Patents Represented by Attorney Roger A. Williams
  • Patent number: 5591749
    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 disturbances (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 19, 1995
    Date of Patent: January 7, 1997
    Assignee: G. D. Searle & Co.
    Inventors: Daniel P. Becker, Daniel L. Flynn, Alan E. Moormann, Roger Nosal, Clara I. Villamil
  • Patent number: 5585252
    Abstract: A process for irreversible regio- and stereoselective enzyme catalyzed acylation of alcohols using enol esters as acylating reagents is disclosed. The present invention permits the selective modification of hydroxyl group(s) of chiral and meso alcohols, including sugars, organometallics, and glycosides. The enol freed upon transesterification rapidly tautomerizes to the corresponding volatile aldehyde or ketone thereby preventing the reverse reaction from occurring.
    Type: Grant
    Filed: September 21, 1994
    Date of Patent: December 17, 1996
    Assignee: G. D. Searle & Co.
    Inventors: Chi-Huey Wong, Yi-Fong Wang, Wiliam J. Hennen
  • Patent number: 5578643
    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: August 4, 1994
    Date of Patent: November 26, 1996
    Assignee: Loyola University of Chicago
    Inventor: Wayne R. Hanson
  • Patent number: 5578640
    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: November 26, 1996
    Assignee: Loyola University of Chicago
    Inventor: Wayne R. Hanson
  • Patent number: 5576447
    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 5, 1995
    Date of Patent: November 19, 1996
    Assignee: G. D. Searle & Co.
    Inventors: Norman A. Abood, Daniel L. Flynn, Scott A. Laneman, Roger Nosal, Lori A. Schretzman
  • Patent number: 5576426
    Abstract: The present invention relates to aldolase catalyzed stereo-selective synthesis of sugars and compositions of matter comprising arabinohexulose, xyloheptulose, threohexulose, and xylohexulose.
    Type: Grant
    Filed: September 8, 1994
    Date of Patent: November 19, 1996
    Assignee: G. D. Searle & Co.
    Inventors: Chi-Huey Wong, John R. Durrwachter, Richard L. Pederson
  • Patent number: 5565585
    Abstract: A new and practical method for synthesizing heterocyclic polyhydroxylated alkaloids using enzymatic aldol condensation and catalytic intramolecular reductive amination is disclosed.
    Type: Grant
    Filed: April 8, 1994
    Date of Patent: October 15, 1996
    Assignee: G. D. Searle & Co.
    Inventors: Chi-Huey Wong, Richard L. Pederson, Yi-Fong Wang
  • Patent number: 5554771
    Abstract: The present invention relates to 2-deoxy-N-acetylneuraminic acid derivatives and methods for their preparation.
    Type: Grant
    Filed: August 16, 1995
    Date of Patent: September 10, 1996
    Assignee: G. D. Searle & Co.
    Inventors: Chi-Huey Wong, William J. Hennen
  • Patent number: 5552431
    Abstract: This invention relates to compounds 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 amidines derivatives.
    Type: Grant
    Filed: March 24, 1995
    Date of Patent: September 3, 1996
    Assignee: G. D. Searle & Co.
    Inventors: Norman A. Abood, Robert B. Garland, Masateru Miyano
  • Patent number: 5550159
    Abstract: This invention relates to compounds having the following formula ##STR1## or pharmaceutically acceptable salt thereof which are useful in the inhibition of platelet aggregation, to pharmaceutical compositions of such phenylamidines derivatives, and to a method of inhibiting platelet aggregation in mammals by administering such compounds and compositions.
    Type: Grant
    Filed: May 18, 1995
    Date of Patent: August 27, 1996
    Assignee: G. D. Searle & Co.
    Inventors: Philippe R. Bovy, Robert B. Garland, Masateru Miyano, Joseph G. Rico, Thomas E. Rogers, Jeffery A. Zablocki
  • Patent number: 5543425
    Abstract: This invention relates to a method of inhibiting platelet aggregation comprising administering compounds having the following formula ##STR1##
    Type: Grant
    Filed: October 28, 1994
    Date of Patent: August 6, 1996
    Assignee: G. D. Searle & Co.
    Inventors: Steven P. Adams, Richard J. Lindmark, Masateru Miyano, Joseph G. Rico
  • Patent number: 5541344
    Abstract: The present invention is directed to intermediates of the formula ##STR1## which are useful in a process for the preparation of aminoazanoradamanatanes.
    Type: Grant
    Filed: May 19, 1995
    Date of Patent: July 30, 1996
    Assignee: G. D. Searle & Co.
    Inventors: Daniel P. Becker, Daniel L. Flynn, Alan E. Moormann, Clara I. Villamil
  • Patent number: 5536869
    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 which comprises treating (trimethylsilyl)acetylene sequentially with n-butyllithium and 4-formylmorpholine followed by acid hydrolysis to give 3-(trimethylsilyl)-2-propynal; treating 3-(trimethylsilyl)-2-propynal with lithium bis(trimethylsilyl)amide to give in situ N,3-bis(trimethylsilyl)-2-propyn-1-imine; condensation of N,3-bis(trimethylsilyl)-2-propyn-1-imine with lithium t-butyl acetate to give (.+-.)1,1-dimethylethyl 3-amino-5-(trimethylsilyl)-4-pentynoate; treating (.+-.)1,1-dimethylethyl 3-amino-5-(trimethylsilyl)-4-pentynoate- with p-toluenesulfonic acid to give (.+-.)1,1-dimethylethyl 3-amino-5-(trimethylsilyl)-4-pentynoate, mono p-toluenesulfonic acid salt, treatment of resulting salt with ethanol in the presence of p-toluenesulfonic acid to give (.+-.
    Type: Grant
    Filed: July 14, 1995
    Date of Patent: July 16, 1996
    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. Ann Hallinan, Donald W. Hansen, Jr., Donald E. Korte, Kathleen T. McLaughlin, 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: 5534521
    Abstract: This invention relates to compounds useful in treating HT.sub.4 and/or HT.sub.3 mediated conditions of the formula ##STR1## or a pharmaceutically acceptable salt thereof; pharmaceutical compositions containing the compounds and a method for treating serotonin mediated condition with the compositionswhich act as 5-HT.sub.4 agonists or antagonists and/or 5-HT.sub.3 antagonists.
    Type: Grant
    Filed: November 8, 1994
    Date of Patent: July 9, 1996
    Assignee: G. D. Searle & Co.
    Inventors: Daniel L. Flynn, Alan E. Moormann, Daniel P. Becker, Michael S. Dappen, Roger Nosal, Robert L. Shone, Clara I. Villamil
  • Patent number: 5532383
    Abstract: This invention relates to compounds of Formula I and the stereoisomers and pharmaceutically acceptable salts thereof ##STR1## wherein R is alkyl, alkenyl, alkynyl, or cycloalkylalkyl;R.sup.1 is alkyl;R.sup.2 is hydrogen, alkyl;R.sup.6 is alkyl;n is 1 to 5;p is 0 to 6;x is 0 or 2; andR.sup.4 and R.sup.5 are independently hydrogen or alkyl or together with N form a cycloalkylamine.The compounds of Formula I are leukotriene B.sub.4 antagonists and are useful as anti-inflammatory agents and in treating disease conditions mediated by LTB.sub.4.
    Type: Grant
    Filed: May 19, 1995
    Date of Patent: July 2, 1996
    Assignee: G. D. Searle & Co.
    Inventors: Stevan W. Djuric, Stephen H. Docter, Stella S. Yu
  • Patent number: 5530018
    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## R.sub.1 is alkoxy of one to six carbon atoms; R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are the same or different and are selected from the group consisting of hydrogen, halogen, CF.sub.3, hydroxy, alkoxy of one to six carbon atoms, acyl of two to seven carbon atoms, amino, amino substituted by one or two alkyl groups of one to six carbon atoms, C.sub.2 -C.sub.7 acylamino, aminocarbonyl, aminosulfonyl optionally substituted by one or two alkyl groups of one to six carbon atoms, C.sub.1 -C.sub.6 alkylsulfonyl and nitro;n is 0, 1 or 2;m is 0 or 1;X is 0 or NR.sub.7 ; andR.sub.7 is hydrogen or alkyl of 1 to 6 carbon atoms.
    Type: Grant
    Filed: February 4, 1994
    Date of Patent: June 25, 1996
    Assignee: G. D. Searle & Co.
    Inventors: Daniel P. Becker, Daniel L. Flynn, Clara I. Villamil
  • Patent number: 5521193
    Abstract: This invention relates to compounds useful in treating HT.sub.4 and/or HT.sub.3 mediated, conditions of the formula ##STR1## or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: May 19, 1995
    Date of Patent: May 28, 1996
    Assignee: G. D. Searle & Co.
    Inventors: Daniel L. Flynn, Alan E. Moormann, Daniel P. Becker, Michael S. Dappen, Roger Nosal, Robert L. Shone, Clara I. Villamil
  • Patent number: 5516917
    Abstract: This invention relates to compounds of Formula I and the stereoisomers and pharmaceutically acceptable salts thereof ##STR1## wherein R is alkyl, alkenyl, alkynyl, or cycloalkylalkyl;R.sup.1 is alkyl;R.sup.2 represents alkyl from 1 to 5 carbon atoms, aryl or aryl substituted with halogen or alkyl from 1 to 5 carbon atoms;R.sup.6 is alkyl;n is 1 to 5;p is 0 to 6;x is 0 or 2; andR.sup.4 and R.sup.5 are independently hydrogen or alkyl or together with N form a cycloalkylamine.The compounds of Formula I are leukotriene B.sub.4 antagonists and are useful as anti-inflammatory agents and in treating disease conditions mediated by LTB.sub.4.
    Type: Grant
    Filed: June 8, 1994
    Date of Patent: May 14, 1996
    Assignee: G. D. Searle & Co.
    Inventors: Steven W. Djuric, Stella S. Yu
  • Patent number: 5516782
    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: May 18, 1995
    Date of Patent: May 14, 1996
    Assignee: G. D. Searle & Co.
    Inventors: Daniel P. Becker, Daniel L. Flynn, Alan E. Moorman, Roger Nosal, Clara I. Villamil
  • Patent number: 5512561
    Abstract: The present invention provides substituted dibenzoxazepine compounds of Formula I: ##STR1## which are useful as analgesic agents for the treatment of pain, and for the treatment of prostaglandin E.sub.2 -mediated diseases, pharmaceutical compositions comprising a therapeutically-effective amount of a compound of Formula I in combination with a pharmaceutically-acceptable carrier, a method for eliminating or ameliorating pain in an animal, and a method for treating prostaglandin E.sub.2 -mediated diseases in an animal, comprising administering a therapeutically-effective amount of a compound of Formula I to the animal.
    Type: Grant
    Filed: March 10, 1995
    Date of Patent: April 30, 1996
    Assignee: G. D. Searle & Co.
    Inventors: Nizal S. Chandrakumar, Horng-Chih Huang, Richard A. Mueller