Patents Represented by Attorney Robert T. Hrubiec
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Patent number: 5859240Abstract: 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: GrantFiled: August 28, 1997Date of Patent: January 12, 1999Assignee: Glaxo Wellcome Inc.Inventor: Lawrence Edward Brieaddy
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Patent number: 5843917Abstract: 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: GrantFiled: May 2, 1996Date of Patent: December 1, 1998Assignee: Glaxo Wellcome Inc.Inventors: Frank Leslie Boyd, Thomas Anthony Krenitsky
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Patent number: 5821236Abstract: 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: GrantFiled: May 24, 1995Date of Patent: October 13, 1998Assignee: Glaxo Wellcome Inc.Inventors: Thomas Anthony Krenitsky, Devron Randolph Averett, George Walter Koszalka
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Patent number: 5817664Abstract: 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: GrantFiled: June 6, 1995Date of Patent: October 6, 1998Assignee: Glaxo Wellcome Inc.Inventors: Thomas Spector, David J. T. Porter, Saad G. Rahim
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Patent number: 5817652Abstract: 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: GrantFiled: August 15, 1995Date of Patent: October 6, 1998Assignee: Glaxo Wellcome Inc.Inventors: Lawrence Edward Brieaddy, Gordon Lewis Hodgson, Jr.
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Patent number: 5733915Abstract: 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: GrantFiled: March 30, 1995Date of Patent: March 31, 1998Assignee: Glaxo Wellcome Inc.Inventor: William J. Sandborn
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Patent number: 5723458Abstract: 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: GrantFiled: August 15, 1995Date of Patent: March 3, 1998Assignee: Glaxo Wellcome Inc.Inventors: Lawrence Edward Brieaddy, Gordon Lewis Hodgson, Jr.
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Patent number: 5719186Abstract: 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: GrantFiled: November 8, 1996Date of Patent: February 17, 1998Assignee: Glaxo Wellcome Inc.Inventors: Barrett Randoph Cooper, James Leroy Kelley, David Lee Musso, Jeffrey Leaman Selph
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Patent number: 5708033Abstract: 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: GrantFiled: November 8, 1996Date of Patent: January 13, 1998Assignee: Glaxo Wellcome Inc.Inventors: James Leroy Kelley, David Lee Musso
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Patent number: 5670482Abstract: The present invention relates to peptides which show improved Neuropeptide Y antagonism to pharmaceutical compositions containing such peptides and their use.Type: GrantFiled: February 17, 1995Date of Patent: September 23, 1997Assignee: Glaxo Wellcome Inc.Inventors: Alejandro Jose Daniels, Dennis Heyer, Antonio Landavazo, Johann Jakob Leban, Andreas Spaltenstein
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Patent number: 5663165Abstract: 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: GrantFiled: December 5, 1994Date of Patent: September 2, 1997Assignee: Glaxo Wellcome Inc.Inventor: Lawrence Edward Brieaddy
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Patent number: 5661155Abstract: The present invention relates to bezoquinazoline thymidylate synthase inhibitors, to pharmaceutical formulations containing them and to their use in medicine.Type: GrantFiled: May 26, 1995Date of Patent: August 26, 1997Assignee: Glaxo Wellcome Inc.Inventors: William Pendergast, Scott Howard Dickerson
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Patent number: 5643913Abstract: Pharmaceutical compositions containing 5-substituted uracil compounds are disclosed. The compositions are preferably in the form of a tablet or capsule.Type: GrantFiled: November 9, 1994Date of Patent: July 1, 1997Assignee: Glaxo Wellcome Inc.Inventors: Thomas Spector, David J. T. Porter, Saad George Rahim
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Patent number: 5620959Abstract: 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: GrantFiled: November 23, 1994Date of Patent: April 15, 1997Assignee: Glaxo Wellcome Inc.Inventors: Johann J. Leban, Frederick C. Kull
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Patent number: 5405851Abstract: The present invention relates to novel benzoquinazoline thymidylate synthase inhibitors, to pharmaceutical formulations containing them and to their use in medicine.Type: GrantFiled: April 16, 1992Date of Patent: April 11, 1995Assignee: Burroughs Wellcome Co.Inventors: William Pendergast, Scott H. Dickerson, Julius V. Johnson, Robert Ferone
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Patent number: 5240937Abstract: 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: GrantFiled: May 1, 1992Date of Patent: August 31, 1993Assignee: Burroughs Wellcome Co.Inventor: James L. Kelley
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Patent number: 5234953Abstract: 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: GrantFiled: May 23, 1991Date of Patent: August 10, 1993Assignee: Burroughs Wellcome Co.Inventors: James W. Crow, Walker A. Long