Abstract: The present invention relates to the discovery that the T1R receptors assemble to form functional taste receptors. Particularly, it has been discovered that co-expression of T1R1 and T1R3 results in a taste receptor that responds to umami taste stimuli, including monosodium glutamate. Also, it has been discovered that co-expression of the T1R2 and T1R3 receptors results in a taste receptor that responds to sweet taste stimuli including naturally occurring and artificial sweeteners. Also the present invention relates to the use of hetero-oligomeric taste receptors comprising T1R1/T1R3 and T1R2/T1R3 in assays to identify compounds that respectively respond to umami taste stimuli and sweet taste stimuli. Further, the invention relates to the constitutive of cell lines that stably or transiently co-express a combination of T1R1 and T1R3; or T1R2 and T1R3; under constitutive or inducible conditions.

Abstract: The invention provides methods and compositions for treating hyperlipidemia and disorders associated with hyperlipidemia in a mammal. Compositions useful in the practice of the invention include a microsomal triglyceride transport protein inhibitor (“MTPI”) and at least two other cholesterol lowering drugs selected from the group consisting of a cholesterol absorption inhibitor (“CAI”), a HMG-CoA reductase inhibitor, a bile acid sequestrant, a fibric acid derivative, niacin, and squalene synthetase inhibitor.

Abstract: Triphenylethylene compounds of formula (I) are provided. The compounds are particularly useful for selective estrogen receptor modulation.

Abstract: A pharmaceutical composition including therapeutically effective amounts of at least one HMG-CoA reductase inhibitor present as a dyhydroxyacid salt and at least one additional therapeutic agent.

Abstract: A method of treating interstitial cystitis is disclosed comprising administering to a patient in need thereof an effective amount of a compound selected from compound 1, its metabolite 2 and pharmaceutically acceptable salts thereof:

Abstract: An anti-viral topical gel formulation comprising at least one loop diuretic and/or cardiac glycoside in a gel carrier medium, said formulation capable of transdermal delivery of the said diuretic and/or glycoside.

Abstract: This invention relates to methods for lowering lipid levels in mammals using compounds that inhibit advanced glycation endproducts (AGEs), LR-9, LR-74 and LR-90. These compounds, which inhibit non-enzymatic protein glycation, also inhibit the formation of advanced lipoxidation endproducts (ALES) on target proteins by trapping intermediates in glycoxidation and lopoxidation and inhibiting oxidation reactions important in the formation of AGEs and ALEs.

Abstract: Compounds, compositions, and methods of treating or preventing PPAR?-mediated diseases, including cancer, using phenoxy acetic acid derivatives and prodrugs are provided.

Abstract: Compounds of the formula (I): in which R, R1, R2 and R3 are as defined in the description, the use thereof for the treatment of dyslipidaemia, atherosclerosis and diabetes, pharmaceutical compositions comprising them, and processes for the preparation of these compounds.

Abstract: Cyanophenoxy carboxylic acid compounds and compositions for the delivery of active agents are provided. Methods of administration, treatment of disease and preparation are provided as well.

Abstract: The invention relates to substituted phenoxyacetic acids of formula (I), where the variables are as defined in claim 1, as useful pharmaceutical compounds for treating respiratory disorders, pharmaceutical compositions containing them, and processes for their preparation.

Abstract: Disclosed are methods of treating subjects having conditions related to angiogenesis including administering an effective amount of a polymeric form of thyroid hormone, or an antagonist thereof, to promote or inhibit angiogenesis in the subject. Compositions of the polymeric forms of thyroid hormone, or thyroid hormone analogs, are also disclosed.

Abstract: Aggressively lowering cholesterol in patients suffering from coronary artery disease prevents or delays the need for catheter-based revascularization.

Abstract: The invention features a method of treating or preventing a disease associated with the use of antibiotics in a patient in need thereof by administering to the patient ramoplanin in an amount and for a duration effective to treat said disease. The disease may be caused, for example, by the presence of a bacterium such as enterotoxin producing strains of C. difficile, C. perfringens, or S. aureus.

Abstract: A pharmaceutical composition comprising a compound of formula (1) in polymorphic crystalline Form A: together with a pharmaceutically acceptable carrier or excipient, wherein the compound of formula (1) is present in polymorphic Form A (see, e.g., FIG. 6) substantially free of other polymorphic forms.

Abstract: A composition which causes adult boring bark beetles to discontinue boring, discontinue laying eggs and become disoriented and bore out of the tree or cease boring altogether and die is described. Additional tests have shown that beetles will not infest a tree which has been treated with the composition. Furthermore, the composition also causes beetle larvae to cease boring and die and also causes egg sacks to shrivel and die.

Abstract: A compound or a salt thereof having the atom corresponding to N3 and the two or more atoms selected from N1, N2, N4 and N5, said atoms constitute the pharmacophore represented by the following formula: and inhibits the activity of transcription factor AP-1 and is useful as an agent for preventing and treating the diseases into which over expression of AP-1 participates and as an AP-1 inhibitor.

Abstract: A compound of formula (I) wherein T represents O, S or NR and wherein R represents a H, a C1-6alkyl group or a phenyl C1-6alkyl group and pharmaceutically acceptable salts thereof, processes for preparing such compounds, their the utility in treating clinical conditions including lipid disorders (dyslipidemias) whether or not associated with insulin resistance, methods for their therapeutic use and and pharmaceutical compositions containing them

Abstract: Phenyl amine carboxylic acid compounds and compositions for the delivery of active agents are provided. Methods of administration and preparation are provided as well.

Abstract: Methods and compositions for reducing, preventing or reversing organ damage and/or enhancing organ preservation by administration of a peroxisome-proliferator activated receptor-alpha (PPAR?) agonist to the organ.

Abstract: As described herein, L-FABP is an antioxidant and as such PPAR agonists such as the fibrate and statin class of pharmacological agents (e.g., clofibrate) can be used to induce FABP which in turn induces antioxidant activity. This anti-oxidant activity may be used to treat or prevent diseases characterized by free radical damage. These include but are by no means limited to cholestasis, cirrhosis, nonalcholic liver disease, fatty liver, drug-induced free radical damage (e.g., anticancer agents, acetaminophen overdose, etc.

Abstract: A method is provided for lowering blood pressure in a patient having clinically diagnosed resistant hypertension. The method comprises administering darusentan to the patient adjunctively with a baseline antihypertensive regimen that comprises administration of at least one diuretic and at least two antihypertensive drugs selected from at least two of (a) ACE inhibitors and angiotensin II receptor blockers, (b) beta-adrenergic receptor blockers and (c) calcium channel blockers. The darusentan is orally administered at a dose and frequency effective, in combination with the baseline regimen, to provide a reduction of at least about 3 mmHg in one or more blood pressure parameters selected from trough sitting systolic, trough sitting diastolic, 24-hour ambulatory systolic, 24-hour ambulatory diastolic, maximum diurnal systolic and maximum diurnal diastolic blood pressures.

Abstract: In one aspect, the present invention relates to a formulation in the form of molecular dispersion comprising i) fenofibric acid, a physiologically acceptable salt or derivative thereof and optionally other active substances, ii) a binder component comprising at least one enteric binder, and optionally iii) other physiologically acceptable excipients. In a second aspect, the present invention relates to novel salts of fenofibric acid that are photostable when compared to other salts of fenofibric acid.

Abstract: The invention is concerned with novel hexafluoroisopropanol substituted cyclohexane derivatives of formula (I) wherein R1 to R4, X, m and n are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds bind to LXR alpha and LXR beta and can be used as medicaments.

Abstract: The present invention describes novel methods for using Treprostinil or its derivative, or a pharmaceutically acceptable salt thereof, for improving kidney functions, such as urine output, and treating symptoms associated with kidney malfunction or failure. The invention also relates to kits for the improvement of kidney functions and the treatment of symptoms associated with kidney malfunction or failure, comprising an effective amount of Treprostinil or its derivative, or a pharmaceutically acceptable salt thereof.

Abstract: The invention relates to compounds of the formula I in which the radicals are defined as specified, and also to their physiologically tolerated salts. The compounds are suitable, for example, as medicaments for preventing and treating type 2 diabetes.

Abstract: The present invention relates to ascorbic acid single-phase solution compositions that provide enhanced stability, enhanced solubility and an enhanced photoprotective effect as compared to prior compositions. The compositions comprise L-ascorbic acid; a cinnamic acid derivative such as p-coumaric acid, ferulic acid, caffeic acid, sinapinic acid, a derivative thereof, and a combination thereof; a solvent comprising a glycol ether and an alkanediol; and water; the composition having a pH of no more than about 3.5. The compositions may also comprise a form of Vitamin E and are useful for treatment of radical-induced damage to a subject, particularly the skin of a subject.

Abstract: Novel compounds of the general formula (I), wherein Ar, R1, R2, X1, X2, Y1, Y, and Z are as defined in the specification, the use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds and methods of treatment employing these compounds and compositions. The present compounds may be useful in the treatment and/or prevention of conditions mediated by Peroxisome Proliferator-Activated Receptors (PPAR), in particular the PPAR? subtype.

Abstract: Phenoxy carboxylic acid compounds and compositions for the delivery of active agents are provided. Methods of administration and preparation are provided as well.

Abstract: Cyanophenoxy carboxylic acid compounds and compositions for the delivery of active agents are provided. Methods of administration, treatment of disease and preparation are provided as well.

Abstract: Novel compounds of the general formula (I), the use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds and methods of treatment employing these compounds and compositions. The present compounds may be useful in the treatment and/or prevention of conditions mediated by Peroxisome Proliferator-Activated Receptors (PPAR), in particular the PPAR? suptype.

Abstract: A class of 2-aryloxy-2-arylalkanoic acids comprises compounds that are potent agonists of PPAR alpha and/or gamma, and are therefore useful in the treatment, control or prevention of non-insulin dependent diabetes mellitus (NIDDM), hyperglycemia, dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, atherosclerosis, obesity, vascular restenosis, inflammation, and other PPAR alpha and/or gamma mediated diseases, disorders and conditions.

Abstract: The use of compounds of the formula and pharmaceutically acceptable salts thereof, alone or in combination for the treatment of transplant rejection, wherein the substituents are further defined in the application.

Abstract: The present invention relates to a reduced particle size form of the compound (S)-2-ethoxy-3-[4-(2-{4-methanesulfonyloxyphenyl}ethoxy)phenyl]propanoic acid, as shown in formula (I), or a pharmaceutically acceptable salt thereof or a solvate of either thereof. The invention also concerns methods of treating one or more conditions associated with Insulin Resistance Syndrome using the reduced particle size form of the compound, or a pharmaceutically acceptable salt thereof in the manufacture of a medicament for use in one or more of said conditions. The invention further concerns pharmaceutical compositions containing the reduced particle size form of the compound, or a pharmaceutically acceptable salt thereof, or a solvate thereof, as an active ingredient, as well as processes for the manufacture of the reduced particle size form of the compound, or a pharmaceutically acceptable salt thereof.

Abstract: A pharmaceutical composition, comprising: a compound of formula (1) in polymorphic crystalline Form A: together with a pharmaceutically acceptable carrier or excipient, wherein the compound of formula (1) is present in polymorphic Form A (see, e.g., FIG. 6) substantially free of other polymorphic forms.

Abstract: This invention provides compounds of Formula I having the structure or a pharmaceutically acceptable salt thereof, which are useful in treating metabolic disorders related to insulin resistance or hyperglycemia.

Abstract: This invention relates to new compounds, pharmaceutical compositions and diagnostic kits comprising such compounds, and methods of using such compounds for inhibiting NAALADase enzyme activity, detecting diseases where NAALADase levels are altered, effecting neuronal activity, effecting TGF-? activity, inhibiting angiogenesis, and treating glutamate abnormalities, diabetic neuropathy, pain, compulsive disorders, prostate diseases, cancers and glaucoma.

Abstract: This invention relates to biocidal compositions and methods of using same. Also provided is a process for the manufacturing of a biocidal composition in the form of a tablet and a method of using the biocidal compositions for the disinfection of water that may contain microorganisms and biofilms.

Abstract: The present invention relates to a composition comprising an organic preservative acid and a UV-active indicator substance for preserving wood and for detection of the sufficient preservation of wood.

Abstract: The invention concerns compounds inhibiting LTA4 hydrolase of formula (I). The invention also concerns their therapeutic, in particular anti-inflammatory, applications.

Abstract: Disclosed are anti-viral compositions containing at least one zinc compound and at least one phenolic antioxidant (and optionally other ingredients), and a pharmaceutical carrier. Also disclosed are methods of treating lesionous symptoms of a viral infection involving applying an effective amount of the anti-viral composition to the lesions.

Abstract: Pharmaceutical uses of glycine betaine, such as for the treatment of thromboses not induced by hyperhomocystenemia or homocystinuria, of blood disorders, such as blood coagulation, thrombi formation.

Abstract: It has been discovered that certain selected ethers of probucol, and their pharmaceutically acceptable salts or prodrugs, are useful for increasing circulating HDL cholesterol. These compounds may also improve HDL functionality by (a) increasing clearance of cholesteryl esters, (b) increasing HDL-particle affinity for hepatic cell surface receptors or (c) increasing the half life of apoAI-HDL.

Abstract: The present invention provides for a method for inhibiting growth of a bacterium which consists essentially of contacting the bacterium with a compound having the structure: 1

Abstract: An oral dosage form comprises cromolyn sodium (sodium or disodium cromoglycate), and an acylated amino acid delivery agent.

Abstract: A method for treating irritable bowel syndrome (IBS) is included. The method includes the step of administering a fibric acid derivative to a patient diagnosed with IBS in order to alleviate the symptoms associated with IBS.

Abstract: The present invention provides compositions and methods for the treatment of pain, inflammation or inflammation mediated disorders in a subject. More particularly, the invention provides a combination therapy for the treatment of pain, inflammation or inflammation mediated disorders comprising the administration to a subject of a potassium ion channel modulator in combination with a cyclooxygenase-2 selective inhibitor.

Abstract: A method for minimizing scarring and preventing excessive scar formation at an injury site is disclosed. The method involves the topical and/or local application of a therapeutically effective amount of a defibrinogenating agent or of a fibrinolytic agent that may be delivered in an appropriate vehicle in a controlled- or timed-release manner. In accordance with the principles of the invention, the defibrinogenating agent or fibrinolytic agent is applied as a coating on, or is irradiated or impregnated into or onto a delivery vehicle such as, for example, sutures, dissolvable sutures, bandages, gauze pads, or other types of first aid bandaging materials. Such application may take the form of a controlled- or timed-release aspect of either the vehicle, the delivery material or the therapeutic agent, such that the release of the therapeutic agent may be regulated to produce an appropriate therapeutic pattern or defibrinogenation or fibrinolysis.

Abstract: This invention relates to new compounds, pharmaceutical compositions and diagnostic kits comprising such compounds, and methods of using such compounds for inhibiting NAALADase enzyme activity, detecting diseases where NAALADase levels are altered, effecting neuronal activity, effecting TGF-&bgr; activity, inhibiting angiogenesis, and treating glutamate abnormalities, diabetic neuropathy, pain, compulsive disorders, prostate diseases, cancers and glaucoma.

Abstract: The present invention features the combinational use of short-acting anti-histamine agents in combination with long-acting anti-histamine agents to provide rapid, synergistic and long lasting relief towards ocular allergy signs and symptoms.