58088-53-2

Upstream product

• 59576-18-0 phenyl-(3-pyridyl)methanone oxime 
• 423761-52-8 N-(phenyl-pyridin-3-yl-methyl)-formamide 
• 10400-19-8 3-pyridinecarbonyl chloride 
• 5424-19-1 3-Benzoylpyridine 
• 71-43-2 benzene 

Downstream Products

• 96037-77-3 C₁₅H₁₅N₅ 
• 95899-33-5 C₁₆H₁₇N₅ 
• 95899-14-2 C₁₇H₁₇N₅ 
• 478263-07-9 N-(Phenylpyridin-3-ylmethyl)-2-(quinoline-8-sulfonylamino)-benzamide 

Relevant academic research and scientific papers

BICYCLIC HETEROCYCLE DERIVATIVES AND USE THEREOF AS GPR119 MODULATORS

The present invention relates to Bicyclic Heterocycle Derivatives of formula (I), compositions comprising a Bicyclic Heterocycle Derivative, and methods of using the Bicyclic Heterocycle Derivatives for treating or preventing obesity, diabetes, a metabolic disorder, a cardiovascular disease or a disorder related to the activity of GPR1 19 in a patient.

(Partial) agonist/antagonist properties of novel diarylalkyl carbamates on histamine H3 receptors

In the search for new ligands of the histamine H3 receptor, novel diarylalkyl carbamates (1-19 were synthesized as derivatives of 3-(1H- imidazol-4-yl)propanol and -ethanol. Carbamates were built up via isocyanates either from corresponding amines by reaction with diphosgene or from related carboxylic acid/diphenylphosphoryl azide and the alcoholic component. Sterically hindered amines were prepared in a two-step reaction sequence from corresponding ketones. Some of the title compounds showed (partial) agonist activity at the histamine H3 receptor in vitro and in vivo. Diphenylmethyl carbamate 2 was identified as a new lead structure (ED50 = 5.3 ± 2.6 mg/kg po, α = 1.0). Aromatic substitution in ortho- or para-positions of 2 led to a loss of agonist activity. meta-Substitution was tolerated to some extent. These effects seemed to be caused by steric rather than electronic properties of the substituents. An investigation of exchange of one or both phenyl rings of 2 by heterocyclic rings led to the highly active and selective thienyl derivative 18 (ED50 = 3.4 ± 1.4 mg/kg po, α = 1.0). These new (partial) agonists of the histamine H3 receptor might serve as pharmacological tools for investigating molecular aspects of the H3 receptor or as possible centrally acting therapeutic agents with oral bioavailability. (C) 2000 Elsevier Science Ltd.