Abstract: The invention relates to pharmaceutical compositions comprising leukotoxin, including methods to treat lymphoma, and methods to diagnose lymphoma. The lymphoma includes lymphoma cells expressing activated LFA-1, and the leukotoxin binds to the activated LFA-1 on the lymphoma cells and destroys the lymphoma cells by apoptosis or necrosis, thereby treating said lymphoma.

Abstract: In a pharmaceutical composition for external use containing a compound such as luliconazole and/or a salt thereof in an amount of 5% by mass or more, comprised is/are acetone, a polyoxyethylene alkyl (having 8 to 30 carbon atoms) ether, and/or a polyoxyethylene alkenyl (having 8 to 30 carbon atoms) ether. Provided is a preparation using a solvent other than crotamiton, propylene carbonate, and N-methyl-2-pyrrolidone as a solvent for solubilization and steric stabilization and having the following properties: 1) when a compound represented by the general formula (1) and/or a salt thereof has a stereoisomer, the amount of the stereoisomer of the compound and/or a salt thereof produced under a preservation condition of 60° C. for 3 weeks is 1% by mass or less with respect to the total mass of the compound and/or a salt thereof at the beginning of preservation; 2) the preparation is in a clear liquid state when preserved at a constant temperature of 20° C.

Abstract: The present application provides pharmaceutical compositions comprising as the active medicinal ingredient nebivolol, a nebivolol analog or a pharmaceutically acceptable acid addition salt thereof and a wetting agent. The invention also relates to methods of preparing and using said compositions.

Abstract: The present invention relates to a novel pentadienoyl piperidine derivative, a pharmaceutical composition containing the same for prevention or treatment of metabolic diseases, and a functional food composition using the same for improvement or relief of metabolic diseases. The pentadienoyl piperidine derivative of the present invention inhibits the differentiation of preadipocytes, reduces body weight, visceral fat, blood lipid levels, and blood glucose levels, improves a blood liver function index, and suppresses metabolic inflammation responses. Thus, ultimately, the derivative can be usefully used as a medicine or a functional food composition, which exhibits the preventive or therapeutic activity for metabolic diseases selected from the group consisting of obesity, diabetes, dyslipidemia, fatty liver and insulin resistance syndrome.

Abstract: The present invention provides a compound having the structure: wherein R1, R2, R3, R4, and R5 are each independently H, halogen, CF3 or C1-C4 alkyl, wherein two or more of R1, R2, R3, R4, or R5 are other than H; R6 is H, OH, or halogen; and B is a substituted or unsubstituted heterobicycle, wherein when R1 is CF3, R2 is H, R3 is F, R4 is H, and R5 is H, or R1 is H, R2 is CF3, R3 is H, R4 is CF3, and R5 is H, or R1 is Cl, R2 is H, R3 is H, R4 is F, and R5 is H, or R1 is CF3, R2 is H, R3 is F, R4 is H, and R5 is H, or R1 is CF3, R2 is F, R3 is H, R4 is H, and R5 is H, or R1 is Cl, R2 is F, R3 is H, R4 is H, and R5 is H, then B is other than or a pharmaceutically acceptable salt thereof.

Abstract: Described are controlled-release solid dosage forms of mesalamine. In one aspect of the invention the controlled-release solid dosage forms of mesalamine are capsules comprising a plurality of coated mini-tablets. Another aspect of the invention relates to a method of treating a patient suffering from inflammatory bowel disease, comprising the step of administering to the patient a therapeutically effective amount of the solid dosage form. The invention also relates to methods of inducing remission of inflammatory bowel disease and maintaining remission of inflammatory bowel disease. In certain aspects, the inflammatory bowel disease is ulcerative colitis or Crohn's disease.

Abstract: The disclosure relates to Compounds of Formula (1): and pharmaceutically acceptable salts thereof wherein Z1, Z2, Z3, Xa, Xb, Xc, Y, X2, and X4 are as defined herein, compositions comprising an effective amount of a Compound of Formula (1) or a pharmaceutically acceptable salt thereof, and methods to treat or prevent a condition, such as cancer which overexpresses Her-kinases, comprising administering to an patient in need thereof a therapeutically effective amount of a Compound of Formula (1) or a pharmaceutically acceptable salt thereof.

Abstract: The present invention relates to a use of alpha-(8-quinolinyloxy) mono-substituted phthalocyanine zinc for the treatment of psoriasis. The use is suitable for various type of psoriasis by utilizing photodynamic therapy. The photosensitizer is used to treat psoriasis by utilizing laser wave length of 670 nm, with high light sensitivity, fast photobleaching, short time needed in protection from light, and avoiding potential toxic and side-effect of photochemistry therapy by using ultraviolet irradiation. The preparation used in the use of ?-(8-quinolinyloxy) mono-substituted phthalocyanine zinc for the treatment of psoriasis includes solution, cream, nanomicelle, microsphere etc, and mode of administration can be systemic or topical administration. The practicability of treating psoriasis by photodynamic therapy has been validated on cell and animal model. The use achieves perfect effect.

Abstract: The present invention relates to an epidithiodioxopiperazine derivative represented by the following Chemical Formula 1 or its reduced derivative; a method for preparing a compound represented by Chemical Formula 1 having improved intracellular permeability and mimicking the activity of 2-Cys-Prx in its reduced form in the cells; a pharmaceutical composition for preventing or treating vascular diseases comprising an epidithiodioxopiperazine compound or its derivatives or pharmaceutically acceptable salts thereof as an active ingredient; a drug delivery device for local administration including the pharmaceutical composition; and a pharmaceutical composition for inhibiting melanoma metastasis comprising the epidithiodioxopiperazine compound or its derivatives or pharmaceutically acceptable salts thereof as an active ingredient.

Abstract: Disclosed are compounds of Formula (I): or a salt thereof, wherein Q is: or; and X, R1a, R1b, R3, R4, and R5 are defined herein. Also disclosed are methods of using such compounds as inhibitors of Bruton's tyrosine kinase (Btk), and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.

Abstract: The present invention relates to a method of treating a disease in a subject, comprising administering to a subject in need thereof a solid pharmaceutical composition biopterin derivatives.

Abstract: Alpha-helix mimetic structures and compounds represented by the formula (I) wherein the general formula and the definition of each symbol are as defined in the specification, a chemical library relating thereto, and methods relating thereto, are disclosed. Applications of these compounds in the treatment of medical conditions, e.g., cancer diseases, fibrotic diseases, and pharmaceutical compositions comprising the mimetics are further disclosed.

Abstract: The present invention relates to the use of novel compounds of formula (I), wherein all variable substituents are defined as described herein, which are SYK inhibitors and are useful for the treatment of auto-immune and inflammatory diseases.

Abstract: Methods for treating erectile dysfunction with therapeutic neuromodulation and associated systems and methods are disclosed herein. Erectile dysfunction can be characterized by the inability to develop and/or maintain an erection during sexual arousal or activity. One aspect of the present technology is directed to methods that at least partially inhibit sympathetic neural activity in nerves innervating the penis of a patient. Sympathetic drive in the patient can thereby be reduced in a manner that treats the patient for erectile dysfunction. Sympathetic nerve activity can be modulated along afferent and/or efferent pathways. The modulation can be achieved, for example, using an intravascularly positioned catheter carrying a therapeutic assembly, e.g., a therapeutic assembly configured to use electrically-induced, thermally-induced, and/or chemically-induced approaches to modulate the nerves.

Abstract: An antimicrobial coating system and method are described. In some embodiments, a system may include a composition. The composition may include one or more bridged polycyclic compounds. At least one of the bridged polycyclic compounds may include at least two cyclic groups, and at least two of the cyclic groups may include quaternary ammonium moieties. In some embodiments, a method may include applying an antimicrobial coating to an oral surface, a surface of a construction substrate, a surface of a marine substrate, a surface of a medical device, or a surface of a personal care device. The protective coating may be antimicrobial. A protective coating may include antimicrobial bridged polycyclic compounds. Bridged polycyclic compounds may include quaternary ammonium compounds. Bridged polycyclic compounds based coating systems may impart self-cleaning properties to a surface (e.g., a tooth surface).

Abstract: Therapeutic combinations of a Janus kinase-2 (JAK-2) inhibitor, a Bruton's tyrosine kinase (BTK) inhibitor, and/or a phosphoinositide 3-kinase (PI3K) inhibitor, including PI3K inhibitors selective for the ?- and ?-isoforms and selective for both ?- and ?-isoforms, are described. In some embodiments, the invention provides pharmaceutical compositions comprising combinations of (1) a PI3K-? inhibitor and a BTK inhibitor, (2) a JAK-2 inhibitor and a BTK inhibitor, or (3) a JAK-2 inhibitor, PI3K-? inhibitor, and BTK inhibitor, and methods of using the pharmaceutical compositions for treating a disease, in particular a cancer.

Abstract: The present disclosure relates to a novel active compound having the formula Ia: solid preparations, uses and methods for the treatment or prevention of respiratory diseases comprising said compound as well as process of preparation thereof.

Abstract: Described herein are compounds and pharmaceutical compositions useful for treating inflammatory diseases.

Abstract: Disclosed are 1-(arylmethyl)quinazoline-2,4(1H,3H)-diones represented by the Formula (I): wherein Ar, R1-R6 are defined herein. Compounds having Formula (I) are PARP inhibitors. Therefore, compounds of the invention may be used to treat clinical conditions that are responsive to the inhibition of PARP activity.

Abstract: Disclosed is a new method for preparing an azetidinone compound represented by formula (I). The carboxylic ketoester represented by formula (II) serves as the raw material and is subjected to Grignard addition, stereoselective dehydration, ester group reduction, hydroxyl group protection, addition with imine after condensation with a chiral auxiliary, cyclization and deprotection to obtain the compound represented by formula (I). The present invention has advantages of easily available raw material, a few synthetic steps, simple operation, high yield, good stereoselectivity and low cost, and can be used for industrial production.

Abstract: Provided are 4?-O substituted isoindoline compounds, and pharmaceutically acceptable salts, solvates, clathrates, stereoisomers, and prodrugs thereof. Methods of use, and pharmaceutical compositions of these compounds are disclosed.

Abstract: Provided herein are prostaglandin F2alpha analog compositions and methods for treating migraines by topical administration. The method involves administering topically to a subject in need thereof a composition including a prostaglandin F2apha analog or pharmaceutically acceptable salt thereof, in an amount effective to treat migraine. The treatment may be administered prophylactically or therapeutically. Topical administration is to the epidermis, conjunctival surface or other mucous membranes, typically to a nail, the skin, the hair, the surface of the eye or the inner surface of the eyelid, and the like. The prostaglandin F2a analog can be latanoprost, isopropyl unoprostone, bimatoprost, travoprost, or tafluprost; or pharmaceutically acceptable salt thereof.

Abstract: The present invention relates to a novel crystalline form of a benzimidazole derivative and a preparation method thereof. The novel crystalline form according to the present invention is hardly changed chemically and/or physically under a long-term photo-stressed condition, has a low hygroscopicity, and has an extremely low static-electricity-inducing capability, thus being advantageous for formulation, and due to the excellent stability of the crystal form itself, it is very useful for long-term storage of the compound.

Abstract: Described herein are 1,4-substituted piperidine compounds according to Formula I that have demonstrated activity as fatty acid synthase inhibitors. Also described herein are pharmaceutical compositions containing the described 1,4-substituted piperidine compounds, and methods of treating diseases mediated by fatty acid synthase, by administering one or more of the compounds or pharmaceutical formulations described herein. Also described herein are methods of synthesizing the compounds described, including the described 1,4-substituted piperidine compounds and synthetic intermediates useful in those syntheses.

Abstract: The present invention is directed to compounds of formula I and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of Syk kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition Syk kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by Syk kinase activity, such as Non Hodgkin's Lymphoma.

Abstract: The present invention relates to solid pharmaceutical compositions comprising biopterin derivatives as well as methods for obtaining such solid pharmaceutical compositions. The invention also relates to the solid pharmaceutical compositions of the invention for treating diseases.

Abstract: A topical composition for skin repair comprising selenosugars of formula (1): (Formula (I)) wherein, n is 1, 2 or 3; m is 2, 3, 4; or 5; and each R1 is independently-(optionally substituted C1-C3 alkyiene)p-OH, where p is 0 or 1 or a pharmaceutically acceptable salt thereof.

Abstract: Compounds according to Formulas I, IA or IB: to pharmaceutically acceptable composition, salts thereof, their synthesis and their use as SIK2 inhibitors including such compounds and methods of using said compounds in the treatment of various diseases and/or disorders such as cancer, stroke, cardiovascular, obesity and type II diabetes.

Abstract: The present invention is related to the use of compounds or pharmaceutically acceptable salts thereof that modulate astrocytic release of substances through connexin and pannexin hemichannels, for the treatment of psychiatric disorders. Compounds or pharmaceutically acceptable salts thereof used in the present invention comprise any compound that differentially modulates, blocks, opens, inhibits, and/or activates connexin and/or pannexin hemichannels from astrocytes while not affecting gap junctions. The invention is also related to a method for treating psychiatric disorders, comprising administering to a mammal or human a therapeutically effective amount of a compound or a pharmaceutically acceptable salt thereof, that modulates astrocytic release of substances through connexin and pannexin hemichannels. Pharmaceutical compositions and a screening method are also considered in the present invention.

Abstract: The present invention provides a method for promoting plant growth, which comprises treating a plant with a compound represented by the following Formula (1): provided that a method for promoting plant growth which comprises treating plants with a compound corresponding to the following (1) or an agriculturally acceptable salt thereof are excluded, (1) benzo[b]thiophene-3-carboxylic acid. The method set forth in one of the above, the plant being soybeans. The method set forth in one of the above, the plant being cotton. A plant seed resulting from treatment with the compound of claim 1 containing an effective quantity of the compound indicated in formula (1). A composition for promoting plant growth and containing an inert component and the compound indicated in formula (1).

Abstract: Ingenol angelate is a potent anticancer agent, and can be stabilized by dissolving it in an aprotic solvent in the presence of an acidic buffer.

Abstract: Ingenol angelate is a potent anticancer agent, and can be stabilized by dissolving it in an aprotic solvent in the presence of an acidic buffer.

Abstract: Ingenol angelate is a potent anticancer agent, and can be stabilized by dissolving it in an aprotic solvent in the presence of an acidic buffer.

Abstract: The present invention provides spiro-oxazolones, which act as V1a receptor modulators, and in particular as V1a receptor antagonists, their manufacture, pharmaceutical compositions containing them and their use as medicaments. The present compounds are useful as therapeutics acting peripherally and centrally in the conditions of inappropriate secretion of vasopressin, anxiety, depressive disorders, obsessive compulsive disorder, autistic spectrum disorders, schizophrenia, aggressive behavior and phase shift sleep disorders, in particular jetlag.

Abstract: Ingenol angelate is a potent anticancer agent, and can be stabilized by dissolving it in an aprotic solvent in the presence of an acidic buffer.

Abstract: Methods for treating cancer by activation of the Bmp pathway are disclosed. In particular, the invention relates to methods of treating cancer using agents that activate BMP signaling, e.g., FK506 (tacrolimus), to treat a subject for cancer.

Abstract: Disclosed is a personalized diagnostic and treatment solution for cardiovascular disease. The invention comprises methods for devising a personalized treatment plan for a patient via the use of an extended CVD risk assessment panel measuring markers of cholesterol absorption and production and HDL subfractions. This solution provides a more complete risk assessment of an individual than merely measuring traditional CVD risk markers alone, and enables the healthcare practitioner to optimize therapy for patients with or without established CVD. This solution presents the advantages of greater accuracy, savings in time and cost over existing testing and treatment methods.

Abstract: The present disclosure provides a method for killing persister cells with mitomycin C and/or cisplatin, or derivatives thereof. Recalcitrant infections are difficult to treat due to persister cells, a subpopulation of all bacterial populations that is highly tolerant against all traditional antibiotics since the cells are dormant and antibiotics are designed to kill growing cells. Here, we show that MMC and cisplatin eradicate persister cells through a growth-independent mechanism, cross-linking DNA. We find both agents are effective against both planktonic cultures and highly robust biofilm cultures for a broad range of bacterial species, including commensal Escherichia coli K-12 as well as pathogenic species of E. coli, Staphylococcus aureus, and Pseudomonas aeruginosa. In certain approaches cisplatin is superior to MMC.

Abstract: The present invention relates to a thiophene derivative of the following general formula I or an enantiomer, diastereoisomer, hydrate, solvate, tautomer, racemic mixture or pharmaceutically acceptable salt thereof or to its use as a drug in particular intended for treating and/or preventing diabetes, its complications and/or associated pathologies, advantageously diabetes of type II and hyperglycemia.

Abstract: Aspects of the present disclosure relate to compounds which have enhanced oral bioavailability. A transition metal complex includes a transition metal coordinated by a macrocycle comprising the pentaaza 15-membered macrocyclic ring corresponding to Formula A and two axial ligands having the formula —OC(O)X1. each of the two axial ligands has the formula —OC(?O)X1 wherein each X1 is independently substituted or unsubstituted phenyl or —C(—X2)(—X3)(—X4); each X2 is independently substituted or unsubstituted phenyl, or substituted or unsubstituted alkyl; each X3 is independently hydrogen, hydroxyl, alkyl, amino, —X5C(?O)R13 where X5 is NH or O, and R13 is C1-C18 alkyl, substituted or unsubstituted aryl or C1-C18 aralkyl, or —OR14, where R14 is C1-C18 alkyl, substituted or unsubstituted aryl or C1-C18 aralkyl, or together with X4 is (?O); and each X4 is independently hydrogen or together with X3 is (?O).

Abstract: Aspects of the present disclosure relate to compounds which have enhanced oral bioavailability. A transition metal complex includes a transition metal coordinated by a macrocycle comprising the pentaaza 15-membered macrocyclic ring corresponding to Formula A and two axial ligands having the formula —OC(O)X1. each of the two axial ligands has the formula —OC(?O)X1 wherein each X1 is independently substituted or unsubstituted phenyl or —C(—X2)(—X3)(—X4); each X2 is independently substituted or unsubstituted phenyl, or substituted or unsubstituted alkyl; each X3 is independently hydrogen, hydroxyl, alkyl, amino, —X5C(?O)R13 where X5 is NH or O, and R13 is C1-C18 alkyl, substituted or unsubstituted aryl or C1-C18 aralkyl, or —OR14, where R14 is C1-C18 alkyl, substituted or unsubstituted aryl or C1-C18 aralkyl, or together with X4 is (?O); and each X4 is independently hydrogen or together with X3 is (?O).

Abstract: Compounds of the formula I in which R, R1 and R2 have the meanings indicated in claim 1, are inhibitors of Syk, and can be employed, inter alia, for the treatment of cancer, rheumatoid arthritis and/or systemic lupus.

Abstract: The invention relates to Histamine type 4 receptor (H4R) inhibitors for treating tinnitus.

Abstract: It is an object of the present invention to provide a novel form of (S)-trans-{4-[({2-[({1-[3,5-bis(trifluoromethyl)phenyl]ethyl}{5-[2-(methylsulfonyl)ethoxy]pyrimidin-2-yl}amino)methyl]-4-(trifluoromethyl)phenyl}(ethyl)amino)methyl]cyclohexyl}acetic acid, which is useful for preventing and/or treating diseases such as dyslipidemia. (S)-trans-{4-[({2-[({1-[3,5-bis(Trifluoromethyl)phenyl]ethyl}{5-[2-(methylsulfonyl)ethoxy]pyrimidin-2-yl}amino)methyl]-4-(trifluoromethyl)phenyl}(ethyl)amino)methyl]cyclohexyl}acetic acid hydrochloride.

Abstract: Compositions comprising hydroxytyrosol-containing formulations and treatment regiments comprising hydroxytyrosol and/or oleuropein and chemotherapeutic agents are disclosed. Compositions and/or regiments may optionally include the administration of vitamins, minerals, and anti-oxidants. Methods for using these compositions and treatment regimens for treating subjects for diseases, such as a malignancy, and for inducing or enhancing angiogenesis, treating or preventing oxidative stress, for treating or preventing high glucose-induced dysfunction, treating or preventing chemotherapy-induced dysfunction, and for improving cell viability are provided. Various methods for use of the hydroxytyrosol compositions for inhibition of lysine specific demethylase 1 (LSD1) in various cancers are also provided.

Abstract: The invention discloses a method of treating cancer in a patient, comprising administering to the patient a radiation sensitizer selected from nitroimidazoles in an amount effective to sensitize a patient to radiation and subjecting the patient to radiation therapy. In certain embodiments the radiation sensitizer is etanidazole or doranidazole.

Abstract: The present invention provides a novel hypertension therapeutic agent. The hypertension therapeutic agent of the present invention contains, as an active ingredient, a compound represented by formula (1): [F1] or a pharmaceutically acceptable salt thereof.

Abstract: Methods are provided for reducing chronic inflammatory pain, increasing the levels of endogenous opioid peptides, as well as increasing the pain threshold of a subject having symptoms of androgen deficiency, comprising transdermally administering a composition comprising a bioactive androgen on a daily basis. In addition, the invention also relates to increasing the levels of endogenous opioid peptides in a human subject by administering an androgen composition to the subject. The invention also encompasses administration of a composition consisting essentially of an androgen for the treatment of chronic inflammatory pain, and for increasing the pain-threshold in a subject.

Abstract: Disclosed herein are compounds of Formula (I) that are useful as inhibitors of Bruton's tyrosine kinase: where R6-R10 are as defined herein. Also disclosed are pharmaceutical compositions that include the compounds. The compounds may be used, for example, to treat autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.

Abstract: Described herein is pure amorphous darunavir, methods of making pure amorphous darunavir and pharmaceutical compositions containing amorphous darunavir and a pharmaceutically acceptable excipient.