- 专利标题: PIPERAZINE DERIVATIVES AND PROCESS FOR THE PREPARATION THEREOF
- 专利标题(中): 哌嗪及其制备方法
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申请号: EP00908085.4申请日: 2000-03-03
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公开(公告)号: EP1075469A1公开(公告)日: 2001-02-14
- 发明人: CHO, Eui-Hwan , CHUNG, Sun-Gan , LEE, Sun-Hwan , KWON, Ho-Seok , KANG, Dong-Wook , JOO, Jeong-Ho , LEE, Young-Hee
- 申请人: Samjin Pharmaceutical Co., Ltd.
- 申请人地址: 338-8, Seogyo-dong,Mapo-ku Seoul 121-739 KR
- 专利权人: Samjin Pharmaceutical Co., Ltd.
- 当前专利权人: Samjin Pharmaceutical Co., Ltd.
- 当前专利权人地址: 338-8, Seogyo-dong,Mapo-ku Seoul 121-739 KR
- 代理机构: Van kan, Johan Joseph Hubert, Ir.
- 优先权: KR9906890 19990303; KR9907266 19990305; KR9908088 19990311; KR9911254 19990331
- 国际公布: WO0052001 20000908
- 主分类号: C07D295/108
- IPC分类号: C07D295/108 ; C07D295/13 ; C07D401/12 ; C07D403/12 ; C07D213/65 ; C07D241/28
摘要:
The present invention relates to a novel compound of general formula (I) and its pharmaceutically acceptable acid addition salt, and process for the preparation thereof, which have strong antitumor activities and very low toxicity, wherein R1 and R2 are independently hydrogen, C1-C4 alkyl, C1-C4 alkylcarboxyl, C1-C4 alkylcarbonyl, C1-C4 alkoxy, C1-C4 hydroxyalkyl, C1-C4 aminoalkyl or C1-C4 hydroxyiminoalkyl, or R1 and R2 are fused to form C3-C4 unsaturated ring; R3, R4, R5, R6 and R7 are independently hydrogen, halogen, hydroxy, nitro, amino, C1-C4 alkyl, C1-C4 alkylcarboxyl, C1-C4 alkylcarbonyl, C1-C4 alkoxy or C1-C4 thioalkoxy; R8 is C1-C4 alkyl; Y is oxygen, sulphur, amino, substituted amino or C1-C4 thioalkyl; Z is C1-C4 alkoxy, C1-C4 alkyl, C1-C4 alkylamino or C1-C4 thioalkoxy; X1 and X2 are independently carbon or nitrogen; and -N--C- and -C--Y- may form a single bond or a double bond provided that if -N--C- forms a single bond, -C--Y- forms a double bond, and if -C--Y- forms a single bond, -N--C- forms a double bond and R8 is nonexistent.
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