21900-55-0

Upstream product

• 59748-90-2 4-Bromo-2-chloro-benzoic Acid 
• 89794-02-5 4-bromo-2-chlorotoluene 
• 119-32-4 4-Methyl-3-nitroanilin 
• 79-37-8 oxalyl dichloride 

Downstream Products

• 119878-34-1 4-Bromo-2-chloro-N-methyl-N-((5S,6R)-1-methyl-1-aza-spiro[4.5]dec-6-yl)-benzamide 
• 220461-97-2 (4-bromo-2-chloro-phenyl)-(5H,11H-pyrrolo[2,1-c][1,4]benzodiazepin-10-yl)-methanone 
• 252942-04-4 6-[(2-{[4-(4-bromo-2-chlorophenyl)-5-imidazol-2-ylpyrimidin-2-yl]amino}ethyl)amino]pyridine-3-carbonitrile 
• 252942-05-5 [4-(4-bromo-2-chlorophenyl)-5-imidazol-2-ylpyrimidin-2-yl](2-{[5-(trifluoromethyl)(2-pyridyl)]amino}ethyl)amine 
• 1157320-16-5 C₇H₃BrClN₃O 
• 1380546-69-9 4-bromo-2-(3-butylhept-2-enyl)-6-chloro-N-methoxybenzamide 
• 1371391-85-3 4-bromo-2-chloro-N-methoxybenzamide 
• 131994-27-9 ethyl 1-(4-fluorophenyl)-1,4-dihydro-7-<5-(3-methylisoxazolyl)>-4-oxo-3-quinolinecarboxylate 
• 131994-24-6 ethyl 1-(4-fluorophenyl)-1,4-dihydro-4-oxo-7-<(trimethylsilyl)ethynyl>-3-quinolinecarboxylate 
• 131994-28-0 1,4-Dihydro-1-(4-fluorophenyl)-7-(3-methyl-5-isoxazolyl)-4-oxo-3-quinolinecarboxylic acid 
• 131994-26-8 ethyl 7-ethynyl-1,4-dihydro-1-(4-fluorophenyl)-4-oxo-3-quinolinecarboxylate 

Relevant academic research and scientific papers

Synthesis and SAR studies of novel benzodiazepinedione-based inhibitors of Clostridium difficile (C. difficile) toxin B (TcdB)

Synthesis and structure-activity relationships (SAR) of a novel series of benzodiazepinedione-based inhibitors of Clostridium difficile toxin B (TcdB) are described. Compounds demonstrating low nanomolar affinity for TcdB, and which possess improved stability in mouse plasma vs. earlier compounds from this series, have been identified. Optimized compound 11d demonstrates a good pharmacokinetic (PK) profile in mouse and hamster and is efficacious in a hamster survival model of Clostridium difficile infection.

Discovery of 8-Amino-imidazo[1,5-a]pyrazines as Reversible BTK Inhibitors for the Treatment of Rheumatoid Arthritis

Bruton's tyrosine kinase (BTK) is a Tec family kinase with a well-defined role in the B cell receptor (BCR) pathway. It has become an attractive kinase target for selective B cell inhibition and for the treatment of B cell related diseases. We report a series of compounds based on 8-amino-imidazo[1,5-a]pyrazine that are potent reversible BTK inhibitors with excellent kinase selectivity. Selectivity is achieved through specific interactions of the ligand with the kinase hinge and driven by aminopyridine hydrogen bondings with Ser538 and Asp539, and by hydrophobic interaction of trifluoropyridine in the back pocket. These interactions are evident in the X-ray crystal structure of the lead compounds 1 and 3 in the complex with the BTK enzyme. Our lead compounds show desirable PK profiles and efficacy in the preclinical rat collagen induced arthritis model.

NOVEL 3,5-DISUBSTITUTED-3H-IMIDAZO[4,5-B]PYRIDINE AND 3,5- DISUBSTITUTED -3H-[1,2,3]TRIAZOLO[4,5-B] PYRIDINE COMPOUNDS AS MODULATORS OF C-MET PROTEIN, ETC

The present invention provides compounds useful as c-Met protein kinase modulators, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of c-Met kinase mediated disease or disorders with them.

AROMATIC HETEROCYCLIC COMPOUND

The compound represented by the general formula: wherein ring A is benzene which may be substituted and the like; ring B is benzene which may be substituted and the like; X is a single bond and the like; Y is alkyl which may be substituted and the like; Z is CR1 or nitrogen atom; R1 is hydrogen and the like; R2 is alkyl which may be substituted and the like or a pharmaceutically acceptable salt thereof is useful as a prevention/treatment agent of obesity, diabetes, and the like.

2- PYRIDONE COMPOUND

PROBLEM TO BE SOLVED: To provide a compound that has excellent glucokinase (GK) activating action and is useful as a pharmaceutical. SOLUTION: The present invention provides a 2-pyridone compound represented by formula [1], and a tautomer or stereoisomer of the compound, or their pharmacologically acceptable salts, or their solvates (where R1 is RA-ZA-; RA is any of a carboxy group, a sulfo group or formula [5]). COPYRIGHT: (C)2016,JPOandINPIT

Synthesis and SAR of 2,3,3a,4-tetrahydro-1H-pyrrolo[3,4-c]isoquinolin- 5(9bH)-ones as 5-HT2C receptor agonists

A series of 2,3,3a,4-tetrahydro-1H-pyrrolo[3,4-c]isoquinolin-5(9bH)-ones is described, several examples of which exhibit potent 5-HT2C agonism with excellent selectivity over the closely related 5-HT2A and 5-HT2B receptors. Compounds such as 38 and 44 were shown to be effective in reducing food intake in an acute rat feeding model.

Rhodium(I)-catalyzed borylation of nitriles through the cleavage of carbon-cyano bonds

The reaction of aryl cyanides with diboron in the presence of a rhodium/Xantphos catalyst and DABCO affords arylboronic esters via carbon-cyano bond cleavage. This unprecedented mode of reactivity for a borylrhodium species allows the regioselective intro

Highly selective mild stepwise allylation of N-methoxybenzamides with allenes

An efficient Rh(III)-catalyzed stepwise ortho allylation of N-methoxybenzamides 1 with polysubstituted allenes is reported. This C-H functionalization involving allenes is conducted under very mild conditions (-20 °C or room temperature) and compatible wi

ANTAGONISTS OF LYSOPHOSPHATIDIC ACID RECEPTORS

Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases.

Facile preparation of protected benzylic and heteroarylmethyl amines via room temperature Curtius rearrangement

A step-wise, room temperature procedure for acyl azide formation and the subsequent Curtius rearrangement of phenyl and heteroaryl acetic acids is described. We have developed a protocol for room temperature Curtius rearrangement in MeOH or CHCl3 that provides an improvement over standard conditions, avoiding the use of additives or heat. This room temperature optimization of the Curtius rearrangement prevents the formation of side products often observed with benzylic acids, allowing access to a variety of benzylic and heteroarylmethyl amines.