C07C215/68

BETA-SUBSTITUTED BETA-AMINO ACIDS AND ANALOGS AS CHEMOTHERAPEUTIC AGENTS AND USES THEREOF

-Substituted -amino acids, -substituted -amino acid derivatives, and -substituted -amino acid analogs and (bio)isosteres and their use as chemotherapeutic agents are disclosed. The -substituted -amino acid derivatives and -substituted -amino acid analogs and (bio)isosteres are selective LAT1/4F2hc substrates and exhibit rapid uptake and retention in tumors expressing the LAT1/4F2hc transporter. Methods of synthesizing the -substituted -amino acid derivatives and -substituted -amino acid analogs and methods of using the compounds for treating cancer are also disclosed. The -substituted -amino acid derivatives and -substituted -amino acid analogs exhibit selective uptake in tumor cells expressing the LAT1/4F2hc transporter and accumulate in cancerous cells when administered to a subject in vivo. The -substituted -amino acid derivatives and -substituted -amino acid analogs and (bio)isosteres exhibit cytotoxicity toward several tumor types.

BETA-SUBSTITUTED BETA-AMINO ACIDS AND ANALOGS AS CHEMOTHERAPEUTIC AGENTS AND USES THEREOF

-Substituted -amino acids, -substituted -amino acid derivatives, and -substituted -amino acid analogs and (bio)isosteres and their use as chemotherapeutic agents are disclosed. The -substituted -amino acid derivatives and -substituted -amino acid analogs and (bio)isosteres are selective LAT1/4F2hc substrates and exhibit rapid uptake and retention in tumors expressing the LAT1/4F2hc transporter. Methods of synthesizing the -substituted -amino acid derivatives and -substituted -amino acid analogs and methods of using the compounds for treating cancer are also disclosed. The -substituted -amino acid derivatives and -substituted -amino acid analogs exhibit selective uptake in tumor cells expressing the LAT1/4F2hc transporter and accumulate in cancerous cells when administered to a subject in vivo. The -substituted -amino acid derivatives and -substituted -amino acid analogs and (bio)isosteres exhibit cytotoxicity toward several tumor types.

COMPOUNDS FOR THE TREATMENT OF HYPERGLYCAEMIA
20190119196 · 2019-04-25 ·

There is herein provided a compound of formula (I) or a pharmaceutically acceptable salt thereof, for use in the treatment of hyperglycaemia or a disorder characterized by hyperglycaemia, such as type 2 diabetes, wherein X, R.sup.1, R.sup.2, R.sup.3 and n have meanings as provided in the description.

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COMPOUNDS FOR THE TREATMENT OF HYPERGLYCAEMIA
20190119196 · 2019-04-25 ·

There is herein provided a compound of formula (I) or a pharmaceutically acceptable salt thereof, for use in the treatment of hyperglycaemia or a disorder characterized by hyperglycaemia, such as type 2 diabetes, wherein X, R.sup.1, R.sup.2, R.sup.3 and n have meanings as provided in the description.

##STR00001##

A PROCESS FOR PREPARING BETA AGONIST
20190055189 · 2019-02-21 ·

Disclosed is a process for preparing -agonist, 1-(4-amino-3,5-dichlorophenyl)-2-(tert-butylamino) ethanol, of Formula I. The process comprises refluxing 1-(4-amino-3,5-dichlorophenyl) ethanone of Formula II and selenium dioxide in the presence of 1,4-dioxane to form compound of Formula III. Further, compound of Formula III is heated at a temperature below 30 C. in the presence of t-butyl amine to form compound of Formula IV. The compound of Formula IV is treated with sodium borohydride to form compound of Formula I.

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A PROCESS FOR PREPARING BETA AGONIST
20190055189 · 2019-02-21 ·

Disclosed is a process for preparing -agonist, 1-(4-amino-3,5-dichlorophenyl)-2-(tert-butylamino) ethanol, of Formula I. The process comprises refluxing 1-(4-amino-3,5-dichlorophenyl) ethanone of Formula II and selenium dioxide in the presence of 1,4-dioxane to form compound of Formula III. Further, compound of Formula III is heated at a temperature below 30 C. in the presence of t-butyl amine to form compound of Formula IV. The compound of Formula IV is treated with sodium borohydride to form compound of Formula I.

##STR00001##

Compositions and methods of treating retinal disease

Compositions and methods for treating macular degeneration and other forms of retinal disease whose etiology involves the accumulation of A2E and/or lipofuscin, and, more specifically, for preventing the formation and/or accumulation of A2E are disclosed.

Compositions and methods of treating retinal disease

Compositions and methods for treating macular degeneration and other forms of retinal disease whose etiology involves the accumulation of A2E and/or lipofuscin, and, more specifically, for preventing the formation and/or accumulation of A2E are disclosed.

ULTRA BRIGHT DIMERIC OR POLYMERIC DYES
20190016898 · 2019-01-17 ·

Compounds useful as fluorescent or colored dyes are disclosed. The compounds have the following structure (I):

##STR00001##

or a stereoisomer, tautomer or salt thereof, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, L.sup.1, L.sup.2, L.sup.3, L.sup.4, M, m and n are as defined herein. Methods associated with preparation and use of such compounds are also provided.

ULTRA BRIGHT DIMERIC OR POLYMERIC DYES
20240287314 · 2024-08-29 ·

Compounds useful as fluorescent or colored dyes are disclosed. The compounds have the following structure (II):

##STR00001##

or a stereoisomer, tautomer or salt thereof, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, L.sup.1, L.sup.2, L.sup.3, L.sup.4, M, m and n are as defined herein. Methods associated with preparation and use of such compounds are also provided.