89581-64-6Relevant articles and documents
Discovery of Phthalazinone Derivatives as Novel Hepatitis B Virus Capsid Inhibitors
Chen, Wuhong,Liu, Feifei,Zhao, Qiliang,Ma, Xinna,Lu, Dong,Li, Heng,Zeng, Yanping,Tong, Xiankun,Zeng, Limin,Liu, Jia,Yang, Li,Zuo, Jianping,Hu, Youhong
, p. 8134 - 8145 (2020/08/12)
HBV capsid assembly has been viewed as an attractive target for new antiviral therapies against HBV. On the basis of a lead compound 4r, we further investigated this target to identify novel active compounds with appropriate anti-HBV potencies and improved pharmacokinetic (PK) properties. Structure-activity relationship studies based on metabolic pathways of 4r led to the identification of a phthalazinone derivative 19f with appropriate anti-HBV potencies (IC50 = 0.014 ± 0.004 μM in vitro), which demonstrated high oral bioavailability and liver exposure. In the AAV-HBV/mouse model, administration of 19f resulted in a 2.67 log reduction of the HBV DNA viral load during a 4-week treatment with 150 mg/kg dosing twice daily.
HETEROCYCLIC CARBOXYLIC ACID AMIDES AS PDK1 INIHIBITORS
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, (2011/11/06)
The present invention encompasses compounds of general formula (1) wherein the groups R1 to R4, Qa, Qb, QH, L and n are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, pharmaceutical preparations which contain such compounds and their use as medicaments.
NEW CHEMICAL COMPOUNDS
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Page/Page column 107, (2010/04/03)
The present invention encompasses compounds of general formula (1) wherein the units W, A, L, Q1 and QH are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and their use as medicaments having the above-mentioned properties.