Abstract: Kappa opioid receptor antagonists are provided that yield significant improvements in functional binding assays to kappa opioid receptors, and the use of these antagonists in treatment of disease states that are ameliorated by binding of the kappa opioid receptor such as heroin or cocaine addictions.

Abstract: The present invention relates to a selective estrogen receptor modulator of formula I or Ia: (I) (Ia); or a pharmaceutical acid addition salt thereof; useful for treating vasomotor symptoms, in particular hot flashes, night sweats and other symptoms that affect women around menopause.

Abstract: A method for treatment of cervical or vaginal cancer and their associated dysplasia, including the steps of identifying a human cervical or vaginal cancer and/or dysplasia patient, administering an effective amount of an estrogen antagonist therapy to the patient, wherein the amount is effective to reduce cancer and dysplasia symptoms, and observing a reduction of cancer and dysplasia symptoms in the patient.

Abstract: Compositions comprising melatonin and one or more carotenoids and methods for using such compositions for enhancing cognitive and related functions such as reducing or preventing a decline of social interaction, reducing or preventing age-related behavioral changes, increasing trainability, improving attention, maintaining optimal brain function, facilitating learning and memory, reducing memory loss, and preventing or treating cognitive decline caused by dementia in an animal. Preferably, the compositions are food compositions useful for enhancing cognitive function in humans and companion animals.

Abstract: Ophthalmic compositions comprising ketotifen and a source of hydrogen peroxide providing an amount of hydrogen peroxide of from about 0.001 to about 0.1% (w/v) of hydrogen peroxide, and methods for the treatment and prevention of allergic conjunctivitis using these compositions are provided herein.

Abstract: The present invention relates to methods and compositions for treating a subject suffering from a sclerosing disorder, comprising administering, to the subject, an effective amount of an estrogen receptor antagonist (“ERANT”), wherein said ERANT has essentially no estrogen receptor agonist activity under physiologic conditions.

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: Methods are provided for the treatment and/or prophylaxis of Huntington's disease. In various embodiments the methods involve administration of one or more serotonin receptor antagonists. In certain embodiments the serotonin receptor antagonists include, but are not limited to loxapine, and/or a loxapine analogue, and/or cyproheptadine, and/or a cyproheptadine analogue (e.g., pizotifen).

Abstract: The claimed subject matter is directed to certain thioxanthene derivatives and phenothiazine derivatives suitable for use as anti-infective agents, in particular, for the treatment of infectious diseases. The claimed subject matter furthermore relates to compositions including said anti-infective agents.

Abstract: There are disclosed racemic or enantiomerically enriched 3- or 4-substituted piperidine compounds represented by the following structural formula (I): or any of their isomers, or pharmaceutically acceptable salts thereof. Also disclosed are pharmaceutical compositions containing the subject compounds.

Abstract: Ophthalmic compositions comprising ketotifen, a source of hydrogen peroxide providing an amount of hydrogen peroxide of from about 0.001 to about 0.1% (w/v), one or more ocular-compatible hydrogen peroxide stabilizers, HPMC and CMC, and methods for the treatment and prevention of allergic conjunctivitis using these ophthalmic compositions are provided herein.

Abstract: The invention is directed to delta opioid receptor modulators. More specifically, the invention relates to tricyclic ?-opioid modulators. Pharmaceutical and veterinary compositions and methods of treating mild to severe pain and various diseases using compounds of the invention are also described.

Abstract: A method for treatment of cervical or vaginal cancer and their associated dysplasia, including the steps of identifying a human cervical or vaginal cancer and/or dysplasia patient, administering an effective amount of an estrogen antagonist therapy to the patient, wherein the amount is effective to reduce cancer and dysplasia symptoms, and observing a reduction of cancer and dysplasia symptoms in the patient.

Abstract: A drug delivery system is disclosed. The drug delivery system includes a recognitive polymeric hydrogel through which a drug is delivered by contacting biological tissue. The recognitive polymeric hydrogel is formed by using a bio-template, which is a drug or is structurally similar to the drug, functionalized monomers, preferably having complexing sites, and cross-linking monomers, which are copolymerized using a suitable initiator. The complexing sites of the recognitive polymeric hydrogel that is formed preferably mimics receptor sites of a target biological tissue, biological recognition, or biological mechanism of action. The system in accordance with an embodiment of the intention is a contact lens for delivering a drug through contact with an eye.

Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein A, B, G, Y, R1, R2, R3, and R4 are defined herein.

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

Abstract: To provide a compound which can be used for treating diseases in which a calcium sensing receptor (CaSR) participates, particularly hyperparathyroidism. It was found that a novel piperidine derivative which is characterized in that one of a 3-position and a 4-position is substituted with an aminomethyl group substituted with an arylalkyl group or the like and the other position is substituted with aryl, heteroaryl or the like, or a salt thereof, has an excellent CaSR agonistic regulatory action, and also has excellent selectivity with a CYP2D6 inhibitory action having a possibility of causing drug interaction. Based on the above, this novel piperidine derivative is useful as a therapeutic agent for diseases in which CaSR participates (hyperparathyroidism, renal osteodystrophy, hypercalcemia, and the like).

Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) and Formula (II) as follows: wherein Y, R1, R2, R3, R4, RA, and RB are defined herein.

Abstract: The present invention includes and provides a method of delivering a medicament to an eye of a subject in need thereof a solution, the method comprising: (a) providing droplets containing the medicament with a specified average size and average initial ejecting velocity; and (b) delivering the medicament to the eye, where the droplets deliver a percentage of the ejected mass of the droplets to the eye.

Abstract: The present disclosure provides products including an endocrine treatment product and a statin as a combined preparation for simultaneous, separate or sequential use in therapy. Further, there is provided a method of treatment of a mammalian breast cancer subject, comprising simultaneous, separate or sequential administration of therapeutically effective amounts of a statin and an endocrine treatment product.

Abstract: A pharmaceutical formulation of compounds with low aqueous solubility and method of manufacture thereof. The formulation may include a pharmacologically active compound having low aqueous solubility and starch in the amount of greater than about 25 weight percent. A manufacturing method may include blending the active compound and starch, compressing the blend into a solid, comminuting the solid into granules, wetting the granules, drying the granules, and tabletting the dried granules to make a solid pharmaceutical formulation.

Abstract: Disclosed are carboxamide, sulfonamide and amine compounds, as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure in which R1, R2, R4, E, T, n and x are as described herein. In certain embodiments, a compound disclosed herein activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.

Abstract: The present invention relates to novel materials, particularly biomaterials, in form of a precipitate, comprising at least an anionic polymeric component which is as such soluble in water and an amphiphilic ammonium-type component, which precipitate is obtainable by a process including the following steps: 1. contacting the anionic polymeric component and an cyclodextrin component in an aqueous medium, and 2. adding to the mixture obtained in step 1 said amphiphilic ammonium-type component, wherein said components are present in amounts effective to form said precipitate, and preferably to corresponding precipitates additionally comprising said cyclodextrin component. Both types of precipitates may optionally comprise one or more further components. The precipitates are particularly useful as controlled-release depot formulations suitable for long-lasting delivery of said further components.

Abstract: The present invention provides a percutaneously absorptive preparation for preventing or treating allergic eye disease, which comprises olopatadine or a salt thereof as an active ingredient. In addition, the present invention provides a method for preventing or treating allergic eye disease, which comprises applying a percutaneously absorptive preparation comprising olopatadine or a salt thereof to the skin surface including the skin surface of an eyelid, thereby casing transfer of a therapeutically effective amount of olopatadine or a salt thereof from the preparation to an anterior ocular segment through the skin of the eyelid rather than a systemic blood flow. The present preparation can exert a pharmacological effect over a prolonged period by a single application, as compared to conventional preparations such as eye drops.

Abstract: A pharmaceutical useful as a therapeutic agent and a preventive agent for hyperlipemia, and a pharmaceutical useful as a therapeutic agent and a preventive agent for hepatic disorders associated with cholestasis, particularly, primary biliary cirrhosis and primary sclerosing cholangitis, and a pharmaceutical useful as a therapeutic agent and a preventive agent for obesity, fatty liver and steatohepatitis are provided.

Abstract: The present invention relates to transdermal pharmaceutical compositions such as gels containing a SERM selected from the group consisting of endoxifen, droloxifene, clomifene, raloxifene, tamoxifen, 4-OH tamoxifen, toremifene, danazol and the pharmaceutically acceptable salts thereof, and to methods of making and using the same.

Abstract: Ophthalmic compositions are provided that comprise or consist essentially of (a) ketotifen or a ketotifen salt, (b) a non-ionic tonicity agent, and (c) water. The concentration of ketotifen or the ketotifen salt is preferably from 0.01% to 0.05%. The non-ionic tonicity agent is preferably glycerol and the concentration of the glycerol is preferably from 4% to 7%. The compositions preferably have an osmolality of from 400 to 875 milliosmoles/Kg. The compositions may also contain an anti-redness agent. Methods of treating allergic conjunctivitis using the ophthalmic compositions and methods of treating dry eye disease using the ophthalmic compositions are also provided.

Abstract: The invention provides compounds of formula I: or a pharmaceutically acceptable salt thereof, wherein R1-3, R5-7, a, X, Y, Y?, Y?, and Z are as defined in the specification. These compounds are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes for preparing such compounds and methods of using such compounds to, for example, treat pulmonary disorders such as chronic obstructive pulmonary disease and asthma.

Abstract: Stable compositions comprising ketotifen or a ketotifen salt and methods of preparing such compositions are provided. The pH of the compositions remains at less than about 5 during storage. The methods comprise preparing pharmaceutical compositions comprising ketotifen or a ketotifen salt, and adjusting their pH to less than 5, thus slowing the changes of the active ingredients.

Abstract: The present invention relates to a selective estrogen receptor modulator of formula I or Ia: (I) (Ia); or a pharmaceutical acid addition salt thereof; useful for treating vasomotor symptoms, in particular hot flashes, night sweats and other symptoms that affect women around menopause.

Abstract: The present invention provides methods, uses and means for breast cancer prognostics and treatment prediction. Provided methods comprises the steps of: providing a sample earlier obtained from a breast cancer subject; evaluating the amount of ANLN protein present in at least part of said sample, and determining a sample value corresponding to said amount; comparing the sample value with a reference value; and, if said sample value is higher than said reference value, concluding that the subject is not likely to benefit from an endocrine treatment or that a prognosis for said subject is worse than a reference prognosis associated with the reference value.

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: Methods for facilitating joint immobilization or fusion using selective estrogen receptor modulator (SERM) such as raloxifene are disclosed. The SERM may be administered systemically or locally. In conjunction with SERM, other therapeutic agents such as calcium, vitamin D, bone morphogenetic protein may be administered simultaneously. The method can similarly be applied to facilitate bone repair, bone healing, and connective tissue healing processes in a patient.

Abstract: The invention provides methods to identify agents useful to prevent, inhibit or treat viral infections, e.g. filovirus infections, as well as compositions having one or more agents to prevent, inhibit or treat viral infection.

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: This invention provides compounds of formula I and pharmaceutically acceptable salts and solvates thereof, characterized that the compound is in particulate form and having a specific size range. The present invention further provides pharmaceutical compositions containing or formulated using compounds of formula I, and the use of such compounds for alleviating human pathologies, including osteoporosis, serum lipid lowering, and breast cancer.

Abstract: The present invention related to the administration of bioactive agents via oral fast dispersing/dissolving drug delivery systems for treating illnesses of patient with critical buccal condition, leading to difficulties in swallowing oral medicine forms and thus difficulties in treating said illnesses. Particularly, the present invention discloses the administration of bioactive agents via oral fast dispersing/dissolving drug delivery systems for treating illnesses of patient with dysphagia and/or odynophagia and/or aspiration risk. Another aspect of the present invention is the administration of bioactive agents via oral fast dispersing/dissolving drug delivery systems for the treatment of dysphagia and/or odynophagia and/or aspiration risk.

Abstract: An agent for treating various kinds of diseases which contains at least one selected from the group consisting of sexual steroid hormone such as estrogen or its metabolites, its derivative, structural analogues thereof, estrogen acting substance or SERM non-feminizing estrogen (non-hormonal estrogen), and an activator of sirtuin and has a form of eye drops or eye washes, oral preparation, etc. An agent for treating eye diseases which has excellent treatment effects, reduced in side action can be provided.

Abstract: The invention relates to fatty acid raloxifene derivatives; compositions comprising an effective amount of a fatty acid raloxifene derivative; and methods for treating osteoporosis or preventing invasive breast cancer in postmenopausal women comprising the administration of an effective amount of a fatty acid raloxifene derivative.

Abstract: An agent for treating various kinds of diseases which contains at least one selected from the group consisting of sexual steroid hormone such as estrogen or its metabolites, its derivative, structural analogues thereof, estrogen acting substance or SERM non-feminizing estrogen (non-hormonal estrogen), and an activator of sirtuin and has a form of eye drops or eye washes, oral preparation, etc. An agent for treating eye diseases which has excellent treatment effects, reduced in side action can be provided.

Abstract: Methods of the prophylaxis of the development of allergy in a patient at risk of sensitization to an antigen(s) or allergen(s) due to impaired gastrointestinal functions include administering a mast cell inhibitor, e.g., ketotifen, e.g., ketotifen fumarate. Methods for prophylactically treating, reducing, delaying or controlling gastrointestinal disorders include administering a mast cell stabilizer, e.g., ketotifen to a patient in need thereof. Pharmaceutical preparation, composition for use in methods described, are also disclosed. Also disclosed are methods of prophylaxis or treating gastrointestinal and esophageal inflammation, and methods for the prophylaxis of the development of additional allergies to a newly introduced substance in a patient with a preexisting allergy. Such methods include delivery of a mast cell stabilizer, e.g., ketotifen. Oral and topical administration are contemplated within the scope of the methods.

Abstract: The invention is a gel composition for delivery to a breast milk duct prior to surgical excision of breast tissue including cancerous lesions. The invention also provides methods of mapping all or nearly all of a breast milk duct prior to surgical excision of breast tissue, and method of identifying part or all of a breast duct or ducts as a surgical aide to a breast surgeon. Kits to support these methods and including these compositions are also provided.

Abstract: Pyrazole urea compounds, pharmaceutical compositions which contain them and methods for treating cancer using them.

Abstract: A pharmaceutical useful as a therapeutic agent and a preventive agent for hyperlipemia, and a pharmaceutical useful as a therapeutic agent and a preventive agent for hepatic disorders associated with cholestasis, particularly, primary biliary cirrhosis and primary sclerosing cholangitis, and a pharmaceutical useful as a therapeutic agent and a preventive agent for obesity, fatty liver and steatohepatitis are provided.

Abstract: Pharmaceutical formulations comprising raloxifene or its salts, esters, polymorphs, isomers, hydrates, solvates, or derivatives thereof having defined particle sizes. Also described are processes for preparing formulations and methods of using such formulations.

Abstract: The present invention relates to an aralkyl alcohol piperidine derivative and use as antidepressant thereo. The said aralkyl alcohol piperidine derivative has a triple inhibition effect on the reuptaking of 5-HT, NA and DA. The derivative may be administered to the patient in need of such treatment in the form of composition by oral administration, injection and the like.

Abstract: Raloxifene acid addition salts or solvates thereof, having improved dissolution properties in media comprising hydrochloric acid are described, compared with similar preparations based on raloxifene or raloxifene hydrochloride. The disclosed acid addition salts or solvates thereof show an improved bioavailability in media comprising hydrochloric acid, such as the gastric juice. The acid addition salts or solvates thereof are addition salts or solvates of raloxifene and a pharmaceutical acceptable acid selected among succinic acid, lactic acid, malonic acid or sulphuric acid. Further, crystalline forms of the raloxifene salts and solvates thereof are disclosed. The raloxifene acid addition salts and/or solvates thereof are useful for the preparation of pharmaceutical composition for oral administration capable of fast and reliable release of the active ingredients in the stomach of the patient, in particular for the treatment of cancer or osteoporosis, or for inhibiting cartilage degradation.

Abstract: The present invention provides a method for determining whether a mammalian subject having a breast cancer is likely to benefit from an endocrine treatment, comprising the steps of: providing a sample earlier obtained from said subject; evaluating the amount of HMGCR protein or HMGCR mRNA present in at least part of said sample, and determining a sample value corresponding to said amount; comparing the sample value obtained in step b) with a reference value; and, if said sample value is higher than said reference value, concluding that the subject is likely to benefit from an endocrine treatment. Further, a corresponding method of treatment is provided as well as further methods uses and means which may be employed in connection with breast cancer treatment or treatment prediction.

Abstract: Compounds of structure (I): including stereoisomers and pharmaceutically acceptable salts thereof, wherein X, R1, R2, R3, R4, R5, R6 and R7 are as defined herein. Such compounds have activity as SHIP1 modulators, and thus may be used to treat any of a variety of diseases, disorders or conditions that would benefit from SHIP1 modulation. Compositions comprising a compound of structure (I) in combination with a pharmaceutically acceptable carrier or diluent are also disclosed, as are methods of SHIP1 modulation by administration of such compounds to an animal in need thereof.

Abstract: Molecular signature for antipsychotics and SERMs has been identified, namely their upregulation of genes that alter lipid homeostasis, preferably of one or more of the following genes: TNSIG1, SCD, FADS2, LDLR, FDPS, ACAT2, FDFT1, CYP51A1, FASN, DHCR7, RAB26, TM7SF2, SATB1, FAM117, GPNMB, NUPR1, VAC14, and LSS.