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.

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.

Abstract: The present invention relates to 1-aza-2-oxa-dibenzo[e,h]azulenes, their pharmacologically acceptable salts and solvates, processes and intermediates for the preparation thereof and to the use thereof in pharmaceutical formulations 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.

Abstract: The present invention relates to the use of derivatives from the group of 1-thia-3-aza-dibenzo[e,h]azulenes and of their pharmaceutically 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.

Abstract: The present invention relates to 1,3-diaza-dibenzoazulene derivatives, 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 tumor necrosis factor-? (TNF-?) production and the inhibition of interleukin-1 (IL-1) production as well as to their analgetic action.

Abstract: 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.

Abstract: The present invention relates to the use of compounds from the group of 2-thia-dibenzo[e,h]azulenes and of their pharmacologically acceptable salts and solvates for the manufacture of 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.

Abstract: 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, D represents a nonsteroidal subunit (nonsteroidal moiety) derived from nonsteroid drug with anti-inflammatory, analgesic and/or antipyretic activity (NSAID) and L represents a linking group covalently linking M and D; (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 diseases and conditions in humans and animals.

Abstract: The present invention is directed to methods for the prevention and treatment of inflammatory diseases, disorders, and conditions of gastrointestinal tract by administering to a patient in need of such treatment, conjugate compounds of Formula VII having low oral-bioavailability, or pharmaceutically acceptable salts, prodrugs, or solvate thereof: wherein M represents a macrolide subunit possessing the property of accumulation in inflammatory cells, T represents an anti-inflammatory subunit that can be a steroid or nonsteroid (nonsteroidal moiety) derived from a non-steroid drug with anti-inflammatory, analgesic and/or antipyretic activity (NSAID) and L represents a linker covalently linking M and T. The present disclosure is also directed to pharmaceutical compositions containing conjugate compounds of Formula VII having low oral-bioavailability.

Abstract: 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, S represents a steroid subunit (steroid moiety) derived from steroid drug with anti-inflammatory activity and L represents a linker molecule linking M and S, (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 diseases and conditions in humans and animals. Such compounds inhibit many cytokines and immune mediators involved in immune responses which cause inflammation, allergy, or alloimmunity, including without limitation IL-1, 2, 4, 5, 6, 10, 12, GMCSF, ICAM, and TNF-?. Importantly, anti-inflammatory steroids exert a direct anti-inflammatory effect through binding to the glucocorticosteroid receptor.

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.

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 diesases and/or conditions in humans.

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.

Abstract: The present invention relates to (a) novel 1-thiadibenzoazulene derivatives of the formula (I), (b) to their pharmacologically acceptable esters, salts and solvates, (c) to processes and intermediates for the preparation thereof, (d) to a process for preparing pharmaceutical formulations for the treatment of inflammatory diseases and conditions and (e) to the use thereof in the treatment of inflammatory diseases and conditions in humans and animals. These compounds inhibit tumour necrosis factor-? (TNF-?) production and interleukin-1 (IL-1) production and exhibit an analgetic action.

Abstract: The present invention is directed to methods for the prevention and treatment of inflammatory diseases, disorders, and conditions of gastrointestinal tract by administering to a patient in need of such treatment, conjugate compounds of Formula VII having low oral-bioavailability, or pharmaceutically acceptable salts, prodrugs, or solvate thereof: wherein M represents a macrolide subunit possessing the property of accumulation in inflammatory cells, T represents an anti-inflammatory subunit that can be a steroid or nonsteroid (nonsteroidal moiety) derived from a non-steroid drug with anti-inflammatory, analgesic and/or antipyretic activity (NSAID) and L represents a linker covalently linking M and T. The present disclosure is also directed to pharmaceutical compositions containing conjugate compounds of Formula VII having low oral-bioavailability.

Abstract: The present invention relates to 1,3-diaza-dibenzoazulene derivatives, 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.

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 tumour necrosis factor-? (TNF-?) production and the inhibition of interleukin-1 (IL-1) production as well as to their analgetic action.

Abstract: The present invention relates to 1-oxa-dibenzoazulene derivatives, 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.

Abstract: The present invention relates to 1-aza-dibenzoazulene derivatives, 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.

Abstract: The present invention relates to compounds of 2-thia-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.