1249463-71-5Relevant academic research and scientific papers
Design of an orally efficacious hydroxyethylamine (HEA) BACE-1 inhibitor in a preclinical animal model
Truong, Anh P.,Tóth, Gergley,Probst, Gary D.,Sealy, Jennifer M.,Bowers, Simeon,Wone, David W.G.,Dressen, Darren,Hom, Roy K.,Konradi, Andrei W.,Sham, Hing L.,Wu, Jing,Peterson, Brian T.,Ruslim, Lany,Bova, Michael P.,Kholodenko, Dora,Motter, Ruth N.,Bard, Frédérique,Santiago, Pamela,Ni, Huifang,Chian, David,Soriano, Ferdie,Cole, Tracy,Brigham, Elizabeth F.,Wong, Karina,Zmolek, Wes,Goldbach, Erich,Samant, Bhushan,Chen, Linda,Zhang, Hongbing,Nakamura, David F.,Quinn, Kevin P.,Yednock, Ted A.,Sauer, John-Michael
, p. 6231 - 6236 (2010)
In this Letter, we describe our efforts to design HEA BACE-1 inhibitors that are highly permeable coupled with negligible levels of permeability- glycoprotein activity. These efforts culminate in producing 16 which lowers Αβ by 28% and 32% in the cortex and CSF, respectively, in the preclinical wild type Hartley guinea pig animal model when dosed orally at 30 mpk BID for 2.5 days.
Pyridineacetamide derivative serving as CDK inhibitor, and preparation method and application thereof
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Paragraph 0235; 0238; 0241-0242, (2021/07/28)
The invention belongs to the technical field of pyridineacetamide derivatives, and particularly relates to a pyridineacetamide derivative serving as a CDK inhibitor and a preparation method and application of the pyridine acetamide derivative. The pyridineacetamide derivative shows excellent CDK9/CDK7 enzyme inhibitory activity, and can be used for preparing drugs used for treating cancers, especially hematologic cancers including acute myeloid leukemia, multiple myeloma, chronic lymphocytic leukemia, follicular lymphoma and the like and solid tumors such as breast cancer, prostate cancer, ovarian cancer, hepatocellular carcinoma, pancreatic cancer, kidney cancer, stomach cancer, colorectal cancer, lung cancer and the like.
Palladium-Catalyzed α-Arylation of Carboxylic Acids and Secondary Amides via a Traceless Protecting Strategy
He, Zhi-Tao,Hartwig, John F.
supporting information, p. 11749 - 11753 (2019/08/26)
A novel traceless protecting strategy is presented for the long-standing challenge of conducting the palladium-catalyzed α-arylation of carboxylic aids and secondary amides with aryl halides. Both of the presented coupling processes occur with a variety of carboxylic acids and amides and with a variety of aryl bromides containing a broad range of functional groups, including base-sensitive functionality like acyl, alkoxycarbonyl, nitro, cyano, and even hydroxyl groups. Five commercial drugs were prepared through this method in one step in 81-96% yield. Gram-scale synthesis of medication Naproxen and Flurbiprofen with low palladium loading further highlights the practical value of this method.
AMINE SUBSTITUTED METHANESULFONAMIDE DERIVATIVES AS VANILLOID RECEPTOR LIGANDS
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, (2013/04/13)
The invention relates to amine substituted methanesulfonamide derivatives of formula (I) as vanilloid receptor ligands, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.
Amine Substituted Methanesulfonamide Derivatives as Vanilloid Receptor Ligands
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, (2013/04/10)
The invention relates to amine substituted methanesulfonamide derivatives as vanilloid receptor ligands, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.
