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48th week of 2008 patent applcation highlights part 47
Patent application numberTitlePublished
20080293673N-ACETYGLUCOSAMINE DERIVATIVES AND USE THEREOF - The present invention relates to An N-acetylglucosamine derivative represented by the following formula (1), and a hyaluronic acid production promoting agent containing the same and a skin external preparation containing the same:2008-11-27
20080293674Azinyl Imidazoazine and Azinyl Carboxamide - The invention relates to azinylimidazoazines of structure (I) and their salts and N-oxides,2008-11-27
20080293675ANTIBIOTICS CONTAINING BORINIC ACID COMPLEXES AND METHODS OF USE - The structure and preparation of antibiotics incorporating borinic acid complexes are disclosed, especially hydroxyquinoline, imidazole and picolinic acid derivatives, along with compositions of these antibiotics and methods of using the antibiotics and compositions as bactericidal and fungicidal agents as well as therapeutic agents for the treatment of diseases caused by bacteria and fungi. 2008-11-27
20080293676Insecticidal Agents Based on Selected Insecticides and Safeners - Insecticidal compositions characterized by an effective amount of an active ingredient combination comprising 2008-11-27
20080293677Use of Alternating Amine and Non-Amine Bisphosphonate Combinations For Treating Osteoporosis - A method of treating osteoporosis in a human in need thereof by administering alternating amine and non-amine bisphosphonates in a defined dosing schedule. The invention demonstrates an effective response and sustained benefit in the treatment of osteoporosis. Particularly, the method involves administration of a time-dependent dose of more than one bisphosphonate, specifically, alternating administration of a first bisphosphonate with a second bisphosphonate, wherein at least one bisphosphonate is administered in a stepped-up dosage amount.2008-11-27
20080293678Organic Nitric Oxide Donor Salts of Angiotensin Converting Enzyme Inhibitors, Compositions and Methods of Use - The invention describes compositions and kits comprising at least qrie organic nitric oxide enhancing salt of an angiotensin converting enzyme inhibitor, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The invention also provides methods for (a) treating cardiovascular diseases; (b) treating renovascular diseases; (c) treating diabetes; (d) treating diseases resulting from oxidative stress; (e) treating endothelial dysfunctions; (f) treating diseases caused by endothelial dysfunctions; (g) treating cirrhosis; (h) treating pre-eclampsia; Q) treating osteoporosis; (k) treating nephropathy; (l) treating peripheral vascular diseases; (m) treating portal hypertension; (n) treating ophthalmic disorders; (o) treating metabolic syndrome; and (p) treating hyperlipidemia. The organic nitric oxide enhancing compounds that form salts with the angiotensin converting enzyme inhibitors are organic nitrates, organic nitrites, nitrosothiols, thionitrites, thionitrates, NONOates, heterocyclic nitric oxide donors and/or nitroxides. The heterocyclic nitric oxide donors are furoxans, sydnonimines, oxatriazole-5-ones and/or oxatriazole-5-imines.2008-11-27
20080293679Use of carotenoids and/or carotenoid derivatives/analogs for reduction/inhibition of certain negative effects of COX inhibitors - Administering carotenoids, and in particular xanthophyll carotenoids, or analogs or derivatives of astaxanthin, lutein, zeaxanthin, lycoxanthin, lycophyll, or lycopene to a subject undergoing treatment with COX-2 inhibitor drugs may reduce at least a portion of the adverse side effects associated with administration of COX-2 selective inhibitor drugs. The carotenoids, or analogs or derivatives thereof may be administered to a subject prior to, at the same time as, or after the commencement of COX-2 selective inhibitor drug therapy. The carotenoids, or analogs or derivatives thereof may be administered to a subject concurrently with COX-2 selective inhibitor drugs therapy. The carotenoids, or analogs or derivatives thereof may be incorporated into pharmaceutical preparation in combination with the COX-2 selective inhibitor drug or may be administered separately. Administration of the analogs or derivatives described herein may reduce peroxidation of LDL and other lipids in the serum and plasma cell membranes of subjects undergoing COX-2 selective inhibitor drug therapy. Administration of the analogs or derivatives described herein may reduce the incidence of deleterious clinical cardiovascular events undergoing COX-2 selective inhibitor drug therapy.2008-11-27
20080293680Substituted Ethane-1,2-Diamines for the Treatment of Alzheimer's Disease II - The invention relates to a compound of the formula (I), wherein R2008-11-27
20080293681SPRAYABLE PHARMACEUTICAL COMPOSITIONS COMPRISING A VITAMIN D DERIVATIVE AND AN OILY PHASE - Anhydrous sprayable physically and chemically stable pharmaceutical/dermatological compositions containing a vitamin D derivative as an active pharmaceutical ingredient, particularly calcitriol, and an oily phase are formulated into a physiologically-acceptable medium, and are useful for the treatment of a variety of conditions and afflictions, notably psoriasis.2008-11-27
20080293682Novel Betulinic Acid Derivatives - The invention relates to novel betulinic acid derivatives of formula (I), wherein R is C(═CH2008-11-27
20080293683Hormone Replacement Therapy - A hormone replacement therapy formulation and method comprising selective estrogenic compounds which preferentially stimulate the estrogen receptor alpha over the estrogen receptor beta.2008-11-27
20080293684Heterocyclic Acetophenone Potentiators of Metabotropic Glutamate Receptors - The present invention is directed to compounds which are potentiators of metabotropic glutamate receptors, including the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.2008-11-27
20080293685SPIRO AND OTHER DERIVATIVES OF DIAMONDOIDS POSSESSING THERAPEUTIC ACTIVITY IN THE TREATMENT OF VIRAL DISORDERS - This invention relates to diamondoid derivatives which exhibit therapeutic activity. Specifically, the diamondoid derivatives herein exhibit therapeutic effects in the treatment of viral disorders. Also provided are methods of treatment, prevention and inhibition of viral disorders in a subject in need.2008-11-27
20080293686SEMI-SOLID SYSTEMS CONTAINING AZETIDINE DERIVATIVES - The present invention relates to novel formulations of azetidine derivatives for oral administration comprising at least one azetidine compound of formula (Ia) or (Ib):2008-11-27
20080293687Benzamide Compounds - The invention concerns benzamide compounds of Formula (I), wherein R2008-11-27
20080293688AMINOAZACYCLYL-3-SULFONYLINDAZOLES AS 5-HYDROXYTRYPTAMINE-6 LIGANDS - The present invention provides a compound of formula I and the use thereof in the therapeutic treatment of disorders related to or affected by the 5-HT6 receptor.2008-11-27
20080293689Compounds with Atypical Antipsychotic Activity - Formula (I) compounds with atypical antipsychotic activity2008-11-27
20080293690[6,6] AND [6,7]-BICYCLIC GPR119 G PROTEIN-COUPLED RECEPTOR AGONISTS - Novel compounds are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR119 G protein-coupled receptor modulator therapy. These novel compounds have the structure:2008-11-27
20080293691Treatment Method - The present invention is directed to methods of treating an ocular neovascular disorder in a mammal by administration of pyrimidine derivatives, benzodiazepinyl derivatives and pharmaceutical compositions containing the same. The invention encompasses methods of treating an ocular neovascular disorder by administration of 5-[[4-[(2,3-Dimethyl-2H-indazol-6-yl)methylamino]-2-pyrimidinyl]amino]-2-methylbenzenesulfonamide, (S)-3-oxo-8-[3-(pyridin-2-ylamino)-1-propyloxy]-2-(2,2,2-trifluoroethyl)-2,3,4,5-tetrahydro-1H-2-benzazepine-4-acetic acid or salts or solvates thereof. Combination therapies for the treatment of ocular neovascular disorders are also encompassed.2008-11-27
20080293692SUCCINOYLAMINO LACTAMS AS INHIBITORS OF A-BETA PROTEIN PRODUCTION - This invention relates to novel lactams having drug and bio-affecting properties, their pharmaceutical compositions and methods of use. These novel compounds inhibit the processing of amyloid precursor protein and, more specifically, inhibit the production of Aβ-peptide, thereby acting to prevent the formation of neurological deposits of amyloid protein. More particularly, the present invention relates to the treatment of neurological disorders related to β-amyloid production such as Alzheimer's disease and Down's Syndrome.2008-11-27
20080293693Treatment or Prevention of Ovarian Hyperstimulation Syndrome (Ohss) Using a Dopamine Agonist - Disclosed herein is a method for preventing ovarian hyperstimulation syndrome in a subject by administering an effective amount of a dopamine agonist in a pharmaceutically acceptable carrier. Also disclosed herein is a method for treating ovarian hyperstimulation syndrome by administering an effective amount of a dopamine agonist in a pharmaceutically acceptable carrier.2008-11-27
20080293694New compounds - The present invention relates to novel compounds of formula (I):2008-11-27
20080293695Salts of physiologically active and psychoactive alkaloids and amines simultaneously exhibiting bioavailability and abuse resistance - Drug substances comprising a pharmaceutically acceptable organic acid addition salt 6f amine containing pharmaceutically active compounds useful for the treatment of a therapeutic ailment administration and exhibiting prophylactic properties when employed in non-therapeutic administration.2008-11-27
200802936962-Aminoarylcarboxamides Useful as Cancer Chemotherapeutic Agents - A compound having the formula (1)2008-11-27
20080293697Pyrazolo[4,3-D]Pyrimidines - This invention relates to compounds of formula (I).2008-11-27
20080293698Methods and Compositions for Treating Arg - The invention provides dilute and concentrated, aqueous, pharmaceutical compositions comprising gamma-hydroxybutyric acid or pharmaceutically acceptable salts thereof; gamma-butyryl lactone; 1,4-butanediol; 4-hydroxyl pentanoic acid or pharmaceutically acceptable salts thereof; 4-hydroxyl pentanoic acid lactone, or combinations thereof, and a coloring agent and/or flavoring agent that is useful in preventing sexual assault or date rape. Methods of treating conditions responsive to the administration of gamma-hydroxyl butyric acid and/or its pharmaceutically acceptable salts; gamma-butyryl lactone; 1,4-butanediol; 4-hydroxyl pentanoic acid and/or its pharmaceutically acceptable salts; and 4-hydroxyl pentanoic acid lactone are also described. The invention provides methods for treating patients with acquired resistance to GABAnergic agents.2008-11-27
20080293699Inhibitors of thapsigargin-induced cell death - Methods for screening for inhibitors of endoplasmic reticulum (ER) stress are provided. These methods involve the addition of thapsigargin, which induces ER stress, and a test agent to mammalian cells in multi-well plates. Cell survival can be readily monitored by measuring intracellular ATP content using a bioluminescent reagent. Screening a commercially available library of 50,000 compounds led to the identification of 93 hit compounds that were subjected to secondary assays to confirm their ability to rescue cells from thapsigargin-induced cell death.2008-11-27
20080293700Compositions and Methods Relating to Novel Compounds and Targets Thereof - The present invention relates to novel chemical compounds, methods for their discovery, and their therapeutic use. In particular, the present invention provides benzodiazepine derivatives and methods of using benzodiazepine derivatives as therapeutic agents to treat a number of conditions associated with the faulty regulation of the processes of programmed cell death, autoimmunity, inflammation, and hyperproliferation, and the like.2008-11-27
200802937011-Acylamino-2-Hydroxy-3-Amino- -Arylalkanes as Renin Inhibitors - 1-Acylamino-2-hydroxy-3-amino-ω-arylalkanes of formula I. and the salts thereof, have renin-inhibiting properties and can be used as antihypertensive, medicinally active ingredients.2008-11-27
20080293702Nitric Oxide Enhancing Pyruvate Compounds, Compositions and Methods of Use - The invention provides novel compositions and kits comprising at least one nitric oxide enhancing pyruvate compound, or a pharmaceutically acceptable salt thereof, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The invention also provides methods for (a) treating cardiovascular diseases; (b) treating renovascular diseases; (c) treating diabetes; (d) treating diseases resulting from oxidative stress; (e) treating endothelial dysfunctions; (f) treating diseases caused by endothelial dysfunctions; (g) treating cirrhosis; (h) treating pre-eclampsia; (j) treating osteoporosis; (k) treating nephropathy; (l) treating peripheral vascular diseases; (m) treating portal hypertension (n) treating reperfusion injury following ischemia; and/or (m) preserving tissues, organs, organ parts and/or limbs. The nitric oxide enhancing pyruvate compounds comprise at least one nitroxide group.2008-11-27
20080293703Topical Preparation and Method for Transdermal Delivery and Localization of Therapeutic Agents - Disclosed herein is a preparation for topically delivering and localizing therapeutic agents, comprising: a vasoconstrictor for retarding vascular dispersion of a therapeutic agent; and a penetration enhancer for facilitating penetration of the vasoconstrictor and the therapeutic agent through a patient's skin. Further disclosed is an associated method of topically delivering and localizing therapeutic agents, comprising the steps of: using a vasoconstrictor for retarding vascular dispersion of a therapeutic agent; in combination with using a penetration enhancer for facilitating penetration of the vasoconstrictor and the therapeutic agent through a patient's skin. Also disclosed are various courses of treatment, which comprise applying the various disclosed combinations of agents to the patient's skin.2008-11-27
20080293704FACTOR Xa INHIBITORS - The present invention is directed to compounds represented by Formula (I) or a pharmaceutically acceptable salt, ester, or prodrug thereof which are inhibitors of Factor Xa. The present invention is also directed to intermediates used in making such compounds, pharmaceutical compositions containing such compounds, methods to prevent or treat certain conditions characterized by undesired thrombosis and methods of inhibiting the coagulation of a blood sample.2008-11-27
20080293705A1 ADENOSINE RECEPTOR ANTAGONISTS - Compounds of the general formula (I) are described:2008-11-27
20080293706QUINOXALINE DERIVATIVES AS PI3 KINASE INHIBITORS - Invented is a method of inhibiting the activity/function of PI3 kinases using quinoxaline derivatives. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries by the administration of quinoxaline derivatives.2008-11-27
20080293707Use of Kiralaxyl for Protecting Phytopathogens, and Corresponding Methods and Compositions - The invention relates to a method for protecting against phytopathogens which comprises treating seed with kiralaxyl (methyl N-(phenylacetyl)-N-(2,6-xylyl)-D-alaninate) in combination with at least one further pesticide and furthermore to the corresponding use of kiralaxyl in combination with at least one further pesticide and to corresponding compositions. Also described is special seed.2008-11-27
20080293708Pyrimidine Derivatives - Novel pyrimidine derivatives of formula I2008-11-27
20080293709Novel 2-Amino-Heterocycles Useful in the Treatment of Abeta-Related Pathologies - This invention relates to novel compounds having the structural formula I below: and to their pharmaceutically acceptable salts, compositions and methods of use. These novel compounds provide a treatment or prophylaxis of cognitive impairment, Alzheimer Disease, neurodegeneration and dementia.2008-11-27
20080293710Aerosol formulation for the inhalation of beta-agonists - The present invention relates to a propellant-free aerosol formulation which [contains] one or more compounds of general formula 12008-11-27
20080293711Chemokine receptor modulators - The invention provides compounds of Formula (I)2008-11-27
20080293712Benzo[C][2,7]Naphtyridine Derivatives, Methods of Making Thereof and Methods of Use Thereof - The present invention relates to Benzo[c][2,7]naphthyridine Derivatives, compositions comprising an effective amount of a Benzo[c][2,7]naphthyridine Derivative, methods for treating or preventing a proliferative disorder or an autoimmune disease, comprising administering to a subject in need thereof an effective amount of a Benzo[c][2,7]naphthyridine Derivative, methods for modulating PDK-1 activity, PKA activity, Akt activity, S6K activity, or PKC activity, comprising administering to a subject in need thereof an effective amount of a Benzo[c][2,7]naphthyridine Derivative. The invention also relates to processes for preparing a Benzo[c][2,7]naphthyridine Derivative.2008-11-27
20080293713Inhibitors of Diacylglycerol O-acyltransferase Type 1 Enzyme - The present invention relates to compounds of formula (I):2008-11-27
20080293714Tec Kinase Inhibitors - Disclosed are compounds of formula (I): (F) wherein Ri, R2, X and Ar are defined herein. The compounds of the invention inhibit Itk kinase and are therefore useful for treating diseases and pathological conditions involving inflammation, immunological disorders and allergic disorders. Also disclosed are processes for preparing these compounds and to pharmaceutical compositions comprising these compounds.2008-11-27
20080293715Therapeutic Pyrazolo[3,4-b]Pyridines and Indazoles - The present invention provides for compounds of Formula I:2008-11-27
20080293716Chemical Compounds - There is provided a compound of Formula (I) or a salt, solvate, or physiologically functional derivative thereof:2008-11-27
20080293717ARYL SULFONAMIDES - Compounds are provided that act as potent antagonists of the CCR9 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists.2008-11-27
20080293718Novel 2-Amino-Imidazole-4-One Compounds and Their Use in the Manufacture of a Medicament to Be Used in the Treatment of Cognitive Impairment, Alzheimer's Disease, Neurodegeneration and Dementia - This invention relates to novel compounds having the structural formula I below: and to their pharmaceutically acceptable salt, compositions and methods of use. These novel compounds provide a treatment or prophylaxis of cognitive impairment, Alzheimer Disease, neurodegeneration and dementia.2008-11-27
20080293719Pyridiazinone Derivatives for the Treatment of Tumours - Compounds of the formula (I), in which R2008-11-27
20080293720Pyridinyl Sulfonamide Modulators of Chemokine Receptors - The present invention relates to compounds of following formula:2008-11-27
20080293721ARYLTHIOACETAMIDE CARBOXYLATE DERIVATIVES AS FKBP INHIBITORS FOR THE TREATMENT OF NEUROLOGICAL DISEASES - The present invention provides compounds having the general structure I, or a pharmaceutically acceptable salt thereof:2008-11-27
20080293722Ion Channel Modulators - The invention relates to compounds, compositions comprising the compounds, and methods of using the compounds and compound compositions. The compounds, compositions, and methods described herein can be used for the therapeutic modulation of ion channel function, and treatment of disease and disease symptoms, particularly those mediated by certain calcium channel subtype targets.2008-11-27
20080293723SPIROINDOLINONE DERIVATIVES - There are provided spiroindolinone derivatives of the formula2008-11-27
20080293724Methods Using Hydralazine Compounds and Isosorbide Dinitrate or Isosorbide Mononitrate - The invention provides methods for (a) treating decompensated heart failure; (b) treating compensated heart failure; (c) treating renovascular diseases and (d) treating end-stage renal diseases in a patient in need thereof comprising administering an effective amount of (i) at least one hydralazine compound or a pharmaceutically acceptable salt thereof, (ii) isosorbide dinitrate and/or isosorbide mononitrate, and (iii) optionally at least one compound selected from the group consisting of an angiotensin converting enzyme inhibitor, a β-adrenergic antagonist, an angiotensin II antagonist, an aldosterone antagonist, a cardiac glycoside (digitalis) and a diuretic compound or a combination of two or more thereof. The hydralazine compound may be hydralazine hydrochloride.2008-11-27
20080293725Prognostic Molecular Markers - The present invention relates to the use of ecteinascidin 743 in patients having certain levels of molecular markers who can predict the outcome of chemotherapy, in particular in patients having low levels of BRCA1 expression.2008-11-27
20080293726Combinations of Eszopiclone and Trans 4-(3,4-Dichlorophenyl)-1,2,3,4-Tetrahydro-N-Methyl-1-Napthalenamine or Trans 4-(3,4-Dichlorophenyl)-1,2,3,4-Tetrahydro-1-Napthalenamine, and Methods of Treatment of Menopause and Mood, Anxiety, and Cognitive Disorders - One aspect of the present invention relates to pharmaceutical compositions containing two or more active agents that when taken together can be used to treat, e.g., menopause, mood disorders, anxiety disorders, or cognitive disorders. The first component of the pharmaceutical composition is a sedative eszopiclone. The second component of the pharmaceutical composition is trans 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-N-methyl-1-napthalenamine or trans 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-napthalenamine. The present invention also relates to a method of treating menopause, perimenopause, mood disorders, anxiety disorders, and cognitive disorders.2008-11-27
20080293727Novel sulfonamide inhibitors of aspartyl protease - The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.2008-11-27
20080293728Complexes Comprising alpha2-Adrenergic Receptor Agonists and Compositions - A complex comprises at least an α2008-11-27
20080293729COMPOSITION AND METHOD OF DECREASING RENAL ISCHEMIC DAMAGE - A method of decreasing renal ischemic damage comprising a) identifying an organism having a kidney that is susceptible to renal ischemic damage from an ischemic event; and b) administering to the organism one or more than one effective dose of an agent prior to the ischemic event; where administering to the organism the one or more than one effective dose of the agent serves to at least partially protect the organism's kidney from damage during a subsequent ischemic event. A composition for decreasing renal ischemic damage comprising one or more than one phosphodiesterase inhibitor, and one or more than one HMG-CoA reductase inhibitor.2008-11-27
20080293730Tricyclo Substituted Amides - Compounds of Formula (I): (formula) or pharmaceutically acceptable salts thereof, are useful in the prophylactic and therapeutic treatment of hyperglycemia and diabetes.2008-11-27
20080293731Organic Compounds - The present invention relates to 1-aza-bicycloalkyl derivatives of Formula (I)2008-11-27
20080293732Substituted pyrazoles - Substituted pyrazoles, methods of manufacturing them, compositions containing them, and methods of using them to treat, for example, autoimmune diseases mediated by cathepsin S.2008-11-27
20080293733AXL KINASE INHIBITORS - Axl kinase inhibitory compounds are disclosed, as well as compositions and methods of using the same in the treatment of cancer and other conditions mediated by and/or associated with Axl kinase.2008-11-27
20080293734PHARMACEUTICAL COMPOSITIONS - Disclosed are useful pharmaceutical compositions.2008-11-27
20080293735Therapeutic treatment for metabolic syndrome, type 2 diabetes, obesity, or prediabetes - The present invention is directed to a method for treating a patient suffering from the metabolic syndrome, Type 2 diabetes, obesity, or prediabetes, comprising the step of increasing the ratio of dopaminergic neuronal to noradrenergic neuronal activity within the central nervous system and particularly the hypothalamus of the central nervous system of the patient.2008-11-27
20080293736Compositions, Synthesis, and Methods of Using Quinolinone Based Atypical Antipsychotic Agents - The present invention provides novel quinolinone derivatives which can be advantageously used for treating schizophrenia and related psychoses such as acute manic, bipolar disorder, autistic disorder, and depression.2008-11-27
20080293737ION CHANNEL MODULATORS AND METHODS OF USE - In general, the invention relates to compounds useful as ion channel modulators. It has now been found that compounds of this invention, and pharmaceutically acceptable compositions thereof, are useful as inhibitors of voltage-gated sodium channels.2008-11-27
20080293738Formulation of Quinolinones - A pharmaceutical formulation, comprising: a compound of formula (I), a tautomer of the compound, a salt of the compound, a salt of the tautomer, or a mixture thereof and at least one ingredient selected from the group consisting of (i) cellulose; (ii) silicon dioxide; (iii) magnesium stearate; and (iv) an ingredient selected from crospovidone, starch, or lactose.2008-11-27
20080293739COMPOUNDS FOR MODULATING T-CELLS - Disclosed are compounds and compositions that modulate T-cells. Such compounds can be used to treat T-cell mediated disease like T-ALL, rheumatoid arthritis, multiple sclerosis, and graft-vs-host disease (GvHD), to name but a few. The compounds have a general structure as shown in Formula I.2008-11-27
20080293740METHOD OF TREATING ACID-SENSING ION CHANNEL MEDIATED PAIN, COUGH SUPPRESSION, AND CENTRAL NERVOUS SYSTEM DISORDERS - The present invention provides a variety of methods of treatment of acid-sensing ion channel (ASIC) mediated pain, cough, and central nervous system disorders by ASICs inhibition with a series of pyrazinoylguanidine compounds represented by formula (I) as defined herein.2008-11-27
20080293741Tricyclo Substituted Amides as Glucokinase Modulators - Compounds of Formula (I): (I) or pharmaceutically acceptable salts thereof, are useful in the prophylactic and therapeutic treatment of hyperglycemia and diabetes.2008-11-27
20080293742Novel N-(Fluoro-Pyrazinyl)-Phenylsulfonamides as Modulators of Chemokine Receptor Ccr4 - The invention provides N-(fluoro-pyrazinyl)-phenylsulfonamides of formula (I) wherein R2008-11-27
20080293743Novel Hydantoin Derivatives as Metalloproteinase Inhibitors - The invention provides compounds of formula (I): wherein R2008-11-27
20080293744Enantiomers of Selected Fused Pyrimidones and Uses in the Treatment and Prevention of Cancer - This invention relates to novel compounds having the structural formula (I) and to their pharmaceutical compositions and to their methods of use. These novel compounds provide a treatment or prophylaxis of cancer.2008-11-27
20080293745New amino-alkyl-amide derivatives as CCR3 receptor ligands - The invention relates to a compound of the general formula (I),2008-11-27
20080293746COMBINATIONS COMPRISING PREGABALIN - The invention relates to a combination of pregabalin and 1-(2-ethoxyethyl)-5-[ethyl(methyl)amino]-N-mesyl-7-[(4-methyl-2-pyridyl)amino]-1H-pyrazolo[4,3-d]pyrimidine-3-carboxamide, to pharmaceutical compositions containing the combination, and to the use of the combination in the treatment of pain.2008-11-27
20080293747Chemical Synthesis of a Highly Potent Epothilone - A highly active synthetic epothilone compound whose activity exceeds that of either epothilone EpoA or EpoB when assayed as a cytotoxic agent against a cancer cell line is disclosed as is a pharmaceutical composition containing the synthetic epothilone.2008-11-27
20080293748Thioxanthine Derivatives as Myeloperoxidase Inhibitors - There is disclosed the use of a compound of formula (Ia) or (Ib)2008-11-27
20080293749Pyrrolidine(thi)ones Substituted by Heterocyclic Substituents in The 3-Position - Pyrrolidine(thi)one compounds substituted by heterocyclic substituents in the 3-position, their preparation and use in pharmaceutical compositions, in particular as immunomodulators for treatment and/or inhibition of inflammatory and autoimmune diseases and haematological-oncological diseases.2008-11-27
20080293750Susceptibility Gene for Myocardial Infarction, Stroke, Paod and Methods of Treatment - Linkage of myocardial infarction (MI) and a locus on chromosome 13q12 is disclosed. In particular, the FLAP gene within this locus is shown by genetic association analysis to be a susceptibility gene for MI and ACS, as well as stroke and PAOD. Pathway targeting for treatment and diagnostic applications in identifying those who are at risk of developing MI, ACS, stroke or PAOD, in particular are described. The invention also provides for compositions comprising a leukotriene synthesis inhibitor and a stating and methods of using these compositions to reduce C-reactive protein in a human subject at risk of MI, ACS, stroke and/or PAOD.2008-11-27
20080293751Tetralin and indane derivatives and uses thereof - Compounds of the formula I:2008-11-27
20080293752Antiseptic body glide - An antiseptic body glide is a body glide with antiseptic properties. The antiseptic components do not interfere with other body glide components such as lubricants or preservatives. Additionally, the antiseptic body glide does not react unfavorably with latex. The antiseptic components do not have a bad taste or react with the other components to produce a bad taste. As such, the antiseptic body glide enhances intimate activities without compromising those activities in any way.2008-11-27
20080293753Novel Compounds - The invention relates to quaternary α-aminocarboxyamide derivatives of formula (I), wherein R2008-11-27
20080293754CYCLOPAMINE ANALOGS - The invention provides novel derivatives of cyclopamine having the following formula:2008-11-27
20080293755HETEROCYCLIC CYCLOPAMINE ANALOGS AND METHODS OF USE THEREOF - The present invention relates to steroidal alkaloids that can be used in the treatment of hedgehog pathway related disorders, particularly cancer.2008-11-27
200802937564,4-DISUBSTITUTED PIPERIDINE DERIVATIVES - This invention relates to 4,4-disubstituted piperidine derivatives of the formula2008-11-27
20080293757ABCA1 ELEVATING COMPOUNDS - The present invention provides compounds useful for increasing cellular ATP binding cassette transporter ABCA1 production in mammals, and to methods of using such compounds in the treatment of coronary artery diseases, dyslipidiemias and metabolic syndrome. The invention also relates to methods for the preparation of such compounds, and to pharmaceutical compositions containing them.2008-11-27
20080293758Combination of a Steroid Sulfatase Inhibitor and an Ascomycin - A combination of a steroid sulfatase inhibitor and an ascomycin, which combination is useful as a pharmaceutical.2008-11-27
20080293759Method for Treating Cancer Based on the Modulation of Calcineurin - The present invention relates to methods for treating a haematopoietic tumor by administering a drug inhibiting calcineurin and/or the calcineurin/NFAT pathway, alone or in combination with other cancer therapy, pharmaceutical compositions useful in such methods, and screening methods for identifying a compound useful for treating a haematopoietic tumor.2008-11-27
20080293760Gemifloxacin Process and Polymorphs - The present invention provides a novel process for the preparation of gemifloxacin and its pharmaceutically acceptable acid addition salts in high yield. The present invention also relates to novel polymorphs of gemifloxacin free base and its hydrates to the processes for their preparation and to pharmaceutical compositions comprising them. The present invention also relates to infusion solutions of gemifloxacin and to processes for their preparation. Thus, 7-chloro-1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-1,8-naphthyridine-3-carboxylic acid is reacted with a mixture of acetic anhydride, acetic acid and boric acid to give borane compound, which is then treated with 4-Aminomethyl-3-methoxyimino-pyrrolidinium dimethanesulfonate in presence of triethylamine, followed by treatment with 3.5% sodium hydroxide solution to give gemifloxacin free base.2008-11-27
20080293761Pyrrolopyridine-2-Carboxylic Acid Amide Derivative Useful as Inhibitor of Glycogen Phosphorylase - The present invention is directed to a novel form of a pyrrolopyridine-2-carboxylic acid amide of formula (I), which is an inhibitor of glycogen phosphorylase, compositions containing it and their use in therapy. The invention is also directed to processes for production of the novel form, novel intermediates used in said processes and processes for the production of said intermediates.2008-11-27
20080293762Preventive and Therapeutic medicament for gastroesophageal reflux disease - The compound of the following formula:2008-11-27
20080293763NOVEL NITROGEN-CONTAINING HETEROARYL COMPOUNDS AND METHODS OF USE THEREOF - The present invention relates to compounds suitable for use in mediating hypoxia inducible factor and for treating erythropoietin-associated conditions by increasing endogenous erythropoietin in vitro and in vivo.2008-11-27
20080293764LPA RECEPTOR ANTAGONIST - A compound of the general formula (I):2008-11-27
20080293765Alkylsulphonamide Quinolines - Compounds of Formula I2008-11-27
20080293766SMALL-MOLECULE INHIBITORS OF THE ANDROGEN RECEPTOR - The present invention provides a method of inhibiting an androgen receptor by administering a compound of Formula I:2008-11-27
200802937671-Isopropyl-2-Oxo-1,2-Dihydropyridine-3-Carboxamide Derivatives Having 5-Ht4 Receptor Agonistic Activity - This invention provides a compound of formula (I): wherein R2008-11-27
20080293768Novel Compounds Derived From 5-Thioxylose And Their Use In Therapeutics - The invention relates to novel 5-thioxylose compounds, preferably derivatives of the 5-thioxylopyranose type, to the process for their preparation and to their use as active principles of drugs intended especially for the treatment or prevention of thrombosis or cardiac insufficiency.2008-11-27
20080293769Polymorphs of a C-Met/Hgfr Inhibitor - This invention relates to polymorphs of (R)-3-[1-(2,6-Dichloro-3-fluoro-phenyl)-ethoxy]-5-(1-piperidin-4-yl-1H-pyrazol-4-yl)-pyridin-2-ylamine that are useful in the treatment of abnormal cell growth, such as cancer, in mammals. This invention also relates to compositions including such salts and polymorphs, and to methods of using such compositions in the treatment of abnormal cell growth in mammals, especially humans.2008-11-27
20080293770Compounds Which Have Activity at M1 Receptor and Their Uses In Medicine - Compounds of formula (I) and salts are provided:2008-11-27
20080293771AZACYCLYLBENZAMIDE DERIVATIVES AS HISTAMINE-3 ANTAGONISTS - The present invention provides a compound of formula I and the use thereof for the treatment of a central nervous system disorder related to or affected by the histamine-3 receptor2008-11-27
20080293772SALTS OF PICOTAMIDE - The invention relates to salts of picotamide (N,N′-bis-(3-picolyl)-4-methoxyisophthalamide) with strong acids, to pharmaceutical compositions containing picotamide salts, and to a method of treatment of cardiovascular and related diseases using picotamide salts. Particularly useful are picotamide hydrochloride and picotamide mesylate, preferably on a carbohydrate carrier such as hydroxymethylpropylcellulose.2008-11-27