Entries |
Document | Title | Date |
20080200433 | Molecular Chaperone Function Regulator - According to the present invention, a molecular chaperone function regulator containing a quinazoline derivative represented by the following formula (I) | 08-21-2008 |
20080200434 | Chemical Target-Binding Compositions - Herein is described compositions and methods for modulating and regulating the concentration of a chemical target in an organism or in an ecosystem. In one embodiment, the concentration is regulated such that it is maintained below or above a certain threshold, thus avoiding toxic or harmful effects of the chemical target. The described compositions may, for example, be implanted in a human body or placed in the ecosystem. The compositions comprise binding moieties that reversibly bind to a chemical target in the organism or ecosystem. The binding capacity and the binding constants for a chemical target are designed such that the composition maintains the concentration of the chemical target substantially within a beneficial range of concentrations. | 08-21-2008 |
20080214501 | BRUTON'S TYROSINE KINASE ACTIVITY PROBE AND METHOD OF USING - Described herein are probes for Bruton's tyrosine kinase (Btk). Such probes are used to characterize and develop Btk-selective inhibitors intended for therapeutic use. | 09-04-2008 |
20080221067 | Wood preservative composition - A wood preservative composition comprising a mixture of a fungicide which is a combination of a boric acid ester, which is soluble in an organic solvent and has a sterically hindered di-alcohol or tri-alcohol group, such as trihexylene glycol biborate, an organo-iodine compound, a triazole, and a synthetic pyrethroid insecticide, said fungicide and the insecticide being present in a sufficient amount that wood treated with the wood treatment material contains fungicide and insecticide in an amount of about 1 ppm to 5000 ppm, based on the weight of the wood after treatment. | 09-11-2008 |
20080221068 | ANTI-TUMOR AGENTS - A method for treating subjects with abnormal cell proliferation is provided. The method involves administering to subjects in need of such treatment an effective amount of an agent of Formula I, to inhibit cell proliferation such as that associated with tumor growth and metastasis. A method for inhibiting angiogenesis in an abnormal proliferative cell mass by the administration of an agent of Formula I is also provided. | 09-11-2008 |
20080221069 | Novel Therapeutic Agents for the Treatment of Cancer, Metabolic Diseases and Skin Disorders - The present invention is directed to novel compounds according to formula (I) wherein R | 09-11-2008 |
20080234228 | Boronic acid salts - Salts of a peptide boronic add drug, for example of Cbz-(R)-Phe-(S)-Pro-(R)-Mpg-B(OH) | 09-25-2008 |
20080234229 | Novel Therapeutic Agents for the Treatment of Cancer, Metabolic Diseases and Skin Disorders - The present invention is directed to compounds having the structure Formula (I) wherein R | 09-25-2008 |
20080261921 | FUSED RING HETEROCYCLE KINASE MODULATORS - The present invention provides fused ring heterocycles as kinase modulators, pharmaceutical compositions containing these modulators, and methods of using these modulators to treat diseases mediated by kinase activity. | 10-23-2008 |
20080280856 | Fibroblast Activation Protein Inhibitor Compounds and Methods - Amino terminus-blocked peptide boronate compounds of Formulas I and II are useful for inhibiting Fibroblast Activation Protein (FAP) and other proteases, and for treating disorders mediated by FAP. Methods of using the amino terminus blocked peptide boronate compounds, and stereoisomers, tautomers, solvates and pharmaceutically acceptable salts thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed. | 11-13-2008 |
20080287394 | Hiv Integrase Inhibitors - Hydroxy-substituted pyrazinopyrrolopyridazine dione compounds are inhibitors of HIV integrase and inhibitors of HIV replication. In one embodiment, the dione compounds are of Formula (I) wherein R | 11-20-2008 |
20090005344 | Compounds and Methods of Use Thereof - Imidazole and benzimidazole boronic acid compounds, analogs thereof, and pharmaceutical formulations are described, along with methods of use thereof for inhibiting inflammatory cytokines such as tumor necrosis factor alpha (TNF-α) in a subject in need thereof. | 01-01-2009 |
20090012044 | Novel Hiv Protease Inhibitors - The present invention provides novel HIV protease inhibitors containing substituted borane, carborane or metallacarborane clusters with 6 to 12 boron atoms in each cluster. The charge of each borane, carborane or metallacarborane cluster is 0, −1 or −2. The number of borane, carborane or metallacarborane clusters in the inhibitor molecule is 1 to 9, and the carborane clusters in metallacarborane inhibitors are coordinated to transition metal atom, selected from the group containing cobalt, iron, nickel and ruthenium. In the cluster, heteroatoms can be present, such as nitrogen, phosphorus, silicon, germanium, tin and sulphur. The present invention covers pharmaceutical compositions containing these inhibitors and their use, both in vitro and in vivo. They are characterized by high effectiveness and stability. | 01-08-2009 |
20090018104 | Triarylcarboxylic Acid Derivative - Provided is a triarylcarboxylic acid derivative, or an isomer, a prodrug, a hydrate, a solvate, a polymorph, or a pharmaceutically acceptable salt thereof, represented by the following general formula (I): | 01-15-2009 |
20090042836 | Proteasome inhibitors - The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases. | 02-12-2009 |
20090042837 | LEPTOMYCIN COMPOUNDS - Leptomycin-type compounds according to formula I | 02-12-2009 |
20090062235 | Inhibitors of Dipeptidylpeptidase IV - The present invention relates to inhibitors of post-proline cleaving enzymes, such as inhibitors of dipeptidyl peptidase IV, as well as pharmaceutical compositions thereof, and methods for using such inhibitors. In particular, the inhibitors of the present invention are improved over those in the prior art by selection of particular classes of sidechains in the P1 and/or P2 position of the inhibitor that contain a carboxylic acid moiety. The compounds of the present invention can have a better therapeutic index, owing in part to reduced toxicity and/or improved specificity for the targeted protease. | 03-05-2009 |
20090069271 | WOOD TREATMENT - A method of introducing boron as a boron ester into timber via a non-aqueous liquid medium. The borate ester may have the formula I: (R | 03-12-2009 |
20090075936 | Proteasome inhibitors and methods of using the same - The present invention provides boronic acid compounds, boronic esters, and compositions thereof that can modulate apoptosis such as by inhibition of proteasome activity. The compounds and compositions can be used in methods of inducing apoptosis and treating diseases such as cancer and other disorders associated directly or indirectly with proteasome activity. | 03-19-2009 |
20090082309 | Method of Regulating Glucose Metabolism, and Reagents Related Thereto - The present invention provides methods and compositions for modification and regulation of glucose and lipid metabolism, generally to reduce insulin resistance, hyperglycemia, hyperinsulinemia, obesity, hyperlipidemia, hyperlipoprotein-emia (such as chylomicrons, VLDL and LDL), and to regulate body fat and more generally lipid stores, and, more generally, for the improvement of metabolism disorders, especially those associated with diabetes, obesity and/or atherosclerosis. | 03-26-2009 |
20090093443 | COMBINATIONS OF 4- BROMO-2-(4-CHLOROPHENYL)-5-(TRIFLUOROMETHYL)-1H-PYRROLE-3-CARBONITRILE AND BIOCIDAL COMPOUNDS - The present invention relates to combinations of 4-bromo-2-(4-chloro-phenyl)-5-(trifluoromethyl)-1H-pyrrole-3-carbonitrile, or a salt thereof, and a biocidal compound which provide an improved protecting effect against fouling organisms. More particularly, the present invention relates to compositions comprising a combination of 4-bromo-2-(4-chlorophenyl)-5-(trifluoromethyl)-1H-pyrrole-3-carbonitrile, or a salt thereof, together with one or more biocidal compounds selected from (4-isopropyl-pyridinio)methyldiphenylboron, triphenylboron pyridine, benzalkonium chloride, capsaicine, clonidine, fenazaquin, glutaric dialdehyde, menadione sodium bisulfite, menadione piperazine bisulfite, menadione triaminetriazine bisulfite, menthol or a derivative thereof, N,N-bis(3-aminopropyl)dodecylamine, coco(fractionated)benzyldimethylammonium chloride, peracetic acid, pyridaben, tebufenpyrad, and zosteric acid; in respective proportions to provide a synergistic effect against fouling organisms and the use of these compositions for protecting materials against fouling organisms. | 04-09-2009 |
20090099131 | INHIBITORS OF FATTY ACID AMIDE HYDROLASE - The present invention provide compounds, and pharmaceutical compositions thereof, encompassed by the formulae (I), (II) or (III). | 04-16-2009 |
20090099132 | Proteasome inhibitors - The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases. | 04-16-2009 |
20090124577 | Intermediate Compounds for the Preparation of an Angiotensin II Receptor Antagonist - It comprises new substituted 4-valinylmethylphenyl boronic acids of formula (II) and their derivatives and also its preparation process. It also comprises a preparation process of Valsartan (I) from such intermediates. The process comprises the reaction of the new 4-valinylmethylphenyl boronic compounds with a (halophenyl)tetrazole compound which proceeds with high yields. The process is particularly advantageous in its practical industrial realization because it avoids the use of azide derivatives and also the use of expensive biphenyl intermediates. | 05-14-2009 |
20090124578 | SPIRO-OXAZOLIDINONE COMPOUNDS AND THEIR USE AS METABOTROPIC GLUTAMATE RECEPTOR POTENTIATORS - Compounds in accord with Formula I: | 05-14-2009 |
20090131366 | Use of Amine-Borane Compounds as Anti-Microbial Agents - Use of amine-borane compounds such as amine cyanoboranes and amino carboxy boranes in the treatment of medical conditions associated with pathogenic microorganisms and particularly against drug-resistant microorganisms, in the treatment of fungal and protozoal infections is disclosed. Use of amine-borane compounds for reducing the load of microorganisms in various substrates and products is further disclosed. | 05-21-2009 |
20090131367 | Combinations of HDAC Inhibitors and Proteasome Inhibitors - Provided herein are pharmaceutical agents, pharmaceutical compositions, methods of treatment, treatment regimens and kits for the treatment of cancer. | 05-21-2009 |
20090176739 | OPTICAL ISOMERS OF AN ILOPERIDONE METABOLITE - The present invention relates to novel isomers of a metabolite of Iloperidone, their preparation, their use as pharmaceuticals and pharmaceutical compositions containing them. | 07-09-2009 |
20090209491 | Lactams as conformationally constrained peptidomimetic inhibitors - The present invention relates to inhibitors of post-proline cleaving enzyme, such as inhibitors of dipeptidyl peptidase IV, as well as pharmaceutical compositions thereof, and methods for using such inhibitors. In particular, the inhibitors of the present invention incorporate a lactam ring in the backbone of the inhibitors. The compounds of the present invention can have a better therapeutic index, owing in part to reduced toxicity and/or improved specificity for the target protease. | 08-20-2009 |
20090209492 | Lipase Inhibitors - The present invention relates to inhibitors of lipases, such as inhibitors of endothelial lipase, as well as pharmaceutical compositions thereof, and methods for using such inhibitors. The prototype of these inhibitors has lipophilic portion and an electrophilic site. | 08-20-2009 |
20090221527 | TUMOR NECROSIS FACTOR INHIBITORS - The present invention is directed to compounds that are allosteric inhibitors of tumor necrosis factor receptor I, compositions comprising such compounds, and methods of using such compounds and compositions thereof in the treatment of TNF-α mediated conditions. | 09-03-2009 |
20090239824 | HYDROLYTICALLY-RESISTANT BORON-CONTAINING THERAPEUTICS AND METHODS OF USE - Compositions and methods of use of borole derivatives, including benzoxaboroles, benzazaboroles and benzthiaboroles, as therapeutic agents for treatment of diseases caused by bacteria or viruses are disclosed, as well as methods for synthesis of said agents and compositions thereof. | 09-24-2009 |
20090253653 | ANALOGS OF BENZOQUINONE-CONTAINING ANSAMYCINS AND METHODS OF USE THEREOF - The present invention provides analogs of benzoquinone-containing ansamycins and uses thereof for treating and modulating disorders associated with hyperproliferation, such as cancer. The present invention provides analogs of benzoquinone-containing ansamycins where the benzoquinone is reduced to a hydroquinone and trapped by reaction with a suitable acid, preferably ones that increase the solubility and air stability of the resulting 17-ammonium hydroquinone ansamycin analog. | 10-08-2009 |
20090264384 | INDOLE, BENZIMIDAZOLE, AND BENZOLACTAM BORONIC ACID COMPOUNDS, ANALOGS THEREOF AND METHODS OF USE THEREOF - Benzimidazole, indole and benzolactam boronic acid compounds, analogs thereof, and pharmaceutical formulations are described, along with methods of use thereof for inhibiting inflammatory cytokines such as tumor necrosis factor alpha (TNF-α) in a subject in need thereof. | 10-22-2009 |
20090291917 | Boron-Containing Small Molecules as Anti-Inflammatory Agents - Compounds and methods of treating anti-inflammatory conditions are disclosed. | 11-26-2009 |
20090291918 | PROTEASOME INHIBITORS AND METHODS OF USING THE SAME - The present invention provides boronic acid compounds, boronic esters, and compositions thereof that can modulate apoptosis such as by inhibition of proteasome activity. The compounds and compositions can be used in methods of inducing apoptosis and treating diseases such as cancer and other disorders associated directly of indirectly with proteasome activity. | 11-26-2009 |
20090312284 | HISTONE DEACETYLASE INHIBITORS WITH COMBINED ACTIVITY ON CLASS-I AND CLASS-IIB HISTONE DEACETYLASES IN COMBINATION WITH PROTEASOME INHIBITORS - The present invention is concerned with combinations of a proteasome inhibitor and a histone deacetylase inhibitor with combined activity on class-I and class-IIb histone deacetylases, for inhibiting the growth of tumor cells, useful in the treatment of cancer. | 12-17-2009 |
20090325903 | BORONATE ESTER COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS THEREOF - The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases. | 12-31-2009 |
20100004204 | ROS-SENSITIVE IRON CHELATORS AND METHODS OF USING THE SAME - The present invention provides compounds of Formula (I): along with compositions containing the same and methods of use thereof in treating oxidative stress. | 01-07-2010 |
20100004205 | PHARMACEUTICAL COMPOSITIONS - Synergistic combinations of a squalene epoxidase inhibitor and a leucyl-tRNA synthetase inhibitor are provided, which are useful in particular in the treatment of diseases involving fungal or suspected fungal infection, for immunomodulation or immunosuppression in conditions in which fungal or suspected fungal colonisation of e.g. the skin or nail plays a role, such as atopic dermatitis, acne vulgaris, seborrhoeic dermatitis, rosacea or onychomycosis, and in situations of fungal resistance. | 01-07-2010 |
20100009934 | BETA ADRENERGIC RECEPTOR AGONISTS FOR THE TREATMENT OF B-CELL PROLIFERATIVE DISORDERS - The invention features a method of treating a B-cell proliferative disorder by administering to a patient a BAR agonist, e.g., formulated for administration by a route other than inhalation (such as for oral or intravenous administration), in an amount effective to treat the B-cell proliferative disorder. The BAR agonist may be administered as a monotherapy or in combination with one or more other agents, e.g., a PDE inhibitor, an A2A receptor agonist, or an antiproliferative compound, in amounts that together are effective to treat the B-cell proliferative disorder. The invention further features pharmaceutical compositions and kits including a BAR agonist, alone or in combination with additional agents, for the treatment of a B-cell proliferative disorder. | 01-14-2010 |
20100041628 | NOVEL INDOLE DERIVATIVE HAVING IKAPPAB KINASE BETA INHIBITORY ACTIVITY - Disclosed is a compound represented by the general formula (1) or a salt thereof. The compound or a salt thereof has an inhibitory activity on IKKβ and is therefore useful as preventive and/or therapeutic agent for a disease associated with IKKβ. In the formula, R | 02-18-2010 |
20100056478 | Useful Combinations of Monobactam Antibiotics With Beta-Lactamase Inhibitors - A pharmaceutically composition, comprising a combination of an antibiotically active compound of the formula (I): with a β-lactamase inhibitor of one of the formulae (II) to (XIII) are active against Gram-negative bacteria, in particular such bacteria which have become resistant against antibiotics such as aztreonam, carumonam and tigemonam. Optionally the compositions may comprise another β-lactamase inhibitor of one of the formulae (II) to (XIII), particularly of formula (V) or formula (VI). | 03-04-2010 |
20100056479 | THE USE OF QUATERNARY AMMONIUM COMPOUNDS IN THE REMEDIATION OF MOLD, MILDEW, AND FUNGUSES - The present invention relates to the use of quaternary ammonium compounds in the remediation of microbial growth such as mold, funguses, and mildew. | 03-04-2010 |
20100056480 | USE OF ARGINASE INHIBITORS IN THE TREATMENT OF ASTHMA AND ALLERGIC RHINITIS - The present invention relates to the use of an arginase inhibitor for the preparation of a medicament for the prophylactic maintenance therapy of an asthmatic or allergic patient by preventing obstruction of upper and lower airways, in particular allergen-induced bronchial obstruction and/or airway hyperresponsiveness. The patients are either asthmatic or have allergic rhinitis. Preferably, the arginase inhibitor is 2(S)-amino-6-boronohexanoic acid (ABH). | 03-04-2010 |
20100069331 | TREATMENT OR PREVENTION OF CANCER AND PRECANCEROUS DISORDERS - The NSAID, sulindac and/or its metabolites and derivatives, in combination with an agent that generates or induces reactive oxygen species (ROS), significantly enhances the killing of abnormal cells but does not affect normal cells. This effect occurs at concentrations of each compound that individually have little or no activity directed against the abnormal cells. | 03-18-2010 |
20100075925 | Hyperthermic Technologies And Therapeutic Uses Thereof - The present invention provides nanoscale and microscale compositions useful for a variety of purposes, including the diagnosis and treatment of diseases. In one embodiment, the present invention provides a disease treatment system comprising a thermal induction agent and a radiation source, wherein the thermal induction agent comprises at least one carbon nanotube, at least one carbon microtube, or a mixture thereof. | 03-25-2010 |
20100081632 | High-content and high throughput assays for identification of lipid-regulating pathways, and novel therapeutic agents for lipid disorders - A method of assaying protein-protein interactions associated with proteins involved in lipid pathways using a protein fragment complementation assays, said method comprising the steps of: (a) identifying protein molecules that interact with said protein associated with lipid pathways; (b) selecting a protein reporter molecule; (c) effecting fragmentation of said protein reporter molecule such that said fragmentation results in reversible loss of reporter function; (d) fusing or attaching fragments of said protein reporter molecule separately to said interacting protein molecules as defined in step (a); (e) transfecting cells with nucleic acid constructs coding for the products of step (d); (f) reassociating said reporter fragments through interactions of the protein molecules that are fused or attached to said fragments; and (g) measuring directly or Indirectly the activity of said reporter molecule resulting from the reassociation of said reporter fragments. | 04-01-2010 |
20100081633 | Derivatives of 1-amino-2-cyclobutylethylboronic acid - The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases. | 04-01-2010 |
20100087396 | Novel Compounds Having Selective Inhibiting Effect at GSK3 - The present invention relates to new compounds of formula I | 04-08-2010 |
20100113392 | METHODS OF USING SAHA AND BORTEZOMIB FOR TREATING MULTIPLE MYELOMA - The present invention relates to a method of treating cancer in a subject in need thereof, by administering to a subject in need thereof a first amount of a histone deacetylase (HDAC) inhibitor such as suberoylanilide hydroxamic acid (SAHA), or a pharmaceutically acceptable salt or hydrate thereof, and a second amount of one or more anti-cancer agents, including Bortezomib. The HDAC inhibitor and the anti-cancer agent may be administered to comprise therapeutically effective amounts. In various aspects, the effect of the HDAC inhibitor and the anti-cancer agent may be additive or synergistic. | 05-06-2010 |
20100113393 | Boronic Acid Salts - Salts of a peptide boronic acid drug, for example of Cbz-(R)-Phe-(S)-Pro-(R)-Mpg-B(OH) | 05-06-2010 |
20100120715 | BETA-LACTAMASE INHIBITORS - Disclosed herein are α-aminoboronic acids and their derivatives which act as inhibitors of beta-lactamases. Also disclosed herein are pharmaceutical compositions comprising α-aminoboronic acids and methods of use thereof. | 05-13-2010 |
20100120716 | MACROCYCLIC HEPATITIS C SERINE PROTEASE INHIBITORS AND USES THEREFOR - Macrocyclic inhibitors of Hepatitis C protease are provided, the inhibitors including a boronic acid or ester group, a macrocyclic ring of about 13 to 25 atoms including at least two amide linkages, a proline-analogous group, and a connecting segment joining moieties on either side of the proline-analogous group. Methods of making the HCV protease-inhibitory compounds, methods of using the compounds, formulations of the compounds, and pharmaceutical combinations including the compounds, are provided. | 05-13-2010 |
20100137246 | Anti-inflammatory compositions and methods - Certain embodiments disclosed relate to compositions, including therapeutic compositions, methods, devices, and systems that modulate at least one inflammatory response or reaction. According to various embodiments, the compositions, methods, devices, and systems relate to modulating one or more of Toll-like receptors, Src family kinases, NF-kB molecules, proteases, or proteasomes. | 06-03-2010 |
20100137247 | Anti-inflammatory compositions and methods - Certain embodiments disclosed relate to compositions, including therapeutic compositions, methods, devices, and systems that modulate at least one inflammatory response or reaction. According to various embodiments, the compositions, methods, devices, and systems relate to modulating one or more of Toll-like receptors, Src family kinases, NF-kB molecules, proteases, or proteasomes. | 06-03-2010 |
20100137248 | BORON-CONTAINING COMPOUNDS, USES AND PREPARATION THEREOF - There are provided compounds of formulas (I) to (XIV) and compositions comprising such compounds. Such compounds and compositions are particularly useful for treating inflammation and/or pain, or for water treatment. | 06-03-2010 |
20100137249 | COMPOSITIONS FOR REGULATING OR MODULATING QUORUM SENSING IN BACTERIA, METHODS OF USING THE COMPOUNDS, AND METHODS OF REGULATING OR MODULATING QUORUM SENSING IN BACTERIA - The present disclosure encompasses compounds and compositions that are useful as specific AI-2 antagonists for the control of bacterial quorum sensing. Although the AI-2 antagonists according to the present disclosure may not have bactericidal effect, their ability to attenuate virulence, drug resistance, and/or biofilm formation have therapeutic benefits. In addition, the AI-2 antagonists of the present disclosure can also be used as tools to probe bacterial AI-2 functions. The present disclosure also encompasses methods for inhibiting or attenuating microbial virulence, biofilm formation, and drug resistance. The methods are suitable for preventing bacteria from accruing and forming extensive biofilms that may be a health or hygiene hazard or a physical issue, such as in the blockage of water or fuel lines. | 06-03-2010 |
20100137250 | NAPHTHYLACETIC ACIDS - The invention is concerned with the compounds of formula I: | 06-03-2010 |
20100144673 | Diagnosis, prognosis and identification of potential therapeutic targets of multiple myeloma based on gene expression profiling - Gene expression profiling is a powerful tool that has varied utility. It enables classification of multiple myeloma into subtypes and identifying genes directly involved in disease pathogensis and clinical manifestation. The present invention used gene expression profiling in large uniformly treated population of patients with myeloma to identify genes associated with poor prognosis. It also demonstrated that over-expression of CKS1B gene, mainly due to gene amplification that was determined by Fluorescent in-situ hybridization to impart a poor prognosis in multiple myleoma. It is further contemplated that therapeutic strategies that directly target CKS1B or related pathways may represent novel, and more specific means of treating high risk myeloma and may prevent its secondary evolution. | 06-10-2010 |
20100152136 | TP53 Gene expression and uses thereof - The present invention is drawn to diagnosis, prognosis and treatment of multiple myeloma. In this regard, the present invention discloses importance of down-regulation of TP3 gene in multiple myeloma and its use as an independent progostic indicator of multiple myeloma. Additionally, the present invention also discloses novel-TP53 associated genes and demonstrates the clinical relevance of these alterations to disease progression. | 06-17-2010 |
20100160257 | USE OF HDAC INHIBITORS FOR THE TREATMENT OF MYELOMA - The present invention relates to the use of an HDAC inhibitor, especially an HDAC inhibitor of formula (I) | 06-24-2010 |
20100168062 | Quinoxaline Derivatives as Tyrosine Kinase Activity Inhibitors - The present invention relates to quinoxaline compound of the formula (I): | 07-01-2010 |
20100190748 | BORON-CONTAINING SMALL MOLECULES - This invention relates to compounds useful for treating fungal infections, more specifically topical treatment of onychomycosis and/or cutaneous fungal infections. This invention is directed to compounds that are active against fungi and have properties that allow the compound, when placed in contact with a patient, to reach the particular part of the skin, nail, hair, claw or hoof infected by the fungus. In particular the present compounds have physiochemical properties that facilitate penetration of the nail plate. | 07-29-2010 |
20100190749 | Benzoxazole kinase inhibitors and methods of use - The present invention provides chemical entities or compounds and pharmaceutical compositions thereof that are capable of modulating certain protein kinases such as mTor, tyrosine kinases, and/or lipid kinases such as PI3 kinase. Also provided in the present invention are methods of using these compositions to modulate activities of one or more of these kinases, especially for therapeutic applications. | 07-29-2010 |
20100190750 | GPR119 Receptor Agonists in Methods of Increasing Bone Mass and of Treating Osteoporosis and Other Conditions Characterized by Low Bone Mass, and Combination Therapy Relating Thereto - The present invention relates to the use of GPR119 receptor agonists for treating or preventing a condition characterized by low bone mass, such as osteoporosis, and for increasing bone mass in an individual. The present invention further relates to the use of a GPR119 receptor agonist in combination with a dipeptidyl peptidase IV (DPP-IV) inhibitor for treating or preventing a condition characterized by low bone mass, such as osteoporosis, and for increasing bone mass in an individual. A GPR119 receptor agonist and the combination of a GPR119 receptor agonist and a DPP-IV inhibitor promote bone formation in an individual. | 07-29-2010 |
20100197634 | INHIBITORS OF JANUS KINASES - The instant invention provides for compounds that inhibit the four known mammalian JAK kinases (JAK1, JAK2, JAK3 and TYK2) and PDK1. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting the activity of JAK1, JAK2, JAK3 TYK2 and PDK1 by administering the compound to a patient in need of treatment for myeloproliferative disorders or cancer. | 08-05-2010 |
20100204180 | PROTEASOME INHIBITORS - The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases. | 08-12-2010 |
20100210593 | Pyridine- and Pyrimidinecarboxamides as CXCR2 Modulators - There is disclosed pyridine- and pyrimidinecarboxamide compounds useful as pharmaceutical agents, synthesis processes, and pharmaceutical compositions which include pyridine- and pyrimidinecarboxamides compounds. More specifically, there is disclosed a genus of CXCR2 inhibitor compounds that are useful for treating a variety of inflammatory and neoplastic disorders. | 08-19-2010 |
20100222301 | TOPICAL DRUG FOR TREATMENT AND/OR PREVENTION OF DIABETIC NEUROPATHY, MICROANGIOPATHY AND DIABETIC AND NON DIABETIC ULCERS AND WOUND INFECTION - The various embodiments herein provide a topical drug composition for the treatment of diabetes-related complications. According to one embodiment herein, the composition comprises of a compound belonging to a group of chemicals containing borates. Boric acid is used as the base material of the drug. Boric acid is dissolved in saline 0.9% or half saline serum or water, distilled water or boiled water to obtain a boric acid solution with given concentration. The best concentration is 3-5% solution. Alcohol at preset concentration is added to the boric acid solution. According to another embodiment, a method is provided for preparing a topical drug composition for the treatment of diabetes-related disorders. | 09-02-2010 |
20100240611 | METHODS FOR PREPARING DPP-IV INHIBITOR COMPOUNDS - Methods for preparing an inhibitor of dipeptidyl peptidase IV, as well as formulations of such inhibitors of dipeptidyl peptidase IV that have a high degree of stability including under warm, humid storage conditions. | 09-23-2010 |
20100249065 | Biomarkers for Assessing Peripheral Neuropathy Response to Cancer Treatment - The present invention provides methods for identifying patients at increased risk of developing an adverse neurological event in response to a cancer treatment. Methods also include modifying the treatment regimen of said patent dependent on the presence or absence of biomarkers in the patient. | 09-30-2010 |
20100249066 | METHODS OF MODULATING INFLAMMATORY CELL RECRUITMENT AND GENE EXPRESSION USING HALOARYL SUBSTITUTED AMINOPURINES - Provided herein are Aminopurine Compounds having the following structure: | 09-30-2010 |
20100261674 | THERAPEUTIC APPLICATIONS OF FATTY ACID AMIDE HYDROLASE INHIBITORS - Fatty acid amide hydrolase (FAAH) is an enzyme responsible for the degradation of oleamide (an endogenous sleep-inducing lipid) and anandamide (an endogenous ligand for cannabinoid receptors). Disclosed herein are potent inhibitors of FAAH and methods for their use for treating a variety of disorder, including hypertension and cardiac hypertrophy. | 10-14-2010 |
20100267671 | COMPOSITIONS AND METHODS FOR APOPTOSIS MODULATORS - The present invention includes and relates generally to compounds which modulate apoptosis in cells. The present invention also provides pharmaceutical compositions containing these compounds, methods of making these compounds, and methods of using these compounds and pharmaceutical compositions for treatment of diseases associated with irregular apoptosis in cells. | 10-21-2010 |
20100286090 | Treatment of Multiple Myeloma - Methods for treating multiple myeloma comprising administering a therapeutically effective amount of dasatinib to a patient in need of treatment thereof. Dasatinib can be administered alone or in combination with a second anti-neoplastic agent such as dexamethasone or bortezomib. The patient may be refractory to prior treatment with an anti-neoplastic agent other than dasatinib. | 11-11-2010 |
20100286091 | IMIDAZOLIDINONE COMPOUNDS, METHODS TO INHIBIT DEUBIQUITINATION AND METHODS OF TREATMENT - The present invention features imidazolidinone compounds and pharmaceutical compositions of imidazolidinone compounds. The compounds of the invention are utilized in methods of treating a deubiquitination-related disorder in a subject and inhibiting p97-associated deubiquitination. | 11-11-2010 |
20100286092 | BETA-LACTAMASE INHIBITORS - Disclosed herein are α-aminoboronic acids and their derivatives which act as inhibitors of beta-lactamases. Also disclosed herein are pharmaceutical compositions comprising α-aminoboronic acids and methods of use thereof. | 11-11-2010 |
20100292185 | BETA-LACTAMASE INHIBITORS - Disclosed herein are α-aminoboronic acids and their derivatives which act as inhibitors of beta-lactamases. Also disclosed herein are pharmaceutical compositions comprising α-aminoboronic acids and methods of use thereof. | 11-18-2010 |
20100298268 | CONTROLLED RELEASE FORMULATIONS OF LEVODOPA AND USES THEREOF - The current invention provides a controlled release oral solid formulation of levodopa comprising levodopa, a decarboxylase inhibitor, and a carboxylic acid. Also provided by this invention is multiparticulate, controlled release oral solid formulations of levodopa comprising: i) a controlled release component comprising a mixture of levodopa, a decarboxylase inhibitor and a rate controlling excipient; ii) a carboxylic acid component; and iii) an immediate release component comprising a mixture of levodopa and a decarboxylase inhibitor. | 11-25-2010 |
20100305067 | ANTIBACTERIAL CONDENSED THIAZOLES - Compound of formula (I) have antibacterial activity: wherein: m is 0 or 1; Q is hydrogen or cyclopropyl; AIk is an optionally substituted, divalent C | 12-02-2010 |
20100317621 | BETA-LACTAMASE INHIBITORS - Disclosed herein are α-aminoboronic acids and their derivatives which act as inhibitors of beta-lactamases. Also disclosed herein are pharmaceutical compositions comprising α-aminoboronic acids and methods of use thereof. | 12-16-2010 |
20100323988 | SOLID CITRATE AND TARTRATE SALTS OF DPP-IV INHIBITORS - This invention relates to DPP-IV inhibitory citrate or tartrate salts of pyrrolidinylaminoacetyl pyrrolid acid compounds that are physically and chemically stable, substantially non-deliquescent solids under ambient conditions. | 12-23-2010 |
20110003771 | Wood Preservative Composition - A wood preservative composition comprising a mixture of a fungicide which is a combination of a boric acid ester, which is soluble in an organic solvent and has a sterically hindered di-alcohol or tri-alcohol group, such as trihexylene glycol biborate, an organo-iodine compound, a triazole, and a synthetic pyrethroid insecticide, said fungicide and the insecticide being present in a sufficient amount that wood treated with the wood treatment material contains fungicide and insecticide in an amount of about 1 ppm to 5000 ppm, based on the weight of the wood after treatment. | 01-06-2011 |
20110021461 | COMBINATIONS TO IMPROVE ANIMAL HEALTH AND PERFORMANCE - The present invention provides combinations of dietary supplements and methods of using of these combinations to improve the health and production performance of animals. In particular, the combinations of the invention comprise antioxidants, trace minerals, organic acids, essential amino acids, and mixtures thereof. | 01-27-2011 |
20110021462 | SUBSTITUTED TETRAHYDRO-2H-ISOQUINOLIN-1-ONE DERIVATIVES, AND METHODS FOR THE PRODUCTION AND USE THEREOF - This invention relates to compounds according to the general formula (I), where the definitions of the substituents R1, R2, Ar and X are as specified in the description, and to their physiologically tolerated salts, methods for the preparation of these compounds and their use as medicaments. | 01-27-2011 |
20110071112 | Compositions and Methods for Preserving Colors and Patterns of Plants - The present invention relates to a composition for preserving plants, which comprises 5 carbon alcohol, at least one alcohol selected from the group consisting of 3 carbon alcohol and 4 carbon alcohol, a thiourea and at least one acid selected from the group consisting of tartaric acid and boric acid. The composition is used to preserve colors, patterns and DNA of plants. The composition can also be used to change colors of flowers. The present invention also relates to a method for preserving plants, which comprises soaking the plants in the composition of the present invention. | 03-24-2011 |
20110071113 | Thiazole Derivatives and Use Thereof - The present invention is related to thiazole derivatives of Formula (I) in particular for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries. | 03-24-2011 |
20110082108 | Peptidomimetic Inhibitors of Post-Proline Cleaving Enzymes - The present invention relates to inhibitors of post-proline cleavage enzymes, such as inhibitors of dipeptidyl peptidase IV, as well as pharmaceutical compositions thereof, and methods for using such inhibitors. In particular, the inhibitors of the present invention are improved over those in the prior art by selection of particular classes of side chains in the P1 and/or P2 position of the inhibitor. The compounds of the present invention can have a better therapeutic index, owing in part to reduced toxicity and/or improved specificity for the targeted protease. | 04-07-2011 |
20110082109 | NOVEL ACYL GUANIDINE DERIVATIVES - The present invention provides a pharmaceutical which possesses an excellent inhibitory effect on NHE3 (Na | 04-07-2011 |
20110086818 | METHODS, COMPOSITIONS, AND KITS FOR TREATING PAIN AND PRURITUS - The invention features methods, compositions, and kits for selective inhibition of pain-and itch sensing neurons (nociceptors and pruriceptors) by drug molecules of small molecule weight, while minimizing effects on non-pain-sensing neurons or other types of cells. | 04-14-2011 |
20110098248 | MODULATORS OF TOLL-LIKE RECEPTORS - The present application includes novel modulators of TLRs, compositions containing such compounds, therapeutic methods that include the administration of such compounds. | 04-28-2011 |
20110105431 | Boronic Acid Aryl Analogs - The present invention relates to novel boronic acid aryl derivatives which are useful as antitumor/anticancer agents. The present compounds, which are inexpensive to synthesize, exhibit unexpectedly good inhibitors of the growth of human breast cancer cells. The present invention also relates to the use of the novel boronic acid aryl derivatives to treat cancer. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment and prevention of cancer. | 05-05-2011 |
20110105432 | AMINOCARBOXYLIC ACID DERIVATIVE AND MEDICINAL USE THEREOF - The present invention relates to a compound represented by the formula (I), a salt thereof, an N-oxide form thereof, a solvate thereof, or a prodrug thereof, and a medicament containing the same. The compound represented by the formula (I) has an ability to bind to an S1P receptor (particularly, EDG-1, EDG-6, and/or EDG-8) and is useful for preventing and/or treating for rejection to transplantation, graft-versus-host disease, autoimmune diseases, allergic diseases, neurodegenerating diseases, and the like. | 05-05-2011 |
20110112051 | Dipeptidyl Peptidase-IV Inhibitors - The present invention relates generally to pyrrolidine and thiazolidine DPP-IV inhibitor compounds. The present invention also provides synthetic methods for preparation of such compounds, methods of inhibiting DPP-IV using such compounds and pharmaceutical formulations containing them for treatment of DPP-IV mediated diseases, in particular, Type-2 diabetes. | 05-12-2011 |
20110118208 | Thiazolyl-Dihydro-Indazoles - The present invention encompasses compounds of general formula (1) | 05-19-2011 |
20110124597 | BORON CONTAINING SMALL MOLECULES - This invention provides, among other things, novel compounds useful for treating bacterial infections, pharmaceutical compositions containing such compounds, as well as combinations of these compounds with at least one additional therapeutically effective agent. | 05-26-2011 |
20110130363 | BENZOPYRAN AND BENZOXEPIN PI3K INHIBITOR COMPOUNDS AND METHODS OF USE - Benzopyran and benzoxepin compounds of Formulas I and II, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formulas I and II for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed. | 06-02-2011 |
20110136763 | TRISUBSTITUTED BORON-CONTAINING MOLECULES - This invention largely relates to 3,4,6-trisubstituted benzoxaborole compounds, and their use for treating bacterial infections. | 06-09-2011 |
20110152217 | POLYMORPHS OF (S)-3-AMINOMETHYL-7-(3-HYDROXY-PROPOXY)-3H-BENZO[C][1,2]OXABOROL-1-OL - This invention provides, among other things, polymorphs of the hydrochloride salt of (S)-3-aminomethyl-7-(3-hydroxy-propoxy)-3H-benzo[c][1,2]oxaborol-1-ol. | 06-23-2011 |
20110160160 | METHODS FOR HEAT SHOCK PROTEIN DEPENDENT CANCER TREATMENT - The present invention provides a method of treating an Hsp70 dependent cancer, including: providing at least one Hsp70 dependent cancer cell; contacting the at least one cell with a sub-effective concentration of a dihydropyrimidinone compound; and contacting the at least one cell with a sub-effective concentration of a proteasome inhibitor, wherein the sub-effective concentration of the dihydropyrimidinone compound and the sub-effective concentration of the proteasome inhibitor have a synergistic effect upon the at least one cell. | 06-30-2011 |
20110166103 | BORON-CONTAINING SMALL MOLECULES - This invention provides, among other things, novel compounds useful for treating inflammatory conditions, pharmaceutical compositions containing such compounds, as well as combinations of these compounds with at least one additional therapeutically effective agent. | 07-07-2011 |
20110166104 | BORON-CONTAINING SMALL MOLECULES - This invention provides, among other things, novel compounds useful for treating inflammatory conditions, pharmaceutical compositions containing such compounds, as well as combinations of these compounds with at least one additional therapeutically effective agent. | 07-07-2011 |
20110172186 | INHIBITORS OF FATTY ACID AMIDE HYDROLASE - The present invention provides compounds, and pharmaceutically acceptable compositions thereof, encompassed by any of formulae (I), (II), (III), (IV), (V), or (VI), or subgenera thereof. The present invention also provides methods for treating an FAAH mediated disease, disorder or condition by administering a therapeutically effective amount of a compound or composition comprising a compound of any of formulae (I), (II), (III), (IV), (V), or (VI), or subgenera thereof, to a patient in need thereof. Additionally, the present invention provides methods for inhibiting FAAH by administering a therapeutically effective amount of a compound or composition comprising a compound of any of formulae (I), (II), (III), (IV), (V), or (VI), or subgenera thereof, to a patient in need thereof. | 07-14-2011 |
20110172187 | BORON-CONTAINING SMALL MOLECULES - This invention relates to, among other items, 6-substituted benzoxaborole compounds and their use for treating bacterial infections. | 07-14-2011 |
20110172188 | USE OF ANTI-CONNEXIN AGENTS FOR MODULATING THE THERAPEUTIC EFFECT OF PSYCHOTROPIC DRUGS - The invention first relates to a product containing at least one connexin-blocking agent and a psychotropic drug as combination products for use simultaneously, separately, or spread over time in patients suffering from psychiatric and/or neurodegenerative disorders. The connexin-blocking agent is advantageously selected from the group comprising meclofenamic acid, 18-β-glycyrrhetinic acid, carbenoxolone, mefloquine, and 2-APB, and preferably consists of meclofenamic acid. The invention first relates to a product containing at least one connexin-blocking agent and a psychotropic drug as combination products for use simultaneously, separately, or spread over time in patients suffering from psychiatric and/or neurodegenerative disorders. The connexin-blocking agent is advantageously selected from the group comprising meclofenamic acid, 18-β-glycyrrhetinic acid, carbenoxolone, mefloquine, and 2-APB, and preferably consists of meclofenamic acid. | 07-14-2011 |
20110172189 | Aryl-Phenyl-Sulfonamido-Cycloalkyl Compounds and Their Use - The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain aryl-phenyl-sulfonamido-cycloalkyl compounds of the following formula (collectively referred to herein as “APSAC compounds”). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, in treatment, for example, of inflammation and/or joint destruction and/or bone loss; of disorders mediated by excessive and/or inappropriate and/or prolonged activation of the immune system; of inflammatory and autoimmune disorders, for example, rheumatoid arthritis, psoriasis, psoriatic arthritis, chronic obstructive pulmonary disease (COPD), atherosclerosis, inflammatory bowel disease, ankylosing spondylitis, and the like; of disorders associated with bone loss, such as bone loss associated with excessive osteoclast activity in rheumatoid arthritis, osteoporosis, cancer-associated bone disease, Paget's disease and the like, etc.; and of cancer, such as a haematological malignancy, a solid tumour, etc. Formula (I). | 07-14-2011 |
20110178040 | METHOD FOR TREATING FIBROSIS AND CANCER WITH IMIDAZOLIUM AND IMIDAZOLINIUM COMPOUNDS - There is presently provided methods for delivering an anti-fibrotic or anti-cancer agent to a cell. The methods comprise contacting a cell with an effective amount of imidazolium and imidazolinium compounds as described herein, including imidazolium and imidazolinium salts. | 07-21-2011 |
20110178041 | HETEROCYCLIC BIARYL DERIVATIVE AND PDE INHIBITOR COMPRISING SAME AS ACTIVE INGREDIENT - Novel heterocyclic biaryl derivatives were disclosed which are useful as pharmaceutical agents and which exhibit a phosphodiesterase-inhibitory action. | 07-21-2011 |
20110190235 | BORON-CONTAINING SMALL MOLECULES AS ANTIPROTOZOAL AGENTS - This invention provides, among other things, novel compounds useful for treating protozoal infections, pharmaceutical compositions containing such compounds, as well as combinations of these compounds with at least one additional therapeutically effective agent. | 08-04-2011 |
20110195931 | METHODS AND COMPOSITIONS FOR REDUCING NEURONAL CELL DEATH - Methods and compositions involving a class of boron-protected phenylphosphine agents having increased cell permeability and having improved chemical stability for treating or for preventing neuronal cell death-related diseases or conditions in a human or a non-human animal. | 08-11-2011 |
20110201574 | FATTY ACID AMIDE HYDROLASE INHIBITORS - The present invention provides fatty acid amide hydrolase inhibitors, solid forms thereof, compositions thereof, and methods of making and using the same. | 08-18-2011 |
20110207701 | BORON-CONTAINING SMALL MOLECULES AS ANTIPROTOZOAL AGENTS - This invention provides, among other things, novel compounds useful for treating protozoal infections, pharmaceutical compositions containing such compounds, as well as combinations of these compounds with at least one additional therapeutically effective agent. | 08-25-2011 |
20110207702 | BORON-CONTAINING SMALL MOLECULES AS ANTI-PROTOZOAL AGENTS - This invention provides, among other things, novel compounds useful for treating protozoal infections, pharmaceutical compositions containing such compounds, as well as combinations of these compounds with at least one additional therapeutically effective agent. | 08-25-2011 |
20110212918 | BORON-CONTAINING SMALL MOLECULES - This invention relates to, among other items, 6-substituted benzoxaborole compounds and their use for treating bacterial infections. | 09-01-2011 |
20110212919 | PROTEIN CROSS-LINKING INHIBITOR - The present invention provides a protein cross-linking inhibitor containing a compound represented by any of the following formulas ( | 09-01-2011 |
20110212920 | N-Substituted Benzene Sulfonamides - Disclosed are N-substituted benzenesulfonamides for use in treating or preventing cognitive disorders, such as Alzheimer's Disease. | 09-01-2011 |
20110224171 | INHIBITORS OF FATTY ACID AMIDE HYDROLASE - The present invention provide compounds, and pharmaceutical compositions thereof, encompassed by the formulae (I), (II) or (III). | 09-15-2011 |
20110230440 | INHIBITORS OF FATTY ACID AMIDE HYDROLASE - The present invention provide compounds, and pharmaceutical compositions thereof, encompassed by the formulae (I), (II) or (III). | 09-22-2011 |
20110230441 | STABLE BORTEZOMIB FORMULATIONS - Multi-dose formulations for bortezomib are presented in which bortezomib has significantly improved stability. Especially preferred formulations include those in which bortezomib is in a liquid form suitable for injection, wherein the solvent system predominantly comprises propylene glycol. In other preferred aspects, bortezomib is present as a Lewis donor-acceptor complex with a hetero-bifunctional Lewis base. | 09-22-2011 |
20110230442 | NA CHANNELS, DISEASE, AND RELATED ASSAYS AND COMPOSITIONS - Disclosed are molecules and their synthesis, for use in blocking gated ion channels such as voltage-gated sodium channels (VGSCs) and prostate voltage sodium channels (PVSCs). These inhibitors have superior blocking efficacy, for instance in displacing the radioligand [ | 09-22-2011 |
20110237547 | PHARMACEUTICAL COMPOSITIONS FOR THE TREATMENT OF FUNGAL INFECTIONS - Synergistic combinations of a squalene epoxidase inhibitor and a leucyl-tRNA synthetase inhibitor are provided, which are useful in particular in the treatment of diseases involving fungal or suspected fungal infection, for immunomodulation or immunosuppression in conditions in which fungal or suspected fungal colonisation of e.g. the skin or nail plays a role, such as atopic dermatitis, acne vulgaris, seborrhoeic dermatitis, rosacea or onychomycosis, and in situations of fungal resistance. | 09-29-2011 |
20110245203 | DERIVATIVES OF 1-AMINO-2-CYCLOPROPYLETHYLBORONIC ACID - The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases. | 10-06-2011 |
20110263530 | Aurora Kinase Modulators and Method of Use - The present invention relates to chemical compounds having a general formula I | 10-27-2011 |
20110269715 | ABNORMAL CANNABIDIOLS AS AGENTS FOR LOWERING INTRAOCULAR PRESSURE - The present invention provides a method of treating glaucoma or ocular hypertension which comprises applying to the eye of a person in need thereof an amount sufficient to treat glaucoma or ocular hypertension of a compound of formula I | 11-03-2011 |
20110275596 | METHODS FOR TREATING NEOPLASIA AND FOR IDENTIFYING COMPOSITIONS USEFUL IN SUCH THERAPY - Various methods for treating a patient with neoplasia are disclosed, in particular, methods using topoisomerase Ila-preferential poisons, methods using a combination of a topoisomerase Illi-preferential inhibitor and a topoisomerase II poison, and methods using a combination of a topoisomerase II poison and a proteasome inhibitor are disclosed. Novel topoisomerase Ila-preferential poisons are disclosed, particularly, several novel 13-carboline derivatives are identified. Methods for identifying the novel topoisomerase Ila-preferential poisons and methods for identifying the novel topoisomerase EP-preferential inhibitors are also provided herein. | 11-10-2011 |
20110275597 | PHARMACEUTICAL COMPOSITION - The present invention relates to a parenteral pharmaceutical composition comprising therapeutically effective amounts of N-(2-pyrazine)carbonyl-L-phenylalanine-L-leucine boronic acid or its salts or its derivatives and tromethamine wherein the composition is stable. | 11-10-2011 |
20110288052 | NOVEL COMPOUNDS, PHARMACEUTICAL COMPOSITIONS CONTAINING SAME, AND METHODS OF USE FOR SAME - The class compounds of the present invention may be represented by Formula (I), wherein X may be O, S, or N. R | 11-24-2011 |
20110301124 | PROTEASOME INHIBITORS - The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases. | 12-08-2011 |
20110319360 | Method of including apoptosis/Cell death in leukemia cell using a purine nucleoside analogue - A method of inducing apoptosis or cell death in a leukemia cell includes subjecting the cell to a purine nucleotide analogue, LMP-420 (2-amino-6-chloro-9-[5(dihydroxyboryl)-pentyl] purine). | 12-29-2011 |
20110319361 | BORON-CONTAINING SMALL MOLECULES - This invention relates to compounds useful for treating fungal infections, more specifically topical treatment of onychomycosis and/or cutaneous fungal infections. This invention is directed to compounds that are active against fungi and have properties that allow the compound, when placed in contact with a patient, to reach the particular part of the skin, nail, hair, claw or hoof infected by the fungus. In particular the present compounds have physiochemical properties that facilitate penetration of the nail plate. | 12-29-2011 |
20120004197 | PROPHYLACTIC AND/OR THERAPEUTIC AGENT FOR ANEMIA COMPRISING TETRAHYDROQUINOLINE COMPOUND AS ACTIVE INGREDIENT - Disclosed is a compound which has a low molecular weight and has an activity of enhancing the production of EPO and/or an activity of enhancing the production of hemoglobin. Specifically disclosed is and EPO production enhancer and/or a hemoglobin production enhancer comprising a 1-acyl-4-(substituted oxy, substituted amino, or substituted thio)-1,2,3,4-tetrahydroquinoline derivative, more specifically a tetrahydroquinoline compound represented by general formula (1) [wherein R | 01-05-2012 |
20120015906 | USES OF BORTEZOMIB IN PREDICTING SURVIVAL IN MULTIPLE MYELOMA PATIENTS - The present invention provides a method of predicting outcome of treatment for multiple myeloma based on determining certain cytogenetic anomalies and considering gene expression profiling risks. Also provided are statistical methods employed to define variables independently impacting outcomes. Further provided is method of treatment of myeloma patients. | 01-19-2012 |
20120035132 | BORON-CONTAINING SMALL MOLECULES - Compounds, pharmaceutical formulations, and methods of treating anti-inflammatory conditions and/or helminth-associated diseases are disclosed. | 02-09-2012 |
20120035133 | Lyophilization Cakes of Proteasome Inhibitors - Lyophilized cakes of proteasome inhibitors are described, as well as methods for their production and use. | 02-09-2012 |
20120040932 | CYCLIC BORONIC ACID ESTER DERIVATIVES AND THERAPEUTIC USES THEREOF - Disclosed herein are antimicrobial compounds compositions, pharmaceutical compositions, the use and preparation thereof. Some embodiments relate to 1 cyclic boronic acid ester derivatives and their use as therapeutic agents. | 02-16-2012 |
20120040933 | 9-(PIPERAZINYLALKYL) CARBAZOLES AS BAX-MODULATORS - piperazine compounds for use as pharmaceutically active compounds and in pharmaceutical formulations that are useful for the treatment of disorders associated with apoptosis, including neurodegenerative disorders, diseases associated with polyglutamine tracts, epilepsy, ischemia, infertility, cardiovascular disorders, renal hypoxia, hepatitis and AIDS, where the piperazine compounds are represented by formula (I) and the terms R | 02-16-2012 |
20120046243 | Aminopyridine- and Aminopyrimidinecarboxamides as CXCR2 Modulators - There is disclosed aminopyridine-and aminopyrimidinecarboxamide compounds useful as pharmaceutical agents, synthesis processes, and pharmaceutical compositions which include aminopyridine- and aminopyrimidinecarboxamides compounds. More specifically, there is disclosed a genus of CXCR2 inhibitor compounds that are useful for treating a variety of inflammatory and neoplastic disorders. | 02-23-2012 |
20120065165 | COMPOSITIONS AND METHODS OF TREATING ENDOTHELIAL DISORDERS - Compositions and methods of treating endothelial disorders, including: asthma, erectile dysfunction, pulmonary hypertension, cardiovascular disorders, and other disorders, using a synergistic combination of at least one arginase inhibitor and at least one phosphodiesterase (PDE1), (PDE2) and/or (PDE5) inhibitor are described. | 03-15-2012 |
20120071445 | Combination Therapy for the Treatment of Multiple Myeloma - The present invention provides a method for treating multiple myeloma in a subject, comprising the step of administering to the subject a combination of COMPOUND 1 and bortezomib. The invention further provides a method for treating multiple myeloma in a subject, comprising the step of administering to the subject a combination of COMPOUND 1 and melphalan. | 03-22-2012 |
20120077778 | Ladder-Frame Polyether Conjugates - Disclosed are compounds that are conjugates of ladder frame polyether compounds and biologically active compounds or research compounds, pharmaceutical formulations comprising the conjugates, and methods of transporting the conjugates across biological membranes. | 03-29-2012 |
20120077779 | Inhibitors of Fibroblast Activation Protein Alpha - Disclosed are peptide-based compounds that include boronic acid or cyano functionality, which efficiently and selectively inhibit fibroblast activation protein alpha. Among other therapeutic utilities, the peptide-based compounds may be useful for the treatment of cancer. | 03-29-2012 |
20120083469 | INHIBITORS OF ARGINASE AND THEIR THERAPEUTIC APPLICATIONS - Compounds according to Formula I and Formula II are potent inhibitors of Arginase I and II activity: | 04-05-2012 |
20120088738 | INHIBITORS OF FATTY ACID AMIDE HYDROLASE - Provided herein are compounds of formula (I): or pharmaceutically acceptable salts, solvates or prodrugs thereof or mixtures thereof, wherein Z | 04-12-2012 |
20120094957 | INHIBITORS OF FATTY ACID AMIDE HYDROLASE - Provided herein are compounds of formula (I) or pharmaceutically acceptable salts, solvates or prodrugs thereof, or mixtures thereof, wherein Z | 04-19-2012 |
20120101062 | Lipase Inhibitors - The present invention relates to inhibitors of lipases, such as inhibitors of endothelial lipase, as well as pharmaceutical compositions thereof, and methods for using such inhibitors. The prototype of these inhibitors has lipophilic portion and an electrophilic site. | 04-26-2012 |
20120115813 | BORON-CONTAINING SMALL MOLECULES - This invention relates to, among other items, benzoxaborole compounds and their use for treating bacterial infections. | 05-10-2012 |
20120129806 | ARGINASE INHIBITORS AS THERAPEUTICS - Compounds according to Formula I are potent inhibitors of Arginase I and II activity: | 05-24-2012 |
20120129807 | METHODS OF TREATMENT, IMPROVEMENT AND PREVENTION USING HALOARYL SUBSTITUTED AMINOPURINES - Provided herein are Aminopurine Compounds having the following structure: | 05-24-2012 |
20120135959 | Metalloprotein inhibitors containing nitrogen based ligands - Provided herein metalloproteinase inhibitors containing nitrogen or mixed nitrogen/oxygen donating zinc binding groups. Also provided are pharmaceutical compositions containing the compounds and methods of treating preventing or ameliorating the diseases associated with metalloproteinase activity using the compounds and compositions. | 05-31-2012 |
20120142634 | Method of Treating Cancer with a Combination of a Proteasome Inhibitor and Salubrinal - The disclosure provides methods for treating or preventing a cancerous condition, such as multiple myeloma, by administering a therapeutically effective combination of a proteasome inhibitor and salubrinal. | 06-07-2012 |
20120149663 | BORONIC ACID COMPOSITIONS AND METHODS RELATED TO CANCER - Disclosed are compounds and methods related to boronic acid derivatives of resveratrol. Certain of these derivatives have enhanced efficacy relative to resveratrol, function as irreversible modulators, and act at the GI/S phase of the cell cycle. | 06-14-2012 |
20120172335 | SUBSTITUTED BENZIMIDAZOLONE DERIVATIVES, MEDICAMENTS COMPRISING THEM AND THEIR USE - The present invention relates to novel benzimidazolone derivatives of the general formula (I) in which the substituents R | 07-05-2012 |
20120190646 | Compositions Comprising Thalidomide and Artemisinin for the Treatment of Cancer - The present invention relates to pharmaceutical compositions for the treatment of cancer and especially for the treatment of hematological malignancies such as multiple myeloma. Specifically, the present invention relates to pharmaceutical composition for the treatment of cancer comprising: thalidomide, or a derivative thereof, or salts or solvates thereof; one or more artemisinin compounds, or salts or solvates thereof; and one or more pharmaceutically acceptable carriers and/or excipients. | 07-26-2012 |
20120202775 | SUBSTITUTED INDOLE AND AZAINDOLE OXOACETYL PIPERAZINAMIDE DERIVATIVES - Compounds having drug and bio-affecting properties are described herein, including their properties, pharmaceutical compositions and methods of use. In particular, tricyclic aryl or heteroaryl piperazine diamide derivatives that possess unique antiviral activity are set forth. These compounds are useful for the treatment of HIV and AIDS. The compounds herein have the general Formula I: | 08-09-2012 |
20120214765 | BORON-CONTAINING SMALL MOLECULES AS ANTI-INFLAMMATORY AGENTS - Compounds and methods of treating anti-inflammatory conditions are disclosed. | 08-23-2012 |
20120225846 | HETEROCYCLIC COMPOUNDS FOR THE INHIBITION OF PASK - Disclosed herein are new heterocyclic compounds and compositions and their application as pharmaceuticals for the treatment of disease. Methods of inhibiting PAS Kinase (PASK) activity in a human or animal subject are also provided for the treatment of diseases such as diabetes mellitus. | 09-06-2012 |
20120258933 | COMBINATION - The present invention relates to a method of treating cancer in a human and to pharmaceutical combinations useful in such treatment. In particular, the method relates to a cancer treatment method that includes administering a proteasome inhibiting compound, and N-{(1S)-2-amino-1-[(3-fluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-thiophenecarboxamide, or a pharmaceutically acceptable salt thereof, and optional additional antineoplastic agents, to a human in need thereof. | 10-11-2012 |
20120264714 | BORON-CONTAINING SMALL MOLECULES AS ANTI-INFLAMMATORY AGENTS - Methods of treating anti-inflammatory conditions through the use of boron-containing small molecules are disclosed. | 10-18-2012 |
20120270840 | Proteasome inhibitors and processes for their preparation, purification and use - The invention provides boronic esters of Formula I | 10-25-2012 |
20120295874 | COFERONS AND METHODS OF MAKING AND USING THEM - The present invention is directed to a monomer useful in preparing therapeutic compounds. The monomer includes one or more pharmacophores which potentially binds to a target molecule with a dissociation constant of less than 300 μM and a linker element connected to the pharmacophore. The linker element has a molecular weight less than 500 daltons, is connected, directly or indirectly through a connector, to the pharmacophore. | 11-22-2012 |
20120295875 | BORON-CONTAINING SMALL MOLECULES AS ANTIPROTOZOAL AGENTS - This invention provides, among other things, novel compounds useful for treating protozoal infections, pharmaceutical compositions containing such compounds, as well as combinations of these compounds with at least one additional therapeutically effective agent. | 11-22-2012 |
20120322762 | Stable Bortezomib Formulations - Multi-dose formulations for bortezomib are presented in which bortezomib has significantly improved stability. Especially preferred formulations include those in which bortezomib is in a liquid form suitable for injection, wherein the solvent system predominantly comprises propylene glycol. In other preferred aspects, bortezomib is present as a Lewis donor-acceptor complex with a hetero-bifunctional Lewis base. | 12-20-2012 |
20120322763 | Stable Bortezomib Formulations - Multi-dose formulations for bortezomib are presented in which bortezomib has significantly improved stability. Especially preferred formulations include those in which bortezomib is in a liquid form suitable for injection, wherein the solvent system predominantly comprises propylene glycol. In other preferred aspects, bortezomib is present as a Lewis donor-acceptor complex with a hetero-bifunctional Lewis base. | 12-20-2012 |
20130023494 | MODULATORS OF THE GPR119 RECEPTOR AND THE TREATMENT OF DISORDERS RELATED THERETO - The present invention relates to compounds of Formula (Ia) and pharmaceutically acceptable salts, solvates, and hydrates thereof, that are useful as a single agent or in combination with one or more additional pharmaceutical agents, such as, an inhibitor of DPP-IV, a biguanide, an SGLT2 inhibitor, or an alpha-glucosidase inhibitor, in the treatment of, for example, a disorder selected from: a GPR119-receptor-related disorder; a condition ameliorated by increasing a blood incretin level; a metabolic-related disorder; type 2 diabetes; obesity; and complications related thereto. | 01-24-2013 |
20130035311 | PROCHELATORS FOR INHIBITING METAL-PROMOTED OXIDATIVE STRESS - The present invention provides compounds of Formula I along with compositions containing the same and methods of use thereof in treating oxidative stress. | 02-07-2013 |
20130035312 | CATHEPSIN CYSTEINE PROTEASE INHIBIORS - This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis. | 02-07-2013 |
20130040912 | PIPERAZINOTRIAZINES AS PI3K INHIBITORS FOR USE IN THE TREATMENT ANTIPROLIFERATIVE DISORDERS - The invention relates to compounds of formula (I) R1 is methyl, n-hexyl, aminoethyl, methylaminoethyl, ethylaminoethyl, dimethylaminoethyl, acryloylaminoethyl, methacryloylaminoethyl, methoxyethyl, ethoxyethyl, d-C4-alkyl-sulfonyl, acryloyl, or methacryloyl; or R1 is aminoethyl, acryloyl or acryloylaminoethyl carrying a linker and a tag, and R2 and R3, independently of each other, are hydrogen or CrC4-alkyl, or R2 and R3 together form a methylene or an ethylene bridge; and tautomers, solvates and pharmaceutically acceptable salts thereof. These compounds are effective in preventing or treating a disease or disorder modulated by PI3 kinases and/or mTOR, in particular treating a hyperproliferative disorder. | 02-14-2013 |
20130045949 | ANTI-CANCER AGENTS - Described herein are compounds that may be selectively activated to produce active anti-cancer agents in tumor cells. Also disclosed are pharmaceutical compositions comprising the compounds, and methods of treating cancer using the compounds. | 02-21-2013 |
20130053343 | COMPOUNDS AND METHODS FOR INHIBITING SEROTONIN SYNTHESIS - Compounds having the structures below that are TPH1 inhibitors are provided: The compounds are useful of, e.g., to increase bone mass. In preferred embodiments, the patient is known to have, or to be at risk for, a low bone mass disease such as osteoporosis. | 02-28-2013 |
20130059819 | INHIBITORS OF FATTY ACID AMIDE HYDROLASE - The present invention provide compounds, and pharmaceutical compositions thereof, encompassed by the formulae (I), (II) or (III). | 03-07-2013 |
20130079303 | Inhibitors of PI3 Kinase and/or mTOR - The present invention relates to compounds of Formula I, or a pharmaceutically acceptable salt thereof; | 03-28-2013 |
20130079304 | Pharmaceutical Compositions for the Treatment of Fungal Infections - Synergistic combinations of a squalene epoxidase inhibitor and a leucyl-tRNA synthetase inhibitor are provided, which are useful in particular in the treatment of diseases involving fungal or suspected fungal infection, for immunomodulation or immunosuppression in conditions in which fungal or suspected fungal colonisation of e.g. the skin or nail plays a role, such as atopic dermatitis, acne vulgaris, seborrhoeic dermatitis, rosacea or onychomycosis, and in situations of fungal resistance. | 03-28-2013 |
20130079305 | 3-SUBSTITUTED VINYLBORONATES AND USES THEREOF - 3-substituted vinylboronates and their use in the treatment of cancer such as colorectal cancer are disclosed. In some embodiments, the 3-substituted vinylboronates have the general Formula I: | 03-28-2013 |
20130079306 | HETEROCYCLIC COMPOUND AND p27Kip1 DEGRADATION INHIBITOR - A novel heterocyclic compound or a salt thereof useful for selectively inhibiting the degradation of p27 | 03-28-2013 |
20130090309 | AMINO-PYRIDINE-CONTAINING SPLEEN TYROSINE KINASE (SYK) INHIBITORS - The invention provides certain amino-pyridine-containing compounds of the Formula (I) or pharmaceutically acceptable salts thereof, wherein R | 04-11-2013 |
20130096085 | PROCHELATORS USEFUL FOR INHIBITING METAL-ASSOCIATED TOXICITY - Prochelator compounds of Formula (I) or Formula (II) are described, along with methods of using the same and pharmaceutical formulations or compositions containing the same. | 04-18-2013 |
20130096086 | MITOCHONDRIA AND HUMAN IMMUNODEFIENCY VIRUS TYPE 1 - Methods described herein relate to mitochondria and their role in Human immunodeficiency virus type 1 (HIV-1) infection and cell-to-cell HIV-1 transmission and compositions and methods for modulating mitochondrial mediated cell-to-cell transmission of HIV-1. Methods for screening to identify inhibitors of mitochondrial mediated cell-to-cell transmission of HIV-1 are also envisioned herein. | 04-18-2013 |
20130131016 | BORON-CONTAINING SMALL MOLECULES - This invention provides novel compounds, methods of using the compounds, and pharmaceutical formulations comprising the compounds. | 05-23-2013 |
20130131017 | BORON-CONTAINING SMALL MOLECULES - This invention provides novel compounds, methods of using the compounds, and pharmaceutical compositions containing the compounds. | 05-23-2013 |
20130150326 | AUTOTAXIN INHIBITORS AND USES THEREOF - Described herein are compounds that are inhibitors of autotaxin. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such inhibitors, alone and in combination with other compounds, for treating autotaxin-dependent or autotaxin-mediated conditions or diseases. | 06-13-2013 |
20130157977 | Benzimidazole Boronic Acid Derivatives As PI3 Kinase Inhibitors - This invention relates to the use of benzimidazole boronic acid derivatives for the modulation, notably the inhibition of the activity or function of the phosphoinositide 3′ OH kinase family (hereinafter PI3 kinases), suitably, PI3Kα, PI3Kδ, PI3Kβ, and/or PI3Kγ. Suitably, the present invention relates to the use of benzimidazole boronic acids in the treatment of one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries. More suitably, the present invention relates to PI3Kβ selective benzimidazole boronic acid compounds for treating cancer. | 06-20-2013 |
20130165411 | TRICYCLIC BORON COMPOUNDS FOR ANTIMICROBIAL THERAPY - Provided herein are antimicrobial tricyclic boron compounds of the following formula I: | 06-27-2013 |
20130190273 | Methods for Treating Amyotrophic Lateral Sclerosis Using Pro-Neurogenic Compounds - This technology relates generally to compounds and methods for stimulating neurogenesis (e.g., post-natal neurogenesis, including post-natal hippocampal and hypothalamic neurogenesis) and/or protecting neuronal cell from cell death. Various compounds are disclosed herein. In vivo activity tests suggest that these compounds may have therapeutic benefits in neuropsychiatric and/or neurodegenerative diseases such as schizophrenia, major depression, bipolar disorder, normal aging, epilepsy, traumatic brain injury, post-traumatic stress disorder, Parkinson's disease, Alzheimer's disease, Down syndrome, spinocerebellar ataxia, amyotrophic lateral sclerosis, Huntington's disease, stroke, radiation therapy, chronic stress, abuse of a neuro-active drug, retinal degeneration, spinal cord injury, peripheral nerve injury, physiological weight loss associated with various conditions, as well as cognitive decline associated with normal aging, chemotherapy, and the like. | 07-25-2013 |
20130210770 | PHARMACEUTICAL FORMULATIONS - This invention relates to compounds useful for treating fungal infections, more specifically topical treatment of onychomycosis and/or cutaneous fungal infections. This invention is directed to compounds that are active against fungi and have properties that allow the compound, when placed in contact with a patient, to reach the particular part of the skin, nail, hair, claw or hoof infected by the fungus. In particular the present compounds have physiochemical properties that facilitate penetration of the nail plate. | 08-15-2013 |
20130225524 | Chemical Compounds - The invention is directed to substituted quinoline derivatives. Specifically, the invention is directed to compounds according to Formula I: | 08-29-2013 |
20130231304 | BORON-CONTAINING SMALL MOLECULES AS ANTI-PROTOZOAL AGENT - This invention provides, among other things, novel compounds useful for treating protozoal infections, pharmaceutical compositions containing such compounds, as well as combinations of these compounds with at least one additional therapeutically effective agent. | 09-05-2013 |
20130237501 | Benzofuran Compounds For The Treatment Of Hepatitis C Virus Infections - The present invention features compounds of formula (I): | 09-12-2013 |
20130244980 | BORON-CONTAINING SMALL MOLECULES - This invention relates to compounds useful for treating fungal infections, more specifically topical treatment of onychomycosis and/or cutaneous fungal infections. This invention is directed to compounds that are active against fungi and have properties that allow the compound, when placed in contact with a patient, to reach the particular part of the skin, nail, hair, claw or hoof infected by the fungus. In particular the present compounds have physiochemical properties that facilitate penetration of the nail plate. | 09-19-2013 |
20130261082 | Combination Therapy With Organic Arsenicals - The invention provides a combination therapy wherein one or more other therapeutic agents are administered with an organic arsenical, preferably SGLU-I or a pharmaceutically acceptable salt thereof. The invention also relates to methods for the treatment of cancer, comprising administering SGLU-I in combination with another therapeutic agent. Another aspect of the invention relates to a kit comprising SGLU-I and another therapeutic agent. | 10-03-2013 |
20130267479 | Solutions Containing A Boron Complex, Method for Preparing Said Solutions, and Uses of Said Solutions - The present invention relates to solutions including at least one boron complex obtained through the reaction between at least one boron salt, consisting of a borate anion selected from within the group consisting of metaborate anions, tetraborate anions, pentaborate anions, octaborate anions, decaborate anions, and the mixtures thereof, and a cation selected from within the group including sodium cations, potassium cations, ammonium cations, and the mixtures thereof, and at least one polyol and at least one amino compound. The basic boron concentration is greater than 2 wt % of the total weight of the solution. The invention also relates to a method for preparing said solutions and to the uses of said solutions, particularly in the field of agriculture. | 10-10-2013 |
20130274227 | 3,5-DIAMINOPYRAZOLE KINASE INHIBITORS - Provided herein are 3,5-diaminopyrazoles, for example, compounds of Formula IA, that are useful for modulating regulated-in-COPD kinase activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a RC kinase-mediated disorder, disease, or condition. | 10-17-2013 |
20130281403 | COMPOUNDS AND COMPOSITIONS FOR THE TREATMENT OF PARASITIC DISEASES - The invention provides a class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent malaria. | 10-24-2013 |
20130289000 | BORON-CONTAINING SMALL MOLECULES - This invention provides, among other things, novel compounds useful for treating inflammatory conditions, pharmaceutical compositions containing such compounds, as well as combinations of these compounds with at least one additional therapeutically effective agent. | 10-31-2013 |
20130296273 | TREATMENT OF BLOOD CANCER - Hypoxia activated prodrugs, such as, e.g., TH-281, TH-302, and TH-308, are useful for the treatment of various blood cancers, such as acute leukemias, chronic leukemias, MDS, MF, and multiple myeloma. | 11-07-2013 |
20130296274 | PYRROLIDINONES AS METAP-2 INHIBITORS - Compounds of the formula I in which R | 11-07-2013 |
20130316978 | BORONIC ACID DERIVATIVES AND THERAPEUTIC USES THEREOF - Disclosed herein are antimicrobial compounds compositions, pharmaceutical compositions, the use and preparation thereof. Some embodiments relate to boronic acid derivatives and their use as therapeutic agents. | 11-28-2013 |
20130316979 | BORON-CONTAINING SMALL MOLECULES AS ANTI-INFLAMMATORY AGENTS - Methods of treating anti-inflammatory conditions through the use of boron-containing small molecules are disclosed. | 11-28-2013 |
20130331355 | CYCLIC BORONIC ACID ESTER DERIVATIVES AND THERAPEUTIC USES THEREOF - Method of treating or ameliorating a bacterial infection comprising administering a composition comprising a cyclic boronic acid ester compound in combination with a carbapenem antibacterial agent such as Biapenem, and the pharmacokinetics studies thereof are provided. | 12-12-2013 |
20130331356 | Proteasome Inhibitors - The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases. | 12-12-2013 |
20130331357 | COMBINATION THERAPY OF HSP90 INHIBITORY COMPOUNDS WITH PROTEASOME INHIBITORS - A composition comprising a proteasome inhibitor, and an Hsp90 inhibitor according to the following formulae (I) or (Ia), a tautomer, or a pharmaceutically acceptable salt thereof, wherein the variables in the structural formulae are defined herein. Also provided are methods for treating a proliferative disorder such as cancer in a subject in need thereof, using pharmaceutical combinations described herein. | 12-12-2013 |
20130338107 | INHIBITORS OF FATTY ACID AMIDE HYDROLASE - Provided herein are compounds of formula (I): or pharmaceutically acceptable salts, solvates or prodrugs thereof or mixtures thereof, wherein Z | 12-19-2013 |
20130345172 | CYCLIC BORONIC ACID ESTER DERIVATIVES AND THERAPEUTIC USES THEREOF - Disclosed herein are antimicrobial compounds compositions, pharmaceutical compositions, the use and preparation thereof. Some embodiments relate to 1 cyclic boronic acid ester derivatives and their use as therapeutic agents. | 12-26-2013 |
20130345173 | INHIBITORS OF FATTY ACID AMIDE HYDROLASE - Provided herein are compounds of formula (I) or pharmaceutically acceptable salts, solvates or prodrugs thereof, or mixtures thereof, wherein Z | 12-26-2013 |
20130345174 | PROTEASOME INHIBITOR DELANZOMIB FOR USE IN THE TREATMENT OF LUPUS - The present invention provides a method for treating lupus in a subject, comprising the step of administering to the subject Compound A. | 12-26-2013 |
20140018317 | TARGETED NITROXIDE AGENTS - A compound having a structure of: | 01-16-2014 |
20140018318 | N1- and N2-CARBAMOYL-1,2,3-TRIAZOLE SERINE HYDROLASE INHIBITORS AND METHODS - The present invention provides inhibitors of a wide variety of serine hydrolase enzymes. The inhibitors of the present invention are N1- and N2-carbamoyl-1,2,3-triazole compounds such as those of Formula (I): | 01-16-2014 |
20140051661 | NOVEL LIPOGENIC INHIBITORS AND USES THEREOF - The present invention provides resveratrol-based boron-containing analog! methods of use thereof in treatment of dyslipidemias and cancer. | 02-20-2014 |
20140051662 | TREATMENT OF MULTIPLE MYELOMA WITH MASITINIB - The present invention relates to the treatment of multiple myeloma, especially for the treatment of those patients with refractory or first relapsed multiple myeloma, and in particular patients with t(4;14) multiple myeloma, comprising administration of a tyrosine kinase inhibitor or a mast cell inhibitor, especially masitinib or a pharmaceutically acceptable salt thereof, administered in association with an additional care in multiple myeloma; for example, autologous stem-cell transplantation, targeted therapies, anti-myeloma agents such as alkylating agents, corticosteroids, or immunomodulatory agents, including bortezomib, lenalidomide, and dexamethasone. | 02-20-2014 |
20140057871 | CYCLIC AMIDE DERIVATIVE | 02-27-2014 |
20140073603 | Phenylboronic Acid - The present invention relates to a specific phenylboronic acid compound having anti-cancer, anti-inflammatory, and anti-microbial activity, in addition to a pharmaceutical composition comprising the same. The present invention also discloses a process for preparing said compound. The compound is represented by the formula (I): | 03-13-2014 |
20140073604 | Ladder-Frame Polyether Conjugates - Disclosed are compounds that are conjugates of ladder frame polyether compounds and biologically active compounds or research compounds, pharmaceutical formulations comprising the conjugates, and methods of transporting the conjugates across biological membranes. | 03-13-2014 |
20140080787 | Method for the Treatment of Neuropathies Associated with Charcot-Marie-Tooth 1A (CMT1A) Disease - The present invention relates to compositions and methods for the treatment, prevention, and diagnosis of neuropathies due to PMP22 mis-expression in a subject having Charcot-Marie-Tooth disease, especially Charcot-Marie-Tooth 1A disease. The present invention incorporates the use of small molecule proteasome inhibitors such as, but not limited to, Bortezomib to inhibit or reduce the overexpression of the PMP2 gene. | 03-20-2014 |
20140088041 | FUNGICIDAL PENFLUFEN MIXTURES - The invention relates to mixtures comprising penflufen, to the use of these mixtures for protecting industrial materials and to a method for treating industrial materials with the penflufen mixtures. | 03-27-2014 |
20140088042 | Proteasome Inhibitors And Methods Of Using The Same - The present invention provides boronic acid compounds, boronic esters, and compositions thereof that can modulate apoptosis such as by inhibition of proteasome activity. The compounds and compositions can be used in methods of inducing apoptosis and treating diseases such as cancer and other disorders associated directly of indirectly with proteasome activity. | 03-27-2014 |
20140121182 | PROTEASOME INHIBITORS AND PROCESSES FOR THEIR PREPARATION, PURIFICATION AND USE - The invention provides boronic esters of Formula (I) wherein R is H or methyl, and methods for the preparation and purification thereof. | 05-01-2014 |
20140121183 | INHIBITORS OF FATTY ACID AMIDE HYDROLASE - The present invention provide compounds, and pharmaceutical compositions thereof, encompassed by the formulae (I), (II) or (III). | 05-01-2014 |
20140128344 | Soft Protease Inhibitors and Pro-Soft Forms Thereof - The invention provides compounds and methods for inhibiting proteases. One aspect of the invention features pro-soft inhibitors which react with an activating protease to release an active inhibitor moiety in proximity to a target protease. In certain instances, compounds inhibit proteasomes and/or post-proline cleaving enzymes (PPCE), such as dipeptidyl peptidase IV. The compounds of the invention provide a better therapeutic index, owing in part to reduced toxicity and/or improved specificity for the targeted protease. | 05-08-2014 |
20140135288 | SELECTING USE OF PROTEASOME INHIBITORS BASED ON NF-KB2 SEQUENCE - Provided herein are methods for selecting use of proteasome inhibitors. | 05-15-2014 |
20140142064 | BORON-CONTAINING SMALL MOLECULES - This invention relates to compounds useful for treating fungal infections, more specifically topical treatment of onychomycosis and/or cutaneous fungal infections. This invention is directed to compounds that are active against fungi and have properties that allow the compound, when placed in contact with a patient, to reach the particular part of the skin, nail, hair, claw or hoof infected by the fungus. In particular the present compounds have physiochemical properties that facilitate penetration of the nail plate. | 05-22-2014 |
20140148413 | COMPOSITIONS AND METHODS FOR PREVENTING AND TREATING ORGAN INJURY AND/OR DYSFUNCTION - The present embodiments relate to compositions and methods for treating the inflammatory response in a tissue or organ, such as the liver, by contacting the tissue with a tissue-specific gap junction inhibitor; and compositions and methods of reducing the toxicity of an agent by administering a gap junction inhibitor either simultaneously or sequentially with exposure to the agent. For example, inhibition of the liver-specific gap junction connexin 32 by 2 aminoethyoxydiphenyl-borate, effectively treats and/or prevents hepatotoxicity. | 05-29-2014 |
20140148414 | PROCHELATORS USEFUL FOR INHIBITING METAL-ASSOCIATED TOXICITY - Prochelator compounds of Formula I or Formula II: | 05-29-2014 |
20140162983 | Compositions and Methods for the Production of Pyrimidine and Pyridine Compounds with BTK Inhibitory Activity - The present invention provides novel pyrimidine and pyridine compounds according to Formula (I), Formula (II), Formula (III), Formula (IV) and Formula (V) their manufacture and use for the treatment of hyperproliferative diseases including, but not limited to, cancer, lupus, allergic disorders, Sjogren's disease and rheumatoid arthritis. In preferred embodiments, the present invention describes irreversible kinase inhibitors including, but not limited to, inhibitors of Bruton's tyrosine kinase. | 06-12-2014 |
20140171389 | METHODS FOR TREATING CANCER - Administration of TH-302 or another hypoxia activated prodrug in combination with a pharmacological agent that down-regulates or inhibits homology directed repair (HDR) is useful for treating cancer. | 06-19-2014 |
20140171390 | BETA-LACTAMASE INHIBITORS - Described herein are compounds and compositions that modulate the activity of beta-lactamases. In some embodiments, the compounds described herein inhibit beta-lactamase. In certain embodiments, the compounds described herein are useful in the treatment of bacterial infections. | 06-19-2014 |
20140179631 | DERIVATIVES OF 1-AMINO-2-CYCLOPROPYLETHYLBORONIC ACID - The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases. | 06-26-2014 |
20140194381 | BORONIC ACID DERIVATIVES AND THERAPEUTIC USES THEREOF - Disclosed herein are antimicrobial compounds compositions, pharmaceutical compositions, the use and preparation thereof. Some embodiments relate to boronic acid derivatives and their use as therapeutic agents. | 07-10-2014 |
20140194382 | BORONIC ACID DERIVATIVES AND THERAPEUTIC USES THEREOF - Disclosed herein are antimicrobial compounds compositions, pharmaceutical compositions, the use and preparation thereof. Some embodiments relate to boronic acid derivatives and their use as therapeutic agents. | 07-10-2014 |
20140194383 | MONOMERS CAPABLE OF DIMERIZING IN AN AQUEOUS SOLUTION, AND METHODS OF USING SAME - Described herein are monomers capable of forming a biologically useful multimer when in contact with one, two, three or more other monomers in an aqueous media. In one aspect, such monomers may be capable of binding to another monomer in an aqueous media (e.g. in vivo) to form a multimer, (e.g. a dimer). Contemplated monomers may include a ligand moiety, a linker element, and a connector element that joins the ligand moiety and the linker element. In an aqueous media, such contemplated monomers may join together via each linker element and may thus be capable of modulating one or more biomolecules substantially simultaneously, e.g., modulate two or more binding domains on a protein or on different proteins. | 07-10-2014 |
20140194384 | BORONIC ACID DERIVATIVES AND THERAPEUTIC USES THEREOF - Disclosed herein are antimicrobial compounds compositions, pharmaceutical compositions, the use and preparation thereof. Some embodiments relate to boronic acid derivatives and their use as therapeutic agents. | 07-10-2014 |
20140194385 | BORONIC ACID DERIVATIVES AND THERAPEUTIC USES THEREOF - Disclosed herein are antimicrobial compounds compositions, pharmaceutical compositions, the use and preparation thereof. Some embodiments relate to boronic acid derivatives and their use as therapeutic agents. Other embodiments relate to pharmaceutical compositions containing boronic acid derivatives and additional excipient such as meglumine. | 07-10-2014 |
20140194386 | BETA-LACTAMASE INHIBITORS - Described herein are compounds and compositions that modulate the activity of beta-lactamases. In some embodiments, the compounds described herein inhibit beta-lactamase. In certain embodiments, the compounds described herein are useful in the treatment of bacterial infections. | 07-10-2014 |
20140194387 | DERIVATIVES OF 1-AMINO-2-CYCLOBUTYLETHYLBORONIC ACID - The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases. | 07-10-2014 |
20140200198 | BORON-CONTAINING SMALL MOLECULES - Compounds, pharmaceutical formulations, and methods of treating anti-inflammatory conditions and/or helminth-associated diseases are disclosed. | 07-17-2014 |
20140206647 | PYRIMIDINECARBOXAMIDES AS CXCR2 MODULATORS - There is disclosed pyridine- and pyrimidinecarboxamide compounds useful as pharmaceutical agents, synthesis processes, and pharmaceutical compositions which include pyridine- and pyrimidinecarboxamides compounds. More specifically, there is disclosed a genus of CXCR2 inhibitor compounds that are useful for treating a variety of inflammatory and neoplastic disorders. | 07-24-2014 |
20140206648 | HETEROCYCLIC BORONIC ACID ESTER DERIVATIVES AND THERAPEUTIC USES THEREOF - Disclosed herein are antimicrobial compounds compositions, pharmaceutical compositions, the use and preparation thereof. Some embodiments relate to cyclic boronate compounds and their use as therapeutic agents. | 07-24-2014 |
20140213551 | COMPOUNDS AND COMPOSITIONS - This invention is related to compounds and/or compositions useful against pathogens affecting meats, plants, or plant parts. In one embodiment, the provided compounds are products of certain oxaborole moieties. In a further embodiment, the compound comprises a di-oxaborole compound. Delivery systems are also provided to take advantage of the volatile nature of these compounds and/or compositions. | 07-31-2014 |
20140213552 | CYCLOHEXYLAMINES - The present application provides novel compounds and methods for preparing and using these compounds. These compounds are useful in treating pain, itch, overactive bladder and/or interstitial cystitis in patients by administering one or more of the compounds to a patient. The methods include administering a compound of formula (I) and a TRPV1 receptor activator. In one embodiment, the TRPV1 receptor activator is lidocaine. | 07-31-2014 |
20140221312 | USE OF BENZOXABOROLES AS VOLATILE ANTIMICROBIAL AGENTS ON MEATS, PLANTS, OR PLANT PARTS - This invention is related to use of a volatile antimicrobial compound against pathogens affecting meats, plants, or plant parts. The volatile antimicrobial compounds provided include certain oxaborole compounds, for example benzoxaboroles. Delivery systems are provided to take advantage of the volatile nature of these antimicrobial compounds. Also combinations with a volatile plant growth regulator, for example 1-methylcyclopropene, are disclosed. | 08-07-2014 |
20140221313 | A NEW CLASSIFIER FOR THE MOLECULAR CLASSIFICATION OF MULTIPLE MYELOMA - The present invention is in the field of molecular diagnostics and relates to a method for classifying samples obtained from patients diagnosed with multiple myeloma into three newly defined clusters. The invention also relates to a method for determining the prognosis of an individual diagnosed with multiple myeloma as well as a method for the prediction of the response to treatment of an individual diagnosed with multiple myeloma. More in particular, the invention provides a method for determining the disease outcome or the prognosis of a patient diagnosed with multiple myeloma by classifying said patient into a high risk or a low risk category, based on a 92 gene classifier. | 08-07-2014 |
20140235578 | METHODS FOR TREATING NEOPLASIA AND FOR IDENTIFYING COMPOSITIONS USEFUL IN SUCH THERAPY - Various methods for treating a patient with neoplasia are disclosed, in particular, methods using topoisomerase Ila-preferential poisons, methods using a combination of a topoisomerase Illi-preferential inhibitor and a topoisomerase II poison, and methods using a combination of a topoisomerase II poison and a proteasome inhibitor are disclosed. Novel topoisomerase Ila-preferential poisons are disclosed, particularly, several novel 13-carboline derivatives are identified. Methods for identifying the novel topoisomerase Ila-preferential poisons and methods for identifying the novel topoisomerase EP-preferential inhibitors are also provided herein. | 08-21-2014 |
20140235579 | HETEROCYCLIC COMPOUNDS FOR THE INHIBITION OF PASK - Disclosed herein are new heterocyclic compounds and compositions and their application as pharmaceuticals for the treatment of disease. Methods of inhibiting PAS Kinase (PASK) activity in a human or animal subject are also provided for the treatment of diseases such as diabetes mellitus. | 08-21-2014 |
20140235580 | INHIBITORS OF MONOACYLGLYCEROL LIPASE AND METHODS OF THEIR USE - Provided herein are compounds which mediate the activity of monoacyglycerol lipase (MAGL). Also provided are pharmaceutical compositions comprising a compound provided herein, and methods for treating, preventing and/or managing a MAGL mediated condition using a compound or pharmaceutical composition as provided herein. | 08-21-2014 |
20140256678 | Aminopyrimidinecarboxamides as CXCR2 Modulators - There are disclosed aminopyrimidinecarboxamide compounds useful as pharmaceutical agents, synthesis processes, and pharmaceutical compositions which include aminopyrimidinecarboxamides compounds. More specifically, there is disclosed a genus of CXCR2 inhibitor compounds that are useful for treating a variety of inflammatory and neoplastic disorders. | 09-11-2014 |
20140274953 | EX VIVO HUMAN MULTIPLE MYELOMA CANCER NICHE AND ITS USE AS A MODEL FOR PERSONALIZED TREATMENT OF MULTIPLE MYELOMA - The described invention provides an ex vivo dynamic multiple myeloma (MM) cancer niche contained in a microfluidic device. The dynamic MM cancer niche includes (a) a three-dimensional tissue construct containing a dynamic ex vivo bone marrow (BM) niche, which contains a mineralized bone-like tissue containing viable osteoblasts self-organized into cohesive multiple cell layers and an extracellular matrix secreted by the viable adherent osteoblasts; and a microenvironment dynamically perfused by nutrients and dissolved gas molecules; and (b) human myeloma cells seeded from a biospecimen composition comprising mononuclear cells and the multiple myeloma cells. The human myeloma cells are in contact with osteoblasts of the BM niche, and the viability of the human myeloma cells is maintained by the MM cancer niche. | 09-18-2014 |
20140274954 | Boron-Containing Diacylhydrazines - The present disclosure provides boron-containing diacylhydrazines having Formula I: | 09-18-2014 |
20140274955 | PROCHELATORS AS BROAD-SPECTRUM ANTIMICROBIAL AGENTS AND METHODS OF USE - The present disclosure provides methods of treating (including ameliorating and/or preventing) pathogenic infections by administering a therapeutically effective amount of a prochelator. The present disclosure further provides pharmaceutical compositions and a kit comprising the prochelator therein. | 09-18-2014 |
20140303120 | METHODS FOR THE TREATMENT OF CANCER - The present invention is directed to methods for treating cancer in a subject, such as a cancer of the endocrine system. In some aspects, the method includes administering to the subject one or more of a polo-like kinase 1 inhibitor, a mouse double minute 2 inhibitor, and/or a mitotic catastrophe inducing compound. In other aspects, the method includes measuring an expression level of one or more markers, including caspase 8 and caspase 9, to assess the functionality of the caspase cascade in the subject. | 10-09-2014 |
20140315859 | Proteasome Inhibitors as Ovoprotective Agents to Shield the Ovary from Chemotherapy Toxicity - A method of reducing damage to the ovary of a subject receiving chemotherapy is described. The method comprises the step of administering to the subject an amount of a proteasome inhibitor effective to reduce damage to the subject's ovary within a therapeutic time window prior to administration of a chemotherapeutic agent. | 10-23-2014 |
20140315860 | BORON-CONTAINING SMALL MOLECULES - This invention relates to, among other items, benzoxaborole compounds and their use for treating bacterial infections. | 10-23-2014 |
20140315861 | BETA-LACTAMASE INHIBITORS - Disclosed herein inter alia are Boron containing compounds and methods for treating infections related to antibiotic resistant microorganisms. | 10-23-2014 |
20140323439 | THERAPIES FOR HEMATOLOGIC MALIGNANCIES - The invention provides methods that relate to a novel therapeutic strategy for the treatment of hematological malignancies and inflammatory diseases. In particular, the method comprises administration of a compound of formula A, | 10-30-2014 |
20140323440 | AMINO-PYRIDINE-CONTAINING SPLEEN TYROSINE KINASE (SYK) INHIBITORS - The invention provides certain amino-pyridine-containing compounds of the Formula (I) | 10-30-2014 |
20140329771 | STRUCTURAL VARIANTS OF MYCOLACTONES FOR USE IN MODULATING INFLAMMATION, IMMUNITY AND PAIN - The present invention is related to variants of mycolactones of formula (I), processes for the preparation thereof, pharmaceutical compositions thereof and their use in modulating inflammation, immunity and pain. Y—O—W (I), wherein Y and W are as defined in claim | 11-06-2014 |
20140336153 | SUBSTITUTED PYRIDINE DERIVATIVES AS FABI INHIBITORS - The present invention provides substituted pyridine derivatives of formula (I), which may be therapeutically useful as as anti-bacterial agents, more particularly FabI inhibitors. Formula (I) in which R1 to R5 and L have the meanings given in the specification, and pharmaceutically acceptable salts thereof that are useful in the treatment and prevention in diseases or disorder, in particular their use in diseases or disorder where there is an advantage anti-bacterial agents, more particularly FabI inhibitors. The present invention also provides methods for synthesizing and administering the FabI inhibitor compounds. The present invention also provides pharmaceutical formulations comprising at least one of the FabI inhibitor compounds together with a pharmaceutically acceptable carrier, diluent or excipient therefor. | 11-13-2014 |
20140336154 | BENZOPYRAN AND BENZOXEPIN PI3K INHIBITOR COMPOUNDS AND METHODS OF USE - Benzopyran and benzoxepin compounds of Formulas I and II, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formulas I and II for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed. | 11-13-2014 |
20140343018 | Anti-depression Compounds - This technology relates generally to compounds and methods for stimulating neurogenesis (e.g., post-natal neurogenesis, including post-natal hippocampal and hypothalamic neurogenesis) and/or protecting neuronal cell from cell death. Various compounds are disclosed herein. In vivo activity tests suggest that these compounds may have therapeutic benefits in neuropsychiatric and/or neurodegenerative diseases such as schizophrenia, major depression, bipolar disorder, normal aging, epilepsy, traumatic brain injury, post-traumatic stress disorder, Parkinson's disease, Alzheimer's disease, Down syndrome, spinocerebellar ataxia, amyotrophic lateral sclerosis, Huntington's disease, stroke, radiation therapy, chronic stress, abuse of a neuro-active drug, retinal degeneration, spinal cord injury, peripheral nerve injury, physiological weight loss associated with various conditions, as well as cognitive decline associated with normal aging, chemotherapy, and the like. | 11-20-2014 |
20140343019 | INHIBITORS OF ARGINASE AND THEIR THERAPEUTIC APPLICATIONS - The inventive compounds are small molecule therapeutics that are potent inhibitors of Arginase I and II activity. The invention also provides pharmaceutical compositions of the inventive compounds and methods for using the inventive compounds for treating or preventing a disease or a condition associated with arginase activity. | 11-20-2014 |
20140349965 | COMPOSITIONS AND METHODS FOR TREATING NEOPLASTIC DISEASES - Disclosed herein are compositions and methods for treating neoplastic diseases. Included are compositions and methods that are effective against multiple myeloma cells resistant to conventional and bortezomib treatment. Furthermore, combination treatment with two different proteosome inhibitors is shown to be synergistic for treating multiple myeloma. | 11-27-2014 |
20140349966 | BORONATE ESTER COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS THEREOF - The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases. | 11-27-2014 |
20140357596 | METHOD OF TREATMENT OF NASOPHARYNGEAL CANCER - The present invention provides a method of treating nasopharyngeal cancer with a proteasome inhibitor of formula (7). The invention also provides a method of treating a patient with nasopharyngeal cancer based on elevated expression levels of NFkB, as measured by a H-score of the patient's nasopharyngeal cancer tumor sample using a “NFkB p65 IHC assay. The invention also provides a method of determining whether to treat a patient with the compound of formula (I) based on the level of NFkB p65 in the patient's nasopharyngeal cancer tumor sample. | 12-04-2014 |
20140364396 | Alpha-amino boronic acid derivatives, selective immunoproteasome inhibitors - The present invention provides compounds of Formula (I) as inhibitors of LMP7 for the treatment of autoimmune and inflammatory diseases. | 12-11-2014 |
20140371175 | INHIBITORS OF ARGINASE AND THEIR THERAPEUTIC APPLICATIONS - Compounds according to Formula I and Formula II are potent inhibitors of Arginase I and II activity: | 12-18-2014 |
20140371176 | CYCLOPROPYLAMINES AS LSD1 INHIBITORS - This invention relates to the use of cyclopropylamine derivatives for the modulation, notably the inhibition of the activity of Lysine-specific demethylase 1 (LSD1). Suitably, the present invention relates to the use of cyclopropylamines in the treatment of cancer. | 12-18-2014 |
20150011506 | Proteasome Inhibitors - The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases. | 01-08-2015 |
20150018311 | THERAPEUTIC BORON-CONTAINING COMPOUNDS - The present invention relates to compounds of Formula (I) wherein R | 01-15-2015 |
20150025038 | BORON-CONTAINING SMALL MOLECULES - This invention provides novel compounds, methods of using the compounds, and pharmaceutical formulations comprising the compounds. | 01-22-2015 |
20150038461 | THIOPYRIMIDINECARBOXAMIDES AS CXCR1/2 MODULATORS - There is disclosed a pyrimidinecarboxamide compound useful as a pharmaceutical agent, synthetic processes, and pharmaceutical compositions which include the pyrimidinecarboxamide compound. More specifically, there is disclosed a CXCR1/2 inhibitor useful for treating a variety of inflammatory and neoplastic disorders. | 02-05-2015 |
20150051172 | PHARMACEUTICAL COMPOSITIONS COMPRISING BORONIC ACID COMPOUNDS - A pharmaceutical composition and preparing processes thereof. The composition comprises bortezomib or pharmaceutically acceptable salt or solvate thereof, tromethamine and an organic carboxylic acid, and the pH of the composition is from about 3.0 to 6.0. | 02-19-2015 |
20150051173 | BORONIC ACID BEARING LIPHAGANE COMPOUNDS AS INHIBITORS OF P13K- a AND/OR B - Compounds with unique liphagane meroterpenoid scaffold having boronic acid functionality in the skeleton are described (formula 1) together with pharmacological potential of these compounds as anticancer agents. A method of preparation and inhibiting the activity of phosphoinositide-3-kinase (PI3K-alpha and beta) has been presented. In particular, the invention describes a method of inhibiting PI3K isoforms, wherein the compounds are novel structures based on liphagane scaffold with unique boronic acid functionality. The methods and uses thereof are described herein this invention. | 02-19-2015 |
20150057248 | BIVALENT AMPA RECEPTOR POSITIVE ALLOSTERIC MODULATORS - Embodiments of the invention are directed to compounds that are positive allosteric modulators of AMPA receptors. | 02-26-2015 |
20150065459 | BORON-CONTAINING SMALL MOLECULES - This invention relates to compounds useful for treating fungal infections, more specifically topical treatment of onychomycosis and/or cutaneous fungal infections. This invention is directed to compounds that are active against fungi and have properties that allow the compound, when placed in contact with a patient, to reach the particular part of the skin, nail, hair, claw or hoof infected by the fungus. In particular the present compounds have physiochemical properties that facilitate penetration of the nail plate. | 03-05-2015 |
20150072956 | CLUSTER BORON COMPOUNDS AND USES THEREOF - The present invention relates to novel cluster boron compounds and their use as sodium channel blockers. In particular, the novel cluster boron compounds may be lidocaine analogs where the aromatic ring of the lidocaine molecule is replaced with a cluster boron group. The invention also provides methods for making the cluster boron compounds comprising contacting a halogenated cluster boron with an amino acetamide in the presence of a catalyst, a proton acceptor, and a ligand. | 03-12-2015 |
20150080339 | BORON-BASED 4-HYDROXYTAMOXIFEN AND ENDOXIFEN PRODRUGS AS TREATMENT FOR BREAST CANCER - The present disclosure relates to boron-based 4-hydroxytamoxifen and endoxifen prodrugs and the synthesis of the same. Further, the present disclosure teaches the utilization of the boron-based 4-hydroxytamoxifen and endoxifen prodrugs in a treatment for breast cancer. | 03-19-2015 |
20150080340 | BORONIC ACID CONJUGATES OF OLIGONUCLEOTIDE ANALOGUES - Oligonucleotide analogues comprising boronic acid and/or boronic ester moieties are provided. The disclosed compounds are useful for the treatment of diseases where inhibition of protein expression or correction of aberrant mRNA splice products produces beneficial therapeutic effects. | 03-19-2015 |
20150080341 | RING CONSTRAINED ANALOGS AS ARGINASE INHIBITORS - The inventive boronic acid analogs are potent inhibitors of Arginase I and II activity. These compounds are candidate therapeutics for treating a disease or disorder associated with an imbalance in the activity or concentration of cellular arginase I and arginase II enzymes. The invention also provides pharmaceutical compositions of the inventive compounds and methods for using the compositions for therapy. | 03-19-2015 |
20150080342 | BENZOXABOROLE COMPOUNDS AND USES THEREOF - Norvaline and/or other amino acids that are capable of being acylated onto tRNA | 03-19-2015 |
20150080343 | Benzofuran Compounds For The Treatment Of Hepatitis C Virus Infections - The present invention features compounds of formula (I): | 03-19-2015 |
20150105348 | COMPOSITIONS AND METHODS FOR REDUCING LACTATE LEVELS - The present disclosure provides methods of reducing levels of lactate in a fluid or tissue in an individual. The present disclosure provides pharmaceutical compositions suitable for use in the methods. | 04-16-2015 |
20150119362 | HETEROARYL INHIBITORS OF PDE4 - The present invention relates to compounds and methods useful as inhibitors of phosphodiesterase 4 (PDE4) for the treatment or prevention of disease. | 04-30-2015 |
20150119363 | METHODS OF TREATING BACTERIAL INFECTIONS - The present invention relates to compounds, compositions and methods for treating bacterial infections. Embodiments of the present invention include antibiotics and β-lactamase inhibitors to treat resistant infections. | 04-30-2015 |
20150119364 | BORON-CONTAINING SMALL MOLECULES - This invention relates to compounds useful for treating fungal infections, more specifically topical treatment of onychomycosis and/or cutaneous fungal infections. This invention is directed to compounds that are active against fungi and have properties that allow the compound, when placed in contact with a patient, to reach the particular part of the skin, nail, hair, claw or hoof infected by the fungus. In particular the present compounds have physiochemical properties that facilitate penetration of the nail plate. | 04-30-2015 |
20150133401 | COMBINATION THERAPY INVOLVING A VASCULAR DISRUPTING AGENT AND AN AGENT WHICH TARGETS HYPOXIA - The present invention provides a method for treating a proliferative disease in a patient. The method comprises administering to a patient in need thereof: a) a vascular disrupting agent and (b) at least one hypoxia targeting agent. Preferred combinations are BNC105 and Pazopanib and BNC 105 and Bortezomib. | 05-14-2015 |
20150133402 | BORON-CONTAINING SMALL MOLECULES - This invention provides, among other things, novel compounds useful for treating bacterial infections, pharmaceutical compositions containing such compounds, as well as combinations of these compounds with at least one additional therapeutically effective agent. | 05-14-2015 |
20150290322 | SUSTAINED-RELEASE LIPID PRE-CONCENTRATE OF ANIONIC PHARMACOLOGICALLY ACTIVE SUBSTANCES AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME - Disclosed is a sustained-release lipid pre-concentrate, comprising: a) at least one liquid crystal former; b) at least one phospholipid; c) at least one liquid crystal hardener; and d) at least one bi- or multivalent metal salt, wherein the sustained-release pre-concentrate exists as a lipid liquid phase in the absence of aqueous fluid and forms into a liquid crystal upon exposure to aqueous fluid. The sustained-release lipid pre-concentrate is configured to enhance the sustained release of anionic pharmacologically active substances through ionic interaction between the bi- or multivalent metal salt and the anionic pharmacologically active substances. | 10-15-2015 |
20150291630 | BETA-LACTAMASE INHIBITORS - Described herein are compounds and compositions that modulate the activity of beta-lactamases. In some embodiments, the compounds described herein inhibit beta-lactamase. In certain embodiments, the compounds described herein are useful in the treatment of bacterial infections. | 10-15-2015 |
20150297616 | A METHOD OF INHIBITING THE EXPRESSION OF IL-22 IN ACTIVATED T-CELLS - The present invention relates to a method of inhibiting the upregulation of the expression of the proinflammatory cytokine interleukin-22 (IL-22) in activated and differentiated human T-cells, said upregulation being induced by administration of a therapeutically effective amount of a phosphodiesterase 4 (PDE4) inhibitor. The method comprises administering, either sequentially to or simultaneously with the administration of the PDE4 inhibitor, a vitamin D receptor agonist in an amount 3) sufficient to inhibit the upregulation of IL-22 expression. | 10-22-2015 |
20150299227 | INHIBITORS OF CATECHOL O-METHYL TRANSFERASE AND THEIR USE IN THE TREATMENT OF PSYCHOTIC DISORDERS - The present invention relates to 4-pyridinone compounds which are inhibitors of catechol O-methyltransferase (COMT), and are useful in the treatment and prevention of neurological and psychiatric disorders and diseases in which COMT enzyme is involved. The present invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which COMT is involved. | 10-22-2015 |
20150307523 | BORONATE ESTER COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS THEREOF - The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases. | 10-29-2015 |
20150320776 | METHOD OF INHIBITING HELICOBACTER PYLORI - The present invention relates to a method of inhibiting | 11-12-2015 |
20150322092 | Boron-Containing Diacylhydrazines - The present disclosure provides boron-containing diacylhydrazines having Formula I: | 11-12-2015 |
20150322093 | SMALL MOLECULE INHIBITORS OF NICOTINAMIDE PHOSPHORIBOSYLTRANSFERASE (NAMPT) - The present invention relates to novel compounds, their use as anti-cancer agents and their synthesis. In particular, the compounds contain cluster boron moieties such as carborane or a borohydride and act as inhibitors for the enzyme Nampt. The biological properties of the inventive cluster boron compounds, in terms of biological inhibition and antiproliferative effect, are greater than other small molecule inhibitors of Nampt. | 11-12-2015 |
20150329565 | SUBSTITUTED TRIAZOLE BORONIC ACID COMPOUNDS - The invention is concerned with the compounds of formula (I) and pharmaceutically acceptable salts thereof. In addition, the present invention relates to methods of manufacturing and using the compounds of formula I as well as pharmaceutical compositions containing such compounds. The compounds of formula I are LMP7 inhibitors and may be useful in treating associated inflammatory diseases and disorders such as, for example, rheumatoid arthritis, lupus and irritable bowel disease. | 11-19-2015 |
20150353581 | 1-HYDROXY-BENZOOXABOROLES AS ANTIPARASITIC AGENTS - Provided are compounds useful for controlling endoparasites both in animals and agriculture. Further provided are methods for controlling endoparasite infestations of an animal by administering an effective amount of a compound as described above, or a pharmaceutically acceptable salt thereof, to an animal, as well as formulations for controlling endoparasite infestations using the compounds described above or an acceptable salt thereof, and an acceptable carrier. The claimed compounds are described by the following Markush formula: A typical example for a compound according to above formula is: A typical example for a compound according to above formula is: | 12-10-2015 |
20150361104 | BORON-CONTAINING SMALL MOLECULES AS ANTIPROTOZOAL AGENTS - This invention provides, among other things, novel compounds useful for treating protozoal infections, pharmaceutical compositions containing such compounds, as well as combinations of these compounds with at least one additional therapeutically effective agent. | 12-17-2015 |
20150361105 | PROTEASOME INHIBITORS - The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases. | 12-17-2015 |
20150361106 | BETA-LACTAMASE INHIBITORS - Described herein are compounds and compositions that modulate the activity of beta-lactamases. In some embodiments, the compounds described herein inhibit beta-lactamase. In certain embodiments, the compounds described herein are useful in the treatment of bacterial infections. | 12-17-2015 |
20150361107 | ORALLY BIOAVAILABLE BETA-LACTAMASE INHIBITORS - Described herein are compounds and compositions that modulate the activity of beta-lactamases. In some embodiments, the compounds described herein inhibit beta-lactamase. In certain embodiments, the compounds described herein are useful in the treatment of bacterial infections. | 12-17-2015 |
20150361108 | ORALLY BIOAVAILABLE BETA-LACTAMASE INHIBITORS - Described herein are compounds and compositions that modulate the activity of beta-lactamases and methods thereof. In some embodiments, the compounds described herein are biologically hydrolyzed to a beta-lactamase inhibitor. In certain embodiments, the compounds described herein are useful for the treatment of bacterial infections. | 12-17-2015 |
20150368278 | INHIBITORS OF FATTY ACID AMIDE HYDROLASE - The present invention provides compounds, and pharmaceutically acceptable compositions thereof, encompassed by any of formulae (I), (II), (III), (IV), (V), or (VI), or subgenera thereof. The present invention also provides methods for treating an FAAH mediated disease, disorder or condition by administering a therapeutically effective amount of a compound or composition comprising a compound of any of formulae (I), (II), (III), (IV), (V), or (VI), or subgenera thereof, to a patient in need thereof. Additionally, the present invention provides methods for inhibiting FAAH by administering a therapeutically effective amount of a compound or composition comprising a compound of any of formulae (I), (II), (III), (IV), (V), or (VI), or subgenera thereof, to a patient in need thereof. | 12-24-2015 |
20150376210 | BORON-CONTAINING SMALL MOLECULES - Compounds, pharmaceutical formulations, and methods of treating anti-inflammatory conditions and/or helminth-associated diseases are disclosed. | 12-31-2015 |
20160000813 | BORON-CONTAINING SMALL MOLECULES - This invention provides novel compounds, methods of using the compounds, and pharmaceutical formulations comprising the compounds. | 01-07-2016 |
20160008307 | METHODS AND AGENTS FOR PREVENTING AND TREATING PLASMA CELL DYSCRASIAS | 01-14-2016 |
20160016978 | BETA-LACTAMASE INHIBITORS - Described herein are compounds and compositions that modulate the activity of beta-lactamases. In some embodiments, the compounds described herein inhibit beta-lactamase. In certain embodiments, the compounds described herein are useful in the treatment of bacterial infections. | 01-21-2016 |
20160024084 | DEUTERATED PALBOCICLIB - This invention relates to novel pyrido[2,3-d]pyrimidinones and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by administering a CDK-4 and/or CDK-6 inhibitor. | 01-28-2016 |
20160024121 | BETA-LACTAMASE INHIBITORS - Described herein are compounds and compositions that modulate the activity of beta-lactamases. In some embodiments, the compounds described herein inhibit beta-lactamase. In certain embodiments, the compounds described herein are useful in the treatment of bacterial infections. | 01-28-2016 |
20160030451 | SUBSTITUTED TETRACYCLINE COMPOUNDS FOR TREATMENT OF BACILLUS ANTHRACIS INFECTIONS - Methods and compositions for the treatment of | 02-04-2016 |
20160031912 | CLUSTER BORON COMPOUNDS AND USES THEREOF - The present invention relates to novel cluster boron compounds and their use as sodium channel blockers. The invention also provides methods for making and using the compounds. | 02-04-2016 |
20160037780 | BORON CONTAINING COMPOUNDS AND USES THEREOF - Provided herein is a boron-containing compound, or salt thereof, as described herein and an excipient for the treatment of a cellulosic material. Also provided are compositions, polymers and articles including a cellulosic material and a boron-containing compound, and a process for preparing such an article. The boron-containing compound and compositions including the same can be used, for example, as a wood preservative or fire retardant. | 02-11-2016 |
20160038503 | METHODS AND COMPOSITIONS USEFUL FOR TREATING DISEASES INVOLVING BCL-2 FAMILY PROTEINS WITH ISOQUINOLINE AND QUINOLINE DERIVATIVES - The present invention relates to a compositions for and methods for cancer treatment, for example, hematopoietic cancers (e.g. B-cell Lymphoma). In other aspects, the invention provides methods for treating particular types of hematopoietic cancers, such as B-cell lymphoma, using a combination of one or more of the disclosed compounds and, for example, 26S proteasome inhibitors, such as, for example, Bortezomib. In another aspect the present invention relates to autoimmune treatment with the disclosed compounds. In another aspect, this invention relates to methods for identifying compounds, for example, compounds of the BH3 mimic class, that have unique in vitro properties that predict in vivo efficacy against B-cell lymphoma tumors and other cancers as well as autoimmune disease. | 02-11-2016 |
20160083403 | Boron-Containing Diacylhydrazine Compounds - The present disclosure provides boron-containing diacylhydrazines having Formula I: | 03-24-2016 |
20160102080 | PYRIDYL BENZOTHIOPHENES AS KINASE INHIBITORS - This invention is directed to compounds, which are useful as protein kinase (PK) inhibitors and can be used to treat such diseases as cancer, blood vessel proliferative disorders, fibrotic disorders, mesangial cell proliferative disorders, metabolic diseases inflammatory disorders and neurodegenerative disorders. | 04-14-2016 |
20160108063 | BORON-CONTAINING SMALL MOLECULES - This invention relates to compounds useful for treating fungal infections, more specifically topical treatment of onychomycosis and/or cutaneous fungal infections. This invention is directed to compounds that are active against fungi and have properties that allow the compound, when placed in contact with a patient, to reach the particular part of the skin, nail, hair, claw or hoof infected by the fungus. In particular the present compounds have physiochemical properties that facilitate penetration of the nail plate. | 04-21-2016 |
20160113951 | COMPOSITIONS AND METHODS FOR IMPROVING GLUCOSE UPTAKE - A method of treating a disease comprising administering to a subject a therapeutically effective amount of a compound that includes the structure of general Formula II, pharmaceutically acceptable salts thereof, and/or solvates thereof: | 04-28-2016 |
20160122366 | BORONIC ACID INHIBITORS OF HIV PROTEASE - Protease inhibitors, particularly aspartyl protease inhibitors, and more particularly HIV protease inhibitors which are boronated to enhance activity or to enhance entry into cells. Compounds, prodrugs and salts thereof of this invention contain phenylboronate groups, in particular p-B(OH) | 05-05-2016 |
20160128933 | Therapeutic Methods and Compositions - Methods and compositions are described for stimulating therapeutic points of a mammal subject by applying therapeutically effective amount of one or more TRP channel agonists. | 05-12-2016 |
20160129117 | Novel Boronic Acid Compound Preparation - The purpose of the present invention is to avoid side effects from contained medicines. Provided are: a preparation obtained by mixing a boronic acid compound and a block copolymer represented by general formula (I); and a production method therefor. | 05-12-2016 |
20160137672 | HETEROARYL INHIBITORS OF PDE4 - The present invention relates to compounds and methods useful as inhibitors of phosphodiesterase 4 (PDE4) for the treatment or prevention of disease. | 05-19-2016 |
20160151399 | BORON-CONTAINING SMALL MOLECULES | 06-02-2016 |
20160166592 | BORONIC ACID DERIVATIVES OF RESVERATROL FOR ACTIVATING DEACETYLASE ENZYMES | 06-16-2016 |
20160168167 | Tricyclic Benzoxaborole Compound, Preparation Method and Use Thereof | 06-16-2016 |
20160175334 | ANTIFUNGAL COMBINATION THERAPY OF TAVABOROLE AND CICLOPIROX | 06-23-2016 |
20160175335 | ANTIFUNGAL COMBINATION THERAPY OF TAVABOROLE AND EFINACONAZOLE | 06-23-2016 |
20160176875 | SPIROCYCLIC EBI2 MODULATORS | 06-23-2016 |
20160194340 | ARGINASE INHIBITORS AND METHODS OF USE | 07-07-2016 |
20160200743 | BORON-CONTAINING SMALL MOLECULES AS ANTI-INFLAMMATORY AGENTS | 07-14-2016 |
20160202243 | MITOCHONDRIA AND HUMAN IMMUNODEFIENCY VIRUS TYPE 1 TRANSMISSION | 07-14-2016 |
20160250238 | Method for the Prophylaxis or Treatment of Systemic Lupus Erythematosus and/or Lupus Nephritis | 09-01-2016 |
20160251376 | TYK2 INHIBITORS AND USES THEREOF | 09-01-2016 |
20160375044 | Compositions and Methods for Inhibiting Arginase Activity - The invention relates to methods of treating cancer, with a combination of an arginase inhibitor and a chemotherapeutic agent. The invention further relates to methods of assessing efficacy of a cancer treatment by measuring arginine levels in a tumor. | 12-29-2016 |
20190144470 | PROTEASOME INHIBITORS | 05-16-2019 |