Patent classifications
A61K31/7048
ESCALATING DOSING REGIMEN FOR EFFECTING WEIGHT LOSS AND TREATING OBESITY
The present invention is drawn to novel topiramate compositions as well as methods for effecting weight loss, e.g., in the treatment of obesity and related conditions, including conditions associated with and/or caused by obesity per se. The present invention features an escalating dosing regimen adapted for the administration of topiramate and optionally a sympathomimetic agent such as phentermine or bupropion, in the treatment of obesity and related conditions.
ENHANCING AUTOPHAGY OR INCREASING LONGEVITY BY ADMINISTRATION OF UROLITHINS
Disclosed are methods, compounds, and compositions useful for increasing autophagy and promoting longevity. The methods, compounds, and compositions relate to urolithins and urolithin precursors and use thereof. Certain urolithins are represented by Formula I, while certain urolithin precursors are represented by Formula IV. The urolithin may be urolithin A, urolithin B, urolithin C, or urolithin D. The urolithin precursor may be ellagic acid or an ellagitannin. The methods include in vivo, ex vivo, and in vitro uses of the compounds and compositions.
ENHANCING AUTOPHAGY OR INCREASING LONGEVITY BY ADMINISTRATION OF UROLITHINS
Disclosed are methods, compounds, and compositions useful for increasing autophagy and promoting longevity. The methods, compounds, and compositions relate to urolithins and urolithin precursors and use thereof. Certain urolithins are represented by Formula I, while certain urolithin precursors are represented by Formula IV. The urolithin may be urolithin A, urolithin B, urolithin C, or urolithin D. The urolithin precursor may be ellagic acid or an ellagitannin. The methods include in vivo, ex vivo, and in vitro uses of the compounds and compositions.
COMPOSITIONS AND METHODS FOR PREVENTING AND TREATING RADIATION-INDUCED BYSTANDER EFFECTS CAUSED BY RADIATION OR RADIOTHERAPY
The invention provides novel compositions and methods for the treatment of Radiation-Induced Bystander Effects (RIBE), resulting from radiation exposure. In one preferred embodiment the inventions includes novel therapeutic agents, including but not limited to quercetin and quercetin analogs, as well as E64, CA074, CA074Me, that interfere with the activity of Cathepsin B.
COMPOSITIONS AND METHODS FOR PREVENTING AND TREATING RADIATION-INDUCED BYSTANDER EFFECTS CAUSED BY RADIATION OR RADIOTHERAPY
The invention provides novel compositions and methods for the treatment of Radiation-Induced Bystander Effects (RIBE), resulting from radiation exposure. In one preferred embodiment the inventions includes novel therapeutic agents, including but not limited to quercetin and quercetin analogs, as well as E64, CA074, CA074Me, that interfere with the activity of Cathepsin B.
DERIVATIVES OF DOLASTATIN 10 AND AURISTATINS
The present invention concerns a compound of following formula (I): where: —R.sub.1 is H or OH, —R.sub.2 is a (C.sub.1-C.sub.6)alkyl, COOH, COO—((C.sub.1-C.sub.6)alkyl) or thiazolyl group, —R.sub.3 is H or a (C.sub.1-C.sub.6)alkyl group, and —R.sub.4 is: .square-solid.a straight-chain or branched, saturated or unsaturated hydrocarbon group having 1 to 8 carbon atoms substituted by one or more groups chosen from among OH and NR.sub.5R.sub.6, .square-solid.—(CH.sub.2CH.sub.2X.sub.1)(CH.sub.2CH.sub.2X.sub.2).sub.a2(CH.sub.2CH.sub.2X.sub.3).sub.a3(CH.sub.2CH.sub.2X.sub.4).sub.a4(CH.sub.2CH.sub.2X.sub.5).sub.a5R.sub.7, .square-solid.an aryl-(C.sub.1-C.sub.8)alkyl group substituted by one or more groups chosen from among OH and NR.sub.9R.sub.10 groups, or .square-solid.a heterocycle-(C.sub.1-C.sub.8)alkyl group optionally substituted by one or more groups chosen from among (C.sub.1-C.sub.6)alkyl, OH and NR.sub.12R.sub.13 groups, or a pharmaceutically acceptable salt, hydrate or solvate thereof, and its uses in particular for the treatment of cancer, pharmaceutical compositions containing the same and the preparation methods thereof.
##STR00001##
DERIVATIVES OF DOLASTATIN 10 AND AURISTATINS
The present invention concerns a compound of following formula (I): where: —R.sub.1 is H or OH, —R.sub.2 is a (C.sub.1-C.sub.6)alkyl, COOH, COO—((C.sub.1-C.sub.6)alkyl) or thiazolyl group, —R.sub.3 is H or a (C.sub.1-C.sub.6)alkyl group, and —R.sub.4 is: .square-solid.a straight-chain or branched, saturated or unsaturated hydrocarbon group having 1 to 8 carbon atoms substituted by one or more groups chosen from among OH and NR.sub.5R.sub.6, .square-solid.—(CH.sub.2CH.sub.2X.sub.1)(CH.sub.2CH.sub.2X.sub.2).sub.a2(CH.sub.2CH.sub.2X.sub.3).sub.a3(CH.sub.2CH.sub.2X.sub.4).sub.a4(CH.sub.2CH.sub.2X.sub.5).sub.a5R.sub.7, .square-solid.an aryl-(C.sub.1-C.sub.8)alkyl group substituted by one or more groups chosen from among OH and NR.sub.9R.sub.10 groups, or .square-solid.a heterocycle-(C.sub.1-C.sub.8)alkyl group optionally substituted by one or more groups chosen from among (C.sub.1-C.sub.6)alkyl, OH and NR.sub.12R.sub.13 groups, or a pharmaceutically acceptable salt, hydrate or solvate thereof, and its uses in particular for the treatment of cancer, pharmaceutical compositions containing the same and the preparation methods thereof.
##STR00001##
DERIVATIVES OF DOLASTATIN 10 AND AURISTATINS
The present invention concerns a compound of following formula (I): where: —R.sub.1 is H or OH, —R.sub.2 is a (C.sub.1-C.sub.6)alkyl, COOH, COO—((C.sub.1-C.sub.6)alkyl) or thiazolyl group, —R.sub.3 is H or a (C.sub.1-C.sub.6)alkyl group, and —R.sub.4 is: .square-solid.a straight-chain or branched, saturated or unsaturated hydrocarbon group having 1 to 8 carbon atoms substituted by one or more groups chosen from among OH and NR.sub.5R.sub.6, .square-solid.—(CH.sub.2CH.sub.2X.sub.1)(CH.sub.2CH.sub.2X.sub.2).sub.a2(CH.sub.2CH.sub.2X.sub.3).sub.a3(CH.sub.2CH.sub.2X.sub.4).sub.a4(CH.sub.2CH.sub.2X.sub.5).sub.a5R.sub.7, .square-solid.an aryl-(C.sub.1-C.sub.8)alkyl group substituted by one or more groups chosen from among OH and NR.sub.9R.sub.10 groups, or .square-solid.a heterocycle-(C.sub.1-C.sub.8)alkyl group optionally substituted by one or more groups chosen from among (C.sub.1-C.sub.6)alkyl, OH and NR.sub.12R.sub.13 groups, or a pharmaceutically acceptable salt, hydrate or solvate thereof, and its uses in particular for the treatment of cancer, pharmaceutical compositions containing the same and the preparation methods thereof.
##STR00001##
METHOD AND COMPOSITION FOR PRODUCTION OF A PHYTONUTRIENT IN A MICROBIOME
A method useful for providing a phytonutrient to a subject via mediation of the subject’s microbiome is disclosed. The method includes administering a phytofunctional composition to a subject change the phytonutrient producer status of the subject. The method may also include identifying a phytonutrient producer status of the subject by assessing a level of at least one of a preselected phytonutrient and a preselected phytonutrient precursor compound within the subject. A phytofunctional composition useful in the method is also disclosed, and comprises a phytonutrient precursor compound and an active agent. The active agent comprises a probiotic and/or a prebiotic, and is adapted to mediate production of the preselected phytonutrient in the gastrointestinal tract of the subject, thereby changing the phytonutrient producer status of the subject.
METHOD AND COMPOSITION FOR PRODUCTION OF A PHYTONUTRIENT IN A MICROBIOME
A method useful for providing a phytonutrient to a subject via mediation of the subject’s microbiome is disclosed. The method includes administering a phytofunctional composition to a subject change the phytonutrient producer status of the subject. The method may also include identifying a phytonutrient producer status of the subject by assessing a level of at least one of a preselected phytonutrient and a preselected phytonutrient precursor compound within the subject. A phytofunctional composition useful in the method is also disclosed, and comprises a phytonutrient precursor compound and an active agent. The active agent comprises a probiotic and/or a prebiotic, and is adapted to mediate production of the preselected phytonutrient in the gastrointestinal tract of the subject, thereby changing the phytonutrient producer status of the subject.