Abstract: Pharmaceutical formulations exhibit a desirably low Cmax, among other properties, that contain particles of amorphous bardoxolone methyl, either in pure form or in the form of a solid dispersion, admixed with particles of a hydrophilic binding agent. Such formulations possess the advantage of higher oral bioavailability, relative to formulations based on the crystalline form of bardoxolone methyl.

Abstract: Provided are compounds for inhibiting Snail-p53 binding and therapeutic agents for cancer including the compounds as an effective component. The Snail-p53 binding inhibitors induce expression of p53 in K-Ras mutant cell lines, thereby enabling effective treatment or prevention of K-Ras mutant cancer, such as, pancreatic cancer, lung cancer, cholangioma, and colon cancer, of which diagnosis or treatment is not easy.

Abstract: The present invention is directed to compositions and methods for pain management, and for treating inflammation or an inflammation-associated disorder in a subject comprising administering to the subject a therapeutically effective amount of a COX-2 inhibitor and a therapeutically effective amount of a prostacyclin analog, such as treprostinil, a pharmaceutically acceptable salt thereof, or a treprostinil derivative described herein.

Abstract: The present invention relates to the discovery of biodegradable multi-armed oligomers wherein the end groups of these oligomers have been functionalized with biologically active molecules. The resultant multi-armed oligomers end-functionalized with biologically active molecules have a controllable degradation profile. The hydrolytic degradation of oligomers of the present invention releases the biologically active compound as such with no change in native chemical structure.

Abstract: A drug effective for the treatment and prevention of psychiatric disorders such as schizophrenia, anxiety and related ailments thereof, depression, bipolar disorder and epilepsy. The drug antagonizes the action of group II metabotropic glutamate receptors and shows high activity in oral administration A 2-amino-bicyclo[3.1.0]hexane-2,6-dicarboxylic ester derivative represented by formula [I] [wherein R1 and R2 are identical or different, and each represents a hydrogen atom, a C1-10alkyl group or the like; X represents a hydrogen atom or a fluorine atom; Y represents —OCHR3R4 or the like (wherein R3 and R4 are identical or different, and each represents a hydrogen atom, a C1-10alkyl group or the like; and n represents integer 1 or 2)], a pharmaceutically acceptable salt thereof or a hydrate thereof.

Abstract: A method of preventing or treating diseases caused by Mycobacterium, comprising administering to a subject in need of such treatment an effective amount of a pleuromutilin.

Abstract: A triterpenoid compound, methyl 2-cyano-3,12-dioxoleana-1,9(11)-dien-28-oate (CDDO methyl ester), has a non-crystalline, glassy solid form and a non-hydrous crystalline form that can prepared, for example, from a saturated methanol solution. The glassy form displays an enhanced bioavailability over the non-hydrous crystalline form. Each form of CDDO methyl ester is a superior candidate for use, typically in solid dosage form, for treating a variety of disease states, generally associated with inflammation.

Abstract: The invention relates to methods of treatment of hepatitis C, dyslipidemia, insulin resistance, and inflammation, with flavonoid-sugar complexes.

Abstract: The present invention provides a controlled release pharmaceutical composition which exhibits reduced food effect.

Abstract: The present invention provides a compound of formula I, II, III and IV as defined herein and pharmaceutically acceptable derivatives thereof. The present invention further provides use of the compounds of the present invention in the treatment of bacterial infection and in the treatment of HIV infection. Also provided are pharmaceutical compositions comprising the compounds of the present invention.

Abstract: The novel active ingredient combinations which consist of the compounds of the formula (I) in combination with further active insecticidal ingredients (II) are very suitable for control of animal pests such as insects and/or unwanted acarids.

Abstract: A compound (particularly useful for inhibiting cancer) according to formula I: or a pharmaceutically acceptable salt thereof, wherein: x is 0 or 1; R1-R6 are each independently H, —CN, —NO2, —NO, —OH, halogen, hydroxyalkyl, carboxyl, substituted carboxyl, aminocarbonyl, alkoxy, carbonyl or substituted carbonyl; R7 is H, alkyl, alkyl amino, aminoacyl, hydroxyacyl, heteroaryl, heterocycloalkyl, alkyl heteroaryl or alkyl heterocycloalkyl; R8 is H or alkyl; A is O or N; and Ar is an aryl, substituted aryl, heteroaryl, or substituted heteroaryl, provided that if R7 is H then Ar is aryl substituted with alkyl amino.

Abstract: The invention provides novel omega-3 oil formulations of one or more statins. These formulations are readily bioavailable. Notably, because the formulations of the invention contain an omega-3 oils as the major ingredient, they not only provide an antihypercholesterolemic effect due to the statin active ingredient, they also provide recommended daily dosages of omega-3 oils (i.e., approximately 1 gram of omega-3 oil per day), or a portion thereof. The invention also provides novel salts of one or more statins.

Abstract: The present invention provides a nitrogen-containing compound represented by formula (I1) (in formula (I1), R0 represents a nitro group or the like, Z represents an optionally substituted aryl group or the like, R3 represents a hydrogen atom or the like, Y represents a nitro group or the like, n represents an integer of 0 to 3, D represents an optionally substituted 5-membered to 8-membered hydrocarbon ring group or heterocyclic group having or not having a substituent other than substituent X, X represents a group represented by formula (II-1) (in formula (II-1), R1 and R2 respectively and independently represent a hydrogen atom or the like), A represents a carbon atom or the like, n1 represents an integer of 0 to 2) or a salt thereof, and an insecticide, miticide, sanitary insect pest control agent, or harmful organism control agent including as an active ingredient thereof the nitrogen-containing compound or the salt thereof.

Abstract: This invention describes novel tricyclic-bis-enone derivatives (TBEs), such as TBE-31, TBE-34, TBE-45 and water-soluble TBEs. The methods of preparing these compounds are also disclosed. The inventors demonstrate the ability of these new TBEs to inhibit proliferation of human myeloma cells, inhibit the induction of iNOS in cells stimulated with interferon-?, induce heme oxygenase-1 (HO-1), induce CD11b expression—a leukemia differentiation marker, inhibit proliferation of leukemia cells, induce apoptosis in human lung cancer, and induce apoptosis in other cancerous cells. The TBEs of this invention are expected to be useful agents for the treatment and prevention of many diseases, including cancer, neurological disorders, inflammation, and pathologies involving oxidative stress.

Abstract: A prostate cancer progression inhibitor comprises 4-(4-cyano-2-{[2-(4-fluoro-1-naphthyl)propanoyl]amino}phenyl)butyric acid, a salt thereof, a solvate thereof, or a prodrug thereof. 4-(4-Cyano-2-{[2-(4-fluoro-1-naphthyl)propanoyl]amino}phenyl)butyric acid is useful as a prostate cancer progression inhibitor because this butyric acid has, for example, a growth inhibiting effect and a hormone responsiveness recovering effect on prostate cancer that has acquired hormone resistance.

Abstract: The present invention provides therapeutically active compounds and compositions as receptor antagonists and methods of use thereof. In one aspect, the compounds are useful in modulating pain, inflammation and acute phase reactions by inhibiting the PGE2 receptors including PGE2 EP1, EP2 and EP4 receptors.

Abstract: This invention provides a method for inhibiting pancreatic islet ?-cell dysfunction, comprising administering to a subject in need thereof an inhibitory effective amount of a rhein compound having the general formula (I) or a pharmaceutically acceptable salt thereof,

Abstract: The present invention relates to a pharmaceutical composition for preventing or treating Hepatitis C, comprising the roots extract of Platycodon grandiflorum and/or saponin components in Platycodon grandiflorum useful as an antiviral agent. The composition of the present invention has no harm to human and inhibits the proliferation of Hepatitis C virus, so that it can be effectively used as a preventive or therapeutic agent for Hepatitis C.

Abstract: Novel combinations comprising HMG CoA reductase inhibitors, or statins, with partial fatty acid oxidation inhibitors (pFOXi), and methods for their use, are disclosed. These combinations are useful in preventing or reducing the risk of developing diabetes which results from therapy with a statin.

Abstract: The invention relates to novel tetralone based amines and their use in the treatment of central nervous system (CNS) disorders, such as depression, attention deficit hyperactivity disorder (ADHD) and Parkinson's disease. The invention further relates to pharmaceutical compositions containing the compounds and compositions of the invention as well as methods of inhibiting reuptake of one or more monoamine, such as such as dopamine and norepinephrine, from the synaptic cleft, and methods of modulating one or more monoamine transporter.

Abstract: The present invention relates to a complex made up of at least one molecule of statin or a derivative thereof, covalently bonded to at least one hydrocarbon radical including at least 18 carbon atoms and containing at least one 2-methyl-buta-2-ene unit, to nanoparticles of such a complex, and to a method for preparing same, said complex and/or said nanoparticles optionally being in the form of a lyophilisate. The present invention also relates to a pharmaceutical composition including at least one complex and/or nanoparticles such as previously defined. The invention finally relates to said complex and/or to said nanoparticles for the treatment and/or prevention of hyperlipemia and hypercholesterolemia.

Abstract: The present invention relates to nitric oxide releasing prodrugs of known drugs or therapeutic agents which are represented herein as compounds of formula (I) wherein the drugs or therapeutic agents contain one or more functional groups independently selected from a carboxylic acid, an amino, a hydroxyl and a sulfhydryl group. The invention also relates to processes for the preparation of the nitric oxide releasing prodrugs (the compounds of formula (I)), to pharmaceutical compositions containing them and to methods of using the prodrugs.

Abstract: Disclosed herein are novel protoilludane norsesquiterpenoid ester compounds isolated from mycelium of Armillaria mellea that are useful for treating tumors or proliferative diseases such as breast cancers, lung cancers, colon cancers or leukemia.

Abstract: The present invention provides the use of pelorol analogs of Formula, (I) and pharmaceutical compositions thereof as modulators of SHIP 1 activity. A compound or a pharmaceutical composition of the present invention may be used for the treatment or prophylaxis of an inflammatory, neoplastic, hematopoetic or immune disorder or condition in addition to other disorders and conditions.

Abstract: Described herein are methods for treating inflammatory disorders or for inhibiting the build-up of arterial plaque. The methods comprise administering to a subject in need thereof a therapeutically effective amount of a synthetically modified fullerene.

Abstract: The present invention provides a controlled-release composition which provides a therapeutically effective plasma concentration of N-acetylcysteine over prolonged period of time. The present invention also includes the use of the controlled-release composition, either alone or in combination with at least one additional active agent, for reduction of vascular inflammation marker and treatment of diseases, conditions, and/or symptoms associated with systemic and/or vascular inflammation in a patient. Furthermore, the present invention provides a process of making granules comprising N-acetylcysteine, or a salt, solvate, prodrug, and/or analog thereof.

Abstract: Provided are methods and compositions for the prevention and/or treatment of viral conditions, virally-induced conditions and inflammatory conditions. The methods can comprise administering to a subject a viral inducing agent with an antiviral agent, and optionally an additional agent. The viral inducing agent can be a HDAC inhibitor administered orally.

Abstract: This invention provides, but is not limited to, novel oleanolic acid derivatives having the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds and compositions.

Abstract: The invention provides methods for optimizing therapeutic efficacy for treating hypercholesterolemia in a subject having a cardiovascular disease (CVD), comprising (a) determining subject characteristics that affect the likelihood of reaching a goal level of low density lipoprotein (LDL); and (b) obtaining success probabilities of a variety of statin treatments for reaching said goal level of LDL using said subject characteristics and a multivariate model; and (c) administrating the optimal statin treatment with the highest success probability of step (b) to said subject thereby optimizing therapeutic efficacy for treating hypercholesterolemia in said subject.

Abstract: The present invention relates to a composition comprising PKC agonist as an active ingredient. More precisely, the present inventors confirmed that absence seizure specific SWD was reduced by administrating PKC agonist into an animal model. Therefore, the composition of the present invention comprising PKC agonist as an active ingredient can be effectively used for the prevention and treatment of absence seizure and for the production of health improving functional food.

Abstract: A material comprising from 30 to 80% by weight of ursolic acid, from 2 to 25% by weight of oleanolic acid and from 1 to 68% by weight of triterpenoic acids other than ursolic acid or oleanolic acid, or derivatives of any of these acids, said percentages being based on total weight of said acids or derivatives and the percentages of said acids or derivatives adding up to 100%, can be used in the prevention or treatment of hypersensitivity and/or hyper-reactivity.

Abstract: Disclosed are formulations of ladostigil tartrate, including pharmaceutical compositions, process for the manufacture, and use thereof.

Abstract: The present invention relates to certain novel salts of Betulinic acid derivatives, to process for preparing such compounds, to use the compounds in treating diseases or disorders mediated by HIV infection, to methods for their therapeutic use and to pharmaceutical compositions containing them.

Abstract: Small molecule choline kinase inhibitors, pharmaceutical compositions thereof, and screening methods for identifying and evaluating choline kinase inhibitors are provided. Safe and effective methods for treating subjects suffering from a disorder or disease characterized by neoplastic cell proliferation employing the choline kinase inhibitors are also provided.

Abstract: The subject invention concerns compounds having activity as inhibitors of proteasomes and methods of using the subject compounds.

Abstract: A class of compounds useful in pharmaceutical compositions and methods for treating or preventing cancer is described. The compounds' ability to inhibit RET kinase is quantified, i.e., their respective RET IC50 and EC50 values are described. One such compound, known as cyclobenzaprine and herein as SW-01, has been identified as RET-specific with an IC50 of 300 nM. SW-01 inhibits RET autophosphorylation and blocks the growth and transformation of thyroid cancer cell lines. It has been further tested in pancreatic cancer, breast cancer, and SCLC cell lines. The compounds show utility for inhibition of survival and proliferation of tumour cells.

Abstract: The present invention provides compounds useful, for example, for treating metabolic disorders in a subject. Such compounds have the general formula IA, IB, I?A or I?B: where the definitions of the variables are provided herein. The present invention also provides compositions that include, and methods for using, the compounds in preparing medicaments and for treating metabolic disorders such as, for example, type II diabetes.

Abstract: Therapeutic compounds, methods, and compositions are disclosed herein for treating glaucoma and baldness in mammals. The specific compounds are described herein and are modified prostaglandin derivates.

Abstract: Several ursolic acid derivatives and pharmaceutical compositions thereof are provided. The ursolic acid derivatives and the pharmaceutical compositions thereof have at least one of an anticancer and an anti-inflammatory effects. A method for increasing a reactive oxygen species in a cell is also provided. The method comprises a step of providing the cell with a pharmaceutical composition including an ursolic acid derivative.

Abstract: Disclosed herein are methods of inhibiting the build-up of arterial plaque in a subject in need thereof. These methods comprise administering to the subject in need thereof a therapeutically effective amount of fullerenes.

Abstract: The main object here is the use of omega-3 polyunsaturated fatty acids (as ethyl esters, hereinafter called “n-3 PUFA”) as a medicament, either alone or in combination with other therapeutic agents, for reducing mortality for a cardiovascular cause, in particular arrhythmia or for reducing hospitalization for any cause, in particular a cardiovascular cause and for the daily administration to patients with symptomatic heart failure (HF) for more than 3.5 years.

Abstract: The present invention relates to application of compounds of formula (1) (Gibberellins) and their derivatives for the preparation of a pharmaceutical composition or medicaments for the treatment of diabetes, its complications and associated conditions, including obesity, micro and macro vascular diseases, nephropathy, neuropathy, eye diseases, diabetic ulcerations and the like. The method results the normalization of serum glucose level and other physiological conditions.

Abstract: The present invention relates to the use of compounds of isopimarane diterpene type, e.g. obtainable as or from extracts from Orthosiphon species, especially certain enriched or purified specific compounds therefrom, as well as said compounds or extracts for use or methods of using said compounds or extracts in the management of cognitive performance; in mammals, especially humans, respectively. The isopimarane diterpene type compounds can be of the formula wherein the symbols are as defined in the description and claims.

Abstract: The invention involves methods for characterizing an individual's risk profile of developing a future cardiovascular disorder by obtaining a level of the marker of systemic inflammation in the individual. The invention also involves methods for evaluating the likelihood that an individual will benefit from treatment with an agent for reducing the risk of future cardiovascular disorder.

Abstract: A drug effective for the treatment and prevention of psychiatric disorders such as schizophrenia, anxiety and related ailments thereof, depression, bipolar disorder and epilepsy. The drug antagonizes the action of group II metabotropic glutamate receptors and shows high activity in oral administration A 2-amino-bicyclo[3.1.0]hexane-2,6-dicarboxylic ester derivative represented by formula [I] [wherein R1 and R2 are identical or different, and each represents a hydrogen atom, a C1-10alkyl group or the like; X represents a hydrogen atom or a fluorine atom; Y represents —OCHR3R4 or the like (wherein R3 and R4 are identical or different, and each represents a hydrogen atom, a C1-10alkyl group or the like; and n represents integer 1 or 2)], a pharmaceutically acceptable salt thereof or a hydrate thereof.

Abstract: The present invention relates to the use of agomelatine, or N-[2-(7-methoxy-1-naphthyl)ethyl]acetamide, on its own or in association, in obtaining medicaments intended for the treatment of bipolar disorders, especially bipolar disorders of types I and II, and more especially bipolar disorders of type I.

Abstract: It is intended to provide a bicyclic ?-amino acid derivative having excellent activity as an ?2? ligand. The present invention provides a compound represented by the general formula (I): wherein R1, R2, R2?, R4, R5, R6, R7, R8, and R8? are a hydrogen atom or the like; and R3 is a hydrogen atom, a halogen atom, a C1-C6 alkyl group, or the like.

Abstract: Disclosed herein are compositions and methods for decreasing vascular permeability in a blood vessel and treating or preventing conditions associated with defects or injuries of vascular endothelium. For example, the disclosed compositions and methods can be used to treat a vascular dysplasia such as cerebral cavernous malformation (CCM). These methods relate generally to the use of compositions that inhibit RhoA GTPase levels or activity, such as inhibitors of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase.

Abstract: The present invention provides a pharmaceutical preparation including a compartment containing a renin inhibitor as a pharmacologically active ingredient, and a compartment containing an HMG-CoA reductase inhibitor as a pharmacologically active ingredient, wherein one compartment is a prior-release compartment and the other compartment is a delayed-release compartment. The combination preparation of the present invention can deliver a renin inhibitor and an HMG-CoA reductase inhibitor with a time interval at a specific speed, thus reducing undesirable side-effects, improving the drug efficacy and promoting the patient compliance. Further, the pharmaceutical preparation of the present invention has pharmacological, clinical, scientific and economical advantages in the prevention or treatment of metabolic syndromes, cardiovascular diseases, renal diseases and the like, as compared with the complex drug regimens in which medicament ingredients are taken individually or simultaneously.