Abstract: The present invention relates to the fields of genetics, immunology and medicine. The present invention more specifically relates to in vitro or ex vivo methods for determining the susceptibility to a cancer treatment of a subject having a tumour. These methods comprise a step of determining the ability of the treatment, of the subject and/or of the tumour to induce an anticancer immune response, the inability of at least one of the treatment, the subject and the tumor to induce an anticancer immune response being indicative of a resistance of the subject to the therapeutic treatment of cancer. Inventors in particular identify genes specific of a human subject or of cancerous cells which can be used to predict or assess the sensitivity of a subject to a treatment of cancer. The invention also relates to particular compounds capable of activating or enhancing the immune system of a particular subject, when the subject is exposed to a therapeutic treatment of cancer or before such an exposition.

Abstract: The present invention relates to novel crystalline forms of naltrexone methobromide including hydrated and solvated forms. The invention also describes methods of preparing the various crystalline forms. The present invention also relates to pharmaceutical compositions containing crystalline forms of naltrexone methobromide, as well as methods of treating or preventing opioid induced side effects by administering the pharmaceutical compositions.

Abstract: The present invention provides a preparation with improved disintegration property, a preparation showing improved bioavailability of a medicament, production methods thereof and the like. A rapidly disintegrating preparation comprising granules comprising a medicament coated with a coating layer containing sugar or sugar alcohol; and a disintegrant. A production method of a rapidly disintegrating preparation including a step of producing granules comprising a medicament, a step of forming a coating layer containing sugar or sugar alcohol on the obtained granules and a step of mixing the coated granules with a disintegrant and molding the mixture.

Abstract: The present invention provides a preparation with improved disintegration property, a preparation showing improved bioavailability of a medicament, production methods thereof and the like. A rapidly disintegrating preparation comprising granules comprising a medicament coated with a coating layer containing sugar or sugar alcohol; and a disintegrant. A production method of a rapidly disintegrating preparation including a step of producing granules comprising a medicament, a step of forming a coating layer containing sugar or sugar alcohol on the obtained granules and a step of mixing the coated granules with a disintegrant and molding the mixture.

Abstract: The invention provides naphthofuran compounds, polymorphs of naphthofuran compounds, naphthofuran compounds in particle form, purified compositions that contain one or more naphthofuran compounds, purified compositions that contain one or more naphthofuran compounds in particle form, methods of producing these naphthofuran compounds, polymorphs, purified compositions and/or particle forms, and methods of using these naphthofuran compounds, polymorphs, purified compositions and/or particle forms to treat subjects in need thereof.

Abstract: The invention provides naphthofuran compounds, polymorphs of naphthofuran compounds, naphthofuran compounds in particle form, purified compositions that contain one or more naphthofuran compounds, purified compositions that contain one or more naphthofuran compounds in particle form, methods of producing these naphthofuran compounds, polymorphs, purified compositions and/or particle forms, and methods of using these naphthofuran compounds, polymorphs, purified compositions and/or particle forms to treat subjects in need thereof.

Abstract: A pharmaceutical composition for use in treating, inhibiting, and/or preventing breast and/or ovarian cancer can include: a molecule having a structure of one of Compounds 1-38, pharmaceutically acceptable salt thereof, or analog thereof; and a pharmaceutically acceptable carrier containing the compound. The pharmaceutically acceptable carrier can be configured for oral, systemic, transdermal, intranasal, suppository, parenteral, intramuscular, intravenous, or subcutaneous administration. The compound can be present in the composition in a therapeutically effective amount for treating, inhibiting, and/or preventing breast and/or ovarian cancer. Also, the compound can be present in a therapeutically effective amount for enhancing production of BRCA1.

Abstract: The present invention relates to methods of treatment of clinical disorders associated with protein aggregation comprising administering, to a subject, an effective amount of an anti-protein aggregate (“APA”) compound selected from the group consisting of pimozide, fluphenazine (e.g., fluphenazine hydrochloride), tamoxifen (e.g., tamoxifen citrate), taxol, cantharidin, cantharidic acid, salts thereof and their structurally related compounds. It is based, at least in part, on the discovery that each of the aforelisted compounds were able to promote degradation of aggregated ATZ protein in a Caenorhabditis elegans model system. According to the invention, treatment with one or more of these APA compounds may be used to ameliorate the symptoms and signs of AT deficiency as well as other disorders marked by protein aggregation, including, but not limited to, Alzheimer's Disease, Parkinson's Disease, and Huntington's Disease.

Abstract: A compound of the formula I, wherein the symbols are as defined in the remaining specification, or a mixture of two or more compounds of the formula I, for use as active ingredient in the therapeutic—including prophylactic—treatment of a warm-blooded animal for the regulation of body weight (preferred) and/or fat loss (preferred) and/or for the management of obesity and/or for improving the total cholesterol HDL/LDL ratio; where the compound(s) of the formula I may be present in free form, in the form of a pharmaceutically and/or nutraceutically acceptable salt, in the form of tautomers, in the form of esters and/or in the form of solvates, as well as related invention embodiments.

Abstract: Therapeutic agents for treatment of Galactosemia and disorders thereof, and other enzyme related disorders thereof are identified. The compounds inhibit galactokinase (GALK) and other kinase activity and are identified by a high throughput screening assay.

Abstract: A composition comprising a cannabinoid receptor binding agent attached to a particle for the treatment of skin conditions. The particle may be a nanoparticle, such as nanocrystalline cellulose. The particle may further be modified with functional moieties. Drug delivery properties may be modified by coating the particles or using vesicles to deliver the cannabinoid receptor binding agent and particle. A substrate may be used to deliver the composition to the skin.

Abstract: Compounds of formula (I): wherein R1, R2, A1, A2, A3, A4, X and Y are as defined herein, are useful as inhibitors of HIV replication.

Abstract: The present disclosure is directed to compositions and methods which utilize the tetracycline scaffold, preferably the scaffold of tetracycline or minocycline, and which significantly lack antibiotic activity. The compounds have neuroprotective attributes without interfering with the drugs capacity to pass through the blood brain barrier. These compounds have neuroprotective activity because of their inhibition of neuronal cell cycle progression. The compounds are characterized in part by a fifth ring joining positions 9 and 10.

Abstract: The present invention relates to the field of therapeutic methods to screen for compounds on the basis of their ability to influence Wnt activity. The screening process is applied to both a physical library of a series of compounds and a virtual library of compounds that affect Wnt activity. In one aspect, the virtual screening process could be carried out where a permutational library of small peptides is substituted for the small organic molecules. The inventive methods may be used to empirically test for effects on Wnt activity and may also be applied to any pair of proteins involved in protein-protein interactions.

Abstract: The present invention is directed at methods for preventing or minimizing the intensity of the serotonin syndrome in humans and lower animals which comprises administering proserotonergic agents and serotonin surge protectors. The present invention is also directed to pharmaceutical compositions comprising proserotonergic agents and serotonin surge protectors useful for carrying out the method of the present invention.

Abstract: Percutaneous absorption preparations which make it possible to absorb compounds having a melatonin receptor agonist activity via a convenient administration system, have favorable blood-drug-concentration-time profile and can exert a therapeutic effect on a disease caused by a decrease in secretion of melatonin at night.

Abstract: The present invention provides a therapeutic agent for substance dependence, which prevents relapse/recurrence of compulsive substance-taking behavior based on craving for addictive substances such as stimulant substances, opioids, barbiturate type anesthetics, hallucinogens, cocaine, hemp, cannabis, alcohol, or volatile organic solvents. (?)-1-(Benzofuran-2-yl)-2-propylaminopentane or a pharmacologically acceptable acid addition salt thereof is useful as a therapeutic agent for substance dependence, which prevents relapse/recurrence of compulsive substance-taking behavior associated with craving for addictive substances.

Abstract: The present invention relates to a composition for treating or preventing hearing loss comprising naphthoquinone-based compounds.

Abstract: GPR120 agonists are provided. These compounds are useful for the treatment of metabolic diseases, including Type II diabetes and diseases associated with poor glycemic control.

Abstract: The present invention provides a preparation with improved disintegration property, a preparation showing improved bioavailability of a medicament, production methods thereof and the like. A rapidly disintegrating preparation comprising granules comprising a medicament coated with a coating layer containing sugar or sugar alcohol; and a disintegrant. A production method of a rapidly disintegrating preparation including a step of producing granules comprising a medicament, a step of forming a coating layer containing sugar or sugar alcohol on the obtained granules and a step of mixing the coated granules with a disintegrant and molding the mixture.

Abstract: The present invention provides methods for attenuating neuronal inflammation and neuronal damage in case of acute or chronic injury of nerve cells of the central nervous system through prostaglandin E2 EP4 receptor activation. Methods for treating neuropathic pain are also provided.

Abstract: Combinations of compounds are provided that produce a synergistic effect when administered.

Abstract: The present invention relates to sodium tanshinone IIA sulfonate hydrates as well as preparation methods and uses thereof. The sodium tanshinone IIA sulfonate hydrates have molecular formula of C19H17NaO6S.nH2O, wherein n=0.5-4.0. The sodium tanshinone IIA sulfonate hydrates of the present invention have better storage stability than anhydrous sodium tanshinone IIA sulfonate.

Abstract: An antimicrobial and/or anti-acne formulation containing either usnic acid or an usnate, together with (a) a primary solvent or solvent system in which the usnic acid or usnate is at least partially dissolved; (b) a glycol; and (c) a hydrophobic fatty acid, fatty alcohol or derivative thereof. The formulation may also contain (d) an alkylene glycol derivative.

Abstract: A pharmaceutical composition for use in treating, inhibiting, and/or preventing breast and/or ovarian cancer can include: a molecule having a structure of one of Compounds 1-38, pharmaceutically acceptable salt thereof, or analog thereof; and a pharmaceutically acceptable carrier containing the compound. The pharmaceutically acceptable carrier can be configured for oral, systemic, transdermal, intranasal, suppository, parenteral, intramuscular, intravenous, or subcutaneous administration. The compound can be present in the composition in a therapeutically effective amount for treating, inhibiting, and/or preventing breast and/or ovarian cancer. Also, the compound can be present in a therapeutically effective amount for enhancing production of BRCA1.

Abstract: The present invention relates to the use of a novel class of cancer stem cell pathway (CSCP) inhibitors; to methods of using such compounds to treat refractory, recurrent, or metastatic cancers; to methods of selective killing cancer cells by using such compounds with specific administration regimen; to methods of targeting cancer stem cells by inhibiting Stat3 pathway; to methods of using novel compounds in the treatment of conditions or disorders in a mammal related to aberrant Stat3 pathway activity; and to processes for preparing such compounds and intermediates thereof, and to the pharmaceutical composition of relevant compounds, and to the specific methods of administration of these compounds.

Abstract: The present invention provides a preparation with improved disintegration property, a preparation showing improved bioavailability of a medicament, production methods thereof and the like. A rapidly disintegrating preparation comprising granules comprising a medicament coated with a coating layer containing sugar or sugar alcohol; and a disintegrant. A production method of a rapidly disintegrating preparation including a step of producing granules comprising a medicament, a step of forming a coating layer containing sugar or sugar alcohol on the obtained granules and a step of mixing the coated granules with a disintegrant and molding the mixture.

Abstract: The use or methods of use of extracts comprising one or more special clerodane compounds against inflammatory (including allergic) diseases or conditions, as well as novel compounds of this type, said clerodane derivatives for use against inflammatory (including allergic) diseases or conditions, pharmaceutical formulations comprising them especially for use against inflammatory disease or conditions, and related embodiments; said extract and/or compound(s) for use in the treatment or in the preparation of a medicament (including a nutraceutical) for the prophylactic and/or therapeutic treatment of said disease or condition, as well as their preparation; pharmaceutical or nutraceutical formulations comprising said extract and/or natural compound(s) which are useful in said prophylactic and/or therapeutic treatment, and related embodiments.

Abstract: This invention concerns novel substituted unsaturated tetracyclic tetrahydrofuran derivatives with binding affinities towards serotonine 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: Disclosed are compounds based on C- and D-ring modifications of triptolide and hydroxylated triptolide, for use in therapy, such as antiproliferative, anticancer, and immunosuppressive therapy.

Abstract: The present invention embraces methods for the diagnosis and treatment of learning or mental disorders, as well as the identification of agents useful in the treatment of such disorders based upon the identified involvement of Sarcoplasmic Ca2+-ATPase type 2 Protein in synaptic plasticity and neurotransmitter release in 22q11 deletion/DiGeorge Syndrome.

Abstract: The present invention relates to novel heterocyclic compounds that are useful as phosphodiesterase inhibitors (PDEs) in particular phosphodiesterase type 4 (PDE IV) inhibitors and phosphodiesterase type 10 (PDE 10) inhibitors, processes for their preparation, pharmaceutical compositions containing them and their use in treating allergic and inflammatory diseases as well as for inhibiting the production of Tumor Necrosis Factor (TNF-?).

Abstract: The invention relates to a method for producing triptolide from a suspension cell culture of Tripterygium sp., to a triptolide-enriched extract obtainable by means of extraction from the culture medium of an in vitro culture of dedifferentiated cells of the species Tripterygium, and to the therapeutic applications of said extract.

Abstract: An object of the present invention is to provide organic solvent extracts of red algae laurencia sp., compounds isolated and identified therefrom, and an agent for preventing attachment of barnacles comprising them. The present invention relates to a barnacle attachment preventive agent consisting of at least one selected from the group consisting of Laurencin, Thyrsiferol, Magireol A, Omaezallene, Hachijojimallene A and organic solvent extracts of red algae laurencia sp.

Abstract: Compounds originally isolated from marine fungi are useful as antifouling (antibacterial and/or anti-larval settlement) agents. The compounds are 3-chloro-2,5-dihydroxy benzyl alcohol, cyclo-(Pro-Phe),3-methyl-N-(2-phenylethyl) butanamide, and succinic acid. The compounds are non-toxic or low-toxic. They can be used alone or in combination, as active ingredients for making environment-friendly antifouling formulations/coatings.

Abstract: The present invention provides for the use of a dimeric phthalide compound, the dimeric phthalide compound has broad anti-tumor activity, can directly inhibit the proliferation of tumor cells and induce cell death, but also indirectly inhibit the development of tumors by suppressing neovascularization. And further, the dimeric phthalide compound can be used alone or in combination to treat cancer, as well as in combination with chemotherapeutics to increase the efficacy of chemotherapeutics and decrease the toxicity of chemotherapeutics.

Abstract: The present invention relates to oral pharmaceutical compositions with controlled and/or programmed release containing at least one active ingredient having antimicrobial and/or anti-infectious activity for the treatment of infections of the large intestine, in particular the colon.

Abstract: Embodiments of the invention are based upon the discovery that exposure of cleavage-stage embryos to a stress inducer, e.g. heat shock or chemical, renders the exposed embryos more sensitive to a secondary treatment with a stress inducer, e.g. heat shock or chemical inducer. Accordingly, the present invention is directed to methods for making embryos, embryonic cells arising from them, and animals and plants that are sensitized to stress, e.g. physiologic or chemical stressors. Methods of screening for inducers and inhibitors of stress using, as test model systems, embryonic cells, embryos, animals, and plants that are sensitized to stress are also disclosed.

Abstract: The present invention is directed to the use of EP2 and/or EP4 agonists as therapeutics for the treatment of diseases associated with influenza A viruses, such as for example H5N1 and mutations thereof.

Abstract: Therapeutics which employ a combination of an antiviral agent and an EP4 receptor agonist for the treatment of human respiratory diseases associated with viral infections are described. Viral infections may include an influenza A virus, for example H1N1, H3N2 and H5N1, and mutations thereof, and/or a coronavirus, for example a virus that causes severe acute respiratory syndrome, “SARS”.

Abstract: The present invention relates to benzofuro[3,2-c]pyridine and azepine analogs as serotonin sub-type 6 (5-HT6) modulators, pharmaceutical compositions including these compounds, methods of preparation, and use thereof. These compounds are useful in the treatment of central nervous system disorders including obesity, metabolic syndrome, cognition, schizophrenia, attention deficit hyperactivity disorder, bipolar disorder, rare and orphan diseases, and sleep disorders. The subject compounds have the structure of formula (I) with the substituents being described herein.

Abstract: The present invention provides compounds of the formula (I) or a pharmaceutically acceptable salt, ester or prodrug thereof.

Abstract: Disclosed in certain embodiments is a pharmaceutical packaging system comprising: a receptacle comprising an openable seal for accessing the interior of the receptacle; a pharmaceutical dosage form contained in the receptacle; and an activatable color-changing material, wherein upon activation, the material exhibits a visually discernible color change upon the lapsing of a predetermined time period.

Abstract: The present invention relates to compounds of formual (I): wherein Y is a single bond or double bound; and R1 is —C(CH3)C2H5 or —C(CH3)?CHCH3, when Y is a single bound; R1 is —C(CH3)?CH2, is —C(CH3)2, —C(CH3)?CHCH3, —C(CH3)C2H5, or —CH2C(CH3)2, when Y is a double bound. These compounds are bombesin receptor subtype 3 (BRS3) modulating agents, more specifically that they are BRS3 agonists. The invention is also related to the use of such compounds to treat diseases associated with inappropriate BRS3 activity.

Abstract: Provided herein are methods, drug formulations, and dosing regimens for improving cognitive function in a normal or cognitively impaired subject. For instance, methods provided herein comprise administering a GABAA receptor antagonist so that peak concentration of the GABAA receptor antagonist occurs when the subject is asleep.

Abstract: Methods of treating lung diseases comprising administering inducers of NAD(P)H:quinone oxidoreductase 1 (NQO1) are disclosed. Inducers of NQO1 include naphthoquinones such as ?-lapachone. Methods of predicting whether a subject with a lung disease will respond to treatment with a naphthoquinone are also described herein.

Abstract: The subject application provides small compounds that are able to increase/enhance autophagy in various cells. These compounds are useful in augmenting existing treatments of various cancers, microbial/viral infections, and neurodegenerative diseases. Thus, the subject application also provides methods of treating various types of cancers, microbial/viral infections, and neurodegenerative diseases.

Abstract: Cadherin-11 inhibitors and methods for the prevention and treatment of cadherin-11 related diseases are described herein. Cadherin-11 related diseases include cancer and rheumatoid arthritis.

Abstract: In accordance with the present invention, novel methods and formulations are provided for treating and preventing the incidence of drug-induced pro-arrhythmia, including torsades de pointes. The methods and formulations comprise a combination of a drug that induces torsade de pointes, such as Class III antiarrhythmics, certain antimicrobials, antihistamines, antidepressants, antipsychotics, diuretics, with an aspirin and/or a statin. In certain embodiments, the compositions and methods for treatment comprise azimilide and aspirin and/or a statin. These compositions may be administered by different routes, including orally. In certain embodiments where the antiarrhythmic is azimilide it may be administered orally in a dose of about 25 mg to about 300 mg.

Abstract: The present invention provides a therapeutic agent and methods thereof for the treatment for irritable bowel syndrome. The agent comprises a compound represented by formula (I): wherein, R1 represents an optionally substituted hydrocarbon group, etc., R2 represents a hydrogen atom or an optionally substituted hydrocarbon group, R3 represents a hydrogen atom, an optionally substituted hydrocarbon group, etc., X represents CHR4, NR4, CO, O or S (wherein, R4 represents a hydrogen atom, an optionally substituted hydrocarbon group, etc.), Y represents C, CH or N, represents a single bond or double bond, ring A represents an optionally substituted 5- to 7-membered oxygen-containing heterocyclic ring, ring B represents an optionally substituted benzene ring, and m represents an integer of 1 to 4, or a salt thereof, wherein the compound represented by formula (I) or a salt thereof is (S)—N-[2-(1,6,7,8-tetrahydro-2H-indeno[5,4-b]furan-8-yl)ethyl]propionamide.