Abstract: The invention encompasses novel compounds of Formula I or pharmaceutically acceptable salts thereof. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and are therefore useful to treat pain and/or inflammation from a variety of diseases or conditions, such as osteoarthritis, rheumatoid arthritis and acute or chronic pain. Methods of treating diseases or conditions mediated by the mPGES-1 enzyme and pharmaceutical compositions are also encompassed.

Abstract: The present invention provides a preventive or therapeutic agent for cerebral ischemic injury or cerebral ischemic reperfusion injury in stroke such as cerebral infarction and cerebral hemorrhage which exerts its effect through a different mechanism from that of conventional therapeutic agents and can be taken for along period. The present invention is a preventive or therapeutic agent for cerebral ischemic injury or cerebral ischemic reperfusion injury in stroke which contains 6-fluoro-2?,5?-dioxospiro[chroman-4,4?-imidazolidine]-2-carboxamide as an active ingredient. A particularly preferable compound is an optically resolved (2S,4S)-form of fidarestat.

Abstract: or a pharmaceutically acceptable salt or N-oxide thereof, are useful in the treatment of tumors and cancers.

Abstract: The present invention relates to a controlled release capsule preparation for oral administration, which contains (i) a granule containing a physiologically active substance which is a compound represented by the formula: wherein n is an integer of 1 to 3, and Ar is an aromatic ring optionally having substituent(s), or a salt thereof, and a hydrophilic polymer, and coated with an enteric coating agent and the like, and (ii) a fluidizer. According to the present invention, a controlled release composition for oral administration of an imidazole derivative, which has steroid C17,20-lyase inhibiting activity and which has remarkably improved sustainability of the blood concentration, is provided.

Abstract: The present invention is directed to certain hexahydrpyrrolidinone compounds which are useful as neurokinin-1 (NK-1) receptor antagonists, and inhibitors of tachykinin and in particular substance P. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including emesis, urinary incontinence, depression, and anxiety.

Abstract: The present invention relates to methods, compounds, and compositions for inhibiting angiogenesis. More particularly, the present invention relates to methods, compounds, and compositions for inhibiting VEGF production.

Abstract: The present application describes novel hydantoin derivatives of formula (I): or pharmaceutically acceptable salt or prodrug forms thereof, wherein A, B, R1, R2, R3, R4, R5, R6, R7, R11, and n are defined in the present specification, which are useful as inhibitors of matrix metalloproteinases (MMP), TNF-? converting enzyme (TACE), aggrecanase, or a combination thereof.

Abstract: A method of treating weight loss due to underlying disease in a patient, the method comprising administering to the patient an effective amount of an agent which reduces sympathetic nervous system activity. A method of treating weight loss due to underlying disease in a patient the method comprising administering to the patient an effective amount of any one or more of the following: a compound which inhibits the effect of aldosterone such as an aldosterone antagonist; a chymase inhibitor; a cathepsin B inhibitor; a ? receptor blocker; an imidazoline receptor antagonist; a centrally acting ? receptor antagonist; a peripherally acting ? receptor antagonist; a ganglion blocking agent; a drug that has an effect on cardiovascular reflexes and thereby reduces SNS activity such as an opiate; scopolamine; an endothelin receptor antagonist; and a xanthine oxidase inhibitor. The methods are particularly useful in treating cardiac cachexia.

Abstract: This invention concerns novel substituted tetracyclic tetrahydrofuran, pyrrolidine and tetrahydrothiophene derivatives with binding affinities towards serotonin receptors, in particular 5-HT2A and 5-HT2C receptors, and towards dopamine receptors, in particular dopamine D2 receptors and with norepinephrine reuptake inhibition properties, pharmaceutical compositions comprising the compounds according to the invention, the use thereof as a medicine, in particular for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic, cardiovascular and gastrokinetic disorders and processes for their production. The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in Claim 1.

Abstract: The invention relates generally to biotin-containing compounds that are useful as imaging agents and drug-delivery agents. Another aspect of the invention relates to the aforementioned compounds chelated to a metal atom. In a preferred embodiment, the metal atom is a gadolinium. Another aspect of the invention relates to a compound comprising three biotin moieties and a pharmaceutical agent covalently bound to a heterocyclic core. In certain embodiments, the pharmaceutical agent is an antibiotic, antiviral, or radionuclide. Another aspect of the present invention relates to a method of treating disease involving administering the compounds of the invention to a mammal. Another aspect of the present invention relates to a method of acquiring a magnetic resonance image using the compounds of the invention.

Abstract: This invention relates to unit dosage forms of temozolomide. These unit dosage forms are particularly well-suited for decreasing the pill burden and increasing patient compliance. The invention also relates to methods of treating proliferative disorders in a patient with these unit dosage forms. The invention additionally relates to kits comprising these unit dosage forms.

Abstract: The present invention is directed to a method for treating a patient suffering from the metabolic syndrome, Type 2 diabetes, obesity, or prediabetes, comprising the step of increasing the ratio of dopaminergic neuronal to noradrenergic neuronal activity within the central nervous system and particularly the hypothalamus of the central nervous system of the patient.

Abstract: The present invention is directed to novel cyclohexylglycine derivatives which are inhibitors of the dipeptidyl peptidase-IV enzyme (“DP-IV inhibitors”) and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly type 2 diabetes. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which the dipeptidyl peptidase-IV enzyme is involved.

Abstract: It is demonstrated in the present invention that G-quadruplex ligands can be used to both shorten telomeres and inhibit telomerase by causing telomere uncapping. The invention relates to compositions and methods of treating cancer stem cells comprising the administration of G-quadruplex ligands, such as 3,11-difluoro-6,8,13-trimethyl-8H-quino[4,3,2-kl]acridinium methosulfate (RHPS4), which can effectively inhibit or reduce the growth of cancer stem cells. The invention also relates to a synergistic effect in inhibiting or reducing the growth cancer stem cells when a G-quadruplex ligand is combined with a mitotic spindle poison, such as paclitaxel, or other agents used in the treatment of cancer and disease. The invention also relates to RHPS4 inducing non-cancerous cell and non-cancerous stem cell proliferation.

Abstract: Disclosed herein is a method for protecting humans in need of such protection from physical damage caused by ionizing radiation comprising administering to said humans on a defined basis prior to and after exposure to such radiation a plurality of antioxidants at a dosage level directly proportional to the radiation level likely to be encountered.

Abstract: Provided are MC4-R binding compounds of the formula XVII: wherein L2 is a linker group, and P1, P2, P3, P4, Z1, Z2, Z3, Z4, Z5, t, s, and R are as described in the specification. Methods of using the compounds to treat MC4-R associated disorders, such as disorders associated with weight loss, are also provided.

Abstract: Inhibitors of poly(ADP-ribose)polymerase, ways to make them and methods of treating patients using them are disclosed.

Abstract: Provided are compositions and methods for increasing diet induced thermogenesis. Typically, the compositions are comprised of L-histidine, L-isoleucine, L-leucine, L-lysine, L-methionine, L-phenylalanine, L-valine and L-threonine.

Abstract: Novel substituted 2-aminoimidazoles of formula I, process for their preparation, their use as medicament or diagnostic aid, and medicament containing them.

Abstract: Lipoic acid derivatives and pharmaceutical formulations containing lipoic acid derivatives are useful in the treatment and prevention of disease characterized by disease cells that are sensitive to lipoic acid derivatives.

Abstract: 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.

Abstract: A compound represented by formula (I) (wherein ring A is a nitrogen-containing ring which may have a substituent(s), E is a binding bond or a spacer of which main chain has an atom number of 1-8, Q is a hydrogen atom, a hydrocarbon group which may have a substituent(s) or a cyclic group which may have a substituent(s).), a salt thereof, an N-oxide thereof, a solvate thereof, or a prodrug thereof. Since the compounds of the present invention represented by formula (I), a salt thereof, an N-oxide thereof or a solvate thereof, or a prodrug thereof have the affinity to MBR, they are useful for the prevention and/or treatment for disease caused by stress.

Abstract: The present invention relates to compounds of the formula (I), wherein R1, R2, A, B, D, E, F, G and Ar are as defined herein, and pharmaceutically acceptable salts thereof, useful in the prevention and treatment of hepatitis C infections.

Abstract: A method for prevention, inhibition or treatment of neuronal degeneration caused by injury, disease, disorder or condition in the central nervous system (CNS) comprises administering a glycoluril derivative to an individual in need thereof.

Abstract: Disclosed herein are methods of treating lentigo maligna, superficial spreading malignant melanoma, acral lentiginous malignant melanoma or nodular malignant melanoma with bis(thio-hydrazide amides) represented by a formula selected from structural formulas (i)-(ix) or pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising these bis(thio-hydrazide amides) and compositions comprising these bis(thiohydrazide)amides and one or more anti-cancer agent.

Abstract: Compounds represented by Formula (I): or a pharmaceutically acceptable salt or N-oxide thereof, are useful in the treatment of tumors. Combinatorial libraries composed of compounds represented by Formula (I) or benzimidazole compounds represented by Formula (II): are useful in providing compounds to assay for such therapeutically useful compounds.

Abstract: A Composition to provide nutritional support for mammals having glycemic control and deficit concerns, and assist in managing glycemic controls deficits, with a synergistic combination of natural ingredients.

Abstract: The use of compound of formula I in the preparation of a medicament, e.g. for the treatment of condition mediated by CCR3.

Abstract: The invention provides methods of treating cancer using a compound of formula (1) or a pharmaceutically acceptable salt thereof, particularly a malate salt, in combination with various additional therapeutic agents. The invention also provides therapeutic dosing regimens, using the compound of formula (1) and an additional therapeutic agent.

Abstract: Compounds of formula (I) wherein RF1, RF2, Z, R1, R2, Ar, X and Y are as defined in the specification as well as salts and pharmaceutical compositions including the compounds were prepared. These compounds are useful in therapy, in particular in the management of pain.

Abstract: Disclosure is provided for imidazole derivative compounds that prevent, remove and/or inhibit the formation of biofilms, compositions comprising these compounds, devices comprising these compounds, and methods of using the same.

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: The invention is directed to formulations comprised of multiple dietary and endogenously made antioxidants and B-vitamins and the use of these formulations in preventing and treating coronary artery disease.

Abstract: Substituted pyrazoles are provided that are useful for the treatment of, for example, diabetes, obesity and metabolic syndrome.

Abstract: The present invention describes benzimidazole derivatives of Formula (I) which constitute potent PARP inhibitors in combination with radiotherapy or in combination with other chemotherapeutic agents.

Abstract: A dibenzylamine compound represented by the formula (1) wherein R1 and R2 are each a C1-6 allyl group optionally substituted by halogen atoms and the like; R3, R4 and R5 are each a hydrogen atom, a halogen atom and the like, or R3 and R4 may form, together with carbon atoms bonded thereto, a homocyclic or heterocyclic ring optionally having substituent(s); A is —N(R7)(R8) and the like; ring B is an aryl group or a heterocyclic residue; R6 is a hydrogen atom, a halogen atom, a nitro group, a C1-6 allyl group and the like; n is an integer of 1 to 3, a prodrug thereof and a pharmaceutically acceptable salt thereof show selective and potent CETP inhibitory activity, and therefore, they can be provided as therapeutic or prophylactic agents for hyperlipidemia or arteriosclerosis and the like.

Abstract: Formulations for minimizing damage to at least one of cells, organs and systems within the body of a subject afflicted with Diabetes Mellitus. The invention additionally encompasses methods for minimizing said damage which comprise administering to subjects in need thereof a therapeutic amount of a formulation(s) according to the invention.

Abstract: The invention relates to condensed tricyclic benzimidazoles of formula (I) in which the substituents and symbols have the meanings indicated in the description. The compounds have gastric secretion inhibiting and excellent gastric and intestinal protective action properties.

Abstract: A natural composition formulated to modulate multiple pathophysiological processes in order to facilitate homeostatic glucose metabolism in a patient, and more particularly to increase insulin sensitivity in the same. The natural composition is a safe and effective formulation for the etiological prevention and treatment of diseases, complications, conditions, or disorders associated with chronic or long-term destabilization of glucose metabolism.

Abstract: The invention relates to compounds of the formula I where R1, R2, R3, R4 and R5 have the meanings given in claim 1. The compound is suitable in particular for use in skin care compositions. They protect, firstly, against harmful oxidation reactions and, secondly, also act as UV filters.

Abstract: Disclosed are pharmaceutical compositions comprising brimondine and timolol for topical ophthalmic delivery and a method of treatment comprising administering said composition when indicated for glaucoma and associated conditions such as elevated intraocular pressure in the eyes of humans.

Abstract: Disclosed are pharmaceutical compositions comprising brimondine and timolol for topical ophthalmic delivery and a method of treatment comprising administering said composition when indicated for glaucoma and associated conditions such as elevated intraocular pressure in the eyes of humans.

Abstract: The present invention provides novel compounds of formula I and their use in the inhibition of c-Jun N-terminal kinases. The present invention further provides the use of these compounds in medicine, in particular in the prevention and/or treatment of neurodegenerative disorders related to apoptosis and/or inflammation.

Abstract: The present invention relates to a method and transdermal pharmaceutical composition for preventing or reducing the likelihood of calcium deficiency or imbalances caused by calcium deficiency. The transdermal pharmaceutical composition includes a therapeutically effective amount of a pharmaceutically acceptable salt of calcium and a pharmaceutically acceptable carrier constituting a pluronic lecithin organogel.

Abstract: A vitamin, mineral, herbal, and micronutrient treatment for acne via support of the physiologic processes in the body which cause acne is disclosed. It is a targeted formula, designed specifically to address the causes of acne. This specific, unique formulation preferably in a gummy substrate for ease of administration, to induce a willingness on the part of the target population to take it, and to increase the bioavailability of the active ingredients. Other types of confection or edible vehicle can be used.

Abstract: The present invention provides a fused ring compound of the following formula [I] wherein each symbol is as defined in the specification, a pharmaceutically acceptable salt thereof, and a therapeutic agent for hepatitis C, which contains this compound. The compound of the present invention shows an anti-hepatitis C virus (HCV) action based on the HCV polymerase inhibitory activity, and is useful as a therapeutic agent or prophylactic agent for hepatitis C.

Abstract: Disclosed are fungicidal mixtures containing a synergistically effective amount of A) a triazolopyrimidine of formula I, and B) imidazole derivatives of formula II, wherein X1 and X2 represent halogen and phenyl which can be substituted by halogen or alkyl, or X1 and X2 form a difluoromethylendioxyphenyl group along with the bridging C?C double bond, X3 represents cyano or halogen, and X4 represents dialkylamino or isoxazol-4yl that can carry two alkyl radicals. The invention also relates to methods for controlling destructive fungi by means of mixtures of compounds I and II, agents containing said mixtures, and the use of compounds I and II for producing such mixtures.

Abstract: The present invention relates to compositions and methods for promoting tissue regeneration, preferably neural tissue regeneration. Compositions of the invention include (i) certain diphenyl sulfides, diphenyl sulfoxides, diphenyl sulfones, and sulfide, sulfoxide and sulfones of dibenzothiophene and thioxanthene, as well as various analogues and derivatives of these compounds; (ii) one or more cells harvested from an animal or organism subsequent to the administration of a composition comprising a compound of (i); or (iii) any combination of (i) and (ii). The invention can be useful in treating decreases in neuronal function, for example from injury or disease.

Abstract: Compounds of formula (I): or pharmaceutically acceptable derivatives thereof, and their use as pharmaceuticals, particularly as p38 kinase inhibitors.

Abstract: The present invention relates to method and means for treating a solid tumor using a number of, in vitro prepared, anticellular agent(s)-carrying blood platelets to induce a thrombus formation within the tumor vasculature, and at the same time to deliver a high concentration of an anticellular agent within the tumor. The blood platelets are targeted and attached to the tumor vasculature using in vivo assembled binding complexes, each having at least one binding site specifically binding to tumor cells or to tumor-associated vasculature, and at least one binding site specifically binding to a blood platelet surface. The platelet-mediated thrombus formed within the tumor vasculature leads to occlusion of the tumor vasculature, with ultimate destruction of the centrally located tumor cells. This is followed by destruction or impairing the growth or cell division of the peripherally located tumor cells, by the anticellular agent(s) carried by the blood platelets.