867256-62-0Relevant academic research and scientific papers
Synthesis and structure-activity relationships of 1,2,3,4-tetrahydropyrido[2,3-b]pyrazines as potent and selective inhibitors of the anaplastic lymphoma kinase
Milkiewicz, Karen L.,Weinberg, Linda R.,Albom, Mark S.,Angeles, Thelma S.,Cheng, Mangeng,Ghose, Arup K.,Roemmele, Renee C.,Theroff, Jay P.,Underiner, Ted L.,Zificsak, Craig A.,Dorsey, Bruce D.
experimental part, p. 4351 - 4362 (2010/09/12)
Dysregulation of the anaplastic lymphoma kinase (ALK) is implicated in a variety of cancers. A series of tetrahydropyrido[2,3-b]pyrazines was constructed as ring-constrained analogs of a known aminopyridine kinase scaffold. Chemistry was developed to rapidly elaborate the SAR, structural elements impacting ALK inhibitory activity were exploited, and kinase selective analogs were identified that inhibit ALK with IC50 values ~10 nM (enzyme) and ~150 nM (cell).
HISTAMINE H3 RECEPTOR AGENTS, PREPARATION AND THERAPEUTIC USES
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Page/Page column 22, (2010/03/31)
The present invention discloses novel compounds of Formula (I) or pharmaceutically acceptable salts thereof, which have histamine-H3 receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula (I) as well as methods of using them to treat obesity, cognitive deficiencies, narcolepsy, and other histamine H3 receptor-related diseases
HISTAMINE H3 RECEPTOR AGENTS, PREPARATION AND THERAPEUTIC USES
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Page/Page column 55, (2008/06/13)
The present invention discloses novel compounds of Formula (I) or pharmaceutically acceptable salts thereof, which have histamine-H3 receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula (I) as well as methods of using them to treat obesity, cognitive deficiencies, narcolepsy, and other histamine H3 receptor-related diseases
