Patents Represented by Attorney, Agent or Law Firm Charles T. Joyner
  • Patent number: 5302589
    Abstract: The present invention relates to certain substituted 17 .beta.-substituted carbonyl-6-azaandrost-4-en-3-ones of formula (I): ##STR1## wherein R.sup.1 and R.sup.2 arei) independently hydrogen or lower alkyl and the bond between the carbons bearing R.sup.1 and R.sup.2 is a single or a double bond, orii) taken together are a --CH.sub.2 -- group to form a cyclopropane ring, and the bond between the carbons bearing R.sup.1 and R.sup.2 is a single bond;X is ##STR2## wherein R.sup.5, R.sup.6, R.sup.7 and R.sup.8 are independently hydrogen or lower alkyl,p and q are independently either 0 or 1;R.sup.3 is lower alkyl, lower alkenyl, lower cycloalkyl, lower alkoxy, thiopyridyl, adamantyl, --NR.sup.9 R.sup.10 or --Ar--NR.sup.9 R.sup.10whereinR.sup.9 and R.sup.
    Type: Grant
    Filed: August 7, 1992
    Date of Patent: April 12, 1994
    Assignee: Glaxo, Inc.
    Inventors: Stephen V. Frye, David Middlemiss, Francis G. Fang
  • Patent number: 5261538
    Abstract: The present invention comprises a method for measuring the amount, i.e., mass, of a volatile liquid which comprises passing the mass over a heat loss measuring device, calculating the amount of heat loss accompanying the vaporization of the mass and correlating the heat loss to measurement of heat loss of known liquid aerosol mass made with the same device.
    Type: Grant
    Filed: April 21, 1992
    Date of Patent: November 16, 1993
    Assignee: Glaxo Inc.
    Inventors: Rix E. Evans, Alec P. Flowers, Jr., David E. Hockaday, David W. Loar, James K. Proctor
  • Patent number: 5258519
    Abstract: Compounds of the following formula (I): ##STR1## where R.sup.1 and R.sup.2 are alkyl or cycloalkyl, which may be substituted, R.sup.4 is aryl such as phenyl which may be substituted, L is a direct bond or an oxygen containing linking group, R is a hydrogen, alkyloxy, alkyl, halogen or haloalkyl and Het is a pyridinyl or pyridazinyl group. The compounds can be used antihypertensives or myocardial relaxants. Also part of the invention are pharmaceutical compositions, intermediates and methods of synthesis.
    Type: Grant
    Filed: December 10, 1991
    Date of Patent: November 2, 1993
    Assignee: Glaxo Inc.
    Inventors: Thomas N. Wheeler, Terrence P. Kenakin
  • Patent number: 5241069
    Abstract: This invention relates to the new process for preparing the 1R-cis isomer of carbovir, (1R-cis)-amino-1,9-dihydro-9-[4-(hydroxymethyl)-2-cyclopenten-1-yl]-6H-pur in-6-one, an antiviral agent and intermediates of the formula (Vlb) use in that process ##STR1## wherein X is chloro, bromo or iodo and R is (C.sub.1-6) alkyl.
    Type: Grant
    Filed: November 6, 1991
    Date of Patent: August 31, 1993
    Assignees: Glaxo Inc., Univeristy of Minnesoota
    Inventors: Robert Vince, Mark L. Peterson, John W. Lackey, Robert A. Mook, Jr., John J. Partridge
  • Patent number: 5223506
    Abstract: The present invention relates to certain substituted tetracyclic fused quinoline derivatives of formula (I): ##STR1## wherein: R.sup.1 is hydrogen, hydroxy, fluoro, chloro, bromo, iodo, methoxy or amino;R.sup.2 is hydrogen, hydroxy, methoxy or amino;R.sup.3 is hydrogen, hydroxy, methoxy, methoxymethoxy, amino, --OCONH.sub.2, [2(5H)-3,4-dihydro-3-oxyfuranone], 2-hydroxyethoxy, 2-aminoethoxy, 3-hydroxypropoxy or 3-aminopropoxy; or taken together with R.sup.2 or R.sup.4, methylenedioxy or ethylenedioxy;R.sup.4 is hydrogen, hydroxy or amino;Z is --CH.sub.2 --, --O-- or --NH--; anda) X.sup.1 is hydrogen; X.sup.2 is hydrogen, hydroxy, fluoro, chloro, bromo, iodo or methoxy; and X.sup.3 is hydrogen or hydroxy; orb) X.sup.2 taken together with X.sup.3 is methylenedioxy or ethylenedioxy, and X.sup.1 is hydrogenor a pharmaceutically acceptable salt thereof provided that:i) at least one of R.sup.1 through R.sup.4 is other than hydrogen;ii) when R.sup.1 is methoxy, R.sup.2 is hydroxy or methoxy, R.sup.
    Type: Grant
    Filed: June 4, 1991
    Date of Patent: June 29, 1993
    Assignee: Glaxo Inc.
    Inventors: Michael J. Luzzio, Jeffrey M. Besterman, Michael G. Evans, M. Ross Johnson, Milana Dezube, Salvatore Profeta, Jr.
  • Patent number: 5204463
    Abstract: Pyridazinones of the following formula (I): ##STR1## where R.sup.1 -R.sup.4 are a variety of substituents and L is a linking group, a pharmaceutical composition for treating congestive heart failure, novel intermediates, methods for such treatment and processes for preparing compounds of formula (I).
    Type: Grant
    Filed: September 4, 1991
    Date of Patent: April 20, 1993
    Assignee: Glaxo Inc.
    Inventors: Thomas N. Wheeler, Terrence P. Kenakin, Joel E. Shaffer
  • Patent number: 5192757
    Abstract: Cobalt prophyrins of the following formula (l): ##STR1## or a salt or ligand complex thereof and their synthesis, pharmaceutical compositions and use in controlling obesity.
    Type: Grant
    Filed: December 20, 1990
    Date of Patent: March 9, 1993
    Assignee: Glaxo Inc.
    Inventors: Michael R. Johnson, Stephen V. Frye
  • Patent number: 5187368
    Abstract: A method for detecting the presence or absence of microorganisms in a liquid test sample is provided without need for withdrawing an aliquot or destroying the sample. The method comprises taking near-infrared spectra of the sample and comparing it visually or mathematically to the spectra of a standard, which may be the values of the spectra known to the operator or may be a standard sample that is provided and run side-by-side.
    Type: Grant
    Filed: September 12, 1990
    Date of Patent: February 16, 1993
    Assignees: Glaxo Inc., The University of Kentucky
    Inventors: Leonard J. Galante, Robert A. Lodder
  • Patent number: 5187305
    Abstract: The present invention relates to the compounds of formula (I), ##STR1## wherein R.sup.1 is C.sub.1-8 alkyl; C.sub.5-8 cycloalkyl;--(CH.sub.2).sub.n --Si(CH.sub.3).sub.3, wherein n is 1 to 5; C.sub.2-5 alkylenyl; arylmethylene; aryl; heteroaryl; or wherein such aryl or heteoaryl bears 1 to 3 substituents independently selected from halogen, amino, C.sub.1-8 alkyl mono- or disubstituted amino, C.sub.1-8 alkyl and C.sub.1-8 alkoxy and R.sup.2 is C.sub.1-8 alkoxy, pharmaceutical formulations containing these compounds and their use as vasodilators and in the treatment of cardiovascular disorders.
    Type: Grant
    Filed: November 26, 1990
    Date of Patent: February 16, 1993
    Assignee: Glaxo Inc.
    Inventors: Stephen A. Thompson, Joel E. Shaffer
  • Patent number: 5153209
    Abstract: Pyridones of formula (I) for treating congestive heart failure: ##STR1## wherein: R.sup.1 and R.sup.2 are a variety of phenyl substituents, L is a divalent alkylene linking group. Pharmaceutical composition, methods for their use in treating cardiovascular conditions, processes used in synthesis and intermediates used in such processes.
    Type: Grant
    Filed: June 13, 1991
    Date of Patent: October 6, 1992
    Assignee: Glaxo Inc.
    Inventors: Thomas N. Wheeler, Terrence P. Kenakin, Joel E. Shaffer
  • Patent number: 5149697
    Abstract: Pharmaceutical compositions containing cobalt porphyrins of the following formula (I): ##STR1## wherein R.sup.1 =--CH.sub.2 CH.sub.2 CN and R.sup.2 =--CH.sub.2 CH.sub.2 COOH or R.sup.1 and R.sup.2 =--CH.sub.2 CH.sub.2 COOH or R.sup.1 =--H and R.sup.2 =--CH.sub.2 lCH.sub.2 COOH or a salt or ligand complex thereof and their use in controlling obesity.
    Type: Grant
    Filed: April 18, 1991
    Date of Patent: September 22, 1992
    Assignee: Glaxo Inc.
    Inventors: Michael R. Johnson, Stephen V. Frye
  • Patent number: 5144034
    Abstract: This invention relates to a new process for preparing certain optically active cyclopentene derivatives and novel intermediates used in this process. In particular, the invention concerns the synthesis of the 1'R-cis isomer of carbovir, (1'R-cis)-2-amino-1,9-dihydro-9[4-(hydroxymethyl)-2-cyclopenten-1-yl]-6H-p urin-6-one, an antiviral agent.
    Type: Grant
    Filed: April 6, 1990
    Date of Patent: September 1, 1992
    Assignee: Glaxo Inc.
    Inventors: M. Ross Johnson, Michael R. Peel, Daniel D. Sternbach
  • Patent number: 5126452
    Abstract: This invention relates to new process for preparing certain optically active purine substituted cyclopentene derivatives and novel intermediates used in this process. In particular, the invention concerns the synthesis of the 1R-cis isomer of carbovir, (1R-cis)-amino-1,9-dihydro-9-[4-(hydroxymethyl)-2-cyclopenten-1-yl]-6H-pur in-6-one, an antiviral agent, and certain intermediates.
    Type: Grant
    Filed: April 6, 1990
    Date of Patent: June 30, 1992
    Assignee: Glaxo Inc.
    Inventors: Robert Vince, Mark L. Peterson, John W. Lackey, Robert A. Mook, Jr., John J. Partridge
  • Patent number: 5126123
    Abstract: This invention relates to aerosol inhalation drug formulations comprising one or more drugs and one or more soluble surfactants in propellant 134a.
    Type: Grant
    Filed: February 1, 1991
    Date of Patent: June 30, 1992
    Assignee: Glaxo, Inc.
    Inventor: Keith A. Johnson
  • Patent number: 5126351
    Abstract: The present invention relates to the compounds of formula (I), ##STR1## wherein: R.sup.1 is hydrogen, hydroxy or amino;R.sup.2 is hydrogen, hydroxy, methoxy or methoxymethoxy;R.sup.3 is hydrogen, hydroxy, amino, methoxy, methoxymethyoxy, or taken together with R.sup.2, methylenedioxy (also known as 1,3-dioxolo);R.sup.4 is hydrogen, hydroxy, methoxy, methoxymethoxy, benzyl, di(C.sub.1-4)alkylaminomethyl or, taken together with R.sup.3, methylenedioxy;R.sup.5 is hydrogen or hydroxy; provided that at least one of R.sup.1 through R.sup.5 is other than hydrogen; andi) X.sup.2 is hydroxy or methoxy with X.sup.1, X.sup.3 and X.sup.4 being hydrogen; orii) X.sup.1 taken together with X.sup.2,X.sup.2 taken together with X.sup.3 or X.sup.3 taken together with X.sup.4, is methylenedioxy, provided that each of the remaining respective X.sup.1, X.sup.2, X.sup.3 and X.sup.
    Type: Grant
    Filed: January 24, 1991
    Date of Patent: June 30, 1992
    Assignee: Glaxo Inc.
    Inventors: Michael J. Luzzio, Jeffrey M. Besterman, Michael G. Evans, M. Ross Johnson
  • Patent number: 5100892
    Abstract: Compounds of the following formula (I): ##STR1## where R.sup.1 and R.sup.2 are alkyl or cycloalkyl, which may be substituted, R.sup.4 is aryl such as phenyl which may be substituted, L is a direct bond or an oxygen containing linking group, R is a hydrogen, alkyloxy, alkyl, halogen or haloalkyl and Het is a pyridinyl or pyridazinyl group. The compounds can be used antihypertensives or myocardial relaxants. Also part of the invention are pharmaceutical compositions, intermediates and methods of synthesis.
    Type: Grant
    Filed: November 13, 1990
    Date of Patent: March 31, 1992
    Assignee: Glaxo Inc.
    Inventors: Thomas N. Wheeler, Terrence P. Kenakin
  • Patent number: 5096904
    Abstract: Pyridazinones of the following formula (I): ##STR1## where R.sup.1 -R.sup.4 are a variety of substituents and L is a linking group, a pharmaceutical composition for treating congestive heart failure, novel intermediates, methods for such treatment and processes for preparing compounds of formula (I).
    Type: Grant
    Filed: July 20, 1990
    Date of Patent: March 17, 1992
    Assignee: Glaxo Inc.
    Inventors: Thomas N. Wheeler, Terrence P. Kenakin, Joel E. Shaffer
  • Patent number: 5087631
    Abstract: The present invention relates to the compounds of formula (I). ##STR1## wherein R.sup.1 is C.sub.1-8 alkyl, C.sub.2-8 alkenyl, C.sub.5-8 cycloalkyl, aryl-C.sub.1-4 alkyl, aryl or heteroaryl; or aryl or heteroaryl which is mono-, di-, or trisubstituted independently with halogen, nitro, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, trifluoromethyl, amino or C.sub.1-4 alkyl mono or disubstituted amino, pharmaceutical formulations containing these compounds and their use as vasodilators in the treatment of cardiovascular disorders.
    Type: Grant
    Filed: December 18, 1990
    Date of Patent: February 11, 1992
    Assignee: Glaxo Inc.
    Inventors: Joel E. Shaffer, Stephen A. Thomson
  • Patent number: 5057630
    Abstract: This invention relates to a new process for preparing certain optically active purine substituted cyclopentene derivatives including the antiviral agent, carbovir, and novel intermediates used in this process. In particular, this invention concerns a synthesis of (1R-cis)-4-hydroxymethyl-2-cyclopenten-1-ol, an intermediate in this process.
    Type: Grant
    Filed: April 6, 1990
    Date of Patent: October 15, 1991
    Assignee: Glaxo Inc.
    Inventors: John W. Lackey, Robert A. Mook, Jr., John J. Partridge