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US 2003/0153750 A1Published application
Thienodibenzoazulene compounds as tumor necrosis factor inhibitors
AssigneePLIVA, farmaceutska industrija, dionicko drustvo
InventorsMladen Mercep, Milan Mesic, Dijana Pesic, Zeljko Zupanovic, Boska Hrvacic
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Abstract
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.
Claims15
Dibenzoazulene derivatives, their pharmacologically acceptable salts and solvates represented by formula I
- 4
- characterized in that
- X can represent CH2 or a heteroatom such as O, S, S(═O), S(═O)2 or NR13, wherein R13 means hydrogen, C1-6 alkyl, C1-6 alkylcarbonyl, arylcarbonyl, C1-6 alkylsulfonyl or arylsulfonyl and R1, R2, R3, R4, R5, R6, R7, R8, R9 independently from each other represent substituents, which can be hydrogen, halogens (fluorine, chlorine or bromine);
- or C1-C7 alkyls, alkenyls, aryls or heteroaryls;
- or can represent different groups:
- halomethyl, hydroxy, C1-C7 alkoxy or aryloxy, C1-C7 alkylthio or arylthio, C1-C7 alkylsulfonyl, ciano, amino, mono- and di-C1-C7 substituted amines, derivatives of carboxylic group (C1-C7 carboxylic acids and their anhydrides, C1-C7 unsubstituted, mono-, di-substituted amides, C1-C7 alkyl or aryl esters), C1-C7 derivatives of carbonyl group (C1-C7 alkyl or aryl carbonyls), and R10 can represent substituents such as:
- C2-C15 alkyls, C2-C15 alkenyls, C2-C15 alkinyls, aryls or heteroaryls, C1-C15 haloalkyls, C1-C15 hydroxyalkyls, C1-C15 alkyloxy, C1-C15 alkylthio, C3-C15 alkylcarbonyls, C2-C15 alkylcarboxylic acid, C2-C15 alkylsters, C1-C15 alkylsulfonyls, C1-C15 alkylarylsulfonyls, arysulfonyls and C1-C15 alkylamines represented by the general formula
- —(CH2)n—A
- wherein
- n means l-15, and
- one or more methylene groups that can be substituted with an oxygen or sulfur atom, and
- A represents a five- or six-membered, saturated or unsaturated ring with one, two or three heteroatoms, or
- 5
- wherein R11 and R12 independently from each other represent hydrogen, C1-C7 alkyl, C alkenyl, alkinyl, aryl or heteroaryl, or a heterocycle with 1-3 beteroatoms.
11 more elements
Dependencies are inferred from the claim text.