Abstract: Compositions, formulations, methods, and systems for treating regional fat deposits comprise contacting a targeted fat deposit with a composition comprising long acting beta-2 adrenergic receptor agonist and a compound that reduces desensitization of the target tissue to the long acting beta-2 adrenergic receptor agonist, for example, glucocorticosteroids and/or ketotifen. Embodiments of the composition are administered, for example, by injection, and/or transdermally.

Abstract: The present invention provides methods for boosting mucosal immunity in the female reproductive tract of pre- and post-menopausal women using a TGF-beta inhibitor, a Selective Estrogen Receptor Modulator, and/or a recombinant commensal bacterium that expresses endogenous microbicides into the intestinal tract or reproductive tract of a subject. It also provides methods for boosting innate and adaptive immunity by providing a glucocorticoid. Methods for preventing sexually transmitted infections including HIV infection are also provided.

Abstract: The invention provides a topical pharmaceutical composition for application to the nasal or ocular mucosa which comprises (1) a pharmaceutical excipient suitable for topical administration, (2) a mucosal adjuvant, (3) an antihistamine drug and (4) a mast cell stabilizer, a non-steroidal anti-inflammatory drug, a phosphodiesterase inhibitor, an anti-IgE agent, heparin, a topical steroid or a leukotriene blocker.

Abstract: The invention relates to the use of one or more cannabinoids, particularly THC and/or CBD in combination with a non-cannabinoid chemotherapeutic agent in the manufacture of a medicament for use in the treatment of cancer. In particular the cancer to be treated is a brain tumour, more particularly a glioma, more particularly still a glioblastoma multiforme (GBM). The non-cannabinoid chemotherapeutic agent may be a selective estrogen receptor modulator or an alkylating agent.

Abstract: The present invention relates to a pharmaceutical formulation of solid dosage forms comprising a therapeutically effective amount of a selective estrogen receptor modulator, and especially Raloxifene or a pharmaceutical acceptable salt thereof, in combination with a super disintegrant such as Primojel, and a process for the preparation thereof by wet granulation.

Abstract: A method to determine the clinical outcome of breast tumour affecting a patient if treated with an antitumoural agent against breast tumour. The method includes the step of assaying a sample of a breast tumour from the patient for an expression level of selected genes, by contacting mRNA sequences from the cells of this breast tumour with a set of more than 3 nucleotide sequences related to human mutated PIK3CA.

Abstract: It was an object of the present invention to provide novel compounds that are suitable in particular as active substances in medicaments, preferably in medicaments for the regulation of neuropeptide Y receptors, particularly preferably of neuropeptide Y5 (NPY5) receptor, for the regulation of food ingestion (food intake), preferably for the prophylaxis and/or treatment of disorders of food ingestion, such as obesity, anorexia, cachexia, bulimia or type II (non insulin dependent) diabetes, for the prophylaxis and/or treatment of disorders of the peripheral nervous system, disorders of the central nervous system, anxiety, depression, cognitive disorders, preferably memory disorders, cardiovascular diseases, pain, epilepsy, arthritis, hypertensive syndrome, inflammatory diseases, immune diseases and other NPY5 mediated disorders in animals and mammals, including man.

Abstract: 3,4-Disubstituted-4-aryl-piperidine compounds are disclosed. Pharmaceutical compositions containing the 3,4-disubstituted-4-aryl-piperidine compounds and methods of their pharmaceutical uses are also disclosed. The compounds disclosed are useful, inter alia, as antagonists of opioid receptors.

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: Urethral suppositories containing a mixed-activity anti-cholinergic drug and methods of use for treatment of over-active bladder are provided. Buffering drugs to pH near their pKas can result in a desired proportion of uncharged drug and can enhance absorption of the agents into urethral tissues.

Abstract: This patent describes a method and materials to treat cancer diagnosed at an early stage, particularly breast cancer. It considers that metastatic breast cancer growth includes periods of dormancy, that surgery to remove a primary tumor can induce metastatic growth, and that women with Down Syndrome rarely get breast cancer. It elevates the level of an antiangiogenic drug produced by chromosome 21 preferably Endostatin in plasma preferably at least one day prior to surgery and kept at that high level preferably indefinitely. In one embodiment, the therapy specifically excludes drugs that significantly inhibit the VEGF pathway since that is important for wound healing. This method will prevent results of surgery from stimulating tumor growth and angiogenesis of micrometastatic disease that is much easier to prevent than control after the fact. This can be done indefinitely since there is no acquired resistance that develops, as happens in most cancer therapies.

Abstract: Described herein are methods for effectively and accurately measuring a patient response upon administration of one or more drugs to the patient. The methods are more sensitive than current methodologies. Also described herein are compositions comprising an analgesic and a sufficient amount of an antihistamine to enhance the analgesic properties of the analgesic. With respect to these compositions, the methods described herein are useful for evaluating qualities of pain, definite improvement, and one or more bodily functions of a subject afflicted with pain. The compositions described herein are useful in improving the quality of pain in a subject or a bodily function of a subject afflicted with pain or definite improvement of a subject afflicted with pain.

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

Abstract: Racemic norketotifen, racemic 10-hydroxy-ketotifen, racemic 10-hydroxy-nor-ketotifen and optically active isomers of ketotifen, norketotifen, 10-hydroxy-ketotifen and 10-hydroxy-norketotifen were found to have antiallergic and anti-inflammatory effects while being devoid of the severe dose-limiting sedative side effects of Ketotifen.

Abstract: Crystalline raloxifene hydrochloride in hydrated form, particularly the monohydrate, processes for its preparation, pharmaceutical compositions comprising it and uses thereof.

Abstract: The present invention provides a new method and means for determining whether a mammalian subject having a breast cancer is likely to benefit from an endocrine treatment. The method comprise the steps of: providing a sample earlier obtained from said subject; evaluating the amount of CRABP2 protein present in at least part of said sample, and determining a sample value corresponding to said amount; comparing the obtained sample value 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.

Abstract: The present invention provides a compound a piperidine derivative having excellent histamine receptor antagonistic action, which is useful as active ingredients of a pharmaceutical composition, especially an antihistamine. The piperidine derivative of the present invention has a potent histamine receptor antagonistic action. Further, the compound of the present invention shows low brain transfer even in a cerebral receptor binding test where a mouse is orally administered with the compound, so that the compound has preferred properties of alleviating side effects in the central nervous system, such as drowsiness. The piperidine derivative of the present invention is very useful as a novel antihistamine having smaller side effects in the central nervous system, such as drowsiness.

Abstract: Substituted sulfonamide derivatives, a process for their preparation, pharmaceutical compositions containing these compounds, and to the use of substituted sulfonamide derivatives in the treatment or inhibition of pain and/or various disorders or disease states.

Abstract: The invention relates to pharmaceutical combinations of retigabine and sodium channel inhibitors for treating, pains which are accompanied by an increase in muscle tone.

Abstract: Substituted sulfonamide derivatives, a process for their preparation, pharmaceutical compositions containing these compounds, and to the use of substituted sulfonamide derivatives in the treatment or inhibition of pain and/or various disorders or disease states.

Abstract: Products of a general formula (I) and their use in the manufacture of medicines useful for the treatment of neurodegenerative diseases such as Alzheimer's disease or, in general, any disease or pathology produced by alterations of biological functions that can be treated or therapeutically modified by these products.

Abstract: This invention concerns a method for treatment or prevention of lower urinary tract symptoms with or without pelvic pain in an individual, said method comprising administering to the individual an effective amount of a selective estrogen receptor modulator, or an isomer, isomer mixture or a pharmaceutically acceptable salt thereof.

Abstract: The invention is directed to compounds of formula I: wherein R1, R2, R3, R4, R5, R6, R7a, R7b, W, G1, G2, a, b, c, d and m are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.

Abstract: The invention is directed to compounds of formula I: wherein R1, R2, R3, R4, R5, R6, R7a, R7b, W, G1, G2, a, b, c, d and m are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.

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

Abstract: 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 provides topical formulations of ketotifen that provide a comfortable formulation when instilled in the eye and are effective in the treatment and prevention of ocular allergy, particularly allergic conjunctivitis. The invention further provides methods of treating and preventing ocular allergy by in a subject in need of such treatment by topical application of the ketotifen formulations of the invention to the eye of a subject in need thereof.

Abstract: Compounds of formula (I) as defined herein: are useful for treating behavioral disorders associated with dementia, psychoses, in particular schizophrenia (deficient form and productive form) and acute or chronic extrapyramidal symptoms induced by neuroleptics; for the treatment of various forms of anxiety, panic attacks, phobias, and compulsive obsessive disorders; for treating various forms of depression, including psychotic depression; for treating disorders caused by alcohol abuse or weaning from alcohol, sexual behavior disorders, eating disorders and for treating migraine.

Abstract: Compositions comprising one or more unsaturated fatty acids and one or more nitric oxide releasing compounds, and methods for using such compositions for enhancing cognitive function, reducing or preventing a decline of social interaction, reducing or preventing age-related behavioral changes, increasing trainability, maintaining optimal brain function, facilitating learning and memory, reducing memory loss, retarding brain aging, preventing or treating strokes, and preventing or treating dementia in an animal. Preferably, the compositions are food compositions useful for enhancing cognitive function in humans and companion animals.

Abstract: This invention relates to novel compounds useful in the treatment of diseases associated with TRPV4 channel receptor. More specifically, this invention relates to certain substituted piperidines, according to Formula I Specifically, the invention is directed to compounds according to Formula I wherein R1 is optionally substituted aryl; X is CH2, S, or SO2; and n=1 or 2.

Abstract: The present invention relates to a method for forming an ophthalmic composition comprising mixing at least one hydroxide and pentetic acid with water and at least one oxidatively unstable component to form an ophthalmic composition comprising at least one salt of diethylenetriamine pentaacetic acid and a pH between about 6 and about 8.

Abstract: Compounds of formula (I) as defined herein: are useful for treating behavioral disorders associated with dementia, psychoses, in particular schizophrenia (deficient form and productive form) and acute or chronic extrapyramidal symptoms induced by neuroleptics; for the treatment of various forms of anxiety, panic attacks, phobias, and compulsive obsessive disorders; for treating various forms of depression, including psychotic depression; for treating disorders caused by alcohol abuse or weaning from alcohol, sexual behavior disorders, eating disorders and for treating migraine.

Abstract: Substituted 3-phenylpiperidine compounds corresponding to Formula I in which R1 and R2 have the meanings defined in the specification, methods for preparing such compounds, pharmaceutical compositions containing such compounds, and the use of such compounds for treating or inhibiting various conditions, especially pain.

Abstract: This invention is concerned with compounds of the formula and pharmaceutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are associated with the modulation of SST receptors subtype 5.

Abstract: The present invention relates to an in-vitro method of identifying a tumor resulting from a proliferative disease of the endometrium or ovary as responsive to anti-estrogen treatment. Further, the invention relates to an in-vitro method of identifying a candidate patient with a proliferative disease of the endometrium or ovary as suitable for anti-estrogen treatment. In a further aspect, the invention provides an in-vitro method of identifying an individual with a non-cancerous proliferative disease of the endometrium or ovary who is at risk of developing endometrial or ovarian cancer. The invention also provides kits for performing the above methods.

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: The present invention provides a chroman compound of formula (I) and its pharmaceutical salt, methods of its preparation and its pharmaceutical applications. Wherein: X is O or S; n is for 2, 3 or 4; R1 is 6-substituted or 7-substituted halogen, C1-4alkyl, C1-4alkoxyl, benzyloxy, carbamoyl; R2 is nitrogen-containing five-membered or six-membered substituted heterocyclic ring selected from piperidinyl, morpholinyl, N-methyl-piperazinyl, N-(2-ethoxyl)piperazinyl, pyrrolyl, pyrazolyl or imidazolyl. The compounds are useful to prepare medicaments for treating cardiovascular diseases, their preparation employs mild reaction conditions, the raw material are plenty and easy to be obtained, and the operation and post-treatment in the preparation are simple.

Abstract: A novel class of substituted piperidines, pharmaceutical compositions comprising them and use thereof in the treatment and/or prevention of diseases and disorders related to the histamine H3 receptor. More particularly, the compounds are useful for the treatment and/or prevention of diseases and disorders in which an interaction with the histamine H3 receptor is beneficial.

Abstract: Provided herein are methods of decreasing glial fibrillary acidic protein (GFAP) levels in a cell. Such methods include administering an effective amount of a GFAP lowering compound to the cell. Also provided are compounds useful for the treatment of Alexander disease in subjects at risk of or diagnosed with Alexander disease and methods for the identification of such compounds.

Abstract: There is provided combination products comprising (a) a mast cell inhibitor, or a pharmaceutically-acceptable salt or solvate thereof; and (b) a PPARY agonist, or a pharmaceutically-acceptable salt or solvate thereof. Such combination products find particular utility in atherosclerosis and related conditions.

Abstract: Compounds of formula (I) as defined herein: are useful for treating behavioral disorders associated with dementia, psychoses, in particular schizophrenia (deficient form and productive form) and acute or chronic extrapyramidal symptoms induced by neuroleptics; for the treatment of various forms of anxiety, panic attacks, phobias, and compulsive obsessive disorders; for treating various forms of depression, including psychotic depression; for treating disorders caused by alcohol abuse or weaning from alcohol, sexual behavior disorders, eating disorders and for treating migraine.

Abstract: The present invention relates to methods of prophylactically treating, reducing, delaying or controlling severe allergic reaction, e.g., to food and/or hymenoptera allergen, e.g. peanut allergen or bee venom allergen, in patients at risk of systemic anaphylaxis, e.g., patients receiving allergen desensitization therapy, through the use of a mast cell stabilizer, e.g., ketotifen and/or its metabolites or derivatives in free or pharmaceutically acceptable acid addition salts thereof. The invention further provides methods to desensitize a patient to one or more allergens comprising administering (i) one or more allergen to induce tolerance and (ii) one or more mast cell stabilizers in free or pharmaceutically acceptable salt thereof.

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 Y, R1, R2, R3, R4, RA, and RB are defined herein.

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 relates to new bicyclic modulators of H1 receptor activity, pharmaceutical compositions thereof, and methods of use thereof

Abstract: An ophthalmic solid pharmaceutical preparation for external use is disclosed which can be used to continuously administer with ease a pharmacologically active agent to ocular local tissues. The pharmaceutical preparation is a solid pharmaceutical preparation containing a pharmacologically active ingredient in a base, which may comprise an oily base, and designed to be applied by being rubbed on the surface of the skin including the surface of either of the eyelids to deliver, through the skin of the eyelids, the pharmacologically active ingredient to the local tissues of the eye located on the backside of the eyelids.

Abstract: A transdermal drug delivery system for treatment of ophthalmic diseases comprising a structure that a plaster layer containing a remedy for ophthalmic diseases is provided on a support, wherein the system is applied to a skin surface including a front surface of an eyelid to administer the remedy for ophthalmic diseases in the plaster layer to an ophthalmic topical tissue by percutaneous permeation substantially without being administered through a systemic blood flow. Use of the transdermal drug delivery system for treatment of ophthalmic diseases, comprising applying the transdermal drug delivery system to a skin surface including a front surface of an eyelid to transfer the remedy for ophthalmic diseases in the plaster layer to an ophthalmic topical tissue by percutaneous permeation substantially without being administered through a systemic blood flow, and a method for transferring the remedy for ophthalmic diseases to the ophthalmic topical tissue.

Abstract: Compounds of formula (I): formula (I) wherein variables are as defined herein and their pharmaceutical compositions and methods of use are disclosed as useful for treating dyslipidemia and diseases related to dyslipidemia.

Abstract: The invention provides a method for the treatment of H4R modulated diseases and/or conditions comprising administering to the subject an effective amount of a H4R agonist. The invention also provides a method for treating COPD comprising administering to the subject an effective amount of a H4R agonist, a H1R antagonist and an anticholinergic drug. Further, the invention provides a pharmaceutical formulation comprising a H4R agonist, a second active agent and a pharmaceutically acceptable carrier.

Abstract: Ophthalmic compositions containing norketotifen and methods of making the same and the use thereof are disclosed. The methods also comprise administering to the eyes of a mammal in need thereof topical ophthalmic compositions containing norketotifen.