Abstract: The disclosure relates to crystalline form 1 of 5-hydroxy-N,N,N-trimethyl-tryptammonium (5-HTQ) iodide, and to pharmaceutical compositions containing the compound and to methods of treatment using it.

Abstract: The present disclosure provides methods of identifying patients who have partial or total resistance to HIF-2 inhibitors or who develop partial or total resistance to HIF-2 inhibitors after treatment and providing suitable treatment to these patients.

Abstract: A compound represented by the general formula (V) wherein all the symbols are as defined in the specification, has an improved balance of the agonist activity against the S1P5 receptor relative to the S1P1 receptor, and can thus serve as a therapeutic agent for S1P5-mediated diseases such as schizophrenia and Binswanger's disease and other neurodegenerative diseases.

Abstract: Provided herein are compounds of Formula (I), (I-A), (I-B), (II), (II-A), (II-B), (III), (M-A), (IV), and (IV-A), or pharmaceutically acceptable salt thereof described herein. Also provided herein are pharmaceutical compositions comprising a compound Formula (I), (I-A), (I-B), (II), (II-A), (II-B), (III), (III-A), (IV), and (IV-A), or pharmaceutically acceptable salt thereof, and methods of using a compound of Formula (I), (I-A), (I-B), (II), (II-A), (II-B), (III), (III-A), (IV), and (IV-A), or pharmaceutically acceptable salt thereof, e.g., in the treatment of a mental health disease or disorder.

Abstract: A gel composition for treating bowel diseases comprising about 0.1 to about 2.5 wt. % of an anti-epileptic agent; about 0.8 to about 2.0% wt. % of a collagen complexed with a date palm extract of Khalas cultivar and carboxymethylcellulose; about 10 to about 50 ?g/mL of vanillic acid; about 0.1 to about 0.3 ?g of stearic acid; and water; wherein all wt. % are based on g/100 g of the gel composition. This gel composition can be topically administered to the rectum of a patient to treat one or more bowel diseases, disorders, or conditions.

Abstract: The present disclosure provides methods of identifying patients who have partial or total resistance to HIF-2 inhibitors or who develop partial or total resistance to HIF-2 inhibitors after treatment and providing suitable treatment to these patients.

Abstract: The present disclosure is in the field of pharmaceutical compositions suitable for the treatment of diseases in mammals. The disclosure provides novel compositions comprising non-pathogenic fecal microbes or a sterile fecal filtrate for treating Parkinson's disease and related diseases. The disclosure also provides methods for treating a subject with the compositions disclosed herein.

Abstract: Provided herein are naphthoquinones compounds such as those with a hydrogen bond donating group of the formula (I): wherein: R1, R2, R3, R4, R5, and n are as defined herein. Also provided herein are pharmaceutical composition of the present compounds and methods of treatment using the compounds including their use in the treatment of cancer.

Abstract: A composition for the treatment of emesis comprising 8-hydroxy-2-(dipropylamino)tetralin in which the ratio of the S enantiomer of the 8-hydroxy-2-(dipropylamino)tetralin to the R enantiomer of the 8-hydroxy-2-(dipropylamino)tetralin is between 2:1 and 10:1, and a method of treating or preventing emesis with such a composition.

Abstract: A convenient method for converting oximes into enamides is disclosed. The process produces enamides without the concomitant production of a large volume of metallic waste. The enamides are useful precursors to amides and amines.

Abstract: Methods and compositions utilizing 2-aminoindan derivatives collectively represented by Formula I as described and defined in the specification for regulating binge behavior, particularly binge drinking, are disclosed.

Abstract: A composition for the treatment of emesis comprising 8-hydroxy-2-(dipropylamino)tetralin in which the ratio of the S enantiomer of the 8-hydroxy-2-(dipropylamino)tetralin to the R enantiomer of the 8-hydroxy-2-(dipropylamino)tetralin is between 2:1 and 10:1, and a method of treating or preventing emesis with such a composition.

Abstract: Methods and compositions utilizing 2-aminoindan derivatives collectively represented by Formula I as described and defined in the specification for regulating binge behavior, particularly binge drinking, are disclosed.

Abstract: This invention provides a convenient method for converting oximes into enamides. The process does not require the use of metallic reagents. Accordingly, it produces the desired compounds without the concomitant production of a large volume of metallic waste. The enamides are useful precursors to amides and amines. The invention provides a process to convert a prochiral enamide into the corresponding chiral amide. In an exemplary process, a chiral amino center is introduced during hydrogenation through the use of a chiral hydrogenation catalyst. In selected embodiments, the invention provides methods of preparing amides and amines that include the 1,2,3,4-tetrahydro-N-alkyl-1-naphthalenamine or 1,2,3,4-tetrahydro-1-naphthalenamine substructure.

Abstract: A method of treating or preventing emesis through the administration of an effective dosage of a 2-(amino)tetralin compound in which one of the S or R enantiomers of the 2-(amino) tetralin compound is present in the composition in excess of the other enantiomer, and compositions comprising such a 2-(amino)tetralin compound in which the ratio of the S and R enantiomers is at least 2:1.

Abstract: The present invention relates to new indene derivatives of formula (I) having a great affinity for sigma receptors, especially sigma-1 receptors, as well as to the process for the preparation thereof, to compositions comprising them, and to their use as medicaments.

Abstract: Uses of a compound of any of Formulas I-VI as a cytotoxic inhibitor of undifferentiated cells are disclosed herein, as well as pharmaceutical compositions comprising a compound of any of Formulas I-VI, and methods for identifying a lead candidate for inhibiting undifferentiated cells. Further disclosed are uses of an SCD-1 inhibitor as a cytotoxic inhibitor of undifferentiated cells.

Abstract: The invention relates to the compounds of formula I or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I; and methods for treating or preventing neurological degenerative disorders, may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of Alzheimer's disease, Lewy body disease, Huntington's disease, Amyotrophic lateral sclerosis (ALS) and Parkinson's disease.

Abstract: Propynylaminoindan (e.g., Rasagiline) transdermal compositions are provided. Aspects of the transdermal compositions include a matrix of the propynylaminoindan in a pressure sensitive adhesive comprising a carboxylated polymer. In some instances, the matrix further includes a cationic acrylic copolymer. Also provided are methods of using the transdermal compositions and kits containing the transdermal compositions.

Abstract: The present invention is directed to methods and assays for identifying subjects participating in clinical trials that may exhibit a placebo response and identifying treatments for subjects with varying degrees of placebo responses. In one aspect, a method of selecting subjects to participate in a clinical trial is disclosed. In another aspect, methods for treating a subject and determining a treatment dosage are disclosed. In an exemplary embodiment, a method for determining a response to a treatment of a subject having, suspected of having, or at risk for developing a disorder, such as cardiovascular disorder, irritable bowel syndrome, diabetes, autoimmune disorders, inflammation, neurological disorders, chronic pain, cancer, cancer treatments, allergies, depression, migraines, addiction, obesity, and other disorders, syndromes, or diseases, is disclosed.

Abstract: The invention relates to selective oestrogen receptor modulators (SERMs) and to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular of bleeding disorders, osteoporosis, endometriosis, myomata, hormone-dependent tumours, for hormone replacement therapy and for contraception.

Abstract: A drug in a solubility-improved form is combined with a concentration-enhancing polymer in a sufficient amount so that the combination provides substantially enhanced drug concentration in a use environment relative to a control comprising the same amount of the same solubility-improved form of drug without the concentration-enhancing polymer.

Abstract: Methods are provided to inhibit proliferation of Trypanosoma cruzi with imido-substituted 1,4-naphthoquinones, including novel compounds. Administering an imido-substituted 1,4-naphthoquinone can be used to provide prophylaxis or treatment to a patient in need of treatment against Chagas disease.

Abstract: The invention provides a tamper-resistant dosage form including a therapeutic agent-substrate complex embedded in a thermo-formable matrix; such that the complex includes at least one therapeutic agent bound to at least one substrate to form the therapeutic agent-substrate complex. The at least one substrate is being selected from the group consisting of a polyelectrolyte, an organic counter-ion, a pharmacologically inert organic component of a prodrug, an inclusion compound and an inorganic adsorbent; and the thermo-formable matrix includes one or more thermoplastic polymers and optionally at least one pharmaceutical additive.

Abstract: Disclosed are methods of enhancing cognitive impairment in a patient wherein the cognitive impairment is due to ADDL neurotoxicity. The methods employ non-peptidic compounds having a molecular weight of less than 1000 and which can antagonize against formation of neurotoxic ADDLs from A?1-42 monomers.

Abstract: The subject invention provides a pharmaceutical composition containing N-propargyl-1(R)-aminoindan or a pharmaceutically acceptable salt thereof, and a compound of 3-keto-N-propargyl-1-aminoindan or a salt thereof.

Abstract: The present invention relates to salts of rasagiline and pharmaceutical preparations thereof. The invention further provides a method of preparing the salts of rasagiline.

Abstract: Methods of halogenating a carbon containing compound having an sp3 C—H bond are provided. Methods of fluorinating a carbon containing compound comprising halogenation with Cl or Br followed by nucleophilic substitution with F are provided. Methods of direct oxidative C—H fluorination of a carbon containing compound having an sp3 C—H bond are provided. The halogenated products of the methods are provided.

Abstract: This invention relates to novel compounds suitable for labelling or already labelled by 18F, methods of preparing such a compound, compositions comprising such compounds, kits comprising such compounds or compositions and uses of such compounds, compositions or kits for diagnostic imaging by positron emission tomography (PET).

Abstract: This invention provides a solid pharmaceutical composition comprising rasagiline or a pharmaceutically acceptable salt of rasagiline, and particles having a non-filamentous microstructure of at least two sugar alcohols. This invention also provides a solid pharmaceutical composition comprising rasagiline or a pharmaceutically acceptable salt of rasagiline, a mixture of a disintegrant, a flow agent and particles having a non-filamentous microstructure of at least two sugar alcohols, a supplemental sugar alcohol, a supplemental flow agent, and a supplemental disintegrant. This invention further provides a method of treating a subject afflicted with Parkinson's disease comprising administering to the subject a therapeutically effective amount of the solid pharmaceutical composition, thereby treating the subject. Finally, this invention provides a process of making such solid pharmaceutical compositions.

Abstract: A method of treating or preventing emesis through the administration of an effective dosage of a 2-(amino)tetralin compound in which one of the S or R enantiomers of the 2-(amino) tetralin compound is present in the composition in excess of the other enantiomer, and compositions comprising such a 2-(amino)tetralin compound in which the ratio of the S and R enantiomers is at least 2:1.

Abstract: The subject invention provides deuterated rasagiline, its salts and uses.

Abstract: Methods are provided to inhibit proliferation of Leishmania parasites, and in particular Leshmania donovani with imido-substituted 1,4-naphthoquinones, including novel compounds. Administering an imido-substituted 1,4-naphthoquinone can used to provide prophylaxis or treatment to a patient in need of treatment against leishmaniasis disease.

Abstract: The invention is directed to methods to identify predisposition or risk to develop Parkinson's disease, methods to identify agents which have therapeutic effect on Parkinson's disease, and methods to determine the therapeutic effect of an agent in a subject suffering from Parkinson's disease, and to kits and reagents for carrying out the methods of the invention.

Abstract: A drug in a solubility-improved form is combined with a concentration-enhancing polymer in a sufficient amount so that the combination provides substantially enhanced drug concentration in a use environment relative to a control comprising the same amount of the same solubility-improved form of drug without the concentration-enhancing polymer.

Abstract: The present invention provides a stable composition of rasagiline comprising an effective dosage of rasagiline or its pharmaceutically acceptable salts and an antioxidant used as a stabilizer. The dosage forms of the composition are pharmaceutically common transdermal-drug delivery dosage form and mucoadhesive delivery dosage form, such as patch, gel, ointment, cream, cataplasm, film, spray and solution, etc. The composition can be used to prevent or treat mental disorders.

Abstract: The present disclosure provides polymer conjugates comprising a polymer and an agent, the agent linked to the polymer via a linking group containing a cleavable moiety.

Abstract: The present invention is directed to a crosslinked or non-crosslinked polymer particle, wherein the crosslinked polymer particle comprises a copolymer of poly(alkylene glycol-graft-acrylate) that is crosslinked by at least one hydrolysable monomer or crosslinking agent. The present invention is also directed to a polymer particle comprising a crosslinked polymer particle that is a product of starting materials comprising (a) a hydrophilic monomer, (b) a hydrophobic monomer, and (c) a hydrolysable crosslinking agent (the crosslinking agent may be absent in the case of non-crosslinked particles). The present invention is still further directed to a polymer particle comprising a crosslinked copolymer, where the crosslinked copolymer includes structures represented by Formulas (I), (II), and (III), as defined in the specification. Other embodiments of the present invention also include methods of manufacturing polymer particles.

Abstract: A pharmaceutical composition, comprising a GluR2-lacking AMPAR antagonist as an active ingredient, is effective for preventing or treating mental diseases selected from the group consisting of posttraumatic stress disorder (PTSD), drug addiction, and phobia.

Abstract: A method is provided for the treatment of vision problems in a subject suffering from one of various forms of albinism, including, for example, oculocutaneous albinism types OCA1a and OCA1b, as well as ocular albinism type 1, resulting from mutations in the GPR143 gene, as well as the OCA2, OCA3 or OCA4 genes, by administering to the subject a pharmaceutical composition comprising a therapeutically effective amount of the compound (2-[2-nitro-4-(trifluoromethyl)benzoyl]cyclohexane-1,3-dione), also known as NTBC for a sufficient period of time. The administration of NTBC is believed to increase the amount of pigmentation in the subject and alleviate certain symptoms caused by lack of pigmentation in the eye tissues. Also described are methods of use of NTBC for increasing the pigmentation of a subject for cosmetic purposes, by administering to the subject a therapeutically effective amount of NTBC.

Abstract: A method for modifying Parkinson's disease by periodically administering a pharmaceutical composition comprising a therapeutically effective amount of rasagiline or a pharmaceutically acceptable salt of rasagiline to the patient, thereby modifying the disease. The method includes reducing the rate of progression; delaying the need for symptomatic anti-Parkinsonian therapy; reducing the risk of a Parkinson's disease patient requiring symptomatic anti-Parkinsonian therapy; and reducing the functional decline.

Abstract: The present invention provides pharmaceutical compositions comprising substituted 1,4 naphthoquinones that are effective in preventing oligomerization of beta amyloid and subsequent pathologies associated with amyloid fibrils. These compositions are useful for the treatment of disease involving amyloidogenesis including neurodegenerative diseases such as Alzheimer's Disease or senile dementia. Particularly effective compositions comprise 1,4 naphthoquinones substituted with an amino acid residue selected from a heterocyclic or aromatic amino acid.

Abstract: The subject invention provides a solid dispersion of rasagiline citrate, a composition and a process for the manufacture thereof.

Abstract: Propynylaminoindan (e.g., Rasagiline) transdermal compositions are provided. Aspects of the transdermal compositions include a matrix which includes the propynylaminoindan, a pressure sensitive adhesive that includes an acrylate copolymer and a cationic acrylic copolymer. Also provided are methods of using the transdermal compositions and kits containing the transdermal compositions.

Abstract: A method for preparing a transdermal patch comprising a substrate layer is provided, the method comprising the steps of contacting an active pharmaceutical ingredient with a retaining means to provide a composition, applying the composition obtained in step (a) to a carrier material to form a substrate layer of the transdermal patch, wherein the retaining means remain within the final transdermal patch.

Abstract: A novel pathogenesis underlying certain types of seizures and migraines is disclosed and the validated set of premises presented enable the deductive conclusion to be made that drugs that reduce the amount of calcium ions (Ca++) released from bone reduce seizure and migraine risk. The premises validated as true in the specifications include: 1) Known seizure and migraine triggers increase osteoclast mediated release of Ca++ from bone. 2) Increased Ca++ released from bone increases seizure and migraine risk by a) depolarization of nerve membranes, b) enhanced calcium channel mediated neurotransmitter release and increases muscle contractility by c) enhanced neurotransmitter release at the neuromuscular junction and d) enhanced removal of the tropomyosin block between actin and myosin. 3) Conversely, reducing Ca++ released from bone reduces seizure and migraine risk. 4) Cinacalcet reduces Ca++ released from bone. Therefore, cinacalcet reduces migraine risk.

Abstract: Provided are methods of treating obesity and effecting desired weight loss or preventing undesired weight gain by administration of a preferential muscarinic acetylcholine receptor M1 antagonist, optionally with at least one antidepressant other than a selective muscarinic acetylcholine receptor M1 antagonist. The preferential muscarinic acetylcholine receptor M1 antagonist, optionally can be administered with an anti-obesity agent, for example, an anorexiant. The invention also provides for pharmaceutical compositions and kits for administration of at least one selective muscarinic acetylcholine receptor M1 antagonist in combination with at least one antidepressant other than a selective muscarinic acetylcholine receptor M1 antagonist.

Abstract: An agent for the prophylaxis or treatment of stress urinary incontinence, which contains a substance that activates a serotonin 5-HT2C receptor, an agent for the prophylaxis or treatment of stress urinary incontinence, which contains a substance that stimulates an androgen binding site, and a method of screening for a drug for the prophylaxis or treatment of abdominal pressure incontinence, which includes electrostimulating the abdominal muscles or a nerve controlling them of an animal to increase the abdominal pressure, and measuring the leak point pressure at that time.

Abstract: The present invention relates to an improved process for the preparation of Rasagiline or pharmaceutically acceptable salts thereof. The present invention also relates to Rasagiline salts, polymorphs thereof and process for preparation thereof.

Abstract: Propynylaminoindan (e.g., Rasagiline) transdermal compositions are provided. Aspects of the transdermal compositions include a matrix which includes the propynylaminoindan, a pressure sensitive adhesive that includes an acrylate copolymer and a cationic acrylic copolymer. Also provided are methods of using the transdermal compositions and kits containing the transdermal compositions.