Abstract: The invention encompasses an active metabolite of the 18-membered macrocyclic antimicrobial agents, specifically, a metabolite of tiacumicin B and in certain embodiments, R-Tiacumicin B or and its related compounds. In particular, the invention encompasses a compound that acts as a potent antibiotic agent for the treatment of bacterial infections, specifically GI infections caused by toxin producing strains of Clostridium difficile (C. difficile) and Clostridium perfringens (C. perfringens).
Type:
Grant
Filed:
March 15, 2013
Date of Patent:
December 23, 2014
Assignee:
Optimer Pharmaceuticals, Inc.
Inventors:
Yoshi Ichikawa, Yu-Hung Chiu, Youe-Kong Shue, Farah Kondori Babakhani
Abstract: Provided is a novel antimicrobial agent. More specifically, provided is a novel antimicrobial agent capable of effectively acting on various resistant bacteria such as VSSA, MRSA, VISA, VRE, and VRSA. A novel flavanone derivative having a six-membered monosaccharide derivative, specifically, a glucose derivative or a galactose derivative is capable of effectively acting on the bacteria. More specifically, a compound represented by the general formula (I) is capable of effectively acting on the bacteria. (In the formula: X represents a six-membered monosaccharide derivative; and Y is substituted by a hydroxyl group.
Type:
Grant
Filed:
July 29, 2010
Date of Patent:
December 23, 2014
Assignee:
National University Corporation Okayama University
Abstract: A method of treating hemorrhoids is disclosed. The method includes locally administering a composition including an effective amount of one or more macrocyclic lactone compounds, including avermectin compounds, milbemycin compounds, or mixture thereof and a pharmaceutically acceptable carrier to the affected anorectal region of an individual suffering from hemorrhoid.
Abstract: A method of treating herpes simplex virus infection or varicella zoster virus infection is disclosed. The method includes topically applying a composition containing an effective amount of one or more macrocyclic lactone compounds, including avermectin compounds or milbemycin compounds and a pharmaceutically acceptable carrier to the affected area of an individual suffering from herpes simplex virus infection or varicella zoster virus infection.
Abstract: A method of treating otitis externa is disclosed. The method includes topically applying an otic composition containing an effective amount of one or more macrocyclic lactone compounds, including avermectin compounds or milbemycin compounds and a pharmaceutically acceptable carrier into the external auditory canal and the auricle of an affected ear of an individual suffering from otitis externa.
Abstract: The invention relates to an amorphous non-crystalline glass form (Form-II) of 3R,4S,5S,6R,7R,9R,11S,12R,13S,14R-6-[(2S,3R,4S,6R)-4-dimethylamino-3-hydroxy-6-methyloxan-2-yl]oxy-14-ethyl-7,12,13-trihydroxy-4-[(2R,4R,5S,6S)-5-hydroxy-4-methoxy-4,6-dimethyloxan-2-yl]oxy-10-(2-methoxyethoxymethoxyimino)-3,5,7,9,11,13-hexamethyl-1-oxa-cyclotetradecan-2-one or roxithromycin having at least one characteristic infra-red spectrum peak at approximately 3580 to 3464 cm?1. The invention further relates to a preparation method of increasing the solubility of roxithromycin including the steps of selecting anhydrous roxithromycin or monohydrated roxithromycin; elevating the temperature of the roxithromycin to above the melting point thereof; and reducing the temperature of the melt sufficiently to allow it to set into an amorphous non-crystalline glass form (Form-II) of roxithromycin having relatively increased solubility without decreasing the stability of thereof.
Type:
Grant
Filed:
December 15, 2010
Date of Patent:
December 2, 2014
Assignee:
North-West University
Inventors:
Wilna Liebenberg, Marique Aucamp, Melgardt M De Villiers
Abstract: A composition comprising a carboxamide compound represented by following formula (I), wherein R1 represents a hydrogen atom or a methyl group, and R2 represents a methyl group, a difluoromethyl group or a trifluoromethyl group, and abamectin is provided by the present invention, and this composition has an excellent pesticidal effect.
Abstract: This application pertains to compositions and use of platinum(IV) compounds to alter zinc-binding sites, zinc-binding domains, zinc metalloproteins or zinc-associated proteins. Such interactions alter specific activities of these zinc-binding sites and associated protein functions, therefore offering therapeutic value.
Abstract: The present invention relates to novel polymorphs of the trisaccharide 2?-O-fucosyllactose (2-FL) of formula (1), methods for producing said polymorphs and their use in pharmaceutical or nutritional compositions.
Type:
Grant
Filed:
June 1, 2011
Date of Patent:
November 18, 2014
Assignee:
Glycom A/S
Inventors:
Károly Ágoston, István Bajza, Gyula Dekany, Péter Trinka, Ágnes Ágoston, Gábor Kádár, Sándor Demkó, Ignacio Figueroa-Pérez, Markus Hederos, Ferenc Horváth, Andreas Schroven, Ioannis Vrasidas, Piroska Kovács-Pénzes, Christian Risinger, László Kalmár, Gergely Pipa, Julien Boutet, Lars Kröger, Christoph Röhrig
Abstract: A pest controlling composition comprising spinetoram and a cyclic keto-enol compound having an acetyl CoA carboxylase-inhibiting activity as active ingredients.
Abstract: Disclosed are compounds represented by formula (I), pharmaceutically acceptable salts thereof, solvates thereof, and solvates of the pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, W and are as defined in the present application.
Abstract: Oral pentosan polysulfate (PPS) compositions treat diseases such as diabetes, inflammation, atherosclerosis. The compositions are also effective in reducing matrix metalloproteinases (MMPs).
Type:
Grant
Filed:
January 14, 2011
Date of Patent:
October 28, 2014
Assignee:
Icahn School of Medicine at Mount Sinai
Inventors:
Gary E. Striker, Helen Vlassara, Feng Zheng
Abstract: Compounds of Formula I or II, and methods of making and using thereof, are described herein. M represents a macrolide subunit, E is a C1-6 group, optionally containing one or more heteroatoms, D is an alkyl or aryl group, A is a linking group connected to D, B is an alkyl, alkylaryl or alkylheteroaryl spacer group, ZBG is a Zinc Binding Group, R1, R2 and R4 are independently are selected from hydrogen, a C1-6 alkyl group, a C2-6 alkenyl group, a C2-6 alkynyl group, a C1-6 alkanoate group, a C2-6 carbamate group, a C2-6 carbonate group, a C2-6 carbamate group, or a C2-6 thiocarbamate group, R3 is hydrogen or —OR5, R5 is selected from a group consisting of Hydrogen, a C1-6 alkyl group, a C2-6 alkenyl group, a C2-6 alkynyl group, C1-6 alkanoate group, C2-6 carbamate group, C2-6 carbonate group, C2-6 carbamate group, or C2-6 thiocarbamate group.
Abstract: A separating agent for optical isomers that uses a polysaccharide derivative provided by replacing all or a portion of the hydrogen atoms on the hydroxyl groups present in a polysaccharide with two specific atomic groups that act on optical isomers targeted for separation in an optical resolution, wherein the sum of the average introduction ratios of specific terminal substituents in these atomic groups is greater than 3.0 per monosaccharide unit.
Abstract: Described herein are polysaccharide gel formulations including at least one inhibitor of polysaccharide degradation and methods of making the same. The methods described herein involve the steps of providing at least one polysaccharide and incorporating at least one inhibitor of degradation into the polysaccharide. In some embodiments, the incorporating step comprises 1) mixing the at least one inhibitor with the at least one polysaccharide at a highly hydrated state thereby encapsulating the at least one inhibitor in a polysaccharide network, and 2) dehydrating the polysaccharide network thereby controlling release kinetics or final swell ratio. In another embodiment, the incorporating step comprises 1) encapsulating at least one inhibitor into a biocompatible or biodegradable vessel and 2) combining the polysaccharide and the vessel into a gel formulation. The polysaccharide gel formulations described herein can be used for a variety of cosmetic applications.
Type:
Grant
Filed:
March 27, 2013
Date of Patent:
October 7, 2014
Assignee:
Allergan, Inc.
Inventors:
Dimitrios Stroumpoulis, Christopher S. Mudd, Ahmet Tezel
Abstract: The present invention relates to novel C-glycoside compounds of given absolute configuration, to a process for synthesizing them and to compositions containing them. The invention also relates to the cosmetic use of these C-glycoside compounds as agents to stimulate the synthesis of glycosaminoglycans containing a D-glucosamine and/or N-acetyl-D-glucosamine residue, advantageously hyaluronic acid, and/or of proteoglycans, advantageously proteoglycans containing hyaluronic acid, by fibroblasts and/or keratinocytes. The invention also relates to a cosmetic process for treating keratin materials using a composition containing at least one C-glycoside compound according to the invention.
Type:
Grant
Filed:
February 26, 2008
Date of Patent:
October 7, 2014
Assignee:
L'Oreal
Inventors:
Simon Trouille, Alexandre Cavezza, Patrick Pichaud
Abstract: The present invention provides an anti-plant virus agent which exhibits preventative and therapeutic effects on plant virus diseases. The anti-plant virus agent of the present invention is characterized by containing at least one compound selected from the group consisting of ascorbic acid derivatives represented by Formula (I) (wherein, R1 to R4 each independently represents a hydrogen atom, —SO3H, —PO3H2, a glycosyl group, or —COR11, wherein R11 represents an unsubstituted or substituted C1-30 alkyl group, or an unsubstituted or substituted C2-30 alkenyl group, with the proviso that R1 to R4 may not all be hydrogen atoms at the same time), and salts thereof.
Type:
Grant
Filed:
September 9, 2010
Date of Patent:
October 7, 2014
Assignees:
National University Corporation Hokkaido University, Nippon Soda Co., Ltd.