637348-81-3Relevant articles and documents
HETEROARYL PYRIDONE AND AZA-PYRIDONE COMPOUNDS AS INHIBITORS OF BTK ACTIVITY
-
Paragraph 0844; 0845, (2015/11/16)
Heteroaryl pyridone and aza-pyridone compounds of Formula I are provided, where one or two of X, X, and Xare N, and including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I foranddiagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
8-FLUOROPHTHALAZIN-1(2H)-ONE COMPOUNDS
-
Paragraph 0467, (2013/05/21)
8-Fluorophthalazin-1(2h)-one compounds of Formula II where one or two of X1, X2, and X3 are N, are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula II for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
Novel styrylpyridines as probes for SPECT imaging of amyloid plaques
Qu, Wenchao,Kung, Mei-Ping,Hou, Catherine,Benedum, Tyler E.,Kung, Hank F.
, p. 2157 - 2165 (2008/02/05)
We report a series of radioiodinated styrylpyridines as single photon emission computed tomography probes for imaging Aβ plaques in the brain of patients with Alzheimer's disease (AD). In vitro binding showed that all of the styrylpyridines displayed very good binding affinities in postmortem AD brain homogenates (Ki = 3.6 to 15.5 nM). No-carrier-added samples of 13a, 13b, 16a, 16b, and 16e (radioiodinated with 125I) were successfully prepared. The in vivo biodistribution in normal mice, at 2 min after injection, showed excellent initial brain penetrations (4.03, 6.22, 5.43, and 8.04% dose/g for [125I]13a, 13b, 16a, and 16b, respectively). Furthermore, in vitro autoradiography of AD brain sections showed that the high binding signal was specifically due to the presence of Aβ plaques. Taken together, these results strongly suggest that these styrylpyridines are useful for imaging Aβ plaques in the living human brain.
STYRYLPYRIDINE DERIVATIVES AND THEIR USE FOR BINDING AND IMAGING AMYLOID PLAQUES
-
Page/Page column 33; 46-47, (2008/06/13)
This invention relates to a method of imaging amyloid deposits and to styrylpyridine compounds, and methods of making radiolabeled styrylpyridine compounds useful in imaging amyloid deposits. This invention also relates to compounds, and methods of making
Efficient regioselective preparation of monobromo and bromoiodo hydroxy pyridines from dibromoderivatives via bromine-lithium exchange
Meana, ángela,Rodríguez, Justo F.,Sanz-Tejedor, M. Ascensión,García-Ruano, José L.
, p. 1678 - 1682 (2007/10/03)
Annular dibromination of hydroxypyridines with NBS in acetonitrile followed by bromine-lithium exchange with RLi and subsequent trapping with H2O or I2 afforded monobromo and bromoiodo derivatives in a completely regioselective way. Iodination of bromo hydroxypyridines with NIS is totally regioselective.