Abstract: A highly efficient process is provided for producing an optically active compound having high optical purity by an asymmetric reaction using as a catalyst a transition metal complex having an optically active nitrogen-containing compound as an asymmetric ligand.

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 provides a compound of 1-calcium phosphate-uracil of the following structure. The compound can be a flavourless, white crystal or crystalline powder with a molecular weight of 216.

Abstract: A process for preparing a phosphoric ester, comprising: Step (1) of reacting naphthol with phosphorus oxychloride in a molar ratio of 1:1.3 or more in the presence of a metallic halide and removing unreacted phosphorus oxychloride and Step (2) of reacting the reaction product of Step (1) with phenol in a molar ratio (molar ratio of chlorine contained in the reaction product to phenol) of 1:1–1.5 and removing hydrogen chloride produced as a by-product to thereby obtain a phosphoric ester represented by the general formula (I): wherein n is 1 or 2.

Abstract: This invention relates to pyrimidine derivatives of general formula I in which R1, R2, X, A and B have the meanings that are contained in the description, as inhibitors of the cyclin-dependent kinases, their production as well as their use as medications for treating various diseases.

Abstract: Benzoyl derivatives of the formula I where the variables have the following meanings: R1, R2 are hydrogen, nitro, halogen, cyano, alkyl, haloalkyl, alkoxy, haloalkoxy, alkylthio, haloalkylthio, alkylsulfinyl, haloalkylsulfinyl, alkylsulfonyl or C1–C6-haloalkylsulfonyl; R3 is hydrogen, halogen or alkyl; R4, R5 are hydrogen, halogen, cyano, nitro, alkyl, alkoxy, alkylthio, dialkylamino, phenyl or carbonyl, it being possible for the 6 last-mentioned radicals to be substituted; X is O, S, NR9, CO or CR10R11; Y is O, S, NR12, CO or CR13R14; R15 is pyrazole which is unsubstituted or substituted, linked in the 4-position and has attached to it in the 5-position a hydroxyl or sulfonyloxy radical; and the agriculturally useful salts thereof; processes and intermediates for the preparation of the 3-heterocyclyl-substituted benzoyl derivatives, compositions comprising them; and the use of these derivatives or compositions comprising them for controlling undesirable plants.

Abstract: Pyridoxal analogues can be useful for treating B6 deficiency and related diseases; cardiovascular and related diseases; melanoma and related diseases; and symptoms thereof. One such analogue is a compound of the formula: or a pharmaceutically acceptable acid addition salt thereof, in which R1 is alkyl, alkenyl, in which alkyl or alkenyl can be interrupted by nitrogen, oxygen, or sulfur, and can be substituted at the terminal carbon by hydroxy, alkoxy, alkanoyloxy, alkanoyloxyaryl, alkoxyalkanoyl, alkoxycarbonyl, or dialkylcarbamoyloxy; alkoxy; dialkylamino; alkanoyloxy; alkanoyloxyaryl; alkoxyalkanoyl; alkoxycarbonyl; dialkylcarbamoyloxy; or aryl, aryloxy, arylthio, or aralkyl, in which aryl can be substituted by alkyl, alkoxy, amino, hydroxy, halo, nito, or alkanoyloxy. These analogues can be administered, either alone or concurrently with known medications, to treat the above-described diseases.

Abstract: An isomer, enantiomer, diastereoisomer or tautomer of a compound, represented by formula I: wherein wherein A, B, R2, R3, L, M1, M2, M3, M4, Y1, Y0, Z and Sp are as defined in claim 1, or a salt thereof, as an inhibitor of HCV NS5B polymerase.

Abstract: A method is provided for producing a specific crosscoupling compound and a specific catalyst for producing the compound. The method includes reacting in the presence of a base and a nickel compound catalyst organic halide of the formula n?(R1X1n), wherein R1 is a hydrocarbon group and the ? and ? carbons to X? are sp3 carbon atoms; X1 is a chlorine, bromine, or iodine atoms, and n and n1 and 1 or 2 but not both 2, with a compound having the formula m{R2(BX22)n?} where an R2 is an aryl, heteroaryl, or alkenyl group, and n? is 1 or 2, X2 is independently a hydroxyl group, an alkoxy or arylalkoxy group or X22 together form an alkylenedioxy or arylenedioxy group, and m represents 1 or 2 but m?n, and the boron atom is bonded to a sp2 carbon atom of R2 group or a boronic acid trimer anhydride.

Abstract: The invention relates to the use of alkoxyamines of formula (I): for the preparation of polymerized or non-polymerized mono- or polyalkoxyamines of formula (II):

Abstract: A derivative of phosphoric acid ester salt or adduct or a mixture thereof is obtained from a reaction product, polycondensed with at least one aldehyde, of at least one polyol phosphoric acid ester with at least one organic nitrogen base. The derivative is advantageously used as a flame-inhibiting and/or intumescent treatment in plastic mouldings, on porous carriers or in paint or coating systems. The production of the derivative or a mixture thereof by reacting at least one polyol with phosphorus pentoxide and reacting the polyol phosphoric acid ester obtained in that way with at least one organic nitrogen base forming a phosphoric acid ester salt or adduct, is characterized in that the amount of phosphorus pentoxide required for the esterification operation is suspended in an amount of the ester or ester mixture to be produced, then at a temperature in the range of 20–180° C.

Abstract: The present invention is constituted with crystal of 2-amino-3-cyano-4-methyl-5-(2-fluorophenyl)pyrrole, which show diffraction peaks at diffraction angles (2?±0.2 degree) of 10.3 degree, 14.3 degree, 15.5 degree, 15.9 degree, 25.1 degree and 25.7 degree in a powder X-ray diffraction spectrum, and also show absorption peaks at wavenumbers (cm?1, ±0.2%) of 3373, 3322, 2201, 762, 687 and 640 in an infrared absorption spectrum. The crystal of the present invention is superior in stability and is useful as a pharmaceutical bulk.

Abstract: Methods are described for the production of hydrogen-bis(chelato)borates of the general formula H[BL1L2] and of alkali metal-bis(chelato)borates of the general formula M[BL1L2] where M=Li, Na, K, Rb, Cs L1=—OC(O)—(CR1R2)n—C(O)O— or —OC(O)—(CR3R4)—O— where n=0 or 1, R1, R2, R3, R4 independently of one another denote H, alkyl, aryl or silyl, L2=—OC(O)—(CR5R6)n—C(O)O— or —OC(O)—(CR7R8)—O— where n=0 or 1, R5, R6, R7, R8 independently of one another denote H, alkyl, aryl or silyl, wherein the respective raw materials are mixed in solid form without the addition of solvents and are reacted. Lithium-bis(oxalato)borate, lithium-bis(malonato)borate, caesium-bis-(oxalato)borate, caesium-bis-(malonato)borate and the mixed salts lithium(lactato,oxalato)borate and lithium(glycolato,oxalato)borate for example may be produced in this way.

Abstract: A method for preparing aryllithium compounds of the formulae (IV) and (VI) includes reacting halogen compounds (I) with lithium metal to obtain a lithium compound of formula (II) and reacting the lithium compound of formula (II) with aromatic compounds of the formulae (III) and/or (V) to form lithium aromatics (IV) and (VI).

Abstract: A compound of the formula (I): or a pharmaceutically acceptable salt thereof is disclosed, as well as processes for and intermediates in the preparation thereof, a method of antagonizing endothelin, methods for the inhibition of bone metastases, methods for the prevention of growth of new metastases, methods for the inhibition of bone turnover, and methods for the prevention of bone loss in patients, including cancer patients, using an endothelin ET-A receptor antagonist.

Abstract: The invention provides novel ?-lactamase inhibitors, which are structurally unrelated to the natural product and semi-synthetic ?-lactamase inhibitors presently available, and which do not possess a ?-lactam pharmacophore. These new inhibitors are fully synthetic, allowing ready access to a wide variety of structurally related analogs. Certain embodiments of these new inhibitors also bind bacterial DD-peptidases, thus potentially acting both as ?-lactamase inhibitors and as antibiotics.

Abstract: The present invention is concerned with compounds of formula the N-oxides, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein R1 is hydrogen, hydroxy, C1-6alkyl or aryl; R2 is hydrogen; optionally substituted C1-12alkyl; C3-7cycloalkyl; C2-8alkenyl, optionally substituted pyrrolidinyl or aryl; R3 is hydrogen, optionally substituted C1-6alkyl or aryl; Het is an optionally substituted unsaturated heterocycle selected from imidazolyl, triazolyl, tetrazolyl and pyridinyl; is an optionally substituted unsaturated mono- or bicyclic heterocycle; and aryl is optionally substituted phenyl. The present invention also relates to processes for their preparation and compositions comprising said new compounds, as well as their use as a medicine.

Abstract: The invention relates to a multimeric compound or a pharmaceutically acceptable salt or derivative thereof which comprises three or more neuraminidase-binding groups attached to a spacer or linking group, in which the neuraminidase-binding group is a compound which binds to the active site of influenza virus neuraminidase, but is not cleaved by the neuraminidase. The invention also relates to processes for the preparation of the multimeric compound defined above, pharmaceutical compositions containing them or methods for the treatment and/or prophylaxis of a viral infection involving them.

Abstract: The present application describes lactam-containing cyclic diamines and derivatives thereof of Formula I: P4-M-M4I or pharmaceutically acceptable salt forms thereof, wherein M is a non-aromatic carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.

Abstract: The invention relates to substituted 1 and 2 naphthol Mannich bases, a method for the production thereof, medicaments containing said compounds and the use of said compounds in the production of medicaments.