IMRE BATA,MARIA BALOGH,SANDOR BATORI,ZOLTAN KAPUI,ENDRE MIKUS,LAJOS T. NAGY,LASZLO BALAZS,GEZA TIMARI,KING BOER,OLIVIER FINANCE,ZSUZSANNA SZAMOSVOELGYI,GABOR SZELECZKY,KATALIN URBAN-SZABO,PETER ARANYI
申请号：
IS7052
公开号：
IS2773B
申请日:
2003.11.26
申请国别(地区):
IS
年份:
2012
代理人:
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.
