118454-24-3Relevant articles and documents
Synthesis and SAR of aminothiazole fused benzazepines as selective dopamine D2 partial agonists
Urbanek, Rebecca A.,Xiong, Hui,Wu, Ye,Blackwell, William,Steelman, Gary,Rosamond, Jim,Wesolowski, Steven S.,Campbell, James B.,Zhang, Minli,Brockel, Becky,Widzowski, Daniel V.
, p. 543 - 547 (2013)
Dopamine (D2) partial agonists (D2PAs) have been regarded as a potential treatment for schizophrenia patients with expected better side effect profiles than currently marketed antipsychotics. Herein we report the synthesis and SAR of a series of aminothiazole fused benzazepines as selective D 2 partial agonists. These compounds have good selectivity, CNS drug-like properties and tunable D2 partial agonism. One of the key compounds, 8h, has good in vitro/in vivo ADME characteristics, and is active in a rat amphetamine-induced locomotor activity model.
CYANOINDOLINE DERIVATIVES AS NIK INHIBITORS
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Page/Page column 284, (2018/02/03)
Fused aromatic bicyclic substituted 5-(2-amino-4-pyrimidinyl)- cyanoindoline derivatives (I) useful for therapy and/or prophylaxis in a mammal, and in particular to inhibitors of NF-KB-inducing kinase (NIK - also known as MAP3K14) useful for treating diseases such as cancer, inflammatory disorders, metabolic disorders and autoimmune disorders. The invention is also directed to pharmaceutical compositions comprising such compounds, and to the use of such compounds or pharmaceutical compositions for the prevention or treatment of diseases such as cancer, inflammatory disorders, metabolic disorders including obesity and diabetes, and autoimmune disorders.
HETEROARYL COMPOUNDS AND USES THEREOF
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, (2016/06/28)
The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same. It has now been found that compounds of this invention, and pharmaceutically acceptable compositions thereof, are effective as inhibitors of one or more protein kinases. Such compounds have general formula I or a pharmaceutically acceptable salt thereof, wherein Ring A, Ring B, W, Ry, R3 and R4 are as defined herein.
