Patents Represented by Attorney Robert T. Hrubiec
  • Patent number: 5859240
    Abstract: The present invention is concerned with processes for preparing hypolipidaemic benzothiazepine compounds of formula (I) ##STR1## wherein l is an integer of from 0 to 4; m is an integer of from 0 to 5; n is an integer of from 0 to 2; R and R' are atoms or groups independently selected from halogen, nitro, phenylalkoxy, C.sub.1-4 alkoxy, C.sub.1-6 alkyl and --O(CH.sub.2).sub.p SO.sub.3 R" wherein p is an integer of from 1 to 4 and R" is hydrogen or C.sub.1-6 alkyl, wherein said phenylalkoxy, alkoxy and alkyl groups are optionally substituted by one or more halogen atoms; R.sup.4 is C.sub.1-6 straight alkyl group; and R.sup.5 is a C.sub.2-6 straight alkyl group; and their salts, solvates and physiologically functional derivatives; and intermediates useful in said processes.
    Type: Grant
    Filed: August 28, 1997
    Date of Patent: January 12, 1999
    Assignee: Glaxo Wellcome Inc.
    Inventor: Lawrence Edward Brieaddy
  • Patent number: 5843917
    Abstract: Novel compounds comprising 5-fluorouracil or 5-fluorouridine covalently linked to 5-ethynyluracil, 5-ethynyluridine or 5-propynyluracil and pharmaceutical compositions comprising such compounds are disclosed.
    Type: Grant
    Filed: May 2, 1996
    Date of Patent: December 1, 1998
    Assignee: Glaxo Wellcome Inc.
    Inventors: Frank Leslie Boyd, Thomas Anthony Krenitsky
  • Patent number: 5821236
    Abstract: 6-Alkoxy derivatives of Ara-G, and pharmaceutically acceptable esters thereof, are described as being useful in tumor therapy. Novel pharmaceutically acceptable esters, their preparation and pharmaceutical formulations containing them are also disclosed.
    Type: Grant
    Filed: May 24, 1995
    Date of Patent: October 13, 1998
    Assignee: Glaxo Wellcome Inc.
    Inventors: Thomas Anthony Krenitsky, Devron Randolph Averett, George Walter Koszalka
  • Patent number: 5817664
    Abstract: The present invention relates to a group of 5-substituted uracil derivatives which are inactivators of uracil reductase and which are particularily useful in cancer chemotherapy, especially in combination with antimetabolite antineoplastic agents such as 5-fluorouracil (5-FU).
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: October 6, 1998
    Assignee: Glaxo Wellcome Inc.
    Inventors: Thomas Spector, David J. T. Porter, Saad G. Rahim
  • Patent number: 5817652
    Abstract: The invention provides a compound of formula (I), wherein n is an integer of from 0 to 2; R is an optional substituent; R.sup.1 is hydrogen or C.sub.1-6 alkyl; R.sup.2 is an atom or group selected from hydrogen, C.sub.1-4 alkyl (including cycloalkyl and cycloalkylalkyl), C.sub.1-4 alkoxy, pyrryl, thienyl, pyridyl, 1,3-benzodioxolo, phenyl and naphthyl, which groups are optionally substituted; R.sup.3 is hydrogen, OH, C.sub.1-6 alkyl, C.sub.1-6 alkoxy or --O C.sub.1-6 acyl; R.sup.4 is a group independently selected from C.sub.1-6 alkyl (including cycloalkyl and cycloalkylalkyl), C.sub.2-6 alkenyl, and C.sub.2-6 -alkynyl which groups are optionally substituted; R.sup.5 is a group independently selected from C.sub.2-6 alkyl (including cycloalkyl and cycloalkylalkyl), C.sub.2-6 alkenyl and C.sub.2-6 alkynyl, which groups are optionally substituted; or R.sup.4 and R.sup.5, together with the carbon atom to which they are attached, form a C.sub.3-7 spiro cycloalkyl group which is optionally substituted; R.sup.
    Type: Grant
    Filed: August 15, 1995
    Date of Patent: October 6, 1998
    Assignee: Glaxo Wellcome Inc.
    Inventors: Lawrence Edward Brieaddy, Gordon Lewis Hodgson, Jr.
  • Patent number: 5733915
    Abstract: A therapeutic method for the treatment of Crohn's disease is provided, comprising administering to a patient in need of said treatment an intravenous dose of azathioprine or a pharmaceutically acceptable derivative thereof.
    Type: Grant
    Filed: March 30, 1995
    Date of Patent: March 31, 1998
    Assignee: Glaxo Wellcome Inc.
    Inventor: William J. Sandborn
  • Patent number: 5723458
    Abstract: The invention provides novel 1,4-benzothiazepine compounds substituted with hydroxy or a group containing hydroxy, compositions comprising such compounds and their use in the treatment or prophylaxis of treating clinical conditions in which inhibition of bile acid uptake is indicated, for example, hyperlipidemia and atherosclerosis.
    Type: Grant
    Filed: August 15, 1995
    Date of Patent: March 3, 1998
    Assignee: Glaxo Wellcome Inc.
    Inventors: Lawrence Edward Brieaddy, Gordon Lewis Hodgson, Jr.
  • Patent number: 5719186
    Abstract: Novel carbocyclic amides together with their salts, solvates and physiologically active derivatives which have a number of uses in medicine, in particular as central muscle relaxants, and in the treatment or prophylaxis of anxiety, inflammation, arthritis and pain.
    Type: Grant
    Filed: November 8, 1996
    Date of Patent: February 17, 1998
    Assignee: Glaxo Wellcome Inc.
    Inventors: Barrett Randoph Cooper, James Leroy Kelley, David Lee Musso, Jeffrey Leaman Selph
  • Patent number: 5708033
    Abstract: A compound of formula (I), wherein R.sup.1 and R.sup.2 are independently selected from chloro, fluoro, bromo, C.sub.1-6 alkyl, C.sub.1-6 alkoxy or C.sub.1-6 haloalkyl provided that both R.sup.1 and R.sup.2 are not fluoro; R.sup.3 and R.sup.4 are independently selected from hydrogen and C.sub.1-6 alkyl, and pharmaceutically acceptable salts, solvates or physiologically functional derivatives thereof, their use in medicine, particularly the phrophylaxis or treatment of conditions associated with inflammation, arthritis, or pain, pharmaceutical compositions comprising them, and processes for their preparation are disclosed.
    Type: Grant
    Filed: November 8, 1996
    Date of Patent: January 13, 1998
    Assignee: Glaxo Wellcome Inc.
    Inventors: James Leroy Kelley, David Lee Musso
  • Patent number: 5670482
    Abstract: The present invention relates to peptides which show improved Neuropeptide Y antagonism to pharmaceutical compositions containing such peptides and their use.
    Type: Grant
    Filed: February 17, 1995
    Date of Patent: September 23, 1997
    Assignee: Glaxo Wellcome Inc.
    Inventors: Alejandro Jose Daniels, Dennis Heyer, Antonio Landavazo, Johann Jakob Leban, Andreas Spaltenstein
  • Patent number: 5663165
    Abstract: The present invention is directed to the following compounds of formula (I): ##STR1## wherein l is an integer of from 0 to 4; m is an integer of from 0 to 5; n is an integer of from 0 to 2; R and R' are atoms or groups independently selected from halogen, nitro, phenylalkoxy, C.sub.1-4 alkoxy, C.sub.1-6 alkyl and --O(CH.sub.2).sub.p SO.sub.3 R" wherein p is an integer of from 1 to 4 and R" is hydrogen or C.sub.1-6 alkyl, wherein said phenylalkoxy, alkoxy and alkyl groups are optionally substituted by one or more halogen atoms; R.sup.4 is a C.sub.1-6 straight alkyl group; and R.sup.5 is a C.sub.2-6 straight alkyl group; and their salts, solvates and physiologically functional derivatives, with processes and novel intermediates for their preparation, with pharmaceutical compositions containing them and with their use in medicine, particularly in the prophylaxis and treatment of hyperlipidaemic conditions, such as atherosclerosis.
    Type: Grant
    Filed: December 5, 1994
    Date of Patent: September 2, 1997
    Assignee: Glaxo Wellcome Inc.
    Inventor: Lawrence Edward Brieaddy
  • Patent number: 5661155
    Abstract: The present invention relates to bezoquinazoline thymidylate synthase inhibitors, to pharmaceutical formulations containing them and to their use in medicine.
    Type: Grant
    Filed: May 26, 1995
    Date of Patent: August 26, 1997
    Assignee: Glaxo Wellcome Inc.
    Inventors: William Pendergast, Scott Howard Dickerson
  • Patent number: 5643913
    Abstract: Pharmaceutical compositions containing 5-substituted uracil compounds are disclosed. The compositions are preferably in the form of a tablet or capsule.
    Type: Grant
    Filed: November 9, 1994
    Date of Patent: July 1, 1997
    Assignee: Glaxo Wellcome Inc.
    Inventors: Thomas Spector, David J. T. Porter, Saad George Rahim
  • Patent number: 5620959
    Abstract: The present invention provides polypeptides of the formula XX.sup.1 TrpX.sup.2 X.sup.3 X.sup.4 X.sup.5 X.sup.6 X.sup.7 NH.sub.2, methods of treatment using the polypeptides, pharmaceutical compositions comprising such polypeptides, and processes for their preparation. The polypeptides possess antagonist properties against bombesin and bombesin-like peptides and are useful in the treatment of malignant disease. M, X, X.sup.1, X.sup.2, X.sup.3, X.sup.4, X.sup.5, X.sup.6, and X.sup.7 are as defined in the specification.
    Type: Grant
    Filed: November 23, 1994
    Date of Patent: April 15, 1997
    Assignee: Glaxo Wellcome Inc.
    Inventors: Johann J. Leban, Frederick C. Kull
  • Patent number: 5405851
    Abstract: The present invention relates to novel benzoquinazoline thymidylate synthase inhibitors, to pharmaceutical formulations containing them and to their use in medicine.
    Type: Grant
    Filed: April 16, 1992
    Date of Patent: April 11, 1995
    Assignee: Burroughs Wellcome Co.
    Inventors: William Pendergast, Scott H. Dickerson, Julius V. Johnson, Robert Ferone
  • Patent number: 5240937
    Abstract: This invention describes the preparation and use of anticonvulsant agents. In particular, triazolopyridine compounds are described which have utility in the treatment of epilepsy in mammals.
    Type: Grant
    Filed: May 1, 1992
    Date of Patent: August 31, 1993
    Assignee: Burroughs Wellcome Co.
    Inventor: James L. Kelley
  • Patent number: 5234953
    Abstract: The present invention is concerned with the use of a compound of formula (I) ##STR1## wherein --W-- is ##STR2## wherein Z is --V(CH.sub.2).sub.b CO.sub.2 H where b is 1 or 2 and V is oxygen when b is 1 or methylene when b is 2;X is hydrogen, cyano, or --C.tbd.CH; andthe dotted line represents an optional double bond;and physiologically functional derivatives thereof,in the treatment of congestive heart failure.
    Type: Grant
    Filed: May 23, 1991
    Date of Patent: August 10, 1993
    Assignee: Burroughs Wellcome Co.
    Inventors: James W. Crow, Walker A. Long