480423-17-4Relevant articles and documents
Development of Potent PfCLK3 Inhibitors Based on TCMDC-135051 as a New Class of Antimalarials
Mahindra, Amit,Janha, Omar,Mapesa, Kopano,Sanchez-Azqueta, Ana,Alam, Mahmood M.,Amambua-Ngwa, Alfred,Nwakanma, Davis C.,Tobin, Andrew B.,Jamieson, Andrew G.
supporting information, p. 9300 - 9315 (2020/10/19)
The protein kinase PfCLK3 plays a critical role in the regulation of malarial parasite RNA splicing and is essential for the survival of blood stage Plasmodium falciparum. We recently validated PfCLK3 as a drug target in malaria that offers prophylactic,
DIHYDROISOQUINOLINE-2(1H)-CARBOXAMIDE AND RELATED COMPOUNDS AND THEIR USE IN TREATING MEDICAL CONDITIONS
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Paragraph 000552, (2019/11/04)
The invention provides dihydroisoquinoline-2(1H)-carboxamide and related compounds, pharmaceutical compositions, and their use in the treatment of medical conditions, such as cancer, and in inhibiting HPK1 activity.
General methods for the synthesis and late-stage diversification of 2,4-substituted 7-azaindoles
Varnes, Jeffrey G.,McGuire, Thomas,Meadows, Rebecca E.,Barlaam, Bernard,Clark, Jemma,Cook, Calum R.,Davison, Gemma,Dishington, Allan,De Savi, Chris,Donald, Craig,Grebe, Tyler,Hande, Sudhir,Hawkins, Janet,Hird, Alexander W.,Holmes, Jane,Lister, Andrew,Lucas, Simon,Moore, Jane,Moore, Esther,Patel, Anil,Pike, Kurt G.,Roberts, Bryan,Stark, Andrew,Stead, Darren,Thakur, Kumar,Turner, Paul,Vasbinder, Melissa,Yang, Bin
supporting information, p. 4718 - 4722 (2016/09/28)
As part of a medicinal chemistry program, we adapted known synthetic methods for the late-stage diversification of 2,4-substituted 7-azaindoles. The strengths and weaknesses of these strategies are discussed. In the course of this work, three optimized co
TETRACYCLIC CDK9 KINASE INHIBITORS
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Paragraph 1139, (2015/09/22)
Disclosed are compounds of Formula (Ia), and pharmaceutically acceptable salts thereof, wherein X, Y, R1, R2, R3A, R3B, and R4 are as described herein. The compounds may be used as agents in the treatment of diseases, including cancer. Also disclosed are pharmaceutical compositions comprising one or more compounds of Formula (Ia).
PYRROLO[2,3-B]PYRIDINE CDK9 KINASE INHIBITORS
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Page/Page column 455, (2014/09/29)
Disclosed are compounds of Formula (IIa), wherein R1, R2, R3A, R3B, R3C, R3D, R3E, and R4 are as defined in the specification, and pharmaceutically acceptable salts thereof. The compounds may be used as agents in the treatment of diseases, including cancer. Also provided are pharmaceutical compositions comprising one or more compounds of Formula (IIa)
CDK9 KINASE INHIBITORS
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Paragraph 0617, (2014/09/30)
Disclosed are compound of Formula (Ia), wherein R1A, R1, R2, R10, J, L, T, X, Y, and Z are as defined in the specification, and pharmaceutically acceptable salts thereof. The compounds may be used as agents in the treatment of diseases, including cancer. Also provided are pharmaceutical compositions, comprising one or more compounds of Formula (Ia).
PYRROLOPYRIDINE AND PYRROLOPYRIMIDINE INHIBITORS OF KINASES
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Page/Page column 32, (2011/11/30)
The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein A, B, R1, R2, R3, R4a, R5, and Z are defined in the description. The present invention relates also to methods of making said compounds, and compositions containing said compounds which are useful for inhibiting kinases such as aurora.
NOVEL COMPOUNDS
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Page/Page column 42; 90, (2009/01/20)
The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds according to formula (I) and salts thereof. The compounds of the invention are inhibitors of kinase activity, in particular IKK2 activity.