99847-13-9

Upstream product

• 99419-89-3 3-nitro-biphenyl-4-carbonitrile 
• 106166-59-0 3-nitro-biphenyl-4-carboxylic acid amide 
• 158580-57-5 methyl 4-bromo-2-nitrobenzoate 
• 98-80-6 phenylboronic acid 
• 2113-58-8 3-nitro-1,1'-biphenyl 
• 99277-71-1 4-bromo-2-nitrobenzoic acid 
• 42087-80-9 methyl 4-chloro-2-nitrobenzoate 
• 154605-88-6 methyl 2-nitro-4-phenylbenzoate 
• 515878-88-3 3-nitro-biphenyl-4-carbaldehyde 

Downstream Products

• 4445-43-6 3-amino-[1,1'-biphenyl]-4-carboxylic acid 
• 887242-95-7 1,1-dimethylethyl (2S)-cyclohexyl-{[(3-nitro-4-biphenylyl)carbonyl]amino}-ethanoate 
• 1431382-12-5 C₁₇H₁₂BrNO₄S₂ 
• 1447083-18-2 C₁₈H₁₄BrNO₄S₂ 
• 1352638-16-4 3-nitrobiphenyl-4-carboxylic acid (3,4-dihydroxy-5-methoxyphenyl)amide 
• 1352637-93-4 3-nitrobiphenyl-4-carboxylic acid (3,4,5-trimethoxyphenyl)amide 
• 100965-88-6 3-nitro-7-phenyl-quinolin-4-ol 
• 108618-34-4 3-amino-7-phenyl-quinolin-4-ol 
• 515878-89-4 3-nitro-biphenyl-4-carboxylic acid [3-methoxy-4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-amide 
• 515878-90-7 3-amino-biphenyl-4-carboxylic acid [3-methoxy-4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-amide 

Relevant academic research and scientific papers

Copper-catalyzed oxidative decarboxylative C-H arylation of benzoxazoles with 2-nitrobenzoic acids

A copper-catalyzed oxidative decarboxylative coupling of benzoxazoles with 2-nitrobenzoic acids was developed. This methodology favors electron-rich benzoxazoles and electron-deficient benzoic acids and enables the preparation of a variety of arylated benzoxazoles in good yields. The trends in product yields suggest a delicate balance between the decarboxylation and C-H arylation steps.

Discovery of a novel series of non-nucleoside thumb pocket 2 HCV NS5B polymerase inhibitors

A novel series of non-nucleoside thumb pocket 2 HCV NS5B polymerase inhibitors were derived from a fragment-based approach using information from X-ray crystallographic analysis of NS5B-inhibitor complexes and iterative rounds of parallel synthesis. Structure-based drug design strategies led to the discovery of potent sub-micromolar inhibitors 11a-c and 12a-c from a weak-binding fragment-like structure 1 as a starting point.

Potent galloyl-based selective modulators targeting multidrug resistance associated protein 1 and P-glycoprotein

The multifactorial nature of chemotherapy failure in controlling cancer is often associated with the occurrence of multidrug resistance (MDR), a phenomenon likely related to the increased expression of members of the ATP binding cassette (ABC) transporter superfamily. In this respect, the most extensively characterized MDR transporters include ABCB1 (also known as MDR1 or P-glycoprotein) and ABCC1 (also known as MRP1) whose inhibition remains a priority to circumvent drug resistance. Herein, we report how the simple galloyl benzamide scaffold can be easily and properly decorated for the preparation of either MRP1 or P-gp highly selective inhibitors. In particular, some gallamides and pyrogallol-1-monomethyl ethers showed remarkable affinity and selectivity toward MRP1. On the other hand, trimethyl ether galloyl anilides, with few exceptions, exhibited moderate to very high and selective P-gp inhibition.

Anthranilimide based glycogen phosphorylase inhibitors for the treatment of type 2 diabetes. Part 3: X-ray crystallographic characterization, core and urea optimization and in vivo efficacy

Key binding interactions of the anthranilimide based glycogen phosphorylase a (GPa) inhibitor 2 from X-ray crystallography studies are described. This series of compounds bind to the AMP site of GP. Using the binding information the core and the phenyl ur

Discovery of potent and stable conformationally constrained analogues of the MCH R1 antagonist SB-568849

A strategy of systematically targeting more rigid analogues of the known MCH R1 receptor antagonist, SB-568849, serendipitously uncovered a binding mode accessible to N-aryl-phthalimide ligands. Optimisation to improve the stability of this compound class led to the discovery of novel N-aryl-quinazolinones, benzotriazinones and thienopyrimidinones as selective ligands with good affinity for human melanin-concentrating hormone receptor 1.

GLYCOGEN PHOSPHORYLASE INHIBITOR COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS THEREOF

The invention relates to glycogen phosphorylase inhibitor compounds, pharmaceutical compositions of these compounds, methods of treatment using the pharmaceutical compositions to treat diabetes, conditions associated with diabetes, and/or tissue ischemia,

New carboxamide compounds having melanin concentrating hormone antagonistic activity, pharmaceutical preparations comprising these compounds and process for their manufacture

The present invention relates to carboxamide compounds of general formula I wherein the groups and residues A, B, W, X, Y, Z, R1, R2, R3 and k have the meanings given in claim 1. Moreover the invention relates to process for preparing the above mentioned carboxamides as well as pharmaceutical compositions containing at least one carboxamide according to the invention. In view of their MCH-receptor antagonistic activity the pharmaceutical compositions according to the invention are suitable for the treatment of metabolic disorders and/or eating disorders, particularly obesity, bulimia, anorexia, hyperphagia and diabetes.

Biaryl substituted alkylboronate esters as thrombin inhibitors

Thrombin is a serine protease that plays an important role in the blood coagulation cascade, and is a target enzyme for new therapeutic agents. Ac- (D)-Phe-Pro-boroArg-OH (DuP 714) was found to be a highly effective thrombin inhibitor. In order to reduce the peptidic nature of DuP 714, we have designed a series of novel biaryl substituted alkylboronate esters as potent thrombin inhibitors. The most potent compounds have subnanomolar affinity for thrombin.