131364-64-2Relevant academic research and scientific papers
Discovery and optimization of thieno[2,3-d]pyrimidines as B-Raf inhibitors
Packard, Garrick K.,Papa, Patrick,Riggs, Jennifer R.,Erdman, Paul,Tehrani, Lida,Robinson, Dale,Harris, Roy,Shevlin, Graziella,Perrin-Ninkovic, Sophie,Hilgraf, Robert,McCarrick, Margaret A.,Tran, Tam,Fleming, Yuedi,Bai, April,Richardson, Samantha,Katz, Jason,Tang, Yang,Leisten, Jim,Moghaddam, Mehran,Cathers, Brian,Zhu, Dan,Sakata, Steven
scheme or table, p. 747 - 752 (2012/03/11)
The serine/threonine specific protein kinase B-Raf is part of the MAPK pathway and is an interesting oncology target. We have identified thieno[2,3-d]pyrimidines as a core scaffold of small molecule B-Raf inhibitors. The SAR of analogs in this series will be described.
INHIBITORS OF TNFα, PDE4 AND B-RAF, COMPOSITIONS THEREOF AND METHODS OF USE THEREWITH
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Page/Page column 116, (2010/11/28)
Provided herein are compounds having TNFα and/or PDE4 and/or B-RAF inhibitory activity, and compositions thereof. In particular, provided herein are compounds of the formula (I) and pharmaceutically acceptable salts, solvates, hydrates, clathrates, stereoisomers, polymorphs and prodrugs thereof, wherein Ar, R1, R2, R3, R4, n and Z are as described herein. Further provided herein are methods for treating or preventing various diseases and disorders by administering to a patient one or more TNFα and/or PDE4 and/or B-RAF inhibitors. In particular, provided herein are methods for preventing or treating cancer, inflammatory disorders, cognition and memory disorders and autoimmune disorders, or one or more symptoms thereof by administering to a patient one or more TNFα and/or PDE4 and/or B-RAF inhibitors.
Chemotherapeutic agents, XVIII: Synthesis of pi-deficient pyrimidines and fused pyrimidines as leishmanicidal agents.
Ram
, p. 895 - 899 (2007/10/02)
Synthesis of 6-aryl-5-cyano-2-thiouracils 1a-d from the condensation-cyclization of an aromatic aldehyde, thiourea and ethyl cyanoacetate has been described. Alkylation of 1a-d under different reaction conditions with mono- and dihalo-alkanes yielded 2, 3, and 6. Interaction of 1 with POCl3 provided halopyrimidines 8a,b. Nucleophilic substitution on 8 and 3 with aromatic amines gave 9a-d and 7a-d respectively. 6-Chloro-5-nitro-3-methyluracil (11) obtained by nitration of 10 underwent nucleophilic substitution with amines providing 12. Some of the compounds screened as leishmanicides did not exhibit any significant activity.
