83848-59-3

Upstream product

• 56-81-5 glycerol 
• 619-17-0 4-Nitroanthranilic acid 
• 611-32-5 8-methylquinoline 
• 205046-59-9 8-cyano-5-nitroquinoline 
• 64976-62-1 8-methyl-5-nitroquinoline 

Downstream Products

• 205046-59-9 8-cyano-5-nitroquinoline 
• 80690-06-8 5-aminoquinoline-8-carboxylic acid 

Relevant academic research and scientific papers

IMMUNOMODULATORY COMPOUNDS

Disclosed are immunomodulatory compounds, pharmaceutical compositions containing them, and methods of making and using the compounds to treat diseases and disorders characterized by aberrant protein activity that can be targeted by cereblon.

Cathepsin B inhibitors: Further exploration of the nitroxoline core

Human cathepsin B is a cysteine protease with many house-keeping functions, such as intracellular proteolysis within lysosomes. Its increased activity and expression have been strongly associated with many pathological processes, including cancers. We present here the design and synthesis of novel derivatives of nitroxoline as inhibitors of cathepsin B. These were prepared either by omitting the pyridine part, or by modifying positions 2, 7, and 8 of nitroxoline. All compounds were evaluated for their ability to inhibit endopeptidase and exopeptidase activities of cathepsin B. For the most promising inhibitors, the ability to reduce extracellular and intracellular collagen IV degradation was determined, followed by their evaluation in cell-based in vitro models of tumor invasion. The presented data show that we have further defined the structural requirements for cathepsin B inhibition by nitroxoline derivatives and provided additional knowledge that could lead to non-peptidic compounds with usefulness against tumor progression.

Bicyclic modulators of androgen receptor function

The invention provides for a pharmaceutical composition capable of modulating the androgen receptor comprising a compound of formula I wherein the substitutents are as described herein. Further provided are methods of using such compounds for the treatment of nuclear hormone receptor-associated conditions, such as age related diseases, for example sarcopenia. Also provided are pharmaceutical compositions containing such compounds and processes for preparing some of the compounds of the invention.

BICYCLIC MODULATORS OF ANDROGEN RECEPTOR FUNCTION

The invention provides compounds according to formula I wherein the substitutents are as described herein. Further provided are methods of using such compounds for the treatment of nuclear hormone receptor-associated conditions, such as age related diseases, for example sarcopenia. Also provided are pharmaceutical compositions containing such compounds and processes for preparing some of the compounds of the invention.

Hetaroyl cyclohexanedione derivatives with herbicidal effect

Hetaroyl derivatives of the formula I where: R1and R2are each hydrogen, nitro, halogen, cyano, thiocyanato, hydroxyl, mercapto, C1-C6-alkyl, C1-C6-alkoxy, C1-C6-alkylthio, C1-C6-alkylsulfinyl, C1-C6-alkylsulfonyl or C1-C6-alkoxysulfonyl, where the last 6 radicals may be substituted and/or functionalized; phenyl, phenoxy, phenylthio, phenylsulfinyl or phenylsulfonyl, where the last 5 radicals may be substituted; Z is an unsubstituted or substituted four-membered unsaturated, partially or fully saturated chain consisting of three carbons and one nitrogen; Q is unsubstituted or substituted cyclohexane-1,3-dione linked at position 2; and their agriculturally useful salts. A process for preparing the hetaroyl derivatives, compositions comprising them, and the use of these derivatives or these compositions comprising them for controlling undesirable plants.

4-Hetaroylpyrazol derivatives and the use thereof as herbicides

Hetaroyl derivatives of the formula I where: R1and R2are each hydrogen, nitro, halogen, cyano, thiocyanato, hydroxyl, mercapto, C1-C6-alkyl, C1-C6-alkoxy, C1-C6-alkylthio, C1-C6-alkylsulfinyl, C1-C6-alkylsulfonyl or C1-C6-alkoxysulfonyl, where the last 6 radicals may be substituted and/or functionalized; phenyl, phenoxy, phenylthio, phenylsulfinyl or phenylsulfonyl, where the last 5 radicals may be substituted; Z is an unsubstituted or substituted four-membered unsaturated, partially or fully saturated chain consisting of three carbons and one nitrogen; Q is unsubstituted or substituted hydroxypyrazole linked at position 4; and their agriculturally useful salts. A process for preparing the hetaroyl derivatives, compositions comprising them, and the use of these derivatives or these compositions comprising them for controlling undesirable plants.