C07D209/28

Curcumin Conjugates and Methods of Use Thereof
20180110861 · 2018-04-26 ·

Curcumin-based conjugates and methods of use thereof are provided. Pharmaceutical compositions including an effective amount of one or more curcumin conjugates are also provided. In particular embodiments, the compositions are formulated for oral delivery. The conjugates and pharmaceutical compositions thereof can be administered to a subject in need thereof to treat a host of diseases and disorders including but not limited to, cancer, inflammation, and microbial growth.

UNIQUE DUAL-ACTION THERAPEUTICS

A new family of therapeutics which provides a controlled-release delivery platform for non-steroidal anti-inflammatory agents on an ester or an ester-carbonate backbone is disclosed herein. These agents are reversible inhibitors of acetylcholinesterase and are thus useful for clinical conditions benefiting from inflammation suppression and cholinergic intervention. These compounds are of the general formula wherein n=0, 1; XC, Si, and N+ and NSAID=ibuprofen, naproxen, indomethacin and diclofenac. Other embodiments are also disclosed.

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UNIQUE DUAL-ACTION THERAPEUTICS

A new family of therapeutics which provides a controlled-release delivery platform for non-steroidal anti-inflammatory agents on an ester or an ester-carbonate backbone is disclosed herein. These agents are reversible inhibitors of acetylcholinesterase and are thus useful for clinical conditions benefiting from inflammation suppression and cholinergic intervention. These compounds are of the general formula wherein n=0, 1; XC, Si, and N+ and NSAID=ibuprofen, naproxen, indomethacin and diclofenac. Other embodiments are also disclosed.

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Liver targeted conjugates

Therapeutic conjugates containing a statin or a modified statin (collectively statin) linked to a therapeutic agent (also referred to as a drug herein) are targeted to the liver by the statin or modified statin and thereby deliver the therapeutic agent to liver cells.

Liver targeted conjugates

Therapeutic conjugates containing a statin or a modified statin (collectively statin) linked to a therapeutic agent (also referred to as a drug herein) are targeted to the liver by the statin or modified statin and thereby deliver the therapeutic agent to liver cells.

Stable heavy isotopes in amide functional groups and uses thereof

There are provided isotope-enriched compounds containing stable heavy isotope-enriched amide functional groups for modulating the pharmacokinetic profile, metabolic profile, and/or delivery efficiency of a drug or prodrug, as well as its therapeutic or prophylactic efficacy and/or adverse effects. Use of the isotope-enriched amide-containing drugs and prodrugs for the treatment or prevention of disease states and conditions is also provided. ##STR00001##

PROCESS FOR THE PREPARATION OF INDOMETHACIN

An improved process for the preparation of Indomethacin of formula (I):

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is provided by means of the precipitation, crystallization, re-crystallization or re-slurry of the intermediate 4-chloro-N-(4-methoxyphenyl)benzohydrazide in a mixture containing tetrahydrofuran and a C.sub.1-C.sub.4 linear or branched alkyl alcohol.

PROCESS FOR THE PREPARATION OF INDOMETHACIN

An improved process for the preparation of Indomethacin of formula (I):

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is provided by means of the precipitation, crystallization, re-crystallization or re-slurry of the intermediate 4-chloro-N-(4-methoxyphenyl)benzohydrazide in a mixture containing tetrahydrofuran and a C.sub.1-C.sub.4 linear or branched alkyl alcohol.

2,3-DIMETHOXY-5-METHYL-1,4-BENZOQUINONE ALKYL ALCOHOL DERIVATIVE AND USE THEREOF

Disclosed is a 2,3-dimethoxy-5-methyl-1,4-benzoquinone alkyl alcohol derivative, a pharmaceutical composition containing the compound, and the use of the compound in the prevention and treatment of tumors.

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