Abstract: The present invention provides analogues of autoinducer molecules that are derivatized to allow their attachment to other molecules and surfaces. Libraries of the autoinducer analogues are also contemplated. Also provided are methods for using the compounds of the invention to produce compositions, such as immunoconjugates, antibodies and vaccines, which are useful for treating and preventing disease states in a subject. The compositions of the invention are also useful in various assays, including assessing the autoinducer load in a subject.

Abstract: A production method of a compound represented by the formula wherein R1 and R2 are each a hydrogen atom, an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, R3 is an electron-withdrawing group, and R4, R5 and R6 are each a hydrogen atom or an optionally substituted hydrocarbon group, or a salt thereof, is provided as an industrially advantageous production. method for forming a carbon-carbon bond at the 5-position of oxazole, which method includes reacting a compound represented by the formula wherein the symbols in the formula are as defined above, or a salt thereof, with a compound represented by the formula wherein the symbols in the formula are as defined above, or a salt thereof, in the presence of an acid or a base.

Abstract: Compounds of formula (I), their salts and solvates, wherein the substituents are as described herein, are FKBP inhibitors.

Abstract: This invention relates to new oxazolidinones having a cyclopropyl moiety, which are effective against aerobic and anerobic pathogens such as multi-resistant staphylococci, streptococci and enterococci, Bacteroides spp., Clostridia spp. species, as well as acid-fast organisms such as Mycobacterium tuberculosis and other mycobacterial species. The compounds are represented by structural formula I: its enantiomer, diastereomer, or pharmaceutically acceptable salt or ester thereof.

Abstract: The present invention concerns novel sugar derivatives of indolocarbazoles and pharmaceutical formulations thereof which exhibit topoisomerase-I activity and are useful in inhibiting the proliferation of tumor cells.

Abstract: The instant invention provides crystal forms of 5-chloro-N-[(1S,2R)-3-[3R,4S]-3,4-dihydroxy-1-pyrrolidinyl]-2-hydroxy-3-oxo-1-(phenyl) methyl)propyl]-1H-indole-2-carboxamide (I) processes for the production of such crystal forms; pharmaceutical compositions comprising such crystal forms; and methods of treating glycogen phosphorylase dependent diseases, or conditions with such crystal forms, or such pharmaceutical compositions.

Abstract: A compound selected from the group consisting of a compound of formula I a compound of formula II and when the compound of formula I and II comprises an amino group pharmaceutically acceptable ammonium salts thereof, wherein R1, R2, Cx, n, R3, R4, R5, Y are as defined in the specification.

Abstract: Compounds are provided which have the structure wherein Q is C or N, X1 is CH or N and, A, E, M, G, X2, X3, X4, R1, R2, R2a, R2b, R2c, R3, Y, x, m, and n are as defined herein, which compounds are useful as antidiabetic, hypolipidemic, and antiobesity agents.

Abstract: The present invention relates to novel indolin-2-one derivatives of formula: to the preparation and to the pharmaceutical compositions comprising them. These compounds have an affinity for oxytocin receptors.

Abstract: This invention relates to the use of compounds as inhibitors of the fatty acid synthase FabH.

Abstract: Dyes and pigments present in candle wax compositions are particularly well stabilized against color fade or color change by a combination of a UV absorber and a metal compound, particularly a tin compound. The further addition of a hindered amine or antioxidant is highly beneficial.

Abstract: Heterocyclic compounds of formula (I), wherein R1 is carboxy or protected carboxy, R2 is aryl which may have suitable sustituent(s), R3 is aryl which may have suitable substituent(s), R4 is hydrogen, lower alkyl, hydroxy or aryl, A1 is lower alkylene, (a) is (b), etc., —A3— is (c), etc. and n is 0 or 1, and pharmaceutically acceptable salts thereof which are useful as a medicament.

Abstract: This invention relates to phthalimido derivatives of the formula wherein X is —N═ or —CH═, and R1 to R4 and m are as defined in the specification, as well as their pharmaceutically acceptable salts. The invention further relates to pharmaceutical compositions containing these compounds, a method of treating a disease by administering a therapeutically effective amount of at least one of these compounds, and a process for their preparation for the treatment or prevention of diseases in which MAO-B inhibitors might be beneficial.

Abstract: This invention relates to novel thiazolo[3,2-a]benzoimidazole derivatives represented by the following general formula (I). The compounds provided by the invention act specifically on metabotropic glutamate receptors and are used as medicaments. The invention also provides novel compounds useful as intermediates for the synthesis of the compounds of the invention. (Symbols in the formula represent the following meanings. R1: carbamoyl, carbonyl, oxy, amino, carbonylamino or the like which may be substituted; R2: hydrogen, lower alkyl or the like; and R3, R4 and R5: hydrogen, lower alkyl and the like which may be the same or different from one another.

Abstract: The present invention includes nuclear receptor heterodimer and nuclear receptor-coactivator pepetide assays for identifying ligands for nuclear receptors, utilizing scintillation proximity and fluorescence resonance energy transfer (FRET), and methods of using identified ligands.

Abstract: Process for preparing purified citalopram or one of its salts that comprises the purification of citalopram by selective extractions of citalopram or of its impurities with organic solvents and water under specific conditions of pH and temperature. The crude citalopram can be prepared by a process that comprises reacting 1-[3-(dimethylamine)propyl]-1-(4-fluorophenyl)-1,3-dihydro-5-bromoisobenzofuran with copper cyanide.

Abstract: Compounds of the formula: where the formula variables are as defined in the disclosure, advantageously inhibit or block the biological activity of the picornaviral 3C protease. These compounds, as well as pharmaceutical compositions containing these compounds, are useful for treating patients or hosts infected with one or more picornaviruses, such as RVP. Intermediates and synthetic methods for preparing such compounds are also described.

Abstract: Novel processes and intermediates are provided for the synthesis of derivatives of 4-amino-3-hydroxypyrrole-2-carboxylic acids that are useful as monomers for polyamides capable of binding dsDNA. According to one preferred reaction scheme, an alkyl alkoxymethylene nitroacetate (Formula VIII) is prepared by reaction of a trialkyl orthoformate or orthoacetate with a nitroacetate ester in the presence of a carboxylic anhydride. The compound of Formula VIII is condensed with an N-substituted glycine to yield an N-substituted (2-nitro-2-alkoxycarbonyl)vinyl glycinate ester (Formula VII). Ring closure in the presence of an alkali metal alkoxide yields a 4-nitro-3-hydroxypyrrole-2-carboxylic ester (Formula V). After blocking of the 3-hydroxy group to produce a further intermediate (Formula IV), the 4-nitro group is reduced to a 4-amino group (Formula III), and the 4-amino group is then blocked by reaction with a dicarbonate diester to produce the fully blocked intermediate (Formula II).

Abstract: The invention provides compounds of general formula (I) wherein R1 is H or C1-C6 alkyl; R2 and R3, together with the interconnecting atoms form a 4 to 8-membered saturated ring containing one or two heteroatoms (including the nitrogen to which R2 is attached) wherein a second heteroatom, if present, is selected from oxygen, nitrogen and sulfur, with the proviso that said ring cannot contain two adjacent heteroatoms; Z is CF3, OCF3, C1-C6alkylthio or C1-C6alkoxy; Y is hydrogen, halogen, —ORa, Ra or C1-C6alkylthio, and wherein Ra is C1-C4 alkyl optionally substituted with fluorine atoms; or when Z and Y are attached para and meta to the ether linkage linking rings A and B, Z and Y are linked so that, together with the interconnecting atoms, Z and Y form a fused 5 to 7-membered carbocyclic or heterocyclic ring which may be saturated, unsaturated or aromatic, and wherein when Z and Y form a heterocyclic ring, in addition to carbon atoms, the linkage contains one or two heteroatoms independently selected fro

Abstract: Novel compounds are provided that comprise esters of antiviral phosphonomethoxy nucleotide analogs with carbonates and/or carbamates having the structure —OC(R2)2OC(O)X(R)a, wherein R2 independently is H, C1-C12 alkyl, aryl, alkenyl, alkynyl, alkyenylaryl, alkynylaryl, alkaryl, arylalkynyl, arylalkenyl or arylalkyl which is unsubstituted or is substituted with halo, azido, nitro or OR3 in which R3 is C1-C12 alkyl; X is N or O; R is independently H, C1-C12 alkyl, aryl, alkenyl, alkynyl, alkyenylaryl, alkynylaryl, alkaryl, arylalkynyl, arylalkenyl or arylalkyl which is unsubstituted or is substituted with halo, azido, nitro, —O—, —N═, —NR4—, —N(R4)2— or OR3, R4 independently is —H or C1-C8 alkyl, provided that at least one R is not H; and a is 1 or 2, with the proviso that when a is 2 and X is N, (a) two R groups can be taken together to form a carbocycle or oxygen-containing heterocycle, or (b) one R additionally can be OR3.