Patents Represented by Attorney Robert F. Boswell, Jr.
  • Patent number: 5162322
    Abstract: This invention discloses the antianxiety properties of compounds of the formula: ##STR1## wherein n is 3 or 4, R is C.sub.1 -C.sub.4 alkyl or phenyl, and Ar is ##STR2## where Z is selected from H, C.sub.1 -C.sub.4 alkoxy, C.sub.2 -C.sub.4 alkenyloxy or hydroxy.
    Type: Grant
    Filed: March 6, 1991
    Date of Patent: November 10, 1992
    Assignee: A. H. Robbins Company, Incorporated
    Inventors: Chandler R. Taylor, Jr., L. Meredith Moses, Brian F. Kilpatrick
  • Patent number: 5151418
    Abstract: A method of treating animals to obtain muscle relaxation and/or to relieve anxiety is disclosed utilizing novel and known 3-aryloxy and 3-arylthioazetidinecarboxamides having the formula: ##STR1## wherein Z is oxygen or sulfur; B is oxygen or sulfur; Ar is pyridyl or halo substituted pyridyl, phenyl or substituted phenyl; R.sup.1 and R.sup.2 are hydrogen, loweralkyl, aryl, allyl groups, propargyl, cycloalkyl, loweralkylcycloalkyl, cycloalkylloweralkyl, arylloweralkyl and diloweralkylaminoalkyl, and R.sup.1 and R.sup.2 when taken together with the adjacent nitrogen atom may form a heterocyclic amine radical; R.sup.3 is hydrogen, loweralkyl, aryl or arylloweralkyl, and the geometrical isomers thereof and pharmaceutical salts thereof and hydrates thereof when they are possible.
    Type: Grant
    Filed: August 9, 1991
    Date of Patent: September 29, 1992
    Assignee: A. H. Robins Company, Incorporated
    Inventors: Chandler R. Taylor, Jr., Albert D. Cale, Jr., David N. Johnson, Harold F. Stauffer, Jr.
  • Patent number: 5151413
    Abstract: Derivatives of Rapamycin where the hydroxy group at position 31 and/or 42 are reacted with acetal forming reagents have been shown to have immunosuppressant and antifungal properties. These derivatives are represented by the formula: ##STR1## wherein R.sup.1 and R.sup.2 independently are hydrogen, --CH.sub.2 YX, --C(CH.sub.3).sub.2 YX, --CH.sub.2 (CH.sub.3)YX, or L;Y is O or S; X is --CH.sub.3, --(CH.sub.2).sub.n CH.sub.3, --CH.sub.2 C.sub.6 H.sub.6, --(CH.sub.2).sub.2 OCH.sub.3, --CH.sub.2 Cl.sub.3 or --CH.sub.2 CH.sub.2 Si(CH.sub.3).sub.3 and L is selected from tetrahydrofuran-2-yl, tetrahydrothiophen-2-yl, tetrahydrothiopyran-2-yl, tetrahydropyran-2-yl, 4-methoxytetrahydropyran-2-yl, 4-methoxytetrahydrothiopyran-2-yl, or 4-methoxytetrahydrothiopyran-S, S-dioxide-2-yl with a proviso that R.sup.1 and R.sup.2 cannot simultaneously be hydrogen and n is 1-5.
    Type: Grant
    Filed: November 6, 1991
    Date of Patent: September 29, 1992
    Assignee: American Home Products Corporation
    Inventors: Craig E. Caufield, Guy A. Schiehser
  • Patent number: 5140026
    Abstract: Compounds of this invention are represented by the formula: ##STR1## wherein Z is a C.sub.1 -C.sub.6 alkylene group and R is an alkyl or substituted alkyl group. Class III antiarrhythmic activity is determined in vitro using an electrophysiological test where prolongation of the action potential duration is an indication of activity.
    Type: Grant
    Filed: May 9, 1991
    Date of Patent: August 18, 1992
    Assignee: A. H. Robins Company, Incorporated
    Inventors: Mark R. Hellberg, James R. Shanklin, Jr.
  • Patent number: 5138051
    Abstract: Reduction of C-33 ketone of rapamycin gives the C-33 hydroxy analog of Formula I. ##STR1## The reduction product prevents cleavage of the C-31/C-32 bond due to base degradation. The Formula I compounds exhibit immunosuppressant, antifungal, and antiinflammatory activities.
    Type: Grant
    Filed: August 7, 1991
    Date of Patent: August 11, 1992
    Assignee: American Home Products Corporation
    Inventors: Philip F. Hughes, John H. Musser
  • Patent number: 5130309
    Abstract: Methods of treating cardiac arrhythmias and convulsions in warm-blooded animas and pharmaceutical compositions therefor are disclosed. The compounds useful in the methods of treatment and compositions are represented by the formula ##STR1## where n is 0 to 3 and R is H, C.sub.1 -C.sub.4 alkyl or arylalkyl and Ar is phenyl or substituted phenyl.
    Type: Grant
    Filed: April 12, 1991
    Date of Patent: July 14, 1992
    Assignee: A. H. Robins Company, Incorporated
    Inventors: James R. Shanklin, Jr., Mark R. Hellberg
  • Patent number: 5106857
    Abstract: A method of treating cardiac arrhythmias and muscle tension and spasticity with N-(1-methyl-3-pyrrolidinyl)-1-(phenylmethyl)-1H-benzimidazol-2-amine and analogs and the pharmaceutical compositions are herein disclosed. Illustratively, the compound having the structure: ##STR1## corrects an induced arrhythmia in 7 out of 8 dogs at 7 mg/kg IV and has an ED.sub.50 of 21 mg/kg in the mouse Straub-tail test.
    Type: Grant
    Filed: May 9, 1991
    Date of Patent: April 21, 1992
    Assignee: A. H. Robins Company, Incorporated
    Inventors: Albert D. Cale, Jr., Thomas W. Gero
  • Patent number: 5102876
    Abstract: Reduction of rapamycin with DIBAL furnishes either the 15-hydroxyrapamycin or 15,27-bis(hydroxy)rapamycin, depending upon the reaction conditions, having the general structure ##STR1## where Y is --CO-- --CH(OH)--. The compounds of this invention are useful in treating transplant rejection, host vs. graft disease, autoimmune diseases, diseases of inflammation, and fungal infections.
    Type: Grant
    Filed: May 7, 1991
    Date of Patent: April 7, 1992
    Assignee: American Home Products Corporation
    Inventor: Craig E. Caufield