Title:
BENZISOXAZOLE DERIVATIVES HAVING D4-ANTAGONISTIC ACTIVITY
Document Type and Number:
WIPO Patent Application WO1999040067
Kind Code:
A3
Abstract:
The present invention relates to a group of novel benzisoxazole derivatives which are potent and selective antagonists of the dopamine D4-receptor. The compounds have general formula (I) wherein (R1)n represents 0, 1, or 2 substituents, which can be the same or different, from the group C1-3-alkyl or alkoxy, halogen, trifluoromethyl, nitro, amino mono- or dialkyl (C1-2)-amino, sulfonyl-(C1-3)alkyl or -alkoxy, sulfonyl trifluoromethyl, sulfonyl amino, and sulfonyl mono- or dialkyl (C1-2)-amino, X is O, S, NH or NCH3, Y represents CH2 or (CH2)2, (R2)m represents 0, 1, or 2 substituents, which can be the same or different, from the group methyl and ethyl, or (R2)m is a methylene bridge or ethylene bridge, A is a group -CH2-(CRH)p- wherein R is hydrogen or methyl and p is 0 or 1, and B represents 2- or 3-indolyl or 2-benzimidazolyl, which groups may be substituted at carbon with 1 or 2 substituents from the group C-1-3-alkyl or alkoxy, halogen, trifluoromethyl, nitro, amino, mono- or dialkyl (C1-2)amino, sulfonyl-(C1-3)alkyl or -alkoxy, sulfonyl trifluoromethyl, sulfonyl amino, and sulfonyl mono- or dialkyl (C1-2)-amino.
Inventors:
DEN HARTOG JACOBUS A J (NL)
VISSER GERBEN M (NL)
VAN STEEN BARTHOLOMEUS J (NL)
TULP MARTINUS T M (NL)
RONKEN ERIC (NL)
KRUSE CORNELIS G (NL)
LANGE JOSEPHUS H M (NL)
VISSER GERBEN M (NL)
VAN STEEN BARTHOLOMEUS J (NL)
TULP MARTINUS T M (NL)
RONKEN ERIC (NL)
KRUSE CORNELIS G (NL)
LANGE JOSEPHUS H M (NL)
Application Number:
PCT/EP1999/000852
Publication Date:
November 25, 1999
Filing Date:
February 05, 1999
Export Citation:
Assignee:
DUPHAR INT RES (NL)
HARTOG JACOBUS A J (NL)
VISSER GERBEN M (NL)
STEEN BARTHOLOMEUS J VAN (NL)
TULP MARTINUS T M (NL)
RONKEN ERIC (NL)
KRUSE CORNELIS G (NL)
LANGE JOSEPHUS H M (NL)
HARTOG JACOBUS A J (NL)
VISSER GERBEN M (NL)
STEEN BARTHOLOMEUS J VAN (NL)
TULP MARTINUS T M (NL)
RONKEN ERIC (NL)
KRUSE CORNELIS G (NL)
LANGE JOSEPHUS H M (NL)
International Classes:
A61K31/445; A61K31/454; A61K31/55; A61P25/00; A61P25/16; A61P25/22; A61P25/24; A61P25/28; A61P43/00; C07D413/14; (IPC1-7): C07D413/14; A61K31/445
Domestic Patent References:
| WO1994027994A1 | 1994-12-08 | |||
| WO1999040067A2 | 1999-08-12 |
Foreign References:
| US4352811A | 1982-10-05 | |||
| EP0602242A1 | 1994-06-22 | |||
| EP0811622A1 | 1997-12-10 |
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