Abstract: The invention relates to compounds of general formula (I); in which R is an amino or guanidino group; R2 is acetyl or trifluoroacetyl; X is CONH, NHCO or O; n is an integer from 2 to 6; and Y is C2–C8 alkyl C3-8 cycloalkyl, C1–C4 alkoxyalkyl, an amino acid or dipeptide, or a pharmaceutically acceptable derivative thereof, methods for their preparation, pharmaceutical formulations containing them or their use in the prevention or treatment of a viral infection

Abstract: Compounds complying with the general formula (I) in which R either represents a halogen atom or a phenyl group substituted by one or more groups chosen from halogen atoms and (C1–C6)alkyl, (C1–C6)alkoxy, nitro, amino, trifluoromethyl, cyano, hydroxy, acetyl or methylenedioxy groups, or represents a pyridinyl group, a thienyl group, an indolyl group, or a pyrimidinyl group optionally substituted by one or more (C1–C6)alkoxy groups, where, of the two carbon-carbon bonds represented by , one is single and the other may be single or double. Therapeutic application.

Abstract: There are described novel rhodamine dye compounds and imaging members and imaging methods, including thermal imaging members and imaging methods, utilizing the compounds. The dye compounds exhibit a first color when in the crystalline form and a second color, different from the first color, when in the liquid, amorphous form.

Abstract: Lutein and zeaxanthin, the main carotenoids in marigold flowers, and capsanthin and capsorubin, the main carotenoids in red peppers are esterified mainly with C-18 fatty acids. The pigments were re-esterified without isolating them from the natural saponified extract using carboxylic acids in the range of C-1 to C-12 and their corresponding metallic salts in the presence of a catalyzing agent. Both the diester and monoester forms were obtained. It is expected that the pigment esters with a fatty acid of 12 or less carbons will have a better digestibility than the esters of xanthophylls in their natural state and better stability than the hydrolyzed xanthophylls. This will result in a better pigmentation capacity of the carotenoids for poultry or aquaculture.

Abstract: The present invention relates to substituted benzopyran derivatives, stereoisomers, and pharmaceutical acceptable salts thereof and processes for the preparation of the same. The compounds of the present invention are useful as Estrogen Receptor ? agonists. Such agonists are useful for the treating Estrogen Receptor ? mediated diseases such as prostate cancer.

Abstract: The present invention provides compounds of formula (I) wherein X, Y, R1, R2 and R3 are as defined hereinabove. The compounds of the present invention are modulators, especially antagonists, of the activity of chemokine CCR5 receptors. Modulators of the CCR5 receptor may be useful in the treatment of various inflammatory diseases and conditions, and in the treatment of infection by HIV and genetically related retroviruses.

Abstract: The invention relates to compounds of general formula (I), in which: R is an amino or guanidino group; R2 is acetyl or trifluoroacetyl; n and q are either the same or different and selected from 0, 1 or 2; and X is an optionally substituted phenyl, optionally substituted naphthyl or optionally substituted phenyl-Y-optionally substituted phenyl in which Y is selected from a covalent bond, CH2, CH2CH2, O or SO2, or a pharmaceutically acceptable derivative thereof, with the proviso that when X is phenyl or naphthyl, n and q are both 2 and when X is phenyl-Y-phenyl in which Y is a covalent bond, then n and q are not both 0, methods for their preparation, pharmaceutical formulations containing them or their use in the prevention or treatment of a viral infection

Abstract: This invention pertains to novel multiple quaternary ammonium salts and their derivatives represented by the formula: wherein each R1, R?1, R2, R?2, R3, R?3, R4 or R5 is independently selected from the group consisting alkyl, aryl, aralkyl and —CH2—CH(OR6)—CH2N+R1R2R3; wherein one or more R6 group is selected from the group consisting of: and wherein An? is an anion. This invention also pertains to novel multiple quaternary ammonium salts and their derivatives represented by the formula: wherein each R1, R?1, R2, R?2, R3 or R?3 group is independently selected from the group consisting of alkyl, aryl, aralkyl and —CH2—CH(OR4)—CH2N+R1R2R3; wherein one or more R4 group is selected from the group consisting of: and wherein An? is an anion.

Abstract: A compound which is a carbamate of formula: wherein R1 represents R2 represents a benzyl, phenethyl, furan-2-ylmethyl, furan-3-ylmethyl, thiophen-2-ylmethyl or thiophen-3-ylmethyl group or a straight or branched alkyl group having 3 to 8 carbon atoms, an alkenyl group having 3 to 8 carbon atoms, or a cycloalkyl group of 3 to 6 carbon atoms; p is 1 or 2 and the substitution in the azoniabicyclic ring may be in the 2, 3 or 4 position including all possible configurations of the asymmetric carbons; or a pharmaceutically acceptable salt thereof.

Abstract: The present invention relates to a ?3 adrenergic receptor agonist of Formula (I) or a pharmaceutical salt thereof; useful for treating Type II diabetes and/or obesity

Abstract: Process for manufacturing an oxirane by reaction between an olefin and hydrogen peroxide in the presence of a catalyst and an organic diluent, according to which the hydrogen peroxide is an aqueous hydrogen peroxide solution obtained by extraction, with substantially pure water, of the mixture derived from the oxidation of at least one alkylanthrahydroquinone, without subsequent washing and/or purification treatment.

Abstract: The present invention relates to a new deoxoartemisinin dimer and trimer, which have excellent anticancer activity and lower toxicity and are stable to acids, to a new deoxoartemisinin monomer of intermediate thereof, to preparations thereof, and to anticancer agents comprising the deoxoartemisinin dimer or trimer.

Abstract: This invention relates to processes for the preparation of 7-carboxy substituted steroid compounds of Formula I, wherein R1 is selected from H or COR4; R4 is C1–C6 alkyl or C1–C6 alkoxy; R3 is C1–C6 alkyl; Z1 is —CH2— or ?wherein O—COR4 is in the ? configuration; Z2 is —CH—; or Z1 and Z2 may be taken together to form a carbon-carbon double bond; Q is These intermediates are useful in the preparation of 7-carboxy substituted steroid compounds, and particularly, the invention is directed to novel and advantageous methods for the preparation of 9,11-?-epoxy-17-?-hydroxy-3-oxopregn-4-ene-?-7-21-dicarboxylic acid, ?-lactone, methyl ester (eplerenone; epoxymexrenone).

Abstract: A process for preparing an alkylene oxide, which process comprises: (i) oxidizing an alkylbenzene to obtain a stream comprising alkylbenzene hydroperoxide, (ii) contacting at least part of the alkylbenzene hydroperoxide obtained in step (i) with an olefin to obtain a product stream comprising an alkylene oxide (iii) separating alkylene oxide compound from the product stream of step (ii) to obtain (a) a residual product stream comprising alkylphenyl alcohol, and (b) alkylene oxide, (iv) feeding at least a part of the residual product stream comprising alkylphenyl alcohol to a reactor having a catalytic distillation zone, and concurrently in the reactor, (a) contacting the residual product stream comprising alkylphenyl alcohol with hydrogen in the catalytic distillation zone to convert the alkylphenyl alcohol in the residual product stream to alkylbenzene and form a reaction mixture, and (b) separating alkylbenzene from the reaction mixture by fractional distillation, (v) withdrawing a stream comprising a

Abstract: A class of binding ligands for cocaine receptors and other receptors in the brain. Specifically, a novel family of compounds shows high binding specificity and activity, and, in a radiolabeled form, can be used to bind to these receptors, for biochemical assays and imaging techniques. Such imaging is useful for determining effective doses of new drug candidates in human populations. In addition, the high specificity, slow onset and long duration of the action of these compounds at the receptors makes them particularly well suited for therapeutic uses, for example as substitute medication for psychostimulant abuse. Some of these compounds may be useful in treating Parkinson's Disease or depression, by virtue of their inhibitory properties at monoamine transporters.

Abstract: The present invention relates to new compounds of general formula having thrombin-inhibiting activity. Exemplary are: 1-Methyl-2-[4-(N-hydroxyamidino)-phenylaminomethyl]-benzimidazol-5-yl-carboxylic acid-(N-2-pyridyl-N-2-ethoxycarbonylethyl)-amide, and 1-Methyl-2-[4-(N-methoxycarbonylamidino)-phenylaminomethyl]-benzimidazol-5-yl-carboxylic acid-(N-2-pyridyl-N-2-hydroxycarbonylethyl)-amide.

Abstract: The present invention provides an improved process for the production of [(±)-endo]-4-amino-5-chloro-2-methoxy-N-(1-azabicyclo[3.3.1]non-4-yl)benzamide hydrochloride, compositions thereof, and intermediates thereto.

Abstract: Compounds of Formula I are useful as mediators of protein kinases and have activity as cell proliferation inhibitors: where X, R1–R7 and R9 are as defined herein.

Abstract: This invention is directed towards substituted aminoquinuclidine compounds useful as delta-opioid receptor modulators, delta-opioid receptor agonists useful as analgesics and delta-opioid receptor antagonists useful as immunosuppressants, antiinflammatory agents, agents for the treatment of neurological and psychiatric conditions, medicaments for drug and alcohol abuse, agents for treating gastritis and diarrhea, cardiovascular agents and agents for the treatment of respiratory diseases.

Abstract: Etoposide analogs with improved water-solubility such as 4?-O-Demethyl-4?-(N?,N?-dimethyl-glycyl)-4?-(4?-nitroanilino)-4-desoxy-podophyllotoxin (8) and 4?-O-Demethyl-4?-(N?,N?-dimethyl-glycyl)-4?-(4?-fluoroanilino)-4-desoxy-podophyllotoxin (9) are described, along with pharmaceutical formulations containing the same, methods of use thereof, and intermediates and methods of making the same.