Abstract: The present invention relates to inhibitors of 11-? hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-? hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess.

Abstract: Chemical entities that modulate smooth muscle myosin and/or non-muscle myosin, pharmaceutical compositions and methods of treatment of diseases and conditions associated with smooth muscle myosin and/or non-muscle myosin are described.

Abstract: The present invention is related to chemical compositions, processes for the preparation thereof and uses of the composition. Particularly, the present invention relates to compositions of compounds of Formula (A): wherein Ar, X, Y, R1, R2, R3, and q are as defined herein; and their use in the treatment of diseases, including treatment of sleepiness, promotion of wakefulness, treatment of Parkinson's disease, cerebral ischemia, stroke, sleep apneas, eating disorders, stimulation of appetite and weight gain, treatment of attention deficit hyperactivity disorder (“ADHD”), enhancing function in disorders associated with hypofunctionality of the cerebral cortex, including, but not limited to, depression, schizophrenia, fatigue, in particular, fatigue associated with neurologic disease, such as multiple sclerosis, chronic fatigue syndrome, and improvement of cognitive dysfunction.

Abstract: Films containing microsphere particles and processes for forming thereof are disclosed. The microsphere particles encapsulate one or more bioactive agents and may be deposited on a surface of medical devices or be used to form a medical device.

Abstract: Aryl GPR119 agonists are provided. These compounds are useful for the treatment of diabetic diseases, including Type II diabetes and other diseases associated with poor glycemic control.

Abstract: The present invention provides compositions and methods that are useful for treatment of pain associated with acute herpes zoster. The aqueous compositions are non-stinging and non-irritating.

Abstract: A multiple total daily dose regimen is developed in order to decrease the use by a patient of a tolerance-inducing pharmacological agent. In one example, the method reduces or phases out altogether a patient's chronic use of opioid drugs by use of a successive reduction of the total daily dose of an opioid drug in sub-therapeutic decrements over the course of 3-7 days per therapeutic dose.

Abstract: Compounds are provided that are modulators of the C5a receptor. The compounds are substituted piperidines and are useful in pharmaceutical compositions, methods for the treatment of diseases and disorders involving the pathologic activation of C5a receptors.

Abstract: Inhibitors of BACE1 and compositions containing them are described. Use of the inhibitors and compositions containing them to treat Alzheimer's disease are described.

Abstract: Disclosed is a compound of formula (I). Wherein R1, R2Ar and Cy are as defined herein, or a pharmaceutically acceptable salt thereof. Also disclosed are pharmaceutical compositions of the compound of formula (I), methods of making the compounds of formula I, and methods of using the compounds of formula (I) to treat a disorder associated with activation of CCR10.

Abstract: A composition for modulating generation of pro-inflammatory cytokines comprises levocabastine or a pharmaceutically acceptable salt or ester thereof. Such composition is useful for treating or controlling diseases having an inflammatory component, such as ocular diseases that are caused by inflammation or have inflammatory sequelae.

Abstract: 3,4-substituted piperidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; pharmaceutical formulations comprising a 3,4-substituted piperidine compound, and/or a method of treatment comprising administering a 3,4substituted piperidine compound, a method for the manufacture of a 3,4-substituted piperidine compound, and novel intermediates and partial steps for their synthesis are disclosed. The 3,4-disubstituted piperidine compounds have the formula (I), wherein the symbols have the meanings defined in the specification.

Abstract: The present invention is related to N-hydroxyamide derivatives of Formula (I) and use thereof in particular for the treatment and/or prophylaxis of autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, cancer, respiratory diseases and fibrosis, including multiple sclerosis, arthritis, emphysema, chronic obstructive pulmonary disease, liver and pulmonary fibrosis.

Abstract: The present invention relates to novel compounds having anti-cancer activity, methods of making these compounds, and their use for treating cancer and drug-resistant tumors, e.g. melanoma, metastatic melanoma, drug resistant melanoma, prostate cancer and drug resistant prostate cancer.

Abstract: The present invention relates to compounds of the general formula as dual modulators of the 5-HT2a and D3 receptors useful against CNS disorders, wherein A, R1, R2, n, p, q and r are as defined in the specification.

Abstract: The invention relates to methods for the treatment or prevention of substance use disorders.

Abstract: The present disclosure provides a liposomal system comprising an aqueous medium having dispersed therein liposomes encapsulating in their intraliposomal aqueous compartment at least one active agent, the aqueous medium being in iso-osmotic equilibrium with said intraliposomal aqueous compartment, the liposomes having a membrane comprising a liposome forming lipids, at least one of which being sphingomyelin (SPM), the liposomal system having increased stability as compared to the same liposomes free of SPM, and in one embodiment being stable during long-term storage, said stability being characterized in that no more than 30% of the at least one active agent is present in the aqueous medium after said storage.

Abstract: The present invention generally relates to the field of pharmaceutical sciences. More specifically, the present invention includes apparatus and devices for the preparation of pharmaceutical formulations containing large diameter synthetic membrane vesicles, such as multivesicular liposomes, methods for preparing such formulations, and the use of specific formulations for therapeutic treatment of subjects in need thereof. Formation and use of the pharmaceutical formulations containing large diameter synthetic membrane vesicles produced by using the apparatus and devices for therapeutic treatment of subjects in need thereof is also contemplated.

Abstract: The present application describes substituted piperidinyl modulators of MIP-1? or CCR-1 or stereoisomers or pharmaceutically acceptable salts thereof. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and transplant rejection using said modulators are disclosed.

Abstract: The present disclosure provides a composition of matter comprising liposomes encapsulating in their intraliposomal aqueous compartment at least one active agent, the liposomes having a diameter of at least 200 nm and being embedded in a water insoluble, water absorbed cross-linked polymeric matrix. In one embodiment, the composition of matter is held within an aqueous medium, preferably being in iso-osmotic equilibrium with the intraliposomal aqueous compartments of the liposomes.

Abstract: Novel compounds of the general formula (I), the use of these compounds as pharmaceutical compositions, pharmaceutical compositions comprising the compounds and methods of treatment employing these compounds and compositions. The present compounds are activators of PPAR? and should be useful for treating conditions mediated by the same.

Abstract: Surgical implants of the present disclosed include a film comprising a first therapeutic agent and a mesh comprising a second therapeutic agent. The surgical implant includes a film in direct contact with a mesh. The first therapeutic agent may be released at a first rate and the second therapeutic agent may be released at a second rate.

Abstract: Surgical implants of the present disclosed include a film comprising a first therapeutic agent and a mesh comprising a second therapeutic agent. The surgical implant includes a film in direct contact with a mesh. The first therapeutic agent may be released at a first rate and the second therapeutic agent may be released at a second rate.

Abstract: A drug delivery device may include a base to be percutaneously affixable in an attachment zone of a synovial joint and a sustained-release drug carrier coupled to the base. The drug delivery device may also include an access device to provide access to the attachment zone. The attachment zone may comprise a non-articulating portion of a bone and/or cartilage with the synovial joint and the drug carrier may elute the drug into the synovial fluid sufficient to sustain a therapeutically effective concentration of the drug in the synovial fluid for at least 8 hours.

Abstract: The present invention relates to substituted amido phenoxybenzamide compounds of general formula (I): in which A, R1, R2, R3, R4, R5, R6, R7, R8, R9 and n are as defined in the claims, to pharmaceutical compositions and combinations containing said compounds, to methods of preparing said compounds, and to the use of said compounds or compositions for treating hyper-proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients.

Abstract: The invention relates to a compound of formula (I): Wherein m, n, X, Y, R1, R2, R3 and R4 are as defined herein. The invention also relates to the use of same in therapeutics.

Abstract: The present disclosure provides hydrogels that are suitable for drug delivery. In embodiments, hydrogels of the present disclosure may be used for transdermal delivery of bioactive agents, including drugs. The hydrogels of the present disclosure may also be useful as conductive compositions for use with electrodes.

Abstract: The present invention is directed to biologically active amides which are ligands at the NPY Y5 receptor. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a method of treating a subject suffering from certain disorders which comprises administering to the subject an amount of a compound of the subject invention. Furthermore, this invention also provides uses of a compound of the invention for the manufacture of a medicament for treating a subject suffering from certain disorders.

Abstract: The present invention is directed to 4,4-di-substituted piperidine derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by DPP-1.

Abstract: The invention relates to a pH-dependent controlled release pharmaceutical composition, comprising a core, and an opioid, wherein the core is coated at least by one coating layer, controlling the release of the pharmaceutical composition, wherein the coating layer comprises a polymer mixture of i) 40 95% by weight, based on dry weight of the polymer mixture, of at least one water insoluble essentially neutral vinyl polymer, and ii) 5 60% by weight, based on dry weight of the polymer mixture, of at least one anionic polymer or copolymer, which is insoluble in a buffered medium below pH 4.0 and soluble at least in the range from pH 7.0 to pH 8.0, characterized in that the coating layer further comprises 110 to 250 % by weight of a non-porous inert lubricant, 1 to 35 % by weight of a neutral cellulosic compound and 1 to 25 % by weight of an emulsifier, each calculated on dry weight of the polymer mixture.

Abstract: The present invention is directed to compounds that inhibit amyloid aggregation and methods of treatment there-with.

Abstract: The invention relates to compounds of formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.

Abstract: The present invention provides compounds of formula (I) in which n, y, X1, X2, A, B, R1, R2, R3, R4 and R5 are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them and their use in therapy.

Abstract: Compounds comprising or a pharmaceutically acceptable salt or a prodrug thereof are disclosed herein. Details are provided herein. Compositions, methods, and medicaments related thereto are also disclosed.

Abstract: A medical device includes a substrate having at least one surface. The surface has a central portion and a peripheral portion. At least one bioactive agent is disposed over at least a portion of the surface. The medical device having a concentration gradient of the at least one bioactive between the central and peripheral portions.

Abstract: Effective compositions and methods for treating an intervertebral disc are provided. The compositions and methods comprise a bulking agent or sealing agent, the bulking agent or sealing agent adapted to be administered at or within the intervertebral disc, the bulking or sealing agent having a drug depot comprising an effective amount of a therapeutic agent disposed therein, wherein the drug depot is capable of releasing an effective amount of the therapeutic agent over a period of at least one day.

Abstract: The present application describes substituted piperidinyl modulators of MIP-1? or CCR-1 or stereoisomers or pharmaceutically acceptable salts thereof. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and transplant rejection using said modulators are disclosed.

Abstract: The present invention provides compounds and methods for antagonizing the anticoagulant effect of an anticoagulant agent that is selected from UFH, LMWH, and a heparin/LMWH derivative in a patient comprising administering to the patient a compound of the invention or a salt thereof, or a composition comprising the same.

Abstract: The eye is effectively treated by providing it with formulations including uncoated cationically charged microparticles of reversed cubic phase or reversed hexagonal phase material. The treatment methods are effective; for a variety of diseases and conditions including dry eye. The structure, charge and components of the microparticles in dispersion, with or without an active ingredient, provide mucoadhesion, layering, protection and prolonged duration of ophthalmic action.

Abstract: The invention comprises systems and methods for treating nociceptive pain including at least one force-regulatable device in mechanical, electrical, or chemical communication with at least one brain area identified as processing nociceptive pain signals. The force-regulatable device acts to alter the nociceptive pain signals in a brain area to alleviate nociceptive pain.

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: A compound of Formula I and enantiomers, diastereomers and pharmaceutically-acceptable salts thereof. Also disclosed are pharmaceutical compositions containing compounds of Formula I, and methods of treating conditions associated with the activity of p38 kinase.

Abstract: Methods of attenuating the toxic or medically undesirable effects of drugs and toxins in a human by administering to a human an injectable formulation comprised of a dispersion of particles comprised of reversed cubic or reversed hexagonal lyotropic liquid crystalline material. The particles absorb or adsorb or otherwise sequester and attenuate the effect of drugs and toxins, and may be used as a rescue or reversal agent, or as a prophylaxis. The invention is especially applicable in reversing adverse effects of local anesthetics inadvertently delivered systemically, and attenuating the therapeutic effects of general anesthetics in the course of treatment.

Abstract: A transdermal patch having a top region containing an antagonist followed by a bottom region containing an agonist, whereby the bottommost end of the bottom region is secured to the skin of the patient for delivering a prescribed dosage of agonist to the patient over a predetermined period of time, the antagonist will be released by migrating or moving from the top region through the bottom region to the patient to prevent overdose. Visual indicators are provided in the patch for changing color to separately indicate the operation of the patch, delivery of prescribed dosage, and/or overdosage.

Abstract: The invention relates to novel modulators of the cold menthol receptor TRPM8, to a method for modulating the TRPM8 receptor using said modulators; to the use of the modulators for induction of cold sensation; and to objects and means produced using said modulators.

Abstract: Described herein are compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions that include the compounds described herein, and methods of using such antagonists of PGD2 receptors, alone or in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.

Abstract: Deeply scored pharmaceutical tablets are disclosed, along with pharmaceutical tablets with a score in a segment that adjoins a segment lacking a pharmacologically effective dose of any drug.

Abstract: A compound of formula A1 or A2 for use in the treatment of a demyelinating peripheral neuropathy: wherein A is COOR5, OPO(OR5)2, PO(OR5)2, SO2OR5, POR5OR5 or 1H-tetrazol-5-yl, R5 being H or an ester-forming group, optionally C1-6alkyl; W is a bond, C1-3alkylene or C2-3alkenylene; Y is C6-10aryl or C2-9heteroaryl eg C3-9heteroaryl, optionally substituted by 1 to 3 radicals selected from halogen, OH, NO2, C1-6alkyl, C1-6alkoxy; halo-substituted C1-6alkyl and halo-substituted C1-6alkoxy; Z is chosen from: wherein the asterisks of Z indicate the point of attachment between —C(R3)(R4)— and A of Formula Ia or Ib, respectively; R6 is chosen from hydrogen and C1-6alkyl; and J1 and J2 are independently methylene or a heteroatom chosen from S, O and NR5; wherein R5 is chosen from hydrogen and C1-6alkyl; and any alkylene of Z can be further substituted by one to three radicals chosen from halo, hydroxy, C1-6alkyl; or R6 can be attached to a carbon atom of Y to form a 5-7 member ring; R1 is C6-10aryl or C

Abstract: The present invention relates to compounds of Formula (I) wherein Ar is optionally substituted phenyl or 6-membered heteroaryl moiety, or a benzisoxazole, pyrrolopyridine, or benzotriazole group; or a pharmaceutically acceptable salt thereof; processes for the preparation of the compounds; intermediates used in the preparation of the compounds; compositions containing the compounds; and uses of the compounds in treating diseases or conditions associated with fatty acid amide hydrolase (FAAH) activity, including pain, urinary incontinence, overactive bladder, emesis, cognitive disorders, anxiety, depression, sleeping disorders, eating disorders, movement disorders, glaucoma, psoriasis, multiple sclerosis, cerebrovascular disorders, brain injury, gastrointestinal disorders, hypertension, or cardiovascular disease.

Abstract: The present invention concerns a composition useful as bone substitute comprising one or more calcium-phosphate compounds in association with an analgesic. It also refers to a preparation process of said composition, a preparation process of a drug-combined device comprising said composition, the drug combined device thus obtained, a kit comprising said composition and the use of said composition for the preparation of a drug-combined device useful for filling a bony defect caused in the iliac crest by collection of auto-graft bone, as a scaffold for tissue engineering and to produce a dental or bony implant.