288569-60-8

Usage

Uses

Used in Pharmaceutical Industry:
1-cyanocyclopropyl 4-methylbenzenesulfonate is used as a key intermediate in the synthesis of various pharmaceuticals for its ability to facilitate the formation of new chemical entities through substitution reactions.
Used in Agrochemical Industry:
In the agrochemical sector, 1-cyanocyclopropyl 4-methylbenzenesulfonate is utilized as a precursor in the development of new agrochemicals, contributing to the creation of innovative products for crop protection and enhancement.
Used in Organic Synthesis:
As a building block in organic synthesis, 1-cyanocyclopropyl 4-methylbenzenesulfonate is employed for the preparation of a wide range of organic compounds, expanding the scope of chemical research and development.

Upstream product

• 4124-41-8 p-toluenesulfonylanhydride 
• 98730-77-9 1-hydroxymethyl-cyclopropanecarbonitrile 
• 98-59-9 p-toluenesulfonyl chloride 

Downstream Products

• 1162670-03-2 1-(4-chloro-2-formyl-phenoxymethyl)-cyclopropanecarbonitrile 

Relevant academic research and scientific papers

XANTHINE CB1 INHIBITORS

Disclosed are compounds having structural formula (I), and related pharmaceutical compositions. Also disclosed are therapeutic methods, e.g., of treating diseases such as diabetic kidney disease, diabetic nephropathy, obesity-related kidney disease, focal segmental glomerular sclerosis, IgA nephropathy, nephrotic syndrome, kidney fibrosis, Prader Willi syndrome, metabolic syndrome, gastrointestinal diseases, non-alcoholic liver disease, alcoholic liver disease, or non-alcoholic fatty liver disease, using the compounds of Formula (I).

AZD0284, a Potent, Selective, and Orally Bioavailable Inverse Agonist of Retinoic Acid Receptor-Related Orphan Receptor C2

Inverse agonists of the nuclear receptor RORC2 have been widely pursued as a potential treatment for a variety of autoimmune diseases. We have discovered a novel series of isoindoline-based inverse agonists of the nuclear receptor RORC2, derived from our recently disclosed RORC2 inverse agonist 2 . Extensive structure-activity relationship (SAR) studies resulted in AZD0284 ( 20 ), which combined potent inhibition of IL-17A secretion from primary human TH17 cells with excellent metabolic stability and good PK in preclinical species. In two preclinicalin vivostudies, compound 20 reduced thymocyte numbers in mice and showed dose-dependent reduction of IL-17A containing γδ-T cells and of IL-17A and IL-22 RNA in the imiquimod induced inflammation model. Based on these data and a favorable safety profile, 20 was progressed to phase 1 clinical studies.

Novel Compounds

The present specification provides a compound of formula (I): or a pharmaceutically acceptable salt thereof; a process for preparing such a compound; and to the use of such a compound in the treatment of an RORγ and/or RORγt mediated disease state.

HETEROCYCLIC COMPOUND

Provided is a compound having a melanin-concentrating hormone receptor antagonistic action and is useful as an agent for the prophylaxis or treatment of obesity and the like. A compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof.

MACROCYCLIC FACTOR VIIA INHIBITORS

The present invention provides compounds of Formula (I): as defined in the specification and compositions comprising any of such novel compounds. These compounds are Factor VIIa inhibitors which may be used as medicaments.

Discovery and optimization of piperidyl benzamide derivatives as a novel class of 11β-HSD1 inhibitors

Discovery and optimization of a piperidyl benzamide series of 11β-HSD1 inhibitors is described. This series was derived from a cyclohexyl benzamide lead structures to address PXR selectivity, high non-specific protein binding, poor solubility, limited in

Spiroindolinone Derivatives

There are provided compounds of the formula and pharmaceutically acceptable salts and esters and enantiomers thereof wherein W, X, X′, Y, V, V′, A, B and R are as described herein. The compounds have utility as antiproliferative agents, especially, as anticancer agents.

Distinctive molecular inhibition mechanisms for selective inhibitors of human 11β-hydroxysteroid dehydrogenase type 1

11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) catalyzes the NADPH dependent interconversion of inactive cortisone to active cortisol. Excess 11β-HSD1 or cortisol leads to insulin resistance and metabolic syndrome in animal models and in humans. Inhibiting 11β-HSD1 activity signifies a promising therapeutic strategy in the treatment of Type 2 diabetes and related diseases. Herein, we report two highly potent and selective small molecule inhibitors of human 11β-HSD1. While compound 1, a sulfonamide, functions as a simple substrate competitive inhibitor, compound 2, a triazole, shows the kinetic profile of a mixed inhibitor. Co-crystal structures reveal that both compounds occupy the 11β-HSD1 catalytic site, but present distinct molecular interactions with the protein. Strikingly, compound 2 interacts much closer to the cofactor NADP+ and likely modifies its binding. Together, the structural and kinetic analyses demonstrate two distinctive molecular inhibition mechanisms, providing valuable information for future inhibitor design.

Cyclic substituted fused pyrrolocarbazoles and isoindolones

The present invention is directed to cyclic substituted fused pyrrolocarbazoles and isoindolones. The invention also is directed to methods for making and using the cyclic substituted fused pyrrolocarbazoles and isoindolones.