Abstract: A pharmaceutical composition for prophylaxis and/or treatment of infections and/or infectious diseases occurring in cystic fibrosis includes at least one antidepressant; at least one dispersant; and at least one pharmaceutically tolerable carrier material.

Abstract: Phenylboronic acid and water soluble derivatives thereof and related boronic acid compounds are used for treating fungal and bacterial infections.

Abstract: The present invention relates to topical antifungal formulations terbinafine or a pharmaceutically acceptable salt thereof, a lipid, and a surfactant, and uses thereof for the treatment of skin and nail fungal infections.

Abstract: Disclosed are pharmaceutical preparations of R(+)-N-propargyl-1-aminoindan salts having enhanced content uniformity, processes for preparation of the compositions, and their uses.

Abstract: The invention relates to a process for producing mouldings by injection moulding the steps in the process being a) melting and mixing of a (meth)acrylate copolymer composed of from 85 to 98% by weight of C1-C4-alkyl (meth)acrylates capable of free-radical polymerization and from 15 to 2% by weight of (meth)acrylate monomers having a quaternary ammonium group in the alkyl radical, with from 10 to 25% by weight of a plasticizer, and also from 10 to 50% by weight of a dryers [sic] and/or from 0.1 to 3% by weight of a release agent, and, where appropriate, with other conventional pharmaceutical additives or auxiliaries and/or with an active pharmaceutical ingredient, b) devolatilizing the mixture at temperatures of at least 120° C., thus reducing the content of the low-boiling constituents with a vapour pressure of at least 1.9 bar at 120° C. to not more than 0.5% by weight, and c) injecting the devolatilized mixture at a temperature of from 80 to 160° C.

Abstract: The present invention relates to novel pharmaceutical compositions based on telmisartan 1 and anticholinergics 2 processes for preparing them and their use for the treatment of respiratory diseases.

Abstract: The invention provides Beta-blocker drugs that are chemically modified by covalent attachment of a water soluble oligomer. A conjugate of the invention, when administered by any of a number of administration routes, exhibits a different biological membrane crossing rate as compared to the biological membrane crossing rate of the Beta-blocker drug not attached to the water soluble oligomer.

Abstract: The invention relates to protein binding interacting/binding compounds and methods of identifying and using them. The invention further relates to pharmaceutical compositions and methods for treating 5-HT2C disorders, including diseases and disorders mediated by GPCRs.

Abstract: This invention relates to methods of imaging amyloid deposits, radiolabeled compounds, and methods of making radiolabeled compounds useful in imaging amyloid deposits. This invention also relates to compounds and methods of making compounds for inhibiting the aggregation of amyloid proteins to form amyloid deposits and methods of delivering therapeutic agents to amyloid deposits.

Abstract: The invention provides a compound of formula (I) or a pharmaceutically acceptable ester, amide, solvate or salt thereof, including a salt of such an ester or amide, and a solvate of such an ester, amide or salt, wherein W, X, Y, Z, R1, R2, R7, R8, R9, R10, R11, R12, R13, R14, R15 and R16 are as defined in the specification. The invention also provides also provides the use of such compounds in the treatment or prophylaxis of a condition associated with a disease or disorder associated with estrogen receptor activity.

Abstract: The invention relates to formulations of an antimicrobial agent, a lipid, and optionally a surfactant, and uses thereof for reducing the proliferation and viability of microbial agents.

Abstract: Disclosed are formulations which are designed to delay release of rasagiline while maintaining specific pharmacokinetic properties.

Abstract: Disclosed are formulations which are designed to delay release of rasagiline while maintaining specific pharmacokinetic properties.

Abstract: Disclosed are formulations which are designed to delay release of rasagiline while maintaining specific pharmacokinetic properties.

Abstract: The subject invention provides crystalline R(+)-N-propargyl-1-aminoindan, pharmaceutical compositions and methods of manufacture thereof.

Abstract: Disclosed are pharmaceutical preparations of R(+)-N-propargyl-1-aminoindan salts having enhanced content uniformity, processes for preparation of the compositions, and their uses.

Abstract: The invention provides novel compounds of formulae I and II: that are monoamine oxidase-B inhibitors, which can be useful in treating obesity, diabetes, and/or cardiometabolic disorders (e.g., hypertension, dyslipidemias, high blood pressure, and insulin resistance).

Abstract: Compositions and methods for treating disorders of the outer retina with compounds with 5-HT1A agonist activity are disclosed.

Abstract: The subject invention provides crystalline R(+)-N-propargyl-1-aminoindan, pharmaceutical compositions and methods of manufacture thereof.

Abstract: The present invention relates to an adsorbate of a pharmaceutically compatible rasagiline salt comprising at least one pharmaceutically compatible adjuvant, wherein the at least one pharmaceutically compatible adjuvant is a water-soluble, organic solvent and the rasagiline salt is present in the adsorbate as an amorphous substance.

Abstract: The invention relates to compounds of formula (I), wherein R1, R2, R1a, R2a, R3, R4, A, B, X, W and n are as defined in the description, and pharmaceutically acceptable salts of such compounds. These compounds are useful as calcium channel blockers.

Abstract: The present invention provides a method for treating or preventing a disease or disorder treatable by the inhibition of serotonin reuptake in a patient, and/or norepinephrine reuptake and/or dopamine reuptake in a patient, the method comprising administering to the patient a neurotransmitter reuptake inhibiting-effective amount of at least one compound of the formula A-L-B (I) or a pharmaceutically acceptable salt, ester or prodrug thereof, wherein A is a psychotropic derivative; L is a linking group comprising two carbon atoms; and B is an alkyl, alkenyl, alkynyl or aralkyl comprising at least one substituent of the formula Q, wherein: the alkyl, alkenyl, alkynyl or aralkyl is optionally substituted with one or more halogean halogens, hydroxyl, cyano, nitro, amino or thiol; and Q is OR6, OC(O)R6, C(O)R6, C(S)R6, CO2R6, C(O)SR6, C(O)NR6R7, C(S)NR6R7, NR6R7, NR6C(O)R7, NR6C(S)R7, NR6C(O)NR7R8, NR6C(S)NR7R8, NR6SO2R7, NR6SO2NR7R8, SR6, SC(O)R6, SC(O)NR6R7, S(O)R6, SO2R6, SO2NR6R7, or NR6SO2NR7R8.

Abstract: Provided herein are methods of treating gastrointestinal motility disorders by targeting the dopamine 3 receptor (D3R). A D3R agonist is administered to a subject to decrease gastrointestinal motility to treat the disorder. A D3R antagonist is administered to a subject to decrease gastrointestinal motility to treat the disorder.

Abstract: A compound of the general formula (I) as an active principle for treating cancer, specifically tumors, in particular diseases involving inhibition of metalloproteases, such as Aminopeptidase-N. Pharmaceutical compositions comprising the compound of general formula (I). Methods of treatment using the compound of general formula (I).

Abstract: The present invention relates to compounds useful for detecting the activity of human aldoketoreductase 1Cs, compounds useful for competitively inhibiting human aldoketoreductase 1Cs and compounds useful for treating human aldoketoreductase 1C-related cancers, as well as pharmaceutical compositions and methods of manufacture thereof.

Abstract: The invention relates to tetrahydronaphthalene derivatives, process for their production and their use as anti-inflammatory agents.

Abstract: An antifungal liquid composition for topical administration is provided that contains turpentine and at least one of peppermint oil, mineral oil, and essential oil alcohols, and one or more antifungal medications selected from ciclopirox olamine, terbinafine, tolnaftate, microconazole, itraconazole, ketoconazole, econazole, and fluconazole, and optionally one or more antifungal essential oils, and its use in the topical treatment of fungal infection, particularly of the nail.

Abstract: The present invention relates to heterocyclyl-substituted-tetrahydro-naphthalen compounds of general formula (I), methods for their preparation, and compositions comprising these compounds as well as their use for the treatment or prophylaxis of various disorders in humans or animals.

Abstract: The invention provides novel compounds of formulae I and II: that are monoamine oxidase-B inhibitors, which can be useful in treating obesity, diabetes, and/or cardiometabolic disorders (e.g., hypertension, dyslipidemias, high blood pressure, and insulin resistance).

Abstract: Disclosed are formulations which are designed to release rasagiline mesylate while maintaining specific pharmacokinetic properties.

Abstract: A polymorph of rasagiline hydrochloride displays improved stability and is useful in forming pharmaceutical compositions for treating Parkinson's disease. Another polymorph is useful as an intermediate in forming the stable crystalline form.

Abstract: Disclosed is crystalline R(+)-N-propargyl-l-aminoindan containing water at an amount of less than 0.5% by weight and a pharmaceutical composition comprising the same, and the process for the manufacture and the validation thereof. Also disclosed is a process for the preparation of solid rasagiline base.

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: Treatment of CNS disorders with (1R,4S)-trans 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-napthalenamine; and (1S,4R)-trans 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-napthalenamine is disclosed. A process for preparing 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-1-napthalenamine is also disclosed. The process includes the preparation of all four isomers of N-[4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydronaphthalen-1-yl]formamide, which are also useful.

Abstract: The inventors have found that vitamin K3 and vitamin K5 which may be used in pharmaceuticals and foods or ACNQ, DHNA, or the like which can stimulate the growth of bifidobacteria can inhibit degranulation of basophil-like cells, exhibit a potent degranulation-inhibiting effect, and are useful anti-allergic agents or foods. The present invention provides an anti-allergic agent containing, as an active ingredient, one or more species selected from among 2-amino-3-carboxy-1,4-naphthoquinone, 1,4-dihydroxy-2-naphthoic acid, 1,4-naphthoquinone, 4-amino-2-methyl-1-naphthol, 2-methyl-1,4-naphthoquinone, 2-amino-3-chloro-1,4-naphthoquinone, and a salt thereof.

Abstract: The present invention relates to dispersions of stable amorphous cinacalcet hydrochloride in a matrix material, methods for the preparation thereof, and pharmaceutical compositions comprising said dispersions.

Abstract: Methods for preventing or treating bruxism, including alleviating or eliminating one or more symptoms, diseases or conditions associated with or resulting from bruxism, using dopaminergic agents such as monoamine oxidase inhibitors that increase dopaminergic activity and dopamine agonists, are disclosed.

Abstract: The invention provides preparations, formulations, kits and other products of manufacture (e.g., blister packs) comprising combinations of beneficial ingredients that are serviceable as therapies for improving states and disease symptoms such as involving inflammation, excessive sympathoneural drive, cachexia, anorexia, and anorexia-cachexia, as well as stress or anxiety related thereto, and methods of making and using them. The invention provides compositions and therapies comprising use of a beta adrenergic antagonist (also called “beta blockers”, e.g., propranolol) in combination with an anti-inflammatory agent, e.g., a nonsteroidal anti-inflammatory drug (NSAID), an angiotensin-converting enzyme (ACE) inhibitor, an angiotensin receptor blocker (ARB), an anabolic steroid, a natural oil or fatty acid or any combination thereof.

Abstract: This invention relates to compounds which modulate receptors of the 5-HT2 family of receptors, and particularly to compounds which modulate 5-HT2C receptors. Compounds of the invention include agonists and selective agonists for the 5-HT2C receptor Compounds of the invention include selective agonists for the 5-HT2C receptor which exhibit significantly less or no agonist activity on the 5-HT2A receptor and/or the 5-HT2B receptor. Compounds of this invention are those of Formula I and pharmaceutically acceptable salts, esters and solvates (including hydrates) wherein variables are defined in the specification hereof.

Abstract: Provided herein are substituted aminoglycidyl compounds of Formula (1), processes of preparation, and pharmaceutical compositions thereof and methods of their use for treating, preventing, or ameliorating one or more symptoms of a social anxiety disorder, an anxiety disorder, hyperthyroidism, tremor, glaucoma, hypertension, coronary artery bypass graft, chronic stable angina, atrial arrhythmia, migraine, bleeding esophageal varices, hypertrophic subaortic stenosis, heart failure, post-myocardial infarction, decreased left ventricular function after recent myocardial infarction, and/or any disorder ameliorated by beta adrenergic receptor modulators.

Abstract: The subject invention provides rasagiline tannate, compositions and a process for manufacture thereof.

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: The present invention relates to a rasagiline transdermal patch for treatment or prophylaxis of nervous system diseases, in which the patch comprises an inert backing layer chemically inert to substrate ingredients, a substrate layer comprising rasagiline or a pharmaceutically acceptable salt thereof, and a protective layer to be peeled off before use. The substrate layer is an adhesive system comprising an organic polymer material as basis and an inorganic or organic material as filler, and a plurality of micro-reservoirs containing rasagiline. The substrate further comprises one or more substances for enhancing the transdermal absorption of rasagiline, in which the above organic polymer material in the substrate is used for the reservoir of rasagiline and as adhesive.

Abstract: The subject invention provides derivatives of propargylamino indan (PAI) and propargylamino tetralin that selectively inhibit monoamine oxidase (MAO) in the brain, having the structure: wherein R1 is OC(O)R9 and R2 is H, wherein R9 is branched or unbranched C1 to C6 alkyl, aryl, or aralkyl, or R1 is OC(O)R4 and R2 is OC(O)R4, wherein R4 is branched or unbranched C1 to C6 alkyl, aryl, aralkyl or NR5R6, wherein R5 and R6 are each independently H, C1 to C8 alkyl, C6 to C12 aryl, C6 to C12 aralkyl or C6 to C12 cycloalkyl, each optionally substituted; wherein R3 is H or C1 to C6 alkyl; wherein n is 0 or 1; and wherein m is 1 or 2, or a pharmaceutically acceptable salt thereof. Additionally, the subject invention provides methods of treating neurological disorders using these compounds, uses of these compounds for the manufacture of medicaments for treating neurological disorders and processes for synthesis of these compounds.

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: The present application describes deuterium-enriched sertraline, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.

Abstract: Disclosed is a method of reducing glaucoma in a subject afflicted with glaucoma, comprising administering to the subject an amount of R(+)-N-propargyl-1-aminoindan or a pharmaceutically acceptably salt thereof effective to reduce glaucoma.

Abstract: This disclosure ascribes new functions to derivatives of tetralin, anthraquinone, naphthylamine, tri-amino-pyrimidine, xanthen-3-one, and/or cinnamic acid (including, for example, NSC270718R, NSC117285R, NSC170008Y, NSC306711P, NSC119913X, NSC119915Z, NSC119911V, NSC119910U, NSC128437O, NSC125908P, NSC9600Q, or NSC13778J, each obtained from the Structure Diversity Set, National Institutes of Health, National Cancer Institute, Developmental Therapeutics Program). These compounds are shown to be effective inhibitors of viral essential protein kinases (such as poxvirus B1 and/or F10 protein kinases). Exemplary chemical structures for viral protein kinase (VPK) inhibitors are provided, as are methods of using such compounds, for instance, to inhibit VPK activity and/or poxvirus growth, and/or for the treatment of poxvirus infection. Also provided are pharmaceutical compositions including disclosed VPK inhibitors.

Abstract: An agent for the treatment of allergic eye disease containing a 3-anilino-2-cycloalkenone derivative having the formula (I): wherein R1 is an unsubstituted or substituted C1 to C8 alkyl group provided that an unsubstituted methyl group is excluded, a C3 to C7 cycloalkyl group, a C6 to C10 bicycloalkyl group or an indanyl group, etc., R2 is a C1 to C4 alkyl group, R3 is a hydrogen atom, a C1 to C5 alkyl group, a C3 to C7 cycloalkyl group, etc., R4 is a hydrogen atom, an unsubstituted or substituted C1 to C5 alkyl group, a halogen atom, etc., R5, R6, R7 and R8 are independently a hydrogen atom, a C1 to C5 alkyl group, etc., X is —(CR11R12)n— or NR13—, wherein n is 0 to 2, R11, R12 and R13 are independently a hydrogen atom, a C1 to C5 alkyl group, etc.

Abstract: The invention provides pyrrolidino-substituted 1,4-naphthoquinone derivatives that modulate the activity of protein kinases, and it relates to the use of the derivatives in pharmaceutical compositions for treating cardiovascular disorders and malignancies. The invention particularly provides medicaments for treating disorders associated with MAPKs signaling, ERKs signaling, p38 signaling, and JNKs signaling.