175867-59-1Relevant articles and documents
DOPAMINE D3 RECEPTOR ANTAGONISTS COMPOUNDS
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Page/Page column 146; 147, (2016/05/19)
The disclosure is directed to novel dopamine D3 receptor antagonists, processes for their preparation, intermediates used in these processes, pharmaceutical compositions containing them and their use in therapy, including treating drug dependency and psychosis.
Discovery of small molecule Mer kinase inhibitors for the treatment of pediatric acute lymphoblastic leukemia
Liu, Jing,Yang, Chao,Simpson, Catherine,Deryckere, Deborah,Van Deusen, Amy,Miley, Michael J.,Kireev, Dmitri,Norris-Drouin, Jacqueline,Sather, Susan,Hunter, Debra,Korboukh, Victoria K.,Patel, Hari S.,Janzen, William P.,MacHius, Mischa,Johnson, Gary L.,Earp, H. Shelton,Graham, Douglas K.,Frye, Stephen V.,Wang, Xiaodong
supporting information; experimental part, p. 129 - 134 (2012/04/04)
Ectopic Mer expression promotes pro-survival signaling and contributes to leukemogenesis and chemoresistance in childhood acute lymphoblastic leukemia (ALL). Consequently, Mer kinase inhibitors may promote leukemic cell death and further act as chemosensitizers increasing efficacy and reducing toxicities of current ALL regimens. We have applied a structure-based design approach to discover novel small molecule Mer kinase inhibitors. Several pyrazolopyrimidine derivatives effectively inhibit Mer kinase activity at subnanomolar concentrations. Furthermore, the lead compound shows a promising selectivity profile against a panel of 72 kinases and has excellent pharmacokinetic properties. We also describe the crystal structure of the complex between the lead compound and Mer, opening new opportunities for further optimization and new template design.
N-SUBSTITUTED PHENYLACETAMIDE DERIVATIVE AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME
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Page/Page column 104-105, (2008/06/13)
A compound represented by the formula: (I) wherein R1 represents a methoxy group, a hydroxyl group or a hydrogen atom; R2 represents a hydrogen atom, a C1-4 alkyl group, a C1-4 alkylcarbonyl group or an arylcarbonyl group; and D represents a group represented by the formula (A), (B) or (C) below. (A) (B) (C) This compound is useful as a therapeutic agent for a pain or inflammation induced by any one of various morbid conditions such as neuropathic pain, rheumatoid arthritis and osteoarthritis.