Abstract:
A method of reducing glutamate efflux from skeletal muscle by inhibiting system Xc- activity is provided. The method is useful for the treatment of statin-induced myalgia. Pharmaceutical compositions useful to treat statin-induced myalgia are also provided, as well as a kit.
Abstract:
Disclosed are a monosubstituted or polysubstituted amphiphilic hypocrellin derivative, preparation method therefor, and uses thereof. In the present invention, the amphiphilic hypocrellin derivative having substituted functional groups such as condensed ethylene glycol and quaternary ammonium salt shows in its absorption spectrum a substantial redshift and an enhanced molar extinction coefficient compared to hypocrellin precursor, and can highly effectively produce reactive oxygen species such as singlet state oxygen under light-sensitive conditions. By adjusting the hydrophobicity and hydrophilicity of said derivative, said derivative can have different amphiphilicity and enhanced biocompatibility with cells or tissues. The amphiphilic hypocrellin derivative can satisfy the requirements for different clinical medications and addresses the conflict between medicinal hydrophilicity and lipophilicity caused by different administration methods. Compared to the first and second generation commercial photosensitizer, under the same conditions, the amphiphilic hypocrellin derivative photosensitizer of the present invention has higher photodynamic capabilities in the eradication of live tumor cells.
Abstract:
A compound of formula the following formula:(I). In this formula, moieties A, B, X, R 1 , R 2 , and R 3 are defined herein. Also disclosed are a nanocomplex that is formed of such a compound and a pharmaceutical agent, and a nanocomplex that is formed of a protein and a bioreducible compound.
Abstract:
The present application discloses novel amino-sulfide metal catalysts for organic chemical syntheses including hydrogenation (reduction) of unsaturated compounds or dehydrogenation of substrates. The range of hydrogenation substrate compounds includes esters, lactones, oils and fats, resulting in alcohols, diols, and triols as reaction products. The catalysts of current application can be used to catalyze a hydrogenation reaction under solvent free conditions. The present catalysts also allow the hydrogenation to proceed without added base, and it can be used in place of the conventional reduction methods employing hydrides of the main-group elements. Furthermore, the catalysts of the present application can catalyze a dehydrogenation reaction under homogenous and/or acceptorless conditions. As such, the catalysts provided herein can be useful in substantially reducing cost and improving the environmental profile of manufacturing processes for a variety of chemicals.
Abstract:
Gegenstand der vorliegenden Erfindung ist ein Verfahren zur Herstellung von primären Aminen umfassend die Verfahrensschritte A) Bereitstellung einer Lösung eines primären Alkohols in einer fluiden, nicht gasförmigen Phase, B) in Kontakt Bringen der Phase mit freiem Ammoniak und/oder mindestens einer Ammoniak freisetzenden Verbindung und einem homogenen Katalysator und gegebenenfalls C) Isolierung des in Verfahrensschritt B) gebildeten primären Amins, dadurch gekennzeichnet, dass das Volumenverhältnis des Volumens der Flüssigphase zu dem Volumen der Gasphase im Verfahrensschritt B größer 0,05 ist und/oder dass Verfahrensschritt B bei Drücken größer als 10 bar durchgeführt wird.
Abstract:
The present invention relates to a novel process for the preparation of compounds of the formula (I) by mixing in a first step amino alcohols of the formula (II) with sulfuric acid to yield the salt, by then reacting them in a second step in a drying device to give sulfuric acid esters of the general formula (III) and by reacting these sulfuric acid esters in a third step with mercaptans or salts thereof of the general formula (IV): RSM in each formula, where applicable, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R, n and M have the meanings given in the description, in the presence of a diluent and in the presence of a base.
Abstract:
The invention describes compositions and kits comprising organic nitric oxide enhancing salts of cyclooxygenase 2 (COX-2) selective inhibitors, and compositions comprising at least one organic nitric oxide enhancing salt of a COX-2 selective inhibitor, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The invention also provides methods for (a) treating inflammation, pain and fever; (b) treating gastrointestinal disorders and/or improving the gastrointestinal properties of COX-2 selective inhibitors; (c) facilitating wound healing; (d) treating renal and/or respiratory toxicities; (e) treating disorders resulting from elevated levels of cyclooxygenase-2; (f) improving the cardiovascular profile of COX-2 selective inhibitors; (g) treating diseases resulting from oxidative stress; (h) treating endothelial dysfunctions; (j) treating diseases caused by endothelial dysfunctions; (k) treating inflammatory disease states and/or disorders; (1) treating ophthalmic disorders; and (m) treating peripheral vascular diseases. The organic nitric oxide enhancing compounds that form salts with the COX-2 selective inhibitor are organic nitrates, organic nitrites, nitrosothiols, thionitrites, thionitrates, NONOates, heterocyclic nitric oxide donors and/or nitroxides. The heterocyclic nitric oxide donors are furoxans, sydnonimines, oxatriazole-5-ones and/or oxatriazole-5-imines. The organic nitric oxide enhancing salts of cyclooxygenase 2 selective inhibitors of the invention are organic nitric oxide enhancing salts of 2(2-((2-chloro-6-fluorophenyl) amino)5- methylphenyl)acetic acid derivatives.