5734-67-8Relevant articles and documents
4-(3-Aminoazetidin-1-yl)pyrimidin-2-amines as High-Affinity Non-imidazole Histamine H3 Receptor Agonists with in Vivo Central Nervous System Activity
Wágner, Gábor,Mocking, Tamara A. M.,Arimont, Marta,Provensi, Gustavo,Rani, Barbara,Silva-Marques, Bruna,Latacz, Gniewomir,Da Costa Pereira, Daniel,Karatzidou, Christina,Vischer, Henry F.,Wijtmans, Maikel,Kie?-Kononowicz, Katarzyna,De Esch, Iwan J. P.,Leurs, Rob
, p. 10848 - 10866 (2019/11/28)
Despite the high diversity of histamine H3 receptor (H3R) antagonist/inverse agonist structures, partial or full H3R agonists have typically been imidazole derivatives. An in-house screening campaign intriguingly afforded
CHEMICAL COMPOUNDS
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Page/Page column 121, (2010/11/04)
The invention is directed to to substituted indazole derivatives. Specifically, the invention is directed to compounds according to Formula I: wherein R1 - R6 and X are defined herein. The compounds of the invention are inhibitors of PDK1 and can be useful in the treatment of disorders characterized by constitutively activated ACG kinases such as cancer and more specifically leukemia and cancers of the breast, colon, and lung. Accordingly, the invention is further directed to pharmaceutical compositions comprising a compound of the invention. The invention is still further directed to methods of inhibiting PDK1 activity and treatment of disorders associated therewith using a compound of the invention or a pharmaceutical composition comprising a compound of the invention.
Structural studies on bioactive compounds. Part 37. Suzuki coupling of diaminopyrimidines: A new synthesis of the antimalarial drug pyrimethamine
Richardson, Marianne L.,Stevens, Malcolm F.G.
, p. 482 - 484 (2007/10/03)
Suzuki reactions have been used successfully to effect cross-coupling of 5-halopyrimidines with 4-chlorobenzeneboronic acid and 2,4-diamino-5-(4-chloro-3-halo)-6-ethylpyrimidines with 4-methoxybenzeneboronic acid. The antimalarial drug pyrimethamine has been prepared by coupling 2,4-diamino-6-ethyl-5-iodopyrimidine with 4-chlorobenzeneboronic acid.