Abstract: The present invention relates to bicyclic himbacine derivatives of the formula or a pharmaceutically acceptable salt thereof wherein: R1 is W is and the remaining variables are described herein. The compounds of the invention are effective inhibitors of the PAR-1 receptor. The inventive compounds may be used for the treatment or prophylaxis of disease states such as ASC, secondary prevention of myocardial infarction or stroke, or PAD.

Abstract: A pro-apoptotic solid dispersion comprises, in essentially non-crystalline form, a Bcl-2 family protein inhibitory compound of Formula I as defined herein, dispersed in a solid matrix that comprises (a) a pharmaceutically acceptable water-soluble polymeric carrier and (b) a pharmaceutically acceptable surfactant. A process for preparing such a solid dispersion comprises dissolving the compound, the polymeric carrier and the surfactant in a suitable solvent, and removing the solvent to provide a solid matrix comprising the polymeric carrier and the surfactant and having the compound dispersed in essentially non-crystalline form therein. The solid dispersion is suitable for oral administration to a subject in need thereof for treatment of a disease characterized by overexpression of one or more anti-apoptotic Bcl-2 family proteins, for example cancer.

Abstract: A topical pharmaceutical or cosmetic composition for treatment of irritation of mucous cells such as mucosal cells of the eye, nose, and vagina is disclosed. The composition comprises an aqueous solution of at least one polyol selected from the group consisting of xylitol, myoinositol and mannitol and at least one substance selected from the group consisting of glycerol and urea. The composition contains less than 0.01% inorganic salt and is free of any oil-in-water or wax-in-water emulsion. In particularly preferred embodiments, the composition comprises an aqueous solution containing 1.5-5% (w/v) xylitol and 0.9-2.0% (w/v) glycerol.

Abstract: An agent enhances the therapeutic or prophylactic effect of a renin-angiotensin system inhibitor on renal diseases, including a specific prostaglandin I derivative such as beraprost sodium as an effective ingredient.

Abstract: A stable pharmaceutical composition consisting of (a) benazepril, in free or pharmaceutically acceptable salt form; and (b) amlodipine, in free or pharmaceutically acceptable salt form. The composition is free of alkali and alkaline earth metal carbonates and phosphates. The composition is also free of excipients which increase the pH of microenvironment above 5. It is therefore not required to physically separate the two drugs from each other.

Abstract: The invention relates to pyrazolyl substituted tetrahydropyranylsulfones as voltage gated calcium channel blockers, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.

Abstract: The present invention relates to novel heterocyclic compounds which are useful for inhibiting glycogen synthase kinase 3 (GSK-3), methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.

Abstract: The present invention provides a compound of formula I: a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.

Abstract: The present invention provides a composition for preventing or treating kidney disease, the composition comprising a pyrazole derivative compound or a pharmaceutically acceptable salt thereof; and the composition of the present invention is effective in reducing proteinuria, reducing cell formation between glomerular blood vessels and suppressing kidney fibrosis.

Abstract: The present invention relates to A method for promoting the differentiation of myoblasts comprising treating myoblasts with butylpyridinium, a derivative thereof, or a pharmaceutically acceptable salt thereof; a method for strengthening muscles comprising administering butylpyridinium, a derivative thereof, or a pharmaceutically acceptable salt thereof to a subject in need thereof; a feed or feed additive for strengthening muscles comprising butylpyridinium, a derivative thereof, or a pharmaceutically acceptable salt thereof; a method for treating a disease associated with muscle weakness comprising administering butylpyridinium, a derivative thereof, or a pharmaceutically acceptable salt thereof to a subject in need thereof.

Abstract: The present invention provides methods and compositions for reducing pigmentation.

Abstract: The present invention provides a foamable composition comprising water and an organic solvent, wherein the organic solvent comprises a fatty acid. The composition may further comprise a pharmaceutically active agent. The composition of the invention is also useful for the treatment of a dermatological disorder in a mammal by the topical administration of the composition.

Abstract: Disclosed are methods for treating a subject suffering from phenylketonuria and/or phenylalanemia. The methods include, in part, enterally administering to the subject a LNAA supplement in which the weight ratio of Leu to Val is greater than 2:1; in which the weight ratio of Leu to iLeu is greater than 3:1; or which includes one or more LNAAs and which further includes Lys. LNAA supplements are also disclosed. Also disclosed are methods for treating a subject suffering from a condition involving a metabolic disorder involving the metabolism of a first amino acid X. The method includes enterally administering to the subject a composition which (i) is substantially free from the first amino acid X and (ii) which includes a second amino acid Y that competes with amino acid X at a gastrointestinal tract transporter.

Abstract: The present invention provides, inter alia, methods for treating or ameliorating the effects of a glioma. Methods of this invention include administering to a subject in need thereof an effective amount of a first active agent, such as e.g., an angiotensin receptor blocker, an antifungal agent, a bisphosphonate, an oxytocin inhibitor, an interleukin-1 (IL-1) inhibitor, a cyclooxygenase inhibitor, an ?2? voltage-dependent calcium channel (VDCC) inhibitor, a dihydroorotate dehydrogenase inhibitor, a calcium channel blocker, a renal sodium-chloride symporter inhibitor, an a2 adrenergic agonist, a phenothiazine antipsychotic, a calcineurin inhibitor, a 5-HT agonist, an angiotensin-converting enzyme (ACE) inhibitor, a direct rennin inhibitor, or combinations thereof, and a second active agent, which is a chemotherapeutic agent. Compositions for treating or ameliorating the effects of a glioma are also provided.

Abstract: Disclosed herein are compositions which include nicotinic receptor agonists, specifically of the ?7 nAChR subtype, and methods for suppressing cough.

Abstract: The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein R1, R2, R3, R4, and B are defined in the description. The present invention relates also to compositions containing said compounds which are useful for inhibiting kinases such as wee-1 and methods of treating diseases such as cancer.

Abstract: Use of a composition comprising a compound of any of formulae I, II, Ila, III and Illa; or a combination thereof wherein each R1 is independently C7-11 alkyl; A and B are independently H or CO—R1; R2 is H or C1-4 alkyl; M is a metal monocation (k=1) or dication (k=2); Y is 0 or NH; and Z is 0, NH, CH2O or a bond; for the manufacture of a medicament for stimulating erythropoiesis. Preferably, the composition further comprises human erythroporietin.

Abstract: The invention relates to compositions, such as pharmaceuticals, foods, food additives, or dietary supplements, containing A-type procyanidins, and methods of use thereof, for prophylactic or therapeutic treatment of a human or a veterinary animal to treat or prevent NO-responsive health conditions, treat hypertension, cardiovascular disease, coronary artery disease and/or vascular circulation disorders, prevent or reduce the risk of heart attack, stroke, congestive heart failure and/or kidney failure, or to improve blood flow, for example renal blood flow. The composition may optionally contain an additional NO modulating agent and/or a cardiovascular-protective or therapeutic agent, or may be administered in combination with such an agent.

Abstract: The present invention provides a novel hypertension therapeutic agent. The hypertension therapeutic agent of the present invention contains, as an active ingredient, a compound represented by formula (1): [F1] or a pharmaceutically acceptable salt thereof.

Abstract: A formulation and method for delivery of bioactive substances when applied to, or within, the skin or other exterior region of a mammal. for example, a patient, includes a vasoactive agent; an osmolyte; and an active ingredient. The formulation is sufficiently hygroscopic so as to create a condition of hypertonicity when absorbed by the skin. When the formulation is applied to the skin, the vasoactive agent can be delivered to the dermis so as to contact the vasculature of a patient.