| 摘要 |
Imidazoquinoline derivatives (I), their salts, solvates and optically active isomers and salts or solvates, are new. Imidazoquinoline derivatives of formula (I), their salts, solvates and optically active isomers and salts or solvates, are new. [Image] R 1>, R 2>H or 1-4C alkyl; R 3>1-4C alkyl, 3-6C cycloalkyl, phenyl, thienyl, furyl (optionally substituted by at least one 1-4C alkyl, 1-4C alkoxy or halo), H, 5 - 6 membered heteroaromatic ring containing 1 - 3 N atoms or 5-membered heteroaromatic ring (containing one nitrogen atom and one oxygen atom or one nitrogen atom and one sulfur atom and optionally substituted by at least one 1-4C alkyl, 1-4C alkoxy or halo); R 4> - R 7>H, 1-4C alkyl, 1-4C alkoxy, OH or halo; or R 5>+R 6>methylenedioxy; R 8>H, cyano, aminocarbonyl, 1-4C alkoxycarbonyl or carboxy; R 9>, R 1> 0>T 1> or (CH 2) p-NR 1> 2>R 1> 3>; T 1>phenyl, phenyl-(1-4C)alkyl, thienyl-(1-4C)alkyl, furyl-(1-4C)alkyl (optionally substituted by methylenedioxy or at least one straight or branched 1-4C alkyl, straight or branched 1-4C alkoxy, OH, trifluoromethyl, cyano or halo), H, straight or branched 1-4C alkyl, 3-6C cycloalkyl, -(CH 2) m-OH, 5 - 6 membered heteroaromatic ring containing 1 - 3 N atoms or 5-membered heteroaromatic ring (containing one nitrogen atom and one oxygen atom or one nitrogen atom and one sulfur atom and optionally substituted by at least one straight or branched 1-4C alkyl, 1-4C alkoxy or halo); R 1> 2>, R 1> 3>T 1>; or NR 9>R 1> 0>, NR 1> 2>R 1> 3>3 - 7-membered heterocyclic group (optionally substituted by straight or branched 1-4C alkyl; X : -CH 2-, -NH-, -NR 1> 1>-, S, O, sulfo or sulfoxy; R 1> 1>1-4C alkyl or 3-6C cycloalkyl; n : 0 - 2; m : 1 - 4; p : 0 - 4; and provided that R 5>+R 6> is only methylenedioxy when R 4> and R 7> are H. Independent claims are also included for the following: (a) preparation of (I); and (b) new intermediates, imidazoquinoline acid compound of formula (II) and imidazoquinoline ester compound of formula (III). [Image] [Image] R 1> 4>1-4C alkyl. ACTIVITY : Cardiant; Nephrotropic; CNS Gen.; Respiratory Gen.; Antiallergic; Antiinflammatory; Dermatological; Antipsoriatic; Hypotensive; Ophthalmological; Antidiabetic; Antiasthmatic; Immunosuppressive; Antirheumatic; Cytostatic; Vasotropic; Antiarrhythmic; Antiparkinsonian; Antiarthritic; Antidepressant; Nootropic. MECHANISM OF ACTION : Adenosine A 3 Receptor Antagonist; Cytokine Production Inhibitor; TNF-alpha Release Inhibitor; Eosinophil, Neutrophil and Immune Cell Migration Inhibitor; Bronchoconstriction and Plasma Extravasation Inhibitor. The compounds were tested for adenosine A 3 receptor antagonistic activity using HEK293 cells. The general compound (I) showed a K i of 1.6 and 0.38 nM. No results for specific compounds given. |
