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The present invention relates to O-GlcNAc hydrolase (OGA) inhibitors. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which inhibition of OGA is beneficial, such as tauopathies, in particular Alzheimer’s disease or progressive supranuclear palsy; and neurodegenerative diseases accompanied by a tau pathology, in particular amyotrophic lateral sclerosis or frontotemporal lobe dementia caused by C9ORF72 mutations.

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Piperidine – Wikipedia,
Piperidine | C5H16551N – PubChem

 

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The invention relates to compounds of formula (I) wherein Z, R1-3 and A have the meaning as cited in the description and the claims. Said compounds are useful as DPP-IV inhibitors. The invention also relates to the preparation of such compounds as well as the production and use thereof as medicament.

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Compounds having formula (I) (IX), and enantiomers, and diastereomers, stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, are useful as kinase modulators, including RIPK1 modulation. All the variables are as defined herein: (I), (II), (III), (IV), (V), (VI), (VII), (VIII), (IX).

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The present invention relates to new compounds of formula (I) wherein Y1 and Y2 selected from the group consisting of hydrogen, halogen atom, C1-4 alkyl, C1-4 alkoxy or cyano group, X is oxygen or two hydrogen atoms; Z is-(CH2)n-group or S; n is 1 or 2; R is selected from the group consisting of optionally substituted C1-7 alkyl, C1-4 haloalkyl, C1-4 hydroxyalkyl, C1-3OC1-3 alkyl, C1-4 cyanoalkyl, C0-2(NR1R2)alkyl, C1-4-alkylCOOC1-4-alkyl, C1-4-alkylOCOC1-4-alkyl, C1-4-alkylNHCOC1-4-alkyl, C2-7 alkenyl, C2-7 alkynyl, CH2O-(CH2)1-3-OCH3; an optionally substituted C3-7 cycloalkyl; phenyl; C3-7 saturated or unsaturated heterocyclyl or heteroaryl group containing 1-4 heteroatom; R1 and R2 are independently selected from hydrogen, C1-7 alkyl or C1-6 alkanoyl group-and/or enantiomers and/or racemates and/or diastereomers and/or geometric isomers and/or pharmaceutically acceptable salts thereof formed with acids and bases, to the process for producing said compounds, to pharmaceutical compositions containing said compounds and to their use in the prevention and/or treatment of mGluR5 receptor-mediated disorders.

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Piperidine – Wikipedia,
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A series of 5,6-dihydro-1-benzothiophen-7(4H)-one derivatives, and analogues thereof, which are substituted in the 2-position by an optionally substituted morpholin-4-yl moiety, being selective inhibitors of PI3 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions.

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The disclosure relates to compounds of formula I which are useful as kinase modulators including RIPK1 modulation. The disclosure also provides methods of making and using the compounds for example in treatments related to necrosis or inflammation as well as other indications.

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The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.

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Catalysts function by providing an alternate reaction mechanism that has a lower activation energy than would be found in the absence of the catalyst. In some cases, the catalyzed mechanism may include additional steps.In a article, 118156-93-7, molcular formula is C11H19NO3, introducing its new discovery. Formula: C11H19NO3

The resurgence of interest in monoamine oxidases (MAOs) has been fueled by recent correlations of this enzymatic activity with cardiovascular, neurological, and oncological disorders. This has promoted increased research into selective MAO-A and MAO-B inhibitors. Here, we shed light on how selective inhibition of MAO-A and MAO-B can be achieved by geometric isomers of cis-and trans-1-propargyl-4-styrylpiperidines. While the cis isomers are potent human MAO-A inhibitors, the trans analogues selectively target only the MAO-B isoform. The inhibition was studied by kinetic analysis, UV-vis spectrum measurements, and X-ray crystallography. The selective inhibition of the MAO-A and MAO-B isoforms was confirmed ex vivo in mouse brain homogenates, and additional in vivo studies in mice show the therapeutic potential of 1-propargyl-4-styrylpiperidines for central nervous system disorders. This study represents a unique case of stereoselective activity of cis/trans isomers that can discriminate between structurally related enzyme isoforms.

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A compound of formula (I) or a salt thereof; which is an inhibitor of spleen tyrosine kinase (Syk) and therefore potentially of use in treating diseases resulting from inappropriate activation of mast cells, macrophages, and B-cells and related inflammatory responses and tissue damage, for instance inflammatory disease and/or allergic disorders, and in cancer therapy, specifically heme malignancies, and autoimmune conditions.

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The present invention relates to new compounds of formula (I) wherein A, B, P, Q, W, Rl and R2 are defined in the description; invention compounds are useful in the prevention or treatment of central nervous system disorders as well as other disorders modulated by mGluR5 receptors.

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Piperidine – Wikipedia,
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