Abstract: The present invention relates to a novel method for producing a compound of the formula [11] wherein R is an optionally substituted aromatic hydrocarbon group, an optionally substituted alicyclic hydrocarbon group, an optionally substituted heterocyclic group or an optionally substituted condensed heterocyclic group, which is useful as a therapeutic agent for diabetes. The method of the present invention is an industrially utilizable method that enables efficient production of the objective compound [11] from &bgr;-methyl L-aspartate via an important intermediate compound [6] wherein R is as defined above, at high yield.

Abstract: Azole compounds of the formula: wherein R1 is lower alkyl substituted with carboxy, etc., R2 is hydrogen or lower alkyl, R3 is aryl, etc. R4 is aryl, etc. Q is  etc., and X is O, NH or S, and its salt, which are useful as medicament.

Abstract: A 3-anilino-2-cycloalkenone derivative of the formula (I): wherein, R1 represents a C1 to C8 alkyl group, which may have a substituent, except for a methyl group, a C3 to C7 cycloalkyl group, a 3-tetrahydrofuryl group, an 2-indanyl group, etc., R2 represents a C1 to C4 alkyl group, R3 represents a hydrogen atom, a C3 to C7 alkyl group, which may have a substituent, a C3 to C7 cycloalkyl group, etc., R4 represents a hydrogen atom, a C1 to C5 alkyl group, which may have a substituent, a halogen atom, etc., R5, R6, R7, and R8 independently represent a hydrogen atom, a C1 to C5 alkyl group, which may have a substituent, etc., X represents —(CR11R12)n—, wherein n is 0 to 2, R11 and R12 independently represent a hydrogen atom, a C1 to C5 alkyl group, which may have a substituent, etc.

Abstract: The invention relates to polycyclc 2-aminodihydrothiazole systems and their physiologically tolerated salts and physiologically functional derivatives. Compounds of the formula I, in which the radicals have the stated meanings, and their physiologically tolerated salts and processes for their preparation are described. The compounds are suitable, for example, as anorectics.

Abstract: Water soluble prodrugs of azole antifungal agents are provided by quaternizing a nitrogen atom of the azole ring with a phosphonooxymethyl group.

Abstract: According to the invention are provided compounds of formula (I) (relative stereochemistry indicated) wherein R1, R2 and R3 are as defined in the specification. Compounds of formula (I) are useful inter alia in the treatment of inflammatory diseases of the respiratory tract.

Abstract: The use of certain heterocyclic derivatives for treating parasitic protozoa infections in mammals, in particular bovine trichomoniasis and giardiasis, is disclosed.

Abstract: The invention relates to a process of preparing a chiral compound of the formula: wherein R1 is selected from the group consisting of hydrogen and lower alkyl, and R2 and R2′ are the same, and R2 and R2′ are selected from a group consisting of hydrogen and primary alkyl, or R2 and R2′ taken together form a C3 to C6 cycloalkyl, comprising the steps of chirally reducing a &bgr;-keto ester to afford a &bgr;-hydroxy ester, activating the &bgr;-hydroxy ester by treatment with a sulfonic acid or a derivative thereof to provide an activated compound having sulfonate leaving group, displacing the sulfonate leaving group with an azido moiety, or treating the activated compound with an alkylamine, deprotecting and cyclizing to afford a pyrrolidinone, and reducing the pyrrolidinone to afford a stereoisomerically preferred 3-aminopyrrolidine derivative.

Abstract: The present invention provides convergent processes for preparing epothilone A and B, desoxyepothilones A and B, and analogues thereof, useful in the treatment of cancer and cancer which has developed a multidrug-resistant phenotype. Also provided are intermediates useful for preparing said epothilones.

Abstract: The invention relates to a process of preparing a chiral compound of the formula: wherein R1 is selected from the group consisting of hydrogen and lower alkyl, and R2 and R2′ are the same, and R2 and R2′ are selected from a group consisting of hydrogen and primary alkyl, or R2 and R2′ taken together form a C3 to C6 cycloalkyl, comprising the steps of chirally reducing a &bgr;-keto ester to afford a &bgr;-hydroxy ester, activating the &bgr;-hydroxy ester by treatment with a sulfonic acid or a derivative thereof to provide an activated compound having sulfonate leaving group, displacing the sulfonate leaving group with an azido moiety, or treating the activated compound with an alkylamine, deprotecting and cyclizing to afford a pyrrolidinone, and reducing the pyrrolidinone to afford a stereoisomerically preferred 3-aminopyrrolidine derivative.

Abstract: Compounds of the formula (I) are prepared by reacting a compound of the formula (V) with a compound of the formula (X) and hydrolyzing the product; or converting the compound of the formula (V) into the hydrazide, and cyclizing and hydrolyzing the latter to give the oxadiazole. para-Oxadiazolylphenylboronic acids are valuable precursors for active ingredients.

Abstract: A 4-aryl-4-substituted pyrazolidine-3,5-dione derivative represented by the formula (1) is useful as an effective component of a miticide, insecticide or herbicide wherein R1 and R2 are each independently alkyl group having 1 to 4 carbon atoms, or R1 and R2, when taken together, represent saturated or unsaturated bivalent hydrocarbon group having 3 or 4 carbon atoms which may optionally be substituted with alkyl group having 1 to 4 carbon atoms, or halogen atom, X is alkyl group having 1 to 4 carbon atoms, haloalkyl group having 1 to 4 carbon atoms or halogen atom, Y is halogen atom or nitro group, and n is an integer of 0 to 3.

Abstract: The invention relates to 1,2,5-trisubstituted 1,2-dihydroindazol-3-ones of formula (I) wherein X is —SO2—, —SO—, —(CH2)p—, —(CH2)p—O—, —(CH2)p—(C═O)—, —(CH2)p—(C═O)—NH—, —(CH2)p—CHOH—, —CHOH—(CH2)p—, —(CH2)p—CH═CH—, —CH═CH—(CH2)p—, Y is —(C═O)—, —(C═O)—NH—, —(C═O)—NH—(CH2)p—, —C═O)—(CH2)p—, —(CH2)p—, —(CH2)p—O—, —(CH2)p—(C═O)—, —(CH2)p—(C═O)—NH—, —(CH2)p—(C═O)—NH—(CH2)p—, —(CH2)p—CHOH—, —CHOH—(CH2)p—, —(CH2)p—CH═CH—, —CH═CH—(CH2)p—, Z is —O—, —O—(CH2)p—, —NH—, —NH—(

Abstract: Disclosed is a process for the preparation of a mixture of benzoxazolyl-stilbene compounds by the reaction of unsubstituted 4,4′-bis(benzoxazol-2-yl)stilbene with a substituted o-aminophenol or o-aminonaphthol to obtain a mixture comprising the unsubstituted 4,4′-bis(benzoxazol-2-yl)stilbene and at least one substituted 4,4′-bis(benzoxazol-2-yl)stilbene, 4-naphthoxazol-2-yl-4′-benzoxazol-2-ylstilbene and/or 4,4′-bis(naphthoxazol-2-yl)stilbene. These mixtures are useful as fluorescent brightening agents and light stabilizers for synthetic polymeric materials such as polyesters, polyamide and polyolefin textile materials and shaped articles.

Abstract: Process for the production of alkoxycarbonyldipeptides intermediates in the synthesis of the lisinopril which comprises protecting both amino functions of the L-lysine with an alkoxycarbonyl group, subsequently making the N-carboxyanhydride of the N6-[alkoxycarbonyl]-L-lysine by treatment with thionyl chloride and making the desired alkoxycarbonyldipeptide by reaction with L-proline in alkaline medium.

Abstract: A method for racemization of an optically active N-substituted azetidine-2-carboxylic acid ester of the formula (1): ##STR1## wherein * represents an asymmetric carbon atom, R.sup.1 represents an aryl,R.sup.2 represents a saturated hydrocarbon group which may be substituted,which is characterized byheating the ester at 100.degree. C. or higher, orsubjecting the ester to contact with a basic compound selected from an alkali metal hydride, an alkali metal alcoholate of tertiary alcohol and an organic amine.

Abstract: The invention relates to 1,5- and 3-O-substituted 1H-indazoles of formula (I) ##STR1##

Abstract: A process for preparing methyl 2-(2-methylphenyl)-3-methoxyacrylate (I) by formylation of methyl 2-methylphenylacetate (II) ##STR1## in an inert solvent in the presence of a base, and subsequent methylation of the enolate III formed ##STR2## where M.sup.+ is an alkali metal cation.

Abstract: Inhibition of farnesyl transferase, which is an enzyme involved in ras oncogene expression, is effected by compounds of the formula ##STR1## and their enantiomers, diastereomers, and their pharmaceutically acceptable salts, including prodrugs and solvates thereof.The compounds of formula I are useful in the treatment of a variety of cancers. In addition, the formula I compounds may also be useful in the treatment of diseases other than cancer.

Abstract: A process for producing 2-azabicyclo[2.2.1]hept-5-en-3-one is provided by reacting a sulfonyl cyanide represented by the general formula R--SO.sub.2 CN (in which R represents an alkyl group or a phenyl group which may have a substituent), in the presence of water and in a hydrocarbon solvent at a pH of 4 to 7 inclusive. 2-Azabicyclo[2.2.1]hept-5-en-3-one can be produced in a high yield and a high purity in one step process, with a reduced amount of solvent used, safely and with good productivity. A method of crystallizing 2-azabicyclo[2.2.1]hept-5-en-3-one is also provided, which includes dissolving 2-azabicyclo[2.2.1]hept-5-en-3-one into an organic solvent mainly including at least one of diisopropyl ether and methyl tertiary butyl ether, cooling the solution to deposit crystals of 2-azabicyclo[2.2.1]hept-5-en-3-one. Finely divided particulate crystals of 2-azabicyclo[2.2.1]hept-5-en-3-one excellent in fluidity and handleability can be obtained with a simple procedure and in a high recovery rate.