Abstract: A series of new 6-piperazinyl-3,4-dihydroquinazolin-2(1H)-ones have been synthesized. The compounds are structurally related to adoprazine, a potential atypical antipsychotics bearing potent D2 receptor antagonist and 5-HT1A receptor agonist properties. Buchwald-Hartwig coupling of suitably modified aryl bromides with tert-butyl piperazine-1-carboxylate afforded the advanced intermediate piperazinyl-3,4-dihydroquinazolin-2(1H)-one. The reductive amination of the latter with appropriately designed biarylaldehydes accomplished the synthesis of these compounds.

Abstract: The present invention generally relates to protein signalling. In particular, compounds that inhibit the Wnt protein signalling pathway are disclosed. Such compounds may be used in the treatment of Wnt protein signalling-related diseases and conditions such as cancer, degenerative diseases, type II diabetes and osteopetrosis.

Abstract: The present invention relates to compounds and compositions useful for inhibiting and/or reducing platelet deposition, adhesion and/or aggregation. The present invention further relates to methods for the treatment or prophylaxis of thrombotic disorders, including stroke, myocardial infarction, unstable angina, peripheral vascular disease, abrupt closure following angioplasty or stent placement and thrombosis as a result of vascular surgery.

Abstract: Compositions and methods for treating preeclampsia in a subject in need thereof are disclosed.

Abstract: The invention relates to the administration of inhibitors of phosphodiesterase 1 (PDE1) for the treatment of diseases or disorders characterized by disruption of or damage to various cGMP/PKG mediated pathways. In one embodiment the invention relates to inhibitors of phosphodiesterase 1 (PDE1) for treatment of cardiovascular disease and related disorders, e.g., congestive heart disease, atherosclerosis, myocardial infarction, and stroke.

Abstract: The present invention relates to chemical compounds of Formula (I) are as herein defined, pharmaceutical compositions, and methods of use in the treatment of conditions or disorders mediated by TNF-? or by PDE4, including but not limited to rheumatoid arthritis.

Abstract: Described herein is pyrrolo {2,3-d}pyrimidine compounds, their use as Janus Kinase (JAK) inhibitors, pharmaceutical compositions containing this compounds, and methods for the preparation of these compounds.

Abstract: The present invention provides an anticancer adjuvant containing pentoxifylline. Pentoxifylline inhibits a collagen synthesis in tumors and consequently increases the distribution of an anticancer drug or sensitivity of cancer cells, which thus provides an improved anticancer treatment effect.

Abstract: The present invention relates to compositions containing stimulant and anti-histamine compounds, to methods for treating symptoms related to inflammation using the combination compounds, and to a method for preparing the compositions.

Abstract: Compositions and methods for treating disordered and/or prodromal stage tissue infected with by a virus in a mammal by co-administering a systemic anti-virus drug and topically administered anti-infective composition. The systemic anti-virus drug is internally administered and disrupts or inhibits virus replication systemically within the mammal. Examples include nucleoside analogues, nucleoside analogue precursors, and nucleotide analogues. The topically administered anti-infective composition includes at least one anti-infective agent, such as an organohalide (e.g., benzalkonium chloride), and is formulated to penetrate below the skin surface and allow the anti-infective agent to kill viruses at a treatment site. The topical anti-infective composition enhances efficacy of the systemic anti-virus drug and reduces the time and/or number of dosages otherwise required for the systemic anti-virus drug to treat the viral infection.

Abstract: Disclosed is the use of an inverse agonist for alpha-subunit-containing gamma-aminobutyric acid A receptor in the preparation of a medicine for the prevention, alleviation, or treatment of pain.

Abstract: The present invention includes compositions that are useful in the treatment of breathing control diseases or disorders in a subject in need thereof. The present invention also includes a method of treating a respiratory disease or disorder in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of a pharmaceutical formulation of the invention. The present invention further includes a method of preventing destabilization or stabilizing breathing rhythm in a subject in need thereof, comprising administering to the subject a therapeutically effective amount of a pharmaceutical formulation of the invention.

Abstract: Methods for inhibiting translation, treating a cellular proliferative disorder, and inhibiting proliferation of cells using the compounds disclosed herein are provided.

Abstract: Disubstituted 3,4-diamino-3-cyclobutene-1,2-dione compounds represented by the general formula (I) are described. Also described, are pharmaceutical compositions including these compounds and the use of these compounds and compositions for the treatment of chemokine-mediated pathologies.

Abstract: Disclosed are nordihydroguaiarctic acid derivative compounds including various end groups bonded by a carbon atom or heteroatom though a side chain bonded to the respective hydroxy residue O groups by an ether bond or a carbamate bond, pharmaceutical compositions, methods of making them, and methods of using them and kits including them for the treatment of diseases and disorders, in particular, diseases resulting from or associated with a virus infection, such as HIV infection, HPV infection, or HSV infection, an inflammatory disease, such as various types of arthritis and inflammatory bowel diseases, a metabolic disease, such as diabetes, a vascular disease, such as hypertension and macular degeneration, or a proliferative disease, such as diverse types of cancers.

Abstract: Disclosed are compounds that modulate the physiological action of the proprotein convertase subtilisin kexin type 9 (PCSK9), as well as therapeutic methods for use of such compounds to reduce LDL-cholesterol levels and/or for the treatment and/or prevention of cardiovascular disease (CVD), including treatment of hypercholesterolemia. Examples of compounds include thiadiazole, isoxazole, 1,2,4-triazole, thiazole, indole, pyrazole, and pyrrolinone derivatives.

Abstract: The invention relates to 2-(R2-thio)-10-[3-(4-R1-piperazin-1-yl)propyl]- 10H-phenothiazine according to general formula I, for treating a ?-amyloidopathy or an ?-synucleinopathy accompanied by a cerebral protein deposit and a reduced activity of the cerebral ABCC1-transporter. The invention also relates to a method for the diagnosis or prediagnosis of a ?-amyloidopathy or an ?-synucleopathy accompanied by a cerebral protein deposit and a reduced activity of the cerebral ABCC1-transporter, or for determining the risk of a proband suffering from such an illness, the proband already having accumulated substances transported by the cerebral ABCC1 transporter.

Abstract: Methods of treating and or preventing substance abuse/dependence, and alcohol abuse/dependence in particular. Combinations of medications are also disclosed.

Abstract: The present invention relates to a stable pharmaceutical composition of amiodipine and benazepril or salts thereof. In particular, the invention relates to a stable pharmaceutical composition comprising at least one amiodipine component and at least two benazepril components in which physical contact between amiodipine and benazepril components is limited. The invention also includes a process of preparing such compositions and method of treating hypertension by administering the composition to a patient in need thereof.

Abstract: Nanoparticles containing a photosensitizer configured to generate a reactive oxygen species when exposed to an appropriate wavelength of light can be used to enhance immunogenicity of cancer cells, such as breast cancer cells. Such enhanced immunogenicity cancer cells, or supernatants thereof, can be used to activate dendritic cells or cause dendritic cells to produce INF-gamma. Nanoparticles having mitochondria-targeting moieties are more effective at enhancing the immunogenicity of the cancer cells, or causing the dendritic cells to produce IFN-gamma, than nanoparticle lacking mitochondria-targeting moieties or free photo sensitizer.

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: Aqueous suspension formulations containing dexamethasone and ciprofloxacin are disclosed for the treatment of middle ear infections in human patients having an open tympanic membrane.

Abstract: The present disclosure relates to the compound having the following formula (I): which may be in base form or in the form of a hydrate or a solvate, in combination with prednisone or prednisolone, for its use for the treatment of castration resistant or hormone-refractory metastatic prostate cancer in patients not at risk of developing gastrointestinal disorders chosen from the group consisting of: gastrointestinal bleeding and perforation, gastritis, enterocolitis, neutropenic enterocolitis, colitis, intestinal obstruction, and ileus.

Abstract: Zhankuic acid A (ZAA) is the major pharmacologically active compound of Taiwanofungus camphoratus. We analyzed the structure of human TLR4/MD-2 complex with ZAA by X-score and HotLig modeling approaches. Two antibodies against MD-2 were used to verify the MD-2/ZAA interaction. The inflammation and survival of the mice pretreated with ZAA and injected with LPS were monitored. The modeling structure shows that ZAA binds the MD-2 hydrophobic pocket exclusively via specific molecular recognition; the contact interface is dominated by hydrophobic interactions. Binding of ZAA to MD-2 reduced antibody recognition to native MD-2, similar to the effect of LPS binding. Furthermore, ZAA significantly ameliorated LPS-induced endotoxemia and Salmonella-induced diarrhea in mice. Our results indicate that ZAA, which can compete with LPS for binding to MD-2 as a TLR4/MD-2 antagonist, is a potential therapeutic agent for Gram-negative bacterial infections.

Abstract: Disclosed herein are methods of treating fungal infections in a patient, comprising identifying a patient in need of treatment and administering a therapeutically effective amount of at least one cationic steroid antimicrobial (CSA), or a pharmaceutically acceptable salt thereof. Kits comprising such compositions and instructions on such methods are also contemplated herein.

Abstract: Disclosed are methods for increasing the rate of healing of a tissue wound by administering a composition including a therapeutically effective amount of at least one cationic steroid antimicrobial (CSA). Also disclosed herein are methods of promoting wound healing in a subject in need of such promotion, comprising administering a composition comprising a therapeutically effective amount of at least one CSA. Additionally, disclosed herein are compounds and compositions comprising at least one CSA, or a pharmaceutically acceptable salt thereof, for use in the treatment of a tissue wound. Kits comprising such compositions and instructions on such methods are also contemplated herein.

Abstract: Described herein are methods and compositions for the treatment of prostate cancer in a subject in need thereof. The prostate cancer may be a castration resistant and an androgen receptor antagonist-resistant prostate cancer. The methods may comprise administering to the subject a CYP17-lyase inhibitor of Formula II.

Abstract: An oral dosage form comprising a single dose of 25-hydroxy-vitamin D3 sufficient to elevate the serum level in a human to a concentration in the range of 30 ng/ml to 200 ng/ml for at least 7 days and a pharmaceutically suitable oral carrier system, wherein subsequent single doses at least every 7 days are sufficient to sustain the serum level in a human to a concentration in the range of 30 ng/ml to 200 ng/ml at steady-state pharmacokinetics is disclosed.

Abstract: Methods of using azide-modified biomolecules, such as fatty acids, carbohydrates and lipids, to treat a plant, an insect or an animal infected with a virus or to inhibit infectivity of a virus, such as the human immunodeficiency virus, are provided. Also provided are methods of labeling a virus, such as human immunodeficiency virus, with an azide-modified biomolecule, such as a fatty acid, a carbohydrate, or an isoprenoid lipid. Also, provided are methods of tracking a virus in vivo, with an azide-modified biomolecule, such as a fatty acid, a carbohydrate, or an isoprenoid lipid. The azide-modified biomolecules may be combined with a pharmaceutically acceptable excipient to produce a pharmaceutical composition, optionally containing another anti-viral agent and/or a delivery agent, such as a liposome.

Abstract: A method for providing a therapeutic benefit for a subject having a cancer is provided. A compound with an arene ruthenium (II) compound with an iminophosphorane ligand is administered to the subject.

Abstract: Methods and compositions for treating and preventing intestinal injury are described. In particular, methods and delayed-release enteric coated compositions of glycerophosphate salts for treating and preventing an intestinal injury, such as exercise-induced intestinal injury, intestinal injury induced or aggravated by ingestion of a nonsteroidal anti-inflammatory drug (NSAID), or exercise-induced intestinal injury aggravated by an NSAID, are described. Orally or nasally administering a therapeutically effective amount of a glycerophosphate salt, particularly calcium glycerophosphate, to a subject engaging in exercise, particularly a subject engaging in exercise and ingesting a NSAID for the treatment or prevention of musculoskeletal pain resulting from exercise, reduces exercise-induced intestinal injury, particularly exercise-induced intestinal injury aggravated by the NSAID. A method of increasing tight junction integrity in a subject in need thereof is also described.

Abstract: The present invention provides a compound of formula I; or a pharmaceutically acceptable salt thereof, wherein R1, R2 and R3 are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides pharmaceutical composition of the compounds of the invention and a combination of pharmacologically active agents and a compound of the invention.

Abstract: The present invention relates to a pharmaceutical composition for treating the human immunodeficiency virus (HIV) in humans, including three or four active principles selected as: a nucleoside reverse transcriptase inhibitor (NRTI) selected from lamivudine and emtricitabine; a nucleoside or nucleotide reverse transcriptase inhibitor (NRTI) selected from didanosine, abacavir and tenofovir; and the combination of a boosted or unboosted protease inhibitor (PI) selected from lopinavir, fosamprenavir, atazanavir and darunavir; or an non-nucleoside reverse transcriptase inhibitor (NNRTI) selected from efavirenz and etravirine; or an integrase inhibitor; for daily administration to said human being one to four days per week.

Abstract: The invention provides methods and compositions for treating symptoms associated with lactose intolerance and for overall improvement in gastrointestinal health. Described herein are methods and compositions for improving overall gastrointestinal health or for decreasing symptoms of lactose intolerance by administering to subject in need thereof a prebiotic composition, optionally in combination with effective amount of a probiotic microbe or microbes.

Abstract: The invention relates to methods and kits for use in reducing microbial counts on a patient's skin prior to surgery. Such a kit may be sealed, and include a dry substrate, a container of antiseptic composition, a tray with recessed portion(s), and a cover in sealing contact with a top rim of the tray to seal the contents in the tray. Such a kit may include two (e.g., identical) trays, which are initially attached to one another, each tray providing contents sufficient for one use (e.g., one use within 2 hours of the scheduled surgery, and a prior use done earlier (e.g., the night before). The related method may include providing the kit, removing the cover, dosing the substrate with the antiseptic composition in the tray's recessed region, and using the dosed substrate to apply the composition to skin proximate a location of the invasive procedure to be performed.

Abstract: The invention provides a cancer chemotherapeutic agent which has fewer side effects and excellent efficacy. The cancer chemotherapeutic agent of the invention includes a cholestanol derivative represented by formula (1): (wherein G represents GlcNAc-Gal-, GlcNAc-Gal-Glc-, Fuc-Gal-, Gal-Glc-, Gal-, or GlcNAc-) or a cyclodextrin inclusion compound thereof, and an anti-cancer agent.

Abstract: The present invention relates to a method of treating and/or preventing cancer comprising administering a combination of an effective amount of a DNA hypomethylating agent and an effective amount of at least one immunomodulatory agent and/or optionally an effective amount of at least one targeted therapy agent.

Abstract: The present disclosure provides pharmaceutical compositions comprising cytidine analogs for oral administration, wherein the compositions release the cytidine analog substantially in the stomach. Also provided are methods of treating diseases and disorders using the oral formulations provided herein.

Abstract: The present invention relates to a method for treating an individual having Cerebral Amyloid Angiopathy by using pharmacological chaperones to increase the activity of gangliosidase and/or sialidase enzymes involved in ganglioside catabolism.

Abstract: The present invention relates to particulate entity, such as a nanoparticle or conjugate, for use in particular as adjuvant in vaccine or immunotherapy. More specifically, the invention relates to a particulate entity comprising: iv. an iNKT cell agonist such as ? Gal Car compound, and, v. one or more antigenic determinant(s) such as a tumour antigen(s) or pathogen-derived antigen(s), vi. a targeting agent that targets in vivo said iNKT cell agonist to dendritic cells, such as human BDCA3+ dendritic cells.

Abstract: New drugs useful in the prevention or treatment of constipation are provided, in which SGLT1 inhibiting compounds, in particular, a 4-isopropylphenyl glucitol compound represented by the following formula (I), or pharmaceutically acceptable salts thereof are contained as an active ingredient:

Abstract: The present invention provides for compositions and methods for administering one or more UDP compound, alone or in combination with another hematopoietic progenitor cell mobillizing compound (for example, but not limited to G-CSF), to mobilize hematopoietic progenitor cells for transplant or other purposes. The methods of the invention may be particularly advantageous as applied to improve the stem cell yield in so-called “poor mobilizing” patients.

Abstract: The present invention provides therapeutic agents for preventing and treating neurodegenerative diseases. These agents synergistically target both the adenosine A2A receptor (A2AR) and the equilibrative nucleoside transporter 1 (ENT1).

Abstract: The invention relates to the field of basic biology, practical regenerative medicine, veterinary, cell biology and can be used to treat and prevent diseases, disorders or conditions associated with the violation of proliferation and differentiation of cells of different organs and tissues to activate the regeneration potential of human and animal organs and tissues at age-related changes and after extreme impacts, as well as for biomedical research. The present invention can be widely applied in the field of blood transfusion, organ transplantation, as well as serve as a general approach to the development of reliable methods to correct age-related changes in the elderly. The invention may also be used in the cosmetic industry for producing active ingredients for enhancing regeneration and improving the scalp, face and body, in particular for the manufacture of active additives to combat deep wrinkles, removal of skin defects, stimulation and acceleration of hair growth, controlling hirsutism, etc.

Abstract: The invention provides methods and compositions for treating symptoms associated with lactose intolerance and for overall improvement in gastrointestinal health. Described herein are methods and compositions for improving overall gastrointestinal health or for decreasing symptoms of lactose intolerance by administering to subject in need thereof a prebiotic composition, optionally in combination with effective amount of a probiotic microbe or microbes.

Abstract: Disclosed herein is a method for promoting reduction of heat stress in animals, as well as a composition for use in the disclosed method. The composition comprises a glucan, silica, mineral clay, mannan, and optionally an endoglucanohydrolase, and may be administered to an animal that is susceptible to or suffers from heat stress.

Abstract: Disclosed herein are methods for maintaining a population of therapeutic cells administered to a treatment site in a subject in need of cell therapy for a period of time. The methods include administering a therapeutically-effective amount of therapeutic cells and an effective amount of a biodegradable material to the treatment site. The biodegradable material includes a hyaluronan compound and has an in vivo degradation profile similar to that of a hyaluronic acid having a molecular weight of 20 kDa to 2,000 kDa.

Abstract: Disclosed is a method for preparing a composition enriched for receptors (typically molecular impringet polymers, MIPs) that bind an agent, where said receptors each specifically bind at least two discrete sites on said agent, by subjecting a sample of receptors to a first step of affinity purification with the agent where one binding site on the agent is non-accessible for binding to the receptors and subsequently subjecting the purified receptors to at least one further step of affinity purification with the agent where a second binding site on the agent is non-accessible.

Abstract: An object of the present invention is to provide an orally administered adsorbent capable of adsorbing large quantities of tryptophan or indoxyl sulfate in the presence of bile acid. The problem can be solved by an orally administered adsorbent comprising spherical active carbon having bulk density from 0.30 to 0.46 g/mL, specific surface area determined by the Brunauer-Emmett-Teller (BET) method of not less than 2000 m2/g, total acid group content of less than 0.30 meq/g, pore volume of pore diameter from 20 to 10,000 nm of not more than 0.21 mL/g; and a micropore volume ratio (Vm) of not less than 1.0, determined by Formula (1): Vm=(V2.0?V1.1)/(V1.1?V0.64) (1) [in Formula (1), V2.0, V1.1, and V0.64 are cumulative pore volumes of pore diameters not greater than 2.0 nm, not greater than 1.1 nm, and not greater than 0.64 nm, respectively, calculated by the SF method from nitrogen adsorbed quantity].

Abstract: The present invention relates to an oral pharmaceutical composition of aliphatic amine polymer or salts thereof comprising mixture of water and organic solvent(s) and/or less than of about 10% of plasticizing agent in the coating composition. In particular, present invention relates to a coated pharmaceutical composition of aliphatic amine polymer or salt thereof which comprises mixture of water and organic solvent(s) and less than of about 10% of plasticizing agent in coating. The invention also includes process of preparing such composition.