| 摘要 |
Aminoquinoline and aminopyridine derivatives (I) are new. Aminoquinoline and aminopyridine derivatives of formula (I), their optically active isomers, salts and solvates are new. [Image] R 1>, R 2>H or 1-4C alkyl; R 3>phenyl, thienyl, furyl (all optionally substituted by at least one 1-4C alkyl, 1-4C alkoxy or halo), 5-6 membered heteroaromatic ring (optionally substituted by 1-4C alkyl, 1-4C alkoxy or halo and containing either 1-3 N, N or S, or N or O atoms), H or R 1>; R 4>, R 5>H; or R 4>+R 5>1,3-butadienyl group optionally substituted by methylenedioxy, 1-4C alkyl, 1-4C alkoxy, halo or OH; R 6>H, CN, aminocarbonyl, 1-4C alkoxycarbonyl or carboxy; R 7>phenyl, benzyl, thienyl, furyl (all optionally substituted by at least one 1-4C alkyl, 1-4C alkoxy, halo, methylenedioxy, OH, CF 3 or CN), 5-6 membered heteroaromatic ring (optionally substituted by 1-4C alkyl, 1-4C alkoxy or halo and containing either 1-3 N, N or S, or N or O atoms) or H; X : -CH 2, -NH, -NR 8>, S, O, sulfo or sulfoxy group; R 8>1-4C alkyl or 3-6C cycloalkyl; and n : 0-2. Independent claims are also included for: (1) preparation of (I); and (2) intermediate compounds of formula (II)-(IV) (structures not given in the specification. ACTIVITY : Antiinflammatory; Antiallergic; Hypotensive; Dermatological; Antiarthritic; Immunosuppressive; Antipsoriatic; Ophthalmological; Antidiabetic; Antirheumatic; Vasotropic; Antiarrhythmic; Antiasthmatic; Cardiant; Nephrotropic; Antitumor. MECHANISM OF ACTION : Adenosine A3 Antagonist In tests, compounds (I) displayed K i values of 0.14-0.15 nM. No specific data given. |
