Abstract: Compounds of the pregnane series are described having general formula (I) or their solvates in which R.sub.1 individually represents --OC(.dbd.O)C.sub.1-6 alkyl; R.sub.2 individually represents hydrogen, methyl (which may be in the .alpha. or .beta. configuration) or methylene; or R.sub.1 and R.sub.2 together represent formula (a) where R.sub.5 and R.sub.6 are the same or different and each represents hydrogen or C.sub.1-6 alkyl; R.sub.3 and R.sub.4 are the same or different and each represents hydrogen or halogen; and represents a single or a double bond. Compounds of formula (I) and their solvates are useful as anti-inflammatory or anti-allergic agents.
Abstract: The present invention relates to pharmaceutical formulations containing (2R, cis)-4-amino-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-(1H)-pyrimidin-2 -one (-)-2',3'-dideoxy,3'-thiacytidine, lamivudine, that are substantially free of ethanol and ethylenediamine-tetraacitic acid, and their use in medical therapy.
Type:
Grant
Filed:
March 20, 1998
Date of Patent:
December 21, 1999
Assignee:
Glaxo Wellcome Inc.
Inventors:
Warren Michael Casey, Ngoc-Anh Thi Nguyen
Abstract: The present invention relates to compounds of formula (I), wherein carbons 1 and 2 are joined by either a single or a double bond; R.sup.1 is hydrogen or methyl; R.sup.2 is hydrogen or methyl; R.sup.3 is (B) wherein X, R.sup.6, R.sup.7 and R.sup.8 are various groups, and pharmaceutically acceptable solvates thereof and their use in the treatment of androgen responsive and mediated diseases.
Type:
Grant
Filed:
May 14, 1998
Date of Patent:
December 7, 1999
Assignee:
Glaxo Wellcome Inc.
Inventors:
Kenneth William Batchelor, Stephen Vernon Frye
Abstract: The present invention relates to benzimidazole derivatives of formula (I) wherein: R.sup.1 represents H, C.sub.1-4 alkyl, C.sub.3-5 cycloalkyl; R.sup.2 represents H, C.sub.1-4 alkyl; or R.sup.1 and R.sup.2 together form with the nitrogen a 4 or 5 membered heterocyclic ring; R.sup.3 represents BR.sup.4 or R.sup.4 wherein B represents a bridging group --C(O)NH--, --C(O)NC.sub.1-4 alkyl-, or C(O)O-- and R.sup.4 represents H, C.sub.1-4 alkyl, C.sub.2-6 alkenyl or halo (preferably fluoro); and each n is an integer independently selected from 0, 1, or 2 (preferably 0 or 1); and geometric isomers or mixtures thereof; and physiologically functional derivatives thereof, and their use in medical therapy particularly for the treatment or prophylaxis of virus infections such as those caused by herpes viruses. The invention also relates to their preparation and pharmaceutical formulations containing them.
Type:
Grant
Filed:
July 1, 1998
Date of Patent:
December 7, 1999
Assignee:
Glaxo Wellcome Inc.
Inventors:
Susan Mary Daluge, Marc Werner Andersen
Abstract: The present invention relates to benzimidazole derivatives and their use in medical therapy particularly for the treatment or prophylaxis of virus infections such as those caused by herpes viruses. The invention also relates to the preparation of the benzimidazole derivatives and pharmaceutical formulations containing them.
Type:
Grant
Filed:
December 18, 1998
Date of Patent:
December 7, 1999
Assignee:
Glaxo Wellcome Inc.
Inventors:
Stanley Dawes Chamberlain, Susan Mary Daluge, George Walter Koszalka
Abstract: The invention is concerned with novel hypolipidemic compounds of formula (I), with processes and novel intermediates for their preparation, pharmaceutical compositions containing them and with their use in medicine, particularly in the prophylaxis and treatment of hyperlipidemic conditions, and associated diseases such as atherosclerosis.
Type:
Grant
Filed:
May 1, 1997
Date of Patent:
December 7, 1999
Assignee:
Glaxo Wellcome Inc.
Inventors:
Lawrence Edward Brieaddy, Anthony Louis Handlon, Gordon Lewis Hodgson, Jr.
Abstract: This invention relates to novel adenosine derivatives, to processes for their preparation, to pharmaceutical compositions containing them and to their use in medicine. Thus the invention provides compounds of formula (I) which are agonists at the adenosine A1 receptor. ##STR1## wherein R.sup.1 represents phenyl optionally substituted by one or more substituents selected from halogen, C.sub.1-3 alkyl, trifluoromethyl, nitro, cyano, --CO.sub.2 R.sup.a.sub.1 --CONR.sup.a R.sup.b, --COR.sup.a, --SOR.sup.c, --SO.sub.2 R.sup.c, --SO.sub.3 H, --SO.sub.2 NR.sup.a R.sup.b, --OR.sup.a, --NHSO.sub.2 R.sup.c, --NHCOR.sup.a and --NR.sup.a R.sup.b,R.sup.2 represents a C.sub.1-6 alkyl or C.sub.3-6 alkenyl group; R.sup.3 represents C.sub.1-3 alkyl;R.sup.a and R.sup.b may each independently represent hydrogen or C.sub.1-3 alkyl or, when --NR.sup.a R.sup.b is directly attached to said phenyl, R.sup.a and R.sup.
Type:
Grant
Filed:
November 6, 1998
Date of Patent:
December 7, 1999
Assignee:
Glaxo Wellcome Inc.
Inventors:
Frank Ellis, Stephen Swanson, Richard Peter Charles, Brian Cox, Andrew Michael Kenneth Pennell, Colin David Eldred
Abstract: The invention relates to combinations of atovaquone and proguanil, their use in the treatment and propinylaxis of parasitic infections, such as protozoal parasitic infections, e.g. malaria and toxoplasmosis, and infections caused by P.carinii and their use in the manunfacture of medicaments for the treatment and/or prophylaxis of such infections. The combinations can conveniently be administered in a single pharmaceutical formulation. Preferably, atovaquone and proguanil are administered in a potentiating ratio so that they act in synergy.
Type:
Grant
Filed:
October 31, 1997
Date of Patent:
December 7, 1999
Assignee:
Glaxo Wellcome Inc.
Inventors:
Winston Edward Gutteridge, David Brian Ashton Hutchinson, Victoria Susan Latter, Mary Pudney
Abstract: The present invention provides radiolabeled 5-{4-[2-(Methyl-pyridine-2-yl-amino)-ethoxy]-benzyl}-thiazolidine-2,4-dion e. In another aspect, the present invention provides a method for determining whether a compound does or does not interact directly with PPAR-gamma, comprising the step of specifically binding a radiolabeled compound of this invention to the ligand binding domain of PPAR-gamma.
Type:
Grant
Filed:
December 9, 1998
Date of Patent:
November 30, 1999
Assignee:
Glaxo Wellcome Inc.
Inventors:
Steven Anthony Kliewer, Jurgen M. Lehmann, Timothy M. Willson
Abstract: There are described according to the invention compounds of formula (I) (relative stereochemistry indicated), wherein R.sub.1, R.sub.2, R.sub.3 and X are as defined in the specification, together with processes for preparing them, compositions containing them and their use as pharmaceuticals. Compounds of formula (I) are indicated inter alia for the treatment of chronic bronchitis.
Type:
Grant
Filed:
September 25, 1998
Date of Patent:
November 30, 1999
Assignee:
Glaxo Wellcome Inc.
Inventors:
Michael Dennis Dowle, Harry Finch, Lee Andrew Harrison, Graham George Inglis, Martin Redpath Johnson, Simon John Fawcett Macdonald, Pritom Shah, Robin Andrew Smith
Abstract: The invention thus provides compounds of Formula (I) ##STR1## wherein R.sup.1 and R.sup.2 which may be the same or different represent H, C.sub.1-6 alkyl or substituted alkyl or C.sub.3-7 cycloalkyl; or aryl;R.sup.3, and R.sup.4 which may be the same or different represent H, halogen, C.sub.1-6 alkyl; or substituted aryl;R.sup.5 is H or C.sub.1-6 alkyl;n is an integer 0, 1 or 2and m is an integer 1, 2, 3, or 4;the dotted line indicates the presence or absence of an additional bond; and pharmaceutically acceptable solvates (e.g. hydrates) thereof.
Type:
Grant
Filed:
November 6, 1998
Date of Patent:
November 9, 1999
Assignee:
Glaxo Wellcome Inc.
Inventors:
Frank Ellis, Terence Aaron Panchal, Peter Charles North, Jason William Beames Cooke, Simon Charles Dolan
Abstract: Attenuated microorganism for use in immunoprophylaxis in which the attenuation is brought about by the presence of a mutation in the DNA sequence of the microorganism which encodes, or which regulates the expression of DNA encoding a protein that is produced in response to environmental stress, the microorganism optionally being capable of expressing DNA encoding a heterologous antigen.
Type:
Grant
Filed:
June 5, 1995
Date of Patent:
November 9, 1999
Assignee:
Glaxo Wellcome Inc.
Inventors:
Gordan Dougan, Ian George Charles, Carlos Estenio Hormaeche, Kevin Stuart Johnson, Steven Neville Chatfield
Abstract: The present invention relates to methods for preparing and using compounds of formula (I), wherein carbons 1 and 2 are joined by either a single or a double bond; R.sup.1 is hydrogen or methyl; R.sup.2 is hydrogen or methyl; R.sup.3 is (A) wherein X, W, Z, R.sup.4, and R.sup.5, are various groups, and pharmaceutically acceptable solvates thereof and their use in the treatment of androgen responsive and mediated diseases.
Type:
Grant
Filed:
May 14, 1998
Date of Patent:
November 2, 1999
Assignee:
Glaxo Wellcome Inc.
Inventors:
Kenneth William Batchelor, Stephen Vernon Frye
Abstract: A process and apparatus for freeze drying of liquid material in a vessel in which the vessels are moved automatically through various stages including loading vessels onto racks, washing vessels in an inverted position, sterilizing vessels and racks, filling vessels with a liquid material, rotating the vessels and the liquid material contained within each vessel at a speed that allows the liquid to form a shell against the inner surface of the vessel, subjecting the vessels and the liquid material contained therein to freezing conditions sufficient to freeze the material into the form of a shell and then moving the rack and the vessels containing the frozen material through a vacuum drying chamber in which the frozen liquid material is dried.
Type:
Grant
Filed:
November 17, 1997
Date of Patent:
October 12, 1999
Assignee:
Glaxo Wellcome Inc.
Inventors:
Dominic M. A. Oughton, Philip R. J. Smith, Donald B. A. MacMichael
Abstract: The present invention relates to the use of 4-(2-formyl-3-hydroxyphenoxymethyl) benzoic acid or physiologically acceptable salts thereof as an immunopotentiatory agent, compositions containing such a compound and their manufacture, combinations of such a compound with anti-tumour or anti-infective drugs and the use of such combinations in the prophylaxis or treatment of such diseases arising from tumours or infections.
Abstract: A exit chute for a pharmaceutical tablet press machine comprising a first exit chute portion having a first end and a second end wherein the first end is adapted to be secured to the tablet press for receiving tablets formed thereby. A second exit chute portion is provided that has a first end and a second end and the first end is adapted to be removably secured to the second end of the first exit chute portion to form an extended tablet pathway, and the second chute portion includes an aperture therein whereby rejected tablets can be diverted to pass therethrough and accepted tablets will be allowed to pass through the second exit chute portion and out of the second end thereof.
Type:
Grant
Filed:
February 12, 1997
Date of Patent:
September 28, 1999
Assignee:
Glaxo Wellcome Inc.
Inventors:
Herbert Dale Coble, Robin Cary Maples, Ross Vincent Martin, Jr.
Abstract: The invention relates to a freeze-dried dosage form for oral administration capable of being rapidly disintegrated in the mouth comprising ondansetron in the form of its free base or a pharmaceutically acceptable solvate thereof and one or more pharmaceutically acceptable excipients. Methods for the manufacture of such compositions and for their use in the treatment of conditions mediated through the action of 5-hydroxytryptamine (5HT) at 5HT.sub.3 receptors are also described.
Abstract: A lyophilized formulation of lamotrigine having been prepared by lyophilizing a frozen sterile aqueous solution of Imotrigine mesylate in which the pH is from 2.4 to 4.
Abstract: Described are peptides and peptide mimetics that bind to and activate the thrombopoietin receptor. Such peptides and peptide mimetics are useful in methods for treating hematological disorders and particularly, thrombocytopenia resulting from chemotherapy, radiation therapy, or bone marrow transfusions as well as in diagnostic methods employing labeled peptides and peptide mimetics.
Type:
Grant
Filed:
October 4, 1996
Date of Patent:
August 3, 1999
Assignee:
Glaxo Wellcome Inc.
Inventors:
Ronald W. Barrett, William J. Dower, Steven E. Cwirla, Sherril S. Johnson, Nicholas C. Wrighton, David J. Duffin, Christopher R. Wagstrom