79568-32-4

Upstream product

• 53244-68-1 2-(methylthio)-4,4-dimethyl-4,5-dihydro-1,3-oxazole 
• 22873-28-5 p-ethylphenylmagnesium bromide 
• 619-64-7 p-ethylbenzoic acid 
• 124-68-5 2-Amino-2-methyl-1-propanol 
• 16331-45-6 p-ethylbenzoyl chloride 
• 1156590-09-8 C₁₃H₁₉NO₂ 

Relevant academic research and scientific papers

Analogues of doxanthrine reveal differences between the dopamine D 1 receptor binding properties of chromanoisoquinolines and hexahydrobenzo[a]phenanthridines

Efforts to develop selective agonists for dopamine D1-like receptors led to the discovery of dihydrexidine and doxanthrine, two bioisosteric β-phenyldopamine-type full agonist ligands that display selectivity and potency at D1-like receptors. We report herein an improved methodology for the synthesis of substituted chromanoisoquinolines (doxanthrine derivatives) and the evaluation of several new compounds for their ability to bind to D1- and D2-like receptors. Identical pendant phenyl ring substitutions on the dihydrexidine and doxanthrine templates surprisingly led to different effects on D1-like receptor binding, suggesting important differences between the interactions of these ligands with the D1 receptor. We propose, based on the biological results and molecular modeling studies, that slight conformational differences between the tetralin and chroman-based compounds lead to a shift in the location of the pendant ring substituents within the receptor.

Bioavailable diacylhydrazine ligands for modulating the expression of exogenous genes via an ecdysone receptor complex

The present invention relates to non-steroidal ligands for use in nuclear receptor-based inducible gene expression system, and a method to modulate exogenous gene expression in which an ecdysone receptor complex comprising: a DNA binding domain; a ligand binding domain; a transactivation domain; and a ligand is contacted with a DNA construct comprising: the exogenous gene and a response element; wherein the exogenous gene is under the control of the response element and binding of the DNA binding domain to the response element in the presence of the ligand results in activation or suppression of the gene.

Spiro compounds

Compounds of the general formula (I): wherein Ar1represents optionally substituted aryl or heteroaryl; n represents 0 or 1; T, U, V, and W each independently represent nitrogen atom or optionally substituted methine group, where at least two of them represent the said methine group; X represents methine or hydroxy substituted methine; Y represents an optionally substituted imino or oxygen atom are described and claimed. These novel spiro compounds are useful as neuropeptide Y receptor antagonists and as agents for the treatment of various kinds of cardiovascular disorders, central nervous system disorders, metabolic diseases and the like.

Novel spiro compounds

Compounds of the general formula (I): wherein Ar1 represents optionally substituted aryl or heteroaryl; n represents 0 or 1; T, U, V, and W each independently represent nitrogen atom or optionally substituted methine group, where at least two of them represent the said methine group; X represents methine or hydroxy substituted methine; Y represents an optionally substituted imino or oxygen atom are described and claimed. These novel spiro compounds are useful as neuropeptide Y receptor antagonists and as agents for the treatment of various kinds of cardiovascular disorders, central nervous system disorders, metabolic diseases and the like.

Spiro compounds

Spiro compounds of the general formula (I): wherein Ar1represents an optionally substituted aryl or heteroaryl; n represents 0 or 1; T, U, V and W each represent a nitrogen atom or an optionally substituted methine group, wherein at least two of which represent said methine group; X represents methine; Y represents an optionally substituted imino or oxygen atom. These novel spiro compounds exhibit neuropeptide Y receptor (NPY) antagonistic activities and are useful as agents for the treatment of various diseases related to NPY, for example, cardiovascular disorders, central nervous system disorders, metobolic diseases and the like.

Spiro compounds

Spiro compounds of the general formula (I): wherein Ar1represents an optionally substituted aryl or heteroaryl; n represents 0 or 1; T, U, V and W each represent a nitrogen atom or an optionally substituted methine group, wherein at least two of which represent said methine group; X represents nitrogen; Y represents an optionally substituted imino or oxygen atom, which exhibit neuropeptide Y receptor (NPY) antagonistic activities and are useful as agents for the treatment of various diseases related to NPY, for example, cardiovascular disorders, central nervous system disorders, metobolic diseases and the like.

2,4-Dithi(oxo)-pyrimidin-5-yl compounds bearing a tricyclic substituent useful as P2 purinoceptor antagonists

PCT No. PCT/SE98/01240 Sec. 371 Date Sep. 30, 1998 Sec. 102(e) Date Sep. 30, 1998 PCT Filed Jun. 25, 1998 PCT Pub. No. WO99/02501 PCT Pub. Date Jan. 21, 1999The invention relates to new pharmaceutically active compounds which are P2-purinoceptor 7-transmembrane (TM) G-protein coupled receptor antagonists, compositions containing them and processes for their preparation.

New Synthesis of 2-Substituted 2-Oxazolines: Transition-Metal-Catalyzed Cross-Coupling of Grignards with 2-(Methylthio)-4,4-dimethyl-2-oxazoline

A new synthesis of 2-aryl-4,4-dimethyl-2-oxazolines (18a-e) using nickel- and palladium-phosphine complexes to catalyze cross-coupling of Grignard reagents 17 with 2-(methylthio)-4,4-dimethyl-2-oxazoline (16) is described.This reaction represents the firs