Abstract: Included in the present invention are methods of inhibiting sperm capacitation, inhibiting the phosphorylation of a protein at tyrosine residues, inhibiting an acrosomal reaction, and inhibiting fertilization of an egg by sperm with the administration of a CRISP polypeptide.

Abstract: The present invention is directed to a pharmaceutical composition comprising 0.5 ng to 20 ?g desmopressin and a pharmaceutically acceptable carrier. The present invention is also directed to a pharmaceutical composition comprising desmopressin and a pharmaceutically acceptable carrier, wherein the pharmaceutical composition is effective to establish a steady plasma/serum desmopressin concentration in the range of from about 0.1 picograms desmopressin per mL plasma/serum to about 10.0 picogram desmopressin per mL plasma/serum. Articles of manufacture and methods of using the above invention are also disclosed.

Abstract: Disclosed are compounds, compositions and methods for treating viral infections caused by a Flaviviridae family virus, such as hepatitis C virus.

Abstract: Compounds and methods for modulating cell proliferation, preferably inhibiting the proliferation of tumor cells are described. Compounds that may be used to modulate cell proliferation include antisense oligonucleotides complementary to regions of the mammalian ribonucleotide reductase genes.

Abstract: There are provided compounds of formula (I) wherein R1 represents O, S or NH; R2 represents —C(?O)-aryl or —C(?O)-heteroaryl; R3 represents hydrogen, methyl (which may be in either the ? or ? configuration) or methylene; R4 and R5 are the same or different and each represents hydrogen or halogen; and represents a single or a double bond; and salts and solvates thereof; process for preparing them, compositions containing them and their use in therapy.

Abstract: This invention relates to a sealed container containing a powder formulation comprising a dehydroepiandrosterone, its analogue(s) or salt(s) by itself or with a pharmaceutically or veterinarily acceptable carrier or diluent, and having a particle size of about 0.1 ?m to about 100 ?m. The formulation can be used to treat or prevent asthma, chronic obstructive pulmonary disease, lung inflammation, and other respiratory diseases or conditions. The formulation may be prepared by jet milling, and may be delivered through the respiratory tract or other routes using a nebulizer. The sealed container is provided in a device and/or a therapeutic kit.

Abstract: The invention relates to benzoquinone ansamycin analogs useful for the treatment of cancer and other diseases or conditions characterized by undesired cellular proliferation or hyperproliferation. Therapies involving the administration of such benzoquinone ansamycin analogs, optionally in combination with an inhibitor of an HSP90 client protein, are useful to treat cancer and non-cancerous disease conditions.

Abstract: The present invention provides 4-amino-azepan-3-one protease inhibitors and pharmaceutically acceptable salts, hydrates and solvates thereof which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, novel intermediates of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia of malignancy; and metabolic bone disease, comprising inhibiting said bone loss or excessive cartilage or matrix degradation by administering to a patient in need thereof a compound of the present invention.

Abstract: Compounds represented by Formula (I): or pharmaceutically acceptable salts thereof, are inhibitors of glycogen phosphorylase and are useful in the prophylactic or therapeutic treatment of diabetes, hyperglycemia, hypercholesterolemia, hyperinsulinemia, hyperlipidemia, hypertension, atherosclerosis or tissue ischemia e.g. myocardial ischemia, and as cardioprotectants.

Abstract: Morpholino-substituted pyridopyrimidine, quinolone, and benzopyranone derivatives inhibit phosphoinositide (PI) 3-kinase, an enzyme that regulates platelet-adhesion processes. As a consequence, the compounds in question have anti-thrombotic activity, as well as other pharmaceutical properties. The compounds claimed are represented by formula (I), (II) and (III). PI 3-kinase generates 3-phosphorylated PI second messengers which stimulate platelet adhesion under blood-flow conditions. Because platelet adhesion is a necessary step in the formation of a thrombus, inhibition by these compounds of PI 3-kinase under such conditions inhibits or prevents thrombus formation.

Abstract: Compounds which mimic the secondary structure of helical regions of biologically active peptides and proteins having the following structure: including pharmaceutically acceptable salts and stereoisomers thereof, wherein Y, A, B, R1 and R2 are as defined herein. Such compounds have utility over a wide range of applications, including use as diagnostic and therapeutic agents. In particular, compounds of this invention, and pharmaceutical compositions containing the same, are neurokinin (tachykinin) antagonists. Libraries containing the compounds of this invention are also disclosed, as well as methods for screening such libraries to identify biologically active members.

Abstract: The invention relates to at least one pyrrolotriazine derivative, at least one pharmaceutical composition comprising at least one pyrrolotriazine derivative, and at least one method of using at least one pyrrolotriazine derivative to treat at least one kinase associated condition.

Abstract: The present invention relates to nucleoside derivatives represented by general formulas I and II, their synthetic methods and their pharmacologically acceptable salts thereof, and compositions containing such compounds. Methods for treating hyperproliferative disorders by administering the compounds are also included.

Abstract: 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 D2 and its metabolites or certain thromboxane metabolites to the CRTH2 receptor and to treat disorders responsive to such inhibition.

Abstract: The invention relates to a stable polymorphic form of the compound 7-[4-([1,1?-biphenyl]-3-ylmethyl)-1-piperazinyl]-2(3H)-benzoxazolone monomethanesulfonate (INNM bifeprunox mesylate), a method for the preparation of said polymorphic form and its use in pharmaceutical products, especially in pharmaceutical products for the treatment of psychotic disorders and Parkinson's disease.

Abstract: This invention relates to N-aroyl cyclic amino derivatives and their use as pharmaceuticals.

Abstract: The present invention relates to compounds of the formula 1 and to pharmaceutically acceptable salts, prodrugs and solvates thereof, wherein X1, R1, R2 and R3 are as defined herein. The invention also relates to pharmaceutical compositions containing the above compounds and to methods treating hyperproliferative disorders in mammals by administering the above compounds.

Abstract: The use of a compound of formula (I): wherein R1 is selected from H, alkyl, aryl, alkoxy, aryloxy, alkylthio, arylthio, halogen, CN, NR5R6, NR4COR5, NR4CONR5R6, NR4CO2R7 and NR4SO2R7; R2 is selected from aryl attached via an unsaturated carbon; R3 is selected from H, alkyl, COR5, CO2R7, CONR5R6, CONR4NR5R6 and SO2R7; R4, R5 and R6 are independently selected from H, alkyl and aryl or where R5 and R6 are in an NR5R6 group, R5 and R6 may be linked to form a heterocyclic group, or where R4, R5 and R6 are in a (CONR4NR5R6) group, R4 and R5 may be linked to form a heterocyclic group; and R7 is selected from alkyl and aryl, or a pharmaceutically acceptable salt thereof or prodrug thereof, in the treatment or prevention of a disorder in which the blocking of purine receptors, particularly adenosine receptors and more particularly A2A receptors, may be beneficial, particularly wherein said disorder is a movement disorder such as Parkinson's disease or said disorder is depression, cognitive or memory impairment,

Abstract: Novel pyrazolopyrimidines of formula (I): are discussed. These pyrazolopyrimidines are capable of inhibiting the activity of cyclin-dependent kinases, most particularly cyclin-dependent kinase 1 (Cdk1), cyclin-dependent kinase 2 (Cdk2), and cyclin-dependent kinase 4 (Cdk4) and are thus useful, inter alia, in the treatment or control of cancer, in particular solid tumors. This invention also provides pharmaceutical compositions containing such compounds and to methods of treating or controlling cancer, most particularly the treatment or control of breast, lung, colon and prostate tumors.

Abstract: 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, 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.

Abstract: Disclosed are methods and compositions for treatment of male sexual dysfunction. A method of treating male sexual dysfunction includes administering a pharmaceutical composition effective to cause said male to sustain an erection. The composition is formulated based on diagnostic assessment and an individualized formulation test step. Also within the invention is a method of treating male sexual dysfunction in a population of subjects. The invention further provides kits for treatment of male erectile dysfunction.

Abstract: A method of treating and/or preventing allergic and inflammatory conditions of the skin or upper and lower airway passages, e.g. seasonal allergic rhinitis, perennial allergic rhinitis, or chronic idopathic urticaria, in a human more 12 years old, by administering an amount of desloratadine, e.g. 2×2.5 mg or 5 mg/day for a time sufficient to produce a geometric mean steady state maximum plasma concentration of desloratadine in the range of about 2.90 ng/mL to about 4.54 ng/mL, or a arithmetic mean steady state maximum plasma concentration of desloratadine in the range of about 3.2 ng/mL to about 5.0 ng/mL is disclosed.

Abstract: Xanthenecarboxylates of formula 1 wherein: A is a group selected from X? is an anion with a single negative charge; R is hydroxy, methyl, hydroxymethyl, ethyl, —CF3, —CHF2, or fluorine; R1 and R2, which are identical or different, are each C1-C5-alkyl which is optionally substituted by C3-C6-cycloalkyl, hydroxy, or halogen, or R1 and R2 together denote a —C3-C5-alkylene-bridge; and R3, R4, R3?, and R4?, which are identical or different, are each hydrogen, —C1-C4-alkyl, —C4-alkyloxy, hydroxy, —CF3, —CHF2, —CN, —NO2, or halogen, or a physiologically acceptable salt thereof, processes for preparing, them and their use in pharmaceutical compositions.

Abstract: Disclosed are compounds of formula (I): wherein R1 and R2 are defined herein, which are useful as inhibitors of the kinase activity of the I?B kinase (IKK) complex. The compounds are therefore useful in the treatment of IKK mediated diseases including autoimmune diseases inflammatory diseases and cancer. Also disclosed are pharmaceutical compositions comprising these compounds and processes for preparing these compounds.

Abstract: The present invention relates to novel cycloalkyl-hydroxyl compounds, compositions comprising hydroxyl compounds, and methods useful for treating and preventing a variety of diseases and conditions such as, but not limited to aging, Alzheimer's Disease, cancer, cardiovascular disease, diabetic nephropathy, diabetic retinopathy, a disorder of glucose metabolism, dyslipidemia, dyslipoproteinemia, hypertension, impotence, inflammation, insulin resistance, lipid elimination in bile, obesity, oxysterol elimination in bile, pancreatitis, Parkinson's disease, a peroxisome proliferator activated receptor-associated disorder, phospholipid elimination in bile, renal disease, septicemia, Syndrome X, thrombotic disorder. Compounds and methods of the invention can also be used to modulate C reactive protein or enhance bile production in a patient.

Abstract: Methods of treating ovarian cancer, endometrium cancer, cervical cancer, pancreatic cancer, bladder cancer, eve cancer, central nervous system cancer, thyroid cancer and lung cancer are disclosed. Specifically disclosed are methods of treating ovarian adenocarcinoma that has migrated into the abdominal cavity, a transitional cell carcinoma of the bladder, an epithelioid carcinoma in a pancreatic duct, an adenocarcinoma in a pancreatic duct, an adenocarcinoma in the cervical epithelium. The methods comprise administering to a patient a therapeutically effective amount of a compound of formula (Ia) wherein R1, R2, R3, R4, and R5 are described herein, wherein at least two of the five R1, R2, R3, R4, and R5 substituents are always hydrogen, at least one of the five substituents is always nitro, and at least one substituent positioned adjacent to a nitro is always iodo, and pharmaceutically acceptable salts thereof.

Abstract: The present invention provides agents having high antimicrobial activity for preventing and treating infectious diseases. Thus, the present invention provides novel cyano-(substituted)-methylenepiperidinophenyl oxazolidinone derivatives, processes for making the compounds, as well as antimicrobial compositions containing said derivatives as active ingredients and methods of treating bacterial infections with the said derivatives.

Abstract: This invention relates to a class of compounds having the general formula (I) which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.

Abstract: 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: wherein R1, R2, R3 and R4 are as defined herein.

Abstract: The present invention provides the compounds of formula I their pharmaceutically acceptable salts or esters, enantiomeric forms, diastereoisomers and racemates, the preparation of the above-mentioned compounds, pharmaceutical compositions containing them and their manufacture, as well as the use of the above-mentioned compounds in the control or prevention of illnesses such as cancer.

Abstract: A compound of formula 1 wherein the groups R1, R2, R3, R4 and n may have the meanings given in the claims and in the specification, and methods for preparing a pharmaceutical composition for the treatment of inflammatory and obstructive respiratory complaints.

Abstract: The invention encompasses ureido substituted benzoic acid compounds, compositions comprising the compounds and methods for treating or preventing diseases associated with nonsense mutations of mRNA by administering these compounds or compositions.

Abstract: The invention provides compounds according to formula I wherein the substitutents are as described herein. Further provided are methods of using such compounds for the treatment of nuclear hormone receptor-associated conditions, such as age related diseases, for example sarcopenia. Also provided are pharmaceutical compositions containing such compounds and processes for preparing some of the compounds of the invention.

Abstract: Substituted benzoimidazole compounds useful as anti-infectives that decrease resistance, virulence, or growth of microbes are provided. Methods of making and using substituted benzoimidazole compounds, as well as pharmaceutical preparations thereof, in, e.g., reducing antibiotic resistance and inhibiting biofilms.

Abstract: This invention is directed to compounds of the formula (I): wherein one of R6, R7, R8 and R9 is and X, R1 to R12, m, n and o are as defined in the description, and pharmaceutically acceptable salts and/or esters thereof. The invention is also directed to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are modulated by PPAR? and/or PPAR? agonists.

Abstract: Novel isoindoline compounds are disclosed. Methods of treating, preventing and/or managing cancer, diseases and disorders associated with, or characterized by, undesired angiogenesis, and diseases and disorders mediated by PDE 4, using the compounds are also disclosed.

Abstract: Drugs intended for absorption in the stomach or upper intestinal tract are administered in oral drug delivery systems in conjunction with any of various substances that have been discovered to function as potent agents for inducing the fed mode. By inducing the onset of the fed mode, these agents cause the stomach to prolong its retention of the drug delivery system, which is either large enough to be retained in the stomach during the fed mode or swells or expands to such a size upon ingestion. The fed mode inducing agents include the following compounds and their salts: glycine and glycylglycine, xylitol and related sugar alcohols, sodium and other metal docusates, ?-casomorphins, ?-lipoic acid and similarly structured acids, 2,2-diaryl-4-(4?-aryl-4?-hydroxypipendino)butyramides, arginine, Trp-Trp, alkylpyridinium halides, dihydroxybenzoic acids, and potent sweeteners such as aspartame, aspartic acid, acesulfame, and stevioside.

Abstract: The invention relates to acylhydrazone derivatives of formula (I), which are SGK inhibitors and can be used for the treatment of diseases and afflictions associated with SGK, such as diabetes, obesity, metabolic syndrome (dyslipidaemia), systematic and pulmonary hypertension, cardiovascular diseases and kidney diseases and in general for all types of fibroses and inflammatory processes. In said formula: R1 and R5 independently of one another represent H, OH, OA, OAc or methyl; R2, R3, R4, R6, R7, R8, R9 and R10 independently of one another represent H, OH, OA, OAc, OCF3, Hal, NO2, CF3, A, CN, OSO2CH3, SO2CH3, NH2, or COOH; R11 represents H or CH3; A represents an alkyl comprising 1, 2, 3, or 4 C atoms; X represents CH2, CH2CH2, OCH2 or —CH(OH)— and Hal represents F, Cl, Br or I.

Abstract: The compounds disclosed herein are useful for treating glaucoma, ocular hypertension, and baldness.

Abstract: A medicinal composition and method to treat or minimize post-ischemic brain cell deterioration that comprises nitrous oxide or a nitrous oxide donor and xenon or a xenon donor. The medicinal composition may be administered prior to or subsequent to a stroke.

Abstract: An aerosol composition which is prepared from a biliquid foam, an aqueous phase and a propellant, and wherein an oil soluble functional material is incorporated into the biliquid foam during preparation to enable this material to be more readily incorporated into the composition. The aerosol composition can be contained in a pressurized aerosol can and can be a polish, an air freshener, a repellant. a pre- or post-shave preparation, a shaving preparation or a follicle softener.

Abstract: The invention relates to a process for producing a hydrogen-rich stream from a hydrogen-depleted stream. More particularly, the invention relates to a hydrocarbon synthesis process, by way of example, a Fischer Tropsch process, from which both hydrocarbons and high purity hydrogen are obtained. The process comprises contacting the hydrogen-depleted stream with a first reverse-selective membrane and a second reverse-selective membrane to provide a CO2-enriched permeate and a hydrogen-containing retentate. The high purity hydrogen is produced from the hydrogen-containing retentate. The high purity hydrogen thus obtained may be used in a process selected from the group consisting of upgrading hydrocarbons produced from the hydrocarbon synthesis process, hydrotreating a natural gas stream, recycling to the hydrocarbon synthesis reaction unit, high purity hydrogen production, catalyst rejuvenation, and combinations thereof.

Abstract: A solvent-free resin composition comprising (a) a polyimide silicone resin having repeating units represented by the following general formulas (1-1) and (1-2), wherein X is a tetravalent organic group, Y is a divalent organic group, and Z is a divalent organic group having an organosiloxane moiety, (b) a reactive diluent, and (c) a photo-polymerization initiator, characterized in that a film of said resin composition with a film thickness of 100 ?m prepared on a quartz glass substrate shows a light transmittance of 80% or higher at wavelengths of from 350 nm to 450 nm.

Abstract: To provide an aqueous ink composition which, without impairing ejection stability, is excellent in light-fastness and water-fastness, does not cause cohesion differential, gloss differential, bronzing phenomenon, color-bleeding, and the like, and has improved fixing ability and coloring property. An aqueous ink composition comprising at least water, a pigment dispersed by polymer, a sulfonyl group-containing (co)polymer, and an ultra-penetrating agent.

Abstract: A cure system including a compatiblized and passivated refectory solid dispersed within a low temperature liquid curing agent is provided. An adhesive system including the cure system is provided, and an associated method. A device including the cured adhesive system is provided.

Abstract: A reworkable conductive adhesive composition, comprising an epoxy based conductive adhesive containing conductive metal filler particles dispersed in a solvent-free hybrid epoxy polymer matrix.

Abstract: The object of the present invention is to provide board-like molded elements that can be produced in a simple manner, at low cost, and that will be more flexible and possess a more precise standard of quality than can be achieved with conventional methods, and a method for producing said elements. In order to attain this object, a method for producing board-like molded elements made from natural fibers is proposed pursuant to the invention, wherein natural fibers are mixed with bonding agents, the mixture is placed on a molding platform where it may be shaped, after which the elements are bonded, characterized in that the bonding agent is admixed in the form of material elements that at least partially form bonding agents following an activation.

Abstract: A high flow polyester composition is disclosed, which comprises at least one polyester, at least one flow enhancing ingredient of structure (III), wherein R3 is a C1-C20 alkyl group optionally having one or more hydroxy group substituents, a C3-C20 cycloalkyl group, a C6-C20 aryl group, a C1-C20 alkoxy group optionally having one or more hydroxy group substituents, or a C6-C20 aryloxy group; and an aromatic epoxy compound, in an amount sufficient to provide 5 to 300 milliequivalents of epoxy per kilogram of polyester. The composition further optionally comprises reinforcing fillers, impact modifiers, a property-enhancing thermoplastic such as polycarbonate and flame retardant chemicals. The compositions are suitable for making automotive, electric and electronic parts.

Abstract: A high flow polyester composition is disclosed, which comprises at least one polyester, at least one flow enhancing ingredient of structure (III), wherein R3 is a C1-C20 alkyl group optionally having one or more hydroxy group substituents, a C3-C20 cycloalkyl group, a C6-C20 aryl group, a C1-C20 alkoxy group optionally having one or more hydroxy group substituents, or a C6-C20 aryloxy group; and a dicycloaliphatic diepoxy compound, in an amount sufficient to provide 5 to 300 milliequivalents of epoxy per kilogram of polyester. The composition further optionally comprises reinforcing fillers, impact modifiers, a property-enhancing thermoplastic such as polycarbonate and flame retardant chemicals. The compositions are suitable for making automotive, electric and electronic parts.

Abstract: This invention relates to a flame retardant composition comprising: (a) 81 to 99.99 weight percent of a thermoplastic resin, thermoset resin, thermoplastic resin blend, or thermoset resin blend which upon burning forms a char and (b) 0.01-19 weight percent of a silsesquioxane resin having a weight average molecular weight of greater than 300.