Abstract: 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:
Grant
Filed:
January 13, 2006
Date of Patent:
August 2, 2011
Assignee:
GlaxoSmithKline Istrazivacki Centar Zagreb D.O.O.
Inventors:
Ognjen Culic, Martina Bosnar, Nikola Marjanovic, Boris Mildner, Linda Tomaskovic, Sulejman Alihodzic
Abstract: 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:
Grant
Filed:
September 16, 2008
Date of Patent:
April 19, 2011
Assignee:
GlaxoSmithKline Istrazivacki Centar Zagreb D.O.O.
Inventors:
Mladen Mercep, Milan Mesic, Linda Tomaskovic, Marijana Komac, Boska Hrvacic, Stribor Markovic
Abstract: 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:
Grant
Filed:
January 13, 2006
Date of Patent:
March 22, 2011
Assignee:
GlaxoSmithKline istrazivacki centar Zagreb d.o.o.
Abstract: 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:
Grant
Filed:
May 20, 2003
Date of Patent:
June 23, 2009
Assignee:
GlaxoSmithKline Istrazivacki Centar Zagreb d.o.o.
Inventors:
Mladen Mercep, Milan Mesic, Dijana Pesic
Abstract: 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:
Application
Filed:
September 16, 2008
Publication date:
April 23, 2009
Applicant:
GLAXOSMITHKLINE ISTRAZIVACKI CENTAR ZAGREB D.O.O.
Inventors:
Mladen MERCEP, Milan MESIC, Linda TOMASKOVIC, Marijana KOMAC, Boska HRVACIC, Stribor MARKOVIC
Abstract: 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:
Grant
Filed:
January 3, 2002
Date of Patent:
November 4, 2008
Assignee:
Glaxosmithkline Istrazivacki Centar Zagreb D.O.O
Inventors:
Mladen Mercep, Milan Mesic, Linda Tomaskovic, Marijana Komac, Boska Hrvacic, Stribor Markovic
Abstract: 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:
Application
Filed:
January 13, 2006
Publication date:
October 2, 2008
Applicant:
GLAXOSMITHKLINE ISTRAZIVACKI CENTAR ZAGREB D.O.O.
Inventors:
Ognjen Culic, Martina Bosnar, Nikola Marianovic, Boris Mildner, Linda Tomaskovic, Sulejman Alihodzic
Abstract: 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:
Application
Filed:
January 13, 2006
Publication date:
September 25, 2008
Applicant:
GLAXOSMITHKLINE ISTRAZIVACKI CENTAR ZAGREB D.O.O.
Abstract: 9a-carbamoyl and thiocarbamoyl azalides A and their pharmaceutically acceptable derivatives are useful for treatment and prevention of malaria.
Type:
Application
Filed:
January 12, 2006
Publication date:
September 18, 2008
Applicant:
GLAXOSMITHKLINE ISTRAZIVACKI CENTAR ZAGREB D.O.O.
Inventors:
Stjepan Mutak, Zrinka Ivezic, Sulejman Alihodzic
Abstract: 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:
Grant
Filed:
January 20, 2006
Date of Patent:
June 10, 2008
Assignee:
GlaxoSmithKline Istrazivacki Centar Zagreb d.o.o.
Abstract: 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:
Application
Filed:
November 10, 2003
Publication date:
November 22, 2007
Applicant:
GLAXOSMITHKLINE ISTRAZIVACKI CENTAR ZAGREB D.O.O.
Abstract: 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:
Grant
Filed:
May 20, 2003
Date of Patent:
August 28, 2007
Assignee:
GlaxoSmithKline Istrazivacki Centar Zagreb, D.O.O.
Abstract: 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:
Application
Filed:
November 19, 2004
Publication date:
May 17, 2007
Applicant:
GLAXOSMITHKLINE ISTRAZIVACKI CENTAR ZAGREB D.O.O.
Inventors:
Mladen Mercep, Milan Mesic, Dijana Pesic
Abstract: 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:
Application
Filed:
November 19, 2004
Publication date:
May 17, 2007
Applicant:
GLAXOSMITHKLINE ISTRAZIVACKI CENTAR ZAGREB D.O.O.
Inventors:
Mladen Mercep, Milan Mesic, Dijana Pesic, Iva Dzapo
Abstract: 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:
Grant
Filed:
January 23, 2006
Date of Patent:
April 24, 2007
Assignee:
GlaxoSmithKline Istrazivacki Centar Zagreb D.O.O.
Abstract: 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:
Application
Filed:
May 11, 2004
Publication date:
March 22, 2007
Applicant:
GlaxoSmithKline Istrazivacki centar Zagreb d.o.o.
Inventors:
Zorica Marusic-Istuk, Nedjeljko Kujundzic, Stjepan Mutak