C07D211/00

N-ACYLPIPERIDINE ETHER TROPOMYOSIN-RELATED KINASE INHIBITORS

The present invention relates to compounds of Formula (I) described herein and their pharmaceutically acceptable salts, and their use in medicine, in particular as Trk antagonists.

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ELECTROLYTE SOLUTION AND ELECTROCHEMICAL DEVICE
20170309412 · 2017-10-26 · ·

The present invention aims to provide an electrolyte solution containing a quaternary ammonium salt as an electrolyte salt and is capable of providing an electrochemical device having a high capacitance retention and reducing generation of gas. The electrolyte solution of the present invention contains a solvent, a quaternary ammonium salt, and a nitrogen-containing unsaturated cyclic compound. The unsaturated cyclic compound is a nitrogen-containing unsaturated heterocyclic compound. The unsaturated cyclic compound excludes salts of the unsaturated cyclic compound and ionic liquids obtainable from the unsaturated cyclic compound.

Piperidine derivatives as HDAC1/2 inhibitors

Provided herein are compounds, pharmaceutical compositions comprising such compounds, and methods of using such compounds to treat diseases or disorders associated with HDAC1 and/or HDAC2 activity.

Novel Methyl-Piperidine Compounds Useful for Inhibiting Microsomal Prostaglandin E2 Synthase-1

The present invention provides compounds of Formula (1), or a pharmaceutically acceptable salt thereof, formula (1), where R, R1, and G are as described herein; methods of preparing the compounds; and use of the compounds to treat pain and/or inflammation associated with arthritis or osteoarthritis.

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3-ester-4 substituted orexin receptor antagonists

The present invention is directed to 3-ester-4-substituted compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the 3-ester-4-substituted compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved.

Process for the transition metal catalyzed cyanation of aryl/vinyl halides
11161805 · 2021-11-02 · ·

The present invention refers to a process for a transition metal, particularly nickel-catalyzed cyanation reaction of aryl/vinyl halide using organic nitrile compounds. This new reaction provides a strategically distinct approach to the safe preparation of aryl/vinyl cyanides, which are essential compounds in agrochemistry and medicinal chemistry.

PEPTIDOMIMETIC INHIBITORS OF THE PEPTIDYL-PROLYL CIS/TRANS ISOMERASE (PIN1)

Disclosed are compounds which inhibit Pin1 activity, methods of making the compounds, pharmaceutical compositions containing the compounds, and methods of using the compounds to treat diseases or disorders characterized or mediated by dysregulated Pin1 activity.

FLUORESCENT PROBES FOR QUANTIFICATION OF DNA DAMAGE AND REPAIR
20210147932 · 2021-05-20 ·

Probes, methods and kits for detecting and measuring abasic (AP) sites in a nucleic acid are provided. Aspects of the methods include determining glycosylase enzyme activity. Further provided herein are methods of quantifying AP sites in genomic DNA, and quantifying the amount of DNA damage. The subject probes include a fluorophore linked to an alpha nucleophile that reacts with the AP site of the nucleic acid to produce a highly fluorescent conjugate.

FLUORESCENT PROBES FOR QUANTIFICATION OF DNA DAMAGE AND REPAIR
20210147932 · 2021-05-20 ·

Probes, methods and kits for detecting and measuring abasic (AP) sites in a nucleic acid are provided. Aspects of the methods include determining glycosylase enzyme activity. Further provided herein are methods of quantifying AP sites in genomic DNA, and quantifying the amount of DNA damage. The subject probes include a fluorophore linked to an alpha nucleophile that reacts with the AP site of the nucleic acid to produce a highly fluorescent conjugate.

Charged ion channel blockers and methods for use

The invention provides compounds of Formula (I), or pharmaceutically acceptable salts thereof: ##STR00001##
The compounds, compositions, methods and kits of the invention are useful for the treatment of pain, itch, and neurogenic inflammation.