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42nd week of 2008 patent applcation highlights part 46
Patent application numberTitlePublished
20080255038PHARMACEUTICAL COMPOSITIONS - This invention relates to a compound of general formula (I):2008-10-16
20080255039Il-15 Binding Site for Il 15-Ralpha and Specific Il-15 Mutants Having Agonists/Antagonists Activity - The present invention relates to the identification of an epitope in human Interleukin-15 (IL-15) that is responsible for binding to the interleukin-15 receptor α-chain. Two IL-15 regions are involved in the formation of this epitope: the first region (2008-10-16
20080255040GLYCOSYLATION OF PEPTIDES VIA O-LINKED GLYCOSYLATION SEQUENCES - The present invention provides sequon polypeptides with an amino acid sequence including one or more exogenous O-linked glycosylation sequence of the invention. In addition, the present invention provides methods of making polypeptide conjugates as well as methods of using such conjugates and their pharmaceutical compositions. The invention further provides libraries of sequon polypeptides, wherein each member of such library includes at least one exogenous O-linked glycosylation sequence of the invention. Also provided are methods of making and using such libraries.2008-10-16
20080255041Treatment of annulus fibrosis defects - Compositions and methods for treating an annulus fibrosis defect comprising an angiogenic factor and a carrier. Methods include administering the composition to the annulus fibrosis defect, where the administering can include injecting the composition. The present compositions can stimulate angiogenesis and revascularization thereby facilitating repair of the defect.2008-10-16
20080255042CaSR Antagonist - A compound represented by the following formula (1), a pharmaceutically acceptable salt thereof or an optically active form thereof:2008-10-16
20080255043HUMAN LUNG SURFACTANT PROTEIN, SP-D, MODULATES EOSINOPHIL ACTIVATION AND SURVIVAL AND ENHANCES PHAGOCYTOSIS OF APOPTOTIC BOSINOPHILS - The present invention provides the use of formulation with surfactant protein-D (SP-D) in the modulation of activity of human eosinophils derived from hypereosinophilic patients to an increased activation state and increased apoptosis. Accordingly the utility of the invention can be extended in human subjects in resolution of eosinophilic inflammations in related diseases and disorders like neuromuscular and respiratory diseases with eosinophilia other than airway-hyperresponsiveness, allergy and asthma, hypereosinophilic leukemias, hypereosinophilc syndromes (rare hematological diseases), skin diseases like eosinophilia-Myalgia syndrome, eosinophilic fascitis, capillary leak syndromes (IL-2), Churg-Strauss syndrome, toxic oil syndrome, parasitosis, etc., where a large number of stimulated eosinophils accumulate and release a series of growth factors, cytokines, chemokines, bioactive lipid mediators, toxic oxygen metabolites.2008-10-16
20080255044Method of treatment - The present invention relates generally to a method of treatment and in particular a method of treating disorders of the nervous system such as arising from or during disease or injury. The method of the present invention involves manipulating expression of Eph receptors or their functional equivalents to increase or decrease expression or function depending on the condition being treated.2008-10-16
20080255045Modified FGF-21 Polypeptides and Their Uses - Modified FGF-21 polypeptides and uses thereof are provided.2008-10-16
20080255046Y2 Selective Receptor Agonists for Therapeutic Interventions - The modified human PP peptides (i) [Lys4,Leu17,Ser30,Gln34]hPP, (ii) Lys4,Leu17,Thr30,Gln34]hPP; and (iii) [Lys4,Leu17,oxidised Met30,Gln34]hPP wherein “oxidised Met” may be the sulfoxide or sulfone, and certain analogues and derivativatised forms thereof as referred to in the specification, are selective agonists of the Y2 receptor relative to the Y1 and Y4 receptors, and are useful for, for example, appetite control and therapeutic angiogenesis.2008-10-16
20080255047Method of Treating Acute Renal Failure with Thrombomobulin Variant - The present invention provides a method for preventing and/or treating subjects with acute renal failure caused by a variety of conditions. The method comprises administering to the subject soluble thrombomodulin. In conjunction with standard of care, soluble thrombomodulin will reduce tissue injury and subsequent morbidity and mortality.2008-10-16
20080255048Pharmaceutical Composition - The present invention provides oral pharmaceutical compositions that enable the successful delivery of drugs in a pharmaceutically effective amount, particularly poly (amino acids) such as peptides, peptidomimetics and proteins, e.g. hormones to a subject via oral administration to accomplish the desired therapeutic effect. The oral pharmaceutical composition comprising a poly (amino acid) as the active ingredient, e.g. a peptide or protein, shows a rapid disintegration and/or dissolution such that the active ingredient is able to attain a therapeutic effect.2008-10-16
20080255049COMBINED USE OF ULTRASOUND AND GROWTH FACTORS TO STIMULATE BONE FORMATION - The combination of low intensity pulsed ultrasound with administration of an osteogenic protein or proteins or their genes enhances bone repair in mammals. This combination avoids thermal activation of tissue repair mechanisms and allows the osteogenic protein or proteins or their genes to act at the site of bone fracture or lowered bone density to enhance or accelerate bone formation, thereby improving the prognosis of a patient. The combination may be used to treat fractures, to prevent or treat osteoporosis, to improve outcomes for bone replacement and to prevent or treat bone loss due to other physiologic disorders.2008-10-16
20080255050METHOD OF TREATING ATHEROSCLEROSIS - A method of treating atherosclerosis in a subject is carried out by administering the subject 2-aminopurine or a pharmaceutically salt thereof in a treatment effective amount. Optionally, the subject may also be administered an additional hypolipidemic agent. Compositions useful for carrying out the present invention are also described.2008-10-16
20080255051Novel Peptides That Promote Lipid Efflux - Disclosed herein are peptides with domains that promote lipid efflux from cells and optionally possess at least one anti-inflammatory domain or a domain that stimulates LCAT activity. Provided herein are methods of using the peptides to treat or inhibit diseases including dyslipidemic disorders, stroke and myocardial infarction. Also provided are methods of detecting plaque in vessels using the labeled peptides of the present invention.2008-10-16
20080255052Immunologic regulation by theta defensins - The invention provides a method of inhibiting undesirable microbial contamination, invasion, or growth in an individual by administering to the individual an effective amount of a theta defensin. The invention additionally provides a method of inhibiting deleterious effects resulting from microbial contamination, invasion, or growth in an individual by administering to an individual an effective amount of a theta defensin, whereby immune-mediated pathology is limited and immune function is improved.2008-10-16
20080255053METHOD FOR THE THERAPEUTIC MANAGEMENT OF ENDOMETRIOSIS - The present inventions provides a method for therapeutic management of extrauterine proliferation of endometrial tissue, chronic pelvic pain and fallopian tube obstruction by short term induction treatment with an LH-RH antagonist for 4 to 12 weeks. According to another aspect of the present invention, the short term LH-RH treatment is followed by the combined or separate administration of one or more active agents selected from the group consisting of a contraceptive, preferably an oral contraceptive, a non-steroidal anti-rheumatic agent, an analgetic, an androgen other than a 17-alpha-alkyl substituted testosterone or any combinations thereof. According to a further aspect of the present invention a pharmaceutical composition comprising an LHRH antagonist and one ore more active agents selected from the group consisting of a contraceptive, preferably an oral contraceptive, a non-steroidal anti-rheumatic agent, an analgetic, an androgen other than a 17-alpha-alkyl substituted testosterone or any combinations thereof are provided.2008-10-16
20080255054STERILE SUSPENSIONS OF SLIGHTLY SOLUBLE BASIC PEPTIDE COMPLEXES AND PHARMACEUTICAL FORMULATIONS CONTAINING THEM - The invention provides sterile suspensions and sterile lyophilizates of slightly soluble basic peptide complexes, and pharmaceutical formulations comprising them. The provided sterile suspensions, sterile lyophilizates and pharmaceutical formulations comprising them are particularly suitable for use in a parenteral dosage form as medicaments for the treatment and prophylaxis of diseases and pathological states in mammals, especially in humans.2008-10-16
20080255055Use of Derivatives of Dipeptides for the Manufacture of of a Medicament for the Treamtent of Microbial Infections - The invention relates to compositions comprising a compound based on the general formula (I) R2008-10-16
20080255056Salts of isophosphoramide mustard and analogs thereof - Disclosed herein are crystalline compounds of formula (I)2008-10-16
20080255057PRODRUG SUBSTITUTED BENZOXAZOLES AS ESTROGENIC AGENTS - This invention provides estrogen receptor modulators of formula I, having the structure2008-10-16
20080255058Composition for Oral Cavity - The present invention relates to an oral care composition, which contains a compound represented by the formula (A):2008-10-16
20080255059Regulators of the hedgehog pathway, compositions and uses related thereto - The present invention makes available, inter alia, methods and reagents for modulating smoothened-dependent pathway activation. In certain embodiments, the subject methods can be used to counteract the phenotypic effects of unwanted activation of a hedgehog pathway, such as resulting from hedgehog gain-of-function, ptc loss-of-function or smoothened gain-of-function mutations.2008-10-16
20080255060Ester Linked Macrolides Useful For The Treatment of Microbial Infections - The present invention relates to 14- or 15-membered macrolides substituted at the 4″ position of formula (I)2008-10-16
20080255061Use of Phthalide Derivatives - Disclosed a class of phthalide derivatives and the use of which to manufacture the sensitizer or reverser of the antineoplastic agent. The phthalide derivatives according to the invention can enhance the sensitivity of drug-resistance tumor cells against chemotherapy and decrease the drug-resistance of tumor cells 5-30 folder and enhance notably several chemotherapy agents-induced apoptosis of tumor cells2008-10-16
20080255062AXON REGENERATION FROM ADULT SENSORY NEURONS - A method for rapidly screening small molecules to identify small molecules that stimulate axon regeneration and outgrowth from adult sensory neurons. The method generally comprises preparing a purified individualized dorsal root ganglia cell suspension (DRG), coating well surfaces of a suitably prepared multi-well microplate with the DRG, then dispensing dosages of selected small molecules into selected wells. The microplates are incubated under sterile conditions at about 37° C. for at least 24 hours. The DRG suspension in each well is then morphometrically assessed to assess the extent of axon regeneration and outgrowth that occurred, and the effects of the selected small molecules are determined by comparison to control treatments. The method is suitable for screening chemically derived small molecules and biologically derived small molecules.2008-10-16
200802550633-B-D-RIBOFURANOSYLTHIAZOLO[4,5-d]PYRIMIDINE NUCLEOSIDES AND USES THEREOF - The invention is directed to 3-β-D-ribofuranosylthiazolo[4,5-d]pyrimidine nucleosides and pharmaceutical compositions containing such compounds that have immunomodulatory activity. The invention is also directed to the therapeutic or prophylactic use of such compounds and compositions, and to methods of treating diseases and disorders described herein, by administering effective amounts of such compounds.2008-10-16
20080255064Methods for modulating cholecystokinin expression - The invention provides a method for upregulating cholecystokinin (CCK) expression in mammalian pancreatic islets by administrating a CCK upregulating agent. The increased CCK expression activates islet cell proliferation triggering an increase in pancreatic β-cell mass and plasma insulin levels. Accordingly, methods to produce a replenishable supply of islet cells and to ameliorate the symptoms associated with diabetes are also disclosed.2008-10-16
20080255065Small Interfering Rna Molecules Against Ribonucleotide Reductase and Uses Thereof - Small interfering RNA (siRNA) molecules that target a mammalian ribonucleotide reductase gene, and which are capable of inhibiting the expression of their target gene are provided. The siRNA molecules of the invention are capable of attenuating neoplastic cell growth and/or proliferation in vitro and in vivo and, therefore, can be used to attenuate the growth and/or metastasis of various types of mammalian cancers.2008-10-16
20080255066ANTISENSE OLIGONUCLEOTIDE STRATEGIES FOR THE ENHANCEMENT OF CANCER THERAPIES - Effective combinations of antisense agents directed against thymidylate synthase mRNA are provided for use in cancer therapies. Combinations of antisense agents have enhanced activity compared to the activity of the individual antisense agents when used alone. The combinations may be used in conjunction with one or more chemotherapeutic agents to enhance the effects of the chemotherapeutic(s). Such antisense agent combinations constitute improved antisense therapies with application to a variety of cancers or proliferative disorders, including drug resistant cancers.2008-10-16
20080255067CYANOCOBALAMIN LOW VISCOSITY AQUEOUS FORMULATIONS FOR INTRANASAL DELIVERY - A stable pharmaceutical mercury-free aqueous solution of cyanocobalamin comprised of cyanocobalamin and water wherein said solution of cyanocobalamin is suitable for intranasal administration, has a viscosity less than about 1000 cPs, and wherein said solution of cyanocobalamin has a bioavailability of cyanocobalamin when administered intranasally of at least about 7% relative to an intramuscular injection of cyanocobalamin with the proviso that the solution is essentially free of mercury and mercury-containing compounds. The present invention is also directed towards a method for elevating the vitamin B12 levels in the cerebral spinal fluid (CSF) comprising administering intranasally a sufficient amount of a mercury-free cyanocobalamin solution so as to increase the average ratio of vitamin B12 in the CSF to that in the blood serum (B12 CSF/B12 Serum×100) to at least about 1.1 comprising intranasally administering an aqueous solution of a cyanocobalamin, wherein said solution of cyanocobalamin has a bioavailability of at least 7% relative to an intramuscular injection of a cyanocobalamin.2008-10-16
20080255068Chemical Compound and Its Use - The present application relates to a novel tetrahydroquinoline derivative, to a process for its preparation, to its use on its own or in combination for treating and/or preventing diseases and to its use for preparing medicaments, in particular as an inhibitor of the cholesterol ester transfer protein (CETP) for the treatment and/or prevention of cardiovascular disorders, in particular hypolipoproteinaemias, dyslipidaemias, hypertriglyceridaemias, hyperlipidaemias, hypercholesterolaemias and arteriosclerosis.2008-10-16
20080255069Medicament for Preventive and/or Therapeutic Treatment of Bowel Disease - A medicament for preventive and/or therapeutic treatment of a bowel diseases such as inflammatory bowel diseases including Crohn's disease, which comprises as an active ingredient a retinoid such as, for example, 4-[(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthalenyl)carbamoyl]benzoic acid.2008-10-16
20080255070Bisphosphonate Compounds and Methods with Enhanced Potency for Multiple Targets including FPPS, GGPPS, AND DPPS - The disclosure provides, inter alia, novel bisphosphonate compounds and methods of making and using such compounds. In certain embodiments, compounds of the invention include bisphosphonates that are capable of selectively inhibiting one or more of farnesyl diphosphate synthase (FPPS), geranylgeranyl diphosphate synthase (GGPPS), and decaprenyl pyrophosphate synthase (DPPS). In preferred embodiments, compounds of the invention are capable of selectively inhibiting two or more of FPPS, GGPPS, and DPPS. In embodiments, compounds and methods of the invention demonstrate superior activity levels, such as in the anti-cancer context, immunostimulation context, and other contexts, which in several cases exceed the activity levels of previous generation bisphosphonate drugs by orders of magnitude. In embodiments, the invention provides compounds and methods in connection with research and therapeutic applications, e.g., for tumor or cancer cell growth inhibition, activation of gammadelta T cells, inhibition of certain enzymes related to the mevalonate metabolic pathway, bone resorption diseases, cancer, immune disorders, immunotherapy, and infectious diseases.2008-10-16
20080255071Synergistic Fungicidal Active Compound Combinations - The novel active compound combinations comprising a carboxamide of the general formula (I) (group 1)2008-10-16
20080255072Composition for Inhibition of Cathepsin K - The present invention relates to the a method of inhibiting bone resorption in a mammal in need thereof with an oral pharmaceutical composition comprising a cathepsin K inhibitor, or a pharmaceutically acceptable salt thereof, or a mixture thereof, according to a continuous schedule having a dosage interval of once weekly, biweekly, twice monthly or once monthly.2008-10-16
20080255073COMPOUNDS FOR SUSTAINED RELEASE OF ORALLY DELIVERED DRUGS - Disclosed are methods for providing sustained systemic blood concentrations of orally delivered drugs. Still further, disclosed are compounds and pharmaceutical compositions that are used in such methods.2008-10-16
20080255074Drug Combination Comprising A Selective Serotonin Reuptake Inhibitor And A Glucocorticoid Receptor Antagonist For The Treatment Of Depression - The invention provides for a combination comprising an amount of an SSRI, or a pharmaceutically acceptable salt or solvate thereof, and an amount of a GR antagonist, or a pharmaceutically acceptable salt or solvate thereof, optionally in association with one or more pharmaceutically acceptable carriers for use as therapy for depression and related disorders.2008-10-16
20080255075SUBSTITUTED ESTRATRIENE DERIVATIVES AS 17BETA HSD INHIBITORS - Substituted estratriene compounds of formula (I) useful in therapy, especially in the treatment or inhibition of a steroid hormone dependent disorder requiring the inhibition of a 17β-hydroxysteroid dehydrogenase (17β-HSD) type 1, type 2 and/or type 3 enzyme, as well as their salts, pharmaceutical compositions containing such compounds and processes for preparing such compounds.2008-10-16
20080255076Steroid-Derived Pharmaceutical Compositions - The present invention relates to the use of specific steroid derivatives in the preparation of medicaments for the treatment or prevention and/or amelioration of disorders relating to pathological processes in lipid rafts.2008-10-16
20080255077Drug and Food or Drink for Improving Pancreatic Functions - Compounds such as 4-methylcholest-7-en-3-ol, 4-methylergost-7-en-3-ol and 4-methylstigmast-7-en-3-ol which have an activity for improving pancreatic function are used as an active ingredient of a pancreas function improving drug and food or drink.2008-10-16
20080255078Triphenylethylene Compounds Useful as Selective Estrogen Receptor Modulators - Triphenylethylene compounds of formula (I) are provided. The compounds are particularly useful for selective estrogen receptor modulation.2008-10-16
20080255079Therapeutic Use of Nefopam and Analogues Thereof - Nefopam or an analogue thereof is useful in the treatment of a syndrome characterized by chronic pain and fatigue.2008-10-16
20080255080Hydroquinone Ansamycin Formulations - Pharmaceutical compositions of hydroquinone geldanamycin analogs, and uses of such compositions, are provided.2008-10-16
20080255081Antioxidant and radical scavenging activity of synthetic analogs of desferrithiocin - Free radicals and reactive oxygen species have the potential to damage a wide variety of organic molecules, typically by oxidizing certain moieties. These damaging species can, for example, be produced by an organism as a by-product of cellular respiration or by the reaction of iron(II) and peroxide. The present invention includes methods of using aryl-substituted heterocyclic iron chelating compounds as antioxidants, as well as preventing the reduction of iron(III) to iron(II). In addition, the present invention provides methods of treating conditions such as inflammatory disease, neoplastic disease, and ischemic episodes.2008-10-16
20080255082Hair and/or Scalp Care Compositions Incorporating Terpenoid Compounds - The invention provides a hair and/or scalp care composition comprising a terpenoid compound of formula (I), (II) or (III) in which R2008-10-16
20080255083NEW PYRIDONE DERIVATES WITH MCH ANTAGONISTIC ACTIVITY AND MEDICAMENTS COMPRISING THESE COMPOUNDS - The present invention relates to compounds of general formula I2008-10-16
20080255084Combination of Organic Compounds - The invention relates to a combination, such as a combined preparation or a pharmaceutical composition, respectively comprising 2008-10-16
20080255085Novel Imidazo [4,5-b] Pyridine Derivatives as Inhibitors of Glycogen Synthase Kinase 3 for Use in the Treatment of Dementia and Neurodegenerative Disorders - Compounds of formula I2008-10-16
20080255086Heterocyclic Derivatives - The present invention relates to a heterocyclic derivative according to formula I2008-10-16
20080255087COMPOSITIONS AND METHODS FOR THE TREATMENT OF CANCER - The present invention relates to the use of specific compounds related to the indolocarbazole K252a, for the preparation of pharmaceutical compositions for the treatment of various forms of cancer.2008-10-16
20080255088DIBENZO[b,f][1,4]OXAZAPINE COMPOUNDS - The present invention relates to 11-(piperazin-1-yl)dibenzo[b,f][1,4]oxazapine compounds of the formula:2008-10-16
20080255089Triphenylethylene Compounds Useful as Selective Estrogen Receptor Modulators - Triphenylethylene compounds of formula (I) are provided. The compounds are particularly useful for selective estrogen receptor modulation.2008-10-16
20080255090Ceratamines A and B, and Analogues, Syntheses and Pharmaceutical Compositions Thereof - Antimitotic compounds and salts are provided in which the compound has the structure (formula (I)): wherein X and Y are substituted or unsubstituted and are selected from carbon atoms and atoms of groups 15 and 16 of the periodic table; Z is selected from N—R, O and S; U is selected from CR2008-10-16
20080255091COMPOUNDS TO TREAT AMYLOIDOSIS AND PREVENT DEATH OF BETA-CELLS IN TYPE 2 DIABETES MELLITUS - The invention discloses aromatic amides and sulfonates to treat or prevent type 2 diabetes mellitus (T2DM), the pathological consequences of T2DM, to inhibit amyloidosis or to prevent death of β-cells of the pancreas.2008-10-16
200802550926-Substituted-2,3,4,5-Tetrahydro-1H-Benzo[d]Azepines as 5-Ht2c Receptor Agonists - The present invention provides 6-substituted 2,3,4,5-tetrahydro-1H-benzo[d]azepines of Formula (I) as selective 5-HT2C receptor agonists for the treatment of 5-HT2c associated disorders including obesity, obsessive/compulsive disorder, depression, and anxiety: R6 D R?N—R″R* where R6 is —(CrC3)alkyl-S—(C0-C3)alkyl-R10, —(C1-C3)alkyl-NR11R12, —(CrC3)alkyl-O—R13. and other substituents are as defined in the specification.2008-10-16
20080255093COMPOSITIONS AND METHODS FOR TREATING OBESITY AND RELATED DISORDERS - The present invention is drawn to combinations of pharmaceutical agents having similar chemical and/or pharmacological properties, wherein the combinations maximize the therapeutic effect of the drug while minimizing their adverse effects. The methods and compositions of the invention are particularly useful in the treatment of obesity and related conditions which involves treating a subject with a sympathomimetic agent (e.g., phentermine or a phentermine-like drug) or bupropion in combination with an anti-epileptic agent (e.g., topiramate, zonisamide), CB1 antagonists (e.g., rimonabant), or a 5HT2008-10-16
20080255094THIAZOLIDINE CARBOXAMIDE DERIVATIVES AS MODULATORS OF THE PROSTAGLANDIN F RECEPTOR - The present invention is related to thiazolidine carboxamide derivatives of formula (II) for the treatment and/or prophylaxis of preterm labor, premature birth, dysmenorrhea and for stopping labor prior to cesarean delivery.2008-10-16
20080255095Benzylamine analogues - A compound of the formula (I):2008-10-16
20080255096Phantom Phenomena Treatment - The present invention relates to a substance for the treatment of the phantom phenomena of acute tinnitus and/or phantom pain, a method for the diagnosis and for the treatment of these phantom phenomena.2008-10-16
20080255097Methods for the Treatment of Substance Abuse and Dependence - The present invention relates to methods of and compositions for treating and relieving symptoms and disease associated with indications caused by a physiological drive to alleviate a sensation of anxiety. More specifically, the present invention relates to methods of and compositions for treating and relieving symptoms associated with substance abuse and withdrawal. The present invention relates to methods of and compositions for treating and relieving symptoms associated with addiction to antidepressants, opiates, nicotine or marijuana. In one method, a patient is treated with a composition that directly or indirectly modulates GABA2008-10-16
20080255098Compositions and Methods for Treatment of Psychiatric Disorders - Compositions and methods for the treatment of a unipolar depression containing betaine, and folate. Formulations for oral administration optionally also contain L-methionine.2008-10-16
20080255099Use of Diketodithiopiperazine Antibiotics for the Preparation of Antiangiogenic Pharmaceutical Compositions - The invention relates to the use of diketodithiopiperazine antibiotics, in particular chaetocin and gliotoxin, for the preparation of pharmaceutical compositions for antitumor therapy.2008-10-16
20080255100INDOLE ACETIC ACIDS EXHIBITING CRTH2 RECEPTOR ANTAGONISM AND USES THEREOF - The invention relates to indole acetic acid compounds which function as antagonists of the CRTH2 receptor. The invention also relates to the use of these compounds to inhibit the binding of prostaglandin D2008-10-16
20080255101NITRIC OXIDE DONATING DIURETIC COMPOUNDS, COMPOSITIONS AND METHODS OF USE - The invention describes novel compositions and kits comprising at least one nitric oxide enhancing diuretic compound, or pharmaceutically acceptable salts 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 conditions resulting from excessive water and/or electrolyte retention; (b) treating cardiovascular diseases; (c) treating renovascular diseases; (d) treating diabetes; (e) treating diseases resulting from oxidative stress; (f) treating endothelial dysfunctions; (g) treating diseases caused by endothelial dysfunctions; (h) treating cirrhosis; (j) treating pre-eclampsia; (k) treating osteoporosis; (l) treating nephropathy; (m) treating peripheral vascular diseases; (n) treating portal hypertension; (o) treating central nervous system disorders; (p) treating metabolic syndrome; (q) treating sexual dysfunctions; and (r) hyperlipidemia. The nitric oxide enhancing diuretic compounds comprise at least one nitric oxide enhancing group linked to the diuretic compound through one or more sites such as carbon, oxygen and/or nitrogen via a bond or moiety that cannot be hydrolyzed.2008-10-16
20080255102Phenylaminopropanol Derivatives and Methods of Their Use - The present invention is directed to phenylaminopropanol derivatives of formula I:2008-10-16
20080255103Antihistamine and anti-nausea pharmaceutical compositions for topical application - A topical pharmaceutical preparation suitable for use as an antihistamine or anti-nausea drug comprises an emu oil gel base and a therapeutic amount of promethazine.HCl. The preparation may further comprise an antioxidant. The preparation is preferably packaged as a single unit dose. A method for preparing the topical pharmaceutical preparation comprises the steps of combining a clear gel with an emu oil mixture and adding a therapeutic amount of promethazine.HCl solution.2008-10-16
20080255104Nsaid Compositions - The invention is directed to a composition and method for treating acute pain using a composition comprising one or more NSAID's, a metasilicate and optionally a fatty acid ester resulting in increased absorption of poorly soluble active NSAID's and increased absorption in suppressed vagal systems. The preferred composition comprises meloxicam on a metasilicate matrix; and one or more of the following: sodium bicarbonate, Gelucire®, and tartaric acid.2008-10-16
20080255105Biphenyl Derivatives and Their Use in Treating Hepatitis C - A compound which is a biphenyl derivative of formula (I), or a pharmaceutically acceptable salt thereof wherein: R2008-10-16
20080255106Novel 2-Phenyl-Imidazo[4,5-B]Pyridine Derivatives as Inhibitors of Glycogen Synthase Kinase for the Treatment of Dementia and Neurodegenerative Disorders - Compounds of formula I2008-10-16
20080255107Fungicidal Mixtures Comprising N-[2-(Haloalk(Enyl)Oxy)Phenyl]Carboxamides - Fungicidal mixtures comprising, as active components, 2008-10-16
20080255108NOVEL THIOPHENE SULFOXIMINES, COMPOSITIONS THEREOF, AND METHODS OF TREATING COMPLEMENT-MEDIATED DISEASES AND CONDITIONS - Disclosed are compounds for treating the symptoms of an acute or chronic disorder mediated by the classical pathway of the complement cascade. Said compounds are of Formula I2008-10-16
20080255109Non-peptide GnRH antagonists - Compounds according to general formula 1, wherein A2008-10-16
20080255110IMIDAZOQUINOLINE DERIVATIVES AS ADENOSINE A3 RECEPTOR LIGANDS - This invention is directed to a compound of formula (I),2008-10-16
20080255111Tissue Factor Production Inhibitor - A medicament which has an activity of inhibiting production of tissue factor and comprises an LXR ligand as an active ingredient; and a medicament for treatment and/or prophylaxis of vascular restenosis following angioplasty, endarterectomy, percutaneous transluminal coronary angioplasty (PTCA) or stent implantation, or treatment and/or prophylaxis of blood coagulation diseases, diseases induced by platelet aggregation including stable or unstable angina pectoris, cardiovascular and cerebrovascular diseases including thromboembolism formation diseases accompanying diabetes, rethrombosis following thrombolysis, cerebral ischemic attack, infarction, stroke, ischemia-derived dementia, peripheral artery disease, thromboembolism formation diseases during use of an aorta-coronary artery bypass, glomerulosclerosis, renal embolism, tumor or cancer metastasis, which comprises an LXR ligand as an active ingredient.2008-10-16
20080255112Pyrimidine-Substituted Benzimidazole Derivatives 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 Alk, Abl, BRK, Blk, BMX, CSK, c-Src, c-Raf, EGFR, Fes, FGFR3, Fms, Fyn, IGF-IR, IR, IKKα, IKKβ, JAK2, JAK3, KDR, Lck, Met, p70S6k, Ros, Rsk1, SAPK2α, SAPK2β, SAPK3, SIK, Tie2, TrkB and/or WNK3 kinases.2008-10-16
20080255113Quinolonecarboxylic Acid Compounds Having 5-Ht4 Receptor Agonistic Activity - This invention provides a compound of the formula (I): wherein Het represents a heterocyclic group having one nitrogen atom, to which B binds directly, and from 4 to 7 carbon atoms, and said heterocyclic group being unsubstituted or substituted by 1 to 4 substituents independently selected from the group consisting of substituents α2008-10-16
200802551142-AMINOBENZOXAZOLE CARBOXAMIDES AS 5HT3 MODULATORS - Compounds of formulae I, II and III:2008-10-16
20080255115THIAZOLIDINEDIONE DERIVATIVES AS PI3 KINASE INHIBITORS - Invented is a method of inhibiting the activity/function of PI3 kinases using thiazolidinedione 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 thiazolidinedione derivatives.2008-10-16
20080255116Quinoline Derivatives as Antibacterial Agents - Use of a compound for the manufacture of a medicament for the treatment of a bacterial infection provided that the bacterial infection is other than a Mycobacterial infection, said compound being a compound of Formula (Ia) or (Ib)2008-10-16
20080255117SULFONYLTRYPTOPHANOLS - The present invention relates to sulfonyltryptophanols of the general formula I,2008-10-16
20080255118Cyanopyrimidinones - The invention relates to novel cyanopyrimidinones, process for their preparation, and the use thereof for producing medicaments for improving perception, concentration, learning and/or memory.2008-10-16
20080255119DIPHENYL-DIHYDRO-IMIDAZOPYRIDINONES2008-10-16
20080255120SUBSTITUTED 2,5-HETEROCYCLIC DERIVATIVES - The present invention relates to new substituted five-membered compounds and pharmaceutically acceptable salts, esters or prodrugs thereof, compositions of the new compounds together with pharmaceutically acceptable carriers, and uses of the new compounds. The compounds of the invention have the following general formula:2008-10-16
20080255121Combination Drug for Treating Autoimmune Disease - It is intended to provide a combination drug for preventing and/or treating an autoimmune disease. More specifically speaking, a combination drug for preventing and/or treating an autoimmune disease which contains a CaMKII inhibitor and a disease-modifying antirheumatic drug; a medicinal composition, a commercial package, a kit, etc. for the combination; an enhancer for the effect of preventing and/or treating an autoimmune disease of a disease-modifying antirheumatic drug which contains a CaMKII inhibitor as the active ingredient; a method of screening a CaMKII inhibitor appropriately usable in combination, and so on.2008-10-16
20080255122Derivatives of Isothiazol-3(2H)-One 1,1-Dioxides as Liver X Receptor Modulators - The present invention relates to certain novel compounds of the formula (I) to processes for preparing such compounds, to their the utility in modulation of nuclear hormone receptors Liver X Receptor (LXR) α (NR1H3) and/or β (NR1H2) and in treating and/or preventing clinical conditions including cardiovascular diseases such as atherosclerosis; inflammatory diseases, Alzheimer's disease, lipid disorders (dyslipidemias) whether or not associated with insulin resistance, type 2 diabetes and other manifestations of the metabolic syndrome, to methods for their therapeutic use and to pharmaceutical compositions containing them.2008-10-16
20080255123NOVEL COMPOUNDS AS CANNABINOID RECEPTOR LIGANDS - The present invention relates to compounds of formula (I)2008-10-16
20080255124Chemical Compounds - This invention relates to non-steroidal compounds that are modulators of androgen, glucocorticoid, mineralocorticoid, and progesterone receptors, and also to the methods for the making and use of such compounds.2008-10-16
20080255125Topically Applied Medicament for Animals - The invention relates to pharmaceutical preparations, which are applied to the pelt or skin of animals and are then absorbed by the latter orally.2008-10-16
20080255126Inhibitors of post-proline cleaving proteases - Novel compounds that are inhibitors of one or most post-proline cleaving proteases, e.g. dipeptidyl peptidase IV, according to general formula (1). R2008-10-16
20080255127Pesticide Formulations with a Crystallization Risk, and a Method for Their Preparation - Pesticide formulations with a crystallization risk are provided. Also provided are methods of making and using such formulations.2008-10-16
20080255128PHTHALAZINONE DERIVATIVES - A compound of the formula (I):2008-10-16
200802551293-Heteroaryl-3,5-dihydro-4-oxo-4H-pyridazino[4,5-b]indole-1-acetamide derivatives, their preparation and their application in therapeutics - The invention discloses and claims therapeutic uses of compounds of general formula (I)2008-10-16
20080255130Bicyclic Nitrogen-containing Heterocyclic compounds for use as Stearoyl CoA Desaturase inhibitors - The present invention discloses bicyclic nitrogen-containing heterocyclic compounds for use as inhibitors of stearoyl-CoA desaturase. The compounds are useful in treating and/or preventing various human diseases, mediated by stearoyl-CoA desaturase (SCD) enzymes, especially diseases related to abnormal lipid levels, cardiovascular disease, diabetes, obesity, oily skin conditions, metabolic syndrome, and the like.2008-10-16
20080255131N-(HETEROARYL)-1H-INDOLE-2-CARBOXAMIDE DERIVATIVES AND THEIR USE AS VANILLOID TRPV1 RECEPTOR LIGANDS - The invention concerns therapeutic uses of compounds of general formula (I), wherein n, X2008-10-16
20080255132Combination Therapy Comprising the Use of Et-743 and Paclitaxel for Treating Cancer - Methods of treating a human body for cancer are provided. In one aspect, an effective therapeutic amount of paclitaxel is administered in combination with ET-743 in a dose range between 0.5 and 1 mg/m2008-10-16
20080255133Inhibitors of MEK - This invention concerns to N-(2-aylamino)aryl sulfonamides, which are inhibitors of MEK, methods of using such compounds in the treatment of hyperproliferative diseases, and to pharmaceutical compositions containing such compounds.2008-10-16
20080255134Cardiotonic Compounds With Inhibitory Activity Against Beta-Adrenergic Receptors And Phosphodiesterase - The present invention provides compounds of formula (I) possessing inhibitory activity against β adrenergic receptors and phosphodiesterase (PDE), including type 3 phosphodiesterase (PDE-3). The present invention further provides pharmaceutical compositions comprising such compounds, methods of preparing such compounds, and methods of using such compounds for regulating calcium homeostasis, for treating a disease, disorder or condition in which disregulation of calcium homeostasis is implicated and for treating cardiovascular disease, stroke, epilepsy, an ophthalmic disorder or migraine.2008-10-16
20080255135Novel 1-Aza-Bicycloalkyl Derivatives - The present invention provides a compound of formula (I)2008-10-16
20080255136PYRROLIDONES WITH ANTI-HIV ACTIVITY - The present invention relates to inhibition of viruses, e.g., HIV using pyrrolidones and compounds related to pyrrolidones. The invention further relates to methods for identifying and using agents, including small molecule chemical compositions that inhibit HIV in a cell; as well as to methods of prophylaxis, and therapy related to HIV infection and related disease states such as AIDS.2008-10-16
20080255137N-Biaryl and N-Arylheteroaryl 2-Substituted Piperazine Derivatives as Modulators of the 5ht2c Receptor Useful for the Treatment of Disorders Related Thereto - The present invention relates to certain N-biaryl and N-arylheteroaryl 2-substituted piperazine derivatives of Formula (Ia) that are modulators of the 5HT2C receptor. Accordingly, compounds of the present invention are useful for the treatment of 5HT2C receptor associated diseases or disorders, such as, obesity, Alzheimer Disease, erectile dysfunction and related disorders.2008-10-16