Abstract: The present invention relates to an improved process for the preparation of (2R,3R)-3-(3-methoxyphenyl)-N,N,2-trimethylpentanamine which is an intermediate for the preparation of the analgesic tapentadol.

Abstract: Crystalline modifications of (1R,2R)-3-(3-dimethylamino-1-ethyl-2-methyl-propyl)-phenol, pharmaceutical compositions which contain these modifications, and the use thereof to treat pain or other conditions.

Abstract: Provided is a novel amine compound represented by the following formula (I) having a superior peripheral blood lymphocyte decreasing action and superior in the immunosuppressive action, rejection suppressive action and the like, which shows decreased side effects of, for example, bradycardia and the like, or a pharmaceutically acceptable acid addition salt thereof, or a hydrate thereof, or a solvate thereof. wherein each symbol is as defined in the specification.

Abstract: Provided are amine derivative compounds, pharmaceutical compositions thereof, and methods of treating ophthalmic diseases and disorders, such as age-related macular degeneration and Stargardt's Disease, using said compounds and compositions.

Abstract: Provided are amine derivative compounds, pharmaceutical compositions thereof, and methods of treating ophthalmic diseases and disorders, such as age-related macular degeneration and Stargardt's Disease, using said compounds and compositions.

Abstract: The present invention relates to the compounds of formula I, processes for their production and their use as anti-inflammatory agents.

Abstract: Disclosed is a process for producing 1-hydroxy-4-aminoadamantane.

Abstract: Provided are crystalline forms of O-desmethylvenlafaxine fumarate, methods for their preparation, and pharmaceutical composition thereof.

Abstract: A process for preparing N-[(1R)-1-(1-naphthyl)ethyl]-3-[3-(trifluoromethyl)-phenyl]propan-1-amine of formula (I) i.e. Cinacalcet and its intermediates of formulae (V), (Va) and (Vb).

Abstract: A compound of formula V or formula VI for use in the treatment of a demyelinating peripheral neuropathy: wherein X is O, S, SO or SO2, R1 is halogen, trihalomethyl, OH, C1-7alkyl, C1-4alkoxy, trifluoromethoxy, phenoxy, cyclohexylmethyloxy, pyridylmethoxy, cinnamyloxy, naphthylmethoxy, phenoxymethyl, CH2—OH, CH2—CH2—OH, C1-4alkylthio, C1-4alkylsulfinyl, C1-4alkylsulfonyl, benzylthio, acetyl, nitro or cyano, or phenyl, phenylC1-4alkyl or phenyl-C1-4alkoxy each phenyl group thereof being optionally substituted by halogen, CF3, C1-4alkyl or C1-4alkoxy; R2 is H, halogen, trihalomethyl, C1-4alkoxy, C1-7alkyl, phenethyl or benzyloxy; R3 is H, halogen, CF3, OH, C1-7alkyl, C1-4alkoxy, benzyloxy, phenyl or CMalkoxymethyl; each of R4 and R5, independently is H or a residue of formula (a), wherein each of R8 and R9, independently, is H or C1-4alkyl optionally substituted by halogen; and n is an integer from 1 to 4; and the N-oxide derivatives thereof or prodrugs thereof, or a pharmaceutically acceptable salt, solvate or

Abstract: The present invention relates to a process for the preparation of (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl(1S,2R)-3-[[(4-aminophenyl)sulfonyl](isobutyl)amino]-1-benzyl-2-hydroxypropylcarbamate as well as novel intermediates for use in said process. (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl(1S,2R)-3-[[(4-aminophenyl)sulfonyl](isobutyl)amino]-1-benzyl-2-hydroxypropylcarbamate is particularly useful as an HIV protease inhibitor.

Abstract: A new class of compounds, namely diamino alcohols, is described, along with a process for their production and their use as dispersing additives for coating formulations.

Abstract: The present invention relates to pharmaceutical compositions comprising a 2-amino-2-[2-(4-C2-20-alkyl-phenyl)ethyl]propane-1,3-diol compound or a pharmaceutically acceptable salt thereof, and to the use thereof for treating, preventing or delaying the progression of multiple sclerosis in a pediatric patient or a patient suffering from a specific condition.

Abstract: Disclosed is a method for maintaining induced remission of an immune disease, which can alleviate or reduce any serious side effect and the burdens exerted on a patient suffering from the same. The method comprises carrying out the remission induction for an immune disease by the use of a biological agent or a nucleic acid synthesis-inhibitory agent and then using an agonist for sphingosine-1-phosphate receptor to the patient.

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

Abstract: The present invention pertains to a process for preparing a compound of Formula I that is achiral, racemic or enantiomerically enriched at the hydroxylation center indicated by * comprising contacting a compound of Formula II with an oxidant selected from oxygen, hydrogen peroxide, peracids or alkyl hydroperoxides in the presence of a zirconium complex, wherein R1, R2 and R3 are as defined in the disclosure. This invention also pertains to zirconium complexes useful in this procedure comprising zirconium and a ligand of Formula III or its enantiomer wherein J, R6 and n are as defined in the disclosure. This invention further pertains to a compound of Formula III or its enantiomer.

Abstract: The invention provides three polymorphic forms of crystalline levosalbutamol sulphate designated herein as Forms I, II and III. Crystalline levosalbutamol sulphate Form I is characterised by a powder XRD pattern with peaks at 10.8, 11.9, 13.0, 18.3, 28.5±0.2 degrees 2 theta. Crystalline levosalbutamol sulphate Form II is characterised by a powder XRD pattern with peaks at 8.7, 9.6, 15.2, 15.7, 19.1, 27.2, 30.7±0.2 degrees 2 theta. Crystalline levosalbutamol sulphate Form III is characterised by a powder XRD pattern with peaks at 5.5, 6.9, 7.3, 18.7±0.2 degrees 2 theta. Processes for making the new polymorphic forms and pharmaceutical compositions comprising them are also provided.

Abstract: The invention is concerned with novel hexafluoroisopropanol derivatives of formula (I) wherein R1 to R6, m and n are as defined in the description and in the claims, as well as physiologically acceptable salts and esters thereof. These compounds bind to LXR alpha and LXR beta and can be used as medicaments.

Abstract: The present invention relates to solid forms of (±)-O-desmethylvenlafaxine salts, processes for preparation, pharmaceutical compositions, and method of treating thereof. More particularly, the present invention provides solid forms of acid addition salts of (±)-O-desmethylvenlafaxine wherein the acid counter ion is provided by an acid selected from the group consisting of oxalic acid, benzoic acid and lactic acid.

Abstract: A process is disclosed for the preparation of a compound of formula and/or an addition salt of a proton acid, wherein R1 and R2 independently represent alkyl, cycloalkyl, aryl or aralkyl, each aryl or aralkyl being optionally further substituted with alkyl, alkoxy and/or halogen. The process involves reacting a mixture comprising a methyl ketone of formula and a compound of formula H2N—R2 (V) and/or an addition salt of proton acid, and formaldehyde in the presence of a solvent selected from the group consisting of water, aliphatic alcohols, cycloaliphatic alcohols and mixtures thereof, and optionally a proton acid to afford a ?-amino ketone of formula and/or an addition salt of a proton acid, and reducing the carbonyl group of said ?-amino ketone to afford a compound of formula I, and/or an addition salt of a proton acid wherein the first step is carried out at a pressure above 1.5 bar.

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: Aspects of the invention relate to substituted aryl propylamino-oxy-analogs and uses thereof. Aspects of the invention relate to compositions that are inhibitors of ?-secretase and uses thereof for treating subjects having, or at risk of developing, Alzheimer's disease.

Abstract: Provided are novel compositions and analogs which are useful in a number of applications, indications and diseases, as well as for monitoring pharmakinetics and patient management. These compounds and analogs are applicable to treating tumors of the central nervous system, e.g., glioblastoma (GBM).

Abstract: The invention provides a novel process, novel process steps and novel intermediates useful in the synthesis of pharmaceutically active compounds, especially renin inhibitors, such as Allskiren. Inter alia, the invention provides a process for the manufacture of a compound of the formula III, wherein R, R1, R2, R3 and PG are as defined in the specification, or a salt thereof. The manufacture comprises (preferably consists of) reacting a compound of the formula I, with a reagent able to transform hydroxy into X where X is for example a leaving group.

Abstract: Compounds of formula in free or salt or solvate form, where Ar is a group of formula Y is carbon or nitrogen and R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, X, n, p, q and r are as defined in the specification, their preparation and their use as pharmaceuticals, particularly for the treatment of obstructive or inflammatory airways diseases.

Abstract: A process for the industrial production of 2-amino-2-[2-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]ethyl]-1,3-propanediol hydrochloride (Compound I), an effective immunosuppressant. The process for producing 2-amino-2-[2-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]ethyl]-1,3-propanediol hydrochloride or a hydrate thereof includes the steps of reacting 4-(3-benzyloxyphenylthio)-2-chlorobenzaldehyde with ethyl diethylphosphonoacetate in a solvent in the presence of a base to form ethyl 3-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]acrylate; reducing the resulting ethyl 3-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]acrylate, followed by mesylation, iodination and nitration, to form 1-benzyloxy-3-[3-chloro-4-(3-nitropropyl)phenylthio]benzene; forming 2-[2-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]ethyl]-2-nitro-1,3-propanediol using a formaldehyde solution; and reducing the resulting 2-[2-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]ethyl]-2-nitro-1,3-propanediol to form the desired product.

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

Abstract: Processes for preparing desvenlafaxine and stable amorphous O-desmethylvenlafaxine succinate solid dispersions with one or more pharmaceutically acceptable carriers.

Abstract: An amino alcohol derivative represented by the following general formula (1) (for example, (±)-2-amino-5-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]-2-methylpentane-1-ol) exhibits strong immunosuppressive effect while causing less side effects: .

Abstract: Provided is a novel amine compound represented by the following formula (I) having a superior peripheral blood lymphocyte decreasing action and superior in the immunosuppressive action, rejection suppressive action and the like, which shows decreased side effects of, for example, bradycardia and the like, or a pharmaceutically acceptable acid addition salt thereof, or a hydrate thereof, or a solvate thereof. wherein each symbol is as defined in the specification.

Abstract: The invention relates to amine compounds as well as methods and materials involved in modulating neurotransmitter reuptake. Specifically, the invention provides amine compounds, methods for synthesizing amine compounds, and methods for inhibiting neurotransmitter reuptake.

Abstract: S1P receptor modulators or agonists are administered following a dosage regimen whereby during the initial days of treatment the daily dosage is lower than the standard daily dosage

Abstract: The present invention pertains to a process for preparing a compound of Formula I that is achiral, racemic or enantiomerically enriched at the hydroxylation center indicated by * comprising contacting a compound of Formula II with an oxidant selected from oxygen, hydrogen peroxide, peracids or alkyl hydroperoxides in the presence of a zirconium complex, wherein R1, R2 and R3 are as defined in the disclosure. This invention also pertains to zirconium complexes useful in this procedure comprising zirconium and a ligand of Formula III or its enantiomer wherein J, R6 and n are as defined in the disclosure. This invention further pertains to a compound of Formula III or its enantiomer.

Abstract: Provided are compounds, pharmaceutical compositions thereof, and methods of treating ophthalmic diseases and disorders, such as age-related macular degeneration and Stargardt's Disease, using said compounds and compositions.

Abstract: Disclosed are intermediates and processes for preparing epoxides of the formula: where R and PROT are defined herein. These epoxides are useful as intermediates in the production of biologically active compounds, i.e., in the production of pharmaceutical agents.

Abstract: The present invention relates to a process for the preparation of (1R,2R)-3-dimethylamino-1-ethyl-2-methyl-propyl)-phenol.

Abstract: The invention provides methods and compounds for the treatment of neurological disorders, including Alzheimer's disease, Parkinson's disease, Huntington's disease, ALS (Amyotrophic Lateral Sclerosis), traumatic brain injury, ischemic brain injury or a stroke. In one aspect the compounds are HDAC1 activators. Exemplary HDAC1 activators include metal chelators, iron chelators, deferoxamin, flavonoids, compounds comprising a catechol moity, ginkgetin K, Chembridge 5104434, sciadopilysin, tetrahydrogamboic acid, TAM-11, LY 235959, CGS 19755, SK&F 97541, etidronic acid, levonordefrin, methyldopa, ampicillin trihydrate, D-aspartic acid, gamma-D-glutamylaminomethylsulfonic acid, phenazopyridine to hydrochloride, oxalamine citrate salt, podophyllotoxin, SK&F 97541, (+-)-4-amino-3-(5-chloro-2-thienyl)-butanoic acid, (RS)-(tetrazol-5-yl) glycine, R(+)-SKF-81297, gambogic acid, and derivatives thereof.

Abstract: Optically active bisoxazoline compounds represented by the general formula (1), a process for producing the compounds, and a process for producing cyclopropanecarboxylic esters by using the same: wherein R1 and R2 are the same and each represents C1-6 alkyl, substituted or unsubstituted aralkyl, or substituted or unsubstituted phenyl or R1 and R2 are bonded each other together with the carbon atom of oxazoline ring to which they are bonded to form a ring; R3 is substituted or unsubstituted naphthyl; R4 and R5 are the same and each represent hydrogen or C1-6 alkyl, or R4 and R5 are bonded each other together with the carbon atom to which they are bonded to form a cycloalkyl ring having 3 to 6 carbon atoms; and * represents an asymmetric center.

Abstract: The present invention is directed to arylamino-arylpropanolamine derivatives of formula I: or a pharmaceutically acceptable salt thereof, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions ameliorated by monoamine reuptake including, inter alia, vasomotor symptoms (VMS), sexual dysfunction, gastrointestinal and genitourinary disorders, chronic fatigue syndrome, fibromyalgia syndrome, nervous system disorders, and combinations thereof, particularly those conditions selected from the group consisting of major depressive disorder, vasomotor symptoms, stress and urge urinary incontinence, fibromyalgia, pain, diabetic neuropathy, and combinations thereof.

Abstract: Provided are novel compositions which uniquely inhibit sphingosine kinase Type 1 (SphK1) and which are useful in a number of applications including killing or damaging cancer cells, inducing apoptosis, inhibiting growth, metastasis and development of chemoresistance in cancer cells, leukemia, increasing the effectiveness of anti-cancer agents, attenuating immune reactivity, inhibiting survival signaling in cancer cells, and reducing symptoms of multiple sclerosis.

Abstract: Novel calcilytic compounds of Formula (I), pharmaceutical compositions, methods of synthesis, and methods of using them are provided.

Abstract: 1R,2S-Methoxamine may be used topically for effective treatment of faecal incontinence at low doses without local or systemic side effects, for example, without affecting blood pressure. 1R,2S-Methoxamine may be used to treat other disturbances and disorders of the gastrointestinal, as a pressor agent, as a nasal decongestant and in ophthalmology, at low does and without significant side effects.

Abstract: The present invention relates to an improved process for the preparation of 3-[(1R,2R)-3-(dimethylamino)-1-ethyl-2-methylpropyl]phenol monohydrochloride.

Abstract: Certain ethanolamine analogs and related compounds useful in the control of nematodes that infest plants or the situs of plants are described.

Abstract: The invention provides a novel immobilized Lewis acid catalyst which exhibits high catalytic activity in an aqueous solution and which permits recovery and reuse or long-term continuous use. The invention relates to an immobilized Lewis acid catalyst comprising a solid substance and a Lewis acid supported on the surface of the solid substance by chemical bonding, wherein the surface of the solid substance and the peripheries of the Lewis acid are coated with an ionic liquid, more specifically, an immobilized Lewis acid catalyst comprising a solid substance such as silica gel or an organic polymer and a Lewis acid stable even in water which is supported on the surface of the solid substance by chemical bonding, wherein the surface of the solid substance and the peripheries of the Lewis acid are completely or partially coated with a hydrophobic ionic liquid; a process for the production of the catalyst; use thereof; and a process for the preparation of compounds with the catalyst.

Abstract: The present invention relates to an improved process for the preparation of (2R,3R)-3-(3-methoxyphenyl)-N,N,2-trimethylpentanamine which is an intermediate for the preparation of the analgesic tapentadol.

Abstract: Methods for preparing substantially pure O-desmethylvenlafaxine are described.

Abstract: Pharmaceutical compositions comprising phenylephrine or a pharmaceutically acceptable salt thereof and methods for administering the pharmaceutical compositions wherein the composition is formulated for systemic absorption of phenylephrine that avoids first pass metabolism. The compositions of the invention are formulated to be applied to oral mucosa of an animal to allow for enhanced systemic delivery of therapeutically active form of phenylephrine.

Abstract: Compounds of formula I wherein R1, R2, R3, R4 and R5 are as defined in the specification, processes for their production, their uses and pharmaceutical compositions containing them.

Abstract: Drug substances comprising a pharmaceutically acceptable organic acid addition salt of amine containing pharmaceutically active compounds useful for the treatment of a therapeutic ailment administration and exhibiting prophylactic properties when employed in non-therapeutic administration.