- SYK INHIBITORS
-
The present disclosure a Syk compound inhibitors, including state cancer and inflammation and various disease States thereof in the treatment of relates to the use of. In one aspect a particular embodiment, . given by formula I which is marked as a chemical structure of compound. In formula said, X 1, X 2, X 3, R 2, R 3, R 4, R 5, and Y has described herein is. The present disclosure of a formula I compounds or a pharmaceutically acceptable salt of pharmaceutical compositions including, mediated by Syk and to treat conditions a employing these compounds and compositions further provides a method. (by machine translation)
- -
-
Paragraph 1081-1083
(2016/10/07)
-
- 7-Alkyl-N2-substituted-3-deazaguanines. Synthesis, DNA polymerase III inhibition and antibacterial activity
-
Several 2-anilino- and 2-benzylamino-3-deaza-6-oxopurines [3-deazaguanines] and selected 8-methyl and 8-aza analogs have been synthesized. 7-Substituted N2-(3-ethyl-4-methylphenyl)-3-deazaguanines were potent and selective inhibitors of Gram+ bacterial DNA polymerase (pol) IIIC, and 7-substituted N2-(3,4-dichlorobenzyl)-3-deazaguanines were potent inhibitors of both pol IIIC and pol IIIE from Gram+ bacteria, but weakly inhibited pol IIIE from Gram- bacteria. Potent enzyme inhibitors in both classes inhibited the growth of Gram+ bacteria (MICs 2.5-10 μg/ml), and were inactive against the Gram- organism Escherichia coli. Several derivatives had moderate protective activity in Staphylococcus aureus-infected mice.
- Xu, Wei-Chu,Wright, George E.,Brown, Neal C.,Long, Zheng-Yu,Zhi, Cheng-Xin,Dvoskin, Sofya,Gambino, Joseph J.,Barnes, Marjorie H.,Butler, Michelle M.
-
scheme or table
p. 4197 - 4202
(2011/08/10)
-
- Purine and isosteric antibacterial compounds
-
The invention features 2,7-disubstituted purines and their isosteres such as the corresponding 3-deazapurines and 3-deaza-8-azapurines. The compounds disclosed herein have potent anti-microbial, e.g., anti-bacterial and anti-mycoplasmal properties. The compounds described herein inhibit DNA polymerase IIIC and DNA polymerase IIIE species; the compounds thus inhibit the growth of bacteria and mycoplasmata. The compounds can be administered to prevent or to treat Gram-positive or Gram-negative bacterial or mycoplasmal infections, e.g., in eukaryotic cell cultures, animals, or humans.
- -
-
Page/Page column 8; 11
(2010/02/05)
-