| 18th week of 2012 patent applcation highlights part 60 |
| Patent application number | Title | Published |
|---|
| 20120108519 | NEO-TRYPTOPHAN - Methods of inducing antinociception in a human are described. The method includes the step of administering an effective dose of a polypeptide comprising L-neo-tryptophan to the human extracranially. The polypeptide containing L-neo-tryptophan could be, but is not limited to, NT64L, NT65L, NT66L, NT67L, NT69L, NT69L′, NT71, NT72, NT73, NT74, NT75, NT76, or NT77. | 2012-05-03 |
| 20120108520 | Antimicrobial Compounds and Formulations - The invention relates to the use of a molecule comprising a backbone of 2 to 35 non-hydrogen atoms in length, having covalently attached thereto at least two bulky and lipophilic groups and having at least one more cationic than anionic moiety, in the manufacture of a medicament for destabilising microbial cell membranes and the use as a membrane acting antimicrobial agent of a molecule comprising a backbone of 2 to 35 non-hydrogen atoms in length, having covalently attached thereto a super bulky and lipophilic group comprising at least 9 non-hydrogen atoms and having at least two more cationic than anionic moieties and to methods of treatment involving such molecules, in particular peptides including peptide derivatives, and peptidomimetics. | 2012-05-03 |
| 20120108521 | IMMUNOSTIMULATORY COMPOSITIONS AND USES THEREOF - The present invention provides novel immune-stimulatory polypeptides, and methods for their use and identification. | 2012-05-03 |
| 20120108522 | HDAC INHIBITORS AND HORMONE TARGETED DRUGS FOR THE TREATMENT OF CANCER - The present invention relates to the methods of treating endocrine-regulated cancers, including hormone resistant cancers, for example. More specifically, the present invention relates to a method of increasing the sensitivity of hormone resistant cancers to hormonal therapeutic agents. In particular embodiments, the present invention concerns delivery of a histone deacetylase inhibitor and a hormone targeted drug to an individual with cancer. In specific embodiments, the histone deacetylase inhibitor and the hormone targeted drug act synergistically to treat the cancer, including by overcoming resistance to a cancer therapy. | 2012-05-03 |
| 20120108523 | DISEASE-ASSOCIATED PROTEIN - Disclosed are methods and compositions for early diagnosis, monitoring and treatment of retinal dystrophy, age-related macular degeneration, Bardet-Biedel syndrome, Bassen-kornzweig syndrome, best disease, choroidema, gyrate atrophy, congenital amourosis, refsun syndrome, stargardt disease and Usher syndrome. In particular, the invention relates to a protein, termed “Rdcvf1,” that is differentially transcribed and expressed in subjects suffering from retinal dystrophies and the like, such as retinal dystrophy and age-related macular degeneration compared with nonsufferers, antibodies which recognize this protein, and methods for diagnosing such conditions. | 2012-05-03 |
| 20120108524 | VACCINE COMPRISING AMB A 1 PEPTIDES FOR USE IN THE TREATMENT OF RAGWEED ALLERGY - The present invention relates to compositions for preventing or treating allergy to ragweed by tolerisation. The compositions are based on combinations of peptide fragments derived from the major allergen in ragweed pollen, Amb a 1. The invention also relates to products, vectors and formulations which may be used to provide polypeptides of the invention in combination. The invention further relates to in vitro methods for determining whether T cells recognize a polypeptide of the invention, and for determining whether an individual has or is at risk of a condition characterized by allergic symptoms in response to a ragweed allergen. | 2012-05-03 |
| 20120108525 | Methods and Compositions for the Treatment of Gastrointestinal Disorders - Compositions and related methods for treating IBS and other gastrointestinal disorders and conditions (e.g., gastrointestinal motility disorders, functional gastrointestinal disorders, gastroesophageal reflux disease (GERD), duodenogastric reflux, Crohn's disease, ulcerative colitis, inflammatory bowel disease, functional heartburn, dyspepsia (including functional dyspepsia or nonulcer dyspepsia), gastroparesis, chronic intestinal pseudo-obstruction (or colonic pseudoobstruction), and disorders and conditions associated with constipation, e.g., constipation associated with use of opiate pain killers, post-surgical constipation, and constipation associated with neuropathic disorders as well as other conditions and disorders are described. The compositions feature peptides that activate the guanylate cyclase C (GC-C) receptor. | 2012-05-03 |
| 20120108526 | ANTI-MICROBIAL COMPOSITIONS - Antimicrobial compounds from | 2012-05-03 |
| 20120108527 | POLYMERIC TOPICAL COMPOSITIONS - The present invention relates to topical antibacterial compositions. The compositions comprise an antibacterial agent such as mupirocin, water, a polymer and a volatile solvent present in an amount of less than about 40%. The invention also relates to methods of treatment by administering the compositions to a patient in need thereof, and to the use of such compositions in the treatment of bacterial conditions. | 2012-05-03 |
| 20120108528 | NEW THERAPEUTIC APPROACHES FOR TREATING NEUROINFLAMMATORY CONDITIONS - The present invention relates to novel compositions which can be used for the treatment of neuroinflammation, in particular in subjects having a neurodegenerative, autoimmune, infectious, toxic or traumatic disorder. More particularly, the invention relates to combined therapies for treating neuroinflammation. The invention also discloses new methods for treating neuroinflammation pathological conditions in a subject. | 2012-05-03 |
| 20120108529 | PROTEASE INHIBITORS - Compounds useful as protease inhibitors are provided, as are methods of use and preparation of such compounds and compositions containing such compounds. In one embodiment, the compounds are useful for inhibiting HIV protease enzymes, and are therefore useful in slowing the proliferation of HIV. | 2012-05-03 |
| 20120108530 | Enhanced Neoglycosides Through Neoglycosylation and Methods of Use Thereof - Using neoglycosylation, the impact of differential glycosylation upon the divergent anticancer and anti-HIV properties of the triterpenoid betulinic acid (BA) was examined. Each member from a library of 37 differentially glycosylated BA variants was tested for anticancer and anti-HIV activities. Enhanced analogs for both desired activities were discovered with the corresponding antitumor or antiviral enhancements diverging, based upon the appended sugar, into two distinct compound subsets. | 2012-05-03 |
| 20120108531 | PHOSPHONATE NUCLEOSIDES USEFUL AS ACTIVE INGREDIENTS IN PHARMACEUTICAL COMPOSITIONS FOR THE TREATMENT OF VIRAL INFECTIONS, AND INTERMEDIATES FOR THEIR PRODUCTION - Disclosed herein are novel phosphonate nucleosides and thiophosphonate nucleosides comprising a phosphonalkoxy-substituted or phosphonothioalkyl-substituted five-membered, saturated or unsaturated, oxygen-containing or sulfur-containing ring coupled to a heterocyclic nucleobase such as a pyrimidine or purine base. The invention further relates to compounds having HIV (Human Immunodeficiency Virus) replication inhibiting properties and to compounds having antiviral activities with respect to other viruses. The invention also relates to methods for preparation of all such compounds and pharmaceutical compositions comprising them. The invention further relates to the use of said compounds as a medicine and in the manufacture of a medicament useful for the treatment of subjects suffering from HIV infection, as well as for treatment of other viral, retroviral or lentiviral infections and to the treatment of animals suffering from FIV, viral, retroviral or lentiviral infections. | 2012-05-03 |
| 20120108532 | PHARMACEUTICAL COMPOSITION FOR NEUROPROTECTIVE TREATMENT IN PATIENTS WITH ICTUS COMPRISING CITICOLINE AND URIC ACID - A pharmaceutical composition comprised of uric acid and citicoline is for the neuroprotective treatment of patients with ictus. | 2012-05-03 |
| 20120108533 | NOVEL PHOSPHATE MODIFIED NUCLEOSIDES USEFUL AS SUBSTRATES FOR POLYMERASES AND AS ANTIVIRAL AGENTS - This invention provides phosphate-modified nucleosides represented by the structural formula: wherein W is O or S, and wherein B, R | 2012-05-03 |
| 20120108534 | Dihydrothienopyrimidines for the treatment of inflammatory Diseases - The invention relates to new dihydrothienopyrimidine of formula | 2012-05-03 |
| 20120108535 | 2-FLUORINATED RIBOSES AND ARABINOSES AND METHODS OF USE AND SYNTHESIS - Disclosed are halogenated 2-deoxy-lactone, 2′-deoxy-nucleosides, and derivatives thereof, for example, a compound of formula (I). Also disclosed are a composition comprising a pharmaceutically acceptable carrier and at least one compound or salt of the invention, and a method of treating a disorder is selected from the group consisting of an abnormal cellular proliferation, a viral infection, and an autoimmune disorder. | 2012-05-03 |
| 20120108536 | PHARMACEUTICAL COMPOSITION AND METHOD FOR INHIBITING INFLAMMATION - A pharmaceutical composition for inhibiting inflammation, comprising (a) hyaluronic acid, (b) a 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase inhibitor, and (c) a pharmaceutically acceptable carrier, is provided. Also provided is a method for inhibiting inflammation in a mammal, comprising administrating to the mammal an effective amount of a composition comprising (a) hyaluronic acid and (b) an HMG-CoA reductase inhibitor. | 2012-05-03 |
| 20120108537 | PROCESS FOR PREPARING A CROSSLINKED GEL - A process for preparing a crosslinked gel of at least one polymer or one of its salts, including a) providing an aqueous medium containing at least one polymer, b) forming a homogenous gel from the medium from step a), c) bringing the gel obtained in step b) into contact with an effective amount of at least one crosslinking agent; d) crossliking the mixture formed in step c); and e) recovering the crosslinked hydrogel, wherein at least steps a) to d) are carried out within a hermetic cavity delimited at least partially by a deformable wall, the mixture present in the cavity being exposed, in step d), to conditions conducive to crosslinking. | 2012-05-03 |
| 20120108538 | SULFATED POLYSACCHARIDES HAVING ANTIPLASMODIAL ACTIVITY AND METHODS AND PRODUCTS FOR IDENTIFYING ANTIPLASMODIAL ACTIVITY - This invention relates to methods for identifying, producing or rationally designing sulfated polysaccharide molecules that have antiplasmodial activity. Also provided are sulfated polysaccharide molecules having antiplasmodial activity, as well as methods for treating and preventing diseases including malaria with such molecules. | 2012-05-03 |
| 20120108539 | Medicinal Anti Acne Cream And A Process To Make It - The present invention relates to a composition for treating acne along with skin rejuvenation. More particularly, the present invention relates to a pharmaceutical cream comprising a biopolymer, and an antiacne active ingredient. It discloses a composition for treating acne along with skin rejuvenation containing a) a biopolymer in the form of Chitosan, b) an active pharmaceutical ingredient (API) alone or in combination used in treating acne, c) a cream base containing primary and secondary emulsifiers, waxy materials, co-solvents, acids, preservatives, buffering agents, anti oxidants, chelating agents, and humectants, d) water. The active ingredients, namely chitosan, and an antiacne agent, are incorporated in cream base for use in treating acne. | 2012-05-03 |
| 20120108540 | Preservatives from Chitin Derivatives - The invention comprises a process for producing a chitosan derivative, and a product prepared thereby, by activating chitosan or a chitosan precursor chitin in alcohol that contains water from 0% to maximum of about 30% and preparing derivatives by reacting with a reagent to get derivatives that have various uses including an antimicrobial, or a microbiostatic, or an antitranspirant, or an antifungal, or a fruit preservative properties or as carrier of active molecules or functional groups etc. or a combination thereof. Illustrated derivatives include acid, succinic, enzymatically deacetylated, enzymatically hydrolysed by chitinolysis, sugar, formaldehyde, phosphoric acid, hydrochloric acid and copper sulfate derivatives that are obtained by reaction individually or in a combination of consecutive reactions. A novel class of thermostable proteo-chitinase is also disclosed prepared from | 2012-05-03 |
| 20120108541 | ACYLATED 1,6-ANHYDRO DECASACCHARIDE AND ITS USE AS AN ANTITHROMBOTIC AGENT - The instant invention relates to the decasaccharide of formula (I), wherein Ac represents an acetyl group: | 2012-05-03 |
| 20120108542 | SULFATED OCTASACCHARIDE AND ITS USE AS ANTITHROMBOTIC AGENT - The instant invention relates to the octasaccharide of formula (I): | 2012-05-03 |
| 20120108543 | SULFATED HEPTASACCHARIDE AND ITS USE AS AN ANTITHROMBOTIC AGENT - The instant invention relates to the heptasaccharide of formula (I): | 2012-05-03 |
| 20120108544 | ACYLATED DECASACCHARIDES AND THEIR USE AS ANTITHROMBOTIC AGENTS - The instant invention relates to decasaccharides of formula (I): | 2012-05-03 |
| 20120108545 | Trioxane Monomers and Dimers - Monomeric and dimeric trioxane fluoroaryl amides, 5-carbon-linked, C-10 non-acetal trioxane dimer esters; trioxane silylamides; and trioxane dimer orthoesters and methods of their use for treating subjects infected with malaria or other parasitic infectious diseases including, but not limited to, toxoplasmic infection; subjects afflicted with psychiatric conditions associated with toxoplasmic infection; and subjects afflicted with cancer. | 2012-05-03 |
| 20120108546 | SYNERGISTIC ANTIMICROBIAL COMPOSITION - A synergistic antimicrobial composition comprising:
| 2012-05-03 |
| 20120108547 | INHIBITORS OF TYROSINE KINASES AND USES THEREOF - Disclosed herein are compounds that inhibit the activity of particular tyrosine kinases. Methods for the preparation of such compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the compounds disclosed, alone or in combination with other therapeutic agents, for the treatment of tyrosine kinase-mediated diseases or conditions or tyrosine kinase-dependent diseases or conditions are provided. | 2012-05-03 |
| 20120108548 | MOLECULAR TWEEZERS FOR THE TREATMENT OF AMYLOID-RELATED DISEASES - This invention provides novel compositions to inhibit the aggregation of amyloid proteins. In various embodiments the compositions comprise a molecular tweezers that binds lysine and/or arginine and thereby inhibits the aggregation of amyloidogenic proteins. | 2012-05-03 |
| 20120108549 | NEUROPROTECTIVE COMPOUNDS AND THEIR USE - Apocynin derivative compounds, active pharmaceutical ingredients, dosage forms, and methods of use thereof as neuroprotectants in the brain of mammals. | 2012-05-03 |
| 20120108550 | Use of Derivatives of Polyunsaturated Fatty Acids as Medicaments - Use of polyunsaturated fatty acid derivatives as medicaments or functional foods. The present invention relates to the use of 1,2-fatty acid derivatives in the treatment or prevention of common diseases whose etiology is based on alterations (of any type) of the cell membrane lipids, for example, changes in levels, in the composition or in the structure of these lipids. In addition, for diseases in which the regulation of lipid composition and of the structure of the membranes (or proteins that interact with membranes) causes the reversion of pathological state. | 2012-05-03 |
| 20120108551 | OPHTHALMIC COMPOSITIONS - The present invention relates to compositions that may alleviate symptoms of ocular stress, as well as methods of their production, use, and storage compositions. The compositions comprise at least one ocular epithelial cell associating group and at least one hydrophilic group. In one embodiment the at least one ocular epithelial cell associating group and at least one hydrophilic group are substituents on a conjugated polyaromatic core. | 2012-05-03 |
| 20120108552 | METHODS OF TREATING ACNE - A method of treating acne in a human in need thereof comprising administering systemically to said human a tetracycline compound in an amount that is effective to treat acne but has substantially no antibiotic activity, without administering a bisphosphonate compound. | 2012-05-03 |
| 20120108553 | Combination Therapy with Non-Selective COX Inhibitors to Prevent COX-Related Gastric Injuries - The present invention is directed to nicotinamide, nicotinamide derivatives and prostaglandin mimetics, alone or in combination with an NSAID, and their use in treating pain, inflammation, and/or gastrointestinal toxicty, | 2012-05-03 |
| 20120108554 | PROCESS FOR PREPARING HIGH PURITY 1alpha-HYDROXY VITAMIN D2 - The present invention relates to a process for purifying Doxercalciferol, a synthetic vitamin D analog, also known as 1α-hydroxy vitamin D | 2012-05-03 |
| 20120108555 | Mixtures or Organic Compounds for the Treatment of Airway Diseases - A medicament comprising, separately or together, (A) a compound of formula (I) in free or pharmaceutically acceptable salt or solvate form and (B) a corticosteroid, for simultaneous, sequential or separate administration in the treatment of an inflammatory or obstructive airways disease, the molar ratio of (A) to (B) being from 100:1 to 1:300. | 2012-05-03 |
| 20120108556 | METHODS AND DOSAGE FORMS FOR THE TREATMENT OF HUMAN CANCERS - Methods for the treatment of human cancers, daily dosage forms for cancer patients, and methods of formulating the dosage forms are provided wherein the daily dosage form contains from about 10-6,000 mg of each of β-sitosterol, isovanillin, and linolenic acid. Preferably, the dosage forms are formulated by first creating an aqueous decoction of | 2012-05-03 |
| 20120108557 | FLUOROQUINOLONE DERIVATIVES FOR OPHTHALMIC APPLICATIONS - The present invention relates to fluoroquinolone derivatives having enhanced ocular penetration characteristics and/or antimicrobial activity, and to compositions comprising such derivatives. The derivatives and compositions are particularly well suited for treating ophthalmic bacterial infections. The present invention more particularly relates to the discovery that a 2-methyl substitution on a diazabicyclo group attached to a fluoroquinolone ring system produces improved permeability characteristics, and that a 5-amino substitution on a fluoroquinolone ring system results in improved anti-microbial activity. | 2012-05-03 |
| 20120108558 | Treatment of Hot Flashes - 16α,17α-Epoxy-10β-hydroxyestr-4-en-3-one is useful in the treatment of hot flashes by vomeronasal administration. | 2012-05-03 |
| 20120108559 | RECEPTOR ACTIVATOR OF THE RANK RECEPTOR COMPLEX INHIBITOR - Methods and pharmaceutical compositions utilizing compounds of Formula II: for inhibiting osteoclastogenesis and the activity of osteoclasts in patients. | 2012-05-03 |
| 20120108560 | SINGLE PHASE SILICONE ACRYLATE FORMULATION - This invention provides a single phase silicone acrylate formulation that resists phase separation and includes (A) at least one of a silicone, an acrylate, and combinations thereof. The single phase silicone acrylate formulation also includes (B) a silicone acrylate hybrid compatibilizing agent including silicone functionality and (meth)acrylate functionality and that is the reaction product of a silicon-containing pressure sensitive adhesive composition, a (meth)acrylate, and an initiator. A method of minimizing phase separation of the single phase silicone acrylate formulation includes the step of combining (A) and (B) to form the single phase silicone acrylate formulation. | 2012-05-03 |
| 20120108561 | STORAGE-STABLE, ANTI-MICROBIAL COMPOSITIONS INCLUDING CERAGENIN COMPOUNDS AND METHODS OF USE - Storage-stable, anti-microbial compositions and products include a carrier and a ceragenin compound suspended in the carrier. Ceragenin compounds suspended in the carrier include a sterol backbone and a number of cationic groups attached to the sterol backbone via hydrolysable linkages. The carrier has a pH of 5.5 or less, which acts to stabilize the hydrolysable linkages and increase the shelf-life of the anti-microbial compositions and anti-microbial products. Nevertheless, the ceragenin compounds described herein are designed to break down relatively quickly (e.g., within about 5 days) if the pH environment of the ceragenin compounds is raised to about pH 6.5 or greater. | 2012-05-03 |
| 20120108562 | THERAPEUTIC COMPOSITIONS AND METHODS - PAD4 inhibitory compositions and methods for their use in treatment of cancer and autoimmune disease are provided according to embodiments of the present invention. | 2012-05-03 |
| 20120108563 | Methods Of Treating Liposarcoma - Provided herein are methods of treating liposarcoma in a subject, the method comprising administering to the subject a therapeutically effective amount of an Hsp90 inhibitor. | 2012-05-03 |
| 20120108564 | 1,3,4,8-Tetrahydro-2H-Pyrido[1,2-a]Pyradine Derivatives and Use Thereof as HIV Integrase Inhibitor - [Problem] Provided is a novel 1,3,4,8-tetrahydro-2H-pyrido[1,2-a]pyrazine derivative or a pharmaceutically acceptable salt thereof, or a solvate thereof, which is useful as an anti-HIV agent. | 2012-05-03 |
| 20120108565 | PYRROLE CARBOXYLIC ACID DERIVATIVES AS ANTIBACTERIAL AGENTS - The present invention provides DNA Gyrase and/or Topo IV inhibitors of Formula (I), which can be used as antibacterial agents. Compounds disclosed herein can be used for treating or preventing conditions caused by or contributed by gram positive, gram negative and anaerobic bacteria, more particularly against, for example, | 2012-05-03 |
| 20120108566 | NICOTINAMIDES AS JAK KINASE MODULATORS - The present invention is directed to compounds of formula I and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of JAK kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition JAK kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by JAK kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma. | 2012-05-03 |
| 20120108567 | Thiazolyl-Dihydro-Indazoles - The present invention encompasses compounds of general formula (1) | 2012-05-03 |
| 20120108568 | SUBSTITUTED PYRAZOLO[1,5-a]PYRIMIDINE COMPOUNDS AS TRK KINASE INHIBITORS - Compounds of Formula (I) and salts thereof in which R | 2012-05-03 |
| 20120108569 | 8-AZA Tetracycline Compounds - The present invention is directed to a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. The variables for Structural Formula I are defined herein. Also described is a pharmaceutical composition comprising the compound of Structural Formula I and its therapeutic use. | 2012-05-03 |
| 20120108570 | Pharmacological Treatment for Sleep Apnea - The present invention relates generally to pharmacological methods for the prevention of amelioration of sleep-related breathing disorders via administration of agents or combinations of agents that possess serotonin-related pharmacological activity. | 2012-05-03 |
| 20120108571 | SUBSTITUTED PHENOXY N-ALKYLATED THIAZOLIDINEDIONES AS ESTROGEN RELATED RECEPTOR-ALPHA MODULATORS - The present invention relates to compounds of Formula (I), | 2012-05-03 |
| 20120108572 | NOVEL BENZAMIDES, PRODUCTION THEREOF, AND USE THEREOF AS MEDICAMENTS - Heteroaryloxy-substituted benzoic acid amides of general formula I | 2012-05-03 |
| 20120108573 | SULFUR SUBSTITUTED SULFONYLAMINOCARBOXYLIC ACID N-ARYLAMIDES, THEIR PREPARATION, THEIR USE AND PHARMACEUTICAL PREPARATIONS COMPRISING THEM - The present invention relates to compounds of the formula I | 2012-05-03 |
| 20120108574 | Substituted Benzo-Imidazo-Pyrido-Diazepine Compounds - The present invention relates to substituted benzo-imidazo-pyrido-diazepine compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted benzo-imidazo-pyrido-diazepine compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds and pharmaceutical compositions to subjects in need thereof. | 2012-05-03 |
| 20120108575 | HETEROCYCLIC-SUBSTITUTED PIPERIDINE COMPOUNDS AND THE USES THEREOF - The invention relates to Heterocyclic-Substituted Piperidine Compounds, compositions comprising an effective amount of a Heterocyclic-Substituted Piperidine Compound and methods to treat or prevent a condition, such as pain, comprising administering to an animal in need thereof an effective amount of a Heterocyclic-Substituted Piperidine Compound. | 2012-05-03 |
| 20120108576 | THIAZOLE COMPOUNDS AND METHODS OF USE - The present invention provides compounds, salts and hydrates of Formula I, | 2012-05-03 |
| 20120108577 | COMPOUNDS FOR THE TREATMENT OF MULTI-DRUG RESISTANT BACTERIAL INFECTIONS - The present invention relates to compounds that demonstrate antibacterial activity, processes for their preparation, pharmaceutical compositions containing them as the active ingredient, to their use as medicaments and to their use in the manufacture of medicaments for use in the treatment of bacterial infections in warm-blooded animals such as humans. In particular this invention relates to compounds useful for the treatment of bacterial infections in warm-blooded animals such as humans, more particularly to the use of these compounds in the manufacture of medicaments for use in the treatment of bacterial infections in warm-blooded animals such as humans. | 2012-05-03 |
| 20120108578 | INHIBITORS OF 11beta-HYDROXYSTEROID DEHYDROGENASE 1 - This invention relates to novel compounds of the Formula (I), (Ia | 2012-05-03 |
| 20120108579 | CYCLIC INHIBITORS OF 11BETA-HYDROXYSTEROID DEHYDROGENASE 1 - This invention relates to novel compounds of the Formula Ik, Im | 2012-05-03 |
| 20120108580 | Use of Fungicidal Active Substances For Controlling Mycoses on Plants of the Palm Family - The present invention relates to the use of specific fungicidal active substances, alone or in combination, for controlling mycoses in plants of the palm family and to a method for using said specific fungicidal active substances for controlling said mycoses in the field of plant protection and the protection of materials. | 2012-05-03 |
| 20120108581 | FUSED PIPERIDINE COMPOUND AND PHARMACEUTICAL CONTAINING SAME - The present invention provides a low molecular weight compound having EPO production-promoting action and/or hemoglobin production-promoting action. The present invention relates to a fused piperidine compound represented by the following general formula (1): | 2012-05-03 |
| 20120108582 | Fused substituted aminopyrrolidine derivative - A quinolone synthetic antibacterial agent having excellent properties as a medicine is provided, which has strong antibacterial activity not only to Gram-negative bacteria but also to Gram-positive cocci that have low sensitivity to quinolone antibacterial agents, and which exhibits high safety and excellent pharmacokinetics. A compound represented by the formula (I) or a salt thereof, or a hydrate thereof. Specifically, a quinolone derivative of the formula (I) wherein substituents R6 and R7 taken together with the carbon atoms to which they are bonded form a cyclic structure which may contain an oxygen atom as a ring constituent atom, the cyclic structure forming a 5-4, 5-5, or 5-6 fused bicyclic pyrrolidinyl substituent, the substituent being bonded to a quinolone mother skeleton Q containing a pyridobenzoxazine structure. | 2012-05-03 |
| 20120108583 | Tricyclic Compounds As mPGES-1 Inhibitors - The present invention relates to tricyclic compounds of formula (I) or pharmaceutically acceptable salt thereof as mPGES-1 inhibitors. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful in the treatment of pain and/or inflammation from a variety of diseases or conditions, such as asthma, osteoarthritis, rheumatoid arthritis, acute or chronic pain and neurodegenerative diseases. | 2012-05-03 |
| 20120108584 | 2H OR 3H-BENZO[E]INDAZOL-1-YL CARBAMATE DERIVATIVES, THE PREPARATION AND THERAPEUTIC USE THEREOF - Compounds corresponding to the formula (I) | 2012-05-03 |
| 20120108585 | BENZOXAZOLES, BENZTHIAZOLES AND RELATED ANALOGS AS SIRTUIN MODULATORS - Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent. | 2012-05-03 |
| 20120108586 | ARTHROPOD PEST CONTROL METHOD AND COMPOSITION - Disclosed is a harmful arthropod control composition comprising, as an active ingredient, a fused heterocyclic compound represented by formula (1) [wherein A | 2012-05-03 |
| 20120108587 | Aza- and Diaza-Phthalazine Compounds as P38 Map Kinase Modulators and Methods of Use Thereof - The present invention comprises a new class of compounds useful for the prophylaxis and treatment of protein kinase mediated diseases, including inflammation and related conditions. The compounds have a general Formula (I) wherein A | 2012-05-03 |
| 20120108588 | NOVEL 3-AMIDO-PYRROLO[3,4-C]PYRAZOLE-5(1H, 4H,6H) CARBALDEHYDE DERIVATIVES - The present invention relates to compounds and pharmaceutically acceptable salts of Formula (I): | 2012-05-03 |
| 20120108589 | AZABICYCLO COMPOUND AND SALT THEREOF - It is intended to provide a novel azabicyclo compound which exhibits both HSP90 inhibitory activity and cell proliferation inhibitory effect. Specifically disclosed is a compound represented by the following general formula (I) or a salt thereof: wherein X | 2012-05-03 |
| 20120108590 | MELT-EXTRUDED SOLID DISPERSIONS CONTAINING AN APOPTOSIS-INDUCING AGENT - A pro-apoptotic solid dispersion comprises, in essentially non-crystalline form, a Bcl-2 family protein inhibitory compound of Formula I as defined herein, dispersed in a solid matrix that comprises (a) a pharmaceutically acceptable water-soluble polymeric carrier and (b) a pharmaceutically acceptable surfactant. A process for preparing such a solid dispersion comprises subjecting to elevated temperature the compound of Formula I, the water-soluble polymeric carrier and the surfactant, to provide an extrudable semi-solid mixture; extruding the semi-solid mixture; and cooling the resulting extrudate to to provide a solid matrix comprising the polymeric carrier and the surfactant and having the compound dispersed in essentially non-crystalline form therein. The solid dispersion is suitable for oral administration to a subject in need thereof for treatment of a disease characterized by overexpression of one or more anti-apoptotic Bcl-2 family proteins, for example cancer or an immune or autoimmune disease. | 2012-05-03 |
| 20120108591 | ALKYLSULFINYL-SUBSTITUTED THIAZOLIDE COMPOUNDS - A new class of alkylsulfinyl thiazolides is described. These compounds show strong activity against hepatitis viruses. | 2012-05-03 |
| 20120108592 | PHARMACEUTICAL COMPOSITIONS AND METHODS OF USE OF SALICYLANILIDES FOR TREATMENT OF HEPATITIS VIRUSES - A new class of salicylanilides is described. These compounds show strong activity against hepatitis viruses. | 2012-05-03 |
| 20120108593 | Extreme temperature aqueous decontamination composition - An extreme temperature decontamination composition such as a solution for destroying microorganisms, chemical warfare and bioterrorism agents is utilized that generally does not freeze at low temperatures down to about minus 25° F. and also has no significant evaporation or decomposition at temperatures up to about 120° F. The solution is effective against nerve agents and vesicants such as VX and HD, and various biological agents. The composition comprises a metallic salt of dichloroisocyanuric acid or dibromoisocyanuric acid, an aqueous solvent system comprising polar compounds such as water and an alkyl glycol, and a quasi hydrophilic compound. The composition can be formulated as a one part system wherein all components are blended together. | 2012-05-03 |
| 20120108594 | PROCESS FOR PREPARING SALTS OF 4-[[5-[(CYCLOPROPYLAMINO)CARBONYL]-2-METHYLPHENYL]AMINO]-5-METHYL-N-PROPY- LPYRROLO[2,1-f][1,2,4]TRIAZINE-6-CARBOXAMIDE AND NOVEL STABLE FORMS PRODUCED THEREIN - Processes are provided for selectively preparing novel stable crystalline salt forms, selectively and consistently, namely, preparing Form N-1 of the methanesulfonic acid salt, and Form N-1 and Form N-4 of the hydrochloric acid salt of the p38 kinase inhibitor 4-[[5-[(cyclopropylamino)carbonyl]-2-methylphenyl]amino]-5-methyl-N-propylpyrrolo[2,1-f][1,2,4]triazine-6-carboxamide. The processes preferably employ solvent systems including formic acid/acetone and formic acid/methylethyl ketone which produce crystals having suitable flow properties and desired particle size, and solvents such as N,N-dimethylformamide and N,N-dimethylacetamide may be employed as well. | 2012-05-03 |
| 20120108595 | PLATELET-ACTIVATING FACTOR RECEPTOR ANTAGONISTS - Cyclohexyl sulfonamide compounds which are platelet-activating factor (PAF) receptor antagonists. Said compounds may be useful, for example, for the treatment of atherosclerosis or other PAF-mediated disorders, including inflammatory, cardiovascular, and immune disorders. | 2012-05-03 |
| 20120108596 | Aza-Bicyclic Amine N-Oxide Compounds as Alpha-7 Nicotinic Acetylcholine Receptor Ligand Pro-Drugs - The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are prodrugs for ligands, agonists, and partial agonists for the nicotinic α7 receptor and may be useful for the treatment of various disorders of the central nervous system, especially affective and neurodegenerative disorders. | 2012-05-03 |
| 20120108597 | Azaquinazolinediones Chymase Inhibitors - Disclosed are small molecule inhibitors of the formula (I), which are useful in treating various diseases and conditions involving chymase. | 2012-05-03 |
| 20120108598 | SITAGLIPTIN SYNTHESIS - The present invention relates to novel processes for the preparation of enantiomerically enriched β-amino acid derivatives such as β-amino esters useful for the synthesis of enantiomerically enriched biologically active molecules such as sitagliptin. The key step involves the resolution of the racemate with mandelic acid. | 2012-05-03 |
| 20120108599 | METHODS AND COMPOSITIONS FOR THE TREATMENT OF METABOLIC DISORDERS - The present invention is directed to a novel methods and compositions for the therapeutic intervention in hyperphenylalaninemia. More specifically, the specification describes methods and compositions for treating various types of phenylketonurias using compositions comprising BH4. Combination therapies of BH4 and other therapeutic regimens are contemplated. | 2012-05-03 |
| 20120108600 | SUBSTITUTED 4-HYDROXYPYRIMIDINE-5-CARBOXAMIDES - The present invention relates to substituted 4-hydroxypyrimidine-5-carboxamides useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions. | 2012-05-03 |
| 20120108601 | CRYSTALLINE PYRIDAZINE COMPOUND - A crystalline compound of formula (1) and its salts and solvates are provided for the treatment or prophylaxis of hepatitis C virus infections | 2012-05-03 |
| 20120108602 | Carbamoyl Compounds as DGAT1 Inhibitors 190 - DGAT-1 inhibitor compounds of formula (1), pharmaceutically-acceptable salts and pro-drugs thereof are described, together with pharmaceutical compositions, processes for making them and their use in treating, for example, obesity | 2012-05-03 |
| 20120108603 | AMINOCARBONYL-DERIVATIVES AS NOVEL INHIBITORS OF HISTONE DEACETYLASE - This invention comprises the novel compounds of formula (I) | 2012-05-03 |
| 20120108604 | PROCESSES FOR PREPARING AMINE SALTS OF SILDENAFIL-ANALOGUES AND USE THEREOF - A series of amine salts including a structure of formula (I) and formula (III) have provided. In formula I or formula (III), R | 2012-05-03 |
| 20120108605 | O-GLCNAC TRANSFERASE INHIBITORS AND USES THEREOF - The present invention provides inhibitors of O-GIcNAc transferase. Typically, the inhibitors are quinolinone-6-sulfonamides. The invention also provides pharmaceutical compositions thereof and methods for using the same in diabetes and complications thereof, neurodegenerative diseases, cancers, autoimmune diseases, and inflammatory diseases. | 2012-05-03 |
| 20120108606 | Carboxamide, Sulfonamide and Amine Compounds and Methods for Using The Same - Disclosed are carboxamide, sulfonamide and amine compounds, as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure | 2012-05-03 |
| 20120108607 | OPTICALLY ACTIVE 3-[(PHENYLPIPERAZIN-1-YL)ALKYL]-3- ALKYL-OXINDOLE DERIVATIVES HAVING CNS ACTIVITY - The present invention relates to the enantiomers of 5,7-dichloro-3-{4-[4-(4-chlorophenyl)-piperazin-1-yl]butyl}-3-ethyl-1,3-dihydro-2H-indol-2-one of the Formula (II) pharmaceutically acceptable salts thereof, process for the preparation thereof, medicinal products containing said enantiomers and the use thereof and their pharmaceutically acceptable salts in the treatment of the disorders of the central nervous system. | 2012-05-03 |
| 20120108608 | INJECTABLE MECLIZINE FORMULATIONS AND METHODS - Methods of treating or preventing a vertigo, nausea, or vomiting condition comprising injecting a subject with a pharmaceutically acceptable formulation consisting essentially of an effective amount of meclizine or a pharmaceutically acceptable salt thereof, a chemically modified cyclodextrin, and an aqueous carrier medium having a pH between about 2 and about 7 are disclosed. An injectable pharmaceutical formulation for treating or preventing a vertigo, nausea, or vomiting condition consisting essentially of an effective amount of meclizine, a chemically modified cyclodextrin, and an aqueous carrier medium having a pH between about 2 and about 7 is also disclosed. | 2012-05-03 |
| 20120108609 | DIHYDROOXAZOL-2-AMINE DERIVATIVES - The invention relates to compounds of formula | 2012-05-03 |
| 20120108610 | 2-PYRAZINONE DERIVATIVES FOR THE TREATMENT OF DISEASE OR CONDITION IN WHICH INHIBITION OF NEUTROPHIL ELASTASE ACTIVITY IS BENEFICIAL - The invention provides compounds of formula | 2012-05-03 |
| 20120108611 | 5, 6-BISARYL-2-PYRIDINE-CARBOXAMIDE DERIVATIVES, PREPARATION AND APPLICATION THEREOF IN THERAPEUTICS AS UROTENSIN II RECEPTOR ANTAGONISTS - The present invention relates to derivatives of 5,6-bisaryl-2-pyridine-carboxamide, their preparation and their application in therapeutics as antagonists of urotensin II receptors. | 2012-05-03 |
| 20120108612 | INHIBITORS OF BRUTON'S TYROSINE KINASE - Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. Methods for the preparation of the compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions. | 2012-05-03 |
| 20120108613 | COMPOUNDS AND COMPOSITIONS FOR TREATING CHEMICAL WARFARE AGENT-INDUCED INJURIES - Compounds and compositions for treating injuries caused by exposure to chemical warfare agents are described herein. | 2012-05-03 |
| 20120108614 | COMPOUNDS AND COMPOSITIONS FOR TREATING CHEMICAL WARFARE AGENT-INDUCED INJURIES - Compounds and compositions for treating injuries caused by exposure to chemical warfare agents are described herein. | 2012-05-03 |
| 20120108615 | SMALL MOLECULE INHIBITORS OF BACTERIAL MOTILITY AND A HIGH THROUGHPUT SCREENING ASSAY FOR THEIR IDENTIFICATION - Certain compounds are provided that can selectively inhibit motile bacteria such as | 2012-05-03 |
| 20120108616 | SUBSTITUTED OXAZOLE DERIVATIVES AND THEIR USE AS TYROSINE KINASE INHIBITORS - The present invention relates to novel compounds selected from substituted oxazole derivatives of formula (I) that selectively modulate, regulate, and/or inhibit signal transduction mediated by certain native and/or mutant tyrosine kinases implicated in a variety of human and animal diseases such as cell proliferative, metabolic, allergic, and degenerative disorders. More particularly, these compounds are potent and selective c-kit, bcr-abl and Flt-3 inhibitors. | 2012-05-03 |
| 20120108617 | METHODS AND COMPOSITIONS INVOLVING (S)-BUCINDOLOL - Disclosed is bucindolol substantially free of its R-stereoisomer. Also disclosed are pharmaceutical compositions that include bucindolol substantially free of its R-stereoisomer or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier. Also disclosed are methods of treating a patient that involve administering to the patient a therapeutically effective amount of a composition of the present invention. Formula (I). | 2012-05-03 |
| 20120108618 | THIA-TRIAZA-INDACENES - The present invention encompasses compounds of general formula (1) wherein R | 2012-05-03 |
