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Current drugs for the treatment of seizure disorders, although effective in many patients, still suffer from a number of failures and are not effective in some forms of resistant epilepsies. Historically,many of these drugs have multiple mechanisms of action including calcium and sodium channel blockade as well as GABAergic activity and thus a number of associated side effects. Modulation of the M-current through opening ofKCNQ channels has been proposed as a way to attenuate neuroexcitability and have a therapeutic benefit for the treatment of seizure disorders. Therefore, as part of our program to identify new treatments for epilepsy, we set out to identify agonists of KCNQ channels. High throughput screening of our corporate collection led to the identification of 1, adamantane-1-carboxylic acid (3-methyl-3H-benzothiazol-2-ylidine) hydrazide, a potent KCNQ2/Q3 agonist. Herein, we describe the syntheses and structure – activity relationships of analogues of 1 as well as their in vivo activity in animal models of epilepsy and neuropathic pain. 2009 American Chemical Society.

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Reference:
Tetrahydrofuran – Wikipedia,
Tetrahydrofuran | (CH2)3CH2O – PubChem

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This work develops a photocatalysis method for the synthesis of gamma-spirolactams through a tandem intramolecular 1,5-HAT reaction-cyclization process. A variety of novel gamma-spirolactams are prepared in good to excellent yields with this method. This transformation features mild reaction conditions and exceptional functional group tolerance. Additionally, gamma-terpinene is applied to this transformation as a hydrogen atom donor for the first time.

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Tetrahydrofuran – Wikipedia,
Tetrahydrofuran | (CH2)3CH2O – PubChem

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The synthesis of alpha,alpha-disubstituted beta-amino esters and peptide derivatives from readily available 4-spiro-beta-lactams 1 is described. The geminally disubstituted beta-amino esters are obtained from the N-Boc spiro beta-lactams 2 by treatment with potassium cyanide in methanol. Alternatively, the use of spiro beta-lactams 2 as acylating agents of the amino group of C-protected amino acids, allowed its direct incorporation into a peptidic chain.

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Tetrahydrofuran – Wikipedia,
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A novel class of small molecule NPY Y5 antagonists based around an azabicyclo[3.1.0]hexane scaffold was identified through modification of a screening hit. Structure-activity relationships and efforts undertaken to achieve a favourable pharmacokinetic profile in rat are described.

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Reference:
Tetrahydrofuran – Wikipedia,
Tetrahydrofuran | (CH2)3CH2O – PubChem

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The present teachings provide compounds of Formula (I): and pharmaceutically acceptable salts, hydrates, and esters thereof, wherein Ar, R1, R2, R3, p, and X are defined herein. The present teachings also provide processes for producing said compounds and their pharmaceutically acceptable salts, hydrates and esters, and methods of treating a pathological condition or disorder, or alleviating a symptom thereof, using said compounds including their pharmaceutically acceptable salts, hydrates and esters. The compounds can be useful in modulating ion channel activity including treating a variety of conditions associated with the abnormal modulation of one or more voltage-gated calcium channels.

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Tetrahydrofuran – Wikipedia,
Tetrahydrofuran | (CH2)3CH2O – PubChem

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Electrochemical fluorination (ECF) of the ester derivatives of oxolane-2-yl-carboxylic acid (1), oxolane-2-yl-methanol (2) and oxane-2-yl-methanol (3) were investigated. Perfluoro(oxolane-2-yl- carbonylfluoride) (4) was obtained from derivatives of 1 and 2, and perfluoro(oxane-2-yl-carbonylfluoride) (5) was obtained from derivatives of 3 as the desired compounds, respectively. From the ECF of acetates of 2 and 3, perfluorospiroethers having a dioxolane ring were also obtained as the cyclization product in low yield together with the desired perfluoroacid fluoride (4 and 5). The structure of these perfluorospiroethers was confirmed by analyzing the chlorinated products, which were obtained by the reaction with AlCl3.

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Reference:
Tetrahydrofuran – Wikipedia,
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Method of Flavoring

A method of providing a desirable vanilla beany flavor in an orally-receivable product, includes adding to a product base at least one of divanillyl succinate or at least one compound according to Formula I or Formula II in which R? is selected from the group consisting of hydrogen, methyl and ?CHO, and R is selected from the group consisting of hydrogen. C1-C10 linear alkyl. C3-C10 branched alkyl, C2-C10 linear alkenyl, C3-C10 branched alkenyl, C1-C10 hydroxyalkyl, C2-C10 carboxyalkyl, and tetrahydrofuranyl.

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Tetrahydrofuran – Wikipedia,
Tetrahydrofuran | (CH2)3CH2O – PubChem

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QUINOLINE COMPOUND

A compound, which has a melanin-concentrating hormone antagonistic action and useful as an agent for preventing or treating obesity, and which is represented by the formula: wherein Aris a cyclic group optionally having substituent(s) ;Xis a bond or a spacer having a main chain of 1 to 6 atoms;R1 and R2are the same or different and each is a hydrogen atom or a hydrocarbon group optionally having substituent(s), or R1 and R2 may form, together with the adjacent nitrogen atom, a nitrogen-containing heterocycle optionally having substituent(s);Yis a divalent hydrocarbon group optionally having substituent(s) (except CO);R3is a hydrogen atom or a hydrocarbon group optionally having substituent(s); andring A and ring Bmay further have substituents, and when ring B further has a substituent, the substituent may be linked to R1 to form a ring, or a salt thereof, or a prodrug thereof, is provided.

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Tetrahydrofuran – Wikipedia,
Tetrahydrofuran | (CH2)3CH2O – PubChem

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HETEROCYCLIC COMPOUND

Provided is a compound useful for the prophylaxis or treatment of cancer. The present invention relates to a compound represented by formula (I): wherein each symbol in the formula is as defined in the specification, or a salt thereof or a prodrug thereof, which is useful for the prophylaxis or treatment of cancer.

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Tetrahydrofuran – Wikipedia,
Tetrahydrofuran | (CH2)3CH2O – PubChem

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Structure-based design, synthesis, and biological evaluation of irreversible human rhinovirus 3C protease inhibitors. 6. Structure-activity studies of orally bioavailable, 2-pyridone-containing peptidomimetics

The structure-based design, chemical synthesis, and biological evaluation of various 2-pyridone-containing human rhinovirus (HRV) 3C protease (3CP) inhibitors are described. These compounds are comprised of a peptidomimetic binding determinant and a Michael acceptor moiety, which forms an irreversible covalent adduct with the active site cysteine residue of the 3C enzyme. The 2-pyridone-containing inhibitors typically display improved 3CP inhibition properties relative to related peptide-derived molecules along with more favorable antiviral properties. The cocrystal structure of one pyridone-derived 3CP inhibitor complexed with HRV-2 3CP is also described along with certain ab initio conformation analyses. Optimization of the 2-pyridone-containing compounds is shown to provide several highly active 3CP inhibitors (kobs/[I] > 500 000 M-1 s-1) that function as potent antirhinoviral agents (EC50 = <0.05 muM) against multiple virus serotypes in cell culture. One 2-pyridone-containing 3CP inhibitor is shown to be bioavailable in the dog after oral dosing (F = 48%). Sometimes chemists are able to propose two or more mechanisms that are consistent with the available data. HPLC of Formula: C5H7ClO2, If a proposed mechanism predicts the wrong experimental rate law, however, the mechanism must be incorrect.Welcome to check out more blogs about 52449-98-6, in my other articles.

Reference:
Tetrahydrofuran – Wikipedia,
Tetrahydrofuran | (CH2)3CH2O – PubChem