Patents Represented by Attorney Paul D. Matukaitis

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  • Spiro-hydantoins as aldose reductase inhibitors
    Patent number: 4853401
    Abstract: The invention relates to spirohydantoins of the formula I ##STR1## where R.sub.1 and R.sub.2 are defined hereinbelow. Also disclosed are methods of preparation, pharmaceutical compositions containing at least one of these compounds, and methods of using said compounds for treatment and prevention of complications of diabetes and galactosemia.
    Type: Grant
    Filed: April 1, 1987
    Date of Patent: August 1, 1989
    Assignee: G. D. Searle & Co.
    Inventors: Philippe R. Bovy, Claude Gillet, Albert Lenaers, Paul Niebes, Joseph Roba, Georges Lambelin
  • Phenolic thioethers as inhibitors of 5-lipoxygenase
    Patent number: 4847305
    Abstract: The compounds of the present invention comprise substituted phenolic thioether derivatives that are specific inhibitors of 5-lipoxygenase and which, therefore, are useful in the treatment of local and systemic inflammation, allergy and hypersensitivity reactions and other disorders in which agents formed in the 5-lipoxygenase metabolic pathway are involved.
    Type: Grant
    Filed: May 23, 1988
    Date of Patent: July 11, 1989
    Assignee: G. D. Searle & Co.
    Inventors: Richard A. Mueller, Richard A. Partis
  • Tetraenyl prostaglandins
    Patent number: 4847293
    Abstract: This invention encompasses prostaglandins of the formula ##STR1## wherein R represents hydrogen or lower alkyl having 1 to 6 carbon atoms; R.sub.1 represents hydrogen, vinyl, or lower alkyl having 1 to 4 carbon atoms and a wavy line represents R or S stereochemistry; R.sub.2, R.sub.3, and R.sub.4 are hydrogen or lower alkyl having 1 to 4 carbon atoms or R.sub.2 and R.sub.3 together with carbon Y form a cycloalkenyl having 4 to 6 carbon atoms or R.sub.3 and R.sub.4 together with carbons X and Y form a cycloalkenyl having 4 to 6 carbons. Compounds of this invention have potent gastric antisecretory and cytoprotective properties with unexpectedly low diarrheogenic side effects.
    Type: Grant
    Filed: June 10, 1988
    Date of Patent: July 11, 1989
    Assignee: G. D. Searle & Co.
    Inventors: Paul W. Collins, Alan F. Gasiecki
  • Fluorenyl substituted tyrosyl dipeptide amides which are useful in treating pain
    Patent number: 4847241
    Abstract: The invention relates to novel substituted tyrosyl alanine dipeptide amides of the formula: ##STR1## and the pharmaceutically acceptable acid addition salts thereof wherein R.sup.1 is hydrogen, lower alkyl, hydroxy, --OCO.sub.2 lower alkyl, lower alkoxy, --O(CH.sub.2).sub.n --phenyl with the phenyl optionally substituted by halogen, --NO.sub.2, --CN, --NH.sub.2 or lower alkyl wherein n is 1 to 4; R.sup.2 and R.sup.3 represent lower alkyl, halogen, or lower alkoxy, or either one of R.sup.2 or R.sup.3 is hydrogen and the other is lower alkyl, lower alkoxy or halogen; R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, and R.sup.9 may be the same or different and represent hydrogen or lower alkyl; R.sup.
    Type: Grant
    Filed: January 20, 1988
    Date of Patent: July 11, 1989
    Assignee: G. D. Searle & Co.
    Inventors: Donald W. Hansen, Jr., Robert W. Hamilton, Barnett S. Pitzele, Michael Clare
  • Modified interferon gammas
    Patent number: 4845196
    Abstract: Described are modified human gamma interferons, genes coding for their synthesis and plasmids containing and capable of expressing these genes.
    Type: Grant
    Filed: June 24, 1985
    Date of Patent: July 4, 1989
    Assignee: G. D. Searle & Co.
    Inventor: Graham J. Cowling
  • Substituted alkylidene imidazoles
    Patent number: 4837333
    Abstract: This disclosure relates to a class of novel substituted alkylidene imidazole derivatives and pharmaceutically acceptable salts thereof. The disclosure further describes pharmaceutical compositions containing such compounds and to the use of such compounds and compositions as agents for selectively inhibiting the action of the enzyme thromboxane synthetase.
    Type: Grant
    Filed: May 14, 1987
    Date of Patent: June 6, 1989
    Assignee: G. D. Searle & Co.
    Inventors: Paul W. Manley, Roderick A. Porter, Mun F. Lai
  • Alkylated bicycloalkaneamines for treatment of neurotoxic injury
    Patent number: 4837218
    Abstract: Compounds, compositions and methods of treatment are described to control brain damage associated with anoxia or ischemia which typically follows such conditions as stroke, cardiac arrest or perinatal asphyxia. The treatment includes administration of an alkylated bicycloalkaneamine compound as an antagonist to inhibit excitotoxic actions at major neuronal exzcitatory amino acid receptor sites.
    Type: Grant
    Filed: October 23, 1987
    Date of Patent: June 6, 1989
    Assignee: Washington University
    Inventor: John W. Olney
  • Phenolic thioalkylamides as inhibitors of 5-lipoxygenase
    Patent number: 4835189
    Abstract: The compounds of the present invention comprise substituted phenolic thioalkylamides that are specific inhibitors of 5-lipoxygenase and which, therefore, are useful in the treatment of local and systemic inflammation, allergy and hypersensitivity reactions and other disorders in which agents formed in the 5-lipoxygenase metabolic pathway are involved.
    Type: Grant
    Filed: June 5, 1987
    Date of Patent: May 30, 1989
    Assignee: G. D. Searle & Co.
    Inventors: Richard A. Mueller, Richard A. Partis
  • Phenolic thioethers as inhbitors of 5-lipoxygenase
    Patent number: 4835190
    Abstract: The compounds of the present invention comprise substituted phenolic thioether derivatives that are specific inhibitors of 5-lipoxygenase and which, therefore, are useful in the treatment of local and systemic inflammation, allergy and hypersensitivity reactions and other disorders in which agents formed in the 5-lipoxygenase metabolic pathway are involved.
    Type: Grant
    Filed: June 5, 1987
    Date of Patent: May 30, 1989
    Assignee: G. D. Searle & Co.
    Inventors: Richard A. Mueller, Richard A. Partis
  • Method of using alkenyl- or alkynyl-substituted thiobarbiturates to reduce neurotoxic injury
    Patent number: 4833148
    Abstract: Methods and compositions are described for treatment to control brain damage associated with anoxia or ischemia which typically follows stroke, cardiac arrest or perinatal asphyxia. The treatment includes administration of an alkenyl-substituted or alkynyl-substituted thiobarbiturate characterized in having broad-spectrum activity as an antagonist to inhibit excitotoxic actions at major neuronal excitatory amino acid receptor sites.
    Type: Grant
    Filed: April 9, 1987
    Date of Patent: May 23, 1989
    Assignee: Washington University
    Inventor: John W. Olney
  • Phenyl substituted dipeptide amides
    Patent number: 4822775
    Abstract: The invention relates to novel substituted tyrosyl alanine dipeptide amides of the formula: ##STR1## and the pharmaceutically acceptable acid addition salts thereof wherein R.sup.1 is hydrogen, lower alkyl, hydroxy, --OCO.sub.2 lower alkyl, lower alkoxy, --O(CH.sub.2).sub.n -phenyl with the phenyl optionally substituted by halogen, --NO.sub.2, --CN, --NH.sub.2 or lower alkyl wherein n is 1 to 4; R.sup.2 and R.sup.3 represent lower alkyl, halogen, or lower alkoxy, or either one of R.sup.2 or R.sup.3 is hydrogen and the other is lower alkyl, lower alkoxy or halogen; R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, and R.sup.9 may be the same or different and represent hydrogen or lower alkyl; R.sup.
    Type: Grant
    Filed: July 14, 1986
    Date of Patent: April 18, 1989
    Assignee: G. D. Searle & Co.
    Inventors: Donald W. Hansen, Jr., Barnett S. Pitzele, Michael Clare, Robert W. Hamilton
  • Tetraenyl prostaglandins
    Patent number: 4820728
    Abstract: This invention encompasses prostaglandins of the formula ##STR1## wherein R represents hydrogen or lower alkyl having 1 to 6 carbon atoms; R.sub.1 represents hydrogen, vinyl, or lower alkyl having 1 to 4 carbon atoms and the wavy line represents R or S stereochemistry; R.sub.2, R.sub.3, and R.sub.4 are hydrogen or lower alkyl having 1 to 4 carbom atoms or R.sub.2 and R.sub.3 together with carbon Y form a cycloalkenyl having 4 to 6 carbon atoms or R.sub.3 and R.sub.4 together with carbons X and Y form a cycloalkenyl having 4 to 6 carbons. Compounds of this invention have potent gastric antisecretory and cytoprotective properties with unexpectedly low diarrheogenic side effects.
    Type: Grant
    Filed: June 30, 1987
    Date of Patent: April 11, 1989
    Assignee: G. D. Searle & Co.
    Inventors: Paul W. Collins, Alan F. Gasiecki
  • Kojic acid ether-ester derivatives
    Patent number: 4812474
    Abstract: Kojic acid ether-ester derivatives of formula I ##STR1## are useful pharmacological agents for the prevention, management or alleviation of elastase mediated diseases or conditions.
    Type: Grant
    Filed: January 12, 1988
    Date of Patent: March 14, 1989
    Assignee: G. D. Searle & Co.
    Inventors: Arthur L. Campbell, Masateru Miyano
  • Aralkoxy and aryloxyalkoxy kojic acid derivatives
    Patent number: 4812584
    Abstract: This invention relates to substituted aralkoxy and aryloxyalkoxy kojic acid derivatives, which are useful as leukotriene D.sub.4 (LTD.sub.4) inhibitors and therefore useful in the treatment of allergies, inflammatory conditions, and coronary vasoconstriction.
    Type: Grant
    Filed: July 24, 1987
    Date of Patent: March 14, 1989
    Assignee: G. D. Searle & Co.
    Inventors: Miyano Masateru, Robert L. Shone
  • Leukotriene LTD.sub.4 and LTB.sub.4 antagonists
    Patent number: 4808729
    Abstract: The invention encompasses compounds of Formula I ##STR1## and the pharmaceutically acceptable salts and geometrical and optical isomers thereof wherein:X, Y, and Z are each independently O or S with S optionally oxidized to S.dbd.O;Alk is alkylene or hydroxyalkylene containing 1-6 carbon atoms;R.sub.1 is hydrogen or lower alkyl;n is 0 to 5;R.sub.2 is hydrogen, lower alkyl, cycloalkyl, --(CH.sub.2).sub.n --CO.sub.2 R.sub.1, phenyl, phenyl substituted with halo, lower alkyl or lower alkoxy; andAr is 5,6,7,8-tetrahydro-1-naphthalenyl, phenyl, or phenyl substituted with lower alkyl, hydroxy, lower alkoxy, or lower alkanoyl. The compounds are useful as anti-allergy agents and anti-inflammatory agents.
    Type: Grant
    Filed: September 24, 1987
    Date of Patent: February 28, 1989
    Assignee: G. D. Searle & Co.
    Inventors: James R. Deason, Michael A. Stealey, Richard M. Weier
  • Process for preparing the combination products of triamterene and hydrochlorothiazide
    Patent number: 4804540
    Abstract: A combination pharmaceutical composition is described, together with the process for manufacturing said pharmaceutical composition wherein the active ingredients, namely triamterene and hydrochlorothiazide, are incorporated into a solid dosage form via a single wet granulation process utilizing an acid component. Said process simplifies the formulation and manufacturing, permits greater uniformity, and increases in vitro dissolution.
    Type: Grant
    Filed: December 16, 1987
    Date of Patent: February 14, 1989
    Assignee: G. D. Searle & Co.
    Inventors: Frederic J. Nugent, John K. C. Yen
  • Imidazopyridine derivatives and pharmaceutical compositions
    Patent number: 4804658
    Abstract: This invention relates to novel imidazopyridine derivatives useful in the treatment of diseases or disorders mediated by platelet-activating factor. This invention further relates to pharmaceutical compositions of such imidazopyridine derivatives.
    Type: Grant
    Filed: September 15, 1986
    Date of Patent: February 14, 1989
    Assignee: G. D. Searle & Co.
    Inventors: Paul W. Manley, Roderick A. Porter
  • Process and intermediates for the preparation of halogenated protease inhibitors
    Patent number: 4803294
    Abstract: This invention relates to novel intermediate compounds which are useful for producing the halogenated protease inhibitors that are the subject matter of U.S. Pat. No. 4,469,885. In particular, the invention relates to novel methods and intermediates for making said protease inhibitors, the intermediate compounds being of the formula: ##STR1## wherein R.sub.1 is: (a) straight or branched chain lower alkyl having 1-6 carbon atoms; or(b) H;wherein R.sub.6 is:(a) straight or branched chain higher alkyl having 13-25 carbon atoms; or(b) straight or branched chain higher alkenyl having 13-25 carbon atoms;wherein R.sub.5 is:(a) straight or branched chain lower alkyl having 1-6 carbon atoms; or(b) benzyl;wherein R.sub.7 is:(a) straight or branched chain lower alkyl having 1-6 carbon atoms; or(b) H;wherein R.sub.2 is:(a) --Cl, --Br, or --I; or(b) --CF.sub.3.
    Type: Grant
    Filed: October 29, 1987
    Date of Patent: February 7, 1989
    Assignee: G. D. Searle & Co.
    Inventors: Richard A. Mueller, Richard A. Partis
  • 5-lipoxygenase inhibitors
    Patent number: 4801611
    Abstract: This invention encompasses compounds and methods for inhibiting lipoxygenase and includes a pharmaceutical composition comprising a pharmaceutical carrier and an effective lipoxygenase inhibiting amount of a compound of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are the same or different members of the group consisting of tert-alkyl of 4 to 10 carbon atoms; and R.sub.3 is ##STR2## wherein R.sub.4 is hydrogen or lower alkyl; ##STR3## wherein R.sub.6 and R.sub.7 may be the same or different and are alkyl of 1 to 4 carbon atoms; or ##STR4## and the pharmaceuticlaly acceptable salts thereof. The compounds and pharmaceutical formulations of the present invention are 5-lipoxygenase inhibitors and, therefore, are useful in the treatment of local and systemic inflammation, allergy and hypersensitivity reactions and other disorders in which agents formed in the 5-lipoxygenase metabolic pathway are involved.
    Type: Grant
    Filed: May 7, 1987
    Date of Patent: January 31, 1989
    Assignee: G. D. Searle & Co.
    Inventors: Leland J. Chinn, Bipinchandra N. Desai, Richard A. Mueller
  • Phenolic ester derivatives as elastase inhibitors
    Patent number: 4801610
    Abstract: Phenolic esters of the general formula I ##STR1## are useful for the prevention, management or alleviation of elastase mediated diseases or conditions.
    Type: Grant
    Filed: June 5, 1987
    Date of Patent: January 31, 1989
    Assignee: G. D. Searle & Co.
    Inventors: Masateru Miyano, James R. Deason