Abstract: This invention provides estrogen receptor modulators of formula I, having the structure wherein R1, R2, R2a, R3, R3a, and R4, and X as defined in the specification, or a pharmaceutically acceptable salt thereof.

Abstract: A process for preparation of a compound with enhanced optical purity is disclosed wherein a mixture of the enantiomers of a chiral amine is brought into contact with an enzyme having peptide deformylase activity with a bivalent metal ion as a cofactor.

Abstract: Substituted alkylmetal reagents such as (trimethylsilylmethyl)lithium are reacted with azaaromatic compounds and/or nitrogen heterocycle compounds to produce functionalized azaaromatic compounds and functionalized nitrogen heterocycle compounds.

Abstract: An oxidation catalyst is prepared by pyrolyzing a source of iron and a source of nitrogen on a carbon support. Preferably, a noble metal is deposited over the modified support which comprises iron and nitrogen bound to the carbon support. The catalyst is effective for oxidation reactions such as the oxidative cleavage of tertiary amines to produce secondary amines, especially the oxidation of N-(phosphonomethyl)iminodiacetic acid to N-(phosphonomethyl)glycine.

Abstract: The present invention provides processes for removing organic solvent from crystals of atorvastatin hemi-calcium containing organic solvent. In one process, the organic solvent is displaced by vapor diffusion of water in a vessel maintained at elevated humidity. In a second process, the organic solvent is removed by fluidized bed drying. The present invention further provides atorvastatin hemi-calcium containing 1% or less organic solvent, which can be obtained from atorvastatin hemi-calcium that has been crystallized from an organic solvent-containing solution by practice of the processes of the invention.

Abstract: Compounds, compositions and methods are provided which are useful in the treatment of diseases through the modulation of potassium ion flux through voltage-dependent potassium channels. More particularly, the invention provides sulfonamides, and compositions and methods utilizing sulfonamides that are useful in the treatment of diseases by blocking potassium channels associated with the onset or recurrence of the indicated conditions. Exemplary diseases treatable with the compounds, compositions and methods of the invention include sickle cell disease and glaucoma.

Abstract: An excellent squalene synthase inhibitor is provided. Specifically, what is provided is a compound (I) represented by the following formula, a salt thereof or a hydrate of them. In formula (I), R1 represents an optionally substituted vinyl group or an aromatic ring which may be substituted. Also, n is an integer of 0 to 2. Further, X, Y and Z are the same as or different from each other and each represents an optionally substituted carbon atom, or an optionally substituted nitrogen atom, sulfur atom or oxygen atom, and Y optionally represents a single bond, and when Y represents the single bond, the ring to which X, Y and Z belong is a 5-membered ring. Also in the formula, CyA represents a 5- to 14 membered non-aromatic cyclic amino group or non-aromatic cyclic amido group which may be substituted, and the non-aromatic cyclic amino group or the non-aromatic cyclic amido group optionally having an oxygen atom or a sulfur atom.

Abstract: The present invention relates to a process for producing an aliphatic oligocarbonate diol comprising a) reacting an aliphatic diol with dimethyl carbonate at an elevated pressure in a reaction mixture, and b) subsequently removing unreacted methanol and dimethyl carbonate under a reduced pressure to uncap the terminal OH groups.

Abstract: The invention concerns 3-arylthio-propyl-amino-3,4-dihydro-2H-1,5-aryloxathiepin derivatives of general formula (I), wherein: R1 and R2, identical or different, represent a hydrogen atom, a fluorine atom or a chlorine atom, a hydroxy group, an alkyl, cyclopropyl, alkoxy, cyclopropoxy radical or when they occupy adjacent positions, form with the carbon atoms bearing them a carbon-containing cycle or an oxygen-containing heterocycle with five non-aromatic rings; R3 represents an alkyl radical, a hydroxy group or a methoxy radical; R4 represents a hydrogen atom or a methyl radical; and R5 and R6, identical or different represent a hydrogen atom, an alkyl, alkoxy, alkylthio, alkylamino radical, or the groups OR4 and R5 form with the carbons which bear them a non-aromatic heterocycle with five or six rings containing at least an oxygen atom; and their pharmaceutically acceptable additions salts

Abstract: This invention discloses compounds that alter PPAR activity. The invention also discloses pharmaceutically acceptable salts of the compounds, pharmaceutically acceptable compositions comprising the compounds or their salts, and methods of using them as therapeutic agents for treating or preventing hyperlipidemia and hypercholesteremia in a mammal. The present invention also discloses method for making the disclosed compounds.

Abstract: Imidazolium salts are the immediate precursors to N-heterocyclic carbenes (NHC) yet a simple, general synthetic route to a wide variety of imidazolium salts is not yet available. Such a straightforward route is described for two specific members of this family of ligand precursor: 1,3-Bis(2,4,6-trimethylphenyl)imidazolium chloride (IMes.HCl) and 1,3-Bis(2,6-diispropylphenyl)imidazolium chloride (IPr.HCl). The procedure appears general and similar protocols can be used to isolate various imidazolium salts.

Abstract: The compounds disclosed herein are indolocarbazoles of Formula (I), which are potent CDK4 inhibitors, and are useful in the treatment of cell proliferative disorders, including cancer. Formula (I).

Abstract: The invention relates to novel pesticidal pyrrolcarboxamide of the formula (I), wherein X is oxygen or sulfur; R1 is CF3, CF2H or CFH2; R2 is C1–C3alkyl, C1–C3haloalkyl, C1–C3alkoxy-C1–C3alkyl or C1–C3haloalkoxy-C1–C3alkyl; R3 is hydrogen, methyl, CF3 or fluoro; Q is (Q1), (Q2), (Q3), (Q4); R4 is C6–C14bicycloalkyl unsubstituted or substituted by methyl, ethyl or CF3; C6–C14bicycloalkenyl unsubstituted or substituted by methyl, ethyl or CF3; C6–C14bicycloalkadienyl unsubstituted or substituted by methyl, ethyl or CF3; a group of the form (a) wherein R7, R8, R9 are independently of each other C1–C3alkyl or C1–C3haloalkyl; or a group (b) wherein R10 and R11 are independently of each other hydrogen or halogen and n=1 or 2; and R5 and R6 are independently of each other hydrogen or halogen. The novel compounds have plant-protecting properties and are suitable for protecting plants against infestation by phytopathogenic microorganisms.

Abstract: The invention concerns a method for hydrocyanation of ethylenically unsaturated organic compounds comprising at least a nitrile function. The invention provides a method for hydrocyanation of an ethylenically unsaturated hydrocarbon compound by reacting in liquid medium the hydrogen cyanide in the presence of a catalyst comprising a metal element selected among transition metals and an organophosphorous ligand, characterised in that the organophosphorous ligand is a furylphosphine. The invention is in particular useful for synthesizing adiponitrile from butadiene.

Abstract: The present invention relates to novel morpholin-acetamide compounds of formula (I) useful for the treatment of inflammatory diseases. Compounds of formula (I) wherein R1, R2, R3, R4, R5, X, a, b and Z are as defined in the specification, processes for preparing them, formulations containing them and their use in therapy for the treatment of inflammatory diseases.

Abstract: Disclosed is an agent for inducing receptor potential, which comprises an organic dye compound capable of inducing/evoking receptor potential in response to photostimulation in the optic nerve, wherein the organic dye compound is a polymethine organic dye compound. Also disclosed is a substituent material for the retina comprising the agent.

Abstract: The present invention relates to a process for preparing haptens for immunoassay of phosphorothioate pesticides, which comprises the steps of reacting O-methyl(ethyl) dichlorothiophosphate with a phenolic compound to obtain O-methyl(ethyl) O-aryl chlorothiophosphate, and reacting the O-(methyl)ethyl O-aryl chlorothiophosphate thus obtained with aminocarboxylic acid to give desired haptens. In accordance with the present invention, haptens having a structure of O-methyl(ethyl) O-aryl N-(carboxyalkyl)phosphoramidothioate or O-methyl(ethyl) O-aryl N-alkyl-N-(carboxyalkyl)phosphoramidothioate can be simply prepared with a high yield by employing two-step processes in a cost-efficient manner.

Abstract: A compound represented by formula (I) wherein R1 represents hydrogen atom and R2 represents hydroxyl group, or R1 and R2 may combine together to represent oxo group or oxime group; R3 represents hydrogen atom and R4 represents hydroxyl group, or R3 and R4 may combine together to represent oxo group or oxime group; R5 represents hydrogen atom and R6 represents hydroxyl group, or R5 and R6 may combine together to represent oxo group or oxime group; R7 represents hydrogen atom and R8 represents hydrogen atom, or R7 and R8 may combine together to represent oxo group or oxime group; R9 and R10 represent hydrogen atom, an alkyl group, or an alkenyl group.

Abstract: A new polymorphic crystalline form of bicifadine hydrochloride, designated form B, which is more thermodynamically stable than the previously known polymorphic form of bicifadine hydrochloride, designated as form A, methods for preparing said crystalline form B and pharmaceutical compositions containing said crystalline form B.

Abstract: Chemical agents of the general formula (I) and (II), such as derivatives of 3-hydroxy-pyrrole containing hydroxamic acid, and including salts thereof, that modulate levels of gene expression in cellular systems, including cancer cells, are disclosed, along with methods for preparing such agents, as well as pharmaceutical compositions containing such agents as active ingredients and methods of using these as therapeutic agents.