Abstract: The invention features methods and compositions for the synthesis of multimerizing agents.

Abstract: The instant invention relates to mesogenic media comprising one or more compounds of formula D wherein the parameters are as specified in the text, preferably to mesogenic media showing a blue phase, preferably stabilised by a polymer, and their use in electro-optical light modulation elements and their respective use in displays, as well as to such devices.

Abstract: The invention features methods and compositions for the synthesis of multimerizing agents. An exemplary method for producing AP20187 may comprise: (a) coupling 2-N,Ndimethylaminomethyl-1,3-diaminopropane with AP20792 to produce the dimeric alcohol, AP20793; and (b) coupling the AP20793 so produced with API7362 to yield AP20187. In particular embodiments, the method further includes the step of producing API7362 by coupling API7360 with methyl-L-pipecolic acid, or a salt thereof.

Abstract: An amide compound represented by formula (I) has an excellent pest control effect. (In the formula, Y represents a 3-7 membered saturated heterocyclic ring which contains, as ring-forming components(s), one or more atoms or groups that are selected from the group consisting of an oxygen atom and —S(O)t—, the saturated heterocyclic ring may have one to three atoms or groups selected from group D and t represents 0 or the like; X represents a C1-C10 chain hydrocarbon group which may have one or more atoms or groups that are selected from group A, or the like; W represents —CR8— or the like; r represents 1 or the like; R1, R2, R3, R4, R5, R6, R7 and R8 may be the same or different and each represents a hydrogen atom or the like; and n represents 1 or the like.

Abstract: The present invention relates to prodrugs of compounds containing 1,3-dioxane moiety, pharmaceutical compositions thereof, and the use of the compounds and compositions for the modulation of thromboxane A2 or a peroxisome proliferator-activated receptor. The prodrugs of the compounds, analogs, and pharmaceutically acceptable salts thereof, and pharmaceutical compositions can be used in the treatment and prevention of cancer.

Abstract: Industrial synthesis process for the compound of formula (I):

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

Abstract: There are disclosed sulfonic acid precursor compositions, as are methods of using these compositions in, for example, photolithography. Other embodiments are also disclosed.

Abstract: A compound of Formula (1), is disclosed wherein P1 and P2 are alcohol protecting groups or 1,3-diol protecting group, R is selected from: wherein R4a is selected from alkyl, aryl, arylalkyl and cycloalkyl, Rc is selected from H, alkyl, aryl, alkaoxy, haloalkyl, monohaloalkyloxy, and dihaloalkyloxy, Rd is selected from alkyl, aryl, arylalkyl, CF3, halo and NO2 and X is selected from O, N—H, N-alkyl and S, Ra and Rb are same or different and each represents hydrogen, an alkyl group of 1 to 12 carbon atoms, an aryl group of 6 to 12 carbon atoms, or an aralkyl group of 7 to 12 carbon atoms.

Abstract: The invention features methods and compositions for the synthesis of multimerizing agents. An exemplary method for producing AP20187 may comprise: (a) coupling 2-N,Ndimethylaminomethyl-1,3-diaminopropane with AP20792 to produce the dimeric alcohol, AP20793; and (b) coupling the AP20793 so produced with API7362 to yield AP20187. In particular embodiments, the method further includes the step of producing API7362 by coupling API7360 with methyl-L-pipecolic acid, or a salt thereof.

Abstract: Industrial synthesis process for the compound of formula (I):

Abstract: There are disclosed sulfonic acid precursor compositions, as are methods of using these compositions in, for example, photolithography.

Abstract: The present invention relates to a catalyst system. In particular the invention relates to a catalyst in the form of metal or an alloy that is encapsulated within a polymer shell or matrix. More specifically the invention is directed towards reactive catalytic metals that may be pyrophoric or otherwise reactive in air and/or susceptible to oxidation. In particular, the invention is concerned with catalysts based on nickel.

Abstract: The invention relates to salts of acids with 2-propyl esters of general formula (2) The invention also relates to a method for the preparation of salts of acids with compounds of general formula (2) and to the use thereof in the preparation of atorvastatin.

Abstract: The present invention relates to prodrugs of compounds containing 1,3-dioxane moiety, pharmaceutical compositions thereof, and the use of the compounds and compositions for the modulation of thromboxane A2 or a peroxisome proliferator-activated receptor. The prodrugs of the compounds, analogs, and pharmaceutically acceptable salts thereof, and pharmaceutical compositions can be used in the treatment and prevention of cancer.

Abstract: The present invention provides prodrugs of GABA analogs, pharmaceutical compositions of prodrugs of GABA analogs and methods for making prodrugs of GABA analogs. The present invention also provides methods for using prodrugs of GABA analogs and methods for using pharmaceutical compositions of prodrugs of GABA analogs for treating or preventing common diseases and/or disorders.

Abstract: The present invention provides compositions and methods for the delivery of therapeutic agents to cells. In particular, these include novel cationic lipids and nucleic acid-lipid particles that provide efficient encapsulation of nucleic acids and efficient delivery of the encapsulated nucleic acid to cells in vivo. The compositions of the present invention are highly potent, thereby allowing effective knock-down of a specific target protein at relatively low doses. In addition, the compositions and methods of the present invention are less toxic and provide a greater therapeutic index compared to compositions and methods previously known in the art.

Abstract: The invention concerns A continuous process for the production of compounds having the general formula (6): wherein R is a straight or branched chain alkyl group, R1 is a straight or branched chain alkyl group substituted with a nitrile group, a hydroxy group or a halogen atom, R2 is a hydroxy group or a keto group, and each R3 is, independently, hydrogen or a straight or branched chain alkyl group, comprising providing to a reaction zone a continuous stream of an alkyl acetate and a continuous stream of an alkali metal or alkaline earth metal amide base and contacting the continuous streams together in the reaction zone to yield an enolate compound, providing to the or a separate reaction zone a continuous stream of a compound of formula (5): wherein R1 is as previously defined, and contacting the continuous stream of compound (5) with a continuous stream of the enolate (4) in the or the separate reaction zone at a temperature above 20° C.

Abstract: The present invention relates to an electro-optical light modulation element and to electro-optical displays and display systems, such as television screens and computer monitors, containing elements of this type. The light modulation elements according to the invention contain a mesogenic modulation medium which is in the isotropic phase during operation of the light modulation elements and are particularly distinguished by very short response times in addition to good contrast and low viewing-angle dependence. The mesogenic modulation media used in the electro-optical light modulation elements are likewise a subject-matter of the present invention.

Abstract: Process for the synthesis of ivabradine of formula (I): and addition salts thereof with a pharmaceutically acceptable acid.

Abstract: The present invention relates to a preparation process useful in synthesis of atorvastatin, more particularly a process for preparing atorvastatin is effective in treating hyperlipemia, comprising protecting the dihydroxy group at C3 and C5 positions of the starting material cis-t-butyl-6-substituted-3,5-dihydroxy-hexanoate with trialkyl orthoformate, reducing the terminal nitro or cyano group to amine group, performing JV-alkylation by sequentially reacting with ethyl 4-fluorobenzene-2-haloacetate and isobutyryl chloride, cyclizing with JV,3-diphenylpropynamide, and performing deprotection and hydrolysis.

Abstract: Disclosed are ?-amino-?-hydroxy-?-aryl-alkanoic acid amide compounds of formula (I) and the salts thereof, having renin-inhibiting properties. Also disclosed are pharmaceutical compositions comprising these compounds and methods of administering them for the treatment of hypertension, atherosclerosis, unstable coronary syndrome, congestive heart failure, cardiac hypertrophy, cardiac fibrosis, cardiomyopathy postinfarction, unstable coronary syndrome, diastolic dysfunction, chronic kidney disease, hepatic fibrosis, complications resulting from diabetes, such as nephropathy, vasculopathy and neuropathy, diseases of the coronary vessels, restenosis following angioplasty, raised intra-ocular pressure, glaucoma, abnormal vascular growth, hyperaldosteronism, cognitive impairment, alzheimers, dementia, anxiety states and cognitive disorders.

Abstract: The present invention relates to a catalyst system. In particular the invention relates to a catalyst in the form of metal or an alloy that is encapsulated within a polymer shell or matrix. More specifically the invention is directed towards reactive catalytic metals that may be pyrophoric or otherwise reactive in air and/or susceptible to oxidation. In particular, the invention is concerned with catalysts based on nickel. Raney or sponge nickel is highly hazardous: a self-igniting solid; produces hazardous fumes when burning; causes irritation of the respiratory tract, nasal cavities; causes pulmonary fibrosis if inhaled; ingestion may lead to convulsions and intestinal disorders; causes eye and skin irritation; and chronic exposure may lead to pneumonitis and sensitization (“nickel itch”). The invention provides metal catalysts that avoid such problems and have a good shelf life and working life.

Abstract: Novel ketal compounds can be made from an oxocarboxylate and a triol. Novel polymeric structures are, in turn, synthesized from the ketal compounds. Such ketal compounds and associated polymers are useful in a broad range of applications as a substitute for materials derived from petroleum or other such nonrenewable resources.

Abstract: The present invention provides novel cycloalkylmethylamine analogs, and methods of preparing cycloalkylmethylamine analogs. The present invention also provides methods of using cycloalkylmethylamine analogs and compositions of cycloalkylmethylamine analogs. The pharmaceutical compositions of the compounds of the present invention can be advantageously used for treating and/or preventing obesity and obesity related co-morbid indications.

Abstract: The present invention provides superior compositions and methods for the delivery of therapeutic agents to cells. In particular, these include novel lipids and nucleic acid-lipid particles that provide efficient encapsulation of nucleic acids and efficient delivery of the encapsulated nucleic acid to cells in vivo. The compositions of the present invention are highly potent, thereby allowing effective knock-down of specific target proteins at relatively low doses. In addition, the compositions and methods of the present invention are less toxic and provide a greater therapeutic index compared to compositions and methods previously known in the art.

Abstract: A liquid crystal compound represented by formula (1), a liquid crystal composition comprising the compound, and a liquid crystal display device comprising the composition: For example, R1 is alkyl having 1 to 20; ring A1, ring A2, ring A3, ring A4, ring A5, and ring A6 are 1,4-cyclohexylene or 1,4-phenylene; Z1, Z2, Z3, Z4, Z5, and Z6 is a single bond; X1 is hydrogen or halogen; l, m, n, o, p, and q are 0 or 1, and l+m+n+o+p+q is 3.

Abstract: The present invention relates to a preparation process useful in synthesis of atorvastatin, more particularly a process for preparing atorvastatin is effective in treating hyperlipemia, comprising protecting the dihydroxy group at C3 and C5 positions of the starting material cis-t-butyl-6-substituted-3,5-dihydroxy-hexanoate with trialkyl orthoformate, reducing the terminal nitro or cyano group to amine group, performing JV-alkylation by sequentially reacting with ethyl 4-fluorobenzene-2-haloacetate and isobutyryl chloride, cyclizing with JV,3-diphenylpropynamide, and performing deprotection and hydrolysis.

Abstract: An embodiment of the composition contains any of compounds of the formula A-LG in which A represents any of residues of general formula (A-1) below and LG represents any of groups that are cleaved to generate acids of the formula A-H when acted on by an acid. The composition further contains at least one of a compound that generates an acid when exposed to actinic rays or radiation and a compound that generates an acid when heated.

Abstract: The present invention concerns a synthesis process comprising the following steps (i) reacting 3-ethyl-4-nitrobenzoic acid with thionyl chloride to produce a 3-ethyl-4-nitrobenzoic acid chloride or a 3-ethyl-4-nitrobenzoic acid anhydride from 3-ethyl-4-nitrobenzoic acid by means of water cleavage and (ii) Friedel-Crafts acylation by reacting the 3-ethyl-4-nitrobenzoic acid chloride or the 3-ethyl-4-nitrobenzoic acid anhydride with an optionally substituted aryl-H to form an optionally substituted (3-ethyl-4-nitrophenyl)-aryl-methanone. In addition the present invention concerns compounds containing (3-ethyl-4-nitrophenyl)-aryl-methanone, characterized in that the optionally substituted aryl is an optionally substituted condensed aromate.

Abstract: Methods of inhibiting the cytokine or biological activity of Macrophage Migration Inhibitory Factor (MIF) comprising contacting MIF with a compound of formula (I) are provided. The invention also relates to methods of treating diseases or conditions where MIF cytokine or biological activity is implicated comprising administration of compounds of formula (I), either alone or as a part of combination therapy. Novel compounds of formula (I) are also provided for.

Abstract: The present invention relates to an electro-optical light modulation element and to electro-optical displays and display systems, such as television screens and computer monitors, containing elements of this type. The light modulation elements according to the invention contain a mesogenic modulation medium which is in the isotropic phase during operation of the light modulation elements and are particularly distinguished by very short response times in addition to good contrast and low viewing-angle dependence. The mesogenic modulation media used in the electro-optical light modulation elements are likewise a subject-matter of the present invention.

Abstract: A compound corresponding to general formula (I): in which R1 represents a phenyl or naphthalenyl group optionally substituted with one or more halogen atoms or hydroxyl, cyano, nitro, (C1-C3)alkyl, (C1-C3)alkoxy, trifluoromethyl, trifluoromethoxy, benzyloxy, (C3-C6)cycloalkyl-O— or (C3-C6)cycloalkyl(C1-C3)alkoxy groups; R2 represents either a group of general formula CHR3CONHR4 in which R3 represents a hydrogen atom or a methyl group and R4 represents a hydrogen atom or a (C1-C3)alkyl, (C3-C5)cycloalkyl or (pyridin-4-yl)methyl group; or a 2,2,2-trifluoroethyl group; or an (imidazol-2-yl)methyl group; or a (benzimidazol-2-yl)methyl group; or a phenyl group optionally substituted with one or more halogen atoms or cyano, nitro, (C1-C3)alkyl, (C1-C3)alkoxy, trifluoromethyl or trifluoromethoxy groups; and n represents a number ranging from 1 to 3; in the form of a base, of an addition salt with an acid, of a hydrate or of a solvate.

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 compounds of formula (I) in which R is selected from halogen, alkyl, alkoxy, aryl and heteroaryl; R1 is selected from 2-hydroxyethyl, 2,3-dihydroxypropyl, 3-hydroxypropyl, 2,2-dihydroxyethyl, 3,3-dihydroxypropyl, 1,3-dioxolane-ethyl, 1,3-dioxane-methyl, 1,3-dioxolane-methyl, 1,3-dioxane-ethyl, 3-fluoro-2-hydroxypropyl, 3-carboxy-2-hydroxy-propyl, 3-chloro-2-hydroxypropyl, 2-hydroxypropyl, 2-hydroxy-propen-2-yl, morpholinoethyl, piperazinoethyl, hydroxymethyl, benzyl, 4-(hydroxymethyl)benzyl, 4-chlorobenzyl, 4-fluorobenzyl, and 4-hydroxybenzyl. R2 is te/t-butyl or trifluoromethyl; R3 is independently selected from hydrogen, carboxy, cyano, alkyl or hydroxyalkyl, The compounds of formula (I) can be used for the preparation of pharmaceutical compositions for the therapy of inflammatory states, such as chronic neuropathic pain, over-active bladder syndrome, tumor pain, hemorrhoids, inflammatory hyperalgesia, post-intervention pain, dental extraction, airway and gastro-intestinal diseases.

Abstract: This invention describes the new 6-alkenyl- and 6-alkinyl-epothilone derivatives of general formula (I) in which R1a, R1b, R2b, R3a, R3b, R4, R5, R6, R7, A, Y, D, E, G, Y and Z have the meanings that are indicated in the description. The new compounds interact with tubulin by stabilizing microtubuli that are formed. They are able to influence the cell-splitting in a phase-specific manner and thus find use in treating diseases or conditions associated with the need for cell growth, division and/or proliferation. Thus the compounds are suitable for treating malignant tumors, for example, ovarian, stomach, colon, adeno-, breast, lung, head and neck carcinomas, malignant melanoma, acute lymphocytic and myelocytic leukemia. In addition, they are suitable for anti-angiogenesis therapy as well as for treatment of chronic inflammatory diseases (such as psoriasis, arthritis). Methods of use and preparation of the compounds are also described.

Abstract: In recognition of the need to develop novel therapeutic agents and efficient methods for the synthesis thereof, the present invention provides novel bifunctional, trifunctional, or multifunctional compounds for inhibiting histone deacetylases, and pharmaceutically acceptable salts and derivatives thereof. The present invention further provides methods for treating disorders regulated by histone deacetylase activity (e.g., proliferative diseases, cancer, inflammatory diseases, protozoal infections, hair loss, etc.) comprising administering a therapeutically effective amount of an inventive compound to a subject in need thereof. The present invention also provides methods for preparing compounds of the invention.

Abstract: A liquid crystal compound represented by formula (1), a liquid crystal composition comprising the compound, and a liquid crystal display device comprising the composition: For example, R1 is alkyl having 1 to 20; ring A1, ring A2, ring A3, ring A4, ring A5, and ring A6 are 1,4-cyclohexylene or 1,4-phenylene; Z1, Z2, Z3, Z4, Z5, and Z6 is a single bond; X1 is hydrogen or halogen; l, m, n, o, p, and q are 0 or 1, and l+m+n+o+p+q is 3.

Abstract: A compound corresponding to general formula (I): in which R1 represents a phenyl or naphthalenyl group optionally substituted with one or more halogen atoms or hydroxyl, cyano, nitro, (C1-C3)alkyl, (C1-C3)alkoxy, trifluoromethyl, trifluoromethoxy, benzyloxy, (C3-C6)cycloalkyl-O— or (C3-C6)cycloalkyl(C1-C3)alkoxy groups; R2 represents either a group of general formula CHR3CONHR4 in which R3 represents a hydrogen atom or a methyl group and R4 represents a hydrogen atom or a (C1-C3)alkyl, (C3-C5)cycloalkyl or (pyridin-4-yl)methyl group; or a 2,2,2-trifluoroethyl group; or an (imidazol-2-yl)methyl group; or a (benzimidazol-2-yl)methyl group; or a phenyl group optionally substituted with one or more halogen atoms or cyano, nitro, (C1-C3)alkyl, (C1-C3)alkoxy, trifluoromethyl or trifluoromethoxy groups; and n represents a number ranging from 1 to 3; in the form of a base, of an addition salt with an acid, of a hydrate or of a solvate.

Abstract: The present invention provides a novel modulator of the TRPV1-receptor function, comprising a compound of the formula; wherein ring A is an optionally substituted carbocycle or heterocycle, ring B is an optionally substituted benzene ring or an optionally substituted 6-membered heteroaromatic ring containing N atom, a dashed line means existence or absence of a bond, n is 1 or 2, R1 and R2 are hydrogen etc., R3 is lower alkyl, R4 is lower alkyl or aryloxy, or R3 and R4 taken together may form optionally substituted 5- or 6-membered non-aromatic heterocycle.

Abstract: Disclosed are ?-amino-?-hydroxy-?-aryl-alkanoic acid amide compounds of formula (I) and the salts thereof, having renin-inhibiting properties. Also disclosed are pharmaceutical compositions comprising these compounds and methods of administering them for the treatment of hypertension, atherosclerosis, unstable coronary syndrome, congestive heart failure, cardiac hypertrophy, cardiac fibrosis, cardiomyopathy postinfarction, unstable coronary syndrome, diastolic dysfunction, chronic kidney disease, hepatic fibrosis, complications resulting from diabetes, such as nephropathy, vasculopathy and neuropathy, diseases of the coronary vessels, restenosis following angioplasty, raised intra-ocular pressure, glaucoma, abnormal vascular growth, hyperaldosteronism, cognitive impairment, alzheimers, dementia, anxiety states and cognitive disorders.

Abstract: A process for preparing intermediate compounds useful in the preparation of statins. The process is particularly useful for the preparation of atorvastatin. The process involves the reduction of two ketone groups at the same time using either a chiral transition metal catalyst or an enzyme based system.

Abstract: A compound corresponding to general formula (I): in which R1 represents a phenyl or naphthalenyl group optionally substituted with one or more halogen atoms or hydroxyl, cyano, nitro, (C1–C3)alkyl, (C1–C3)alkoxy, trifluoromethyl, trifluoromethoxy, benzyloxy, (C3–C6)cycloalkyl-O— or (C3–C6)cycloalkyl(C1–C3)alkoxy groups; R2 represents either a group of general formula CHR3CONHR4 in which R3 represents a hydrogen atom or a methyl group and R4 represents a hydrogen atom or a (C1–C3)alkyl, (C3–C5)cycloalkyl or (pyridin-4-yl)methyl group; or a 2,2,2-trifluoroethyl group; or an (imidazol-2-yl)methyl group; or a (benzimidazol-2-yl)methyl group; or a phenyl group optionally substituted with one or more halogen atoms or cyano, nitro, (C1–C3)alkyl, (C1–C3)alkoxy, trifluoromethyl or trifluoromethoxy groups; and n represents a number ranging from 1 to 3; in the form of a base, of an addition salt with an acid, of a hydrate or of a solvate.

Abstract: Aldehydes containing a difluorooxymethylene bridge, of the general formula I OHC-(A11)m-Z11-(A12-Z12)n-(A13-Z13)p-A14I and the use and preparation thereof and the preparation of 1,3-dioxane compounds.

Abstract: The invention relates to 3,5-dihydroxy-2,2-dimethyl-valeronitriles for the synthesis of epothilones and epothilone derivatives and process for the production of these new intermediate products in the synthesis and the use for the production of epothilones or epothilone derivatives.

Abstract: The invention relates to substituted aromatic polycyclic tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases.

Abstract: A novel class of compounds, which act to antagonize the action of the glucagon hormone on the glucagon receptor. Owing to their antagonizing effect of the glucagon receptor the compounds may be suitable for the treatment and/or prevention of any diseases and disorders, wherein a glucagon antagonistic action is beneficial, such as hyperglycemia, Type 1 diabetes, Type 2 diabetes, disorders of the lipid metabolism and obesity.

Abstract: Multidentate phosphite ligands are disclosed for use in reactions such as hydrocyanation and isomerization. The catalyst compositions made therefrom and the various catalytic processes which employ such multidentate phosphite ligands are also disclosed. In particular, the ligands have heteroatom-containing substituents on the carbon attached to the ortho position of the terminal phenol group.

Abstract: Described are dialkyne compounds of the formula I in which n, m, R1, R2, X1, X2, X3, X4, Z1, Z2, A1, A2, Q, Y1 and Y2 are as defined herein and the use of such compounds in liquid-crystal media.

Abstract: A medicament for treatment of cancer comprising a compound represented by the following general formula (I) or a physiologically acceptable salt thereof: Ar1—S—R1—S—Ar2 wherein R1 represents a nonmetal bridging group; Ar1 and Ar2 independently represent a group selected from the group consisting of an aryl group which has, on its ring, one to three hydroxyl groups optionally substituted with a monovalent group and said aryl group may have one to three substituents other than hydroxyl group on its ring; and a heteroaryl group which has, on its ring, one to three hydroxyl groups optionally substituted with a monovalent group, and said heteroaryl group may have one to three substituents other than hydroxyl group on its ring.