Title:
新規なプリン誘導体、それらの製造方法、医薬品としての適用、薬学的組成物、および新規な使用
Document Type and Number:
Japanese Patent JP2006517955
Kind Code:
A
Abstract:
Purine derivatives (I), are new. Purine derivatives of formula (I), their racemic mixtures, enantiomers, diastereoisomers and salts with acids and bases, are new. [Image] Y : N, O, S, CHR 3or =CR 3; R, R 1upto 6C alkyl or upto 6C alkoxy (both optionally substituted by at least one T), or aryl or heteroaryl (both optionally substituted by at least one T or T 1and optionally aryl substituted by dioxolyl), H, halo, OH, , CN, NO 2, NR 4R 5, CF 3, CF 3O, or S(O) n-NR 4R 5; n : 0-2; R 3upto 6C alkyl (optionally substituted by at least one T) or aryl (optionally substituted by at least one T, T 1or dioxolyl), H, halo, CN, NO 2, NR 4R 5, CF 3or CF 3O; R 2R 4, OR 4, SR or NR 4R 5; R 4, R 5upto 6C alkyl or upto 6C cycloalkyl (both optionally substituted by at least one T) or aryl (optionally substituted by at least one T, T 1or dioxolyl), or H, or NR 4R 54-6 membered heterocyclyl optionally containing at least one O, N or S heteroatom (optionally substituted by at least one T or T 1); T : halo, OH, CN, CF 3, CF 3O, upto 6C alkoxy, aryl, heterocyclyl, acid groups, NHR 4, N-alkyl-R 4, COR 4, COOR 4, CON-(upto 6C alkyl)-R 4or CONHR 4, and T 1alkyl, hydroxyalkyl or phenylalkyl. An independent claim is also included for the preparation of (I). ACTIVITY : Fungicide; Dermatological; Antipsoriatic; Cytostatic; Nootropic; Neuroprotective; Antiallergic; Immunosuppressive; Vasotropic; Antiinflammatory; Cardiovascular-Gen. MECHANISM OF ACTION : Protein kinase inhibitor. In a test for determining inhibition of JNK3 kinase, results showed that trans-N-[6-(5,6-dichloro-2,3-dihydro-1H-indol-1-yl)-9H-purin-2-yl]-1,4-cyclohexane diamine dihydrochloride (Ia) exhibited an IC 50value of 0.29 mu M.
Inventors:
Florence Boldon-Parrier
Jean-Luc Heslen
Jean-Luc Heslen
Application Number:
JP2006502145A
Publication Date:
August 03, 2006
Filing Date:
February 13, 2004
Export Citation:
Assignee:
Aventis Pharma Societe Anonym
International Classes:
C07D473/16; A61K31/52; A61P9/00; A61P17/06; A61P25/00; A61P25/28; A61P25/34; A61P29/00; A61P31/04; A61P31/10; A61P33/00; A61P33/02; A61P35/00; A61P37/00; A61P37/02; A61P43/00
Domestic Patent References:
| JP2003500407A | 2003-01-07 | |||
| JPH10508875A | 1998-09-02 | |||
| JP2003500407A | 2003-01-07 |
Foreign References:
| WO2002042303A2 | 2002-05-30 | |||
| WO2002051843A1 | 2002-07-04 | |||
| WO2002042303A2 | 2002-05-30 | |||
| WO2002051843A1 | 2002-07-04 |
Other References:
JPN6010038978, Ｍ． ＨＡＩＤＯＵＮＥ ｅｔ ａｌ．, Ｊ． Ｈｅｔｅｒｏｃｙｃ Ｃｈｅｍ．, 1994, Ｖｏｌ．３１, ｐ．１４６１−４
JPN7010002127, Ｃｈｅｍｉｃａｌ Ａｂｓｔｒａｃｔｓ, 1961, Ｖｏｌ．５５, ｃｏｌｕｍｎ ２２３２４ｅ−ｉ，２２３２５ａ−ｉ，２２３２６ａ−ｇ
JPN7010002127, Ｃｈｅｍｉｃａｌ Ａｂｓｔｒａｃｔｓ, 1961, Ｖｏｌ．５５, ｃｏｌｕｍｎ ２２３２４ｅ−ｉ，２２３２５ａ−ｉ，２２３２６ａ−ｇ
Attorney, Agent or Firm:
Chika Takagi
Junji Yuda
Shoji Miwa
Junji Yuda
Shoji Miwa