发明名称 PHENYLSULFONAMIDE-PHENYLETHYLAMINE DERIVATIVES AND USE THEREOF AS DOPAMINE RECEPTORS
摘要 1. Use of a compound of Formula 1 where in each R<1> is independently H or C1-8 alkyl; and R<2> and R<3> are independently H, C1-3 alkyl, halogen, OCH3, OCF3, CF3, CN, SCH3 or NHCOCH3; or a pharmaceutically acceptable salt thereof as an active ingredient for the manufacture of a medicament for treating a central nervous system disorder associated with dopamine D3 receptors. 2. The use of Claim 1, wherein each R<1> is independently H or C1-6 alkyl. 3. The use of Claim 1 or Claim 2, wherein R<2> and R<3> are each Cl. 4. The use of Claim 1 or Claim 2, wherein R<2> is H and R<3> is Cl. 5. A compound of Formula 1 as defined in Claim 1. 6. A compound as defined in Claim 5, wherein R<3> is Cl or OCF3. 7. A compound of Formula 1 as defined in any of Claims 1 to 4, wherein at least one R<1> is alkyl, excluding 2-[2-(benzenesulfonamido)phenyl]ethyl-1-methylamine and 2-[4-(4-methoxybenzenesulfonamido)phenyl]ethyl-1-diethylamine. 8. A compound of Claim 5 or Claim 6, wherein one R<1> is propyl. 9. A compound of any of Claims 5 to 7, wherein R<2> is H and R<3> is OCF3. 10. A compound of Claim 5, which is: 2-[4-(4-chlorobenzenesulfonamido)phenyl]ethyl-1-dipropylamine; 2-[4-(2,4-dichlorobenzenesulfonamido)phenyl]ethyl-1-propylamine; 2-[4-(4-chlorobenzenesulfonamido)phenyl]ethyl-1-propylamine; 2-[4-(2-chloro-4-fluorobenzenesulfonamido)phenyl]ethyl-1-propylamine; 2-[4-(4-bromobenzenesulfonamido)phenyl]ethyl-1-propylamine; 2-[4-[(4-trifluoromethyl)benzenesulfonamido]phenyl]ethyl-1-propylamine; 2-[3-(2-fluorobenzenesulfonamido)phenyl]ethyl-1-propylamine. 11. A compound of Claim 5, which is 2-[4-(4-trifluoromethoxybenzenesulfonamido)phenyl]ethyl-1-propylamine. 12. The use of Claim 1, wherein the compound is of any of Claims 5 to 10. 13. 2-(4-aminophenyl)ethyl-1-(tert-butoxycarbonyl)propylamine.
申请公布号 EA002918(B1) 申请公布日期 2002.10.31
申请号 EA20000001184 申请日期 1999.05.07
申请人 PHARMACIA &AMP;UPJOHN COMPANY 发明人 ROMERO, ARTHUR, GLENN;LEIBY, JEFFREY, A.
分类号 A61P25/00;A61K31/18;A61P25/16;A61P25/18;A61P25/22;A61P25/24;A61P43/00;C07C311/21;C07C311/29;C07C311/46 主分类号 A61P25/00
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