The invention relates to compound of the formula (I) in which the substituents are as defined in the specification; m free form or in salt form; to its preparation, to its use as medicament and to medicaments comprising it.
CDK-INHIBITING PYRROLOPYRIMIDINONE CARBOXAMIDE DERIVATIVE OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME AS ACTIVE INGREDIENT FOR PREVENTING OR TREATING HEPATOCELLULAR CARCINOMA
申请人:Lee Seung Ki
公开号:US20130237495A1
公开(公告)日:2013-09-12
The present invention relates to a CDK-inhibiting pyrrolopyrimidinone carboxamide derivative or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition containing same as an active ingredient for preventing or treating liver cell cancer, and the composition containing the pyrrolopyrimidinone carboxamide derivative of the present invention suppresses the cell growth of SNU-354 cell, which is a liver cancer stem cell in humans, by inhibiting CDK1 and CDK2, and induces cell apoptosis of the cell by inhibiting CDK7 and CDK 7, and thus can be effective in use for preventing or treating liver cell cancer.
There are disclosed a novel α-amino-N-(diaminophosphinyl)lactam derivative represented by general formula (1):
wherein, for example, A is a hydrogen atom or a substituent such as a lower alkyl group or the like; W, X, Y and Z are independently a hydrogen atom or a substituent such as a lower alkyl group, aryl group, arylacyl group, arylaminocarbonyl group or the like; and Q is —(CH
2
)
n
— wherein n is 0 to 3, or its salt, and a therapeutic agent and a prophylactic agent for myelosuppression, a therapeutic agent for infectious diseases, an agent for increasing the number of leukocytes and a dipeptidyl peptidase IV inhibitor which comprise the above-mentioned derivative or salt thereof as an active ingredient.
A pharmaceutical composition containing a heterocyclic compound of the formula (I)
1
wherein each symbol is as defined in the specification, an isomer thereof, a solvate thereof or a pharmaceutically acceptable salt thereof as an active ingredient has a superior TNF-&agr; production suppressing action. Accordingly, it is useful for the prophylaxis or treatment of various diseases caused by abnormal production of TNF-&agr;.