119744-44-4

Upstream product

• 6555-33-5 3(R)-(4-nitrophenyl)butanoic acid 
• 75-65-0 tert-butyl alcohol 
• 24424-99-5 di-tert-butyl dicarbonate 
• 80258-61-3 3-(4-nitrophenyl)propan-1-amine 
• 2038-57-5 3-Phenylpropan-1-amine 
• 637-59-2 1-Bromo-3-phenylpropane 
• 53712-77-9 1-bromo-3-(4-nitrophenyl)propane 
• 93324-23-3 N-[3-(4-nitrophenyl)propyl]-phthalimide 
• 636-98-6 p-nitrobenzene iodide 
• 78888-18-3 N-tert-butoxycarbonylprop-2-en-1-amine 

Downstream Products

• 56946-60-2 3-(4-nitro-phenyl)-propylamine; hydrochloride 

Relevant academic research and scientific papers

A novel series of 2-carboxytetrahydroquinolines provides new insights into the eastern region of glycine site NMDA antagonists

A series of potent 4-substituted tetrahydroquinolines has been synthesized and biologically tested in order to refine the eastern region of the pharmacophore model for glycine site NMDA antagonists concerning the assessment of lipophilicity, flexibility, and hydrogen bonding. Displacement studies on rat cortical membranes using [3H]-5,7-dichlorokynurenic acid as a radioligand indicated that binding affinities are markedly enhanced when additional hydrogen-accepting groups are introduced into the eastern region of the 2-carboxytetrahydroquinolines. Among the most potent ligands were some urea, sulfonylurea, and crown ether compounds as interesting leads for new diagnostics, especially for the evaluation of PET tracers, which allow biodistribution studies and NMDA receptor studies in the living organism.

SULFONAMIDE COMPOUNDS TARGETING CD73 AND ADENOSINE RECEPTORS

The present invention relates to bispecific compound of formula (I) as dual inhibitors of CD73 and adenosine receptors. The present invention also relates to pharmaceutical compositions comprising said compounds or a pharmaceutically acceptable salt or a stereoisomer or a prodrug thereof and use of such compounds in the treatment of diseases mediated by CD73 and/or adenosine receptors, particularly A2aR or A2bR.

CHLORO-PYRAZINE CARBOXAMIDE DERIVATIVES WITH EPITHELIAL SODIUM CHANNEL BLOCKING ACTIVITY

This invention provides compounds of the formula I: and their pharmaceutically acceptable salts, useful as sodium channel blockers, compositions containing the same, therapeutic methods and uses for the same and processes for preparing the same.

MACROCYCLES AS KINASE INHIBITORS

Compounds of the formula I in which X, Y, Q1, M, Q2 and B have the meanings indicated in Claim 1, are inhibitors of GCN2, and can be employed, inter alia, for the treatment of cancer.

Synthesis and evaluation of novel phenylethanolamine derivatives containing acetanilides as potent and selective b 3-adrenergic receptor agonists

In the search for potent and selective human β3-adrenergic receptor (AR) agonists as potential pharmacotherapies for the treatment of obesity and non-insulin dependent (type II) diabetes, we prepared a novel series of phenylethanolamine derivatives containing acetanilides and evaluated their biological activities at the human β3-, β2-, and β1-ARs. Among these compounds, the 6-amino-2-pyridylacetanilide (36b), 2-amino-5- methylthiazol- 4-ylacetanilide (36g), and 5-amino-1,2,4-thiadiazol-3- ylacetanilide (36h) derivatives showed potent agonistic activity at the β3-AR with functional selectivity over the β1- and β2-ARs. In addition, these compounds exhibited significant hypoglycemic activity in a rodent diabetic model.

A new type of ketolides bearing an N-aryl-alkyl acetamide moiety at the C-9 iminoether synthesis and structure-activity relationships

A new type of ketolides, bearing an N-aryl-alkyl acetamide moiety at the C-9 iminoether and a cyclic carbonate at the C-11,12 position was prepared and the antibacterial activities of the compounds were evaluated. Some of the derivatives showed potent ant

Peripherally Acting Enkephalin Analogues. 2. Polar Tri- and Tetrapeptides

The design, synthesis, and biological activity of a series of -Arg2-enkephalin-derived tetrapeptide amides and tripeptide aralkylamides are reported.These polar analogues were designed to be excluded from the central nervous system with their action thus limited to peripheral opioid receptors.The effects of the nature of the aromatic ring, aryl ring substitution, and aralkylamine chain length on activity were investigated; in a number of cases the N-terminal amino group of Tyr1 was converted to a guanidino group to further increase hydrophilicity.The peptides were all synthesized by classical solution methodology.The opioid activit y of the peptides was assessed in vitro on the guinea pig ileum and their antinociceptive activity was determined in vivo in chemically induced writhing models (peripheral activity) and in the hot-plate test (central activity), in rodents.That the analgesic effects were predominantly mediated in the periphery was demonstrated by antagonism of antinociception by the peripheral opioid antagonist N-methylnalorphine and by comparison of the activities in the writhing and hot-plate tests.As a class, the tetrapeptides were more potent than the tripeptides; Nα-amidination generally increased activity.A number of compounds exhibited very potent opioid activity and had the desired pharmacological profile, indicating a high degree of peripheral selectivity.