Class / Patent application number | Description | Number of patent applications / Date published |
514376000 | Chalcogen bonded directly to ring carbon of the oxazole ring | 75 |
20080221181 | COMPOUNDS FOR TREATING TUMORS - The invention provides compounds of formula (I): | 09-11-2008 |
20080221182 | ANTI-CANCER AND ANTI-MICROBIAL OXAZOLIDINONES - Disclosed herein are various novel oxazolidinone, imidazolidinone, and thiazolidinone analogs and methods of treating cancer and/or microbial infection using these analogs. Particular 4-oxazolidinone compounds are shown to have anti-cancer and anti-microbial activity. | 09-11-2008 |
20080221183 | ANTI-CANCER AND ANTI-MICROBIAL OXAZOLIDINONES - Disclosed herein are various novel oxazolidinone, imidazolidinone, and thiazolidinone analogs and methods of treating cancer and/or microbial infection using these analogs. Particular 4-oxazolidinone compounds are shown to have anti-cancer and anti-microbial activity. | 09-11-2008 |
20080234340 | Synthesis and characterization of polymorph form II of 4-(2-(4,4-dimethyl-2-oxooxazolidin-3-YL)thiazol-4-YL)benzonitrile - A polymorph Form II of 4-(2-(4,4-dimethyl-2-oxooxazolidin-3-yl)thiazol-4-yl)benzonitrile and methods of preparing Form II are described. Also provided are methods of contraception, treating or preventing fibroids, uterine leiomyomata, endometriosis, dysfunctional bleeding, polycystic ovary syndrome, and hormone-dependent carcinomas, providing hormone replacement therapy, stimulating food intake, and synchronizing estrus including using polymorph Form II of 4-(2-(4,4-dimethyl-2-oxooxazolidin-3-yl)thiazol-4-yl)benzonitrile. | 09-25-2008 |
20080242711 | INHIBITORS OF CHOLESTEROL ESTER TRANSFER PROTEIN - The invention relates to novel oxazolidinones their derivatives, pharmaceutically acceptable salts, solvates, and hydrates thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering cholesterol ester transfer protein inhibitors. | 10-02-2008 |
20080249148 | Synthesis and characterization of polymorph form III 4-(2-(4,4-dimethyl-2-oxooxazolidin-3-yl)thiazol-4-yl)benzonitrile - A polymorph Form III of 4-(2-(4,4-dimethyl-2-oxooxazolidin-3-yl)thiazol-4-yl)benzonitrile and methods of preparing Form III are described. Also provided are methods of contraception, treating or preventing fibroids, uterine leiomyomata, endometriosis, dysfunctional bleeding, polycystic ovary syndrome, and hormone-dependent carcinomas, providing hormone replacement therapy, stimulating food intake, and synchronizing estrus including using polymorph Form III of 4-(2-(4,4-dimethyl-2-oxooxazolidin-3-yl)thiazol-4-yl)benzonitrile. | 10-09-2008 |
20080262056 | Oxindole Oxazolidinones as Antibacterial Agents - The present invention relates to novel oxazolidinones derivatives of oxindoles of formula I or a pharmaceutically acceptable salt thereof wherein: Y | 10-23-2008 |
20090023791 | PH-dependent NMDA receptor antagonists - NMDA receptor blockers, including pH-sensitive NMDA receptor blockers, are provided as neurprotective drugs that are useful in stroke, traumatic brain injury, epilepsy, and other neurologic events that involve acidification of brain or spinal cord tissue. Compositions and methods of this invention are used for treating neurodegeneration resulting from NMDA receptor activation. The compounds described herein have enhanced activity in brain tissue having lower than normal pH due to pathological conditions such as hypoxia resulting from stroke, traumatic brain injury, global ischemia that may occur during cardiac surgery, hypoxia that may occur following cessation of breathing, pre-eclampsia, spinal cord trauma, epilepsy, chrounic pain, vascular dementia and glioma rumors. Compounds described herein are also useful in preventing neurodegeneration in patients with Parkinson's Alzheimer's, Huntington's chorea, ALS, and other neurodegenerative conditions known to the art to be responsive to treatment using NMDA receptor blockers. Prefebably the compounds provided herein are allosteric NMDA inhibitors. | 01-22-2009 |
20090036504 | 2-Aminoethoxyacetic Acid Derivatives and Their Use - The present application relates to novel 2-aminoethoxyacetic acid derivatives, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and also to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular thromboembolic disorders. | 02-05-2009 |
20090143450 | METHOD FOR TREATING CENTRAL PAIN SYNDROM OR FOR INDUCING CENTRALLY GENERATED PAIN IN AN ANIMAL MODEL - The present invention provides a method for treating central pain syndrome in a mammal by administering an effective amount of a thalamic anticonvulsant compound. Also provided are methods for inducing centrally generated pain responses in an animal model and for screening and identifying a compound that inhibits T-type calcium channels. | 06-04-2009 |
20090149520 | OXAZOLIDINONES CONTAINING OXINDOLES AS ANTIBACTERIAL AGENTS - The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof wherein X is C | 06-11-2009 |
20090156653 | Amino alcohol derivatives, salts thereof and immunosuppresive agents - An amino alcohol derivative represented by the following general formula (1) (for example, (±)-2-amino-5-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]-2-methylpentane- | 06-18-2009 |
20090156654 | DERIVATIVE N-THIOLATED 2-OXAZOLIDINONE ANTIBIOTICS - This invention describes the discovery and synthesis of N-thiolated 2-oxazolidinones as a new class of anti bacterial agents. These compounds can be synthesized from 2-oxazolidinones by Ndeprotection and N-sulfenylation. These new substances were found to exhibit potent anti-bacterial activity, including bacteriostatic properties against | 06-18-2009 |
20090163561 | AMORPHOUS METAXALONE AND AMORPHOUS DISPERSIONS THEREOF - The present invention provides various amorphous forms of the compound metaxalone (I), such as solid amorphous metaxalone and amorphous dispersions comprising metaxalone. The present invention further provides pharmaceutical compositions comprising these amorphous forms, and methods of their preparation. The present invention additionally provides methods of treating painful conditions (e.g., such as painful musculoskeletal conditions) comprising administering a therapeutically effective amount of any one of these amorphous forms to a subject in need thereof. | 06-25-2009 |
20090186926 | Self-Emulsifying Formulations of CETP Inhibitors - A liquid formulation for oral administration of the CETP inhibitor of formula (I) has improved bioavailability compared with conventional solid formulations. The formulation comprises the CETP inhibitor, or a pharmaceutically acceptable salt thereof; an oil; and one or more nonionic surfactants having a hydrophilic lipophilic balance (HLB)>10. | 07-23-2009 |
20090221655 | ANTIBACTERIAL AGENTS - The present invention provides a compound of Formula (I) Or a pharmaceutically acceptable salt thereof wherein: W is CH | 09-03-2009 |
20090264487 | HEMIASTERLIN ANALOGS - This invention provides analogs of hemiasterlin, methods of synthesis of the analogs and use of the analogs as a cytotoxic anti-mitotic agents. | 10-22-2009 |
20090270469 | SUBSTITUTED OXAZOLIDINONES - The present invention relates to new oxazolidinone modulators of skeletal muscle function and tone, pharmaceutical compositions thereof, and methods of use thereof. | 10-29-2009 |
20090318515 | SUCCINIMIDE DERIVATIVES AS OCULAR HYPOTENSIVE AGENTS - The invention provides a method for treating ocular disorders associated with ocular hypertension by administrating an effective amount of a pharmaceutical composition comprising a succinimide derivative. | 12-24-2009 |
20100041724 | Process For Synthesizing A CETP Inhibitor - An efficient process is disclosed for producing a compound that is an inhibitor of CETP. The last step of the process is the coupling of an oxazolidinone derivative with a biphenyl moiety to provide a compound of formula (I). In a specific embodiment of this synthesis, a crystalline product is produced which is characterized as a non-solvated crystalline polymorph. | 02-18-2010 |
20100048651 | PRODRUGS OF METHYL HYDROGEN FUMARATE, PHARMACEUTICAL COMPOSITIONS THEREOF, AND METHODS OF USE - Prodrugs of methyl hydrogen fumarate, pharmaceutical compositions comprising prodrugs of methyl hydrogen fumarate, and methods of using prodrugs of methyl hydrogen fumarate and pharmaceutical compositions thereof for treating diseases such as psoriasis, asthma, multiple sclerosis, inflammatory bowel disease, and arthritis are disclosed. | 02-25-2010 |
20100056588 | HISTONE DEACETYLASE INHIBITORS - In recognition of the need to develop novel therapeutic agents, the present invention provides novel histone deacetylase inhibitors. These compounds include an ester bond making them sensitive to deactivation by esterases. Therefore, these compounds are particularly useful in the treatment of skin disorders. When the compounds reaches the bloodstream, an esterase or an enzyme with esterase activity cleaves the compound into biologically inactive fragments or fragments with greatly reduced activity Ideally these degradation products exhibit a short serum and/or systemic half-life and are eliminated rapidly. These compounds and pharmaceutical compositions thereof are particularly useful in treating cutaneous T-cell lymphoma, neurofibromatosis, psoriasis, hair loss, skin pigmentation, and dermatitis, for example. The present invention also provides methods for preparing compounds of the invention and intermediates thereto. | 03-04-2010 |
20100063117 | Novel oxazolidinone derivative with difluorophenyl moiety, pharmaceutically acceptable salt thereof, preparation method thereof and antibiotic composition containing the same as an active ingredient - Novel oxazolidinone derivatives with a difluorophenyl moiety, represented by Chemical Formula 1, pharmaceutically acceptable salts thereof, a preparation method thereof, and a pharmaceutical composition containing the same as an active ingredient are provided. Exhibiting potent inhibitory activity against Gram-positive bacteria including | 03-11-2010 |
20100069449 | NOVEL OXAZOLIDINONE DERIVATIVE WITH DIFLUOROPHENYL MOIETY, PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, PREPARATION METHOD THEREOF AND ANTIBIOTIC COMPOSITION CONTAINING THE SAME AS AN ACTIVE INGREDIENT - Novel oxazolidinone derivatives with a difluorophenyl moiety, represented by Chemical Formula 1, pharmaceutically acceptable salts thereof, a preparation method thereof, and a pharmaceutical composition containing the same as an active ingredient are provided. Exhibiting potent inhibitory activity against Gram-positive bacteria including | 03-18-2010 |
20100099723 | BIOAVAILABLE COMPOSITIONS OF METAXALONE AND PROCESSES FOR PRODUCING THE SAME - Pharmaceutical compositions comprising metaxalone which demonstrate improved dissolution and bioavailability characteristics compared to the commercially available product, and methods of producing them are provided. In a preferred embodiment, a dosage form comprising metaxalone and at least one inactive powder excipient is bioequivalent to its commercially available counterpart (Skelaxin® 400-mg tablets) after oral administration to fasting or non-fasting human subjects, while at the same time displaying faster drug dissolution rates than the Skelaxin® tablets as demonstrated from three different dissolution tests. In another preferred embodiment, a dosage form comprising metaxalone, at least one inactive powder excipient and a nonvolatile liquid is significantly more bioavailable than the commercially available Skelaxin® 400-mg tablets after oral administration to fasting human subjects. | 04-22-2010 |
20100105747 | HYDROXYMETHYL ETHER HYDROISOINDOLINE TACHYKININ RECEPTOR ANTAGONISTS - The present invention is directed to certain hydroxymethyl ether hydroisoindoline compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, LUTS, depression, and anxiety. | 04-29-2010 |
20100179202 | ORALLY DISINTEGRATING COMPOSITION OF ZOLMITRIPTAN - A composition containing Zolmitriptan in the form of oral disintegrating tablet for the acute treatment of migraines is disclosed. The said composition comprises (a) Zolmitriptan, a salt or solvate or polymorph thereof as active ingredient, (b) mannitol, and (c) calcium silicate, and (d) optionally, one or more polysaccharides along with one or more pharmaceutically acceptable excipients. | 07-15-2010 |
20100227903 | Polymer Formulations of CETP Inhibitors - A pharmaceutical composition comprises (a) a CETP inhibiting compound, or a pharmaceutically acceptable salt thereof; (b) a concentration-enhancing polymer, and (c) optionally one or more surfactants; wherein the compound has the structure shown as Formula I below. The composition raises HDL-cholesterol and lowers LDL-cholesterol. | 09-09-2010 |
20100261771 | SUBSTITUTED 2-ACETAMIDO-5-ARYL-1,2,4-TRIAZOLONES AND USE THEREOF - The present application relates to new, substituted 2-acetamido-5-aryl-1,2,4-triazolones, to processes for preparing them, to their use alone or in combinations for the treatment and/or prevention of diseases and also to their use for the production of medicaments for the treatment and/or prevention of diseases, more particularly for the treatment and/or prevention of cardiovascular disorders. | 10-14-2010 |
20110021583 | ENHANCED TRANSMUCOSAL COMPOSITION AND DOSAGE FORM - The invention provides a transmucosal pharmaceutical composition comprising an active compound, a bile salt and an osmolality adjusting ingredient, wherein the osmolality adjusting ingredient generates a localized hyperosmotic environment and maintains an osmolality level for a period of time sufficient to produce hypertonicity-facilitated transmucosal transport of said active compound across the mucosal tissue. The invention also provides a solid transmucosal dosage form containing the composition, as well as a method of treatment comprising administering the same. In one embodiment, the active compound is a triptan compound, e.g., sumatriptan and zolmitriptan. | 01-27-2011 |
20110065763 | Compositions for Topical Application Having Androgenic Actions - A composition comprising at least one physiologically tolerated film-forming agent, at least one physiologically tolerated solvent, at least one plasticizer and a compound of the formula I | 03-17-2011 |
20110112157 | PROCESS FOR THE PREPARATION OF ZOLMITRIPTAN, SALTS AND SOLVATES THEREOF - The present invention relates to an improved process for the preparation of the active pharmaceutical ingredient zolmitriptan. In particular, it relates to an efficient process for the preparation of zolmitriptan and its pharmaceutically acceptable salts and solvates. | 05-12-2011 |
20110124694 | BIOAVAILABLE COMPOSITIONS OF METAXALONE AND PROCESSES FOR PRODUCING THE SAME - Pharmaceutical compositions comprising metaxalone which demonstrate improved dissolution and bioavailability characteristics compared to the commercially available product, and methods of producing them are provided. In a preferred embodiment, a dosage form comprising metaxalone and at least one inactive powder excipient is bioequivalent to its commercially available counterpart (Skelaxin® 400-mg tablets) after oral administration to fasting or non-fasting human subjects, while at the same time displaying faster drug dissolution rates than the Skelaxin® tablets as demonstrated from three different dissolution tests. In another preferred embodiment, a dosage form comprising metaxalone, at least one inactive powder excipient and a nonvolatile liquid is significantly more bioavailable than the commercially available Skelaxin® 400-mg tablets after oral administration to fasting human subjects. | 05-26-2011 |
20110144169 | Inhibitors of cellular necrosis - The present invention relates to compounds and pharmaceutical preparations and their use in therapy for preventing or treating trauma, ischemia, stroke and degenerative diseases associated with cell death. Methods and compositions of the invention are particularly useful for treating neurological disorders associated with cellular necrosis. | 06-16-2011 |
20110152332 | Pesticidal Heterocyclic Compounds - The present invention relates to novel pesticidal azolidine derivatives as well as to oxazolidinone derivatives and their use as pesticides for combating animal parasites which occur in the agrochemical field and in the field of veterinary medicine, respectively. | 06-23-2011 |
20110152333 | 3-CYANOPYRROLIDINYL-PHENYL-OXAZOLIDINONES AS ANTIBACTERIAL AGENTS - The invention provides new oxazolidinone compounds of formula (I) wherein R | 06-23-2011 |
20110218223 | TOPICAL VASOCONSTRICTOR PREPARATIONS AND METHODS FOR PROTECTING CELLS DURING CANCER CHEMOTHERAPY AND RADIOTHERAPY - Vasoconstrictors are administered topically to provide protection against the adverse effects, e.g., alopecia, mucositis or dermatitis, induced by chemotherapy or radiotherapy. Appropriate dosages and formulations of topical vasoconstrictors are provided. Methods for the use of such compositions are also provided. | 09-08-2011 |
20110288138 | ORALLY DISINTEGRATING TABLETS OF ZOLMITRIPTAN AND PROCESS FOR PREPARING THE SAME - Silicon dioxide free orally disintegrating tablet formulations of zolmitriptan or a pharmaceutically acceptable salt thereof having magnesium carbonate heavy and sodium stearyl fumarate with one or more pharmaceutically acceptable excipients and a process for preparing such a formulation and its use in the treatment of migraines. | 11-24-2011 |
20120004272 | BIOCIDAL COMPOSITION OF 2,6-DIMETHYL-M-DIOXANE-4-OL ACETATE AND METHODS OF USE - Provided are compositions comprising 2,6-dimethyl-m-dioxane-4-ol acetate and a biocidal compound selected from the group consisting of: a biocidal oxazolidine; 1-(3-chloroallyl)-3,5,7-triaza-1-azoniaadamantane; and tris(hydroxymethyl)-nitromethane. The compositions are useful for controlling microorganisms in aqueous or water containing systems. | 01-05-2012 |
20120122940 | POLYUNSATURATED FATTY ACIDS FOR THE TREATMENT OF DISEASES RELATED TO CARDIOVASCULAR, METABOLIC AND INFLAMMATORY DISEASE AREAS - The present disclosure relates to lipid compounds of the general formula (I): | 05-17-2012 |
20120208857 | Pharmaceutical Compositions - The present invention relates to pharmaceutical compositions useful for administration for treating, preventing, or reducing the risk of microbial infections. | 08-16-2012 |
20120238607 | SUBSTITUTED 2-ACETAMIDO-5-ARYL-1,2,4-TRIAZOLONES AND USE THEREOF - The present application relates to new, substituted 2-acetamido-5-aryl-1,2,4-triazolones, to processes for preparing them, to their use alone or in combinations for the treatment and/or prevention of diseases and also to their use for the production of medicaments for the treatment and/or prevention of diseases, more particularly for the treatment and/or prevention of cardiovascular disorders. | 09-20-2012 |
20130012554 | OXAZOLIDINONE DERIVATIVES CONTAINING NEW BICYCLIC GROUP, HAVING ANTIBACTERIAL ACTIVITY, AND METHOD FOR TREATING PATHOGENIC BACTERIAL INFECTIONS USING THE SAME - The present invention relates to oxazolidinone derivatives containing new bicyclic group, having antibacterial activity, or a pharmaceutically acceptable salt thereof, a method for preparing the same, an antibacterial composition comprising the oxazolidinone derivative or a pharmaceutically acceptable salt thereof as an active ingredient, and a method for treating an infectious disease caused by pathogen using the same. The oxazolidinone derivative or a pharmaceutically acceptable salt thereof may exhibit excellent antibacterial activity against gram positive bacteria including various resistant strains. | 01-10-2013 |
20130158083 | METAXALONE COCRYSTALS - The invention relates to improvements of the physiochemical and/or the pharmaceutical properties of metaxalone. Disclosed herein are several new cocrystals of metaxalone, including: a 1:1 metaxalone adipic acid cocrystal, a 1:0.5 metaxalone fumaric acid cocrystal, a 1:1 metaxalone salicyclic acid cocrystal, a 1:0.5 metaxalone succinic acid cocrystal, and a 1:0.5 metaxalone maleic acid cocrystal. The therapeutic uses of these metaxalone cocrystals are described as well as therapeutic compositions containing them. | 06-20-2013 |
20130184320 | Imine Compounds - The present invention relates to imine compounds which are useful for combating or controlling invertebrate pests, in particular arthropod pests and nematodes. The invention also relates to a method for controlling invertebrate pests by using these compounds and to plant propagation material and to an agricultural and a veterinary composition comprising said compounds. | 07-18-2013 |
20130231377 | PACTAMYCIN ANALOGS AND METHODS OF USE - Disclosed are pactamycin analogs, pharmaceutical compositions including the analogs, and methods of using the analogs, such as to inhibit tumor growth or a pathogenic infection such as a bacterial or parasitic infection. The pactamycin analogs have a general formula | 09-05-2013 |
20130245082 | BIOAVAILABLE COMPOSITIONS OF METAXOLONE COMPRISING NONVOLATILE LIQUIDS AND PROCESSES FOR PRODUCING THE SAME - Pharmaceutical compositions comprising metaxalone which demonstrate improved dissolution and bioavailability characteristics compared to the commercially available product, and methods of producing them are provided. In a preferred embodiment, a dosage form comprising metaxalone and at least one inactive powder excipient is bioequivalent to its commercially available counterpart (Skelaxin® 400-mg tablets) after oral administration to fasting or non-fasting human subjects, while at the same time displaying faster drug dissolution rates than the Skelaxin® tablets as demonstrated from three different dissolution tests. In another preferred embodiment, a dosage form comprising metaxalone, at least one inactive powder excipient and a nonvolatile liquid is significantly more bioavailable than the commercially available Skelaxin® 400-mg tablets after oral administration to fasting human subjects. | 09-19-2013 |
20130245083 | METHODS OF TREATMENT WITH BIOAVAILABLE COMPOSITIONS OF METAXALONE COMPRISING NONVOLATILE LIQUIDS - Pharmaceutical compositions comprising metaxalone which demonstrate improved dissolution and bioavailability characteristics compared to the commercially available product, and methods of producing them are provided. In a preferred embodiment, a dosage form comprising metaxalone and at least one inactive powder excipient is bioequivalent to its commercially available counterpart (Skelaxin® 400-mg tablets) after oral administration to fasting or non-fasting human subjects, while at the same time displaying faster drug dissolution rates than the Skelaxin® tablets as demonstrated from three different dissolution tests. In another preferred embodiment, a dosage form comprising metaxalone, at least one inactive powder excipient and a nonvolatile liquid is significantly more bioavailable than the commercially available Skelaxin® 400-mg tablets after oral administration to fasting human subjects. | 09-19-2013 |
20130261160 | METHOD OF PREPARATION OF METAXALONE - The present invention relates to a method of preparation of metaxalone comprising reaction of triglycidyl isocyanurate (TGIC) with m-xylenol, characterized in that said reaction is carried out in a solvent mixture comprising an aprotic polar solvent with dielectric constant greater than or equal to 30 and at least one other solvent selected from the group comprising apolar solvents and aprotic polar solvents with dielectric constant below 30 said solvent mixture comprising from 5 to 40 wt. % of said first solvent and from 95 to 60 wt. % of said second solvent, adding the TGIC at a temperature between 30° C. and 50° C., and after adding the TGIC, raising the temperature of the reaction solution to a value between 80° C. and 180° C. in a time between 120 and 180 minutes at a rate of increase not greater that 1.25° C. per minute. The invention also relates to a metaxalone with a reduced content of impurities derived from incomplete reactions and/or side reactions of the method of production. | 10-03-2013 |
20130281500 | Synergistic Fungicidal Active Substance Combinations - The novel active compound combinations of a carboxamide of the general formula (I) (group 1) | 10-24-2013 |
20130345269 | METHODS OF TREATMENT USING LIPID COMPOUNDS - Methods are disclosed to treat or prevent at least one disease or condition in a subject in need thereof comprising administering a compound of Formula (I): | 12-26-2013 |
20140031402 | Process for the Syntheses of Triazoles - The present invention relates to processes for the preparation of triazoles. These compounds are useful as anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents. | 01-30-2014 |
20140088164 | Pharmaceutical Compositions - The present invention relates to pharmaceutical compositions useful for administration for treating, preventing, or reducing the risk of microbial infections. | 03-27-2014 |
20140094495 | Antimicrobial Haloalkyl Heterocycle Compounds - This application describes compounds useful as anti-microbial agents, including as antibacterial, disinfectant, antifungal, germicidal or antiviral agents. | 04-03-2014 |
20140100254 | Radezolid salts and polymorphic forms thereof - Disclosed are compounds of Formula 1a, | 04-10-2014 |
20140135368 | SYNTHESIS OF INTERMEDIATES FOR PREPARING ANACETRAPIB AND DERIVATIVES THEREOF - The present invention relates to the field of organic chemistry, more specifically to the synthesis of intermediate compounds which can be used in the synthesis of pharmaceutically active agents such as anacetrapib or derivatives thereof. | 05-15-2014 |
20140135369 | TRPV4 ANTAGONISTS - The present invention relates to spirocarbamate analogs, pharmaceutical compositions containing them and their use as TRPV4 antagonists. | 05-15-2014 |
20140155442 | ANTI-OBESITY AGENT COMPRISING HIGH-PURITY EPA - The present invention provides an agent for preventing the increase in a body weight (or for decreasing a body weight) or an anti-obesity agent each comprising at least one component selected from the group consisting of EPA and pharmaceutically acceptable salts, esters and derivatives thereof as an active ingredient for obesity in which the increase in the formation of hepatic lipid or the occurrence of fatty liver is mild, preferably the increase in the formation of hepatic lipid or the occurrence of fatty liver is not observed. | 06-05-2014 |
20140155443 | COMPOSITIONS AND METHODS OF TREATMENT FOR PSORIASIS - The present invention provides for a composition comprising a tryptamine based drug that acts as a 5-hydroxytryptamine-1 inhibitor in an amount sufficient to reduce the effects of psoriasis and wherein the composition is formulated for topical or oral administration. | 06-05-2014 |
20140213620 | HISTONE DEACETYLASE INHIBITORS - In recognition of the need to develop novel therapeutic agents, the present invention provides novel histone deacetylase inhibitors. These compounds include an ester bond making them sensitive to deactivation by esterases. Therefore, these compounds are particularly useful in the treatment of skin disorders. When the compounds reaches the bloodstream, an esterase or an enzyme with esterase activity cleaves the compound into biologically inactive fragments or fragments with greatly reduced activity Ideally these degradation products exhibit a short serum and/or systemic half-life and are eliminated rapidly. These compounds and pharmaceutical compositions thereof are particularly useful in treating cutaneous T-cell lymphoma, neurofibromatosis, psoriasis, hair loss, skin pigmentation, and dermatitis, for example. The present invention also provides methods for preparing compounds of the invention and intermediates thereto. | 07-31-2014 |
20140221439 | POLYUNSATURATED FATTY ACIDS FOR THE TREATMENT OF DISEASES RELATED TO CARDIOVASCULAR, METABOLIC AND INFLAMMATORY DISEASE AREAS - The present disclosure relates to lipid compounds of the general formula (I): | 08-07-2014 |
20140336229 | PHARMACEUTICAL COMPOSITION FOR PREVENTING OR TREATING HYPERLIPIDEMIA - Provided is a pharmaceutical composition for preventing or treating hyperlipidemia comprising (4S,5R)-5-[3,5-bis(trifluoromethyl)phenyl]-3-({2-[4-fluoro-2-methoxy-5-(propan-2-yl)phenyl]-5-(trifluoromethyl)phenyl}methyl)-4-methyl-1,3-oxazolidin-2-one or its pharmaceutically acceptable salt; and an angiotensin II receptor blocker as active ingredients. | 11-13-2014 |
20150011595 | Inhibitors of Cholesterol Ester Transfer Protein - The invention relates to novel oxazolidinones their derivatives, pharmaceutically acceptable salts, solvates, and hydrates thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering cholesterol ester transfer protein inhibitors. | 01-08-2015 |
20150080442 | TRANSMUCOSAL DRUG DELIVERY SYSTEM - Disclosed are preparations and formulations of high thermodynamic activity lipophilic associations (LA), in which there is pairing between an ionizable pharmaceutical agent and a lipophilic species having ionic characteristics opposite to that of the pharmaceutical agent. Such lipophilic associations manifest high thermodynamic activity, as evidenced by their being predominantly in a liquid phase at room temperature or solvated in a lower-than-water dielectric solvent. Further the pharmaceutical agent being solubilized means that dissolution is not rate limiting to transmucosal absorption. This LA or LA-solvate is formulated into a low dielectric dosage form, from whence, upon the dosage form's hydration, the pharmaceutical agent is driven through the mucosal tissue and into systemic circulation. The invention therefore provides an enhanced transmucosal drug delivery system for ionizable pharmaceutical agents at or near physiological pH. | 03-19-2015 |
20150119431 | (R)-Nifuratel, its use for the treatment of infections and synthesis of (R) and (S)-Nifuratel - (R)-Nifuratel is disclosed together with its use as bactericide and bacteriostatic agent as well as the pharmaceutical compositions containing the same; (R)-nifuratel has been surprisingly found to possess a better antimicrobial profile than either nifuratel racemate or (S)-nifuratel. A new procedure for the synthesis of both (R)-Nifuratel and (S)-Nifuratel is also disclosed. | 04-30-2015 |
20150148386 | Oxazolidinone derivatives and composition for preventing or treating Hepatitis C containing the same - The present invention relates to oxazolidinone compounds represented by Chemical Formula 1, pharmaceutically acceptable salts thereof or hydrates, a method of preparing the same, and a pharmaceutical composition for preventing or treating Hepatitis C infection: | 05-28-2015 |
20150307482 | METHODS AND COMPOSITIONS FOR INHIBITING CNKSR1 - Embodiments include compositions and methods of inhibiting CNKSR1 and methods of identifying inhibitors of CNKSR1. | 10-29-2015 |
20150352080 | BIOAVAILABLE COMPOSITIONS OF METAXALONE COMPRISING NONVOLATILE LIQUIDS AND PROCESSES FOR PRODUCING THE SAME - Pharmaceutical compositions comprising metaxalone which demonstrate improved dissolution and bioavailability characteristics compared to the commercially available product, and methods of producing them are provided. In a preferred embodiment, a dosage form comprising metaxalone and at least one inactive powder excipient is bioequivalent to its commercially available counterpart (Skelaxin® 400-mg tablets) after oral administration to fasting or non-fasting human subjects, while at the same time displaying faster drug dissolution rates than the Skelaxin® tablets as demonstrated from three different dissolution tests. In another preferred embodiment, a dosage form comprising metaxalone, at least one inactive powder excipient and a nonvolatile liquid is significantly more bioavailable than the commercially available Skelaxin® 400-mg tablets after oral administration to fasting human subjects. | 12-10-2015 |
20160002184 | NEW BACTERIAL QUORUM SENSING REGULATOR AND MEDICAL USE THEREOF - The invention relates to a compound of formula I, and a preparation method and use thereof. The compound has a bacterial quorum-sensing regulatory effect, and can be used for prevention and/or treatment of a disease caused by a bacterial infection. | 01-07-2016 |
20160031869 | NOVEL INHIBITORS - The invention relates to a compound of formula (I) or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof, wherein R | 02-04-2016 |
20160108009 | Novel formulation of metaxalone - The present invention relates to methods for producing particles of metaxalone using dry milling processes as well as compositions comprising metaxalone, medicaments produced using metaxalone in particulate form and/or compositions, and to methods of treatment of an animal, including man, using a therapeutically effective amount of metaxalone administered by way of said medicaments. | 04-21-2016 |
20160120983 | PHARMACEUTICAL COMPOSITION WITH INCREASED SOLUBILITY BY USING SACCHARIN - The present invention provides a pharmaceutical composition including an ionic liquid composed of a triptan compound and saccharin. Since a triptan compound and saccharin form an ionic liquid to increase the solubility of the triptan compound in the present invention, it is possible to expect a rapid and high dissolution of the triptan compound when a pharmaceutical composition is prepared. In addition, large amounts of organic solvents and acidic solvents need not be used in order to dissolve the triptan compound. | 05-05-2016 |
20160136137 | METHOD FOR TREATING, PREVENTING, OR REDUCING THE RISK OF SKIN INFECTION - The present invention relates to methods for treating acne and other skin infections caused or mediated by | 05-19-2016 |
20160152579 | OXAZOLIDINONE DERIVATIVES AS PPAR LIGANDS | 06-02-2016 |
20160374995 | Pharmaceutical Compositions - The present invention relates to pharmaceutical compositions useful for administration for treating, preventing, or reducing the risk of microbial infections. | 12-29-2016 |