Patents Represented by Attorney Joseph W. Bulock
  • Patent number: 5663180
    Abstract: A class of 1,2-diarylcyclopentenyl compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula III: ##STR1## wherein each of R.sup.1 and R.sup.2 is independently selected from alkyl, hydrido, hydroxyalkyl, halo, haloalkyl, alkoxycarbonyl and carboxyl; wherein R.sup.5 is selected from alkylsulfonyl, haloalkylsulfonyl and sulfamyl; and wherein B is phenyl or pyridyl, wherein B is optionally substituted at a substitutable position with alkyl, halo, alkylthio, cyano, haloalkyl, alkoxy, hydroxyalkyl and alkoxyalkyl; or a pharmaceutically-acceptable salt thereof.
    Type: Grant
    Filed: July 15, 1994
    Date of Patent: September 2, 1997
    Assignee: G.D. Searle & Co.
    Inventors: David B. Reitz, Jinglin Li
  • Patent number: 5643933
    Abstract: This invention is in the field of antiinflammatory pharmaceutical agents and specifically relates to compounds, compositions and methods for treating disorders mediated by cyclooxygenase-2 or 5-lipoxygenase, such as inflammation.
    Type: Grant
    Filed: June 2, 1995
    Date of Patent: July 1, 1997
    Assignee: G. D. Searle & Co.
    Inventors: John J. Talley, James A. Sikorski, Bryan H. Norman, Roland S. Rogers, deceased, Balekudru Devadas, Matthew J. Graneto, Jeffery S. Carter
  • Patent number: 5643947
    Abstract: A class of .omega.-amino-.alpha.-phenylalkanonitrile derivatives is described having use in treatment of cardiovascular dysfunctions such as hypertension. Compounds of most interest are those of the formula: ##STR1## wherein each of R.sub.1 and R.sub.2 is methoxy, R.sub.3 is hydrido, R.sub.4 is isopropyl, R.sub.5 is methyl and R.sub.6 is selected from linear alkyl, phenylpropyl, phenylbutyl and phenylpentyl.
    Type: Grant
    Filed: May 24, 1995
    Date of Patent: July 1, 1997
    Assignee: G. D. Searle & Co.
    Inventors: Claude L. Gillet, Philippe R. Bovy, Hugo Gorissen, Michel P. Snyers
  • Patent number: 5639777
    Abstract: A class of 1,4,5-triphenyl pyrazoles is described for the treatment of inflammation, including treatment of pain and disorders such as arthritis. Compounds of particular interest are of Formula II ##STR1## wherein R.sup.1 is selected from the group hydrido, halo, alkyl, alkylthio, alkylsulfinyl, alkylsulfonyl, nitro, amino, N-monoalkylamino, N,N-dialkylamino, acylamino, acylaminoalkyl, haloalkyl, hydroxy and alkoxy; wherein R.sup.2 is selected from hydrido, alkyl, cyano and haloalkyl; wherein R.sup.3 is selected from the group hydrido, halo, alkyl, alkylthio, alkylsulfinyl, alkylsulfonyl, nitro, amino, N-monoalkylamino, N,N-dialkylamino, acylamino, acylaminoalkyl, haloalkyl, hydroxy and alkoxy; and wherein R.sup.4 is alkyl or amino; or a pharmaceutically-acceptable salt thereof.
    Type: Grant
    Filed: May 21, 1996
    Date of Patent: June 17, 1997
    Assignee: G.D. Searle & Co.
    Inventor: Len F. Lee
  • Patent number: 5633237
    Abstract: A class of imidazo[1,2-a]pyridinylalkyl phosphonic acid 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## and the carboxylic and phosphonic alkyl esters and salts thereof; wherein R.sup.9 is 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: July 6, 1994
    Date of Patent: May 27, 1997
    Assignee: G.D. Searle & Co.
    Inventors: Donald W. Hansen, Jr., Gilbert W. Adelstein, Karen B. Peterson, Sofya Tsymbalov
  • Patent number: 5633272
    Abstract: A class of substituted isoxazolyl 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 hydroxyl, lower alkyl, carboxyl, lower carboxyalkyl, lower aminocarbonylalkyl, lower alkoxycarbonylalkyl, lower aralkyl, lower alkoxyalkyl, lower aralkoxyalkyl, lower alkylthioalkyl, lower aralkylthioalkyl, lower alkylaminoalkyl, lower aryloxyalkyl, lower arylthioalkyl, lower haloalkyl, lower hydroxylalkyl, cycloalkyl, cycloalkylalkyl, and aralkyl; wherein R.sup.3 is selected from cycloalkyl, cycloalkenyl, aryl, and heteroaryl; wherein R.sup.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: May 27, 1997
    Inventors: John J. Talley, David L. Brown, Srinivasan Nagarajan, Jeffery S. Carter, Richard M. Weier, Michael A. Stealey, Paul W. Collins, Roland S. Rogers, deceased, Karen Seibert
  • Patent number: 5620999
    Abstract: A class of imidazolyl 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 lower alkyl, lower haloalkyl, lower hydroxyalkyl, lower aralkenyl, lower aryloxyalkyl, lower arylthioalkyl and heteroaryl; wherein R.sup.3 is selected from lower alkyl and amino; and wherein R.sup.4 is one or more radicals selected from hydrido, halo, lower alkyl and lower alkoxy; or where R.sup.4 together with the phenyl radical forms naphthyl or benzodioxolyl; provided R.sup.1 is not lower alkyl when R.sup.3 is methyl and when R.sup.4 is hydrido, methyl, methoxy or chloro; or a pharmaceutically-acceptable salt thereof.
    Type: Grant
    Filed: July 28, 1994
    Date of Patent: April 15, 1997
    Inventors: Richard M. Weier, Paul W. Collins, Michael A. Stealey, Thomas E. Barta
  • Patent number: 5616601
    Abstract: A class of imidazolyl compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula I: ##STR1## wherein R.sup.1 -R.sup.6 are as described in the specification; or a pharmaceutically-acceptable salt thereof.
    Type: Grant
    Filed: June 5, 1995
    Date of Patent: April 1, 1997
    Assignee: GD Searle & Co
    Inventors: Ish K. Khanna, Richard M. Weier, Paul W. Collins, Yi Yu, Xiangdong Xu, Richard A. Partis, Francis J. Koszyk
  • Patent number: 5595905
    Abstract: A method for controlling nutrient concentration levels in a fermentation broth containing bacteria or a yeast and a nutrient is disclosed. A computer calculates the nutrient consumption rate of the broth for selected intervals of time between successive samples in real time by comparing the nutrient concentrations of the samples. Thus, the computer having the capability to predict an estimated rate at which the nutrient concentration is expected to decrease at selected sample intervals. Further, adding fresh nutrient to the fermentation broth at a rate and quantity based on the estimated rate to control nutrient concentration levels. Furthermore, a means for obtaining a series of samples and measuring nutrient concentrations is also disclosed.
    Type: Grant
    Filed: August 12, 1994
    Date of Patent: January 21, 1997
    Assignee: G.D. Searle & Co.
    Inventors: Bruce F. Bishop, Rodney G. Combs, Saied Banankhah
  • Patent number: 5596008
    Abstract: A class of substitute pyridyl compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula I ##STR1## wherein R.sup.1 is haloalkyl; wherein R.sup.2 is aryl optionally substituted at a substitutable position with one or more radicals independently selected from alkylsulfinyl, alkyl, cyano, carboxyl, alkoxycarbonyl, haloalkyl, hydroxyl, hydroxyalkyl, haloalkoxy, amino, alkylamino, arylamino, nitro, halo, alkoxy and alkylthio; wherein R.sup.3 is aryl substituted at a substitutable position with a radical selected from alkylsulfonyl and sulfamyl; and wherein R.sup.4 is selected from halo, alkoxy and alkynyloxy; or a pharmaceutically-acceptable salt thereof.
    Type: Grant
    Filed: February 10, 1995
    Date of Patent: January 21, 1997
    Assignee: G. D. Searle & Co.
    Inventor: Len F. Lee
  • Patent number: 5580985
    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, heterocyciicalkyl, 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 28, 1995
    Date of Patent: December 3, 1996
    Assignee: G. D. Searle & Co.
    Inventors: Len F. Lee, Thomas D. Penning, Steven W. Kramer
  • Patent number: 5576339
    Abstract: A class of 2,3-substituted cyclopenta-2,4-dienyl 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.1 and R.sup.2 is independently selected from hydrido, lower alkyl, lower hydroxyalkyl, halo, lower haloalkyl, lower alkoxycarbonyl and carboxyl; and wherein each of R.sup.3 through R.sup.12 is independently selected from hydrido, halo, lower alkyl, lower alkylthio, cyano, hydroxyl, mercapto, lower haloalkyl, lower haloalkoxy, lower alkoxy, lower hydroxyalkyl, lower alkoxyalkyl, lower alkylsulfonyl, lower haloalkylsulfonyl and sulfamyl; provided R.sup.5 and R.sup.10 are not both hydrido or methoxy; or a pharmaceutically suitable salt or prodrug thereof.
    Type: Grant
    Filed: April 5, 1995
    Date of Patent: November 19, 1996
    Inventors: Horng-Chih Huang, David R. Reitz
  • Patent number: 5565482
    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 29, 1995
    Date of Patent: October 15, 1996
    Assignee: G.D. Searle & Co.
    Inventors: John J. Talley, Stephen R. Bertenshaw, Matthew J. Graneto, Donald J. Rogier
  • Patent number: 5563165
    Abstract: A class of pyrazolyl benzenesulfonamide compounds is described for use in treating inflammation and inflammation-related disorders.
    Type: Grant
    Filed: June 1, 1995
    Date of Patent: October 8, 1996
    Assignee: G. D. Searl & 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
  • Patent number: 5547975
    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 20, 1994
    Date of Patent: August 20, 1996
    Inventors: John J. Talley, Stephen R. Bertenshaw, Matthew J. Graneto, Donald J. Rogier
  • Patent number: 5521207
    Abstract: A class of pyrazolyl benzenesulfonamide compounds is described for use in treating inflammation and inflammation-related disorders.
    Type: Grant
    Filed: April 6, 1994
    Date of Patent: May 28, 1996
    Assignee: G.D. Searle & Co.
    Inventor: Matthew J. Graneto
  • Patent number: 5516907
    Abstract: A class of pyrazolyl benzenesulfonamido 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: June 1, 1995
    Date of Patent: May 14, 1996
    Assignee: G.D. Searle & Co.
    Inventors: John J. Talley, Donald J. Rogier, Jr.
  • Patent number: 5510496
    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## wherein R.sup.1 is selected from sulfamyl, fluoro, chloro, methyl, hydroxyl, methoxy and trifluoromethyl: wherein R.sup.2 is selected from hydrido, difiuoromethyl, trifluoromethyl, amido, dichloromethyl, trichloromethyl, pentafluoroethyl, cyano, heptatluoropropyl, difluorochloromethyl, methoxycarbonyl, dichlorofluoromethyl, N-phenylamido, N-3-fluorophenyl) amido, 2-pyridylamido, N-(4-methylphenyl)amido, hydroxypropyl, N-(3-chlorophenyl)amido, N-(4-methoxyphenyl)amido, hydroxymethyl, hydroxyethyl, carboxylpropyl, carboxymethyl and carboxyethyl; wherein R.sup.3 is selected from hydrido, methyl, triflouromethyl, fluoro, chloro and bromo; wherein R.sup.4 is selected from phenyl, biphenyl, pyrazinyl, cyclohexyl, cyclohexenyl and thienyl; and wherein R.sup.
    Type: Grant
    Filed: June 1, 1995
    Date of Patent: April 23, 1996
    Assignee: G.D. Searle & Co.
    Inventors: John J. Talley, Thomas D. Penning, Paul W. Collins, James W. Malecha, Stephen R. Bertenshaw, Matthew J. Graneto
  • Patent number: 5508426
    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: June 1, 1995
    Date of Patent: April 16, 1996
    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
  • Patent number: 5506115
    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. Compounds of particular interest are defined by Formula II ##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-aminonicotinic 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: April 29, 1994
    Date of Patent: April 9, 1996
    Assignee: G. D. Searle & Co.
    Inventors: Mihaly V. Toth, Arthur J. Wittwer, Barry C. Holwerda