发明名称 |
AMINOQUINOLINE AND AMINOPYRIDINE DERIVATIVES AND THEIR USE AS ADENOSINE A3 LIGANDS |
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. |
申请公布号 |
WO02096879(A1) |
申请公布日期 |
2002.12.05 |
申请号 |
WO2002HU00048 |
申请日期 |
2002.05.29 |
申请人 |
SANOFI-SYNTHELABO;ARANYI, PETER;BALAZS, LASZLO;BALOGH, MARIA;BATA, IMRE;BATORI, SANDOR;T. NAGY, LAJOS;TIMARI, GEZA;BOER, KINGA;FINANCE, OLIVIER;KAPUI, ZOLTAN;MIKUS, ENDRE;SZAMOSVOELGYI, ZSUZSANNA;SZELECZKY, GABOR;URBAN-SZABO, KATALIN |
发明人 |
ARANYI, PETER;BALAZS, LASZLO;BALOGH, MARIA;BATA, IMRE;BATORI, SANDOR;T. NAGY, LAJOS;TIMARI, GEZA;BOER, KINGA;FINANCE, OLIVIER;KAPUI, ZOLTAN;MIKUS, ENDRE;SZAMOSVOELGYI, ZSUZSANNA;SZELECZKY, GABOR;URBAN-SZABO, KATALIN |
分类号 |
C07D215/54;A61K;A61K31/4706;A61K31/4709;A61P;A61P3/10;A61P9/00;A61P9/10;A61P9/12;A61P11/00;A61P11/06;A61P13/12;A61P17/06;A61P25/00;A61P25/16;A61P25/24;A61P27/06;A61P29/00;A61P35/00;A61P37/08;A61P43/00;C07D;C07D213/75;C07D213/85;C07D215/46;C07D215/48;C07D401/12;C07D405/12;C07D405/14;C07D409/12;C07D409/14 |
主分类号 |
C07D215/54 |
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