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1. WO2003097648 - 1-AZA-DIBENZOAZULENES AS INHIBITORS OF TUMOUR NECROSIS FACTOR PRODUCTION AND INTERMEDIATES FOR THE PREPARTION THEREOF

Publication Number WO/2003/097648
Publication Date 27.11.2003
International Application No. PCT/HR2003/000026
International Filing Date 20.05.2003
Chapter 2 Demand Filed 01.12.2003
IPC
C07D 491/04 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
491Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/-C07D459/290
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
C07D 495/04 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
495Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
CPC
A61P 1/04
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
1Drugs for disorders of the alimentary tract or the digestive system
04for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
A61P 11/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
11Drugs for disorders of the respiratory system
06Antiasthmatics
A61P 17/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
17Drugs for dermatological disorders
A61P 17/04
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
17Drugs for dermatological disorders
04Antipruritics
A61P 19/02
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
19Drugs for skeletal disorders
02for joint disorders, e.g. arthritis, arthrosis
A61P 19/08
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
19Drugs for skeletal disorders
08for bone diseases, e.g. rachitism, Paget's disease
Applicants
  • PLIVA - ISTRAZIVACKI INSTITUT D.O.O. [HR]/[HR] (AllExceptUS)
  • MERCEP, Mladen [HR]/[HR] (UsOnly)
  • MESIC, Milan [HR]/[HR] (UsOnly)
  • PESIC, Dijana [HR]/[HR] (UsOnly)
Inventors
  • MERCEP, Mladen
  • MESIC, Milan
  • PESIC, Dijana
Agents
  • PLIVA - ISTRAZIVACKI INSTITUT D.O.O.
Priority Data
P20020440A21.05.2002HR
Publication Language English (en)
Filing Language English (EN)
Designated States
Title
(EN) 1-AZA-DIBENZOAZULENES AS INHIBITORS OF TUMOUR NECROSIS FACTOR PRODUCTION AND INTERMEDIATES FOR THE PREPARTION THEREOF
(FR) 1-AZA-DIBENZOAZULENES UTILISES COMME INHIBITEURS DE PRODUCTION DU FACTEUR DE NECROSE TUMORALE, ET INTERMEDIAIRES SERVANT A LEUR PREPARATION
Abstract
(EN) 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-&agr; (TNF-&agr;) 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, oxo­C1-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.
(FR) La présente invention concerne des dérivés de 1-aza-dibenzoazulène de formule (I), leurs sels et solvats pharmacologiquement acceptables, une méthode et des intermédiaires destinés à leur préparation ainsi que leurs effets inflammatoires, en particulier l'inhibition de la production du facteur de nécrose tumorale alpha (TNF-?) et l'inhibition de la production de l'interleukine 1 (IL-1) ainsi que leur action analgésique. Dans ladite formule, X peut être CH2 ou un hétéroatome tel que 0, S, S(=0), S(=0)2, ou NRa (Ra étant hydrogène ou un groupe protecteur); RI peut être hydrogène, halogène, un alkyle C1-C7 ou alcényle C2-C7 éventuellement substitué, alkinyle C2-C7, un aryle ou hétéroaryle éventuellement substitué et un hétérocycle, hydroxy, hydroxy-alcényle C2-C7, hydroxy-alkinyle C2-C7, alkoxy C1-C7, thiol, thio-alcényle C2-C7, thio-alkinyle C2-C7, alkylthio C1-C7, amino, N-alkylamino(C1-C7), N,N-di(alkyle C1-C7)amino, (alkyle C1-C7)amino, amino-alcényle C2-C7, amino-alkinyle C2-C7, amino-alkoxy C1-C7, alcanoyle C1-C7, aroyle, oxo-alkyle C1-C7, alcanoyloxy C1-C7, carboxy, alkyloxycarbonyle ou aryloxycarbonyle C1-C7 éventuellement substitué, carbamoyle, N-(alkyle C1-C7)carbamoyle, N,N-di(alkyle C1-C7)carbamoyle, cyano, cyano-alkyle C1-C7, sulfonyle, alkylsulfonyle C1-C7, sulfinyle, alkylsulfinyle C1-C7, nitro, ou un substituant de formule (II).
Related patent documents
YUP-995/04This application is not viewable in PATENTSCOPE because the national phase entry has not been published yet or the national entry is issued from a country that does not share data with WIPO or there is a formatting issue or an unavailability of the application.
IS7569This application is not viewable in PATENTSCOPE because the national phase entry has not been published yet or the national entry is issued from a country that does not share data with WIPO or there is a formatting issue or an unavailability of the application.
IN2861/CHENP/2004This application is not viewable in PATENTSCOPE because the national phase entry has not been published yet or the national entry is issued from a country that does not share data with WIPO or there is a formatting issue or an unavailability of the application.
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