Title:
1-ベンジルピラゾール誘導体、その調製方法および治療的使用
Document Type and Number:
Japanese Patent JP2010529093
Kind Code:
A
Abstract:
1-Benzylpyrazole compounds (I) and their acid or base addition salts, hydrates or solvates are new. 1-Benzylpyrazole compounds of formula (I) and their acid or base addition salts, hydrates or solvates are new. Y 1-N(R 7)CO-, -N(R 7)CO-N(R 7)-, -OCO- or -N(R 7)S(O) n; R 1H or 1-4C alkyl; R 2, R 4H, halo, 1-4C alkyl, 1-4C alkoxy or -CF 3; R 3, R 5halo, 1-4C alkyl, 1-4C alkoxy, -CF 3, -OCF 3, CN or S(O) mAlk; R 61-6C alkyl (optionally substituted by one or more substituents comprising halo, OH, 1-4C alkoxy or OCF 3), phenyl (optionally substituted by R 8), benzyl or benzhydryl, heterocyclic radical comprising thienyl, furyl or pyrrolyl (optionally substituted by halo, 1-4C alkyl or CF 3), 3-12C non-aromatic carbocyclic radical (optionally substituted by one or more halo, 1-4C alkyl, 1-4C alkoxy, OH or CN), 3-7C cycloalkylmethyl (optionally substituted by one or more 1-4C alkyl) or aryloxymethyl (optionally substituted on methyl by one or more two alkyl groups, in which aryloxy represents phenoxy group (optionally substituted by one or more R 8)); R 7H or 1-4C alkyl; R 8halo, 1-4C alkyl, CF 3, CN, 1-4C alkoxy, OCF 3, phenyl, 3-7C cycloalkyl or NHS(O) nAlk; n : 1 or 2; m : 0-2; and Alk : 1-4C alkyl. Independent claims are included for: (1) the preparation of (I); and (2) a substituted 1-benzylpyrazole compound of formula (XII). W 1OH or NH 2; and R 3, R 5halo, 1-4C alkyl, 1-4C alkoxy or -CF 3. [Image] [Image] ACTIVITY : Immunomodulator; Analgesic; Gastrointestinal-Gen; Cardiovascular-Gen; Nephrotropic; Cytostatic. MECHANISM OF ACTION : Cannabinoid receptor antagonist. The ability of (I) to inhibit cannabinoid receptor was tested in cell lines. The result showed that (I) exhibited an IC 5 0 value of 0.1-500 nM.
Inventors:
Baltic, francis
Brieu, Laurent
Milan, Joseph
Rinal Day-Carmona, Miuriel
Brieu, Laurent
Milan, Joseph
Rinal Day-Carmona, Miuriel
Application Number:
JP2010510841A
Publication Date:
August 26, 2010
Filing Date:
June 02, 2008
Export Citation:
Assignee:
Sanofui-Aventice
International Classes:
C07D231/12; A61K31/415; A61P1/00; A61P9/00; A61P13/12; A61P25/04; A61P35/00; A61P37/02; A61P43/00; C07D405/12; C07D409/12
Domestic Patent References:
| JP2000502080A | 2000-02-22 |
Foreign References:
| FR2887550A1 | 2006-12-29 |
Attorney, Agent or Firm:
Yoshio Kawaguchi
Chihiro Watanabe
Katsuma Osaki
Mitsuaki Tsubokura
Chihiro Watanabe
Katsuma Osaki
Mitsuaki Tsubokura