35212-91-0Relevant academic research and scientific papers
Microwave-assisted synthesis of 3-aminobenzo[b]thiophene scaffolds for the preparation of kinase inhibitors
Bagley, Mark C.,Dwyer, Jessica E.,Molina, Maria D. Beltran,Rand, Alexander W.,Rand, Hayley L.,Tomkinson, Nicholas C. O.
, p. 6814 - 6824 (2015/06/25)
Microwave irradiation of 2-halobenzonitriles and methyl thioglycolate in the presence of triethylamine in DMSO at 130°C provides rapid access to 3-aminobenzo[b]thiophenes in 58-96% yield. This transformation has been applied in the synthesis of the thieno
Tricyclic aminopyrimidine histamine H4 receptor antagonists
Savall, Brad M.,Gomez, Laurent,Chavez, Frank,Curtis, Michael,Meduna, Steven P.,Kearney, Aaron,Dunford, Paul,Cowden, Jeffery,Thurmond, Robin L.,Grice, Cheryl,Edwards, James P.
scheme or table, p. 6577 - 6581 (2011/12/04)
This report discloses the development of a series of tricyclic histamine H4 receptor antagonists. Starting with a low nanomolar benzofuranopyrimidine HTS hit devoid of pharmaceutically acceptable properties, we navigated issues with metabolism and solubility to furnish a potent, stable and water soluble tricyclic histamine H4 receptor antagonist with desirable physiochemical parameters which demonstrated efficacy a mouse ova model.
Novel heterocyclic urea derivatives and their use as dopamine D3 receptor ligands
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Page 41, (2010/02/06)
The invention relates to heterocyclic substituted urea derivatives that display selective binding to dopamine D3 receptors. In another aspect, the invention relates to a method for treating central nervous system disorders associated with the dopamine D3 receptor activity in a patient in need of such treatment comprising administering to the subject a therapeutically effective amount of said compounds for alleviation of such disorder. The central nervous system disorders that may be treated with these compounds include Psychotic Disorders, Substance Dependence, Substance Abuse, Dyskinetic Disorders (e.g. Parkinson's Disease, Parkinsonism, Neuroleptic-Induced Tardive Dyskinesia, Gilles de la Tourette Syndrome and Huntington's Disease), Dementia, Anxiety Disorders, Sleep Disorders, Circadian Rhythm Disorders and Mood Disorders. The subject invention is also directed towards processes for the preparation of the compounds described herein as well as methods for making and using the compounds as imaging agents for dopamine D3 receptors.
