Category: 85064-61-5

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A new metallo-beta-lactamase inhibitor which acts as a medicament for inhibiting the inactivation of beta-lactam antibiotics and recovering anti-bacterial activities is disclosed. The maleic acid derivatives having the general formula (I) have metallo-beta-lactamase inhibiting activities. It is possible to recover the anti-bacterial activities of beta-lactam antibiotics against metallo-beta-lactamase producing bacteria by combining the compound of the general formula (I) with beta-lactam antibiotics.

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Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics

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Use of compounds of the general formula (I) and pharmaceutically acceptable salt thereof, in which R, R1 and X have the definitions illustrated in detail in the description, as beta-secretase, cathepsin D, plasmepsin Il and/or HIV protease inhibitors.

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Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics

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Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, triterpenoids that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formula I: with X selected from C4-8 cycloalkyl, C4-8 cycloalkenyl, C4-9 spirocycloalkyl, C4-9 spirocycloalkenyl, C4-8 oxacycloalkyl, C4-8 dioxacycloalkyl, C6-8 oxacycloalkenyl, C6-8 dioxacycloalkenyl, C6 cyclodialkenyl, C6 oxacyclodialkenyl, C6-9 oxaspirocycloalkyl and C6-9 oxaspirocycloalkenyl ring, such that X is substituted with A, wherein A is -C1-6 alkyl- halo. These compounds are useful for the treatment of HIV and AIDS.

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Reference：
Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics

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A mild, practical protocol for the decarboxylative alkylation of heteroarenes has been accomplished via iron photocatalysis. A diverse range of carboxylic acids readily undergo oxidative decarboxylation and then couple with a broad array of heteroarenes in this transformation. The photoexcited state lifetimes of iron complexes are typically much shorter than those of iridium and ruthenium complexes. Here we describe our effort on iron photocatalysis by utilizing the intramolecular charge transfer pathway of iron-carboxylate complexes.

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Tetrahydropyran – Wikipedia,
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ATAD2 is a cancer-associated protein whose bromodomain has been described as among the least druggable of its class. In our recent disclosure of the first chemical probe against this bromodomain, GSK8814 (6), we described the use of a conformationally constrained methoxy piperidine to gain selectivity over the BET bromodomains. Here we describe an orthogonal conformational restriction strategy of the piperidine ring to give potent and selective tropane inhibitors and show structural insights into why this was more challenging than expected. Greater understanding of why different rational approaches succeeded or failed should help in the future design of selectivity in the bromodomain family.

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Tetrahydropyran – Wikipedia,
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Phosphatidylinositol-3-kinase (PI3K)delta inhibition is one of the most attractive approaches to the treatment of autoimmune diseases and leukocyte malignancies. Through the exploration of pyrazolopyridine derivatives as potential PI3Kdelta inhibitors, compound 12a was identified as a potent PI3Kdelta inhibitor but suffered from poor oral exposure in mice. With a modified amide linkage group, compound 15a was developed as an orally available PI3Kdelta inhibitor with reduced selectivity against other PI3Ks. To improve the trade-off between selectivity and PK profile, structure?activity relationship (SAR) studies of terminal substituents on the pyrolidine ring were conducted. As a result, we developed potent PI3Kdelta inhibitors with good oral availability. In particular, the representative compound 15j showed excellent selectivity for PI3Kdelta over other PI3Ks with good oral exposure in mice.

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Tetrahydropyran – Wikipedia,
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The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.85064-61-5, Name is Tetrahydropyranyl-4-acetic acid, molecular formula is C7H12O3. In a Patent£¬once mentioned of 85064-61-5, Formula: C7H12O3

The application relates to 2,5-disubstituted piperidines, their preparation and use as medicines, especially as renin inhibitors, of the general formula (I) in which R, R1 and X are each as defined in detail in the description, and pharmaceutical preparations comprising these compounds.

The reactant in an enzyme-catalyzed reaction is called a substrate. Enzyme inhibitors cause a decrease in the reaction rate of an enzyme-catalyzed reaction.I hope my blog about 85064-61-5 is helpful to your research., Formula: C7H12O3

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Tetrahydropyran – Wikipedia,
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Mitigating hERG inhibition: Design of orally bioavailable CCR5 antagonists as potent inhibitors of R5 HIV-1 replication

A series of CCR5 antagonists representing the thiophene-3-yl-methyl ureas were designed that met the pharmacological criteria for HIV-1 inhibition and mitigated a human ether-a-go-go related gene (hERG) inhibition liability. Reducing lipophilicity was the main design criteria used to identify compounds that did not inhibit the hERG channel, but subtle structural modifications were also important. Interestingly, within this series, compounds with low hERG inhibition prolonged the action potential duration (APD) in dog Purkinje fibers, suggesting a mixed effect on cardiac ion channels.

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Reference：
Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics

The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.85064-61-5, Name is Tetrahydropyranyl-4-acetic acid, molecular formula is C7H12O3. In a Patent，once mentioned of 85064-61-5, SDS of cas: 85064-61-5

ARYL ANNULATED MACROCYCLIC INDOLE DERIVATIVES

The present invention relates to aryl annulated macrocyclic indole derivatives of general formula (I): in which R1, R2, R3, R4, R5, R6, A and L are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds, and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of hyperproliferative disorders, as a sole agent or in combination with other active ingredients.

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Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics

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The retinoic acid receptor-related orphan receptor-gamma-t (RORgammat) is a promising therapeutic target for treatment of Th17 cell-mediated autoimmune diseases. Based on a scaffold hopping/conformational restriction strategy, a series of N-indanyl benzamides as novel RORgammat inverse agonists was discovered. Exploration of structure-activity relationship on the piperazine ring, benzoyl moiety and cyclopentyl moiety of N-indanyl benzamides 2a and 2d led to identification of potent RORgammat inverse agonists. Compound 5c with (S)-enantiomer was found having an IC50 of 153.7 nM in Fluorescence Resonance Energy Transfer (FRET) assay, and an IC50 of 47.1 nM in mouse Th17 cell differentiation assay, which represents a promising starting point for developing potent small molecule RORgammat inverse agonists. Binding modes of the two enantiomers 5c and 5d in RORgammat ligand binding domain were also discussed.

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Reference£º
Tetrahydropyran – Wikipedia,
Tetrahydropyran – an overview | ScienceDirect Topics