Abstract: This invention relates to compounds of the formula wherein X is N and Y is S or O; or X is S or O and Y is N; R1 is hydrogen or C1-7-alkyl; R2 and R3 independently from each other are selected from the group consisting of hydrogen, C1-7-alkyl and C1-7-alkoxy; R4, R5, R6, and R7 independently from each other are selected from the group consisting of hydrogen, C1-7-alkyl, C3-7-cycloalkyl, halogen, C1-7-alkoxy, C1-7-alkyl-C1-7-alkoxy-C1-7-alkyl, C2-7-alkenyl, C2-7-alkinyl, fluoro-C1-7-alkyl and cyano; R8 is selected from the group consisting of hydrogen, C1-7-alkyl, C3-7-cycloalkyl and fluoro-C1-7-alkyl; R9 is selected from the group consisting of hydrogen, C1-7-alkyl, C2-7-alkinyl, C3-7-cycloalkyl and fluoro-C1-7-alkyl; R10 is selected from the group consisting of hydrogen, C1-7-alkyl, C2-7-alkinyl, C3-7-cycloalkyl and fluoro-C1-7-alkyl; R11 is aryl or heteroaryl; N is 0, 1 or 2; and all enantiomers and pharmaceutically acceptable salts and/or esters thereof and their use as PPAR activators.

Abstract: The present invention provides a photochromic compound that is colored when irradiated with visible light and quickly faded when set in a dark place. The photochromic compound according to the present invention is expressed by the following general formula (I): where each of A1, A2 and A3 is a five-member rings forming a 6?-electron system, the three rings being identical, partially identical or totally different from each other, and each ring may have a substituent; B1 and B2 are functional groups, each having an atomic number of five or larger, including a ring compound, and bonded to the 2-carbon of each of A2 and A3, respectively; and R1, R2 and R3 are substituents identical to or different from each other. This compound is highly colorable and durable even when it is dispersed into plastic macromolecular materials. Therefore, it is suitable as a dye material for sunglasses or similar products.

Abstract: The present invention relates to compounds of the Formula: wherein R1 to R6, X, Z and A are as defined. These compounds have activity inhibiting production of A?-peptide. The invention also relates to pharmaceutical compositions and methods for treating diseases, for example, neurodegenerative diseases, e.g., Alzheimer's disease, in a mammal comprising compounds of the present Formula.

Abstract: Electron acceptor compounds, nonlinear optical chromophores, methods for making the compounds and chromophores, and materials and electro-optic devices that include the chromophores.

Abstract: The present invention relates to substituted thiazole derivatives that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin and MCAK activity, and for inhibiting KSP kinesin and MCAK. The invention also relates to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.

Abstract: Provided herein are novel substituted thiazoles and oxazoles of the Formula (I): as well as compositions, including pharmaceutical compositions, containing the same, and the use thereof in the treatment of various neurological and psychological disorders, e.g., affective disorder, anxiety and depression, treatable by antagonizing CRF receptors.

Abstract: Novel pesticides of formula (I) wherein the substituents, R, R1, R2, R2?, T, U, X and Y are as defined in claim 1, are described. Also described are compositions suitable for use as parasiticides comprising those compounds as active ingredient and to methods of controlling parasites that are based on the administration of those compounds or compositions, and to the use of the said compounds and compositions in a method of controlling parasites and in the manufacture of pesticides for use against parasites. Also described are intermediates of formula (XX) wherein R1, R2, R2?, T, U, X and Y are as defined in claim 1; and Hal is halogen. The latter also exhibit parasiticidal activity and are suitable for the preparation of the compounds of formula (I).

Abstract: A compound of the formula Ia or Ib; where, in the formula Ia, E1 is O, S, Se, Te, NR, CR2, or PR; E2, E3 are each CR, N, or P; E4 is N, or P; E5 is OH, SH, NHR, OR?, SR?, or NRR?; E6 is NH, PH, NR?, or PR?; R5, R6 are each hydrogen or a linear, branched or cyclic alkyl radical or an aryl radical; R1, R2, R3, R4 are each hydrogen, a linear, branched or cyclic alkyl radical, an aryl radical, a halogen or a nitro group; R is hydrogen, a linear, branched or cyclic alkyl radical; R? is a linear, branched or cyclic alkyl radical; where at least one of the groups E5 and E6 contains a hydrogen atom; and in the formula Ib, the symbols E1, E4, E5, E6, R5, R6, R1, R2, R3, R4, R and R? are as defined in formula Ia; and E?2 and E?3 are each O, S, Se, Te, NR, CR2, or PR.

Abstract: Compounds represented by Formula (I): or pharmaceutically acceptable salts thereof, are effective as NMDA NR2B antagonists useful for relieving pain.

Abstract: There are presented compounds of formula (I) their pharmaceutically acceptable salts, enantiomeric forms thereof, diastereoisomers and racemates, the preparation of the above-mentioned compounds, medicaments containing them and their manufacture, as well as the use of the above-mentioned compounds in the control or prevention of illnesses such as cancer.

Abstract: The pharmaceutical composition comprising the compound of the invention having 8-azaprostaglandin skeleton represented by formula (I) (wherein, all the symbols have the same meanings as that of the specification) a salt thereof, a solvate thereof or a cyclodextrin clathrate thereof, or a prodrug thereof and them as active ingredient have EP4 agonistic action and thus are considered useful for the prevention and/or treatment of immunological diseases, asthma, neuronal cell death, arthritis, lung failure, pulmonary fibrosis, pulmonary emphysema, bronchitis, chronic obstructive pulmonary disease, liver damage, acute hepatitis, nephritis, renal insufficiency, hypertension, myocardial ischemia, systemic inflammatory response syndrome, sepsis, hemophagous syndrome, macrophage activation syndrome, Still's disease, Kawasaki disease, burn, systemic granulomatosis, ulcerative colitis, Crohn's disease, hypercytokinemia at dialysis, multiple organ failure, shock and glaucoma, etc.

Abstract: The invention relates to a process for the preparation of liquid, storage-stable isocyanate mixtures of low color number and which contain carbodiimide (CD) and/or uretonimine (UI) groups, the isocyanate mixtures obtainable by this process, and to a process for the preparation of blends of these isocyanates with additional isocyanate components and to a process for the preparation of prepolymers containing isocyanate groups and of polyurethane plastics, preferably polyurethane foams.

Abstract: Novel compounds, compositions, and kits are provided. Methods of modulating A? levels, and methods of treating a disease associated with aberrant A? levels are also provided.

Abstract: The present invention relates to compounds of the formula in which the variables G, W, Q, X, Y, B1, B2, Z1, Z2, and R1–R7 are as defined herein, methods for the preparation of the derivatives and intermediates thereof.

Abstract: This invention concerns the use of a compound of formula (I?), a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein Z is halo; C1-6alkyl; C1-6alkylcarbonyl; C1-6alkyloxy -carbonyl; aminocarbonyl; C1-6alkyl substituted with hydroxy, carboxyl, cyano, amino, amino substituted with piperidinyl, amino substituted with C1-4alkyl substituted piperidinyl, mono- or di(C1-6alkyl)amino, aminocarbonyl, mono- or di(C1-6alkyl)aminocarbonyl, C1-6alkyloxycarbonyl, C1-6alkyloxy, piperidinyl, piperazinyl, morpholinyl, thiomorpholinyl; polyhaloC1-4alkyl; cyano; amino; mono- or di(C1-6alkyl)aminocarbonyl; C1-6alkyloxycarbonyl; C1-6alkylcarbonyloxy; aminoS(?O)2—; mono- or di(C1-6alkyl)aminoS(?O)2; —C(?N—Rx)NRyRz; Q is optionally substituted C3-6cycloalkyl, phenyl, pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, benzthiazolyl, benzoxazolyl, benzimidazolyl, indazolyl, or imidazopyridyl, or Q is a radical of formula (b-1), (b-2), or (b-3), L is optionally subs

Abstract: A process for the preparation of a compound of formula (I) wherein Q is CH or N; Y is NO2 or CN; Z is CHR3, O, NR3 or S; R1 and R2 are C1-C8 alkyl or together form an alkylene bridge having two or three carbon atoms; by reacting a compound of formula H2C=C(X)CH2NCS wherein X is a leaving group, with a chlorinating agent in the presence of a catalytic amount of SO2. to form a compound of formula (III) and the compound of formula (III) is reacted with a compound of formula R1NHC(=QY)ZR2 wherein R1, R2, Y, Z and Q are as defined for compound (I).

Abstract: The present invention relates to inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention, processes for preparing the compounds and methods of using the compositions in the treatment of various disorders.

Abstract: The present invention relates to new bromo- and chlorothiazolium salts of the formula (I) in which R1, R2, R3, R4, n and X? have the meaning indicated in the disclosure, a process for their preparation, their use as condensation reagents, particularly as peptide coupling reagents, and intermediates for the preparation of these compounds.

Abstract: Compounds of formula I: inhibit gamma-secretase and hence find use in treatment of Alzheimer's disease.

Abstract: Designed epoxide and cyclopropane epothilone analogs with substituted side-chains are disclosed and characterized with respect to their biological activities against a series of human cancer cell lines. Among the several bioactive analogs, the epothilone B analog with a thiomethyl thiazole ring stands out as the most potent.

Abstract: The present invention is directed to compounds of formula (I), or a pharmaceutically suitable salt or prodrug thereof, which are useful for the selective inhibition of protein tyrosine phosphatase-1B (PTP1B), and are useful for the treatment of disorders caused by overexpressed or altered protein tyrosine phosphatase 1B.

Abstract: The present invention relates generally to the field of anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents. More particularly, the invention relates to a family of compounds having both a biaryl moiety and at least one heterocylic moiety that are useful as such agents.

Abstract: The present invention relates to prodrugs of pharmacologically active five-membered heterocyclic amidines from which are produced in vivo compounds which are competitive inhibitors of trypsin-like serine proteases, in particular thrombin and kininogenases such as kallikrein, to the preparation thereof and to the use thereof as medicines. The invention also relates to pharmaceutical compositions which comprise the prodrugs of the active compounds as ingredients, and to the use of the compounds as thrombin inhibitors, anticoagulants and as antiinflammatory agents.

Abstract: This invention provides compounds of Formula I having the structure or a pharmaceutically acceptable salt thereof, which are useful in treating metabolic disorders related to insulin resistance or hyperglycemia.

Abstract: The present invention relates to phthalimide carboxylic acid derivatives of formula (I), methods for their preparation, pharmaceutical compositions containing them and their use in medicine, specifically in the treatment of cancer. (I), wherein X is O or S; R1 is a phthalimide carboxylic acid group of formula (II).

Abstract: The present invention relates to compounds of formula (I) wherein R1, R2, R3, R4, R5, R6 and R7 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prophylaxis of diseases which are associated with the modulation of CB1 receptors.

Abstract: The invention relates to novel imidazolamino compounds. Also disclosed are methods of treating cancer by using one of these compounds and pharmaceutical compositions containing one of these compounds.

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

Abstract: The present invention relates to new bromo- and chlorothiazolium salts of the formula (I) in which R1, R2, R3, R4, n and X? have the meaning indicated in the disclosure, a process for their preparation, their use as condensation reagents, particularly as peptide coupling reagents, and intermediates for the preparation of these compounds.

Abstract: The present invention relates to new hetaryl-substituted homotetramic and homotetronic acids of the formula (I) in which A, B, Q1, Q2, W, G and Het have the meanings stated in the disclosure, to a plurality of processes for their preparation, and to their use as pesticides, microbicides, and herbicides.

Abstract: The present invention relates to compositions and methods for inhibiting and reversing nonenzymatic cross-linking (protein aging). Accordingly, compositions are disclosed which comprise an agent capable of inhibiting the formation of advanced glycosylation endproducts of target proteins, and which additionally reverse pre-formed crosslinks in the advanced glycosylation endproducts by cleaving alpha-dicarbonyl-based protein crosslinks present in the advanced glycosylation endproducts. Certain useful agents are thiazolium salts. The method comprises contacting the target protein with the composition. Both industrial and therapeutic applications for the invention are envisioned, as food spoilage and animal protein aging can be treated. A novel immunoassay for detection of the reversal of the nonenzymatic crosslinking is also disclosed.

Abstract: The invention concerns drug precursors with antimalarial effect, characterised in that it consists in quaternary bis-ammonium salts of general formula (I) wherein A and A?, identical or different, are respectively either a group A1 and A?1 of formula (1) wherein n=2 to 4; R?1 is hydrogen, C1-C5 alkyl, optionally substituted by an aryl, a hydroxy, an alkoxy, wherein the alkyl comprises 1 to 5 C, or aryloxy and W is halogen or a nucleofuge group; or a group A2 which represents formyl-CHO, or acetyl-COCH3.

Abstract: The present invention provides convergent processes for preparing epothilone A and B, desoxyepothilones A and B, and analogues thereof. Also provided are analogues related to epothilone A and B and intermediates useful for preparing same. The present invention further provides novel compositions based on analogues of the epothilones and methods for the treatment of cancer and cancer which has developed a multidrug-resistant phenotype.

Abstract: This invention provides a compound of the formula (I): wherein: R1 represents a hydrogen atom, an alkyl group, etc.; R2 represents a hydrogen atom, a halogen atom, etc.; R3 represents a hydrogen atom, an alkyl group, etc.; R4 represents an aryl group, etc.; A represents an aryl1, etc; B represents an alkylene etc.; X represents NH, etc.; or a pharmaceutically acceptable ester of such compound, and pharmaceutically acceptable salts thereof. These compounds are useful for the treatment of medical conditions mediated by prostaglamndin such as pain, fever or inflammation, etc. This invention also provides a pharmaceutical composition comprising the above compound.

Abstract: The invention relates to a novel amide derivative which is an N-({[4-(substituted thiazol-4-yl)phenyl]carbamoyl}methyl)amide derivative having a characteristic in that an aryl or heteroaryl group as an aromatic ring group is directly substituted on the N atom of amido group. Since said amide derivative has excellent anti-herpesvirus action, it is useful as medicaments and antiviral agents, particularly as preventive or therapeutic agents for various diseases accompanied by Herpesviridae virus infections, illustratively, varicella (chickenpox) accompanied by varicella zoster virus infection, shingles accompanied by the recurrent infection of latent varicella zoster virus, labial herpes and herpes encephalitis accompanied by HSV-1 infection, genital herpes accompanied by HSV-2 and the like various herpesvirus infections.

Abstract: The invention relates to methods of increasing the bioavailability of orally administered epothilones. Epothilones administered by the methods of the invention are sufficiently bioavailable to have a pharmacological effect. The invention further relates to pharmaceutical compositions, pharmaceutical dosage forms, and kits for use in the methods of the invention.

Abstract: The present invention relates to compounds of the formula I: where Ring A is a thiazole, oxazole, imidazole or pyrazole and the substituents are as described in the specification, and pharmaceutically acceptable salts thereof. The compounds inhibit bacterial gyrase activity and therefore are useful for treating bacterial infections in mammals.

Abstract: The present invention provides compounds of formula (I): as described generally and in classes and subclasses herein. The present invention additionally provides pharmaceutical compositions comprising compounds of formula (I) and provides methods of treating cancer comprising administering a compound of formula (I).

Abstract: Novel compounds that act to antagonize the action of the glucagon peptide hormone on the glucagon receptor. More particularly, it relates to glucagon antagonists or inverse agonists.

Abstract: The invention concerns an electro-luminescent device in which the luminescent layer contains a compound of general formula I as doping agent or as luminescent compound, whereby the radicals R1 to R12 are identical or are different, and mean hydrogen, straight chain or branched C1-C6 alkyl, aralkyl, aryl or substituted aryl; R1 and R2 and/or R3 and R4 and/or R4 and R5 and/or R5 and R11 and/or R8 and R5 and/or R4 and R12 can form an alicyclic, heterocyclic or aromatic ring; R5 can furthermore be H, OH, OR9, N,N-di-(C1-C6) alkylamino, acetylamino or halogen; R6 and R7 together can form an alicyclic or heterocyclic ring; A1 and A2 are identical or different and are —CN, —NO2 or —COOR8; X is —CH, —CR11 or N; and Y is O, —NH, —NR12, S or Se. The doping agents together luminesce predominately red with very good quantum efficiency together with the luminescent compound as a function of concentration.

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 process for the preparation of a compound of the formula in which Q is CH or N; Y is NO2 or CN; Z is CHR3, O, NR3 or S; R1 and R2 are, for example, together an alkylene bridge which optionally contains an O; R3 is H or unsubstituted or R4-substituted C1-C12alkyl, R4 is unsubstituted or substituted aryl or heteroaryl; wherein said compound has pesticidal activity.

Abstract: The present invention relates to epothilon derivatives and to their use.

Abstract: The invention relates to a method for producing 2-chloro-5-chloromethyl-1,3-thiazol from compounds of formula (I), wherein X means Cl, —OR, —SR or NR2, R being H or a suitable protective group; Y means H or Cl and Z means Cl or O, the compounds of formula (I) having at most one double bond between C* and C″ or between C″ and Z, on the condition that the bond between C″ and Z is a double bond when Z is the same as O and a single bond when Z is the same as Cl; with the following intermediate stage: A1) reacting 2,3-dichloropropanal with rhodanide and acetalising to 3-chloro-1,1-dialkoxy-2-isothiocyanato-propane or a2) reacting 2,3-dichloropropanal with thiourea to form a mixture of the hydrochlorides of the compounds N-[[5-(2-aminothiazol)yl]methyl]thiourea and [5-(2-aminothiazol)yl]methylthioformamidine and splitting to obtain the corresponding thiol or amine or b) reacting a compound of formula (I) wherein X means OR, SR or NR2, Y means clorine and Z

Abstract: The present invention is directed to compounds of formula (I), 1

Abstract: This invention provides azoles which may be useful as inhibitors of protein tyrosine phosphatases (PTPases). The present invention provides compounds of Formula (I), methods of their preparation, pharmaceutical compositions comprising the compounds and their use in treating human or animal disorders. The compounds of the invention may be useful as inhibitors of protein tyrosine phosphatases and thus can be useful for the management, treatment, control and adjunct treatment of diseases mediated by PTPase activity. Such diseases include Type I diabetes, Type II diabetes.

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

Abstract: A process for the preparation of 2-chloro-5-chloromethyl-1,3-thiazole, in which allyl isothiocyanate of formula CH2═CH—CH2—NCS is reacted at from −40° C. to +30° C., in a solvent that is inert under the reaction conditions, with from 1 to 2 mol of a chlorinating agent per mol of allyl isothiocyanate; to the reaction mixture so obtained there is added, at a reaction temperature of from 0° C. to the boiling temperature of the solvent used, from 1 to 5 mol of oxidising agent per mol of allyl isothiocyanate, and then 2-chloro-5-chloromethyl-1,3-thiazole is isolated from the reaction mixture and is optionally converted by crystallisation into high-purity 2-chloro-5-chloromethyl-1,3-thiazole.

Abstract: The invention concerns 2-oxo-1-pyrrolidine derivatives of formula (I) wherein the substituents are as defined in the specification, as well as their use as pharmaceuticals. The compounds of the invention are particularly suited for treating neurological disorders such as epilepsy.

Abstract: The present invention is directed to compounds of formula (I), 1