Abstract: Compounds that have agonist activity at one or more of the S1P receptors are provided. The compounds are sphingosine analogs that, after phosphorylation, can behave as agonists at S1P receptors.

Abstract: The present invention relates generally to pharmacological methods for the prevention of amelioration of sleep-related breathing disorders via administration of agents or combinations of agents that possess serotonin-related pharmacological activity.

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

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

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: Propargylamine, propargylamine derivatives including N-propargyl-l-aminoindan, enantiomers and analogs thereof, and pharmaceutically acceptable salts thereof, are useful for prevention or treatment of cardiovascular disorders, diseases and conditions.

Abstract: The invention provides a method for improving hair biology, e.g., hair growth. The method comprises administering to a subject a monoamine oxidase inhibitor and a vasodilator, a zinc salt of a carboxylic acid, a xanthine compound, pyrithione or a salt thereof, saponin, tritapene, crataegolic acid, celastrol, asiatic acid, an inhibitor of 5-alpha-reductase, 1,4-methyl-4-azasteroid, an androgen receptor antagonist, azelaic acid or a derivate thereof, cyclosporin, triiodothyronine, diazoxide, retinoic acid, a prostaglandin analogue, aminexil, carnitine tartrate, apigenin, procapil, or adenosine, in an amount effective to achieve a desired effect. The invention further provides a method of reducing or delaying the appearance of an age-related skin imperfection. The method comprises administering to the subject a composition comprising an MAO inhibitor. A kit for improving hair growth also is provided.

Abstract: The present invention relates to allosteric binding compounds of formula (I), especially for the treatment of CNS disorders, together with pharmaceutical compositions and methods of treatment including these compounds.

Abstract: The invention relates to novel salts of the active substance rasagiline. The salts show excellent processability even after prolonged storage and an excellent storage stability usually superior to known salts after being processed into tablets.

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

Abstract: Disclosed are methods of treating olfactory dysfunction by periodically administering a therapeutically effective amount of rasagiline or a pharmaceutically acceptable salt of rasagiline to a subject.

Abstract: Novel classes of molecular chaperone Heat shock protein 90 (Hsp90) inhibitors are disclosed. These compounds are useful in treating and preventing cancer and other Hsp90-related diseases and conditions, such as inflammation and neurodegenerative disorders. Methods of treating and preventing cancer and other Hsp90 related diseases and conditions are disclosed that include administering to the subject a therapeutically effective amount of an Hsp90 inhibitor. Methods of preparing the novel Hsp90 inhibitors are also provided.

Abstract: Propargylamine, propargylamine derivatives including N-propargyl-1-aminoindan, enantiomers and analogs thereof, and pharmaceutically acceptable salts thereof, are useful for prevention or treatment of cardiovascular disorders, diseases and conditions.

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: Disclosed are formulations of rasagiline base which are designed to delay release of rasagiline while maintaining specific pharmacokinetic properties. Also, disclosed are rasagiline citrate salt and the use and process of manufacture thereof.

Abstract: Compounds of formula (I) have muscarinic M3 receptor modulating activity; wherein A is an oxygen atom or group —N(R12)—; (i) R1 is C1-C6-alkyl or a hydrogen atom; and R2 is a hydrogen atom or a group —R5, —Z—Y—R5, —Z—NR9R10; —Z—CO—NR9R10; —Z—NR9—CO—R5; or —Z—CO2H; and R3 is a lone pair, or C1-C6-alkyl in which case the nitrogen atom to which it is attached is a quaternary nitrogen and carries a positive charge; or (ii) R1 and R3 together with the nitrogen to which they are attached form a heterocycloalkyl ring, and R2 is a hydrogen atom; or a group —R5, —Z—Y—R5, —Z—NR9R10, —Z—CO—NR9R10, —Z—NR9—CO—R5, or —Z—CO2H, in which cases the nitrogen atom to which it is attached is a quaternary nitrogen and carries a positive charge; or (iii) R1 and R2 together with the nitrogen to which they are attached form a heterocycloalkyl ring, said ring being substituted by a group —Y—R5, —Z—Y—R5, —Z—NR9R10; —Z—CO—NR9R10; —Z—NR9—CO—R5; or —Z—CO2H and R3 is a lone pair, or C1-C6-alkyl in which case the nitrogen atom to whi

Abstract: The present invention relates to a solid composition containing at least one pharmaceutically compatible auxiliary ingredient and rasagiline or a pharmaceutically compatible salt thereof as an active ingredient. The invention further relates to a method for producing said solid composition and to a medicine comprising said solid composition.

Abstract: A method and composition that allows for the penetration of lipid insoluble medicaments through cell membranes using small S-Allyl-containing molecules with phospholipid permeable molecules as carrier molecules. S-Allyl-containing compounds can include alliin, allicin, Allium sativum extract and DMSO. Lipid insoluble medicaments can include 1% xylocaine, curcumin, acyclovir, valacyclovir, famciclovir, terbenafin, griseofulvin, clotrimazole, ketoconazole, clindamycin, neomycin, polysporin, bactricin, among others. The lipid insoluble medicaments are mixed with the phospholipid permeable molecules and painted on the skin using a swab or other suitable tool, thereby allowing for penetration of the medicament and providing relief from pain potentially caused by a subsequent injection. The composition can also be administered through an inhaler or directly into mucous membranes.

Abstract: The present invention relates N-cycloalkyl-N-bicyclicmethylene-carboxamide, thiocarboxamide or N-substituted carboximidamide derivatives of formula (I) wherein A represents a carbo-linked, 5-membered heterocyclyl group, T represents O or S, Z1 represents a C3-C7-cycloalkyl group, X represents N or a CZ7 and Y1, Y2, Z2, Z3, L1 and L2 represent various substituents, their process of preparation, the preparation of intermediate compounds, their use as fungicide active agents, particularly in the form of fungicide compositions and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions.

Abstract: The present invention provides a nitrogen-containing compound represented by formula (I1) (in formula (I1), R0 represents a nitro group or the like, Z represents an optionally substituted aryl group or the like, R3 represents a hydrogen atom or the like, Y represents a nitro group or the like, n represents an integer of 0 to 3, D represents an optionally substituted 5-membered to 8-membered hydrocarbon ring group or heterocyclic group having or not having a substituent other than substituent X, X represents a group represented by formula (II-1) (in formula (II-1), R1 and R2 respectively and independently represent a hydrogen atom or the like), A represents a carbon atom or the like, n1 represents an integer of 0 to 2) or a salt thereof, and an insecticide, miticide, sanitary insect pest control agent, or harmful organism control agent including as an active ingredient thereof the nitrogen-containing compound or the salt thereof.

Abstract: Disclosed is crystalline R(+)-N-propargyl-1-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: Methods of preparing cinacalcet, cinacalcet derivatives, and salts thereof is disclosed herein. Also disclosed herein are polymorphs of cinacalcet, compositions of cinacalcet, and methods of treating a subject by administering cinacalcet, wherein cinacalcet is prepared by the disclosed methods.

Abstract: Intracellular kinase inhibitors and their therapeutic uses for patients with T cell malignancies, B cell malignancies, autoimmune disorders, and transplanted organs.

Abstract: The invention relates to novel tetralone based amines and their use in the treatment of central nervous system (CNS) disorders, such as depression, attention deficit hyperactivity disorder (ADHD) and Parkinson's disease. The invention further relates to pharmaceutical compositions containing the compounds and compositions of the invention as well as methods of inhibiting reuptake of one or more monoamine, such as such as dopamine and norepinephrine, from the synaptic cleft, and methods of modulating one or more monoamine transporter.

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 relates to a novel crystalline form of rasagiline mesylate and a pure form of rasagiline mesylate and processes for their preparation. Further, the invention relates to pharmaceutical compositions comprising said forms and use of said compositions in the treatment of patients suffering from Parkinson's Disease, dementia, Alzheimer's Disease, depression, hyperactive syndrome, stroke, brain ischemia, neurotrauma, schizophrenia and multiple sclerosis.

Abstract: The present invention relates to an improved process for the preparation of (R)-1-aminoindan (2), rasagiline (1) and pharmaceutically acceptable salts of rasagiline.

Abstract: The present inventions provide combination therapies, kits, and methods for providing relief and/or for improving one or more symptoms associated with an auditory system disorder in a subject diagnosed with the auditory system disorder, comprising an effective amount of at least one pharmaceutical agent and at least one auditory system disorder device, as well as methods for using at least one pharmaceutical agent and/or at least one auditory system disorder device in the manufacture of said kits.

Abstract: Pharmaceutical compositions are provided for treatment of Parkinson's disease comprising a pharmaceutically acceptable carrier and a fixed dose combination of two active agents selected from compounds having either neuroprotective or symptomatic effects, or both, in Parkinson's disease patients, wherein the molar ratio of the two compounds is in the range of 1:1 to 1:100.

Abstract: The invention features methods, kits, and compositions for the treatment of psychiatric disorders using therapeutic imprinting in pre-pubescent subjects.

Abstract: Cytosine deaminase inhibitors and methods for identifying inhibitors of the anti-retroviral activity of APOBEC3G are described.

Abstract: Propargylamine, propargylamine derivatives including N-propargyl-1-aminoindan, enantiomers and analogs thereof, and pharmaceutically acceptable salts thereof, are useful for prevention or treatment of cardiovascular disorders, diseases and conditions.

Abstract: Ion channel modulating compounds are disclosed. The compounds of the present invention may be incorporated in compositions and kits. The present invention also discloses a variety of in vitro and in vivo uses for the compounds and compositions, including the treatment of arrhythmia and the production of analgesia and local anesthesia.

Abstract: Compounds that have agonist activity at one or more of the S1P receptors are provided. The compounds are sphingosine analogs that, after phosphorylation, can behave as agonists at S1P receptors.

Abstract: The present invention relates to an improved process for the preparation of rasagiline (1) and its pharmaceutically acceptable salts. In particular it relates to a process for preparing rasagiline (1) and its salts substantially free from impurities.

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: A method for the treatment of Progressive Supranuclear Palsy. Such method includes administering to a subject an amount of R(+)-N-propargyl-1-aminoindan or a pharmaceutically acceptable salt thereof.

Abstract: Provided herein is rasagiline mesylate having a 90 volume-percent of the particles (D90) with a size of about 600 microns to about 1500 microns, and a process for the preparation thereof. Provided also herein are pharmaceutical compositions comprising rasagiline mesylate particles having a particle size which is suitable for homogeneous distribution of the drug substance in a tablet blend, in particular 90 volume-percent of the particles (D90) have a size of about 255 microns to about 1500 microns, and a process the preparation thereof.

Abstract: Methods and compositions for treating disease caused by infectious agents, particularly tuberculosis. In particular, methods and compositions comprising substituted ethylene diamines for the treatment of infectious diseases are provided. In one embodiment, these methods and compositions are used for the treatment of mycobacterial infections, including, but not limited to, tuberculosis.

Abstract: Certain novel substituted 3-(phenoxymethyl) benzyl amines and personal care compositions comprising such, which are particularly beneficial for skin lightening and achieving evenness of color, especially for face and underarm skin.

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: This invention pertains to development of a new animal model for Parkinson's Disease (PD) and to the discovery that elevated monoamine oxygenase B (MOA-B) expression and/or activity is a strong prognostic indicator for the disease. Accordingly, in certain embodiments, methods are provided for identifying a mammal at risk for Parkinson's disease. The methods typically involve determining level of expression or activity of monoamine oxidase B (MAO-B) in a sample from the mammal wherein an elevated level of MAO-B expression and/or activity as compared to a control (reference) is an indicator that the mammal has an increased likelihood of developing Parkinson's disease.

Abstract: The present invention relates to indane-amine compounds of general formula (I) and compositions thereof, methods for their preparation, and the use of said compounds for the preparation of a medicament for the treatment of humans or animals.

Abstract: The present invention relates to a compound of formula (I) including any stereochemically isomeric form thereof, wherein the substituents are as defined in the specification and the claims; a N-oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof; provided that the compound is other than or a pharmaceutically acceptable salt thereof. The claimed compounds are useful for the treatment of a disease, the treatment of which is affected, mediated or facilitated by activating the GHS1A-r receptor.

Abstract: The invention features compositions, methods, and kits useful for the treatment of filovirus-mediated diseases, e.g., hemorrhagic fever caused by Ebola virus, in an animal.

Abstract: The invention discloses the use of cholinesterase inhibitors in treating vascular depression.

Abstract: The present disclosure relates generally to rasagiline mesylate with improved flowability and with advantageously reduced stickiness, to processes for the preparation thereof, and to the use thereof for milling and for preparing pharmaceutical formulations. Methods for improving the flowability and/or alleviating the stickiness of rasagiline mesylate having a very poor flowability and/or showing undesirable stickiness are also disclosed.

Abstract: Novel ligand compounds having the structural formula (I): in which: Ar is a radical selected from among the radical of formulae (a) to (c) below: are formulated into pharmaceutical compositions suited for administration in human or veterinary medicine, or, alternatively, into cosmetic compositions.

Abstract: The subject invention provides rasagiline citrate, its compositions and processes for the manufacture thereof.

Abstract: The present invention is embodied by a composition capable inducing weight loss in a patient in need thereof.