Abstract: Methods, compounds, and topical formulations for reduction of skin sagging, creasing and/or wrinkling are disclosed. The methods comprise topically applying a composition comprising an ?2 adrenergic receptor agonist. Amelioration of skin sagging, creasing and/or wrinkling begins within minutes after topical application of a disclosed composition. A single application can significantly reduce skin sagging, creasing and/or wrinkling for at least about 8 hours.

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: The present invention provides compositions and methods for treating or preventing atrial fibrillation (AF). In particular, the present invention provides administration of muscarinic receptor antagonists (e.g., M2-selective muscarinic receptor blockers), administered alone or in combination with other therapeutic agents (e.g., beta-adrenergic receptor blockers) to treat and/or prevent atrial fibrillation.

Abstract: Small molecule inhibitors of bacterial nicotinamide adenine dinucleotide synthetase (NADs), bacterial nicotinic acid mononucleotide adenylyltransferase (NaMNAT), and human nicotinamide mononucleotide adenylyltransferase (NMNAT) are provided, as well as methods of making and using the inhibitors.

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 compounds of formula (I) wherein X, R1, R2, R3, R4 and R5 are as defined herein, which are useful for treating diseases which respond to CXCR2 receptor mediators. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.

Abstract: The present invention relates to compounds of formula (I) wherein X, R1, R2, R3, R4 and R5 are as defined herein, which are useful for treating diseases which respond to CXCR2 receptor mediators. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.

Abstract: The invention relates to a population of tamsulosin-comprising pellets for oral administration of a combination dosage form containing physically separated a tamsulosin dose in the form of the population of the tamsulosin comprising pellets and at least one other dose of a pharmaceutically active substance, said pellets comprising tamsulosin hydrochloride uniformly dispersed in a carrier matrix, wherein (i) said pellets in the population have a size of less than about 1.4 mm and, advantageously, at least 90% of the pellets have a size of larger than 0.30 mm; and (ii) an average content of tamsulosin hydrochloride in the population of pellets is between about 0.15-3.00 weight percent, calculated on a dry pellet basis, to a process of making such population of pellets, and to their use.

Abstract: A tamsulosin controlled release tablet is formed using a water-swellable matrix-forming composition as a release controlling mechanism. The matrix forming composition comprises (i) a pH-sensitive swellable hydrophilic polymer, which is a cross-linked polyacrylic acid polymer, and (ii) a pH-insensitive swellable hydrophilic polymer. The tablet optionally contains a water insoluble binder as well.

Abstract: The invention relates to inhibitors of tissue transglutaminase II activity and their use as a tocolytic agent.

Abstract: This invention relates generally to methods and pharmaceutical formulations useful in treating patients suffering from obstructive sleep apnea syndrome (OSAS). Treatment of OSAS is effected by administering a carbonic anhydrase inhibitor to the patient in combination with at least one additional active agent. Examples of additional active agents include modafinil, eszopiclone, zolpidem, zaleplon, and phentermine.

Abstract: A preparation for external use which, even when ingredients such as a drug, absorption accelerator, and plasticizer are contained therein in a large amount, is excellent in pressure-sensitive adhesive properties including cohesive force and which, when a drug is contained therein, enables the drug to have excellent percutaneous absorbability. The preparation for external use includes a pressure-sensitive-adhesive matrix layer, wherein the pressure-sensitive-adhesive matrix layer comprises a pressure-sensitive adhesive base comprising a hydroxylated polymer, a boron compound, and silicic acid.

Abstract: The present invention provides compositions containing one or more antimicrobial peptide sequestering compounds and methods for topical application of such compositions to the skin to treat skin diseases and disorders such as rosacea in humans.

Abstract: Disclosed is a controlled-release microparticle: including a matrix comprising a pharmacologically active component; and a controlled-release layer comprising a substance which forms a controlled-release stratum on the matrix. The disclosed controlled-release microparticle not only allows effective dual release control of a drug but can also exhibit outstanding dissolution characteristics even when a small amount of coating substance is used.

Abstract: The subject invention concerns compounds having activity as inhibitors of proteasomes and methods of using the subject compounds.

Abstract: Acrylamido derivatives useful as therapeutic agents, particularly for the prevention and/or treatment of diseases and conditions associated with the activity of the mitochondrial permeability transition pore (MPTP), such as the diseases characterized by ischemia/reperfusion, oxidative or degenerative tissue damage, are herein described. These compounds belong to the structural formula (I) wherein R, R?, R?, W and a are as defined in the specification. The invention also relates to the preparation of these compounds, as well as to pharmaceutical compositions comprising them.

Abstract: A compound of formula (I) as well as pharmaceutically acceptable salt thereof, wherein R1 to R4 and Ar are as defined in description and in claims, can be used as a medicament.

Abstract: Organosulfur compounds of the general formula (2) are described, wherein R1 and R2 are linear or branched C1-C5 alkyl; linear or branched C1-C5 alkenyl with the proviso that R1 is not prop-1-enyl (allyl); substituted linear or branched C1-C5 alkenyl or substituted linear or branched C1-C5 alkyl, in which the substituents are selected from OR3, NR4R5, COOR6, CON—R7R8, in which R3 is selected from H, COR9, para-methoxybenzyl and trialkylsilyl, in which R9 is alkyl or substituted alkyl; R4 N and R5 are alkyl or R4 and R5 together form a phthalimido group; R6 is alkyl or substituted alkyl; and R7 and R8 are alkyl or substituted alkyl; substituted or unsubstituted aromatic specifically where R1 and R2 are benzyl, para-methoxybenzyl and/or ortho,para-methoxybenzyl and substituted or unsubstituted heteroaromatic. The compounds can be used for inhibiting the growth of tumour cells and for treating cancer. A pharmaceutical composition and a method of preparing the compounds are also described.

Abstract: Compounds, including 3-carboxy aryl sulfonamide compounds, which agonize or antagonize aquaporin channels and methods of using them to treat disorders or diseases mediated by aquaporins.

Abstract: The present invention provides compositions and methods for noninvasive delivery of therapeutic agents across an intact tympanic membrane. For example, the compositions include a penetration enhancer which increases the flux of a therapeutic agent (e.g., antibiotic) across the tympanic membrane. Such compositions are particularly useful in the treatment of otitis media. Additionally, the composition may include a sustained release agents that, in some embodiments form sustained release reservoirs, in situ, once administered to a patient.

Abstract: The invention relates to methods of treating, preventing or delaying the onset or development of pulmonary hypertension using hydroxyl donors or pharmaceutically acceptable salts thereof. The invention further relates to methods of reducing mean pulmonary arterial pressure using hydroxyl donors or pharmaceutically acceptable salts thereof.

Abstract: This invention relates to novel derivatives of tolterodine, 5-hydroxymethyl tolterodine, fesoterodine and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by muscarinic receptor antagonists.

Abstract: The present invention pertains to compounds of the following formula (wherein RP, r, q, RN, Ralk, and Q are as defined herein) and compositions comprising those compounds. The compounds may be used to inhibit osteoclast survival, formation, and/or activity; to inhibit conditions mediated by osteoclasts and/or characterised by bone resorption; in the treatment of bone disorders such as osteoporosis, rheumatoid arthritis, cancer associated bone disease, Paget's disease; and/or in the treatment of conditions associated with inflammation or activation of the immune system.

Abstract: A pest control agent containing a compound represented by the following Formula (1), wherein A represents a carbon atom, a nitrogen atom, or the like, K represents a non-metal atom group necessary for forming a cyclic linking group derived from a 5- or 6-membered aromatic ring, in combination with A and two carbon atoms to which A bonds, X represents a hydrogen atom, a halogen atom, or the like, n represents an integer of from 0 to 4, T represents —C(=G1)-Q1 (wherein G1 and G2 represent an oxygen atom or the like, Q1 represents a phenyl group which may have a substituent, a heterocyclic group which may have a substituent, or the like), or the like, Q2 represents a phenyl group or the like, G3 represents an oxygen atom or the like, and R1 and R2 each independently represent a hydrogen atom, a C1-C6 alkyl group, or a group represented by -L-D, or the like (provided that at least either R1 or R2 represents a group represented by -L-D); as an active ingredient exhibits an excellent effect.

Abstract: The present invention provides a method for producing spherical fine particles containing tamsulosin hydrochloride, the method includes the steps of: (1) mixing and stirring tamsulosin hydrochloride (a), microcrystalline cellulose (b), and water until a mixture of the component (a) and the component (b) is uniformly impregnated with the water; (2) granulating the mixture obtained in step (1) using an stirring granulator whose peripheral speed is set to be 5.5 to 9.0 m/s; and (3) drying the granules obtained in step (2). The present invention also provides spherical fine particles obtained according to the method, coated fine particles obtained by applying a coating to the spherical fine particles, and an orally disintegrating tablet containing the coated fine particles.

Abstract: Composite structures composed of a device as a core structure, being a medical device or article, and a porous polymeric coat and designed capable of encapsulating bioactive agents while retaining the activity of these agents are disclosed. Further disclosed are processes of preparing such composite structures.

Abstract: The present invention relates to extended release dosage forms of metoprolol or salts thereof comprising a water insoluble and non-swellable inert core and one or more pharmaceutically acceptable excipients. The invention also relates to processes for the preparation of an inert core and extended release dosage forms.

Abstract: Use of chemical compounds obtained in silico for the preparation of pharmaceutical compositions to attenuate or inhibit Dengue virus infection. Particularly, through the interference or the modulation of several stages of viral replication cycle related with the entry of virus into host cells and the assembly of mature progeny virions. The invention also comprises the use of such pharmaceutical compositions for prophylactic and/or therapeutic treatment of infection caused by all four serotypes of Dengue virus and other flaviviruses.

Abstract: The present invention relates to a controlled release preparation of tamsulosin hydrochloride comprising hydroxypropylcellulose and polyethylene oxide, and the process for making such pharmaceutical composition.

Abstract: The present invention relates to the use of sulfonyl-substituted 2-sulfonylaminobenzoic acid N-phenylamides of the formula I, wherein A and R1 to R6 have the meanings indicated in the claims, for treating pain and for manufacturing a medicament for the treatment of pain.

Abstract: The invention provides compounds of formula wherein R1, R3, L1, L2, G1, G2, A and m are as defined in the specification and optical isomers, racemates and tautomers thereof, and pharmaceutically acceptable salts thereof; together with processes for their preparation, pharmaceutical compositions containing them and their use in therapy. The compounds are inhibitors of microsomal prostaglandin E synthase-1.

Abstract: The present invention provides a compound of formula (I): said compound is inhibitor of MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12 and/or MMP-13, and thus can be employed for the treatment of a disorder or disease characterized by abnormal activity of MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12 and/or MMP-13. Accordingly, the compound of formula (I) can be used in treatment of disorders or diseases mediated by MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12, and/or MMP-13. Finally, the present invention also provides a pharmaceutical composition.

Abstract: Multi-dose active agent packages and methods for using the same for treating a subject for a condition are provided. Aspects of the invention include a multi-dose active agent package containing a plurality of unit dosage forms of an active agent configured to modulate at least a portion of a subject's autonomic nervous system during at least one season of the year. The active agent is present in an amount sufficient to alter the parasympathetic activity/sympathetic activity ratio of the subject in a manner effective to treat the subject for the condition. The subject active agent packages and methods find use in the treatment of a variety of different conditions, including disease conditions that increase in severity and/or occurrence during one or more seasons of the year. Also provided are kits for use in practicing the subject methods.

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 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: 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 invention provides compounds of formula (I) wherein R1,R3,L1,L2,G1,G2, A and m are as defined in the specification and optical isomers, racemates and tautomers thereof, and pharmaceutically acceptable salts thereof; together with processes for their preparation, pharmaceutical compositions containing them and their use in therapy. The compounds are inhibitors of microsomal prostaglandin E synthase-1.

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: Disclosed are methods and compositions relating to modulators, such as agonists and antagonists, of HNF4?.

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 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: In an aspect of the invention, a composition for making a patch for the transdermal delivery of tamsulosin is provided. The composition comprises (a) at least about 1 wt % tamsulosin or a pharmaceutically acceptable salt of tamsulosin, (b) at least about 40 wt % polyisobutylene adhesive or hydrophobic synthetic rubber adhesive, (c) about 1-20 wt % of an aprotic solvent in which tamsulosin dissolves readily, (d) about 1-20 wt % of an unsaturated fatty acid or an alpha-hydroxy acid or a mixture of unsaturated fatty acids or alpha-hydroxy acids or of both unsaturated fatty acids and alpha-hydroxy acids, (e) a lipophilic permeation enhancer, and (f) a matrix modifier.

Abstract: The invention provides compounds of formula wherein R1, R2, R3, A and m are as defined in the specification and optical isomers, racemates and tautomers thereof, and pharmaceutically acceptable salts thereof; together with processes for their preparation, pharmaceutical compositions containing them and their use in therapy. The compounds are inhibitors of microsomal prostaglandin E synthase-1.

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: The present invention relates to methods and compounds for regulating or enhancing erthropoiesis and iron metabolism, and for treating or preventing iron deficiency and anemia of chronic disease.

Abstract: The invention relates to substituted enaminones of Formula I and their derivatives and the discovery that these compounds modulate the effect of ?-aminobutyric acid (GABA) on the GABAA receptor complex in a therapeutically relevant fashion and may be used to ameliorate CNS disorders amenable to modulation of the GABAA receptor complex.

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: 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: An adjunctive accessory article (25) for controlled release of at least a single physiologically active agent form an indwelling medical device so equipped is provided. The article is configurable as a tubular element upon a portion of the indwelling medical device, with barriers or facilitating coverings overlaying the carrier in furtherance of the controlled release of the active agent. To the extent that requires, affixation means for stable placement upon an indwelling device are further contemplated. Finally, a variety of application systems are described in connection to deployment of sleeve articles upon a portion of an indwelling device.

Abstract: Disclosed are compounds which inhibit the activity of anti-apoptotic protein family members, compositions containing the compounds and uses of the compounds for preparing medicaments for treating diseases during which occurs expression one or more than one of an anti-apoptotic protein family member.