Abstract: Disclosed and claimed are cocoa extracts such as polyphenols or procyanidins, methods for preparing such extracts, as well as uses for them, especially as antineoplastic agents and antioxidants. Disclosed and claimed are antineoplastic compositions containing cocoa polyphenols or procyanidins and methods for treating patients employing the compositions. Additionally disclosed and claimed is a kit for treating a patient in need of treatment with an antineoplastic agent containing cocoa polyphenols or procyanidins as well as a lyophilized antineoplastic composition containing cocoa polyphenols or procyanidins. Further, disclosed and claimed is the use of the invention in antioxidant, preservative and topiosomerase-inhibiting compositions and methods.

Abstract: A sulfonamide compound of the formula (I): R1—SO2NHCO—A—X—R2  (I) wherein R1 is alky, alkenyl, alkynyl and the like; A is an optionally substitutedheteropolycyclic group except benzimidazolyl, indolyl, 4,7-dihydrobenzimidazolyland 2,3-dihydrobenzoxazinyl; X is alkylene, oxa, oxa(lower)alkylene and the like; and R2 is optionally substituted aryl, substituted biphenylyl and the like, a salt thereof and a pharmaceutical composition comprising the same. The sulfonamide compound is effective for the diseases treatable based on their blood sugar level-depressing activity, cGMP-PDE (especially PDE-V)-inhibiting activity, smooth muscle relaxing activity, bronchodilating activity, vasodilating activity, smooth muscle cell suppressing activity, and antiallergic activity.

Abstract: Sordarin derivatives prepared from C-11-hydroxysordarin are antifungal agents useful in the treatment and/or prevention of human and animal fungal infections, as well as in the control of phytopathogenic fungi in crops.

Abstract: The present invention is directed to a continuous process for the preparation of fructopyranose sulfamate derivatives of the general formula (I) 1

Abstract: A compound of the formula wherein the substituents are defined as in the specification and their pharmaceutically acceptable salts having NOS and ROS activity.

Abstract: Bicyclic cyclopropane derivatives of the general Formula (I) 1

Abstract: The present invention provides a novel 7a-alkoxy-4H-pyrano-[3,2-d]-oxazol-2(3H)-one represented by the formula (I): wherein R1 and R2 each represent a hydrogen atom, an alkyl group, an alkenyl group, an aryl group or an aralkyl group; R3 represents an alkyl group, a cyclo-alkyl group, an alkenyl group, an aryl group or an aralkyl group, provided that a 2-alkenyl group is excluded from the alkenyl group of R3; and R4 represents an alkyl group, an aryl group, an alkoxycarbonyl group or a cyano group, and a process for producing the same which comprises reacting 5-alkoxy-2(3H)-oxazolone with an &agr;,&bgr;-unsaturated ketone in the presence of a Lewis acid in a solvent.

Abstract: The present invention relates to substituted cyclohexenes, to their use as well as to their preparation method. These compounds have powerful long lasting natural fruity grapefruit notes with minty and fresh green tonalities.

Abstract: The invention describes novel substituted aryl compounds that are cyclooxygenase 2 (COX-2) selective inhibitors and novel compositions comprising at least one cyclooxygenase 2 (COX-2) selective inhibitor, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or, optionally, at least one therapeutic agent, such as, steroids, nonsterodal antiinflammatory compounds (NSAID), 5-lipoxygenase (5-LO) inhibitors, leukotriene B4 (LTB4) receptor antagonists, leukotriene A4 (LTA4) hydrolase inhibitors, 5-HT agonists, 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) inhibitors, H2 antagonists, antineoplastic agents, antiplatelet agents, thrombin inhibitors, thromboxane inhibitors, decongestants, diuretics, sedating or non-sedating anti-histamines, inducible nitric oxide synthase inhibitors, opioids, analgesics, Helicobacter pyl

Abstract: Disclosed are processes for producing a (2S) or (2R) 4-oxo-chroman-2-yl acyl compounds and chroman-2-yl acyl compounds, esters or amides thereof as well as derivatives thereof. Such processes may involve chiral synthesis or achiral synthesis, preferably coupled with a resolution procedure. Such compounds, particularly (2S) or (2R) acetic acid esters, are useful intermedates for producing platelet aggregation inhibitors and/or are themselves potent platelet aggregation inhibitors. Further disclosed are processes for making derivatives of such substantially pure, or enhanced compositions of single (2R) or (2S) enantiomer intermediates or processes for producing final products or salts from such desired enantiomers.

Abstract: The invention concerns an electro-luminescent device in which the luminescent layer contains a compound of general formula I as doping agent or as luminescent compound, whereby the radicals R1 to R12 are identical or are different, and mean hydrogen, straight chain or branched C1-C6 alkyl, aralkyl, aryl or substituted aryl; R1 and R2 and/or R3 and R4 and/or R4 and R5 and/or R5 and R11 and/or R8 and R5 and/or R4 and R12 can form an alicyclic, heterocyclic or aromatic ring; R5 can furthermore be H, OH, OR9, N,N-di-(C1-C6) alkylamino, acetylamino or halogen; R6 and R7 together can form an alicyclic or heterocyclic ring; A1 and A2 are identical or different and are -CN, -NO2 or -COOR8; X is -CH, -CR11 or N; and Y is O, -NH, -NR12, S or Se. The doping agents together luminesce predominately red with very good quantum efficiency together with the luminescent compound as a function of concentration.

Abstract: The use of cyclic sugar ketones of the formula in which R1 and R2 are hydrogen, C1-C22-alkyl, C2-C22-alkenyl or phenyl, R3 is C1-C4-alkoxy, phenyl-CH2—O— or a group of the formula R4 is hydrogen or R3 and R4 together are a group of the formula and n is zero or 1, as catalysts for peroxygen compounds.

Abstract: Novel, enantiopure, substituted 4-deoxypentenosides (4-DPs) and related dihydropyrans (DHPS) are prepared from common carbohydrates via a novel process. The 4-DPs and related DHPs are amenable to a broad range of stereoselective transformations and are used as synthetic intermediates to prepare a variety of enantiopure tetrahydropyrans (THPs), including rare or exotic sugars and other complex THPs of commercial or medicinal value. In one embodiment of the instant invention, 4-DPs are converted to L-sugars in a novel process that offers distinct advantages over known synthetic methods.

Abstract: A method for treating tissue of a patient comprising, in combination, mixing a drug with a solidifiable biological material, chemically treating the drug with the biological material with a crosslinking agent, loading the solidifiable drug-containing biological material onto a medical device, solidifying the drug-containing biological material; and delivering the medical device to a target tissue for treating the tissue.

Abstract: Compounds of formula (1) are described, wherein q is zero or the integer 1, 2 or 3; R which when present may be attached to any available carbon or nitrogen atom of the bicyclic heteroaromatic ring of formula (1) is an atom or group -L3(Alk3)wL4(R8)u; X is an O atom or a S(O)m atom or group in which m is zero or the integer 1 or 2 or an NR group; Y is a N atom or a CR1a group in which R1a is a group R or a group R1; R1 which may he on any available carbon atom of the bicyclic heteroaromatic ring of formula (1) is a hydrogen atom or a group -Alk1L1CyAlk2L2D; provided that at least one but not both of R1 and R1a is the group -Alk1L1CyAlk2L2D. The compounds are potent inhibitors of the interaction between CCR-3 and it chemokine ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders in which inhibition of this interaction can have a beneficial effect.

Abstract: The present invention relates to a novel class of sulfonamides of formula I which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity. The sulfonamides of formula I have the structure: wherein A, B, D, D′, E, G and R7 are as defined above.

Abstract: Disclosed is a novel composition comprising a novel bi-cyclic compound, which is expected to be pharmaceutically active, and a glyceride. The stability of the bi-cyclic compound can be improved significantly by dissolving the same in a glyceride.

Abstract: Disclosed is a novel methine compound, for examples, which is represented by the following formula (I): 1

Abstract: Compounds of the formula 1

Abstract: A light emitting device material comprising a compound represented by the following formula (I): wherein R1, R2 and R3, which may be the same or different, each represents an aryl group, a heterocyclic group or an aliphatic hydrocarbon group, provided that at least one of R1, R2 and R3 represents an aryl group or a heterocyclic group, containing a group represented by the following formula (II): wherein R4, R5 and R6, which may be the same or different, each represents a hydrogen atom or a substituent; X1 represents an oxygen atom, a sulfur atom, N—RX1 or CRX2RX3; RX1, RX2, RX3, which may be the same or different, each represents a hydrogen atom or a substituent; R4, R5, R6 and X1 may be linked to each other to form a ring; Y represents an oxygen atom, a sulfur atom, or N—RY1; and RY1 represents a hydrogen atom or a substituent.

Abstract: The present invention relates to 3-methyl-chromane or thiochromane derivatives, pharmaceutically acceptable salts, stereoisomers or hydrates thereof, and an anti-estrogenic pharmaceutical composition which comprises the above compound as an active component.

Abstract: This invention is related to novel carboxyl substituted chroman derivatives which are useful in the treatment of beta-3 receptor mediated conditions.

Abstract: This invention is directed to substituted (aminoiminomethyl or aminomethyl) dihydrobenzofurans and benzopyrans that inhibit Factor Xa, pharmaceutical compositions comprising these compounds and their use for inhibiting Factor Xa or treating pathological conditions in a patient that may be ameliorated by administration of such compounds. This invention is also is also directed to substituted (aminoiminomethyl or aminomethyl) dihydrobenzofurans and benzopyrans which directly inhibit both Factor Xa and Factor IIa (thrombin), to pharmaceutical compositions comprising these compounds, to intermediates useful for preparing these compounds and to a method of simultaneously directly inhibiting both Factor Xa and Factor IIa (thrombin).

Abstract: Ortho-sulfonamido aryl hydroxamic acids are provided which are useful, inter alia, for the inhibition of matrix metalloproteinases and the treatment of conditions associated with overexpression of MMPs.

Abstract: Novel intermediates of the formula They are used in the preparation of macrocyclic analogs.

Abstract: The present application relates to new carboxylic acid amides of general formula 1

Abstract: The invention relates to novel heteroethynylenic compounds having the general formula (I): as well as to the use of these compounds in pharmaceutical compositions intended for use in human or veterinary medicine (dermatological, rheumatic, respiratory, cardiovascular and ophthalmological complaints in particular), or alternatively in cosmetic compositions.

Abstract: 2-Alkoxydecahydro-2,3a,4,4,7-pentamethyl-3,7a-methano-7aH-indeno[5,6-b]furans are valuable novel woody fragrances for the preparation of perfume oils.

Abstract: Compounds of Formula 1 1

Abstract: The present invention provides novel compounds, novel compositions, methods of their use, and methods of their manufacture, where such compounds are pharmacologically useful inhibitors of Protein Tyrosine Phosphatases (PTPase's) such as PTP1B. CD45, SHP-1, SHP-2, PTP&agr;, LAR and HePTP or the like. The compounds are useful in the treatment of type I diabetes, type II diabetes, impaired glucose tolerance, insulin resistance, obesity, immune dysfunctions including autoimmunity diseases with dysfunctions of the coagulation system, allergic diseases including asthma, osteoporosis, proliferative disorders including cancer and psoriasis, diseases with decreased or increased synthesis or effects of growth hormone, diseases with decreased or increased synthesis of hormones or cytokines that regulate the release of/or response to growth hormone, diseases of the brain including Alzheimer's disease and schizophrenia, and infectious diseases.

Abstract: Intermediate compounds of the formulas for use in the preparation of macrocyclic analogs.

Abstract: The present invention relates to novel 3-(cycloalkano-heteroarylidenyl)-2-indolinone compounds and physiologically acceptable salts and prodrugs thereof which are expected to modulate the activity of protein tyrosine kinases and therefore to be useful in the prevention and treatment of protein tyrosine kinase related cellular disorders such as cancer.

Abstract: Compounds of formula (I) 1

Abstract: The present invention provides novel compounds of formula I 1

Abstract: The present invention provides novel compounds of formula I 1

Abstract: Compounds and methods for treating prostaglandin mediated diseases, and certain pharmaceutical compositions thereof are disclosed.

Abstract: The present invention relates to a linker shown by the following formula (I):

Abstract: The present invention relates to novel genipin derivatives which have an excellent liver protection activity with little cytotoxicity, and these compounds are so stable in vivo that they do not induce any side effects.

Abstract: A 1,2-dioxetane derivative represented by the general formula: wherein R1, R2, R3, R4, R5, R6 and R7 each independently represents hydrogen atom, an alkyl group, or an aryl group, or one or more than one pair of R2 and R3, R4 and R5, and R6 and R7 can together form a cyclic alkyl group. The compound is easily handled because the compound itself is very stable, and it is capable of emitting light with a very high efficiency.

Abstract: This invention involves compounds having the following structure: 1

Abstract: The present invention relates to a novel genipin derivative represented by formula (I), which has anti hepatitis B virus (HBV) activity, in which R.sub.1 represents lower alkyl, benzyl, etc., R.sub.2 represents hydroxymethyl, formyl, acetyl, etc., R.sub.3 represents methoxycarbonyl, formyl, etc., its pharmaceutically acceptable salt, and stereoisomer.

Abstract: The present invention provides a novel amino acid dysiherbaine which is a non-NMDA type glutamate receptor agonist as well as salts and biological precursors thereof, which are useful as experimental materials for elucidating neuronal death or the functions of signal transduction of the central nervous system associated with glutamate receptors and which provide a possibility for the development of a glutamate receptor blocker.A novel amino acid dysiherbaine represented by the formula (1): ##STR1## is obtained by purifying an aqueous extract of a sponge such as D. herbacea on the basis of toxicity to mice by liquid chromatography using Sephadex LH20 or the like and HPLC using a C18 column, and optionally converting it into a biological precursor thereof.

Abstract: 5-(Dioxabicyclohept-6-yl)cyclohexenone oxime ethers of the formula I ##STR1## where: R.sup.1 is hydrogen, the equivalent of an agriculturally useful cation, C.sub.1 -C.sub.10 -alkylcarbonyl, C.sub.1 -C.sub.10 -alkylsulfonyl, C.sub.1 -C.sub.10 -alkylphosphonyl, benzoyl, benzenesulfonyl or benzenephosphonyl;R.sup.2 is C.sub.1 -C.sub.6 -alkyl;R.sup.3 is in each case, independently of the others, hydrogen or C.sub.1 -C.sub.4 -alkyl;Z is a C.sub.1 -C.sub.6 -alkylene, C.sub.3 -C.sub.6 -alkenylene or C.sub.3 -C.sub.6 -alkynylene chain which may carry an exo-methylene substituent (.dbd.CH.sub.2) and/or in each case one to three additional substituents selected from the group consisting of C.sub.1 -C.sub.3 -alkyl substituents and halogen atoms,is a C.sub.3 --C.sub.6 -alkylene or C.sub.4 --C.sub.6 -alkenylene chain which may carry one to three C.sub.1 -C.sub.3 -alkyl substituents and which contains, in addition to methylene or methine units, one of the following bridge members: oxygen, sulfur, --SO--, --SO.sub.

Abstract: Novel iridoid derivatives represented by general formula (I): and a vascularization inhibitor having for its active ingredient said derivative are disclosed. This vascularization inhibitor has remarkable vascularization inhibitory effects unaccompanied by serious adverse side effects, which is useful for the treatment and prevention of various diseases accompanied by abnormal acceleration of vascularization.

Abstract: This invention relates to compounds of formula (I) ##STR1## which are useful as modulators of D.sub.3 receptors, in particular as antipsychotic agents.

Abstract: The compounds of Formula I ##STR1## are useful as immunosuppressive agents.

Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention.

Abstract: The invention thus provides compounds of Formula (I) ##STR1## wherein R.sup.1 and R.sup.2 which may be the same or different represent H, C.sub.1-6 alkyl or substituted alkyl or C.sub.3-7 cycloalkyl; or aryl;R.sup.3, and R.sup.4 which may be the same or different represent H, halogen, C.sub.1-6 alkyl; or substituted aryl;R.sup.5 is H or C.sub.1-6 alkyl;n is an integer 0, 1 or 2and m is an integer 1, 2, 3, or 4;the dotted line indicates the presence or absence of an additional bond; and pharmaceutically acceptable solvates (e.g. hydrates) thereof.

Abstract: 4-Cyano-4-deformylsordarin derivatives are antifungal agents useful in the treatment and/or prevention of human and animal fungal infections, as well as in the control of phytopathogenic fungi in crops.

Abstract: A compound having the structure: ##STR1## wherein (a) n is from about 1 to about 3;(b) X is selected from the group consisting of O, S, SO, or SO.sub.2 ;(c) Y is independently hydrogen or straight, branched or cyclic alkyl having from 1 to about 4 carbon atoms, or the Y's are bonded together to form an alkanyl ring having from about 3 to about 7 atoms;(d) Z is hydrogen or straight, branched or cyclic alkyl having from 3 to about 10 atoms other than hydrogen; and(e) Het is a heteroaryl group comprising one or more rings each ring containing from about 5 to about 6 atoms other than hydrogen and wherein the group contains at least one heteroatom selected from O, N, or S.Pharmaceutical compositions comprising such compounds, and methods of treating inflammation or pair using such compounds.