C07D417/02

SUBSTITUTED N-[2-(4-PHENOXYPIPERIDIN-1-YL)-2-(1,3-THIAZOL-5-YL)ETHYL]BENZAMIDE AND N-[2-(4-BENZYLOXYPIPERIDIN-1-YL)-2-(1,3-THIAZOL-5-YL)ETHYL]BENZAMIDE DERIVATIVES P2X7 RECEPTOR ANTAGONISTS
20190194180 · 2019-06-27 · ·

The present invention relates to novel substituted phenoxy- and benzyloxy-piperidine compounds of formula (I) having P2X7 receptor (P2X7) antagonistic properties, pharmaceutical compositions comprising these compounds, chemical processes for preparing these compounds and their use in the treatment or prophylaxis of diseases associated with P2X7 receptor activity in animals, in particular humans.

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NOL3 is a predictor of patient outcome

The present invention features a method for determining the prognosis for survival of a cancer patient. Methods for measuring the level of NOL3 expression in a cancer cell-containing sample from a patient, and comparing the level of NOL3 expression in the sample to a reference level of NOL3 expression are also included. A higher level of NOL3 relative to the reference level correlates with decreased survival of the patient, and an equivalent or lower level of NOL3 relative to the reference level correlates with increased survival of the patient.

NOL3 is a predictor of patient outcome

The present invention features a method for determining the prognosis for survival of a cancer patient. Methods for measuring the level of NOL3 expression in a cancer cell-containing sample from a patient, and comparing the level of NOL3 expression in the sample to a reference level of NOL3 expression are also included. A higher level of NOL3 relative to the reference level correlates with decreased survival of the patient, and an equivalent or lower level of NOL3 relative to the reference level correlates with increased survival of the patient.

2-ACETYL-6-(2-(2-(4-BROMOBENZYLIDENE)HYDRAZINYL)THIAZOLE-4-YL)-3,7,9-TRIHYDROXY-8,9B-DIMETHYLDIBENZO[B,D]FURAN-1(9BH)-ONE EXHIBITING AN INHIBITORY EFFECT ON HUMAN TYROSYL-DNA-PHOSPHODIESTERASE 1 ENZYME

The present invention relates to the field of molecular biology, biochemistry and biotechnology, namely, to compound 2-acetyl-6-(2-(2-(4-bromobenzylidene)hydrazinyl) thiazole-4-yl)-3,7,9-trihydroxy-8,9b-dimethyldibenzo[b,d]furan-1(9bh)-one, which is a hydrazine-thiazole derivative of usnic acid of formula I and which is able to inhibit the action of human tyrosyl-DNA-phosphodiesterase 1 enzyme. Technical result: increase in inhibitory action towards human tyrosyl-DNA-phosphodiesterase 1 enzyme (Tdp1) and increase in the number of inhibitors of this enzyme.

Orexin receptor antagonists

The disclosures herein relate to novel compounds of formula wherein W, X and Y.sub.1, Y.sub.2, Y.sub.3 and Y.sub.4 are defined herein, and their use in treating, preventing, ameliorating, controlling or reducing the risk of neurological or psychiatric disorders associated with orexin receptors. ##STR00001##

Orexin receptor antagonists

The disclosures herein relate to novel compounds of formula wherein W, X and Y.sub.1, Y.sub.2, Y.sub.3 and Y.sub.4 are defined herein, and their use in treating, preventing, ameliorating, controlling or reducing the risk of neurological or psychiatric disorders associated with orexin receptors. ##STR00001##

HETEROAROMATIC COMPOUNDS AS BTK INHIBITORS

The present invention encompasses compounds of the formula (I)

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wherein the groups A, Cy, X1 and Y are defined herein, which are suitable for the treatment of diseases related to BTK, process of making, pharmaceutical preparations which contain compounds and their methods of use.

HETEROAROMATIC COMPOUNDS AS BTK INHIBITORS

The present invention encompasses compounds of the formula (I)

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wherein the groups A, Cy, X1 and Y are defined herein, which are suitable for the treatment of diseases related to BTK, process of making, pharmaceutical preparations which contain compounds and their methods of use.

OREXIN RECEPTOR ANTAGONISTS

The disclosures herein relate to novel compounds of formula wherein W, X and Y.sub.1, Y.sub.2, Y.sub.3 and Y.sub.4 are defined herein, and their use in treating, preventing, ameliorating, controlling or reducing the risk of neurological or psychiatric disorders associated with orexin receptors.

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OREXIN RECEPTOR ANTAGONISTS

The disclosures herein relate to novel compounds of formula wherein W, X and Y.sub.1, Y.sub.2, Y.sub.3 and Y.sub.4 are defined herein, and their use in treating, preventing, ameliorating, controlling or reducing the risk of neurological or psychiatric disorders associated with orexin receptors.

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