Abstract: The invention is directed to a system for treating vomiting comprising a topical gel placed within a syringe. The topical gel includes (a) between 10 to 40% Phenergen by weight, (b) between 30 to 50% of lecithin isopropyl palmitate solution by weight, and (c) between 30 to 70% of pluronic gel by weight. The syringe includes a cylindrical chamber having a front end, a back end, an interior side and exterior side. The syringe has a disposing opening located on the front end of the cylindrical chamber; a stopper of a sufficient size and dimension to engage the disposing opening; a plunger located within the cylindrical chamber; a rigid shaft having a sufficient size and dimension to fit within the cylindrical chamber and a plate affixed to a distal end of the rigid shaft. The syringe is plastic having a dark color to prevent degradation of the topical gel.

Abstract: The present invention relates to therapeutic combinations and kits useful in treating CFTR-related diseases, such as cystic fibrosis.

Abstract: This invention provides caspase inhibitors of formula I: wherein Z is oxygen or sulfur; R1 is hydrogen, —CHN2, R, CH2OR, CH2SR, or —CH2Y; between R3 and R4 represents a single or double bond; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; R3 is a group capable of fitting into the S2 subsite of a caspase enzyme; R4 is a hydrogen or C1-6 alkyl or R3 and R4 taken together form a ring; Ring A and Ring B are each heterocyclic rings, and R and R5 are as described in the specification. The compounds are effective inhibitors of apoptosis and IL-1? secretion.

Abstract: A method for the synthesis of a diaminophenothiazinium compound of the following formula: comprising (a) purifying a corresponding reduced compound which is N-acylated at the heterocyclic nitrogen; (b) deacylating the purified compound to provide the corresponding reduced compound; and (c) oxidizing the reduced compound to provide the diaminophenothiazinium compound. Optional purification may performed, for example, after deacylating and after oxidizing. The method provides high purity diaminophenothiazinium compounds which are suitable for pharmaceutical and related therapeutic uses. Such uses include inactivating pathogens, the treatment of the infectious diseases, and for the treatment of diseases of protein aggregation, such as tauopathies, including Alzheimer's disease.

Abstract: The present invention relates to new cyclohexyl urea modulators of D2 receptors and/or modulators of D3 receptors, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: This invention pertains generally to the field of phenothiazine compounds, and more particularly to certain stably reduced phenothiazine compounds, specifically, certain 3,7-diamino-10H-phenothiazine (DAPTZ) compounds of the following formula: wherein: each of R1 and R9 is independently selected from: —H; C1-4alkyl; C2-4alkenyl; and halogenated C1-4alkyl; each of R3NA and R3NB is independently selected from: —H; C1-4alkyl; C2-4alkenyl; and halogenated C1-4alkyl; each of R7NA and R7NB is independently selected from: —H; C1-4alkyl; C2-4alkenyl; and halogenated C1-4alkyl; each of HX1 and HX2 is independently a protic acid; and pharmaceutically acceptable salts, solvates, and hydrates thereof. These compounds are useful as drugs, for example, in the treatment of tauopathies, such as Alzheimer's disease, and also as prodrugs for the corresponding oxidized thioninium drugs (for example, methylthioninium chloride, MTC).

Abstract: Novel chemical conjugates of psychotropic drugs and organic acids, uses thereof in the treatment of psychotic and/or proliferative disorders and diseases and as chemosensitizing agents, and their syntheses are disclosed. The organic acids are selected to reduce side effects induced by the psychotropic drugs and/or to exert an anti-proliferative activity.

Abstract: The current invention provides formulations for transdermal delivery of promethazine which achieve delivery of the drug with consistent plasma levels. The topical formulations of the invention are superior to both rectal suppositories and oral dosage forms in that variable blood levels, first-pass metabolism, unpredictable peaks in blood levels, and variable bioavailability are minimized. Formulations of the invention provide antiemetic and antipruritic relief to patients in need of treatment while minimizing side effects and adverse reactions known to occur with other routes of administration and other formulations.

Abstract: This invention pertains generally to the field of phenothiazine compounds, and more particularly to certain stably reduced phenothiazine compounds, specifically, certain 3,7 diamino-10H-phenothiazine (DAPTZ) compounds of the following formula wherein: each of R1 and R9 is independently selected from: —H; C1-4alkyl; C2-4alkenyl; and halogenated C1-4alkyl; each of R3NA and R3NB is independently selected from: —H; C1-4alkyl; C2-4alkenyl; and halogenated C1-4alkyl; each of R7NA and R7NB is independently selected from: —H; C1-4alkyl; C2-4alkenyl; and halogenated C1-4alkyl; each of HX1 and HX2 is independently a protic acid; and pharmaceutically acceptable salts, solvates, and hydrates thereof. These compounds are useful as drugs, for example, in the treatment of tauopathies, such as Alzheimer's disease, and also as prodrugs for the corresponding oxidized thioninium drugs (for example, methythioninium chloride, MTC).

Abstract: Disclosed is a transformed cell (a cell model) which can form a cytoplasmic inclusion body derived from TAR DNA-binding protein of 43 kDa (TDP-43) that is found in the brain of a patient suffering from a neurodegenerative disease such as FTLD and ALS. The transformed cell is characterized by having, introduced therein, a promoter capable of functioning in a host cell and a mutant TDP-43 gene.

Abstract: A phenothiazinium compound, compositions and medicaments for use in promoting wound healing and a method for promoting wound healing or cosmetic use by applying or administering a phenothiazinium compound to a wound site or the skin, and optionally exposing the wound site or skin to light.

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: A method of reducing a vasodilatory response comprising administering to an individual in need of such treatment an effective amount of a guanylate cyclase pathway inhibitor selected from the group consisting of methylene blue, ODQ, LY83583 and a protein kinase G inhibitor or an H2O2 reducing agent selected from the group consisting of Aspergillus niger catalase and hydroxyl scavengers, hydroquinone and mannitol.

Abstract: The disclosure relates to a biomaterial that comprises an aqueous phase, polymer network, a second polymer included in said disclosure invention more particularly relates to a biomaterial including an aqueous phase and a first polymer network made of a first proteic or saccharidic polymer or a mixture of first proteic and saccharidic polymers, wherein the first polymer network and the aqueous phase define a first gel (A), the biomaterial including: a second proteic or saccharidic polymer or a mixture of the second proteic and saccharidic polymers, either in solution in the aqueous phase of the gel (A) or in the form of a gel (B), and a first enzyme for degrading said second polymer or second polymer network. The disclosure also relates to a method for making biomaterials, and to the uses of the biomaterial particularly for releasing active substances, and to a device for the controlled release of active substances that include the biomaterial.

Abstract: The present invention relates to a series of substituted bicyclic[3.1.0]heteroaryl amides of the Formula I, wherein A, Q, X, Y, Z and R1-R5 groups are defined as in the specification, that exhibit activity as glycine transport inhibitors, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, and their use for the enhancement of cognition and the treatment of the positive and negative symptoms of schizophrenia and other psychoses in mammals, including humans.

Abstract: This invention provides molecular markers that are prognostic and/or diagnostic for a psychiatric disorder. In particular, genes are identified whose expression is altered in schizophrenia and/or bipolar disorder thereby providing prognostic and diagnostic markers for the disorder. In addition genes are identified whose dysregulation provides markers that allow diagnostic distinction between schizophrenia and bipolar disorder.

Abstract: Enantomerically purified phenothiazines are provided as active ingredients of medicaments to limit activity of bone resorbing cells so as to reduce bone loss. Novel phenothiazine derivatives are provided. A method of synthesizing enantiomerically pure phenothiazine derivatives is provided that avoids post-synthetic enantiomeric resolution.

Abstract: The present invention relates to serotonin receptor antagonists for treating inflammatory arthritis and related conditions. The present invention also relates to a kit comprising a pharmaceutical composition comprising a serotonin receptor antagonist and instructions indicating that the composition is for use in treating inflammatory arthritis and related conditions. In addition, the present invention relates to a method of treating inflammatory arthritis and related conditions comprising administration of a serotonin receptor antagonist. The method is preferably carried out on a subject in need of treatment. The inflammatory arthritis is preferably rheumatoid arthritis.

Abstract: A method of treating oral cancer is provided. The method comprises the steps of providing at least one photodynamic treatment comprising the steps of (i) applying a composition comprising improved toluidine blue to oral cells; wherein the composition comprises a greater percentage by weight of the conformational isomers of toluidine blue compared to the N-demethylated derivatives thereof; and wherein the composition localizes to oral cancer cells; and activating the applied composition, thereby killing the oral cancer cells.

Abstract: The present invention relates to a quickly decomposing oral drug preparation, for the application of active ingredient combinations for smoking withdrawal, which contains nicotine, a nicotine salt, a nicotine derivative, or a substance that reacts to nicotine, in combination with another active ingredient, and the use of such a drug preparation for the treatment of smoking withdrawal, and the use of nicotine, and/or nicotine salts or derivatives, for the production of medications for the treatment of smoking withdrawal. The active ingredient that is to be administered, in combination, for this purpose is a centrally active ingredient, preferably an antidepressant for the fighting of psychic dependency in terms of a smoking withdrawal therapy. The administration of the active ingredient combination to the patient should be handled in a simple and reliable way and should exclude side effects to a large extent.

Abstract: This invention relates to novel pharmaceutical compositions comprising therapeutically effective combination of a positive allosteric modulator of nicotine receptors; and a cognitive enhancer selected from the group consisting of a nicotine acetylcholine receptor agonist, an acetylcholine esterase inhibitor, a positive AMPA receptor modulator, an antipsychotic drug, an antidepressant drug and an anti Parkinson drug. The pharmaceutical compositions for use according to the invention are contemplated particularly useful for combating cognitive disorders.

Abstract: Sustained release pharmaceutical composition comprising at least one poorly soluble active agent(s), at least one solubilizer, a release rate controlling polymer system consisting of an acid-soluble polymer and a pH-dependent polymer, and optionally other pharmaceutically acceptable excipients. The present invention also describes a process for preparation of such compositions and method of using such compositions. The sustained release compositions are useful in providing therapeutically effective levels of active agent(s) for extended periods of time.

Abstract: The invention provides a class of dopamine transporter inhibitors of formula (I) (DAT inhibitors), packaged pharmaceuticals comprising such inhibitors, and their uses in treating, or manufacturing medicaments for treating disease conditions including Parkinson's disease, when assessed by one or more of Hoehn and Yahr Staging of Parkinson's Disease, Unified Parkinson Disease Rating Scale (UPDRS), and Schwab and England Activities of Daily Living Scale. Related business methods such as marketing the inhibitors to healthcare providers are also provided.

Abstract: The present invention provides methods for treating neurological diseases and disorders. Compounds that replace or enhance the function of SMN or alleviate or reduce a phenotype of cells with low SMN protein levels are provided. Screening methods and kits for identifying such compounds also are provided.

Abstract: The present invention discloses dye-sulfenate derivatives and their bioconjugates for dual phototherapy of tumors and other lesions. The compounds of the present invention may contain either a mixture of Type 1 and Type 2 agents or a single entity that integrates both units in the same molecules. The compounds are designed to produce both Type 1 and Type 2 phototherapeutic effect at once using dual wavelength light source that will produce singlet oxygen and free radicals at the lesion of interest.

Abstract: The present invention relates to new 7,8,10,10a-tetrahydro-6H-benzo[c]chromen-9(6aH)-one modulators of cannabinoid receptors, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: The present invention relates to new benzisoxazole modulators of D2 receptors and/or 5-HT2A receptors, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: The present invention relates to new pyrrolidinone inhibitors of PDE-4 activity, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: Pharmaceutical compositions are provided which comprise effective amounts of analgesic to treat a subject, including to reduce or eliminate an adverse effect associated with the analgesic.

Abstract: The present disclosure encompasses compounds and compositions that are useful as specific AI-2 antagonists for the control of bacterial quorum sensing. Although the AI-2 antagonists according to the present disclosure may not have bactericidal effect, their ability to attenuate virulence, drug resistance, and/or biofilm formation have therapeutic benefits. In addition, the AI-2 antagonists of the present disclosure can also be used as tools to probe bacterial AI-2 functions. The present disclosure also encompasses methods for inhibiting or attenuating microbial virulence, biofilm formation, and drug resistance. The methods are suitable for preventing bacteria from accruing and forming extensive biofilms that may be a health or hygiene hazard or a physical issue, such as in the blockage of water or fuel lines.

Abstract: The present invention relates to new phenothiazine modulators of H1 receptors, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: The present invention relates to new 3H-benzooxazol-2-one modulators of D2 receptors and/or 5-HT1A receptors, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: A method for causing a permanent increase in the length and girth of a male subject's penis, the method comprising treatment comprising the step of (a) administering to the male an effective amount of a vasodilator selected from the group consisting of a vasodilator per se and compositions thereof comprising a pharmaceutically-acceptable diluent or carrier, to induce a cumulative prolonged engorgement of the subject's penis; and (b) repeating step (a) as necessary to cause the increase during the treatment. A potentiator which enhances the effect of the vasodilator may also be used.

Abstract: The present invention relates to new N-methyl piperazine modulators of H1 receptor activity, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: The present invention relates to new methylindazole modulators of 5-HT3 receptor activity, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: The present invention relates to new phenothiazine modulators of D2 receptor activity and/or 5-HT2 receptor activity, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: A galenical form for the transmucous administration of at least one active ingredient, characterized in that the active ingredient is paracetamol in a stable and complete dissolved state in a hydroalcoholic solution that includes at least 10% by mass of alcohol so as to allow fast absorption of the active ingredient through the mucous membranes of the buccal cavity and/or the oropharynx. A process for production and the uses of the galenical form are also disclosed.

Abstract: The present invention relates to new thioxanthene modulators of dopamine D2 receptors, pharmaceutical compositions thereof, and methods of use thereof.

Abstract: Pharmaceutical compositions comprising phenylephrine in a sustained release oral dosage formulation. Compositions can comprise phenylephrine alone or phenylephrine in combination additional pharmaceutically active substances such as an antihistamine and/or an analgesic.

Abstract: The present invention provides a method of promoting bone growth in a subject in need thereof, by administering to the subject a therapeutically effective amount of a compound of Formula I. The present invention also provides methods for the treatment of renal disease and cancer.

Abstract: A method of treatment for the prevention or therapy of a protein aggregation disease includes the administration in combination of a first active medicament and a second active medicament, wherein the first active medicament is active to impede aggregation of amyloid protein and the second active medicament is active to disaggregate previously formed aggregates of amyloid protein.

Abstract: A compound having formula I. R1, R2, R3 and R4 are independently H or lower alkyl. R5 is aryl, heteroaryl, cycloalkyl, heterocycloalkyl, aryloxy, heteroaryloxy, cycloalkyloxy, heterocycloalkyloxy, arylamino, heteroarylamino, cycloalkylamino, heterocycloalkyl amino, arylthio, heteroarylthio, cycloalkylthio, heterocycloalkylthio, or cyclic olefin, any of which may be substituted or non-substituted; or substituted alkyl, substituted alkyl oxy or substituted alkyl amino wherein the substituent is an aryl, a heteroaryl, a cycloalkyl, a heterocycloalkyl or a cyclic olefin, any of which may be substituted or non-substituted. X is C or N. n and p are independently whole numbers selected from 0, 1 and 2. (CH2)n and (CH2)p may be substituted or non-substituted. Ar1 and Ar2 are independently aryl or heteroaryl groups which may be substituted or non-substituted. Certain specific compounds are excluded.

Abstract: Process for preparing compounds of the diaminophenothiazinium type comprising a step for purification of derivatives (II). The products resulting from this process have a high degree of purity. Use of these compounds for the preparation of medicaments.

Abstract: The photostability of oxymetazoline in a topical decongestant composition is enhanced by lowering the pH of the composition using a buffer solution.

Abstract: This invention provides caspase inhibitors of formula I: wherein Z is oxygen or sulfur; R1 is hydrogen, —CHN2, R, CH2OR, CH2SR, or —CH2Y; between R3 and R4 represents a single or double bond; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; R3 is a group capable of fitting into the S2 subsite of a caspase enzyme; R4 is a hydrogen or C1-6 alkyl or R3 and R4 taken together form a ring; Ring A and Ring B are each heterocyclic rings, and R and R5 are as described in the specification. The compounds are effective inhibitors of apoptosis and IL-1? secretion.

Abstract: Methods and compositions are provided which comprise effective amounts of analgesic to treat a subject, including reducing or eliminating an adverse effect associated with the analgesic.

Abstract: Compounds, pharmaceutical compositions including the compounds, and methods of preparation and use thereof are disclosed. The compounds are triphenyl methane analogs. The compounds and compositions can be used to treat and/or prevent a wide variety of cancers, including drug resistant cancers, inflammatory, degenerative and vascular diseases, including various ocular diseases, and parasitic infections. Representative triphenyl methane analogs include triphenyl methane analogues of various dyes, hormones, sugars, peptides, oligonucleotides, amino acids, nucleotides, nucleosides, and polyols. The compounds are believed to function by inhibiting tNOX expression, the effects of ROS, and/or the production of HIF2. Thus, the compounds are novel therapeutic agents for a variety of cancers and other diseases.

Abstract: The disclosure provides compounds, compositions, and methods for modulating PPAR? receptor. In one embodiment, the compounds of the disclosure comprise a tri-substituted thiazole group. The substituent at the 2-position of the thiazole group provides steric bulk to the compounds. The compounds, compositions, and methods may be useful, for example, in the treatment of cancer.

Abstract: The present invention provides screening methods for the detection of agents that affect various aspects of ?-cell biology, particularly insulin gene expression. Screening methods are also provided for detection of agents that affect ?-cell differentiation from progenitor cells. Additionally, agents identified using such methods are provided and are useful for increasing insulin gene expression and reducing lipotoxicity.

Abstract: The present invention relates to the application of 2-cyano-10-(2-methyl-3-(methylamino)-propyl)phenothiazine or a pharmaceutically acceptable salt thereof to produce a medicament intended for the treatment of sleep disorders, anxiety disorders, mood disorders, mixed anxiety-depression disorder, acute and chronic psychotic state, addiction to and withdrawal from a substance, extrapyramidal events induced by antipsychotics, or symptomatic dimensions during acute or chronic psychotic states as monotherapy or in combination with other antipsychotics.