Entries |
Document | Title | Date |
20080221142 | EFTU INHIBITORS OR AMINOTHIAZOLES AND THEIR USES - The present application describes organic compounds that are useful for the treatment, prevention and/or amelioration of diseases. | 09-11-2008 |
20080262012 | PHARMACEUTICAL 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. | 10-23-2008 |
20080280934 | Method of Preparing Porphyrin Derivatives, Porphyrin Derivatives, Uses Thereof and Pharmaceutical Compositions - Method of preparing a porphyrin derivative starting from a meso-substituted porphyrin compound. According to the invention, the meso-substituted porphyrin compound used is a meso-(2′-cyanovinyl)-substituted porphyrin compound, wherein said meso-(2′-cyanovinyl)-substituted porphyrin compound, in a form in which its porphyrin ring is complexed with a bivalent metal ion is converted, in the present of an acid for which | 11-13-2008 |
20090042922 | NOVEL BELACTOSIN DERIVATIVES AS THERAPEUTIC AGENTS/BIOLOGICAL PROBES AND THEIR SYNTHESIS - Derivatives of belactosin and their synthesis are disclosed. In certain embodiments, compounds of the present invention exhibit anti-cancer, antiviral, antibiotic, and/or auto-immune therapeutic abilities. In general, methods of synthesis disclosed herein allow for introduction of a variety of substituents at numerous positions as well as the facile introduction of a beta-lactone ring moiety. The synthetic steps comprise, in preferred embodiments, a tandem Mukaiyama aldol lactonization reaction. Data demonstrating the utility of some of the derivatives as proteasome inhibitors is also disclosed. | 02-12-2009 |
20090156627 | THERAPEUTIC COMPOUNDS - The invention provides compounds of formula I: | 06-18-2009 |
20090156628 | Aminothiazoles and their Uses - The present application describes organic compounds that are useful for the treatment, prevention and/or amelioration of diseases particularly bacterial infections. | 06-18-2009 |
20090163528 | Pharmaceutical composition having analgesic effects - The pharmaceutical compositions having analgesic effect referred to in this invention are composed of the aconitine ingredients as the active medical ingredients and other acceptable auxiliary ingredients. The active medical ingredients shall at least include the fuziline compound of Formula (I). The drugs exert desirable analgesic effect with low toxicity. They can be made into commonly used oral preparations, injectable preparations and/or external preparations, including ointments, suppositories lotions, medicinal dressings, etc. | 06-25-2009 |
20090239891 | Sustained Release Dosage Forms of Analgesic Medications - Parenteral extravascular administration of a composition containing an analgesic medication of low water solubility that is dissolved, suspended, or emulsified in a solvent system results in the deposition of the analgesic medication at the site of administration and provides a controlled release of the analgesic medication from the site and a prolonged analgesia that may persist for several days following administration. | 09-24-2009 |
20090239892 | PYRIDOMORPHINANS, PYRIDAZINOMORPHINANS AND USE THEREOF - Compounds represented by the formula: | 09-24-2009 |
20090270437 | Use of Buprenorphine or N-Alkylated Derivatives Thereof for Wound Healing - This invention relates to opioid compounds such as burenorphine or N-alkylated derivatives thereof for wound healing. | 10-29-2009 |
20090312357 | Rifaximin - 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. | 12-17-2009 |
20090325994 | METHODS OF TREATING DIARRHEA CAUSED BY SMALL INTESTINAL BACTERIAL OVERGROWTH - Disclosed is a method of diagnosing irritable bowel syndrome, fibromyalgia, chronic fatigue syndrome, depression, attention deficit/hyperactivity disorder, autoimmune diseases, such as multiple sclerosis and systemic lupus erythematosus, or Crohn's disease, which involves detecting the presence of small intestinal bacterial overgrowth (SIBO) in a human subject having at least one symptom associated with a suspected diagnosis of any of those diagnostic categories. Also disclosed is a method of treating these disorders, and other disorders caused by SIBO, that involves at least partially eradicating a SIBO condition in the human subject. The method includes administration of anti-microbial or probiotic agents, or normalizing intestinal motility by employing a prokinetic agent. The method improves symptoms, including hyperalgesia related to SIBO and disorders caused by SIBO. Also disclosed is a kit for the diagnosis or treatment of irritable bowel syndrome, fibromyalgia, chronic fatigue syndrome, depression, attention deficit/hyperactivity disorder, autoimmune diseases, or Crohn's disease. | 12-31-2009 |
20100010028 | USE 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. In this invention a method to prepare formulations constituted by pure and stable polymorphous forms able to give a pharmaceutical product is described. | 01-14-2010 |
20100063082 | CAMPTOTHECIN DERIVATIVES WITH ANTITUMOR ACTIVITY - Novel camptothecin derivatives having antitumor activity, the processes for the preparation thereof, the use thereof as antitumor drugs and pharmaceutical compositions containing them. | 03-11-2010 |
20100069421 | COMPOSITIONS AND METHODS FOR THE TREATMENT OF RADIATION PROCTOSIGMOITIS - The present invention provides a new method of preventing, ameliorating and/or treating enteritis induced by abdominopelvic therapies. The present invention also relates to the prophylactic treatment of traveler's diarrhea. | 03-18-2010 |
20100087469 | Natural product derivatives with antimalarial activity - The present invention provides new chemical compositions with desirable biological activity and toxicity profiles for the enhanced treatment of malaria. | 04-08-2010 |
20100087470 | Buprenorphine-Wafer for Drug Substitution Therapy - The present invention relates to oral pharmaceutical dosage forms comprising buprenorphine with the dosage form releasing buprenorphine instantly upon oral, preferably sublingual, application of the dosage form. The present invention also relates to the use of such dosage forms for treating pain in a human or animal or for drug substitution therapy in drug-dependent human subjects. | 04-08-2010 |
20100093778 | SUSTAINED RELEASE PARENTERAL FORMULATIONS OF BUPRENORPHINE - An oil-in-water buprenorphine formulation including buprenorphine and a surfactant that emulsifies the buprenorphine in oil, wherein the drug release is controlled by varying the oil concentration and/or pH. A buprenorphine aqueous suspension formulation including a free base buprenorphine and a suspension stabilizer. A buprenorphine oil formulation including a buprenorphine salt suspended in a pharmaceutically acceptable oil. Methods of providing sustained release of buprenorphine over a period of time. | 04-15-2010 |
20100173926 | Methods for Regulating Neurotransmitter Systems by Inducing Counteradaptations - The present invention relates to methods for regulating neurotransmitter systems by inducing a counteradaptation response. According to one embodiment of the invention, a method for regulating a neurotransmitter includes the step of repeatedly administering a ligand for a receptor in the neurotransmitter system, with a ratio of administration half-life to period between administrations of no greater than ½. The methods of the present invention may be used to address a whole host of undesirable mental, neurological and physiological conditions. | 07-08-2010 |
20100184796 | AGONISTS OF BITTER TASTE RECEPTORS AND USES THEREOF - The present invention relates to agonists of the human bitter-taste receptors hTAS2R46, hTAS2R47 and hTAS2R50 and their role in bitter taste transduction. The invention also relates to methods for identifying molecules that modulate, e.g. suppress, or enhance hTAS2R46, hTAS2R47 and hTAS2R50 bitter taste transduction or bitter taste response. | 07-22-2010 |
20100234412 | Buprenorphine Derivatives and Uses Thereof - Ester derivatives of the phenolic hydroxyl group of buprenorphine can be used in the treatment of opiate dependency and/or moderate to severe pain. The esters have an enhanced bioavailability, an enhanced duration of action, and a reduced abuse potential. | 09-16-2010 |
20100249168 | Compounds and Formulations Suitable for Radical Scavenging - The present invention relates to compositions and methods of using free radical scavengers with reduced | 09-30-2010 |
20100267757 | AMINOTHIAZOLES AND THEIR USES - The present application describes organic compounds that are useful for the treatment, prevention and/or amelioration of diseases. | 10-21-2010 |
20100286184 | AQUEOUS SOLUTION OF CONOPHYLLINE AND/OR CONOPHYLLIDINE - PROBLEMS TO BE SOLVED BY THE INVENTION To provide aqueous solutions of conophylline and/or conophyllidine; methods for purifying conophylline and/or conophyllidine from the aqueous solutions; methods for producing the aqueous solutions, water-soluble compositions containing conophylline and/or a conophyllidine useful for food compositions or pharmaceutical compositions or methods for preparing the same; as well as food compositions or pharmaceutical compositions containing the water-soluble compositions.
| 11-11-2010 |
20100286185 | HCV NS3 Protease Inhibitors - The present invention relates to macrocyclic compounds of formula (I) that are useful as inhibitors of the hepatitis C virus (HCV) NS3 protease, their synthesis, and their use for treating or preventing HCV infections. | 11-11-2010 |
20100292264 | Small molecules with antiprotozoal activity - The present invention provides new chemical compositions with desirable biological activity and toxicity profiles for the enhanced treatment of malaria. | 11-18-2010 |
20100292265 | Pack Of Medicinal Tablets - A water- and oxygen-occlusive pack is described. The pack encloses an inert atmosphere containing medicinal tablets, wherein the tablets contain buprenorphine or a salt or ester thereof. | 11-18-2010 |
20100298369 | BERBAMINE DERIVATIVES - The invention provides novel berbamine derivatives, and compositions or pharmaceutical compositions thereof. These berbamine derivatives have shown higher potency in killing cancer/tumor cells comparing to berbamine, and can be used in cancer/tumor treatments. | 11-25-2010 |
20100317681 | MODULATION OF SYSTEMIC EXPOSURE TO RIFAXIMIN - The present invention relates to the effect of hepatic insufficiency on the pharmacokinetics of rifaximin. Also provided are methods of determining an appropriate dose of rifaximin for a subject suffering from hepatic insufficiency. In addition, methods of treatment are provided subjects having or susceptible to hepatic insufficiency to be treated with rifaximin. | 12-16-2010 |
20110034501 | METHOD OF RESTORING THE INCRETIN EFFECT - The present invention relates to methods of treating metabolic syndrome, Type 2 diabetes mellitus, atherogenic dyslipidemia and/or obesity. The present invention also relates to methods of restoring the incretin effect, to restoring physiologic control of glucagon levels, to restoring first-phase insulin secretion, and to restoring the physiologic glucose-dependent insulin secretion. The methods of the present invention comprise administration of a selective κ-receptor antagonist, such as guanidinylated naltrindole (GNTI), or pharmaceutically acceptable derivatives thereof to a subject in need thereof. | 02-10-2011 |
20110065740 | METHODS OF TREATING TRAVELERS DIARRHEA AND HEPATIC ENCEPHALOPATHY - Treatment of traveler's diarrhea using in subjects having hepatic encephalopathy using gastrointestinal specific antibiotics is disclosed. One example of a gastrointestinal specific antibiotic is rifaximin. | 03-17-2011 |
20110086871 | RIFAXIMIN COMPOSITIONS AND METHOD OF USE - Forms of rifaximin (INN) antibiotic, such as the poorly crystalline form named rifaximin γ are described, along with the production of medicinal preparations containing rifaximin for oral and topical use. | 04-14-2011 |
20110105550 | FORMS OF RIFAXIMIN AND USES THEREOF - The present invention relates to Rifaximin polymorphic, salt, hydrate, and amorphous forms, to their use in medicinal preparations and to therapeutic methods using them. | 05-05-2011 |
20110105551 | Analgesics for nasal administration - An analgesic and a delivery agent are combined in a pharmaceutical composition such that, on introduction into the nasal cavity of a patient to be treated, the analgesic may be delivered to the bloodstream to produce within 30 minutes a therapeutic plasma concentration, C | 05-05-2011 |
20110118293 | METHOD OF RESTORING THE INCRETIN EFFECT - The present invention relates to methods of treating metabolic syndrome, Type 2 diabetes mellitus, atherogenic dyslipidemia and/or obesity. The present invention also relates to methods of restoring the incretin effect, to restoring physiologic control of glucagon levels, to restoring first-phase insulin secretion, and to restoring the physiologic glucose-dependent insulin secretion. The methods of the present invention comprise administration of a selective κ-receptor antagonist, such as guanidinylated naltrindole (GNTI), or pharmaceutically acceptable derivatives thereof to a subject in need thereof. | 05-19-2011 |
20110136846 | Buprenorphine Analogs - The present invention is directed to Buprenorphine Analog compounds of the Formula I, Formula II or Formula III shown below, wherein R | 06-09-2011 |
20110166170 | SYNTHESIS OF AVRAINVILLAMIDE, STEPHACIDIN B, AND ANALOGUES THEREOF - The syntheses of the natural products, avrainvillamide and stephacidin B, are provided. The α,β-unsaturated nitrone functionality of avrainvillamide and its 3-alkylidene-3H-indole 1-oxide core is shown to covalently and reversibly bond to heteroatom-based nucleophiles. This capability may allow these molecules to bind active site nucleophiles and may provide the basis for designing potent and selective enzyme inhibitors. Both avrainvillamide and its dimer stephacidin B have been reported to exhibit antiproliferative activity, and avrainvillamide has been reported to exhibit antimicrobial activity against multi-drug resistant bacteria. Avrainvillamide has been found to target cytoskeleton-linking membrane protein (CLIMP-63) thereby preventing cells from undergoing mitosis. The invention provides syntheses of these natural products as well as analogs of these natural products and their functional cores. The compounds of the invention may be used in the treatment of diseases such as cancer, autoimmune diseases, and bacterial infection. | 07-07-2011 |
20110178113 | METHODS OF TREATING TRAVELER'S DIARRHEA AND HEPATIC ENCEPHALOPATHY - Treatment of traveler's diarrhea using in subjects having hepatic encephalopathy using gastrointestinal specific antibiotics is disclosed. One example of a gastrointestinal specific antibiotic is rifaximin. | 07-21-2011 |
20110301187 | BIS [O-(14-BENZOYLACONINE-8-YL)] ESTERS - The present invention concerns novel compounds having the structure (I). Another object of the invention is the use of compounds (I) for the fabrication of a medicament which is used for the treatment of tumour diseases. | 12-08-2011 |
20120004254 | G PROTEIN-COUPLED RECEPTOR ANTAGONIST AND ITS USE FOR PREVENTING AND TREATING ALZHEIMER'S DISEASE - The invention discloses methods for screening a reagent for treating or preventing Alzheimer's disease or related neurological pathology. A method according to the invention includes the steps of: (a) activating a receptor and determining a first extent of endocytosis of the receptor, wherein the receptor is a G-protein coupled receptor that associates with presenilin-1; (b) activating the receptor under the same conditions as in step (a), in the presence of a candidate reagent, and determining a second extent of endocytosis of the receptor; (c) determining a difference between the first extent of endocytosis and the second extent of endocytosis; and (d) repeating steps (a)-(c), if the difference is less than a threshold. The invention also disclose uses of receptor antagonists for manufacturing medicaments for treating or preventing Alzheimer's disease or related neurological pathology, wherein the receptor antagonists inhibit endocytosis of a G-protein coupled receptor that associates with presenilin-1 during endocytosis. | 01-05-2012 |
20120010231 | Dihydroetorphines and Their Preparation - The present invention provides a process for the preparation of a compound of formula (VI), or a salt or derivative thereof, wherein R | 01-12-2012 |
20120035202 | RIFAXIMIN COMPOSITIONS AND METHOD OF USE - Forms of rifaximin (INN) antibiotic, such as the poorly crystalline form named rifaximin γ are described, along with the production of medicinal preparations containing rifaximin for oral and topical use. | 02-09-2012 |
20120059023 | USE OF POLYMORPHIC FORMS OF RIFAXIMIN FOR MEDICAL PREPARATIONS - The present invention relates to Rifaximin polymorphic forms α, β and γ, to their use in medicinal preparations for the oral or topical route and to therapeutic methods using them. | 03-08-2012 |
20120077835 | FORMULATIONS OF RIFAXIMIN AND USES THEREOF - The present invention relates to new rifaximin forms comprising solid dispersions of rifaximin, methods of making same and to their use in medicinal preparations and therapeutic methods. | 03-29-2012 |
20120108620 | FORMS OF RIFAXIMIN AND USES THEREOF - The present invention relates to new rifaximin forms kappa, theta, rifaximin:piperazine cocrystal 1 and rifaximin:piperazine cocrystal 2, methods of making same and to their use in medicinal preparations and therapeutic methods. | 05-03-2012 |
20120196887 | METHODS AND COMPOSITIONS FOR IMPROVED RIFAMYCIN THERAPIES - Compositions comprising one or more rifamycin antibiotics and one or more bile acids, and methods of using the compositions for the treatment of infection. | 08-02-2012 |
20120196888 | PROCESS FOR PREPARING OXYMORPHONE, NALTREXONE, AND BUPRENORPHINE - Methods are provided which include converting oripavine to other opiates, including converting oripavine to naltrexone, buprenorphine, 14-hydroxymorphinone and/or converting 14-hydroxymorphinone to oxymorphone. Purification and salt formation are optionally included. | 08-02-2012 |
20120208835 | Method and dosage regimens for eliminating a chemical substance in blood - A method of reducing the concentration of a chemical or drug substance in the blood plasma comprising titrating an initial peak concentration of the chemical or drug substance in the blood for a predefined dosing period, titrating a lowest concentration level of the chemical or drug substance in the blood immediately before the end of the dosing period, and providing a plurality of subsequent dosing periods where each subsequent dosing period requires administration of a dosing amount of the chemical or drug substance and titrating of the peak concentration and the lowest concentration level to ensure that the lowest concentration level of the chemical or drug substance in the blood plasma for the subsequent dosing period is decreased by not more than five percent of the lowest concentration level of the previous dosing period and where the plurality of dosing periods added together is seventy days or more. | 08-16-2012 |
20120220617 | Fluorescent Perylene Derivatives for Direct Detection of Heparin - The invention relates to a perylene diimide derivative and to an in vitro method for preparing the same. In addition, the invention relates to a method for detecting heparin in a sample using perylene diimide derivatives, wherein the interaction of the perylene diimide derivative with heparin modulates the intensity of the fluorescent signal of the mixture compared to the solution. The invention also comprises a diagnostic kit for detecting heparin in a sample in vitro, comprising the perylene diimide derivative, as well as the use of the perylene diimide derivative for neutralizing the anticoagulant activity of heparin. | 08-30-2012 |
20120238595 | THERAPEUTIC COMPOUNDS - The invention provides compounds of formula (I) wherein u, d, v, m, n, R | 09-20-2012 |
20120245192 | PHARMACEUTICAL FORMULATIONS CONTAINING RIFAXIMIN, PROCESSES FOR THEIR OBTAINMENT AND METHOD OF TREATING INTESTINAL DISEASE - Disclosed herein are methods of treating a patient having an intestinal disorder, the methods comprising: administering to a patient in need thereof a pharmaceutical composition comprising a hydrate or solvate form of rifaximin in polymorphic form β, alone or in a mixture with other crystalline, hydrate, solvate or amorphous forms of rifaximin, in gastroresistant microgranules, wherein the rifaximin is administered at a dose of at least 800 mg per day for a period of at least 7 days. | 09-27-2012 |
20120264774 | FORMS OF RIFAXIMIN AND USES THEREOF - Embodiments relate to Rifaximin polymorphic, salt, and hydrate forms, methods of producing polymorphic forms and to their use in medicinal preparations and to therapeutic methods using them. | 10-18-2012 |
20120289532 | METHOD FOR THE PRODUCTION OF AMORPHOUS RIFAXIMIN - The present invention relates to a new amorphous form of rifaximin and to methods for the preparation thereof by means of high energy milling or Spray drying. The present invention further relates to a new amorphous form for use as medicament and to the pharmaceutical compositions composing it. | 11-15-2012 |
20130023552 | Small molecules with antimalarial activity - The present invention provides new chemical compositions with desirable biological activity and toxicity profiles for the enhanced treatment of malaria. | 01-24-2013 |
20130059875 | METHODS OF TREATING TRAVELER'S DIARRHEA AND HEPATIC ENCEPHALOPATHY - Treatment of traveler's diarrhea using in subjects having hepatic encephalopathy using gastrointestinal specific antibiotics is disclosed. One example of a gastrointestinal specific antibiotic is rifaximin. | 03-07-2013 |
20130072512 | RIFAXIMIN READY-TO-USE SUSPENSION - A stable, taste-masked, ready-to-use suspension comprising rifaximin dispersed in a suspension base and one or more pharmaceutically acceptable additive(s). Also provided is a process for preparing a stable, taste-masked, ready-to-use suspension of rifaximin comprising the steps of mixing rifaximin with the suspension base and further sizing the particles of rifaximin by milling the suspension to obtain a homogenously dispersed rifaximin suspension. | 03-21-2013 |
20130090348 | POLYMORPHIC FORMS OF RIFAXIMIN - Provided for in the instant application are two additional polymorphic forms of rifaximin; namely substantially pure APO-I and APO-II. Also provided are processes for preparing substantially pure APO-I and APO-II. Rifaximin is a non-aminoglycoside antibiotic that has previously been found to be useful for the treatment of traveller's diarrhea caused by | 04-11-2013 |
20130137713 | METHODS FOR TREATING BOWEL DISEASES - The present invention provides new methods of treating bowel disease (BD) by increasing a durability of response; treating BD in males; treating BD in adolescent subjects; treating bloating due to BD in males; and methods of maintaining remission of BD. | 05-30-2013 |
20130172380 | METHOD OF RESTORING THE INCRETIN EFFECT - The present invention relates to methods of treating metabolic syndrome, Type 2 diabetes mellitus, atherogenic dyslipidemia and/or obesity. The present invention also relates to methods of restoring the incretin effect, to restoring physiologic control of glucagon levels, to restoring first-phase insulin secretion, and to restoring the physiologic glucose-dependent insulin secretion. The methods of the present invention comprise administration of a selective κ-receptor antagonist, such as guanidinylated naltrindole (GNTI), or pharmaceutically acceptable derivatives thereof to a subject in need thereof. | 07-04-2013 |
20130184302 | METHODS FOR TREATING IRRITABLE BOWEL SYNDROME (IBS) AND INFECTIONS - The present invention provides new methods and kits for the retreatment of IBS, for reducing commonly-occurring infections in patients suffering from hepatic encephalopathy, and for reducing frequency of incidence of | 07-18-2013 |
20130203795 | METHODS FOR TREATING IRRITABLE BOWEL SYNDROME (IBS) - The present invention provides new methods and kits for treating IBS; treating IBS in females; treating IBS in older subjects; and treating IBS in non-white subjects. | 08-08-2013 |
20130203796 | INJECTABLE FLOWABLE COMPOSITION COMPRISING BUPRENORPHINE - The present invention is directed to a buprenorphine sustained release delivery system capable of delivering buprenorphine, a metabolite, or a prodrug thereof for a duration of about 14 days to about 3 months. The buprenorphine sustained release delivery system includes a flowable composition and a solid implant for the sustained release of buprenorphine, a metabolite, or a prodrug thereof. The implant is produced from the flowable composition. The buprenorphine sustained release delivery system provides in situ 1-month and 3-month release profiles characterized by an exceptionally high bioavailability and minimal risk of permanent tissue damage and typically no risk of muscle necrosis. | 08-08-2013 |
20130210852 | METHODS FOR TREATING INFECTION - The present invention provides new methods and kits for treating and preventing bacterial infection. | 08-15-2013 |
20130310409 | FORMS OF RIFAXIMIN AND USES THEREOF - Embodiments relate to Rifaximin polymorphic, salt, and hydrate forms, methods of producing polymorphic forms and to their use in medicinal preparations and to therapeutic methods using them. | 11-21-2013 |
20130310410 | POLYMORPHOUS FORMS OF RIFAXIMIN, PROCESSES FOR THEIR PRODUCTION AND USE THEREOF IN THE MEDICINAL PREPARATIONS - Crystalline polymorphous forms of the rifaximin (INN) antibiotic named rifaximin δ and rifaximin ε useful in the production of medicinal preparations 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 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. | 11-21-2013 |
20130324569 | PEGYLATED CYCLOPAMINE ANALOGUE, PREPARATION METHOD AND USES THEREOF - A PEGylated cyclopamine analog, preparation method, uses thereof and methods for treating proliferative diseases using the same are disclosed. The PEGylated cyclopamine analog is a compound represented by the following formula I, a compound comprising at least one group represented by the following formula I (in formula I, R is straight or branched polyethylene glycol having a molecular weight between 200 and 200,000 Dalton, L and X are linking groups), or their single enantiomers, mixture of enantiomers, mixture of diastereomers, pharmaceutically acceptable salts, solvates, or hydrates. | 12-05-2013 |
20140011828 | FORMS OF RIFAXIMIN AND USES THEREOF - The present invention relates to Rifaximin amorphous forms, to their use in medicinal preparations and to therapeutic methods using them. | 01-09-2014 |
20140057931 | BUPRENORPHINE ANALOGS - The present invention is directed to Buprenorphine Analog compounds of the Formula (I), Formula (IA) or Formula (IB) shown below, wherein R | 02-27-2014 |
20140057932 | 1,3-Dioxanomorphides and 1,3-Dioxanocodides - The application is directed to compounds of Formula I | 02-27-2014 |
20140066470 | NOVEL FORMULATIONS OF WATER-INSOLUBLE CHEMICAL COMPOUNDS AND METHODS OF USING A FORMULATION OF COMPOUND FL118 FOR CANCER THERAPY - Provided are compositions, methods of making the compositions, and methods of using the compositions. The compositions can be provided as pharmaceutical preparations for use in disease treatment, such as cancer therapy. The compositions include novel pharmaceutical preparations which contain effective concentrations of a chemical compound. One compound used is 10H-1,3-Dioxolo[4,5-g]pyrano[3′,4′:6,7]indolizino[1,2-b]quinoline-8,11(7H,12H)-dione, 7-ethyl-7-hydroxy-, (S)-. The invention also provides methodologies for preparing pharmaceutical preparations for use in intravenous and oral pharmaceutical preparations that contain drug compounds that are difficult to dissolve in water. | 03-06-2014 |
20140073663 | METHOD OF PROVIDING SUSTAINED ANALGESIA WITH BUPRENORPHINE - A method of effectively treating pain in humans is achieved by administering buprenorphine in accordance with first order kinetics over an initial three-day dosing interval, such that a maximum plasma concentration from about 20 pg/ml to about 1052 pg/ml is attained, and thereafter maintaining the administration of buprenorphine for at least an additional two-day dosing interval in accordance with substantially zero order kinetics, such that the patients experience analgesia throughout the at least two-day additional dosing interval. | 03-13-2014 |
20140080853 | Compounds and Formulations Suitable for Radical Scavenging - The present invention relates to compositions and methods of using free radical scavengers with reduced | 03-20-2014 |
20140100240 | Natural product derivatives with antiprotozoal activity - The present invention provides new chemical compositions with desirable biological activity and toxicity profiles for the enhanced treatment of malaria. | 04-10-2014 |
20140100241 | DRUG DETOXIFICATION PROTOCOL USING MICRODOSING - This invention relates to use of an opioid receptor agonist in microdose quantities to reduce or eliminate the withdrawal symptoms associated with discontinuing drug use. The dosage of the agonist is reduced over an extended period of time. | 04-10-2014 |
20140107144 | POLYMORPH OF RIFAXIMIN AND PROCESS FOR THE PREPARATION THEREOF - The present invention relates to a new polymorph of Rifaximin, designated κ, and to a process for the preparation thereof. Under certain aspects, the invention also relates to pharmaceutical compositions comprising an effective amount of the polymorphic form κ of Rifaximin and a pharmaceutically acceptable carrier and its uses in the treatment of gastrointestinal conditions. | 04-17-2014 |
20140113924 | NOVEL CLASS OF NON-STIMULANT TREATMENT AND ADHD AND RELATED DISORDERS - Described is a method of administering nor-binaltorphimine (nor-BNI) or a nor-BNI analog to an individual having Attention Deficit/Hyperactivity Disorder (ADHD) to thereby reduce the effects of ADHD in the individual. | 04-24-2014 |
20140128419 | Rifaximin - 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. | 05-08-2014 |
20140135354 | TETRANDRINE PHARMACEUTICAL FORMULATIONS AND METHOD - Drug formulations, methods and their use in treatment of diseases using the free base formulations of tetrandrine family members, especially d-tetrandrine, combined with a pharmaceutical diluent or carrier. | 05-15-2014 |
20140142131 | LONG-ACTING INJECTABLE ANALGESIC FORMULATIONS FOR ANIMALS - Long acting injectable analgesic formulations and methods for providing long lasting pain relief in animals are disclosed. | 05-22-2014 |
20140155422 | New Process for the Synthesis of Rifaximin and a New Pseudo-Crystalline Form of Rifaximin Obtained Thereby - Process for the preparation of rifaximin, pseudo-crystalline rifaximin and a new pseudo-crystalline form of rifaximin with fewer impurities obtained thereby. | 06-05-2014 |
20140155423 | BERBAMINE DERIVATIVES - The invention provides novel berbamine derivatives, and compositions or pharmaceutical compositions thereof. These berbamine derivatives have shown higher potency in killing cancer/tumor cells comparing to berbamine, and can be used in cancer/tumor treatments. | 06-05-2014 |
20140163057 | Implantable Polymeric Device for Sustained Release of Buprenorphine - The present invention provides compositions, methods, and kits for treatment of opiate addiction and pain. The invention provides a biocompatible nonerodible polymeric device which releases buprenorphine continuously with generally linear release kinetics for extended periods of time. Buprenorphine is released through pores that open to the surface of the polymeric matrix in which it is encapsulated. The device may be administered subcutaneously to an individual in need of continuous treatment with buprenorphine. | 06-12-2014 |
20140163058 | BUPRENORPHINE ANALOGS - The present invention is directed to Buprenorphine Analog compounds of the Formula I, Formula II, Formula III, Formula IV, and Formula V, wherein R | 06-12-2014 |
20140171457 | Implantable Polymeric Device for Sustained Release of Buprenorphine - The present invention provides compositions, methods, and kits for treatment of opiate addiction and pain. The invention provides a biocompatible nonerodible polymeric device which releases buprenorphine continuously with generally linear release kinetics for extended periods of time. Buprenorphine is released through pores that open to the surface of the polymeric matrix in which it is encapsulated. The device may be administered subcutaneously to an individual in need of continuous treatment with buprenorphine. | 06-19-2014 |
20140179726 | GUT MICROFLORA AS BIOMARKERS FOR THE PROGNOSIS OF CIRRHOSIS AND BRAIN DYSFUNCTION - A systems biology approach is used to characterize and relate the intestinal (gut) microbiome of a host organism (e.g. a human) to physiological processes within the host. Information regarding the types and relative amounts of gut microflora is correlated with physiological processes indicative of e.g., a patient's risk of developing a disease or condition, likelihood of responding to a particular treatment, for adjusting treatment protocols, etc. The information is also used to identify novel suitable therapeutic targets and/or to develop and monitor the outcome of therapeutic treatments. An exemplary disease/condition is the development of hepatic encephalopathy (HE), particularly in patients with liver cirrhosis. | 06-26-2014 |
20140187571 | 7,8-Cyclicmorphinan Analogs - The application is directed to compounds of Formula I-A | 07-03-2014 |
20140221413 | PREOPERATIVE TREATMENT OF POST OPERATIVE PAIN - A method of treating postoperative pain in a patient undergoing a surgery is described. The method is based on preoperative administration of a buprenorphine-containing transdermal dosage form. The dosage form can be administered to the patient, for example, 1-4 days prior to surgery. Alternative embodiments of the invention include subsequent transdermal dosage forms to treat the postoperative pain. | 08-07-2014 |
20140221414 | SOLID DISPERSION OF RIFAXIMIN - A solid dispersion of rifaximin comprising rifaximin and pharmaceutically acceptable carrier. A pharmaceutical composition comprising the solid dispersion of rifaximin. | 08-07-2014 |
20140235662 | RIFAXIMIN POWDER, PROCESS FOR PREPARING THE SAME AND CONTROLLED RELEASE COMPOSITIONS CONTAINING SAID RIFAXIMIN USEFUL FOR OBTAINING A LONG-LASTING EFFECT - The present invention describes rifaximin powder and to a process for preparing the same. The invention relates also to a pharmaceutical composition in solid form comprising said rifaximin, pharmaceutically acceptable excipients and optionally other ingredients. The compositions according to the invention are suitable for oral administration and are characterized by producing a controlled release of rifaximin, whereby a long-lasting effect is obtained in a patient. | 08-21-2014 |
20140235663 | BUPRENORPHINE FOR THE TREATMENT OF ACUTE SUICIDALITY - Methods and compositions for treating acute suicidality by administration of buprenorphine are disclosed herein. An exemplary method is effected by administering to a subject determined as having acute suicidality a first therapeutically effective amount of buprenorphine, or a pharmaceutically acceptable salt thereof, whereby the administration is ceased once the subject is no longer determined as having acute suicidality. The first therapeutically effective amount is less than 0.2 mg per day. A higher therapeutically effective amount may optionally be administered if the subject is determined as not fully responsive to the first therapeutically effective amount. Unit dosage forms of buprenorphine, comprising less than 0.2 mg (e.g., 0.1 mg) buprenorphine are also disclosed. | 08-21-2014 |
20140275137 | TETRANDRINE FAMILY PHARMACEUTICAL FORMULATIONS AND METHOD - Drug formulations, methods and their use in treatment of diseases using formulations of pure di-acid salts of tetrandrine family members, especially d-tetrandrine di-hydrochloride, combined with a pharmaceutical diluent or carrier. | 09-18-2014 |
20140275138 | METHOD AND PRODUCTS FOR TREATING DIABETES - Treating diabetes by administering one or more members of the d-tetrandrine family, either alone or with other Type 2 diabetes drugs or dietary supplements which mediate diabetes. | 09-18-2014 |
20140275139 | MDR METHOD AND PRODUCTS FOR TREATING HIV/AIDS - Multidrug resistance reversers of the d-tetrandrine family are used concurrently with protease inhibitors to treat HIV/AIDS. | 09-18-2014 |
20140275140 | METHOD AND PRODUCTS FOR ENHANCING DRUG AND DIETARY SUPPLEMENT BIOAVAILABILITY - Enhancing the bioavailability of a drug or dietary supplement by administering it concurrently with one or more members of the d-tetrandrine family. | 09-18-2014 |
20140303199 | INHIBITORS OF RGS PROTEINS - G-protein coupled receptors are a diverse group that are the target of over 50% of marketed drugs. Activation of these receptors results in the exchange of bound GDP for GTP in the Gα subunit of the heterotrimeric G-protein. The Gα subunit dissociates from the β/γ subunits and both proceed to affect downstream signaling targets. The signal terminates by the hydrolysis of GTP to GDP and is regulated by Regulators of G-protein Signaling (RGS) proteins that act as GTPase Activating Proteins (GAPs). This makes RGS proteins potentially desirable targets for “tuning” the effects of current therapies as well as developing novel pharmacotherapies. The present invention provides a convenient assay for identifying modulators of RGS proteins that can be adapted for high throughput screening utilizing the colorimetric dye, malachite green, to detect free phosphate in the presence of a test compound. | 10-09-2014 |
20140329843 | HIGH DOSE BUPRENORPHINE COMPOSITIONS AND USE AS ANALGESIC - The present disclosure relates to a method of providing prolonged analgesia to a mammal in need thereof. Specifically, the current disclosure is directed to a method of treating pain in a mammal for a prolonged period of time using a single high dose of a buprenorphine formulation. | 11-06-2014 |
20140329844 | METHOD OF RESTORING THE INCRETIN EFFECT - The present invention relates to methods of treating metabolic syndrome, Type 2 diabetes mellitus, atherogenic dyslipidemia and/or obesity. The present invention also relates to methods of restoring the incretin effect, to restoring physiologic control of glucagon levels, to restoring first-phase insulin secretion, and to restoring the physiologic glucose-dependent insulin secretion. The methods of the present invention comprise administration of a selective κ-receptor antagonist, such as guanidinylated naltrindole (GNTI), or pharmaceutically acceptable derivatives thereof to a subject in need thereof. | 11-06-2014 |
20140364448 | QUARTERNIZED BUPRENORPHINE ANALOGS - The present invention is directed to Buprenorphine Analog compounds of the Formula (I), Formula (IA) or Formula (IB) shown below, wherein R | 12-11-2014 |
20140371254 | NOVEL TREATMENT OF GEFITINIB-RESISTANT NON-SMALL-CELL LUNG CANCER - The present invention discloses a method of preventing and treating Gefitinib-resistant non-small-cell lung cancer, comprising administering an effective amount of an alkaloid. A pharmaceutical composition comprising an alkaloid admixed with a pharmaceutical carrier for treating Gefitinib-resistant non-small-cell lung cancer is also disclosed therein. | 12-18-2014 |
20140378495 | RIFAXIMIN DERIVATIVE AND USES THEREOF - 25-desacetyl rifaximin or a pharmaceutically acceptable salt thereof is provided. Methods of treatment of bowl related disorders using isolated and/or purified 25-desacetyl rifaximin or a pharmaceutically acceptable salt thereof are also provided. | 12-25-2014 |
20150025099 | USE OF 7-ALKOXY FANGCHINOLINE COMPOUNDS IN PREVENTING, ALLEVIATING AND/OR TREATING DEPRESSION - The present invention provides a method of preventing, alleviating and/or treating depression, comprising the step of administering to a subject in need thereof a therapeutically effective amount of a 7-alkoxy fangchinoline compound or a pharmaceutically acceptable derivative thereof. | 01-22-2015 |
20150045382 | RIFAXIMIN COMPLEXES - There is provided a complex comprising rifaximin and a complexing agent, wherein the complexing agent is a polyvinyl pyrrolidone (PVP) or a cyclodextrin. There is also provided a process for preparing the complex, a pharmaceutical composition including the complex and therapeutic uses of the complex. | 02-12-2015 |
20150065535 | METHOD OF RESTORING THE INCRETIN EFFECT - The present invention relates to methods of treating metabolic syndrome Type 2 diabetes mellitus atherogenic dyslipidemia and/or obesity. The present invention also relates to methods of restoring the incretin effect, to restoring physiologic control of glucagon levels, to restoring first-phase insulin secretion, and to restoring the physiologic glucose-dependent insulin secretion. The methods of the present invention comprise administration of a selective κ-receptor antagonist, such as guanidinylated naltrindole (GNTI), or pharmaceutically acceptable derivatives thereof to a subject in need thereof. | 03-05-2015 |
20150073007 | POLYMORPHOUS FORMS OF RIFAXIMIN, PROCESSES FOR THEIR PRODUCTION AND USE THEREOF IN THE MEDICINAL PREPARATIONS - Crystalline polymorphous forms of the rifaximin (INN) antibiotic named rifaximin δ and rifaximin ε useful in the production of medicinal preparations 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 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. | 03-12-2015 |
20150080421 | PHARMACEUTICAL FORMULATIONS CONTAINING RIFAXIMIN, PROCESSES FOR THEIR OBTAINMENT AND METHOD OF TREATING INTESTINAL DISEASE - Disclosed herein are methods of treating a patient having an intestinal disorder, the methods comprising: administering to a patient in need thereof a pharmaceutical composition comprising a hydrate or solvate form of rifaximin in polymorphic form β, alone or in a mixture with other crystalline, hydrate, solvate or amorphous forms of rifaximin, in gastroresistant microgranules, wherein the rifaximin is administered at a dose of at least 800 mg per day for a period of at least 7 days. | 03-19-2015 |
20150094324 | HETEROCYCLE-FUSED MORPHINANS, USE THEREOF AND PREPARATION THEREOF - The present disclosure is concerned with a process for the preparation of the above disclosed compounds, pharmaceutically acceptable salts thereof, deuterated forms thereof, isomers thereof, solvates thereof, or mixtures thereof which comprises subjecting a 17-substituted-3,14-dihydroxypyridomorphinan to dialkylation at the phenolic hydroxyl at the 3-position and the tertiary alcohol at the 14-position followed by selective dealkylation of the phenolic ether function. | 04-02-2015 |
20150133482 | FORMULATIONS OF RIFAXIMIN AND USES THEREOF - The present invention relates to new rifaximin forms comprising solid dispersions of rifaximin, methods of making same and to their use in medicinal preparations and therapeutic methods. | 05-14-2015 |
20150133483 | Dihydroetorphines and Their Preparation - The present invention provides a process for the preparation of a compound of formula (VI), or a salt or derivative thereof, | 05-14-2015 |
20150141450 | METHODS OF TREATING TRAVELER'S DIARRHEA AND HEPATIC ENCEPHALOPATHY - Treatment of traveler's diarrhea using in subjects having hepatic encephalopathy using gastrointestinal specific antibiotics is disclosed. One example of a gastrointestinal specific antibiotic is rifaximin. | 05-21-2015 |
20150307504 | BUPRENORPHINE DIMER AND ITS USE IN TREATMENT OF GASTROINTESTINAL DISORDERS - The present invention provides a buprenorphine dimer compound, wherein the two buprenorphine portions are linked via an ethylene spacer, wherein the spacer is bonded to the two opioid molecules via an ether bond. Pharmaceutical compositions comprising such a buprenorphine dimer drug are also disclosed, and the use of such compounds in the treatment of gastrointestinal hyperalgesia generally and in particular diarrhea-predominant irritable bowel syndrome. | 10-29-2015 |
20150313848 | PHARMACEUTICAL COMPOSITIONS OF RIFAXIMIN - The present invention relates to stable pharmaceutical compositions comprising rifaximin and processes for their pre-paration. | 11-05-2015 |
20150342934 | RIFAXIMIN DERIVATIVE AND USES THEREOF - 25-desacetyl rifaximin or a pharmaceutically acceptable salt thereof is provided. Methods of treatment of bowl related disorders using isolated and/or purified 25-desacetyl rifaximin or a pharmaceutically acceptable salt thereof are also provided. | 12-03-2015 |
20160000765 | METHODS FOR TREATING BOWEL DISEASES - The present invention provides new methods of treating bowel disease (BD) by increasing a durability of response; treating BD in males; treating BD in adolescent subjects; treating bloating due to BD in males; and methods of maintaining remission of BD. | 01-07-2016 |
20160009727 | SANGUINARINE ANALOG PP2C INHIBITORS FOR CANCER TREATMENT | 01-14-2016 |
20160068538 | PROCESS FOR PREPARING 7BETA-SUBSTITUTED 6ALPHA,14ALPHA-ETHENOMORPHINANS AND 7BETA-SUBSTITUTED 6ALPHA,14ALPHA-ETHANOMORPHINANS - The application is directed to a process for increasing the proportion of 7β-epimer in an 7α/7β-epimer mixture of a 7-substituted 6α,14α-ethenomorphinan or a 7-substituted 6α,14α-ethanomorphinan, and specifically of compounds of Formula (I), wherein G, R | 03-10-2016 |
20160106736 | DIHYDROETORPHINE FOR THE PROVISION OF PAIN RELIEF AND ANAESTHESIA - The present invention provides a method of providing pain relief in a human subject in need thereof comprising administering (R)-dihydroetorphine to said subject, wherein said (R)-dihydroetorphine is administered in a dose of at least 0.01 μg/kg, preferably at least 0.05 μg/kg, and the level of respiratory depression in said subject is 65 or less % relative to the baseline level pre-administration of (R)-dihydroetorphine. | 04-21-2016 |
20160115174 | DIHYDROETORPHINES AND THEIR PREPARATION - The present invention provides a process for the preparation of a compound of formula (VI), or a salt or derivative thereof, | 04-28-2016 |
20160128934 | INJECTABLE FLOWABLE COMPOSITION COMPRISING BUPRENORPHINE - The present invention is directed to a buprenorphine sustained release delivery system capable of delivering buprenorphine, a metabolite, or a prodrug thereof for a duration of about 14 days to about 3 months. The buprenorphine sustained release delivery system includes a flowable composition and a solid implant for the sustained release of buprenorphine, a metabolite, or a prodrug thereof. The implant is produced from the flowable composition. The buprenorphine sustained release delivery system provides in situ 1-month and 3-month release profiles characterized by an exceptionally high bioavailability and minimal risk of permanent tissue damage and typically no risk of muscle necrosis. | 05-12-2016 |
20160128990 | METHODS OF USING RIFAXIMIN IN POSITION EMISSION TOMOGRAPHY (PET) SCANS - The present invention provides new methods and kits for the reduction, prevention or inhibition of substrate uptake by non-metastatic, metabolically active cells in a subject who will undergo a position emission tomography (PET) scan. | 05-12-2016 |
20160128997 | SUSTAINED-RELEASE BUPRENORPHINE FORMULATIONS - The disclosure is directed to sustained-release buprenorphine formulations that provide long-term, therapeutic levels of buprenorphine for the treatment of pain and the maintenance treatment of opioid use disorders, such as opioid dependence. | 05-12-2016 |
20160136141 | RIFAXIMIN READY-TO-USE SUSPENSION - A stable, taste-masked, ready-to-use suspension comprising rifaximin dispersed in a suspension base and one or more pharmaceutically acceptable additive(s). Also provided is a process for preparing a stable, taste-masked, ready-to-use suspension of rifaximin comprising the steps of mixing rifaximin with the suspension base and further sizing the particles of rifaximin by milling the suspension to obtain a homogenously dispersed rifaximin suspension. | 05-19-2016 |
20160136151 | Orvinol and Thevinol Derivatives Useful in the Treatment of Anxiety or a Compulsive Disorder - The invention provides a method of treating anxiety or a compulsive disorder in a subject comprising administering to the subject a compound having formula 2: | 05-19-2016 |
20160144528 | PATCH DEVICES, METHODS AND APPARATUS FOR FORMING, AND TESTING PHARMACEUTICAL AGENT DELIVERY PATCH DEVICES - A method for manufacturing a plurality of pharmaceutical agent delivery patch devices includes: providing a supply web including an active layer containing a pharmaceutically active agent; and cutting the supply web to form cut lines through the active layer. The cut lines define in the active layer: a first active layer patch having a first peripheral edge formed by the cutting step; and a second active layer patch having a second peripheral edge formed by the cutting step. The first and second peripheral edges each include a corner portion. At least a first segment of the first peripheral edge and an opposing second segment of the second peripheral edge are formed by a shared one of the cut lines. | 05-26-2016 |
20160151360 | Pharmaceutical Formulation Containing Gelling Agent | 06-02-2016 |
20160374999 | RIFAXIMIN - 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. | 12-29-2016 |