221255-77-2Relevant academic research and scientific papers
COMPOUNDS FOR INHIBITING LRRK2 KINASE ACTIVITY
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Page/Page column 49, (2018/09/08)
Compounds of Formula (I) or pharmaceutically acceptable salt thereof, a pharmaceutical compositions comprising these compounds, the use of these compounds and compositions in the treatment of diseases in which LRRK-2 kinase is involved.
COMPOUNDS FOR REGULATING FAK AND/OR SRC PATHWAYS
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Page/Page column 96, (2015/03/28)
The present application provides novel optionally substituted fused pyridine and pyrimidine bicyclic compounds and pharmaceutically acceptable salts thereof. Also provided are methods for preparing these compounds. These compounds are useful in co-regulating FAK and/or Src activity by administering a therapeutically effective amount of one or more of the compounds to a subject. By doing so, these compounds are effective in treating conditions associated with the dysregulation of the FAK and/or Src pathway. Advantageously, these compounds perform as dual FAK and/or Src inhibitors. A variety of conditions can be treated using these compounds and include diseases which are characterized by inflammation or abnormal cellular proliferation. In one embodiment, the disease is cancer.
Structure-activity relationship studies on unifiram (DM232) and sunifiram (DM235), two novel and potent cognition enhancing drugs
Scapecchi, Serena,Martini, Elisabetta,Manetti, Dina,Ghelardini, Carla,Martelli, Cecilia,Dei, Silvia,Galeotti, Nicoletta,Guandalini, Luca,Romanelli, Maria Novella,Teodori, Elisabetta
, p. 71 - 85 (2007/10/03)
Structure-activity relationships on two novel potent cognition enhancing drugs, unifiram (DM232, 1) and sunifiram (DM235, 2), are reported. Although none of the compounds synthesised reached the potency of the parent drugs, some fairly active compounds have been identified that may represent new leads to develop other cognition enhancing drugs. An interesting result of this research is the identification of two compounds (13 and 14) that are endowed with amnesing activity (the opposite of the activity of the original molecules) and are nearly equipotent to scopolamine. Moreover, two compounds of the series (5 and 6) were found endowed with analgesic activity on a rat model of neuropathic pain at the dose of 1 mg/kg.
Dual antagonists of platelet activating factor and histamine. Part 3. Synthesis, biological activity and conformational implications of substituted N-acyl-bis-arylcycloheptapiperazines
Piwinski, John J.,Wong, Jesse K.,Green, Michael J.,Kaminski, James J.,Colizzo, Frank,Albanese, Margaret M.,Ganguly, Ashit K.,Billah, M. Motasim,Anthes, John C.,West Jr., Robert E.
, p. 3469 - 3474 (2007/10/03)
A series of N-acyl-4-(5,6-dihydro-11-H-benzo[5,6]cyclohepta[1,2- b]pyridin-11-ylidene)piperazines is described that are dual antagonists of PAF and histamine. The structural requirements for activity in this series parallel those of their previously reported piperidinylidene counterparts. Whereas their global minimum energy conformations are different for both series of compounds, computer assisted molecular modeling suggests that a common bioactive conformation is possible.
