| 摘要 |
Triazolo-quinoline derivatives are new. Triazolo-quinoline derivatives of formula (I), their salts, solvates and optically active isomers and the salts or solvates are new. [Image] R 1> and R 2>H or straight or branched 1-4C alkyl; R 3>straight or branched 1-4C alkyl, phenyl, thienyl, furyl (optionally substituted by at least one straight or branched 1-4C alkyl, straight or branched 1-4C alkoxy or halo), H, 5 - 6 membered heteroaromatic ring containing 1 - 3 N atom or 5-membered heteroaromatic ring containing one nitrogen atom and one oxygen atom or one nitrogen atom and one sulfur atom (optionally substituted by at least one straight or branched 1-4C alkyl, straight or branched 1-4C alkoxy or halo); R 4> and R 5>H; R 4>+R 5>1,3-butadienyl (optionally substituted by methylenedioxy or at least one straight or branched 1-4C alkyl, straight or branched 1-4C alkoxy, OH or halo); R 6>H, cyano, aminocarbonyl, 1-4C alkoxycarbonyl or carboxy; R 7>phenyl, benzyl, thienyl, furyl (all 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 or 1-4C alkylene (optionally substituted by phenyl), amino, mono- or dialkylamino, 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 (optionally substituted by at least one straight or branched 1-4C alkyl, straight or branched 1-4C alkoxy or halo); X : -CH 2-, -NH-, -NR 1> 2>-, S, O, sulfo or sulfoxy; R 1> 2>a straight or branched 1-4C alkyl or 3-6C cycloalkyl; and n : 0 - 2. Independent claims are also included for: (1) Preparation of (I); and (2) New intermediate, 1,2-diamino-pyridium salt of formula (II). [Image] ACTIVITY : Cardiant; Nephrotropic; Antiallergic; Antiinflammatory; Dermatological; Antipsoriatic; Hypotensive; Ophthalmological; Antidiabetic; Antiasthmatic; Immunosuppressive; Antirheumatic; Cytostatic; Vasotropic; Antiarrhythmic. MECHANISM OF ACTION : Adenosine A 3 receptor antagonist. The compounds were tested for adenosine A 3 receptor antagonistic activity using HEK-293 cells. Test details are described but no results for the specific compounds given. In general compound (I) showed a K i of 3.5 and 0.78 nM. |
