- COMPOUNDS AND USES THEREOF
-
The present invention features compounds useful in the treatment of neurological disorders. The compounds of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing neurological disorders.
- -
-
Page/Page column 183; 184
(2018/05/17)
-
- ALKYNYL ALCOHOLS AND METHODS OF USE
-
The invention relates to compounds of Formula (0): wherein Q, A1-A8, R4 and R5 and each has the meaning as described herein. Compounds of Formula (0) and pharmaceutical compositions thereof are useful in the treatment of diseases and disorders in which undesired or over- activation of NF-kB signaling is observed.
- -
-
Page/Page column 231
(2015/03/13)
-
- Identification of novel inhibitors of Aurora A with a 3-(pyrrolopyridin-2-yl)indazole scaffold
-
A novel series of 3-(pyrrolopyridin-2-yl)indazole derivatives were synthesized and biologically evaluated for their anti-proliferative effects on five human cancer cell lines. As a result, all of them exhibited vigorous potency against HL60 cell line with IC50 values ranging from singe digital nanomolar to micromolar level. Besides, a majority of them displayed modest to good antiproliferative activities against the other four cell lines, including KB, SMMC-7721, HCT116, and A549. Particularly, compound 2y, as the most distinguished one in this series, demonstrated IC50 values of 8.3 nM and 1.3 nM against HL60 and HCT116 cell lines, respectively. Afterwards, for exploring the molecular target, compounds2d, 2g and 2y were further selected to evaluate the inhibitory activities against a panel of kinases. Finally, they were identified to be targeting Aurora A kinase with significant selectivity over other kinases, such as CHK1, CDK2, MEK1, GSK3β, BRAF, IKKβ and PKC.
- Song, Pinrao,Chen, Ming,Ma, Xiaodong,Xu, Lei,Liu, Tao,Zhou, Yubo,Hu, Yongzhou
-
p. 1858 - 1868
(2015/03/18)
-
- HETERO COMPOUND
-
[Problems] To provide a useful compound as an active ingredient for a preventing and/or treating agent for rejection in the transplantation of an organ, bone marrow, or a tissue, an autoimmune disease, or the like, which has an excellent S1P1 a
- -
-
Page/Page column 24
(2009/01/24)
-
- IDENTIFICATION OF COMPOUNDS SUITABLE FOR TREATING AD
-
The invention provides a method of screening for compounds which inhibit the hyperphosphorylation of tau, and hence are suitable for treating AD and related conditions.
- -
-
Page/Page column 13
(2008/06/13)
-
- THROMBIN INHIBITORS
-
Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: or a pharmaceutically acceptable salt thereof, wherein b is N Y 1 or O; c is CY 2 or N; d is CY 2; e is CY 1 or N; f is CY 1 or N; g is CY 1 or N; Y 1 is hydrogen, C 1-4 alkyl, or halogen; Y 2 is hydrogen, C 1-4 alkyl, C 3-7 cycloalkyl, halogen, NH 2, OH or C 1-4 alkoxy;A is and W, X, Z, R 3, R 4 and R 5 are defined in the specification.
- -
-
-
