Patents Represented by Attorney, Agent or Law Firm Charles T. Joyner
-
Patent number: 5302589Abstract: 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: GrantFiled: August 7, 1992Date of Patent: April 12, 1994Assignee: Glaxo, Inc.Inventors: Stephen V. Frye, David Middlemiss, Francis G. Fang
-
Patent number: 5261538Abstract: 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: GrantFiled: April 21, 1992Date of Patent: November 16, 1993Assignee: Glaxo Inc.Inventors: Rix E. Evans, Alec P. Flowers, Jr., David E. Hockaday, David W. Loar, James K. Proctor
-
Patent number: 5258519Abstract: 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: GrantFiled: December 10, 1991Date of Patent: November 2, 1993Assignee: Glaxo Inc.Inventors: Thomas N. Wheeler, Terrence P. Kenakin
-
Patent number: 5241069Abstract: 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: GrantFiled: November 6, 1991Date of Patent: August 31, 1993Assignees: Glaxo Inc., Univeristy of MinnesootaInventors: Robert Vince, Mark L. Peterson, John W. Lackey, Robert A. Mook, Jr., John J. Partridge
-
Patent number: 5223506Abstract: 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: GrantFiled: June 4, 1991Date of Patent: June 29, 1993Assignee: Glaxo Inc.Inventors: Michael J. Luzzio, Jeffrey M. Besterman, Michael G. Evans, M. Ross Johnson, Milana Dezube, Salvatore Profeta, Jr.
-
Patent number: 5204463Abstract: 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: GrantFiled: September 4, 1991Date of Patent: April 20, 1993Assignee: Glaxo Inc.Inventors: Thomas N. Wheeler, Terrence P. Kenakin, Joel E. Shaffer
-
Patent number: 5192757Abstract: 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: GrantFiled: December 20, 1990Date of Patent: March 9, 1993Assignee: Glaxo Inc.Inventors: Michael R. Johnson, Stephen V. Frye
-
Patent number: 5187368Abstract: 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: GrantFiled: September 12, 1990Date of Patent: February 16, 1993Assignees: Glaxo Inc., The University of KentuckyInventors: Leonard J. Galante, Robert A. Lodder
-
Patent number: 5187305Abstract: 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: GrantFiled: November 26, 1990Date of Patent: February 16, 1993Assignee: Glaxo Inc.Inventors: Stephen A. Thompson, Joel E. Shaffer
-
Patent number: 5153209Abstract: 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: GrantFiled: June 13, 1991Date of Patent: October 6, 1992Assignee: Glaxo Inc.Inventors: Thomas N. Wheeler, Terrence P. Kenakin, Joel E. Shaffer
-
Patent number: 5149697Abstract: 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: GrantFiled: April 18, 1991Date of Patent: September 22, 1992Assignee: Glaxo Inc.Inventors: Michael R. Johnson, Stephen V. Frye
-
Patent number: 5144034Abstract: 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: GrantFiled: April 6, 1990Date of Patent: September 1, 1992Assignee: Glaxo Inc.Inventors: M. Ross Johnson, Michael R. Peel, Daniel D. Sternbach
-
Patent number: 5126452Abstract: 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: GrantFiled: April 6, 1990Date of Patent: June 30, 1992Assignee: Glaxo Inc.Inventors: Robert Vince, Mark L. Peterson, John W. Lackey, Robert A. Mook, Jr., John J. Partridge
-
Patent number: 5126123Abstract: This invention relates to aerosol inhalation drug formulations comprising one or more drugs and one or more soluble surfactants in propellant 134a.Type: GrantFiled: February 1, 1991Date of Patent: June 30, 1992Assignee: Glaxo, Inc.Inventor: Keith A. Johnson
-
Patent number: 5126351Abstract: 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: GrantFiled: January 24, 1991Date of Patent: June 30, 1992Assignee: Glaxo Inc.Inventors: Michael J. Luzzio, Jeffrey M. Besterman, Michael G. Evans, M. Ross Johnson
-
Patent number: 5100892Abstract: 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: GrantFiled: November 13, 1990Date of Patent: March 31, 1992Assignee: Glaxo Inc.Inventors: Thomas N. Wheeler, Terrence P. Kenakin
-
Patent number: 5096904Abstract: 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: GrantFiled: July 20, 1990Date of Patent: March 17, 1992Assignee: Glaxo Inc.Inventors: Thomas N. Wheeler, Terrence P. Kenakin, Joel E. Shaffer
-
Patent number: 5087631Abstract: 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: GrantFiled: December 18, 1990Date of Patent: February 11, 1992Assignee: Glaxo Inc.Inventors: Joel E. Shaffer, Stephen A. Thomson
-
Patent number: 5057630Abstract: 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: GrantFiled: April 6, 1990Date of Patent: October 15, 1991Assignee: Glaxo Inc.Inventors: John W. Lackey, Robert A. Mook, Jr., John J. Partridge