Phenyl carbamate compound and a composition for preventing or treating a memory loss-related disease comprising the same

Inventors

Choi, Yong Moon

Assignees

Bio Pharm Solutions Co Ltd

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Publication Number

US-9566261-B2

Patent

Publication Date

2017-02-14

Expiration Date


Abstract

The present invention relates to a composition for preventing or treating a memory loss related disease comprising a phenyl carbamate compound and a method for preventing or treating various diseases related to loss of memory therewith. The present invention ensures the enhancement of neuroprotection, such that it is promising for preventing or treating memory loss-related diseases such as dementia and Alzheimer's disease.

Core Innovation

The patent describes phenyl carbamate derivatives represented by Formula 1, including compounds and pharmaceutically acceptable salts, for preventing or treating memory loss-related diseases. The disclosed therapeutic activity is characterized as neuroprotecting activity, and the problem addressed includes dementia and Alzheimer’s disease.

The structural scope is defined by substituent selections on R1 through R5, each independently hydrogen or halogen, together with R6/R7 options, A1 selection, and R8 selected from methyl, isopropyl or butyl. The disclosure also includes pharmaceutically acceptable salt and formulation options and allows stereochemical forms including racemate, enantiomer, and diastereomer.

Example carbamate compounds within the Formula 1 scaffold are enumerated, including halogen-substituted phenyl and N-substituted carbamate variants. The examples also include regioisomerically separated monocarbamate derivatives, with structural variation across phenyl ring substitution patterns, hydroxyalkyl sidechains, and stereochemical forms.

Claims Coverage

The independent claim covers a method of treating a memory loss-related disease by administering a therapeutically effective amount of a pharmaceutical composition containing a Formula 1 phenyl carbamate derivative or pharmaceutically acceptable salt, with claim-limited substituent selections. Across the provided claims, the key inventive features are the Formula 1 compound definition, the permitted substituent classes, the specified stereochemical and salt forms, the enumerated carbamate embodiments, and the narrowing of the treated condition to dementia and Alzheimer’s disease.

Formula 1 phenyl carbamate for memory loss treatment

Administering a therapeutically effective amount of a pharmaceutical composition comprising a compound represented by Formula 1 or a pharmaceutically acceptable salt thereof as an active ingredient, wherein R1, R2, R3, R4 and R5 are each independently selected from hydrogen and halogen; R6 and R7 are selected in H/allowed configurations; A1 is selected from hydrogen, C1-C5 alkyl, C3-C8 cycloalkyl, C6-C10 aryl C1-C3 alkyl and bridged C6-C8 bicycloalkane; and R8 is methyl, isopropyl or butyl.

Select allowable halogens for R1–R5

R1, R2, R3, R4 and R5 are each independently selected from hydrogen, chlorine, fluorine, or iodine.

Specified carbamate compound examples

The compound is selected from a specified group of carbamate compounds with substituted phenyl, hydroxyalkyl, and N-substituent variants, including dichloro-, fluoro-, and iodo-phenyl analogs.

Allowable stereochemical forms of the active compound

The compound is used in one of several stereochemical forms, including racemate, enantiomer, diastereomer, or mixtures thereof.

Pharmaceutically acceptable salt formation by specified acid or ion types

A pharmaceutically acceptable salt is produced by reacting the compound with one of several specified acid or ion types including inorganic acid, organic acid, amino acid, sulfonic acid, alkali metal, and ammonium ion.

Alzheimer’s disease within dementia

The treated dementia is Alzheimer’s disease.

The claims are grounded on administering a Formula 1 phenyl carbamate derivative or pharmaceutically acceptable salt with defined substituent classes, with dependent limitations specifying particular halogen substitution patterns, enumerated carbamate embodiments, allowable stereochemical forms, constrained pharmaceutically acceptable salt production, and narrowing to Alzheimer’s disease.

Stated Advantages

Neuroprotecting activity.

Documented Applications

Preventing or treating memory loss-related diseases.

Dementia.

Alzheimer’s disease.

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