Researchers from Janssen Pharmaceutica NV have reported the discovery of novel hepatitis B virus (HBV) capsid assembly modulators (CAMs) as potential therapeutic candidates against HBV infection. Synthesis and optimization of a new series of di-fluoro azepane HBV CAMs resulted in the identification of compound [I] as the lead candidate with DNA EC50 value of 8.5 nM when assessed in the HepG2.2.15 cellular assay.
“I am not a fortune teller, nor am I a gambler. I will make no bets,” Lorraine Kalia told the audience at the 2023 International Congress of Parkinson’s Disease and Movement Disorders. “But I am optimistic.” At the meeting, which is being held in Copenhagen this week, Kalia, who is a scientist at Toronto Western Hospital’s Krembil Brain Institute and at the University of Toronto’s Tanz Centre for Research in Neurodegenerative Diseases, was giving an overview of “Emerging targets in the clinic” in a plenary session on “Therapeutic strategies for the future.”
Eikonizo Therapeutics Inc. has described histone deacetylase 6 (HDAC6) inhibitors reported to be useful for the treatment of cancer, multiple sclerosis, systemic lupus erythematosus, neurodegeneration, obesity, Alzheimer’s disease, Parkinson’s disease and Huntington’s disease, among others.
Janssen Pharmaceutica NV has divulged pyrazolopyrimidines acting as spermine oxidase (polyamine oxidase 1; SMOX) inhibitors reported to be useful for the treatment of colorectal cancer.
Merck Sharp & Dohme Corp. has synthesized plasma kallikrein (KLKB1) inhibitors reported to be useful for the treatment of hereditary angioedema, diabetic macular edema, retinal vein occlusion, diabetic retinopathy, wet macular degeneration (exudative) and uveitis.
Researchers at Jiangsu Hengrui Medicine Co. Ltd., Shanghai Senhui Pharmaceutical Co. Ltd. and Shanghai Shengdi Pharmaceutical Co. Ltd. have disclosed antibody-drug conjugates (ADCs) comprising monoclonal antibodies targeting IL-4R covalently linked to glucocorticoid analogues through a linker. They are reported to be useful for the treatment of asthma and skin allergy.
Verastem Oncology Inc. has entered into a discovery and development collaboration with Genfleet Therapeutics (Shanghai) Ltd. to advance three oncology discovery programs targeting RAS pathway-driven cancers.
Researchers from Nanjing Medical University have published data from a study that aimed to assess the potential of targeting fascin homologue 1 (FSCN1) as novel therapeutic strategy for the treatment of ocular neovascularization.
Researchers from Jinggangshan University reported on the synthesis of a series of novel celastrol derivatives that led to the identification of [I] as the main compound with water solubility of 11.8 mg/mL and antiproliferative effects accounting for IC50 values of 0.58, 0.32, 0.32, 0.75, 0.29 and 4.30 µM against BEL-7402, AGS, HCT 116, HepG-2, MGC-803 and A549 human cancer cell lines, respectively.
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