- PYRROLE DERIVATIVES AS ACC INHIBITORS
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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).
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Page/Page column 78; 81
(2020/12/29)
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- Nickel-Catalyzed Formal Aminocarbonylation of Unactivated Alkyl Iodides with Isocyanides
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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.
- Chen, Yifeng,Huang, Wenyi,Qu, Jingping,Shrestha, Mohini,Wang, Yun,Weng, Yangyang
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supporting information
p. 3245 - 3250
(2020/04/21)
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- POLYCYCLIC COMPOUNDS AND METHODS FOR THE TARGETED DEGRADATION OF RAPIDLY ACCELERATED FIBROSARCOMA POLYPEPTIDES
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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.
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Paragraph 1460; 1461
(2020/03/29)
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- A benzenesulfonamide derivative as a novel PET radioligand for CXCR4
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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
- Goodman, Mark M.,Liang, Zhongxing,Oum, Yoon Hyeun,Shetty, Dinesh,Shim, Hyunsuk,Voll, Ronald J.,Yoon, Younghyoun
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- Visible-Light-Mediated Aerobic Oxidation of Organoboron Compounds Using in Situ Generated Hydrogen Peroxide
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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.
- Weng, Wei-Zhi,Liang, Hao,Zhang, Bo
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supporting information
p. 4979 - 4983
(2018/08/24)
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- Polymerizable compound optical element
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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.
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Paragraph 0175; 0176
(2017/08/26)
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- METHYLSULFONAMIDE DERIVATIVES AND USES RELATED THERETO
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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
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Page/Page column 72-73
(2017/02/28)
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- A robust and simple protocol for the synthesis of arylfluorophosphonates
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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.
- Leypold, Mario,Wallace, Paal W.,Kljajic, Marko,Schittmayer, Matthias,Pletz, Jakob,Illaszewicz-Trattner, Carina,Guebitz, Georg M.,Birner-Gruenberger, Ruth,Breinbauer, Rolf
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supporting information
p. 5619 - 5622
(2015/09/21)
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- For organic electronic device, modified stable electrode having a work function and method
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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.
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Paragraph 0065
(2017/01/05)
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- INDOLE AND INDAZOLE COMPOUNDS THAT ACTIVATE AMPK
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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.
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Paragraph 0853
(2013/10/22)
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- Click chemistry based synthesis of dopamine D4 selective receptor ligands for the selection of potential PET tracers
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Taking advantage of click chemistry, a library of N-arylpiperazinylmethyl triazoles bearing fluoro substituted appendages was synthesized and the target compounds were investigated for dopamine and serotonin receptor binding. With the aim to bias their hydrophilicity and to optimize their D4 receptor affinity and selectivity, a concise series of triazoles containing fluoroalkyl, fluoroalkoxy, fluoroalkoxyphenyl, and deoxyfluoroglucosyl substituents was studied. The D4 receptor affinity and selectivity could be tuned by altering the chemical moiety attached to the triazole unit. Among the test compounds, the fluoroethoxyphenyl derivative 15b showed weak partial agonism at D4 and a K i value of 14 nM, while its fluoropropoxyphenyl homologue 16a turned out to act as a neutral D4 antagonist (Ki = 5.1 nM). Both, 15b and 16a revealed an excellent balance between D4 receptor affinity and subtype selectivity, providing lead candidates for the development of 18F-labeled radioligands for D4 receptor imaging studies by positron emission tomography (PET).
- Banerjee, Ashutosh,Maschauer, Simone,Hübner, Harald,Gmeiner, Peter,Prante, Olaf
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p. 6079 - 6082
(2013/11/06)
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- Stable electrodes with modified work functions and methods for organic electronic devices
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One embodiment is a method, comprising: depositing a molecule on an electrode, wherein the electrode has a surface and the molecule has a binding group (e.g., an anchoring group) that binds to the surface, thereby providing a work function that is stable for at least 100 hours under ambient conditions.
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- 2-PYRIDONE COMPOUNDS
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A 2-pyridone compound represented by the formula [1]: {wherein in the formula [1], the ring represented by A represents a benzene ring or a pyridine ring, X represents any of the structures represented by the formulas [3] shown below: V represents a single bond or a lower alkylene group, and W represents a single bond, an ether bond or a lower alkylene group (wherein the lower alkylene group may contain an ether bond)}, a tautomer or stereoisomer of the compound, a pharmaceutically acceptable salt thereof, or a solvate thereof is a compound that has an excellent GK activating effect and is useful as a pharmaceutical.
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Page/Page column 81
(2011/10/12)
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- ELECTRONIC DEVICES COMPRISING NOVEL PHOSPHONIC ACID SURFACE MODIFIERS
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In some embodiments, the inventions described herein relate to a composition of matter comprising a molecule having the structure: wherein: independently at each occurrence, R1 is a halogen, a alkyl group, a heteroalkyl group, an aryl group, or a heteroaryl group; R2 comprises from 3 to 30 CH2- groups, n = 0-5, m = 0-5, q = 1-3, and R2 comprises at least one ether linkage
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Page/Page column 28; 29
(2010/11/03)
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- An efficient F-18 labeling method for PET study: Huisgen 1,3-dipolar cycloaddition of bioactive substances and F-18-labeled compounds
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The Cu(I)-catalyzed, 1,3-dipolar cycloaddition reaction was applied successfully to the synthesis of small, F-18-labeled biomolecules, and an optimal condition was developed for one-pot, two-step reaction without any interim purifications. This technique was employed in various F-18-labeled, 1,2,3-triazole syntheses with high radiochemical yield.
- Sirion, Uthaiwan,Kim, Hee Jun,Lee, Jae Hak,Seo, Jai Woong,Lee, Byoung Se,Lee, Sang Ju,Oh, Seung Jun,Chi, Dae Yoon
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p. 3953 - 3957
(2008/02/04)
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- Polymerizable liquid crystalline dioxetanes, their preparation and use
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New photopolymerizable liquid crystalline dioxetane compounds are provided. having the general formula I: wherein R1 and R2 are independently selected from straight or branched C1-C4 alkyl and hydrogen; X and X′ are independently selected from oxygen, sulfur, a single covalent bond, —O—CO—, —CO—O—, and —O—CO—O—; Y and Y′ are spacer groups having each independently 1 to 30 carbon atoms (linear or branched), in which the carbon chain may be interrupted by oxygen in the ether function or by sulfur in the thioether function; Z and Z′ are independently selected from oxygen, sulfur, a single covalent bond, —O—CO—, —CO—O—, and —O—CO—O—; and M is any suitable mesogenic group. Also, compositions are provided containing one or more compounds of formula I, as well as methods of preparing said compounds and compositions. These compounds and compositions show excellent characteristics upon polymerization, such as improved non-shrinking properties, and are useful in a variety of applications, in particular in liquid crystal devices, sensors, and optical precision instruments. ?
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- Synthesis of photo-crosslinkable hole-transport polymers with tunable oxidation potentials and their use in organic light-emitting diodes
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A series of photo-crosslinkable arylamine-based hole-transport copolymers has been synthesized. The synthetic methodology employed allows for the redox potential of the polymer to be tuned by the incorporation of electron-donating or -withdrawing moieties. Upon exposure to ultraviolet radiation, the polymers become insoluble, as evidenced by UV/Vis absorption spectroscopy, a feature that is useful for the fabrication of multilayer organic light-emitting diodes (OLEDs) by solution processing techniques. OLEDs based on these hole-transport polymers have been fabricated and the performance of the devices has been evaluated. The photo-crosslinking process has been optimized so that it no longer adversely impacts device performance.
- Hreha, Richard D.,Zhang, Ya-Dong,Domercq, Benoit,Larribeau, Nathalie,Haddock, Joshua N.,Kippelen, Bernard,Marder, Seth R.
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p. 1201 - 1212
(2007/10/03)
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- Anilide derivative, production and use thereof
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This invention is to provide a compound of the formula: wherein R1is an optionally substituted 5- to 6-membered ring; the ring A is an optionally substituted 6- to 7-membered ring; the ring B is an optionally substituted benzene ring; n is an integer of 1 or 2; Z is a chemical bond or a divalent group; R2is (1) an optionally substituted amino group in which a nitrogen atom may form a quaternary ammonium, (2) an optionally substituted nitrogen-containing heterocyclic ring group which may contain a sulfur atom or an oxygen atom as ring constituting atoms and wherein a nitrogen atom may form a quaternary ammonium, (3) a group binding through a sulfur atom or (4) a group of the formula: ?wherein k is 0 or 1, and when k is 0, a phosphorus atom may form a phosphonium; and R5and R6are independently an optionally substituted hydrocarbon group, an optionally substituted hydroxy group or an optionally substituted amino group, and R5and R6may bind to each other to form a cyclic group together with the adjacent phosphorus atom, or a salt thereof , which is useful for antagonizing CCR5 and also for the prevention and treatment of infectious disease of HIV.
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- BIS(ARYLOXY)ALKANES AS INHIBITORS OF PHOSPHOLIPASE A2 ENZYMES
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Compounds having the formula I: STR1 are inhibitors of the PLA 2 s enzymes. These compounds are useful as anti-allergic, anti-asthmatic, they are also useful in treating various inflammatory diseases such as rheumatoid arthritis, osteoarthritis, bursitis,
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