Abstract: The present invention is directed to compounds of Formulae (I), (IIa-IIh), (IIIa-IIIe), (IVa-IVc), (Va-V1), (VIa-VII), (VII), (VIII) and (IX), pharmaceutical compositions thereof and methods of use thereof in the treatment of conditions associated with a dysfunction in proteostasis.

Abstract: The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.

Abstract: the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein Z represents O, S, NR6, SO or SO2; R1 represents hydrogen, cyano, hydroxy, or C1-4alkyl optionally substituted with halo, R2 represents hydrogen, C1-4alkyl, or C1-4alkyloxy-; R3 represents hydrogen, C1-4alkyl, C1-4alkyloxy- or R3 combined with R2 form together a divalent radical selected from the group consisting of —O—CH2— (a), —NR7—CH2— (b), —(CR8R9)m- (c) and —CR10? (d) wherein m represents 1 or 2 and R7, R8, R9 and R10 are each independently selected from hydrogen or C1-4alkyl; R4 represents hydrogen, halo, hydroxy, cyano, amino, NR11R12, C1-4alkyloxy- optionally substituted with one or where possible two or three substituents selected from hydroxy and halo or R4 represents C1-4alkyl optionally substituted with one or where possible two or three substituents selected from hydroxy and halo; R5 represents hydrogen, halo, cyano, amino, phenyl, hydroxy, C1-4alkyloxycarbonyl, hydrox

Abstract: Methods and compositions for the treatment and/or management of cancer are disclosed, which comprise the use of tryptophan hydroxylase inhibitors.

Abstract: The present invention provides a novel process for the preparation of a compound of Formula III, and novel processes for preparing escitalopram using the compound of Formula III.

Abstract: The present invention is directed to novel process for the preparation of sulfonylimine and sulfamide derivatives.

Abstract: An agent for treating fibromyalgia containing a 5-HT2C receptor agonist as an active ingredient

Abstract: Methods for forming maleimide functionalized polymers are provided. In one such embodiment, a maleimide functionalized polymer is prepared in a method that includes a step of carrying out a reverse Diels-Alder reaction. Intermediates useful in the methods, as well as methods for preparing the intermediates, are also provided. Also provided are polymeric reagents, methods of using polymeric reagents, compounds and conjugates.

Abstract: The present invention relates to Escitalopram having a small median particle size and a solid pharmaceutical composition comprising the same.

Abstract: Disclosed herein are novel 1,3-dihydro-5-isobenzofurancarbonitrile derivatives represented by Formula 1, or pharmaceutically acceptable salts thereof. Also disclosed is a pharmaceutical composition for treating or preventing premature ejaculation including the compound. The 1,3-dihydro-5-isobenzofurancarbonitrile derivatives have a short half-life and inhibit the ejaculation process by selectively inhibiting serotonin reuptake via a serotonin reuptake transporter present in a presynaptic neuron. Thus, the compounds are useful in the treatment and prevention of premature ejaculation.

Abstract: The present invention relates to the discovery that certain non-naturally occurring, non-peptide amide compounds and amide derivatives, such as oxalamides, ureas, and acrylamides, are useful flavor or taste modifiers, such as a flavoring or flavoring agents and flavor or taste enhancer, more particularly, savory (the “umami” taste of monosodium glutamate) or sweet taste modifiers, —savory or sweet flavoring agents and savory or sweet flavor enhancers, for food, beverages, and other comestible or orally administered medicinal products or compositions.

Abstract: A compound represented by the formula (I): wherein each symbol is as defined in the specification, and a salt thereof have a GPR40 receptor activation action and is useful as an insulin secretagogue or a prophylactic or therapeutic drug for diabetes and the like.

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 relates generally to substituted benzofurans, benzothiophenes, and indoles and their use as tubulin polymerization inhibitors.

Abstract: The present invention concerns an apparatus and a method for stimulating brain tissue with pulsed electromagnetic fields weaker than the limit for elicitation of the action potentials of the cells of the tissue to be stimulated, the apparatus comprising: at least one electrically conducting coil positioned at a bitemporal position such that hippocampus is stimulated by at least one magnetic field upon supplying a pulse to said coil as well as a coil positioned at a occipital and parietal position; and a pulse generation means operationally connected to said at least one coil for supplying a series of current pulses for conduction, allowing generation of pulsed electromagnetic fields sufficiently strong to cause protein activation, and weaker than the limit for elicitation of the action potentials of the cells of the tissue to be stimulated.

Abstract: The present invention relates to a use of a cyclic imidate as a ligand for catalysis in which the ligand contains sub-structure (Y) as a minimal structural motive, wherein the carbon atoms and the nitrogen atom can be optionally substituted by a chemical substituent.

Abstract: The present invention provides a process for the synthesis of substituted phenoxymethylpropionic acid and related compounds. The compounds are useful for inhibiting the formation of AGEs (Advanced Glycation End Products).

Abstract: Disclosed is a compound represented by Formula (I) or a pharmaceutically acceptable salt thereof: wherein R1 is 1: a C3-8 cycloalkyl C1-4 alkyl group, 2: a C7-14 aralkyl group, in which the aryl moiety thereof is optionally substituted with the same or different 1 to 3 groups selected from the group consisting of: (a) halogen, (b) C1-4 alkyl, which is optionally substituted with 1 to 3 fluorine atoms, (c) C1-4 alkoxy, which is optionally substituted with 1 to 3 fluorine atoms, and (d) C1-4 alkylcarbonyl, which is optionally substituted with C1-4 alkoxy, 3: a five- to ten-membered heteroaryl-C1-4 alkyl group, in which the heteroaryl moiety thereof is optionally substituted with the same or different 1 to 3 groups selected from the group consisting of: (a) halogen, and (b) C1-4 alkyl, or 4: a C6-10 aryl C2-6 alkenyl group; and R2 is a cyano group or a nitro group.

Abstract: This invention provides new 2,3-dihydro-benzofuran compounds, their use for the treatment or prevention of melatoninergic disorders and its compositions.

Abstract: A novel compound, a novel ?1 adrenergic receptor antagonistic agent, and a novel composition are provided which are capable of exerting a therapeutic effect on treatment of hypertension as well as treatment of prostatic hypertrophy and the like.

Abstract: The present invention provides a compound having an ACC inhibitory action, which is useful as an agent for the prophylaxis or treatment of obesity, diabetes, hypertension, hyperlipidemia, cardiac failure, diabetic complications, metabolic syndrome, sarcopenia, cancer and the like, and has superior efficacy. The present invention relates to a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof.

Abstract: The present invention relates to methods of reducing blood pressure in a subject by administering a plasma kallikrein inhibitor.

Abstract: The present invention relates to a compound having a leukotriene (particularly leukotriene B4) inhibitory action, and useful for the prophylaxis or treatment of diseases such as allergy, asthma, inflammation, cancer and the like.

Abstract: The present application discloses derivatives of 8-epiblechnic acid and use thereof in treating a disease related to endothelin receptor A or endothelin-1 (ET-1) over-expression, such as hypertension, cancer, atherosclerosis, and myocardial infarction.

Abstract: The present invention provides a 1-heterodiene derivative represented by formula (2) or salt thereof: (in formula (2), W represents hydrogen atom or the like, A represents oxygen atom or the like, R1 represents an optionally substituted C1-6 alkyl group or the like, m represents an integer of 0 to 10, n represents an integer of 1 to 4, X1 represents oxygen atom or the like, p represents an integer of 0 to 5, R3 represents an optionally substituted C1-6 alkyl group or the like, r presents an integer of 0 to 5, the 1-heterodiene derivative exists in E-form, Z-form or a mixture thereof according to the carbon-carbon undefined double stereo bond in formula (2)).

Abstract: The present invention provides a process for preparation of 1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-5-isobenzofuran car-bonitrile comprising reacting a compound of formula IVa, in the presence of a base with a compound of formula RX, wherein R is selected from alkyl, alkenyl, aryl and heteroaryl which may be optionally substituted with electron withdrawing groups and X is selected from F, Cl, Br, I, CN, OTf and OR1, wherein Tf represents trifluoromethanesulfonyl group, and R1 is optionally substituted alkyl, Z is a cyano group or a group that may be converted to a cyano group; further wherein RX is selected such that an intermediate ether derivative, a compound of formula Va formed from said reaction cyclizes to a compound of formula VI, and where Z is not a cyano group, conversion of the group Z in the compound of formula VI to a cyano group to form 1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-5-isobenzofuran carbonitrile.

Abstract: The invention provides methods, PCR primers and sequence determination oligonucleotides for determining a human's capacity to metabolise a substrate of the CYP2C19 enzyme using genetic analysis.

Abstract: The present patent application relates to an improved process for the separation of enantiomerically pure compounds. Specifically it relates to separation of enantiomerically enriched Rivastigmine, Duloxetine, Escitalopram and their intermediates in high yields.

Abstract: This patent discloses a method for resolution of 4-[4-(dimethylamino)-1-(4?-fluorophenyl)-1-hydroxybutyl]-3-(hydroxymethyl)-benzonitrile as a racemic or non-racemic enantiomer mixture into its isolated enantiomers, said method comprising the step of fractionally crystallizing 4-[4-(dimethylamino)-1-(4?-fluorophenyl)-1-hydroxybutyl]-3-(hydroxymethyl)-benzonitrile as a salt with the (+)-(S,S)- or (?)-(R,R)-enantiomer of O,O?-di-p-toluoyl-tartaric acid in a solvent system comprising 1-propanol, ethanol or acetonitrile.

Abstract: This invention provides compounds of formula (I): wherein ring A, X1, X2, X3, R2, R4b, R10, and G have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention, and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.

Abstract: The present invention relates to pharmaceutical dosage forms of an antidepressant. More particularly, the present invention relates to pharmaceutical dosage forms of Escitalopram oxalate. The present invention also relates to a process for the preparation of pharmaceutical dosage forms of Escitalopram oxalate.

Abstract: The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.

Abstract: The present invention provides a process for preparation of 1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-5-isobenzofuran car-bonitrile comprising reacting a compound of formula IVa, in the presence of a base with a compound of formula RX, wherein R is selected from alkyl, alkenyl, aryl and heteroaryl which may be optionally substituted with electron withdrawing groups and X is selected from F, Cl, Br, I, CN, OTf and OR1, wherein Tf represents trifluoromethanesulfonyl group, and R1 is optionally substituted alkyl, Z is a cyano group or a group that may be converted to a cyano group; further wherein RX is selected such that an intermediate ether derivative, a compound of formula Va formed from said reaction cyclizes to a compound of formula VI, and where Z is not a cyano group, conversion of the group Z in the compound of formula VI to a cyano group to form 1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-5-isobenzofuran carbonitrile.

Abstract: The invention provides a method of sustained delivery of a tertiary amine-containing parent drug comprising administering to a patient an effective amount of a prodrug compound of the invention wherein upon administration to the patient, release of the parent drug from the prodrug is sustained release. Prodrug compounds suitable for use in the methods of the invention are labile quaternary ammonium salts of tertiary amine-containing parent drugs (or tertiary imine-containing parent drugs) that are derivatized through aldehyde-linked prodrug moieties that reduce the solubility of the prodrug compound at a reference pH as compared to the parent drug. The physical, chemical and solubility properties of these derivatives can be further modulated by the choice of counterion X?. In one embodiment, the present invention provides a prodrug compound of Formula I: where R1-R5 are defined in the written description of the invention.

Abstract: Caspace inhibition provides inhibition of viral infection across a wide collection of caspaces and viruses. Caspace inhibition, the prevention of the formation of active caspaces, can be achieved either through gene therapy, protein binding an inhibition, or through small molecule administration. Examples for small molecule inhibition allow the formation of a pharmacaphore to identify more and more active small molecules.

Abstract: The present invention provides a process for preparation of 1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-5-isobenzofuran carbonitrile comprising reacting a compound of formula IVa, in the presence of a base with a compound of formula RX, wherein R is selected from alkyl, alkenyl, aryl and heteroaryl which may be optionally substituted with electron withdrawing groups and X is selected from F, Cl, Br, I, CN, OTf and OR1, wherein Tf represents trifluoromethanesulfonyl group, and R1 is optionally substituted alkyl, Z is a cyano group or a group that may be converted to a cyano group; further wherein RX is selected such that an intermediate ether derivative, a compound of formula Va formed from said reaction cyclizes to a compound of formula VI, and where Z is not a cyano group, conversion of the group Z in the compound of formula VI to a cyano group to form 1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-5-isobenzofuran carbonitrile.

Abstract: Compounds of the general formula (formula I) in which the meanings of the substituents R1 and R6 are as indicated in claim 1, have renin-inhibiting properties and can be used as medicines.

Abstract: The GPR40 receptor function regulator of the present invention, which comprises a compound having an aromatic ring and a group capable of releasing cation is useful as an insulin secretagogue or an agent for the prophylaxis or treatment of diabetes and the like.

Abstract: The present invention provides a process for producing (Z)-1-phenyl-1-(N,N-diethylaminocarbonyl)-2-phthalimidomethylcyclopropane, which includes reacting (Z)-1-phenyl-1-(N,N-diethylaminocarbonyl)-2-hydroxymethylcyclopropane with an orthoester and a brønsted acid, and reacting the reaction product with a phthalimidating agent; and a process for producing (Z)-1-phenyl-1-(N,N-diethylaminocarbonyl)-2-aminomethylcyclopropane hydrochloride through the above process.

Abstract: The present invention relates to an improved process for the preparation of Escitalopram of the Formula (I), which comprises, isolation of Diol compound as an oxalate salt, resolution of Diol compound and cyclization of resolved compound of Formula (VII). The present invention provides a process to obtain pure Diol compound by preparing its Oxalate salt, which is useful for resolution of enantiomers.

Abstract: The present patent application relates to an improved process for the preparation of escitalopram, its salts and intermediates. It also relates to a novel crystalline form S of citalopram diol intermediate, process for preparation and its use in the preparation of citalopram, escitalopram and their salts.

Abstract: The present invention relates to a novel method for the preparation of diol intermediates having the formula (II) and/or the opposite enantiomer of an acylated diol having the formula (IV) useful for the preparation of escitalopram involving selective enzymatic acylation or deacylation.

Abstract: A novel method is provided for the manufacture of escitalopram. The method comprises chromatographic separation of the enantiomers of citalopram or an intermediate in the production of citalopram using a chiral stationary phase such as Chiralpak™ AD or Chiralcel™ OD. Novel chiral intermediates for the synthesis of Escitalopram made by said method are also provided.

Abstract: The present invention relates to the crystalline base of the well known antidepressant drug escitalopram, S-1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-5-isobenzofurancarbonitrile, formulations of said base, a process for the preparation of purified salts of escitalopram, such as the oxalate, using the base, the salts obtained by said process and formulations containing such salts, and a process for the preparation of purified escitalopram free base or salts of escitalopram, such as the oxalate, using the hydrobromide, the salts obtained by said process and formulations containing such salts. Finally the present invention relates to an orodispersible tablet having a hardness of at least 22 N and an oral-disintegration time of less than 120 s and comprising an active pharmaceutical ingredient adsorbed onto a water soluble filler wherein the active pharmaceutical ingredient has a melting point in the range of 40-100° C., as well as a method for making such an orodispersible tablet.

Abstract: Disclosed herein is compound having a formula as described herein. Therapeutic methods, compositions, and medicaments related thereto are also disclosed.

Abstract: The present invention relates to methods of treating the underlying dysregulation of the emotional functionality of mental disorders (i.e. affect instability—hypersensitivity—hyperaesthesia—dissociative phenomena—. . . ) using compounds and compositions of compounds having D4 and/or 5-HT2A antagonistic, partial agonistic or inverse agonistic activity. The invention also relates to methods comprising administering to a patient diagnosed as having a neuropsychiatric disorder a pharmaceutical composition containing (i) compounds having D4 antagonistic, partial agonistic or inverse agonistic activity and/or (ii) compounds having 5-HT2A antagonistic, partial agonistic or inverse agonistic, and/or (iii) any known medicinal compound and compositions of said compounds. The combined D4 and 5-HT2A antagonistic, partial agonistic or inverse agonistic effects may reside within the same chemical or biological compound or in two different chemical and/or biological compounds.

Abstract: The present invention is directed to certain hydroxamate derivatives that are useful in the treatment of hepatitis C. These compounds are also inhibitors of histone deacetylase and are therefore useful in the treatment of diseases associated with histone deacetylase activity. Pharmaceutical compositions and processes for preparing these compounds are also disclosed.

Abstract: The present invention relates to compounds of formula (I): wherein P, R3, W1, and W2 are as described herein, to pharmaceutical compositions comprising the compounds, to processes for their preparation, as well as to the use of the compounds for the preparation of a medicament against 5-HT6 receptor-related disorders.

Abstract: The present invention is directed to a compound of Formula (I): or an enantiomer, diastereomer, polymorph or pharmaceutically acceptable salt thereof and methods for preparing said compounds and compositions, intermediates and derivatives thereof, and methods for treating inflammatory or serine protease mediated disorders.

Abstract: This invention relates to processes and intermediates for the stereoselective alkylation of carbonyl groups. The invention in particular allows the stereoselective preparation of the antidepressant drug escitalopram. It has been found that boric or boronic acid derivatives are useful bridging elements for the attachment of a chiral group to a compound containing a carbonyl group to be alkylated. The said borates and boronates are thus useful in a process for the asymmetric alkylation of a carbonyl group in a compound containing a carbonyl group and an anchor group capable of reacting with a boric or boronic acid derivative. The asymmetric alkylation can be carried out by admixing the compound containing a carbonyl group to be alkylated and the anchor group capable of reacting with a boric or boronic acid derivative with a boric or boronic acid derivative, adding a chiral alcohol, and adding an organometallic compound. After the alkylation reaction, the borate and boronate can be easily removed by hydrolysis.