1160923-86-3Relevant articles and documents
Design and synthesis of 4-(2,3-dihydro-1H-benzo[d]pyrrolo[1,2-a]imidazol-7-yl)-N-(5-(piperazin-1-ylmethyl)pyridine-2-yl)pyrimidin-2-amine as a highly potent and selective cyclin-dependent kinases 4 and 6 inhibitors and the discovery of structure-activity relationships
Wang, Yan,Liu, Wen-Jian,Yin, Lei,Li, Heng,Chen, Zhen-Hua,Zhu, Dian-Xi,Song, Xiu-Qing,Cheng, Zhen-Zhen,Song, Peng,Wang, Zhan,Li, Zhi-Gang
, p. 974 - 978 (2018)
Cyclin-dependent kinases 4/6 play an important role in regulation of cell cycle, and overexpress in a variety of cancers. Up to now, new CDK inhibitors still need to be developed due to its poor selectivity. Herein we report a novel series of 4-(2,3-dihydro-1H-benzo[d]pyrrolo[1,2-a]imidazole-7-yl)-N-(5-(piperazin-1-ylmethyl)pyridine-2-yl)pyrimidin-2-amine anologues as potent CDK 4/6 inhibitors based on LY2835219 (Abemaciclib). Compound 10d, which exhibits approximate potency on CDK4/6 (IC50 = 7.4/0.9 nM), has both good pharmacokinetic characters and high selectivity on CDK1 compared with LY2835219. Overall, compound 10d could be a promising candidate and a good starting point as anticancer drugs.
MERTK DEGRADERS AND USES THEREOF
-
Paragraph 00894, (2020/01/31)
The present invention provides compounds, compositions thereof, and methods of using the same.
2H-INDAZOLE DERIVATIVES AS CDK4 AND CDK6 INHIBITORS AND THERAPEUTIC USES THEREOF
-
Page/Page column 22; 23, (2019/08/12)
2-Aminopyrimidine-substituted 2H-indazole compounds of formula (I), where R1 is hydrogen, and their prodrugs, where R1 is a metabolizable group under physiological conditions, as cyclin-dependent kinase (CDK) and cell-proliferation inhibitors, and therapeutic uses and methods of preparation thereof, are disclosed. These compounds, and pharmaceutically acceptable salts, solvates, prodrugs, and pharmaceutical compositions thereof, are useful for treating diseases and disorders associated with activity of cyclin-dependent kinases, in particular CDK4/6, including but not limited to various cancers and inflammation-related diseases or conditions.
CDK4/6 INHIBITORS AND USE THEREOF
-
Paragraph 635-637, (2019/03/05)
The present disclosure relates to a compound of formula (I), or a pharmaceutically acceptable salt, a solvate, a stereoisomer, or tautomer thereof, a pharmaceutical composition comprising a compound of formula (A) or formula (B), and any subgenera thereof, and use of said compounds and compositions thereof, wherein R1, R2, R3a, R3b, R5, R6, X1, X2, Y and n are described herein.
Protein kinase inhibitor and its preparation method and medical application
-
Paragraph 0283-0286, (2017/05/26)
The invention provides a compound shown in the structural formula I or its tautomer, mesomer, racemate, enantiomer, diastereoisomer or their mixture, or a pharmaceutically acceptable salt or solvate of the compound shown in the structural formula I or its tautomer, mesomer, racemate, enantiomer, diastereoisomer or their mixture. The ring A, R1, R2, R3 and R4 are defined in the specification. The invention also provides a preparation method of the compound shown in the structural formula I and a use of the compound in preparation of a drug for treating cell proliferative disorder.
CERTAIN PROTEIN KINASE INHIBITORS
-
Paragraph 205; 206, (2017/12/27)
Provided are certain CDK4/6 inhibitors, pharmaceutical compositions thereof, and methods of use therefor.
Pyrimidine or pyridine pyridine ketone compound and its preparation method and application (by machine translation)
-
Paragraph 0249, (2016/10/09)
The invention discloses a kind of type I of the pyrimidine or pyridine pyridine ketone compound and its preparation and application, which belongs to the technical field of pharmaceutical preparation. The compounds have high-efficient and selectively inhibit the cell cycle dependent kinases (Cdks) CDK4 and CDK6 active, and then by inhibiting CDK4/CDK6 prevent tumor cell division. Therefore, the compounds of this invention can be used for CDK4 and CDK6 the involved in cell cycle control disorders result in various diseases, especially suitable for the treatment of malignant tumors. (by machine translation)
CERTAIN PROTEIN KINASE INHIBITOR
-
Paragraph 297; 298, (2017/01/09)
Provided are certain CDK4/6 inhibitors, pharmaceutical compositions thereof, and methods of use therefor.
INHIBITORS OF PROTEIN TYROSINE KINASE ACTIVITY
-
Paragraph 000279-000280, (2013/04/13)
The present invention provides new compounds and methods for treating a disease responsive to inhibition of kinase activity, for example a disease responsive to inhibition of protein tyrosine kinase activity, for example a disease responsive to inhibition of protein tyrosine kinase activity of growth factor receptors, for example a disease responsive to inhibition of receptor type tyrosine kinase signaling, or for example, a disease responsive to inhibition of VEGF receptor signaling.
Inhibitors of Protein Tyrosine Kinase Activity
-
Paragraph 0319, (2013/04/24)
The present invention provides new compounds and methods for treating a disease responsive to inhibition of kinase activity, for example a disease responsive to inhibition of protein tyrosine kinase activity, for example a disease responsive to inhibition of protein tyrosine kinase activity of growth factor receptors, for example a disease responsive to inhibition of receptor type tyrosine kinase signaling, or for example, a disease responsive to inhibition of VEGF receptor signaling.
