Patents Represented by Attorney Roger A. Williams
  • Patent number: 5681820
    Abstract: This invention herein relates to a method of treating a condition mediated by inhibition of .alpha..sub.v .beta..sub.3 integrins and a method of inhibiting tumor metastasis by administering a therapeutically effective amount of a compound having the following formula ##STR1## or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: May 16, 1995
    Date of Patent: October 28, 1997
    Assignee: G. D. Searle & Co.
    Inventor: Peter Gerrard Ruminski
  • Patent number: 5668134
    Abstract: The present invention provides a method for preventing or reducing a photosensitivity and/or phototoxicity reaction which may be caused by a once-per-day dose of a medication which causes a photosensitivity and/or phototoxicity reaction in a patient comprising administering the prescribed or suggested dose of the medication to the patient during the evening or early morning hours.
    Type: Grant
    Filed: January 28, 1994
    Date of Patent: September 16, 1997
    Assignee: G. D. Searle & Co.
    Inventors: Paul Dale Klimstra, Barbara Roniker, Edward Allen Swabb
  • Patent number: 5659063
    Abstract: The invention herein is directed to a process for producing a lactam of the formula ##STR1## from a methionine analog of the formula ##STR2## by treating the methionine analog with trimethylsulfonium halide or trimethylsulfoxonium halide in the presence of a base in a suitable aprotic solvent.The invention herein is further directed to the preparation of amidinophenyl pyrrolidinyl .beta.-alanine urea analogs using such methionine and lactam compounds as intermediates, which .beta.-alanine urea analogs are useful as antithrombotics.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: August 19, 1997
    Assignee: G. D. Searle & Co.
    Inventors: Norman Anthony Abood, Daniel Lee Flynn, Scott Anthony Laneman, Roger Nosal, Lori Ann Schretzman
  • Patent number: 5650535
    Abstract: A process for the preparation of a .gamma.-lactone of the formula ##STR1## which can be used to produce a single enantiomer of aminoazanoradamantane which is coupled to aromatic acid moieties to produce compounds useful as 5-HT agonists or antagonists.
    Type: Grant
    Filed: May 19, 1995
    Date of Patent: July 22, 1997
    Assignee: G. D. Searle & Co.
    Inventors: Daniel Paul Becker, Daniel Lee Flynn, Alan Edward Moormann, Clara Ines Villamil
  • Patent number: 5646183
    Abstract: This invention relates to phenyl amidine alkanoic acids and lactones having the following formula ##STR1## or a pharmaceutically acceptable salt which are useful in the inhibition of platelet aggregation. This invention also relates to pharmaceutical compositions of such phenyl amidine derivatives.
    Type: Grant
    Filed: May 25, 1995
    Date of Patent: July 8, 1997
    Assignee: G. D. Searle & Co.
    Inventors: Norman Anthony Abood, Robert Everett Manning, Masateru Miyano
  • Patent number: 5643917
    Abstract: This invention relates to compounds of the formula: ##STR1## or a pharmaceutically acceptable salt thereof wherein Z is selected from the group consisting of ##STR2##
    Type: Grant
    Filed: May 18, 1995
    Date of Patent: July 1, 1997
    Assignee: G. D. Searle & Co.
    Inventors: Daniel Lee Flynn, Robert L. Shone
  • Patent number: 5639765
    Abstract: This invention herein relates to a method of inhibiting bone resorption by administering a therapeutically effective amount of a compound having the following formula ##STR1## or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: January 17, 1995
    Date of Patent: June 17, 1997
    Assignee: G. D. Searle & Co.
    Inventor: Peter Gerrard Ruminski
  • Patent number: 5631399
    Abstract: The present invention relates to a novel process for the preparation of ethyl 3S-[[4-[[4-(aminoiminomethyl)phenyl]amino]-1,4-dioxobutyl]amino]-4-pentyno ate and pharmaceutically acceptable acid addition salt thereof.
    Type: Grant
    Filed: May 14, 1996
    Date of Patent: May 20, 1997
    Assignee: G. D. Searle & Co.
    Inventors: Kevin A. Babiak, Srinivasan Babu, James R. Behling, Mark L. Boys, Kimberly J. Cain-Janicki, Wendel W. Doubleday, Payman Farid, Timothy J. Hagen, E. A. Hallinan, Donald W. Hansen, Jr., Donald E. Korte, Kathleen T. Mc Laughlin, John R. Medich, Sean T. Nugent, Vlasdislav Orlovski, Jung M. Park, Karen B. Peterson, Daniel R. Pilipauskas, Barnett S. Pitzele, Sofya Tsymbalov, Glenn L. Stahl
  • Patent number: 5627190
    Abstract: The imidazopyridines containing meso-azacycle side chains as described herein find utility as antagonists of the serotonin 5-HT.sub.3 receptor. As such they are useful for the treatment of humans and animals wherein antagonism of 5-HT.sub.3 receptors is beneficial. Therapy is indicated for, but not limited to, the treatment of anxiety, psychoses, depression (especially depression accompanied by anxiety), cognitive disorders, substance abuse dependence and/or withdrawal, gastrointestinal motility disturbancies (including esophageal reflux, dyspepsia, irritable bowel syndrome), emesis caused by chemotherapeutic agents, and visceral pain. Additionally, the compounds of the present invention may find utility as enhancers of nasal absorption of bioactive compounds.
    Type: Grant
    Filed: April 6, 1995
    Date of Patent: May 6, 1997
    Assignee: G. D. Searle & Co.
    Inventors: Daniel P. Becker, Daniel L. Flynn, Alan E. Moormann, Clara I. Villamil
  • Patent number: 5625093
    Abstract: Novel substituted amino acid derivatives are provided which inhibit platelet aggregation and which are useful in pharmaceutical compositions and methods of inhibiting platelet aggregation.
    Type: Grant
    Filed: May 25, 1995
    Date of Patent: April 29, 1997
    Assignee: G. D. Searle & Co.
    Inventor: Thomas E. Rogers
  • Patent number: 5624956
    Abstract: Novel urea derivatives and pharmaceutical compositions thereof are provided which inhibit platelet aggregation.
    Type: Grant
    Filed: May 24, 1995
    Date of Patent: April 29, 1997
    Assignee: The Monsanto Company
    Inventors: Foe S. Tjoeng, Mihaly V. Toth, Dudley E. McMackins, Steven P. Adams
  • Patent number: 5614539
    Abstract: Novel urea derivatives are provided which inhibit platelet aggregation. This invention also pertains to pharmaceutical compositions and methods of using such derivatives.
    Type: Grant
    Filed: June 1, 1995
    Date of Patent: March 25, 1997
    Assignee: G. D. Searle & Co.
    Inventors: Steven P. Adams, Foe S. Tjoeng, Mark E. Zupec
  • Patent number: 5612366
    Abstract: The meso-azacyclic aromatic acid amides and esters of the present invention are useful in the treatment of the central nervous system and gastrointestinal motility disorders such as gastroesophageal reflux, non-ulcer dyspepsia, delayed gastric emptying, ileus, irritable bowel syndrome, and the like. Additionally, the compounds of the present invention find utility as antagonists of serotonin 5-HT.sub.3 receptors. As such they are useful for the treatment of humans and animals wherein antagonism of 5-HT.sub.3 receptors is beneficial. Therapy is indicated for, but not limited to, the treatment of anxiety, psychoses, depression (especially depression accompanied by anxiety), cognitive disorders, substance abuse dependence and/or withdrawal, irritable bowel syndrome, emesis caused by chemotherapeutic agents, and visceral pain. Additionally, the compounds of the present invention may find utility as enhancers of nasal absorption of bioactive compounds.
    Type: Grant
    Filed: April 28, 1994
    Date of Patent: March 18, 1997
    Assignee: G. D. Searle & Co.
    Inventors: Daniel P. Becker, Daniel L. Flynn, Alan E. Moorman, Roger Nosal, Clara I. Villamil
  • Patent number: 5612355
    Abstract: This invention relates to phenyl amidine alkanoic acids and lactones having the following formula ##STR1## or a pharmaceutically acceptable salt which are useful in the inhibition of platelet aggregation. This invention also relates to pharmaceutical compositions of such phenyl amidine derivatives.
    Type: Grant
    Filed: May 26, 1995
    Date of Patent: March 18, 1997
    Assignee: G. D. Searle & Co.
    Inventors: Norman A. Abood, Robert E. Manning, Masateru Miyano
  • Patent number: 5610296
    Abstract: The invention herein is directed to a process for producing a lactam of the formula ##STR1## from a methionine analog of the formula ##STR2## by treating the methionine analog with trimethylsulfonium halide or trimethylsulfoxonium halide in the presence of a base in a suitable aprotic solvent.The invention herein is further directed to the preparation of amidinophenyl pyrrolidinyl .beta.-alanine urea analogs using such methionine and lactam compounds as intermediates, which .beta.-alanine urea analogs are useful as antithrombotics.
    Type: Grant
    Filed: December 5, 1994
    Date of Patent: March 11, 1997
    Assignee: G. D. Searle & Co.
    Inventors: Norman A. Abood, Daniel L. Flynn, Scott A. Laneman, Roger Nosal, Lori A. Schretzman
  • Patent number: 5609884
    Abstract: The present invention relates to controlled release dosage forms composed of a naproxen layer which contains a delayed release granulate of naproxen compressed with an immediate release granulate of naproxen and an immediate release naproxen sodium layer compressed with the naproxen layer, designed to promptly exert a therapeutic effect while also maintaining the therapeutic blood concentration for a prolonged duration of 24 hours.
    Type: Grant
    Filed: August 31, 1992
    Date of Patent: March 11, 1997
    Assignee: G. D. Searle & Co.
    Inventor: Subhash Desai
  • Patent number: 5605931
    Abstract: Prostaglandins of the PGE type can be administered in a therapeutically effective amount to protect tissue from injury resulting from chemotherapeutic agents by administering the PGE-type prostaglandin prior to administration of the chemotherapeutic agent.
    Type: Grant
    Filed: May 11, 1995
    Date of Patent: February 25, 1997
    Assignee: Loyola University of Chicago
    Inventor: Wayne R. Hanson
  • Patent number: 5604239
    Abstract: The imidazopyridines compounds of the present invention are serotonergic 5-HT.sub.3 antagonists. As such they are useful for the treatment of humans and animals wherein antagonism of 5-HT.sub.3 receptors is beneficial. Therapy is indicated for, but not limited to, the treatment of anxiety, psychoses, depression (especially depression accompanied by anxiety), cognitive disorders, substance abuse dependence and withdrawal, gastrointestinal motility disturbancies (including esophageal reflux, dyspepsia, gastric stasis, irritable bowel syndrome), emesis caused by chemotherapeutic agents, and visceral pain. Additionally, the compounds of the present invention may find utility as enhancers of nasal absorption of bioactive compounds.
    Type: Grant
    Filed: April 18, 1995
    Date of Patent: February 18, 1997
    Assignee: G. D. Searle & Co.
    Inventors: Daniel P. Becker, Daniel L. Flynn, Alan E. Moormann, Roger Nosal, Clara I. Villamil
  • Patent number: 5601843
    Abstract: A pharmaceutical composition including a core of an NSAID selected from diclofenac and piroxicam which core is surrounded by a mantle coating of a prostaglandin, wherein an intermediate coating can be present between the NSAID core and prostaglandin mantle coating.
    Type: Grant
    Filed: July 18, 1994
    Date of Patent: February 11, 1997
    Assignee: G. D. Searle & Co.
    Inventors: Rene A. Gimet, Jean C. Jinot, Christian Magnet, Isabelle Maroteaux, Francoise M. Nevoux, Roger E. Scoyer, Barbara J. Struthers
  • Patent number: 5602155
    Abstract: This invention herein relates to compounds having the following formula ##STR1## or a pharmaceutically acceptable salt thereof which are useful in the inhibition of platelet aggregation, to pharmaceutical compositions containing the compound and to a method of inhibiting platelet aggregation in mammals by administering such compounds and compositions.
    Type: Grant
    Filed: January 17, 1995
    Date of Patent: February 11, 1997
    Assignee: G. D. Searle & Co.
    Inventor: Peter G. Ruminski