Abstract: A compound of formula (I): wherein: represents an optionally substituted saturated carbon ring having from 4 to 8 ring members, R1 and R4, which may be identical or different, each represents hydrogen or acyl, R2 and R3, which may be identical or different, each represents hydrogen or alkyl, R5 and R6, which may be identical or different, each represents hydrogen or alkyl, or R5 and R6 together, with the nitrogen atom carrying them, form an optionally substituted nitrogen-containing heterocycle, stereoisomers thereof, and also addition salts thereof with a pharmaceutically acceptable acid. Medicinal products containing the same which are useful for treatment of glucose intolerance or of disorders associated with hyperglycaemia.

Abstract: This invention provides novel compounds, pharmaceutical compositions and methods of treating thrombotic disorders in mammals, the compounds having the formula: Wherein: Ar is phenyl, naphthyl, furanyl, benzofuranyl, indolyl, pyrazolyl, oxazolyl, fluorenyl, phenylcycloalkane where the cycloalkane can be cyclopropyl, cyclobutyl, cyclopentyl or cyclohexyl and Ar can be optionally substituted by 1 to 3 groups selected from C1-C6 alkyl, C1-C6 alkoxy, hydroxy, phenyl-(CH2)0-6—, phenyl-(CH2)0-6O—, C3-C6 cycloalkyl, —(CH2)—C3-C6 cycloalkyl, halogen, C1-C3 perflouroalkyl and C1-C3 perfluoroalkoxy where phenyl can be substituted with from 1 to 3 groups selected from C1-C6 alkyl, C1-C6 alkoxy, phenyl, halogen, trifluoromethyl or trifluoromethoxy; R1 is hydrogen, C1-C6 alkyl or phenyl-(CH2)1-6— where phenyl can be substituted with C1-C6 alkyl, C1-C6 alkoxy, halo, trifluoromethyl or trifluoromethoxy; R2 and R3 are H, C1-C6 alkyl, phenyl-(CH2)0-3—, halo and C1-C3 perflu

Abstract: The present invention contains halogenated 2-amino-3,4 heptenoic acid derivatives useful as nitric oxide synthase inhibitors.

Abstract: A process for conducting coupling reactions of aryl halides with unsaturated silanes is described. The processes use N-heterocyclic carbenes as ancillary ligands in these coupling reactions. A coupling of an aryl halide with an unsaturated silane can be carried out by mixing, in a liquid medium, at least one strong base; at least one aryl halide or aryl pseudohalide in which all substituents are other than silyl groups, wherein the aryl halide has, directly bonded to the aromatic ring(s), at least one chlorine atom, bromine atom, or iodine atom; at least one silane wherein the silicon atom is quaternary, wherein one group bound to the silicon atom is unsaturated at the alpha or beta position, and wherein each of the remaining groups bound to the silicon atom is a saturated hydrocarbyl or a saturated hydrocarbyloxy group; at least one nickel, palladium, or platinum compound, wherein the formal oxidation state of the metal is zero or two; and at least one N-heterocyclic carbene.

Abstract: Condensed heterocyclic compounds of general formula (I) wherein T is carbon or nitrogen; when T is carbon, then the bond between T and A is a double bond, the bond between A and Y is a single bond, and Y is oxygen, sulfur, or optionally substituted NH; or when T is nitrogen, then the bond between T and A is a single bond, the bond between A and Y is a double bond, and Y is nitrogen or optionally substituted CH; A is nitrogen or optionally substituted CH; R1 is hydrogen, halogen, alkyl, haloalkyl, hydroxymethyl, nitro, or cyano; R2 is hydrogen, halogen, alkyl, haloalkyl, hydroxymethyl, nitro, cyano, or the like; R3 is hydrogen, halogen, alkyl, haloalkyl, hydroxymethyl, nitro, cyano, or the like; R4 is hydrogen, halogen, alkyl, halo-alkyl, hydroxymethyl, nitro, or cyano; and Q is a saturated or unsaturated 5- or 6- membered heterocyclic ring containing one to four nitrogen atoms, or a saturated or unsaturated cyclopentylideneamino group containing one or two nitrogen heteroatoms and one oxygen or sulfur heteroa

Abstract: The invention relates to new C13-substituted estra-1,3,5(10)-trien-3-yl sulfamates of general formula I, wherein R1 represents an acyl residue, oxycarbonyl residue, aminocarbonyl residue, sulfonyl residue, or aminosulfonyl residue, and R15 represents ethyl, methods of preparing same, and pharmaceutical compositions containing these compounds. The compounds of the invention of general formula I inhibit the activity of steroid sulfatase (EC 3.1.6.2) and do not exhibit any estrogenic effect.

Abstract: The invention concerns the use of amide derivatives of formula (I) wherein: R1 and R2 are substituents such as hydroxy, C1-6alkoxy, mercapto, C1-6alkylthio, amino, C1-6alkylamino and di-(C1-6alkyl)amino; m and p are independently 0-3; R3 is C1-4alkyl; q is 0-4; and R4 is aryl or cycloalkyl; or a pharmaceutically acceptable salt thereof in the manufacture of a medicament for use in the treatment of diseases or medical conditions mediated by cytokines.

Abstract: This invention relates to novel phenyl oxazoles, thiazoles, oxazolines, oxadiazoles and benzoxazoles useful as neuro-protective agents.

Abstract: A composition containing a compound of the formula: wherein A is a nitrogen-containing heterocyclic group which may be substituted, R1 is a hydrogen atom, hydrocarbon group which may be substituted, or monocyclic aromatic heterocyclic group which may be substituted, R2 is a hydrogen atom or a lower alkyl group which may be substituted, R3, R4, R5, R6, R7, R8 and R9 are independently a hydrogen atom, a hydrocarbon group which may be substituted, a hydroxy group which may be substituted, a thiol group which may be substituted, an amino group which may be substituted, an acyl group or a halogen atom, a salt thereof or a prodrug thereof has steroid C17,20-lyase inhibitory activity, and is useful for preventing and treating for example, primary cancer of malignant tumor, its metastasis and recurrence thereof.

Abstract: This invention is related to new ethylaziridine derivatives of formula (I) and their preparation. The compounds are useful synthetic intermediates for the synthesis of HIV protease inhibitors and oligopeptide mimetics.

Abstract: The object of the present invention are diketopyrrolopyrroles of the general formula (I) wherein, independently of one another, Q1 and Q2 represent an optionally substituted, aromatic, isocyclic or heterocyclic group with 5 to 14 atoms in the ring, the heterocyclic group containing at least one oxygen, nitrogen or sulfur atom, and the R1 and R2 groups, independently of one another represent hydrogen or a Y—B+A− group, with the proviso that at least one of the R1 and R2 groups is not hydrogen; B+ is an aromatic, aliphatic, alicyclic, aromatic heterocyclic or non-aromatic heterocyclic, quaternary ammonium group or a quaternary phosphonium group; Y is an optionally substituted linear or branched C1 to C6 alkylene group and A− is an anion; a method for their synthesis as well as agents, containing compounds of formula (I), for dyeing keratin fibers.

Abstract: The present invention relates to a new substituted benzimidazoles, their preparation and their use as agents against parasitic protazoa.

Abstract: In order to carry out various vapor-phase reactions (e.g., the preparation of aziridine compounds by a vapor-phase intramolecular dehydration reaction) with industrial advantages, there is provided a process which can effectively prevent the adhesion of tarry matter to piping and the like. This process is applicable, for example, to the preparation of aziridine compounds by using a reactor for carrying out the vapor-phase intramolecular dehydration reaction of an alkanolamine, a collection column for collecting an aziridine compound present in the reaction gas, and a distillation column for distilling the collector liquid to obtain a purified aziridine compound, and is characterized in that at least the piping section extending from the outlet of the reactor to the inlet of the collection column is maintained at a temperature which is not lower than 200° C., or in that the reaction gas is brought into contact with a collector prior to its introduction into the collection column.

Abstract: A process for preparing diketopyrrolopyrrole pigments comprises conducting the elementary steps of pigment synthesis (reaction and hydrolysis) in a miniaturized continuous reactor.

Abstract: The present invention provides a compound of formula I which is useful as antiviral agents, in particular, as agents against viruses of the herpes family.

Abstract: The invention is directed to physiologically active compounds of general formula (I): wherein Het is an optionally substituted, saturated, partially saturated or fully unsaturated 8 to 10 membered bicyclic ring system containing at least one heteroatom selected from O, S or N; R1 is optionally substituted aryl, heteroaryl, alkyl, alkenyl, alkynyl, cycloalkyl or heterocycloalkyl; R2 is hydrogen, halogen, lower alkyl or lower alkoxy; Z1 is NR5; L1 is a —R6—R7— linkage (where R6 is alkylene, alkenylene or alkynylene and R7 is a direct bond, cycloalkylene, heterocycloalkylene, aryldiyl, heteroaryldiyl, —C(═Z3)—NR5—, —NR5—C(═Z3)—, —Z3—, —C(═O)—, —C(═NOR5)—, —NR5—, —NR5—C(═Z3)—NR5—, —SO2—NR5—, —NR5—SO2—, —O—C(═O)—, —C(═O)—O—, —NR5—C(═O)—O—

Abstract: The present invention provides a compound of formula I which is useful as antiviral agents, in particular, as agents against viruses of the herpes family.

Abstract: Novel small molecule polyamides that specifically bind with subnanomolar affinity to a predetermined sequence with potential use in molecular biology and human medicine are described. The designed compounds which target the minor groove of B-form double helical DNA offer a general approach for the control of gene-expression. Simple rules are disclosed which provide for rational control of the DNA-binding sequence specificity of synthetic polyamides containing N-methylpyrrole and N-methylimidazole amino acids. A series of molecular templates for polyamide design are disclosed which provide for small molecules which recognize predetermined DNA sequences with affinities and specificities comparable to sequence-specific DNA-binding proteins. The pyrrole-imidazole polyamides described herein represent a class of designed small molecules that can bind any predetermined sequence of double helical DNA.

Abstract: An efficient synthesis for the selective and efficient 1′-N derivatization of biotin is reported. The derivatized biotin acts as a stable analog of the carboxyphosphate intermediate in naturally-occurring biotin-mediated CO2 transfer. The synthesis may readily be scaled up to perform large-scale, selective acylations of biotin. The stable analog of the intermediate can inhibit the activity of the biotin carboxylase enzymes such as acetyl CoA carboxylase, and HIV protease. The functionalization at the 1′-N of biotin results in the attachment of an electrophilic “handle” amenable to reaction with a wide variety of nucleophiles to generate a new family of biotin analogs.

Abstract: The invention relates to a process for preparing 2-nitro-5-(phenylthio)anilines of formula (I) wherein R1 represents hydrogen, C1-C8-alkyl, C3-C8-cycloalkyl, C1-C8-alkoxy, or halogen and R2 represents hydrogen, C1-C8-alkyl, C3-C8-cycloalkyl, C1-C8-alkoxy, halogen, or C6-C10-aryl optionally substituted with C1-C8-alkyl, C1-C8-alkoxy, or halogen, by reacting, in a solvent, a 5-chloro-2-nitroaniline of the formula (II) wherein R1 is as defined for formula (I), with a thiophenol of the formula (III) wherein R2 is as defined for formula (I), and ammonia.