Patents Represented by Attorney Roger A. Williams
  • Patent number: 5439937
    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: March 3, 1994
    Date of Patent: August 8, 1995
    Assignee: G. D. Searle & Co.
    Inventors: Stevan W. Djuric, Stephen H. Docter, Stella S. Yu
  • Patent number: 5436249
    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: May 16, 1994
    Date of Patent: July 25, 1995
    Assignee: G. D. Searle & Co.
    Inventors: Michael S. Dappen, Barnett S. Pitzele, Michael F. Rafferty
  • Patent number: 5434161
    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: November 6, 1992
    Date of Patent: July 18, 1995
    Assignee: G. D. Searle & Co.
    Inventors: Daniel P. Becker, Daniel L. Flynn, Alan E. Moormann, Roger Nosal, Clara I. Villamil
  • Patent number: 5432284
    Abstract: The present invention relates to a novel process for the preparation of heterocyclic alkylamide derivatives having the following formula: ##STR1## and the pharmaceutically acceptable acid addition salt thereof wherein X represents halo, alkyl having 1 to 6 carbon atoms, hydrido, trifluoromethyl, phenyl, or lower alkoxy having 1 to 6 carbon atoms; Y represents the group --CN or --CONH.sub.2 ; R.sub.2 represents alkyl having 1 to 6 carbon atoms; R.sub.
    Type: Grant
    Filed: September 8, 1993
    Date of Patent: July 11, 1995
    Assignee: G. D. Searle & Co.
    Inventors: John H. Dygos, Thomas R. Kowar, Kathleen T. McLaughlin, Gatis Plume, Michael L. Prunier, Richard J. Salzmann, Mike G. Scaros, Joseph J. Wieczorek
  • Patent number: 5430043
    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 of such phenylamidines derivatives, and to a method of inhibiting platelet aggregation in mammals by administering such compounds and compositions.
    Type: Grant
    Filed: August 24, 1993
    Date of Patent: July 4, 1995
    Assignee: G. D. Searle & Co.
    Inventors: Philippe R. Bovy, Joseph G. Rico, Thomas E. Rogers
  • Patent number: 5430040
    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: October 21, 1993
    Date of Patent: July 4, 1995
    Assignee: G. D. Searle & Co.
    Inventors: Daniel P. Becker, Daniel L. Flynn, Alan E. Moormann, Clara I. Villamil
  • Patent number: 5424424
    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: October 7, 1993
    Date of Patent: June 13, 1995
    Assignee: G. D. Searle & Co.
    Inventors: Nizal S. Chandrakumar, Richard A. Mueller
  • Patent number: 5424334
    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: December 19, 1991
    Date of Patent: June 13, 1995
    Assignee: G. D. Searle & Co.
    Inventors: Norman A. Abood, Robert B. Garland, Masateru Miyano
  • Patent number: 5420343
    Abstract: The present invention provides compounds of the formula: ##STR1## and the pharmaceutically acceptable salts thereof, wherein: R.sup.1 and R.sup.2 are each alkyl;n is an integer of from 1 to 4;x is oxygen or --(CH.sub.2).sub.m --;m is an integer of from 1 to 3;y is oxygen or sulfur; andp is an integer of from 1 to 4.These compounds are inhibitors of COX-I and/or COX-II, and are useful for the treatment of inflammation-associated disorders.The present invention also provides pharmaceutical compositions comprising a therapeutically-effective amount of a compound of Formula I in combination with a pharmaceutically-acceptable carrier, and a method for treating inflammation-associated disorders in an animal comprising administering a therapeutically-effective amount of a compound of Formula I to the animal.
    Type: Grant
    Filed: August 31, 1994
    Date of Patent: May 30, 1995
    Assignee: G. D. Searle & Co.
    Inventors: Francis J. Koszyk, Richard M. Weier
  • Patent number: 5420270
    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: October 7, 1993
    Date of Patent: May 30, 1995
    Assignee: G. D. Searle & Co.
    Inventors: Nizal S. Chandrakumar, Horng-Chih Huang, Richard A. Mueller
  • Patent number: 5409939
    Abstract: This invention relates to compounds having the following formula ##STR1## which are useful in the inhibition of platelet aggregation. This invention also relates to pharmaceutical compositions of such phenyl amidine thio derivatives.
    Type: Grant
    Filed: February 12, 1993
    Date of Patent: April 25, 1995
    Assignee: G. D. Searle & Co.
    Inventors: Steven P. Adams, Richard J. Lindmark, Masateru Miyano, Joseph G. Rico
  • Patent number: 5401645
    Abstract: A process for producing N-substituted amino compounds, a process for oxidizing an N-substituted amino compound with a microbe, or cell fragment or cell free extract thereof, and a process for oxidizing an N-substituted amino compound with a microbe, or cell fragment or cell free extract thereof and reducing the oxidized N-substituted amino compound to N-substituted-polyhydroxy piperidines based on N-substituted mannosamines, allosamines and altrosamines, N-substituted polyhydroxy pyrrolidines, and N-substituted polyhydroxy azetidines. In addition, a one pot process for producing N-substituted-polyhydroxy piperidines based on N-substituted mannosamines, allosamines and altrosamines, N-substituted polyhydroxy pyrrolidines, and N-substituted polyhydroxy azetidines from the respective sugar is disclosed.
    Type: Grant
    Filed: March 16, 1992
    Date of Patent: March 28, 1995
    Assignees: Monsanto Company, G. D. Searle & Co.
    Inventors: Roy W. Grabner, Bryan H. Landis, Mike G. Scaros, Rick J. Rutter
  • Patent number: 5399562
    Abstract: This invention relates to compounds of the formula: ##STR1## which are useful as 5-HT.sub.4 agonists or antagonists and 5-HT.sub.3 antagonists.
    Type: Grant
    Filed: February 4, 1994
    Date of Patent: March 21, 1995
    Assignee: G. D. Searle & Co.
    Inventors: Daniel P. Becker, Daniel L. Flynn, Clara I. Villamil
  • Patent number: 5395932
    Abstract: The present invention provides substituted dibenzoxazepine compounds of Formula I: ##STR1## wherein X is oxygen, sulfur ##STR2## A is --CH.sub.2 -- or ##STR3## E and F may be --CH, oxygen, nitrogen or sulfur, and may not be the same; G is oxygen, nitrogen or sulfur; with the proviso that when G is oxygen or sulfur, one of E or F is nitrogen, 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: April 30, 1993
    Date of Patent: March 7, 1995
    Assignee: G. D. Searle & Co.
    Inventors: Nizal S. Chandrakumar, Timothy J. Hagen, Barnett S. Pitzele, Sofya Tsymbalov, E. Ann Hallinan
  • Patent number: 5393764
    Abstract: The compounds of the present invention comprise substituted phenolic thioethers represented by the formula ##STR1## wherein: R.sup.1 and R.sup.2 are the same or different and independently represent tert-alkyl or phenyl; R.sup.3 represents hydrogen or alkyl; X represents --(CH.sub.2).sub.w --B--(CH.sub.2).sub.y -- wherein B represents O, S, or CH.sub.2 and w and y can each independently be an integer from 0 to 3 with the proviso that the sum of w+y is equal to or less than 3; A represents O or S(O).sub.n wherein n is 0, 1 or 2; p is an integer from 1 to 4; and R represents alkyl; OH; OR.sup.4 wherein R.sup.4 is alkyl of 1 to 4 carbon atoms; NR.sup.5 R.sup.6 wherein R.sup.5 is hydrogen or alkyl and R.sup.6 is hydrogen, alkyl, heterocyclealkyl in which the hetercyclic ring may optionally be substituted; cycloalkyl; substituted cycloalkyl; phenyl; substituted phenyl; phenylalkyl; or substituted phenylalkyl; or NR.sup.5 R.sup.6 together form a heterocyclic ring which may optionally be substituted; or R is (CH.
    Type: Grant
    Filed: August 25, 1993
    Date of Patent: February 28, 1995
    Assignee: G. D. Searle & Co.
    Inventors: Richard A. Mueller, Richard A. Partis
  • Patent number: 5393747
    Abstract: The present invention provides methods for treating convulsions, ischemia and other diseases responsive to prostaglandin-E.sub.2 antagonists in an animal comprising administering a therapeutically-effective amount of a substituted dibenzoxazepine compound of Formula I, or a pharmaceutically-acceptable salt thereof, to the animal: ##STR1## wherein Y is oxygen, sulfur, --SO-- or --SO.sub.2 --, R.sup.1 is hydrogen, halogen or --CF.sub.3, R.sup.2 is hydrogen, halogen, --OH or --OCH.sub.3, R.sup.3 is hydrogen, alkyl, aryl, alkyl-substituted aryl or aryl-substituted alkyl, m is an integer of from 1 to 5, X is ##STR2## R.sup.4 is hydrogen, alkyl, aryl, alkyl-substituted aryl, trifluoromethyl-substituted aryl or aryl-substituted alkyl, and R.sup.5 and R.sup.6 are each independently hydrogen, alkyl, aryl, alkyl-substituted aryl or aryl-substituted alkyl.
    Type: Grant
    Filed: November 17, 1993
    Date of Patent: February 28, 1995
    Assignee: G. D. Searle & Co.
    Inventors: E. Ann Hallinan, Robert K. Husa, Karen B. Peterson
  • Patent number: 5389645
    Abstract: The present invention provides substituted tyrosyl diamine amide 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: August 13, 1992
    Date of Patent: February 14, 1995
    Assignee: G. D. Searle & Co.
    Inventors: Donald W. Hansen, Jr., Nizal S. Chandrakumar, Karen B. Peterson, Sofya Tsymbalov
  • Patent number: 5382578
    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 convulsions and ischemia, 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 and for the treatment of convulsions and ischemia, in an animal comprising administering a therapeutically-effective amount of a compound of Formula I to the animal.
    Type: Grant
    Filed: November 19, 1993
    Date of Patent: January 17, 1995
    Assignee: G. D. Searle & Co.
    Inventors: Robert K. Husa, Timothy J. Hagen, E. Ann Hallinan
  • Patent number: 5380740
    Abstract: This invention encompasses compounds of the following formula and the stereoisomers and pharmaceutically acceptable salts thereof. ##STR1## wherein R represents lower alkyl of 1 to 6 carbon atoms, lower alkenyl of 2 to 6 carbon atoms, or --(CH.sub.2).sub.m --R.sup.3 wherein R.sup.3 represents cycloalkyl of 3 to 5 carbon atoms and m is 1, 2 or 3; R.sub.1 is --CONH.sub.2 or ##STR2## NHSO.sub.2 R.sub.2 wherein R.sub.2 is lower alkyl, phenyl, unsubstituted or substituted with loweralkyl, or ##STR3## and n is an integer from 2 to 5. The compounds are useful anti-inflammatory agents for treating, for example, inflammatory bowel disease, rheumatoid arthritis, gout, asthma and psoriasis.
    Type: Grant
    Filed: April 28, 1993
    Date of Patent: January 10, 1995
    Assignee: G. D. Searle & Co.
    Inventors: Stevan W. Djuric, Donald J. Fretland, Stella S. Yu
  • Patent number: 5378727
    Abstract: Novel substituted heterocyclic derivatives are provided which inhibit platelet aggregation. This invention also pertains to pharmaceutical compositions and methods of using such derivatives.
    Type: Grant
    Filed: July 19, 1993
    Date of Patent: January 3, 1995
    Assignee: G. D. Searle & Co.
    Inventors: Philippe R. Bovy, Joseph G. Rico, Thomas E. Rogers, Foe S. Tjoeng, Jeffery A. Zablocki