Abstract: The present invention relates to a block copolymer formed by coupling the following components with each other, as well as a hydrogel composition comprising the block copolymer and a hydrogel formed from the composition: (a) a copolymer of a polyethylene glycol (PEG)-based compound with a biodegradable polymer; and (b) a sulfonamide-based oligomer. The inventive block copolymer shows the sol-gel transition behavior sensitive to changes in not only temperature but also pH. Thus, the inventive block copolymer overcomes the shortcomings of temperature-sensitive copolymers, form a more strong and stable hydrogel, and is stable in vivo. Accordingly, the inventive block copolymer can be used in various applications in the medical and drug delivery fields.

Abstract: The invention provides inhalation devices comprising a compound which is 4-{(1R)-2-[(6-{2-[(2,6-dichlorobenzyl)oxy]ethoxy}hexyl)amino]-1-hydroxyethyl}-2-(hydroxymethyl)phenol; or a salt or solvate thereof, inhalation devices comprising formulations and combinations of the compound or a salt or solvate thereof, and methods for the treatment or prophylaxis of a clinical condition in a mammal by employing the inhalation devices.

Abstract: Macrocyclic compounds of formula (I), in which B1 and X1 taken together are alkylene which is unsubstituted or substituted with ?O and having one CH2 moiety unreplaced or replaced with CH?CH, O, NH or N(alkyl), which inhibit the activity of antiapoptotic Bcl-2 family protein members, compositions containing the compounds and methods of treating diseases during which are expressed one or more than one of an anti-apoptotic family protein member are disclosed.

Abstract: A dermal or transdermal therapeutic system comprising a reservoir that contains at least one active substance, an active substance-permeable membrane which delimits the active-substance reservoir, and a closing layer. The closing layer is impermeable to the active substance at a temperature lying below the skin temperature while being permeable at skin temperature and above.

Abstract: The invention features a method of (i) reducing the appearance of pores or oil on the skin and (ii) evening skin tone or smoothing skin by applying to an area of skin in need of such treatment a composition including an anti-acne agent, an antimicrobial agent, and a lactate.

Abstract: The present invention relates to new benzenesulfonamide modulators of alpha-1A adrenergic receptors, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: The present invention relates to a novel class of modified malonate derivatives. The modified malonate compounds can be used to treat cancer. The modified malonate compounds can also inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.

Abstract: Chemical agents, such as disulfonamide derivatives of fluorene, anthracene, xanthene, dibenzosuberone and acridine, and similar heterocyclic ring structures, including salts thereof, that act as anti-cancer and anti-tumor agents, especially where such agents modulate the activity of the Wnt/?-catenin signaling pathway, and serve to reduce ?-catenin levels present in cells, such as cancer cells, or where the agents modulate levels of gene expression in cellular systems, including cancer cells, are disclosed, along with methods for preparing such agents, as well as pharmaceutical compositions containing such agents as active ingredients and methods of using these as therapeutic agents.

Abstract: Disclosed are compositions and methods for treating diseases associated with G protein ?? subunit activity.

Abstract: The present invention relates to new sulfonamide derivatives of formula (I) wherein R1-R8 and Z are as defined in the claims, and optical antipodes or racemates and/or salts and/or hydrates and/or solvates thereof, which are selective antagonists of bradykinin B1, to processes for producing these same compounds, pharmacological compositions containing them and to their use in therapy or prevention of painful and inflammatory conditions.

Abstract: The present invention is related to the use of sulfonamide derivatives in the treatment of metabolic disorders mediated by insulin resistance or hyperglycemia, comprising diabetes type II, inadequate glucose tolerance, insulin resistance, obesity, polycystic ovary syndrome (PCOS). Formula (I). R1 is selected from the group comprising or consisting of hydrogen, C1-C6-alkoxy, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl, amino, sulfanyl, sulfinyl, sulfonyl, sulfonyloxy, sulfonamide, acylamino, aminocarbonyl, C1-C6 alkoxycarbonyl, aryl, heteroaryl, carboxy, cyano, halogen, hydroxy, nitro, hydrazides. R2 is selected from the group comprising or consisting of hydrogen, COOR3, —CONR3R3?, OH, a C1-C4 alkyl substituted with an OH or amino group, a hydrazido carbonyl group, a sulfate, a sulfonate, an amine or an ammonium salt.

Abstract: Novel injectable compositions are provided comprising an active agent which is tamsulosin or letrozole or its pharmaceutically acceptable salts, derivatives, isomers, polymorphs, solvates, hydrates, analogues, enantiomers, tautomeric forms or mixtures thereof and one or more pharmaceutically acceptable excipient(s) wherein the compositions are preferably formulated as biodegradable microparticles or nanoparticles which can optionally be reconstituted with an aqueous, hydro-alcoholic or oily liquid vehicle prior to administration. The novel injectable compositions of the present invention preferably form a depot upon administration in vivo and are in the form of an in situ gelling composition or an implant composition which provides a prolonged release of tamsulosin or letrozole for extended periods of time. Also described are process for preparation of such novel compositions and method of using them.

Abstract: Provided are sulphur-linked compounds, pharmaceutical compositions thereof, and methods of treating ophthalmic diseases and disorders, such as age-related macular degeneration and Stargardt's Disease, using said compounds and compositions.

Abstract: The invention relates to compounds represented by Structural Formula I, which can bind to CCR9 receptors and block the binding of a ligand (e.g., TECK) to the receptors. The invention also relates to a method of inhibiting a function of CCR9, and to the use compounds represented by Structural Formula I in research, therapeutic, prophylactic and diagnostic methods.

Abstract: Compounds of Formula I are disclosed: (I), wherein XA, k, R1, R2, R3, R4, R5, R5A, R6, R6A, R7 and R8 are defined herein. The compounds encompassed by Formula I include compounds which are HIV protease inhibitors and other compounds which can be metabolized in vivo to HIV protease inhibitors. The compounds and their pharmaceutically acceptable salts are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.

Abstract: Low dose pharmaceuticals can be delivered for a prolonged period using a tablet-in-tablet design wherein the drug is contained in a controlled release matrix in the outer compression coating layer but not in the inner tablet core.

Abstract: The invention relates to the use of magnesium stearate to inhibit or reduce chemical degradation of an active ingredient substance in a formulation comprising a carrier in a solid pharmaceutical formulation, wherein the active ingredient substance is susceptible to chemical degradation.

Abstract: The present invention is directed to a method of enhancing TGF-? signaling in a subject comprising administering to said subject a clathrin-dependent endocytosis inhibitor in an amount sufficient to enhance TGF-? signaling. In another aspect, the invention is directed to a method of treating a condition associated with decreased TGF-? signaling in a patient in need thereof comprising administering to said patient a clathrin-dependent endocytosis inhibitor in a therapeutically effective amount.

Abstract: The application discloses novel polymorphic crystalline forms of 2-[4-Bromo-3-(3-chloro-5-cyano-phenoxy)-2-fluoro-phenyl]-N-(2-chloro-4-propionylsulfamoyl-phenyl)-acetamide, sodium salt (Ib) with improved stability and physical properties which facilitate manufacturing, handling and formulating for treatment or prophylaxis of HIV mediated diseases, AIDS or ARC, in monotherapy or in combination therapy.

Abstract: There is provided a compound of formula (I) wherein R1a, R2a, R3, X1 to X6, a, b and c have meanings given in the description, which compounds are useful as, or are useful as prodrugs of, inhibitors of HDAC enzyme activity, and thus, in particular, in the treatment of conditions where inhibition of HDAC enzyme activity is required.

Abstract: The invention provides sulfonamide compounds of formula (I) as defined herein, pharmaceutical compositions containing the same and methods of treatment using such compounds and pharmaceutical compositions. These compounds have a common wide range of beneficial therapeutic indications, in particular as analgesic and anti-inflammatory agents.

Abstract: The present invention relates to compounds of formula I, in which at least one of R5, R6 and R7 is SR12, S(O)R12 or S(O)2R12 group where R12 is a C1-6haloalkyl group, that act, as chemical uncouplers. Compounds of the invention are useful in the treatment, including prevention, of obesity, diabetes and a number of diseases or conditions associated therewith.

Abstract: The present invention provides compositions for treating an HIV infection comprising administering a compound according to formula I where Ar, R1-R5, R11c and X1 are as defined herein with at least one carrier, excipient or diluent.

Abstract: The present invention is directed to methods of modulating the activity of an isoform of manganese superoxide dismutase which is useful for the treatment of diseases such as heart failure.

Abstract: The present invention relates to novel (2R)-2-phenylpropanamides bearing a 4-sulfonylamino substituent on the 4 position of the phenyl group and to pharmaceutical compositions containing them, which are used as inhibitors of the chemotaxis of polymorphonucleate and mononucleate cells, and which are useful in the treatment of various ELR+CXC chemokine-mediated disorders. In particular, the compounds of the invention are useful in the treatment and control of specific CXCR2 dependent pathologies such as BOS, COPD, angiogenesis and melanoma.

Abstract: The present invention relates to a cosmetic composition which comprises a compound of the formula R2R3N—(CH2)n—SO2R1, in which R1 is OR4 or NR5R6; R2 and R3, independently of one another, are H, C1-C6-alkyl, phenyl-C1-C4-alkyl, HCO or C1-C4-alkyl-CO; R4 is C1-C6-alkyl; R5 and R6, independently of one another, are H or C1-C6-alkyl; and n is 2, 3 or 4. The cosmetic compositions can be used for protecting the hair and the skin against oxidative damage and for regenerating oxidatively damaged hair or oxidatively damaged skin.

Abstract: The present invention features compositions, methods, and kits useful in the treatment of viral diseases. In certain embodiments, the viral disease is caused by a single stranded RNA virus, a flaviviridae virus, or a hepatic virus. In particular embodiments, the viral disease is viral hepatitis (e.g., hepatitis A, hepatitis B, hepatitis C, hepatitis D, hepatitis E) and the agent or combination of agents includes sertraline, a sertraline analog, UK-416244, or a UK-416244 analog. Also featured are screening methods for identification of novel compounds that may be used to treat a viral disease.

Abstract: A method is disclosed utilizing a cannabinoid receptor type 2-receptor-selective agonist for treating or preventing lower urinary tract dysfunction, including overactive bladder, lower urinary tract symptoms and detrusor overactivity.

Abstract: The present invention relates to compositions and methods for treating diabetes mellitus, neuropsychological and neurological disorders in a particular group of patient. More specifically, the invention relates to methods of treating diabetes mellitus, neuropsychological and neurological disorders in patients having defective potassium channels. The invention may be used in human subjects, particularly adults or children, and is appropriate to treat various neurological disorders.

Abstract: A process for forming crystalline lactose suitable for use in a pharmaceutical formulation comprises subjecting a solution comprising a plurality of nanosized lactose particles to conditions sufficient to cause crystallization to occur on the nanosized lactose particles such that a plurality of lactose particles are formed therefrom having a median diameter ranging from about 4 ?m to about 20 ?m.

Abstract: The present invention provides compounds for treating or preventing an HIV infection, or treating AIDS or ARC comprising administering a compound according to formula I where Ar, R1-R5, R11c and X1 are as defined herein.

Abstract: The present invention provides compounds of general formula I: or a pharmaceutically acceptable salt thereof, wherein R1, X, Z, R2, X1, Ar, n, R3 and R4 are defined generally and in subsets herein. Compounds of the invention are inhibitors of CCR8 and accordingly are useful for the treatment of a variety of inflammatory and allergic disorders.

Abstract: The present invention is directed to methods and compositions methods and compositions for determining and inhibiting gene transcription in mammalian cells. The invention relates to novel inhibitors of rho-mediated gene transcription and to compounds that may be used as therapeutic agents.

Abstract: The invention provides amino- and amido-aminotetralin compounds of formula (I): wherein R1, R2, R3, R4, R5, R6, R7, and n are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are antagonists at the mu opioid receptor. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat conditions associated with mu opioid receptor activity, and processes and intermediates useful for preparing such compounds.

Abstract: There is provided compounds of formula (I), wherein R1, R2, X2, X4 and X5 to X8 have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of the activity of a member of the MAPEG family is desired and/or required, and particularly in the treatment of inflammation.

Abstract: The present invention is directed to compounds of formula (I) that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them. Wherein R3 is -alkylene-SO2NR5R6.

Abstract: The present invention relates to a 5-amidino-2-hydroxybenzenesulfonamide derivative represented by the general formula: wherein R1 is a hydrogen atom or an optionally substituted lower alkyl group; R2 is a di(lower alkyl)amino group, a lower alkyl group, a cycloalkyl group, an optionally substituted aryl group, an optionally substituted heterocycloalkyl group, or an optionally substituted aromatic heterocyclic group; T is an oxygen atom, a sulfur atom, a sulfonyl group etc.; Q is a hydrogen atom or an optionally substituted lower alkyl group; and Z is a hydrogen atom, a hydroxy group etc., or a pharmaceutically acceptable salt thereof, which exert a potent and selective activated blood coagulation factor X inhibitory activity and is useful as an agent for the prevention or treatment of a disease occurred associating an activated blood coagulation factor X, a pharmaceutical composition comprising the same, a pharmaceutical use thereof and an intermediate thereof.

Abstract: Provided herein are compounds that bind to androgen receptors and modulate the activity and/or the amount of androgen receptors and to methods for making and using such compounds. Also provided are compositions including such compounds and methods for making and using such compositions.

Abstract: A compound of Formula (I), or pharmaceutically acceptable salts and/or hydrates or prodrugs thereof, wherein Formula (I) has the structure: is provided, wherein R1-R7 are defined herein. These compounds are useful in medicaments for treating a disease selected from the group consisting of Alzheimer's disease, amyloid angiopathy, cerebral amyloid angiopathy, systemic amyloidosis, hereditary cerebral hemorrhage with amyloidosis of the Dutch type, inclusion body myositis, mild cognitive impairment (MCI) and Down's syndrome, in a subject.

Abstract: The invention relates to an orally administrable mucoadhesive film which comprises one or more bioactive ingredients and, as a major film-forming polymer, at least one alginate which is capable of forming a low viscosity aqueous solution. Also provided is a process for preparing such films.

Abstract: Biomacromolecules such as proteins are inactivated by hydrophobic ANSA derivatives of the formula: wherein R1 and R2 are hydrophobic or affinity groups and R3 is selected from the group consisting of aminoacyl groups and peptidyl groups upon nitrosation. ANSA derivatives can be designed to selectively kill tumor cells and various pathogens, including bacteria, viruses, and fungi.

Abstract: The present invention relates to an agent for the prevention or treatment of a renal disease comprising as an active ingredient a 5-amidino-2- hydroxybenzenesulfonamide derivative represented by the general formula: wherein R1 is a hydrogen atom or an optionally substituted alkyl group; R2 is a dialkylamino group, an alkyl group, a cycloalkyl group, an optionally substituted aryl group etc.; T is an oxygen atom, a sulfur atom etc.; Q is a hydrogen atom or an optionally substituted alkyl group; and Z is a hydrogen atom, a hydroxy group etc., or a pharmaceutically acceptable salt thereof which has an inhibitory effect on mesangial cell proliferation and a decreasing effect on protein excretion in urine, and are useful for preventing or treating of various renal diseases such as IgA nephropathy, diabetic nephropathy, nephritic syndrome and the like.

Abstract: The invention relates to a method for determining whether a compound is a neurotrypsin inhibitor, characterized in that the compound is incubated together with neurotrypsin, a variant thereof or a fragment comprising the protease domain and with a protein or peptide comprising agrin, a variant thereof or a fragment comprising the ?- or the ?-cleavage site of agrin, in an aqueous buffer solution, and the amount of cleavage of agrin is measured. Additionally, the invention relates to inhibitors of neurotrypsin found by this method, in particular to compounds of formula wherein Hal1 and Hal2 are fluorine, chlorine or bromine, and the use of such inhibitors for the treatment and/or prophylaxis of diseases caused by deficiency of synapses, for example skeletal muscle atrophy, schizophrenia, and cognitive disturbance.

Abstract: A method for healing a wound comprising the step of topically administering a wound healing composition to a wounded area, wherein the wound healing composition comprises a first medicament characterized as an alpha-adrenergic antagonist and pharmaceutically acceptable salts thereof.

Abstract: The invention relates to N-hydroxylsulfonamide derivatives that donate nitroxyl (HNO) under physiological conditions and are useful in treating and/or preventing the onset and/or development of diseases or conditions that are responsive to nitroxyl therapy, including heart failure and ischemia/reperfusion injury. Novel N-hydroxylsulfonamide derivatives release NHO at a controlled rate under physiological conditions, and the rate of HNO release is modulated by varying the nature and location of functional groups on the N-hydroxylsulfonamide derivatives.

Abstract: This invention relates to pharmaceutical and veterinary formulations providing enhanced solvency and stability for pharmaceutical and veterinary agents for administration to animals, especially ruminants. In addition, the invention relates to pour-on formulations for combating parasites in animals, such as cattle and sheep. In some embodiments, this invention provides glycol-ether-based pour-on formulations comprising a composition comprising a flukicide, such as, for example, clorsulon (4-amino-6-trichloroethenyl-1,3-benzene disulfonamide) and/or a macrolide anthelmintic or antiparasitic agent. In other embodiments, the invention provides pour-on formulations comprising at least one active agent, a glycol ether, and a stability enhancer. This invention also provides for methods for eradicating, controlling, and/or preventing parasite infestation in animals, such as cattle and sheep.

Abstract: A tamsulosin-containing transdermal patch. A transdermal patch comprising a backing-layer and an adhesive layer on the backing-layer, characterized in that the adhesive layer contains an acrylic adhesive, further contains tamsulosin as an active ingredient in an amount of 0.1 to 20% by mass of the total mass of the adhesive layer and, if desired, a polyoxyethylene alkyl ether which is an additive playing a role in increasing solubility and a propylene glycol fatty acid ester which is an additive playing a role in promoting percutaneous absorption is provided. Further, a transdermal patch comprising a backing-layer and an adhesive layer on the backing-layer, characterized in that the adhesive layer contains a synthetic rubber adhesive, further contains tamsulosin as an active ingredient in an amount of 0.1 to 20% by mass of the total mass of the adhesive layer and a propylene glycol fatty acid ester which is an additive playing a role in promoting percutaneous absorption is provided.

Abstract: A medicament for enhancing an effect of a cancer therapy based on a mode of action of DNA injury, which comprises as an active ingredient a compound represented by the general formula (I) or a physiologically acceptable salt thereof: wherein R represents an aryl-substituted alkyl group, an heteroaryl-substituted alkyl group, a cycloalkyl-substituted alkyl group, or a cyclic hydrocarbon group wherein said cyclic hydrocarbon group may be saturated, partly saturated, or aromatic; or Z may bind to R to form a cyclic structure, Z represents a hydrogen atom or a C1 to C6 alkyl group. The medicament enhanced the effect of the cancer therapy and decreases a dose of an anticancer agent and/or radiation, and therefore, can reduce side effects resulting from the cancer therapy.

Abstract: The invention relates to 2-cyano-3-(halo)alkoxy-benzenesulfonamide compounds I where the variables Alk and R1 to R5 are as defined in claim 1, and/or to their agriculturally useful salts.

Abstract: Provided herein are compositions and methods for treating or preventing cancer and autoimmune diseases. Compositions comprise a sirtuin inhibitory compound that decreases the activity of a sirtuin, such as SIRT1 or Sir2. Exemplary methods comprise contacting a cell or a molecule with a sirtuin inhibitory compound that decreases the activity of a sirtuin and thereby reduces the life span of a cell, kills the cell or renders it susceptible to certain cell stresses including radiation and chemotherapy. Other methods include treating pathogens expressing a sirtuin.