Patents Represented by Attorney, Agent or Law Firm Karen L. Prus
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Patent number: 8227428Abstract: The compound 3?-N-demethyl-4?-O-(2-diethylaminoethanoyl)-6-O-methyl-9a-aza-9a-homoerythromycin A, having the Formula (I): or a salt thereof, compositions comprising the compound, its use in the treatment of neutrophil dominated inflammatory diseases, and methods for its preparation.Type: GrantFiled: January 28, 2010Date of Patent: July 24, 2012Assignee: Glaxo Group LimitedInventors: Caroline Jane Day, Julien Bruno Douillet, Darko Filic, Leanda Jane Kindon, Goran Kragol, Zorica Marusic-Istuk
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Patent number: 8080529Abstract: The present invention relates to novel semi-synthetic macrolides having anti-inflammatory activity. More particularly, the invention relates to 14- and 15-membered macrolides substituted at the 4? position, to their pharmaceutically acceptable derivatives, to processes and intermediates for their preparation, to pharmaceutical compositions containing them and to their activity and use in the treatment of inflammatory diseases and conditions in humans and animals, especially those diseases associated with excessive secretion of TNF-?, IL-1, IL-8, IL-2 or IL-5; and/or inhibitor of excessive lymphocyte proliferation; and/or excessive granulocyte degranulation.Type: GrantFiled: January 13, 2006Date of Patent: December 20, 2011Assignee: Glaxo Group LimitedInventors: Sulejman Alihodzic, Martina Bosnar, Ognjen Culic, Vesna Erakovic Haber, Antun Hutinec, Dubravko Jelic, Goran Kragol, Nikola Marjanovic, Zorica Marusic-Istuk, Marija Ribic, Vanja Vela
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Patent number: 7989600Abstract: The present invention relates to new macrolide compounds represented by the general structure I, wherein M is a macrolide, P is a photo-affinity group bearing subunit containing biotin, and L is a linking molecule, and to their pharmaceutically acceptable salts and solvates, to processes and intermediates for their preparation and to the use of these compounds for the macrolide target identification.Type: GrantFiled: January 13, 2006Date of Patent: August 2, 2011Assignee: GlaxoSmithKline Istrazivacki Centar Zagreb D.O.O.Inventors: Ognjen Culic, Martina Bosnar, Nikola Marjanovic, Boris Mildner, Linda Tomaskovic, Sulejman Alihodzic
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Patent number: 7910559Abstract: The present invention relates to novel semi-synthetic macrolides having anti-inflammatory activity. More particularly, the invention relates to 14- and 15-membered macrolides lacking cladinose sugar substituted at the C-3 position, to their pharmaceutically acceptable derivatives, to processes and intermediates for their preparation, to pharmaceutical compositions containing them and to their activity and use in the treatment of inflammatory diseases and conditions in humans and animals, especially those diseases associated with excessive secretion of TNF-?, IL-1, IL-6, IL-8, IL-2 or IL-5; and/or inhibitor of excessive lymphocyte proliferation; and/or excessive granulocyte degranulation.Type: GrantFiled: January 13, 2006Date of Patent: March 22, 2011Assignee: GlaxoSmithKline istrazivacki centar Zagreb d.o.o.Inventors: Ognjen Culic, Martina Bosnar, Sulejman Alihodzic, Gorjana Lazarevski, Zorica Marusic Istuk, Antun Hutinec, Vanja Vela, Goran Kragol
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Patent number: 7812016Abstract: The present invention features compounds that are HIV integrase inhibitors and therefore are useful in the inhibition of HIV replication, the prevention and/or treatment of infection by HIV, and in the treatment of AIDS and/or ARC.Type: GrantFiled: May 12, 2004Date of Patent: October 12, 2010Assignee: SmithKline Beecham CorporationInventor: Brian A. Johns
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Patent number: 7622494Abstract: The present invention relates to compounds that are useful in the treatment of human papillomaviruses, and also to the methods for the making and use of such compounds.Type: GrantFiled: June 7, 2004Date of Patent: November 24, 2009Assignee: SmithKline Beecham CorporationInventors: Sharon Davis Boggs, John G Catalano, Kristjan S Gudmundsson, Leah D'Aurora Richardson, Paul Richard Sebahar
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Patent number: 7557209Abstract: The present invention relates to a process for preparing a chloropurine compound of formula (I)Type: GrantFiled: September 2, 2004Date of Patent: July 7, 2009Assignee: Glaxo Group LimitedInventor: Ronnie Maxwell Lawrence
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Patent number: 7435805Abstract: The present disclosure relates to new 11-O-alkyl macrolides and azalides and pharmaceutically acceptable salts and solvates thereof, and to pharmaceutical compositions thereof. The disclosure also relates to a process for the preparation of 11-O-alkyl macrolides and azalides by regioselective 11-O-alkylation of macrolides and azalides having a vicinal diol system, using diazoalkanes in the presence of transition-metal halides or boric acid as catalysts. In another aspect, the disclosure relates to uses of the 11-O-alkyl macrolides and azalides as antibacterial agents or intermediates for the synthesis of other antibacterial agents.Type: GrantFiled: May 21, 2004Date of Patent: October 14, 2008Assignee: GlaxpSmithkline IstrazivackiInventors: Davor Kidemet, Gorjana Lazarevski, Marko Derek, Marija Leljak
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Patent number: 7419997Abstract: The present invention relates to novel compounds that are useful in the treatment of human papillomaviruses, and also to the methods for the making and use of such compounds.Type: GrantFiled: June 7, 2004Date of Patent: September 2, 2008Assignee: SmithKline Beecham CorporationInventors: Sharon Davis Boggs, Kristjan S Gudmundsson
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Patent number: 7378550Abstract: The present invention is directed to processes for the synthesis of intermediates useful in the preparation of non-nucleoside reverse transcriptase inhibitors.Type: GrantFiled: March 26, 2004Date of Patent: May 27, 2008Assignee: SmithKline Beecham CorporationInventor: Michael Tolar Martin
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Patent number: 7365056Abstract: The invention relates to substituted 9a-N-{N?-[4-(sulfonyl)phenyl]carbamoyl} derivatives of 9-deoxo-9-dihydro-9a-aza-9a-homoerithromycin A and 5-0-desosaminyl-9-deoxo-9-di-hydro-9a-aza-9a-homoerithronolide A, novel semisynthetic macrolide antibiotics of the azalide series general formula (1), wherein R represents H or cladinosyl moiety and R1 represents chloro, amino, phenylamino, 2-pyridylamino, 3,4-dimethyl-4-isoxalylamino and 5-methyl-3-isoxazolylamino group, and pharmaceutically acceptable addition salts thereof with inorganic or organic acids.Type: GrantFiled: November 10, 2003Date of Patent: April 29, 2008Assignee: GlaxoSmithKline istrazivacki centar Zagreb d.oInventors: Nedjeljko Kujundzic, Mirjana Bukvic Krajacic, Karmen Brajsa
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Patent number: 7358367Abstract: The present invention relates to the new 3-decladinosyl derivatives of 9-de-oxo-9a-aza9a-homoerythromycin A 9a,11-cyclic carbamate of the general formula (I), their pharmaceutically acceptable addition salts with inorganic or organic acids and their hydrates, wherein R1 individually stands for hydrogen, hydroxyl or a group of the formula (II), wherein X individually stands for C1-C6alkyl group, C2-C6alkenyl group or X individually stands for C1-C6alkyl group with at least one incorporated O, S or N atom or X individually stands for (CH2)n—Ar or X individually stands for (CH2)n-heterocycloalkyl, wherein (CH2)n individually stands for alkyl, wherein n is 1-10, with or without incorporated atom O, S or N, wherein Ar individually stands for 5-10-membered monocyclic or bycyclic aromatic ring with 0-3 atom O, S or N, unsubstituted or substituted with 1-3 group, which are selected independently from halogen, OH, OMe, NO2, NH2, amino-C1-C3alkyl or amino-C1-C3dialkyl, CN, SO2NH2, C1-C3alkyl, and heterocycloalkyl standType: GrantFiled: September 26, 2003Date of Patent: April 15, 2008Assignee: GlaxoSmithKline istrazivacki Centar Zagreb d.o.Inventors: Andrea Fajdetic, Gabrijela Kobrehel, Gorjana Lazarevski, Stjepan Mutak
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Patent number: 7351733Abstract: The present invention relates to novel compounds that are useful in the treatment of human papillomaviruses, and also to the methods for the making and use of such compounds.Type: GrantFiled: June 7, 2004Date of Patent: April 1, 2008Assignee: SmithKline Beecham CorporationInventors: Sharon Davis Boggs, Kristjan S Gudmundsson, Leah D'Aurora Richardson, Paul Richard Sebahar
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Patent number: 7342000Abstract: The invention relates to N?-substituted 9a-N-(N?-carbamoyl-?-aminopropyl), 9a-N-(N?-thiocarbamoyl-?-aminopropyl), 9a-N-[N?-?-cyanoethyl)-N?-carbamoyl-?-aminopropyl] and 9a-N-[N?-?-cyanoethyl)-N?-thiocarbamoyl-?-am inopropyl] derivatives of 9-deoxo-9-dihydro-9a-aza-9a-homoerithromycin A and 5-O-desosaminyl-9-deoxo-9-dihydro-9a-aza-9a-homoerithronolide A, novel semi-synthetic macrolide antibiotics of the azalide series, of the general formula 1, wherein R represents H or cladinosyl moiety, R1 represents H or ?-cyanoethyl moiety, R2 represents isopropyl, 1-naphtyl, 2-naphtyl, benzyl, 2-(trifluoromethyl)phenyl, 3-phenylpropyl, ?-phenylethyl, ethoxycarbonyl-methyl, 1-(1-naphtyl)ethyl, 3,4,5-trimethoxyphenyl and 2,4-dichlorophenyl group, and X represents O and S, and their acceptable addition salts thereof with inorganic or organic acids, to the process for preparation of their pharmaceutical compositions as well as the use their compositions in the treatment of bacterial infections.Type: GrantFiled: December 10, 2003Date of Patent: March 11, 2008Assignee: GlaxoSmithKline istrazivacki center ZagrebInventors: Nedjeljko Kujundzic, Mirjana Bukvic Krajacic, Karmen Brajsa
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Patent number: 7304087Abstract: Anti-viral agents of Formula (I) wherein: A represents hydroxy; D represents aryl or heteroaryl; E represents hydrogen, C1-6alkyl, aryl, heteroaryl or heterocyclyl; G represents hydrogen or optionally substituted C1-6alkyl; J represents C1-6alkyl, heterocyclylalkyl, arylalkyl or heteroarylalkyl; and salts, solvates and esters thereof; provided that when A is esterified to form —OR where R is selected from straight or branched chain alkyl, aralkyl, aryloxyalkyl, or aryl, then R is other than tert-butyl; processes for their preparation, pharmaceutical compositions comprising them, and methods of using them in HCV treatment are provided.Type: GrantFiled: October 22, 2003Date of Patent: December 4, 2007Assignee: Glaxo Group LimitedInventors: David Haigh, Charles David Hartley, Peter David Howes, Deborah Lynette Jackson, Pritom Shah, Martin John Slater
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Patent number: 7259163Abstract: Novel anti-viral agents of Formula wherein: A represents OR1, NR1R2, or R1 wherein R1 and R2 are hydrogen, C1-6alkyl, aryl, heteroaryl, arylalkyl, or heteroarylalkyl; or R1 and R2 together with the nitrogen atom to which they are attached form a 5 or 6 membered saturated cyclic group; B represents C(O)R3 wherein R3 is C1-6alkyl, aryl, heteroaryl, arylalkyl, or heteroarylalkyl; C represents C1-6alkyl, aryl, heteroaryl or heterocyclyl; D represents a saturated or unsaturated optionally substituted 6-membered heterocyclic ring; E represents hydrogen or C1-6alkyl; F represents hydrogen, C1-6alkyl, aryl or heteroaryl; and G represents hydrogen, C1-6alkyl, heterocyclylalkyl, arylalkyl or heteroarylalkyl; and salts, solvates and esters thereof, processes for their preparation and methods of using them in HCV treatment are provided.Type: GrantFiled: October 30, 2002Date of Patent: August 21, 2007Assignee: Glaxo Group LimitedInventors: Gianpaolo Bravi, Rossella Guidetti, David Haigh, Charles David Hartley, Peter David Howes, Deborah Lynette Jackson, Victoria Lucy Helen Lovegrove, Pritom Shah, Martin John Slater, Katrina Jane Wareing
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Patent number: 6630477Abstract: The present invention relates to (1R,4S)-4-(6-amino-9H-purin-9-yl)-2-cyclopentene-1-methanol and its use in medical therapy for the treatment of hepatitis B infection.Type: GrantFiled: October 12, 2001Date of Patent: October 7, 2003Assignee: SmithKline Beecham CorporationInventor: Susan Mary Daluge
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Patent number: 6514953Abstract: The invention relates to calcium (3S) tetrahydro-3-furanyl(1S,2R)-3-[[(4-aminophenyl)sulfonyl](isobutyl)amino]-1-benzyl-2-(phosphonooxy)propylcarbamate, to processes for its preparation, and to its use in the treatment of diseases caused by retroviruses.Type: GrantFiled: April 20, 2001Date of Patent: February 4, 2003Assignee: SmithKline Beecham CorporationInventors: Ian Gordon Armitage, Andrew David Searle, Hardev Singh
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Patent number: 6432966Abstract: The present invention relates to therapeutic combinations comprising (2R,cis)-4-amino-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-pyrimidin-2-one (lamivudine) and BMS-200475 which have anti-hepatitis B virus (HBV) activity. The present invention is also concerned with pharmaceutical compositions containing said combinations and their use in the treatment of HBV infections including infections with HBV mutants bearing resistance to nucleoside and/or non-nucleoside inhibitors.Type: GrantFiled: October 29, 1999Date of Patent: August 13, 2002Assignee: SmithKline Beecham CorporationInventors: Marc Rubin, Nathaniel A. Brown, Lynn D. Condreay, Douglas Fraser Gray
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Patent number: 6417191Abstract: The present invention relates to therapeutic combinations of (1S,4R)-cis-4-[2-amino-6-(cyclopropylamino)-9H-purin-9-yl)-2-cyclopentene-1-methanol (1592U89), 3′-azido-3′-deoxythymidine (zidovudine) and (2R,cis)-4-amino-]-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-(1H)-pyrimidin-2-one (3TC) (or, alternatively to 3TC, (2R,cis)-4-amino-5-fluoro-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-(1H)-pyrimidin-2-one (FTC)) which have anti-HIV activity. The present invention is also concerned with pharmaceutical compositions containing said combinations and their use in the treatment of HIV infections including infections with HIV mutants bearing resistance to nucleoside and/or non-nucleoside inhibitors.Type: GrantFiled: September 30, 1997Date of Patent: July 9, 2002Assignee: GlaxoSmithKlineInventors: David Walter Barry, Martha Heider St. Clair