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Disclosed are compounds of formula (I) and pharmaceutically acceptable salts thereof. The compounds of formula (I) inhibit tyrosine kinase activity of JAK3, thereby making them useful for the treatment of inflammatory and autoimmune diseases.

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Compounds of the formulas I, II, or III STR1 wherein R is an alkyl group containing 2 to 6 carbon atoms optionally substituted by one or more halogen atoms, a cycloalkyl group containing 3 to 6 ring carbon atoms optionally substituted by one of more alkyl groups containing 1 or 2 carbon atoms, an aryl or aralkyl group containing 6 to 10 carbon atoms optionally ring-substituted by one or more halogen atoms or alkyl groups containing 1 or 2 carbon atoms or an alkoxycarbonyl alkyl group in which the alkyl portions contain from 1 to 6 carbon atoms, are useful as insecticides, particularly against the species of the Order Lepidoptera.

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Chiral porous zirconium phosphonates containing metal complex moieties are provided, synthesized via a molecular building block approach, and characterized by a variety of techniques including TGA, adsorption isotherms, XRD, SEM, IR, and microanalysis. These hybrid solids may be used for enantioselective heterogeneous asymmetric hydrogenation of aromatic ketones with remarkably high e.e. values of up to 99.2%. Similarly prepared chiral porous solids may be used for asymmetric hydrogenation of beta-keto esters with e.e.’s of up to 95%. The solid catalysts can also be easily recycled and reused multiple times without the loss of activity and enantioselectivity. Ready tunability of such a molecular building block approach allows the optimization of these hybrid materials to provide practically useful heterogeneous asymmetric catalysts.

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SAR studies of 7-phenylpyrrolo[1,2-alpha]pyrimid-4-ones 1 and 2, and 2-phenylimidazolo[1,2-alpha]-pyrimidines 3 and 4, as nonpeptide human GnRH receptor antagonists, lead us to believe that the aromatic ring at position-2 of 4 is no longer crucial for the binding once an aryl group is incorporated at postion-6. We report here the use of a 2-alkyl group on the imidazolo[1,2-alpha]- pyrimidone core to generate potent GnRH receptor antagonists. This discovery enabled us to obtain smaller but equally potent GnRH receptor antagonists.

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Polar phosphonic acid-derived Ru-BINAP systems were used to catalyze asymmetric hydrogenation of beta-keto esters in room temperature ionic liquids (RTILs) with complete conversions and ee values higher than those obtained from homogeneous reactions in MeOH (up to 99.3%), and were recycled by simple extraction and used for four times without the loss of activity and enantioselectivity.

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High acid crudes contain large amounts of naphthenic acids (NAs), which lead to severe corrosion in oil refinery equipment and serious environmental problems. The goal of this study is to develop a non-catalytic supercritical methanol (scMeOH) route for effective deacidification of NA mixtures and high acid crudes (Laguna and Bachaquero-13). Various reaction parameters, including temperature, pressure, reaction time, and NA-to-methanol ratio, are explored to find effective reaction conditions for reducing the total acid number (TAN) of the mixtures. Almost complete TAN reduction of naphthenic acid (96.9%) is achieved at 400 C, 10 MPa, and 3 h. The reaction in scMeOH at 400 C, 30 MPa and 1 h is effective in the TAN reaction of high acid crudes (93.6-94.0%). The chemical composition of the liquid products obtained under the different reaction conditions, analyzed using gas chromatography-mass spectroscopy, show that esters are the most abundant species, indicating that esterification with scMeOH is the major reaction pathway. The most recalcitrant NA species, which remained after the reaction, are found to be 2-ethyl-2,3,3-trimethyl-butanoic acid and 2,3-dimethyl-2-(1-methylethyl)-butanoic acid. This is attributed to the branched hydrocarbons located near the carboxylic acid groups, which hinder the access of methanol molecules.

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The invention comprises novel chiral metal complex compounds of the formula (I) wherein M, PR2, R3 and R4 are outlined in the description, its stereoisomers, in the form as a neutral complex or a complex cation with a suitable counter ion. The chiral metal complex compounds can be used in asymmetric reactions, particularly in asymmetric reductions of ketones, imines or oximes.

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Asymmetric hydrogenation of keto esters using a BisP*-RuBr2 catalyst is reported. High enantioselectivities up to 98% were achieved in the hydrogenation of beta-keto esters.

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Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (”ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (”CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.

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Urea-containing hydroxyethylamine peptide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.

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