Abstract: Disclosed are compounds of formula X, which are useful in treating Alzheimer's disease and other similar diseases. Pharmaceutical compositions comprising compounds of formula X and methods of preparing the compounds of formula X are also disclosed.

Abstract: This invention provides new compounds, pharmaceutical compositions and diagnostic kits comprising such compounds, and methods of using such compounds for inhibiting NAALADase enzyme activity, detecting diseases where NAALADase levels are altered, inhibiting angiogenesis, effecting a TGF-? activity or a neuronal activity, and treating a glutamate abnormality, a compulsive disorder, neuropathy, pain, a prostate disease, cancer, Huntington's disease, diabetes, a retinal disorder or glaucoma.

Abstract: A nonlinear optical chromophore having the formula D-?-A, wherein ? is a ? bridge including a thiophene ring having oxygen atoms bonded directly to the 3 and 4 positions of the thiophene ring, D is a donor, A is an acceptor, and the oxygen atoms are further substituted with a fluorinated group comprising at least three fluorines is described. Some examples of fluorinated groups comprising at least three fluorine atoms are 2,2,2-trifluoroethyl; 2,2,3,3,3-pentafluoropropyl; 2,2,3,3,4,4,4-heptafluorobutyl; 2,2,3,3,4,4,5,5,5-octafluoropentyl; 3,3,4,4,-5,5,6,6,7,7,8,8,8-tridecafluoro-1-octyl; 2,2,3,3,4,4,5,5,6,6,7,7,8,8,8 -pentadecafluorooctyl; 1-trifluoromethyl-2,2,2-trifluoroethyl; 1-trifluoromethyl-2,2,3,3,3 -pentafluoropropyl; 2,3,4,5,6-pentafluorobenzyl; and (2,3,4,5,6-pentafluorophenyl)ethyl.

Abstract: A compound or a pharmaceutically acceptable salt or a prodrug thereof, wherein A, B, R1, R2, D, and E are defined herein. Use of the diseases for the treatment of diseases, and compositions and medicaments related thereto are also disclosed.

Abstract: One aspect of the present invention relates to a method for the kinetic resolution of racemic and diastereomeric mixtures of chiral compounds. The critical elements of the method are: a non-racemic chiral tertiary-amine-containing catalyst; a racemic or diastereomeric mixture of a chiral substrate, e.g., a cyclic carbonate or cyclic carbamate; and a nucleophile, e.g., an alcohol, amine or thiol. A preferred embodiment of the present invention relates to a method for achieving the kinetic resolution of racemic and diastereomeric mixtures of derivatives of ?- and ?-amino, hydroxy, and thio carboxylic acids. In certain embodiments, the methods of the present invention achieve dynamic kinetic resolution of a racemic or diastereomeric mixture of a substrate, i.e.

Abstract: Nonlinear optically active compounds, methods for making nonlinear optically active compounds, compounds useful for making nonlinear optically active compounds, methods for making compounds useful for making nonlinear optically active compounds, macrostructures that include nonlinear optically active components, and devices including the nonlinear optically active compounds and the macrostructures.

Abstract: This invention provides a compound of the formula: or its pharmaceutically acceptable salt thereof, wherein A is partially unsaturated or unsaturated five membered heterocyclic, or partially unsaturated or unsaturated five membered carbocyclic, wherein the 4-(sulfonyl)phenyl and the 4-substituted phenyl in the formula (I) are attached to ring atoms of Ring A, which are adjacent to each other; R1 is optionally substituted aryl or heteroaryl, with the proviso that when A is pyrazole, R1 is heteroaryl; R2 is C1-4 alkyl; halo-substituted C1-4 alkyl, C1-4 alkylamino, C1-4 dialkylamino or amino; R3, R4 and R5 are independently hydrogen, halo, C1-4 alkyl, halo-substituted C1-4 alkyl or the like; or two of R3, R4 and R5 are taken together with atoms to which they are attached and form a 4-7 membered ring. R6 and R7 are independently hydrogen, halo, C1-4 alkyl, halo-substituted C1-4 alkyl, C1-4 alkoxy, C1-4 alkylthio, C1-4 alkylamino or N,N-di C1-4 alkylamino; and m and n are independently 1, 2, 3 or 4.

Abstract: The present invention provides a class of sensors prepared from at least a first material having a positive temperature coefficient of resistance and a second non-conductive or insulating material compositionally different than the first material that show an increase sensitivity detection limit for polar and non-polar analytes. The sensors have applications in the detection of analytes in the environment, associated with diseases and microorganisms.

Abstract: The object of the invention are p-aminophenol derivatives of general formula (I) or physiologically tolerated, water-soluble salts thereof and oxidative coloring preparations based on a developer-coupler combination containing at least one p-aminophenol derivative of formula (I).

Abstract: The invention relates to the use of aromatics sulfonamides of the general formula I as peroxynitrite rearrangement catalysts, to the preparation thereof and to the use thereof as medicament for the treatment of various disorders.

Abstract: The present application describes lactam-containing cyclic diamines and derivatives thereof of Formula I:

Abstract: The present invention provides antineoplastic compounds of the formula (D).

Abstract: A nonlinear optical chromophore having the formula D-&pgr;-A, wherein &pgr; is a &pgr; bridge including a thiophene ring having oxygen atoms bonded directly to the 3 and 4 positions of the thiophene ring, D is a donor, A is an acceptor, and the oxygen atoms are further substituted with a fluorinated group comprising at least three fluorines is described. Some examples of fluorinated groups comprising at least three fluorine atoms are 2,2,2-trifluoroethyl; 2,2,3,3,3-pentafluoropropyl; 2,2,3,3,4,4,4-heptafluorobutyl; 2,2,3,3,4,4,5,5,5-octafluoropentyl; 3,3,4,4,-5,5,6,6,7,7,8,8,8-tridecafluoro-1-octyl; 2,2,3,3,4,4,5,5,6,6,7,7,8,8,8 -pentadecafluorooctyl; 1-trifluoromethyl-2,2,2-trifluoroethyl; 1-trifluoromethyl-2,2,3,3,3 -pentafluoropropyl; 2,3,4,5,6-pentafluorobenzyl; and (2,3,4,5,6-pentafluorophenyl)ethyl.

Abstract: The present invention relates to a process for preparing dithioesters in which a dithiocarboxylic acid and/or a dithiocarboxylic salt is reacted with a vinyl compound and/or an alkyl compound which includes a leaving group, the reaction being carried out in a biphasic system in which one of the phases comprises water and the weight ratio of the aqueous phase to the organic phase lies in the range from 95:5 to 5:95.

Abstract: The present invention relates to a process for preparing 3,4-dialkoxythiophenes or 3,4-alkylenedioxythiophenes in high yield via the rapid decarboxylation of 3,4-dialkoxythiophenedicarboxylic acid or 3,4-aklylenedioxythiophenedicarboxylic acid in a water-miscible polar solvent in the presence of copper catalyst under an oxygen atmosphere.

Abstract: Disclosed are compounds which are inhibitors of metalloproteases and which are effective in treating conditions characterized by excess activity of these enzymes.

Abstract: The present invention relates to novel arylphenyl-substituted cyclic ketoenols of the formula (I) 1

Abstract: Compounds are described that bind to tubulin causing tubulin depolymerization and inhibiting tubulin polymerization. The compounds of the invention are therapeutically effective to inhibit cellular proliferation, for example, as effective anti-cancer agents. The compounds can also induce cytotoxicity in cells such as leukemia cells. The chemical structure of the compounds includes a furan, thiophene, thiazole, oxazole, or imidazole group at one end of the molecule (head) and a hydrophobic, aliphatic chain at the other end of the molecule (tail).

Abstract: This invention provides a compound of the formula: or its pharmaceutically acceptable salt thereof, wherein A is partially unsaturated or unsaturated five membered heterocyclic, or partially unsaturated or unsaturated five membered carbocyclic, wherein the 4-(sulfonyl)phenyl and the 4-substituted phenyl in the formula (I) are attached to ring atoms of Ring A, which are adjacent to each other; R1 is optionally substituted aryl or heteroaryl, with the proviso that when A is pyrazole, R1 is heteroaryl; R2 is C1-4 alkyl, halo-substituted C1-4 alkyl, C1-4 alkylamino, C1-4 dialkylamino or amino; R3, R4 and R5 are independently hydrogen, halo,, C1-4 alkyl, halo-substituted C1-4 alkyl or the like; or two of R3, R4 and R5 are taken together with atoms to which they are attached and form a 4-7 membered ring; R6 and R7 are independently hydrogen, halo, C1-4 alkyl, halo-substituted C1-4 alkyl, C1-4 alkoxy, C1-4 alkylthio, C1-4 alkylamino or N,N-di C1-4 alkylamino; and m and n are independently 1, 2, 3 o

Abstract: In various embodiments, chromophores are described that include novel electron acceptors, novel electron donors, and/or novel conjugated bridges that are useful in nonlinear optical applications. In some embodiments, the present invention provides chromophore architectures wherein a chromophore contains more than one electron acceptor in electronic communication with a single electron donor, and/or more than one electron donor in electronic communication with a single electron acceptor. Also described is processes for providing materials comprising the novel chromophores and polymer matrices containing the novel chromophores. Electro-optic devices described herein contain one or more of the described electron acceptors, electron donors, conjugated bridges, or chromophores.

Abstract: The present invention relates to novel aryl-substituted S(O)m cycles of the formula (I) 1

Abstract: The invention relates to novel bicyclic compounds having the general formula (I): as well as to a method for preparing them and to their use in pharmaceutical compositions intended for use in human or veterinary medicine (in dermatology, in carcinology and in the field of autoimmune diseases and that of organ or tissue transplants in particular), or alternatively in cosmetic compositions.

Abstract: Compounds of formula (I): 1

Abstract: It is an object of the invention to provide a method which makes it possible to manufacture the desired sulfonium salts directly without using a metathesis process and without using acids in large excess amounts. An aryl compound (A) in which a hydrogen atom is bonded to at least one of the carbon atoms of the aryl group, and a sulfoxide compound (B) which can be expressed by the formula: R1SOR2 (where R1 and R2 indicate hydrocarbon groups or heterocyclic groups which may be substituted, and which may be the same or different) are reacted in the presence of a strong acid (C) which can be expressed by the formula: HMXmYn (where M indicates an element of group IIIa or group Va of the periodic table, X indicates a halogen atom, Y indicates a hydroxyl group, m and n are integers which are such that m+n=4 and n=0 to 3 in cases where M is an element of group IIIa, and m and n are integers which are such that m+n=6 and n=0 to 2 in cases where M is an element of group Va).

Abstract: The invention relates to novel thienylsulphonylamino(thio)carbonyl compounds of the formula (I), in which Q represents oxygen or sulphur, R1 represents cyano, halogen or in each case optionally cyano-, halogen- or C1-C4-alkoxy-substituted alkyl, alkenyl, alkinyl, alkoxy, alkenyloxy or alkinyloxy having in each case up to 6 carbon atoms, R2 represents cyano, halogen or in each case optionally cyano-, halogen- or C1-C4-alkoxy-substituted alkyl, alkenyl, alkinyl, alkoxy, alkenyloxy or alkinyloxy having in each case up to 6 carbon atoms, and R3 represents in each case optionally substituted heterocyclyl having 5 ring members, at least one of which represents oxygen, sulphur or nitrogen and one to three others may represent nitrogen, and salts of compounds of the formula (I), to processes and novel intermediates for preparing the novel compounds and to their use as herbicides.

Abstract: Compounds of formula I 1

Abstract: The present invention relates to compounds of the formula (I) and/or salts thereof 1

Abstract: Heterocyclic arylsulfonamidobenzylic compounds are provided which are useful in treating lipid disorders, metabolic disorders and cell-proliferative diseases.

Abstract: The present invention relates to novel C2-phenyl-substituted cyclic ketoenols of the formula (I) 1

Abstract: The invention concerns bi-aromatic compounds of formula (I) in which Ar represents (a), Z being O or S, R1 is CH3, —CH2—O—R6, —OR6 or —COR7; R2 is —OR8, —SR8 or a polyether radical if in the latter case R4 is C1-C20alkyl and is in ortho or meta position relative to X—Ar: R3 is alkyl or R2 and R3 together form a cycle optionally interrupted by O or S, R4 is aryl radical; R5 is H, halogen, C1-C20 alkly or —OR8; R6 is H, alkyl or —COR9; R7 is H, alkyl, —N(r′)(r″) or —OR10; R8 is H, alkyl or —COR9; R9 is alkyl; R10 is H, C1-C20 alkyl, alkenyl, monohydroxyalkyl or polyhydroxyalyl, aryl or aralkyl or a sugar residue, r′ and r″ are H, alkyl mono- or polyhydroxyalkyl, aryl, an amino acid or sugar residue or together form a heterocycle, X represents a radical of formula (d) or (e) in which R11 is H or —OR6; R12 is H or alkyl; or R11 and R12 form an oxo radical, and the salts, optical and geometrical isomers of t

Abstract: Thienyl-, furyl- and pyrrolyl-sulfonamides, formulations of pharmaceutically-acceptable salts thereof and methods for modulating or altering the activity of the endothelin family of peptides are provided. In particular, N-(isoxazolyl)thienylsulfonamides, N-(isoxazolyl)furylsulfonamides and N-(isoxazolyl)pyrrolylsulfonamides, formulations thereof and methods using these sulfonamides for inhibiting the binding of an endothelin peptide to an endothelin receptor by contacting the receptor with the sulfonamide are provided. Methods for treating endothelin-mediated disorders by administering effective amounts of one or more of these sulfonamides or prodrugs thereof that inhibit the activity of endothelin are also provided.

Abstract: Compounds of general formula (I): 1

Abstract: A method for synthesizing Salacinol, its stereoisomers, and non-naturally occurring selenium and nitrogen analogues thereof having the general formula (I): 1

Abstract: The present invention relates to a method and catalysts for the stereoselective addition of a nucleophile to a reactive &pgr;-bond of a substrate. The chiral, non-racemic catalysts of the present invention constitute the first examples of catalysts for nucleophilic additions that comprise a main-group metal and a tri- or tetra-dentate ligand.

Abstract: An object of the present invention is to provide a pharmaceutical agents for preventing and/or treating the progressive lesion after the organic damage without inhibiting organic function or regeneration function thereof, by selectively suppressing the induction of cytotoxic effector macrophages which are induced into the damaged organs in response to chemokines and cytokines which are expressed depending on the type of damaged organic tissues.

Abstract: The invention relates to new phenyl-substituted cyclic ketoenols of the formula (I) 1

Abstract: Disclosed are substituted heteroarylalkanoic acids acids of the following formula D-A-C(O)R′, where D, A, and R′ are defined herein. These compounds are useful in the treatment of chronic complications arising from diabetes mellitus. Also disclosed are pharmaceutical compositions containing the compounds and methods of treatment employing the compounds, as well as methods for their synthesis.

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

Abstract: The invention relates to novel spirocyclic phenylketoenols of the formula in which Het represents one of the groups  in which Q represents and X, Y, Z, m, n, R6, R9, R10 and R11 are each as defined in the description, to a plurality of processes and intermediates for their preparation and to their use as pesticides and herbicides.

Abstract: Described herein are compounds related to lactacystin and lactacystin &bgr;-lactone, pharmaceutical compositions containing the compounds, and methods of use.

Abstract: Bi-aromatic compounds linked via a heteroethynylene radical are provided along with pharmaceutical and cosmetic compositions containing these compounds and methods for their use.

Abstract: Compounds of this invention increase plasma levels of high density lipoprotein or HDL, the “good” cholesterol and as such may be useful for treating diseases such as atherosclerosis.

Abstract: Sulfonamide lactams of the following formula wherein X, R1, R2, R3, R4, R4a, R5, R5a, R6, R6a, R7 and R8 are as described herein, are provided which inhibitors of Factor Xa and are useful as anticoagulants in the treatment of cardiovascular diseases associated with thromboses.

Abstract: The present invention relates to novel arylphenyl-substituted cyclic ketoenols of the formula (I) 1

Abstract: Compounds of Formulae Ia and Ic having a lactone structure and an methylene group at the alpha-position of the lactone structure and methods for using and making the compounds have been disclosed. The lactone compounds can be reacted with an neucleaphilic agent to open the lactone ring to a compound of Formula Ib. The lactone of Formula Ia and its functional derivatives have been isolated from Securidaca virgata. These compounds are referred to as LMSV-6 or Securolide™. The purified compounds have demonstrated activity in assays for anti-bacterial and anti-fungal activities, and for treating proliferation disorders such as cancer. Based on the in vitro assays, the lactones are useful for treating proliferation disorders including, for example, breast cancer, colon cancer, rectal cancer, stomach cancer, pancreatic cancer, lung cancer, liver cancer, ovarian cancer, esophageal cancer, and leukemia.

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

Abstract: This invention relates to a series of substituted benzophenone and sulfone compounds of the formula I wherein ring A, Z, Y, R and X are defined as in the specification, that exhibit activity as glycine transport inhibitors, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, and their use for the enhancement of cognition and the treatment of the positive and negative symptoms of schizophrenia and other psychoses in mammals, including humans.

Abstract: The present invention relates to novel arylphenyl-substituted cyclic ketoenols of the formula (I) 1

Abstract: A compound containing an alkylene selenocyanate or an alkylene isoselenocyanate moiety effective to prevent the occurrence or progression of cancer or a precancerous condition. The compound can be provided and administered in the form of a pharmaceutical composition, a cosmetic, a food additive, supplement, or the like. Methods for synthesis and use of the chemopreventive compound of the invention are also provided.

Abstract: A compound selected from the group consisting of a compound of formula I 1