- PROCESS FOR PREPARING 1-[(3R,4S)-4-CYANOTETRAHYDROPYRAN-3-YL]-3-[(2-FLUORO-6-METHOXY-4-PYRIDYL)AMINO]P YRAZOLE-4-CARBOXAMIDE
-
The application relates to processes for the preparation of 1-[(3R,4S) -4-cyanotetrahydropyran-3-yl]-3-[(2-fluoro-6-methoxy-4-pyridyl) amino]pyrazole-4-carboxamide (I) which include (i) a synthesis for bromo and iodo pyridine intermediates, (ii) a synthesis of a pyrazole ester intermediate which can be obtained in enantiopure form and (iii) the combination of these intermediates into compound (I).
- -
-
Page/Page column 22-23
(2020/07/07)
-
- Nitrogen-containing heterocyclic compound and application thereof and organic electroluminescent device (by machine translation)
-
The present disclosure relates to a nitrogen-containing heterocyclic compound having a structure as shown (1) in the following formula (I). The nitrogen-containing heterocyclic compound disclosed by the invention comprises an asymmetric carboline group an
- -
-
Paragraph 0077-0081; 0090-0095
(2019/11/25)
-
- Identification of Potent and Selective RIPK2 Inhibitors for the Treatment of Inflammatory Diseases
-
NOD2 (nucleotide-binding oligomerization domain-containing protein 2) is an internal pattern recognition receptor that recognizes bacterial peptidoglycan and stimulates host immune responses. Dysfunction of NOD2 pathway has been associated with a number of autoinflammatory disorders. To date, direct inhibitors of NOD2 have not been described due to technical challenges of targeting the oligomeric protein complex. Receptor interacting protein kinase 2 (RIPK2) is an intracellular serine/threonine/tyrosine kinase, a key signaling partner, and an obligate kinase for NOD2. As such, RIPK2 represents an attractive target to probe the pathological roles of NOD2 pathway. To search for selective RIPK2 inhibitors, we employed virtual library screening (VLS) and structure based design that eventually led to a potent and selective RIPK2 inhibitor 8 with excellent oral bioavailability, which was used to evaluate the effects of inhibition of RIPK2 in various in vitro assays and ex vivo and in vivo pharmacodynamic models.
- He, Xiaohui,Da Ros, Sara,Nelson, John,Zhu, Xuefeng,Jiang, Tao,Okram, Barun,Jiang, Songchun,Michellys, Pierre-Yves,Iskandar, Maya,Espinola, Sheryll,Jia, Yong,Bursulaya, Badry,Kreusch, Andreas,Gao, Mu-Yun,Spraggon, Glen,Baaten, Janine,Clemmer, Leah,Meeusen, Shelly,Huang, David,Hill, Robert,Nguyen-Tran, Van,Fathman, John,Liu, Bo,Tuntland, Tove,Gordon, Perry,Hollenbeck, Thomas,Ng, Kenneth,Shi, Jian,Bordone, Laura,Liu, Hong
-
supporting information
p. 1048 - 1053
(2017/10/18)
-
- Fluorine-controlled C-H borylation of arenes catalyzed by a PSiN-pincer platinum complex
-
An efficient, regioselective synthesis of fluorine-substituted arylboronic esters was achieved through fluorine-controlled C-H borylation of arenes with diboron catalyzed by a PSiN-platinum complex. The promising utility of the PSiN-platinum catalyst and its unique regioselectivity were demonstrated for the first time, which would complement the well-developed Ir-catalyzed C-H borylation.
- Takaya, Jun,Ito, Shisei,Nomoto, Hironori,Saito, Narumasa,Kirai, Naohiro,Iwasawa, Nobuharu
-
supporting information
p. 17662 - 17665
(2015/12/18)
-
- SERINE/THREONINE KINASE INHIBITORS
-
Compounds having the formula I wherein R1, X1, X2, X3 and X4 as defined herein are inhibitors of ERK kinase. Also disclosed are compositions and methods for treating hyperproliferative disorders.
- -
-
Paragraph 00188
(2015/06/18)
-
- DERIVATIVES OF 2-[2-(BENZO- OR PYRIDO-) THIAZOLYLAMINO]-6-AMINOPYRIDINE, USEFUL IN THE TREATMENT OF RESPIRATORIC, ALLERGIC OR INFLAMMATORY DISEASES
-
The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I): and salts thereof. The compounds of the invention are inhibitors of kinase activity, in particular Itk activity.
- -
-
Page/Page column 74-75
(2011/10/05)
-
