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1. (WO2003097648) 1-AZA-DIBENZOAZULENES AS INHIBITORS OF TUMOUR NECROSIS FACTOR PRODUCTION AND INTERMEDIATES FOR THE PREPARTION THEREOF
Latest bibliographic data on file with the International Bureau   

Pub. No.: WO/2003/097648 International Application No.: PCT/HR2003/000026
Publication Date: 27.11.2003 International Filing Date: 20.05.2003
Chapter 2 Demand Filed: 01.12.2003
IPC:
C07D 491/04 (2006.01) ,C07D 495/04 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
491
Heterocyclic 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
02
in which the condensed system contains two hetero rings
04
Ortho-condensed systems
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
495
Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
02
in which the condensed system contains two hetero rings
04
Ortho-condensed systems
Applicants:
MERCEP, Mladen [HR/HR]; HR (UsOnly)
MESIC, Milan [HR/HR]; HR (UsOnly)
PESIC, Dijana [HR/HR]; HR (UsOnly)
PLIVA - ISTRAZIVACKI INSTITUT D.O.O. [HR/HR]; Prilaz baruna Filipovica 29 HR-10000 Zagreb, HR (AllExceptUS)
Inventors:
MERCEP, Mladen; HR
MESIC, Milan; HR
PESIC, Dijana; HR
Agent:
PLIVA - ISTRAZIVACKI INSTITUT D.O.O.; Attn. Kresimir Sarcevic Prilaz baruna Filipovica 29 HR-10000 Zagreb, HR
Priority Data:
P20020440A21.05.2002HR
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).
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Designated States: AE, AG, AL, AM, AT, AU, AZ, BA, BB, BG, BR, BY, BZ, CA, CH, CN, CO, CR, CU, CZ, DE, DK, DM, DZ, EC, EE, ES, FI, GB, GD, GE, GH, GM, HR, HU, ID, IL, IN, IS, JP, KE, KG, KP, KR, KZ, LC, LK, LR, LS, LT, LU, LV, MA, MD, MG, MK, MN, MW, MX, MZ, NI, NO, NZ, OM, PH, PL, PT, RO, RU, SC, SD, SE, SG, SK, SL, TJ, TM, TN, TR, TZ, UA, UG, US, UZ, VC, VN, YU, ZA, ZM, ZW
African Regional Intellectual Property Organization (ARIPO) (GH, GM, KE, LS, MW, MZ, SD, SL, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Office (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (EPO) (AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HU, IE, IT, LU, MC, NL, PT, RO, SE, SI, SK, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, ML, MR, NE, SN, TD, TG)
Publication Language: English (EN)
Filing Language: English (EN)