35th week of 2013 patent applcation highlights part 61 |
Patent application number | Title | Published |
20130225588 | SUBSTITUTED NAPHTHYLACETIC ACIDS - The invention is concerned with the compounds of formula (I): | 2013-08-29 |
20130225589 | PYRIDOPYRIMIDINONE INHIBITORS OF KINASES - The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, | 2013-08-29 |
20130225590 | SUBSTITUTED TRIAZOLO-PYRIDAZINE DERIVATIVES - This invention relates to novel substituted triazolo-pyridazines, their derivatives, 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 an α1-GABA-A receptor antagonist and/or a α2, α3 and α5 GABA-A receptor agonist. | 2013-08-29 |
20130225591 | IMIDOTHIAZOLE KINASE INHIBITORS - The present invention is directed to novel kinase inhibitors of general formula (I) and pharmaceutically acceptable salts thereof, and to the use of the kinase inhibitors of general formula (I) for treating diseases or disorders in which tau phosphorylation and cell cycle regulation is implicated, such as Alzheimer's Disease and cancer. | 2013-08-29 |
20130225592 | ALDOSE REDUCTASE INHIBITORS AND USES THEREOF - The present invention relates to novel compounds and pharmaceutical compositions thereof, and methods for promoting healthy aging of skin, the treatment of skin disorders, the treatment of cardiovascular disorders, the treatment of renal disorders, the treatment of angiogenesis disorders, such as cancer, treatment of tissue damage, such as non-cardiac tissue damage, the treatment of evolving myocardial infarction, and the treatment of various other disorders, such as complications arising from diabetes with the compounds and compositions of the invention. Other disorders can include, but are not limited to, atherosclerosis, coronary artery disease, diabetic nephropathy, diabetic neuropathy, diabetic retinopathy, infections of the skin, peripheral vascular disease, stroke, and the like. | 2013-08-29 |
20130225593 | DIHYDROPTERIDINONES II - The present invention relates to spiroheterocycl-dihydropyrimidines, their use as modulators of γ-secretase and to pharmaceutical compositions containing said compounds. In particular, the present invention relates to compounds which interfere with γ-secretase and/or its substrate and therefore modulate the formation of Aβ peptides. | 2013-08-29 |
20130225594 | DRUG DERIVATIVES - The present invention relates to derivatives of known active pharmaceutical compounds. These derivatives are differentiated from the parent active compound by virtue of being redox derivatives of the active compound. This means that one or more of the functional groups in the active compound has been converted to another group in one or more reactions which may be considered to represent a change of oxidation state. We refer to these compounds generally as redox derivatives. The derivatives of the invention may be related to the original parent active pharmaceutical compound by only a single step transformation, or may be related via several synthetic steps including one or more changes of oxidation state. In certain cases, the functional group obtained after two or more transformations may be in the same oxidation state as the parent active compound (and we include these compounds in our definition of redox derivatives). In other cases, the oxidation state of the derivative of the invention may be regarded as being different from that of the parent compound. In many cases, the compounds of the invention have inherent therapeutic activity on their own account. In some cases, this activity relative to the same target or targets of the parent compound is as good as or better than the activity which the parent compound has against the target or targets. | 2013-08-29 |
20130225595 | METHOD FOR TREATING PULMONARY ARTERIAL HYPERTENSION IN A PATIENT NOT HAVING IDIOPATHIC PULMONARY FIBROSIS - There is provided a method of treating pulmonary hypertension in a patient in need thereof, said method comprising: administering a therapeutically effective amount of ambrisentan to the patient with pulmonary arterial hypertension, wherein the patient has been determined not to have idiopathic pulmonary fibrosis. | 2013-08-29 |
20130225596 | NOVEL HETEROCYCLIC DERIVATIVE AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME (AS AMENDED) - The present invention provides novel compounds having a P2X | 2013-08-29 |
20130225598 | Stabilized Amorphous Forms of Imatinib Mesylate - The invention relates to the stabilized amorphous form of the methanesulfonic acid addition salt of 4-(4-methylpiperazin-1-ylmethyl)-N-[4-methyl-3-(4-(pyridin-3-yl)-pyrimidin-2-ylamino)-pheny]-benzamide, pharmaceutical compositions such as capsules or tablets containing this form, the use of such form in diagnostic methods or, preferably, for the therapeutic treatment of warm-blooded animals, especially humans, and the use of formulation principles stabilizing the amorphous form of Imatinib mesylate as an intermediate for the preparation of pharmaceutical compositions. | 2013-08-29 |
20130225599 | NOVEL PYRROLIDINE DERIVED BETA 3 ADRENERGIC RECEPTOR AGONISTS - The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of b3-adrenoceptor. Formula (I). | 2013-08-29 |
20130225600 | OXAZOLINE AND ISOXAZOLINE DERIVATIVES AS CRAC MODULATORS - The present invention relates to compounds of Formula (I) along with processes for their preparation that are useful for treating, preventing and/or managing the diseases, disorders, syndromes or conditions associated with the modulation of CRAC. The invention further relates to methods of treating, preventing managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of CRAC of Formula (I). | 2013-08-29 |
20130225601 | NEW COMPOUNDS, PHARMACEUTICAL COMPOSITIONS AND USES THEREOF - The present invention relates to compounds of general formula I, | 2013-08-29 |
20130225602 | 3-SUBSTITUTED-6-(PYRIDINYLMETHOXY)-PYRROLOPYRIDINE COMPOUNDS - The invention provides certain 3-substituted-6-(pyridinylmethoxy)-pyrrolopyridine compounds, particularly compounds of formula I and pharmaceutical compositions thereof. The invention further provides methods of using a compound of formula I to treat Parkinsons disease Formula (I). | 2013-08-29 |
20130225603 | MDM2 INHIBITORS FOR TREATMENT OF OCULAR CONDITIONS - Provided herein are pharmaceutical compositions for the treatment of various ocular diseases characterized by unwanted cellular proliferation. The pharmaceutical compositions may comprise one or more MDM2 inhibitors, and may further comprise one or more additional therapeutic agents. Also provided are methods of use of MDM2 inhibitors and/or formulations thereof for the treatment of ocular diseases characterized by unwanted cellular proliferation. | 2013-08-29 |
20130225605 | ACYLAMINO-SUBSTITUTED FUSED CYCLOPENTANECARBOXYLIC ACID DERIVATIVES AND THEIR USE AS PHARMACEUTICALS - The present invention relates to compounds of the formula I, | 2013-08-29 |
20130225606 | N-HETARYLMETHYL PYRAZOLYLCARBOXAMIDES - The present invention relates to N-Hetarylmethyl pyrazolylcarboxamides derivatives or their thiocarboxamides derivatives, their process of preparation, their use as fungicide, particularly in the form of compositions. Formula (I), and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions. | 2013-08-29 |
20130225607 | METHOD FOR TREATING A PULMONARY HYPERTENSION CONDITION WITHOUT COMPANION DIAGNOSIS - There is provided a method for treating pulmonary hypertension in a subject, comprising: administering to the subject in need thereof a daily dose of ambrisentan from 1 mg to about 15 mg, wherein the method is carried out without drug labeling instruction to monitor liver aminotransferase levels during ambrisentan treatment. | 2013-08-29 |
20130225608 | SUBSTITUTED PYRIMIDINE AMMONIA COMPOUNDS AND USES THEREOF - The invention relates to substituted pyrimidine ammonia compounds. The structure of the compounds is represented as the general formula (I): | 2013-08-29 |
20130225609 | COMBINATIONS OF MEDICAMENTS, CONTAINING PDE4-INHIBITORS AND EP4-RECEPTOR-ANTAGONISTS - The present invention relates to new medicament combinations which contain in addition to one or more PDE4-inhibitors (1) at least one EP4 receptor antagonist (2), as well as the use thereof for the treatment of preferably respiratory complaints such as particularly COPD, chronic sinusitis and asthma. | 2013-08-29 |
20130225610 | ANTIMETASTATIC COMPOUNDS - Screening methods for identifying compounds and compounds and pharmaceutical compositions for treating and preventing cancer are disclosed. The compounds affect signal transduction downstream of the MET receptor. | 2013-08-29 |
20130225611 | Compositions and Methods for Reducing Cancer Cell Proliferation and Modulating Importin-Beta Function - The present disclosure provides methods of reducing proliferation of cancer cells. The methods include contacting the cancer cells with a 2,4-diaminoquinazoline compound. Also provided are methods of modulating importin-beta function (e.g., importin-beta-mediated nuclear import) in eukaryotic cells. The methods include contacting the eukaryotic cells with a 2,4-diaminoquinazoline compound. Pharmaceutical formulations that include a 2,4-diaminoquinazoline compound are also provided. | 2013-08-29 |
20130225612 | QUINAZOLINE DERIVATIVES, COMPOSITIONS, AND USES RELATED THERETO - The invention relates to quinazoline derivatives, compositions, and methods related thereto. In certain embodiments, the invention relates to inhibitors of NADPH-oxidase. | 2013-08-29 |
20130225613 | QUINAZOLINE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS THEREOF - The present invention relates to novel quinazoline derivatives with less skin irritation and an excellent action of strongly suppressing scratching behavior, and pharmaceutical compositions containing a quinazoline derivative as an active ingredient. The present invention is directed to the quinazoline derivatives represented by the general formula [1] or pharmaceutically acceptable salts thereof. In the general formula [1], R | 2013-08-29 |
20130225614 | 4-AZOLYLAMINOQUINAZOLINE DERIVATIVES AND METHODS OF USE THEREOF - Provided herein are 4-azolylaminoquinazoline compounds for treatment of JAK kinase mediated diseases, including JAK2 kinase-, JAK3 kinase- or TYK2 kinase-mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions. | 2013-08-29 |
20130225615 | 2-CYCLOQUINAZOLINE DERIVATIVES AND METHODS OF USE THEREOF - Provided herein are 2-cycloquinazoline compounds for treatment of JAK kinase mediated diseases, including JAK2 kinase-, JAK3 kinase- or TYK2 kinase-mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions. | 2013-08-29 |
20130225616 | CRYSTALLINE FORM OF PYRIMIDIO[6,1-A] ISOQUINOLIN-4-ONE COMPOUND - The current invention is directed towards a polymorph of N-{2-[(2E)-2-(mesitylimino)-9,10-dimethoxy-4-oxo-6,7-dihydro-2H-pyrimido[6,1-a]-isoquinolin-3(4H)-yl]ethyl}urea, in the form of a crystalline solid consisting of greater than 99% by weight of N-{2-[(2E)-2-(mesitylimino)-9,10-dimethoxy-4-oxo-6,7-dihydro-2H-pyrimido[6,1-a]-isoquinolin-3(4H)-yl]ethyl}urea, at least 95% in the polymorphic form of a thermodynamically stable polymorph (I) of N-{2-[(2E)-2-(mesitylimino)-9,10-dimethoxy-4-oxo-6,7-dihydro-2H-pyrimido[6,1-a]-isoquinolin-3(4H)-yl]ethyl}urea, wherein said polymorph is determined by single crystal X-ray structural analysis and X-ray powder diffraction pattern. | 2013-08-29 |
20130225617 | INDOLES AND THEIR THERAPEUTIC USE - Compounds of the invention are ligands of the CRTH2 receptor, useful inter alia for treatment of inflammatory conditions. | 2013-08-29 |
20130225618 | AGENT FOR INHIBITING EXPRESSION OF LIPID METABOLISM RELATED MRNA - The present invention is intended to provide a pharmaceutical product for inhibiting expression of at least one lipid metabolism related mRNA selected from the group consisting of Angptl4 mRNA, SCD-1 mRNA, and SREBP1c mRNA, the present invention is also intended to provide a preventive and/or therapeutic agent for various diseases based on inhibition of expression of at least one lipid metabolism related mRNA selected from the group consisting of Angptl4 mRNA, SCD-1 mRNA, and SREBP1c mRNA, and the present invention relates to an agent for inhibiting expression of at least one lipid metabolism related mRNA selected from the group consisting of Angptl4 mRNA, SCD-1 mRNA, and SREBP1c mRNA, and relates also to a preventive and/or therapeutic agent for various diseases based on the inhibition of the expression of at least one lipid metabolism related mRNA selected from the group consisting of Angptl4 mRNA, SCD-1 mRNA, and SREBP1c mRNA, the agent comprising a compound represented by Formula (I), its salt, or a solvate of any of them as an active ingredient: | 2013-08-29 |
20130225619 | SUBSTITUTED HETEROCYCLIC COMPOUNDS FOR DISEASE TREATMENT - The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are substituted heterocyclic amine derivative compound and pharmaceutical compositions comprising these compounds. The subject compositions are useful for treating and preventing ophthalmic diseases and disorders, including age-related macular degeneration (AMD) and Stargardt's Disease. | 2013-08-29 |
20130225620 | SERINE/THREONINE KINASE INHIBITORS - Compounds having the formula I wherein A, Z, R | 2013-08-29 |
20130225621 | SUBSTITUTED 2-HYDROXY-4-(2-(PHENYLSULFONAMIDO)ACETAMIDO)BENZOIC ACID ANALOGS AS INHIBITORS OF STAT PROTEIN - In one aspect, the invention relates to substituted 2-hydroxy-4-(2-(phenylsulfonamido)acetamido)benzoic acid analogs, derivatives thereof, and related compounds, which are useful as inhibitors of STAT protein activity; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating disorders of uncontrolled cellular proliferation associated with a STAT protein activity dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention. | 2013-08-29 |
20130225622 | Crystalline Form of Bis[(E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]- pyrimidin-5-yl](3R,5S)-3,5-dihydroxyhept-6-enoic acid] Calcium Salt - Two polymorphic forms of bis[(E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]pyrimidin-5-yl](3R,5S)-3,5-dihydroxyhept-6-enoic acid] calcium salt, processes for making them and their use as HMG Co-A reductase inhibitors are described. | 2013-08-29 |
20130225623 | Methods of Treating Psychiatric or Neurological Disorders with MGLUR Antagonists - Methods for treating a psychiatric or neurological disease or disorder using combinations of Group 1 mGluR antagonists are disclosed. In certain aspects, these methods include the treatment of a patient having a neurological or psychiatric disease or disorder associated with a CYFIP1 gene change. | 2013-08-29 |
20130225624 | BICYCLIC HETEROCYCLIC SPIRO COMPOUNDS - There are provided certain bicyclic heterocyclic compounds that act as M1 muscarinic receptor modulators. Compositions containing these compounds and their use are also disclosed. | 2013-08-29 |
20130225625 | TAMPER-RESISTANT PHARMACEUTICAL DOSAGE FORM COMPRISING NONIONIC SURFACTANT - The invention relates to a pharmaceutical dosage form having a breaking strength of at least 500 N and comprising a pharmacologically active compound, a polyalkylene oxide having an average molecular weight of at least 200,000 g/mol, and a nonionic surfactant; wherein the content of the polyalkylene oxide is within the range of from 20 to 75 wt.-%, based on the total weight of the pharmaceutical dosage form. | 2013-08-29 |
20130225626 | SUBLINGUAL FILMS - The invention features sublingual film formulations of dopamine agonists and methods of treating Parkinson's disease, tremors, restless leg syndrome, sexual dysfunction, and depressive disorders therewith. | 2013-08-29 |
20130225627 | DEXTROMETHORPHAN ANTITUSSIVE COMPOSITIONS - The invention provides orally administered antitussive pharmaceutical compositions comprising dextromethorphan, wherein the compositions are free of bromide, sodium and polistirex. | 2013-08-29 |
20130225628 | CARBOXAMIDE BIOISOSTERES OF OPIATES - A compound of formula I is disclosed. | 2013-08-29 |
20130225629 | TARGETING PI3K/MTOR SIGNALLING AND NEUTROPHIL RECRUITMENT FOR TREATMENT OF ENTERITIS - The presently disclosed subject matter generally relates to methods and compositions for treating enteritis. More particularly, the presently disclosed subject matter relates to methods and compositions for modulating a component of a PI3K/mTOR pathway. In some embodiments, the methods and compositions of the presently disclosed subject matter generally relates to the treatment of campylobacteriosis. More particularly, the methods and compositions of the presently disclosed subject matter relate to the treatment of campylobacteriosis by modulating a component of a PI3K/mTOR pathway. | 2013-08-29 |
20130225630 | TOPICAL RAPAMYCIN FOR TREATMENT OF FACIAL ANGIOFIBROMAS IN TUBEROUS SCLEROSIS - The present disclosure provides for a method and a topical composition to treat facial angiofibromas in Tuberous Sclerosis by applying from about | 2013-08-29 |
20130225631 | TOPICAL RAPAMYCIN FOR TREATMENT OF FACIAL ANGIOFIBROMAS IN TUBEROUS SCLEROSIS - The present disclosure provides for a method and a topical composition to treat facial angiofibromas in Tuberous Sclerosis by applying from about 0.25% to about 2% rapamycin to a small body surface area. | 2013-08-29 |
20130225632 | CALCIUM SALT OF PYRROLOQUINOLINE QUINONE - An object of the present invention is to provide an industrially useful method for producing a calcium salt of pyrroloquinoline quinone, without using large amounts of organic solvents, and highly pure crystals produced thereby. According to the present invention, a highly pure calcium salt of pyrroloquinoline quinone can be produced by reacting an alkali metal salt of pyrroloquinoline quinone with a source of calcium ions. | 2013-08-29 |
20130225633 | PHENYL HETEROCYCLOALKYL GLUCOCORTICOID RECEPTOR MODULATORS - The present invention provides phenyl-heterocycloalkyl fused azadecalin compounds and methods of using the compounds as glucocorticoid receptor modulators. | 2013-08-29 |
20130225634 | ANTI-CANCER COMPOUNDS - The present invention relates to anti-cancer compounds, methods for their discovery, and their therapeutic use. In particular, the present invention provides analogs of the known anti-cancer compound amonafide, and structurally and functionally related compounds, and methods of using such compounds as therapeutic agents to treat a number of conditions associated with hyperproliferation. | 2013-08-29 |
20130225635 | FUSED BICYCLIC DIAMINE DERIVATIVES AS HIV ATTACHMENT INHIBITORS - Compounds of Formula I, including pharmaceutically acceptable salts thereof: | 2013-08-29 |
20130225636 | N-(5S,6S,9R)-5-AMINO-6-(2,3-DIFLUOROPHENYL)-6,7,8,9-TETRAHYDRO-5H-CYCLOHEP- TA[B]PYRIDIN-9-YL-4-(2-OXO-2,3-DIHYDRO-1H-IMIDAZO[4,5-B]PYRIDIN-1-YL)PIPER- IDINE-1-CARBOXYLATE SALT - Disclosed is a hemisulfate salt of Compound (I): | 2013-08-29 |
20130225637 | ISATIN DERIVATIVES, PHARMACEUTICAL COMPOSITIONS THEREOF, AND METHODS OF USE THEREOF - One aspect of the invention relates to novel isatin derivative compounds and the pharmaceutical composition thereof. Another aspect of the invention relates to methods of using the isatin derivative compounds disclosed herein and the pharmaceutical compositions thereof. In certain embodiments, the method is used to treat a cancer or a tumor in a subject including, without limitation, prostate cancer, melanoma, pancreatic cancer, ovarian cancer, and lymphoma. In certain embodiment, the method is used to treat a condition in a subject that can be regulated by the activation of one or more proteins such as EGFR, Erk1/2, Her2/Neu, Jak2, Src, Stat3, Akt, Cyclin B1, and Cdc25C. In certain embodiment, the method is used to treat a condition in a subject that can be regulated by the disruption of microtubule formations. | 2013-08-29 |
20130225638 | IMIDAZOLE DERIVATIVES AND PREPARATION METHOD AND USE THEREOF - Disclosed are imidazole derivatives as represented by formula (I), and preparation method and use thereof. The compounds can inhibit cyclooxygenase and treat diseases mediated by cyclooxygenase. | 2013-08-29 |
20130225639 | ALTERING PHARMACOKINETICS OF PIRFENIDONE THERAPY - The invention relates to methods for reducing adverse events in patients receiving pirfenidone (5-methyl-1-phenyl-2-(1H)-pyridone) therapy. | 2013-08-29 |
20130225640 | CYANOACRYLATE-BASED BIO-ADHESIVE COMPOSITION - The present invention relates to a cyanoacrylate-based bio-adhesive composition, and aims to provide a cyanoacrylate-based bio-adhesive composition having an excellent biodegradability and anti-bacterial effect. The present invention provides a cyanoacrylate-based bio-adhesive composition having an enhanced biodegradability by using, as a thickening agent, poly octyl cyanoacrylate generated as a byproduct when preparing octyl cyanoacrylate, and having an excellent anti-bacterial effect by using 3,5-diiodo-4-pyridone-1-acetic acid as an anion stabilizer. | 2013-08-29 |
20130225641 | ANTICANCER COMPOUNDS AND PREPARATION METHODS THEREOF - Two new compounds with anticancer effects of N-[4-chloro-3-(trifluoromethyl)phenyl]-[4-(N-methyl-formamide)(4-pyridyloxy)phenyl]-thiourea and N-[4-chloro-3-(trifluoromethyl)phenyl]-[4-(N-methyl-formamide)(4-pyridylthio)phenyl]-thiourea, and salts thereof are disclosed. Preparation methods of the two new compounds and pharmaceutical compositions containing the new compounds are further disclosed. Experimental studies show that the two new compounds can effectively inhibit the activity of Raf and VEGFR protein kinase, widely inhibit growth of various types of human tumor cell lines and further induce apoptosis of tumor cells. Human tumor heterograft model investigation proves that the two new compounds are effective antineoplastic agents, and can sharply inhibit growth of human liver cancer cells, lung cancer cells and intestinal cancer cells in vivo. Furthermore, the anticancer effects of the compounds are much better than that of Sorafenib. | 2013-08-29 |
20130225642 | PHARMACEUTICAL COMPOSITION FOR PREVENTION AND TREATMENT OF AMYOTROPHIC LATERAL SCLEROSIS - The present invention provides a prophylactic or therapeutic agent for amyotrophic lateral sclerosis, containing a 1,3-diphenylurea derivative or multikinase inhibitor. | 2013-08-29 |
20130225643 | ENDOGENEOUS REPAIR FACTOR PRODUCTION ACCELERATORS - It relates to an endogenous repair factor production accelerator which comprises one or at least two selected from prostaglandin (PG) I2 agonist, EP2 agonist and EP4 agonist. Since prostaglandin (PG) I2 agonist, EP2 agonist or EP4 agonist has various endogenous repair factor production accelerating action, angiogenesis acceleration action and stem cell differentiation induction action, it is useful as preventive and/or therapeutic agents for ischemic organ diseases (e.g., arteriosclerosis obliterans, Buerger disease, Raynaud disease, myocardial infarction, angina pectoris, diabetic neuropathy, spinal canal stenosis, cerebrovascular accidents, cerebral infarction, pulmonary hypertension, bone fracture, Alzheimer disease, etc.) and various cell and organ diseases. | 2013-08-29 |
20130225644 | MODIFIED LYSINE-MIMETIC COMPOUNDS - Lysine mimetic compounds having useful pharmacological activity such as antiarrhythmic activity and desirable bioavailability properties are disclosed. | 2013-08-29 |
20130225645 | ORAL FORMULATIONS FOR TREATING METAL OVERLOAD - The present invention provides, among other things, effective oral formulations based on desazadesferrithiocin polyether (DADFT-PE) analogues, salts and polymorphs thereof, as well as their application for treatment of metal overload, in particular, iron overload, and associated diseases, disorders and conditions. | 2013-08-29 |
20130225646 | SUBSTITUTED N-PHENETHYLTRIAZOLONEACETAMIDES AND USE THEREOF - The present application relates to novel substituted N-phenethyltriazoloneacetamides, to processes for preparing them, to their use alone or in combinations for the treatment and/or prevention of diseases and also to their use for the production of medicaments for the treatment and/or prevention of diseases, more particularly for the treatment and/or prevention of cardiovascular disorders. | 2013-08-29 |
20130225647 | COMBINATION THERAPY WITH PARP INHIBITORS - The present invention describes benzimidazole derivatives of Formula (I) which constitute potent PARP inhibitors in combination with radiotherapy or in combination with other chemotherapeutic agents. | 2013-08-29 |
20130225648 | Methods for Treating Cognitive/Attention Deficit Disorders Using Tetrahydroindolone Analogues and Derivatives - Methods for treating cognitive/attention deficit disorders in general using tetrahydroindolone derivatives and analogues, particularly tetrahydroindolone derivatives or analogues in which the tetrahydroindolone derivative or analogue is covalently linked to another moiety to form a bifunctional conjugate are disclosed. More specifically, methods and compositions for treating attention deficit disorder and attention deficit hyperactivity disorders in adults and children as well as mild cognitive impairment and dementia are provided. The compounds used to treat and/or palliate cognitive/attention deficit disorders in general include a tetrahydroindolone derivative or analogue comprises a 9-atom bicyclic moiety, moiety A, linked through a linker L to a moiety B, where B is a carboxylic acid, a carboxylic acid ester, or a moiety of the structure N(Y | 2013-08-29 |
20130225649 | COMPOUNDS FROM ANTRODIA CINNAMOMEA AND USE THEREOF - The present invention relates to compounds from | 2013-08-29 |
20130225650 | METHOD FOR PROMOTING SYNTHESIS OF TISSUE COLLAGEN - An object of the present invention is to provide an oral preparation for promoting synthesis of tissue collagen, an oral preparation for promoting healing of skin wounds or an oral preparation for preventing or improving skin wrinkles or sagging, which is safe and has an excellent effect. The present invention can provide an oral preparation for promoting synthesis of tissue collagen, an oral preparation for promoting healing of skin wounds or an oral preparation for preventing or improving skin wrinkles or sagging, which comprises hydroxyproline or a salt thereof as an active ingredient. | 2013-08-29 |
20130225651 | siRNA Compositions and Methods for Potently Inhibiting Viral Infection - No antiviral regimen has been consistently successful in treating H5N1 virus infection. We demonstrate that a group of highly effective siRNAs targeting different H5N1 viral genes shares a unique motif, GGAGU/ACUCC. We further demonstrate that the effectiveness of siRNAs containing this motif is not sequence specific. The results suggested that the structure of the unique motif is critical in determining the potency of siRNA-mediated protective effects against viral infection and this potent in vivo protection is associated with early productions of β-defensin and IL-6 induced by the motif. Provided are methods and prophylactic and therapeutic agents useful against other viral infections in addition to the H5N1 influenza virus. | 2013-08-29 |
20130225652 | SEGMENTED MICRO RNA MIMETICS - This invention relates generally to segmented oligonucleotides capable of modulating gene expression. Specifically, the instant invention relates to segmented microRNA (miRNA) oligonucleotides, including segmented miRNA precursors and segmented pre-microRNAs. The invention also relates to compositions comprising such segmented oligonucleotides, as well as to methods of making and using such oligonucleotides for diagnosis and treatment of diseases associated or causally linked to aberrant levels or activities of gene expression, including aberrant levels of coding and/or non-coding RNA. | 2013-08-29 |
20130225653 | MICRORNA-BASED SHORT HAIRPIN RNA FOR GENE KNOCKDOWN OF NR1 SUBUNIT OF N-METHYL-D-ASPARTATE RECEPTOR AND ITS APPLICATION ON PHARMACEUTICS - The present invention relates to a microRNA-based short hairpin RNA for gene silencing the genetic expression of NR1 subunit of N-methyl-D-aspartate receptor comprises a single strand RNA fragment comprising a first fragment, a second fragment and a connecting fragment, wherein the first fragment and the second fragment are complementary to each other, and are spaced and connected by the connecting fragment, with the connecting fragment being randomly arranged nucleotides, with the first fragment having a Drosha recognized cleavage site, a silencing site and a Dicer recognized cleavage site, with the Drosha recognized cleavage site and the Dicer recognized cleavage site being spaced and connected by the silencing site, with the silencing site encoding homologous nucleotides corresponding to NR1 subunit of subcutaneous N-methyl-D-aspartate receptor. | 2013-08-29 |
20130225654 | Compositions And Methods for Inhibiting Expression Of A Gene From the Ebola Virus - The invention relates to a double-stranded ribonucleic acid (dsRNA) for inhibiting the expression of a gene from the Ebola virus. | 2013-08-29 |
20130225655 | Combinations of TGFBeta and COX-2 Inhibitors and Methods for Their Therapeutic Application - The present invention provides compositions and methods for using combinations of TGFβ1 and Cox-2 inhibitors and TGFβ1 and Hoxb13 inhibitors for the treatment of various medical conditions, including skin scaring due to trauma wounds and surgery, corneal and retina scaring due to injury and surgery, internal organ scaring due to injury and surgery, heart tissue scaring due to heart attack and surgery, and lung, liver, and kidney fibrosis due to inflammation and injury. One example is to use siRNA inhibitors to silence TGFβ1 and Cox-2 at the same time, resulting in significant less scar formation. | 2013-08-29 |
20130225656 | ANALYZING SEMAPHORIN7A (Sema7A) LEVELS FOR ASSESSING CANCER METASTATIC POTENTIAL AND METHODS OF TREATMENT - Methods, assays, and kits for determining a cancer's (e.g., breast cancer) metastatic potential and tumor aggressiveness in a subject (e.g., a human patient) and for measuring a subject's response to cancer therapy involve analyzing expression of Sema7A in a biological sample from the subject, and correlating increased expression of Sema7A in the biological sample compared to a control sample with metastatic potential of the cancer, wherein the expression of Sema7A is linearly proportional to the metastatic potential of the cancer in the subject. These methods, kits and assays provide for individualized diagnosis and treatment options for cancer (e.g., breast cancer) patients. They can be used independently, or can be combined with additional diagnostic tests and/or prognostic methods. Compositions, kits and methods for treating a subject having cancer (e.g., breast cancer) include administering a composition for inhibiting Sema7A expression or activity to the subject. | 2013-08-29 |
20130225657 | SiRNA TARGETING ETS1 AND ELK1 AND METHOD OF USING SAME IN THE INHIBITION OF CIP2A GENE IN CANCER TREATMENT - Disclosed are methods of attenuating activity of the gene promoter of CIP2A. siRNAs are used to target against Ets1 and Elk1 transcriptional factors, thereby blocking the binding of Ets1 and Elk1 to the CIP2A gene promoter. It is disclosed that the siRNAs targeted against Ets1 and Elk1 attenuate the gene expression of CIP2A. A kit containing siRNA reagents for attenuating the CIP2A gene expression is also disclosed. | 2013-08-29 |
20130225658 | MICRORNAS THAT REGULATE MUSCLE CELL PROLIFERATION AND DIFFERENTIATION - The presently disclosed subject matter provides methods and compositions for modulating gene expression in myocytes. Also provided are cells comprising the compositions of the presently disclosed subject matter. | 2013-08-29 |
20130225659 | MODULATION OF NUCLEAR-RETAINED RNA - Provided herein are methods, compounds, and compositions for reducing expression of a nrRNA in an animal. Also provided herein are methods, compounds, and compositions for treating, ameliorating, delaying or reducing a symptom of a disease or disorder associated with a nuclear-retained RNA in an animal. Such methods, compounds, and compositions are useful to treat, prevent, delay, or ameliorate a disease or condition associated with a nuclear-retained RNA, or a symptom thereof. | 2013-08-29 |
20130225660 | COMPOSITIONS AND METHODS FOR SPECIFIC CLEAVAGE OF EXOGENOUS RNA IN A CELL - There are provided compositions for cleaving an exogenous RNA of interest only in the presence of an endogenous signal RNA sequence, thereby activating expression of a polynucleotide of interest only in the presence of the endogenous signal RNA sequence. There are provided methods for the preparation of the composition and uses thereof in treatment and diagnosis of various conditions and disorders, for example by selectively activating expression of a toxin only in specific target cell populations. | 2013-08-29 |
20130225661 | Inhibitors Of SP140 And Their Use In Therapy - A method of treating autoimmune and inflammatory diseases or conditions in a mammal, such as a human, which comprises the administration of a inhibitor of bromodomain-containing protein: SP140. | 2013-08-29 |
20130225662 | METHODS AND COMPOSITIONS OF MOLECULAR PROFILING FOR DISEASE DIAGNOSTICS - The present invention relates to compositions, kits, and methods for molecular profiling and cancer diagnostics, including but not limited to gene expression product markers, alternative exon usage markers, and DNA polymorphisms associated with cancer. In particular, the present invention provides molecular profiles associated with thyroid cancer, methods of determining molecular profiles, and methods of analyzing results to provide a diagnosis. | 2013-08-29 |
20130225663 | LIPID DELIVERY FORMULATIONS - The invention provides formulations that contain an immunogenic or immunostimulatory cargo, delivery moiety and/or lipid, and a lipid that functions to reduce or prevent induction in a subject of an immune response which would otherwise occur when the immunogenic or immunostimulatory cargo, delivery moiety and/or lipid is administered to a subject as a component of an appropriate control formulation lacking the immune response reducing lipid. Specific immune response reducing lipids and uses thereof are further provided. | 2013-08-29 |
20130225664 | METHODS AND COMPOSITIONS FOR DECREASING CHRONIC PAIN - The present invention provides compositions and methods for the selective silencing of neurons in pain pathway by using a combination of inhibitory light-sensitive protein gene transfer and wavelength specific illumination. | 2013-08-29 |
20130225665 | MICRORNAS THAT REGULATE MUSCLE CELL PROLIFERATION AND DIFFERENTIATION - The presently disclosed subject matter provides methods and compositions for modulating gene expression in myocytes. Also provided are cells comprising the compositions of the presently disclosed subject matter. | 2013-08-29 |
20130225666 | DELIVERY OF POLYNUCLEOTIDES USING RECOMBINANT AAV9 - The present invention relates to Adeno-associated virus 9 methods and materials useful for systemically delivering polynucleotides across the blood brain barrier. Accordingly, the present invention also relates to methods and materials useful for systemically delivering polynucleotides to the central and peripheral nervous systems. The present invention also relates to Adeno-associated virus type 9 methods and materials useful for intrathecal delivery of polynucleotides. Use of the methods and materials is indicated, for example, for treatment of lower motor neuron diseases such as spinal muscle atrophy and amyotrophic lateral sclerosis as well as Pompe disease and lysosomal storage disorders. Use of the methods and materials is also indicated, for example, for treatment of Rett syndrome. | 2013-08-29 |
20130225667 | siRNA Targeting Cyclin-dependent Kinase Inhibitor 1B (p27, Kip1) (CDKN1B) - Efficient sequence specific gene silencing is possible through the use of siRNA technology. By selecting particular siRNAs by rational design, one can maximize the generation of an effective gene silencing reagent, as well as methods for silencing genes. Methods, compositions, and kits generated through rational design of siRNAs are disclosed including those directed to nucleotide sequences for CDKN1B. | 2013-08-29 |
20130225668 | ANTI-VASCULAR ENDOTHELIAL GROWTH FACTOR RECEPTOR-2 CHIMERIC ANTIGEN RECEPTORS AND USE OF SAME FOR THE TREATMENT OF CANCER - The invention provides chimeric antigen receptors (CARs) comprising an antigen binding domain of a KDR-1121 or DC101 antibody, an extracellular hinge domain, a T cell receptor transmembrane domain, and an intracellular domain T cell receptor signaling domain. Nucleic acids, recombinant expression vectors, host cells, populations of cells, antibodies, or antigen binding portions thereof, and pharmaceutical compositions relating to the CARs are disclosed. Methods of detecting the presence of cancer in a host and methods of treating or preventing cancer in a host are also disclosed. | 2013-08-29 |
20130225669 | STERILIZATION OF PROTEINACEOUS BIOMATERIALS AND TISSUES WITH GENIPIN - The invention contemplates a method for sterilizing protein or collagen-based hard and soft tissues, from animal and human donors or created synthetically by exposure to genipin, an active compound found in gardenia fruit extract. Genipin sterilizes the tissues through crosslinking the organic framework of microbes while maintaining or enhancing mechanical strength of the tissue graft by stabilizing the collagen backbone with crosslinks bone allografts experience significant and repetitive loads during their duty cycle, sterilizing bone allografts without causing a loss in biomechanical properties is quite important. | 2013-08-29 |
20130225670 | Methods of Treating Asthma Using Statins - The present disclosure generally provides methods for assessing a subject's responsiveness to a statin therapy, and selection of a statin dose based upon such methods. The disclosure further provides methods for treating asthma by administering a statin therapy. | 2013-08-29 |
20130225671 | Methods of Treating Seizure Disorders - Seizure disorders are treated by Ras inhibitors. In an embodiment, the Ras inhibitor includes a farnesyl transferase inhibitor. In another embodiment, the farnesyl transferase inhibitor includes a 3-hydroxy-3-methylglutaryl-Coenzyme A reductase inhibitor. In another embodiment, the 3-hydroxy-3-methylglutaryl-Coenzyme A reductase inhibitor is not a Ras inhibitor. Subjects having fragile X syndrome, autism, Angelman syndrome, Costello syndrome, cardio facio cutaneous syndrome, neurofibromatosis type I, Noonan syndrome and Coffin-Lowry syndrome that have seizure disorders can be treated. | 2013-08-29 |
20130225672 | SUBSTITUTED 4-BETA-ACRYLAMIDOPODOPHYLLOTOXIN CONGENERS AS ANTITUMOUR ANTIBIOTICS AND THE PROCESS FOR PREPARATION THEREOF - The present invention provides compounds of general formula (3) as useful potential antitumour agents against human cancer cell lines. The present invention further provides a process for the synthesis of 4β-acrylamidopodophyllotoxin congeners of general formula (3), wherein R and R1 are an aryl group and R is selected from 3,4,5-trimethoxyphenyl or 2-methoxy phenyl and R1 is selected from the group consisting of 4-hydroxy-3-methoxyphenyl, 3-hydroxy-4-methoxyphenyl, 4-fluoro-3-methoxyphenyl, 3-fluoro-4-methoxyphenyl, 2-fluoro-5-methoxyphenyl, 2-fluoro-4-methoxyphenyl, 4-hydroxy-3-nitrophenyl, 4-methoxy-3-nitrophenyl, 4-nitrophenyl, 3-nitrophenyl, 2-nitro phenyl, 4-methoxyphenyl, 3-methoxyphenyl and 4-hydroxyphenyl. | 2013-08-29 |
20130225673 | DEVELOPING POTENT URATE TRANSPORTER INHIBITORS: COMPOUNDS DESIGNED FOR THEIR URICOSURIC ACTION - A compound represented by the general Formula I: | 2013-08-29 |
20130225674 | USE OF DIBENZOFURANONE DERIVATIVES TO INHIBIT KINASES - The invention relates to a pharmaceutical product comprising a dibenzofuranone derivative as the active ingredient. The invention further relates to the use of dibenzofuranone derivatives to inhibit kinases, in particular serine/threonine kinases, to the use of dibenzofuranone derivatives for producing drugs and/or medicinal products for treatment, and to the use of dibenzofuranone derivatives as a diagnostic product for analyzing the role of protein kinases, in particular serine/threonine kinases, in particular protein kinase CK2 in cellular processes, the pathogenesis of diseases, ontogenesis and/or other developmental biological phenomena or relationships. | 2013-08-29 |
20130225675 | BACTERIAL CONTROL OF WATER BASED FLUIDS DURING SUBSURFACE INJECTION AND SUBSEQUENT RESIDENCE TIME IN THE SUBTERRANEAN FORMATION - Apparatus and methods to prevent the proliferation of undesired life forms in a subterranean formation, comprising forming a fluid comprising an inhibitor; and introducing the inhibitor to a surface in the formation. Apparatus and methods to prevent the proliferation of undesired life forms along a surface of tubular or equipment for use in the oil field services industry, comprising forming a coating comprising an inhibitor; and introducing the coating to a surface of the tubular or equipment. Apparatus and methods to prevent the proliferation of undesired life forms along a surface of tubular or equipment for use in the oil field services industry, comprising forming a material comprising an inhibitor; and embedding the material into a surface of the tubular or equipment. | 2013-08-29 |
20130225676 | VIRAL INHIBITOR COMPOSITIONS FOR IN VIVO THERAPEUTIC USE COMPRISING A COMBINATION OF (-) -CARVONE, GERANIOL AND A FURTHER ESSENTIAL OIL COMPONENT - The present invention concerns an antiviral composition comprising the following components: R-(−)-2-methyl-5-(prop-1-en-2-yl)-cyclohex-2-enone (also called (−) carvone) and S-(+)-2-methyl-5-(prop-1-en-2-yl)-cyclohex-2-enone (also called (+) carvone) and ( | 2013-08-29 |
20130225677 | THERAPEUTIC COMPOSITIONS - Ingenol angelate is a potent anticancer agent, and can be stabilised by dissolving it in an aprotic solvent in the presence of an acidic buffer. | 2013-08-29 |
20130225678 | THERAPEUTIC COMPOSITIONS - Ingenol angelate is a potent anticancer agent, and can be stabilised by dissolving it in an aprotic solvent in the presence of an acidic buffer. | 2013-08-29 |
20130225679 | ANALGESIC COMPOUNDS, METHODS, AND FORMULATIONS - Provided are analgesic compounds, and salts thereof, of formula: (I) wherein A is: (A) Additionally, pharmaceutical formulations and methods of use employing the above compounds are provided. | 2013-08-29 |
20130225680 | COMPOUND, COMPOSITION AND USES THEREOF - The disclosure herein provides the compounds of Formulas 1 and its pharmaceutical acceptable salts, as well as polymorphs, solvates, and hydrates thereof. These salts may be formulated as pharmaceutical compositions. The pharmaceutical compositions may be formulated for oral administration, transdermal administration, and/or injection. Such compositions may be used for the treatment of metabolic conditions, cystinosis, non-alcoholic Steatohepatitis, hypertriglyceridemia, and/or neurodegenerative disorders, and/or their associated complications. | 2013-08-29 |
20130225681 | Phenylketone Carboxylate Compounds and Pharmaceutical Uses Thereof - Phenylketone carboxylate compounds of Formula I, wherein n=2-6; R═C(0); —OC(O)— or —CH(OH)—; A is (CH2)mCOOH, W(CH2)mCOOH or YCH(COOH)((CH2)pCH3) when B is Ft B is (CH2)mCOOH, W(CH2)mCOOH or YCH(COOH)((CH2)pCH3) when A is Ft or A and B form a 5-7 membered cycloalkyl substituted with COOFt W=0, S or NFt Y=0,S,NH or CH2; m=0-2; p=1-7; have been prepared. These compounds and their pharmaceutically acceptable salts have beneficial therapeutic effects to prevent or treat a condition related to (l) blood disorders, (ii) inflammation related diseases, (iii) renal disorders and/or renal disorders complications, or (iv) fibrosis-related organ dysfunction. | 2013-08-29 |
20130225682 | Use of Medium Chain Triglycerides for the Treatment and Prevention of Alzheimer's Disease and Other Diseases Resulting from Reduced Neuronal Metabolism II - Methods and compositions for treating or preventing, the occurrence of senile dementia of the Alzheimer's type, or other conditions arising from reduced neuronal metabolism and leading to lessened cognitive function are described. In a preferred embodiment the administration of triglycerides or fatty acids with chain lengths between 5 and 12, to said patient at a level to produce an improvement in cognitive ability. | 2013-08-29 |
20130225683 | Compounds and Pharmaceutical Compositions for Uses in Diabetes - New uses for phenylketone carboxylate compounds and substituted aromatic compounds of Formula I, Formula I, IA, IB and IC, and their pharmaceutical acceptable salts are described for prevention or treatment of diabetes or a diabetes-related disorder in a subject in need thereof. Diabetes and diabetes-related disorder include Type I diabetes, Type II diabetes, maturity-onset diabetes of the young, latent autoimmune diabetes of adults (LADA), gestational diabetes, diabetic nephropathy, proteinuria, ketonuria, obesity, hyperglycemia, glucose intolerance, insulin resistance, hyperinsulinemia, hypercholesterolemia, hypertension, hyperlipoproteinemia, hyperlipidemia, hypertriglyceridemia, dyslipidemia, metabolic syndrome, syndrome X, diabetic neuropathy, diabetic retinopathy, hypoglycemia, cardiovascular disease, atherosclerosis, diabetic kidney disease, ketoacidosis, thrombotic disorders, sexual dysfunction, dermatopathy, edema, metabolic syndrome and renal disorders. The related pharmaceutical compositions and methods are also described. These compounds can be used in combination with comprising a therapeutic agent for lowering or controlling blood glucose level such as metformin or a thiazolidinedione. | 2013-08-29 |
20130225684 | METHODS AND COMPOSITIONS FOR ENHANCEMENT OF VISION PERFORMANCE - A vision performance enhancing composition and method to enhance vision performance using alanylgiutarnine or a salt of alanylglutamine as an active ingredient. | 2013-08-29 |
20130225685 | COMBINATION COMPOSITION - An intravenous composition for providing relief for pain and/or inflammation, the composition having ibuprofen and paracetamol in combination for delivering to a human at each dose:
| 2013-08-29 |
20130225686 | SOLID FORMS OF AN N-(PHENYLMETHYL) PROPANAMIDE DERIVATIVE AND PROCESSES OF PREPARATION - The invention relates to solid forms of the anti-epileptic agent lacosamide (I). The invention also relates to mixtures of solid forms of lacosamide. The invention further relates to mixtures of lacosamide enantiomers crystallized in a conglomerate Form and the use thereof in providing enantiomerically enriched lacosamide, preferably lacosamide enriched with the (R)-enantiomer of lacosamide. | 2013-08-29 |
20130225687 | COMPOUNDS AND METHODS FOR PKC THETA INHIBITION - The present invention provides a method of selectively inhibiting PKCθ in the presence of PKCδ, by administering to a subject in need thereof, a therapeutically effective amount of a compound of Formula I. The present invention also provides a method of inhibiting cytokine synthesis in a T cell, a method of inhibiting T cell proliferation, and a method of inhibiting the replication of and cytokine production by T lymphocytes, while not stimulating or inhibiting the replication of B lymphocytes. | 2013-08-29 |
20130225688 | COMPOSITIONS AND METHODS FOR THE TREATMENT OF SOMATOSENSORY DISORDERS - A method of combating a somatosensory disorder in a subject, comprising administering to the subject an effective amount of a composition comprising bupranolol and/or pharmaceutically acceptable derivative(s) thereof. Compositions useful for such administration are described, including salts, esters, solvates, etc. of tert-butyl[3-(2-chloro-5-methylphenoxy)-2-hydroxypropyl]amine, in which such salt, ester, solvate, etc. compound is in enantiomeric excess or homoenantiomeric in the R isomer thereof, or is formulated with racemic mixtures of the R and S stereoisomers of the salts, esters, solvates, etc. of tert-butyl[3-(2-chloro-5-methylphenoxy)-2-hydroxypropyl]amine. Combination therapy compositions of opioid receptor agonists and such compounds are also described. A method is disclosed of referential genotypic screening of candidate subjects in connection with therapeutic intervention using the compositions of the disclosure to combat the somatosensory disorder. | 2013-08-29 |
20130225689 | PHARMACEUTICAL COMPOSITIONS OF CURCUMIN - The present invention relates to stable liquid pharmaceutical compositions of curcumin or its pharmaceutically acceptable salts or its derivatives with higher curcumin concentration and improved bioavailability without the use of buffer and/or molecular aggregation inhibitor(s). In accordance with present invention the curcumin is in the solubilized form to make a stable liquid pharmaceutical composition. | 2013-08-29 |