868280-49-3Relevant academic research and scientific papers
Discovery of pyrrolopyridazines as novel DGAT1 inhibitors
Fox, Brian M.,Iio, Kiyosei,Li, Kexue,Choi, Rebeka,Inaba, Takashi,Jackson, Simon,Sagawa, Shoichi,Shan, Bei,Tanaka, Masahiro,Yoshida, Atsuhito,Kayser, Frank
scheme or table, p. 6030 - 6033 (2010/11/05)
A new structural class of DGAT1 inhibitors was discovered and the structure-activity relationship was explored. The pyrrolotriazine core of the original lead molecule was changed to a pyrrolopyridazine core providing an increase in potency. Further exploration resulted in optimization of the propyl group at C7 and the discovery that the ester at C6 could be replaced by five-membered heterocyclic rings. The analogs prepared have DGAT1 IC 50 values ranging from >10 μM to 48 nM.
INHIBITORS OF AKT ACTIVITY
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Page/Page column 40, (2010/02/14)
The present invention is directed to compounds which contain substituted pyridazines and pyrimidines moieties which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention.
