50681-26-0Relevant academic research and scientific papers
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.
NEW CHEMICAL COMPOUNDS
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Page/Page column 33-34, (2012/04/23)
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.
HETEROCYCLIC CARBOXYLIC ACID AMIDES AS PDK1 INIHIBITORS
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Page/Page column 62-63, (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.
1H - IMIDAZO [4, 5 - C] QUINOLINES
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Page/Page column 55, (2011/12/04)
The present invention encompasses compounds of general formula (1), wherein the groups R1 to R7, Qa, Qb, L, n and m are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, pharmaceutical preparations containing such compounds and their use as medicaments.
NEW CHEMICAL COMPOUNDS
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Page/Page column 106-107, (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.
Novel heteroaryl substituted piperidine derivatives which are L-CPT1 inhibitors
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Page/Page column 57, (2010/11/27)
The invention is concerned with novel substituted piperidine derivatives of formula (I) wherein R1, R2, R3, R4, R5, R6, R7 and X are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds inhibit L-CPT1 and can be used as medicaments.
PYRIDAZINIL QUINAZOLINE DERIVATIVES FOR USE IN THE TREATMENT OF TUMOURS
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Page 53, (2010/02/09)
The invention concerns quinazoline derivatives of Formula (I) wherein Z is an O, S, SO, SO2, N(R2) or C(R2)(R3) group wherein each R2 or R3 group is hydrogen or (1-8C)alkyl, m is 1, 2 or 3, each R1 group has any of the meanings defined in the description, Ra is halogeno or (1-6C)alkoxy, Rb is halogeno or (1-6C)alkoxy, and Rc is hydrogen, halogeno, (1-8C)alkyl or (1-6C)alkoxy, or a pharmaceutically-acceptable salt thereof; processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use as an anti-invasive agent in the containment and/or treatment of solid tumour disease.
PYRIDAZINONE DERIVATIVES AS GSK-3BETA INHIBITORS
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Page 110, (2008/06/13)
The present invention relates to novel pyridazinone derivatives of the general formula (I) wherein A is A1 or A2; R is unsubstituted or at least monosubstituted C1-C10-alkyl, aryl, aryl (C1-C10-alkyl)-, heteroar
