报道了一系列作用于电压门控钙通道 (Ca v α2δ-1) α2δ-1 亚基的新系列哌嗪基喹唑啉-4-(3 H )-one 衍生物的合成和药理活性。探索了微摩尔 HTS 命中的不同位置,并获得了在 quinazolin-4-(3 H )-one 支架的位置 3 和 3-methyl-piperazin-1-yl- 中含有小烷基的化合物的最佳活性或位置 2 的 3,5-二甲基-哌嗪-1-基-丁基。活性显示在位置 2 的链的R对映异构体中,并且几个 eutomers 达到个位数纳摩尔亲和力。中央支架的最终修饰以降低亲脂性提供了吡啶并[4,3- d]pyrimidin-4(3 H )-one 16RR ,它对 Ca v α2δ-1 和 Ca v α2δ-2表现出高选择性,这可能与其在小鼠中比普瑞巴林提高的镇痛功效-安全比有关。
Hydroxyalkanoylaminolactams and related structures as inhibitors of a beta protein production
申请人:——
公开号:US20020052360A1
公开(公告)日:2002-05-02
This invention relates to novel lactams having the formula (I):
1
to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of A&bgr;-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to &bgr;-amyloid production such as Alzheimer's disease and Down's Syndrome.
Hydroxyalkanoylaminolactams and related structures as inhibitors of A-beta protein production
申请人:——
公开号:US20030166636A1
公开(公告)日:2003-09-04
This invention relates to novel lactams having the formula (I):
1
to their pharmaceutical compositions and to their methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of A&bgr;-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to &bgr;-amyloid production such as Alzheimer's disease and Down's Syndrome.
Control of Acarina by esters of cyclopropane acids
申请人:Zoecon Corporation
公开号:US03995054A1
公开(公告)日:1976-11-30
Methods and compositions for the control of Acarina employing esters of cyclopropane carboxylic acids described herein.
这里描述了利用环丙烷羧酸酯类物质控制蜱的方法和组合物。
Potassium Channel Modulators
申请人:Xu Xiangdong
公开号:US20120122888A1
公开(公告)日:2012-05-17
Disclosed herein are KCNQ potassium channels modulators of formula (I)
wherein R
1
, R
2
, R
3
, R
4
, and R
5
are as defined in the specification. Compositions comprising such compounds; and methods for treating conditions and disorders using such compounds and compositions are also described.
Bisoxime Ester Photoinitiator and Preparation Method and Use Thereof
申请人:CHANGZHOU TRONLY NEW ELECTRONIC MATERIALS CO., LTD.
公开号:US20160376226A1
公开(公告)日:2016-12-29
A bisoxime ester photoinitiator as represented by general formula (I). By introducing a bisoxime ester group and a cycloalkylalkyl group into the chemical structure, this photoinitiator not only has excellent performance in aspects of storage stability, photosensitivity, developability, pattern integrity, and the like, but also exhibits obviously improved photosensitivity and thermal stability compared to similar photoinitiators.