Title:
アミノキノリンおよびアミノピリジン誘導体およびそのアデノシンA3リガンドとしての使用
Document Type and Number:
Japanese Patent JP4409935
Kind Code:
B2
Abstract:
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.
Inventors:
Allani, Peter
Barrage, Larslaw
Barrogue, Maria
Barta, Imre
Burtley, Shendle
The Nagyi, Layos
Teemari, Geza
Bohère, Kinga
Finance, olivier
Capui, Zoltan
Mixle, Endre
Samoshiyu Berujii, Jiujianjina
Seretukii, Garbol
Urban-Sabo, Catalin
Barrage, Larslaw
Barrogue, Maria
Barta, Imre
Burtley, Shendle
The Nagyi, Layos
Teemari, Geza
Bohère, Kinga
Finance, olivier
Capui, Zoltan
Mixle, Endre
Samoshiyu Berujii, Jiujianjina
Seretukii, Garbol
Urban-Sabo, Catalin
Application Number:
JP2003500059A
Publication Date:
February 03, 2010
Filing Date:
May 29, 2002
Export Citation:
Assignee:
Sanofi-Aventis
International Classes:
C07D215/54; C07D401/12; C07D405/12; C07D405/14; C07D409/12; C07D409/14; A61K31/4706; A61K31/4709; 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
Domestic Patent References:
| JP53090297A | ||||
| JP53034800A | ||||
| JP55130961A | ||||
| JP2001114779A |
Foreign References:
| WO2000013681A1 | ||||
| WO2000013682A1 |
Attorney, Agent or Firm:
Yoshio Kawaguchi
Makoto Ono
Chihiro Watanabe
Kenkyo Kanayama
Katsuma Osaki
Mitsuaki Tsubokura
Makoto Ono
Chihiro Watanabe
Kenkyo Kanayama
Katsuma Osaki
Mitsuaki Tsubokura