63731-33-9

Upstream product

• 856835-62-6 2-(α,β-dibromo-phenethyl)-4-methyl-pyridine 
• 4926-28-7 2-Bromo-4-picoline 
• 536-74-3 phenylacetylene 
• 1003-67-4 4-methylpyridine-1-oxide 

Downstream Products

• 1155854-75-3 1-methyl-11-aza-tricyclo[8.3.1.0*2,7*]tetradeca-2.4,6-triene 
• 1155854-72-0 1,4-dimethyl-2-phenethyl-1,2,3,6-tetrahydro-pyridine 
• 342894-91-1 1,4-dimethyl-6-phenethyl-1,2,3,6-tetrahydro-pyridine 
• 75835-06-2 1,4-dimethyl-2-phenethyl-pyridinium iodide 
• 75835-01-7 methyl-4 (phenyl-2 ethyl)-2 pyridine 
• 131470-47-8 1-(Methoxy-phenyl-methyl)-7-methyl-indolizine-2-carboxylic acid methyl ester 
• 3197-57-7 2-phenacyl-4-methylpyridine 

Relevant academic research and scientific papers

Alicyclic carboxylic acid derivatives of benzomorphans and related scaffolds, medicaments containing such compounds and their use

The present invention relates to compounds defined by Formula (I), wherein the groups A, B, X, m, n and o are defined as in claim 1, possessing valuable pharmacological activity. Particularly the compounds are inhibitors of 11β-hydroxysteroid dehydrogenase (HSD) 1 and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases, in particular diabetes type 2, obesity and dyslipidemia.

ARYL- AND HETEROARYLCARBONYL DERIVATIVES OF BENZOMORPHANES AND RELATED SCAFFOLDS, MEDICAMENTS CONTAINING SUCH COMPOUNDS AND THEIR USE

The present invention relates to compounds defined by formula (I), wherein the groups R1 to R3, X, m, n and o are defined as in claim 1, possessing valuable pharmacological activity. Particularly the compounds are inhibitors of 11 β-hydroxysteroid dehydrogenase (HSD) 1 and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases, in particular diabetes type 2, obesity and dyslipidemia.

UREA DERIVATIVES OF BENZOMORPHANES AND RELATED SCAFFOLDS, MEDICAMENTS CONTAINING SUCH COMPOUNDS AND THEIR USE

The present invention relates to compounds defined by formula (I) wherein the groups A, B, X, m, n and o are defined as in claim 1, possessing valuable pharmacological activity. Particularly the compounds are inhibitors of 11 β-hydroxysteroid dehydrogenase (HSD) 1 and thus are suitable for treatment and prevention of diseases which can be influenced by inhibition of this enzyme, such as metabolic diseases, in particular diabetes type 2, obesity and dyslipidemia.

Synthesis and receptor assay of aromatic-ethynyl-aromatic derivatives with potent mGluR5 antagonist activity

Noncompetitive antagonists of the human metabotropic glutamate receptor subtype 5 (mGluR5) have been implicated as potential therapeutics for the treatment of a variety of nervous system disorders, including pain, anxiety, and drug addiction. To discover novel noncompetitive antagonists to the mGluR5, we initiated an SAR study around the known lead compounds MPEP and M-MPEP. Our results pointed out the critical role of the para position of the two aromatic rings, which leads to inactive products and permitted the discovery of potent mGluR5 antagonists (e.g., 16, 25, 28, 34 IC50 = 13.5, 11.9, 21, 15 nM, respectively). Noncompetitive antagonists of the human metabotropic glutamate receptor subtype 5 (mGluR5) have been implicated as potential therapeutics for the treatment of a variety of nervous system disorders, including pain, anxiety, and drug addiction. To discover novel noncompetitive antagonists to the mGluR5, we initiated an SAR study around the known lead compounds MPEP and M-MPEP. Our results pointed out the critical role of the para position of the two aromatic rings, which leads to inactive products and permitted the discovery of potent mGluR5 antagonists (e.g., 16, 25, 28, 34 IC50 = 13.5, 11.9, 21, 15 nM, respectively).

A Novel Ethynylation of Pyridines by Reissert-Henze Type Reaction

Reaction of N-benzoyloxypyridinium chloride, Reissert-Henze salt, with silver acetylide gave the pyridine ethynylated selectively at 2-position.The reaction is applicable to various substituted pyridines and pyridine homologs.