A novel crystalline form of 2,3-dimethyl-1,4-benzoquinone-5-decyl-triphenylphosphonium bromide is provided. The crystalline form was found to have X-ray powder diffraction peaks at 19.25, 21.507, and 23.074 degrees 2 theta, ?0.2 degrees 2 theta. Also provided are industrially feasible methods for manufacture of the crystalline form with high purity.

The present application provides a compound that inhibits TRAP1 or a pharmaceutically acceptable salt thereof. In this case, the compound or the pharmaceutically acceptable salt thereof can inhibit the binding between TRAP1 and the client protein. In addition, the present application provides: a pharmaceutical composition for the treatment of cancer or ocular disease comprising a compound that inhibits TRAP1 or a pharmaceutically acceptable salt thereof; and use thereof.

The invention relates to the chemical synthesis of oligonucleotides, e.g., oligoribonucleotides. In another aspect, the invention relates to compounds of formula (II) processes for making these compounds, and the use thereof in the chemical synthesis of oligonucleotides, e.g., oligoribonucleotides. The invention also relates to methods of synthesis of oligomers, including but not limited to oligopeptides, oligosaccharides and oligonucleotides, particularly oligoribonucleotides and also oligodeoxyribonucleotides, in solution systems, and ionic tag linkers for use in methods provided herein.

The present invention provides a process for preparation of {(2E,4E,6E,8E)-9-(4-methoxy-2,3,6-trimethyl)phenyl-3,7-dimethyl-nona-2,4,6,8}tetraenoate, an acitretin intermediate of formula (VI) with trans isomer 97%, comprising of reacting 3-formyl-crotonic acid butyl ester of formula (V), substantially free of impurities, with 5-(4-methoxy-2,3,6-trimethylphenyl)-3-methyl-penta-2,4-diene-1-triphenyl phosphonium bromide of formula (IV) and isolating resultant compound of formula (VI), treating the filtrate with iodine for isomerization of the undesired cis intermediate and finally obtaining acitretin (I), with desired trans isomer 97%.

The subject of the invention are new mitochondrially targeted E/Z isomers of aliphatic triphenylphosphonium derivatives of tamoxifen where the aliphatic chain is alkyl or alkenyl, and their corresponding tertiary amine salts and/or their mixture (MitoTAX). Alkyl triphenylphosphonium derivatives of tamoxifen have the general formula (I), where n=8 to 12 and where Z is selected from the group of organic salts or inorganic salts. Alkenyl triphenylphosphonium derivatives of tamoxifen have the general formula IA, where n=6 to 10 and where Z has the above mentioned meaning. These compounds are applicable for the treatment of neoplastic disease, especially those with high HER2 protein levels. The drug for the treatment of neoplastic diseases according to the invention contains at least one E/Z isomer of aliphatic triphenylphosphonium derivatives of tamoxifen of the general formula (I) and/or IA or their corresponding salts of tertiary amine.

The present invention provides a phosphonium compound of formula (II). Also provided is a method for producing a quaternary phosphonium compound labeled with a positron emitting radionuclide, the method comprising the step of reacting an electrophile of formula (I): X.sup.1-CH.sub.2-A.sup.1 with triphenylphosphine having one or more radionuclide-labeled substituents on the benzene ring to give a quaternary phosphonium salt.

This disclosure relates to quaternary phosphonium compounds having lipophilic groups. In certain embodiments, this disclosure relates to quaternary phosphonium compounds having chemical formula as reported herein. In certain embodiments, this disclosure relates to compositions and devices comprising or coated with quaternary phosphonium compounds disclosed herein. In certain embodiments, this disclosure relates to preventing or treating a microbial infection or cancer using quaternary phosphonium compounds disclosed herein.

Embodiments of the invention are directed to ONO pincer ligands that can be in a trianionic, protonated or protonated equivalent form. The ONO pincer ligand can be combined with a metal comprising compound to form an ONO pincer ligand comprising transition metal complex. By choice of the ONO pincer ligand structure, the steric and electronic properties of the metal complexes therefrom can be controlled. The ONO pincer ligands comprise a central nitrogen atom that is disubstituted with a pair of three atom comprising bridges where the three atoms are a pair of sp.sup.2 hybridized carbons and an sp.sup.3 hybridized carbon.

The invention relates to novel NO donors which are targeted to the mitochondria. The NO donor compounds of the invention allow NO to be selectively provided to the mitochondria.

The invention relates to novel NO donors which are targeted to the mitochondria. The NO donor compounds of the invention allow NO to be selectively provided to the mitochondria.