Abstract: The present invention relates to compounds of the formula wherein R1 and R2 are as defined herewithin. The compounds of formula I have been found to be adenosine receptor ligands. Specifically, the compounds of the present invention have a good affinity to the A2A-receptor and they are therefore useful in the treatment of diseases, related to this receptor.

Abstract: Diarylcycloalkyl derivatives and their physiologically acceptable salts and physiologically functional derivatives are disclosed. The compounds include those of formula I, in which the radicals are as defined, and their physiologically acceptable salts and processes for their preparation. The compounds typically have lipid- and/or triglyceride-lowering properties and are suitable, for example, for the treatment of disorders of lipid metabolism, of type II diabetes, and of syndrome X.

Abstract: This invention provides a compound of the formula (I): or the pharmaceutically acceptable salts thereof wherein R1 is hydrogen, halo or alkyl; R2 and R3 are independently hydrogen, alkyl, alkenyl, alkynyl, aminoalkyl or hydroxyalkyl; or R2 and R3 taken together with the nitrogen atom to which they are attached may form hetrocyclic; R4 is hydrogen, halo, acyl, amino, amido, aryl, arylalkyl, or heteroaryl; R5 is hydrogen, halo, alkyl alkenyl, alkynyl, acyl, amino, amido, aryl, arylalkyl, or heteroaryl; R6 is hydrogen, alkyl or alkoxyalkyl; X is NR9 wherein R9 is hydrogen or alkyl; and Y is (CR7R8)n wherein n is an integer from 0 to 5. These compounds have 5-HT4 receptor binding activity, and thus are useful for the treatment of gastroesophageal reflux disease, non-ulcer dyspepsia, Functional dyspepsia, irritable bowel syndrome or the like in mammalian, especially humans. This invention also provides a pharmaceutical composition comprising the above compound.

Abstract: The invention relates to compounds of formula: and their solvates and/or hydrates exhibiting affinity for the arginine-vasopressin V1b receptors or for both V1b and V1a receptors. The invention also relates to their process of preparation, to the intermediate compounds of formula (II) of use for their preparation, to the pharmaceutical compositions comprising them and to their use for the preparation of medicaments.

Abstract: The invention provides a compound of formula I: wherein R1, R2, R3, and R4 have any of the values defined in the specification, or a pharmaceutically acceptable salt thereof, as well as processes and intermediates useful for preparing such compounds or salts, and methods of treating a herpesvirus infection, atherosclerosis or restenosis using such compounds or salts.

Abstract: A process for the preparation of a compound of formula (I) comprising oxidizing a compound of formula (II) with trifluoroperacetic acid in the presence of a corrosion inhibiting compound such as boric acid. Also, a process for preparing a compound of formula (II) by adding sulfur dioxide to a mixture of the corresponding disulfide, a formate salt, trifluoromethyl bromide and a polar solvent; and a process for preparing the disulfide comprising adding S2Cl2 to a solution, in an organic solvent, of the corresponding 4-unsubstituted pyrazole.

Abstract: The present invention relates to compounds of the formula wherein R1, A and R are as described within. The compounds of the present invention have been found to be adenosine receptor ligands. Specifically, the compounds of the present invention have an affinity to the A2A-receptor and are therefore useful in the treatment of diseases related to this receptor.

Abstract: A azomethine yellow dye compound of general formula (I): General formula (I) wherein R1 and R2 each independently represent a hydrogen atom or a substituent; R3 represents a substituent; m indicates an integer from 0 to 3; when m is 2 or greater, R3's may be the same or different and may be mutually bonded to form a condensed ring; R3 may be bonded to R1 or R2 to form a condensed ring; R4 represents an aryl group or a heterocyclic group; R5 and R6 each independently represent a hydrogen atom or a substituent; R7 represents a substituent; n indicates an integer from 0 to 4; when n is 2 or greater, R7's may be the same or different and the may be mutually bonded to form a condensed ring; R7 may be bonded to R5 or R6 to form a condensed ring; and R5 and R6 may be bonded to each other to form a ring.

Abstract: Disclosed herein is a method for reducing the rate of degradation of proteins in an animal comprising contacting cells of the animal with certain boronic ester and acid compounds. Also disclosed herein are novel boronic ester and acid compounds, their synthesis and uses.

Abstract: The present invention is in the field of medicine, particularly in the treatment of Type II diabetes and obesity. More specifically, the present invention relates to selective &bgr;3 receptor agonists useful in the treatment of Type II diabetes and obesity. The invention provides compounds and methods of treating type II diabetes and obesity, comprising administering to a mammal in need thereof compounds of the Formula I: or pharmaceutically acceptable salts thereof.

Abstract: 3-(4,5-Dihydroisoxazol-3-yl)-substituted benzoylpyrazoles of the formula I in which R4 is C1-C4-haloalkyl and R1 to R3 and R5 to R10 are as defined in the description are described. The compounds have herbicidal activity.

Abstract: The present invention includes a number of novel intermediates such as the (S)-secondary alcohol of formula (VIIIA) X2—CH2—C*H(OH)—CH2—NH—CO—RN  (VIIIA) and processes for production of pharmacologically useful oxazolidinones.

Abstract: A process for making a compound of formula I wherein the substituents are as described in the specification comprising reacting a ketone of formula II with succinic anhydride and an alkoxide base to form a compound of formula III which is reacted with a compound of formula IV to form a compound of V and reacting with an alcohol to form the corresponding ester of formula VI and reacting the ester with N-methylhydroxylamine.

Abstract: The invention relates to compounds of formula in which R1 to R9, R16 and R17 are as defined in claim 1. These compounds are pharmacologically active.

Abstract: The present invention relates to novel 6-methylnicotinamide derivatives and their pharmaceutically acceptable salts, the process for preparing them, and the pharmaceutical compositions containing said compounds as active ingredients. The 6-methylnicotinamide derivatives of the present invention exhibit their inhibitory activity against the proliferation of human immunodeficiency virus (HIV) as well as hepatitis B virus (HBV) and hepatitis C virus (HCV), such that they can be used for hepatitis B, hepatitis C and acquired immune deficiency syndrome (AIDS).

Abstract: The present invention relates to certain 5-aralkylsulfonyl-3-(pyrrol-2-yl-methylidene)-2-indolinone derivatives that inhibit kinases, in particular met kinase. Pharmaceutical compositions comprising these compounds, methods of treating diseases mediated by kinases utilizing pharmaceutical compositions comprising these compounds, and methods of preparing them are also disclosed.

Abstract: Diaminopyrazole derivatives of the general Formula (I) or their physiological tolerated, water-soluble salts with inorganic or organic acids, and agents, containing these compounds, for the oxidative dyeing of fibers.

Abstract: Herbicidally active haloalkyl-substituted 3-(4,5-dihydroisoxazol-3-yl)benzoylcyclohexenones of the formula I in which R1 to R3 and R5 to R14 are as defined in the description and R4 is C1-C4-haloalkyl are described.

Abstract: A process for preparing compounds of the formula I in which R1 is hydrogen, an aliphatic group having 1-8 carbon atoms, Cl-C6-alkoxycarbonyl, Cl-C6-alkylthiocarbonyl or a cyclic ring system having 3-14 ring atoms, and R2 is hydrogen, an aliphatic group having 1-8 carbon atoms, or R1 and R2 together with the carbon atom to which they are bound form a cyclic or bicyclic ring system having 3-14 ring atoms, comprises the preparation of compounds of the formula II in which R3 and R4 are readily detachable groups and R1 and R2 are as defined above, as starting materials or intermediates and the cyclization of these under suitable reaction conditions to give compounds of the formula I. The intermediates of the formula II are novel.

Abstract: A compound of the formula A compound of formula I has a good affinity to the A2A receptor and is useful for the treatment of diseases mediated by this receptor.