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 application relates to long acting injectable (LAI) formulations for combating ectoparasites and endoparasites in mammals. In particular, this invention provides for a LAI formulation comprising a subcutaneously volatile solvent, a biologically acceptable polymer, a bioactive agents and optionally one or more anti-ectoparasitically or anti-endoparasitically acceptable additive or excipient. Surprisingly, the liquid long acting injectable formulations of the invention solve the problems associates with previous injectable formulations by having long term stability, being able to accommodate smaller needle diameters and achieving long acting effects in the control of pests in a mammal. The unique formulations of the invention also allow for combating ectoparasites and endoparasites which have become resistant to macrolide antibiotics.

Abstract: A compound of the formula is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.

Abstract: The present invention provides a patch having a backing and a pressure-sensitive adhesive layer on the backing, wherein the pressure-sensitive adhesive layer contains a pressure-sensitive adhesive base composed of a polymer having a hydroxyl group, a drug, polyvinylpyrrolidone and a multivalent metal chloride.

Abstract: Methods and compositions for treating inflammatory and proliferative diseases, enabling treatment of MDR tumor cells by using combination of compounds, or a bifunctional compound, that inhibits both fatty acid metabolism and glycolysis. In particular, the invention combines or links a glycolysis inhibitor that is, or that is derived from, hypoglycin A (also referred to as hypoglycine A) and a fatty acid metabolism inhibitor. Preferably, the invention provides bifunctional compounds that link a moiety having the functionality of an oxirane carboxylic acid compound to a moiety having the functionality a hypoglycin A derivative. In specific embodiments, the invention provides a bifunctional compound that links a moiety having the functionality of etomoxir to a moiety having the functionality of hypoglycin A.

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: A method of treating an ocular disorder in a subject associated with aberrant all-trans-retinal clearance in the retina, the method comprising administering to the subject a therapeutically effective amount of a primary amine compound of formula: wherein R1 is an aliphatic and/or aromatic compound.

Abstract: The present invention relates to compounds which are inhibitors of the 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme. The present invention further relates to the use of inhibitors of 11-beta-hydroxysteroid dehydrogenase Type 1 enzyme for the treatment of non-insulin dependent type 2 diabetes, insulin resistance, obesity, lipid disorders, metabolic syndrome and other diseases and conditions that are mediated by excessive glucocorticoid action.

Abstract: Novel histone deacetylase inhibitors, including novel fluorescent histone deacetylase inhibitors, are described. Methods for making and using the same, e.g., to treat cancer, are provided.

Abstract: The present invention concerns a family of sulfanilamide derivatives of formula (I) as anticonvulsant agents, where R is selected from optionally substituted C4-C9 alkyl, optionally substituted C6-C10 aryl, optionally substituted C6-C10 alkylenearyl and optionally substituted C5-C10heteroaryl; R2 is selected from —H and optionally substituted C1-C6 alkyl; each of R3 and R4, independently of each other, is selected from —H, optionally substituted C1-C6 alkyl, optionally substituted C6-C10 aryl and optionally substituted C5-C10 heteroaryl; n is 0, 1, 2, 3 or 4. The derivatives have been prepared and their anticonvulsant profile was evaluated for the control of epileptic seizures.

Abstract: Drug tablets that include a prolonged-release core and an immediate-release layer or shell are prepared with a thin barrier layer of drug-free polymer between the prolonged-release and immediate-release portions of the tablet. The barrier layer is penetrable by gastrointestinal fluid, thereby providing lull access of the gastrointestinal fluid to the prolonged-release core, but remains intact during the application of the immediate-release layer, substantially reducing or eliminating any penetration of the immediate-release drug into the prolonged-release portion.

Abstract: The present invention provides novel methods and formulations for treating anxiety disorders, including Post Traumatic Stress Disorder, in human subjects employing coordinate treatment using ? and ? blockers alone or in combination with additional psychotherapeutic medications to treat the anxiety disorder and reduce symptomology in treated subjects.

Abstract: The invention relates to an process for preparing Tamsulosin hydrochloride of Formula (I) which comprises (i) reacting (R)-(?)-5-(2-amino-propyl)-2-methoxybenzenesulfonamide of Formula (II) with substituted phenoxy compound of Formula (III), wherein Z represents a removing group, such as —OSO2CH3, —OSO2C6H4CH3, —F, —Br, —Cl, or —I, in a solvent in the presence of an alkaline earth metal oxide to obtain Tamsulosin base and (ii) converting Tamsulosin base into hydrochloride salt in a solvent by addition of aqueous hydrochloric acid.

Abstract: The present invention provides compounds that are effective in treating central nervous system disorders and maintaining normal brain function. Methods of making and using the compounds are also provided.

Abstract: A pharmaceutical composition for inhibiting osteoclast growth is disclosed in the present invention. The pharmaceutical composition includes a compound represented by a formula (I), and a pharmaceutically acceptable salt and carrier: wherein R1, R2, R3, R4 can be one selected from a group consisting of hydrogen, halogen, C1?C10 alkyl group, C2?C10 alkynyl group, amino group, haloalkyl group and sulfonamide group.

Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic Bcl-2 proteins, compositions containing the compounds and methods of treating diseases during which is expressed anti-apoptotic Bcl-2 protein.

Abstract: The present invention relates to a sulfonamide derivative which is useful as an active ingredient of pharmaceutical preparations. The sulfonamide derivatives of the present invention have CCR3 (CC type chemokine receptor) antagonistic activity, and can be used for the prophylaxis and treatment of diseases associated with CCR3 activity, in particular for the treatment of asthma, atopic dermatitis, allergic rhinitis and other inflammatory/immunological disorders.

Abstract: The present invention relates to sulphonamide derivatives, whith a urea moiety. The invention also relates to the use of the derivatives as inhibitors of collagen receptor integrins, especially ?2?1 integrin inhibitors e.g. in connection with diseases and medical conditions that involve the action of cells and platelets expressing collagen receptors, their use as a medicament, e.g. for the treatment of thrombosis, inflammation, cancer and vascular diseases, pharmaceutical compositions containing them and a process for preparing them. The sulphonamide derivatives have the general formula (I) or (I?).

Abstract: The various embodiments herein provide a gel based wound dressing comprising a lyophilized powder and a water-based solvent. The lyophilized powder comprises several nanoparticles and water miscible natural or synthetic polymers. The nanoparticles comprises pectin and a wound healing agent or an anti-microbial agent. The anti-microbial agent is nisin. The lyophilized powder and the water-based solvent are kept in two separate sealed packages and are mixed together before applying on a wound. The embodiments herein also provide a method of synthesizing the gel based wound dressing. The nano-particles control a release of the wound healing agent or the antimicrobial agent to a wound.

Abstract: Compounds, methods, uses, compositions, kits and packages for the treatment of imbalance between bone resorption and bone formation, based on uses of 4-phenyl-2-propionamidotetralin (4-P-PDOT) and analogs, derivatives, prodrugs, precursors thereof, and salts thereof, are described.

Abstract: The mechanism by which the high bone mass (HBM) mutation (G171V) of the Wnt coreceptor LRP5 regulates the canonical Wnt signaling was investigated. The mutation was previously shown to reduce Dkk protein-1-mediated antagonism, suggesting that the first YWTD repeat domain where G171 is located may be responsible for Dkk protein-mediated antagonism. However, we found that the third YWTD repeat, but not the first repeat domain, is required for DKK1-mediated antagonism. Instead, we found that the G171V mutation disrupted the interaction of LRP5 with Mesd, a chaperon protein for LRP5/6 that is required for the coreceptors' transport to cell surfaces, resulting in less LRP5 molecules on the cell surface. Although the reduction in the level of cell surface LRP5 molecules led to a reduction in Wnt signaling in a paracrine paradigm, the mutation did not appear to affect the activity of coexpressed Wnt in an autocrine paradigm.

Abstract: A method is provided for the prevention of cancer metastasis in a patient comprising administering an adrenergic receptor antagonist to a patient in need thereof. The invention also includes an adrenergic receptor antagonist for use in the prevention of tumour recurrence in a patient. Also provided is a kit of parts for use in such methods comprising an adrenergic receptor antagonist, and an administration vehicle. A method is further included for identifying a patient at risk of developing cancer comprising the step of assaying for levels of expression of adrenergic receptor genes and proteins in said patient.

Abstract: Substituted sulphonamides having the general formula (I) and salts, hydrates and solvates thereof were prepared and described, wherein R1 is CO or SO2 and R2 is NH or O and where R represents linear or cyclic aliphatic chain and n represents number of linking aliphatic chain carbons (n can be 0, 1, 2 or 3), which are useful in the manufacture of the medicaments due to the carboanhydrase inhibition. These compounds are prepared by nucleophilic reaction of an amine with 4-sulfamoylbenzenesulphonyl chloride in the presence of triethylamine excess in tetrahydrofurane or in ether at temperature 0 to 20° C. The compounds show an antiglaucomatic activity.

Abstract: The invention is directed to compounds of formula I: wherein Ar, r, R3, X, and R5-7 are as defined in the specification, and pharmaceutically acceptable salts thereof. The compounds of formula I have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and a process and intermediates for preparing such compounds.

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: Compounds exhibiting calcium receptor antagonist activity that are safe and orally administrable having Formula (I) or pharmaceutically acceptable salts thereof:

Abstract: New compounds are continually being sought for the treatment and prevention of disorders. The invention relates to N-substituted-N-phenylethylsulfonamides libraries which can be used in the search for, and identification of, new lead compounds that could modulate the functional activity of a biological target.

Abstract: The present invention is directed to, inter alia, methods of treating or ameliorating an effect of a polycystic disease. This method include administering to a patient in need thereof an amount of a modulator of a histone deacetylase (HDAC) path-way, which is sufficient to treat or ameliorate an effect of a polycystic disease, particularly a polycystic kidney disease.

Abstract: PAD4 inhibitory compositions and methods for their use in treatment of cancer and autoimmune disease are provided according to embodiments of the present invention.

Abstract: The invention relates to methods and products for enhancing and improving recovery of lost memories. In particular the methods are accomplished by inhibiting HDAC2 and or selectively inhibiting HDAC1/2 or HDAC1/2/3.

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: Oral dosage forms for poorly soluble amine drugs are provided. Such dosage forms include an ionizable compound such as an organic acid, an amphiphilic polymer and a release rate-controlling membrane. Such dosage forms allow for the consistent release of the active agent in both gastric pH conditions and in the intestine. Methods of making such dosage forms are also provided.

Abstract: The present invention provides a sustained-release pharmaceutical composition, characterized in that there are contained tamsulosin or a pharmaceutically acceptable salt thereof and a carrier for a sustained-release pharmaceutical composition and the ratio (Cmin/Cmax ratio) of the plasma tamsulosin concentration at 24 hours after the administration of the preparation per os (Cmin) to the maximum plasma tamsulosin concentration after the administration (Cmax) is about 0.4 or more.

Abstract: The invention is directed to compounds of formula I: wherein Ar, r, R3, X, and R5-7 are as defined in the specification, and pharmaceutically acceptable salts thereof. The compounds of formula I have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and a process and intermediates for preparing such compounds.

Abstract: Organic compounds showing the ability to inhibit bacterial omptin proteases, specifically Yersinia pestis plasminogen activator (Pla) are disclosed. The disclosed Y. pestis plasminogen activator inhibitor compounds are useful for treating, preventing, or reducing the spread of infections by Y. pestis.

Abstract: The present invention discloses a wound dressing which may be a double-layer wound dressing, comprising a polymer material layer in combination with anti-infective antibiotics or anti-infective Chinese herb medicine at the upper layer of the wound dressing, and a porous carbon material layer capable of loading with skin-associated epithelial cells at the lower layer of the wound dressing. The wound dressing with the antibiotics can block effectively the invasion of bacteria in the external environment, thereby preventing the wound from secondary infection. While covering the wound site, the porous carbon material layer with the epithelial cells can thus provide the healthy epithelial cells and attract the surrounding healthy cells to aggregate for secreting collagen so as to promote the wound healing process. According to the present invention, there is an obviously enhancing effect on wound tissue regeneration, restoration and healing, and there is a grant development potential in clinical applications.

Abstract: Compounds of formula (I) and pharmacologically acceptable salts and pro-drugs wherein: Ar1 and Ar2=aryl or heteroaryl; a=0 to 5; R1=alkyl, halogen, haloalkyl, alkoxy, alkoxycarbonyl, carboxyl, hydroxyl, amino, monalkylamino, dialkylamino, nitro, acylamino, alkoxycarbonylamino, alkylsulphonyl, alkylsulphonylamino and cyano and, where a is >1, each R1 is the same or different; b=0 to 5; R2=alkyl, halogen, haloalkyl, alkoxy, alkoxycarbonyl, carboxyl, hydroxyl, amino, monalkylamino, dialkylamino, nitro, acylamino, alkoxycarbonylamino, alkylsulphonyl, alkylsulphonylamino and cyano and where b is >1, each R2 is the same or different; V=(CR3aR3b)pSO2N(R3b)X and (CR3aR3b)pN(R3b)SO2(X); W=NR4a, O, S, S?O, SO2 and C(R4aR4b)2; X=hydroxyalkyl, alkoxyalkyl, haloalkoxyalkyl, aryloxyalkyl, polyalkylene glycol residues, aminoalkyl, monoalkylaminoalkyl, dialkylaminoalkyl and alkyl groups substituted with ?1 NR8R9 groups wherein R8 and R9+nitrogen atom form a saturated or partially unsaturated heterocyc

Abstract: The present invention relates to a stable orally disintegrating coated tablet containing a drug, wherein the tablet is coated with a coating layer containing a water-soluble substance and a polyvinyl alcohol resin of not less than 5% by weight based on the weight of the coating layer, the water-soluble substance dissolving in an amount of 1 g or more in less than 10 mL of water at 20° C., having a hydroxyl group(s) in its molecule, and having a molecular weight of not more than 200 per a unit hydroxyl group. There is provided a stable orally disintegrating coated tablet which does not cause a crack in the coating layer even when the orally disintegrating tablet has been swollen by moisture absorption under high humidity, while ensuring rapid disintegration properties in an oral cavity. In the case of an orally disintegrating tablet containing a light-unstable drug, degradation of the drug can be suppressed by blending a light shading agent in the coating layer.

Abstract: The present disclosure provides for compounds, pharmaceutical preparations, kits and methods for the inhibition of the Hh pathway and the alleviation of cancer and developmental disorders associated with the Hh pathway.

Abstract: The invention relates to novel compounds that have S1P receptor modulating activity and, preferably, apoptotic activity and/or anti proliferative activity against cancer cells and other cell types. Further, the invention relates to a pharmaceutical comprising at least one compound of the invention for the treatment of diseases and/or conditions caused by or associated with in-appropriate S1P receptor modulating activity or expression, for example, cancer. A further aspect of the invention relates to the use of a pharmaceutical comprising at least one compound of the invention for the manufacture of a medicament for the treatment of diseases and/or conditions caused by or associated with inappropriate S1P receptor modulating activity or expression such as cancer.

Abstract: Polymeric porous films, capable of eluding a bioactive agent when coming in contact with a physiological medium according to a pre-determined and controlled release profile suitable for particular type of drug and indication, and medical devices including the same are disclosed. Also disclosed are processes for producing the polymeric porous films by freeze-drying an inverted emulsion formulation in which the polymer's composition, the polymer's concentration, the polymer's initial molecular weight, the concentration and/or the type of a surfactant, the homogenization rate and/or the oil phase to aqueous phase ratio (O:A) are selected so as to impart a desired release profile of the bioactive agent from the polymeric film.

Abstract: Methods of using apogossypol and its derivatives for treating inflammation is disclosed. Also, there is described a group of compounds having structure A, or a pharmaceutically acceptable salt, hydrate, N-oxide, or solvate thereof are provided: wherein each R is independently H, C(O)X, C(O)NHX, NH(CO)X, SO2NHX, or NHSO2X, wherein X is hydrogen, alkyl, substituted alkyl, aryl, substituted aryl, alkylaryl, substituted alkylaryl, heterocycle, or substituted heterocycle. Compounds of group A may be used for treating various diseases or disorders, such as cancer.

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: This invention is directed to a pharmaceutical composition comprising the sodium-hydrogen exchanger (NHE) inhibitor cariporide and an angiotensin converting enzyme (ACE) inhibitor which exhibits unexpectedly efficacious properties for preventing heart failure and other age-related organ dysfunctions, age-related disorders and for prolonging life, and to methods of preventing heart failure and other age-related organ dysfunctions, age-related disorders and for prolonging life comprising administering pharmaceutically effective amounts of the sodium-hydrogen exchange inhibitor cariporide and an ACE inhibitor.

Abstract: The present invention relates to the use of a sulfonamide compound of formula (I): wherein R1 is selected from the group consisting of H, CN, halogen, trifluoromethyl, methyl, ethyl, hydroxy, methoxy, ethoxy, morpholino, R2 is selected from H, phenyl, substituted phenyl, CN, —SO2R, wherein R is phenyl or morpholino, —NC(O)Me, —NC(O)Et, —CH2C(O)OMe, CH2C(O)OEt, R3 is selected from the group consisting of H, NO2, NH2, halogen, —COOMe, —COOEt, RC(O)N—, morpholino, R4 is selected from the group consisting of H, a branched or unbranched methyl, ethyl, propyl, butyl, pentyl, methoxy, ethoxy, propoxy, butoxy, a substituted or unsubstituted phenyl, alkinyl, Me2SO2—, COOR, wherein R is a branched or unbranched methyl, ethyl, propyl, butyl, pentyl, -MeOC(O)—, a substituted or unsubstituted five or sixmembered aromatic or non-aromatic heterocyclic system with one, two or three heteroatoms, a hetaryl system, a condensed benzoheterocyclic system, X is a linker comprising 2 or 3 atoms, selected from the group consisting of

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 the formula I wherein R1a is H; and R1b is C1-C6 alkyl, Carbocyclyl or Het; or R1a and R1b together define a saturated cyclic amine with 3-6 ring atoms; R2a and R2b are H, halo, C1-C4alkyl, C1-C4haloalkyl, C1-C4alkoxy; or R2a and R2b together with the carbon atom to which they are attached form a C3-C6cycloalkyl; R3 is a branched C5-C10alkyl chain, C2-C4haloalkyl or C3-C7cycloalkylmethyl, R4 is Het, Carbocyclyl, optionally substituted as defined in the specification and pharmaceutically acceptable salts, hydrates and N-oxides thereof; are inhibitors of cathepsin S and have utility in the treatment of psoriasis, autoimmune disorders and other disorders such as asthma, arteriosclerosis, COPD and chronic pain

Abstract: The present invention provides a novel mechanistic pathway and methods related to this pathway for the identification of compounds for the treatment of diseases involving cell proliferation, invasion and/or metastasis such as cancer. In particular, the instant invention relates to the phosphatase activity of Eya and the Eya-Six complex as a target for identifying novel therapeutic agents for the treatment of proliferative, invasive and/or metastatic disorders, and compositions identified using the methods disclosed herein.

Abstract: The present invention provides a film-form base having one or more sugars or sugar alcohols dispersed as fine particles therein, and also provides a film-form preparation containing the base and a drug. The base is produced by dispersing, in an organic solvent having a solubility parameter of 9.7 or higher, an edible polymer soluble in water and the organic solvent, and particles of one or two or more compounds selected from the group consisting of mono- to hexasaccharide sugars and sugar alcohols thereof which have an average particle size of 0.1 ?m to 60 ?m and are insoluble in an organic solvent. The present invention can therefore provide oral film-form base and preparation which have a rapid dissolution profile in the mouth and sufficient film strength, and provide a reduced sticky sensation attributed to the water-soluble polymer in the mouth and an improved feel when handled with the fingers.

Abstract: The disclosed invention provides new polyamine analogs and derivatives containing a hydrophobic region and a polyamine region as well as methods and compositions for their use.