Abstract: The invention relates to compounds of the formula I in which the radicals have the meanings stated in the text, their stereoisomeric forms, and their physiologically tolerated salts, physiologically functional derivatives and process for their preparation. The compounds are suitable for the treatment of disorders of metabolism, such as type 2 diabetes.

Abstract: Disclosed are polymorphs of 1-(5-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl)-3-[4-(2-morpholin-4-yl-ethoxy)-naphthalen-1-yl]-urea and processes from making the same.

Abstract: An alkyl ether represented by the general formula: or its salt. This compound has activity to protect neurons, activity to accelerate nerve regeneration and activity to accelerate neurite extension and hence is useful as a therapeutic agent for diseases in central and peripheral nerves.

Abstract: Phenyl compounds substituted at the 1-position with a fused bicyclo moeity formed from a five-membered heterocycle fused to a six-membered carbocycle, to a six-membered aryl, or to a six-membered hetaryl, and further optionally substituted at the 3,4 positions, are mGluR5 modulators useful in the treatment of psychiatric and mood disorders such as, for example, schizophrenia, anxiety, depression, and panic, as well as in the treatment of pain and other diseases.

Abstract: Bis-heterocyclic compounds of general formula (I) are described which are useful as antitumour and cheomsensitising agents.

Abstract: The invention concerns compounds of general formula (I) wherein: the group X represents a —NR4, —CH?N or —CHR5-NR4-group; the group Y represents an oxygen or sulphur atom or a NR, —CR5, —CHR5-, —CR5=CR6- or —CHR5-CHR6 group provided that when group X represents the —CH?N— or —CHR5-NR4-group, group Y represents an oxygen or a sulphur atom or a Nr, —CR5 or —CHR group; the group R represents a hydrogen atom or an alkyl, aryl or aralkyl group; the groups R1, R5 and R6, identical or different, represent each a hydrogen or halogen atom or an alkyl or alkoxy group; the group R2 represents a hydrogen atom or an alkyl group; the group R3 represents an aryl group; and the group R4 represents a hydrogen atom, an alkyl, aryl, aralkyl, alkylsulphonamide, arylsulphonamide or aralkylsulphonamide group; and their salt with a pharmaceutically acceptable acid, in the form of a racemic mixture and their optically pure isomer.

Abstract: The present invention provides a method for producing an optically active ?-hydroxy ester compound represented by the general formula: wherein R1 represents an optionally substituted hydrocarbon group and the like, R2 represents a nitrogen-containing heterocyclic group different from R1, which is represented by the general formula: wherein the ring may be substituted and the like, R3 represents an optionally substituted hydrocarbon group and the like, R4 and R5 represent, the same or different, a hydrogen atom, a halogen atom and the like, the symbol “*” represents an optically active center, which comprises reacting in the presence of a cinchona alkaloid and the like a compound represented by the general formula: wherein R1 and R2 are as defined above with a compound represented by the general formula: wherein R3, R4 and R5 are as defined above, and X is a halogen atom.

Abstract: The invention relates to compounds of formula (Ic) processes for their preparation, pharmaceutical compositions containing them and to their use in medicine, particularly use in the amelioration of a clinical condition for which a Factor Xa inhibitor is indicated.

Abstract: Pyrrolidone carboxamides of formula (I) where R2=a group of formula (a) or (b), R5=phenyl, heteroalkyl, aryloxy, alkoxy, alkanoyl or —NR6R7 and R1, X, R3, R4, R6 and R7 have the meanings given in the description and the claims, pharmaceutically applicable acid addition salts with basic compounds of formula (I), pharmaceutically applicable salts of acid compounds of formula (I) with bases, pharmaceutically applicable esters of hydroxy- or carboxy-group containing compounds of formula (I) and hydrates and solvates thereof, inhibit the interaction of neuropeptide Y (NPY) with one of the neuropeptide receptor subtypes (NPY-Y5) and are particularly suitable for the prevention and treatment of arthritis, diabetes and especially eating disorders and obesity. The above can be produced by known methods and converted into a galenic dosage form.

Abstract: The invention is concerned with novel heterocyclyl substituted 1-alkoxy acetic acid derivatives of formula (I) wherein R1 to R6 and A are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit the formation of coagulation factors Xa, IXa and thrombin induced by factor VIIa and tissue factor and can be used as medicaments.

Abstract: In its many embodiments, the present invention provides a novel class of compounds as inhibitors of type 3 17?-hydroxysteroid dehydrogenase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with type 3 17?-hydroxysteroid dehydrogenase using such compounds or pharmaceutical compositions.

Abstract: The present invention relates to a new aziridine derivative that is represented herein by general chemical formulae (Ia) or (Ib), and to their preparation method. In the said chemical formulae, R2 and R3 can be the same or different, and they are hydrogen, low-quality alkyl or cycloalkyl respectively; R4 can be selected among hydrogen, alkyl, aryl, or amino protective group; and amino protective group is, for example, (Ph)3C, and FMOC(9-fluorenylmethyloxycarbonyl), alkoxycarbonyl, aryloxycarbonyl, aralkyloxycarbonyl and R5CO, R5SO2 where R5 is alkyl, aryl or aralkyl.

Abstract: The invention relates to a method of preparing O,O-dialkyl S-[2-(alkylthio)alkyl] phosphorodithioates by treating O,O-dialkyl dithiophosphoric acids with a base in the substantial absence of organic solvent to obtain O,O-dialkyl dithiophosphoric acid salts that are in turn treated with thioalcohol derivatives to form the O,O-dialkyl S-[2-(alkylthio)alkyl] phosphorodithioates.

Abstract: The present invention provides a compound of formula I and the use thereof for the therapeutic treatment of a CNS disorder relating to or affected by the 5-HT6 receptor

Abstract: There is provided a heretoaryloxy 3-substituted propanamine compound of formula (I): wherein A is selected from —O— and —S—; X is selected from phenyl optionally substituted with up to 5 substituents selected from halo, C1–C4 alkyl and C1–C4 alkoxy, and thienyl optionally substituted with up to 3 substituents selected from halo and C1–C4 alkyl; Y is selected from benzothienyl, indolyl and benzofuranyl, optionally substituted with up to 5 substituents selected from halo, C1–C4 alkyl, C1–C4 alkoxy, nitro, acetyl and cyano; and when Y is indolyl it may be substituted or further substituted by an N-substituent selected from C1–C4 alkyl; R1 and R2 are each independently H or C1–C4 alkyl; and pharmaceutically acceptable salts thereof.

Abstract: Anticancer agents which contain as the active ingredient, a heme oxygenase inhibitory metalloporphyrin derivatives which are conjugated with amphipathic or water-soluble polymers (in particular, Zn-protoporphyrin (ZnPP) conjugated with polyethylene glycol). Because of being conjugated to amphipathic or water-soluble polymers, such as polyethylene glycol, the active ingredient can be administered by intravenous injection and can exert a remarkable anticancer effect owing to tumor selective delivery.

Abstract: This invention relates aryl substituted benzimidazoles of Formula I: or a pharmaceutically acceptable salt, prodrug or solvate thereof, wherein R1, R2, R10 and n are defined in the specification. The invention is also directed to the use of compounds of Formula I for the treatment of neuronal damage following global and focal ischemia, for the treatment or prevention of neurodegenerative conditions such as amyotrophic lateral sclerosis (ALS), and for the treatment, prevention or amelioration of both acute or chronic pain, as antitinnitus agents, as anticonvulsants, and as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy.

Abstract: Novel benzoxazolyl benzene derivatives of formula (I): wherein R1 is hydrogen, C1-20-alkyl or C2-20-alkenyl; R2 and R3 are independently a group —C(R4,R5)C(R6)?C(R7,R8) (a) or a group —C(R4?,R5?)CH(R6?)CH(R7?,R8?) (b), wherein R4, R5, R6, R7, R8, R4?, R5?, R6?, R7? and R8? are independently, hydrogen, C1-10-alkyl or C2-10-alkenyl, or C2-10-alkyl or C3-10-alkenyl containing at least one oxygen atom interrupting the hydrocarbon chain; or wherein R4, R5, R6, R4?, R5? and R6? are hydrogen, C1-10-alkyl or C2-10-alkyl containing at least one oxygen atom interrupting the hydrocarbon chain, or alkyl substituted by silane or oligosiloxane moiety, and one of R7 and R8 or R7? and R8? is a silane or oligosiloxane moiety and the other one of R7 and R8 or R7? and R8? is hydrogen; and X is phenylene or naphthylene, or substituted phenylene or naphthylene for use as UV screening agents for protecting human skin or hair against radiation, and in UV screening compositions, particularly topical compositions for cosmentic or

Abstract: The invention relates to compounds of the formula I in which the radicals have the stated meanings, their stereoisomeric forms and their physiologically tolerated salts and process for their preparation. The compounds are suitable for the treatment of metabohlic disorders such as type 2 diabetes.

Abstract: This invention relates to compounds of the formula wherein one of R6, R7 and R8 is and X, Y1 to Y4, R1 to R14 and n are as defined in the description, and to all enantiomers and pharmaceutically acceptable salts and/or esters thereof. The invention further relates to pharmaceutical compositions containing such compounds, to a process for their preparation and to their use for the treatment and/or prevention of diseases which are modulated by PPAR? and/or PPAR? agonists.