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Benzimidazolone carboxylic acid derivatives

This invention relates to compounds of the formula (I): [image] wherein R1, R2, R3, A and m are each as described herein or a pharmaceutically acceptable salt or solvate thereof, and compositions containing such compounds and the use of such compounds in the treatment of a condition mediated by 5-HT4 receptor activity such as, but not limited to, gastroesophageal reflux disease, gastrointestinal disease, gastric motility disorder, non-ulcer dyspepsia, functional dyspepsia, irritable bowel syndrome (IBS), constipation, dyspepsia, esophagitis, gastroesophageral disease, nausea, central nervous system disease, Alzheimer”s disease, cognitive disorder, emesis, migraine, neurological disease, pain, cardiovascular disorders such as cardiac failure and heart arrhythmia, diabetes and apnea syndrome.

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

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INHIBITORS OF CYSTATHIONINE BETA SYNTHASE TO REDUCE THE NEUROTOXIC OVERPRODUCTION OF ENDOGENOUS HYDROGEN SULFIDE

The invention is directed to inhibitors of cystathionine beta synthase which, among other biochemical effects, allow reduction of the neurotoxic overproduction of endogenous hydrogen sulphide. These compounds and pharmaceutical compositions containing them are useful for the prevention and treatment of cognitive disorders such as cognitive disorders in Down syndrome. The invention also relates to methods for preventing or treating cognitive disorders including cognitive disorders in Down Syndrome

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

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SUBSTITUTED CYCLIC CARBOXAMIDE AND UREA DERIVATIVES AS LIGANDS OF THE VANILLOID RECEPTOR

Substituted cyclic carboxamide and urea compounds, a process for their preparation, pharmaceutical compositions containing these compounds, and the use of these compounds for the treatment and/or inhibition of pain and other conditions mediated by the vanilloid receptor 1

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

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Identification of SD-0006, a potent diaryl pyrazole inhibitor of p38 MAP kinase

Starting from an initial HTS screening lead, a novel series of C(5)-substituted diaryl pyrazoles were developed that showed potent inhibition of p38alpha kinase. Key to this outcome was the switch from a pyridyl to pyrimidine at the C(4)-position leading to analogs that were potent in human whole blood based cell assay as well as in a number of animal efficacy models for rheumatoid arthritis. Ultimately, we identified a clinical candidate from this substrate; SD-0006.

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

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[…] HETEROCYCLIC COMPOUND, PREPARATION METHOD THEREOF AND ITS APPLICATION ON THE PHARMACOLOGY (by machine translation)

THE PRESENT INVENTION RELATES TO INHIBITORS OF FGFR […] HETEROCYCLIC COMPOUND, PREPARATION METHOD THEREOF AND ITS APPLICATION ON THE PHARMACOLOGY. SPECIFICALLY, THE INVENTION RELATES TO A COMPOUND OF GENERAL FORMULA (I) COMPOUND OF FORMULA AND ITS PHARMACEUTICALLY ACCEPTABLE SALT, CONTAINING THE COMPOUND OR ITS PHARMACEUTICALLY ACCEPTABLE SALT OF THE PHARMACEUTICAL COMPOSITION, THE USE OF THE COMPOUND OR ITS PHARMACEUTICALLY ACCEPTABLE SALTS FOR TREATING AND/OR PREVENTING FGFR-RELATED CONDITIONS, ESPECIALLY A TUMOR OF THE METHOD AND THE COMPOUND OR ITS PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF. THE INVENTION ALSO RELATES TO THE COMPOUND OR ITS PHARMACEUTICALLY ACCEPTABLE SALT OR CONTAINING THE COMPOUND OR ITS PHARMACEUTICALLY ACCEPTABLE SALT IN THE PREPARATION OF A PHARMACEUTICAL COMPOSITION FOR THE TREATMENT AND/OR PREVENTION OF FGFR-RELATED CONDITIONS, IN PARTICULAR THE USE OF THE DRUG IN THE TUMOR. WHEREIN THE GENERAL FORMULA (I) OF EACH SUBSTITUENT IS AS DEFINED IN THE SPECIFICATION. (by machine translation)

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

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CERTAIN TRIAZOLOPYRIDINES AND TRIAZOLOPYRAZINES, COMPOSITIONS THEREOF AND METHODS OF USE THEREFOR

Provided are certain triazolopyridines and triazolopyrazines, compositions thereof and methods of use therefor.

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

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METHODS FOR EVALUATING TUMOR CELL SPHEROIDS USING 3D MICROFLUIDIC CELL CULTURE DEVICE

Provided herein are methods for evaluating tumor cell spheroids in a three-dimensional microfluidic device by determining changes in the relative levels of live cells and dead cells in aliquots cultured under different conditions. Methods described herein allow ex vivo recapitulation of the tumor microenvironment such that the in vivo effectiveness of a test compound in treating tumor tissue may be predicted.

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

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85064-61-5, Name is Tetrahydropyranyl-4-acetic acid, molecular formula is C7H12O3, belongs to Tetrahydropyrans compound, is a common compound. In a patnet, once mentioned the new application about 85064-61-5, category: Tetrahydropyrans

MODULATORS OF HEDGEHOG (HH) SIGNALLING PATHWAY

There are described compounds of formula (I): and there use as a medicament in the treatment of conditions involving abnormal activation and/or malfunction of the of the hedgehog pathway, such as cancer, fibrosis and chronic graft-versus-host disease (cGVHD).

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

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KAPPA OPIOID RECEPTOR ANTAGONISTS AND PRODUCTS AND METHODS RELATED THERETO

Compounds are provided that antagonize the kappa-opioid receptor (KOR) and products containing such compounds, as well as to methods of their use and synthesis. Such compounds have the structure of Formula (I), or a pharmaceutically acceptable isomer, racemate, hydrate, solvate, isotope or salt thereof: (I) wherein X, Y, R1, R2, R4, R5 R6, R7, R8 and R11 are as defined herein.

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

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Synthesis and Bioevaluation of Alicyclic and Heterocyclic Alkanoates as Cockroach Attractants

A series of homo and heterocyclic alkanoates were prepared and evaluated as insect attractants toward Blattella germanica (L.) and Supella longipalpa (F.).Among these compounds, the tetrahydrofurfuryl alkanoates and 4-tetrahydropyranyl hexanoate showed relatively better activity.It was also observed that, in general, the five-membered compounds were better performers than their six-membered counterparts.The introdiction of an oxygen atom in the ring enhanced the activity, irrespective of the ring size.

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