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Chalcogen in the hetero ring

Subclass of:

540 - Organic compounds -- part of the class 532-570 series

540000000 - ORGANIC COMPOUNDS (CLASS 532, SUBCLASS 1)

540001000 - HETEROCYCLIC CARBON COMPOUNDS CONTAINING A HETERO RING HAVING CHALCOGEN (I.E., OXYGEN, SULFUR, SELENIUM OR TELLURIUM) OR NITROGEN AS THE ONLY RING HETERO ATOMS

540450000 - The hetero ring contains at least eight members including nitrogen and carbon

540451000 - Chalcogen double bonded directly to a ring carbon of the hetero ring which is adjacent to the ring nitrogen (e.g., laurolactam, etc.)

Patent class list (only not empty are listed)

Deeper subclasses:

Class / Patent application numberDescriptionNumber of patent applications / Date published
540454000 Chalcogen in the hetero ring 56
20150336915STRUCTURES OF PROTEASOME INHIBITORS AND METHODS FOR SYNTHESIZING AND USE THEREOF - Disclosed herein are novel structures of proteasome inhibitors and methods for synthesizing and use thereof, including novel structures of proteasome inhibitors, such as syrbactins and its analogs, and methods for synthesizing them and using them for effective proteasome inhibition.11-26-2015
540455000 Polycyclo ring system which contains the hetero ring as one of the cyclos 55
20090312540SPATIALLY-DEFINED MACROCYCLES INCORPORATING PEPTIDE BOND SURROGATES - Novel spatially-defined macrocyclic compounds incorporating peptide bond surrogates are disclosed. Libraries of these macrocycles are then used to select one or more macrocycle species that exhibit a specific interaction with a particular biological target, in particular, compounds according to the invention are disclosed as agonists or antagonists of a mammalian motilin receptor and a mammalian ghrelin receptor.12-17-2009
20100113770O-SUBSTITUTED HYDROXYARYL DERIVATIVES - A medicament having inhibitory activity against NF-κB activation which comprises as an active ingredient a substance selected from the group consisting of a compound represented by the following general formula (I) and a pharmacologically acceptable salt thereof, and a hydrate thereof and a solvate thereof:05-06-2010
20130217874METHOD FOR MAKING MACROCYCLES - Disclosed embodiments concern a method for making substantial quantities of desired macrocycles. Disclosed ring closing reactions make the macrocycle with desired olefin geometry in excellent yield and E/Z ratio. Particular embodiments of the current method concern intermediates that are obtained from commercially available starting materials in a small number of steps, thereby illustrating the commercial importance and applicability of the disclosed method. The macrocycle produced by the ring closing reaction can be further derivatized to provide analogs of the macrocyclic compounds.08-22-2013
540456000 Two of the cyclos share at least three ring members or a ring member is shared by three of the cyclos (e.g., bridged, peri-fused, etc.) 52
20080227975METHOD OF PRODUCING FR901228 - Depsipeptides and congeners thereof are disclosed having structure (I), wherein m, n, p, q, X, R1, R2 and R3 are as defined herein. These compounds, including FR901228, have activity as, for example, immunosuppressants, as well as for the prevention or treatment of patients suffering or at risk of suffering from inflammatory, autoimmune or immune system-related diseases including graft-versus-host disease and enhancement of graft/tissue survival following transplant. Also provided are methods for inhibiting lymphocyte activation, proliferation, and/or suppression of IL-2 secretion.09-18-2008
20080269479Process for Isolation of Macrolide Compounds - Although macrolide compounds are insoluble in water, surprisingly high part of the product was found in the liquid phase of the fermentation broth. Therefore, processing the entire fermentation broth, i.e. the suspension obtained by cultivation of a microorganism producing the required macrolide compound, is highly advisable. This invention teaches a method of processing the entire fermentation broth using cheap and environmentally acceptable solvents.10-30-2008
20080287675CASCADE SYSTEM - A method of purifying an active pharmaceutical ingredient sufficient for administration into a human subject can include: obtaining a reaction product composition having the active pharmaceutical ingredient and impurities, wherein said active pharmaceutical ingredient is rapamycin or a rapamycin analog; introducing the reaction product composition into a first column of a chromatography system; directing a first portion of a first elutant from the first column to waste, said first portion having more impurity than active pharmaceutical ingredient; directing a second portion of the first elutant from the first column into a second column, said second portion having more active pharmaceutical ingredient than impurity; collecting factions of a second elutant from the second column that include the active pharmaceutical ingredient; and concentrating the said collected fractions to obtain a purity of the active pharmaceutical ingredient greater than 98% and with less than or about 0.95% being first and second major impurities.11-20-2008
20090264644Novel Macrolide Compounds With Antibiotic and Antineoplastic Properties - The invention is drawn to novel macrolide compounds of formula I having antibiotic and antineoplastic activities, useful as medicaments and/or agrochemicals for microorganism infections, in particularly for infectious diseases involving drug-resistant 10-22-2009
20090292118Process for making Biolimus A9 - A process for making Biolimus A9 comprises reacting sirolimus (or rapamycin) with alkyl benzene sulfonate under the catalyzing of organic base and in the presence of organic solvent to undergo a nucleophilic substitution reaction to obtain the Biolimus A9 with high yield, not only for small-scale laboratory experiment, but also for rendering reproducibility of high yield even after process amplification.11-26-2009
200902990583-3-DI-SUBSTITUTED-OXINDOLES AS INHIBITORS OF TRANSLATION INITIATION - Compositions and methods for inhibiting translation using 3-(5-tert-Butyl-2-Hydroxy-phenyl)-3-phenyl-1,3-dihydro-indol-2-one and/or its derivatives are provided. Compositions, methods and kits for treating (1) cellular proliferative disorders, (2) non-proliferative, degenerative disorders, (3) viral infections, and/or (4) disorders associated with viral infections, using 3-(5-tert-butyl-2-hydroxy-phenyl)-3-phenyl-1,3-dihydro-indol-2-one and/or its derivatives are described.12-03-2009
20100022766BIOSYNTHETIC GENE CLUSTER FOR THE PRODUCTION OF A COMPLEX POLYKETIDE - A polyketide synthase complex composed of polyketide synthase with 15 total modules, a non-ribosomal peptide synthetase with 1 module, and a cytochrome P450 hydroxylase is described. Also provided are novel 01-28-2010
20100099865HEAT SHOCK PROTEIN 90 INHIBITORS - Novel compounds useful for inhibiting the 90kDa heat shock proteins containing a quinone-like moiety and a di-hydroxy phenol like moiety, similar to geldanamycin and radicicol.04-22-2010
20100197907Phosphorus-containing compounds & uses thereof - This invention concerns a new family of phosphorus-containing compounds containing a moiety JQA- in which:08-05-2010
20100204466ONE POT SYNTHESIS OF TETRAZOLE DERIVATIVES OF RAPAMYCIN - A single-step, one-pot process to obtain zotarolimus and other rapamycin derivatives on large scale is presented, which improves currently available synthesis schemes. In one embodiment, dried rapamycin is dissolved in isopropylacetate (IPAc). The solution is cooled, and 2,6-Lutidine is added, followed slowly adding triflic anhydride at −30° C. Salts are then removed by filtration. Tetrazole, followed by a tert-base diisopropylethylamine (DIEA) is added to the triflate solution. After incubation at room temperature, the product is concentrated and purified by a silica gel column using THF/heptane as eluant. The fractions containing the product are collected, concentrated, and purified again using an acetone/heptane column. The product containing fractions are concentrated. The product is dissolved in t-BME and precipitated with heptane. The solids are dissolved in acetone, treated with butylated-hydroxy toluene (BHT), and the solution concentrated. The process is repeated twice with acetone to remove solvents. At least one stabilizing agent is added, such as BHT at 0.5% before drying.08-12-2010
20100280238INTRAMOLECULAR AZIDE-ALKYNE CYCLOADDITION - The Huisgen 1,3-dipolar cycloaddition is a ‘click’ reaction that results from the ligation of azides and alkynes to give a triazole moiety. This reaction has been shown to be effective in the formation of a variety of macrocyclic rings. A key point of interest is the regioselectivity and specificity of the cycloaddition. Disclosed herein are specific, selective, and high-yielding methods of azide-alkyne macrocyclization to form 1,4- and 1,5-triazoles and libraries thereof.11-04-2010
20110009618METHODS OF MANUFACTURING CRYSTALLING FORMS OF RAPAMYCIN ANALOGS - A process for preparing a crystalline rapamycin analog includes: combining the rapamycin analog with an organic medium to form a mixture; incubating the mixture until the rapamycin analog crystallizes; and recovering the crystalline rapamycin analog. The organic medium can be a solvent, and the process can include causing the rapamycin analog to dissolve into the solvent, and incubating the solvent until the rapamycin analog crystallizes. The following can also be performed: forming a slurry of crystalline rapamycin analog; stirring the rapamycin analog mixture until the rapamycin analog crystallizes; saturating the rapamycin analog solution; forming a supersaturated rapamycin analog solution; combining an antisolvent with the rapamycin analog and the solvent to form a biphasic mixture, and incubating the biphasic mixture to cause a liquid-liquid phase split.01-13-2011
201100463673-3-DI-SUBSTITUTED-OXINDOLES AS INHIBITORS OF TRANSLATION INITIATION - Compositions and methods for inhibiting translation using 3-(5-tert-Butyl-2-Hydroxy-phenyl)-3-phenyl-1,3-dihydro-indol-2-one and/or its derivatives are provided. Compositions, methods and kits for treating (1) cellular proliferative disorders, (2) non-proliferative, degenerative disorders, (3) viral infections, and/or (4) disorders associated with viral infections, using 3-(5-tert-butyl-2-hydroxy-phenyl)-3-phenyl-1,3-dihydro-indol-2-one and/or its derivatives are described.02-24-2011
20110092697METHODS OF PREPARATION OF MACROCYCLIC COMPOUNDS - The instant invention describes methods for producing macrocyclic compounds having antiproliferation activity, and useful in methods of treating disorders such as cancer, tumors and cell proliferation related disorders.04-21-2011
20110172413PURIFICATION METHOD OF LACTONE COMPOUNDS CONTAINING UNSATURATED ALKYL GROUP BY EXTRACTION WITH SILVER ION SOLUTION - The present invention relates to a method for separating and purifying a lactone compound with an unsaturated alkyl group from a lactone compound with a saturated alkyl group which is an analog thereof. More specifically, the present invention relates to a method for effectively separating a lactone compound with an unsaturated alkyl group such as FK506 at high purity by extraction with a silver ion (Ag07-14-2011
20110184167PROCESS FOR THE PREPARATION OF TEMSIROLIMUS AND ITS INTERMEDIATES - Novel intermediates, process for their preparation and their use in the preparation of therapeutically effective antineoplastic agents, in particular Temsirolimus of formula (I).07-28-2011
20120041190MACROCYCLES AS FACTOR XIA INHIBITORS - The present invention provides compounds of Formula (I):02-16-2012
20120065393METHOD FOR REFINING OF HIGH PURITY OF TACROLIMUS - The present invention relates to a process of preparing a highly pure tacrolimus, which comprising a pre-purification process carried out by means of crystallization, and particularly to a process of preparing a highly pure tacrolimus, which comprises a pre-purification process comprising the steps of (a) extracting mycelia cake collected by filtering a tacrolimus-containing oily compound with an organic solvent, (b) concentrating the extract under reduced pressure and (c) crystallizing the concentrate. In addition, a highly pure tacrolimus can be obtained by dissolving the pre-purified crystals in an organic solvent, passing through the solution in an adsorption resin and concentrating the eluate under reduced pressure, followed by crystallization. According to a process of the present invention, Tacrolimus as pure as appropriate for a pharmaceutical purpose can be prepared by a simple process and at a relatively low cost.03-15-2012
20120202989PHARMACEUTICAL COMPOSITIONS COMPRISING POLYMORPHIC FORMS ALPHA, BETA, AND GAMMA OF RIFAXIMIN - Crystalline polymorphous forms of rifaximin (INN), referred to as rifaximin α and rifaximin β, and a poorly crystalline form referred to as rifaximin γ, useful in the production of medicaments containing rifaximin for oral and topical use and obtained by means of a crystallization process carried out by hot-dissolving the raw rifaximin in ethyl alcohol and by causing the crystallization of the product by addition of water at a fixed temperature and for a fixed period of time, followed by a drying under controlled conditions until reaching a precise water content in the end product, are the object of the invention.08-09-2012
20120309960MACROCYCLES AS FACTOR XIA INHIBITORS - The present invention provides compounds of Formula (I): or a stereoisomer, a tautomer, or a pharmaceutically acceptable salt thereof, wherein all the variables are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of fXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.12-06-2012
20130035483METHODS OF CONVERTING AMORPHOUS DRUG SUBSTANCE INTO CRYSTALLINE FORM - A method for converting an amorphous drug, such as everolimus, or other macrolide immunosuppressive drug, into a crystalline form. The method utilizes a slurry of the drug in organic liquid phase and ages the slurry to achieve the conversion.02-07-2013
20130274463PROCESS AND INTERMEDIATES FOR PREPARING MACROLACTAMS - The present invention relates to macrolactam compounds, intermediates useful in the preparation of macrolactams, methods for preparing the intermediates, and methods for preparing and modifying macrolactams. One use of the compounds and methods described herein is in the production of macrolactam compounds able to inhibit HCV NS3 protease activity. An example of an HCV inhibitory compound that can be synthesized using the procedures described herein is Compound A and derivative thereof.10-17-2013
20130296550METHOD FOR SYNTHESIZING TEMSIROLIMUS - A method for synthesizing temsirolimus, the method including: using a substituted boric acid to protect 2,2-dimethylol propionic acid to produce intermediate II; carrying out a reaction between the intermediate II and 2,4,6-trichlorobenzoyl chloride; carrying out condensation reaction between a resulting product and rapamycin to produce intermediate III; and finally using a diol to remove a protecting group from the intermediate III to yield temsirolimus.11-07-2013
20140058081METHOD FOR PREPARING 42-(DIMETHYLPHOSPHINATE) RAPAMYCIN - A method for preparing 42-(dimethylphosphinate) Rapamycin (Ridaforolimus) (I) is provided, which has advantages of high conversion rate and no 31,42-bis(dimethyl phosphinate) Rapamycin (III) generated. In the method of the present invention, Rapamycin (II) is firstly reacted with triethyl chlorosilane in a base condition to form 31,42-bis(triethylsilylether) Rapamycin (IV-b), followed by a selective deprotection process to obtain 31-triethylsilylether Rapamycin (V-b). Next, a phosphorylation reaction is performed by using dimethylphosphinic chloride under a base solution to obtain a crude product. Finally, a deprotection reaction is performed in a diluted sulfuric acid solution to obtain a crude product of Ridaforolimus (I). Since the conversion rate of each step of the method of the present invention is higher than 98%, it indicates that the method of the present invention is suitable for industrial production.02-27-2014
20140081016REGIOSELECTIVE ACYLATION OF RAPAMYCIN AT THE C-42 POSITION - The invention refers to the selective acylation of Rapamycin at the 42-position (I) with an acylating agent of the formula (II) wherein R03-20-2014
20140100364Compounds Useful For Making HCV Protease Inhibitors - Compounds useful for making HCV protease inhibitors are described. Methods of using these compounds to make HCV protease inhibitors are also provided.04-10-2014
20140243519METHODS AND INTERMEDIATES FOR PREPARING MACROLACTAMS - The present invention includes compounds useful as intermediates in the preparation of macrolactams, methods for preparing the intermediates, and methods for preparing macrolactams. One use of the methods and intermediates described herein is in the production of macrolactam compounds able to inhibit HCV NS3 protease activity. HCV NS3 inhibitory compounds have therapeutic and research applica08-28-2014
20140343276MACROCYCLES AS FACTOR XIA INHIBITORS - The present invention provides compounds of Formula (I):11-20-2014
20150112058MACROCYCLES AS FACTOR XIA INHIBITORS - The present invention provides compounds of Formula (I):04-23-2015
20150322086LOW TEMPERATURE SYNTHESIS OF RAPAMYCIN DERIVATIVES - The present invention provides improved processes for obtaining rapamycin derivatives including Biolimus A9.11-12-2015
20160002262PURIFICATION OF RAPAMYCIN DERIVATIVES USING TEMPERATURE INDUCED PHASE SEPARATION - The present invention provides methods for obtaining purified rapamycin derivatives, including purified Biolimus A9. A crystalline form of Biolimus A9 is also described.01-07-2016
20160046590SONIC HEDGEHOG MODULATORS - Sonic Hedgehog modulators and methods of use thereof are provided for.02-18-2016
20160139112MECHANISM AND DRUG TARGETS FOR REDUCING CELL EDEMA (NEUROPROTECTION) AND CYTOPLASMIC EXCITABILITY IN ASTROCYTES IN NORMAL AND PATHOLOGICAL STATES - The present invention pertains to a method for screening a compound useful in reducing astroglial edema, said method comprising: (i) providing a compound; (ii) bringing said compound in contact with an astrocyte; and (iii) determining the cAMP level in said astrocyte contacted with said compound; wherein said compound is identified as a compound useful in reducing astroglial edema, if the cAMP level in the astrocyte increases after contact. The present invention further pertains to an agent elevating the cAMP level in astrocytes for use in reducing astroglial edema.05-19-2016
540457000 A five-membered cyclo of the polycyclo ring system consists of four ring carbons and one ring oxygen (e.g., fused rifamycins, etc.) 19
20080262220POLYMORPHIC FORMS ALPHA, BETA AND GAMMA OF RIFAXIMIN - Crystalline polymorphous forms of rifaximin (INN) antibiotic named rifaximin α and rifaximin β, and a poorly crystalline form named rifaximin γ, useful in the production of medicinal preparations containing rifaximin for oral and topical use and obtained by means of a crystallization carried out by hot-dissolving the raw rifaximin in ethyl alcohol and by causing the crystallization of the product by addition of water at a determinate temperature and for a determinate period of time, followed by a drying carried out under controlled conditions until reaching a settled water content in the end product, are the object of the invention.10-23-2008
20090082558Amorphous form of rifaximin and processes for its preparation - A stable amorphous form of rifaximin is disclosed. This form is chemically and polymorphically stable on storage and can be prepared by dissolving rifaximin in a solvent to form a solution, which is precipitated by adding an anti-solvent and isolating of the precipitated amorphous rifaximin as an end product.03-26-2009
20100137580Process for preparing amorphous rifaximin and the amorphous rifaximin thus obtained - A process is described which enables Rifaximin in a completely amorphous form to be obtained. Said process comprises the steps of dissolving crude Rifaximin in absolute ethanol while hot and then collecting after precipitation by cooling the title compound under amorphous form.06-03-2010
20100174064FORMS OF RIFAXIMIN AND USES THEREOF - The present invention relates to Rifaximin polymorphic forms, to their use in medicinal preparations and to therapeutic methods using them.07-08-2010
20110152516PHARMACEUTICAL COMPOSITIONS COMPRISING POLYMORPHIC FORMS ALPHA, BETA, AND GAMMA OF RIFAXIMIN - Crystalline polymorphous forms of rifaximin (INN), referred to as rifaximin α and rifaximin β, and a poorly crystalline form referred to as rifaximin γ, useful in the production of medicaments containing rifaximin for oral and topical use and obtained by means of a crystallization process carried out by hot-dissolving the raw rifaximin in ethyl alcohol and by causing the crystallization of the product by addition of water at a fixed temperature and for a fixed period of time, followed by a drying under controlled conditions until reaching a precise water content in the end product, are the object of the invention.06-23-2011
20110152517AGENT FOR PREVENTING AND/OR TREATING FUNCTIONAL GASTROINTESTINAL DISORDER - A preventive and/or therapeutic agent which improves an abnormal bowel function such as an abdominal pain, a diarrhea, or a constipation and is effective for preventing or treating a functional gastrointestinal disorder is provided.06-23-2011
20110160448POLYMORPHIC FORMS ALPHA, BETA AND GAMMA OF RIFAXIMIN - Crystalline polymorphous forms of rifaximin (INN) antibiotic named rifaximin α and rifaximin β, and a poorly crystalline form named rifaximin γ, useful in the production of medicinal preparations containing rifaximin for oral and topical use and obtained by means of a crystallization carried out by hot-dissolving the raw rifaximin in ethyl alcohol and by causing the crystallization of the product by addition of water at a determinate temperature and for a determinate period of time, followed by a drying carried out under controlled conditions until reaching a settled water content in the end product, are the object of the invention.06-30-2011
20110160449PROCESSES FOR THE PRODUCTION OF POLYMORPHIC FORMS OF RIFAXIMIN - Crystalline polymorphous forms of rifaximin (INN) antibiotic named rifaximin α and rifaximin β, and a poorly crystalline form named rifaximin γ, useful in the production of medicinal preparations containing rifaximin for oral and topical use and obtained by means of a crystallization carried out by hot-dissolving the raw rifaximin in ethyl alcohol and by causing the crystallization of the product by addition of water at a determinate temperature and for a determinate period of time, followed by a drying carried out under controlled conditions until reaching a settled water content in the end product, are the object of the invention.06-30-2011
20120116071Rifaximin - Amorphous rifaximin, methods of making it, and pharmaceutical compositions containing it. Also described are methods of converting amorphous rifaximin to crystalline rifaximin and vice versa.05-10-2012
20120214989PROCESSES FOR THE PRODUCTION OF POLYMORPHIC FORMS OF RIFAXIMIN - Crystalline polymorphous forms of rifaximin (INN) antibiotic named rifaximin α and rifaximin β, and a poorly crystalline form named rifaximin γ, useful in the production of medicinal preparations containing rifaximin for oral and topical use and obtained by means of a crystallization carried out by hot-dissolving the raw rifaximin in ethyl alcohol and by causing the crystallization of the product by addition of water at a determinate temperature and for a determinate period of time, followed by a drying carried out under controlled conditions until reaching a settled water content in the end product, are the object of the invention.08-23-2012
20120316334FORMS OF RIFAXIMIN AND USES THEREOF - The present invention relates to Rifaximin polymorphic forms, to their use in medicinal preparations and to therapeutic methods using them.12-13-2012
20130072676USE OF POLYOLS TO OBTAIN STABLE POLYMORPHOUS FORMS OF RIFAXIMIN - Polyols stabilize polymorphous form of rifaximin, in particular the β form. When polyols having at least two hydroxy groups are added to rifaximin powder, polymorph β is stable and remains stable in time independently from the environment humidity.03-21-2013
20130289269PHARMACEUTICAL COMPOSITIONS COMPRISING POLYMORPHIC FORMS ALPHA, BETA, AND GAMMA OF RIFAXIMIN - Crystalline polymorphous forms of rifaximin (INN), referred to as rifaximin α and rifaximin β, and a poorly crystalline form referred to as rifaximin γ, useful in the production of medicaments containing rifaximin for oral and topical use and obtained by means of a crystallization process carried out by hot-dissolving the raw rifaximin in ethyl alcohol and by causing the crystallization of the product by addition of water at a fixed temperature and for a fixed period of time, followed by a drying under controlled conditions until reaching a precise water content in the end product, are the object of the invention.10-31-2013
20130338355PROCESS FOR PREPARING AMORPHOUS RIFAXMIN AND THE AMORPHOUS RIFAXIMIN THUS OBTAINED - A process is described which enables Rifaximin in a completely amorphous form to be obtained. Said process comprises the steps of dissolving crude Rifaximin in absolute ethanol while hot and then collecting after precipitation by—cooling the title compound under amorphous form.12-19-2013
20140179916FORMS OF RIFAXIMIN AND USES THEREOF - The present invention relates to Rifaximin polymorphic forms, to their use in medicinal preparations and to therapeutic methods using them.06-26-2014
20140200343PROCESS AND INTERMEDIATES FOR PREPARING MACROLACTAMS - The present invention includes compounds useful as intermediates in the preparation of macrolactams, methods for preparing the intermediates, and methods for preparing macrolactams from the intermediates. One use of the methods and intermediates described herein is in the production of macrolactam compounds able to inhibit HCV NS3 protease activity. HCV NS3 inhibitory compounds have therapeutic and research applications.07-17-2014
20150011750PROCESS FOR PREPARING AMORPHOUS RIFAXMIN AND THE AMORPHOUS RIFAXIMIN THUS OBTAINED - A process is described which enables Rifaximin in a completely amorphous form to be obtained. Said process comprises the steps of dissolving crude Rifaximin in absolute ethanol while hot and then collecting after precipitation by—cooling the title compound under amorphous form.01-08-2015
20160168166A PROCESS FOR PREPARING RIFAXIMIN K06-16-2016
20160200738FORMS OF RIFAXIMIN AND USES THEREOF07-14-2016
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