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BROMODOMAIN INHIBITORS AND USES THEREOF

The present invention relates to compounds useful as inhibitors of bromodomain-containing proteins. The invention also provides pharmaceutically acceptable compositions comprising compounds of the present invention and methods of using said compositions in the treatment of various disorders.

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Reference£º
Piperidine – Wikipedia,
Piperidine | C5H22129N – PubChem

 

Properties and Exciting Facts About 1-tert-Butyl 3-ethyl 4-aminopiperidine-1,3-dicarboxylate

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Discovery of a Selective and CNS Penetrant Negative Allosteric Modulator of Metabotropic Glutamate Receptor Subtype 3 with Antidepressant and Anxiolytic Activity in Rodents

Previous preclinical work has demonstrated the therapeutic potential of antagonists of the group II metabotropic glutamate receptors (mGlus). Still, compounds that are selective for the individual group II mGlus (mGlu2 and mGlu3) have been scarce. There remains a need for such compounds with the balance of properties suitable for convenient use in a wide array of rodent behavioral studies. We describe here the discovery of a selective mGlu3 NAM 106 (VU0650786) suitable for in vivo work. Compound 106 is a member of a series of 5-aryl-6,7-dihydropyrazolo[1,5-a]pyrazine-4(5H)-one compounds originally identified as a mGlu5 positive allosteric modulator (PAM) chemotype. Its suitability for use in rodent behavioral models has been established by extensive in vivo PK studies, and the behavioral experiments presented here with compound 106 represent the first examples in which an mGlu3 NAM has demonstrated efficacy in models where prior efficacy had previously been noted with nonselective group II antagonists.

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Piperidine – Wikipedia,
Piperidine | C5H22157N – PubChem

 

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LACTAM COMPOUNDS AND THEIR USE AS PHARMACEUTICALS

The present invention relates to inhibitors of 11-F hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-F hydroxyl steroid dehydrogenase type 1and/or diseases associated with aldosterone excess.

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Piperidine – Wikipedia,
Piperidine | C5H22128N – PubChem

 

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FUNGICIDAL COMPOSITIONS

The instant invention describes tetrazole compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.

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Piperidine – Wikipedia,
Piperidine | C5H22147N – PubChem

 

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Selective synthesis of pyridyl pyridones and oxydipyridines by transition-metal-free hydroxylation and arylation of 2-fluoropyridine derivatives

An efficient protocol for the construction of various pyridyl pyridone and oxydipyridine derivatives through a hydroxylation and arylation tandem reaction of 2-fluoropyridines is reported. Under simple transition-metal-free conditions, the reaction provided a series of products in good to excellent yields, and their structures were confirmed by crystal diffraction analysis. Furthermore, the controlling effect of 6-position substituents on the highly selective synthesis of pyridone and oxydipyridine was studied.

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Piperidine – Wikipedia,
Piperidine | C5H22182N – PubChem

 

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NOVEL PYRIDINE DERIVATIVES

The invention relates to a compound of formula (I) wherein A1, A2 and R1 to R6 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.

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Reference£º
Piperidine – Wikipedia,
Piperidine | C5H22143N – PubChem