Abstract: A novel process for preparing 3,4-di(carbocyclyl or heterocyclyl)thiophenes comprising reacting a compound of Formula IV with a ring cyclizing reagent to form the compound of Formula V to yield a compound of Formula V wherein R1, R2 and R3 are as defined in the specification.

Abstract: The present invention relates to a process for preparing stereoisomerically enriched 3-heteroaryl-3-hydroxycarboxylic esters by reducing 3-heteroaryl-3-oxocarboxylic esters in the presence of ruthenium-containing catalysts.

Abstract: Compounds of formula (I) as defined herein, or a pharmaceutically acceptable salt, or an in-vivo-hydrolysable ester thereof, are useful as antibacterial agents. Processes for their manufacture and pharmaceutical compositions containing them are described.

Abstract: A new process for the preparation of 4-(4-pyridinyl)benzoic acid, or a salt thereof.

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 &agr;- and &bgr;-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: The invention relates to intermediate products and a new process for the production of benzocycloheptene C.

Abstract: Compounds of formula (I): or a pharmaceutically acceptable salt thereof, or solvate of either entity, wherein R4 is a guanidinyl moiety and the other substituents are as defined in the text, are urokinase inhibitors.

Abstract: Compounds of the formula where the symbols have the meaning described in the application, have retinoid-like or retinoid antagonist-like biological activity.

Abstract: This application relates to a compound of formula I (or a prodrug thereof or a pharmaceutically acceptable salt of the compound or prodrug 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: The present invention relates to compounds and pharmaceutical compositions which are proteomimetic and to methods for inhibiting the interaction of an alpha-helical protein with another protein or binding site. Methods for treating diseases or conditions which are modulated through interactions between alpha helical proteins and their binding sites are other aspects of the invention.

Abstract: A prodrug composition containing a cinnamate moiety and a biologically active molecule moiety which can be released by hydrolysis or activated by light is disclosed. The cinnamate moiety can have substituents of various electronically donating or electronically withdrawing groups to modify the cinnamate moiety's electric properties as well as photo reactivities for the purpose of achieving a proper hydrolysis rate of the acyl bond between the biologically active molecule moiety and the cinnamic acid backbone. The biologically active molecule can be any biologically active agent or diagnostic, for example, a chemotherapeutic such as a paclitaxel, campotothecin, doxorubicin, amethopterin, etoposide, or fluconazole. The prodrug composition can be modified to add a carrier moiety on the prodrug composition for targeting or to facilitate uptake of the drug. The prodrug compositions can be activated with an energy source to release the drug at the desired site.

Abstract: Energy-reversible acyl conjugates, intermediates, and related compositions are disclosed.

Abstract: The present invention relates to a single pot process for the preparation of metal picolinates useful as dietary supplement from alpha picoline, said process comprising hydrosulphonation of alpha picoline with sulphuric acid; heating the reaction mixture thus obtained between the range of 150° to 210° C. followed by oxidation with any suitable oxidizing agent to obtain alpha picolinic acid sulphate, and treating the thus obtained alpha picolinic acid sulphate with a metal salt solution to obtain corresponding metal picolinate.

Abstract: Invented is an improved process for preparing aromatic ring-fused cyclopentane derivatives. Preferred compounds prepared by this invention are indane carboxylates and cyclopentano[b]pyridine derivatives. The most preferred compounds prepared by this inventino are (+)(1S, 2R, 3S)-3-[2-(2-hydroxyeth-1-yloxy)-4-methoxyphenyl]-1-(3,4-methylenedioxyphenyl)-5-(prop-1-yloxy)indane-2-carboxylic acid and pharmaceutically acceptable salts thereof and (+)(1S, 2R, 3S)-3-[(2-carboxymethoxy-4-methoxyphenyl)-1- (3,4-methylenedioxyphenyl)-5-(prop-1-yloxy)indane-2-carboxylic acid and pharmaceutically acceptable salts thereof. Also invented are novel intermediates useful in preparing these compounds.

Abstract: Certain imidazo pyridines/quinolines of the formula: where n is 0, 1, 2; X is independently selected from the group consisting of C1-4alkyl, bromine, chlorine, iodide, trifluoromethyl, C1-4alkoxy, —SO2NH2, nitro, and two adjacent X may be fused to form the moiety:  whereby a saturated, partially unsaturated or aromatic six-membered fused ring is formed; Y is independently selected from the group consisting of hydrogen, hydroxy, C1-4alkyl, C1-4alkoxy, trifluoromethyl and phenyl; and Z is independently selected from the group consisting of hydroxy, C1-4alkyl, bromine, chlorine, iodide, trifluoromethyl, C1-4alkoxy, —SO2NH2 and nitro; are &agr;2-adrenoceptor modulators which are useful in the treatment of hypertension, glaucoma, sexual dysfunction, depression, attention deficit hyperactivity disorder, Parkinsonism, the need for anesthesia, cardiac arrythmia or the need for analgesia.

Abstract: Histone deacetylase is a metallo-enzyme with zinc at the active site. Compounds having a zinc-binding moiety, such as, for example, a carboxylic acid group, can inhibit histone deacetylase. Histone deacetylase inhibition can repress gene expression, including expression of genes related to tumor suppression. Accordingly, inhibition of histone deacetylase can provide an alternate route for treating cancer, hematological disorders, e.g., hemoglobinopathies, and genetic related metabolic disorders, e.g., cystic fibrosis and adrenoleukodystrophy.

Abstract: Amidomethyl esters, carbonylmercaptomethyl esters, keto-containing esters, amidomethyl thioesters, amidomethyl amides, and methylene dithioesters are disclosed. The novel compounds have two carbonyl groups connected by a linking moiety having an oxygen, sulfur or nitrogen attached to a methylene group, to which is further attached a sulfur, nitrogen or CH2 group. Methods of treating illnesses and conditions, such as cancer, hemological disorders, inherited metabolic disorders and others, using these compounds are also disclosed.

Abstract: The new process for preparing ethyl 3-(2,5,6-trihalopyridin-3-yl)-3-oxopropionate from 2,5,6-trihalo-3-cyanopyridine in accordance with the present invention comprises reacting 2,5,6-trihalo-3-cyanopyridine with ethyl haloacetate at the presence of a transition metal in powder in anhydrous solvent, and treating the resulting solution with HCl. In particular, the new process for preparing ETPO from THCP comprises heating 2,5,6-trihalo-3-cyanopyridine and a transition metal in powder in anhydrous solvent to the boiling point, reacting 2,5,6-trihalo-3-cyanopyridine with ethyl haloacetate by adding ethyl haloacetate dropwise to the resulting solution, cooling the resulting solution to about 10° C., adding concentrated HCl and distilled water to the resulting solution during agitation thereof, and filtering the product.

Abstract: Substituted 2-phenylpyridines of the formula I in which the substituents and the index m are defined in the specification.

Abstract: The invention relates to a process for preparing substituted pyridines in a simple and cost-effective manner in good yields by reacting substituted 1,4-dihydropyridines with methyl nitrite in the presence of an acid that contains less than 20% by weight of oxidizing components.

Abstract: The invention relates to 2-(3-alkenylbenzoyl)cyclohexane-1,3-diones of the formula I where the variables have the following meanings: R1, R2 are hydrogen, nitro, halogen, cyano, thiocyanato, alkyl, haloalkyl, alkoxyalkyl, alkenyl, alkynyl, —OR6, —OCOR7, —OSO2R7, —SH, —S(O)nR8, —SO2OR6, —SO2NR6R9, —NR9SO2R7 or —NR9COR7; R3 is hydrogen, halogen, alkyl, haloalkyl, alkoxy, alkenyl, alkynyl; R4, R5 are hydrogen, nitro, halogen, cyano, thiocyanato, alkyl, haloalkyl, cycloalkyl, alkenyl, cycloalkenyl, alkynyl, alkoxy, alkylthio, haloalkoxy, —COR10, —CO2R10, —COSR10, —CONR10R11, —C(R12)═NR13, —PO(OR10)(OR11); unsubstituted or substituted alkyl, heterocyclyl, heterocyclylalkyl, phenyl, phenylalkyl, hetaryl or hetarylalkyl; or R4 and R5 together form an alkanediyl chain which can be substituted and/or can be interrupted by a hetero atom; Q is an unsubstituted or substituted cyclohexane-1,3-dione ring wh

Abstract: A process of preparing 4-substituted pyridine compounds via pyridine betaine compounds.

Abstract: This invention relates to a key intermediate in the synthesis of an endothelin antagonist the synthesis of this key intermediate via an asymmetric conjugate addition reaction.

Abstract: The present invention relates to compounds and derivatives thereof, their synthesis, and their use as integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors &agr;v&bgr;3, &agr;v&bgr;5, and/or &agr;v&bgr;6 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation, wound healing, viral disease, tumor growth, and metastasis.

Abstract: N-Heterocyclic derivatives selected from the group consisting of the following formulae: 1

Abstract: Liquid crystalline compounds useful in super twisted nematic liquid crystal displays are described and have the formula: wherein n is 1-5; m is 0-5; p is 0, 1 or 2; q is 0, 1 or 2 p+q is less than or equal to 3; A1, A2, A3 are independently chosen from 1,4-disubstituted benzene, 2,5-disubstituted pyrimidine, 1,5-disubstituted pyridine, 2,6-disubstituted naphthalene which may be laterally substituted with F, Cl, Br or CN, trans-1,4-disubstituted cyclohexane, 2,5-disubstituted dioxane, 2,5-disubstituted thiophene, 2,5-disubstituted furan, 2,5-disubstituted thiodiazole Z1 may be COO, OOC, OCH2, O; Z2, Z3 are independently chosen from a direct bond, COO, OOC, C2H4, CH2O, OCH2, C4H8, C3H6O, (E)—CH═CHC2H4, (E)—CH═CHCH2O, —C≡C—; R1 is alkyl, and may contain up to 20 carbon atoms and may be branched or a straight chain; provided that at least one of, A1, A2, A3 is selected from 1,4-disubstituted thiophene.

Abstract: Compounds, compositions, and methods for modulating processes mediated by Retinoid X Receptors using retinoid-like compounds which have activity selective for members of the subclass of Retinoid X Receptors (RXRs), in preference to members of the subclass of Retinoic Acid Receptors (RARs). Examples of such compounds are bicyclic benzyl, pyridinyl, thiophene, furanyl, and pyrrole derivatives. The disclosed methods employ compounds for modulating processes selectively mediated by Retinoid X Receptors.

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

Abstract: Process for the coupling of

Abstract: This invention relates to stable, quaternized vinlypyridine carboxylate home-, co- and ter-polymers, useful as dye transfer inhibitors and polymers complexable with active agrochemical, pharmaceutical or cosmetic agents for controlled release thereof, and to a commercial process for the synthesis of said polymers in high yield and purity.

Abstract: A cephem compound, wherein the cephem ring has a substituent at the 3-position, which substituent is shown by the formula II, wherein Het is a mono- or polycyclic heterocyclic group comprising one or more hetero atoms selected from the group consisting of N, O and S which may be the same or different from each other; R1 is hydrogen, an optionally substituted lower alkyl or an optionally substituted lower alkenyl; A is an optionally substituted lower alkylene, an optionally substituted lower alkenylene or a single bond; B is an optionally substituted imino or a single bond; or A and B taken together may form a single bond; and D is a single bond or a group of the formula (a): The cephem compounds of the present invention are useful as antibiotic agents.

Abstract: The novel benzamide derivative represented by formula (1) and the novel anilide derivative represented by formula (13) of this invention has differentiation-inducing effect, and are, therefore, useful a therapeutic or improving agent for malignant tumors, autoimmune diseases, dermatologic diseases and parasitism. In particular, they are highly effective as an anticancer drug, specifically to a hematologic malignancy and a solid carcinoma.

Abstract: A poly(oxyalkylene)pyridyl or piperidyl ester having the formula: ##STR1## or a fuel-soluble salt thereof; wherein A is a nitrogen-containing ring selected from the group consisting of 3-pyridyl, 4-pyridyl, 3-piperidyl and 4-piperidyl; R.sub.1 and R.sub.2 are independently hydrogen or lower alkyl having 1 to about 6 carbon atoms and each R.sub.1 and R.sub.2 is independently selected in each --O--CHR.sub.1 --CHR.sub.2 -- unit; R.sub.3 is hydrogen, alkyl having 1 to about 100 carbon atoms, phenyl, aralkyl having about 7 to about 100 carbon atoms or alkaryl having about 7 to about 100 carbon atoms; x is an integer from 0 to 4; and n is an integer from about 5 to about 100.The poly(oxyalkylene)pyridyl and piperidyl esters of the present invention are useful as fuel additives for the prevention and control of engine deposits.

Abstract: Complexes of a selected class of chiral ligands with molybdenum, tungsten or chromium, preferably molybdenum, are effective as catalysts in highly enantioselective and regioselective alkylation of allylic substrates. Such compositions provide a versatile and low-cost alternative to existing catalysts.

Abstract: Liquid crystalline compounds useful in super twisted nematic liquid crystal displays are described and have the formula: ##STR1## wherein n is 1-5;m is 0-5;p is 0, 1 or 2;q is 0, 1 or 2p+q is less than or equal to 3;A.sub.1, A.sub.2, A.sub.3 are independently chosen from 1,4-disubstituted benzene 2,5-disubstituted pyrimidine, 1,5-disubstituted pyridine, 2,6-disubstituted naphthalene which may be laterally substituted with F, Cl, Br or CN, trans-1,4-disubstituted cyclohexane 2,5-disubstituted dioxane, 2,5-disubstituted thiophene, 2,5-disubstituted furan, 2,5-disubstituted thiodiazoleZ.sub.1 may be COO, OOC, OCH.sub.2, O;Z.sub.2, Z.sub.3 are independently chosen from a direct bond, COO, OOC, C.sub.2 H.sub.4, CH.sub.2 O, OCH.sub.2, C.sub.4 H.sub.8, C.sub.3 H.sub.6 O, (E)--CH.dbd.CHC.sub.2 H.sub.4, (E)--CH.dbd.CHCH.sub.2 O, --C.tbd.C--;R.sub.1 is alkyl, and may contain up to 20 carbon atoms and may be branched or a straight chain; provided that at least one of, A.sub.1, A.sub.2, A.sub.

Abstract: Derivatives of mutiline of formula (1A) and pharmaceutically acceptable salts and derivatives thereof, in which R.sup.1 is ethyl or vinyl, Y is a carbamoyloxy group, in which the N-atom is unsubstituted, or mono- or di-substituted, are useful in the treatment of bacterial infections.

Abstract: A process for the preparation of a polycyclic dye of Formula (1) which comprises steps: i) reaction of a compound of formula (2) with a compound of formula (3) or a derivative thereof to form an intermediate of formula (4) and ii) reaction of the intermediate of formula (4) with an aromatic compound of formula (5): B--H optionally in the presence of an oxidizing agent, wherein: A and B each independently is optionally substituted aryl; and X.sup.1 and X.sup.2 each independently is --H, halo, alkyl, or alkoxy.

Abstract: Disclosed is to provide an azine derivative as a novel liquid crystal compound, a novel process for the preparation of an asymmetrical azine in a high reaction yield with an extremely small amount of by-products such as symmetrical azines, a nematic liquid crystal composition containing the azine derivative which exhibits a broad driving temperature range and an excellent response for the desired high birefringence index, a liquid crystal display device such as TN-LCD, STN-LCD and TFT-LCD having improved electro-optical properties comprising the liquid crystal composition as a constituent material, and a light-scattering type liquid crystal display system which exhibits a suppressed memory phenomenon, a higher uniformity in turbidity for display and improved display properties and response against temperature change while maintaining and improving the required display properties such as fast switching time, lower voltage driving, higher light-control layer resistivity and higher contrast ratio even in the for

Abstract: This invention relates to a process for the preparation of a key intermediate using an chiral additive to effect an asymmetric conjugate addition.

Abstract: This invention relates to a compound of formula I ##STR1## These compounds are leukotriene antagonists and as such can be used in treating various diseases associated with leukotrienes.

Abstract: Compounds of the formula ##STR1## and compounds of the formula ##STR2## or their salts have the potent ability to bind to retinoic acid receptors thus useful in treating psoriasis and rheumatoid arthritis.

Abstract: The invention relates to novel .alpha.-fluoroacrylic acid derivatives, to active compound/antidote combinations which comprise .alpha.-fluoroacrylic acid derivatives and are outstandingly suitable for use in crops of useful plants, to their use and to methods for protecting crop plants.

Abstract: Compounds of formula (I), ##STR1## wherein X is a --CO.sub.2 H or --CONHOH group; R.sub.4 is a group --CHR.sup.x R.sup.y wherein R.sup.x and R.sup.y independently represent optionally substituted phenyl or monocyclic heteroaryl rings, which optionally may be linked covalently to each other by a bond or by a C.sub.1 -C.sub.4 alkylene or C.sub.2 -C.sub.4 alkenylene bridge; and R.sub.1, R.sub.2, R.sub.3 and R.sub.5 are as defined in the specification are selective inhibitors of stromelysin-1 and matrilysin relative to human fibroblast collagenase and 72 KDa gelatinase.

Abstract: The invention relates to 7-?5-hydroxy-2-(hydroxyhydrocarbyl or heteroatom-substituted hydroxy hydrocarbyl)-3-hydroxy-cyclopentyl(enyl)! heptanoic or heptenoic acids and derivatives of said acids, wherein one or more of said hydroxy groups are replaced by an ether group. The compounds of the present invention are potent ocular hypotensives, and are particularly suitable for the management of glaucoma.

Abstract: The subject invention features substituted N-heteroaromatic compounds, libraries of substituted N-heteroaromatic compounds, and methods of synthesis thereof. For example, the present invention provides methods for synthesizing substituted N-heteroaromatic compounds, and is particularly amenable to the generation of libraries of substituted N- heteroaromatic compounds by combinatorial chemistry. The methods of the invention generally feature the reaction of O-linked heteroaromatic N-oxides with nucleophiles to produce substituted N-heteroaromatic compounds.

Abstract: The present invention relates to novel 4,4-(disubstituted)cyclohexan-1-carboxylate monomers and related compounds, pharmaceutical compositions containing these compounds, and their use in treating allergic and inflammatory diseases and for inhibiting the production of Tumor Necrosis Factor (TNF).

Abstract: Compounds of Formula 1 ##STR1## wherein Z is selected from the group consisting of the radicals shown in Formula 2 and in Formula 3, ##STR2## Y is cycloalkyl or cycloalkenyl of 3 to 8 carbons optionally substituted with one or two R.sub.4 groups, or Y is selected from phenyl, pyridyl, thienyl, furyl, pyrrolyl, pyridazinyl, pyrimidinyl, pyrazinyl, thiazolyl, oxazolyl, and imidazolyl, said groups being optionally substituted with one or two R.sub.4 groups, the divalent Y radical being substituted by the Z and --CR.sub.1 .dbd.CR.sub.1 --CR.sub.1 .dbd.CR.sub.1 groups on adjacent carbons; X is S, O, or NR.sub.5 ; n is 1 or 2; R.sub.1 and R.sub.2 independently are H, lower alkyl or fluoroalkyl; R.sub.3 is hydrogen, lower alkyl, Cl or Br; R.sub.4 is lower alkyl, fluoroalkyl or halogen; R.sub.5 is H or lower alkyl, and B is hydrogen, COOH or a pharmaceutically acceptable salt thereof, COOR.sub.8, CONR.sub.9 R.sub.10, --CH.sub.2 OH, CH.sub.2 OR.sub.11, CH.sub.2 OCOR.sub.11, CHO, CH(OR.sub.12).sub.2, CHOR.sub.

Abstract: Substituted pyridines of the general formula: ##STR1## wherein R.sup.1 is hydroxyl or chlorine, and a) X is hydrogen or chlorine, R.sup.2 and R.sup.3 together are .dbd.O, R.sup.4 is a group of the formula --OR.sup.5 and R.sup.5 is hydrogen, C.sub.1 -C.sub.4 -alkyl or benzyl, orb) X is hydrogen and R.sup.2, R.sup.3 and R.sup.4 together are .dbd.N--NH--, orc) X and R.sup.2 each is hydrogen and R.sup.3 and R.sup.4 together are --O--, ord) X and R.sup.2 each is hydrogen, R.sup.3 is hydroxyl and R.sup.4 is amino or hydroxyl.The compounds are obtained by subjecting nicotine to microbiological oxidation to give 5-succinoyl-2-pyridone, followed by chemical reactions. The compounds are suitable as intermediates for the preparation of pharmaceutically active compounds.

Abstract: An effective and efficient process for the preparation of dialkyl arylmalonates of formula I, ##STR1## (ring A and R are defined in the specification). In this process, an arylmethylhalide of formula II ##STR2## is treated with magnesium in an inert solvent, the resulting Grignard reagent is treated with a dialkyl carbonate or an alkyl chloroformiate, and the resulting reaction mixture is treated with a base.

Abstract: Substituted 2-phenylpyridines I ##STR1## where substituents have the meaning described in the specification and their use as herbicides; for the desiccation/defoliation of plants.