67900-64-5Relevant articles and documents
PYRROLE DERIVATIVES AS ACC INHIBITORS
-
Page/Page column 78; 81, (2020/12/29)
Novel pyrrole derivatives of Formula (I) are disclosed; as well as processes for their preparation, pharmaceutical compositions comprising them and their use in therapy as inhibitors of Acetyl- CoA carboxylase (ACC).
Nickel-Catalyzed Formal Aminocarbonylation of Unactivated Alkyl Iodides with Isocyanides
Chen, Yifeng,Huang, Wenyi,Qu, Jingping,Shrestha, Mohini,Wang, Yun,Weng, Yangyang
supporting information, p. 3245 - 3250 (2020/04/21)
Herein, we disclose a Ni-catalyzed formal aminocarbonylation of primary and secondary unactivated aliphatic iodides with isocyanides to afford alkyl amide, which proceeds via the selective monomigratory insertion of isocyanides with alkyl iodides, subsequent β-hydride elimination, and hydrolysis process. The reaction features wide functional group tolerance under mild conditions. Additionally, the selective, one-pot hydrolysis of reaction mixture under acid conditions allows for expedient synthesis of the corresponding alkyl carboxylic acid.
POLYCYCLIC COMPOUNDS AND METHODS FOR THE TARGETED DEGRADATION OF RAPIDLY ACCELERATED FIBROSARCOMA POLYPEPTIDES
-
Paragraph 1460; 1461, (2020/03/29)
The present disclosure relates to bifunctional compounds, ULM— L—PTM, which find utility as modulators of Rapidly Accelerated Fibrosarcoma (RAF, such as c-RAF, A- RAF and/or B-RAF; the target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a Von Hippel-Lindau, cereblon, Inhibitors of Apotosis Proteins or mouse double-minute homolog 2 ligand which binds to the respective E3 ubiquitin ligase and on the other end a moiety which binds the target protein RAF, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein, or the constitutive activation of the target protein, are treated or prevented with compounds and compositions of the present disclosure.
A benzenesulfonamide derivative as a novel PET radioligand for CXCR4
Goodman, Mark M.,Liang, Zhongxing,Oum, Yoon Hyeun,Shetty, Dinesh,Shim, Hyunsuk,Voll, Ronald J.,Yoon, Younghyoun
, (2019/12/25)
CXCR4 is involved in various diseases such as inflammation, tumor growth, and cancer metastasis through the interaction with its natural endogenous ligand, chemokine CXCL12. In an effort to develop imaging probes for CXCR4, we developed a novel small mole
Visible-Light-Mediated Aerobic Oxidation of Organoboron Compounds Using in Situ Generated Hydrogen Peroxide
Weng, Wei-Zhi,Liang, Hao,Zhang, Bo
supporting information, p. 4979 - 4983 (2018/08/24)
A simple and general visible-light-mediated oxidation of organoboron compounds has been developed with rose bengal as the photocatalyst, substoichiometric Et3N as the electron donor, as well as air as the oxidant. This mild and metal-free protocol shows a broad substrate scope and provides a wide range of aliphatic alcohols and phenols in moderate to excellent yields. Notably, the robustness of this method is demonstrated on the stereospecific aerobic oxidation of organoboron compounds.
Polymerizable compound optical element
-
Paragraph 0175; 0176, (2017/08/26)
PROBLEM TO BE SOLVED: To provide a polymerizable compound which has high solubility with a liquid crystal material and which has little amount of uncured monomers, high stability of a pretilt angle and hardly causes seizure when the compound is added to a liquid crystal material to manufacture a PSA (polymer sustained alignment) display element, and to provide a liquid crystal material containing the polymerizable compound.SOLUTION: The polymerizable compound is expressed by general formula (I). Further, a composition, a liquid crystal composition and an optical element including the compound are also provided.
METHYLSULFONAMIDE DERIVATIVES AND USES RELATED THERETO
-
Page/Page column 72-73, (2017/02/28)
This disclosure relates to methylsulfonamide derivatives and uses as imaging agents and other uses related to CXCR4 inhibition. In certain embodiments, the disclosure relates to pharmaceutical compositions comprising compounds disclosed herein, derivative
A robust and simple protocol for the synthesis of arylfluorophosphonates
Leypold, Mario,Wallace, Paal W.,Kljajic, Marko,Schittmayer, Matthias,Pletz, Jakob,Illaszewicz-Trattner, Carina,Guebitz, Georg M.,Birner-Gruenberger, Ruth,Breinbauer, Rolf
supporting information, p. 5619 - 5622 (2015/09/21)
Fluorophosphonates represent powerful probes for the identification and analysis of active serine hydrolases in activity based protein profiling. Although alkylphosphonofluoridates are widely used for such purposes, little is known about the synthesis and purification of arylphosphonofluoridates, which may be useful tools for screening enzyme activities toward aromatic esters. Our optimized route makes this subclass of transition state inhibitors broadly accessible for a diverse series of phosphonic acid derivatives using a combination of selective monoesterification with EDC·HCl and subsequent mild fluorination with DAST. All compounds were isolated as pure materials using a simple acid-base extraction protocol in 76-93% yields over two steps. These probes can be stored under an inert atmosphere at -24 °C for several months without significant degradation.
For organic electronic device, modified stable electrode having a work function and method
-
Paragraph 0065, (2017/01/05)
A device including an electrode, the electrode having a surface; a molecule bound to the surface of the electrode through a binding group; an organic electronic material in electrical contact with the electrode, wherein the molecule comprises at least one fluorinated aryl group, wherein the electrode contains a transparent conductive metal oxide, a carbon nanotube, or graphene.
INDOLE AND INDAZOLE COMPOUNDS THAT ACTIVATE AMPK
-
Paragraph 0853, (2013/10/22)
The present invention relates to indole and indazole compounds of Formula (I) that activate 5′ adenosine monophosphate-activated protein kinase (AMPK). The invention also encompasses pharmaceutical compositions containing these compounds and methods for treating or preventing diseases, conditions, or disorders ameliorated by activation of AMPK.
