Patents Represented by Attorney Richard K. Jackson

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  • N,N', N'-trisubstituted-5-bisaminomethylene-1,3-dioxane-4,6-dione inhibitors of acyl-coa:cholesterol-acyl transferase
    Patent number: 5179216
    Abstract: The compounds of the formula: ##STR1## in which X, Y and Z are, independently, hydrogen, halogen, hydroxy, nitro, cyano, carboxyl, trifluoromethyl, phenyl, amino, alkylamino, dialkylamino, alkyl, alkoxy or phenylalkyloxy; R.sub.1 is alkyl, hydroxyalkyl, alkenyl, cycloalkyl, phenylcycloalkyl, 1-hydroxymethylphenethyl, 1-(t-butyl)dimethylsilyloxymethyl-phenethyl, 1-(t-butyl)dimethylsilyloxymethylisopentyl, 1-hydroxymethylisopentyl, phenyl, benzyl or substituted phenyl or benzyl, where the substituents are alkyl, alkoxy, halogen, cyano, trifluoromethyl, amino, alkylamino, dialkylamino, nitro or phenyl, benzyl, phenethyl or R.sub.1 is thienyl, imidazolyl, thiazolyl, pyridinyl, pyrimidinyl, pyrazinyl, benzamidazolyl, phenylalkylpiperidinyl or morpholino; R.sub.
    Type: Grant
    Filed: June 24, 1991
    Date of Patent: January 12, 1993
    Assignee: American Home Products Corporation
    Inventors: William F. Fobare, Donald P. Strike
  • N-phenyl-N'-thienylmethyl-bis-diamino-5-methylene-1,3-dioxane-4,6-dione compounds
    Patent number: 5177219
    Abstract: The compounds of the formula: ##STR1## wherein X, Y and Z are, independently, hydrogen, halogen, hydroxy, nitro, cyano, carboxyl, trifluoromethyl, phenyl, amino, mono and dialkylamino, C.sub.1 -C.sub.12 alkyl or C.sub.1 -C.sub.12 alkoxy; R.sup.1 represents hydrogen, C.sub.1 -C.sub.18 saturated or unsaturated alkyl, cycloalkyl, phenyl, benzyl or substituted phenyl or substituted benzyl where the substituents are C.sub.1 -C.sub.12 alkyl, or C.sub.1 -C.sub.12 alkoxy; R.sup.2 represents a substituted thienyl group where the substituents are, independently, the same as X, Y and Z; or a pharmaceutically acceptable salt thereof, are ACAT inhibitors.
    Type: Grant
    Filed: March 6, 1992
    Date of Patent: January 5, 1993
    Assignee: American Home Products Corporation
    Inventors: William F. Fobare, Donald P. Strike
  • [[2-(amino-3,4-dioxo-1-cyclobuten-1-yl) amino]alkyl]-acid derivatives
    Patent number: 5168103
    Abstract: A compound of the formula: ##STR1## in which R.sup.1 is hydrogen, alkyl or phenylalkyl; R.sup.2 is hydrogen, alkyl, alkenyl or phenylalkyl; or R.sup.1 and R.sup.2 taken together are --Ch.sub.2 CH.sub.2 --, --CH.sub.2 C(R.sup.6)(R.sup.7)CH.sub.2 --or --CH.sub.2 C(R.sup.8)(R.sup.9)--C(R.sup.10)(R.sup.11)CH.sub.2 --, where R.sup.6, R.sup.8 and R.sup.10 are, independently, hydrogen, alkyl of 1 to 6 carbon atoms or hydroxyl and R.sup.7, R.sup.9 and R.sup.11 are, independently, hydrogen or alkyl of 1 to 6 carbon atoms; A is alkylene or alkenylene; X is CO.sub.2 R.sup.3 in which R.sup.3 is hydrogen or alkyl, P(O)(OR.sup.4)(OR.sup.5) in which R.sup.4 and R.sup.5 are, independently, hydrogen or alkyl, 3,5-dioxo-1,2,4-oxadiazolindin-2-yl or 5-tetrazolyl; or a pharmaceutically acceptable salt thereof are useful as neuroprotectants.
    Type: Grant
    Filed: December 17, 1991
    Date of Patent: December 1, 1992
    Assignee: American Home Products Corporation
    Inventors: William A. Kinney, Deanna C. Garrison
  • Antipsychotic benzodioxan derivatives
    Patent number: 5166367
    Abstract: A compound of the formula: ##STR1## wherein the dotted line represents optional unsaturation; R.sup.1 and R.sup.2 are, independently, hydrogen, alkyl, alkoxy, aralkoxy, alkanoyloxy, hydroxy, halo, amino, mono- or dialkylamino, alkanamido or sulfonamido or R.sup.1 and R.sup.2 together are methylenedioxy, ethylenedioxy or propylenedioxy; R.sup.3 is hydrogen or alkyl; n is one of the integers 2,3 or 4; X is O or NR.sup.4, in which R.sup.4 is hydrogen or alkyl; or a pharmaceutically acceptable salt thereof, are antipsychotic agents.
    Type: Grant
    Filed: June 21, 1991
    Date of Patent: November 24, 1992
    Assignee: American Home Products Corporation
    Inventors: Gary P. Stack, Terrance H. Andree, Noreen T. Scherer
  • N-phenyl-N'-alkyl-N'-pyridylmethyl-bis-diamino- 5-methylene-1,3-dioxane-4,6-diones
    Patent number: 5164505
    Abstract: A compound of the formula: ##STR1## wherein: X, Y and Z, independently, are hydrogen, halogen, hydroxy, nitro, cyano, carboxyl, trifluoromethyl, phenyl, amino, mono and di-alkylamino, C.sub.1 -C.sub.12 alkyl or C.sub.1 -C.sub.12 alkoxy; R.sub.1 is hydrogen, C.sub.1 -C.sub.18 saturated or unsaturated alkyl, cycloalkyl, phenyl, benzyl or substituted benzyl where the substituents are C.sub.1 -C.sub.12 alkyl, or C.sub.1 -C.sub.12 alkoxy; and R.sub.2 is represented by 2. ##STR2## in which X, Y, and Z are defined above; or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: May 7, 1992
    Date of Patent: November 17, 1992
    Assignee: American Home Products Corporation
    Inventors: William F. Fobare, Donald P. Strike, Patrick M. Andrae
  • N,N',N'-trisubstituted-bis-amino-3-methylene-2,4(3H,5H)-furandione inhibitors of acyl-CoA:cholesterol-acyl transferase
    Patent number: 5153218
    Abstract: The compound of the formula: ##STR1## in which X, Y and Z are, independently, hydrogen, halogen, hydroxy, nitro, cyano, carboxyl, trifluoromethyl, phenyl, amino, alkylamino, dialkylamino, alkyl or alkoxy; R.sub.1 is alkyl, hydroxyalkyl, alkenyl, cycloalkyl, phenyl, benzyl, phenylethyl or substituted phenyl, benzyl or phenylethyl, alkoxy, halogen, cyano, trifluoromethyl, amino, alkylamino, dialkylamino, nitro, phenyl, benzyl or phenethyl or R.sub.1 is thienyl, imidazolyl, thiazolyl, pyridinyl, pyrimidinyl, pyrazinyl or benzamidazolyl; R.sub.2 is hydrogen, alkyl, cycloalkyl, phenyl, benzyl or substituted phenyl or benzyl, alkoxy, hologen, cyano, trifluoromethyl amino, nitro, alkylamino or dialkylamino; or a pharmaceutically acceptable salt thereof, are useful as ACAT inhibitors.
    Type: Grant
    Filed: October 28, 1991
    Date of Patent: October 6, 1992
    Assignee: American Home Products Corporation
    Inventor: William F. Fobare
  • Anti-arrhythmic agents
    Patent number: 5144072
    Abstract: This invention provides Class III anti-arrhythmic agents of the formula: ##STR1## in which R.sup.1 is alkylsulfonamido, R.sup.2 is ethyl, R.sup.3 is hydrogen, R.sup.4 is ethyl, and n is 2 to 4, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: October 21, 1988
    Date of Patent: September 1, 1992
    Assignee: American Home Products Corporation
    Inventors: George C. Buzby, Jr., Thomas J. Colatsky
  • N,N',N'-trisubstituted-5-bis-aminomethylene-1,3-dioxane-4,6-dione inhibitors of acyl-CoA:cholesterol-acyl transferase
    Patent number: 5136039
    Abstract: A compound of the formula: ##STR1## in which X, Y and Z are, independently, hydrogen, halogen, hydroxy, nitro, cyano, carboxyl, trifluoromethyl, phenyl, amino, alkylamino, dialkylamino, alkyl or alkoxy; R.sub.1 is alkyl, alkenyl, cycloalkyl, phenyl, benzyl or substituted phenyl or benzyl or alkoxy; R.sub.2 is: ##STR2## or a pharmaceutically acceptable salt thereof, are ACAT inhibitors.
    Type: Grant
    Filed: September 6, 1991
    Date of Patent: August 4, 1992
    Assignee: American Home Products Corporation
    Inventors: William F. Fobare, Donald P. Strike
  • Psychotropic benzofuran derivatives
    Patent number: 5134140
    Abstract: The antipsychotic, antidepressant, anxiolytic compounds of the formula: ##STR1## wherein Z is phenyl or phenyl substituted with alkyl, alkoxy, hydroxy, halogen or methylenedioxy or Z is one of the structures ##STR2## in which m is one of the integers 0, 1 or 2; R.sup.6 is hydrogen or alkyl; Y is H.sub.2 or O; or Z, taken with R.sup.1, forms one of the structures ##STR3## R.sup.1 is hydrogen or alkyl; R.sup.2 is hydrogen alkyl or phenyl; R.sup.3 is hydrogen or alkyl; R.sup.4 and R.sup.5 are independently hydrogen, alkyl, alkoxy, aralkoxy, alkanoyloxy, hydroxy, halo, amino, mono- or dialkylamino, alkanamido of 2 to 6 carbon atoms or sulfonamido, or R.sup.4 and R.sup.5 together form methylenedioxy, ethylenedioxy, or propylenedioxy; n is one of the integers 2, 3 or 4; or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: June 21, 1991
    Date of Patent: July 28, 1992
    Assignee: American Home Products Corporation
    Inventor: Gary P. Stack
  • Antidepressant polycyclic imides to treat depression
    Patent number: 5134141
    Abstract: A method for relieving depression with decahydro-3-[4-[4-(2-pyrimidinyl)-1-piperazinyl]butyl]-1,5-methano-6,7,9-m etheno-2H-pentaleno[1,2-d]azepine-2,4(3H)-dione, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: September 6, 1991
    Date of Patent: July 28, 1992
    Assignee: American Home Products Corporation
    Inventors: John A. Moyer, Gary P. Stack
  • Heterocyclic bisphosphonic acid derivatives
    Patent number: 5128328
    Abstract: The compound of the formula: ##STR1## positioned so that the gem-diphosphonic acid carbon atom is in the 4- or 5-position; R.sup.1 is alkyl or arylalkyl; R.sup.2 is hydrogen, 2- or 3-pyridinyl or 3-,5- or 6-alkylpyridin-2-yl; or a pharmaceutically acceptable salt thereof, with the proviso that when the gem-bisphosphonic acid substituted carbon atom is in 4-position, R.sup.1 is other than alkyl, used in the treatment of disease states involving calcium metabolism.
    Type: Grant
    Filed: October 25, 1991
    Date of Patent: July 7, 1992
    Assignee: American Home Products Corporation
    Inventors: Arie Zask, Richard D. Coghlan
  • Aminophenoxyalkyl derivatives of benzodioxan
    Patent number: 5126366
    Abstract: The compounds: ##STR1## wherein R.sup.1 and R.sup.2 are, independently, hydrogen, alkyl, alkoxy, aralkoxy, alkanoyloxy, hydroxy, halo, amino, mono- or dialkylamino, alkanamido, or sulfonamido, or R.sup.1 and R.sup.2 together form methylenedioxy, ethylenedioxy, or propylenedioxy; R.sup.3 is hydrogen or alkyl; n is one of the integers 2, 3 or 4; R.sup.4 and R.sup.5 are, independently, hydrogen, alkyl, cycloalkyl, alkanoyl, aroyl, alkylsulfonyl or arylsulfonyl, or R.sup.4 and R.sup.5 together form a 3-7 membered polymethylene ring; or a pharmaceutically acceptable salt thereof, are antipsychotic, antidepressant and anxiolytic agents useful in the treatment of multi-CNS disease states.
    Type: Grant
    Filed: June 21, 1991
    Date of Patent: June 30, 1992
    Assignee: American Home Products Corporation
    Inventors: Gary P. Stack, Magid A. Abou-Gharbia, Terrance H. Andree, Noreen T. Scherer
  • Psychotropic benzodioxan derivatives
    Patent number: 5126367
    Abstract: A compound of the formula: ##STR1## wherein the dotted line represents optional unsaturation; R.sup.1 is hydrogen, alkyl, alkoxy, alkanoyloxy, hydroxy, halo, nitro, amino, alkylamino, dialkylamino and alkanoylamino; X is O, S or CH.sub.2 ; n is an integer 2, 3 or 4; R.sup.2 is hydrogen or lower alkyl; R.sup.3 is hydrogen, lower alkyl, phenyl or benzyl; R.sup.4 is one of the structures ##STR2## in which m is one of the integers 0, 1 or 2; R.sup.5 is H or CH.sub.3 ; Z is H.sub.2 or O; Y is OCO, NHCO, NHCONH, CONH, and in addition, when R.sup.4 is II, Y may be NHSO.sub.2 CH.sub.2 ; or a pharmaceutically acceptable salt thereof are useful as antipsychotic/anxiolytic agents.
    Type: Grant
    Filed: June 21, 1991
    Date of Patent: June 30, 1992
    Assignee: American Home Products Corporation
    Inventors: Gary P. Stack, Magid A. Abou-Gharbia, Wayne E. Childers, Jr.
  • Quinoxaline phosphono-amino acids
    Patent number: 5118675
    Abstract: The compounds of the formula: ##STR1## in which Q is the quinoxaline nucleus; m is one of the integers 0, 1 or 2; n is one of the integers 1,2 or 3; or a pharmaceutically acceptable salt, alkyl ester or ##STR2## where R.sup.3 and R.sup.4 are, independently, hydrogen, nitro, halo or methoxy, are NMDA antagonists useful in the treatment and prevention of central nervous system related pathological conditions resulting from overstimulation by excitatory amino acids.
    Type: Grant
    Filed: February 15, 1991
    Date of Patent: June 2, 1992
    Assignee: American Home Products Corporation
    Inventors: Ivo L. Jirkovsky, Reinhardt B. Baudy, Lynne P. Greenblatt
  • Biphenyl amide cholesterol ester hydrolase inhibitors
    Patent number: 5112859
    Abstract: The compounds of the formula: ##STR1## in which R.sup.1 is hydrogen or alkyl; R.sup.2 is alkyl, cycloalkyl, cycloalkylalkyl, phenylalkyl or alkylphenylalkyl; or R.sup.1 and R.sup.2 taken together complete a heterocyclic moiety of the formula: ##STR2## in which X is ##STR3## NR.sup.5,--O-- or --S--; where R.sup.3, R.sup.4 and R.sup.5 are, independently hydrogen, alkyl, phenyl or substituted phenyl, in which the substituents are halogeno, alkoxy or trifluoromethyl; R.sup.6 is hydrogen, alkyl of gemdialkyl and n is one of the integers 0, 1 or 2, are cholesterol ester hydrolase inhibitors useful in the treatment of high serum cholesterol levels and associated disease states in the mammal such as coronary heart disease, atherosclerosis, familial hypercholesterolemia, hyperlipemia, and the like.
    Type: Grant
    Filed: September 14, 1990
    Date of Patent: May 12, 1992
    Assignee: American Home Products Corporation
    Inventors: Thomas J. Commons, Richard E. Mewshaw, Donald P. Strike
  • Pharmacologically active amides and esters containing an azabicycloalkane moiety
    Patent number: 5096901
    Abstract: Compounds of formula ##STR1## wherein R.sup.1 is hydrogen or one or more specified substituents,X is --O-- or --NR.sup.2 -- where R.sup.2 is lower alkyl, lower alkenyl, lower alkynyl, aryl or specified substituted lower alkyl or R.sup.2 represents a group --Z-- which is connected to the 8-position of the aromatic ring so as to form a heterocyclic ring of 5 to 7 ring members,Y is O or NR.sup.3 where R.sup.3 is hydrogen or lower alkyl, andB is a saturated azabicyclic ring (eg tropanyl or quinuclidinyl) or a N-oxide thereof and their acid addition salts are 5-HT.sub.3 antagonists which may be used in, for example, the treatment of neuro-psychiatric disorders.
    Type: Grant
    Filed: October 10, 1990
    Date of Patent: March 17, 1992
    Assignee: John Wyeth & Brother Limited
    Inventors: Terence J. Ward, Janet C. White
  • Renin inhibitors
    Patent number: 5095119
    Abstract: A compound of the formula: ##STR1## wherein A is ##STR2## in which X is .dbd.CH-- or .dbd.N--; R.sup.2 is hydrogen, alkyl, phenyl, benzyl or phenethyl; Y is --CH.sub.2--, --NH-- or --O--; and Z is --H.sub.2 or .dbd.O; B is His, Leu, Ile, Nva, Nle, Ala or Val; and R.sup.1 is hydrogen, alkyl, phenyl or phenylalkyl; or a pharmaceutically acceptable salt thereof are renin inhibitors.
    Type: Grant
    Filed: November 16, 1990
    Date of Patent: March 10, 1992
    Assignee: American Home Products Corporation
    Inventors: Timothy D. Ocain, David D. Deininger
  • Method of treating pulmonary inflammation
    Patent number: 5080899
    Abstract: This invention provides a method of preventing or reversing pulmonary inflammation in a mammal by administering an effective amount of rapamycin orally, parenterally, intranasally, or intrabronchially. As such, rapamycin is useful in providing the symptomatic relief of diseases in which pulmonary inflammation is a component such as, asthma, chronic obstructive pulmonary disease, emphysema, acute respiratory distress syndrome, bronchitis, and the like.
    Type: Grant
    Filed: February 22, 1991
    Date of Patent: January 14, 1992
    Assignee: American Home Products Corporation
    Inventors: Robert J. Sturm, Laurel M. Adams, Barry M. Weichman
  • Method of treating systemic lupus erythematosus
    Patent number: 5078999
    Abstract: This invention provides a method of treating systemic lupus erythematosus in a mammal in need thereof which comprises administering an effective amount of rapamycin orally, parenterally, intranasally, intrabronchially, or rectally.
    Type: Grant
    Filed: February 22, 1991
    Date of Patent: January 7, 1992
    Assignee: American Home Products Corporation
    Inventors: Linda M. Warner, Laurel M. Adams
  • Pyrrolimidazolones useful as renin inhibitors
    Patent number: 5075451
    Abstract: A compound of the formula: ##STR1## wherein A is ##STR2## in which X is .dbd.CH-- or .dbd.N--; R.sup.2 is hydrogen, alkyl, phenyl, benzyl or phenethyl; Y is --CH.sub.2 --, --NH-- or --O--; and Z is --H.sub.2 or .dbd.O; B is His, Leu, Ile, Nva, Nle, Ala or Val; and R.sup.1 is hydrogen, alkyl, phenyl or phenylalkyl; or a pharmaceutically acceptable salt thereof are renin inhibitors.
    Type: Grant
    Filed: November 16, 1990
    Date of Patent: December 24, 1991
    Assignee: American Home Products Corporation
    Inventors: Timothy D. Ocain, David D. Deininger