Patents Represented by Attorney Roger A. Williams
  • Patent number: 5378840
    Abstract: The present invention provides dibenzoxazepine compounds of Formula I: ##STR1## which are useful as analgesic agents for the treatment of pain, pharmaceutical compositions comprising a therapeutically-effective amount of a compound of Formula I in combination with a pharmaceutically-acceptable carrier, and a method for eliminating or ameliorating pain in an animal comprising administering a therapeutically-effective amount of a compound of Formula I to the animal.
    Type: Grant
    Filed: August 24, 1993
    Date of Patent: January 3, 1995
    Assignee: G. D. Searle & Co.
    Inventors: Albert C. Lee, E. Ann Hallinan, Timothy J. Hagen, Robert K. Husa, Sofya Tsymbalov, Jean-Pierre Van Hoeck
  • Patent number: 5364850
    Abstract: The present invention provides substituted tyrosyl diamide compounds of general Formula I: ##STR1## and the pharmaceutically-acceptable salts thereof, which are useful for inducing analgesia in animals, pharmaceutical compositions comprising a pharmaceutically-acceptable carrier and a compound of Formula I, and a method for inducing analgesia in an animal in need thereof comprising administering a therapeutically-effective amount of a compound of Formula I to the animal.
    Type: Grant
    Filed: September 24, 1993
    Date of Patent: November 15, 1994
    Assignee: G. D. Searle & Co.
    Inventors: Donald W. Hansen, Jr., Nizal S. Chandrakumar, Karen B. Peterson, Sofya Tsymbalov, Robert K. Husa
  • Patent number: 5360907
    Abstract: The present invention relates to compounds of the formula ##STR1## wherein HET is either ##STR2## and pharmaceutical compositions containing a therapeutically effective amount of the compounds in combination with a pharmaceutically acceptable carrier and a method for treating diseases mediated by platelet activating factor.
    Type: Grant
    Filed: June 14, 1993
    Date of Patent: November 1, 1994
    Assignee: G.D. Searle & Co.
    Inventors: Kirk T. Lentz, Richard M. Weier
  • Patent number: 5356919
    Abstract: This invention relates to a compound of the formula: ##STR1## or a pharmaceutically acceptable salt thereof wherein X is oxygen, sulfur, --CH.dbd.CH--, or --CH.dbd.N--; wherein R.sup.1 is --CO.sub.2 R.sup.2 or tetrazole; wherein R.sup.2 is hydrogen, alkyl of 1 to 6 carbons or a pharmaceutically acceptable cation; wherein R is an alkyl of from 1 to 20 carbons, --(CH.sub.2).sub.p CF.sub.3 or --(CH.sub.2).sub.q R.sup.3 wherein R.sup.3 is alkoxy, phenoxy or alkoxy substituted phenoxy wherein the alkoxy group has from 1 to 8 carbons; wherein p and q are integers from 0 to 20; wherein n is 0 or 1; and wherein m is 0, 1, 2, or 3.
    Type: Grant
    Filed: May 30, 1991
    Date of Patent: October 18, 1994
    Assignee: G. D. Searle & Co.
    Inventors: Stevan W. Djuric, Richard A. Haack, Julie M. Miyashiro
  • Patent number: 5354746
    Abstract: The present invention provides substituted dibenzoxazepine compounds of Formula I: ##STR1## which are useful as analgesic agents for the treatment of pain, and as prostaglandin-E.sub.2 antagonists 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: June 1, 1993
    Date of Patent: October 11, 1994
    Assignee: G. D. Searle & Co.
    Inventors: Nizal S. Chandrakumar, Barnett S. Pitzele
  • Patent number: 5354738
    Abstract: This invention 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 including the compounds, and to a method of inhibiting platelet aggregation in mammals by administering such compounds and compositions.
    Type: Grant
    Filed: September 4, 1992
    Date of Patent: October 11, 1994
    Assignees: G. D. Searle & Co., The Monsanto Company
    Inventors: Foe S. Tjoeng, Jeffery A. Zablocki
  • Patent number: 5354747
    Abstract: The present invention provides substituted dibenzoxazepine and dibenzthiazepine compounds of Formula I: ##STR1## which are useful as analgesic agents for the treatment of pain, and for 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 comprising administering a therapeutically-effective amount of a compound of Formula I to the 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: June 16, 1993
    Date of Patent: October 11, 1994
    Assignee: G. D. Searle & Co.
    Inventors: Donald W. Hansen, Jr., Karen B. Peterson
  • Patent number: 5354863
    Abstract: The present invention provides novel substituted opioid analgesic compounds of Formula I: ##STR1## which are opioid agonists, and which are useful as analgesic agents for the treatment of pain, pharmaceutical compositions comprising a therapeutically-effective amount of a compound of Formula I in combination with a pharmaceutically-acceptable carrier, and a method for eliminating or ameliorating pain in an animal comprising administering a therapeutically-effective amount of a compound of Formula I to the animal.
    Type: Grant
    Filed: February 24, 1993
    Date of Patent: October 11, 1994
    Assignee: G. D. Searle & Co.
    Inventors: Michael S. Dappen, Barnett S. Pitzele, Michael F. Rafferty
  • Patent number: 5354757
    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, aminosulfone optionally substituted by one or two alkyl groups of one to six carbon atoms, C.sub.1 -C.sub.6 alkylsulfone and nitro;n is 0, 1 or 2;m is 0 or 1;X is O or NR.sub.7 ; andR.sub.7 is hydrogen or alkyl of 1 to 6 carbon atoms.
    Type: Grant
    Filed: December 15, 1992
    Date of Patent: October 11, 1994
    Assignee: G. D. Searle & Co.
    Inventors: Daniel L. Flynn, Alan E. Moormann
  • Patent number: 5348158
    Abstract: A reusable dispensing package is provided for dispensing medication in the form of tablets, pills, capsules or the like, in a predetermined sequence, the package includes a hinged container into which is placed a disposable blister pack containing the medicament, the container having a spring-loaded button or a plunger attached thereto which is moved around the cover of the dispenser and when depressed releases a tablet or pill from the blister.
    Type: Grant
    Filed: December 19, 1991
    Date of Patent: September 20, 1994
    Assignee: G. D. Searle & Co.
    Inventors: David G. Honan, Gregory W. Lantz, Thomas E. Salisbury
  • Patent number: 5344837
    Abstract: This invention 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 including the compounds, and to a method of inhibiting platelet aggregation in mammals by administering such compounds and compositions.
    Type: Grant
    Filed: September 23, 1993
    Date of Patent: September 6, 1994
    Assignees: G.D. Searle & Co., Monsanto Company
    Inventors: Foe S. Tjoeng, Jeffery A. Zablocki
  • Patent number: 5342838
    Abstract: The present invention relates to phenolic thioetheramides of the formula ##STR1## wherein R.sup.1 and R.sup.2 are tert-alkyl or phenyl, Alk.sup.1 and Alk.sup.2 are alkylene; X is sulfur or oxygen, m is 0, 1, or 2; and R is ##STR2## wherein R.sup.3 and R.sup.4 are hydrogen or alkyl and Alk.sup.3 is alkylene; or ##STR3## wherein Y is CH, N, O, or S; R.sup.6 is hydrogen, alkyl, phenyl, substituted phenyl, benzyl, substituted benzyl or a heterocyclic amine; and R.sup.7 is hydrogen or alkyl. The compounds inhibit 5-lipoxygenase and are useful in the treatment of inflammation and allergic conditions.
    Type: Grant
    Filed: December 9, 1993
    Date of Patent: August 30, 1994
    Assignee: G. D. Searle & Co.
    Inventors: Richard A. Mueller, Richard A. Partis
  • Patent number: 5334616
    Abstract: The compounds of the present invention comprise substituted phenolic thioethers represented by the formula(I) and the radicals are defined in the claims: ##STR1## The compounds of the present invention are useful in the treatment of local and systemic inflammation and allergy reactions.
    Type: Grant
    Filed: June 22, 1993
    Date of Patent: August 2, 1994
    Assignee: G. D. Searle & Co.
    Inventors: Richard A. Mueller, Richard A. Partis
  • Patent number: 5329025
    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 2, 1992
    Date of Patent: July 12, 1994
    Assignee: G. D. Searle & Co.
    Inventors: Chi-Huey Wong, Richard L. Pederson, Yi-Fong Wang
  • Patent number: 5326907
    Abstract: The present invention relates to compounds of the Formula I ##STR1## wherein R.sup.1 and R.sup.2 are the same or different and independently represent tert-alkyl, halogen, or phenyl; Alk.sup.1 represents straight or branched chain alkylene of 2 to 10 carbon atoms which can optionally be substituted by hydroxy, provided that said hydroxy is not attached to a carbon which is adjacent to sulfur or oxygen, X represents sulfur or oxygen, and Alk.sup.2 represents straight or branched chain alkylene of 1 to 4 carbon atoms; and the pharmaceutically acceptable salts thereof. These compounds are specific 5-lipoxygenase inhibitors and are useful as anti-inflammatory and anti-allergy agents and in the treatment of conditions mediated by 5-lipoxygenase.
    Type: Grant
    Filed: December 18, 1992
    Date of Patent: July 5, 1994
    Assignee: G. D. Searle & Co.
    Inventors: Richard A. Partis, Richard A. Mueller
  • Patent number: 5324722
    Abstract: The present invention provides substituted dibenzoxazepine compounds of Formula I: ##STR1## which are useful as analgesic agents for the treatment of pain, pharmaceutical compositions comprising a therapeutically-effective amount of a compound of Formula I in combination with a pharmaceutically-acceptable carrier, and a method for eliminating or ameliorating pain in an animal comprising administering a therapeutically-effective amount of a compound of Formula I to the animal.
    Type: Grant
    Filed: May 7, 1993
    Date of Patent: June 28, 1994
    Assignee: G. D. Searle & Co.
    Inventors: Timothy J. Hagen, Michael Clare, Michael F. Rafferty, E. Ann Hallinan
  • Patent number: 5318977
    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: November 6, 1992
    Date of Patent: June 7, 1994
    Assignee: G. D. Searle & Co.
    Inventors: Daniel P. Becker, Daniel L. Flynn, Alan E. Moorman, Roger Nosal, Clara I. Villamil
  • Patent number: 5314902
    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: January 27, 1993
    Date of Patent: May 24, 1994
    Assignee: Monsanto Company
    Inventors: Foe S. Tjoeng, Mihaly V. Toth, Dudley E. McMackins, Steven P. Adams
  • Patent number: 5314886
    Abstract: This invention relates to novel N-substituted lactams having the following formula ##STR1## useful in the treatment and prevention of Cholecystokinin (CCK) related disorders of the gastrointestinal, central nervous and appetite regulatory systems of mammals.
    Type: Grant
    Filed: October 29, 1992
    Date of Patent: May 24, 1994
    Assignee: G. D. Searle & Co.
    Inventors: Daniel P. Becker, Daniel L. Flynn, Clara I. Villamil
  • Patent number: 5314895
    Abstract: The present invention relates to compounds of the formula ##STR1## or a pharmaceutically acceptable salt thereof; wherein n is 0, 1 or 2;wherein R is H or lower alkyl of 1 to 6 carbon atoms;wherein X is selected from the group consisting of hydrogen, methane sulfonamide, nitro, cyano, imidazolyl, alkoxy of 1 to 6 carbon atoms and hydroxy; andwherein Ar is selected from the group consisting of pyridinyl and benzofuranyl optionally substituted by methane sulfonamide, nitro, cyano, or imidazolyl with the proviso that when n is 1, Ar is other then phenyl;pharmaceutical compositions containing these compounds and a method for treating cardiac arrhythmias in mammals by administering the compositions.
    Type: Grant
    Filed: March 11, 1993
    Date of Patent: May 24, 1994
    Assignee: G. D. Searle & Co.
    Inventors: Bipinchandra N. Desai, Konrad F. Koehler, Mark A. Russell