Abstract: This invention provides estrogen receptor modulators of formula I, having the structure wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10, are as defined in the specification, or a pharmaceutically acceptable salt thereof.

Abstract: Provided is a bis(diphenylvinyl)arene compound having a reactive functional group on phenyl group, represented by below formula (1), wherein, Ar is an arylene group and has one or more substituents; R1-R22 each independently represent a hydrogen atom, a halogen atom, cyano group, nitro group, etc., and at least one of R1-R20 is a halogen atom, etc. The arene compound has sufficient solubility in an organic solvent and excellent reactivity.

Abstract: There is a significant demand for organic nitriles, based on their versatility in reactions. Compounds prepared from nitriles have properties including superoxide inhibition, ferrielectric liquid crystal dopant, antipicornaviral agents, anti-inflammatory agents, anti-asthma agents, and fibringoen antagonists. The present invention discloses a facile synthesis for 2,4-dihydroxybenzonitrile, and ethers and diethers thereof, from 2,4-dihydroxybenzoic acid. The present invention also discloses a method of preparing a class of iron chelating agents related to desferrithiocin, all of which contain a thiazoline ring. In this method, 2,4-dihydroxybenzonitrile is condensed with (S)-2-methylcysteine.

Abstract: A liquid crystalline compound represented by Formula (1c′): wherein R1 and R2, rings A1, A2, A3, A4 and A5, Z1, Z2, Z3 and Z4, Y1, Y2, Y3 and Y4, and k, l, m and n are as defined in the specification. Also provided is a liquid crystal composition containing at least one of these liquid crystalline compounds.

Abstract: Aldehydes containing a difluorooxymethylene bridge, of the general formula I

Abstract: This invention provides estrogen receptor modulators of formula I, having the structure 1

Abstract: A process for preparing 3,4-dihydroxybenzonitrile includes the steps of reacting a nitrile compound with an alkali metal halide, followed by treating with an acid.

Abstract: Competitive progesterone antagonists, including two novel steroids, viz., 11&bgr;,19-[4-(cyanophenyl)-o-phenylene]-17&bgr;-hydroxy-17&agr;-(3-hydroxyprop-1(Z)-enyl)-4-androsten-3-one and 11&bgr;,19-[4-(3-pyridinyl)-o-phenylene]-17&bgr;-hydroxy-17&agr;-(3-hydroxyprop-1(Z)-enyl)-4-androsten-3-one, inhibit formation of endometrial glands at below their ovulation inhibiting dose and the abortive dose, and thus achieve oral contraception in females without adversely affecting the menstrual cycle and without risk of aborting a previous implanted fertilized egg or a fetus.

Abstract: There is provided a process for the preparation of a chiral insecticidal and acaricidal compound of formula I. Also provided are intermediate compounds useful in the process of the present invention.

Abstract: The invention provides novel 1,2-diphenylethene derivatives and pharmaceutically acceptable salts thereof, the process for production of these compounds and their pharmaceutical composition and the use of these compounds as modulators of T-cells, neutrophils, macrophages and their associated cytokines as agents for treating immune, inflammatory and auto-immune diseases.

Abstract: Derivatives of C2-substituted indan-1-ol compounds of formula I: 1

Abstract: Polysubstituted indan-1-ol compounds, methods for their preparation; and methods for their use are disclosed herein.

Abstract: Compounds of general formula (I) wherein the substituents are as defined in claim 1 are suitable for use as herbicides.

Abstract: This application relates to a compound of formula I (or a pharmaceutically acceptable salt thereof) as defined herein, pharmaceutical compositions thereof, and its use as an inhibitor of factor Xa, as well as a process for its preparation and intermediates therefor.

Abstract: A process for preparing 3,4-dihydroxybenzonitrile includes the steps of reacting a nitrile compound with an alkali metal halide, followed by treating with an acid.

Abstract: The present invention provides a difluoromethyl ether derivative which shows various suitable physical properties as a liquid crystal compound, a liquid crystal composition comprising the compound and a liquid crystal display element containing the composition, and also provides a simple and efficient process for producing the difluoromethyl ether derivative.

Abstract: In a process for the preparation of ring compounds via a combinatorial synthesis, the reaction procedure is based on a Suzuki coupling, subsequent halo-demetallation and finally a further Suzuki coupling. The Suzuki couplings are each carried out with a boronic acid or a boronic acid ester. The reaction procedure uses provides novel ring compounds and uses novel synthesis units used for this purpose. The novel ring compounds are suitable for use as constituents in liquid-crystalline mixtures.

Abstract: The present invention provides a difluoromethyl ether derivative which shows various suitable physical properties as a liquid crystal compound, a liquid crystal composition comprising the compound and a liquid crystal display element containing the composition, and also provides a simple and efficient process for producing the difluoromethyl ether derivative.

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

Abstract: Benzhydryl derivatives of the formula I, 1

Abstract: A compound of formula (I) or (II), wherein X is hydrogen, halogen, alkyl, aralkyl,aryloxy, arylalkoxy or alkoxy, Y is hydrogen, halogen, alkyl, aralkyl, aryloxy, arylalkoxy or alkoxy, or formula (a) wherein A and B are different and one of A and B is CH2 and the other is O, NH, or S or A and B are both CH2 or CH═, and Ra, Rb, and Rc are the same or different and are hydrogen, halogen, alkyl, alkoxy, aryloxy, aralkyl or arylalkoxy. R1 is hydrogen, and R2 is hydrogen, C1-C6 alkyl or aryl which is unsubstituted or substituted by halogen, cyano, hydroxy, C1-C6 alkyl, which is unsubstituted or substituted by halogen, cyano, hydroxy, C1-C6 alkoxy, aralkyl, aryloxy or aryl, C1-C6 alkoxy, aralkyl, arylalkoxy, aryloxy or aryl, which is unsubstituted or substituted by halogen, cyano, hydroxy, C1-C6 alkyl or C1-C6 alkoxy; and pharmaceutically acceptable salts thereof; with the proviso that when R2 is phenyl and Y is hydrogen, X is not chlorine.

Abstract: The present invention relates to certain phenalkyloxy-phenyl derivatives of formula (I) and analogs, to a process for preparing such compounds, which compounds have utility in treating clinical conditions associated with insulin resistance, to methods for their therapeutic use and to pharmaceutical compositions containing them.

Abstract: 3,4-dihydroxybenzonitrile useful as a starting compound for synthesis of medicines and agricultural chemicals is produced, with a high yield by chlorinating 3,4-methylenedioxybenzonitrile with sulfuryl chloride or a mixture of molecular chlorine with a chlorination-promoter including phosphorus trichloride, phosphorus pentachloride, sulfuryl chloride, thionyl chloride, and/or nitrosyl chloride, to prepare 2-chloro-benzo[1,3]dioxole-5-carbonitrile, and hydrolyzing 2-chloro-benzo[1,3]dioxole-5-carbonitrile by contacting it with water to produce 3,4-dihydroxybenzonitrile.

Abstract: The present invention relates to an improved process for preparing 4-substituted resorcinol derivatives, and intermediate compounds useful in the preparation of such resorcinol derivatives.

Abstract: Bis-oxime compounds of the general formula (I) are provided wherein X, Y, R1, R2 R3 and n are as defined in the specification. The bis-oxime compounds possess pesticidal activity, which may provide plants with protection from phytopathogenic microorganisms.

Abstract: The present invention relates to certain phenalkyloxy-phenyl derivatives of formula (I) and analogs, to a process for preparing such compounds, having the utility in clinical conditions associated with insulin resistance, to methods for their therapeutic use and to pharmaceutical compositions containing them.

Abstract: 3,4-dihydroxybenzonitrile useful as a starting compound for synthesis of medicines and agricultural chemicals is produced, with a high yield by chlorinating 3,4-methylenedioxybenzonitrile with sulfuryl chloride or a mixture of molecular chlorine with a chlorination-promoter including phosphorus trichloride, phosphorus pentachloride, sulfuryl chloride, thionyl chloride, and/or nitrosyl chloride, to prepare 2-chloro-benzo[1,3]dioxole-5-carbonitrile, and hydrolyzing 2-chloro-benzo[1,3]dioxole-5-carbonitrile by contacting it with water to produce 3,4-dihydroxybenzonitrile.

Abstract: This invention relates to 1,2-di(4-hydroxyaryl)tetrafluoroethanes of the general formula (I) 1

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

Abstract: The present invention provides a difluoromethyl ether derivative which shows various suitable physical properties as a liquid crystal compound, a liquid crystal composition comprising the compound and a liquid crystal display element containing the composition, and also provides a simple and efficient process for producing the difluoromethyl ether derivative.

Abstract: Disclosed is a method for the preparation of citalopram comprising conversion of a compound of Formula VIII wherein Z is halogen, to a compound of Formula IV followed by conversion of the compound of Formula IV into citalopram. Methods for the preparation of the compound of Formula IV are also disclosed.

Abstract: A new method for producing unsymmetrically substituted fluorenyl compounds, one step of which is the preparation of 2,7-disubstituted fluoren-9-one derivatives via the nucleophilic substitution of a compound of the formula D wherein A′ is selected from the group consisting of —Br, —Cl, —F, —NO2, and —CN; A is selected from the group consisting of —NO2, —CN, —CO2R, —C(O)R, —SO2R, —SO2RF, —C(CN)═C(CN)2 and —CH═C(CN)2; RF is —CpF2p+1, p=from about 0 to about 10; R is an straight, branched or cyclic aliphatic alkyl group having about 1 to 10 carbon atoms, or an aromatic group such as phenyl or naphthyl; and is a carbonyl or a protected carbonyl such as a ketal or thio-ketal such as wherein R′ is —CrH2r+1; R″ is —(CH2)r—; and r is independently 2 or 3, with a nucleophilic reagent in the presence of an aprotic solvent

Abstract: This invention relates to a process for making certain phenyl urea compounds by using a Lewis acid to effect the ring opening of a benzoxazolinone by an amine.

Abstract: Competitive progesterone antagonists, including two novel steroids, viz., 11&bgr;,19-[4-(cyanophenyl)-o-phenylene]-17&bgr;-hydroxy-17&agr;-(3-hydroxyprop-1(Z)-enyl)-4-androsten-3-one and 11&bgr;,19-[4-(3-pyridinyl)-o-phenylene]-17&bgr;-hydroxy-17&agr;-(3-hydroxyprop-1(Z)-enyl)-4-androsten-3-one, inhibit formation of endometrial glands at below their ovulation inhibiting dose and the abortive dose, and thus achieve oral contraception in females without adversely affecting the menstrual cycle and without risk of aborting a previous implanted fertilized egg or a fetus.

Abstract: Compounds and methods useful for chemopreventative treatment of diseases such as cancer, Alzheimer's disease, Parkinson's disease, inflammatory bowel diseases, and multiple sclerosis.

Abstract: A method for the preparation of citalopram is described comprising reduction of the oxo group of a compound of formula (IV), wherein R1 is CN, C1-6 alkyloxycarbonyl or C1-6 alkylaminocarbonyl, ring closure of the resulting hydroxy compound thereby obtaining the corresponding 1-(4-fluorophenyl)-1,3-dihydroisobenzofuran, then if R1 is cyano using it directly in the next step and if R1 is C1-6 alkyloxycarbonyl or C1-6 alkylaminocarbonyl, conversion of the compound to the corresponding compound wherein R1 is a cyano; and alkylation of the resulting 5-cyano compound with 3-dimethyl-aminopropylhalogenide in basic conditions thereby obtaining citalopram.

Abstract: 2-Methoxyethoxy-benzenes are obtained in an advantageous manner from the corresponding phenol compounds by reaction with 2-chloroethyl methyl ether if the process is carried out without the addition of a strong solvent at temperatures above 95° C. and under pressure. The present invention also relates to novel 2-methoxyethoxybenzyl cyanides.

Abstract: A two step process is described for making 2-alkyl-3-hydroxybenzoic acids or derivatives of benzoic acids by first reacting an allenyl ester or equivalent with furan followed by the ring-opening reaction of the derived bicyclo intermediate with base. The benzoic acids thus prepared are useful intermediates for the preparation of agricultural and pharmaceutical materials.

Abstract: Compounds of formula (I) are described wherein R1 is hydrogen, -(lower alkyl)q(CO2R6 or OH), —CN, —C(R7)═NOR8, NO2, —O(lower alkyl)R9, —C≡C—R10, —CR11═C(R12)(R13), —C(═O)CH2C(═O)CO2H, —CO(R14), alkylthio, alkylsulphinyl, alkylsulphonyl, carbamoyl, thiocarbamoyl, substituted carbamoyl, substituted thiocarbamoyl, sulphamoyl or an optionally substituted nitrogen-containing ring, m, n, o and p are independently zero or 1 and R2, R3, R4 and R5 are various groups; and physiologically acceptable salts, N-oxides and prodrugs thereof. The compounds have endothelin antagonist activity and are useful as pharmaceuticals.

Abstract: An industrially advantageous process for producing cyanobenzyl compounds under mild conditions from relatively easily available cyanobenzylamine having a cyano group on the benzene ring or a compound thereof which is ring-substituted with a chlorine atom, a fluorine atom, etc. The process for producing a cyanobenzyl compound includes transforming an aminomethyl group of a cyanobenzylamine compound into a hydroxymethyl group, a halogenomethyl group, or an acyloxymethyl group without causing damage to a cyano group on the benzene ring. The transformation may be carried out by use of nitrosonium ions.

Abstract: Substituted phenylalanines are provided comprising an hydantoin, urea or 2-hydroxyl, 2-methylpropionyl group, dimers thereof and alkyl, polyfluoroamido and haloarylamino derivatives thereof, as well as radiolabeled derivatives thereof. The compounds bind specifically to the androgen receptor and find use in the therapy of indications associated with the androgen receptor, such as, hirsutism, acne and androgenetic alopecia, and in the therapy and diagnosis of cell hyperplasia dependent on androgens.

Abstract: A method for preparing an aryl ether compound is provided in which an alcohol is reacted with an aromatic compound in the presence of a base, and a transition metal catalyst selected from the group consisting of platinum and nickel to form an aryl ether. The aromatic compound comprises an activated substituent, X, said activated substituent being a moiety such that its conjugate acid HX has a pKa of less than 5.0. The catalyst is preferably a soluble palladium complex in the presence of supporting ligands.

Abstract: The invention relates to a preparation process for 4-cyano-4'-hydroxybiphenyl, said process comprising the protection of the hydroxy group of 4-phenyl-phenol, acylation of the protected 4-phenyl-phenol group, conversion of the resulting ketone into an acid, amidification of the acid thus obtained, dehydration of the resulting amide and deprotection of the hydroxy group.

Abstract: The present invention relates to novel 2-aryl-3-hydroxy-cyclopent-2-en-1-one derivatives of the formula (I) ##STR1## in which X represents halogen, nitro, cyano, alkyl, alkoxy, alkenyloxy, alkylthio, alkylsulphinyl, alkylsulphonyl, halogenoalkyl or halogenoalkoxy,Y represents hydrogen, halogen, nitro, cyano, alkyl, alkoxy, alkenyloxy, alkylthio, alkylsulphinyl, alkylsulphonyl, halogenoalkyl or halogenoalkoxy,Z represents halogen, nitro, cyano, alkyl, alkoxy or halogenoalkoxy andA, B, D.sup.1, D.sup.2, G and n have the meaning given in the description,several processes for their preparation and their use as compositions for controlling pests and as herbicides.

Abstract: The present invention provides novel iodopropargyl derivatives represented by the following formula (1): ##STR1## wherein R.sup.1 is a methoxy group or a cyano group, which have a reduced unpleasant smell and also have a wide antimicrobial spectrum and a high antimicrobial activity. Also, the present invention provides antimicrobial, antifungal and preservative or antimold agents comprising the above derivatives as an active ingredient.

Abstract: The invention concerns a method for the production of unsymmetrically substituted cyanobiphenyls by the slow addition of an aryl Grignard compound to an optionally substituted bromobenzonitrile in the presence of a palladium complex catalyst.

Abstract: A process for producing an asymmetric compound using a metal complex containing no rare earth metal element is disclosed. The process affords an optically active compound having high optical purity. Optically active binaphthol having the chemical formula and lithium aluminum hydride are reacted, or the optically active binaphthol, a dialkyl aluminum hydride, and a base containing an alkali metal (or a base containing alkaline earth metal) are reacted to prepare a metal complex comprising optically active binaphthol, aluminum, and alkali metal (or alkaline earth metal). This metal complex can be used as a catalyst to perform an asymmetric Michael reaction, an asymmetric phosphonylation reaction, or the like, to obtain, in a high yield, an asymmetric compound having high optical purity.

Abstract: Phosphoramidite oligonucleotide synthesis is facilitated by the use of fluoride-labile 5' silyl protecting groups. RNA synthesis is improved by the use of 2 orthoester protecting groups. Reactions are conducted on a solid phase support and acidic deprotection conditions are avoided, as is the necessity of oxidizing the phosphite linkage between each coupling reaction.

Abstract: Novel farnesyl derivatives which are inhibitors of the prenylated protein methyltransferase enzyme, and useful as anti-cancer drugs, have the following formula: wherein R1represents farnesyl, geranyl or geranyl-geranyl; Z represents C—R6 or N; R2 represents H, CN, the groups COOR7, SO3R7, CONR7R8 and SO2NR7R7, wherein R7 and R8 are each independently hydrogen, alkyl, alkenyl, and the groups COOM and SO3M, wherein M is a cation; R3, R4, R5 and R6 are each independently hydrogen, carboxyl, alkyl, alkenyl, aminoalkyl, nitroalkyl, nitro, halo, amino, mono- or di-alkylamino, mercapto, mercaptoalkyl, azido, or thiocyanato; X represents O, S, SO, SO2, NH or Se; and the quaternary ammonium salts and N-oxides of the compounds of formula I wherein Z is N.

Abstract: Anisotropic compounds of the formula (1) specified in claim 1 are suitable, owing to their low .DELTA..epsilon./.epsilon..perp. values for liquid crystal displays which have high information densities of for examples up to 10.sup.6 image dots and accordingly need to be highly multiplexible; compared with known compounds they offer improved application properties and are relatively simple to synthesize.