Abstract: Provided are compounds which generally have a triketone structure. Examples of the compounds include derivatives of 1,3-cyclohexanedione, such as: 1,3-cyclohexanedione, 2-propanoyl-5-cyclohexyl-; 1,3-cyclohexanedione, 2-propanoyl-5-[4-fluorophenyl]-; 1,3-cyclohexanedione, 2-acetyl-5-[thien-2-yl]-; 1,3-cyclohexanedione, 2-acetyl-5-butyl-; and 1,3-cyclohexanedione, 2-propanoyl-5-[bicyclo[2.2.1]hept-2-en-5-yl]-. The compounds can be used to alter the lifespan of eukaryotic organisms and treat inflammation.

Abstract: The present invention relates to new biphenyl-3-carboxylic acid modulators of beta-3-adrenoceptor activity, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: Compounds of the formula (I), in which Het, R, X, Y, R1 and p have the meanings indicated in claim 1, are autotaxin inhibitors and can be employed for the treatment of tumors.

Abstract: Treating Sonic Hedgehog-Associated Medulloblastoma comprises inhibiting the synthesis or biologic activity of leukotrienes that drive Nestin expression in cancerous or precancerous granule neuron precursors and that further drive growth and proliferation of medulloblastoma cells through Nestin-mediated aberrant Sonic Hedgehog signaling.

Abstract: An improved pharmaceutical formulation for oral administration includes a therapeutically effective quantity of an active ingredient and a stabilizer. The active ingredient is Fluvastatin, or pharmaceutically acceptable salts thereof, and the stabilizer is a mixture of Carrageenans. The stabilizer inhibits isomerization, and/or elimination, and/or oxidation and/or recrystallization of the active ingredient.

Abstract: Provided herein are methods for identifying a cancer patient at risk for resistance to an HDAC inhibitor therapy, comprising obtaining a tumor sample from the cancer patient; detecting the presence of Testis-specific Y-encoded-like protein 5 (TSPYL5) expression in the sample; quantifying a level of the TSPYL5 expression in the sample, wherein a high level of the TSPYL5 expression, relative to a defined expression threshold of the TSPYL5, correlates with resistance to the HDAC inhibitor therapy; and applying the correlation to identify the cancer patient at risk for resistance to the HDAC inhibitor therapy.

Abstract: The invention relates to FSH receptor antagonist according to general formula I or a pharmaceutically acceptable salt thereof and to a pharmaceutical composition containing the same. The compounds can be used for the treatment and prevention of endometriosis, for the treatment and prevention of pre-menopausal and peri-menopausal hormone-dependent breast cancer, for contraception, and for the treatment of uterine fibroids and other menstrual-related disorders.

Abstract: The present invention provides compounds useful as agents for the prevention or treatment of a disease associated with abnormal serum uric acid level which has a uricosuric activity or the like. The present invention relates to (aza)indole derivatives represented by the following general formula (I) having xanthine oxidase inhibitory activities and useful as agents for the prevention or treatment of a disease associated with abnormality of serum uric acid level, prodrugs thereof, or salts thereof.

Abstract: The present invention is directed to novel indole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor.

Abstract: Oral dosage forms as a biodegradable, water soluble film for delivering pharmaceutically active agents, to patients through insertion into the mouth of patient and methods for administering pharmaceutically active agents to patients by insertion into the mouth to provide selective uptake of said agents through the mucosa and thus avoiding the gastrointestinal tract.

Abstract: The invention relates to the use of melatonin, either alone or in combination with at least one compound selected from the group consisting of L-arginine, a physiologically acceptable salt thereof, one or more other physiologically acceptable compounds associated with the synthesis of nitric oxide and mixtures thereof, for the manufacture of a medicament for the therapeutic treatment, prophylactic treatment and/or prevention of postoperative infectious and/or non-infections complications induced by surgical interventions wherein the infectious complications may be pneumonia, wound infection (wound dehiscence), intra-abdominal abscess, and urinary tract infections (UTI) or wherein the non-infectious complication may be anastomotic leak, a pharmaceutical formulation comprising melatonin and at least one compound selected from the group consisting of L-arginine, a physiologically acceptable salt thereof, one or more other physiologically acceptable compounds associated with the synthesis of nitric oxide and mixt

Abstract: Molecular mimics of Smac are capable of modulating apoptosis through their interaction with cellular IAPs (inhibitor of apoptosis proteins). The mimetics are based on a monomer or dimer of the N-terminal tetrapeptide of IAP-binding proteins, such as Smac/DIABLO, Hid, Grim and Reaper, which interact with a specific surface groove of IAP. Also disclosed are methods of using these peptidomimetics for therapeutic purposes. In various embodiments of the invention the Smac mimetics of the invention are combined with chemotherapeutic agents, including, but not limited to topoisomerase inhibitors, kinase inhibitors, NSAIDs, taxanes and platinum containing compounds use broader language.

Abstract: The present invention provides biaryl oxyacetic acid compounds which may be useful for treating inflammatory disorders, including disorders affecting the respiratory system and skin.

Abstract: Disclosed herein is a species of peptide and non-peptide inhibitors of Akt, an oncogenic protein. Beginning with a residue of Akt target substrate GSK-3, the functional domains of the GSK-3 residue were characterized. Functionally homologous non-peptide groups were substituted for the amino acids of the GSK-3 creating a hybrid peptide-non-peptide and non-peptide compounds capable of binding to Akt. The non-peptide compounds show increased stability and rigidity compared to peptide counterparts and are less susceptible to degradation. The bound non-peptide compounds exhibit an inhibitory effect on Akt, similar to peptide-based Akt inhibitors.

Abstract: The present invention discloses a stable pharmaceutical composition comprising: (a) plurality of granules comprising silodosin or salts thereof and one or more pharmaceutical excipients; and (b) an extragranular portion comprising one or more lubricants and optionally one or more surfactants, wherein the granules are free of partially pregelatinized starch.

Abstract: The present invention relates to the use of a composition comprising melatonin or a derivative thereof at a proportion of 2.5% to 5% w/v for preparing a pharmaceutical composition for treating and/or preventing mucositis. The mucositis is preferably caused by radiotherapy and/or chemotherapy and preferably refers to oral mucositis.

Abstract: The present invention relates to new formulations containing one or more estrogens and 2-Phenyl-1-[4-(2-Aminoethoxy)-Benzyl]-Indole compounds which are useful as estrogenic agents, as well as pharmaceutical compositions and methods of treatment utilizing these compounds, which have the general structures below:

Abstract: The present invention provides a compound represented by the general formula (I) of the present invention, which has EP1 receptor antagonism: wherein A represents a benzene ring, a pyridine ring, or the like; Y1 represents a C1-6 alkylene group or the like; Y2 represents a single bond or the like; Z represents —C(?O)—NHSO2R6, an acidic 5-membered hetero ring group, or the like; R1 represents a hydrogen atom or the like; R2 represents a phenyl group, a 5-membered aromatic heterocyclic group, or the like; R3 represents a halogen atom, a C1-6 alkoxy group, or the like; R4 represents a hydrogen atom, a halogen atom, or the like; R5 represents a hydrogen atom or the like; and R6 represents a C1-6 alkyl group or the like], or a pharmaceutically acceptable salt thereof. Furthermore, the compound (I) of the present invention can be used as an agent for treating or preventing LUTS, in particular, various symptoms of OABs.

Abstract: The present invention relates to the use of derivatives of indoles having a general formula (I) as follow: for the manufacture of a pharmaceutical composition intended for the treatment of cancer.

Abstract: Disclosed herein are new heterocyclic compounds and compositions and their application as pharmaceuticals for the treatment of disease. Methods of inhibiting PAS Kinase (PASK) activity in a human or animal subject are also provided for the treatment of diseases such as diabetes mellitus.

Abstract: The present invention provides a method of inhibiting, suppressing or preventing levodopa-induced dyskinesia in a patient suffering from Parkinson's Disease, comprising the step of administering to the patient a pharmaceutical composition comprising at least one compound of the invention. The present invention further provides a method of inhibiting, suppressing or preventing Parkinson's Disease in a patient, comprising the step of administering to the patient a pharmaceutical composition comprising at least one compound of the invention.

Abstract: The present invention provides a fused heterocyclic compound having an ROR?t inhibitory action. The present invention relates to a compound represented by the formula (I?): wherein each symbol is as defined in the specification, provided that 2-(2-((4-cyanophenyl)amino)-2-oxoethoxy)-N-(9-ethyl-9H-carbazol-3-yl)acetamide and N-(4-cyanophenyl)-N?-(9-ethyl-9H-carbazol-3-yl)-3-methylpentanediamide are excluded, or a salt thereof.

Abstract: The present invention provides a method of inhibiting, suppressing or preventing levodopa-induced dyskinesia in a patient suffering from Parkinson's Disease, comprising the step of administering to the patient a pharmaceutical composition comprising at least one compound of the invention. The present invention further provides a method of inhibiting, suppressing or preventing Parkinson's Disease in a patient, comprising the step of administering to the patient a pharmaceutical composition comprising at least one compound of the invention.

Abstract: Disclosed are methods to treat allergic conditions, including pulmonary and non-pulmonary conditions, in a subject by administering a composition that inhibits Pim kinase. Also disclosed are methods to treat allergic conditions in a subject by administering a composition that induces expression of Runx3.

Abstract: IAP binding molecules and compositions including these are disclosed. The IAP binding molecules interact with IAPB (inhibitor of apoptosis proteins) in cells and may be used to modify apoptosis in cells treated with such molecules. Embodiments of these compounds have a Kd of less than 0.1 micromolar. Methods of using these IAP binding molecules for therapeutic, diagnostic, and assay purposed are also disclosed.

Abstract: The present invention provides a compound represented by the general formula (I) of the present invention, which has EP1 receptor antagonism: wherein A represents a pyridine ring, a furan ring, or the like; Y1 represents a C1-6 alkylene group; Y2 represents a single bond or the like; R1 represents —C(?O)—NH—SO2R6, an acidic 5-membered hetero ring group, or the like; R2 represents an optionally substituted phenyl group, an optionally substituted 5-membered aromatic heterocyclic group, or the like; R3 represents a halogen atom, a C1-6 alkoxy group, or the like; R4 represents a hydrogen atom, a halogen atom, or the like; R5 represents a hydrogen atom or the like; and R6 represents a C1-6 alkyl group or the like], and a pharmaceutically acceptable salt thereof. Furthermore, the compound (I) of the present invention can be used as an agent for treating or preventing LUTS, in particular, various symptoms of OABs.

Abstract: The present invention provides pharmaceutical compositions comprising substituted 1,4 naphthoquinones that are effective in preventing oligomerization of beta amyloid and subsequent pathologies associated with amyloid fibrils. These compositions are useful for the treatment of disease involving amyloidogenesis including neurodegenerative diseases such as Alzheimer's Disease or senile dementia. Particularly effective compositions comprise 1,4 naphthoquinones substituted with an amino acid residue selected from a heterocyclic or aromatic amino acid.

Abstract: Zanthoxylum piperitum (commonly known as Japanese pepper) seeds, including its mature seeds, contain the NMS precursor N-methylserotonin S-O-6-glucoside (“NMS-glucoside”) present in sufficient concentration and are metabolized with sufficient efficiency so as to provide an effective amount of NMS for use in amelioration of menopausal symptoms, including hot flashes/flushes. The Japanese pepper seeds or Japanese pepper seed extracts can also be used to enrich other sources of NMS or NMS precursors in order to provide a nutraceutical or food supplement for controlling hot flashes. This invention relates to the marketing of nutraceuticals and food supplements containing these ingredients. Target customers include perimenopausal women, menopausal women and post menopausal women who wish to reduce the risk of experiencing hot flashes.

Abstract: Disclosed are compounds and compositions of the formula I as described herein which are inhibitors of MMP-13. Also disclosed are methods of using and making compounds of the formula I.

Abstract: A particularly constructed tamoxifen-melatonin hybrid ligand gives new and unexpectedly improved results in the prevention and treatment of cancer, particularly breast cancer. The hybrid ligand comprises either tamoxifen or 4-hydroxytamoxifen and also melatonin, with the tamoxifen or 4-hydroxytamoxifen and melatonin's being linked by an unsubstituted C2-C6 alkyl linker between the tamoxifen amine and the carbonyl of melatonin.

Abstract: The invention relates to formulations for topical use comprising an antiseborrheic agent and an antimicrobial and/or antibacterial agent for the treatment of inflammatory dermatoses. In particular said formulations comprise melatonin and an antimicrobial or antibacterial agent, can be used in the pharmaceutical, cosmetic/cosmeceutical or dermatological field and are particularly suitable for the treatment of acne and of the clinical symptoms associated thereto.

Abstract: Buccal aerosol sprays or capsules using polar and non-polar solvent have now been developed which provide biologically active compounds for rapid absorption through the oral mucosa, resulting in fast onset of effect. The buccal polar compositions of the invention comprise formulation I: aqueous polar solvent, active compound, and optional flavoring agent; formulation II; aqueous polar solvent, active compound, optionally flavoring agent, and propellant; formulation III: non-polar solvent, active compound, and optional flavoring agent; and formulation IV: non-polar solvent, active compound, optional flavoring agent, and propellant.

Abstract: Small molecules are used to inhibit specific receptor-ligand interaction between Alzheimer's amyloid-? peptide (A?) and Receptor for Advanced Gly-cation Endproducts (RAGE). Objectives include treating Alzheimer's disease and other pathologies involving cerebral amyloid angiopathy; improving blood flow to or within the brain; decreasing the level of A? in the brain; reducing neuropathology associated with Alzheimer's disease; reducing inflammation and/or oxidant stress in the brain; improving memory and/or learning; treating other conditions involving A?/RAGE interaction at the blood-brain barrier, RAGE-mediated transport of A? into the brain, or RAGE activation in brain vasculature and/or brain parenchyma (e.g., diabetic complications); or any combination thereof.

Abstract: A method for treating a disorder of the central nervous system includes administering to the respiratory tract of a patient a drug which is delivered to the pulmonary system, for instance to the alveoli or the deep lung. The drug is administered at a dose which is at least about two-fold less than the dose required by oral administration. Particles that include the drug can be employed. Preferred particles have a tap density of less than about 0.4 g/cm3. In addition to the medicament, the particles can include other materials such as, for example, phospholipids, amino acids, combinations thereof and others.

Abstract: The present invention relates to a method of treating a cachexia and/or sarcopenia with an oral dose of S-pindolol or a pharmaceutical formulation thereof and to an oral formulation for use in said method of treatment. The method and oral formulation comprise administering a total daily dose of 2.5 to 20 mg of S-pindolol or a pharmaceutical formulation comprising the same.

Abstract: Described herein are compounds, pharmaceutical compositions and methods for inhibiting the expression of a vitamin D receptor target gene, inhibiting interactions between the vitamin D receptor and at least one vitamin D receptor coactivator, for treating cancer in a subject, and for inhibiting angiogenesis in a subject.

Abstract: A pharmaceutical composition for treating cancer, in particular drug resistant cancer, comprising an effective amount of bifunctional alkylating agent, an effective amount of a DNA repair inhibitor, and a pharmaceutically acceptable carrier.

Abstract: This invention relates to a novel class of compounds which are cysteine protease inhibitors, including but not limited to, inhibitors of cathepsins K, L, S and B. These compounds are useful for treating diseases in which inhibition of bone resorption is indicated, such as osteoporosis.

Abstract: Provided herein are compounds having anti-proliferative effect. Also provided are compounds that can modulate the activity of multi-domain proteins comprising a dimerization arm and interdomain tether, such as EGFR, where an untethered, extended conformation is the active state and a tethered conformation is the inactive state, resulting in an autoinhibited configuration. Also provided are methods and pharmacophores for identifying such compounds. Other aspects provide methods or therapeutic treatment for proliferative diseases, disorders, or conditions, such as those associated with EGFR.

Abstract: The present invention provides a composition for controlling harmful arthropods having an excellent control efficacy on harmful arthropods. A composition for controlling harmful arthropods comprising an amide compound represented by a formula (I); wherein each of symbols are the same as defined in the Description; or salts thereof and at least one kind of neonicotinoid compounds selected from the group (A) consisting of imidacloprid, clothianidin, thiamethoxiam, dinotefuran, acetamiprid, thiacloprid and nitenpyram, shows an excellent controlling efficacy on harmful arthropods.

Abstract: Methods of alleviating the symptoms of hemoglobinopathies, including, but not limited to, sickle cell disease, ?-thalassemia, and hemoglobin H disease are provided. In some embodiments, the methods comprise administering an inhibitor selected from an ERK inhibitor, a MEK inhibitor, and a Raf inhibitor. Methods of inhibiting adhesion of sickle red blood cells to endothelial cells are also provided.

Abstract: The present invention provides compounds of formula (I); or pharmaceutically acceptable salts thereof, wherein the variables are defined as herein. The present invention provides a method for manufacturing the compounds of formula (I), their therapeutic uses, combinations with other of pharmacologically active agents, and a pharmaceutical compositions.

Abstract: A tablet that rapidly disintegrates in the oral cavity comprising a compressed blend of rapidly dispersing microgranules prepared by granulating a sugar alcohol or a saccharide or a mixture thereof having an average particle size less than about 30 microns and a disintegrant, and a taste-masked microcapsule containing at least one drug, the microcapsule being prepared by granulating a pharmaceutically acceptable formulation comprising at least one drug in a therapeutically effective amount and at least one polymeric binder that improves resilience of the microgranules, wet milling the granulated mass, and microencapsulating the milled granules to provide microcapsules.

Abstract: In alternative embodiments the invention provides compositions, e.g., pharmaceutical compositions and preparations, formulations, kits and other products of manufacture, e.g., exemplary drug combinations packaged together or separately in blister packs, lidded blisters or blister cards, or wrapped in paper, plastic or cellophane wrappers (e.g., a shrink wrap), comprising a combination regimen of at least two active ingredients designed to diminish systemic inflammation by targeting (inhibiting) two different, but convergent, signaling pathways, i.e., the sympathetic nervous system and the lipid-derived autacoid system; and methods for making and using these compositions. In alternative embodiments, the compositions of the invention (e.g., the combination of drugs) are used to ameliorate, diminish, treat, block or prevent an inflammatory response secondary to an infection, e.g., a viral infection and/or a reactivation.

Abstract: A method of treating a human subject in need of melatonin therapy comprises administering to a human subject a composition comprising melatonin dispersed in a polymer matrix adapted to cover the melatonin in a melatonin solubility enhancing pH environment after ingestion and to maintain the melatonin solubility enhancing pH environment when said composition is present in said subject's intestines so that an effective amount of melatonin is released into the subject's intestines.

Abstract: The invention provides a method of enhancing the efficacy of antibiotic treatment of tuberculosis, trypanosomiasis, leprosy, and leishmaniasis involving co-administering to a mammal undergoing antibiotic treatment therapeutically effective amounts of a first compound that is an inhibitor of 5-lipoxygenase and optionally a second compound that is a product of the cyclooxygenase pathways. The invention also provides a pharmaceutical composition comprising an antibiotic, an inhibitor of 5-lipoxygenase, and a product of the cyclooxygenase pathways.

Abstract: A melatonin-containing product includes a composition comprising melatonin, a pH lowering agent, and a gel-forming forming polymer. When ingested, the composition forms an acidic aqueous gel matrix having melatonin dissolved therein for releasing melatonin into the intestines for a sustained time period.

Abstract: The present invention relates to polymorphic forms of a compound of formula A: This compound is useful as a glucagon receptor antagonist and serves as a pharmaceutically active ingredient for the treatment of type 2 diabetes and related conditions, such as hyperglycemia, obesity, dyslipidemia, and the metabolic syndrome. Hydrates, hemihydrates, anhydrates and similar polymorphic forms are included.

Abstract: Improved pharmacokinetic profiles for the iontophoretic delivery of sumatriptan are described.

Abstract: An agent for the prophylaxis or treatment of stress urinary incontinence, which contains a substance that activates a serotonin 5-HT2C receptor, an agent for the prophylaxis or treatment of stress urinary incontinence, which contains a substance that stimulates an androgen binding site, and a method of screening for a drug for the prophylaxis or treatment of abdominal pressure incontinence, which includes electrostimulating the abdominal muscles or a nerve controlling them of an animal to increase the abdominal pressure, and measuring the leak point pressure at that time.