Entries |
Document | Title | Date |
20080207676 | Crystalline forms of an 8-Azabicyclo(3.2.1)octane compound - The invention provides a crystalline sulfate salt of 3-endo-(8-{2-[cyclohexylmethyl-((S)-2,3-dihydroxy-propionyl)amino]ethyl}-8-aza-bicyclo[3.2.1]oct-3-yl)benzamide or a solvate thereof. The invention also provides pharmaceutical compositions comprising such crystalline salt forms, methods of using such crystalline salt forms to treat diseases associated with mu opioid receptor activity, and processes useful for preparing such crystalline salt forms. | 08-28-2008 |
20080242693 | Pharmaceutical Compositions and Methods for Relieving Pain and Treating Central Nervous System Disorders - Patients susceptible to or suffering from disorders, such as central nervous system disorders, which are characterized by an alteration in normal neurotransmitter release, such as dopamine release (e.g., Parkinsonism, Parkinson's Disease, Tourette's Syndrome, attention deficient disorder, or schizophrenia), are treated by administering a compound of Formulas 1 or 2, as described herein. The compounds of Formulas 1 and 2 are also useful for treating pain, and treating drug addiction, nicotine addiction, and/or obesity. The compounds can exist as individual stereoisomers, racemic mixtures, diastereomers and the like. | 10-02-2008 |
20080287485 | NOVEL INDOLIZINE DERIVATIVES, METHOD FOR PREPARING SAME, AND THERAPEUTIC COMPOSITIONS COMPRISING SAME - The present invention is directed to compounds of formula (I): | 11-20-2008 |
20080319002 | Xanthine Derivatives a Useful as Muscarinic Receptor Antagonists - This present invention generally relates to xanthine derivatives as muscarinic receptor antagonists which are useful, among other uses, for the treatment of various diseases of the respiratory, urinary and gastrointestinal systems mediated through muscarinic receptors. The invention also relates to the process for the preparation of disclosed compounds, pharmaceutical compositions containing the disclosed compounds, and the methods for treating diseases mediated through muscarinic receptors. | 12-25-2008 |
20080319003 | CYCLIC AMINE COMPOUND AND PEST CONTROL AGENT - A chemical compound represented by the formula [I]: | 12-25-2008 |
20090012114 | Cyclohepta[B]Pyridine-3-Carbonylguanidine Derivative and Pharmaceutical Product Containing Same - The present invention relates to a medicine, particularly a medicine comprising a novel cyclohepta[b]pyridine-3-carbonylguanidine derivative having an inhibitory effect on an Na | 01-08-2009 |
20090030033 | Novel Compounds 894 - The invention relates to 2-aza-bicyclo[2.2.2]octane compounds and uses thereof. Particularly the invention relates to such compounds and their uses as pharmaceuticals in treating pyshoses such as schizophrenia and other diseases, disorders, or conditions. | 01-29-2009 |
20090030034 | USE OF FGF INHIBITING SUBSTITUTED 1,2,3 INDOLIZINE DERIVATIVES IN THE PREPARATION OF MEDICAMENTS WHICH CAN BE USED TO TREAT DISEASES LINKED TO PATHOLOGICAL CHOROIDAL ANGIOGENESIS - The present invention thus relates to the use of 1,2,3-substituted indolizine derivatives in the preparation of medicaments of use in the treatment of diseases related to pathological choroidal angiogenesis, which derivatives correspond to the following general formula (I): | 01-29-2009 |
20090048284 | THERAPEUTIC COMPOUNDS - This invention to antagonists that inhibit transporters and receptors. The invention also relates to partial inhibitors of transporters and receptors that allow partial transport or partial binding of a compound to the transporter or receptor. The invention also relates to compounds that differentially prevent transport or binding through a transporter or to a receptor. The invention also relates to the use of these compounds for treating certain diseases and disorders. | 02-19-2009 |
20090076061 | MUSCARINIC ACETYCHOLINE RECEPTOR ANTAGONISTS - Muscarinic Acetylcholine Receptor Antagonists and methods of using them are provided. | 03-19-2009 |
20090076062 | Organic Compounds - Disclosed are δ-amino-γ-hydroxy-ω-aryl-alkanoic acid amide compounds of formula (I) | 03-19-2009 |
20090076063 | Carboxamide compound and use of the same - A carboxamide compound represented by the formula (I): | 03-19-2009 |
20090076064 | Compounds - Disclosed are compounds of Formula (I) wherein G, R | 03-19-2009 |
20090082389 | PESTICIDAL SUBSTITUTED PIPERIDINES - The invention relates to the use of piperidine derivatives encompassed from the general formula (I) for the control of pests, including arthropods and helminths, and a method for the control of pests. | 03-26-2009 |
20090105296 | INHIBITORS OF C-FMS KINASE - The invention is directed to compounds of Formula I: | 04-23-2009 |
20090137623 | MUSCARINIC RECEPTOR ANTAGONISTS - The present invention relates to muscarinic receptor modulators, specifically, 7-oxo-2-azabicyclo[2.2.1]heptanes of formula (I) which are useful for the treatment of various diseases and conditions, for example, Alzheimer's disease, glaucoma, psychosis, particularly schizophrenia or schizophreniform conditions, mania, pain, bipolar disorder, depression, sleeping disorders, epilepsy, gastrointestinal motility disorders, urinary incontinence, and cognition enhancement. | 05-28-2009 |
20090163534 | Indolizine Derivatives - Compounds of formula (I) are ligands of the CRTH2 receptor and are useful in the treatment of respiratory disease: Formula (I) wherein R | 06-25-2009 |
20090176823 | Secondary Amines as Renin Inhibitors - The invention relates to novel secondary amine derivatives of formula (I) and the use thereof as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as inhibitors of renin. | 07-09-2009 |
20090186916 | AMINOINDANE DERIVATIVE OR SALT THEREOF - Provided is a compound that is an NMDA receptor antagonist having a broader safety margin, and is useful as an agent for treating or preventing Alzheimer's disease, cerebrovascular dementia, Parkinson's disease, ischemic apoplexy, or pain. | 07-23-2009 |
20090247568 | AMINOPIPERIDINYL DERIVATIVES AND USES THEREOF - This application discloses aminopiperidinyl compounds of generic Formulae I-II: | 10-01-2009 |
20090258896 | COMPOSITION COMPRISING AT LEAST ONE HIGHER ALIPHATIC ALCOHOL AND AN EXTRACT OF GRIFFONIA SIMPLICIFOLIA - Novel compositions comprising a combination of at least one higher primary aliphatic alcohol preferably selected from those having 18 to 40 carbon atoms or mixtures thereof, at least one source of 5-hydroxytryptophan (5-HTP) optionally additionally comprising a source of caffeine and/or catechin-polyphenol and/or epigallocatechin gallate as active agents, either alone or in combination with other active agent(s), optionally with one or more excipient(s) are provided. Particularly, the invention relates to compositions and process for preparation of such compositions and method of use thereof for the management of obesity and associated disorders. | 10-15-2009 |
20090281135 | 3-AZABICYCLO [4. 1. 0] HEPTANE DERIVATIVES FOR THE TREATMENT OF DEPRESSION - The present invention relates to novel compounds of formula (I) or pharmaceutically acceptable salts, solvates or prodrugs thereof: | 11-12-2009 |
20090312364 | NOVEL CHROMEN-2-ONE DERIVATIVES AND THEIR USE AS MONOAMINE NEUROTRANSMITTER RE-UPTAKE INHIBITORS - This invention relates to novel chromen-2-one derivatives useful as monoamine neurotransmitter re-uptake inhibitors. | 12-17-2009 |
20090325999 | PERSONALIZED PHARMACEUTICAL KITS, PACKAGING AND COMPOSITIONS FOR THE TREATMENT OF ALLERGIC CONDITIONS - This invention relates to personalized pharmaceutical kits, packaging, compositions, and methods for treatment of a mammal, comprising at least one antihistamine for treating an allergic disease or condition in a mammal, in combination with at least one wakefulness promoting agent for preventing sedative effects during day time use, while promoting the antihistamine and sedating effect during evening use. | 12-31-2009 |
20090326000 | RESVERATROL FORMULATIONS AND METHODS OF USE - A method is provided for preventing or treating obesity and for reducing the percentage body fat content of an individual. The method involves administration, preferably topical administration, of an active agent selected from the group consisting of resveratrol, pharmacologically acceptable salts, esters, amides, and analogs thereof, and combinations of any of the foregoing. Topical formulations for use in conjunction with the method for reducing the percentage body fat content of an individual are provided as well. | 12-31-2009 |
20100010034 | CRTH2 ANTAGONISTS - The following compounds are CRTH2 antagonists, useful in treatment of respiratory disease: [3-(2,4-dichlorophenylsulfanyl)-6-fluoro-2-methylindolizin-1-yl]acetic acid, [6-fluoro-3-(2-fluoro-4-methanesulfonylphenylsulfanyl)-2-methylindolizin-1-yl]acetic acid, [6-fluoro-3-(4-methanesulfonyl-2-trifluoromethylphenylsulfanyl)-2-methylindolizin-1-yl]acetic acid, (R)-2-[6-fluoro-3-(4-methanesulfonylphenylsulfanyl)-2-methylindolizin-1-yl]propionic acid, [3-(4-ethanesulfonylphenylsulfanyl)-6-fluoro-2-methylindolizin-1-yl]acetic acid, (S)-2-[6-fluoro-3-(4-methanesulfonylphenylsulfanyl)-2-methylindolizin-1-yl]propionic acid, ethanesulfonylaminobenzenesulfonyl)-6-fluoro-2-methyiindolizin-1-yl]acetic acid, [7-chloro-6-fluoro-3-(4-methanesulfonylphenylsulfanyl)-2-methylindolizin-1-yl]acetic acid, [3-(2-chloro-4-methanesulfonylphenylsulfanyl)-7-cyano-2-methylindolizin-1-yl]acetic acid, [6-cyano-3-(4-methanesulfonylbenzyl)-2-methylindolizin-1-yl]acetic acid, [3-(4-chlorobenzyl)-7-cyano-2-methylindolizin-1-yl]acetic acid, [6-cyano-3-(6-fluoroquinolin-2-yl-methyl)-2-methylindolizin-1-yl]acetic acid, [6-fluoro-3-(4-methoxyphenylsulfanyl)-2-methylindolizin-1-yl]acetic acid, [7-chloro-6-fluoro-3-(4-methoxyphenylsulfanyl)-2-methylindolizin-1-yl]acetic acid, [3-(4-bromophenylsulfanyl)-6-fluoro-2-methylindolizin-1-yl]acetic acid, and [3-(4-cyclopropylsulfamoylphenylsulfanyl)-6-fluoro-2-methylindolizin-1-yl]acetic acid. | 01-14-2010 |
20100016349 | PSEUDOAZULENYL NITRONES - Disclosed herein are pseudoazulenyl nitrone compounds and methods of using these compounds to trap free radicals and to treat, prevent, or ameliorate various diseases associated with free radicals. | 01-21-2010 |
20100035914 | AZABICYCLIC COMPOUNDS AS INHIBITORS OF MONOAMINES REUPTAKE - The present invention relates to novel compounds of formula (I)′, and pharmaceutically acceptable salts, prodrugs or solvates thereof: | 02-11-2010 |
20100035915 | INDOLIZINE DERIVATIVES AND THE USE THEREOF AS ANTIDIABETICS - Novel compounds of the formula (I), in which X, Y, R, R | 02-11-2010 |
20100035916 | AZABICYCLOALKANE DERIVATIVES, PREPARATION THEREOF AND USE THEREOF IN THERAPY - The invention relates to compounds of the general formula (I): | 02-11-2010 |
20100056559 | PROPELLANT-FREE AEROSOL FORMULATION FOR INHALATION - The present invention relates to propellant-free aerosol formulations for inhalation containing ipratropium bromide and salbutamol. | 03-04-2010 |
20100056560 | USE FOR TREATING OBESITY AND DIABETES - Disclosed herein is the use of a composition, containing isoflavone-containing soybean extract, L-carnitine, caffeine and arginine as active ingredients, for the treatment of obesity and diabetes. The disclosed composition contains isoflavone-containing soybean extract, carnitine, caffeine and arginine in the form of a mixture, and thus shows not only the effect of promoting lipolysis and fat burning, but also anti-obesity and anti-diabetic effects by increasing the expressions of adiponectin and Glut4 genes to restore insulin sensitivity. | 03-04-2010 |
20100056561 | HYDROCHLORIDE SALT OF AN AZABICYCLO[3.2.1]OCTANE DERIVATIVE - The invention relates to a hydrochloride salt of (1R,2R,3S,5S)-3-(3,4-dichlorophenyl)-2-[(methyloxy)methyl]-8-azabicyclo[3.2.1]octane, uses of the salt as a medicament in the treatment inter alia of disorders of the central nervous system and pharmaceutical compositions and dosage forms comprising the salt. | 03-04-2010 |
20100056562 | CHROMEN-2-ONE DERIVATIVES AND THEIR USE AS MONOAMINE NEUROTRANSMITTER RE-UPTAKE INHIBITORS - This invention relates to novel chromen-2-one derivatives useful as monoamine neurotransmitter re-uptake inhibitors. | 03-04-2010 |
20100069429 | Tea Polyphenol Composition and Method for Producing the Same - The objective of the present invention is to provide a tea polyphenol composition that has reduced bitterness and astringency while containing catechins with high purity. The present invention provides a tea polyphenol composition, (A) comprising 85% by weight to 95% by weight of catechins, (B) wherein the catechins contains epigallocatechin gallate and gallocatechin gallate at a ratio of 65% by weight to 80% by weight and (C) wherein the ratio given by (epigallocatechin gallate+gallocatechin gallate)/(epicatechin+catechin+epigallocatechin+gallocatechin+epicatechin gallate+catechin gallate) is from 2 to 4. | 03-18-2010 |
20100093783 | Composition for treatment of common cold - New stable compositions comprising the combination of a topically active vasoconstrictor and a topically active anticholinergic drug are disclosed. Preferably, the composition comprises ipratropium or a salt thereof in combination with xylometazoline hydrochloride and a salt thereof. Upon topically administering such compositions to a nasal mucosa in individuals suffering from the common cold the symptoms of rhinorrhea are significantly reduced. | 04-15-2010 |
20100152226 | SUSTAINED RELEASE IMPLANT FOR GRANISETRON - The main goals of the invention are to develop the long-term release of Granisetron injection implant composition with biodegradable polymer and to develop relative processing. Granisetron is mixed with different biodegradable polymers, and then hot melt extrusion technique with different diameter, temperature, rate of extrusion and holding time is applied to make implant. In vitro dissolution of the Granisetron injection implant composition shows the component continued release of the drug for over 7 days. | 06-17-2010 |
20100152227 | Methods for Enhancing Stability of Polyorthoesters and Their Formulations - Disclosed herein are methods of enhancing the stability of a sustained pharmaceutical composition comprising an active agent and a polymer and methods of preparing such pharmaceutical compositions with enhanced stability. | 06-17-2010 |
20100152228 | PHARMACEUTICAL COMPOSITIONS AND METHODS FOR RELIEVING PAIN AND TREATING CENTRAL NERVOUS SYSTEM DISORDERS - Patients susceptible to or suffering from disorders, such as central nervous system disorders, which are characterized by an alteration in normal neurotransmitter release, such as dopamine release (e.g., Parkinsonism, Parkinson's Disease, Tourette's Syndrome, attention deficient disorder, or schizophrenia), are treated by administering a compound of Formulas 1 or 2, as described herein. The compounds of Formulas 1 and 2 are also useful for treating pain, and treating drug addiction, nicotine addiction, and/or obesity. The compounds can exist as individual stereoisomers, racemic mixtures, diastereomers and the like. | 06-17-2010 |
20100179183 | PHARMACEUTICAL COMPOSITIONS AND METHODS FOR RELIEVING PAIN AND TREATING CENTRAL NERVOUS SYSTEM DISORDERS - Patients susceptible to or suffering from disorders, such as central nervous system disorders, which are characterized by an alteration in normal neurotransmitter release, such as dopamine release (e.g., Parkinsonism, Parkinson's Disease, Tourette's Syndrome, attention deficient disorder, or schizophrenia), are treated by administering a compound of Formulas 1 or 2, as described herein. The compounds of Formulas 1 and 2 are also useful for treating pain, and treating drug addiction, nicotine addiction, and/or obesity. The compounds can exist as individual stereoisomers, racemic mixtures, diastereomers and the like. | 07-15-2010 |
20100204264 | POLYMORPHIC FORM OF GRANISETRON BASE, METHODS FOR OBTAINING IT AND FORMULATION CONTAINING IT - Relates to a new polymorphic form of Granisetron base, Form I, to methods for obtaining thereof, to the method for obtaining Granisetron.HCl and its use for preparing pharmaceutical formulations. The Form I is characterized by the X-ray powder diffractogram shown in FIG. | 08-12-2010 |
20110028509 | Sulfonamides - The invention relates to compounds of formula I | 02-03-2011 |
20110077264 | DERIVATIVES OF 5-PYRIDINYL-1-AZABICYCLO[3.2.1]OCTANE, PREPARATION METHOD THEREOF AND USE OF SAME IN THERAPEUTICS - The invention relates to compounds having general formula (I), wherein R is as defined herein. | 03-31-2011 |
20110130418 | SUBSTITUTED PHENYLENEDIAMINES AS INHIBITORS OF THE INTERACTION BETWEEN MDM2 AND P53 - The present invention provides compounds of formula (I), their use as an inhibitor of a p53-MDM2 interaction as well as pharmaceutical compositions comprising said compounds of formula (I). | 06-02-2011 |
20110136854 | NOVEL 9-AZA-BICYCLO[3.3.1]NON-3-YLOXY CHROMEN-2-ONE DERIVATIVES AND THEIR USE AS MONOAMINE NEUROTRANSMITTER RE-UPTAKE INHIBITORS - This invention relates to novel 9-aza-bicyclo[3.3.1]non-3-yloxy chromen-2-one derivatives useful as monoamine neurotransmitter re-uptake inhibitors. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention. | 06-09-2011 |
20110172264 | NICOTINIC ACETYLCHOLINE RECEPTOR MODULATORS - Provided herein are novel and selective high affinity α3β4 nicotinic acetylcholine receptor ligands and pharmaceutical compositions thereof. In other embodiments, provided herein are methods of treatment, prevention, or amelioration of a variety of medical disorders such as, for example, drug addiction or pain using the compounds and compositions disclosed herein. In still other embodiments, provided herein are methods for modulating a nicotinic acetylcholine receptor (nAChR). In still other embodiments, provided herein are methods of selectively antagonizing receptors such as, for example, the α3β4 nicotinic acetylcholine receptor using the compounds and compositions disclosed herein. | 07-14-2011 |
20110178119 | Bridged N-Bicyclic Sulfonamido Inhibitors of Gamma Secretase - The invention provides N-bicyclic sulfonamido compounds of Formula (I) wherein A is as described in the specification and R | 07-21-2011 |
20110184011 | Compounds - The present invention relates to new therapeutic and prophylactic applications of known compounds of general formula (Ia), novel compounds of formula (Ia) | 07-28-2011 |
20110251233 | FORMULATION FOR THE BUCCAL TRANSMUCOSAL ADMINISTRATION OF SETRONS - The invention provides a formulation for transmucosal administration of at least one active ingredient from the setron family, the formulation comprising said active ingredient in base form and/or in salt form, a hydroalcoholic solution titrating at least 30° alcohol, and optionally a pH correcting agent, said active principle being present in the state of stable and complete dissolution in the hydroalcoholic solution. The invention also provides a method of preparing this formulation and its use for the treatment and prevention of major nausea and/or vomiting syndromes, and also for the treatment and prevention of digestive spasms. | 10-13-2011 |
20110288115 | TREATMENT OF VAGALLY-MEDIATED SPECTRUM DISORDERS - The present invention provides a method of treatment of a vagally-mediated spectrum disorder, comprising administering an effective amount of a 5-HT | 11-24-2011 |
20110294846 | INDOLE DERIVATIVES AS ANTICANCER AGENTS - The present invention provides compounds of formula (I), their use for the treatment of cancer as well as pharmaceutical compositions comprising said compounds of formula (I). | 12-01-2011 |
20110294847 | Novel Polymorphs Of Azabicyclohexane - The invention provides polymorphic crystalline forms of acid addition salts of (+)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane designated as polymorph form A, polymorph form B and polymorph form C, where polymorph form A is more thermodynamically stable than the other forms, methods for preparing and using such polymorph forms and pharmaceutical compositions containing such polymorph forms. | 12-01-2011 |
20110306633 | SELECTIVE M4 RECEPTOR ANTAGONIST AND ITS MEDICAL USE - The present invention provides a selective M4 receptor antagonist, levorotatory demethylated phencynonate or its nontoxic pharmaceutically acceptable salt, a pharmaceutical composition comprising this compound, and a use thereof in the manufacture of a medicament for the treatment of motion dysfunction, such as, tremor, rigor and the like caused by Parkinson's disease (PD). The structure, of the compound is shown in Formula IIa: | 12-15-2011 |
20120010235 | N-SUBSTITUTED PYRROLIDINES - Compounds of formula | 01-12-2012 |
20120041020 | Methods of Treatment Utilizing Semi-Solid Pharmaceutical Compositions - A semi-solid delivery vehicle contains a polyorthoester and an excipient, and a semi-solid pharmaceutical composition contains an active agent and the delivery vehicle. The pharmaceutical composition may be a topical, syringable, or injectable formulation; and is suitable for local delivery of the active agent. Methods of treatment are also disclosed. | 02-16-2012 |
20120041021 | Process for Preparing a Semi-Solid Delivery Vehicle and Pharmaceutical Compositions - A semi-solid delivery vehicle contains a polyorthoester and an excipient, and a semi-solid pharmaceutical composition contains an active agent and the delivery vehicle. The pharmaceutical composition may be a topical, syringable, or injectable formulation; and is suitable for local delivery of the active agent. Methods of treatment are also disclosed. | 02-16-2012 |
20120095033 | Selective Glycosidase Inhibitors and Uses Thereof - The invention provides compounds of Formula (I) for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc. | 04-19-2012 |
20120129883 | BENZENESULFONYL OR SULFONAMIDE COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO THE MODULATION OFTHE SEROTONIN 5-HT6 RECEPTOR - The present invention relates to benzenesulfonyl or sulfonamide compounds of formulae IA and IB | 05-24-2012 |
20120245196 | 1-SUBSTITUTED 2-AZABICYCLO [3.1.1] HEPTYL DERIVATIVES USEFUL AS NICOTINIC ACETYLCHOLINE RECEPTOR MODULATORS FOR TREATING NEUROLOGIC DISORDERS - This invention provides 2-azabicyclo[3.1.1]heptyl derivatives, and methods for producing them, which are useful therapeutic agents for preventing or treating central nervous system disorders and disease mediated by a Nicotinic Acetylcholine Receptor such as, but not limited to, Alzheimer's disease, Parkinson's disease, schizophrenia, epilepsy, dementia, pain and nicotine addiction. | 09-27-2012 |
20130072518 | BICYCLIC COMPOUNDS AS alpha4 beta2 NICOTINIC ACETYLCHOLINE RECEPTOR LIGANDS - The present invention relates to novel bicyclic compounds of the formula (I), and their derivatives, prodrugs, tautomers, stereoisomers, polymorphs, solvates, hydrates, metabolites, N-oxides, pharmaceutically acceptable salts and compositions containing them. The present invention also relates to a process for the preparation of above said novel compounds, and their derivatives, prodrugs, tautomers, stereoisomers, polymorphs, solvates, hydrates, metabolites, N-oxides, pharmaceutically acceptable salts and compositions containing them. These compounds are useful in the treatment and prevention of various disorders that are related to α | 03-21-2013 |
20130072519 | 2-PHENYL BENZOYLAMIDES - Compounds of Formula I that inhibit microsomal triglyceride transfer protein (MTP) and/or apolipoprotein B (Apo B) secretion and their uses in the treatment of diseases linked thereto in animals are described herein. | 03-21-2013 |
20130150399 | INHIBITORS OF THE UNFOLDED PROTEIN RESPONSE AND METHODS FOR THEIR USE - Compounds that are inhibitors of the unfolded protein response and endonuclease IRE1 are provided, together with compositions comprising such compounds, and methods for their use in the treatment of various disorders, such as cancer, autoimmune disorders, and diabetes. Also provided are packaged pharmaceuticals comprising these compositions. The compositions may be administered in combination with another therapeutic agent. | 06-13-2013 |
20140051719 | Selective Glycosidase Inhibitors and Uses Thereof - The invention provides compounds of Formula (I) for selectively inhibiting glycosidases, prodrugs of the compounds, and pharmaceutical compositions including the compounds or prodrugs of the compounds. The invention also provides methods of treating diseases and disorders related to deficiency or overexpression of O-GlcNAcase, accumulation or deficiency of O-GlcNAc. | 02-20-2014 |
20140080861 | HETEROCYCLIC COMPOUNDS IWTH AFFINITY TO MUSCARINIC RECEPTORS - The present invention relates to heterocyclic compounds of formula (I) having affinity to mascarinic receptors, a pharmaceutical composition containing the compounds, as well as the use of the compounds for the preparation of a medicament for treating, alleviating or prevention muscarinic receptor medicated diseases and conditions. | 03-20-2014 |
20140148477 | ANIMAL ECTOPARASITE-CONTROLLING AGENT AND METHOD FOR PREVENTING OR TREATING INFECTION IN ANIMALS CAUSED BY PARASITES BY USING THE CONTROLLING AGENT - The present invention provides an animal ectoparasite-controlling agent and a method for preventing or treating infection in animals caused by parasites by using the controlling agent. An animal ectoparasite-controlling agent exhibiting excellent insecticidal activity, and a method for preventing or treating infection in animals caused by parasites by using the controlling agent are obtained by using a compound having a pyrazole ring at the 4-position of the piperidine ring as an active ingredient. | 05-29-2014 |
20140163060 | Films and Drug Delivery Systems Made Therefrom - The invention relates to the film products and methods of their preparation that demonstrate a non-self-aggregating uniform heterogeneity. Desirably, the films disintegrate in water and may be formed by a controlled drying process, or other process that maintains the required uniformity of the film. The films contain a polymer component, which includes polyethylene oxide optionally blended with hydrophilic cellulosic polymers. Desirably, the films also contain a pharmaceutical and/or cosmetic active agent with no more than a 10% variance of the active agent pharmaceutical and/or cosmetic active agent per unit area of the film. | 06-12-2014 |
20140235665 | ANTI-CONSTIPATION COMPOSITION - An object of the present invention is to provide an anti-constipation composition containing a halogenated-bi-cyclic compound as an active ingredient in a ratio of bi-cyclic/mono-cyclic structure of at least 1:1. The halogenated-bi-cyclic compound is represented by Formula (I): | 08-21-2014 |
20140296282 | COMPOSITIONS OF A POLYORTHOESTER AND AN APROTIC SOLVENT - Delivery systems and compositions comprised of a biodegradable polyorthoester polymer, an aprotic solvent, and a drug are described. The solvent is selected to modulate release of drug from the composition, where, in some embodiments, the solvent is rapidly released after administration and provides a corresponding rapid rate of drug release. Alternatively, in other embodiments, the solvent is slowly released from the composition after its administration, and provides a correspondingly slow rate of drug release. | 10-02-2014 |
20140323517 | COMPOSITIONS AND METHODS FOR INJECTION OF A BIODEGRADABLE POLYMER-BASED DELIVERY SYSTEM - A method for administering a polymeric-based delivery system to a subject is described. The method comprises contacting a housing comprising a polymer-based delivery system with a heat-generating component for a period of time; and injecting the delivery system into the subject. | 10-30-2014 |
20140357662 | THIENO (2,3 - C) PYRAZOLES FOR USE AS POTASSIUM CHANNEL INHIBITORS - The present invention provides compounds of formula (I): wherein A, R | 12-04-2014 |
20140378504 | METHOD OF USING SUBSTITUTED 2-AZA-BICYCLO[2.2.2]OCTANE-3-CARBOXYLIC ACID (BENZYL-CYANO-METHYL)-AMIDES INHIBITORS OF CATHEPSIN C - This invention relates to 2-Aza-bicyclo[2.2.2]octane-3-carboxylic acid (benzyl-cyano-methyl)-amides of formula 1 | 12-25-2014 |
20150025105 | INDOLIZINE DERIVATIVES - Disclosed herein are indolizine compounds of general formula I, wherein R | 01-22-2015 |
20150299187 | ANTIMICROBIAL COMPOUNDS - The present invention relates to certain tetramic acid derivatives that are suitable for use in the preparation and development of antimicrobial (e.g. antibacterial or antifungal) compositions. The present invention also relates to the use of such compounds as antimicrobial (e.g. antibacterial or antifungal agents) and, in particular, as topical antibacterial or antifungal agents. | 10-22-2015 |
20150315201 | INDOLE AND INDOLINE-TYPE PIPERIDINE COMPOUNDS AND USES THEREOF - The disclosure relates to indole-type piperidine compounds, indoline-type piperidine compounds and related piperidine-type bicyclic compounds containing a five-membered nitrogen-containing ring (e.g., pyrrole or dihydropyrrole) fused to a heteroaryl ring, compositions comprising an effective amount of such compounds, and methods to treat or prevent a condition, such as pain, comprising administering to an animal in need thereof an effective amount of an indole-type piperidine compound, indoline-type piperidine compound or related piperidine-type bicyclic compound containing a five-membered nitrogen-containing ring (e.g., pyrrole or dihydropyrrole) fused to a heteroaryl ring. | 11-05-2015 |
20150359897 | METHOD OF TREATING PATIENTS NON-RESPONSIVE TO PALONOSETRON - A method for treating chemotherapy-induced nausea and vomiting in individuals undergoing chemotherapy and previously treated with, and whom failed to respond to, a 5-HT3 antagonist other than granisetron is described. Individuals who fail to respond to, for example, palonosetron, as evidenced by an inadequate prevention or attenuation of acute or delayed chemotherapy-induced nausea and vomiting, are treated with a semi-solid drug delivery vehicle that provides a sustained release of granisetron. | 12-17-2015 |
20160030403 | Novel Dosing Regimens of Celgosivir for the Treatment of Dengue - Methods of treating a dengue virus (DENV) infection in a human subject, comprising administering to the human subject a compound of Formula (I), or pharmaceutical composition comprising a compound of Formula (I): A compound of Formula (I) can be administered within onset of fever to 72 hours of fever onset due to dengue infection and then every 6 to 12 hours until there is an improvement in the infection or between from about 1 day to about 10 days. The methods of the invention can be used to treat primary and secondary DENV1-4 viral infections. | 02-04-2016 |
20160143890 | METHOD AND COMPOSITION FOR TREATING ALZHEIMER-TYPE DEMENTIA - There is described a method for increasing the maximal tolerated dose and thus the efficacy of an acetyl choline esterase inhibitor (AChEI) in a patient suffering from an Alzheimer type dementia by decreasing concomitant adverse effects by administration of said AChEI in combination with a non-anticholinergic antiemetic agent, whereby an enhanced acetyl choline esterase inhibition in the CNS of said patient is achieved and alleviation of the symptoms of Alzheimer type dementia in said patient is thereby improved to a greater extent. The use of a non-anticholinergic antiemetic agent for the preparation of a pharmaceutical composition for the treatment of Alzheimer type dementia in combination with an acetyl choline esterase inhibitor (AChEI) and pharmaceutical compositions comprising (a) a 5HT | 05-26-2016 |
20160144039 | METHODS FOR ENHANCING STABILITY OF POLYORTHOESTERS AND THEIR FORMULATIONS - Disclosed herein are methods of enhancing the stability of a sustained pharmaceutical composition comprising an active agent and a polymer and methods of preparing such pharmaceutical compositions with enhanced stability. | 05-26-2016 |
20160193192 | EXTRACELLULAR ALLOSTERIC INHIBITOR BINDING DOMAIN FROM A TYROSINE KINASE RECEPTOR | 07-07-2016 |
20180021321 | Methods of Treating Apoptosis and Altering Programmed Cell Death | 01-25-2018 |
20190142834 | UBIQUITIN-SPECIFIC-PROCESSING PROTEASE 7 (USP7) MODULATORS AND USES THEREOF | 05-16-2019 |