18th week of 2014 patent applcation highlights part 55 |
Patent application number | Title | Published |
20140121152 | Active Agent Prodrugs with Heterocyclic Linkers - The embodiments provide prodrug compounds of Formulae I-XVII. The present disclosure also provides compositions, and their methods of use, where the compositions comprise a prodrug compound of Formulae I-XVII that provides controlled release of an active agent. Such compositions can optionally provide a trypsin inhibitor that interacts with the enzyme that mediates the controlled release of an active agent from the prodrug so as to attenuate enzymatic cleavage of the prodrug. | 2014-05-01 |
20140121153 | NOVEL POLYPEPTIDES - The present invention relates to an isolated polypeptide comprising (a) the amino acid sequence set forth in SEQ ID NO: 21; or (b) an amino acid sequence that is at least 95% identical to SEQ ID NO: 21, and to therapeutic treatments based thereon. | 2014-05-01 |
20140121154 | Compositions Comprising Glucagon Analogs And Methods Of Making And Using The Same - This invention relates to novel compositions comprising analogs of glucagon, wherein the analog comprises an α-amino acid and at least one β-amino acid. Administration of the compositions may be used for effecting treatment or prevention of a plurality of disease states caused by dysfunctional biochemical or biological pathways, including diabetes and other metabolic disorders. The compositions and methods of this invention are particularly useful to identify novel therapeutic modulators of in-vivo receptor activity with extended half-lives and relevant bioactivity as compared to the naturally translated polypeptides upon which the analogs are derived. | 2014-05-01 |
20140121155 | Crystal Forms of Saxagliptin and Processes for Preparing Same - Physical crystal structures of a compound of the formula I: | 2014-05-01 |
20140121156 | NUTRITIONAL APPROACH TO THE CONTROL OF ANEMIA, DIABETES AND OTHER DISEASES OR CONDITIONS AND PREVENTION OF ASSOCIATED COMORBID STATES WITH THE USE OF ERGOTHIONEINE - Nutritional products, compositions, pharmaceutical preparations and methods of use are disclosed for the prevention, suppression and treatment of anemia and/or diabetes and its various associated comorbidities. Uses of Ergothioneine to neutralize free radicals and/or cytokines, reduce oxidative stress, prevent inflammation, stimulate red blood cell production with increased levels of hemoglobin, and/or stabilize iron in its normal 2 | 2014-05-01 |
20140121157 | METHODS FOR TREATING PROGRESSIVE COGNITIVE DISORDERS RELATED TO NEUROFIBRILLARY TANGLES - The described invention provides methods for treating or preventing progression of a progressive cognitive disease, disorder or condition, and methods for improving resilience of cognitive function in a subject in need thereof. | 2014-05-01 |
20140121158 | METHODS AND SYSTEMS FOR MEASURING AND USING THE OXIDATION-REDUCTION POTENTIAL OF A BIOLOGICAL SAMPLE - Methods and systems for measuring and using the oxidation-reduction characteristics of a biological sample are provided. The system generally includes a test strip and a readout device. A fluid sample is placed in the test strip, and the test strip is in turn operatively connected to the readout device. The readout device provides a controlled current that is sent across the fluid in the sample chamber. In addition, the readout device identifies an inflection point or transition time at which the voltage between contacts of the test strip is changing at the highest rate. The oxidation-reduction capacity of the sample is taken as the integral of the current profile from the time at which current begins to be supplied to the sample to the identified transition time. | 2014-05-01 |
20140121159 | TERMINALLY FUNCTIONALIZED CONJUGATES AND USES THEREOF - The present disclosure provides inter alia conjugates of formula (I): | 2014-05-01 |
20140121160 | Use of VEGF in the Treatment of Retarded Fetal Growth in Pregnancy - An agonist of the VEGF receptor is useful in the treatment of a disease associated with retarded fetal growth, such as intra-uterine growth retardation. The VEGF against may be a VEGF peptide or a gene construct encoding or expressing such a PI-peptide. | 2014-05-01 |
20140121161 | REPAIRING BRUCH'S MEMBRANE WITH HYDROGELS - The invention provides hydrogels and methods for their use in treating disorders of the retina such as age-related macular degeneration (AMD). | 2014-05-01 |
20140121162 | FREEZE-DRIED FORMULATIONS OF FGF-18 - The invention relates to the field of pharmaceutical formulations. More particularly it is directed to freeze-dried formulations of Fibroblast Growth Factor 18 (FGF-18) compound and to methods of producing such formulations. The freeze-dried formulations according to the invention are stable upon storage for an appropriate period of time. They can be used, after reconstitution, for the treatment of cartilage disorders such as osteoarthritis or cartilage injury. | 2014-05-01 |
20140121163 | MFG-E8 AND USES THEREOF - Methods of treating cerebral ischemia using milk fat globule epidermal growth factor-factor VIII (MFG-E8) are disclosed, as are recombinant human MFG-E8 and its uses in pharmaceutical compositions, products and methods for treating inflammation and organ injury after ischemia/reperfusion, sepsis, and lung injury. | 2014-05-01 |
20140121164 | PREVENTION OF KIDNEY INJURY OR DISEASE - The present invention relates to a dosage regime of a peptide analogues of [alpha]-melanocyte-stimulating hormone ([alpha]-MSH), which possesses an increased efficacy compared to the native [alpha]-MSH peptide in the treatment or prevention of kidney injury or disease. | 2014-05-01 |
20140121165 | Induction of the Mitochondrial Permeability Transition - The present invention relates to process for identifying a compound which induces the mitochondrial permeability transition (MPT) in proliferating cells, wherein said process comprises contacting a cell or cell extract with a compound, determining whether the compound binds to adenine nucleotide translocator (ANT), and determining whether the compound selectively induces the MPT in proliferating cells. | 2014-05-01 |
20140121166 | COMPOSITIONS AND METHODS FOR THE TREATMENT OF JUVENILE NEURONAL CEROID LIPOFUSCINOSIS AND RELATED DISORDERS - Provided are materials and methods for the prevention and treatment of Juvenile Neuronal Ceroid Lipofuscinosis comprising administration of an effective amount of at least one of a hemi-channel inhibitor or a phosphodiesterase-4 inhibitor. In some embodiments, the methods comprise administration of an effective amount of each of a hemi-channel inhibitor and a phosphodiesterase-4 inhibitor. Also provided are pharmaceutical compositions comprising a hemi-channel inhibitor or a phosphodiesterase-4 inhibitor, as well as kits comprising at least one effective dose of a hemi-channel inhibitor or a phosphodiesterase-4 inhibitor or a combination of both. | 2014-05-01 |
20140121167 | THERAPEUTIC PEPTIDES AND USE THEREOF AGAINST HUNTINGTON'S DISEASE - Novel therapeutic compounds for use against Huntington's disease. More especially, an isolated peptide of size less than 100 amino acids and containing:
| 2014-05-01 |
20140121168 | ANTAGONISTS OF TRPV1 RECEPTOR - TRPV1 antagonists and associated methods are provided. A TRPV1 channel antagonist can have the structure: Formula (I) wherein R | 2014-05-01 |
20140121169 | Guanylate Cyclase Receptor Agonists For The Treatment Of Tissue Inflammation And Carcinogenesis - A method of treatment of inflamed, pre-cancerous or cancerous tissue or polyps in a mammalian subject is disclosed. The treatment involves administration of a composition of at least one peptide agonist of a guanylate cyclase receptor and/or other small molecules that enhance intracellular production of cGMP. The at least one peptide agonist of a guanylate cyclase receptor may be administered either alone or in combination with an inhibitor of cGMP-dependent phosphodiesterase. The inhibitor may be a small molecule, peptide, protein or other compound that inhibits the degradation of cGMP. Without requiring a particular mechanism of action, this treatment may restore a healthy balance between proliferation and apoptosis in the subject's population of epithelial cells, and also suppress carcinogenesis. Thus, the method may be used to treat, inter alia, inflammation, including gastrointestinal inflammatory disorders, general organ inflammation and asthma, and carcinogenesis of the lung, gastrointestinal tract, bladder, testis, prostate and pancreas, or polyps. | 2014-05-01 |
20140121170 | COMPOSITIONS AND METHODS FOR TREATING AIDS OR CANCER BY INHIBITING THE SECRETION OF MICROPARTICLES - Novel peptides that inhibit the release of microparticles from cells are disclosed. The peptide contains at least one VGFPV motif at the N-terminal and has a length of 10-100 amino acids. Also disclosed is polynucleotide encoding the peptide, expression vectors carrying the polynucleotide, and methods for treating AIDS and tumors using the novel peptides. | 2014-05-01 |
20140121171 | TREATMENT FOR MUSCULAR DYSTROPHIES - miRNA-21 inhibitors and pharmaceutical compositions including an miRNA-21 inhibitor together with pharmaceutical excipients and carriers for use in the treatment of a muscular dystrophy and/or a muscular dystrophy-like myopathy. Particularly, the miRNA-21 inhibitors and pharmaceutical compositions including the same are for use in the regeneration of skeletal muscle in muscular dystrophy and/or a muscular dystrophy-like myopathy patients. | 2014-05-01 |
20140121172 | FORMULATIONS CONTAINING LABELS FOR MEDICAL DIAGNOSTICS - Systems, techniques and methods for estimating the metabolic state or flux, e.g., the body energy state (“BES”) of a patient, are disclosed. The BES provides deep insight into the nutritional needs of the patient, thus allowing for a sort of exquisite glycemic control with regard to the patient. The invention discloses systems and methods for estimating fractional gluconeogenesis, which is the % of glucose production that comes from gluconeogenesis (“GNG”), as opposed to glycogenolysis (“GLY”), the other form of glucose production. Nutritional formulations, materials, cocktails and methods for feeding patients by parenteral and other means are disclosed. The amount, type and rate of such nutritional feeding are typically based upon the above estimating. The invention discloses formulations that contain labels, such as deuterium, for medical diagnostics, such as for estimating BES and fractional gluconeogenesis. The invention is suitable for any sort of patient, including those who are injured, such as with traumatic brain injury, ill, or have other conditions that stress the metabolic system. | 2014-05-01 |
20140121173 | SYSTEMS AND METHODS TO ESTIMATE NUTRITIONAL NEEDS OF HUMAN AND OTHER PATIENTS - Systems, techniques and methods for estimating the metabolic state or flux, e.g., the body energy state (“BES”) of a patient, are disclosed. The BES provides deep insight into the nutritional needs of the patient, thus allowing for a sort of exquisite glycemic control with regard to the patient. The invention discloses systems and methods for estimating fractional gluconeogenesis, which is the % of glucose production that comes from gluconeogenesis (“GNG”), as opposed to glycogenolysis (“GLY”), the other form of glucose production. Nutritional formulations, materials, cocktails and methods for feeding patients by parenteral and other means are disclosed. The amount, type and rate of such nutritional feeding are typically based upon the above estimating. The invention discloses formulations that contain labels, such as deuterium, for medical diagnostics, such as for estimating BES and fractional gluconeogenesis. The invention is suitable for any sort of patient, including those who are injured, such as with traumatic brain injury, ill, or have other conditions that stress the metabolic system. | 2014-05-01 |
20140121174 | ANTI-DANDRUFF HAIR CARE PRODUCTS WITH SELECTIVE ACTIVE INGREDIENTS AND A CATIONIC KERATIN - Hair treatment agents include selected cationic alkyloligoglucosides and selected polyglycerol esters as care-providing substances. | 2014-05-01 |
20140121175 | ANTITUMOR AGENT - The invention is intended to provide an excellent antitumor agent. An antitumor agent contains a glycolipid glycoside compound represented by Formula (1) or a pharmacologically acceptable salt thereof as an active ingredient: | 2014-05-01 |
20140121176 | TOPICAL WASH COMPOSITION FOR USE IN ACNE PATIENTS - Wash compositions for topical application are described. The compositions can be stable and well tolerated. Also described, are methods of using such compositions as cosmetic or pharmaceutical products. For example, the compositions can be used for cleansing the skin, preferably of acne patients, without compromising the skin barrier or resulting in over-compensation of sebum production. A topical wash composition is also described that can include: a) at least one surfactant; b) a zinc salt of gluconic acid; and c) a salt or derivative of glycyrrhizic acid or of glycyrrhetinic acid. | 2014-05-01 |
20140121177 | SOYASAPOGENOL COMPOSITION - A soy saponin composition is provided high bodily absorption characteristics. In an embodiment, a soyasapogenol composition comprises soyasapogenol B and 3-O-D-glucuronopyranosyl soyasapogenol B. The weight ratio (B/A) of the 3-O-D-glucuronopyranosyl soyasapogenol B to the soyasapogenol B is in the range of 0.001-10. The composition can be produced by partial decomposition of a sugar chain residue of a soy saponin B group glycoside utilizing an acid. | 2014-05-01 |
20140121178 | METHOD AND IMPROVED PHARMACEUTICAL COMPOSITION FOR IMPROVING THE ABSORPTION OF AN ESTER PRODRUG - The present invention relates to a method and an improved composition for improving the absorption of an ester prodrug in a subject. The method includes co-administering to the subject an effective amount of the ester prodrug or a pharmaceutical acceptable salt thereof, and a sufficient amount of adjuvant to impede a carboxylesterase-mediated hydrolysis of the ester prodrug in vivo, wherein the adjuvant is selected from the gnzup consisting of triacetin, triethyl citrate and a combination of both. The present invention also relates to a method for impeding carboxylesterase-mediated hydrolysis of esters, including ester prodrugs. | 2014-05-01 |
20140121179 | Novel Galactoside Inhibitor of Galectins - The present invention relates to a compound of the general formula (I): | 2014-05-01 |
20140121180 | SUCROSE OCTASULFATES OF MAGNESIUM, PREPARATION METHOD THEREOF AND PHARMACEUTICAL COSMETIC USES OF SAME - The invention relates to a sucrose octasulfate of magnesium, having general formula I, the preparation method thereof and the use of same in the pharmaceutical and/or cosmetic field, wherein 0≦n≦4, n is an integer and Y represents OH, Cl, Br, I, NO | 2014-05-01 |
20140121181 | HYDROPHOBIC POLYMER COMPOUND HAVING ANTICOAGULANT EFFECT - A hydrophobic polymer compound is capable of inhibiting the blood coagulation reactions in both the primary hemostasis stage involving platelets and the coagulation thrombus formation stage involving blood coagulation factors, which hydrophobic polymer compound can be firmly immobilized on the surface of a medical device or medical material in a state where the compound retains its anticoagulant activity. A hydrophobic polymer compound in which a polymer compound inhibiting platelet adhesion is bound with a compound inhibiting blood coagulation reaction. | 2014-05-01 |
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. | 2014-05-01 |
20140121183 | INHIBITORS OF FATTY ACID AMIDE HYDROLASE - The present invention provide compounds, and pharmaceutical compositions thereof, encompassed by the formulae (I), (II) or (III). | 2014-05-01 |
20140121184 | INSECTICIDAL COMPOSITIONS AND METHODS OF USING THE SAME - Insecticidal compositions have at least one active agent and at least one insecticide. The active agent can include | 2014-05-01 |
20140121185 | COMPOUNDS AND COMPOSITIONS FOR USE IN THE TREATMENT AND PREVENTION OF CANCER AND PRECANCEROUS CONDITIONS, INFLAMMATION-RELATED DISORDERS, PAIN AND FEVER - Novel compounds and pharmaceutical compositions thereof for the treatment and/or prevention of cancer and precancerous conditions, inflammation-related disorders, pain and fever. | 2014-05-01 |
20140121186 | Compounds, Compositions and Methods for Treating Ocular Conditions - The present invention provides methods of treating viral infection of the eye or posterior ocular condition including administering a pharmaceutical composition comprising a compound described in the present application. In some embodiments, the pharmaceutical composition is topically administered. In another embodiment, the pharmaceutical composition is orally administered or intraocularly administered. | 2014-05-01 |
20140121187 | 1,3-DI-OXO-INDENE DERIVATIVE, PHARMACEUTICALLY ACCEPTABLE SALT OR OPTICAL ISOMER THEREOF, PREPARATION METHOD THEREOF, AND PHARMACEUTICAL COMPOSITION CONTAINING SAME AS AN ANTIVIRAL, ACTIVE INGREDIENT - Disclosed are 1,3-Dioxoindene derivatives, pharmaceutically acceptable salts thereof or enantiomers, a preparation method thereof, and a pharmaceutical composition for the prevention or treatment of viral diseases, comprising the same as an active ingredient. The 1,3-Dioxoindene derivatives have excellent inhibitory activity against picornaviruses including coxsackie-, entero-, echo-, Polio-, and rhinoviruses, as well as exhibiting low cytotoxicity, so that they can be useful as an active ingredient of a pharmaceutical composition for the prevention or treatment of viral diseases including poliomyelitis, paralysis, acute hemorrhagic conjunctivitis, viral meningitis, hand-foot-and-mouth disease, vesicular disease, hepatitis A, myositis, myocarditis, pancreatitis, diabetes, epidemic myalgia, encephalitis, flu, herpangina, foot-and-mouth disease, asthma, chronic obstructive pulmonary disease, pneumonia, sinusitis or otitis media. | 2014-05-01 |
20140121188 | COMPOSITIONS FOR THE IMPROVED TREATMENT OF ACNE AND RELATED DISORDERS - Methods of treatment and dosage regimes using hydrophobic gel or foam composition comprising a tetracycline antibiotic in treating or alleviating a disorder including, acne, acne related symptoms, a tetracycline antibiotic responsive acne related disorder, skin disorder caused by a bacteria, and a tetracycline antibiotic responsive sebaceous gland disease, | 2014-05-01 |
20140121191 | Oral Energy Supplement and Related Methods - The present invention relates to oral dosage formulations consisting of at least one active ingredient contained in a plurality of hydrophobic carriers dispersed in an aqueous medium comprising a hydrocolloid. The active ingredients include various energy supplements, such as caffeine and vitamins. The formulations may further include emulsifiers, permeation enhancers, and vasodilators. The invention further relates to methods of making the oral dosage formulations. | 2014-05-01 |
20140121192 | METHODS OF GENERATING BETA-LACTAMASE RESISTANT CARBAPENEM COMPOUNDS - The present invention includes compositions, methods of making and using novel carbapenem compounds including active agents, compounds, antibacterial agents, pharmaceutically acceptable salts of C1α-C1β di-substituted carbapenem compounds, C5α substituted carbapenem compounds, C6α-C6β di-substituted carbapenem compounds and combinations thereof. | 2014-05-01 |
20140121193 | METHODS FOR TREATING FIBROMYALGIA - The invention provides methods for treating or ameliorating cognitive dysfunction, fatigue, energy, concentration, mood, and pain associated with fibromyalgia using compositions containing methylphenidate or pharmaceutically equivalents thereof. | 2014-05-01 |
20140121194 | METHOD FOR ADMINISTERING AGENT FOR CONTROLLING ECTOPARASITE TO DOG - There is provided a method for controlling an animal ectoparasite having excellent controlling effects. The method for controlling an ectoparasite of dogs comprises orally administering an ectoparasite-controlling agent comprising as an active ingredient an isoxazoline compound represented by formula (I): | 2014-05-01 |
20140121195 | SUBSTITUTED BENZIMIDAZOLES AND BENZOPYRAZOLES AS CCR(4) ANTAGONISTS - Benzimidazole, benzopyrazole and benzotriazole compounds are provided which bind to CCR(4) and are useful for the treatment of diseases such as allergic diseases, autoimmune diseases, graft rejection and cancer. | 2014-05-01 |
20140121196 | DISPIROPYRROLIDINE DERIVATIVES - A compound that inhibits interaction between, murine double minute 2 (Mdm2) protein and p53 protein and exhibits anti-tumor activity is provided. The present invention provides a dispiropyrrolidine derivative represented by the following formula (1), which has various substituents, inhibits interaction between Mdm2 protein and p53 protein and exhibits anti-tumor activity, wherein R | 2014-05-01 |
20140121197 | PYRAZOLOPYRIDAZINES AND METHODS FOR TREATING RETINAL-DEGENERATIVE DISEASES AND HEARING LOSS ASSOCIATED WITH USHER SYNDROME - Compounds, compositions and methods for the treatment of retinal degenerative diseases, such as retinitis pigmentosa, Leber's congenital Amaurosis, Syndromic retinal degenerations, age-related macular degeneration and Usher Syndrome, and hearing loss associated with Usher Syndrome are described herein. | 2014-05-01 |
20140121198 | TRICYCLIC FUSED THIOPHENE DERIVATIVES AS JAK INHIBITORS - The present invention provides tricyclic fused thiophene derivatives, as well as their compositions and methods of use, that modulate the activity of Janus kinase (JAK) and are useful in the treatment of diseases related to the activity of JAK including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases. | 2014-05-01 |
20140121199 | (THIENO[2,3-b][1,5]BENZOXAZEPIN-4-YL)PIPERAZIN-1-YL COMPOUNDS AS DUAL ACTIVITY H1 INVERSE AGONISTS/5-HT2A ANTAGONISTS - A dual H1/5-HT | 2014-05-01 |
20140121200 | SUBSTITUTED PYRIDOPYRAZINES AS NOVEL SYK INHIBITORS - Provided are pyridopyrazine compounds of formula (1), pharmaceutical compositions thereof and methods of use therefore, wherein R | 2014-05-01 |
20140121201 | REGULATORY NETWORK FOR Th17 SPECIFICATION AND USES THEREOF - Screening assays and methods of using same for screening to identify modulator agents or compounds that affect Th17 cell specification are described herein. Pharmaceutical compositions comprising agents or compounds that modulate Th17 cell specification are also encompassed. Methods for modulating Th17 cell specification using agents identified using assays described herein in pharmaceutical compositions are also envisioned. Such pharmaceutical compositions are useful for treating inflammatory conditions and autoimmune diseases associated with Th17 cell mediated pathology. | 2014-05-01 |
20140121202 | S-t-BUTYL PROTECTED CYSTEINE DI-PEPTIDE ANALOGS AND RELATED COMPOUNDS - S-t-butyl protected cysteine di-peptide analogs and related compounds and methods of using these compounds for the treatment of diseases and/or conditions, including but not limited to diseases and/or conditions of Central Nervous System (CNS). | 2014-05-01 |
20140121203 | IMIDAZO[1,2-a]PYRIDINE DERIVATIVES: PREPARATION AND PHARMACEUTICAL APPLICATIONS - The present invention relates to hydroxamate compounds which are inhibitors of histone deacetylase. More particularly, the present invention relates to imidazo[1,2-a]pyridine containing compounds and methods for their preparation. These compounds may be useful as medicaments for the treatment of proliferative disorders as well as other diseases involving, relating to or associated with enzymes having histone deacetylase activities (HDAC). | 2014-05-01 |
20140121204 | NOVEL DIHYDROPYRIMIDINOISOQUINOLINONES AND PHARMACEUTICAL COMPOSITIONS THEREOF FOR THE TREATMENT OF INFLAMMATORY DISORDERS. - A compound according to Formula Ia: | 2014-05-01 |
20140121205 | PYRAZOLOPYRIDAZINES AND METHODS FOR TREATING RETINAL-DEGERATIVE DISEASES AND HEARING LOSS ASSOCIATED WITH USHER SYNDROME - Compounds, compositions and methods for the treatment of retinal degenerative diseases, such as retinitis pigmentosa, Leber's congenital Amaurosis, Syndromic retinal degenerations, age-related macular degeneration and Usher Syndrome, and hearing loss associated with Usher Syndrome are described herein. | 2014-05-01 |
20140121206 | TRPV4 ANTAGONISTS - The present invention relates to spirocarbamate compounds of Formula (I) in which R1, (R2)Y, R3, R4, X and A have the meanings given in the specification. The invention further provides pharmaceutical compositions containing the compounds or pharmaceutically acceptable salts thereof and relates to their use of these compounds as TRPV4 antagonists in treating or preventing conditions associated with TRPV4 imbalance. | 2014-05-01 |
20140121207 | QUINOLONE COMPOUND AND PHARMACEUTICAL COMPOSITION - The present invention provides a quinolone compound represented by General Formula (1) | 2014-05-01 |
20140121208 | Compositions for Treatment of Cystic Fibrosis and Other Chronic Diseases - The present invention relates to pharmaceutical compositions comprising an inhibitor of epithelial sodium channel activity in combination with at least one ABC Transporter modulator compound of Formula A, Formula B, Formula C, or Formula D. The invention also relates to pharmaceutical formulations thereof, and to methods of using such compositions in the treatment of CFTR mediated diseases, particularly cystic fibrosis using the pharmaceutical combination compositions. | 2014-05-01 |
20140121209 | COMPOSITIONS & METHODS FOR LOWERING INTRAOCULAR PRESSURE - Disclosed herein are compositions for lowering intraocular pressure (IOP) of an eye comprising a combination IOP-lowering agents bimatoprost, brimonidine, and timolol. Further disclosed are methods for reducing IOP in the eye of a subject. | 2014-05-01 |
20140121210 | ASYMMETRIC UREAS AND MEDICAL USES THEREOF - Disclosed are compounds, compositions and methods for the prevention and/or treatment of diseases which are pathophysiologically mediated by the ghrelin receptor. The compounds have the general formula (I): | 2014-05-01 |
20140121211 | THIOL MEDIATED/ACTIVATED PRODRUGS OF SULFUR DIOXIDE (SO2) HAVING ANTI-BACTERIAL ACTIVITY - Disclosed herein are thiol mediated/activated prodrugs of SO | 2014-05-01 |
20140121212 | Pyrido[2,3-b]pyrazin-8-substituted Compounds and Their Use - The present invention pertains generally to the field of therapeutic compounds for treating proliferative disorders, cancer, etc., and more specifically to certain pyrido[2,3-b]pyrazin-8-substituted compounds, as described herein, which, inter alia, inhibit RAF (e.g., B-RAF) activity. 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, to inhibit RAF (e.g., BRAF) activity, to inhibit receptor tyrosine kinase (RTK) activity, to inhibit cell proliferation, and in the treatment of diseases and disorders that are ameliorated by the inhibition of RAF, RTK, etc., proliferative disorders such as cancer (e.g., colorectal cancer, melanoma), etc. | 2014-05-01 |
20140121213 | VOLTAGE-GATED SODIUM CHANNEL BLOCKERS - In general, the present invention relates to uses of voltage-gated sodium channel blocker compounds, which include corresponding precursors, intermediates, monomers and dimers, corresponding pharmaceutical compositions, compound preparation and treatment methods for respiratory and respiratory tract diseases. | 2014-05-01 |
20140121214 | MATERIALS AND METHODS FOR SUPPRESSING AND/OR TREATING NEUROFIBROMA AND RELATED TUMORS - Germline mutations in the NF1 tumor suppressor gene cause Von Recklinghausen's neurofibromatosis type 1 (NF1), a common genetic disorder of the nervous system characterized by plexiform neurofibroma development. Using adoptive transfer of hematopoietic cells, we establish that NF1 heterozygosity of bone marrow derived cells in the tumor microenvironment is sufficient to allow neurofibroma progression in the context of Schwann cell nullizygosity. Further, genetic or pharmacologic attenuation of the c-kit signaling pathway in hematopoietic cells greatly diminishes neurofibroma initiation and progression. These studies identify haploinsufficient hematopoietic cells and the c-kit receptor as therapeutic targets for preventing plexiform neurofibromas and implicate mast cells as critical mediators of tumor initiation. Administering therapeutically effective doses of a tyrosine kinase inhibitor such as the compound imatinib mesylate to a patient in need thereof to treat tumors in a human patient afflicted with plexiform neurofibroma. | 2014-05-01 |
20140121215 | PROCESS FOR THE PREPARATION OF AMORPHOUS IMATINIB MESYLATE - The field of the invention relates to a process for the preparation of amorphous imatinib mesylate. In particular, the invention relates to a process for the preparation of stable amorphous imatinib mesylate. More particularly, the invention relates to pharmaceutical compositions that includes the stable amorphous imatinib mesylate together along with its excipients. | 2014-05-01 |
20140121216 | INDOLEAMINE DERIVATIVES FOR THE TREATMENT OF CENTRAL NERVOUS SYSTEM DISEASES - Indoleamine derivatives of formula (IA), R | 2014-05-01 |
20140121217 | SUBSTITUTED BIARYL COMPOUNDS FOR INFLAMMATION AND IMMUNE-RELATED USES - The invention relates to compounds of structural formula (I): | 2014-05-01 |
20140121218 | METHOD FOR TREATING OCULAR CANCER - It has now been found that the p53 pathway is inactivated in ocular cancers such as retinoblastoma. As such, the present invention is a method for inducing ocular cancer cell death using a p53 activator. In particular embodiments, the p53 activator blocks the interaction between DM2 or DMX and p53. As the p53 activator induces ocular cancer cell death, a method for preventing or treating ocular cancer is also provided. | 2014-05-01 |
20140121219 | New Compounds I - The present invention relates to compounds of formula (I), | 2014-05-01 |
20140121220 | CRYSTALS OF PHENYLPYRROLE DERIVATIVE - Provided is a monomethanesulfonate of a phenylpyrrole derivative, having superior glucokinase activating activity and demonstrating remarkably improved solubility, hygroscopicity and stability as well as superior oral absorption, and crystals thereof. The present invention provides (2S)-2-(3-{5-[(55)-5-methyl-4,5-dihydro-1,3-oxazol-2-yl]-1H-pyrrol-2-yl}-5-{[5-(methylsulfonyl)pyrazin-2-yl]oxy}phenoxy)propan-1-ol monomethanesulfonate having superior glucokinase activating activity, crystals thereof, a pharmaceutical containing the same, and a preventive and/or therapeutic agent for diabetes and the like. | 2014-05-01 |
20140121221 | SELECTIVE PDE4 B INHIBITION AND IMPROVEMENT IN COGNITION IN SUBJECTS WITH BRAIN INJURY - Provided herein are methods of improving cognitive ability or memory in a subject that has suffered a brain injury or spinal cord injury by administering a selective PDE4 B inhibitor. | 2014-05-01 |
20140121222 | PYRIMIDINONES AS PI3K INHIBITORS - The present invention provides pyrimidinones that modulate the activity of phosphoinositide 3-kinases (PI3Ks) and are useful in the treatment of diseases related to the activity of PI3Ks including, for example, inflammatory disorders, immune-based disorders, cancer, and other diseases. | 2014-05-01 |
20140121223 | QUINAZOLINONES AS INHIBITORS OF HUMAN PHOSPHATIDYLINOSITOL 3-KINASE DELTA - Compounds that inhibit PI3Kδ activity, including compounds that selectively inhibit PI3Kδ activity, are disclosed. Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3Kδ) activity, and methods of treating diseases, such as disorders of immunity and inflammation in which PI3Kδ plays a role in leukocyte function, using the compounds also are disclosed. | 2014-05-01 |
20140121224 | QUINAZOLINONES AS INHIBITORS OF HUMAN PHOSPHATIDYOSITOL 3-KINASE DELTA - Compounds that inhibit PI3Kδ activity, including compounds that selectively inhibit PI3Kδ activity, are disclosed. Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3Kδ) activity, and methods of treating diseases, such as disorders of immunity and inflammation in which PI3Kδ plays a role in leukocyte function, using the compounds also are disclosed. | 2014-05-01 |
20140121225 | POLYMORPH OF LINAGLIPTIN BENZOATE - The present invention relates to a novel polymorph of Linagliptin benzoate and to methods for its preparation. Furthermore the present invention relates to the use of the novel polymorph for the preparation of a medicament. In addition the present invention relates to pharmaceutical compositions comprising an effective amount of the novel polymorph of Linagliptin benzoate. | 2014-05-01 |
20140121226 | SUBSTITUTED XANTHINE DERIVATIVES - This invention relates to novel deuterated compounds that are substituted xanthine derivatives and pharmaceutically acceptable salts thereof. In particular, this invention relates to novel substituted xanthine derivatives that are deuterated derivatives of a pentoxifylline metabolite. This invention also provides compositions comprising one or more compounds of this invention and a carrier and the use of the disclosed deuterated compounds and compositions in methods of treating diseases and conditions for which pentoxifylline and related compounds are beneficial. The compounds of the invention are represented by the following structural formula: | 2014-05-01 |
20140121227 | THERAPEUTIC TREATMENT - The present invention relates to a combination comprising (5)-4-amino-N-(1-(4-chlorophenyl)-3-hydroxypropyl)-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidine-4-carboxamide, or a pharmaceutically acceptable salt thereof, hereafter “Compound (I)”, and a taxane. Taxanes include established cancer drugs such as docetaxel (Taxotere™) and paclitaxel (Taxol™). Such combinations may be useful in the treatment or prophylaxis of cancer. The invention also relates to a pharmaceutical composition comprising such Compound (I) and a taxane. The invention further relates to a method of treatment comprising the simultaneous, sequential or separate administration of Compound (I) and a taxane, to warm-blooded animal, such as man. The invention also relates to a kit comprising Compound (I) and a taxane, optionally with instructions for use. | 2014-05-01 |
20140121228 | Quinazoline Derivatives as VEGF Inhibitors - The invention relates to quinazoline derivatives of formula (I), | 2014-05-01 |
20140121229 | COMBINATION COMPRISING S-[2-([[1-(2-ETHYLBUTYL)CYCLOHEXYL] CARBONYL]AMINO)PHENYL] 2-METHYLPROPANETHIOATE AND AN HMG COA REDUCTASE INHIBITOR - The invention provides a combination comprising (a) S-[2-([[1-(2-ethylbutyl)cyclohexyl]carbonyl]amino)phenyl]2-methylpropanethioate or prodrug of the active form thereof, and (b) at least one HMG CoA reductase inhibitor. Also provided are a pharmaceutical composition, package, and a kit comprising the aforementioned active ingredients, as well as a method for treatment and prophylaxis of a cardiovascular disorder involving the use of the aforementioned active ingredients. | 2014-05-01 |
20140121230 | TOPICAL PARASITICIDAL FORMULATION - The present invention relates to topical parasiticidal formulations comprising a parasiticide, an organo-silicone surfactant and a topically acceptable liquid carrier, and methods of preventing or treating parasites on an animal. | 2014-05-01 |
20140121231 | PYRANOPYRIDONE INHIBITORS OF TANKYRASE - There are provided compounds of the formula | 2014-05-01 |
20140121233 | Synthesis and Characterization of Second Generation Benzofuranone Ring Substituted Noscapine Analogs - Compound of Formula (I) and use thereof as microtubule modulating agents in the treatment of cancer are described herein. | 2014-05-01 |
20140121234 | INHALANT PROPELLANT-FREE AEROSOL FORMULATION - The invention relates to inhalant propellant-free aerosol formulations containing at least one inert, non-volatile auxiliary substance for adjusting defined droplet sizes. | 2014-05-01 |
20140121235 | Method for Treating S6K-Overexpressing Cancers - Disclosed herein are methods for treating an S6K-overexpressing cancer, comprising administering a therapeutically effective amount of leflunomide to a subject in need thereof. | 2014-05-01 |
20140121236 | Compositions and Methods for Treating Myotonic Dystrophy Type 1 - Disclosed is a compound for treatment of Myotonic Dystrophy type 1 having the formula: | 2014-05-01 |
20140121237 | Methods for Inhibiting Virus Replication - The present invention provides methods for treating a subject having, or at risk of having, a viral infection. The methods include, but are not limited to, the use of 4-(dipropylsulfamoyl)benzoic acid, an inhibitor of CDC25B phosphatase, an inhibitor of ICAM-1, an inhibitor of CamK2B, or a combination thereof. | 2014-05-01 |
20140121238 | TOTAL SYNTHESIS OF REDOX-ACTIVE 1.4-NAPHTHOQUINONES AND THEIR METABOLITES AND THEIR THERAPEUTIC USE AS ANTIMALARIAL AND SCHISTOMICIDAL AGENTS - Naphthoquinones, azanaphthoquinones and benxanthones, their process of synthesis and methods of their use as antimalarial or antischistosomal agents. | 2014-05-01 |
20140121239 | METHOD OF TREATING LUNG ADENOCARCINOMA - This invention is directed to the treatment of cancer in a patient, particularly a patient with lung adenocarcinoma, and more particularly a patient with KIF5B-RET fusion-positive non-small cell lung cancer, with an inhibitor of MET, VEGF, and RET which is a compound of Formula I: | 2014-05-01 |
20140121240 | NOVEL PHARMACEUTICAL COMPOSITION - Provided is a novel pharmaceutical composition (antipruritic agent) that is useful for prophylaxis or treatment of itch in conditions such as dermal pruritus. More specifically, provided is a pharmaceutical composition (antipruritic agent) for treatment of itch comprising as an active ingredient a naphthalene compound of the following formula (I): | 2014-05-01 |
20140121241 | Carbostyril Derivatives Including Cilostazol for Treating Fatty Liver - The invention relates to a medicament for preventing and/or treating fatty liver which comprises as an active ingredient cilostazol or a pharmaceutically acceptable salt thereof. | 2014-05-01 |
20140121242 | SUBSTITUTED CINNAMAMIDE DERIVATIVE, PREPARATION METHOD AND USE THEREOF - The present invention relates to substituted cinnamamide derivatives, the method for preparing thereof and the use thereof. Each of said derivatives has a structure of formula (I). The method for preparing the substituted cinnamamides and their derivatives of the present invention is also disclosed. Substituted piperonal derivatives are selected as starting materials to prepare the substituted cinnamamide derivatives of the present invention by Wittig reaction and acid-amine condensation reaction. Further, a use of the present compounds in preventing and treating depressive-type mental diseases is disclosed. | 2014-05-01 |
20140121243 | NOVEL 1-SUBSTITUTED INDAZOLE DERIVATIVE - A medicament for treating diseases associated with cholinergic properties in the central nervous system (CNS) and/or peripheral nervous system (PNS), diseases associated with smooth muscle contraction, endocrine disorders, neurodegenerative disorders and the like, which comprises a compound of Formula (I): | 2014-05-01 |
20140121244 | NOVEL 1-SUBSTITUTED INDAZOLE DERIVATIVE - A medicament for treating diseases associated with cholinergic properties in the central nervous system (CNS) and/or peripheral nervous system (PNS), diseases associated with smooth muscle contraction, endocrine disorders, neurodegenerative disorders and the like, which comprises a compound of Formula (I): | 2014-05-01 |
20140121245 | ANHYDROUS LENALIDOMIDE FORM-I - Anhydrous polymorphic form-I of anti cancer drug, Lenalidomide whose chemical name is 3-(4-amino-1-oxo-1,3-dihydro-isoindole-2-yl)-piperidine-2,6-dione, is disclosed. Alternate methods for making anhydrous polymorphic form-I of Lenalidomide are also disclosed. | 2014-05-01 |
20140121246 | GPR120 RECEPTOR AGONISTS AND USES THEREOF - GPR120 agonists are provided. These compounds are useful for the treatment of metabolic diseases, including Type II diabetes and diseases associated with poor glycemic control. | 2014-05-01 |
20140121247 | Methods for Controlling Blood Pressure and Reducing Dyspnea in Heart Failure - Methods for controlling, maintaining, or reducing blood pressure, and/or for treating, preventing, or alleviating symptoms such as dyspnea, in a patient suffering from or susceptible to acute heart failure. The methods involve the administration of an effective amount of a pharmaceutical composition comprising a short acting dihydropyridine compound such as clevidipine. The pharmaceutical composition may be administered at an initial dose, and if blood pressure is not controlled or maintained within a target blood pressure range or reduced to within a target blood pressure range, the initial dose may be titrated to achieve a blood pressure within the target blood pressure range. The patient may have a systolic blood pressure of about 120 mmHg or above. | 2014-05-01 |
20140121248 | METALLOENZYME INHIBITOR COMPOUNDS - The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes. | 2014-05-01 |
20140121249 | ANTIMICROBIAL SUBSTITUTED THIAZOLES AND METHODS OF USE - Disclosed are compositions having activity against MRSA and/or VRSA, and methods of using the compositions to treat microbial infections. | 2014-05-01 |
20140121250 | ALKYLAMIDOTHIAZOLES, COSMETIC OR DERMATOLOGICAL PREPARATIONS CONTAINING SAID ALKYLAMIDOTHIAZOLES, AND USE THEREOF TO COMBAT OR PREVENT UNDESIRED PIGMENTATION OF THE SKIN - Alkylamidothiazoles of general formula (I), wherein R 1=—C1-C24 alkyl (linear and branched), —C1-C24 alkenyl (linear and branched), —C1-C8 cycloalkyl, —C1-C8 cycloalkyl-alkylhydroxy, —C1-C24 alkylhydroxy (linear and branched), —C1-C24 alkylamine (linear and branched), —C1-C24 alkylaryl (linear and branched), —C1-C24 alkylaryl-alkyl-hydroxy (linear and branched), —C1-C24 alkyl-heteroaryl (linear and branched), —C1-C24-alkyl-O—C1-C24-alkyl (linear and branched), —C1-C24 alkyl morpholino, —C1-C24 alkyl piperidino, —C1-C24 alkyl piperazino, —C1-C24 alkyl-piperazino-N-alkyl, as well as cosmetic or dermatological preparations having an effective content of one or more alkylamidothiazoles, as well as the use thereof for the cosmetic or dermatological treatment and/or prophylaxis of undesired skin pigmentation. | 2014-05-01 |
20140121251 | MICROBICIDAL COMPOSITION - Synergistic microbicidal compositions containing N-methyl-1,2-benzisothiazolin-3-one. | 2014-05-01 |
20140121252 | MICROBICIDAL COMPOSITION - Synergistic microbicidal compositions containing N-methyl-1,2-benzisothiazolin-3-one. | 2014-05-01 |
20140121253 | MICROBICIDAL COMPOSITION - Synergistic microbicidal compositions containing N-methyl-1,2-benzisothiazolin-3-one. | 2014-05-01 |
20140121254 | PHARMACEUTICAL COMPOSITIONS FOR THE TREATMENT OF MOVEMENT DISORDERS - The invention provides a pharmaceutical composition, medical food, dietary supplement or micronutrient for the treatment of a movement disorder comprising an NMDAR agonist or partial agonist as active ingredient therein in combination with a pharmaceutically acceptable carrier. | 2014-05-01 |