KONJUGATE WITH ENTZÜNDUNGSHEMMENDER ACTIVITY

1,2-DIAZA-DIBENZOAZULENE AS INHIBITORS of the PRODUCTION OF TUMOR NECROSIS FACTOR AND INTERMEDIATE PRODUCTS FOR THEIR PRODUCTION

REPRESENTATION OF 1-AZA-2-OXADIBENZOÄE, HÜAZULENEN AND THEIR USE WITH the PRODUCTION of PHARMACEUTICAL FORMULATIONS FOR the TREATMENT AND PREVENTION OF DISEASES AND ILLNESSES the CENTERS of the NERVOUS SYSTEM

MACROLID KONJUGATE ONE WITH ENTZÜNDUNGSHEMMENDER EFFECT

1,2-DIAZA-DIBENZOAZULENES AS INHIBITORS OF TUMOUR NECROSIS FACTOR PRODUCTION AND INTERMEDIATES FOR THE PREPARATION THEREOF

USE OF 3-AZA-AOXA-DIBENZO (E, H) AZULENEN FOR the PRODUCTION OF PHARMACEUTICAL FORMULATION FOR the TREATMENT AND PREVENTION OF ILLNESSES AND DISTURBANCES the CENTERS of the NERVOUS SYSTEM

USE OF 1-OXADIBENZO ÄE, HÜ AZULENEN FOR the PRODUCTION OF PHARMACEUTICAL FORMULATIONS FOR the TREATMENT AND PREVENTION OF ILLNESSES AND DISTURBANCES the CENTERS of the NERVOUS SYSTEM

USE OF 1-THIADIBENZO E, H AZULENEN FOR the PRODUCTION OF PHARMACEUTICAL FORMULATIONS FOR the TREATMENT AND PREVENTION OF ILLNESSES AND DISTURBANCES the CENTERS of the NERVOUS SYSTEM

USE OF 1,3-DIAZADIBENZO (E, H) AZULENEN FOR the PRODUCTION OF PHARMACEUTICAL FORMULATIONS FOR the TREATMENT AND PREVENTION OF ILLNESSES AND DISTURBANCES the CENTERS of the NERVOUS SYSTEM

1-OXA-3-AZA-DIBENZOAZULENE AS INHIBITORS of the PRODUCTION OF TUMOR NECROSIS FACTOR AND INTERMEDIATE PRODUCTS FOR THEIR PRODUCTION

1- OR 3-THIA-BENZONAPHTHOAZULENE AS INHIBITORS of the PRODUCTION OF TUMOR NECROSIS FACTOR AND INTERMEDIATE PRODUCTS FOR THEIR PRODUCTION

2-THIA-DIBENZOAZULENE AS INHIBITORS of the PRODUCTION OF TUMOR NECROSIS FACTOR AND INTERMEDIATE PRODUCTS FOR THEIR PRODUCTION

NEW COMPOUNDS, COMPOSITIONS AND METHODS FOR TREATMENT OF INFLAMMATORY DISEASES AND CONDITIONS

1- OR 3-THIA-BENZONAPHTHOAZULENES AS INHIBITORS OF TUMOUR NECROSIS FACTOR PRODUCTION AND INTERMEDIATES FOR THE PREPARATION THEREOF

1-OXA-3-AZA-DIBENZOAZULENE ALS INHIBITOREN DER PRODUKTION VON TUMORNEKROSEFAKTOR UND ZWISCHENPRODUKTE FÜR DEREN HERSTELLUNG

THIADIBENZOAZULENDERIVATE FOR THE TREATMENT OF INFLAMMATORY ILLNESSES

USE OF 1,2-DIAZADIBENZOÄE, HÜAZULENEN FOR the PRODUCTION OF PHARMACEUTICAL FORMULATIONS FOR the TREATMENT AND PREVENTION OF ILLNESSES AND DISTURBANCES the CENTERS of the NERVOUS SYSTEM

KONJUGATE THERAPY ANTI-INFLAMMATORY OF IMMUNE-CELL-SPECIFIC MACRO EYELID CONNECTIONS WITH ANTI-INFLAMMATORY CONNECTIONS TO THE IMPROVED CELLARRANGED

Conjugates with anti-inflammatory activity

THIENODIBENZAZULENVERBINDUNGEN AS TUMORNEKROSEFAKTORHEMMER

HYBRID MOLECULES OF MAKROLIDEN WITH STEROIDALEN/NICHT STEROIDALEN ANTI-INFLAMMATORY ACTIVE MOLECULES

1,3-DIAZA-DIBENZOAZULENE AS INHIBITORS of the PRODUCTION OF TUMOR NECROSIS FACTOR AND INTERMEDIATE PRODUCTS FOR THEIR PRODUCTION

USE OF 2-THIA-DIBENZO (E, H) AZULENEN FOR TREATMENT AND PREVENTION OF ILLNESSES AND DISTURBANCES the CENTERS of the NERVOUS SYSTEM

1-AZADIBENZOAZULENE AS INHIBITORS of the PRODUCTION OF TUMOR NECROSIS FACTOR AND INTERMEDIATE PRODUCTS FOR THEIR PRODUCTION

USE OF CELL-SPECIFIC CONJUGATES FOR TREATMENT OF INFLAMMATORY DISEASES OF THE GASTROINTESTINAL TRACT

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 oralbioavailability, 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 antiinflammatory, 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. © KIPO & WIPO 2007 ...

New compounds, compositions and methods for treatment of inflammatory diseases and conditions

1,3-diaza-dibenzoazulenes as inhibitors of tumour necrosis factor production and intermediates for the preparation thereof

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-alpha (TNF-alpha) production and the inhibition of interleukin-1 (IL-1) production as well as to their analgetic action.

Hybrid molecules of macrolides with steroid/non-steroid anti-inflammatory, antineoplastic and antiviral active molecules

Conjugates with anti-inflammatory activity

3-Aza-1-oxa-dibenzo[e,h]azulenes for the treatment of central nervous system diseases and disorders

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.

2-THIA-DIBENZOAZULENES AS INHIBITORS OF TUMOUR NECROSIS FACTOR PRODUCTION AND INTERMEDIATES FOR THE PREPARATION THEREOF

Macrolide-conjugates with anti-inflammatory activity

DERIVATIVES OF 1-AZA-2-OXA-DIBENZO [E, H] AZULENOS

Procedimientos e intermediarios para su preparacion y empleo de los mismos en la fabricacion de composiciones farmacéuticas para el tratamiento y la prevencion de enfermedades, danos y trastornos del sistema nervioso central (SNC) causados por trastornos del equilibrio neuroquímico de las aminas biogénicas u otros neurotransmisores. Reivindicacion 1: Un compuesto de formula general (1), en la cual: X significa CH2 o un heteroátomo seleccionado entre el grupo que comprende O, S, S(=O), S(=O)2 y NRa, donde Ra es hidrogeno o un sustituyente seleccionado entre el grupo que comprende alquilo C1-3, alcanoilo C1-3, alcoxicarbonilo C1-7, arilalquiloxicarbonilo C1-10, aroilo C7-10, arilalquilo C7-10, alquilsililo C3-7 y alquilsililalquiloxialquilo C5-10; Y y Z significan, independientemente uno del otro, uno o más sustituyentes idénticos o diferentes unidos a cualquier átomo de carbono disponible seleccionado entre el grupo que comprende hidrogeno, halogeno, alquilo C1-4, alquenilo C2-4, alquinilo ...

1-Thia-3-aza-dibenzo[e,h]azulenes for the treatment of central nervous system diseases and disorders

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.

Use of cell-specific conjugates for treatment of inflammatory diseases of the gastrointestinal tract

Preparation of 1-aza-2-oxa-dibenzo[e,h]azulenes and their medical use

The present invention relates to compounds from the group of 1-aza-2-oxadibenzo[e,h]azulenes, their pharmacologically acceptable salts and solvates, processes and intermediates for the preparation thereof and to the use thereof for the manufacture of 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.

VERWENDUNG VON 1,3-DIAZADIBENZOÄe,hÜ AZULENEN ZUR HERSTELLUNG VON PHARMAZEUTISCHEN FORMULIERUNGEN FÜR DIE BEHANDLUNG UND PRÄVENTION VON ERKRANKUNGEN UND STÖRUNGEN DES ZENTRALEN NERVENSYSTEMS

Thienodibenzoazulene compounds as tumor necrosis factor inhibitors

NEW NONSTEROIDAL ANTI-INFLAMMATORY SUBSTANCE, COMPOSITION AND METHOD FOR USE THEREOF

PROBLEM TO BE SOLVED: To provide a macrolide/NSAID hybrid compound to cope with inflammatory state. SOLUTION: There are provided (a) 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 nonsteroidal drug with anti-inflammatory, analgesic and/or antipyretic activity (NSAID); and L represents a linking group covalently linking M and D], (b) their pharmacologically acceptable salts, prodrugs and solvates, (c) methods and intermediates for their preparation, and (d) their use in the treatment of inflammatory diseases and conditions in humans and animals. COPYRIGHT: (C)2011,JPO&INPIT ...

1-AZA-DIBENZOAZULENES AS INHIBITORS OF TUMOUR NECROSIS FACTOR PRODUCTION AND INTERMEDIATES FOR THE PREPARTION THEREOF

1,2-diaza-dibenzoazulenes as inhibitors of tumour necrosis factor production and intermediates for the preparation thereof

NOVEL COMPOUNDS, COMPOSITIONS AS CARRIERS FOR STEROID/NON-STEROID ANTI-INFLAMMATORY, ANTINEOPLASTIC AND ANTIVIRAL ACTIVE MOLECULES

1,2-DIAZA-DIBENZOAZULENE ALS INHIBITOREN DER PRODUFÜR DEREN HERSTELLUNG

Thienodibenzoazulene compounds as tumor necrosis factor inhibitors

1,3-DIAZA-DIBENZOAZULENES AS INHIBITORS OF TUMOUR NECROSIS FACTOR PRODUCTION AND INTERMEDIATES FOR THE PREPARATION THEREOF

NOVEL NONSTEROIDAL ANTI-INFLAMMATORY SUBSTANCES, COMPOSITIONS AND METHODS FOR THEIR USE

1-OXA-3-AZA-DIBENZOAZULENES AS INHIBITORS OF TUMOUR NECROSIS FACTOR PRODUCTION AND INTERMEDIATES FOR THE PRODUCTION THEREOF

The present invention relates to derivatives of 1-oxa-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 actions, especially to the inhibition of tumour necrosis factor-α (TNF-α) production and the inhibition of interleukin-1 (IL-1) production as well as to their analgetic action. © KIPO & WIPO 2007 ...

THIENODIBENZOAZULENE COMPOUNDS AS TUMOR NECROSIS FACTOR INHIBITORS

VERWENDUNG VON 3-AZA-AOXA-DIBENZO(e,h)AZULENEN ZUR HERSTELLUNG VON PHARMAZEUTISCHEN FORMULIERUNG FÜR DIE BEHANDLUNG UND PRÄVENTION VON ERKRANKUNGEN UND STÖRUNGEN DES ZENTRALEN NERVENSYSTEMS

MACROLIDE-CONJUGATES WITH ANTI-INFLAMMATORY ACTIVITY

The present invention relates to new compounds represented by Formula (I); wherein M represents a macrolide subunit of the substructure II, Formula (II); L represents the chain of the substructure III, Formula (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 processe 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. © KIPO & WIPO 2007 ...

1-THIA-3-AZA-DIBENZOAZULENES AS INHIBITORS OF TUMOUR NECROSIS FACTOR PRODUCTION AND INTERMEDIATES FOR THE PREPARATION THEREOF

1-OXA-3-AZA-DIBENZOAZULENE ALS INHIBITOREN DER PRODUKTION VON TUMORNEKROSEFAKTOR UND ZWISCHENPRODUKTE FÜR DEREN HERSTELLUNG

1-oxa-3-aza-dibenzoazulenes as inhibitors of tumor necrosis factor production and intermediates for the production thereof

The present invention relates to derivatives of 1-oxa-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 actions, especially to the inhibition of tumour necrosis factor-alpha (TNF-alpha) production and the inhibition of interleukin-1 (IL-1) production as well as to their analgetic action.

1-AZADIBENZOAZULENE ALS INHIBITOREN DER PRODUKTION VON TUMORNEKROSEFAKTOR UND ZWISCHENPRODUKTE FÜR DEREN HERSTELLUNG

1-oxa-dibenzoazulenes as inhibitors of tumor necrosis factor production and intermediates for the preparation thereof

1-OXA-DIBENZOAZULENES AS INHIBITORS OF TUMOR NECROSIS FACTOR PRODUCTION AND INTERMEDIATES FOR THE PREPARATION THEREOF

1-OXA-3-AZA-DIBENZOAZULENES AS INHIBITORS OF TUMOUR NECROSIS FACTOR PRODUCTION AND INTERMEDIATES FOR THE PRODUCTION THEREOF

Macrolide-conjugates with anti-inflammatory activity

1-AUNT LIKE INHIBITORS OF the PRODUCTION OF the FACTOR OF TUMORLIKE NECROSIS AND INTERMEDIARIES FOR the PREPARATION OF The same

Derivados de 1-tia-3-aza-dibenzoazuleno, sus sales y solvatos farmacológicamente aceptables, procedimientos e intermediarios para la preparación de los mismos, así como también sus efectos antiinflamatorios, en especial para la inhibición de la producción del factor alfa de necrosis tumoral (TNF-alfa) e inhibición de la producción de interleuquina-1 (IL-1), como así también su acción analgésica. Reivindicación 1: Un compuesto de la fórmula (1) caracterizado porque X puede ser CH2 o un heteroátomo como ser O, S, S(=O), S(=O)2, o NRa, donde Ra es H o un grupo protector; Y y Z representan, independientemente uno del otro, uno o más sustituyentes idénticos o diferentes unidos a cualquier átomo de C disponible, y pueden ser halógeno, alquilo C1-4, alquenilo C2-4, alquinilo C2-4, haloalquilo C1-4, hidroxi, alcoxi C1-4, trifluorometoxi, alcanoilo C1-4, amino, aminoalquilo C1-4, N-(alquil-C1-4)amino, N,N-di(alquil-C1-4)amino, tiol, alquiltio, sulfonilo, alquilsulfonilo C1-4, sulfinilo, alquilsulfinilo ...

Nonsteroidal anti-inflammatory substances, compositions and methods for their use

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.

Use of benzonaphthoazulenes for the manufacture of pharmaceutical formulations for the treatment and prevention of central nervous system diseases and disorders

The present invention relates to the use of compounds from the group of benzonaphthoazulenes and of their pharmaceutically acceptable salts and solvates 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 transmitters, and to methods of manufacture of such compounds.

Thienodibenzoazulene compounds as tumor necrosis factor inhibitors

The present invention relates to the dibenzoazulene compounds represented by formula I as well as to their pharmaceutical preparations for the inhibition of tumor necrosis factor alpha (TNF-alpha) and interleukine 1 (IL-1) in mammals at all diseases and conditions where these mediators are excessively secreted. The compounds of the present invention also demonstrate an analgetic action and can be used to relieve pain.

2-THIA-DIBENZOAZULENE ALS INHIBITOREN DER PRODUKTION VON TUMORNEKROSEFAKTOR UND ZWISCHENPRODUKTE FÜR DEREN HERSTELLUNG

Use of immune cell specific conjugates for treatment of inflammatory diseases of the gastrointestinal tract

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.

MACROLID-KONJUGATE MIT ENTZÜNDUNGSHEMMENDEN EIGENSCHAFTEN

Novel compounds, compositions as carriers for steroid/nonsteroid anti-inflammatory; antienoplastic and antiviral active molecules

THIENODIBENZOAZULENE COMPOUNDS AS TUMOR NECROSIS FACTOR INHIBITORS

DERIVATIVES OF 1-AZA-DIBENZOAZULENOS FOR the INHIBITION OF the PRODUCTION OF the FACTOR OF INTERMEDIARY NECROSIS TUMORALE FOR ITS PREPARATION

Derivados de 1-aza-dibenzoazuleno, sus sales y solvatos farmacéuticamente aceptables, procedimientos e intermediarios para su preparación. El compuesto posee efectos antiinflamatorios, especialmente en la inhibición de la producción del factor-a de necrosis tumoral (TNF-a) y la inhibición de la producción de interleucina-1 (IL-1) como así también una acción analgésica. Reivindicación 1: Un compuesto de fórmula (1) caracterizado porque X puede ser CH2 o un heteroátomo tal como O, S, S(=O), S(=O)2, o NRa, donde Ra es hidrógeno o un grupo protector; Y y Z independientemente entre sí denotan uno o más sustituyentes idénticos o diferentes unidos a cualquier átomo de carbono disponible, y pueden ser halógeno, alquilo C1-4, alquenilo C2-4, alquinilo C2-4, halo-alquilo C1-4, hidroxi, alcoxi C1-4, trifluorometoxi, alcanoilo C1-4, amino, amino-alquilo C1-4, alquilamino C1-4, N-(alquiloC1-4)amino, N,N-di(alquiloC1-4)amino, tiol, alquiltio C1-4, sulfonilo, alquilsulfonilo C1-4, sulfinilo, alquilsulfinilo ...

1- or 3-thia-benzonaphthoazulenes as inhibitors of tumor necrosis factor production and intermediates for the preparation thereof

The present invention relates to benzonaphthoazulene derivatives of tiophene 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 tumor necrosis factor-α (TNF-α) production and the inhibition of interleukin-1 (IL-1) production as well as to their analgetic action.

VERWENDUNG VON 1-THIADIBENZO E,H AZULENEN ZUR HERSTELLUNG VON PHARMAZEUTISCHEN FORMULIERUNGEN FÜR DIE BEHANDLUNG UND PRÄVENTION VON ERKRANKUNGEN UND STÖRUNGEN DES ZENTRALEN NERVENSYSTEMS

VERWENDUNG VON 2-THIA-DIBENZOÄE,HÜAZULENEN ZUR BEHANDLUNG UND PRÄVENTION VON ERKRANKUNGEN UND STÖRUNGEN DES ZENTRALEN NERVENSYSTEMS

1-oxa-dibenzoazulenes as inhibitors of tumor necrosis factor production and intermediates for the preparation thereof

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-alpha (TNF-alpha) production and the inhibition of interleukin-1 (IL-1) production as well as to their analgetic action.

THIADIBENZOAZULENDERIVATE ZUR BEHANDLUNG VON ENTZÜNDLICHEN ERKRANKUNGEN

DARSTELLUNG VON 1-AZA-2-OXADIBENZOÄe,hÜAZULENEN UND DEREN VERWENDUNG BEI DER HERSTELLUNG PHARMAZEUTISCHER FORMULIERUNGEN ZUR BEHANDLUNG UND PRÄVENTIONRVENSYSTEMS

2-THIA-DIBENZOAZULENE ALS INHIBITOREN DER PRODUKTION VON TUMORNEKROSEFAKTOR UND ZWISCHENPRODUKTE FÜR DEREN HERSTELLUNG

1-AZADIBENZOAZULENE ALS INHIBITOREN DER PRODUKTION VON TUMORNEKROSEFAKTOR UND ZWISCHENPRODUKTE FÜR DEREN HERSTELLUNG

1-oxa-3-aza-dibenzoazulenes as inhibitors of tumour necrosis factor production and intermediates for the production thereof

VERWENDUNG VON 1-THIADIBENZO E,H AZULENEN ZUR HERSTELLUNG VON PHARMAZEUTISCHEN FORMULIERUNGEN FÜR DIE BEHANDLUNG UND PRÄVENTION VON ERKRANKUNGEN UND STÖRUNGEN DES ZENTRALEN NERVENSYSTEMS

VERWENDUNG VON 2-THIA-DIBENZOÄE,HÜAZULENEN ZUR BEHANDLUNG UND PRÄVENTION VON ERKRANKUNGEN UND STÖRUNGEN DES ZENTRALEN NERVENSYSTEMS

KONJUGATE MIT ENTZÜNDUNGSHEMMENDER AKTIVITÄT

VERWENDUNG VON 1,2-DIAZADIBENZOÄE,HÜAZULENEN ZUR HERSTELLUNG VON PHARMAZEUTISCHEN FORMULIERUNGEN FÜR DIE BEHANDLUNG UND PRÄVENTION VON ERKRANKUNGEN UND STÖRUNGEN DES ZENTRALEN NERVENSYSTEMS

1-aza-dibenzoazulenes as inhibitors of tumor necrosis factor production and intermediates for the preparation thereof

1-oxa-dibenzoazulenes as inhibitors of tumour necrosis factor production and intermediates for the preparation thereof

1-oxa 3-aza-dibenzoazulenes as inhibitors of tumor necrosis factor production and intermediates for the production thereof

The present invention relates to derivatives of 1-oxa-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 actions, especially to the inhibition of tumour necrosis factor-alpha (TNF-alpha) production and the inhibition of interleukin-1 (IL-1) production as well as to their analgetic action.

VERWENDUNG VON 1,3-DIAZADIBENZOÄe,hÜ AZULENEN ZUR HERSTELLUNG VON PHARMAZEUTISCHEN FORMULIERUNGEN FÜR DIE BEHANDLUNG UND PRÄVENTION VON ERKRANKUNGEN UND STÖRUNGEN DES ZENTRALEN NERVENSYSTEMS

Verwendung von 3-aza-1-oxadibenzo(e,h)azulenen zur Herstellung von pharmazeutischen Formulierungen für die Behandlung und Prävention von Erkrankungen und Störungen des zentralen Nervensystems

1-thia-3-aza-dibenzoazulenes as inhibitors of tumour necrosis factor production and intermediates for the preparation thereof

1- ODER 3-THIA-BENZONAPHTHOAZULENE ALS INHIBITOREN DER PRODUKTION VON TUMORNEKROSEFAKTOR UND ZWISCHENPRODUKTE FÜR DEREN HERSTELLUNG

1- OR 3-THIA-BENZONAPHTHOAZULENES AS INHIBITORS OF TUMOUR NECROSIS FACTOR PRODUCTION AND INTERMEDIATES FOR THE PREPARATION THEREOF

The present invention relates to 1- or 3-thiabenzonaphthoazulene 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-alpha (TNF-alpha) production and the inhibition of interleukin-1 (IL-1) production as well as to their analgetic action. © KIPO & WIPO 2007 ...

TIENODIBENZOAZULENE COMPOUNDS AS TUMOR NECROSIS FACTOR INHIBITORS

The present invention relates to the dibenzoazulene compounds represented by formula as well as to their pharmaceutical preparations for the inhibition of tumour necrosis factor alpha (TNF-alpha) and interleukine 1 (IL-1) in mammals at all diseases and conditions where these mediators are excessively secreted. The compounds of the present invention also demonstrate an analgetic action and can be used to relieve pain. 15 claims ...

KONJUGATE VON IMMUNZELLSPEZIFISCHEN MAKROLIDVERBINDUNGEN MIT ANTI-PHLOGISTISCHEN VERBINDUNGEN ZUR VERBESSERTEN ZELLGERICHTETEN ANTI-PHLOGISTISCHEN THERAPIE

THIENODIBENZAZULENVERBINDUNGEN ALS TUMORNEKROSEFAKTORHEMMER

THIENODIBENZOAZULENE COMPOUNDS AS TUMOR NECROSIS FACTOR INHIBITORS

The present invention relates to the dibenzoazulene compounds represented by formula I as well as to their pharmaceutical preparations for the inhibition of tumor necrosis factor alpha (TNF-α) and interleukine 1 (IL-1) in mammals at all diseases and conditions where these mediators are excessively secreted. The compounds of the present invention also demonstrate an analgetic action and can be used to relieve pain. © KIPO & WIPO 2007 ...

Compounds, compositions and methods for treatment of inflammatory diseases and conditions

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-alpha. Importantly, anti-inflammatory steroids exert a direct anti-inflammatory effect through binding to the glucocorticosteroid receptor.

Substituted furochromene compounds of antiinflammatory action

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.

VERWENDUNG VON 1-OXADIBENZO ÄE,HÜ AZULENEN ZUR HERSTELLUNG VON PHARMAZEUTISCHEN FORMULIERUNGEN FÜR DIE BEHANDLUNG UND PRÄVENTION VON ERKRANKUNGEN UND

2-THIA-DIBENZOAZULENES AS INHIBITORS OF TUMOUR NECROSIS FACTOR PRODUCTION AND INTERMEDIATES FOR THE PREPARATION THEREOF

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-α (TNF-α) production and the inhibition of interleukin-1 (IL-1) production as well as to their analgetic action. © KIPO & WIPO 2007 ...

Thiadibenzoazulene derivatives for the treatment of inflammatory diseases

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-alpha (TNF-alpha) production and interleukin-1 (IL-1) production and exhibit an analgetic action.

Compounds, compositions and methods for treatment of inflammatory diseases and conditions

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-alpha Importantly, anti-inflammatory steroids exert a direct anti-inflammatory effect through binding to the glucocorticosteroid receptor.

Tetracyclic Monoamine Reuptake Inhibitors for Treatment of Cns Diseases and Disorders

Novel tetracyclic dibenzo(e,h)azulene compounds of formula I; their pharmacologically acceptable derivatives; process and intermediates for their preparation; pharmaceutical compositions containing them and their activity and use in the treatment of central nervous system (CNS) diseases and conditions in humans and animals.

Compounds, compositions and methods for treatment of inflammatory diseases and conditions

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-α Importantly, anti-inflammatory steroids exert a direct anti-inflammatory effect through binding to the glucocorticosteroid receptor.

COMPOUNDS WITH ANTI-INFLAMMATORY ACTIVITY

Se refiere también a sales y solvatos farmacéuticamente aceptables de tales compuestos preparados para procesar, y a productos intermedios para su preparación, así como para la acción terapéutica optimizada y el uso en el tratamiento de enfermedades y condiciones inflamatorias en humanos y animales. Reivindicación 1: Un compuesto de acuerdo a la fórmula (1), donde: M representa la subunidad de macrólido de la subestructura de fórmula (2), donde: R1, R2, R3, R4 y R5 son elegidos independientemente entre sí, del grupo constituido por hidrógeno alquilo C1-4, alcanoilo, alcoxicarbonilo, arilmetoxicarbonilo, arilo, arilalquilo, alquilsililo y alquilsililalcoxialquilo; RN representa el enlace covalente con X1 de la cadena L; L representa la cadena de la subestructura: -X1-(CH2)m-Q-(CH2)n-X2-, donde: X1 es -CH2- o -C(O)-; X2 es -NH- o -O-; Q es -NH- o -CH2-; los símbolos m y n, son independientemente, números enteros de 0 a 4; con la condición que si Q=NH, n no puede ser 0; D representa una subunidad anti-inflamatoria no esteroidea o una subunidad esteroidea y las sales farmacéuticamente aceptables de la anteriores y las composiciones farmacéuticamente aceptables que contienen las anteriores. It also refers to pharmaceutically acceptable salts and solvates of such compounds prepared for processing, and intermediates for their preparation, as well as for the optimized therapeutic action and use in the treatment of diseases and inflammatory conditions in humans and animals. Claim 1: A compound according to formula (1), wherein: M represents the macrolide subunit of the substructure of formula (2), wherein: R1, R2, R3, R4 and R5 are independently selected from each other, from the group consisting of hydrogen C1-4 alkyl, alkanoyl, alkoxycarbonyl, arylmethoxycarbonyl, aryl, arylalkyl, alkylsilyl and alkylsilylalkoxyalkyl; RN represents the covalent bond with X1 of the L chain; L represents the substructure chain: -X1- (CH2) m-Q- (CH2) n-X2-, where: X1 is -CH2- or -C (O) -; X2 ...

Use of benzonaphthoazulenes for the manufacture of pharmaceutical formulations for the treatment and prevention of central nervous system diseases and disorders

The present invention relates to the use of compounds from the group of benzonaphthoazulenes and of their pharmaceutically acceptable salts and solvates 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 transmitters, and to methods of manufacture of such compounds.

Use of cell-specific conjugates for treatment of inflammatory diseases of the gastrointestinal tract

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.

1,2-diaza-dibenzoazulen as inhibitor of production of tumor necrosis factors and intermediates for preparation thereof

New compounds, preparations and methods for the treatment of inflammatory diseases and conditions

1-or 3-thia-benznaphthoazulenes as inhibitors of tumour necrosis factor production and intermediates for the preparation thereof

The present invention relates to 1- or 3-thiabenzonaphthoazulene derivafives 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-alpha (TNF-alpha) production and the inhibition of interleukin-1 (IL-1) production as well as to their analgetic action.

Novel nonsteroidal anti-inflammatory substances, compositions and methods for their use

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 activit y (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 t he treatment of inflammatory diseases and conditions in humans and animals.</SD OAB>

2-thia-dibenzoazulenes as inhibitors of tumour necrosis factor production and intermediates for the preparation thereof

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-alpha(TNF-alpha) production and the inhibition of interleukin-1 (IL-1) production as well as to their analgetic action.

1-aza-dibenzoazulenes as inhibitors of tumour necrosis factor production and intermediates for the preparation thereof

The present invention relates to 1-aza-dibenzoazulene derivatives of formula I, to their pharmacologically acceptable salts and solvates, to process and intermediates for the preparation thereof as well as to their antiinflammatory effects, especially to the inhibition of tumour necrosis factor-.alpha. (TNF-.alpha.) production and the inhibition of interleukin-1 (IL-1) production as well as to their analgetic action. Wherein X may be CH2 or a hetero atom such as 0, S, S(=0), S(=0)2, or NRa, wherein Ra is hydrogen or a protecting group; RI may be hydrogen, halogen, an optionally substituted C1-C7 alkyl or C2-C7 alkenyl, C2-C7 alkinyl, an optionally substituted aryl or heteroaryl and a heterocycle, hydroxy, hydroxy-C2-C7 alkenyl, hydroxy-C2-C7 alkinyl, C1-C7 alkoxy, thiol, thio-C2-C7 alkenyl, thio-C2-C7 alkinyl, C1-C7 alkylthio, amino, N-(C1~-C7)alkylamino, N,N-di(C1-C7-a1kyl)amino, (C1-C7-alkyl)amino, amino-C2-C7 alkenyl, amino-C2-C7 alkinyl, amino-C1,-C7 alkoxy, C1-C7 alkanoyl, aroyl, oxo~C1-C7 alkyl, C1-C7 alkanoyloxy, carboxy, an optionally substituted C1-C7 alkyloxycarbonyl or aryloxycarbonyl, carbamoyl, N-(C1-C7-alkyl)carbamoyl, N,N-di(C1-C7-alkyl)carbamoyl, cyano, cyano-C1-C7 alkyl, sulfonyl, C1-C7 alkylsulfonyl, sulfinyl, C1-C7 alkylsulfinyl, nitro, or a substituent of the formula II.

Conjugates of immune cell specific macrolide compounds with anti-inflammatory compounds for improved cellular targeting of anti-inflammatory therapy

Pronalazak se odnosi na nova jedinjenja prikazana strukturom I, i na njihove farmaceutske preparate, za lečenje inflamatornih jedinjenja kod ljudi i životinja.[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.

New compounds, compositions and methods for treatment of inflammatory diseases and conditions

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 t he treatment of inflammatory diseases and conditions in humans and animals. Suc h 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-.alpha.. Importantly, anti-inflammatory steroids exert a direct anti-inflammatory effect through binding to the glucocorticosteroid receptor.

2-thia-dibenzoazulenes as inhibitors of tumour necrosis factor production and intermediates for the preparation thereof

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-α (TNF-α) production and the inhibition of interleukin-1 (IL-1) production as well as to their analgetic action.

Anti-inflammatory macrolide conjugates

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 dibenzo[e,/z]azulene subunit with anti-inflammatory, analgesic and/or antipyretic activity 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.

Substituted furochromene compounds of antiinflammatory action

The present invention relates to novel compounds of the formula (I) including all stereoisomers and tautomers, 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.

1-Thia-3-aza-dibenzoazulenes as inhibitors of tumour necrosis factor production and intermediates for the preparation thereof

1,2-Diaza-dibenzo[e,h]azulenes for the treatment of central nervous system diseases and disorders

The present invention relates to the use of compounds from the group of 1,2-diaza-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.

1-oxa-3-aza-dibenzoazulenes as inhibitors of tumour necrosis factor production and intermediates for the production thereof

The present invention relates to derivatives of 1-oxa-3-aza-dibenzoazulene class, to their pharmacologically acceptable salts and solvates, to processe s and intermediates for the preparation thereof as well as to their antiinflammatory actions, especially to the inhibition of tumour necrosis factor-.alpha. (TNF-.alpha.) production and the inhibition of interleukin-1 (IL-1) production as well as to their analgetic action.

1-OR 3-THIA-BENZONAPHTHOAZULENE AS INHIBITORS OF THE PRODUCTION OF TUMOR NECROSIS FACTOR AND INTERMEDIATE PRODUCTS FOR THEIR PREPARATION

Macrolide-conjugates with anti-inflammatory activity

The present invention relates to new compounds represented by Formula (I); wherein M represents a macrolide subunit of the substructure II, Formula (II); L represents the chain of the substructure III, Formula (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 processe 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.

1,2-DIAZA-DIBENZOAZULENOS FOR THE INHIBITION OF THE PRODUCTION OF THE TUMOR NECROSIS AND INTERMEDIARY FACTOR FOR PREPARATION

Derivados de 1,2-diaza-dibenzoazuleno, sus sales y solvatos farmacéuticamente aceptables, procedimientos e intermediarios para su preparación, como así también sus acciones antiinflamatorias, especialmente a la inhibición de la producción del factor-? de necrosis tumoral (TNF-a), y la inhibición de la producción de interleucina-1 (IL-1) como así también a su acción analgésica. Reivindicación 1: Compuestos de fórmula (1) caracterizados porque X puede ser CH o un heteroátomo tal como O, S, S(=O), S(=O)2, o NRa, donde Ra es H o un grupo protector; Y y Z independientemente entre sí denotan uno o más sustituyentes idénticos o diferentes unidos a cualquier átomo de C disponible, y pueden ser halógeno, C1-4 alquilo, C2-4 alquenilo, C2-4 alquinilo, halo-C1-4 alquilo, hidroxi, C1-4 alcoxi, trifluorometoxi, C1-4 alcanoilo, amino, amino-C1-4 alquilo, N-(C1-4-alquilo)amino, N,N-di(C1-4-alquilo)amino, tiol, C1-4 alquiltio, sulfonilo, C1-4 alquilosulfonilo, sulfinilo, C1-4 alquilosulfinilo, carboxi, C1-4 alcoxicarbonilo, ciano, nitro; R1 puede ser halógeno, un heteroarilo o heterociclo opcionalmente sustituido, hidroxi, C1-7 alcoxi, ariloxi, amino, N-(C1-7) alquiloamino, N,N-di( C1-7-alquilo)amino, (C1-7-alquilo)amino, amino-C1-7 alcoxi, C1-7 alcanoilo, aroilo, C1-7 alcanoiloxi, carboxi, C1-7 alquiloxicarbonilo o ariloxicarbonilo opcionalmente sustituido, carbamoilo, N-(C1-7-alquilo) carbamoilo, N,N-di (C1-7-alquilo)carbamoilo, ciano, nitro, o un sustituyente de fórmula (2) donde R3 y R4 simultánea o independientemente entre sí pueden ser H, C1-4 alquilo, arilo o junto con N tienen el significado de un heterociclo o heteroarilo opcionalmente sustituido; m y n representan un entero de 0 a 3; Q1 y Q2 representan, independientemente entre sí, O, S o grupos de fórmulas (3) donde los sustituyentes Y1 e Y2 independientemente entre sí pueden ser H, halógeno, C1-4 alquilo o arilo opcionalmente sustituidos, hidroxi, C1-4 alcoxi, C1-4 alcanoilo, tiol, C1-4 alquiltio, sulfonilo, C1-4 ...

USE OF 1,3-DIAZA-DIBENZO[e,h] AZULENES FOR THE MANUFACTURE OF PHARMACEUTICAL FORMULATIONS FOR THE TREATMENT AND PREVENTION OF CENTRAL NERVOUS SYSTEM DISEASES AND DISORDERS

The present invention relates to the use of compounds from the group of 1,3-diaza-dibenzo[e,h]azulenes and of their pharmaceutically acceptable salts and solvates for the 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.

Novel nonsteroidal anti-inflammatory substances, compositions and methods for their use

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.

Conjugates with anti-inflammatory activity.

La presente invencion se refiere a nuevos compuestos representados por la formula I (ver formula I): en donde M representa una subunidad macrolida de la subestructura VIII; L representa la cadena de la subestructura IX o XIII; Z representa al subunidad esferoidal o no esferoidal derivada de farmacos esferoidales o no esferoidales (NSAID) con actividad antiinflamatoria; la presente invencion se refiere tambien a sales y solvatos farmaceuticamente aceptables de dichos compuestos preparados, a procedimientos e intermedios para su preparacion, asi como a la accion terapeutica mejorada y al uso en el tratamiento de enfermedades y condiciones inflamatorias en humanos y animales.

Use of benzonaphthoazulenes for the manufacture of pharmaceutical formulations for the treatment and prevention of central nervous system diseases and disorders

The present invention relates to the use of compounds from the group of benzonaphthoazenes and of their pharmaceutically 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 transmitters.

Darstellung von 1-aza-2-oxadibenzoäe,hüazulenen und deren verwendung bei der herstellung pharmazeutischer formulierungen zur behandlung und prävention von krankheiten und erkrankungen des zentralen nervensystems

Macrolid-konjugate mit entzündungshemmender wirkung

Konjugate von immunzellspezifischen makrolidverbindungen mit anti-phlogistischen verbindungen zur verbesserten zellgerichteten anti-phlogistischen therapie

1- oder 3-thia-benzonaphthoazulene als inhibitoren der produktion von tumornekrosefaktor und zwischenprodukte für deren herstellung

Konjugate mit entzündungshemmender aktivität

Hybridmoleküle von makroliden mit steroidalen/nicht-steroidalen antientzündlich aktiven molekülen

2-θεια-διβενζοαζουλενια ως αναστολεις της παραγωγης του παραγοντα νεκρωσης ογκων και ενδιαμεσα για την παρασκευη αυτων

Η παρούσα εφεύρεση σχετίζεται με ενώσεις της κατηγορίας 2-θεια-διβενζοαζουλενίων, με τα φαρμακολογικώς αποδεκτά άλατα και επιδιαλυτωμένα παράγωγα αυτών, με διεργασίες και ενδιάμεσα για την παρασκευή αυτών καθώς και με τις αντιφλεγμονώδεις επιδράσεις τους, ειδικά με την αναστολή της παραγωγής του παράγοντα νέκρωσης όγκων-α (TNF-α) και την αναστολή της παραγωγής της ιντερλευκίνης-1 (IL-1) καθώς και με την αναλγητική δράση αυτών.

2-thia-dibenzoazulene als inhibitoren der produktion von tumornekrosefaktor und zwischenprodukte für deren herstellung

Thiadibenzoazulenderivate zur behandlung von entzündlichen erkrankungen

1,2-diaza-dibenzoazulene als inhibitoren der produktion von tumornekrosefaktor und zwischenprodukte für deren herstellung

1-azadibenzoazulene als inhibitoren der produktion von tumornekrosefaktor und zwischenprodukte für deren herstellung

1-oxa-3-aza-dibenzoazulene als inhibitoren der produktion von tumornekrosefaktor und zwischenprodukte für deren herstellung

Verwendung von 1,2-diazadibenzoäe,hüazulenen zur herstellung von pharmazeutischen formulierungen für die behandlung und prävention von erkrankungen und störungen des zentralen nervensystems

Compuestos derivados de 1-tiadibenzozuleno sustituidos; procedimiento de preparacion; composicion farmaceutica; y uso del compuesto en el tratamiento de artritis reumatoide, espondilitis reumatoide, osteoartritis, eczemas, psoriasis y asma.

Verwendung von 1,3-diazadibenzo(e,h) azulenen zur herstellung von pharmazeutischen formulierungen für die behandlung und prävention von erkrankungen und störungen des zentralen nervensystems

1,3-diaza-dibenzoazulene als inhibitoren der produktion von tumornekrosefaktor und zwischenprodukte für deren herstellung

Ενωσεις θειενοδιβενζοαζουλενιου ως αναστολεις παραγοντα νεκρωσης ογκου

Η παρούσα εφεύρεση αφορά τις νέες ενώσεις διβενζοαζουλενίου που αντιπροσωπεύονται από τον τύπο I, καθώς και τα φαρμακευτικά παρασκευάσματα αυτών για την αναστολή του άλφα παράγοντα νέκρωσης όγκου (TNF-α) και της ιντερλευκίνης 1 (IL-1) σε θηλαστικά σε όλες τις ασθένειες και καταστάσεις όπου αυτοί οι μεσολαβητές εκκρίνονται υπερβολικά. Οι ενώσεις της παρούσας εφεύρεσης επίσης παρουσιάζουν αναλγητική δράση και μπορεί να χρησιμοποιούνται για την ανακούφιση πόνου.

Thienodibenzazulenverbindungen als tumornekrosefaktorhemmer

Use of 3-aza-1-oxa-dibenzo Äe,hÜ azulenes for the manufacture of pharmaceutical formulations for thetreatment and prevention of central nervous syste m disease and disorders

1-oxa-dibenzoazulenes as inhibitors of tumour necrosis facto production and intermediates for the preparation thereof

Ovaj pronalazak se odnosi na derivate 1-oksa-dibenzoazulena, na njihove farmaceutski prihvatljive soli i rastvore, na procese i intermedijere za njihovu proizvodnju, kao i na njihove antiinflamatorne efekte, posebno na inhibiciju produkcije tumor nekrotičnog faktora - α (TNF-α) i produkciju interleukina-1 (IL-1) kao i na njihovo analgetičko delovanje.

Verwendung von 3-aza-aoxa-dibenzo(e,h)azulenen zur herstellung von pharmazeutischen formulierung für die behandlung und prävention von erkrankungen und störungen des zentralen nervensystems

Verwendung von 2-thia-dibenzo(e,h)azulenen zur behandlung und prävention von erkrankungen und störungen des zentralen nervensystems

Verwendung von 1-thiadibenzo e,h azulenen zur herstellung von pharmazeutischen formulierungen für die behandlung und prävention von erkrankungen und störungen des zentralen nervensystems

Thiadibenzoazulene derivatives for the treatment of inflammatory diseases

The present invention relates to novel 1-thia-dibenzoazulene derivatives of the formula (I), wherein X individually denotes a hetero atom -O- or -S-; Y and Z independently from each other individually denote a fragment of the formula (II) to their pharmacologically acceptable esters, salts and solvates, to processes and intermediates for the preparation thereof, to a process for preparing pharmaceutical formulations for the treatment of inflammatory diseases and conditions and to the use thereof in the treatment of inflammatory diseases and conditions in humans and animals. These compounds inhibit tumour necrosis factor-α(TNF-(α) production and interleukin-1 (IL-1) production and exhibit an analgetic action.

1-oxa-dibenzoazulenes as inhibitors of tumor necrosis factor production and intermediates for the preparation thereof

1-oxa-dibenzoazulenes as inhibitors of tumor necrosis factor production and intermediates for the preparation thereof

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-cc (TNF-(x) production and the inhibition of interleukin-1 (IL-1) production as well as to their analgetic action.

1-oxa-dibenzoazulenes as inhibitors of tumor necrosis factor production and intermediates for the preparation thereof

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-cc (TNF-(x) production and the inhibition of interleukin-1 (IL-1) production as well as to their analgetic action.

USE OF 3-AZA-1-OXA-DIBENZO i e,h /i AZULENES FOR TH E MANUFACTURE OF PHARMACEUTICAL FORMULATIONS FOR THE TREATMENT AND PREVENTION OF CENTRAL NERVOUS SYSTEM DISEAS AND DISORDERS

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.

Use of 3-aza-1-oxa-dibenzo [e,h] azulenes for the manufacture of pharmaceutical formulations for the treatment and prevention of central nervous system diseases and disorders

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.

USE OF 3-AZA-1-OXA-DIBENZO [e,h] AZULENES FOR THE MANUFACTURE OF PHARMACEUTICAL FORMULATIONS FOR THE TREATMENT AND PREVENTION OF CENTRAL NERVOUS SYSTEM DISEAS AND DISORDERS

The present invention relates to the use of compounds from the group of 3-aza-l-oxa­dibenzo[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.

Use of 2-thia-dibenzo(e,h) azulenes for the treatment and prevention of central nervous system diseaes and disorders

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.

Verwendung von 1-oxadibenzo äe,hü azulenen zur herstellung von pharmazeutischen formulierungen für die behandlung und prävention von erkrankungen und störungen des zentralen nervensystems

Tetracyclic monoamine reuptake inhibitors for treatment of cns diseases and disorders

Novel tetracyclic dibenzo (e,h) azulene compounds of formula (I); their pharmacologically acceptable derivatives; pharmaceutical compositions containing them and their activity and use in the treatment of central nervous system (CNS) diseases and conditions in humans and animals.

1,3-diaza-dibenzoazulenes as inhibitors of tumour necrosis factor production and intermediates for the preparation thereof

The present invention relates to 1,3-diaza-dibenzoazulene derivatives of formula (I), 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-α (TNF-α) production and the inhibition of interleukin-1 (IL-1) production as well as to their analgetic action.

1,3-diaza-dibenzoazulenes as inhibitors of tumour necrosis factor production and intermediates for the preparation thereof

Predmetni pronalazak se odnosi na derivate 1,3-diaza-dibenzoazuletna, na njihove farmakološki prihvatljive soli i solvate, na procese i međuproizvode za njihovo dobijanje, kao i na njihova antiinflamatorna dejstva, a naročito na inhibiciju stvaranja faktora - α tumorske nekroze (TNF - α) i inhibiciju stvaranja interleukina - 1 (IL -1), te na njihovo analgetsko dejstvo.

Furochromene derivative with anti-inflammatory activity

This invention relates to the novel compound of formula (I): and pharmaceutically acceptable salts and solvates thereof; to the processes and reactive intermediates for the preparation of this compound, pharmaceutical compositions which contain this compound, and the use of this compound in prophylaxis and therapeutic treatment of asthma as well as other diseases, disorders or conditions of human immune system.

Substituted furochromenes, preparation thereof and their antiinflammatory action

The invention relates to novel compounds of formula (I) including all their tautomers to pharmaceutically acceptable salts and solvates thereof, to processes and reactive intermediates for the preparation thereof; to processes and reactive intermediates for the preparation of compounds of 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.

Substituted furochromenes, preparation thereof and their antiinflammatory action

The invention relates to novel compounds of formula (I) including all their tautomers to pharmaceutically acceptable salts and solvates thereof, to processes and reactive intermediates for the preparation thereof; to processes and reactive intermediates for the preparation of compounds of 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.

Substituted furochromenes, preparation thereof and their antiinflammatory action

The invention relates to novel compounds of formula (I) including all their tautomers to pharmaceutically acceptable salts and solvates thereof, to processes and reactive intermediates for the preparation thereof; to processes and reactive intermediates for the preparation of compounds of 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.