Abstract: A medicament comprising as an active ingredient a compound or a physiologically acceptable salt thereof represented by general formula (I): wherein R1 represents a dicarba-closo-dodecaboran-yl which may be substituted with a lower alkyl group, a lower alkenyl group, carboxyl group or the like; R2 represents carboxyl group, a lower alkoxycarbonyl group, or hydroxyl group; and X represents a single bond or a linking group such as —CO—Y1— wherein Y1 represents oxygen or —N(R3)— wherein R3 represents hydrogen or a lower alkyl.

Abstract: The invention provides novel compounds of the Formula (I) that stimulate rates of glucose oxidation in myocardial cells: 1

Abstract: Cyclopropanecarboxylates of lower alcohols are prepared by esterification of the corresponding cyclopropanecarboxylic acids with the corresponding lower alcohols in the presence of an acid catalyst, while maintaining a considerable stoichiometric excess of the cyclopropanecarboxylic acid with respect to the lower alcohol, keeping the temperature at from 100 to 200° C. and distilling off the cyclopropanecarboxylate together with the water of reaction and small amounts of alcohol. Cyclopropanecarboxylates of lower alcohols are valuable intermediates in the pharmaceutical and agrochemical sectors.

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

Abstract: Novel pharmaceutically/cosmetically-active bicyclic aromatic compounds have the structural formula (I): in which Ar1 is a radical having one of the structural formulae (a)-(c): Ar2 is a radical having one of the following formulae (d)-(h): and X is a radical having one of the following formulae (i)-(l): and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.

Abstract: This invention encompasses a method for the treatment or prevention of prostaglandin mediated diseases comprising administering to a mammalian patient a compound of formula I: in an amount that is effective to treat or prevent said prostaglandin mediated disease. Novel compounds are also disclosed.

Abstract: A process for preparing malonic diesters by carbonylation of haloacetic esters and reaction with monohydric alcohols and a base in the presence of a transition metal catalyst, preferably a catalytic cobalt carbonyl complex, using a stirred reactor with one or more internal heat exchangers. The stirred reactor preferably contains a sparging stirrer.

Abstract: The invention relates to a novel process for the preparation of certain cyclopropyl carboxylic acid esters and other cyclopropyl carboxylic acid derivatives; a novel process for the preparation of dimethylsulfoxonium methylide and dimethylsulfonium methylide; to the use of certain cyclopropyl carboxylic acid esters in a process for the preparation of intermediates that can be used in the synthesis of pharmaceutically active entities; and to certain intermediates provided by these processes.

Abstract: A Pd(OAc)2/diazabutadiene system has been developed for the catalytic cross-coupling of aryl halides with arylboronic acids. A combination of the diazabutadiene DAB-Cy (1, N,N′-Dicyclohexyl-1,4-dizabutadiene) and Pd(OAc)2 was found to form an excellent catalyst for the Suzuki-Miyaura cross-coupling of various aryl bromides and activated aryl chlorides with arylboronic acids.

Abstract: This invention relates to compounds of Formula (I) where Z is an amine, alcohol or derivative thereof, and the ketone analog thereof.

Abstract: The invention concerns hydrogenated phenanthrenes of formula I wherein the parameters have the meanings given in the text and their use in liquid crystal compositions.

Abstract: A carboxylic acid tertiary alkyl ester (Chemical formula 1) of high purity is obtained at a high yield ratio, by continually adding an esterification agent possessing a monovalent acid group, which agent is ester-interchangeable with a tertiary alcohol, to a mixed fluid of a carboxylic acid and a tertiary alcohol: R1(COOR2)n.

Abstract: There is disclosed chiral copper complex catalyst composition, which is obtained by contacting an optically active N-salicylideneaminoalcohol compound of formula (1): with a mono-valent or di-valent copper compound in an inert solvent, wherein R1 and R2 represent an alkyl group and the like, X1 and X2 represent a hydrogen atom, a halogen atom, a nitro group, an alkyl group, an alkoxy group, a cyano group or the like, and the amount of the mono-valent or di-valent copper compound is less than 1 mole per 1 mole of the optically active N-salicylideneaminoalcohol compound of formula (1), and a process for producing an optically active cylopropane-carboxylic acid ester using the same.

Abstract: The invention pertains to a process for preparing carbetapentane tannate. The process involves the steps of heating carbetapentane to a temperature of about 80 to about 120° C. and slowly adding tannic acid to the carbetapentane while agitating the reaction mixture. Preferably, no water or any other solvent or diluent is utilized in the process.

Abstract: A compound, of the following formula: Also disclosed is a pharmaceutical composition containing a pharmaceutically effective amount of the compound.

Abstract: A method of preparing a compound of formula I is described.

Abstract: A process for the preparation of 2-(4-methylphenyl)benzoic acid C1-6alkyl esters by reaction of a sulfonic derivative of formula wherein R is C1-6alkyl and R1 is optionally perfluorinated C1-6alkyl or optionally substituted C1-6aryl, with a 4-methylphenylzinc halide.

Abstract: Compounds having the formulas below, where R is H, lower alkyl, or a pharmaceutically acceptable salt, and where R1 represents i-propyl, t-butyl or n-butyl groups, have selective RXR retionoid agonist activity.

Abstract: There is provided a method for producing a cyclopropanecarboxylate of formula (1): 1

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: A process for preparing tert-butyl 4′-methyl-2-biphenylcarboxylate characterized in that 4′-methyl-2-biphenylcarboxylic acid is reacted with isobutene in the presence of an acid catalyst. According to the present invention, tert-butyl 4′-methyl-2-biphenylcarboxylate having high quality can be conveniently and industrially advantageously prepared in a high yield under mild reaction conditions such as ambient temperatures without complicated procedures or any hazardous solvents.

Abstract: This invention provides a process for conducting Kumada coupling reactions. The processes of the present invention make use of N-heterocyclic carbenes as ancillary ligands in Kumada couplings of aryl halides. A Kumada coupling can be carried out by mixing, in a liquid medium, at least one aryl halide, wherein the aryl halide has, directly bonded to the aromatic ring(s), at least one halogen atom selected from the group consisting of a chlorine atom, a bromine atom, and an iodine atom; at least one Grignard reagent; at least one metal compound comprising at least one metal atom selected from nickel, palladium, and platinum, wherein the formal oxidation state of the metal is zero or two; and at least one N-heterocyclic carbene.

Abstract: This invention provides a process for conducting Stille coupling reactions. The processes of the present invention make use of N-heterocyclic carbenes as ancillary ligands in Stille couplings of aryl halides.

Abstract: Applicants have developed a process for the oxidation of ketones to esters. The process involves contacting the ketone with hydrogen peroxide and a catalyst at oxidation conditions. The catalyst is a molecular sieve represented by the empirical formula: (MwSnxTiySi1−x−y−zGez)O2 where M is a trivalent metal such as aluminum or boron. These molecular sieves have a microporous three dimensional framework structure of at least SiO2 and SnO2 tetrahedral units, a crystallographically regular pore system and the characteristic x-ray diffraction pattern of zeolite beta.

Abstract: Retinoid antagonist compounds have been found to be useful in the prevention and/or minimization of surgical adhesion formation. Also provided by the invention are certain novel substituted (5,6)-dihydronaphthalenyl compounds which are retinoid antagonists and possess the above-mentioned property in addition to their use as antiinflammatory agents for chronic skin inflammatory diseases, as agents for the treatment of rheumatic diseases and as agents for the treatment of various tumors as well as non-malignant proliferative skin conditions.

Abstract: “Biphenyl derivatives substituted with an aromatic or heteroaromatic radical, and pharmaceutical and cosmetic compositions containing them” in which: Ar represents an aromatic or a heteroaromatic radical optionally substituted, in particular, with an alkyl or a carboxyl group, R2 and R3 represent, in particular, H or alkyl, or R2 and R3, taken together, form a 5- or 6-membered ring, R4 and R5 represent, in particular, H or halogen, R6 represents, in particular, H or lower alkyl, and the salts of the compounds of formula (I). These compounds can be used in particular in the treatment of dermatological complaints associated with a keratinization disorder, and for combating ageing of the skin.

Abstract: A process is disclosed for preparing 2-aryl-substituted indenes by reacting an indene with an arene compound substituted with an halogen atom, preferably a iodine atom, or with an organosulphonate group, said reaction being carried out in a basic medium in the presence of a palladium catalyst. The compounds obtainable by this process can be used to prepare metallocene compounds with transition metals such as titanium, zirconium or hafnium, which are useful as catalyst components in the polymerization of olefins.

Abstract: A process for the preparation of preparation of farnesyltransferase inhibitors of formula (I) or pharmaceutically acceptable salts or prodrugs thereof, is disclosed.

Abstract: An electoclinic device having two spaced cell walls each bearing electrode structures and treated on at least one facing surface with an alignment layer, a layer of a smectic liquid crystal material enclosed between the cell walls, where the liquid crystal material contains one or more of the compounds described by formula I as defined in the specification.

Abstract: The present invention relates to a process for the preparation of 4′-bromomethyl-biphenyl derivatives of the formula: by reacting a 4′-methyl-biphenyl derivative of the formula: with a brominating agent a in a hydrobromic acid/alkali metal bromate system in a two-phase medium, and under photo-iradiation, where R is as defined in the specification.

Abstract: The invention relates to novel stilbene compounds having the general formula (I): as well as to pharmaceutical compositions for use in human or veterinary medicine, including dermatological, rheumatic, respiratory, cardiovascular and ophthalmic conditions and cosmetic compositions and methods of use thereof.

Abstract: The present invention provides a process for preparing biaryl compounds comprising reacting an arylzinc reagent with an arylchloride in the presence of a nickel catalyst or a palladium catalyst. The present invention specifically provides a process for the preparation of 2-(4′-methylphenyl)benzonitrile comprising reacting a 4-methylphenylzinc reagent with 2-chlorobenzonitrile in the presence of a nickel catalyst or a palladium catalyst.

Abstract: Novel pharmaceutically/cosmetically-active triaromatic compounds have the structural formula (I): ##STR1## and are useful for the treatment of a wide variety of disease states, whether human or veterinary, for example dermatological, rheumatic, respiratory, cardiovascular, bone and ophthalmological disorders, as well as for the treatment of mammalian skin and hair conditions/disorders.

Abstract: Novel phenyl derivatives which are useful as endothelin receptor antagonists.

Abstract: Compounds of Formula 1, Formula 2 or Formula 3 where X is O, S, or (CR.sub.1 R.sub.1).sub.n where n is 0, 1 or 2; Y is a bivalent radical having Formula 4 or Formula 5 where o is an integer from 1 to 4 ##STR1## or Y is a bivalent aryl or 5 or 6 membered heteroaryl radical having 1 to 3 heteroatoms selected from N, S and O, said aryl or heteroaryl groups being unsubstituted, or substituted with 1 to 3 C.sub.1-6 alkyl or with 1 to 3 C.sub.1-6 fluoroalkyl groups; and the remaining symbols have the meaning described in the specification, have RXR selective retinoid agonist-like activity.

Abstract: The present invention relates to specific adamantyl or adamantyl group derivative containing retinoid compounds induce apoptosis of cancer cells. These adamantyl retinoid derivatives are useful for the treatment of many cancers and solid tumors, especially androgen-independent prostate cancer, skin cancer, pancreatic carcinomas, colon cancer, melanoma, ovarian cancer, liver cancer, small cell lung carcinoma, non-small cell lung carcinoma, cervical carcinoma, brain cancer, bladder cancer, breast cancer, neuroblastoma/glioblastoma, and leukemia. Also, the invention relates to novel adamantyl or adamantyl group derivative compounds which are useful as active agents for the treatment or prevention of keratinization disorders and other dermatological conditions, and other diseases.

Abstract: A process for preparing chiral isomers of N-protected 2-azetidinemethanol compounds, particularly N-(phenylmethyl)-2-azetidinemethanol and N-BOC-2-azetidinemethanol, and especially the (R)-isomers thereof, as well as O-substituted derivatives thereof.

Abstract: This invention relates to the use of 2-(diisopropylamino)-ethyl-1-phenyl-cyclopentane-carboxylate or 2-(diisopropylamino)-ethyl-1-phenyl-cyclohexane-carboxylate, or a pharmaceutically accceptable salt thereof, for treatment of urinary incontinence or irritable bowel syndrome (IBS).

Abstract: The invention to provide novel tetralin compounds, liquid crystal materials and liquid crystal compositions, which can constitute a liquid crystal element affording a wide operating temperature range, a high switching speed and a small consumption of electric power as well as a stable contrast.The tetralin compound of the invention is represented by the following formula [I] ##STR1## wherein R.sup.1 is an alkyl group or a polyfluoroalkyl group of 3-20 carbon atoms (wherein one --CH.sub.2 -- or 2 or more --CH.sub.2 -- or --CF.sub.2 -- not adjacent to each other in these groups may be substituted with --O--), X is --COO--, --O-- or a single bond, A is each independently selected from ##STR2## (Z.sup.1 and Z.sup.2 are hydrogen or fluorine), Y is a group selected from --COO--, --CH.sub.2 O--, --OCH.sub.2 --, and --CH.sub.2 CH.sub.2 --, R.sup.1 * is an optically active group represented by the formula --C*H--(CF.sub.3)--(CH.sub.2).sub.m --O--C.sub.n H.sub.2n+1 [II].

Abstract: This invention relates to compositions for and methods of treating, preventing or ameliorating cancer and other proliferative diseases as well as methods of inducing wound healing, treating cutaneous ulcers, treating gastrointestinal disorders, treating blood disorders such as anemias, immunomodulation, enhancing recombinant gene expression, treating insulin-dependent patients, treating cystic fibrosis patients, inhibiting telomerase activity, treating virus-associated tumors, especially EBV-associated tumors, modulating gene expression and particularly augmenting expression of a tumor suppressor gene, inducing tolerance to an antigen and treating, ameliorating or preventing protozoan infection. The methods of the invention use metabolically stabilized oxyalkylene esters.

Abstract: The present invention relates to a process for the preparation of trifluoromethylated derivatives of the formula CF.sub.3 CCl.dbd.CHCH.sub.2 OC(.dbd.O)R, wherein R is unsubstituted or substituted C.sub.1 to C.sub.6 straight chain or branched alkyl, unsubstituted or substituted C.sub.3 to C.sub.7 cycloalkyl, unsubstituted or substituted C.sub.2 to C.sub.12 alkenyl, a benzyl group unsubstituted or substituted with R', a phenyl group unsubstituted or substituted with R'; R' is an unsubstituted or substituted C.sub.1 to C.sub.6 straight chain or branched alkyl; and wherein where R and/or R' are substituted each is substituted with R', by reaction of HCFC-353 with carboxylic acid salts. The trifluoromethylated derivatives, particularly CF.sub.3 CCl.dbd.CHCH.sub.2 OC(.dbd.O)CH.sub.3, are versatile intermediates for the synthesis of a wide variety of trifluoromethylated organic compounds, which find utility as pharmaceuticals, agricultural chemicals, and materials such as liquid crystals.

Abstract: Compositions with protein kinase C-modulatory, anti-inflammatory and other activities are disclosed.

Abstract: The present invention relates to novel substituted acrylic acids, to methods for their preparation, compositions containing them, and their use for treatment of human and animal disorders, to their use for purification of proteins or glycoproteins, and to their use in diagnosis. The invention also relates to modulation of the activity of molecules with phospho-tyrosine recognition units, including protein tyrosine phosphatases (PTPases) and proteins with Src-homology-2 domains, in in vitro systems, microorganisms, eukaryotic cells, whole animals and human beings.

Abstract: The present invention relates to trans-olefin compounds represented by the general formula (1) useful as an ingredient of liquid crystal composition, trans-olefin compounds useful as intermediate of pesticides, medical drugs, liquid crystal materials and the like, a process for producing those trans-olefin compounds, a liquid crystal composition containing the trans-olefin compound as an active ingredient, and a liquid crystal element using the liquid crystal composition. ##STR1## (In the general formula (1), R.sup.1, A.sup.1, A.sup.2, A.sup.3, Z and R.sup.2 are same as defined in the specification. Also, m, p, q, n, r, s and t are each an integer as defined in the specification.

Abstract: The diphenyl-cyclopropene derivatives of the instant invention are kappa opioids useful in the treatment of pain, inflammation, Parkinsonism, dystonia, cerebral ischemia, diuresis, asthma, psoriasis, irritable bowel syndrome, and stroke.The compounds are K-agonists which are centrally acting and peripherally selective acting.

Abstract: The present invention relates to inhibitors of COX-2, compositions which contain such compounds and methods of use. The compounds are represented by formula I: ##STR1## and include pharmaceutically acceptable salts and esters thereof.

Abstract: An acrylonitrile derivative expressed by the following general formula I, a composition comprising the derivative and having an improved viscosity and optical anisotropy, and a liquid crystal display device: ##STR1## wherein rings A.sup.1 to A.sup.3 represent phenylene, cyclohexylene, dioxane, or pyrimidine, R.sup.

Abstract: A swallow-tail-shaped liquid crystal compound of the following general formula (1), ##STR1## wherein A is --O--, --COO-- or a single bond (--), m is an integer of 4 to 12, and n is an integer of 2 to 4.The above swallow-tail-shaped liquid crystal compound of the present invention is a novel achiral anti-ferroelectric liquid crystal and can be converted to an optically active anti-ferroelectric liquid crystal by mixing it with an optically active compound as a chiral dopant.

Abstract: The invention is novel analogs of 9-cis-retinoic acid which are useful for the treatment and prevention of coronary artery disease and to protect against premature atherosclerosis by increasing HDL levels. The invention includes processes for preparing the novel 9-cis-retinoic acid analogs.

Abstract: Compounds having anti-inflammatory and other activities are disclosed. The compounds are derived from phorboids of the diterpene- and benzolactam-classes.