae 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 alkyl, cycloalkyl, aralkyl, or aryl radicals any of which radicals may be substituted, or R.sup.1 and R.sup.2 taken together or R.sup.2 and R.sup.3 taken together, form a 5, 6 or 7 membered ring which may be saturated or unsaturated and substituted or unsubstituted, R.sup.4 and R.sup.5 may also represent 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 R.sup.6 and R.sup.7 represent hydrogen, alkyl, cycloalkyl, or aralkyl radicals.Most of the compounds I, II and III are novel and are claimed. They are intermediates for anti-ulcer agents.
    Type: Grant
    Filed: January 18, 1984
    Date of Patent: June 6, 1989
    Assignee: American Home Products Corporation
    Inventors: Roger Crossley, Kenneth Heatherington
  • Patent number: 4832952
    Abstract: Pharmaceutical compositions produced with liquid, hydrophilic lubricants possessing markedly improved dissolution rates.
    Type: Grant
    Filed: July 21, 1986
    Date of Patent: May 23, 1989
    Assignee: American Home Products Corporation
    Inventors: Marvin Hersh, Charles W. Lentine
  • Patent number: 4826844
    Abstract: Compounds of the formula: ##STR1## in which m is one of the integers 1, 2 or 3; n is one of the integers 0, 1 or 2; o is one of the integers 0, 1 or 2; R.sub.1 and R.sub.2 are, independently, hydrogen, hydroxyl, alkyl, alkoxy, alkanoyloxy, trifluoromethyl, halo, or, when taken together, 3,4-methylenedioxy; R.sub.3 is alkyl, ##STR2## where R.sub.4 and R.sub.5 are, independently, hydrogen, hydroxyl, alkyl, alkoxy, alkanoyloxy, halo or trifluoromethyl; and R.sub.6 is hydrogen or halo; or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: September 30, 1987
    Date of Patent: May 2, 1989
    Assignee: American Home Products Corporation
    Inventors: G. E. M. Husbands, Gary P. Stack
  • Patent number: 4824999
    Abstract: The compound which is 2,3,3a,3b,4,5,6,6a,7,7a-decahydro-4,6,7-metheno-1H-cyclopenta[a]pentalene- 1,3-dicarboxylic acid is useful as an intermediate for production of the corresponding anhydride from which several of the disclosed antipsychotic/anxiolytic agents are prepared.
    Type: Grant
    Filed: September 23, 1988
    Date of Patent: April 25, 1989
    Assignee: American Home Products Corporation
    Inventor: Gary P. Stack
  • Patent number: 4812583
    Abstract: Compounds of the formula: ##STR1## where M is hydrogen or alkyl; R.sup.2 and R.sup.3 are, independently, alkyl; R.sup.4 is hydrogen, alkyl, phenyl or substituted phenyl, trifluoromethyl; and R.sup.5 is alkyl, phenyl or substituted phenyl, alkoxy, or trifluoromethyl; or a pharmaceutically acceptable salt thereof, are hypocholesteremic agents.
    Type: Grant
    Filed: September 11, 1987
    Date of Patent: March 14, 1989
    Assignee: American Home Products Corporation
    Inventors: Thomas J. Commons, Richard E. Mewshaw, Donald P. Strike
  • Patent number: 4803207
    Abstract: Pyrimidoindoles of formula (I) ##STR1## and their pharmaceutically acceptable acid addition salts, wherein R represents lower alkyl a mono- or bicyclic aryl radical or a group of mormula R.sup.3 O--B--[where R.sup.3 O is (lower)alkoxy,aryl(lower)alkoxy or hydroxy and B is a lower alkylene chain optionally containing one double or triple bond], R.sup.1 and R.sup.2 which may be the same or different each represent hydrogen, hydroxyl, lower alkyl, lower alkoxy, halo(lower)alkyl, halogen, amino or mono- or di(lower) alkylamino and A, together with the carbon atom to which it is attached, represents 5, 6 or 7 membered saturated carbocyclic or heterocyclic ring, are useful as hypoglyceamics.
    Type: Grant
    Filed: March 9, 1987
    Date of Patent: February 7, 1989
    Assignee: John Wyeth & Brother Ltd.
    Inventors: Alan C. White, Ian A. Cliffe, Richard S. Todd
  • Patent number: 4798896
    Abstract: This invention provides a group of antipsychotic/anxiolytic agents of the formula. ##STR1## in which R.sup.1 is hydrogen, halogen, hydroxy, alkoxy or alkyl;R.sup.2 is hydrogen, phenyl or phenyl substituted with an alkyl, alkoxy, halogen, trifluoromethyl, cyano or nitro group;R.sup.3 and R.sup.4 are hydrogen or, together, complete the benzo ring; andn is 1 to 7;or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: January 19, 1988
    Date of Patent: January 17, 1989
    Assignee: American Home Products Corporation
    Inventors: Magid A. Abou-Gharbia, John P. Yardley, Cesario O. Tio
  • Patent number: 4797489
    Abstract: The compounds ##STR1## wherein R.sup.1 is 1-adamantyl, 3-methyl-1-adamantyl, 9-fluorenyl or 1-fluorenyl;n is 0 or 1;m is 1, 2, 3, 4 or 5; andX is ##STR2## where R.sup.2 is phenyl, benzyl, pyridinyl, pyrimidinyl, pyrazinyl or substituted phenyl or benzyl in which the substituent is alkyl of 1 to 6 carbon atoms, alkoxy of 1 to 6 carbon atoms, halo, cyano, nitro or trifluoromethyl, ##STR3## where R.sup.3 is hydrogen, alkyl of 1 to 6 carbon atoms, alkoxy of 1 to 6 carbon atoms, halo, cyano or nitro;or pharmaceutically acceptable salts thereof are useful antidepressant and/or anxiolytic agents.
    Type: Grant
    Filed: December 2, 1987
    Date of Patent: January 10, 1989
    Assignee: American Home Products Corp.
    Inventors: Magid A. Abou-Gharbia, Gary P. Stack, John P. Yardley
  • Patent number: 4797488
    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 of 3 to 5 carbon atoms; 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, cyanopyridin-2-yl, halopyridin-2-yl, quinolyl, or haloquinolyl; R.sub.1 and R.sub.2, taken together, are alkylene of 3 to 5 carbon atoms or alkenylene of 3 to 5 carbon atoms, or taken with the carbon atoms to which they are attached, R.sub.1 and R.sub.2 complete a benzene ring, or a group of the formula: ##STR2## where Y is --CH.sub.2 --, --CH.sub.
    Type: Grant
    Filed: April 3, 1987
    Date of Patent: January 10, 1989
    Assignee: American Home Products Corporation
    Inventors: Gary P. Stack, Thomas D. Golobish, Magid A. Abou-Gharbia
  • Patent number: 4794196
    Abstract: N-Aminoalkyl(perfluoroalkanoylaminophenyl)sulfonic acid amides of the formula: ##STR1## in which R.sup.1 is perfluoroalkanoylamino 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; andn is one of the integers 2, 3 or 4;or a pharmaceutically acceptable salt thereof, are Class I anti-arrhythmic agents useful in the treatment of cardiac arrhythmias and conditions characterized by coronary arteries vasospasm and myocardial ischemia.
    Type: Grant
    Filed: February 10, 1987
    Date of Patent: December 27, 1988
    Assignee: American Home Products Corporation
    Inventors: George C. Buzby, Jr., Thomas J. Colatsky
  • Patent number: 4792614
    Abstract: Compounds of the formula: ##STR1## in which ##STR2## where M is hydrogen or alkyl; one of R.sup.2 and R.sup.3 is phenyl or substituted phenyl where the substituent is alkyl, alkoxy, halogen, trifluoromethyl, nitro, amino, cyano or carboxyl; and the other of R.sup.2 and R.sup.3 is hydrogen, alkyl, or a halogen; or a pharmaceutically acceptable salt thereof, are HMG--CoA reductase inhibitors useful in the treatment of atherosclerosis, hypercholesterolaemia, hyperlipaemia and similar disease states characterized by elevated cholesterol levels in the blood.
    Type: Grant
    Filed: August 5, 1987
    Date of Patent: December 20, 1988
    Assignee: American Home Products Corporation
    Inventors: William F. Fobare, Donald P. Strike
  • Patent number: 4789660
    Abstract: A therapeutic composition for trans-mucosal administration in the treatment of diabetes including insulin, as an adjuvant a water-soluble fusidic acid salt and as a co-adjuvant methylparaben and/or propylparaben.
    Type: Grant
    Filed: September 10, 1987
    Date of Patent: December 6, 1988
    Assignee: American Home Products Corporation
    Inventors: Robin P. Enever, Thomas W. Leonard, Karol K. Mikula
  • Patent number: 4788290
    Abstract: The compounds ##STR1## in which X and Y are, independently, --O-- or --S--;R.sup.1 and R.sup.2 are, independently, halo, trifluoromethyl, cyano, hydroxy, amino, alkylamino, dialkylamino, alkoxy, alkyl or alkanoylamino; andn is 1 to 4;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: December 11, 1987
    Date of Patent: November 29, 1988
    Assignee: American Home Products Corporation
    Inventor: Gary P. Stack
  • Patent number: 4784996
    Abstract: Compounds of formula ##STR1## wherein A represents a lower alkylene chain optionally containing one double or triple bond, RO represents (lower)alkoxy, aryl(lower)alkoxy, hydroxy or protected hydroxy, R.sup.1 and R.sup.2 which may be the same or different each represent hydrogen, hydroxyl, lower alkyl, lower alkoxy, halo(lower)alkyl, halogen, amino or mono- or di(lower)alkylamino and R.sup.3 and R.sup.4 each independently represent hydrogen or lower alkyl and their pharmaceutically acceptable acid addition salts are useful as hypoglycaemics or as intermediates for hypoglycaemics.
    Type: Grant
    Filed: March 9, 1987
    Date of Patent: November 15, 1988
    Assignee: John Wyeth & Brother Ltd.
    Inventors: Alan C. White, Ian A. Cliffe, Richard S. Todd
  • Patent number: 4777254
    Abstract: Polycyclic 1,3-dione imides N-alkylated with variously N-substituted alkyl- or cycloalkyl amines afford histamine H.sub.1 -receptor antagonists of the formula ##STR1## wherein R is polycyclic alkyl moiety;R.sup.1 is hydrogen or alkyl;R.sup.4 is an aromatic amine or a cycloalkyl amine containing N-substitution;R.sup.7 and R.sup.8 are hydrogen, alkyl or form a spiro cycloalkyl group.
    Type: Grant
    Filed: December 2, 1986
    Date of Patent: October 11, 1988
    Assignee: American Home Products Corp.
    Inventors: Magid A. Abou-Gharbia, Susan T. Nielsen
  • Patent number: 4777048
    Abstract: Pharmaceutical compositions produced with liquid, hydrophilic lubricants possessing markedly improved dissolution rates.
    Type: Grant
    Filed: July 18, 1986
    Date of Patent: October 11, 1988
    Assignee: American Home Products Corporation
    Inventors: Marvin Hersh, Charles W. Lentine
  • Patent number: 4766124
    Abstract: The method of using compounds of the formula: ##STR1## in which R.sup.1 is hydrogen or 4-halophenyl; R.sup.2 is 4-halophenyl when R.sup.1 is 4-halophenyl and 3-trifluoromethylphenyl and R.sup.1 is hydrogen; and n is one of the integers 2, 3 or 4; or a pharmaceutically acceptable salt thereof as histamine H.sub.1 -receptor antagonists and the novel compound 2,3,4,9-tetrahydro-2-[3-[4-[3-(trifluoromethyl)benzyl]-1-piperazinyl]propy l]-1H-pyridol[3,4-b]indole represent the inventive aspects of this disclosure.
    Type: Grant
    Filed: February 26, 1987
    Date of Patent: August 23, 1988
    Assignee: American Home Products Corporation
    Inventor: Magid A. Abou-Gharbia
  • Patent number: 4766215
    Abstract: The compounds of the following formula are histamine H.sub.1 -receptor antagonists: ##STR1## where R.sup.3 and R.sup.4 are, independently, hydrogen, halo, alkoxy of 1 to 3 carbon atoms or alkyl of 1 to 3 carbon atoms; R.sup.2 is hydrogen or halo;n is one of the integers 0, 1 or 2;p is one of the integers 0 or 1;Y is --N.dbd. or --CH.dbd., with the proviso that when Y is --N.dbd., p is zero, and when Y is --CH.dbd., p is one; andone of X.sub.1 and X.sub.2 is nitrogen and the other is --CH.dbd.; or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: February 27, 1987
    Date of Patent: August 23, 1988
    Assignee: American Home Products Corporation
    Inventors: Magid A. Abou-Gharbia, Usha R. Patel
  • Patent number: 4764623
    Abstract: Compounds of the formula: ##STR1## where R is hydrogen or A--(CF.sub.2).sub.m --CH.sub.2 --; A is --F or --H; n is an integer from 1 to 10, inclusive; m is an integer from 0 to 9, inclusive; p is an integer from 0 to 4, inclusive; and Y is hydrogen, halo, trifluoromethyl, alkyl of 1 to 6 carbon atoms, alkoxy of 1 to 6 carbon atoms, or hydroxy; or a pharmaceutically acceptable salt thereof. The compounds are useful as anti-hyperglycemic and anti-hyperinsulinemic agents.
    Type: Grant
    Filed: June 15, 1987
    Date of Patent: August 16, 1988
    Assignee: American Home Products Corporation
    Inventor: Kenneth L. Kees
  • Patent number: 4761501
    Abstract: This application discloses certain substituted phenylacetamides of the formula: ##STR1## in which the dotted line represents optional unsaturation, R.sub.1 is alkyl;R.sub.2 is alkyl;R.sub.4 is hydrogen or alkyl; R.sub.5 and R.sub.6, one of which may be hydrogen, are independently, hydroxyl, alkyl, alkoxy, aralkoxy, alkanoyloxy, alkylmercapto, N-protected amino, halo or trifluoromethyl;R.sub.7 is hydrogen or alkyl; andn is one of the integers 0, 1, 2, 3 or 4;which are useful in the production of antidepressant agents.
    Type: Grant
    Filed: May 22, 1985
    Date of Patent: August 2, 1988
    Assignee: American Home Products Corporation
    Inventors: G. E. Morris Husbands, John P. Yardley, Eric A. Muth