Abstract: Disclosed are methods for forming a supported catalyst and catalysts formed according to disclosed methods. Methods include contacting a catalyst support with a precursor solution and displacing the solvent of the precursor solution (e.g., water) with a second solvent that has a lower surface tension than the first solvent. The second solvent displaces the first solution according to the Marangoni effect. Methods also include activation of the precursor to form a catalyst, e.g., a supported platinum group metal catalyst or the like.

Abstract: The present invention relates to a method of treating patients who undergo hematopoietic stem cell transplantation (HSCT) with peripheral blood mobilized stem cells for hematological malignancies and for whom the risk for severe acute graft versus host disease (GVHD) is considerable.

Abstract: Chemical syntheses and medical uses of novel inhibitors of the uptake of monoamine neurotransmitters and pharmaceutically acceptable salts and prodrugs thereof, for the treatment and/or management of psychotropic disorders, anxiety disorder, generalized anxiety disorder, depression, post-traumatic stress disorder, obsessive-compulsive disorder, panic disorder, hot flashes, senile dementia, migraine, hepatopulmonary syndrome, chronic pain, nociceptive pain, neuropathic pain, painful diabetic retinopathy, bipolar depression, obstructive sleep apnea, psychiatric disorders, premenstrual dysphoric disorder, social phobia, social anxiety disorder, urinary incontinence, anorexia, bulimia nervosa, obesity, ischemia, head injury, calcium overload in brain cells, drug dependence, attention deficit hyperactivity disorder, fibromyalgia, irritable bowel syndrome, and/or premature ejaculation are described.

Abstract: The present invention provides a method for treating, alleviating, reversing or delaying progression of at least one symptom of Parkinson's Disease in a subject in need thereof by administering to the subject an effective amount of a 2-amino-2[2-(4-octylphenyl)ethyl]propane-1,3-diol composition or a derivative thereof to treat at least one symptom of Parkinson's Disease.

Abstract: The invention relates to novel cyclohexylamine derivatives and their use in the treatment and/or prevention of central nervous system (CNS) disorders, such as depression, anxiety, schizophrenia and sleep disorder as well as methods for their synthesis. The invention also relates to pharmaceutical compositions containing the compounds of the invention, as well as methods of inhibiting reuptake of endogenous monoamines, such as dopamine, serotonin and norepinephrine from the synaptic cleft and methods of modulating one or more monoamine transporter.

Abstract: A library of macrocyclic compounds of the formula (I) where part (A) is a ?bivalent radical, a —(CH2)y— bivalent radical or a covalent bond; where part (B) is a ?bivalent radical, a —(CH2)z— bivalent radical, or a covalent bond; where part (C) is a ?bivalent radical, a —(CH2)t— bivalent radical, or a covalent bond; and where part (T) is a —Y-L-Z— radical wherein Y is CH2 or CO, Z is NH or O and L is a bivalent radical. These compounds are useful for carrying out screening assays or as intermediates for the synthesis of other compounds of pharmaceutical interest. A process for the preparation of these compounds in a combinatorial manner, is also disclosed.

Abstract: The present invention relates to a compound of formula A, wherein R is alkyl. Compound A may be used as an intermediate in the preparation of O-desmethyl venlafaxine or a salt thereof, and the present invention provides such a preparation, as well as a process for preparing the compound of formula A.

Abstract: The present invention discloses polymorphic forms of O-desmethyl-venlafaxine succinate and processes for the preparation thereof.

Abstract: Provided is a ruthenium complex that is represented by general formula (1*) and is useful as an asymmetric reduction catalyst. (In the formula, * is an asymmetric carbon atom; R1 is an arenesulfonyl group, and the like; R2 and R3 are a phenyl group, and the like; R10 through R14 are selected from a hydrogen atom, C1-10 alkyl group, and the like, but R10 through R14 are not simultaneously hydrogen atoms; X is a halogen atom and the like; j and k are each either 0 or 1; and j+k is 0 or 2.

Abstract: One aspect of the invention relates to a method of animation or amidation, comprising the step of combining a substrate, comprising a reactive C—H bond, and an amine or amide, comprising a reactive N—H bond, in the presence of an oxidizing agent and a metal-containing catalyst, thereby forming a product with a covalent bond between the carbon of the reactive C—H bond and the nitrogen of the reactive N—H bond.

Abstract: Photoactive compositions of matter, methods for their design and synthesis, and various applications of such compositions of matter are disclosed. Such photoactive compositions may, for example, include any one or more of the following: a core moiety; a primary electron donor moiety; an electron-withdrawing moiety; and an alkyl tail. Some photoactive compositions may further include multiple additional electron donor moieties, electron-withdrawing moieties, and alkyl tails. Applications of such photoactive compositions of matter may include use in photovoltaic cells (e.g., as a p- or n-type material of the active layer of some photovoltaic cells, or as a dye to be employed in other photovoltaic cells); batteries, field-effect transistors; and light-emitting diodes.

Abstract: Disclosed herein is an improved process for the preparation of 3-[(2R,3R)-1-(dimethylamino)-2-methylpentan-3-yl]phenol of Formula-I and its pharmaceutically acceptable salt which comprises the reaction of (S)-1-(dimethylamino)-2-methylpentan-3-one of formula VIII with 3-bromo anisole of formula II under Grignard conditions to get the compound (2S,3R)-1-(dimethylamino)-3-(3-methoxyphenyl)-2-methyl pentan-3-ol of formula V followed by activation of the —OH group of the formula V to convert into sulfonate esters of formula IX, which are on reductive deoxygenation to yield (2R,3R)-3-(3-methoxyphenyl)-N,N,2-trimethylpentan-1-amine of formula VII and demethylation of formula VII to obtain the compound 3-[(2R,3R)-1-(dimethylamino)-2-methylpentan-3-yl]phenol of Formula-1.

Abstract: According to the present invention, a liquid phenol resin that has excellent characteristics of a phenol resin, such as thermal resistance and hardenability, and can produce a molded product having excellent flexibility, and a method of preparing the resin are provided. The present invention relates to a liquid phenol resin obtained by reacting (A) oils and (B) phenols with (C) a secondary and/or a tertiary alkylamine compound, wherein a nitrogen content based on the whole liquid phenol resin is 3% by weight to 30% by weight, and (A):(B)=10:90 to 90:10.

Abstract: A tau aggregation inhibitor reduces tau aggregation in cells. The tau aggregation inhibitor can include a catechol structure-containing compound or a salt thereof, and the catechol structure-containing compound can be one of isoprenaline, dopamine, dobutamine, levodopa, levodopa/carbidopa, trimetoquinol, hexoprenaline, methyldopa, and droxidopa. One example of the catechol structure-containing compound is isoprenaline, which can be d-enantiomer of isoprenaline or d/l-racemic mixture of isoprenaline. Tauopathies to be prevented or treated by the inhibitor include AD, Down's syndrome, Pick's disease, corticobasal degeneration, and progressive supranuclear palsy.

Abstract: The present disclosure relates to polymorphs of 4-[2-dimethylamino-1-(1-hydroxycyclohexyl)ethyl]phenyl 4-methylbenzoate hydrochloride, methods for preparing the same and use of the same.

Abstract: Multifunctional compounds are provided, comprising two or more functional moieties selected from: (i) a moiety that imparts an iron chelator function; (ii) a moiety that imparts a neuroprotective function; (iii) a moiety that imparts combined antiapoptotic, neuroprotective and/or neurorestorative functions; (iv) a moiety that imparts brain MAO inhibition, preferably with little or no MAO inhibition in liver and small intestine; (v) a moiety that imparts cholinesterase inhibitory function; and (vi) a moiety that imparts an N-methyl-D-aspartic acid receptor (NMDAR) inhibition, and pharmaceutically acceptable salts and optical isomers thereof. The multifunctional compounds are useful in the treatment or prevention of diseases, disorders or conditions that can be prevented and/or treated by iron chelation therapy, and/or neuroprotection and/or neurorestoration, and/or apoptosis inhibition and/or MAO inhibition and/or cholinesterase inhibition and/or NMADR inhibition.

Abstract: The invention deals with new salts of the desvenlafaxine base of formula (I) with oxalic acid, the new salts being the hydrogen oxalate of formula (II) in the proportion of desvenlafaxine:oxalic acid of 1:1 and hemioxalate of formula (III) in the proportion of desvenlafaxine:oxalic acid of 2:1.

Abstract: Antiproliferative compounds having a structure represented by formula (II), where n, R1, R2, R3, R4, and R5 are as defined herein, can be used to treat tumors, optionally when conjugated to a ligand such as an antibody:

Abstract: The present invention provides processes and intermediates for preparing cinacalcet base and pharmaceutically acceptable salts thereof.

Abstract: The present invention relates to a novel process for the preparation of O-desmethyl venlafaxine (ODV) and the pharmaceutically acceptable salts thereof, wherein it comprises (i) provision of spiro-venlafaxine compound as intermediate; (ii) conversion of spiro-venlafaxine intermediate into ODV free base in a one-pot process; and (iii) optionally conversion ODV free base into pharmaceutically acceptable salts. The present invention further relates to novel processes for the preparation of crystalline salts of ODV-succinate and ODV-oxalate.

Abstract: The invention describes antibodies that bind venlafaxine and O-desmethylvenlafaxine. The antibodies are derived from novel haptens and immunogens and are used in methods and kits to detect and quantify venlafaxine and O-desmethylvenlafaxine. The invention also describes novel detecting agents which can be used in the methods and kits of the invention.

Abstract: The present invention refers to a new process for the synthesis of tapentadol comprising the quantitative resolution of the racemic mixture (V) to obtain the stereoisomer of (S)-3-(dimethylamino)-2-methyl-1-(3-nitrophenyl)-propan-1-one (VII) according to the Scheme 2 below using the (2R,3R)—O,O?-dibenzoyltartaric chiral acid wherein said resolution is quantitative. The present invention also refers to some intermediate compounds of the new synthesis process of tapentadol.

Abstract: Compounds having a diphenylmethane skeleton are superior in broad utility and stability, and are useful as a protecting reagent (anchor) of amino acid and/or peptide in the liquid phase synthesis and the like of a peptide having a C-terminal etc., which are of a carboxamide(-CONHR)-type, and in organic synthetic reaction methods (particularly peptide liquid phase synthetic methods), and may be contained in a kit for peptide liquid phase synthesis.

Abstract: Provided are compounds, methods and kits for identifying in cells of interest organelles including nuclei and a wide variety of organelles other than nuclei (non-nuclear organelles), as well as cell regions or cell domains. These compounds and methods can be used with other conventional detection reagents for identifying the location or position or quantity of organelles and even for distinguishing between organelles in cells of interest.

Abstract: The invention is directed to a process for producing intermediates of a compound which exhibits an activated blood coagulation factor Xa inhibitory action and which is a useful preventive and a therapeutic agent for thrombotic diseases. The intermediate production process is represented by the following reaction scheme.

Abstract: This invention relates to certain ceramide-analogues of FTY720 (2-amino-2-[2-(4-octylphenyl)ethyl]propane-1,3-diol; fingolimod). In particular, the present invention relates to pharmaceutical compositions comprising these compounds, as well as processes for their preparation and their use in the treatment of autoimmune conditions, such as multiple sclerosis.

Abstract: A controlled release dosage form of venlafaxine that comprises an immediate release pellet and an extended release pellet.

Abstract: Provided is a ruthenium complex that is represented by general formula (1*) and is useful as an asymmetric reduction catalyst. (In the formula, * is an asymmetric carbon atom; R1 is an arenesulfonyl group, and the like; R2 and R3 are a phenyl group, and the like; R10 through R14 are selected from a hydrogen atom, C1-10 alkyl group, and the like, but R10 through R14 are not simultaneously hydrogen atoms; X is a halogen atom and the like; j and k are each either 0 or 1; and j+k is 0 or 2.

Abstract: The present invention relates to processes for the preparation of 4-hydroxy-??-[[[6-(4-phenylbutoxy)hexyl]amino]methyl]-1,3-benzenedimethanol 1-hydroxy-2-naphthoate (salmeterol xinafoate) (12a), the preparation of 4-hydroxy-??-[[[6-(4-phenylbutoxy)hexyl]amino]methyl]-1,3-benzenedimethanol (salmeterol) (11), the preparation of protected N-[6-(4-phenylbutoxy)hexyl]amine intermediates (7), and the preparation of 6-substituted (4-phenylbutoxy)hexane intermediates (5), shown below, wherein X is a leaving group and Pg is a protecting group.

Abstract: Methods of preparing, and compositions comprising, derivatives of (?)-venlafaxine are disclosed. Also disclosed are methods of treating and preventing diseases and disorders including, but not limited to, affective disorders such as depression, bipolar and manic disorders, attention deficit disorder, attention deficit disorder with hyperactivity, Parkinson's disease, epilepsy, cerebral function disorders, obesity and weight gain, incontinence, dementia and related disorders.

Abstract: Disclosed is a method of making a 2-substituted-1,4-benzenediamine by nucleophilic aromatic substitution.

Abstract: There is described a process for the preparation of cinacalcet hydrochloride (I) which includes the steps of: a) reacting (R)-(+)-1-(1-naphthyl)ethylamine (II) with 3-[3-(trifluoromethyl)phenyl]propenaldehyde (III) to afford the non isolated intermediate (R)—N-[3-[3-(trifluoromethyl)phenyl]-2-propenylimino-N-[1-(1-naphthyl)ethylamine (IV); b) reducing the non isolated intermediate (R)—N-[3-[3-(trifluoromethyl)phenyl]-2-propenylimino-N-[-1-(1-naphthyl)ethylamine (IV) with a sequential addition of:—a solution of sodium borohydride, methanol and a base,—oxalic acid and—a base to obtain (R)—N-[3-[3-(tifluoromethyl)phenyl]-2-propenyl]-1-(1-naphthyl)ethylamine (V) by passing through the precipitation of the oxalate salt of compound (V) after the addition of oxalic acid; c) hydrogenating (R)—N-[3-[3-(trifluoromethyl)phenyl]-2-propenyl]-1-(1-naphthyl)ethylamine (V) thus obtaining (R)—N-(3-(3-(trifluoromethyl)phenyl]propyl]-1-(1-naphthyl)ethylamine cinacalcet base (VI), which is retaken in ethyl acetate; and d) treati

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: The present invention describes a novel process for the preparation of optically active (S)-(?)-2-(N-propylamino)-5-methoxytetraline and (S)-(?)-2-(N-propylamino)-5-hydroxytetraline compounds based on the optical resolution of mixtures of the enantiomers of 2-(N-propylamino)-5-methoxytetraline and 2-(N-propylamino)-5-hydroxytetraline respectively. This process comprises (a) reacting a mixture of the enantiomers of said compounds with an optically active organic acid to form diastereoisomeric salts and separating the salts by crystallization. Said compounds are useful in the preparation of (6S)-(?)-5,6,7,8-tetrahydro-6-[propyl-(2-thienyl)ethyl]amino-1-naphthol (Rotigotine). Rotigotine is a dopamine agonist and is indicated for the treatment of Parkinson's disease.

Abstract: A pharmaceutical composition comprising a drug substance consisting essentially of a pharmaceutically acceptable organic acid addition salt of an amine containing pharmaceutically active compound wherein the amine containing pharmaceutical active compound is selected from the group consisting of racemic or single isomer ritalinic acid or phenethylamine derivatives and the drug substance has a physical form selected from amorphous and polymorphic.

Abstract: There is provided a process for preparing a salt of the (R)- or (S)-isomer of 1-naphthylethylamine with mandelic acid or a derivative thereof, the process comprising reacting racemic 1-naphthylethylamine with mandelic acid or a derivative thereof to obtain the (R)- or (S)-isomer of 1-naphthylethylamine salt (III) with the acid. The salts also form an aspect of the present invention. There is also provided a salt of the (R)- or (S)-isomer of 1-naphthylethylamine with mandelic acid or a derivative thereof. There is also provided a process for preparing cinacalcet (I) or a salt thereof, the process comprising reacting an ester (II) with (R)-1-naphthylethylamine or a salt of (R)-1-naphthylethylamine and mandelic acid or a derivative thereof, to obtain cinacalcet, and optionally converting the cincalcet to a salt thereof.

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

Abstract: The present invention discloses both amine compositions and amine-epoxy compositions containing N,N?-dimethyl-meta-xylylenediamine. A novel process for producing amines such as N,N?-dimethyl-meta-xylylenediamine, and structurally similar amines, is also disclosed.

Abstract: The present invention discloses compounds of formula (I), their optical isomers or pharmaceutically acceptable salts thereof, their preparation and uses thereof, wherein the definitions of R1, R2, R3 and R4 are shown in the description. These compounds are optical isomers or racemic mixtures. After these compounds are uptaken, they are metabolically transformated in vivo into 1-[2-dimethylamino-1-(4-hydroxyphenyl)-ethyl]-cyclohexanol that has neuropharmacological activity, by interrupting reuptake of 5-hydroxytryptamine (5-HT) and/or norepinephrine (NA), which is used for treating diseases associated with central nerve system, such as depression, etc.

Abstract: The present invention provides processes and intermediates for the preparation of 3-benzazepines and salts thereof which can be useful as serotonin (5-HT) receptor agonists for the treatment of, for example, central nervous system disorders such as obesity.

Abstract: The present invention relates to a method of enantioselective addition to imines, including: reacting R3CH?NY with R4ZnR5 in the presence of a compound represented by the following formula (I), in which Y, R1, R2, R3, R4 and R5 are defined the same as the specification. Accordingly, the present invention can prepare secondary amines in high yields and enantiomeric excess by the above-mentioned method.

Abstract: Aromatic amines which have been obtained by reduction of aromatic nitro compounds are purified by mixing the crude amine obtained after phase separation with an aqueous, alkali metal hydroxide solution and subsequent distillation of this mixture over a distillation column. The distillation column has at least an upper and a lower rectifying part and a stripping part. The bottom product of the distillation column is partly to completely sluiced out and is partly evaporated in a main evaporator and at least one downstream re-evaporator and partly recycled back into the column.

Abstract: Resolution of the title compound to its active isomer (R)-1-(3-hydroxyphenyl)-2-methylamino ethanol with (R)-naproxen as a resolving agent.

Abstract: Process for the preparation of 2,2-difluoroethylamine of the formula (I) CHF2CH2NH2??(I) comprising the stages (i) and (ii): stage (i): reaction of 2,2-difluoro-1-haloethane of the general formula (II) CHF2—CH2Hal??(II), with a benzylamine compound of the formula (III) in the presence of an acid scavenger, in which, in formula (II), Hal is chlorine, bromine or iodine, and, in the formulae (III), R1 is hydrogen or C1-C12-alkyl, and R2 is hydrogen, halogen, C1-C12-alkyl or C1-C6-alkoxy; stage (ii): catalytic hydrogenation of the N-benzyl-2,2-difluoroethanamine compound obtained in the stage (i) to give 2,2-difluoroethylamine of the formula (I) or a salt thereof.

Abstract: According to the present invention, a liquid phenol resin that has excellent characteristics of a phenol resin, such as thermal resistance and hardenability, and can produce a molded product having excellent flexibility, and a method of preparing the resin are provided. The present invention relates to a liquid phenol resin obtained by reacting (A) oils and (B) phenols with (C) a secondary and/or a tertiary alkylamine compound, wherein a nitrogen content based on the whole liquid phenol resin is 3% by weight to 30% by weight, and (A):(B)=10:90 to 90:10.

Abstract: The present invention provides pharmaceutical compositions, which are useful for treatment of depression and the like, and which comprises a compound having an adenosine A2A receptor antagonistic activity such as (E)-8-(3,4-dimethoxystyryl)-1,3-diethyl-7-methyl-3,7-dihydro-1H-purine-2,6-dione or a pharmaceutically acceptable salt thereof and an antidepressant drug (for example, a tricyclic antidepressant, a tetracyclic antidepressant, a selective serotonin reuptake inhibitor, a selective noradrenalin reuptake inhibitor, a dopamine reuptake inhibitor, a serotonin-noradrenalin reuptake inhibitor, monoamine oxidase inhibitor, a 5-HT2 antagonist or the like), and the like.

Abstract: The present invention is related to the preparation and pharmaceutical use of novel haloallylamine derivatives as SSAO/VAP-1 inhibitors having the structure of Formula I, as defined in the specification: (I). The invention also relates to methods of using invention compounds, or pharmaceutically acceptable salt or derivatives thereof, for the treatment of a variety of indications, e.g., inflammatory diseases.

Abstract: The present invention is directed to methods and compositions for making and using a new polymorph of cinacalcet hydrochloride.

Abstract: A process for preparing amines of the formula I, by reacting a carbonyl compound of the formula II with an amine of the formula III where R1 and R2 are different and are each an organic radical which has from 1 to 20 carbon atoms and may optionally also comprise heteroatoms, R3 is a C1-C6-alkyl group and R4 is an aryl group which may be partly or fully halogenated and/or may bear from one to three radicals from the group of cyano, nitro, C1-C6-alkyl, C1-C6-haloalkyl, hydroxyl, C1-C6-hydroxyalkyl, C1-C6-alkoxy, C1-C6-haloalkoxy, hydroxycarbonyl, C1-C6-alkoxycarbonyl, C1-C6-alkylamino, di(C1-C6-alkyl)amino, aryl and aryl(C1-C6-alkyl); and * represents the S or R configuration, and ** represents the S and/or R configuration; which comprises performing the reaction in the presence of a heterogeneous imination catalyst, of a hydrogenation catalyst and of hydrogen.

Abstract: The use of polycyclic phenolic compounds which have up to 20 benzene rings per molecule and are obtainable by reacting a tetrahydrobenzoxazine I where R1 is a hydrocarbyl radical and R2, R3, R4 and R5 are each independently hydrogen atoms, hydroxyl groups or hydrocarbyl radicals with one or more of the same or different phenols II where R7, R8, R9 and R10 are each independently hydrogen atoms, hydroxyl groups or hydrocarbyl radicals, and/or with one or more of the same or different tetrahydrobenzoxazines I, with the proviso that at least one of the substituents has from 13 to 3000 carbon atoms and the remaining substituents, when they are hydrocarbyl radicals, have in each case from 1 to 20 carbon atoms as stabilizers for stabilizing inanimate organic material against the action of light, oxygen and heat.