Patent classifications
A61K31/28
PENTAAZA MACROCYCLIC RING COMPLEXES POSSESSING ORAL BIOAVAILABILITY
Aspects of the present disclosure relate to compounds which have enhanced oral bioavailability. A transition metal complex includes a transition metal coordinated by a macrocycle comprising the pentaaza 15-membered macrocyclic ring corresponding to Formula A and two axial ligands having the formula OC(O)X.sub.1.
##STR00001## each of the two axial ligands has the formula OC(O)X.sub.1 wherein each X.sub.1 is independently substituted or unsubstituted phenyl or C(X.sub.2)(X.sub.3)(X.sub.4); each X.sub.2 is independently substituted or unsubstituted phenyl, or substituted or unsubstituted alkyl; each X.sub.3 is independently hydrogen, hydroxyl, alkyl, amino, X.sub.5C(O)R.sub.13 where X.sub.5 is NH or O, and R.sub.13 is C.sub.1-C.sub.18 alkyl, substituted or unsubstituted aryl or C.sub.1-C.sub.18 aralkyl, or OR.sub.14, where R.sub.14 is C.sub.1-C.sub.18 alkyl, substituted or unsubstituted aryl or C.sub.1-C.sub.18 aralkyl, or together with X.sub.4 is (O); and each X.sub.4 is independently hydrogen or together with X.sub.3 is (O).
TRIVALENT AND DIVALENT CATIONS AS ADMINISTRABLE AGENTS FOR INCREASED PROCESSIVITY AND IMPROVED FIDELITY OF REVERSE TRANSCRIPTASE IN TELOMERASE AND IN NUCLEIC ACID POLYMERASES
A novel method of increasing longevity by improving the processivity, fidelity, and activity of the telomerase enzyme is provided by agents which introduce trivalent cations such as scandium 3+ into the nuclei of cells, whereupon there occurs substitution of the trivalent cation into the place of the natural divalent cations such as magnesium or calcium or manganese. This substitution optimizes the adherence of the telomerase enzyme to its nucleic acid template with the result that cellular replicative senescence is delayed and deferred in various cell types. The trivalent cations can be introduced topically, orally as a food additive or supplement, or as a medication for oral, intramuscular, intrathecal or intravenous administration.
TRIVALENT AND DIVALENT CATIONS AS ADMINISTRABLE AGENTS FOR INCREASED PROCESSIVITY AND IMPROVED FIDELITY OF REVERSE TRANSCRIPTASE IN TELOMERASE AND IN NUCLEIC ACID POLYMERASES
A novel method of increasing longevity by improving the processivity, fidelity, and activity of the telomerase enzyme is provided by agents which introduce trivalent cations such as scandium 3+ into the nuclei of cells, whereupon there occurs substitution of the trivalent cation into the place of the natural divalent cations such as magnesium or calcium or manganese. This substitution optimizes the adherence of the telomerase enzyme to its nucleic acid template with the result that cellular replicative senescence is delayed and deferred in various cell types. The trivalent cations can be introduced topically, orally as a food additive or supplement, or as a medication for oral, intramuscular, intrathecal or intravenous administration.
Group 3 metal compounds and use thereof in the treatment of solid tumors
The present invention relates to the compounds of Formula 1 ##STR00001##
wherein M is Sc or Y,
Hal is Cl, Br, F or I
R is alkyl with 1-4 atoms of C
X is Cl, Br, F or I or a group such as that shown hereinafter ##STR00002##
wherein R is alkyl with 1-4 atoms of C
and the use thereof in the treatment of solid tumors.
Group 3 metal compounds and use thereof in the treatment of solid tumors
The present invention relates to the compounds of Formula 1 ##STR00001##
wherein M is Sc or Y,
Hal is Cl, Br, F or I
R is alkyl with 1-4 atoms of C
X is Cl, Br, F or I or a group such as that shown hereinafter ##STR00002##
wherein R is alkyl with 1-4 atoms of C
and the use thereof in the treatment of solid tumors.
LANTHANIDE COMPLEX FORMULATIONS
The present invention relates to a method of removal of metal ion impurities, such as calcium, from lanthanide metal complexes of macrocyclic chelators. The method uses a scavenger resin to remove metal ions, displaced from chelator, by an excess of lanthanide ions. Also provided is a method of preparation of MRI contrast agents, from the purified lanthanide metal complex, by the addition of a defined excess chelator.
LANTHANIDE COMPLEX FORMULATIONS
The present invention relates to a method of removal of metal ion impurities, such as calcium, from lanthanide metal complexes of macrocyclic chelators. The method uses a scavenger resin to remove metal ions, displaced from chelator, by an excess of lanthanide ions. Also provided is a method of preparation of MRI contrast agents, from the purified lanthanide metal complex, by the addition of a defined excess chelator.
Pharmaceutical composition comprising gold-containing agent for preventing or treating liver fibrosis or liver cirrhosis
The present invention relates to a pharmaceutical composition for preventing or treating liver fibrosis or liver cirrhosis, and more specifically, to a pharmaceutical composition for preventing or treating liver fibrosis or liver cirrhosis comprising a gold-containing agent. The pharmaceutical composition of the present invention, by comprising the gold-containing agent as an active ingredient, not only promotes M2-type transformation of macrophages but also inhibits the activation of stellate cells due to the increase of TREM-2 expression, and is thus expected to be effectively used as a pharmaceutical composition, a food composition, etc., for preventing, treating, or ameliorating liver fibrosis or liver cirrhosis. Additionally, gold-containing agents, such as auranofin, sodium aurothiomalate, and aurothioglucose, have long been used for the treatment of a different disease (rheumatoid arthritis), and thus they have an advantage in that they are less likely to cause adverse effects.
Pharmaceutical composition comprising gold-containing agent for preventing or treating liver fibrosis or liver cirrhosis
The present invention relates to a pharmaceutical composition for preventing or treating liver fibrosis or liver cirrhosis, and more specifically, to a pharmaceutical composition for preventing or treating liver fibrosis or liver cirrhosis comprising a gold-containing agent. The pharmaceutical composition of the present invention, by comprising the gold-containing agent as an active ingredient, not only promotes M2-type transformation of macrophages but also inhibits the activation of stellate cells due to the increase of TREM-2 expression, and is thus expected to be effectively used as a pharmaceutical composition, a food composition, etc., for preventing, treating, or ameliorating liver fibrosis or liver cirrhosis. Additionally, gold-containing agents, such as auranofin, sodium aurothiomalate, and aurothioglucose, have long been used for the treatment of a different disease (rheumatoid arthritis), and thus they have an advantage in that they are less likely to cause adverse effects.
Growth control of oral and superficial organisms using gallium compounds
The present invention provides methods for treating or preventing diseases and disorders caused by iron-dependent pathogenic microorganisms, such as bacteria, fungi, and parasites, by applying a gallium compound to an affected area. In particular, the present invention provides methods for treating or preventing dental caries, vaginal infections, skin infections, and so forth. Gallium compounds can be formulated as toothpaste, mouthwash, cream, ointment, gel, solution, eye drops, suppository, and the like. Furthermore, the invention provides methods for controlling microbial growth on environmental surfaces, including those of toothbrush, denture, dental retainer, contact lens, catheter, food stuff, and so forth. In addition, the present invention provides animal feeds which contain gallium compounds that promote the animal growth and prevent the animals from infections as well as protect consumers from post processing infections.