Patents Assigned to GlaxoSmithKline istrazivacki centar Zagreb
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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: 7928078Abstract: The present invention relates to novel compounds represented by the structure I and pharmaceutical preparations thereof for the treatment of inflammatory diseases in humans and animals.Type: GrantFiled: September 16, 2008Date of Patent: April 19, 2011Assignee: GlaxoSmithKline Istrazivacki Centar Zagreb D.O.O.Inventors: Mladen Mercep, Milan Mesic, Linda Tomaskovic, Marijana Komac, Boska Hrvacic, Stribor Markovic
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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: 7579334Abstract: The present invention relates to new compounds represented by Formula I: wherein M represents a macrolide subunit of the substructure II: L represents the chain of the substructure III: —X1—(CH2)m-Q-(CH2)n—X2—??III D represents the steroid or nonsteroidal subunit derived from steroid or nonsteroidal (NSAID) drugs with anti-inflammatory activity; The present invention relates also to pharmaceutically acceptable salts and solvates of such prepared compounds, to process and intermediates for their preparation, as well as to the improved therapeutic action and the use in the treatment of inflammatory diseases and conditions in humans and animals.Type: GrantFiled: April 22, 2004Date of Patent: August 25, 2009Assignee: GlaxoSmithKline Istrazivacki Centar ZagrebInventors: Mladen Mercep, Milan Mesic, Linda Tomaskovic
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Patent number: 7550498Abstract: The present invention relates to derivatives of 1,2-diaza-dibenzoazulene, to their pharmacologically acceptable salts and solvates, to processes and intermediates for the preparation thereof as well as to their antiinflammatory actions, especially to the inhibition of tumor necrosis factor-? (TNF-?) production and the inhibition of interleukin-1 (IL-1) production as well as to their analgetic action.Type: GrantFiled: May 20, 2003Date of Patent: June 23, 2009Assignee: GlaxoSmithKline Istrazivacki Centar Zagreb d.o.o.Inventors: Mladen Mercep, Milan Mesic, Dijana Pesic
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Publication number: 20090105163Abstract: The present invention relates to novel compounds represented by the structure I and pharmaceutical preparations thereof for the treatment of inflammatory diseases in humans and animals.Type: ApplicationFiled: September 16, 2008Publication date: April 23, 2009Applicant: GLAXOSMITHKLINE ISTRAZIVACKI CENTAR ZAGREB D.O.O.Inventors: Mladen MERCEP, Milan MESIC, Linda TOMASKOVIC, Marijana KOMAC, Boska HRVACIC, Stribor MARKOVIC
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Patent number: 7446097Abstract: The present invention relates to novel compounds represented by the structure I and pharmaceutical preparations thereof for the treatment of inflammatory diseases in humans and animals.Type: GrantFiled: January 3, 2002Date of Patent: November 4, 2008Assignee: Glaxosmithkline Istrazivacki Centar Zagreb D.O.OInventors: Mladen Mercep, Milan Mesic, Linda Tomaskovic, Marijana Komac, Boska Hrvacic, Stribor Markovic
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Publication number: 20080241959Abstract: 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: ApplicationFiled: January 13, 2006Publication date: October 2, 2008Applicant: GLAXOSMITHKLINE ISTRAZIVACKI CENTAR ZAGREB D.O.O.Inventors: Ognjen Culic, Martina Bosnar, Nikola Marianovic, Boris Mildner, Linda Tomaskovic, Sulejman Alihodzic
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Publication number: 20080234211Abstract: 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: ApplicationFiled: January 13, 2006Publication date: September 25, 2008Applicant: 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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Publication number: 20080227730Abstract: 9a-carbamoyl and thiocarbamoyl azalides A and their pharmaceutically acceptable derivatives are useful for treatment and prevention of malaria.Type: ApplicationFiled: January 12, 2006Publication date: September 18, 2008Applicant: GLAXOSMITHKLINE ISTRAZIVACKI CENTAR ZAGREB D.O.O.Inventors: Stjepan Mutak, Zrinka Ivezic, Sulejman Alihodzic
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Patent number: 7384975Abstract: The invention relates to novel compounds of the formula (I) including all their tautomers, to pharmaceutically acceptable salts and solvates thereof, to processes and reactive intermediates for the preparation thereof, and to processes and reactive intermediates for the preparation of the compounds of the formula (II) including all their stereoisomers and tautomers to the use of the compounds of the formula (II) as suitable precursors for the preparation of the compounds of the formula (I) as well as to use of the compounds of the formula (I) and of the compounds of the formula (II) as therapeutically active agents in the prophylaxis and treatment of asthma and other inflammatory diesases and conditions in humans.Type: GrantFiled: January 20, 2006Date of Patent: June 10, 2008Assignee: GlaxoSmithKline Istrazivacki Centar Zagreb d.o.o.Inventors: Mladen Mercep, Milan Mesic, Boska Hrvacic, Ivaylo Jivkov Elenkov, Ivica Malnar, Stribor Markovic, Lidija Simicic, Andreja Cempuh Klonkay, Anita Filipovic
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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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Publication number: 20070270356Abstract: The invention relates to substituted 9a-N—[N?-(benzenesulfonyl)carbamoyl-?-aminopropyl] and 9a-N—[N?-(?-cyanoethyl)-N?-(benzenesulfonyl)carbamoyl-?-aminopropyl] derivatives of 9-deoxo-9-dihydro-9a-aza-9a-homoerithromycin A and 5-( )-desosaminyl-9-deoxo-9-dihydro-9a-aza-9a-homoerithronolide A, novel semisynthetic macrolide antibiotics of the azalide series, of the formula (I) wherein R represents H or cladinosyl moiety, R1 represents H or ?-cyanoethyl group an R2 represents II or fluoro, chloro and methyl group, and pharmaceutically acceptable salts thereof with inorganic or organic acids, to the process for the preparation of pharmaceutical compositions as well as to the use their compositions for sterilization rooms and medical instruments as well as for protection of wall and wooden coatings.Type: ApplicationFiled: November 10, 2003Publication date: November 22, 2007Applicant: GLAXOSMITHKLINE ISTRAZIVACKI CENTAR ZAGREB D.O.O.Inventors: Nedjeljko Kujundzic, Mirjana Krajacic, Karmen Brajsa
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Patent number: 7262302Abstract: The present invention relates to derivatives of 1-thia-3-aza-dibenzoazulene class, to their pharmacologically acceptable salts and solvates, to processes and intermediates for the preparation thereof as well as to their antiinflammatory effects, especially to the inhibition of tumour necrosis factor-? (TNF-?) production and the inhibition of interleukin-1 (IL-1) production as well as to their analgetic action.Type: GrantFiled: May 20, 2003Date of Patent: August 28, 2007Assignee: GlaxoSmithKline Istrazivacki Centar Zagreb, D.O.O.Inventors: Mladen Mercep, Milan Mesic, Marina Modric, Dijana Pesic, Davor Kidemet
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Publication number: 20070111968Abstract: The present invention relates to the use of compounds from the group of 1-aza-dibenzo[e,h]azulenes and of their pharmacologically acceptable salts and solvates in a pharmaceutical formulation for the treatment and prevention of diseases, damages and disorders of the central nervous system (CNS) caused by disorders of the neurochemical equilibrium of biogenic amines or other neurotransmitters.Type: ApplicationFiled: November 19, 2004Publication date: May 17, 2007Applicant: GLAXOSMITHKLINE ISTRAZIVACKI CENTAR ZAGREB D.O.O.Inventors: Mladen Mercep, Milan Mesic, Dijana Pesic
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Publication number: 20070111990Abstract: The present invention relates to the use of compounds from the group of 3-aza-1-oxa-dibenzo[e,h]azulenes and of their pharmacologically acceptable salts and solvates for the use in the treatment and prevention of diseases, damages and disorders of the central nervous system (CNS) caused by disorders of the neurochemical equilibrium of biogenic amines or other neurotransmitters.Type: ApplicationFiled: November 19, 2004Publication date: May 17, 2007Applicant: GLAXOSMITHKLINE ISTRAZIVACKI CENTAR ZAGREB D.O.O.Inventors: Mladen Mercep, Milan Mesic, Dijana Pesic, Iva Dzapo
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Patent number: 7208518Abstract: The present invention relates to novel compounds of the formula (I) including all stereoisomers and tautomers thereof, to the pharmaceutically acceptable salts and solvates thereof, to the processes and reactive intermediates for their preparation and to their use in the prophylaxis and treatment of asthma and other inflammatory diseases and/or conditions in humans.Type: GrantFiled: January 23, 2006Date of Patent: April 24, 2007Assignee: GlaxoSmithKline Istrazivacki Centar Zagreb D.O.O.Inventors: Mladen Mercep, Milan Mesic, Boska Hrvacic, Ivaylo Jivkov Elenkov, Ivica Malnar, Stribor Markovic, Lidija Simicic, Andreja Cempuh Klonkay, Anita Filipovic
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Publication number: 20070066544Abstract: The present invention relates to the new 3-decladinosyl derivatives of 9a-N-carbamoyl- and 9a-N-thiocarbamoyl-9-deoxo-9-dihydro-9a-aza-9a-homoerythromycin A of the general formula (I), their pharmaceutically acceptable addition salts with inorganic or organic acids and their hydrates, to intermediates for synthesis of other macrolide compounds with antibacterial activity, to the process for their preparation, to their pharmaceutically acceptable addition salts with inorganic or organic acids and their hydrates, to the process for the preparation of pharmaceutical compositions, as well as the use of pharmaceutical compositions for treating bacterial infections.Type: ApplicationFiled: May 11, 2004Publication date: March 22, 2007Applicant: GlaxoSmithKline Istrazivacki centar Zagreb d.o.o.Inventors: Zorica Marusic-Istuk, Nedjeljko Kujundzic, Stjepan Mutak
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Patent number: 7157433Abstract: The present invention relates (a) to new compounds represented by Formula I: wherein M represents a macrolide subunit (macrolide moiety) derived from macrolide possessing the property of accumulation in inflammatory cells, V represents an anti-inflammatory steroid or nonsteroid subunit, or an antineoplastic or antiviral subunit and L represents a linking group covalently linking M and V; (b) to their pharmacologically acceptable salts, prodrugs and solvates, (c) to processes and intermediates for their preparation, and (d) to their use in the treatment of inflammatory/neoplastic/viral diseases and conditions in humans and animals.Type: GrantFiled: July 8, 2003Date of Patent: January 2, 2007Assignee: GlaxoSmithKline istrazivacki centar ZagrebInventors: Mladen Mercep, Milan Mesic, Linda Tomaskovic, Stribor Markovic