基本信息:
- 专利标题: PRODRUGS OF EXCITATORY AMINO ACIDS
- 专利标题(中):激素氨基酸的产物
- 申请号:PCT/US2002/000488 申请日:2002-01-09
- 公开(公告)号:WO02055485A1 公开(公告)日:2002-07-18
- 主分类号: A61K31/195
- IPC分类号: A61K31/195 ; A61K38/00 ; A61K39/00 ; A61P25/00 ; C07C237/14 ; C07C237/20 ; C07C237/22 ; C07C271/22 ; C07D207/16 ; C07D209/18 ; C07K5/06 ; C07K5/065 ; C07K5/068 ; C07K5/072 ; C07K5/083 ; C07K5/103
摘要:
This invention relates to synthetic excitatory amino acid prodrugs of formula (I), wherein R is CO2R and R is hydrogen or fluoro; or R is hydrogen or fluoro and R is CO2R ; R and R are, independently, hydrogen, (1-10C) alkyl, (2-4C) alkenyl, aryl or arylalkyl; A is (Q)p; p is an integer from 1-10; and Q is independently selected, each time taken, from the group amino acyl; provided that the compound is not one in which R is CO2R ; R , R and R are hydrogen; p is any integer from 1-10; and Q is independently selected, each time taken, from the group amino acyl; provided that the compound is not one in which R is CO2R ; R , R and R are hydrogen; p is 1; and Q is L-alanyl; or a pharmaceutically acceptable salt thereof and processes for their preparation. The invention further relates to methods of using, and pharmaceutical compositions comprising, the compounds for the treatment of neurological disorders and psychiatric disorders.
摘要(中):
本发明涉及式(I)的合成兴奋性氨基酸前药,其中R 11为CO 2 R 14,R 12为氢或氟; 或R 11是氢或氟,R 12是CO 2 R 14; R 13和R 14独立地为氢,(1-10C)烷基,(2-4C)烯基,芳基或芳基烷基; A是(Q)p; p是1-10的整数; 每次从氨基酰基中选择Q独立选择; 条件是该化合物不是其中R 11是CO 2 R 14的化合物; R 12,R 13和R 14是氢; p是1-10的整数; 每次从氨基酰基中选择Q独立选择; 条件是该化合物不是其中R 11是CO 2 R 14的化合物; R 12,R 13和R 14是氢; p为1; Q为L-丙氨酰; 或其药学上可接受的盐及其制备方法。 本发明进一步涉及使用和药物组合物的方法,其包含用于治疗神经障碍和精神障碍的化合物。
IPC结构图谱:
A | 人类生活必需 |
--A61 | 医学或兽医学;卫生学 |
----A61K | 医用、牙科用或梳妆用的配制品 |
------A61K31/00 | 含有机有效成分的医药配制品 |
--------A61K31/045 | .羟基化合物,例如醇类;其盐类,例如醇化物 |
----------A61K31/19 | ..羧酸;例如丙戊酸 |
------------A61K31/195 | ...含氨基的 |