摘要:
The invention relates to methods for treating type 2 diabetes, obesity, metabolic syndrome and conditions associated with these by administering an AICAR-monophosphate (AICAR-MP) enhancing agent that increases endogenous AICAR-MP levels in a cell. Inhibition of AICAR-formyltransferase activity (AICARFT) in a cell that regulates metabolic activity (such as fat, liver, muscle, pancreatic beta or certain brain cells) increases AICAR-monophosphate levels which in turn results in activation of the AMP-kinase (AMPK) pathway, and all of the downstream functions mediated by AMPK including increased fatty acid oxidation, enhanced glucose transport and decreased fatty acid synthesis.
摘要:
The invention relates to N-[2-hydroxy-3-(1-piperidinyl)-propoxy]-pyridine-1-oxide-3-carboxamidine and its optically active enantiomers. (R)-(−)-N-[2-hydroxy-3-(1-piperidinyl)-propoxy]-pyridine-1-oxide-3-carboxamidine and (S)-(+)-N-[2-hydroxy-3-(1-piperidinyl)-propoxy]-pyridine-1-oxide-3-carboxamidine. Furthermore, the invention relates to the preparation of N-[2-hydroxy-3-(1-piperidinyl)-propoxy]-pyridine-1-oxide-3-carboxyimidoyl chloride, which may be used as an active ingredient of medicaments, and the preparation of the optically active enantiomers of this compound using the compounds of the invention as intermediate substances.
摘要:
The present invention comprises novel preparations of polyoxypropylene/polyoxyethylene copolymers which retain the therapeutic activity of the commercial preparations, but substantially reduce the undesirable effects which are inherent in the prior art preparations. Because the preparations of polyoxypropylene/polyoxyethylene copolymers which comprise the present invention are a less polydisperse population of molecules than the prior art polyoxypropylene/polyoxyethylene copolymers, the biological activity of the copolymers is better defined and more predictable and the cardiotoxicity inherent in the native copolymers is substantially reduced.
摘要:
The present invention comprises novel preparations of polyoxypropylene/polyoxyethylene copolymers which retain the therapeutic activity of the commercial preparations, but substantially reduce the undesirable effects which are inherent in the prior art preparations. Because the preparations of polyoxypropylene/polyoxyethylene copolymers which comprise the present invention are a less polydisperse population of molecules than the prior art polyoxypropylene/polyoxyethylene copolymers, the biological activity of the copolymers is better defined and more predictable and the cardiotoxicity inherent in the native copolymers is substantially reduced.
摘要:
A method of increasing expression of a molecular chaperon by a cell and/or enhancing the activity of a molecular chaperon in cells is provided. The method comprises treating a cell that is exposed to a physiological stress which induces expression of a molecular chaperon by the cell with an effective amount of a certain hydroxylamine derivative to increase the stress. Alternatively, an hydroxylamine derivative can be administrated to a cell before it is exposed to a physiological stress which induces expression of a molecular chaperon by the cell. Preferably, the cell to which an hydroxylamine derivative is administered is an eukaryotic cell. The hydroxylamine derivative corresponds to the formulae (I) or (II).The invention also provides novel hydroxylamine derivatives falling within the scope of the formulae (I) and (II) as well as pharmaceutical and/or cosmetical compositions comprising the said compounds.
摘要:
The present invention provides methods of enhancing healing of wound associated with diabetes, comprising administering an effective amount of one or more of certain hydroxylamine derivatives to a subject in need thereof. In another aspect, the instant invention provides methods of treating or preventing peripheral nervous system neuropathies. Peripheral nervous system neuropathies may but need not be diabetic neuropathies, and may but need not be associated with a diabetic wound. The invention also provides pharmaceutical compositions comprising a certain hydroxylamine derivative or a pharmaceutically acceptable salt thereof, optionally in combination with one or more additional therapeutic agents. In certain compositions and methods, the additional therapeutic agent is a second hydroxylamine derivative or a pharmaceutically acceptable salt thereof.
摘要:
The present invention includes novel polyoxyethylene/polyoxypropylene block copolymers as well as methods for making the block copolymers. The block copolymers are high molecular weight molecules and are useful as general surfactants and display enhanced biological efficacy as vaccine adjuvants.
摘要:
The present invention comprises novel preparations of polyoxypropylene/polyoxyethylene copolymers which retain the therapeutic activity of the commercial preparations, but are substantially free from the undesirable effects which are inherent in the prior art preparations. Because the preparations of polyoxypropylene/polyoxyethylene copolymers which comprise the present invention are a less polydisperse population of molecules than the prior art polyoxypropylene/polyoxyethylene copolymers, the biological activity of the copolymers is better defined and more predictable.
摘要:
The present invention relates to a method of treating brain cancer comprising administering a therapeutically effective substance to a patient, wherein the therapeutically effective substance comprises: (I), or a pharmaceutically acceptable salt thereof, wherein X is a moiety that can be cleaved hydrolytically or enzymatically in the body of the patient in a pH-dependent manner.
摘要:
The invention relates to reconstituted formulations comprising an anthracycline compound, ethanol, and water. The invention also relates to injectable compositions comprising the reconstituted formulation and Lactated Ringer's solution. Additionally, the invention relates to methods of using the formulations and compositions.