Entries |
Document | Title | Date |
20080200536 | Pharmaceutical Formulation with High Stability and Dissolution and Manufacturing Process - Disclosed herein are a pharmaceutical formulation with high stability and dissolution, and a method for preparing the pharmaceutical formulation. The pharmaceutical formulation comprises a pharmacologically active substance, a solvent, a solubilizer, a surfactant, an antioxidant, and an adsorbent. According to the pharmaceutical formulation and the method, the pharmacologically active substance is mixed with the solvent, the solubilizer agent and the surfactant for improving the solubility of the pharmacologically active substance to obtain an amorphous liquid or semi-solid state, the antioxidant is melted together with the mixture to solve poor chemical stability of the pharmacologically active substance in an amorphous or liquid state, and the adsorbent is strongly adsorbed to the molten mixture so as to be transformed into a powder form so that the resulting molecules are reconstituted into very tiny crystal forms within the adsorbent to ensure chemical stability. | 08-21-2008 |
20080214655 | Paclitaxel enhancer compounds - Disclosed is a compound represented by the Structural Formula (I): | 09-04-2008 |
20080249159 | Method of using oral lipase inhibitors to reduce plasma ghrelin and to prevent weight regain - A method of reducing ghrelin levels in a human body for weight reduction and to permanently reduce appetite and eliminate weight regain by the step of orally ingesting tetrahydrolipstatin—THL (Orlistat) on a regular basis for a period of at least one to two years. | 10-09-2008 |
20080249160 | Nematicidal Fatty Acid and Fatty Acid Ester Related Compounds - Certain fatty acids and related compounds useful in the control nematodes that infest plants or the situs of plants are described. Nematodes that parasitize animals can also be controlled using the methods and compounds of this invention. | 10-09-2008 |
20080262078 | Pharmaceutical Compositions - The present invention relates to a process for the preparation of a stable lyophilized form of a water insoluble drug suitable for parenteral use and pharmaceutical compositions comprising such lyophilized form of the drug. | 10-23-2008 |
20080269319 | Biologically active taxane analogs and methods of treatment - The present application relates to new taxane analogs, pharmaceutical compositions comprising such analogs and methods of treating cancer comprising such compositions. The compounds according to the present application have the general formula: | 10-30-2008 |
20080287524 | Method of Purifying a Surfactant by Ultrafiltration - A method of purifying a surfactant for use in a pharmaceutical formulation, which comprises mixing the surfactant with a solvent and bringing said mixture into contact with a semi-permeable membrane so as to allow impurities present in the surfactant and having a molecular weight lower than the molecular weight cut-off of the membrane to pass through the membrane, whilst retaining the purified surfactant. | 11-20-2008 |
20080300296 | Coating agent for drug releasing stent, preparation method thereof and drug releasing stent coated therewith - Disclosed are a coating agent for drug releasing stents, a method for preparing the same and a drug releasing stent coated therewith. The coating agent comprises a biologically active material and a coating material selected from among pullulan acetate, represented by the following Chemical Formula 1, and a polyurethane-surfactant mixture. | 12-04-2008 |
20080300297 | Taxane derivative containing pharmaceutical composition with improved therapeutic efficacy - The invention relates to a pharmaceutical combination comprising a mixture of (a) at least one taxane derivative and (b) at least one ω-3 poly-unsaturated acid or a derivative thereof wherein the molar ratio of (b) to (a) is not higher than 2. The invention further relates to a liquid pharmaceutical composition comprising (a) an effective amount of at least one taxane derivative, (b) an effective amount of at least one ω-3 poly-unsaturated fatty acid or a derivative thereof and (c) at least one pharmaceutically acceptable carrier and a process for the preparation of the same. The composition can be used for the therapy of cancers which are sensitive to taxane derivatives. The invention also relates to a kit comprising the individual components of the above mentioned composition placed in separate containers. | 12-04-2008 |
20080306137 | PHARMACEUTICAL COMPOSITIONS COMPRISING DOCETAXEL AND METHODS FOR PREPARATION THEREOF - A pharmaceutical composition of docetaxel comprising an effective amount of docetaxel, a polysorbate (TWEEN® compound) and a co-solvent, wherein the co-solvent is at least one member selected from the group consisting of glycerol and polyethylene glycol. The composition is an injectable solution or a freeze-dried powder for injection. The solubility of decetaxel is improved by adding a polysorbate and a co-solvent. Methods of preparation of the pharmaceutical composition are also disclosed. | 12-11-2008 |
20080312315 | Multifunctional Compounds for Forming Crosslinked Biomaterials and Methods of Preparation and Use - Multifunctional compounds are provided that readily crosslink in situ to provide crosslinked biomaterials. The multifunctional compounds contain a single component having at least three reactive functional groups thereon, with the functional groups selected so as to be non-reactive in an initial environment and inter-reactive in a modified environment. Reaction of a plurality of the multifunctional compounds results in a three-dimensional crosslinked matrix. In one embodiment, a first functional group is nucleophilic, a second functional group is electrophilic, and at least one additional functional group is nucleophilic or electrophilic. Methods for preparing and using the multifunctional compounds, and kits including the multifunctional compounds are also provided. Exemplary uses for the multifunctional compounds include tissue augmentation, biologically active agent delivery, bioadhesion, and prevention of adhesions following surgery or injury. | 12-18-2008 |
20080319048 | Solubilized formulation of docetaxel without tween 80 - Lyophilizates containing docetaxel and the use thereof in preparing concentrated liquid formulations, and ready to use formulations for injection, as well as such concentrates and ready to use formulations themselves are disclosed in which Tween surfactants are avoided so that hypersensitivity reactions to Tween surfactants can be avoided and docetaxel can be administered at higher doses and/or for longer periods of time and/or for additional treatment cycles. | 12-25-2008 |
20090030067 | Anti-proliferative combination therapy comprising satraplatin or jm118 and a taxane - The present invention describes a method of prevention and/or treatment of a cancer or a tumor, and in particular a combination therapy, methods, compositions and pharmaceutical packages comprising a taxane and certain platinum-based chemotherapeutic agents. | 01-29-2009 |
20090036517 | ANTI-ANGIOGENIC COMPOSITIONS AND METHODS OF USE - The present invention provides compositions comprising an anti-angiogenic factor, and a polymeric carrier. Representative examples of anti-angiogenic factors include Anti-Invasive Factor, Retinoic acids and derivatives thereof, and paclitaxel. Also provided are methods for embolizing blood vessels, and eliminating biliary, urethral, esophageal, and tracheal/bronchial obstructions. | 02-05-2009 |
20090048331 | METHODS AND FORMULATIONS FOR THE DELIVERY OF PHARMACOLOGICALLY ACTIVE AGENTS - In accordance with the present invention, novel formulations have been developed which are much more effective for the delivery of hydrophobic drugs to patients in need thereof than are prior art formulations. Invention formulations are capable of delivering more drug in shorter periods of time, with reduced side effects caused by the pharmaceutical carrier employed for delivery. | 02-19-2009 |
20090062376 | Preparation of Taxanes From 9-Dihydro-13-Acetylbaccatin III - The present invention relates to a new process for the preparation of 9-dihydrobaccatin III intermediates as useful precursors for the preparation of paclitaxel, 1, docetaxel, 2, and analogues thereof. More particularly, the process comprises the steps of (i) concomitantly deacetylating esters at the 10-position and 13-position of 9-dihydro-13-acetylbaccatin III to form 9-dihydro-10-deacetylbaccatin III; (ii) protecting a hydroxy group at the 7-position of 9-dihydro-10-deacetylbaccatin III; and (iii) acylating a hydroxy group at the 10-position to form a compound of formula II. | 03-05-2009 |
20090069409 | PROCESS FOR THE PREPARATION OF ANHYDROUS AND HYDRATED ACTIVE PHARMACEUTICAL INGREDIENTS (APIS); STABLE PHARMACEUTICAL COMPOSITIONS PREPARED FROM THE SAME AND USES OF SAID COMPOSITIONS - The invention relates to pharmaceutical compositions comprising anhydrous(2R,3S)4-acetoxy-2-a-benzoyloxy-5β-20-epoxy-1,7-β-10-β-tri-hydroxy-9-oxo-tax-11-en-13α-il 3-tert-butoxycarbonylamino-2-hydroxy-3-phenylpropionate (I)(docetaxel) and 4-acetoxy-2-α-benzoyloxy-5-β-20-epoxy-1,7β-10-β-tri-hydroxy-9-oxo-tax-11-en-13α-il (2R, 3S)3-benzoylamino-2-hydroxy-3-phenylpropionate (II) (paclitaxel), methods for treating neoplastic tumors using anhydrous docetaxel and paclitaxel, and a process for the preparation of the anhydrous docetaxel and paclitaxel. | 03-12-2009 |
20090069410 | DEUTERIUM-ENRICHED PACLITAXEL - The present application describes deuterium-enriched paclitaxel, pharmaceutically acceptable salt forms thereof, and methods of treating using the same. | 03-12-2009 |
20090069411 | SELF-EMULSIFYING AND SELF-MICROEMULSIFYING FORMULATIONS FOR THE ORAL ADMINISTRATION OF TAXOIDS - The present invention relates to novel formulations of taxoids for oral administration. More particularly, the present invention discloses and claims self-emulsifying and self-microemulsifying formulations for the oral administration of taxoids. | 03-12-2009 |
20090076127 | DEUTERIUM-ENRICHED LAROTAXEL - The present application describes deuterium-enriched larotaxel, pharmaceutically acceptable salt forms thereof, and methods of treating using the same. | 03-19-2009 |
20090082424 | SMALL MOLECULE ANTAGONISTS OF BCL-2 FAMILY PROTEINS - The present invention relates to naturally occurring and chemically synthesized small molecule antagonists of Bcl-2 family proteins. In particular, the present invention provides gossypol compounds (e.g., isomers, enantiomers, racemic compounds, metabolites, derivatives, pharmaceutically acceptable salts, in combination with acids or bases, and the like) and methods of using these compounds as antagonists of the anti-apoptotic effects of Bcl-2 family member proteins (e.g., Bcl-2, Bcl-X | 03-26-2009 |
20090099251 | DIETARY AND PHARMACEUTICAL COMPOSITIONS CONTAINING TRICYCLIC DITERPENES AND THEIR DERIVATIVES AND THEIR USES - The present invention refers to tricyclic diterpenes and their derivatives of the formulae (I) and (II), wherein R | 04-16-2009 |
20090105329 | Methods of Treating Cancers with SAHA, Carboplatin, and Paclitaxel and Other Combination Therapies - The present invention relates to a method of treating cancer in a subject in need thereof, by administering to a subject in need thereof an amount of a histone deacetylase (HDAC) inhibitor, e.g., suberoylanilide hydroxamic acid (SAHA), or a pharmaceutically acceptable salt or hydrate thereof, and an amount of one or more anticancer agents such as Carboplatin or Paclitaxel. The HDAC inhibitor and the anticancer agents may be administered to comprise therapeutically effective amounts. | 04-23-2009 |
20090118354 | Liquid Pharmaceutical Formulations of Docetaxel - There is provided a liquid pharmaceutical formulation for parenteral administration comprising: docetaxel or a pharmaceutically acceptable salt thereof; one or more glycols; and a pharmaceutically acceptable nonaqueous solvent system; wherein the formulation has a pH meter reading in the range of from 2.5 to 7. | 05-07-2009 |
20090118355 | Fluorotaxoids - The invention relates to fluorinated second generation taxoid compounds, pharmaceutical formulations thereof, and their use for inhibiting the growth of cancer cells in a mammal. | 05-07-2009 |
20090156659 | SYSTEM AND METHOD FOR COLLECTING, STORING, PROCESSING, TRANSMITTING AND PRESENTING VERY LOW AMPLITUDE SIGNALS - A method and apparatus for producing an effect of a chemical or biochemical agent on a system responsive to such agent, are disclosed. In practicing the method, a plurality of low-frequency time-domain signals of the agent are generated, each at a different at a different noise level within a selected noise level range. The signals are analyzed by producing spectral plots of the time-domain signals, and identifying an optimized agent-specific time-domain signal based on information in the spectral plots. A chemical or biological system responsive to the agent is exposed to the optimized time-domain signal by placing the system within the magnetic field of an electromagnetic transducer, and applying the signal to the transducer at a signal amplitude and for a period sufficient to produce in the system an agent-specific effect on the system. | 06-18-2009 |
20090156660 | PHARMACEUTICAL COMPOSITION CONTAINING TAXANE DERIVATIVE DESTINED FOR THE PREPARATION OF AN INFUSION SOLUTION, METHOD OF PREPARATION THEREOF AND USE THEREOF - A pharmaceutical composition containing a taxane derivative, destined for the preparation of an infusion solution for administration to patients, containing a concentrate consisting of a pharmaceutically effective amount of docetaxel, a suitable solvent, which is preferably ethanol, a surfactant, which is polysorbate 80 and a pharmaceutically effective amount of an appropriate buffer; and optionally a co-solvent, consisting of an aqueous solution of a pharmaceutically effective amount of polysorbate 80 and optionally suitable organic solvent and/or a pharmaceutically effective amount of an appropriate buffer. This composition shows an excellent chemical and physical stability. The invention includes also a method of preparation of the pharmaceutical composition and the use thereof. | 06-18-2009 |
20090163574 | Stable Pharmaceutical Composition Containing Docetaxel and a Method of Manufacturing the Same - The present invention relates to a stable pharmaceutical composition for injection containing docetaxel and a method of preparing the same. More particularly, the present invention relates to a pharmaceutical composition for injection containing docetaxel having better storage stability than conventional medications, which is prepared by dissolving docetaxel, a water-insoluble compound, in distilled water after mixing it with cyclodextrin (CD) and a water-soluble polymer such as hydroxypropyl methylcellulose (HPMC), polyethylene glycol (PEG) or polyvinylpyrrolidone (PVP) and lyophilizing the mixture, and a method of preparing the same. | 06-25-2009 |
20090192214 | DRUG DELIVERY FROM RAPID GELLING POLYMER COMPOSITION - Compositions are disclosed that afford drug delivery from two-part polymer compositions that rapidly form covalent linkages when mixed together. Such compositions are particularly well suited for use in a variety of tissue related applications when rapid adhesion to the tissue and gel formation is desired along with drug delivery. For example, the compositions are useful as tissue sealants, in promoting hemostasis, in effecting tissue adhesion, in providing tissue augmentation, and in the prevention of surgical adhesions. | 07-30-2009 |
20090215882 | LYOPHILIZED SOLID TAXANE COMPOSITION, A PROCESS FOR PREPARING SAID SOLID COMPOSITION, A PHARMACEUTICAL FORMULATION AND A KIT FOR SAID FORMULATION - A lyophilized solid composition of taxane (preferably docetaxel and paclitaxel), is suitable to prepare a pharmaceutical formulation to be administered to mammals, particularly humans, comprising a taxane, a tensoactive, a lyophilizing excipient, and acid; also essentially free from organic solvents. The solid composition is free from polysorbate 80 and polyoxyethylated castor oil; it is sterile; it is soluble in aqueous solutions in the absence of organic solvent and it has an apparent density from 0.05 g/ml to 0.45 g/ml. A procedure of double lyophilization obtains a solid composition of taxane. A pharmaceutical formulation of a taxane comprises a solid composition of lyophilized taxane and a solubilizing composition. A kit comprises the compositions and a syringe. | 08-27-2009 |
20090215883 | Pharmaceutical formulation comprising taxane, a solid composition of taxane, a process for preparing said solid composition of taxane, a solubilizing composition of said solid composition of taxane, and a kit for the injectable formulation of taxane - A pharmaceutical formulation of taxane intended to be administered to mammals, preferably humans, comprises two compositions combined prior to being administered, forming a transparent solution free from precipitates, in which the compositions comprise a solid composition of lyophilized taxane, free from tensoactives, oils, polymers, solubility enhancers, preservatives and excipients; and a solubilizing composition of the lyophilized taxane solid composition that comprises at least one tensoactive. This formulation is free from polysorbate 80 and polyoxyethylated castor oil. A procedure is provided for the preparation of the solid composition by means of the lyophilization of taxane in a lyophilizing organic solvent. A kit for the injectable formulation of taxane comprises a prefilled syringe. Also a pharmaceutical taxane solution for perfusion, free from organic solvent, is provided. | 08-27-2009 |
20090221688 | PHARMACEUTICAL COMPOSITIONS CONTAINING DOCETAXEL AND A DEGRADATION INHIBITOR AND A PROCESS FOR OBTAINING THE SAME - Pharmaceutical compositions containing polysorbate 80, anhydrous docetaxel (I) or its trihydrate and an organic acid with a pKa between 2.5-4.5 employed as a degradation inhibitor. | 09-03-2009 |
20090258937 | Methods for Modulating Tumor Growth and Metastasis - Methods and pharmaceutical compositions for modulating tumor growth or metastasis are provided. | 10-15-2009 |
20090275647 | TAXANE DERIVATIVE COMPOSITION - A stable, absolutely ethanol free composition of docetaxel that prevents alcoholic intoxication or anaphylactic shock. The composition can be in the form of a stable injectable composition that includes a taxane derivative, wherein the composition includes a mixture of docetaxel, one or more stabilizer, one or more surfactant, or more co-solvent and water for injection wherein the composition is absolutely free of ethanol. | 11-05-2009 |
20090281172 | BIS(THIO-HYDRAZIDE AMIDE) SALTS FOR TREATMENT OF CANCERS - Disclosed are bis(thio-hydrazide amide) disalts, which are represented by Structural Formula (I): | 11-12-2009 |
20090286864 | Coating agent for drug releasing stent, preparation method thereof and drug releasing stent coated therewith - Disclosed are a coating agent for drug releasing stents, a method for preparing the same and a drug releasing stent coated therewith. The coating agent for drug releasing stents comprises nanoparticles with a biologically active material entrapped therein, wherein the particles are formed of a polyethyleneimine (PEI)-deoxycholic acid (DOCA) polymer (PDo) in which 1˜8 moles of DOCA are grafted per mole of PEI. | 11-19-2009 |
20090286865 | POTENTIATOR OF ANTITUMORAL AGENTS IN THE TREATMENT OF CANCER - The present invention relates to a potentiator composition for enhancing therapeutical effect of an antitumoral agent, said composition comprising a terpene or derivative thereof in association with a pharmaceutically acceptable carrier. | 11-19-2009 |
20090298926 | PROCESS FOR THE PURIFICATION 10-DEACETYBACCATINE III FROM 10-DEACETYL-2-DEBENZOYL-2-PENTENOYLBACCATINE III - A process for the preparation of 10-deacetyl-7,10-bis-trichloroacetylbaccatine III with HPLC purity higher than 99% and free from 2-debenzoyl-2-pentenoylbaccatine III by purification of 10-deacetyl-7,10-bis-trichloroacetylbaccatineIII followed by alkaline hydrolysis of the protecting groups in position | 12-03-2009 |
20090298927 | Thermal Extraction Method and Product - The present invention is related to a thermal extract of a plant material and methods of extraction thereof. The method of producing a thermal extract from a plant starting material by means of a thermal extraction of the starting material wherein the improvement consists in requiring smaller amounts of costly and/or toxic organic solvents for the extraction and partitioning steps. | 12-03-2009 |
20090306196 | IMINE BASED LIQUID CRYSTALS FOR THE CONTROLLED RELEASE OF BIOACTIVE MATERIALS - The present invention relates to a delivery system based on a film of an imine forming liquid crystalline phase, mixed with at least with one biologically active substance, to which a constant or variable electric field can be applied. The delivery system can be used as a delivery system for biologically active substances such as flavors, fragrances, bactericides, fungicides, insecticides, insect attractants or repellents, agrochemicals or pharmaceuticals. | 12-10-2009 |
20090312405 | Methods to Predict and Prevent Resistance to Taxoid Compounds - Embodiments of the invention are directed to methods for predicting the resistance of cancer to members of the taxoid family by measuring the levels of prohibitin. Methods for treating cancer and taxoid family member resistant cancers using inhibitors of prohibitin, as well as therapeutic complexes that target prohibitin are also provided. | 12-17-2009 |
20100029755 | P-Glycoprotein inhibitor comprising octilonium bromide as an effective ingredient - The present invention relates to a new use of octylonium bromide as p-glycoprotein inhibitor to increase cellular uptake of drugs. More particularly, the present invention provides octylonium bromide as a p-glycoprotein inhibitor to increase cellular uptake of drugs such as anticancer drugs by taking octylonium bromide simultaneously with or proceeding drug administration. | 02-04-2010 |
20100035977 | TWO-COMPONENT TAXANE CONTAINING PHARMACEUTICAL COMPOSITION - A stabilized, injectable pharmaceutical composition for human administration comprises (a) an antineoplastic compound, (b) a solubilizing/dispersing agent, and (c) a stabilizing amount of an anti-oxidant. | 02-11-2010 |
20100041744 | OILY PACLITAXEL COMPOSITION AND FORMULATION FOR CHEMOEMBOLIZATION AND PREPARATION METHOD THEREOF - Oily paclitaxel composition and formulation for chemoembolization and preparation method thereof solubilizing paclitaxel in an oily contrast medium. The composition of the present invention solubilizes paclitaxel and has an advantage of delivering anticancer drug to the target cells by chemoembolization since it is possible to visualize the blood vessel during the chemoembolization process. The present invention also relates to oily paclitaxel composition and formulation additionally comprising chemicals that prevent paclitaxel precipitation for prolonged preservation and the preparation method thereof. Since the composition of the present invention solubilize paclitaxel effectively and can be visualized during chemoembolization, it can be used for TACE to treat hepatoma and other solid tumors. | 02-18-2010 |
20100048685 | PHARMACEUTICAL COMPOSITION CONTAINING DOCETAXEL-CYCLODEXTRIN INCLUSION COMPLEX AND ITS PREPARING PROCESS - A docetaxel inclusion complex having improved water-solubility (up to 15 mg/ml) and stability (stability constant Ka=2056M | 02-25-2010 |
20100056614 | C10 CYCLOPENTYL ESTER SUBSTITUTED TAXANES - A taxane having a cyclopentyl ester substituent at C10, a keto substituent at C9, a hydroxy substituent at C2, a 2-thienyl substituent at C3′ and an isopropoxycarbamate substituent at C3′. | 03-04-2010 |
20100076067 | BIODEGRADABLE BLOCK COPOLYMERIC COMPOSITIONS FOR DRUG DELIVERY - An improved drug delivery composition and method of use is disclosed. The composition comprises one or more biodegradable block copolymer drug carriers; and a reconstitution enhancing and enabling agent comprising polyethylene glycol (PEG), a PEG derivative or a mixture of PEG and a PEG derivative. The composition can be administered as is or after being be dissolved or rapidly reconstituted in an aqueous vehicle to afford a homogeneous solution or uniform colloidal systems. | 03-25-2010 |
20100099753 | Dietary and pharmaceutical compositions containing tricyclic diterpenes and their derivates and their uses - The present invention refers to tricyclic diterpenes and their derivatives of the formulae (I) and (II), wherein R | 04-22-2010 |
20100113580 | COMBINATION THERAPIES FOR THE TREATMENT OF OBESITY - Described are pharmaceutical compositions comprising bupropion, metformin, orlistat, and at least one pharmaceutically acceptable carrier or excipient. Another aspect of the present invention relates to a method of treating a patient suffering from obesity or needing to lose weight, comprising the step of co-administering to said patient a therapeutically effective amount of bupropion, metformin, and orlistat. In certain embodiments, an aforementioned method is practiced in conjunction or tandem with a medical procedure or the use of a medical device or both. | 05-06-2010 |
20100113581 | COMBINATION THERAPIES FOR THE TREATMENT OF OBESITY - Described are pharmaceutical compositions comprising diethylpropion, metformin, orlistat, and at least one pharmaceutically acceptable carrier or excipient. Another aspect of the present invention relates to a method of treating a patient suffering from obesity or needing to lose weight, comprising the step of co-administering to said patient a therapeutically effective amount of diethylpropion, metformin, and orlistat. In certain embodiments, an aforementioned method is practiced in conjunction or tandem with a medical procedure or the use of a medical device or both. | 05-06-2010 |
20100137418 | METHOD FOR TREATING ATHEROSCLEROSIS OR RESTENOSIS USING MICROTUBULE STABILIZING AGENT - The present invention is a method of preventing or reducing atherosclerosis or restenosis, and a pharmaceutical preparation used therefore. In particular, it is a method of preventing or reducing atherosclerosis or restenosis after arterial injury by treatment with a low dose of a microtubule stabilizing agent such as taxol or a water soluble taxol derivative. The low dose used in the present invention prevents artery blockage while minimizing any negative side effects associated with the drug. | 06-03-2010 |
20100144853 | NOVEL COMBINED ADMINISTRATION - The present invention is directed to the combined administration of a thioester therapeutic agent (preferably of formula I) and at least one esterase inhibitor. Also provided are a pharmaceutical composition, package, and a kit comprising the aforementioned active ingredients, as well as a method for increasing the bioavailability of said thioester for the treatment and prophylaxis of a cardiovascular disorder. | 06-10-2010 |
20100173982 | NOVEL METHOD FOR THE ASYMMETRIC SYNTHESIS OF BETA-LACTONE COMPOUNDS - The present invention features methods of treating a cancer in a subject by administering an effective amount of a beta-lactone to the subject. The invention also features methods of inhibiting angiogenesis in a subject by administering an effective amount of an inhibitor of fatty acid synthase to the subject. These methods can be used to treat a variety of cancers and other diseases and conditions. The invention also features methods of identifying beta-lactones and other compounds that can be used in the methods of the invention for the treatment of tumors, inhibition of angiogenesis, and the treatment of diseases and conditions that involve pathological angiogenesis. The invention also features methods of synthesizing beta-lactones and features novel beta-lactone compounds. | 07-08-2010 |
20100197776 | DIRECT DISSOLUTION OF DOCETAXEL IN A SOLVENT IN POLYSORBATE 80 - The disclosure relates to the solubilization of docetaxel in an organic solvent, to the mixture thereof with polysorbate 80, and to the evaporation of the solvent. | 08-05-2010 |
20100204312 | METHODS AND COMPOSITIONS FOR TREATING CANCER - This disclosure provides compositions and method useful for treating cell proliferative disorders including cancer. The disclosure provides cannabidiol derivatives and compositions thereof either alone or in combination with THC or a derivative thereof. | 08-12-2010 |
20100240742 | ANTI-ANGIOGENIC COMPOSITIONS AND METHODS OF USE - The present invention provides compositions comprising an anti-angiogenic factor, and a polymeric carrier. Representative examples of anti-angiogenic factors include Anti-Invasive Factor, Retinoic acids and derivatives thereof, and paclitaxel. Also provided are methods for embolizing blood vessels, and eliminating biliary, urethral, esophageal, and tracheal/bronchial obstructions. | 09-23-2010 |
20100267817 | LYOPHILIZED PHARMACEUTICAL COMPOSITION WITH IMPROVED RECONSTITUTION TIME CONTAINING TAXANE DERIVATIVES AND METHOD OF MANUFACTURING THE SAME - The present invention relates to a lyophilized composition with an improved reconstitution time comprising a taxoid and a method thereof. More specifically, the present invention relates to a lyophilized composition with an improved reconstitution time prepared by mixing and dissolving a taxoid; cyclodextrin (CD); a hydrophilic polymer selected from the group consisting of hydroxypropylmethyl CeIIuIoSe (HPMC), polyethylene glycol (PEG), and polyvinylpyrrolidone (PVP); and a bulking agent of saccharides in water for injection; and lyophilizing the mixture, and a method thereof. | 10-21-2010 |
20100267818 | STABILIZED SINGLE-LIQUID PHARMACEUTICAL COMPOSITION CONTAINING DOCETAXEL - This invention relates to a single-liquid pharmaceutical composition for injection containing docetaxel. The composition includes (A) docetaxel and pharmaceutically acceptable salts thereof, (B) a surfactant selected from the group consisting of polysorbate, polyoxyethylene glycol ester and polyoxyethylene castor oil derivatives, (C) a solvent comprising anhydrous ethanol in a concentration range of 100 to 800 mg/ml, in an injectable solution, and (D) a pH adjuster of an amount suitable for adjusting the pH of the liquid composition to 5 or less. The composition may be directly diluted in a perfusion liquid even without the use of an intermediary dilute solution in case the composition is used for injectable preparations since the composition is in a single liquid phase. Furthermore, the composition is suitable for effective administration of docetaxel since the pharmaceutical stability of the composition is significantly improved. | 10-21-2010 |
20100292314 | ANTI-ANGIOGENIC COMPOSITIONS AND METHODS OF USE - The present invention provides compositions comprising an anti-angiogenic factor, and a polymeric carrier. Representative examples of anti-angiogenic factors include Anti-Invasive Factor, Retinoic acids and derivatives thereof, and paclitaxel. Also provided are methods for embolizing blood vessels, and eliminating biliary, urethral, esophageal, and tracheal/bronchial obstructions. | 11-18-2010 |
20100305201 | Method of Treating a Tumor and Biodistribution of a Drug Delivered by Worm-Like Filomicelles - Provided are filomicelle nanocarrier systems for the controlled transport and bioselective delivery of encapsulatable, cytotoxic active agents contained therein, particularly anticancer agents. Further provided are methods for controlling destabilization of the filomicelle membrane and the resulting hydrolysis-triggered, controlled release of the active agent(s) encapsulated therein by controlling the blend ratio (mol %) of hydrolysable PEO-block copolymer of the hydrophilic component(s) and of the more hydrophobic PEO-block copolymer component(s), wherein bioselective release of the encapsulated cytotoxic agents is distributed intracellularly, and wherein lowered dosage of the drug was delivered to the non-tumor organs. Thus, the filomicelle system offers enhanced tumor-selective biodistribution of a drug, and a reduced toxicity of the encapsulated drug to other organs. | 12-02-2010 |
20100305202 | LYOPHILIZED PHARMACEUTICAL COMPOSITION WITH IMPROVED STABILITY CONTAINING TAXANE DERIVATIVES, AND METHOD OF MANUFACTURING THE SAME - The present invention relates to a lyophilized pharmaceutical composition for injection having superior storage stability comprising a taxoid, and a method thereof. More specifically, the present invention relates to a lyophilized pharmaceutical composition for injection having improved solubility and stability of dilution compared to the conventional preparations by dissolving a water-insoluble taxoid in distilled water added with a hydrophilic polymer such as hydroxypropylmethyl cellulose (HPMC), polyethylene glycol (PEG) or polyvinylpyrrolidone (PVP) cyclodextrin (CD), and lyophilizing the mixture and a method thereof. | 12-02-2010 |
20100317726 | SLCO1B3 GENOTYPE - The invention relates methods of identifying and predicting inter-patient differences in prognostic prediction for survival in androgen independent prostate cancer. It further related to methods for determining and exploiting such differences to improve medical outcomes. Moreover, it provides methods for determining if a subject has prostate cancer. | 12-16-2010 |
20100324128 | 9, 10-Alpha, Alpha-OH-Taxane Analogs and Methods for Production Thereof - The present invention relates to a method for the treatment of cancer in a cancer patient. In particular, the invention provides a method for the treatment comprising administering a taxane compound to a cancer patient, wherein the taxane compound is made by a process comprising treating a first compound represented by either Formula G′ or Formula M′: | 12-23-2010 |
20110015259 | TLE3 AS A MARKER FOR CHEMOTHERAPY - Methods of using TLE3 as a marker for predicting the likelihood that a patient's cancer will respond to chemotherapy. Methods of using TLE3 as a marker for selecting a chemotherapy for a cancer. | 01-20-2011 |
20110039921 | CEPHALOMANNINE DERIVATIVES, THEIR PREPARATION, PHARMACEUTICAL COMPOSITION AND USE THEREOF - The present invention discloses cephalomannine derivatives of general formula (I), a process for preparation of such cephalomannine derivatives, a composition containing such compounds, and use of said compounds in the manufacture of a medicament for the treatment of tumors, especially multidrug resistant tumors. | 02-17-2011 |
20110046211 | COMBINATION THERAPY OF HEDGEHOG INHIBITORS, RADIATION AND CHEMOTHERAPEUTIC AGENTS - The present invention relates to therapeutic combinations and methods of inhibiting the proliferation of cancerous cells, the abnormal growth of cells, and tumor cell growth using the combination of a hedgehog inhibitor with chemotherapy and/or radiation therapy. The present invention also relates to methods of enhancing the antiproliferative effect of chemotherapy and/or radiation therapy in a mammalian cancer patient undergoing either chemotherapy or radiation or a combination of radiation and chemotherapy by co-administering a therapeutically amount of a hedgehog inhibitor, concurrently or sequentially, with the chemotherapy and/or radiation therapy. | 02-24-2011 |
20110060036 | Branched Multifunctional Nanoparticle Conjugates And Their Use - Disclosed herein are compounds and compositions including a polyglycerol nanocarrier, a therapeutic agent or imaging agent, and optionally a targeting agent. In certain aspects the disclosed compounds include biocompatible hyperbranched polymer nanocarriers. Such compounds and compositions are useful for the targeted delivery of antitumor agents and imaging agents to tumors in vivo. Methods are also disclosed for detecting and treating such tumors. | 03-10-2011 |
20110071216 | RECONSTITUTABLE REVERSE THERMAL GELLING POLYMERS - Biodegradable and bioabsorbable block copolymers, which can be in the form of solid powder or powder wax compositions that can be easily reconstituted into an aqueous polymer solution and exhibit reverse thermal gellation properties upon exposure to elevated temperatures, are provided. Methods of making using these copolymers are also provided. | 03-24-2011 |
20110077291 | Preparations of Taxanes for Intravenous Administration and the Preparation Method Thereof - The present invention relates to the field of medical technology. More specifically, the present invention relates to a preparation of taxanes for intravenous administration, which consists of two parts: a drug solution and an emulsion. Said drug solution consists of paclitaxel or docetaxel, a pH regulator and a solvent for injection, wherein said solvent for injection is an organic solvent. Said emulsion includes a fat emulsion and is composed of oil for injection, an emulsifier, an antioxidant, an isotonic regulator, a stabilizer, a pH regulator and water for injection. When used, the drug solution at the clinical dosage can be added and mixed homogeneously in the emulsion to perform intravenous drip directly; or the drug solution at the clinical dosage can also be firstly added into the emulsion with no less than 5 times volume of the drug solution and then a predetermined amount of normal saline or glucose solution for injection is added to perform intravenous drip. The preparation of the present invention does not contain solubilizer and has advantages of little toxicity, safety, effectiveness, stability and economy. The fat emulsion is also used as a nutritional replenishment, thus achieving a better therapeutic effect. In addition, the normal saline or glucose solution for injection can be used to replace a considerable amount of the emulsion, which makes the preparation, therefore, not only cost-efficient, but also convenient for transportation and storage in practice. | 03-31-2011 |
20110082193 | TAXANE DERIVATIVE CONTAINING PHARMACEUTICAL COMPOSITION WITH IMPROVED THERAPEUTIC EFFICACY - The invention relates to a pharmaceutical combination comprising a mixture of (a) at least one taxane derivative and (b) at least one ω-3 poly-unsaturated acid or a derivative thereof wherein the molar ratio of (b) to (a) is not higher than 2. The invention further relates to a liquid pharmaceutical composition comprising (a) an effective amount of at least one taxane derivative, (b) an effective amount of at least one ω-3 poly-unsaturated fatty acid or a derivative thereof and (c) at least one pharmaceutically acceptable carrier and a process for the preparation of the same. The composition can be used for the therapy of cancers which are sensitive to taxane derivatives. The invention also relates to a kit comprising the individual components of the above mentioned composition placed in separate containers. | 04-07-2011 |
20110092579 | Solubilized formulation of docetaxel - Docetaxel containing formulations having TPGS and being substantially free or totally free of polysorbate surfactants are disclosed wherein stability is enhanced and hypersensitivity reactions are reduced. | 04-21-2011 |
20110092580 | Docetaxel formulations with lipoic acid and/or dihydrolipoic acid - Formulations comprising docetaxel or a salt thereof in combination with α-lipoic acid and/or dihydrolipoic acid and/or salts thereof in narrow concentration ranges have improved stability as concentrate liquid formulations and permit longer times between dilution from higher concentrations through completion of infusions prepared therefrom allowing for lesser waste and more efficient use of personnel in infusion preparation. | 04-21-2011 |
20110092581 | Docetaxel Formulations with Lipoic Acid - Pharmaceutical formulations comprising docetaxel, solubilizer, and α-lipoic acid, wherein the formulation is substantially free of polysorbates and polyethoxylated castor oil. The solubilizer may comprise glycofurol, acetic acid, benzyl alcohol, or ethanol. The α-lipoic acid, at certain concentrations, may impart stability and prevent degradation of docetaxel while the formulations are in storage. The formulations may be combined with a diluent, which comprises one or more hydrotropes such as tocopherol polyethylene glycol succinate and polyethylene glycol. The formulations combined with the diluent also exhibit stability after storage. Methods of administering docetaxel comprise preparing the formulation comprising docetaxel, solubilizer, and α-lipoic acid; mixing the formulation with a diluent; diluting the resulting formulation in saline, water for injection, or the like; and then injecting the formulations into patients in need thereof. | 04-21-2011 |
20110105598 | Process for Preparation of Taxane Derivatives - The present disclosure relates to processes for the preparation of taxane derivatives with improved purity and enhanced stability. The taxane derivatives prepared according to the processes described herein are useful for the preparation of pharmaceutical compositions. | 05-05-2011 |
20110118342 | COMPOSITIONS AND METHODS FOR PREPARATION OF POORLY WATER SOLUBLE DRUGS WITH INCREASED STABILITY - The present invention provides stable pharmaceutical compositions of poorly water soluble pharmaceutical agents and stabilizing agents which function to increase stability of the compositions. The use of stabilizing agents provide extended stability of nanoparticle suspensions and other formulations of poorly water soluble pharmaceutical agents such as docetaxel under certain conditions, for example upon dilution for administration. | 05-19-2011 |
20110130445 | SUBSTITUTED 3-PHENYLPROPIONIC ACIDS AND THE USE THEREOF - The present application relates to novel 3-phenylpropionic acid derivatives, to processes for their preparation, to their use for the treatment and/or prevention of diseases and to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of cardiovascular disorders. | 06-02-2011 |
20110130446 | INJECTABLE TAXANE PHARMACEUTICAL COMPOSITION - New injectable taxane pharmaceutical composition. Stable composition with low percentage of ethanol and a lower ethanol/taxane ratio than that of the state-of-the-art taxane pharmaceutical compositions. | 06-02-2011 |
20110144190 | METHOD OF PREPARING A SUPRAMOLECULAR COMPLEX CONTAINING A THERAPEUTIC AGENT AND A MULTI-DIMENSIONAL POLYMER NETWORK - A method of preparing a supramolecular complex containing at least one therapeutic agent and a multi-dimensional polymer network is described. A supramolecular complex prepared by a method of the invention is described. A method of treatment by administering a therapeutically effective amount of a supramolecular complex of the invention is also described. Such a supramolecular complex may be used as a delivery vehicle for various therapeutic agents. | 06-16-2011 |
20110152360 | LIQUID PHARMACEUTICAL FORMULATIONS OF DOCETAXEL - There is provided a liquid pharmaceutical formulation for parenteral administration comprising: docetaxel or a pharmaceutically acceptable salt thereof; one or more glycols; and a pharmaceutically acceptable nonaqueous solvent system; wherein the formulation has a pH meter reading in the range of from 2.5 to 7. | 06-23-2011 |
20110160295 | ANTITUMOR AGENT - An antitumor agent containing, in combination, at least one kind of antitumor agent selected from the group consisting of an antitumor agent that forms a cross-link with DNA and shows an antitumor effect, an antimetabolite antitumor agent and a taxane antitumor agent, and a histone deacetylase inhibitor. According to the present invention, an antitumor agent causing reduced side effects and having a superior antitumor activity can be provided. | 06-30-2011 |
20110166214 | METHODS AND COMPOSITIONS FOR DELIVERY OF TAXANES IN STABLE OIL-IN-WATER EMULSIONS - The present invention provides methods and compositions for delivery of taxanes in stable oil-in-water emulsion. The inventive emulsion formulation includes an oil phase, aqueous and emulsifier phases. The oil portion includes all or substantial amount of taxane, vegetable oil and medium chain triglycerides; aqueous phase includes an emulsion stabilizer; emulsifier phase reduces the surface tension between oil and aqueous phases to produce a stable oil-in-water emulsion. The inventive compositions produce minimal side effects upon administration. | 07-07-2011 |
20110190387 | METHOD FOR TREATING ATHEROSCLEROSIS OR RESTENOSIS USING MICROTUBULE STABILIZING AGENT - The present invention is a method of preventing or reducing atherosclerosis or restenosis, and a pharmaceutical preparation used therefore. In particular, it is a method of preventing or reducing atherosclerosis or restenosis after arterial injury by treatment with a low dose of a microtubule stabilizing agent such as taxol or a water soluble taxol derivative. The low dose used in the present invention prevents artery blockage while minimizing any negative side effects associated with the drug. | 08-04-2011 |
20110196025 | Polymorphs of N-Malonyl-Bis(N'-Methyl-N'-Thiobenzoylhydrazide) - At least 70% by weight of Compound 1 is the single crystalline form, Form A, Form C, or Form D, of the compound. A pharmaceutical composition comprises a pharmaceutically acceptable carrier or diluent, and compound 1, wherein at least 70% by weight of the compound is the single crystalline form, Form A, Form C, or Form D, of the compound. A method of treating a subject with cancer comprises administering to the subject an effective amount of compound 1 or the pharmaceutical composition. | 08-11-2011 |
20110196026 | COMPOSITIONS AND METHODS FOR PREPARATION OF POORLY WATER SOLUBLE DRUGS WITH INCREASED STABILITY - The present invention provides stable pharmaceutical compositions of poorly water soluble pharmaceutical agents and stabilizing agents which function to increase stability of the compositions. The use of stabilizing agents provide extended stability of nanoparticle suspensions and other formulations of poorly water soluble pharmaceutical agents such as docetaxel under certain conditions, for example upon dilution for administration. | 08-11-2011 |
20110196027 | BETA-LACTONES AS ANTIBACTERIAL AGENTS - The present invention relates to specific beta-lactone compounds and compositions thereof for the treatment of infections, such as, e.g., infections with bacteria or infections with protozoa, in particular infections with Gram-positive and/or Gram-negative bacteria and of infectious diseases caused by or related to Gram-positive and/or Gram-negative bacteria, and to the modulation of virulence of Gram-positive and/or Gram-negative bacteria or of protozoa by specific beta-lactone compounds. The invention further relates to the use of the compounds or compositions for preventing or eliminating biofilms. | 08-11-2011 |
20110207803 | Taxane Pro-Emulsion Formulations and Methods Making and Using the Same - Taxane pro-emulsion formulations are provided. Pro-emulsion formulations are dried powders that include a taxane, oil, surfactant and sugar alcohol. Also provided are methods of making and using the pro-emulsion formulations, as well as kits that include the pro-emulsion formulations. | 08-25-2011 |
20110207804 | COMPOSITIONS FOR THE TREATMENT OF NEOPLASTIC DISEASES - Solid pharmaceutical taxane compositions for oral administration which comprise a substantially amorphous taxane, a carrier, and a surfactant, wherein the substantially amorphous taxane is prepared by a solvent evaporation method, such as spray drying. Methods of preparation of the composition and uses of the composition also are included. | 08-25-2011 |
20110224288 | Cancer Cell Targeting Using Nanoparticles - The present invention generally relates to polymers and macromolecules, in particular, to polymers useful in particles such as nanoparticles. One aspect of the invention is directed to a method of developing nanoparticles with desired properties. In one set of embodiments, the method includes producing libraries of nanoparticles having highly controlled properties, which can be formed by mixing together two or more macromolecules in different ratios. One or more of the macromolecules may be a polymeric conjugate of a moiety to a biocompatible polymer. In some cases, the nanoparticle may contain a drug. Other aspects of the invention are directed to methods using nanoparticle libraries. | 09-15-2011 |
20110245332 | INJECTABLE FORMULATIONS OF TAXANES FOR CAD TREATMENT - Medical devices, and in particular implantable medical devices, may be coated to minimize or substantially eliminate a biological organism's reaction to the introduction of the medical device to the organism. The medical devices may be coated with any number of biocompatible materials. Therapeutic drugs, agents or compounds may be mixed with the biocompatible materials and affixed to at least a portion of the medical device. These therapeutic drugs, agents or compounds may also further reduce a biological organism's reaction to the introduction of the medical device to the organism. In addition, these therapeutic drugs, agents and/or compounds may be utilized to promote healing, including the formation of blood clots. The drugs, agents, and/or compounds may also be utilized to treat specific diseases, including vulnerable plaque. Therapeutic agents may also be delivered to the region of a disease site. In regional delivery, liquid formulations may be desirable to increase the efficacy and deliverability of the particular drug. Also, the devices may be modified to promote endothelialization. Various materials and coating methodologies may be utilized to maintain the drugs, agents or compounds on the medical device until delivered and positioned. In addition, the devices utilized to deliver the implantable medical devices may be modified to reduce the potential for damaging the implantable medical device during deployment. Medical devices include stents, grafts, anastomotic devices, perivascular wraps, sutures and staples. In addition, various polymer combinations may be utilized to control the elution rates of the therapeutic drugs, agents and/or compounds from the implantable medical devices. Liquid formulations, including solutions and suspensions of the various drugs, agents and/or compounds, may be locally or regionally delivered. In each of these instances, antioxidants are utilized to prolong product integrity. | 10-06-2011 |
20110251269 | PREPARATION METHOD OF POLYMERIC MICELLES COMPOSITION CONTAINING A POORLY WATER-SOLUBLE DRUG - Provided is a method for preparing a drug-containing polymeric micelle composition, which includes: dissolving a drug and an amphiphilic block copolymer into an organic solvent; and adding an aqueous solution to the resultant mixture in the organic solvent to form polymeric micelles, wherein the method requires no separate operation to remove the organic solvent prior to the formation of micelles. The method for preparing a drug-containing polymeric micelle composition is simple, reduces the processing time, and is amenable to mass production. | 10-13-2011 |
20110257253 | PREPARATION METHOD OF POLYMERIC MICELLAR NANOPARTICLES COMPOSITION CONTAINING A POORLY WATER-SOLUBLE DRUG - Provided is a method for preparing a poorly water-soluble drug-containing polymeric micellar nanoparticle composition, which includes: dissolving a poorly water-soluble drug, a salt of polylactic acid or polylactic acid derivative, whose carboxylic acid end is bound to an alkali metal ion, and an amphiphilic block copolymer into an organic solvent; and adding an aqueous solution to the resultant mixture in the organic solvent to form micelles, wherein the method requires no separate operation to remove the organic solvent prior to the formation of micelles. The method for preparing a poorly water-soluble drug-containing polymeric micellar nanoparticle composition is simple, reduces the processing time, and is amenable to mass production. | 10-20-2011 |
20110269829 | Non-Aqueous Taxane Pro-Emulsion Formulations and Methods of Making and Using the Same - Non-aqueous taxane pro-emulsion formulations are provided. Pro-emulsion formulations of embodiments of the invention include a taxane, an oil component, a surfactant component and, optionally, a non-aqueous solvent component. Also provided are methods of making and using the pro-emulsion formulations, as well as kits that include the pro-emulsion formulations. | 11-03-2011 |
20110275704 | Stable Formulations for Lyophilizing Therapeutic Particles - The present disclosure generally relates to lyophilized pharmaceutical compositions comprising polymeric nanoparticles which, upon reconstitution, have low levels of greater than 10 micron size particles. Other aspects of the invention include methods of making such nanoparticles. | 11-10-2011 |
20110275705 | STABLE INJECTABLE OIL-IN-WATER DOCETAXEL NANOEMULSION - The present invention describes Stable injectable oil-in-water Docetaxel nanoemulsion composition having Docetaxel concentrations as high as 20 mg/ml, devoid of hypersensitivity reaction and fluid retention. It employs Synthetic triglycerides, and DSPE PEG-2000, Natural phosphatides, Polyhydric alcohol and Water for injection. In another embodiment lyophilised products with added Cryoprotectants have been described which on reconstitution gives nanoemulsion suitable for parenteral administration. | 11-10-2011 |
20110275706 | Pharmaceutical Compositions Containing Lipase Inhibitors - A pharmaceutical composition comprises at least one inhibitor of lipases, preferably an inhibitor of gastrointestinal and pancreatic lipases, such as orlistat, at least one surfactant, and at least one dispersant. | 11-10-2011 |
20110288162 | TRANSITION METAL COMPLEXES OF A BIS[THIO-HYDRAZIDE AMIDE] COMPOUNDS - The present invention is directed to a compound comprising a bis[thiohydrazide amide] or a deprotonated form thereof, complexed to a transition metal cation, wherein the bis[thio-hydrazide amide] is represented by Structural Formula (I): or a prodrug, isomer, ester, salt, hydrate, solvate, polymorph or a deprotonated form thereof. The present invention also provides a pharmaceutical composition comprising a compound of the invention and method of use thereof. | 11-24-2011 |
20110301231 | LIPASE INHIBITING COMPOSITION - Pharmaceutical compositions that contain a lipase inhibitor having a melting point ≧37° C., a sucrose fatty acid ester wherein the sucrose fatty acid ester is a mono-, di-, tri- or tetra-ester, and optionally one or more pharmaceutically acceptable excipients, are useful for treatment of obesity. | 12-08-2011 |
20120004293 | Cancer Cell Targeting Using Nanoparticles - The present invention generally relates to polymers and macromolecules, in particular, to polymers useful in particles such as nanoparticles. One aspect of the invention is directed to a method of developing nanoparticles with desired properties. In one set of embodiments, the method includes producing libraries of nanoparticles having highly controlled properties, which can be formed by mixing together two or more macromolecules in different ratios. One or more of the macromolecules may be a polymeric conjugate of a moiety to a biocompatible polymer. In some cases, the nanoparticle may contain a drug. Other aspects of the invention are directed to methods using nanoparticle libraries. | 01-05-2012 |
20120004294 | ANTITUMOR COMBINATION COMBINING AVE8062 AND DOCETAXEL - The invention relates to a sequential antitumor combination of AVE8062, or a salt thereof, and docetaxel, characterized in that AVE8062 is administered to a patient in a dose of 10 to 50 mg/m2, and then, on a different day of the week, preferably after a 24-hour interval, docetaxel is administered in a dose of 50 to 120 mg/m2. | 01-05-2012 |
20120022148 | Curcuminoids in Combination Docetaxel for the Treatment of Cancer and Tumour Metastasis - The present invention relates to a curcuminoid for enhancing the clinical efficacy of Docetaxel for the treatment of cancers and metastases. | 01-26-2012 |
20120065255 | CABAZITAXEL FORMULATIONS AND METHODS OF PREPARING THEREOF - Pharmaceutical formulations comprising cabazitaxel, solubilizer, tocopherol polyethylene glycol succinate (TPGS), one or more hydrotropes, optionally one or more agents having a pK | 03-15-2012 |
20120077871 | 9, 10-Alpha, Alpha-OH-Taxane Analogs and Methods for Production Thereof - Provided herein are compounds, compositions containing the compounds, and methods for the treatment of cancer in a cancer patient. In particular, the compounds are made by a process comprising treating a first compound represented by either Formula G′ or Formula M′: | 03-29-2012 |
20120077872 | PRESERVATIVE-FREE PHARMACEUTICAL TETRAHYDROLIPSTATIN COMPOSITIONS - This invention refers to pharmaceutical compositions that comprise the mixture of an effective amount of leucine-derivative powders or granules and, at least, one pharmaceutically acceptable excipient substance used as carrier. In particular, the main feature of the pharmaceutical composition is the fact that it is free of preservative agents and might be formulated in any usual pharmaceutical oral formulation. | 03-29-2012 |
20120083523 | MEDICAL DEVICES HAVING POLYMERIC REGIONS WITH COPOLYMERS CONTAINING HYDROCARBON AND HETEROATOM-CONTAINING MONOMERIC SPECIES - According to an aspect of the present invention, implantable or insertable medical devices are provided, which contain one or more polymeric regions. These polymeric regions, in turn, contain one or more polymers, at least one of which is a copolymer that includes the following: (a) one or more unsaturated hydrocarbon monomer species and (b) one or more heteroatom-containing monomer species. | 04-05-2012 |
20120088821 | METHOD FOR TREATING ATHEROSCLEROSIS OR RESTENOSIS USING MICROTUBULE STABILIZING AGENT - The present invention is a method of preventing or reducing atherosclerosis or restenosis, and a pharmaceutical preparation used therefore. In particular, it is a method of preventing or reducing atherosclerosis or restenosis after arterial injury by treatment with a low dose of a microtubule stabilizing agent such as taxol or a water soluble taxol derivative. The low dose used in the present invention prevents artery blockage while minimizing any negative side effects associated with the drug. | 04-12-2012 |
20120129922 | DOCETAXEL FORMULATIONS WITH LIPOIC ACID - Pharmaceutical formulations comprising docetaxel or a pharmaceutically acceptable salt thereof, one or more solubilizers, α-lipoic acid, TPGS, one or more hydrotropes, and optionally one or more agents having a pK | 05-24-2012 |
20120157517 | PHARMACEUTICAL SOLUTION OF TAXANES COMPRISING PH REGULATOR AND PREPARATION METHOD THEREOF - A pharmaceutical solution of taxanes, its preparation method, a composition comprising said solution and its pharmaceutical combination package are disclosed. Said pharmaceutical solution comprises taxanes, a pH regulator and a solvent, wherein the pH regulator is a water-soluble acid. | 06-21-2012 |
20120232134 | COMBINATION CANCER THERAPY WITH BIS(THIOHYDRAZIDE) AMIDE COMPOUNDS - Disclosed is a method of treating a subject with cancer, the method comprising the step of co-administering to the subject over three to five weeks, a taxane in an amount of between about 243 μmol/m | 09-13-2012 |
20120264817 | SOLUBILIZED FORMULATION OF DOCETAXEL WITHOUT TWEEN 80 - Lyophilizates containing docetaxel and the use thereof in preparing concentrated liquid formulations, and ready to use formulations for injection, as well as such concentrates and ready to use formulations themselves are disclosed in which Tween surfactants are avoided so that hypersensitivity reactions to Tween surfactants can be avoided and docetaxel can be administered at higher doses and/or for longer periods of time and/or for additional treatment cycles. | 10-18-2012 |
20120277295 | KIT FOR CANCER TREATMENT AND PHARMACEUTICAL COMPOSITION FOR CANCER TREATMENT - To provide a kit for cancer treatment and a pharmaceutical composition for cancer treatment that can inhibit the growth of tumors and cancers in mammals more than ever. | 11-01-2012 |
20120289588 | Lipase Inhibitors for the Treatment of Pancreatitis and Organ Failure - The present invention relates to methods for treating pancreatitis and/or organ failure comprising administering, to a subject in need of such treatment, an effective amount of a lipase inhibitor. It is based, at least in part, on the discoveries that lipotoxicity contributes to inflammation, multisystem organ failure, necrotic pancreatic acinar cell death and in acute pancreatitis, and that inhibition of lipolysis was able to reduce indices associated with these conditions. Accordingly, in various embodiments, the present invention provides for methods and compositions for limiting lipotoxicity and thereby reducing the likelihood of poor outcomes associated with acute pancreatitis and other severe systemic conditions, especially in obese individuals. | 11-15-2012 |
20120302629 | BIOMARKERS FOR GOSSYPOL CHEMOTHERAPY AND METHODS OF TREATING DISEASE - The present invention provides a biomarker for selecting a patient for treatment with gossypol, wherein the biomarker comprises an elevated expression level of c-Myc, Mcl-1, or combination thereof, relative to the normal expression level of c-Myc, Mcl-1, or combination thereof. The present invention also provides methods for targeting patients for treatment with gossypol, wherein the patient has a disease, condition, or disorder that overexpresses c-Myc, Mcl-1, or combination thereof. The present invention also provides methods for treating or ameliorating a disease, condition, or disorder in a patient comprising determining the expression level of c-Myc, Mcl-1, or combination thereof in the patient and administering gossypol to the patient. In certain embodiments of the invention, the disease is cancer, and the cancer cells show elevated expression levels of c-Myc compared to non-cancerous cells. The invention also provides methods for overcoming Mcl-1-mediated chemoresistance comprising administering gossypol to a patient in need thereof. | 11-29-2012 |
20120329861 | TREATMENT OF CANCER USING BENZOIC ACID DERIVATIVES - The present invention provides a method of treating cancer using benzoic acid derivatives, alone or in combination with standard treatments such as chemotherapy and radiotherapy. Also provided are methods of screening for benzoic derivatives based on their ability to inhibit the enzyme tyrosinase or to bind to and activate PXR/SXR xenobiotic receptors. | 12-27-2012 |
20130035378 | FILM DELIVERY SYSTEM FOR TETRAHYDROLIPSTATIN - The present invention includes a pharmaceutical-based film system which includes various small-scale forms of pharmaceutically active agents, including tetrahydrolipstatin, in a film base. Such forms include nanoparticles, microparticles, and combinations thereof. Methods of producing such film and providing a dosage of the pharmaceutical in a film are also provided | 02-07-2013 |
20130053433 | FATTY ACID DERIVATIVES AND ANALOGS OF DRUGS - The present disclosure is directed to fatty acid-drug conjugates, the preparation and use thereof and long-chain (C | 02-28-2013 |
20130065955 | CRYSTALLINE FORMS OF CABAZITAXEL - The present invention provides crystalline forms, including an anhydrate form, of cabazitaxel and processes for the preparation of these forms, designated as Forms C1, C2, C3, C4, C5, C6, C7, C8, C8 | 03-14-2013 |
20130079391 | LIPASE INHIBITING COMPOSITION - Pharmaceutical compositions that contain a lipase inhibitor having a melting point ≧37° C., a sucrose fatty acid ester wherein the sucrose fatty acid ester is a mono-, di-, tri- or tetra-ester, and optionally one or more pharmaceutically acceptable excipients, are useful for treatment of obesity. | 03-28-2013 |
20130079392 | TLE3 AS A MARKER FOR CHEMOTHERAPY - Methods of using TLE3 as a marker for predicting the likelihood that a patient's cancer will respond to chemotherapy. Methods of using TLE3 as a marker for selecting a chemotherapy for a cancer. | 03-28-2013 |
20130102657 | ANTI-ANGIOGENIC COMPOSITIONS AND METHODS OF USE - The present invention provides compositions comprising an anti-angiogenic factor, and a polymeric carrier. Representative examples of anti-angiogenic factors include Anti-Invasive Factor, Retinoic acids and derivatives thereof, and paclitaxel. Also provided are methods for embolizing blood vessels, and eliminating biliary, urethral, esophageal, and tracheal/bronchial obstructions. | 04-25-2013 |
20130123351 | HIGH THROUGHPUT FABRICATION OF NANOPARTICLES - This application provides a high throughput method of making nanoparticles that utilizes plates comprising wells (e.g., 96-well plates). | 05-16-2013 |
20130172406 | Cancer Cell Targeting Using Nanoparticles - The present invention generally relates to polymers and macromolecules, in particular, to polymers useful in particles such as nanoparticles. One aspect of the invention is directed to a method of developing nanoparticles with desired properties. In one set of embodiments, the method includes producing libraries of nanoparticles having highly controlled properties, which can be formed by mixing together two or more macromolecules in different ratios. One or more of the macromolecules may be a polymeric conjugate of a moiety to a biocompatible polymer. In some cases, the nanoparticle may contain a drug. Other aspects of the invention are directed to methods using nanoparticle libraries. | 07-04-2013 |
20130178515 | PREDICTIVE MARKERS FOR TAXANE RESPONSIVENESS AND METHODS OF USE THEREOF - Taxanes are widely used in the treatment of breast cancer, although there are currently no validated predictive markers for taxane responsiveness. While the mechanism by which taxanes induce mitotic arrest is well documented, the signaling pathway that links mitotic arrest to cell death, is ill-defined. As described herein, the BH3-only protein Bad and Bik are prognostic indicators for overall survival after adjuvant taxane chemotherapy and a predictive marker for taxane responsiveness. | 07-11-2013 |
20130261173 | CYCLODEXTRIN-BASED POLYMERS FOR THERAPEUTIC DELIVERY - Methods and compositions relating to CDP-taxane conjugates are described herein. | 10-03-2013 |
20130310447 | PHARMACEUTICAL COMPOSITION OF TAXOIDS - The present invention relates to a stable oral pharmaceutical composition with improved solubility and bioavailability; comprising a taxoid, a solubilizer, a stabilizing agent, a surfactant(s), a solvent(s), and an oil wherein the concentration of taxoid is in the range of 0.1 to 10%. | 11-21-2013 |
20130324594 | METHODS AND COMPOSITIONS FOR PREVENTING AND TREATING AUDITORY DYSFUNCTIONS - The invention provides methods for treating auditory impairments in a subject in need of treatment comprising administering to said subject an effective amount of a composition comprising, as an active agent, one or more of a carboxy alkyl ester, a quinic acid derivative, a caffeic acid derivative, a ferulic acid derivative, or a quinic acid lactone or derivative thereof or pharmaceutically acceptable salt thereof and an acceptable carrier or excipient, so as to treat auditory impairments in the subject. | 12-05-2013 |
20130331443 | MULTI-ARM POLYMERIC PRODRUG CONJUGATES OF TAXANE-BASED COMPOUNDS - Among other aspects, provided herein are multi-arm polymeric prodrug conjugates of taxane-based compounds and/or fluorinated forms thereof. Methods of preparing such conjugates as well as methods of administering the conjugates are also provided. Upon administration to a patient, release of the taxane-based compound is achieved. | 12-12-2013 |
20130338216 | DEUTERATED AND/OR FLUORINATED TAXANE DERIVATIVES - The invention relates to (among other things) deuterated and/or fluorinated docetaxel and cabazitaxel and derivatives thereof, as well as compositions comprising each of the foregoing. | 12-19-2013 |
20130345296 | Compositions Comprising a Taxane for Coating Medical Devices - The present invention relates a pharmaceutical composition comprising a taxane and an inhibitory compound capable of inhibiting the enzyme acetaldehyde dehydrogenase e.g. disulfiram. The pharmaceutical compositions of the invention can be used to coat medical devices such as implants. Such implant can be an expansible hollow part, having at least one opening, which consists of an elastic biocompatible material that comprises elongated micro-cavities in its surface. Medical devices coated with a pharmaceutical composition of the invention exhibit an enhanced transfer of taxane from the surface of said medical device into the target tissue. | 12-26-2013 |
20130345297 | METHOD FOR STABILIZING AMPHIPHILIC BLOCK COPOLYMER MICELLE COMPOSITION CONTAINING POORLY WATER-SOLUBLE DRUG - A method for stabilizing a poorly water-soluble drug-containing amphiphilic block copolymer micelle composition via simplified steps in short time is described. Also described is a stabilized poorly water-soluble drug-containing amphiphilic block copolymer micelle composition having improved stability. | 12-26-2013 |
20130345298 | Multi-Arm Polymeric Prodrug Conjugates of Cabazitaxel-Based Compounds - Among other aspects, provided herein are multi-arm polymeric prodrug conjugates of cabazitaxel-based compounds. Methods of preparing such conjugates as well as methods of administering the conjugates are also provided. Upon administration to a patient, release of the cabazitaxel-based compound is achieved. | 12-26-2013 |
20140005258 | Delivery of Therapeutic Agents Using Oligonucleotide-Modified Nanoparticles as Carriers | 01-02-2014 |
20140011864 | TRANSITION METAL COMPLEXES OF A BIS[THIOHYDRAZIDE AMIDE] COMPOUND - The present invention is directed to a compound comprising a bis[thiohydrazide amide] or a deprotonated form thereof, complexed to a transition metal cation, wherein the bis[thiohydrazide amide] is represented by Structural Formula (I): or a prodrug, isomer, ester, salt, hydrate, solvate, polymorph or a deprotonated form thereof. The present invention also provides a pharmaceutical composition comprising a compound of the invention and method of use thereof. | 01-09-2014 |
20140011865 | SOLID STATE FORMS OF CABAZITAXEL AND PROCESSES FOR PREPARATION THEREOF - The invention relates to solid state forms of Cabazitaxel, and processes for preparation, via novel synthetic intermediates, thereof, and formulations comprising one or more of the solid state forms of Cabazitaxel. The present invention further provides pharmaceutical compositions comprising one or more of the solid state forms of Cabazitaxel, and a method of treating hormone-refractory prostate cancer. | 01-09-2014 |
20140011866 | AKT PHOSPHORYLATION AT SER473 AS AN INDICATOR FOR TAXANE-BASED CHEMOTHERAPY - Methods for determining whether a cancer patient is likely to benefit from treatment with a taxane compound based on Akt-Ser473 phosphorylation status are provided, together with kits for determining Akt-Ser473 phosphorylation status and methods for improving treatment of a cancer patient that include obtaining a determination of the Akt-Ser473 phosphorylation status of the cancer. | 01-09-2014 |
20140024703 | Novel Block Copolymer, Micelle Preparation, And Anticancer Agent Containing The Same As Active Ingredient - A medicinal preparation is desired which has no harmful side effects such as hypersensitive reaction, heightens the water solubility of a sparingly water-soluble anticancer agent, maintains a high drug concentration in the blood, accumulates a drug in a tumor tissue at a high concentration, heightens the pharmacological effect of the sparingly water-soluble anticancer agent, and diminishes the side effects of the anticancer agent. Provided are: a novel block copolymer which can be a drug carrier having no harmful side effects such as hypersensitive reaction; a micelle preparation in which micelles are formed and which contains a sparingly water-soluble anticancer agent, especially paclitaxel, incorporated in the micelles in an amount necessary for a disease treatment without bonding it to the block copolymer and which can heighten the solubility of the drug in water; and an anticancer agent which comprises the micelle preparation as a medical ingredient, maintains a high concentration in the blood, has more potent drug activity, and is reduced in toxicity. | 01-23-2014 |
20140045926 | CRYSTALLINE FORMS OF CABAZITAXEL - The present invention provides crystalline forms, including an anhydrate form, of cabazitaxel and processes for the preparation of these forms, designated as Forms C1, C2, C3, C4, C5, C6, C7, C8, C8b, C9 and C9p. | 02-13-2014 |
20140045927 | PREPARATIONS OF TAXANES FOR INTRAVENOUS ADMINISTRATION AND THE PREPARATION METHOD THEREOF - The present invention relates to the field of medical technology. More specifically, the present invention relates to a preparation of taxanes for intravenous administration, which consists of two parts: a drug solution and an emulsion. Said drug solution consists of paclitaxel or docetaxel, a pH regulator and a solvent for injection, wherein said solvent for injection is an organic solvent. Said emulsion includes a fat emulsion and is composed of oil for injection, an emulsifier, an antioxidant, an isotonic regulator, a stabilizer, a pH regulator and water for injection. When used, the drug solution at the clinical dosage can be added and mixed homogeneously in the emulsion to perform intravenous drip directly; or the drug solution at the clinical dosage can also be firstly added into the emulsion with no less than 5 times volume of the drug solution and then a predetermined amount of normal saline or glucose solution for injection is added to perform intravenous drip. The preparation of the present invention does not contain solubilizer and has advantages of little toxicity, safety, effectiveness, stability and economy. The fat emulsion is also used as a nutritional replenishment, thus achieving a better therapeutic effect. In addition, the normal saline or glucose solution for injection can be used to replace a considerable amount of the emulsion, which makes the preparation, therefore, not only cost-efficient, but also convenient for transportation and storage in practice. | 02-13-2014 |
20140066495 | TRANSMUCOSAL ADMINISTRATION OF TAXANES - The present invention provides a pharmaceutical composition for delivering an active agent taxane through transmucosal administration, more particularly through the buccal mucosa or sublingual mucosa. The present invention provides a method for treating cancer by buccal or sublingual administration of the pharmaceutical composition to a subject. The pharmaceutical composition comprises a taxane, a non-ionic surfactant, a viscosity enhancing agent, an adhesive agent, and an alcohol solvent at pH 4-6. | 03-06-2014 |
20140080901 | NANOPARTICLE FORMULATIONS AND USES THEREOF - The present invention provides compositions comprising nanoparticles comprising: 1) a drug, such as a hydrophobic drug derivative; and 2) a carrier protein. Also provided are methods of treating diseases (such as cancer) using the compositions, as well as kits and unit dosages. | 03-20-2014 |
20140088181 | Taxane Pro-Emulsion Formulations and Methods Making and Using the Same - Taxane pro-emulsion formulations are provided. Pro-emulsion formulations are dried powders that include a taxane, oil, surfactant and sugar alcohol. Also provided are methods of making and using the pro-emulsion formulations, as well as kits that include the pro-emulsion formulations. | 03-27-2014 |
20140094508 | COMPOSITIONS AND METHODS OF INHIBITING N-ACYLETHANOLAMINE-HYDROLYZING ACID AMIDASE - Compounds and pharmaceutical compositions are contemplated that inhibit N-acyl-ethanolamine-hydrolyzing acid amidase (NAAA) to so increase the concentration of the substrate of NAAA, palmitoylethanolamide (PEA). NAAA inhibition is contemplated to be effective to alleviate conditions associated with a reduced concentration of PEA. Among other uses, various NAAA inhibitors are especially contemplated as therapeutic agents in the treatment of inflammatory diseases. | 04-03-2014 |
20140094509 | NON-AQUEOUS TAXANE NANODISPERSION FORMULATIONS AND METHODS OF USING THE SAME - Non-aqueous, ethanol-free taxane nanodispersion formulations are provided. Nanodispersion formulations of embodiments of the invention include a taxane, an oil, a non-ionic surfactant, a non-aqueous solvent, and an organic acid component, wherein the organic acid component is soluble in the non-aqueous solvent and the amount by weight of non-ionic surfactant is equal to or greater than the amount by weight of non-aqueous solvent. Also provided are methods of using the nanodispersion formulations, as well as kits that include the nanodispersion formulations. Non-aqueous, ethanol-free docetaxel nanodispersion formulations are provided. Nanodispersion formulations of embodiments of the invention include docetaxel, an oil, a non-ionic surfactant, a non-aqueous solvent, and an organic acid which is soluble in the non-aqueous solvent and is substantially free of any conjugate base. Also provided are methods of using the nanodispersion formulations, as well as kits that include the nanodispersion formulations. | 04-03-2014 |
20140094510 | NON-AQUEOUS TAXANE NANODISPERSION FORMULATIONS AND METHODS OF USING THE SAME - Non-aqueous, ethanol-free taxane nanodispersion formulations are provided. Nanodispersion formulations of embodiments of the invention include a taxane, an oil, a non-ionic surfactant, a non-aqueous solvent, and an organic acid component, wherein the organic acid component is soluble in the non-aqueous solvent and the amount by weight of non-ionic surfactant is equal to or greater than the amount by weight of non-aqueous solvent. Also provided are non-aqueous, ethanol-free docetaxel nanodispersion formulations. Nanodispersion formulations of embodiments of the invention include docetaxel, an oil, a non-ionic surfactant, a non-aqueous solvent, and an organic acid which is soluble in the non-aqueous solvent and is substantially free of any conjugate base. Also provided are methods of using the nanodispersion formulations, as well as kits that include the nanodispersion formulations. | 04-03-2014 |
20140113961 | MULTI-ARM POLYMERIC ALKANOATE CONJUGATES - Among other aspects, provided herein are multi-armed polymer conjugates comprising an alkanoate-linker, compositions comprising such conjugates, and related methods of making and administering the same. Methods of treatment employing such conjugates and related uses are also provided. The conjugates are prepared with high drug loading efficiencies. | 04-24-2014 |
20140135386 | METHOD FOR TREATING ATHEROSCLEROSIS OR RESTENOSIS USING MICROTUBULE STABILIZING AGENT - The present invention is a method of preventing or reducing atherosclerosis or restenosis, and a pharmaceutical preparation used therefore. In particular, it is a method of preventing or reducing atherosclerosis or restenosis after arterial injury by treatment with a low dose of a microtubule stabilizing agent such as taxol or a water soluble taxol derivative. The low dose used in the present invention prevents artery blockage while minimizing any negative side effects associated with the drug. | 05-15-2014 |
20140142165 | THERAPEUTIC PARTICLES SUITABLE FOR PARENTERAL ADMINISTRATION AND METHODS OF MAKING AND USING SAME - Disclosed herein are therapeutic compositions for treating and preventing diseases such as neointimal hyperplasia (NIH), where the compositions comprise a therapeutic particle that has a localized association with a blood vessel and a therapeutic agent, such as an anti-NIH agent. Methods of use of the therapeutic compositions are also disclosed. | 05-22-2014 |
20140142166 | COMPOSITION AND METHOD FOR DELIVERY OF HYDROPHOBIC ACTIVE AGENTS - Disclosed herein is a delivery composition for administering a hydrophobic active agent. In one embodiment, a delivery composition for local administration of a hydrophobic active agent to a tissue or organ of a patient is disclosed. In one embodiment, the delivery composition includes a cationic delivery agent, a therapeutically effective amount of a hydrophobic active agent and a pharmaceutically acceptable aqueous carrier. In one embodiment, the cationic delivery agent includes polyethyleneimine (PEI). In a more specific embodiment, the cationic delivery agent includes branched PEI. Methods of making the delivery composition, as well as kits and methods of use are also disclosed. | 05-22-2014 |
20140142167 | Micellar Preparation Containing Sparingly Water-Soluble Anticancer Agent And Novel Block Copolymer - Micellar preparation in which the solubility of a sparingly water-soluble anticancer agent has been heightened and which after intravenous administration, enables a high blood concentration to be maintained. The preparation has high medicinal activity and/or reduced side effects, and is formed from a block copolymer represented by formula (1): | 05-22-2014 |
20140142168 | METHODS AND PHARMACEUTICAL COMPOSITIONS FOR THE TREATMENT OF HORMONE-REFRACTORY PROSTATE CANCERS - The present invention relates to a combination of a curcuminoid and a taxane for use in the treatment of a hormone-refractory prostate cancer (HRPC) in a patient in need thereof. | 05-22-2014 |
20140155477 | SUBSTITUTED BIARYL SULFONAMIDES AND THE USE THEREOF - Provided herein are substituted biaryl sulfonamide compounds, pharmaceutical compositions comprising the compounds, methods of their preparation, and methods of their use. The compounds provided herein are useful for the treatment, prevention, and/or amelioration of various disorders, including cancer and proliferative disorders. In one embodiment, the compounds provided herein modulate initiation of protein translation. In one embodiment, the compounds provided herein are used in combination with surgery, radiation therapy, immuno therapy and/or one or more additional anticancer drugs for the treatment, prevention, and/or amelioration of cancer and proliferative disorders. | 06-05-2014 |
20140163094 | BETA-LACTONES AS ANTIBACTERIAL AGENTS - The present invention relates to specific beta-lactone compounds and compositions thereof for the treatment of infections, such as, e.g., infections with bacteria or infections with protozoa, in particular infections with Gram-positive and/or Gram-negative bacteria and of infectious diseases caused by or related to Gram-positive and/or Gram-negative bacteria, and to the modulation of virulence of Gram-positive and/or Gram-negative bacteria or of protozoa by specific beta-lactone compounds. The invention further relates to the use of the compounds or compositions for preventing or eliminating biofilms. | 06-12-2014 |
20140171495 | STABLE PHARMACEUTICAL FORMULATION OF CABAZITAXEL - The present invention relates to a stable liquid cabazitaxel formulation in an enclosed container. The enclosed container comprises a liquid phase and an gaseous phase, wherein the liquid phase comprises cabazitaxel, polysorbate 80, ethanol, and one or more pH adjusters to maintain pH about 2.8-6.0, and the gaseous phase is saturated with CO | 06-19-2014 |
20140206759 | PROCESS FOR THE PRODUCTION OF BIODEGRADEABLE, FUNCTIONALISED POLYMER PARTICLES, AND USE THEREOF AS PHARMACEUTICAL SUPPORTS - The invention relates to a method for producing biodegradable, functionalised polymer particles, and to the use of the same as medicament carriers. | 07-24-2014 |
20140213641 | POLYMERIC NANOPARTICLES FOR DRUG DELIVERY - Disclosed are nanoparticles comprising a block copolymer and optionally one or more active agent(s), compositions comprising said nanoparticles and methods of preparing said nanoparticles. The block copolymer comprises blocks (i) a first polymer that is a polyester or polyamide and (ii) a second polymer comprising a hydrocarbon chain containing ester or ether bonds with hydroxyl number ≧10. The active agent(s) may be present within the nanoparticles or on the surfaces of the nanoparticles. The nanoparticles may optionally be associated with a surface-modifying moiety such that they are useful as drug delivery and molecular imaging devices. The surface-modifying moiety may target the nanoparticles to a desired target, cell, tissue or biomarker. | 07-31-2014 |
20140235706 | CANCER CELL TARGETING USING NANOPARTICLES - The present invention generally relates to polymers and macromolecules, in particular, to polymers useful in particles such as nanoparticles. One aspect of the invention is directed to a method of developing nanoparticles with desired properties. In one set of embodiments, the method includes producing libraries of nanoparticles having highly controlled properties, which can be formed by mixing together two or more macromolecules in different ratios. One or more of the macromolecules may be a polymeric conjugate of a moiety to a biocompatible polymer. In some cases, the nanoparticle may contain a drug. Other aspects of the invention are directed to methods using nanoparticle libraries. | 08-21-2014 |
20140303240 | CRYTALLINE FORM OF 13-[(N-TERT-BUTOXYCARBONYL)-2'-O-HEXANOYL-3-PHENYLISOSERINYL]-10-DEACETYL- BACCATIN III - A crystalline from of 13[(N-tert-butoxycarbonyl)-2′-O-hexanoyl-3-phenylisoserinyl]-10-deacetylbaccatin III. | 10-09-2014 |
20140329892 | ADMINISTRATION OF A BIS(THIOHYDRAZIDE AMIDE) COMPOUND FOR TREATING CANCERS - Administration of a bis(thiohydrazide amide) compound is found to be surprisingly effective at treating subjects with cancer. Methods of treating a subject with cancer comprising continuously administering a bis(thiohydrazide amide) compound, or administering a bis(thiohydrazide amide) compound such that a constant concentration of the compound is achieved in the subject, are disclosed. | 11-06-2014 |
20140336246 | PROCESS FOR PREPARING AMORPHOUS CABAZITAXEL - The present invention provides a non-solvated amorphous form of (2α,5β,7β,10β,13α)-4-acetoxy-13-({(2R,3S)-3[ (tert-butoxy carbonyl) amino]-2-hydroxy-3-phenylpropanoyl}oxy)-1-hydroxy-7,10-dimethoxy-9-oxo-5,20-epoxytax-11-en-2-yl benzoate or Cabazitaxel (I), | 11-13-2014 |
20140343133 | CRYSTALLINE FORM OF CABAZITAXEL AND PROCESS FOR PREPARING THE SAME - The present invention relates to a novel crystalline ethyl acetate solvate form of cabazitaxel or 4α-acetoxy-2α-benzoyloxy-5β,20-epoxy-1β-hydroxy-7β,10β-dimethoxy-9-oxo-11-taxen-13α-yl(2R,3S)-3-tert-butoxycarbonylamino-2-hydroxy-3-phenylpropionate and process for preparing the same. | 11-20-2014 |
20140357706 | Stearate Compounds - Preparation and methods of treating and preventing visceral adiposity and cancer are provided involving the administration of stearate to a subject. It has been unexpectedly discovered that the fatty acid stearate, when introduced in the diet, reduces the amount of visceral fat in the body without decreasing overall body weight or causing measurable negative side effects. It has also been unexpectedly discovered that dietary stearate prevents cancer in healthy subjects and reduces both tumor size and metastasis in subjects already afflicted with cancer. | 12-04-2014 |
20150018412 | HIGH THROUGHPUT FABRICATION OF NANOPARTICLES - This application provides a high throughput method of making nanoparticles that utilizes plates comprising wells (e.g., 96-well plates). | 01-15-2015 |
20150031758 | TRANSITION METAL COMPLEXES OF A BIS[THIOHYDRAZIDE AMIDE] COMPOUND - The present invention is directed to a compound comprising a bis[thiohydrazide amide] or a deprotonated form thereof, complexed to a transition metal cation, wherein the bis[thiohydrazide amide] is represented by Structural Formula (I): or a prodrug, isomer, ester, salt, hydrate, solvate, polymorph or a deprotonated form thereof. The present invention also provides a pharmaceutical composition comprising a compound of the invention and method of use thereof. | 01-29-2015 |
20150038564 | SOLID STATE FORMS OF CABAZITAXEL AND PROCESSES FOR PREPARATION THEREOF - The invention relates to solid state forms of Cabazitaxel and processes for preparing the solid state forms. The invention further relates to pharmaceutical compositions and formulations comprising one or more of the solid state forms. | 02-05-2015 |
20150045419 | REVERSIBLY CROSSLINKED MICELLE SYSTEMS - The present invention provides amphiphilic telodendrimers that aggregate to form nanocarriers characterized by a hydrophobic core and a hydrophilic exterior. The nanocarrier core may include amphiphilic functionality such as cholic acid or cholic acid derivatives, and the exterior may include branched or linear poly(ethylene glycol) segments. Nanocarrier cargo such as hydrophobic drugs and other materials may be sequester in the core via non-covalent means or may be covalently bound to the telodendrimer building blocks. Telodendrimer structure may be tailored to alter loading properties, interactions with materials such as biological membranes, and other characteristics. | 02-12-2015 |
20150051269 | Drug Delivery Conjugate Capable of Controlled Release, and Use Thereof - The present invention relates to a hydrophobic drug delivery conjugate, to which cyclodextrin, poly(maleic anhydride), and a hydrophobic drug are bonded, and to a pharmaceutical composition comprising the hydrophobic drug delivery conjugate as an active ingredient. The hydrophobic drug delivery conjugate according to the present invention can effectively control the release rate and the delivery rate of a hydrophobic drug by regulating the physicochemical bonding and/or composition of the cyclodextrin, poly(maleic anhydride), and hydrophobic drug, and can also increase the effect of the drug by significantly increasing the solubility of the hydrophobic drug. Further, the present invention can enable the type of the hydrophobic drug to be varied, as well as a peptide having target directivity to be introduced into a surface of the conjugate, such that the present invention can be applied to the treatment of various diseases in addition to cancer treatment. | 02-19-2015 |
20150094361 | NON-AQUEOUS TAXANE FORMULATIONS AND METHODS OF USING THE SAME - Non-aqueous, ethanol-free taxane formulations are provided. Formulations of embodiments of the invention include a taxane, an oil, a non-ionic surfactant, a non-aqueous solvent, and an organic acid component, wherein the organic acid component is soluble in the non-aqueous solvent and the amount by weight of non-ionic surfactant is equal to or greater than the amount by weight of non-aqueous solvent. Also provided are methods of using the formulations, as well as kits that include the formulations. Non-aqueous, ethanol-free docetaxel formulations are provided. Formulations of embodiments of the invention include docetaxel, an oil, a non-ionic surfactant, a non-aqueous solvent, and an organic acid which is soluble in the non-aqueous solvent and is substantially free of any conjugate base. Also provided are methods of using the formulations, as well as kits that include the formulations. | 04-02-2015 |
20150094362 | ANTI-CXCR1 COMPOSITIONS AND METHODS - The present invention provides methods of treating cancer by administering an IL8-CXCR1 pathway inhibitor (e.g., an anti-CXCR1 antibody or Repertaxin) alone or in combination with an additional chemotherapeutic agent such that non-tumorigenic and tumorigenic cancer cells in a subject are killed. The present invention also provides compositions and methods for detecting the presence of and isolating solid tumor stem cells in a patient (e.g., based on the presence of CXCR1 or FBXO21). | 04-02-2015 |
20150099800 | NOVEL LIPASE INHIBITORS, REPORTER SUBSTRATES AND USES THEREOF - The invention provides for novel lipase inhibitors, and compositions and devices comprising the same. The invention further provides for methods for treatment of disorders comprising administration of novel diacylglycerol lipase inhibitors, and compositions and devices comprising said inhibitors. In some embodiments, the disorders are pancreatitis, obesity, shock or pancreatic necrosis. The invention further provides for novel ether lipid reporter compounds and methods of assaying enzymatic activity comprising contacting a compound with a novel ether lipid reporter compound. | 04-09-2015 |
20150111960 | NOVEL FORMULATIONS OF PHARMACOLOGICAL AGENTS, METHODS FOR THE PREPARATION THEREOF AND METHODS FOR THE USE THEREOF - In accordance with the present invention, there are provided compositions and methods useful for the in vivo delivery of substantially water insoluble pharmacologically active agents (such as the anticancer drug paclitaxel) in which the pharmacologically active agent is delivered in the form of suspended particles coated with protein (which acts as a stabilizing agent). In particular, protein and pharmacologically active agent in a biocompatible dispersing medium are subjected to high shear, in the absence of any conventional surfactants, and also in the absence of any polymeric core material for the particles. The procedure yields particles with a diameter of less than about 1 micron. The use of specific composition and preparation conditions (e.g., addition of a polar solvent to the organic phase), and careful selection of the proper organic phase and phase fraction, enables the reproducible production of unusually small nanoparticles of less than 200 nm diameter, which can be sterile-filtered. The particulate system produced according to the invention can be converted into a redispersible dry powder comprising nanoparticles of water-insoluble drug coated with a protein, and free protein to which molecules of the pharmacological agent are bound. This results in a unique delivery system, in which part of the pharmacologically active agent is readily bioavailable (in the form of molecules bound to the protein), and part of the agent is present within particles without any polymeric matrix therein. | 04-23-2015 |
20150126594 | LIQUID COMPOSITION CONTAINING TAXANE-BASED ACTIVE INGREDIENT, PROCESS FOR PRODUCING SAME, AND LIQUID PREPARATION - A liquid composition which includes a taxane-based active ingredient (a) selected from the group consisting of docetaxel and a derivative thereof; at least one glycol (b); and at least one surfactant component (c) selected from the group consisting of a polysorbate, a polyoxyethylene glycol ester, and a polyoxyethylene castor oil derivative, in which a volume ratio of the glycol (b) to the surfactant component (c) is in a range of form 45/55 to 55/45, and a total content of the glycol (b) and the surfactant component (c) with respect to a total volume of the liquid composition is 95% (v/v) or more. | 05-07-2015 |
20150133534 | MULTI-ARM POLYMERIC ALKANOATE CONJUGATES - Among other aspects, provided herein are multi-armed polymer conjugates comprising an alkanoate-linker, compositions comprising such conjugates, and related methods of making and administering the same. Methods of treatment employing such conjugates and related uses are also provided. The conjugates are prepared with high drug loading efficiencies. | 05-14-2015 |
20150290130 | PREPARATION METHOD OF POLYMERIC MICELLES COMPOSITION CONTAINING A POORLY WATER-SOLUBLE DRUG - Provided is a method for preparing a drug-containing polymeric micelle composition, which includes: dissolving a drug and an amphiphilic block copolymer into an organic solvent; and adding an aqueous solution to the resultant mixture in the organic solvent to form polymeric micelles, wherein the method requires no separate operation to remove the organic solvent prior to the formation of micelles. The method for preparing a drug-containing polymeric micelle composition is simple, reduces the processing time, and is amenable to mass production. | 10-15-2015 |
20150297554 | TRANSMUCOSAL TAXANE COMPOSITION - The present invention provides a pharmaceutical composition for delivering an active agent taxane through transmucosal administration, more particularly through the buccal mucosa or sublingual mucosa. The present invention provides a method for treating cancer by buccal or sublingual administration of the pharmaceutical composition to a subject. The pharmaceutical composition comprises a taxane, a non-ionic surfactant, a viscosity enhancing agent, an adhesive agent, and an alcohol solvent at pH 4-6. | 10-22-2015 |
20150315164 | PROCESS FOR PREPARING AMORPHOUS CABAZITAXEL - The present invention provides a process for preparing amorphous Cabazitaxel from the solvate form of Cabazitaxel. | 11-05-2015 |
20150328321 | CABAZITAXEL COMPOSITION - The present invention is directed to a composition comprising (a) cabazitaxel and (b) sulfobutyl ether beta cyclodextrin. Such composition exhibits unexpectedly desirable stability in aqueous media, permitting therapeutic dosages of the drug to be administered without the use of either ethanol or surfactants. | 11-19-2015 |
20150359777 | PREPARATION METHOD OF POLYMERIC MICELLAR NANOPARTICLES COMPOSITION CONTAINING A POORLY WATER-SOLUBLE DRUG - Provided is a method for preparing a poorly water-soluble drug-containing polymeric micellar nanoparticle composition, which includes: dissolving a poorly water-soluble drug, a salt of polylactic acid or polylactic acid derivative, whose carboxylic acid end is bound to an alkali metal ion, and an amphiphilic block copolymer into an organic solvent; and adding an aqueous solution to the resultant mixture in the organic solvent to form micelles, wherein the method requires no separate operation to remove the organic solvent prior to the formation of micelles. The method for preparing a poorly water-soluble drug-containing polymeric micellar nanoparticle composition is simple, reduces the processing time, and is amenable to mass production. | 12-17-2015 |
20150366806 | Method of Engineering Nanoparticle - The present invention relates to methods to guide the engineering of nanoparticle drugs for intravenous administration based on various pharmacokinetic parameters and other tests. The methods of the present invention have particular use in formulating nanoparticles containing cytotoxic drugs for the treatment of cancer. The guiding principles are properties which facilitate the release of drugs into the patient including unstable in plasma/blood, low AUC, low C | 12-24-2015 |
20160016899 | SUBSTITUTED BIARYL SULFONAMIDES AND THE USE THEREOF - Provided herein are substituted biaryl sulfonamide compounds, pharmaceutical compositions comprising the compounds, methods of their preparation, and methods of their use. The compounds provided herein are useful for the treatment, prevention, and/or amelioration of various disorders, including cancer and proliferative disorders. In one embodiment, the compounds provided herein modulate initiation of protein translation. In one embodiment, the compounds provided herein are used in combination with surgery, radiation therapy, immuno therapy and/or one or more additional anticancer drugs for the treatment, prevention, and/or amelioration of cancer and proliferative disorders. | 01-21-2016 |
20160030575 | TAXOID - PURIFICATION PRINCIPLE FOR LIQUID EXCIPIENTS - The invention relates to taxoid compositions having improved stability. | 02-04-2016 |
20160074360 | COMBINED DRUG ADMINISTRATION OF DALCETRAPIB AND ORLISTAT - The present invention is directed to the combined administration of a thioester therapeutic agent (preferably of formula I) and at least one esterase inhibitor. Also provided are a pharmaceutical composition, package, and a kit comprising the aforementioned active ingredients, as well as a method for increasing the bioavailability of said thioester for the treatment and prophylaxis of a cardiovascular disorder. | 03-17-2016 |
20160120826 | TREATMENT OF CANCER WITH SPECIFIC RXR AGONISTS - A method of treating cancer is disclosed comprising administering to a patient in need of such treatment a RXR agonist at a level below the RAR activating threshold and at or above the RXR effective dose. | 05-05-2016 |
20160120827 | TREATMENT OF CANCER WITH SPECIFIC RXR AGONISTS - A method of treating cancer is disclosed comprising administering to a patient in need of such treatment a RXR agonist at a level below the RAR activating threshold and at or above the RXR effective dose. | 05-05-2016 |
20160160293 | BREAST CANCER TREATMENT WITH TAXANE THERAPY - The application describes methods for screening subjects with breast cancer to determine if the breast cancer will be responsive to a breast cancer therapy including a taxane or a taxane derivative. The application also describes methods for treating subjects with breast cancer by screening them for the likelihood of the effectiveness of treating the cancer with a therapy including a taxane or a taxane derivative and administering the therapy in subjects when it is found that a taxane or a taxane derivative is likely to be effective. | 06-09-2016 |
20160174883 | METHOD FOR THE DIAGNOSIS AND MONITORING OF CHEMOTHERAPY-INDUCED PERIPHERAL NEUROPATHY | 06-23-2016 |
20160201137 | METHODS AND KITS FOR THE MOLECULAR SUBTYPING OF TUMORS | 07-14-2016 |
20180021295 | METHODS AND MATERIALS FOR ASSESSING CHEMOTHERAPY RESPONSIVENESS AND TREATING CANCER | 01-25-2018 |