Abstract: A series of novel compounds showing anticonvulsant, chemical countermeasure(s), and analgesic activities is described. Such pharmaceutically active compounds may also show utility in the treatment of other central nervous system (“CNS”) diseases and disorders, such as anxiety, depression, insomnia, migraine headaches, schizophrenia, Parkinson's disease, spasticity, Alzheimer's disease, and bipolar disorder. Furthermore, such compounds may additionally find utility as analgesics (e.g., for the treatment of chronic or neuropathic pain) and as neuroprotective agents useful in the treatment of stroke(s), chronic neurodegenerative diseases (such as Alzheimer's disease and Huntington's disease), and/or traumatic brain and/or spinal cord injuries. Moreover, these/such compounds may also be useful in the treatment of status epilepticus and/or as chemical countermeasures.

Abstract: A series of novel compounds showing anticonvulsant activity is described. Such pharmaceutically active compounds may also show utility in the treatment of other central nervous system (“CNS”) diseases and disorders, such as anxiety, depression, insomnia, migraine headaches, schizophrenia, Parkinson's disease, spasticity, Alzheimer's disease, and bipolar disorder. Furthermore, such compounds may additionally find utility as analgesics (e.g., for the treatment of chronic or neuropathic pain) and as neuroprotective agents useful in the treatment of stroke(s), chronic neurodegenerative diseases (such as Alzheimer's disease and Huntington's disease), and/or traumatic brain and/or spinal cord injuries. Moreover, these/such compounds may also be useful in the treatment of status epilepticus and/or as chemical countermeasures.

Abstract: The present invention relates to a para-aminophenol compound of formula (I) the addition salts thereof with an acid and the solvates thereof, dye composition comprising the latter and a dyeing process.

Abstract: The present invention relates to substantially pure metabolites of irara-clomiphene. The invention is also directed to pharmaceutical compositions comprising these metabolites and their use in treating disorders including secondary hypogonadism, type 2 diabetes, elevated cholesterol, elevated triglycerides, wasting, lipodystrophy, female and male infertility, benign prostate hypertrophy, prostate cancer, breast cancer, ovarian cancer and endometrial cancer.

Abstract: The present invention relates to novel substituted phenoxyethylamine derivatives, useful as modulators of cortical and basal ganglia dopaminergic and N-methyl-D-aspartate (NMDA) receptor-mediated glutamatergic neurotransmission. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.

Abstract: The invention provides for a combination comprising an amount of an SSRI, or a pharmaceutically acceptable salt or solvate thereof, and an amount of a GR antagonist, or a pharmaceutically acceptable salt or solvate thereof, optionally in association with one or more pharmaceutically acceptable carriers for use as therapy for depression and related disorders

Abstract: The present disclosure relates to novel cocrystals and novel methods for cocrystallization. In particular, the disclosure includes cocrystals comprising a salt of an active agent, such as a chloride salt of an active pharmaceutical ingredient. The present disclosure also relates to methods of preparing cocrystals and methods for screening for solid state phases.

Abstract: A number of FTY720-derived compounds with antitumor activity are described. These compounds include the compounds of formula I: wherein R1 is independently selected from the group consisting of hydrogen, methyl. methoxy, and hydroxyl; R2 is independently selected from the group consisting of hydrogen, methoxy, and hydroxyl; R3 is independently selected from the group consisting of alkyl and cyclo-alkyl; and n is independently selected from 0 to 6. The compounds have lower immunosuppressive side effects as a result of not being phosphorylated by sphingosine kinase 2.

Abstract: The present invention provides an efficient method for preparing atomoxetine in high yield. (R)-methylhydroxylaminopropanol compound of formula (II) in the present invention is used as an intermediate without the need for resolution processes.

Abstract: A method for preparation of N-methyl-3-(2-tributylstannylphenoxy)-3-phenylpropanamine is provided, which includes formation of N-methyl-3-(2-tributylstannylphenoxy)-3-phenylpropanamine, useful as a precursor of a norepinephrine transporter (NET) contrast label [123Iodine](R)—N-methyl-3-(2-iodophenoxy)-3-phenylpropanamine ([123I]MIPP) with a leaving group Bu3Sn.

Abstract: The present invention relates to nordihydroguaiaretic acid derivative compounds, namely, butane bridge modified nordihydroguaiaretic acid (NDGA) compounds and butane bridge modified tetra-O-substituted NDGA compounds, pharmaceutical compositions containing them, methods of making them, and methods of using them and kits including them for the treatment of diseases and disorders, in particular, diseases resulting from or associated with a virus infection, such as HIV infection, HPV infection, or HSV infection, an inflammatory disease, such as various types of arthritis and inflammatory bowel diseases, metabolic diseases, such as diabetes and hypertension, or a proliferative disease, such as diverse types of cancers.

Abstract: The present disclosure relates to novel cocrystals and novel methods for cocrystallization. In particular, the disclosure includes cocrystals comprising a salt of an active agent, such as a chloride salt of an active pharmaceutical ingredient. The present disclosure also relates to methods of preparing cocrystals and methods for screening for solid state phases.

Abstract: Disclosed are nordihydroguaiaretic acid derivative compounds including various end groups bonded by a carbon atom or heteroatom though a side chain bonded to the respective hydroxy residue O groups by an ether bond or a carbamate bond, pharmaceutical compositions, methods of making them, and methods of using them and kits including them for the treatment of diseases and disorders, in particular, diseases resulting from or associated with a virus infection, such as HIV infection, HPV infection, or HSV infection, an inflammatory disease, such as various types of arthritis and inflammatory bowel diseases, a metabolic disease, such as diabetes, a vascular disease, such as hypertension and macular degeneration, or a proliferative disease, such as diverse types of cancers.

Abstract: Fluorinated compounds and methods of making fluorinated compounds are described herein.

Abstract: The present invention provides an efficient method for preparing atomoxetine in high yield. (R)-methylhydroxylaminopropanol compound of formula (II) in the present invention is used as an intermediate without the need for resolution processes.

Abstract: A method for preparation of N-methyl-3-(2-tributylstannylphenoxy)-3-phenylpropanamine is provided, which includes formation of N-methyl-3-(2-tributylstannylphenoxy)-3-phenylpropanamine, useful as a precursor of a norepinephrine transporter (NET) contrast label [123Iodine](R)—N-methyl-3-(2-iodophenoxy)-3-phenylpropanamine ([123I]MIPP) with a leaving group Bu3Sn.

Abstract: Described herein are methods, compositions and articles of manufacture involving neutral conjugated polymers including methods for synthesis of neutral conjugated water-soluble polymers with linkers along the polymer main chain structure and terminal end capping units. Such polymers may serve in the fabrication of novel optoelectronic devices and in the development of highly efficient biosensors. The invention further relates to the application of these polymers in assay methods.

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, a monoamine oxidase inhibitor, a 5-HT2 antagonist or the like), and the like.

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: A family of polyethylenimine biocides of formula (I): wherein R1 is hydrogen, a branched ethylenimine, a tethered antimicrobial moiety, or a branched ethylenimine having a tethered antimicrobial moiety is described herein. The polyethylenimine biocides may be used in a variety of consumer products, coatings, coating compositions, and medical devices to prevent growth of microorganisms.

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, and/or premature ejaculation are described.

Abstract: The invention provides a thiazole derivative useful as a VAP-1 inhibitor, as well as a pharmaceutical agent for the prophylaxis or treatment of VAP-1 associated diseases and the like, a method of inhibiting VAP-1 in a subject, and a method for the prophylaxis or treatment of VAP-1 associated disease in a subject. The thiazole derivative is a compound represented by the formula (I): R1—NH—X—Y—Z wherein each symbol is as defined in the specification, or a pharmaceutically acceptable salt thereof.

Abstract: Provided herein methods of screening for potential antidepressant compounds effective to increase production of cellular CDP-diacylglycerol and synthesis of inositol phospholipid in depression-related areas of the brain. Also, provided are methods of diagnosing and treating depressive or mood disorders in a subject by administering these screened antidepressant compounds. Further provided is a method of determining the therapeutic efficacy of an antidepressant drug regimen by comparing the ratio of CDP-diacylglycerol/inositol phosphate after treatment to a basal ratio in a subject.

Abstract: The present invention is related to the preparation and pharmaceutical In 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 provides novel crystalline polymorph forms of atomoxetine hydrochloride denominated Forms B and C and methods for their preparation, as well as methods for the preparation of Form A. The present invention provides pharmaceutical compositions that comprise atomoxetine hydrochloride Form B, Form C, or mixtures thereof that can be used to treat attention deficit/hyperactivity disorder.

Abstract: The instant disclosure describes methods for treating diseases and conditions of the central and peripheral nervous system by stimulating or increasing neurogenesis. The disclosure includes compositions and methods based on muscarinic receptor modulation, such as via inhibition of acetylcholine esterase (AChE) activity, alone or in combination with another neurogenic agent to stimulate or activate the formation of new nerve cells.

Abstract: Disclosed are nordihydroguaiaretic acid derivative compounds including various end groups bonded by a carbon atom or heteroatom though a side chain bonded to the respective hydroxy residue O groups by an ether bond or a carbamate bond, pharmaceutical compositions, methods of making them, and methods of using them and kits including them for the treatment of diseases and disorders, in particular, diseases resulting from or associated with a virus infection, such as HIV infection, HPV infection, or HSV infection, an inflammatory disease, such as various types of arthritis and inflammatory bowel diseases, a metabolic disease, such as diabetes, a vascular disease, such as hypertension and macular degeneration, or a proliferative disease, such as diverse types of cancers.

Abstract: A subject matter of the present invention is novel intermediates for the synthesis of (R)-tamsulosin and of its pharmaceutically acceptable salts, and also the associated preparation process.

Abstract: The present invention relates to a novel method for preparing an itopride-hydrochloride mediate of the formula 1, which is useful for digestive tract activator, and more particularly, the present invention provides with a method for preparing 4-[2-(dimethylamino)ethoxy]benzylamine of the formula 1, an itopride-hydrochloride mediate, whereby being capable of manufacturing in a high yield and lowering cost through a simple purification and a selective reaction, and the method is harmless and safe to human and environment due to not generating toxic gas. And specially, a super-high pressure hydrogenation and a reduction reaction using a metal catalyst are not carried out, therefore, it is very safe method, and also special manufacturing equipments are not needed.

Abstract: Stable Atomoxetine hydrochloride, a process for the manufacture thereof, the use of stable Atomoxetine Hydrochloride for making a pharmaceutical formulation, a process for the preparation of any form of Atomoxetine Hydrochloride, and an analytical method for analyzing the stability of Atomoxetine Hydrochloride are provided.

Abstract: The present invention is directed to a new class of 4-cyano-phenoxy-alkyl carboxyl derivatives and to their use as androgen receptor modulators. Other aspects of the invention are directed to the use of these compounds to decrease excess sebum secretions and to stimulate hair growth.

Abstract: The present invention provides improved processes for the preparation of atomoxetine hydrochloride under reaction conditions that improve reaction yields and facilitate commercial synthesis. In particular, the invention is directed to the synthesis of atomoxetine HCl by adding HCl to a mixture of (R)-(?)-tomoxetine (S)-(+)-mandelate with an organic solvent, with or without a base and water.

Abstract: The invention provides compounds of the formula: or a pharmaceutically acceptable salt thereof, where m, n, R1, R2, R3 R4, R5, R6, R7 are those defined herein. The invention also provides pharmaceutical compositions comprising a compound of the invention, methods for using compounds and/or pharmaceutical compositions of the invention, and methods for synthesizing compounds of the invention.

Abstract: The present invention provides enantiomerically pure (R)-(?)-tomoxetine (S)-(+)-mandelate and atomoxetine HCl. The present invention further provides enantiomerically pure (R)-(?)-tomoxetine (S)-(+)-mandelate prepared from racemic tomoxetine. The present invention also provides enantiomerically pure atomoxetine HCl prepared from (R)-(?)-tomoxetine (S)-(+)-mandelate.

Abstract: The present invention provides improved processes for the preparation of atomoxetine hydrochloride under reaction conditions that improve reaction yields and facilitate commercial synthesis. In particular, the invention is directed to the synthesis of atomoxetine HCl by adding HCl to a mixture of (R)-(?)-tomoxetine (S)-(+)-mandelate with an organic solvent, with or without a base and water. In preferred embodiments, the atomoxetine hydrochloride produced is Form A.

Abstract: Thyronamine derivatives and analogs, methods of using such compounds, and pharmaceutical compositions containing them are disclosed. Methods of preparing such compounds are also disclosed.

Abstract: The invention relates to a process for distillatively preparing TDA from a reactant stream comprising TDA, high boilers and low boilers in a dividing wall column in which a dividing wall is disposed in the longitudinal direction of the column to form an upper combined column region (2), a lower combined column region (3), a feed section (4) having a rectifying section (5) and stripping section (6), and also a withdrawal section (7) having a rectifying section (9) and stripping section (8), which comprises the following steps: a. feeding the reactant stream (13) into the feed section (4) of the dividing wall column (1); b. drawing off a low boiler fraction via the top of the column (11); c. drawing off TDA via a side draw (14) in the withdrawal section (7) of the dividing wall column (1); d. drawing off a low boiler fraction via the bottom of the column (12).

Abstract: Thyronamine derivatives and analogs, methods of using such compounds, and pharmaceutical compositions containing them are disclosed. Methods of preparing such compounds are also disclosed.

Abstract: Thyronamine derivatives and analogs, methods of using such compounds, and pharmaceutical compositions containing them are disclosed. Methods of preparing such compounds are also disclosed.

Abstract: Toluenediamine is produced and separated from by-products of the reaction by: a) hydrogenating dinitrotoluene in the presence of a catalyst, b) separating the catalyst, water and optionally solvent from the hydrogenation reaction mixture to give crude toluenediamine, and c) separating by distillation the crude toluenediamine in a separating wall column into at least four product streams P1, P2, P3 and P4. The product stream P1 is a stream containing low boilers. The product stream P2 is a stream containing o-toluenediamine. The product stream P3 is a stream containing m-toluenediamine. The product stream P4 is a stream containing high boilers and m-toluenediamine.

Abstract: The present invention provides a novel diamine which is especially useful as a material for a resin for a liquid crystal alignment film, a polyimide precursor and a polyimide synthesized by using the diamine, and a treating agent for liquid crystal alignment containing such a polymer, which gives a liquid crystal alignment film having a high pretilt angle of liquid crystal, excellent thermal stability of the pretilt angle and small dependence of the pretilt angle on rubbing pressure. A diaminobenzene derivative represented by the formula (1): wherein X1 and X2 are cyclic groups, and X3 is selected from an alkyl group, an alkoxy group, a fluoroalkyl group, a fluoroalkoxy group, a fluorine atom, a chlorine atom, a bromine atom and a cyano group; a polyimide precursor and a polyimide synthesized by using the diaminobenzene derivative as a part of the material; and a treating agent for liquid crystal alignment containing at least one of the polymers.

Abstract: The invention provides sodium channel modulating compounds which are useful for treating diseases or conditions associated with sodium channel activity, such as neuropathic pain. The invention also provides pharmaceutical compositions comprising a compound of the present invention, as well as therapeutic methods comprising administering such a compound or salt to a mammal (e.g. a human).

Abstract: The present invention provides 8-(2-hydroxyphenoxy)octyldiethanolamine) and salts thereof, compositions containing the same and one or more active agents, and methods of administering active agents with the same. The delivery agents of the present invention are well suited for forming non-covalent mixtures with active agents for oral, intracolonic, pulmonary, and other routes of administration to animals.

Abstract: Disclosed are multibinding compounds which are ?2-adrenergic receptor agonists and are useful in the treatment and prevention of respiratory diseases such as asthma, bronchitis. They are also useful in the treatment of nervous system injury and premature labor.

Abstract: Treatment of sexual dysfunction disorders comprising administering an effective amount of atomoxetine.

Abstract: There are provided novel compounds of formula (I), wherein R1, R2, X, Y, V, W and Z are as defined in the specification, and pharmaceutically acceptable salts thereof, and enantiomers and racemates thereof; together with processes for their preparation, compositions containing them and their use in therapy. The compounds are inhibitors of nitric oxide synthase and are thereby particularly useful in the treatment or prophylaxis of inflammatory disease and pain.

Abstract: The present invention concerns a method of synthesizing fluoxetine hydrochloride. The method includes the synthesis of 3-methylamino-1-phenyl-1-propanol by reduction of 1-phenyl-3-methylamino-2-propen-1-one with sodium borohydride and acetic acid.

Abstract: This invention relates to novel substituted amine derivatives. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.

Abstract: The instant invention provides novel substituted naphthyl compounds, intermediates, compositions, pharmaceutical formulations, and methods of use.

Abstract: Elastomers which have excellent stability to prevent oxidative, thermal, dynamic, light-induced and/or ozone-induced degradation comprise, as stabilizers, at least one compound of the formula I