Abstract: Disclosed herein is a novel process for preparation of atovaquone. The process includes reacting 1,4-naphthoquinone with trans-4-(4-chlorophenyl) cyclohexane carboxylic acid followed by halogenation to obtain a dihalo-compound. Further, dehydrohalogenation of the dihalo-compound produces a monohalogeno-compound which under goes hydrolysis to produce atovaquone. The invention also discloses atovaquone in a substantially pure and well defined polymorphic form designated as “Form IPCA-ATO,” and the preparation thereof.

Abstract: Methods of using apogossypol and its derivatives for treating inflammation is disclosed. Also, there is described a group of compounds having structure A, or a pharmaceutically acceptable salt, hydrate, N-oxide, or solvate thereof are provided: wherein each R is independently H, C(O)X, C(O)NHX, NH(CO)X, SO2NHX, or NHSO2X, wherein X is hydrogen, alkyl, substituted alkyl, aryl, substituted aryl, alkylaryl, substituted alkylaryl, heterocycle, or substituted heterocycle. Compounds of group A may be used for treating various diseases or disorders, such as cancer.

Abstract: Disclosed is a method for preparing a compound of Formula 1 wherein R1 is CHX2, CX3, CX2CHX2 or CX2CX3; each X is independently Cl or F; Z is optionally substituted phenyl; and Q is phenyl or 1-naphthalenyl, each optionally substituted as defined in the disclosure; comprising contacting a compound of Formula 2 with hydroxylamine in the presence of a base. The present invention also relates to novel compounds of Formula 2, useful as starting materials for the aforedescribed method.

Abstract: This invention relates to ?-hydroxyketones and ?-alkoxyketones of formula (I), to their use as estrogen receptor modulators, and to methods for their preparation.

Abstract: Compounds that have agonist activity at one or more of the S1P receptors are provided. The compounds are sphingosine analogs that, after phosphorylation, can behave as agonists at S1P receptors.

Abstract: The invention relates to quinoid compounds and their use in semiconductive matrix materials, electronic and optoelectronic structural elements.

Abstract: The present invention relates to two novel and stable crystalline forms of atovaquone, to processes for their preparation and to pharmaceutical compositions comprising them. The present invention also provides crystalline particles of atovaquone having a specific surface area of from about 0.7 m2/g to about 4 m2/g, methods for the manufacture of said crystalline particles and pharmaceutical compositions comprising said crystalline particles. The present invention further provides an improved and commercially viable process for preparation of atovaquone substantially free of its undesired isomeric impurity, namely cis-2-[4-(4-chlorophenyl)cyclohexyl]-3-hydroxy-1,4-naphthoquinone.

Abstract: Disclosed are compounds having the ability to inhibit cytochrome P450 2A6, 2A13, and/or 2B6 and tobacco products comprising them. Also disclosed are pharmaceutical compositions comprising them.

Abstract: Disclosed are compounds having the ability to modulate, namely to improve, enhance and or modify fragrance compositions due to their ability to inhibit cytochrome P450 enzymes, e.g. CYP2A13 and CYP2B6.

Abstract: This invention provides a pharmaceutical and functional food which are made of a safe food ingredient or nutrient which has been used for a long period of time, and which have tranquilizing effect such as anti-anxiety effect, anti-depression effect, and anti-stress effect. The tranquilizer of the invention contains vitamin K as an active ingredient. Vitamin K is preferably menaquinone-4 and/or menaquinone-7. This invention also provides a supplement, health food or functional food for tranquilizing purpose that contains vitamin K as an active ingredient.

Abstract: Compositions suitable for use as signal generation components of an immunoassay, and methods for their use. According to one aspect of the invention, the composition includes a carrier having a coating of an aminodextran and a metal chelate incorporated therein. The metal chelate is present in the amount of at least 0.065 ?Mole per gram of carrier, and the aminodextran coating density averaging at least about 45 ?g per milligram of carrier. In another aspect of the invention, carrier is dyed with a complex having the formula: M(L1)x(L2)y, wherein M is a metal selected from the group consisting of europium, terbium, dysprosium, samarium, osmium and ruthenium; L1 is a ligand selected from the group consisting of DPP, TOPO, TPPO; L2 comprises a ligand having the formula wherein R is one or more substituents, each substituent comprising an electron donating group; n=2-10; x=1-2; and y=2-4.

Abstract: Disclosed herein is a novel process for preparation of atovaquone. The process includes reacting 1,4-naphthoquinone with trans-4-(4-chlorophenyl) cyclohexane carboxylic acid followed by halogenation to obtain a dihalo-compound. Further, dehydrohalogenation of the dihalo-compound produces a monohalogeno-compound which under goes hydrolysis to produce atovaquone. The invention also discloses atovaquone in a substantially pure and well defined polymorphic form designated as “Form IPCA-ATO,” and the preparation thereof.

Abstract: Novel perfluoroketone compounds of formula [I] and [Ia] are described. Also described are uses thereof, such as for inhibition of phospholipase A2 activity. Therapeutic uses thereof are also described, such as for the treatment of neural conditions and/or inflammatory conditions, such as demyelinating (e.g., multiple sclerosis) and neural injury (e.g., spinal cord injury).

Abstract: The present invention provides a novel material capable of realizing excellent color purity of blue, a light-emitting element and a light-emitting device using the novel material. The present invention provides an oligonaphthalene derivative represented by the formula (1). The oligonaphthalene derivatives of the present invention have an extremely large band gap, can emit light with extremely short wavelength, and can emit blue light with favorable color purity. In addition, a light-emitting element that can exhibit excellent color purity of blue can be obtained by applying this material to the light-emitting element or a light-emitting device; therefore the light-emitting element having superior color reproducibility can be provided.

Abstract: Compounds of general formula I: wherein: R1 and R2 are, independently of each other, selected from hydrogen, optionally substituted C1-10alkyl, optionally substituted —CO—(C1-10alkyl), optionally substituted C3-10cycloalkyl, optionally substituted —CO—(C3-10cycloalkyl), optionally substituted C2-10alkenyl, optionally substituted —CO—(C2-10alkenyl), optionally substituted aryl, and optionally substituted —CO-aryl, or R1 and R2 together represent an optionally substituted saturated or unsaturated C1-10alkylidene group, or an optionally substituted saturated or unsaturated C3-10cycloalkylidene group, or R1 and R2 together with the carbon atom to which they are attached represent an optionally substituted saturated or unsaturated organic ring containing 3, 4, 5, 6, 7 or 8 ring carbon atoms and optionally 1, 2 or 3 ring heteroatoms selected from O, N and S; R3, which may be the same as, or different from, either of R1 and R2, is selected from optionally substituted C1-10alkyl, optionally substituted C3-10cycl

Abstract: The present invention is directed to labeled compounds, of the formulae wherein C* is each independently selected from the group consisting of 13C and 12C with the proviso that at least one C* is 13C, each hydrogen of the methylene group can independently be either hydrogen or deuterium, the methyl group includes either zero or three deuterium atoms, Q is from the group of sulfide, sulfinyl, and sulfone, Z is an aryl group from the group of 1-naphthyl, substituted 1-naphthyl, 2-naphthyl, substituted 2-naphthyl, and phenyl groups with the structure wherein R1, R2, R3, R4 and R5 are each independently from the group of hydrogen, a C1-C4 lower alkyl, a halogen, and an amino group from the group of NH2, NHR and NRR? where R and R? are each independently from the group of a C1-C4 lower alkyl, a phenyl, and an alkoxy group, and the methyl group can include either zero or three deuterium atoms.

Abstract: The invention provides methods and compositions for treating and preventing a skin rash secondary to anti-epidermal growth factor receptor (EGFR) therapy, where the method comprises applying a vitamin K analog or a phosphatase inhibitor to the skin.

Abstract: It is found that compounds having PPAR? agonistic activity induced abnormal blood coagulation or muscular disorder. A pharmaceutical combination comprising vitamin K and a compound having PPAR? agonistic activity can prevent the abnormal blood coagulation. A pharmaceutical composition comprising vitamin K can prevent muscular disorder.

Abstract: The present invention provides a process for the preparation of atovaquone exhibiting characteristic peaks (expressed in degrees 2?±0.2°?) at approximately one or more of the positions: about 7.0, 9.7, 14.2, 14.8, 17.0, 19.2, 20.4, 22.1, 22.7, 26.9 and 28.7, which comprises: (a) providing a solution comprising atovaquone in an aprotic polar solvent; (b) adding a suitable antisolvent to precipitate atovaquone; and (c) isolating the precipitate.

Abstract: Methods of using apogossypol and its derivatives for treating inflammation is disclosed. Also, there is described a group of compounds having structure A, or a pharmaceutically acceptable salt, hydrate, N-oxide, or solvate thereof are provided: wherein each R is independently selected from the group consisting of H, C(O)X, C(O)NHX, NH(CO)X, SO2NHX, and NHSO2X, wherein X is selected from the group consisting of an alkyl, a substituted alkyl, an aryl, a substituted aryl, an alkylaryl, and a heterocycle. Compounds of group A may be used for treating various diseases or disorders, such as cancer.

Abstract: The present invention relates to atovaquone particles having d90 value of about 4-15 ?m. It further relates to a pharmaceutical composition comprising said particles.

Abstract: The present invention is directed to compounds having the structure Formula (I) wherein R1, R2, R3, R4, R5 and m are as defined herein. The compounds of this invention are novel therapeutic agents for the treatment of cancer, metabolic diseases and skin disorders in mammalian subjects. These compounds are also useful modulators of gene expression. They exert their activity by interfering with certain cellular signal transduction cascades. The compounds of the invention are thus also useful for regulating cell differentiation and cell cycle processes that are controlled or regulated by various hormones or cytokines. In particular, the invention relates to compounds that induce apoptosis of cancer cells and therefore may be used for the treatment or prevention of cancer, including advanced cancers and pre-cancerous cells. The invention also discloses pharmaceutical compositions and methods of treatment of disease in mammals.

Abstract: This invention provides aryl-substituted acyclic enediyne compounds of formula (I): or a pharmaceutically acceptable salt or solvate thereof, wherein R1=R2=H; or R1 and R2 together form a moiety represented by the formula R3 represents a substituted or unsubstituted alkyl having 4-30 carbon atoms, or a substituted or unsubstituted aryl group having 3-30 carbon atoms; and R4 represents a substituted or unsubstituted aryl group having 3-30 carbon atoms; with the proviso that R3 is not butyl, pentyl, tetrahydropyranyloxymethyl, tetrahydropyranyloxypropyl or phenyl when R1=R2=H and R4 is o-cyanophenyl,; and with the proviso that R3 is not butyl when R1=R2=H and R4 is phenyl. The compounds of formula (I) are found to have inhibitory activities against topoisomerase I or act as a S phase or G2/M phase blocker.

Abstract: The present invention relates to a process for producing 5-nitro-3,4-dihydro-1(2H)-naphthalinone, 1,5-naphthalenediamine and 1,5-naphthalene diisocyanate, in which 4-(2-nitrophenyl)-n-butyronitrile is converted to 4-(2-nitrophenyl)-n-butyric acid.

Abstract: There is provided a process for producing an aromatic compound by Friedel-Crafts reaction product, which comprises reacting an aromatic compound with an ester compound in the presence of a heteropolyacid-containing solid acid catalyst.

Abstract: ?-diketone fluorescent tags are disclosed, particularly those enabling the use of excitation energy in the near visible or visible spectrum. In some cases, these tags allow the use of cost-effective excitation devices such as LED's. The compounds form fluorescent chelates (complexes) with lanthanide (III) rare earth metal ions (such as Eu3+). The fluorescent complex may be included in a latex microparticle, such as a styrene latex particle. Ideally, the complex has an absorption maximum ? equal to or greater than 360 nm, and the compound is characterized by a pKa<9.0. Kits and methods for detecting target molecules (e.g. immunoassays) are also disclosed. Such methods and kits typically use a ligand for binding to the target molecule and a labeling agent attached to the ligand. The fluorescent complexes described above are at least part of the labeling agent.

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: This invention provides estrogen receptor modulators of formula I, having the structure wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10, are as defined in the specification, or a pharmaceutically acceptable salt thereof.

Abstract: To provide a practical method of manufacturing fluorine compounds in a small number of steps that can carry out fluorination reaction of substrates using easily available fluorinating agents that can be inexpensively produced industrially, and recover precursors of the fluorinating agents generated accompanying the reaction quantitatively in an easy operation, and a method of recovery and regeneration of the precursors of the fluorinating agents. N-Fluoro-quaternary-nitrogen-onium tetrafluoroborate salts represented by the general formula (1) as the fluorinating agents are used. N-Hydro-quaternary-nitrogen-onium tetrafluoroborate salts represented by the general formula (2) generated accompanying the reaction are separated and recovered from the reaction mixture by means of depositing as crystals by the addition of solvents with a low affinity to the salts to the reaction mixture after the reaction.

Abstract: A method for the preparation of aryl methyl ketones converts a variety of ethyl arenas to the corresponding aryl methyl ketones using a dioxygen-containing gas as the oxidant. The catalyst used for the reaction is a metal complex bearing general formulas as disclosed.

Abstract: The invention relates to a process for the production of microfluidized particles of atovaquone having improved bioavailability.

Abstract: Aldose redcutase inhibitor and pharmaceutically acceptable derivatives thereof of the formula I below derived from cultures of Aspergillus niger CFR 1046 and useful as a rat lens aldose reductase inhibitor 1

Abstract: The present invention relates to a process for preparing 1-indanones of formula I: and isomers thereof, wherein R1, R2, R3, R4, R5, and R6 independently represent H or a C1-C20 hydrocarbon group or R1 and R2 or R2 and R3 or R3 and R4 and/or R5 and R6 together with the carbon atoms to which they are attached form a saturated or unsaturated 5- or 6-membered ring, said hydrocarbon group and/or said ring optionally containing one or more hetero atoms, said ring optionally being substituted with a C1-C4 hydrocarbon group, said process comprising reacting a compound of formula II: wherein R1, R2, R3, R4, R5, and R6 have the same meaning as defined above, with a chlorinating agent, followed by reaction with a Friedel-Crafts catalyst. The invention further relates to the preparation of the corresponding indenes.

Abstract: The present invention is a fragrance precursor of formula I: for a fragrant ketone of formula II: and a fragrant ester of formula III: wherein, R1 to R5 represent independently H, —NO2, linear or branched C1-C6-alkyl, C1-C6-alkenyl, C1-C6-alkinyl or C1-C4-alkoxy, R1 and R2,R2 and R3, R3 and R4, and R4 and R5 may form together one or two aliphatic or aromatic rings, R6 and R7 are independently H, linear or branched C1-C6-alkyl-, C1-C6-alkenyl, C1-C6-alkinyl, and R8 and R9 are the residues of an acid R8-COOH and an alcohol R9OH respectively forming the fragrant ester of formula III. A method for providing an odor by admixing with a product a fragrance precursor as detailed above.

Abstract: The present invention provides a liquid phase process for the acylation of aromatic compound by an acylating agent of the formula (R5R6R7)—Y—Z to obtain the corresponding acylated compound using a solid catalyst comprising a metal oxide of the formula AOx with or without a catalyst support, wherein A is a metallic element selected from Ga, In, Ti, Fe and a mixture of two or more thereof, and x is the number of oxygen atoms required to fulfil the valance requirement of A, wherein the catalyst is pretreated with a dry gas comprising a hydrogen halide in the presence or absence of the aromatic compound to be acylated, contacting the hydrogen halide pretreated catalyst with a liquid reaction mixture comprising the aromatic compound and the acylating agent, cooling the reaction mixture, removing the catalyst from the reaction mixture and then separating the reaction products from the reaction mixture.

Abstract: The invention relates to new compounds of the formula (I) in which R is phenyl, C1-4alkyl-, C1-4alkoxy- or halogen-substituted phenyl, naphthyl or an aromatic ring containing heteroatoms; X is O or S; R1 and R2 are each a methyl radical or R1 and R2 together are a C4-8alkylene radical; Y is hydroxyl, C1-12alkoxy, C1-4alkylamino, di-C1-4alkylamino or a piperidine or morpholine ring that is attached by its nitrogen atom; to a process for preparing them and to their use as photoinitiators and/or photosensitizers.

Abstract: This invention relates to a novel, inventive process for the preparation of biphenyls or aromatic olefins by coupling reactions of the Suzuki coupling and Heck coupling type, using allylpalladium catalysts of the &mgr;-halo(triisopropylphosphine)(&eegr;3-allyl)palladium(II) type.

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: Biradical initiators and methods using the same are disclosed. Polymerization of compositions which include the compounds of the invention may be activated by irradiating the composition with radiation.

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 present invention relates to novel 2-aryl-3-hydroxy-&Dgr;2-cyclopentene-1-one derivatives of the formula (I) in which A, B, D1, D2, G, W, X, Y and Z are each as defined in the description, to processes for their preparation and to their use as herbicides and pesticides.

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: A method for acylating an aromatic compound, specifically an activated or deactivated aromatic compound, is disclosed. The method is suitable for preparing aromatic ketones. The preparation of a catalyst and novel bismuth compounds is also disclosed. Said aromatic compound acylation method comprises reacting said aromatic compound with an acylating agent in the presence of a catalyst, and is characterised in that the acylation reaction is performed in the presence of an effective amount of at least one bismuth salt of trifluoromethanesulphonic acid.

Abstract: Methoxy and ethoxy substituted 3-aroyl-2-arylbenzo[b]thiophenes and benzo[b]thiophene analogues are described for use in inhibiting tubulin polymerization. The compounds' use for treating tumor cells is also described.

Abstract: The present invention provides compounds of formula I: ##STR1## wherein R.sup.1 is hydrogen or methyl and R.sup.2 is alkyl. These compounds are useful as fixatives in fragrance compositions. Processes of making such compounds are also provided.

Abstract: Found is a pharmaceutical preparation which provides Tamoxifen Citrate in a liquid dosage form, viz. as an oral solution. The finding is based on a solvent comprising the following components: (a) of from 10% to 20% by weight of ethanol, (b) of from 10% to 60% by weight of a glycol; and (c) water, optionally containing additives, in a volume percentage adding up to 100% by volume. A preferred additive is sorbitol.

Abstract: Optically pure enantiomers of avarol are obtained. The enantiomers of avarol are demonstrated to be highly effective inhibitors of .alpha.-glucosidase and .alpha.-mannosidase. Other enzymes assayed were not inhibited by these optically pure compounds. Inhibition of these two enzymes is useful for a variety of assays and probes, and offers particular utility in the treatment of retroviral infection-associated syndromes, such as AIDS.

Abstract: A compound comprising a non-steroidal antiinflammatory agent to which is directly or indirectly linked an NO group, a pharmaceutical composition including the compounds and methods of treatment of pain and/or inflammation using the compounds and compositions are disclosed. Also disclosed is a composition comprising a non-steroidal antiinflammatory agent and a compound that donates, transfers or releases nitric oxide.

Abstract: Tetralone derivatives of the formula ##STR1## where R.sup.1 is halo, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, (aryl)alkenyl, (aryl)alkynyl, alkoxy, O-alkenyl, O-aryl, O-alkyl(heterocyclo), COO-alkyl,alkanoyl, CO-amino, CO-substituted amino, alkyl-CO-amino, alkyl-CO-substituted amino, NHCO-alkyl, NHCO-aryl, NHCO-alkyl(heterocyclo), N(alkyl)CO-alkyl, N(alkyl)CO-aryl, N(alkyl)CO-heterocyclo, N(alkyl)CO-alkyl(heterocyclo);R.sup.2 is hydrogen, alkyl, halo, aryl, alkoxy, amino, substituted amino;R.sup.3 is oxo, hydroxy, alkoxy, O--COalkyl, --O--COaryl, --O--COheterocyclo, NOH, NO-alkyl, N-amino, N-substituted amino, N-NHCONHalkyl, N-NHSO.sub.2 alkyl, N-NHSO.sub.2 aryl, amino, substituted amino, NHCO-alkyl, NHCO-aryl, NHCO-heterocyclo, spiroheterocyclo;R.sup.4 is hydrogen, alkyl, alkyl(COalkyl), alkyl(COOalkyl); orR.sup.3 and R.sup.4 taken together with the atoms to which they are attached form a five- to seven-membered ring which can contain up to three heteroatoms selected from oxygen, nitrogen and sulfur;R.sup.

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.