Abstract: The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including: bone loss, bone fractures, osteoporosis, metastatic bone disease, Pagets disease, periodontal disease, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, cerebral degenerative disorders, restenosis, gynecomastia, vascular smooth muscle cell proliferation, obesity, incontinence, and cancer, in particular of the breast, uterus and prostate.

Abstract: The use of a hydroxyphenylalkadione derivative of the formula (I) wherein, for X, a and Y: X is a —CH2—, —NH— or —O— group, Y is a —CH2— group and a is a single bond or X and Y are in each case a —CH— group and a is a double bond in the Z or E configuration, wherein, for R1, R2 and R3 R1 denotes hydrogen, an aliphatic radical having 1 to 4 C atoms or a —O—R5, —S—R5 or —NR5R6 group and R2 and R3 independently of one another denote hydrogen or an alkyl having 1, 2, 3, 4 or 5 C atoms which is optionally substituted by one or more oxo groups or R7—O— groups or R1 and R2 together form an aliphatic ring which contains a total of 4 to 10 carbon atoms and 0 or 1 oxygen atom, wherein the ring constituent represented by R1 and R2 is optionally substituted by one or more oxo groups and/or R7—O— groups and/or aliphatic radicals having 1 to 4 C atoms and R3 denotes hydrogen or an alkyl having 1, 2, 3, 4 or 5 C atoms which is optionally substituted by one or more oxo groups or R7—O— groups or R2 and

Abstract: The present invention provides compounds having estrogenic activity selected from the group consisting of RRR-?-tocopherol, hydro-Q9 chromene, coenzyme Q9, cycloartane, 1-Feruloyl glycerol, ?-tocopherol-9, and analogues thereof. The compounds of the present invention activate ER? and ER?, and express high estrogenic activity.

Abstract: The present invention relates to an agent for improving renal dysfunction comprising as an active ingredient a compound represented by the following formula (1): wherein each R1, R2, and R3 represents a hydrogen atom or a methyl group, and X represents a linear or branched alkylene or alkenylene group having 10 to 28 carbon atoms.

Abstract: Provided is a liquid-crystalline, polymerizable vinyl ketone compound of formula (1): Preferably, R1 is hydrogen, halogen, —CN, —CF3, —CF2H, —CFH2, —OCF3, —OCF2H, or alkyl, alkoxy, alkoxyalkyl or alkenyl having from 1 to 10 carbon atoms; R2, R3 and R5 are hydrogen; A1 to A4 are independently 1,4-cyclohexylene, 1,4-cyclohexenylene or 1,4-phenylene where any hydrogen may be substituted with halogen; Z1 to Z3 are independently a single bond, —(CH2)2—, —CH?CH—, —CF?CF—, —OCF2— or —CF2O—; Z4 is a single bond, —(CH2)3— or —(CH2)4—; m, n and q are independently 0, 1 or 2. The uppermost temperature of the liquid crystalline phase of the compound is high, and the compound has good compatibility with other compounds and has the necessary characteristics such as optical anisotropy.

Abstract: The use of 2-methyl-benzoic acid methyl ester as a fragrance chemical, suitable for use in creating fragrance, and scents in items such as perfumes, colognes and personal care products is disclosed.

Abstract: Compounds of formula (I), wherein R1 is hydrogen or alkyl; R2 is C1-C4alkoxy or a morpholino radical; and R3 is hydrogen or C1-C4alkoxy, are suitable for improving the solubility of specific photoinitiators in formulations and accordingly enhance the storage stability of formulations comprising a photoinitiator and compounds of formula (I)

Abstract: Chelating ligand precursors for the preparation of olefin metathesis catalysts are disclosed. The resulting catalysts are air stable monomeric species capable of promoting various metathesis reactions efficiently, which can be recovered from the reaction mixture and reused. Internal olefin compounds, specifically beta-substituted styrenes, are used as ligand precursors. Compared to terminal olefin compounds such as unsubstituted styrenes, the beta-substituted styrenes are easier and less costly to prepare, and more stable since they are less prone to spontaneous polymerization. Methods of preparing chelating-carbene metathesis catalysts without the use of CuCl are disclosed. This eliminates the need for CuCl by replacing it with organic acids, mineral acids, mild oxidants or even water, resulting in high yields of Hoveyda-type metathesis catalysts.

Abstract: Histone deacetylase is a metallo-enzyme with zinc at the active site. Compounds having a zinc-binding moiety, for example, an alpha-chalcogenmethylcarbonyl group, such as an alpha-ketothio group, can inhibit histone deacetylase. Histone deacetylase inhibition can repress gene expression, including expression of genes related to tumor suppression. Accordingly, inhibition of histone deacetylase can provide an alternate route for treating cancer, hematological disorders, e.g., hemoglobinopathies, autosomal dominant disorders, e.g. spinal muscular atrophy and Huntington's disease, genetic related metabolic disorders, e.g., cystic fibrosis and adrenoleukodystrophy, or for stimulating hematopoietic cells ex vivo.

Abstract: The invention provides novel tetradentate enediyne ligands that are themselves thermally stable, yet react at about room temperature or slightly higher upon addition of metal ions or under photothermal conditions. In another aspect of the invention, a method of treating a disorder in a mammal comprising administering a therapeutically effective amount of a compound or composition is provided. In addition, the free ligand can be delivered to the mammal prior to complexation to metals, such that the ligand is exposed to a metal in the body and forms a metal complex in vivo. Furthermore, a metal complex of the invention can be administered to the mammal such that the complex exchanges the first metal center with another endogenous metal in order to form a second metal complex in vivo. The second metal complex is capable of forming a benzenoid diradical under physiological conditions and/or under photothermal conditions.

Abstract: It has been discovered certain 1,3-bis-(substituted-phenyl)-2-propen-1-ones, including compounds of formula (I) inhibit the expression of VCAM-1, and thus can be used to treat a patient with a disorder mediated by VCAM-1. Examples of inflammatory disorders that are mediated by VCAM-1 include, but are not limited to arthritis, asthma, dermatitis, cystic fibrosis, post transplantation late and chronic solid organ rejection, multiple sclerosis, systemic lupus erythematosis, inflammatory bowel diseases, autoimmune diabetes, diabetic retinopathy, rhinitis, ischemia-reperfusion injury, post-angioplasty restenosis, chronic obstructive pulmonary disease (COPD), glomerulonephritis, Graves disease, gastrointestinal allergies, conjunctivitis, atherosclerosis, coronary artery disease, angina and small artery disease.

Abstract: This invention relates to 1-[(4-methyl thio)phenyl]-2-(phenyl acetoxy)-1-ethanone. This compound is convertible into 4-(4-methyl thio phenyl)-3-phenyl-2 (5H)-furanone by an economically viable process. This substituted furanone is an intermediate or starting compound for synthesising COX II inhibitor Rofecoxib. This invention also includes a process for preparing the ethanone derivative by halogenating methyl thio aceto phenone and coupling the resulting 2 halosubstituted ethanone with sodium salt of phenyl acetic acid to obtain 1-[(4-methyl thio) phenyl]-2-(phenyl acetoxy)-1-ethanone.

Abstract: Disclosed are processes for preparing modifiable poly(aralkyl ketone)s having active methylene group(s) in the main chain comprising reacting an aralkanoic acid or mixtures thereof in the presence of one alkane or aryl sulfonic acid and a condensing agent. Also disclosed are novel modifiable poly(aralkyl ketone)s obtainable by the processes of the inventions.

Abstract: The invention relates to 1,2-substituted 2,3-dihydro-1H-5,9-dioxacyclohepta[f]inden-7-ones and 7-substituted benzo[b][1,4]dioxepin-3-ones and to the use of these compounds in fragrance compositions.

Abstract: The present invention relates to compounds of the formula (I): which are produced by the plant Garcinia punctata, chemical derivatives derived therefrom, a process for their preparation, and their use as pharmaceuticals, in particular for the treatment and/or prophylaxis of bacterial infectious diseases.

Abstract: The present invention provides a fragrance precursor of formula I: that is capable of forming a fragrant ketone of formula II: and a fragrant lactone of formula III:

Abstract: It is described a process for the synthesis of optically active anthracyclines by the fact that the key intermediate (R)2-acetyl-2-hydroxy-1,2,3,4-tetrahydronaphtalene 5,8-dialkoxy-3,4-dihydronaphtalene by acylation asymmetric dihydroxylation, transformation into chloroacetate, dehydrochloridation and final hydrolysis.

Abstract: The present invention concerns alkyl aryl carbonyl compounds that possess anti-infective activity. The compounds of the invention can be used to target specific nuclear localization signal, thereby blocking importation of specific proteins or molecular complex into the nucleus of a cell. The invention encompasses methods of use of such compounds for treatment or prevention of infectious diseases, such as parasitic and viral diseases, including, for example, malaria and acquired immunodeficiency syndrome. The use of the compounds to detect certain specific protein structures which are present in nuclear localization sequences is also taught.

Abstract: A compound having the formula (I) wherein the substituents are defined herein. Also provided are pharmaceutical compositions including a compound of formula (I) in a pharmaceutical carrier, for treating a disease caused by a picornavirus. Also provided is a method of treating a subject with a disease caused by a picornavirus, including a compound of formula (I) in a pharmaceutical carrier.

Abstract: Provided are processes for the preparation of the compound of the formula wherein R1, R3 and R4 are independently selected from the group consisting of hydrogen, halogen, hydroxyl, nitro, lower alkyl, lower alkoxy, carboxy, C1-C6 trihaloalkyl, and cyano; and R2 is amino or lower alkyl. Also provided are synthetic intermediates that are useful as intermediates in the preparation of the compound of the formula 1.

Abstract: Methods and compositions are provided for the direct catalytic asymmetric aldol reaction of aldehydes with donor molecules selected from ketones and nitroalkyl compounds. The reactions employ as catalyst a Group 2A or Group 2B metal complex of a ligand of formula I, as defined further herein.

Abstract: A method of forming a polymer layer on a support surface by the use of a coating agent and polymerizable compounds. The coating agent provides photoreactive groups adapted to attach the agent to the surface, as well as photoreactive groups adapted to remain unattached to the surface, and thus serve as photoinitiators for the activation of polymerizable compounds in order to form a polymer layer thereon. Also provided are coating agents, per se, as well as a method of using such agents and the resultant surfaces and devices fabricated therefrom.

Abstract: Provided are processes for the preparation of the compound of the formula 1

Abstract: The present invention relates to nonlinear optical (NLO) materials, compositions thereof and NLO devices using polymeric matrices supporting a second order NLO material defined by the formula ED—B—EW  (I) where ED is an electron donating moiety, B is a bridging moiety, and EW is the electron withdrawing moiety (terminal acceptor group) defined by formula II, where C1 is a carbon atom linked through a double bond to a cyclic or an acylic carbon atom in the bridging moiety, and A1, A2, A3 or A4are the same or different from one another, each of which is an electron withdrawing group such as CN, COR, COOR, COOH or CH═C(R)2 where R is a C1-6 alkyl.

Abstract: Commercially feasible methods for synthesizing various epothilones precursors needed for the preparation of final epothilones are provided, including techniques for the synthesis of epothilone segment A and C precursors. Segment C precursors are prepared using starting nitriles, which can alternately be oxidized to ketones and converted, or reacted to form the diol with subsequent conversion to the segment. Segment A precursors are prepared by reacting a starting enone with a chiral catalyst to give an intermediate alcohol in high enantomeric excess, followed by conversion of the alcohol to the desired Segment A precursor.

Abstract: This disclosure relates to the use of &agr;,&agr;-dibromo-&agr;-chloroacetophenone compounds as intermediates for the preparation of aromatic carbonyl compounds, especially aromatic amides. The compound 2,5-bis(2,2,2-trifluoroethoxy)-&agr;,&agr;-dibromo-&agr;-chloroacetophenone is especially useful as an intermediate for the preparation of flecainide, a known pharmaceutical.

Abstract: The invention deals with the derivatives of benzilidine having basic formula as follows (I): wherein X can be cyclohexanone, cyclopentanone, or acetone, while Y and Z can be either electron withdrawing, electron donating or steric group. Y may or may not be the same with Z. Methyl, ethyl, methoxy group or halogen were prefered in the experiment. The benzilidine cyclohexanone, benzilidine cyclopentanone, and benzilidine acetone derivates were found to be novel compounds showing anti-bacterial, antioxidant, and anti-inflammatory activities that enable them to be used for drug.

Abstract: The invention relates to novel heteroethynylenic compounds having the general formula (I): 1

Abstract: The invention relates to novel phenyl-substituted cyclic ketoenols of the formula (I) in which Het represents one of the groups in which A, B, D, G, X and Z are each as defined in the description, to a plurality of processes and intermediates for their preparation, and to their use as pesticides.

Abstract: This invention is directed to a process for the solid phase synthesis of aldehyde, ketone, oxime, amine, hydroxamic acid and (&agr;,&bgr;-unsaturated carboxylic acid and aldehyde compounds and to polymeric hydroxylamine resin compounds useful therefor.

Abstract: Various epothilone precursors needed for the preparation of final epothilones are provided.

Abstract: Lubricating oil compositions providing superior soot dispersing characteristics, which contain a combination of a high molecular weight dispersant and a soot dispersant comprising a linked aromatic oligomer.

Abstract: The invention relates to a process for preparing substituted arylpyrazoles of the general formula (I) in which R1, R2, R3 and R4 are each as defined in the description, and to novel intermediates for preparing these arylpyrazoles.

Abstract: Inhibitors of the cytosolic phospholipase A2 enzymes are provided which are of use in controlling a wide variety of inflammatory diseases. The inhibitors of the present invention have the general formula where X, Z, R1, R2, R3, R4, Ra and Rb are as defined in the specification.

Abstract: The invention involves the formation of a prodrug from a fatty acid carrier and a neuroactive drug. The prodrug is stable in the environment of both the stomach and the bloodstream and may be delivered by ingestion. The prodrug passes readily through the blood brain barrier. Once in the central nervous system, the prodrug is hydrolyzed into the fatty acid carrier and the drug to release the drug. In a preferred embodiment, the carrier is 4, 7, 10, 13, 16, 19 docosahexa-enoic acid and the drug is dopamine. Both are normal components of the central nervous system. The covalent bond between the drug and the carrier preferably is an amide bond, which bond may survive the conditions in the stomach. Thus, the prodrug may be ingested and will not be hydrolyzed completely into the carrier molecule and drug molecule in the stomach.

Abstract: The invention is directed to multiply-substituted fullerene derivatives of novel configurations, and methods for their preparation and use. The methods involve the combinatorial synthesis of a library of fullerene derivatives and comprises the steps of forming a mixture of fullerene derivatives by reacting the Cn fullerene with two or more reactive precursor compounds, and removing the unreacted compounds to yield the fullerene derivatives having the desired activity. Methods for the identification and screening of a combinatorial library of fullerenes by 3He-nuclear magnetic resonance and electrospray mass spectrometry to define members with the optimal desired activity are also provided.

Abstract: A cyclic anthraquinone process for producing hydrogen peroxide using at least two differently substituted 2-alkylanthraquinones and/or their tetrahydro derivatives. The working solution to be used contains (i) at least one reaction carrier from the series 2-(4-methyl-3-pentenyl) anthraquinone (IHEAQ), 2-(4-methylpentyl) anthraquinone (IHAQ) and their di- and tetrahydro derivatives such as, in particular 2-(4-methylpentyl)-&bgr;-tetrahydroanthraquinone (THIHAQ), and (ii) at least one reaction carrier from the series of the 2-(C1- to C5)-alkylanthraquinones, especially 2-ethylanthraquinone (EAQ), and their tetrahydro derivatives. The reaction carriers according to (i) make up 5 to 95 molar %, especially 20 to 50 molar % of all reaction carrier. The method is distinguished by greater H2O2 capacity, improved hydrogenation kinetics and lesser susceptibility to disturbances. A method for making THIHAQ is also disclosed.

Abstract: The present invention is related to a novel intermediates and processes which are useful in the preparation of certain antihistaminic piperidine derivatives of the formula wherein W represents —C(═O)— or —CH(OH)—; R1 represents hydrogen or hydroxy; R2 represents hydrogen; R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2; n is an integer of from 1 to 5; m is an integer 0 or 1; R3 is —COOH or —COOalkyl wherein the alkyl moiety has from 1 to 6 carbon atoms and is straight or branched each of A is hydrogen or hydroxy; and pharmaceutically acceptable salts and individual optical isomers thereof, with the proviso that where R1 and R2 are taken together to form a second bond between the carbon atoms bearing R1 and R2 or where R1 represented hydroxy, m is an integer 0.

Abstract: The invention relates to a method for producing a novel optically active compound represented by the general formula [IV]. This method includes the step of reacting a vinyl ether with a halogenated acetaldehyde in the presence of an optically active binaphthol-titanium complex. With this, the novel optically active compound can be produced very easily. Furthermore, the novel optically active compound can easily be oxidized to a novel optically active &agr;,&bgr;-dihydrexyketone represented by the general formula [V]. These novel optically active compounds can each be used as useful intermediates.

Abstract: Hybrid electron donor compounds, suitable for use as adhesives or as components in adhesives, contain a carbon to carbon double bond attached to an aromatic ring and conjugated with the unsaturation in the aromatic ring and a vinyl ether moiety.

Abstract: Compounds containing both electron donor and electron acceptor functionality are suitable for use in adhesives. The electron donor group is a carbon to carbon double bond attached to an aromatic ring and conjugated with the unsaturation in the ring. The electron acceptor group is a maleimide, acrylate, fumarate or maleate.

Abstract: The invention discloses ketones of formula I: wherein, Y is an optionally substituted alkyl, cycloalkyl, or cycloalkylalkyl, wherein each alkyl group is straight or branched and each alkyl and cycloalkyl group is saturated or unsaturated; R1 is hydrogen or a C1-6 alkyl group that is substituted, saturated or unsaturated, straight or branched; A is a chromophoric substituted aromatic ring or ring system; n is an integer; and with the proviso that formula I is not 2-ethoxy-1-phenyl-ethanone. These compositions are useful for the delivery of organoleptic compounds, especially of flavors, fragrances, masking agents and antimicrobial compounds.

Abstract: The invention involves the formation of a prodrug from a fatty acid carrier and a neuroactive drug. The prodrug is stable in the environment of both the stomach and the bloodstream and may be delivered by ingestion. The prodrug passes readily through the blood brain barrier. Once in the central nervous system, the prodrug is hydrolyzed into the fatty acid carrier and the drug to release the drug. In a preferred embodiment, the carrier is 4, 7, 10, 13, 16, 19 docosahexa-enoic acid and the drug is dopamine. Both are normal components of the central nervous system. The covalent bond between the drug and the carrier preferably is an amide bond, which bond may survive the conditions in the stomach. Thus, the prodrug may be ingested and will not be hydrolyzed completely into the carrier molecule and drug molecule in the stomach.

Abstract: Acetophenones which are di- or polysubstituted by fluoroalkyl groups on the aromatic ring are prepared in a particularly advantageous manner from the corresponding fluoroalkylanilines and acetaldoxime by preparing a corresponding diazonium salt mixture from the fluoroalkylaniline, reacting this mixture with acetaldoxime in the presence of at least one copper and/or palladium compound, without adding buffer salts or a reducing agent, carrying out the reaction with acetaldoxime at 5 to 50° C. and in the presence of halide ions and at least one strong acid that is not a hydrohalic acid, and finally heating the mixture to a temperature in the range 70 to 160° C.

Abstract: A series of aryl piperazine compounds of the formula: or the pharmaceutically acceptable salts thereof, are effective pharmaceuticals for the treatment of conditions related to or affected by the serotonin 1A receptor; the compounds are particularly effective antagonists at that receptor, and are particularly useful for alleviating the symptoms of nicotine and tobacco withdrawal.

Abstract: This invention provides an improved process for cis-1-{2-[4-(6-methoxy-2-phenyl-1,2,3,4-tetrahydronaphthalen-1-yl)phenoxy]ethyl}pyrrolidine which is an intermediate for the preparation of (-)cis-6-phenyl-5-[4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-5,6,7,8-tetrahydronaphthalene-2-ol which is useful for the treatment of osteoporosis.

Abstract: Xanthene compounds represented by the formula: wherein R1 is a carboxyl group which may be esterified or amidated; R2 is a hydrogen atom, a hydroxyl group, or a hydrocarbon group which may be substituted; R3 and R4 are the same or different and are a hydroxyl group which may be substituted; R5 and R6 are a hydrogen atom or a halogen atom; R7 is a hydrogen atom, a nitro group, a halogen atom, a hydrocarbon group which may be substituted, a heterocyclic group which may be substituted, or an acyl group which may be substituted; n is an integer of 0 to 2; and Y is an oxygen atom or two hydrogen atoms; and when n is 0, R2 may be a group represented by the formula: wherein the symbols have the same meanings as defined above, or a salt thereof inhibit a binding of B7-1 to CD28, prevent the B7-1-dependent activation of T cells and inhibit IL-2 production from T cells, thus being used as an immunomodulator such as a graft rejection inhibitor or a pharmaceutical composition for thera

Abstract: A process for preparing a compound of Formula (I); where Q completes an optionally substituted 5-or 6-member saturated carbocyclic ring and R is optionally substituted phenyl or optionally substituted C3-C6 cycloalkyl which comprises the rearrangement of a compound of Formula (II); where Q and R are as defined in relation to Formula (I) in a polar aprotic, dipolar aprotic or aromatic hydrocarbon solvent in the presence of a moderate base and an azole.

Abstract: A process for the preparation of &agr;-chloromethylene-triorganylphosphorane derivatives I (radicals R are C-organic substituents and A stands for CN or CO-B where B is a C-organic or O-organic radical which is inert under chlorination conditions) by chlorination of phosphoranes II with chlorine, wherein the chlorination is carried out in the presence of a mineral base as hydrogen chloride acceptor and the chlorine and base are fed to the reaction mixture concurrently but separately at the rates at which they are consumed. The reaction products I are important intermediates for plant protectants.

Abstract: Novel pharmaceutically/cosmetically-active aromatic polyenic compounds have the structural formula (I): and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular, bone and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.