Patents Represented by Attorney Joseph W. Bulock
  • Patent number: 5886016
    Abstract: A class of benzopyranopyrazolyl derivatives is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula I ##STR1## wherein A, wherein X, m, n, p, B, R.sup.1, R.sup.2, and R.sup.4 are as described in the specification.
    Type: Grant
    Filed: June 9, 1997
    Date of Patent: March 23, 1999
    Assignee: G.D. Searle & Co.
    Inventors: John J Talley, Stephen R Bertenshaw, Donald J Rogier, Jr., Matthew J Graneto
  • Patent number: 5859257
    Abstract: A class of substituted isoxazolyl compounds is described for use in treating cyclooxygenase-2 related disorders. Compounds of particular interest are defined by Formula I ##STR1## wherein R.sup.1, R.sup.2, and R.sup.3, are described in the specification.
    Type: Grant
    Filed: August 14, 1996
    Date of Patent: January 12, 1999
    Assignee: G. D. Searle & Co.
    Inventor: John J Talley
  • Patent number: 5760068
    Abstract: A class of pyrazolyl benzenesulfonamide compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula II: ##STR1## or a pharmaceutically-acceptable salt thereof.
    Type: Grant
    Filed: September 6, 1996
    Date of Patent: June 2, 1998
    Assignee: G.D. Searle & Co.
    Inventors: John J. Talley, Thomas D. Penning, Paul W. Collins, Donald J. Rogier, Jr., James W. Malecha, Julie M. Miyashiro, Stephen R. Bertenshaw, Ish K. Khanna, Matthew J. Graneto, Roland S. Rogers, Jeffery S. Carter, Stephen H. Docter, Stella S. Yu
  • Patent number: 5756530
    Abstract: A class of pyrazolyl compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula II: ##STR1## wherein R.sup.1 is selected from hydrido, alkyl, alkenyl, aralkyl, alkynyl, cyanoalkyl, carboxyalkyl, aminocarbonylalkyl, arylaminocarbonylalkyl, heterocyclicalkyl, and alkoxycarbonylalkyl; wherein R.sup.3 is aryl substituted at a substitutable position with halo; wherein R.sup.4 is selected from hydrido and haloalkyl; and wherein R.sup.5 is selected from alkyl and amino; or a pharmaceutically-acceptable salt or prodrug thereof.
    Type: Grant
    Filed: September 25, 1996
    Date of Patent: May 26, 1998
    Assignee: G. D. Searle & Co.
    Inventors: Len F. Lee, Thomas D. Penning, Steven W. Kramer
  • Patent number: 5756529
    Abstract: A method of using pyrazolyl benzenesulfonamide compounds in treating inflammation and inflammation-related disorders in companion animals is disclosed.
    Type: Grant
    Filed: September 29, 1995
    Date of Patent: May 26, 1998
    Assignee: G.D. Searle & Co.
    Inventors: Peter C. Isakson, John J. Talley
  • Patent number: 5753688
    Abstract: A class of pyrazolyl benzenesulfonamide compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula I: ##STR1## or a pharmaceutically-acceptable salt thereof.
    Type: Grant
    Filed: September 27, 1995
    Date of Patent: May 19, 1998
    Inventors: John J. Talley, Thomas D. Penning, Paul W. Collins, Donald J. Rogier, Jr., James W. Malecha, Julie M. Miyashiro, Stephen R. Bertenshaw, Ish K. Khanna, Matthew J. Graneto, Roland S. Rogers, Jeffery S. Carter
  • Patent number: 5739166
    Abstract: A class of terphenyl compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula II: ##STR1## wherein each of R.sup.2 and R.sup.3 is independently selected from hydrido and halo; or wherein R.sup.2 and R.sup.3 together form --OCH.sub.2 O--; wherein each of R.sup.6 through R.sup.8 is independently selected from hydrido, lower alkyl, halo, lower alkoxy, lower haloalkyl, and lower dialkylamino; or wherein R.sup.6 and R.sup.7 together form --OCH.sub.2 O; and wherein R.sup.12 is selected from lower alkylsulfonyl and aminosulfonyl; or a pharmaceutically-acceptable salt thereof.
    Type: Grant
    Filed: November 29, 1994
    Date of Patent: April 14, 1998
    Assignee: G.D. Searle & Co.
    Inventors: David B. Reitz, Jinglin Li, Monica B. Norton
  • Patent number: 5736579
    Abstract: A class of substituted spiro compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula III: ##STR1## wherein n is a number selected from 0, 1 and 2; wherein R.sup.3 is methylsulfonyl or sulfamyl; and wherein R.sup.8 is selected from hydrido, fluoro, chloro, bromo, iodo, methyl, ethyl, n-propyl, isopropyl, butyl, tert-butyl, isobutyl, methoxy, ethoxy, propoxy, butoxy, hydroxyl, mercapto, methylthio, ethylthio, cyano, fluoromethyl, difluoromethyl, trifluoromethyl, chloromethyl, dichloromethyl, trichloromethyl, pentafluoroethyl, heptafluoropropyl, difluorochloromethyl, dichlorofluoromethyl, difluoroethyl, difluoropropyl, dichloroethyl, dichloropropyl, trifluoromethoxy, hydroxymethyl, methoxymethyl and ethoxymethyl; or a pharmaceutically-acceptable salt thereof.
    Type: Grant
    Filed: November 18, 1994
    Date of Patent: April 7, 1998
    Assignee: G.D. Searle & Co.
    Inventors: David B. Reitz, Robert E. Manning, Horng-Chi Huang, Jinglin Li
  • Patent number: 5721223
    Abstract: A class of imidazo?1,2-a!pyridinyldiacid compounds is described for cognitive enhancement and for treatment of cognitive disorders and which have activity as a cognitive enhancer. Such compounds are also useful to reduce neurotoxic injury associated with anoxia or ischemia which typically follows stroke, cardiac arrest or perinatal asphyxia. The treatment includes administration of a compound of this class alone or in a composition in an amount effective as an agonist or partial agonist to modulate, or as an antagonist to inhibit, excitotoxic actions at major neuronal excitatory amino acid receptor sites. Compounds of most interest are those of the formula: ##STR1## wherein each R.sup.20 is independently selected from hydrogen, methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl, tert-butyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl and cycloheptyl; wherein each of Y.sub.m and Y.sub.
    Type: Grant
    Filed: October 3, 1995
    Date of Patent: February 24, 1998
    Inventors: Donald W. Hansen, Jr., Karen B. Peterson, Joseph B. Monahan
  • Patent number: 5716964
    Abstract: A class of imidazo?1,2-a!pyridinylalkyl compounds is described for treatment to reduce neurotoxic injury associated with anoxia or ischemia which typically follows stroke, cardiac arrest or perinatal asphyxia. The treatment includes administration of a compound of this class alone or in a composition in an amount effective as an antagonist to inhibit excitotoxic actions at major neuronal excitatory amino acid receptor sites. Compounds of most interest are those of the formula: ##STR1## wherein each of R.sup.22, R.sup.23 and R.sup.24 is independently selected from hydrido, methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl, tert-butyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl and cycloheptyl; wherein each of Y.sub.m and Y.sub.
    Type: Grant
    Filed: April 18, 1995
    Date of Patent: February 10, 1998
    Assignee: G.D. Searle & Co.
    Inventors: Donald W. Hansen, Jr., Gilbert W. Adelstein, Karen B. Peterson, Sofya Tsymbalov
  • Patent number: 5708137
    Abstract: A class of compounds is described for use as fluorogenic substrates for herpesvirus proteases and for use in an assay to identify inhibitors of herpesvirus proteases. ##STR1## wherein W is selected from glycine, 4-aminobutyric acid, 5-aminopentanoic acid, 6-aminocaproic acid and 7-aminoheptanoic acid; wherein Y is selected from EDANS, Abz, DANSYL, nicotinic acid, 4-guanidino-benzoic acid, N-methyl-Abz, 4-chloro-Abz, 5-chloro-Abz, 6-chloro-Abz, 3,5-dibromo-Abz, 6-amino-nicotinic acid, 2-amino-nicotinic acid, 2-chloronicotinic acid, niflumic acid and fluorogenic derivatives thereof; and wherein Z is selected from tryptophan, tyrosine, phenylalanine, p-nitrophenylalanine, m-nitrophenylalanine, DABSYL, DABCYL and halogenated derivatives thereof.
    Type: Grant
    Filed: October 18, 1995
    Date of Patent: January 13, 1998
    Assignee: G.D. Searle & Co.
    Inventors: Mihaly V. Toth, Arthur J. Wittwer, Barry C. Holwerda
  • Patent number: 5700816
    Abstract: Combinations of a cyclooxygenase-2 inhibitor and a leukotriene A.sub.4 hydrolase inhibitor are described for treatment of inflammation and inflammation-related disorders.
    Type: Grant
    Filed: June 12, 1995
    Date of Patent: December 23, 1997
    Inventors: Peter C. Isakson, Gary D. Anderson, Susan A. Gregory
  • Patent number: 5686470
    Abstract: A class of substituted pyridyl compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula II ##STR1## wherein R.sup.1 is selected from hydrido, halo, alkoxy, haloalkoxy, aryl, alkylthio, alkylamino, aralkoxy, azido and allyloxy; wherein R.sup.2 is selected from hydrido, cyano, hydroxyalkyl, haloalkyl, aminoalkyl, aminocarbonyl and alkylcarbonylaminoalkyl; and wherein R.sup.5 and R.sup.6 are one or more radicals independently selected from halo, alkylsulfonyl, aminosulfonyl, alkoxy and alkylthio; provided one of R.sup.5 and R.sup.6 is substituted with alkylsulfonyl, aminosulfonyl, or haloalkylsulfonyl; or a pharmaceutically-acceptable salt thereof.
    Type: Grant
    Filed: February 10, 1995
    Date of Patent: November 11, 1997
    Inventors: Richard M. Weier, Len F. Lee, Richard A. Partis, Francis J. Koszyk
  • Patent number: 5684195
    Abstract: A one-pot synthesis of sulfonamides from sulfones has been developed. Conversion of sulfones to the corresponding sulfinic acid salts is followed by oxidative-amination to give the sulfonamides.
    Type: Grant
    Filed: May 31, 1995
    Date of Patent: November 4, 1997
    Assignee: G. D. Searle & Co.
    Inventors: Horng-Chih Huang, Scott R. Harring
  • Patent number: 5674879
    Abstract: Conformationally restricted compounds are described which are therapeutically effective as angiotensin II antagonists for the treatment of circulatory disorders.
    Type: Grant
    Filed: March 3, 1995
    Date of Patent: October 7, 1997
    Assignee: G.D. Searle & Co.
    Inventors: Robert E. Manning, Horng-Chih Huang
  • Patent number: 5672627
    Abstract: A class of substituted spirodienes is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula III: ##STR1## wherein R.sup.3 is methylsulfonyl or sulfamyl; and wherein R.sup.8 is selected from hydrido, fluoro, chloro, bromo, iodo, methyl, ethyl, n-propyl, isopropyl, butyl, tert-butyl, isobutyl, methoxy, ethoxy, propoxy, butoxy, hydroxyl, mercapto, methylthio, ethylthio, cyano, fluoromethyl, difluoromethyl, trifluoromethyl, chloromethyl, dichloromethyl, trichloromethyl, pentafluoroethyl, heptafluoropropyl, difluorochloromethyl, dichlorofluoromethyl, difluoroethyl, difluoropropyl, dichloroethyl, dichloropropyl, trifluoromethoxy, hydroxymethyl, methoxymethyl and ethoxymethyl; or a pharmaceutically-acceptable salt thereof.
    Type: Grant
    Filed: July 9, 1996
    Date of Patent: September 30, 1997
    Assignee: G.D. Searle & Co.
    Inventors: Horng-Chih Huang, David R. Reitz
  • Patent number: 5672626
    Abstract: A class of substituted spirodienes is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula II: ##STR1## wherein each of R.sup.1, R.sup.2, R.sup.4 and R.sup.5 is hydrido; wherein R.sup.3 is methylsulfonyl or sulfamyl; and wherein each of R.sup.6 through R.sup.10 is independently selected from hydrido, halo, alkyl, alkoxy, alkylthio, cyano, haloalkyl, haloalkoxy, hydroxyalkyl, alkoxyalkyl, hydroxyl, and mercapto; and wherein n is 1, 2 or 3; or a pharmaceutically-acceptable salt thereof.
    Type: Grant
    Filed: July 9, 1996
    Date of Patent: September 30, 1997
    Assignee: G. D. Searle & Co.
    Inventors: Horng-Chih Huang, David R. Reitz
  • Patent number: 5670532
    Abstract: A class of benzopyranopyrazolyl derivatives is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula I ##STR1## wherein A is --(CH.sub.2).sub.m --X--(CH.sub.2).sub.n --; wherein X is S(O).sub.p or O; wherein m is 0 or 1; wherein n is 0 or 1; wherein p is 0 or 1; wherein B is selected from phenyl and five and six membered heteroaryl; wherein R.sup.1 is selected from lower haloalkyl, cyano, formyl, lower alkoxycarbonyl, lower alkoxy, lower N-alkylaminocarbonyl, N-phenylaminocarbonyl, lower N,N-dialkylaminocarbonyl and lower N-alkyl-N-phenylaminocarbonyl; wherein R.sup.2 is phenyl substituted at a substitutable position with a radical selected from lower alkylsulfonyl and sulfamyl; and wherein R.sup.
    Type: Grant
    Filed: September 25, 1996
    Date of Patent: September 23, 1997
    Assignee: G. D. Searle & Co.
    Inventors: John J. Talley, Stephen R. Bertenshaw, Matthew J. Graneto, Donald J. Rogier
  • Patent number: 5670510
    Abstract: A class of substituted spirodienes is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula I: ##STR1## wherein A is selected from ##STR2## wherein each of R.sup.1 through R.sup.10 is independently selected from hydrido, halo, alkyl, alkoxy, alkylthio, cyano, haloalkyl, haloalkoxy, hydroxyalkyl; alkoxyalkyl, hydroxyl, mercapto, alkylsulfonyl, haloalkylsulfonyl, and sulfamyl; and wherein n is a number selected from 0, 1, 2 and 3; or a pharmaceutically-acceptable salt thereof.
    Type: Grant
    Filed: July 9, 1996
    Date of Patent: September 23, 1997
    Assignee: G. D. Searle & Co.
    Inventors: Horng-Chih Huang, David R. Reitz
  • Patent number: 5668161
    Abstract: A class of substituted thiazolyl compounds is described for use in treating inflammation disorders. Compounds are defined by Formula II ##STR1## wherein R.sup.1 is selected from hydrido, alkyl, haloalkyl, cyanoalkyl, alkylamino, aralkyl, arylamino, heteroarylsulfonylalkyl, heteroarylsulfonylhaloalkyl, aralkylamino, aryloxyalkyl, alkoxycarbonyl, aryl optionally substituted at a substitutable position with one or more radicals selected from halo and alkoxy, and heterocyclic optionally substituted at a substitutable position with one or more radicals selected from halo and alkyl; wherein R.sup.4 is selected from alkyl and amino; and wherein R.sup.5 is selected from aryl and heteroaryl; wherein R.sup.5 is optionally substituted at a substitutable position with one or more radicals selected from halo, alkyl and alkoxy; provided R.sup.5 is not phenyl at position 4 when R.sup.1 is .alpha.,.alpha.-bis(trifluoromethyl)methanol and R.sup.4 is methyl; or a pharmaceutically-acceptable salt thereof.
    Type: Grant
    Filed: July 9, 1996
    Date of Patent: September 16, 1997
    Assignee: G.D. Searle & Co.
    Inventors: John J. Talley, Jeffery S. Carter, Paul W. Collins, Steven W. Kramer, Thomas D. Penning, Donald J. Rogier, Jr., Roland S. Rogers