05th week of 2010 patent applcation highlights part 56 |
Patent application number | Title | Published |
20100029597 | RECA INHIBITORS WITH ANTIBIOTIC ACTIVITY, COMPOSITIONS AND METHODS OF USE - The present invention is directed to the use of RecA inhibitors as antibiotic agents, and provides RecA inhibitors useful in treating infections. Also provided are various compositions and methods associated with RecA inhibition. | 2010-02-04 |
20100029598 | Extended Benzamide Derivatives as Modulators of the EP2 Receptor - The present invention relates to extended benzamide derivatives of the general formula I, to processes for preparation thereof and to use thereof for production of pharmaceutical compositions for treatment of disorders and indications associated with the EP | 2010-02-04 |
20100029599 | Indolylamides as modulators of the EP2 receptor - The present invention relates to indolylamide derivatives of the general formula (I), to processes for preparation thereof and to use thereof for production of pharmaceutical compositions for treatment of disorders and indications associated with the EP | 2010-02-04 |
20100029600 | DIHYDRO-TRITERPENES IN THE TREATMENT OF VIRAL INFECTIONS, CARDIOVASCULAR DISEASE, INFLAMMATION, HYPERSENSITIVITY OR PAIN - The present invention relates to compositions comprising the triterpenes, dihydrobutyrospermol, dihydrolupeol and/or dihydroparkeol, the composition being applicable as a pharmaceutical, a dietary supplement or as a cosmetic. Further, the invention relates to the use of such compositions for the preparation of a medicament, a dietary supplement or a cosmetic for immunomodulating in a mammal such as suppression of viral infections, cardiovascular diseases, cancer, hypersensitivity and/or inflammatory reactions. The triterpenes may be in form of the free alcohol or derivatised, preferably with cinnamic acid, acetic acid or fatty acids. Furthermore, the triterpenes may be an extract obtainable from a natural source or synthetically made. | 2010-02-04 |
20100029601 | Administration of fluocinolone acetonide, tretinoin and hydroquinone cream in melasma maintenance therapy - Topical application of a triple combination immixture of fluocinolone acetonide, tretinoin and hydroquinone is useful for the maintenance therapy of melasma to prevent hyperpigmentation recurrence or reduce the severity of the hyperpigmentation recurrence. | 2010-02-04 |
20100029602 | LOW-DOSE MOMETASONE FORMULATIONS - Provided is a topical cream composition for the delivery of mometasone furoate comprising low dose mometasone furoate for the treatment of corticosteroid responsive dermatoses. The composition of the present invention can be safely applied over large surface areas of the skin (including areas with wrinkles and/or hair), and can be used therapeutically for extended periods of time (e.g., greater than 3 weeks). Treatment with the composition of the present invention carries reduced and/or fewer side effects compared with commercially available mometasone furoate cream products. The cream composition of the present invention is safe for the use of babies and infants under 2 years old. Additionally provided are methods of preparing and using the composition of the invention. | 2010-02-04 |
20100029603 | 16ALPHA-METHYL OR ETHYL SUBSTITUTED ESTROGENS - The invention makes a 16α-substituted steroidal compound available having formula 1, | 2010-02-04 |
20100029604 | ANTIBACTERIAL COMBINATION AND ITS USE - The invention relates to a pharmaceutical composition comprising an ethylene derivatives of tricyclic carbapenems of the general Formula (I) in the form of pure diastereoisomers and in the form of pure geometric isomers or a salt, ester or amide derivate thereof and an antibiotic and the use of this composition as a broad band spectrum β-lactamase inhibitor. | 2010-02-04 |
20100029605 | COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHIBITORS - The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the Abl, ARG, BCR-Abl, BRK, EphB, Fms, Fyn, KDR, c-Kit, LCK, PDGF-R, b-Raf, c-Raf, SAPK2, Src, Tie2 and TrkB kinases. | 2010-02-04 |
20100029606 | MODULATORS OF ALPHA7 NICOTINIC ACETYLCHOLINE RECEPTORS AND THERAPEUTIC USES THEREOF - The present invention provides compounds of formula (I) and compositions thereof, methods of making them, and methods of using them to modulate alpha7 nicotinic acetylcholine receptors and/or to treat any of a variety of disorders, diseases, and conditions. Provided compounds can affect, among other things, neurological, psychiatric and/or inflammatory system. | 2010-02-04 |
20100029607 | Substituted Piperazines as CB1 Antagonists - Compounds of Formula (I): | 2010-02-04 |
20100029608 | Histamine H3 Receptor Agents, Preparation and Therapeutic Uses - The present invention provides a novel compound of Formula (I) or a pharmaceutically acceptable salt thereof, having histamine-113 receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another, embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula (I) as well as methods of using them to treat obesity, cognitive deficiencies, narcolepsy, and other histamine H3 receptor-related diseases. | 2010-02-04 |
20100029609 | BIARYL SULFONAMIDE DERIVATIVES - A compound of formula (I) or a pharmaceutically acceptable salt or prodrug ester thereof: | 2010-02-04 |
20100029610 | Heteroaryl Compounds and Uses Thereof - The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same. | 2010-02-04 |
20100029611 | S1P1 receptor agonists and use thereof - The present invention relates to compounds of Formula (I): | 2010-02-04 |
20100029612 | 2-Aminoethyl Substituted Pyrimidin-2-Ones Cyclopropanes, Pyrazolines, Pyrimidines and Benzothiazepines and Their Uses as Urotensin II and Somatostatin 5 Receptor Ligands - The present invention provides a combinatorial approach to a library of novel compounds having four diversity points. The compounds provide for the mapping of urotensin II and somatostatin 5 receptors by differential binding of said receptors. The present invention further relates to a method of treating diseases for which modulation of the urotensin II receptor produces a physiologically beneficial response in said disease, such as those associated with CNS function and cardiovascular diseases. The present invention further relates to pharmaceutical compositions comprising these agents for the treatment of these diseases adapted to modulate the urotensin II receptor. | 2010-02-04 |
20100029613 | TREATMENT AND PREVENTION OF EPILEPSY - The present invention is directed to a method of treating or preventing epileptic seizures in a subject and a method of inhibiting hypersynchronous burst activity of neurons by administering an agent which interferes with glutamate, aspartate, and/or ATP release from astrocytes. Also presented is a method of identifying agents suitable for treating or preventing epileptic seizures. | 2010-02-04 |
20100029614 | SPIROCYCLIC HETEROCYCLIC DERIVATIVES AND METHODS OF THEIR USE - Spirocyclic heterocyclic derivatives, pharmaceutical compositions containing these compounds, and methods for their pharmaceutical use are disclosed. In certain embodiments, the spirocyclic heterocyclic derivatives are ligands of the δ opioid receptor and may be useful, inter alia, for treating and/or preventing pain, anxiety, gastrointestinal disorders, and other δ opioid receptor-mediated conditions. | 2010-02-04 |
20100029615 | BENZIMIDAZOLE DERIVATIVES - The present invention relates to a compound of the formula (I) or a pharmaceutically acceptable salt thereof, wherein R | 2010-02-04 |
20100029616 | UROTENSIN II RECEPTOR ANTAGONISTS - The present invention is directed to compounds of formula (I) | 2010-02-04 |
20100029617 | 1,4,5,6,7,8-HEXAHYDRO-1,2,5-TRIAZA-AZULENE DERIVATIVES AS OREXIN RECEPTOR ANTAGONISTS - The invention relates to 1,4,5,6,7,8-hexahydro-1,2,5-triaza-azulene derivatives and their use as orexin receptor antagonists. | 2010-02-04 |
20100029618 | ALPHA-2 RECEPTOR PAN AGONIST AND ANTICONVULSANT COMPOSITIONS FOR TREATING CHRONIC PAIN - Disclosed herein is a pharmaceutical composition comprising a pain-relieving anticonvulsant and an pan-alpha-2 adrenergic receptor agonist. The composition is effective for treating chronic pain, and methods of treating chronic pain using the composition and the compounds comprising it are also disclosed. | 2010-02-04 |
20100029619 | FUSED HETEROCYCLIC COMPOUND - The present invention provides a compound represented by the formula (I): | 2010-02-04 |
20100029620 | SUBSTITUTED TRIAZOLINE, TETRAZOLONE AND IMIDAZOLONE DERIVATIVES FOR USE AS A MEDICINE - The present invention concerns substituted triazolone, tetrazolone and imidazolone derivatives according to the general Formula (I) | 2010-02-04 |
20100029621 | HEXAFLUOROISOPROPANOL DERIVATIVES - The present invention relates to hexafluoroisopropanol derivatives having the general formula I | 2010-02-04 |
20100029622 | MICROEMULSIONS - Pharmaceutical compositions in the form of microemulsions comprising the following components, in amounts expressed as % by weight, the sum of the components being 100%:
| 2010-02-04 |
20100029623 | 4-(1-AMINO-ETHYL)-CYCLOHEXYLAMINE DERIVATIVES - The invention relates to compounds of formula (I) wherein R | 2010-02-04 |
20100029624 | Male Contraceptive - A compound having formula I. R | 2010-02-04 |
20100029625 | Therapeutic Agent for Restenosis - A therapeutic and/or prophylactic agent for restenosis, which comprises a thiadiazoline derivative represented by the general formula (0), or a pharmaceutically acceptable salt thereof: | 2010-02-04 |
20100029626 | Cyclic sulfones useful as mitochondrial sodium-calcium exchangers - The invention relates to novel compounds of formula (I) and their use in the treatment of the animal or human body, to pharmaceutical compositions comprising a compound of formula (I) and to the use of a compound of formula (I) for the preparation of pharmaceutical compositions for use in the treatment of protein kinase dependent diseases, especially of proliferative diseases, such as in particular tumour diseases. | 2010-02-04 |
20100029627 | MTKI QUINAZOLINE DERIVATIVES - The present invention concerns the compounds of formula | 2010-02-04 |
20100029628 | 2,4,5-Substituted Piperidines as Renin Inhibitors - SP-P2140 ATE-132—Abstract Novel substituted piperidines of the general formula (I) and (II) with the substituent definitions as explained in detail in the description are described. The compounds are suitable in particular as renin inhibitors and are highly potent. | 2010-02-04 |
20100029629 | ACYCLIC COMPOUNDS HAVING 5-HT6 RECEPTOR AFFINITY - The present disclosure provides compounds having affinity for the 5-HT | 2010-02-04 |
20100029630 | REVERSE-TURN MIMETICS AND METHOD RELATING THERETO - Conformationally constrained compounds that mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins are disclosed. Such reverse-turn mimetic structures have utility over a wide range of fields, including use as diagnostic and therapeutic agents. Libraries containing the reverse-turn mimetic structures of this invention are also disclosed as well as methods for screening the same to identify biologically active members. The invention also relates to the use of such compounds for inhibiting or treating disorders modulated by Wnt-signaling pathway, such as cancer, especially colorectal cancer, restenosis associated with angioplasty, polycystic kidney disease, aberrant angiogenesis disease, rheumatoid arthritis disease, tuberous sclerosis complex, Alzheimer's disease, excess hair growth or loss, or ulcerative colitis. | 2010-02-04 |
20100029631 | CARBOXYLIC ACID COMPOUNDS AND MEDICINAL COMPOSITIONS CONTAINING THE SAME AS THE ACTIVE INGREDIENT - A compound represented by formula (I) | 2010-02-04 |
20100029632 | BROADSPECTRUM 2-AMINO-BENZOXAZOLE SULFONAMIDE HIV PROTEASE INHIBITORS - The present invention concerns the compounds having the formula | 2010-02-04 |
20100029633 | IMIDAZO[1,2-A]PYRIDINE COMPOUNDS AS RECEPTOR TYROSINE KINASE INHIBITORS - Compounds of Formula I: in which A, B, R | 2010-02-04 |
20100029634 | Chemokine Receptor Modulators - The invention provides compounds of Formula (I) | 2010-02-04 |
20100029635 | 6,7,8,9-SUBSTITUTED 1-PHENYL-1,5-DIHYDRO-PYRIDO[3,2-B]INDOL-2-ONES USEFUL AS ANTI-INFECTIVE PHARMACEUTICAL AGENTS - This invention concerns the compounds | 2010-02-04 |
20100029636 | Lck inhibitors - The invention relates to novel pyrazolo[1,5-A]pyrimidine compounds of Formula I | 2010-02-04 |
20100029637 | Chymase Inhibitors - Disclosed are small molecule inhibitors which are useful in treating various diseases and conditions involving chymase. | 2010-02-04 |
20100029638 | FUSED HETEROCYCLYC INHIBITOR COMPOUNDS - The present invention provides a compound of general Formula (I) having histone deacetylase (HDAC) and/or Cyclin-dependent kinase (CDK) inhibitory activity, a pharmaceutical composition comprising the compound, and a method useful to treat diseases using the compound. | 2010-02-04 |
20100029639 | ION CHANNEL MODULATING COMPOUNDS AND USES THEREOF - Ion channel modulating compounds are disclosed. The compounds of the present invention may be incorporated in compositions and kits. The present invention also discloses a variety of in vitro and in vivo uses for the compounds and compositions, including the treatment of arrhythmia and the production of analgesia and local anesthesia. | 2010-02-04 |
20100029640 | Neuroprotective agents for the prevention and treatment of neurodegenerative diseases - Disclosed herein are methods of treating neurodegenerative diseases comprising administering to the subject a compound having the structure: | 2010-02-04 |
20100029641 | ARYL SULFAMIDE DERIVATIVES AND METHODS OF THEIR USE - The present invention is directed to aryl sulfamide derivatives of formula I: | 2010-02-04 |
20100029642 | Methods of Using Pyridodihydropyrazinones - Disclosed are pyridodihydropyrazinone compounds, processes for preparing them and their use as pharmaceutical compositions. The compounds according to the invention correspond to general formula (I), | 2010-02-04 |
20100029643 | HETEROCYCLYC SULFONAMIDES HAVING EDG-1 ANTAGONISTIC ACTIVITY - The invention relates to chemical compounds of formula (I), (Ia) and (Ib) or pharmaceutically acceptable salts thereof, which possess Edg-1 antagonistic activity and are accordingly useful for their anti-cancer activity and thus in methods of treatment of the human or animal body. The invention also relates to processes for the manufacture of said chemical compounds, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments for use in the production of an anti-cancer effect in a warm-blooded animal, such as man. | 2010-02-04 |
20100029644 | Compounds Which Modulate The CB2 Receptor - Compounds of formula (I) are disclosed. Compounds according to the invention are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain. | 2010-02-04 |
20100029645 | Inhibitors of Cytosolic Phospholipase A2 - This invention provides chemical inhibitors of the activity of various phospholipase enzymes, particularly cytosolic phospholipase A | 2010-02-04 |
20100029646 | PRODRUGS OF DIPHENYL OX-INDOL-2-ONE COMPOUNDS - The present application discloses prodrugs of substituted 3,3-diphenyl-1,3-dihydro-indol-2-one compounds having the general formula (I). The 4-position of the phenyl moieties and the N-position of the indole represent useful handles for the introduction of particular prodrug groups, in particular those comprising an amino acid moiety. The prodrug compounds are believed to be useful for the treatment of cancer in a mammal, possibly in combination with one or more other chemotherapeutic agents. The application also discloses the compounds for use in a method of treating a mammal suffering from or being susceptible to cancer | 2010-02-04 |
20100029647 | 3,4,(5)-SUBSTITUTED TETRAHYDROPHYRIDINES - 3,4(,5)-substituted tetrahydropyridine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease that depends on activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; pharmaceutical formulations comprising a 3,4(,5)-substituted tetrahydropyridine compound, and/or a method of treatment comprising administering a 3,4(,5)-substituted tetrahydropyridine compound, a method for the manufacture of a 3,4(,5)-substituted tetrahydropyridine compound, and novel intermediates and partial steps for its synthesis. | 2010-02-04 |
20100029648 | 11-Beta HSD1 Inhibitors - This invention relates to inhibiting 11βHSD1. | 2010-02-04 |
20100029649 | PHENYL-SUBSTITUTED PYRIMIDINE COMPOUNDS USEFUL AS KINASE INHIBITORS - Compounds having the formula (I), | 2010-02-04 |
20100029650 | BICYCLIC COMPOUNDS AND USE AS ANTIDIABETICS - The present invention relates to novel compounds that are useful in the treatment of metabolic disorders, particularly type II diabetes mellitus and related disorders, and also to the methods for the making and use of such compounds. | 2010-02-04 |
20100029651 | ARYL-SUBSTITUTED HETEROCYCLES, AND USE THEREOF - The invention relates to aryl-substituted heterocycles, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular of thromboembolic disorders. | 2010-02-04 |
20100029652 | Combination Therapy For Treating Hepatitis C Infections - The invention provides a method of treating hepatitis C, by providing compound of Formula I (shown below) in combination with a second active agent to a patient infected with the hepatitis C virus. Also provided herein are pharmaceutical combinations comprising a compound of Formula I and a second active agent. The pharmaceutical combination may be a unit dosage form or a packaged pharmaceutical composition. Packaged pharmaceutical combinations include a compound of Formula I and a second active agent in a package with instructions for using the formulation to treat a hepatitis C infection. | 2010-02-04 |
20100029653 | PYRAZOLOPYRIDINE, INDAZOLE, IMIDAZOPYRIDINE, IMIDAZOPYRIMIDINE, PYRAZOLOPYRAZINE AND PYRAZOLOPYRIDINE DERIVATIVES AS STIMULATORS OF GUANYLATE CYCLASE FOR CARDIOVASCULAR DISORDERS - The present application relates to novel azabicyclic compounds, processes for their preparation, their use alone or in combinations for the treatment and/or prevention of diseases, and their use for producing medicaments for the treatment and/or prevention of diseases, especially for the treatment and/or prevention of cardiovascular disorders. | 2010-02-04 |
20100029654 | CARDIOVASCULAR COMPOSITIONS AND USE OF THE SAME FOR THE TREATMENT OF ALZHEIMER'S DISEASE - Methods and compositions for the treatment of Alzheimer's Disease are described. More specifically, the invention demonstrates that administration of cardiovascular agents to a mammal suffering from the symptoms of Alzheimer's Disease causes an amelioration of those symptoms. The finding of the present invention can be used in treatment regimens designed to attenuate or prevent Alzheimer's Disease. | 2010-02-04 |
20100029655 | Processes For The Preparation Of Anti-Viral Compounds And Compositions Containing Them - Disclosed are processes for the preparation of compounds of formula I and compositions that comprise said compounds of formula I. | 2010-02-04 |
20100029656 | AZABICYCLIC HETEROCYCLES AS CANNABINOID RECEPTOR MODULATORS - The present application describes CB-1 inverse agonists according to Formula (I) and (Ia), pharmaceutical compositions comprising at least one compound according to Formula (I) or (Ia), and optionally one or more additional therapeutic agents and methods of treatment using the compounds according to Formula (I) or (Ia), both alone and in combination with one or more additional therapeutic agents. The preferred compounds have the general Formula (Ia), including all prodrugs, pharmaceutically acceptable salts and stereoisomer, thereof, wherein R | 2010-02-04 |
20100029657 | Bridged, Bicyclic Heterocyclic or Spiro Bicyclic Heterocyclic Derivatives of Pyrazolo[1, 5-A]Pyrimidines, Methods for Preparation and Uses Thereof - Compounds of formula A: | 2010-02-04 |
20100029658 | HETEROCYCLIC DERIVATIVES, PHARMACEUTICAL COMPOSITIONS AND METHODS OF USE THEREOF - The present invention relates to novel quinoxaline, quinazoline and phthalazine derivatives as well as multimeric derivatives, methods for their preparation, pharmaceutical compositions including such compounds, and methods of using these compounds for the treatment and prevention of brain damage resulting from brain injury, especially secondary brain damage due to traumatic brain injury (TBI). The compounds of the invention are also useful in treating and preventing neurodegenerative diseases. | 2010-02-04 |
20100029659 | Preferential vasoconstriction compositions and methods of use - The invention generally relates to compositions and methods for preferential vasoconstriction of smaller blood vessels relative to larger blood vessels. The compositions comprise highly selective alpha-2 adrenergic receptor agonists, at low concentrations, such as below 0.05% weight by volume. The compositions preferably comprise brimonidine. The compositions preferably have pH between about 5.5 and about 6.5. | 2010-02-04 |
20100029660 | Compositions and methods for reversing rebound hyperemia - The invention generally relates to compositions and methods for inducing vasoconstriction with low incidence of rebound hyperemia. The compositions comprise highly selective alpha-2 adrenergic receptor agonists, at low concentrations, such as below 0.05% weight by volume. The compositions preferably comprise brimonidine. The compositions preferably have pH between about 5.5 and about 6.5. | 2010-02-04 |
20100029661 | Anesthetic compositions and methods of use - The invention generally relates to anesthetic compositions comprising low doses of a selective a-2 adrenergic receptor agonists in combination with anesthetic agents. The invention also relates to methods of using these compositions; in particular, the use of these compositions in humans to enhance the efficacy of a local peripheral anesthetic injection. The compositions and the methods are particularly useful in regional block anesthetic injections, and more particularly, in dental anesthetic injections. | 2010-02-04 |
20100029662 | Vasoconstriction compositions and methods of use - The invention generally relates to compositions for inducing vasoconstriction. The compositions comprise highly selective alpha-2 adrenergic receptor agonists, at low concentrations, such as below 0.05% weight by volume. The compositions preferably comprise brimonidine. The compositions preferably have pH between about 5.5 and about 6.5. | 2010-02-04 |
20100029663 | Compositions and methods for reducing activation of alpha-1 receptors - The invention generally relates to compositions and methods for reducing activation of a-1 adrenergic receptors. The compositions comprise highly selective a-2 adrenergic receptor agonists, at low concentrations, such as below 0.05% weight by volume. The compositions preferably comprise brimonidine. The compositions preferably have pH between about 5.5 and about 6.5. | 2010-02-04 |
20100029664 | PYRROLIDIN-3-YLMETHYL-AMINE AS OREXIN ANTAGONISTS - The present invention is concerned with novel sulfonamides of formula I | 2010-02-04 |
20100029665 | Methods and Compositions for Treating Migraine Pain - The present invention provides novel methods and compositions for the treatment and prevention of headaches, vascular headaches, migraine headaches, cluster headaches, and migraine. One of the headaches, vascular headaches, migraine headaches, cluster headaches, and migraine treated by the methods and compositions of the invention is migraine. | 2010-02-04 |
20100029666 | Macrocyclic Quinoxaline Compounds as HCV NS3 Protease Inhibitors - The present invention relates to macrocyclic a compound of formula (I) and its use as inhibitors of the hepatitis C virus (HCV) NS3 protease, and in treating or preventing HCV infections. | 2010-02-04 |
20100029667 | Spray dried formulation - Pharmaceutical compositions comprising a poorly water soluble ionizable drug, a cationic species and a dispersion polymer are disclosed, together with a process for forming the compositions. The neutral form of the drug has (i) a solubility of less than 1 mg/ml, in aqueous solution at a pH between 6 and 7, (ii) a solubility of less than 20 mg/mL in a volatile organic solvent, and (iii) an acidic pKa value of greater than 5. At least 90 wt % of the drug in the solid dispersion being in a non-crystalline form. The drug, the cationic species, and the dispersion polymer constitute at least 80 wt % of the solid dispersion. | 2010-02-04 |
20100029668 | NOVEL PYRIDAZINE DERIVATIVES - The present invention relates to novel pyridazine derivatives of formula (I) as active ingredients which have microbiocidal activity, in particular fungicidal activity: wherein R | 2010-02-04 |
20100029669 | 3-(SUBSTITUTED ETHYL)-RIFAMYCIN DERIVATIVES USEFUL AS ANTIMICROBIAL AGENTS - The present invention is directed to novel 3-(substituted ethyl) rifamycin derivatives, pharmaceutical compositions containing them and the use of said derivatives and pharmaceutical compositions as antimicrobial agents against pathogenic microorganisms, particularly against resistant microbes. | 2010-02-04 |
20100029670 | ORGANIC COMPOUNDS - The present invention relates to compounds of formula (I) | 2010-02-04 |
20100029672 | METHOD OF TREATING LIVER DISEASE - Treating diseased or damaged tissue, particularly the liver, using stem cells. The hepatic stem cell population of a subject suffering from disease or damaged tissue can be expanded by administering at least one regulator of the sympathetic nervous system. The regulator can be an adrenoceptor agonist or antagonist, adrenoceptor antagonists, prazosin, being particularly preferred. The invention also includes the use of agents which mobilize stem cells in the manufacture of medicaments for the treatment of diseased or damaged tissue. | 2010-02-04 |
20100029673 | THERAPEUTIC AGENTS COMPRISING AN ANTI-ANGIOGENIC AGENT IN COMBINATION WITH AN SRC-INHIBITOR AND THEIR THERAPEUTIC USE - The invention relates to a method for the production of an anti-cancer effect or a method for the treatment of a sold tumour disease by administration of an anti-angiogenic agent selected from 4-(4-fluoro-2-methylindol-5-yloxy)-6-methoxy-7-(3-(pyrrolidin-1-yl)propoxy)quinazoline and 4-(4-bromo-2-fluoroanilino)-6-methoxy-7-(1-methylpiperidin-4-ylmethoxy)quinazoline and pharmaceutically-acceptable acid-addition salts thereof, in combination with a Src kinase inhibitor selected from 4-(6-chloro-2,3-methylenedioxyanilino)-7-[2-(4-methylpiperazin-1-yl)ethoxy]-5-tetrahydropyran-4-yloxyquinazoline and pharmaceutically-acceptable acid-addition salts thereof. | 2010-02-04 |
20100029674 | Methods of Using Phosphoantigen for the Treatment of Cancer - The present invention relates to compositions and methods useful for treating a cancer in mammals, including humans. The methods and compositions typically comprise use of a chemotherapeutic agent and a γδ T cell activator such that the composition is effective for treating a cancer. Preferably the composition enhances the effect of the γδ T cell activator and/or prevents or delays the escape of a tumor from control chemotherapy, particularly an anti-angiogenic chemotherapeutic agent. | 2010-02-04 |
20100029675 | Pyrimidine-2, 4-diamine JAK2 Kinase inhibiting anti-inflammation use - A method of treatment or prevention of Castleman's disease, atherosclerosis, coronary artery disease, peripheral edema, peripheral vascular disease, glaucoma, and wet or dry age-related macular degeneration (AMD), asthma; chronic bronchitis; chronic obstructive pulmonary disease; adult respiratory distress syndrome; infant respiratory distress syndrome; cough; chronic obstructive pulmonary disease in animals; adult respiratory distress syndrome; ulcerative colitis; Crohn's disease; hypersecretion of gastric acid; bacterial, fungal, or viral induced sepsis or septic shock; endotoxic shock; laminitis or colic in horses; spinal cord trauma; head injury; neurogenic inflammation; pain; reperfusion injury of the brain; psoriatic arthritis; rheumatoid arthritis; alkylosing spondylitis; osteoarthritis; inflammation; or cytokine-mediated chronic tissue degeneration comprises the step of administering a therapeutically effective amount, or a prophylactically effective amount, of a compound having the following structure (I): | 2010-02-04 |
20100029676 | T315A AND F317I MUTATIONS OF BCR-ABL KINASE DOMAIN - The present invention relates to mutant BCR-ABL kinase proteins, and to diagnostic and therapeutic methods and compositions useful in the management of disorders, for example cancers, involving cells that express such mutant BCR-ABL kinase proteins. | 2010-02-04 |
20100029677 | 4-ANILINO-3-QUINOLINECARBONITRILES FOR THE TREATMENT OF CHRONIC MYELOGENOUS LEUKEMIA (CML) - Compounds of the formula: | 2010-02-04 |
20100029678 | DIURETICS - A compound having the structure | 2010-02-04 |
20100029679 | ANTIBACTERIAL QUINOLINE DERIVATIVES - The present invention relates to novel substituted quinoline derivatives according to the general Formula (Ia) or Formula (Ib): | 2010-02-04 |
20100029680 | Certain Chemical Entities, Compositions and Methods - Certain substituted urea derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure. | 2010-02-04 |
20100029681 | HETEROCYCLIC COMPOUNDS AS CALCIUM CHANNEL BLOCKERS - Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted N-type calcium channel activity are disclosed. Specifically, a series of heterocyclic compounds are disclosed of the general formula (1) where X | 2010-02-04 |
20100029682 | NOVEL CHROMENE AND THIOCHROMENE CARBOXAMIDE DERIVATIVES, METHODS FOR PREPARING SAME AND THERAPEUTIC APPLICATIONS OF SAME - The present invention relates to novel chromene or thiochromene carboxamide derivatives, the preparation of same, pharmaceutical compositions of same and the use of same as dopamine D3 ligands as a medicament for central nervous system disorders. | 2010-02-04 |
20100029683 | Methods for regulating cell mitosis by inhibiting serine/threonine phosphateses - Disclosed herein are methods of inhibiting proliferation of a cancer cell or inducing apoptosis of a cancer cell, which does not overexpress N—CoR. Also disclosed herein are methods of inhibiting proliferation or inducing apoptosis of a cancer cell that overexpresses TCTP and methods for determining whether a compound is effective in inducing cell death. | 2010-02-04 |
20100029684 | Pyrazinone Modulator of Corticotropin-Releasing Factor Receptor Activity - The invention relates to the compound (S)-4-(1-cyclopropyl-2-methoxyethyl)-6-(6-(difluoromethoxy)-2,5-dimethylpyridin-3-ylamino)-5-oxo-4,5-dihydropyrazine-2-carbonitrile, pharmaceutical compositions of the compound, and methods of using the compound for the treatment of psychiatric disorders and neurological diseases including depression, anxiety related disorders, irritable bowel syndrome, addiction and negative aspects of drug and alcohol withdrawal, and other conditions associated with CRF. | 2010-02-04 |
20100029685 | OXADIAZOLE AND THIADIAZOLE COMPOUNDS AND THEIR USE AS NICOTINIC ACETYLCHOLINE RECEPTOR MODULATORS - This invention relates to oxadiazolyl and thiadiazolyl derivatives, which are found to be modulators of the nicotinic acetylcholine receptors. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances. | 2010-02-04 |
20100029686 | HCV PROTEASE INHIBITORS AND USES THEREOF - This invention relates to: (a) compounds of formula I and salts thereof that, inter alia, are useful as hepatitis C virus (HCV) inhibitors; (b) intermediates useful for the preparation of such compounds and salts; (c) pharmaceutical compositions comprising such compounds and salts; and (d) methods of use of such compounds, salts, and compositions. | 2010-02-04 |
20100029687 | PIPERIDINE DERIVATIVE OR SALT THEREOF - [Problem] To provide a compound which can be used for treating diseases in which a calcium sensing receptor (CaSR) participates, particularly hyperparathyroidism. | 2010-02-04 |
20100029688 | BIPIPERIDINYL COMPOUNDS, COMPOSITIONS CONTAINING SUCH COMPOUNDS AND METHODS OF TREATMENT - Bipiperidinyl compounds of the formula I, are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. Pharmaceutically acceptable salts and solvates are included as well. The compounds are useful as agonists of the g-protein coupled receptor GPR-119. | 2010-02-04 |
20100029689 | PHOSPHODIESTERASE 4 INHIBITORS - PDE4 inhibition is achieved by novel compounds, e.g., N-substituted aniline and diphenylamine analogs. The compounds of the present invention are of Formula I: | 2010-02-04 |
20100029690 | NITROGEN-CONTAINING HETEROCYCLIC COMPOUNDS - Nitrogen-containing heterocyclic compounds represented by the following Formula (1) are provided. The compounds or salts thereof have a strong EP1 antagonistic activity when they are administered to a human or an animal, and they are useful as an effective component of a pharmaceutical agent for prophylaxis and/or treatment of an overactive bladder, for example. Furthermore, they are useful as an effective component of a pharmaceutical agent for the prophylaxis and/or treatment of symptoms including frequent urination, urinary urgency and urinary incontinence. | 2010-02-04 |
20100029691 | FAST ONSET ORODISPERSABLE TABLETS - The present invention provides orodispersable tablets and methods of using the same. The tablets and methods are useful, for example, for reducing first pass metabolism of orally administered active agents, enhancing bioavailability of active agents, and/or reducing the time it takes for an active agent to achieve maximal effect in a subject. The tablets, when taken orally, disintegrate or dissolve rapidly such that active agent included in the tablets is absorbed in the buccal cavity. The invention further provides methods of manufacturing any of the tablets disclosed herein and containers that include any of the tablets disclosed herein. | 2010-02-04 |
20100029692 | METHODS OF OPTIMIZING DRUG THERAPEUTIC EFFICACY FOR TREATMENT OF IMMUNE-MEDIATED GASTROINTESTINAL DISORDERS - The present invention provides a method of optimizing therapeutic efficacy and reducing toxicity associated with 6-mercaptopurine drug treatment of an immune-mediated gastrointestinal disorder such as inflammatory bowel disease. The method of the invention includes the step of determining the level of one or more 6-mercaptopurine metabolites in the patient having an immune-mediated gastrointestinal disorder. | 2010-02-04 |
20100029693 | NOVEL PI3K DELTA INHIBITORS AND METHODS OF USE THEREOF - The present invention relates generally to phosphoinositide 3-kinases (PI3Ks), and more particularly to specific, selective, improved PI3Kδ inhibitors and methods of inhibiting undesirable levels of PI3Kδ activity using these PI3Kδ inhibitors to treat disorders mediated by PI3Kδ. | 2010-02-04 |
20100029694 | Heterocyclic compounds and their use as aldosterone synthase inhibitors - Heterocyclic compounds of the general formula (I) | 2010-02-04 |
20100029695 | METHOD OF TREATING DERMATITIS COMPRISING ADMINISTERING A CHYMASE INHIBITOR - A medicament safe and free from side effects, for the prevention or treatment of dermatitis exhibiting a biphasic inflammation reaction or dermatitis induced by repeated exposure to an antigen, which suppresses the progress of the condition and improves the quality of life of the patient, which medicament treats dermatitis exhibiting a biphasic inflammation reaction or dermatitis induced by repeated exposure to an antigen by including a quiazoline derivative having the formula (I) or (II) or its pharmaceutically acceptable salt as an effective ingredient: | 2010-02-04 |
20100029696 | INDOLYLAMINO QUINAZOLINE DERIVATIVES AS ANTITUMOR AGENTS - A quinazoline derivative of the Formula (I) wherein the substituents are as defined in the text for use in the production of an anti proliferative effect which effect is produced alone or in part by inhibiting erbB2 receptor tyrosine kinase in a warm blooded animal such as man. | 2010-02-04 |
20100029697 | SUBSTITUTED PYRIDO[3,2-E][1,2,4]TRIAZOLO[4,3-C]PYRIMIDINE DERIVATIVES AS CANNABINOID-1 RECEPTOR MODULATORS - Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, Alzheimer s disease, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson s disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, cirrhosis of the liver, non-alcoholic fatty liver disease (NAFLD), non-alcoholic steatohepatitis (NASH), and the promotion of wakefulness. | 2010-02-04 |