Title:
QUINOLINE DERIVATIVES SUBSTITUTED BY ALIPHATIC AMINO GROUPS, THE PREPARATION AND THE PHARMACEUTICAL USE THEREOF
Document Type and Number:
WIPO Patent Application WO/2005/054203
Kind Code:
A1
Abstract:
The invention discloses quinoline derivatives substituted by aliphatic amino groups, their preparation and their use in preparing antitumor medicaments. The structure of the compounds is (I) in which, R1 and R2 are a group independently selected from the group of: H, F, Cl, Br, C1-6alkyl and C3-6 cycloalkyl, and R1= R2 or R1≠ R2; R3 is a group selected from the group of : OH, NH3, NHR4, NR5R6 and (a) wherein R4, R5 and R6 are C1-6 alkyl or C3-6 cycloalkyl, and R5= R6 or R5&num R6; X is CH2, NH, O or S; n=l, 2, 3 or 4. The compounds have very powerful inhibitory effects to a variety of tumour cell strain and have lower toxicity to normal cells. Therefore, they can be used in preparing antitumour medicines.
Inventors:
GU LIANQUAN (CN)
ZHOU JINLIN (CN)
ZHU XIAOFENG (CN)
HUANG ZHISHU (CN)
LI YUEMING (CN)
ZHOU JUNMIN (CN)
LIU ZONGCHAO (CN)
MA LIN (CN)
CHUI CHUNG HIN (CN)
TANG CHEUK ON (CN)
CHAN ALBERT SUN-CHI (CN)
ZHOU JINLIN (CN)
ZHU XIAOFENG (CN)
HUANG ZHISHU (CN)
LI YUEMING (CN)
ZHOU JUNMIN (CN)
LIU ZONGCHAO (CN)
MA LIN (CN)
CHUI CHUNG HIN (CN)
TANG CHEUK ON (CN)
CHAN ALBERT SUN-CHI (CN)
Application Number:
PCT/CN2004/000175
Publication Date:
June 16, 2005
Filing Date:
March 04, 2004
Export Citation:
Assignee:
UNIV SUN YAT SEN (CN)
UNIV HONG KONG POLYTECHNIC (CN)
GU LIANQUAN (CN)
ZHOU JINLIN (CN)
ZHU XIAOFENG (CN)
HUANG ZHISHU (CN)
LI YUEMING (CN)
ZHOU JUNMIN (CN)
LIU ZONGCHAO (CN)
MA LIN (CN)
CHUI CHUNG HIN (CN)
TANG CHEUK ON (CN)
CHAN ALBERT SUN-CHI (CN)
UNIV HONG KONG POLYTECHNIC (CN)
GU LIANQUAN (CN)
ZHOU JINLIN (CN)
ZHU XIAOFENG (CN)
HUANG ZHISHU (CN)
LI YUEMING (CN)
ZHOU JUNMIN (CN)
LIU ZONGCHAO (CN)
MA LIN (CN)
CHUI CHUNG HIN (CN)
TANG CHEUK ON (CN)
CHAN ALBERT SUN-CHI (CN)
International Classes:
A61K31/435; C07D471/04; C07D491/04; (IPC1-7): C07D221/18; A61K31/435; A61P35/00; C07D471/04; C07D491/048; C07D495/04
Other References:
YAMATO M. ET AL: "Synthesis and antitumor activity of fused tetracyclic quinoline derivatives", JOURNAL OF MEDICINAL CHEMISTRY, vol. 32, no. 6, 1989, pages 1295 - 1300
STREKOWSKI L. ET AL: "Further studies on the cyclization of aromatic azomethines ortho-substituted with a trifluoromethyl group: synthesis of 2,4-di- or 2,3,4-trisubstituted quinolines", JOURNAL OF ORGANIC CHEMISTRY, vol. 57, no. 1, 1992, pages 196 - 201
TAKEUCHI Y. ET AL: "Synthesis and antitumor activity of fused quinoline derivatives.IV.Novel 11-aminoindolo[3.2-b]quinolines", CHEMICAL & PHARMACEUTICAL BULLETIN, vol. 45, no. 2, 1997, pages 406 - 411
STREKOWSKI L. ET AL: "Further studies on the cyclization of aromatic azomethines ortho-substituted with a trifluoromethyl group: synthesis of 2,4-di- or 2,3,4-trisubstituted quinolines", JOURNAL OF ORGANIC CHEMISTRY, vol. 57, no. 1, 1992, pages 196 - 201
TAKEUCHI Y. ET AL: "Synthesis and antitumor activity of fused quinoline derivatives.IV.Novel 11-aminoindolo[3.2-b]quinolines", CHEMICAL & PHARMACEUTICAL BULLETIN, vol. 45, no. 2, 1997, pages 406 - 411
Attorney, Agent or Firm:
GUANGZHOU SCIHEAD PATENT AGENT CO., LTD. (Huihua Commercial & Trade Building No 80,
XianLie Zhong Roa, Guangzhou Guangdong 0, CN)
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