Abstract: Disclosed are cyclic dione derivatives represented by formula (I), wherein the substituents are as defined in the description. The preparation method, intermediate and use thereof are also provided.

Abstract: Provided herein are methods of treating or ameliorating hypercholemia or a cholestatic liver disease by administering to an individual in need thereof a therapeutically effective amount of an Apical Sodium-dependent Bile Acid Transporter Inhibitor (ASBTI) or a pharmaceutically acceptable salt thereof. Also provided are methods for treating or ameliorating a liver disease, decreasing the levels of serum bile acids or hepatic bile acids, treating or ameliorating pruritis, reducing liver enzymes, or reducing bilirubin comprising administering to an individual in need thereof a therapeutically effective amount of ASBTI or a pharmaceutically acceptable salt thereof.

Abstract: The application discloses a process for the preparation of 5-deoxy-L-arabinose of formula (VI); comprising the conversion of a compound of formula (XII); wherein n is 0, 1 or 2; which can be used as intermediate for the synthesis of sapropterin.

Abstract: The present invention relates to chemical compounds comprising a [Y(CHRa)n—CH(Ra)SO3]? anion, their preparation and application. The chemical compounds are preferably ionic liquids.

Abstract: A description is given of (4-haloalkyl-3-thiobenzoyl)cyclohexanediones of the formula (I) and of their use as herbicides. In this formula (I), X, Y, R1, R2, R3, and R4 are radicals such as hydrogen and organic radicals such as alkyl. A and Z are oxygen or alkylene.

Abstract: A description is given of (4-trifluoromethyl-3-thiobenzoyl)cyclohexanediones of the formula (I) and of their use as herbicides. In this formula (I), X, R1, R2, R3, and R4 are radicals such as hydrogen and organic radicals such as alkyl. A and Z are oxygen or alkylene.

Abstract: The invention relates to a method for producing 1,4-benzothiepin-1,1-dioxide derivatives substituted with benzyl groups.

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 compounds having formula (I): (I) wherein n, R1-R5, Ra-Rb, Q, Y1 and Y2 are as defined herein; and additionally provides methods for the synthesis thereof, compositions thereof, and methods for the use thereof in the treatment of various disorders including cancer, metastasis and disorders involving increased angiogenesis.

Abstract: A compound represented by the following general formula (II): wherein R21 represents hydrogen atom or one to four monovalent substituents substituting on the benzene ring, and when R21 represents two or more substituents, the substituents may be the same or different; R22, R24, R25, and R27 independently represent hydrogen atom, or a monovalent substituent; R23 represents —OH or —N(R28)(R29) (wherein R28 and R29 independently represent an alkyl group which may be substituted); R26 represents —N(R30)(R31) (wherein R30 and R31 independently represent an alkyl group which may be substituted); n represents an integer of 1 to 3; and Y represents —S— or —O—, which is useful for selective measurement of hypochlorite ion.

Abstract: The invention relates to a method for producing 1,4-benzothiepin-1,1-dioxide derivatives substituted with benzyl groups.

Abstract: A pharmaceutical useful as a therapeutic agent and a preventive agent for hyperlipemia, and a pharmaceutical useful as a therapeutic agent and a preventive agent for hepatic disorders associated with cholestasis, particularly, primary biliary cirrhosis and primary sclerosing cholangitis, and a pharmaceutical useful as a therapeutic agent and a preventive agent for obesity, fatty liver and steatohepatitis are provided.

Abstract: This invention relates to Novel 1,4-benzothiepine 1,1-dioxide derivatives substituted by benzyl radicals, method for their preparation, pharmaceuticals comprising these compounds, and the use thereof.

Abstract: In the liquid immersion lithography process, by simultaneously preventing deterioration of a resist film and deterioration of an immersion liquid employed during liquid immersion lithography which uses various immersion liquids, including water, resistance to post exposure delay of the resist film can be improved without increasing the number of processes, thereby making it possible to form a high resolution resist pattern using liquid immersion lithography. Using an alkaline soluble polymer, a crosslinking agent, and a solvent capable of dissolving them as at least constituent component, a composition is prepared and a protective film is formed on the surface of the resist film to be used, using the composition.

Abstract: Compositions comprising cyclic amino acids or pharmaceutically acceptable salts thereof and a pharmaceutically acceptable carrier. Said composition are for use in the treatment of pain. Pain includes both acute and chronic forms of pain. The preferred cyclic amino acid is 1-aminocyclobutane-1-carboxylic acid (ACBC).

Abstract: This invention relates to Novel 1,4-benzothiepin-1,1-dioxide derivatives which are substituted with cyclohexyl groups, method for producing the same, drugs containing said compounds and use thereof.

Abstract: In the liquid immersion lithography process, by simultaneously preventing deterioration of a resist film and deterioration of an immersion liquid employed during liquid immersion lithography which uses various immersion liquids, including water, resistance to post exposure delay of the resist film can be improved without increasing the number of processes, thereby making it possible to form a high resolution resist pattern using liquid immersion lithography. Furthermore, it is possible to apply a high refractive index liquid immersion medium, used in combination with the high refractive index liquid immersion medium, thus making it possible to further improve pattern accuracy. Using a composition comprising an acrylic resin component having characteristics which have substantially no compatibility with a liquid in which a resist film is immersed, particularly water, and are also soluble in alkaline, a protective film is formed on the surface of a resist film used.

Abstract: The invention relates to substituted benzo-condensed cycloheptanone derivatives, to methods for producing them, to drugs containing said compounds and to the use of said compounds for producing drugs.

Abstract: The present invention relates to novel compounds of general formula (I), their regioisomers, tautomeric forms, novel intermediates involved in their synthesis. The present invention also relates to a process of preparing compounds of general formula (I), their regioisomers, their tautomeric forms, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, and novel intermediates involved in their synthesis.

Abstract: Quaternary salt compounds of Formula (I) or pharmaceutically acceptable forms thereof, which are CCR2 antagonists and are useful in preventing, treating or ameliorating CCR2 mediated inflammatory syndromes, disorders or diseases in a subject in need thereof.

Abstract: The present invention provides curcumol derivatives of the following formula (I) or pharmaceutical acceptable salts thereof: wherein, Y is selected from the group consisting of ?CHR2, —CH2R2, ?O, ?—OH or —OR1;R1 is selected from H, R, RCO or HO3S; and R is selected from the group consisting of H; saturated or unsaturated linear C1-10 hydrocarbon group and the like; R2 is selected from the group consisting of F; Cl; Br; I; H; —OH; —OR; —HSO3 and the like; with the proviso that both R1 and R2 are not H. The present invention also provides anti-tumor or antiviral pharmaceutical compositions comprising said derivatives or pharmaceutical acceptable salts thereof. The present invention further provides the use of said derivatives or pharmaceutical acceptable salts thereof in the preparation of a medicament for prophylaxis and/or treatment tumor or an antiviral medicament.

Abstract: This Invention relates to Novel 1,4-benzothiepin-1,1-dioxide derivatives which are substituted with cyclohexyl groups, method for producing the same, drugs containing said compounds and use thereof.

Abstract: This invention relates to Novel 1,4-benzothiepine 1,1-dioxide derivatives substituted by benzyl radicals, method for their preparation, pharmaceuticals comprising these compounds, and the use thereof.

Abstract: The object of the present invention is, in methods for producing cyclic phenol sulfides, to provide methods for producing a number of more macrocyclic products, which comprise the steps of producing a mixture of cyclic phenol sulfides from an inexpensive raw material in one step without inducing the reduction in yield of a cyclic quatromer; and easily separating and purifying a single component from the mixture of cyclic phenol sulfides. The present invention discloses methods for producing a cyclic phenol sulfide which comprises the step of reacting a phenol compound as a raw material, in a one-step reaction, with 1.7 to 2.5 molar equivalent of sulfur and 0.25 to 0.75 molar equivalent of an alkali metal reagent per 1 mol of the phenol compound to obtain a mixture of cyclic phenol sulfide wherein m=4 and at least one kind(s) of cyclic phenol sulfide wherein m=5 to 9, or each separate cyclic phenol sulfide comprised in the mixture.

Abstract: The present invention discloses an oxidized mixed cyclic phenol sulfide which is a mixture of the oxidized cyclic phenol sulfide wherein m is 8 and the oxidized cyclic phenol sulfide wherein m is an integer other than 8, the oxidized cyclic phenol sulfide being represented by the following formula (1): wherein R is a straight or branched alkyl group having 1 to 6 carbon atoms, m is an integer from 4 to 9, and n is 1 or 2; or an oxidized cyclic phenol sulfide of formula (1) wherein m is 8. The present invention also discloses a charge control agent which comprises the above sulfide(s) as the active ingredient; and a toner which comprises the charge control agent, a coloring agent and a binder resin. This charge control agent is particularly useful for color toners, and it speeds up charging risetime, and has a high charge amount and charging characteristics excellent in environmental stability. Further, the charge control agent is safe since it does not have any problem with the waste regulations.

Abstract: [Problems] To provide an agent useful for the prevention or treatment of various diseases associated with the infection with acyclovir-resistant viruses of the family Herpesviridae, specifically various infectious caused by herpes viruses, such as varicella associated with varicella-zoster virus infection, herpes zoster associated with recurrent infection with latent varicella-zoster virus, and herpes labialis, herpes encephalitis and genital herpes associated with HSV-1 and HSV-2 infection, and the like. [Means for Solving Problems] An N-[2-[(4-substituted phenyl)amino]-2-oxoethyl]tetrahydro-2H-thiopyran-4-carboxamide derivative in which the phenyl group is substituted at position 4 by a specific 5- or 6-membered heteroaryl group. This derivative has an excellent anti-viral activity against acyclovir-resistant herpes viruses and, therefore, is effective for the treatment of the diseases as mentioned above.

Abstract: The present invention relates to methods of treating CNS disorders with a compound of formula I wherein X, R1, R2, R3, R4, R5, R6, R7, and R8 are as defined in the specification and pharmaceutically acceptable acid addition salts thereof.

Abstract: A process for making montelukast, a pharmaceutically useful compound of the following formula and salts thereof: using a compound of formula (11) is provided.

Abstract: This invention to antagonists that inhibit transporters and receptors. The invention also relates to partial inhibitors of transporters and receptors that allow partial transport or partial binding of a compound to the transporter or receptor. The invention also relates to compounds that differentially prevent transport or binding through a transporter or to a receptor. The invention also relates to the use of these compounds for treating certain diseases and disorders.

Abstract: The alicyclic compound of the present invention has a five- or more membered ring structure having an epithioethylene linkage and/or an epidithioethylene linkage, and has tow or more sulfur atoms in its molecule. Optical materials produced by curing the alicyclic compound or a composition containing the alicyclic compound by polymerization show high refractive index.

Abstract: The present invention provides a compound of the formula (I) wherein R1 is —H, —OH, —O(C1-C4 alkyl), —OCOC6H5, —OCO(C1-C6 alkyl), or —OSO2(C2-C6 alkyl); R0, R2 and R3 are each independently —H, —OH, —O(C1-C4 alkyl), —OCOC6H5, —OCO(C1-C6 alkyl), —OSO2(C2-C6 alkyl) or halo; R4 is 1-piperidinyl, 1-pyrrolidinyl, methyl- 1-pyrrolidinyl, dimethyl-1-pyrrolidiny, 4-morpholino, dimethylamino, diethylamino, diisopropylamino, or 1-hexamethyleneimino; n is 2 or 3 X is —S— or —HC?CH—; G is —O—, —S—, —SO—, SO2, or —N(R5)—, wherein R5 is —H or C1-C4 alkyl; and Y is —O—, —S—, —NH—, —NMe—, or —CH2—; or a pharmaceutically acceptable salt thereof; pharmaceutical compositions thereof, optionally in combination with estrogen and progestin; methods of inhibiting a disease associated with estrogen deprivation; and methods for inhibiting a disease associated with an aberrant physiological response to endogenous estrogen.

Abstract: The present invention relates to cyclic sulfone moiety-containing hydroxyethylamine protease inhibitor compounds and pharmaceutical or method of use therefor, particularly as an inhibitor of HIV protease.

Abstract: Provided are novel benzothiepines, derivatives, and analogs thereof; pharmaceutical compositions containing them; and methods of using these compounds and compositions in medicine, particularly in the prophylaxis and treatment of hyperlipidemic conditions such as those associated with atherosclerosis or hypercholesterolemia, in mammals. Also provided are compositions and methods for combination therapy employing ileal bile acid transport inhibitors and HMG Co-A reductase inhibitors for the treatment of hyperlipidemic conditions.

Abstract: The present invention relates to cyclic sulfone moiety-containing hydroxyethylamine protease inhibitor compounds and pharmaceutical or method of use therefor, particularly as an inhibitor of HIV protease.

Abstract: A process for preparing enantiomerically enriched tetrahydrobenzothipeine oxides comprises cyclizing an enantiomerically enriched aryl-3-propanalsulfoxide wherein the sulfur atom of the aryl-3-propanalsulfoxide is a chiral center.

Abstract: Thiepine apical sodium co-dependent bile acid transport (ASBT) inhibitors are disclosed together with methods of making the same, methods of using the same to treat hyperlipidemic conditions as well as pharmaceutical compositions containing the same compounds.

Abstract: The invention relates to photoisomerizable compounds of formula I wherein A, Z, L, R, R1, k, m and r are defined herein.

Abstract: Photoacid generators comprising sulfonium salt compounds represented by the following general formula (2) wherein R1 and R2 represent each an alkyl group optionally having oxo, or R1 and R2 may be cyclized together to form an alkylene group optionally having oxo; R3, R4 and R5 represent each hydrogen or a linear, branched, monocyclic, polycyclic or crosslinked cyclic alkyl group; and Y? represents a counter ion.

Abstract: Provided are novel benzothiepines, derivatives, and analogs thereof; pharmaceutical compositions containing them; and methods of using these compounds and compositions in medicine, particularly in the prophylaxis and treatment of hyperlipidemic conditions such as those associated with atherosclerosis or hypercholesterolemia, in mammals.

Abstract: Mono-flourinated and di-fluorinated benzothiepine apical sodium co-dependent bile acid transport (ASBT) inhibitors are disclosed together with methods of making the same, methods of using the same to treat hyperlipidemic conditions as well as pharmaceutical compositions containing the same compounds.

Abstract: Substituted benzothiepine 1,1-dioxide derivatives of formula I: in which R1, R2, R3, R4, R5 and Z have the meanings indicated, and their physiologically tolerable salts and physiologically functional derivatives and a process for their preparation are described. The compounds are suitable, for example, as hypolipidemics.

Abstract: Thiepine apical sodium co-dependent bile acid transport (ASBT) inhibitors are disclosed together with methods of making the same, methods of using the same to treat hyperlipidemic conditions as well as pharmaceutical compositions containing the same compounds.

Abstract: Compounds of general formula (1) R1—X1—W—X2—Z1—Z2—R2 or salts thereof, exhibiting preventive and therapeutic effects against HIV infectious diseases wherein R1 is an optionally substituted five- or six-membered ring group; X1 is a free valency or the like; W is a divalent group represented by, e. g., general formula (2) (wherein A and B are each an optionally substituted five- to seven-membered ring; E1 and E4 are each optionally substituted carbon or the like; E2 and E3 are each oxygen or the like; and a and b are each a single bond or a double bond); X2 is a divalent group constituting a straight chain moiety; Z1 is a divalent cyclic group or the like; Z2 is a free valency or the like; and R2 is optionally substituted amino or the like.

Abstract: The present invention provides compounds of formula (I): 1

Abstract: Among its several embodiments, the present invention provides an improved process for the preparation of tetrahydrobenzothiepine-1,1-dioxide compounds; the provision of a process for preparing a diastereomeric mixture of tetrahydrobenzothiepine-1,1-dioxide compounds from a single diastereomer of such compounds; the provision of a process for the preparation of 3-bromo-2-substituted propionaldehyde compounds; and the provision of a process for the preparation of 3-thio-2-substituted propionaldehyde compounds.

Abstract: The present invention relates to cyclic sulfone moiety-containing hydroxyethylamine protease inhibitor compounds and pharmaceutical or method of use therefor, particularly as an inhibitor of HIV protease.

Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.

Abstract: This invention relates to new selective retinoid acid receptor agonists of formula I wherein the symbols are as defined in the specification to their pharmaceutically acceptable salts, individual isomers or to a racemic or non-racemic mixture; to pharmaceutical compositions containing them, and to methods for their use as therapeutic agents.

Abstract: Matrix metalloproteinases (MMPs) are a group of enzymes that have been implicated in the pathological destruction of connective tissue and basement membranes. These zinc containing endopeptidases consist of several subsets of enzymes including collagenases, stromelysins and gelatinases. TNF-&agr; converting enzyme (TACE), a pro-inflmatory cytokine, catalyzes the formation of TNF-&agr; from membrane bound TNF-&agr; precursor protein. It is expected that small molecule inhibitors of MMPs and TACE therefore have the potential for treating a variety of disease states.

Abstract: The present invention relates to compounds of the general formula (I) 1