453548-65-7Relevant articles and documents
Discovery and Characterization of Selective and Ligand-Efficient DYRK Inhibitors
Ashall-Kelly, Alexander,Bennett, James,Elkins, Jonathan M.,Fedorov, Oleg,Godoi, Paulo H.,Hanley, Marcus T.,Henderson, Scott H.,Hopkins Navratilova, Iva,Robinson, Sean,Ruela De Sousa, Roberta,Sorrell, Fiona,Walter, Daryl S.,Ward, Simon E.
supporting information, p. 11709 - 11728 (2021/08/24)
Dual-specificity tyrosine-regulated kinase 1A (DYRK1A) regulates the proliferation and differentiation of neuronal progenitor cells during brain development. Consequently, DYRK1A has attracted interest as a target for the treatment of neurodegenerative diseases, including Alzheimer's disease (AD) and Down's syndrome. Recently, the inhibition of DYRK1A has been investigated as a potential treatment for diabetes, while DYRK1A's role as a mediator in the cell cycle has garnered interest in oncologic indications. Structure-activity relationship (SAR) analysis in combination with high-resolution X-ray crystallography leads to a series of pyrazolo[1,5-b]pyridazine inhibitors with excellent ligand efficiencies, good physicochemical properties, and a high degree of selectivity over the kinome. Compound 11 exhibited good permeability and cellular activity without P-glycoprotein liability, extending the utility of 11 in an in vivo setting. These pyrazolo[1,5-b]pyridazines are a viable lead series in the discovery of new therapies for the treatment of diseases linked to DYRK1A function.
A novel benzoyl amide compounds
-
, (2016/11/21)
The invention relates to the field of medicinal chemistry, in particular to a novel benzamides compound or a salt acceptable in parmacy of the novel benzamides compound, a preparation method of the novel benzamides compound, a pharmaceutical composition containing the novel benzamides compound and an application of the pharmaceutical composition in preparation of antineoplastic drugs.
NEW SOMATOSTATIN RECEPTOR SUBTYPE 4 (SSTR4) AGONISTS
-
Page/Page column 189; 190, (2014/12/12)
The invention relates to 3-aza-bicyclo[3.1.0]hexane-6-carboxylic acid amide derivatives of general formula (I), which are agonists of somatostatin receptor subtype 4 (SSTR4), useful for preventing or treating medical disorders related to SSTR4. In addition, the invention relates to processes for preparing pharmaceutical compositions as well as processes for manufacture of the compounds according to the invention.
New Somatostatin receptor subtype 4 (SSTR4) agonists
-
Paragraph 0785; 0786; 0787; 0788, (2014/12/09)
3-aza-bicyclo[3.1.0]hexane-6-carboxylic acid amide derivatives which are agonists of somatostatin receptor subtype 4 (SSTR4), useful for preventing or treating medical disorders related to SSTR4.
IMIDAZO[1,2-a]PYRIDINES AND IMIDAZO[1,2-b]PYRIDAZINES AS MARK INHIBITORS
-
Page/Page column 56-57, (2010/08/08)
The invention encompasses imidazo[1,2-a]pyridine and imidazo[1,2-b]pyridazine derivatives which selectively inhibit microtubule affinity regulating kinase (MARK) and are therefore useful for the treatment or prevention of Alzheimer's disease. Pharmaceutical compositions and methods of use are also included.
Imidazo[1,2-b]pyridazines: A potent and selective class of cyclin-dependent kinase inhibitors
Byth, Kate F.,Cooper, Nicola,Culshaw, Janet D.,Heaton, David W.,Oakes, Sandra E.,Minshull, Claire A.,Norman, Richard A.,Pauptit, Richard A.,Tucker, Julie A.,Breed, Jason,Pannifer, Andrew,Rowsell, Sian,Stanway, Judith J.,Valentine, Anna L.,Thomas, Andrew P.
, p. 2249 - 2252 (2007/10/03)
Modification of imidazo[1,2-a]pyridine CDK inhibitors lead to identification of less lipophilic imidazo[1,2-b]pyridazine series of CDK inhibitors. Although several equivalent compounds from these two series have similar structure and show similar CDK acti