Abstract: There are disclosed compounds of the formula 1

Abstract: The formation of risperidone is enhanced by the use of enriched Z-isomer oxime intermediate(s) of formula (3) or (7).

Abstract: The present invention relates to biguanide derivatives of formula (I), wherein R1, R2, R3 and R4 have the meanings as given in claim (1). Compounds are useful in the treatment of pathologies associated with hyperglycaemia, such as diabetes.

Abstract: Compounds of the formula (I) in which R1, R2 and X1 have the meanings given in the specification, modulate metabotopic glotamate receptor function and are useful in treating disorders of the central nervous system.

Abstract: Methods of treating cyclooxygenase-2 mediated disorders comprising administering to a subject a therapeutically effective amount of one or more 2-fluorobenzenesulfonyl compounds corresponding to Formula (I) wherein A, R1, R2, and R3 are as described in the specification, and novel 2-fluorobenzenesulfonyl compounds within Formula (I).

Abstract: This invention relates generally to amino-thio-acrylonitriles of formula Ia or Ib: 1

Abstract: Substituted phenylpiperidines and phenylpyrrolidines of formula (I), compositions containing them, and methods of making and using them to treat histamine-mediated conditions.

Abstract: Novel compounds of the formula (I) formula (I) in which W, E, X, Y, T, R1, R2, R2′, and R2″ are as defined in Patent claim 1, are inhibitors of coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic disorders and for the treatment of tumours.

Abstract: The present invention relates to novel florfenicol compounds having the chemical structure: 1

Abstract: The invention is directed to piperidinyl compounds that selectively bind integrin receptors and methods for treating an integrin mediated disorder.

Abstract: The present invention is related to substantially hydrophilic sulfonamide derivatives, or sulfonamide derivatives having a substantially hydrophilic moiety, of formula I notably for use as pharmaceutically active compounds, as well as to pharmaceutical formulations containing such sulfonamide derivatives. Said sulfonamide derivatives are efficient modulators of the JNK pathway, they are in particular efficient and selective inhibitors of JNK 3. The present invention is furthermore related to novel sulfonamide derivatives as well as to methods of their preparation.

Abstract: There are provided compounds having an anticoagulant action on the basis of inhibition of activated blood coagulation factor X and being useful as anticoagulants or preventive/therapeutic agents for diseases induced by thrombosis or embolism. Effective ingredients are the compounds such as 4′-bromo-2′-[(5-chloro-2-pyridyl)carbamoyl]-6′-&bgr;-D-galactopyranosyloxy-1-isopropylpiperidine-4-carboxanilide, 2′-(2-acetamido-2-deoxy-&bgr;-D-glucopyranosyloxy)-4′-bromo-6′-[(5-chloro-2-pyridyl)carbamoyl]-1-isopropylpiperidine-4-carboxanilide, etc. or salts thereof.

Abstract: The invention provides novel selective estrogen receptor modulator compounds of the general formula: wherein R1 and R2 , which are the same or different are a) H, halogen, OCH3, OH; or where X is O, NH or S; and n is an integer from 1 to 4; and R4 and R5, which are the same or different, are a 1 to 4 carbon alkyl, H, —CH2C≡CH or —CH2CH2OH; or R4 and R5 form an N-containing five- or six-membered ring or heteroaromatic ring; or c) —Y—(CH2)nCH2—O—R6 where Y is O, NH or S and n is an integer from 1 to 4; and R6 is H, —CH2CH2OH, or —CH2CH2Cl; or d) 2,3-dihydroxypropoxy, 2-methylsulfamylethoxy, 2-chloroethoxy, 1-ethyl-2-hydroxyethoxy, 2,2-diethyl-2-hydroxyethoxy or carboxymethoxy; and R3 is H, halogen, OH or —OCH3; stereoisomers thereof and their non-toxic pharmaceutically acceptable salts and esters and mixtures thereof, which compounds exhibit valuable pharmacological properties.

Abstract: This invention is directed to compounds which are selective antagonists for melanin concentrating hormone-1 (MCH1) receptors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier. This invention provides a pharmaceutical composition made by combining a therapeutically effective amount of the compound of this invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a method of reducing the body mass of a subject which comprises administering to the subject an amount of a compound of the invention effective to reduce the body mass of the subject.

Abstract: A class of acyl sulfamides comprises compounds that are potent ligands for PPAR gamma and generally have antagonist or partial agonist activity. The compounds may be useful in the treatment, control or prevention of obesity, non-insulin dependent diabetes mellitus (NIDDM), hyperglycemia, dyslipidemia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, atherosclerosis, vascular restenosis, inflammation, and other PPAR gamma mediated diseases, disorders and conditions.

Abstract: The invention concerns a compound of formula (I), wherein Ar1 represents phenyl, naphthyl or phenyl fused by a C3-8cycloalkyl, where each group is substituted by a group —O-Z and optionally one to three further groups independently represented by R1; Ar2 represents phenyl or 5-6 membered heteroaromatic group, where each group is optionally substituted by one to four groups independently selected from halogen, C1-4 alkyl and C1-4 alkoxy; Ar3 represents a phenyl or a 5-6 membered heteroaromatic group, where each group is optionally substituted by one to four groups independently selected from hydroxy, alkyl, C1-4 alkoxy, C2-4 alkenyl, C2-4 alkenyloxy, C1-4 perfluoroalkoxy, C1-4 acylamino or an electron withdrawing group; A represents —C(H)—; E represents —C1-6alkylene-; X represents —CON(H or C1-4alkyl)- or —N(H or C1-4alkyl)CO—; Y represents a direct link, —N(H or C1-4alkyl)CO— or —CON(H or C1-4alkyl)-; Z represents a metabolically labile group; R1 re

Abstract: The present application describes novel &bgr;-amino acid derivatives of formula I: 1

Abstract: A process for the production of a compound represented by the following Formula (IV) or a salt thereof, comprising the steps of condensing with dehydration a compound represent by the following Formula (I) and 4-(aminomethyl)piperidine to obtain a compound represented by the following Formula (II); protecting the secondary amine of the piperidine moiety to give a compound represented by the following Formula (III); and then reducing the imine moiety (in the Formulas, the wavy line may be, relative to the double bond, any of an E form, a Z form, or a mixture thereof, R represents a hydrogen atom, a C1-8 alkyl group etc., and R′ represents a C1-8 alkylcarbonyl group, an arylcarbonyl group etc.).

Abstract: The present invention relates N-substituted glycine derivatives for treating or preventing neuronal damage associated with neurological diseases. The invention also provides compositions comprising the compounds of the present invention and methods of utilizing those compositions for treating or preventing neuronal damage.

Abstract: The present application describes modulators of chemokine receptors of formula (I): 1

Abstract: Novel quaternary amine containing compounds including their pharmaceutically acceptable isomers, salts, hydrates, solvates and prodrug derivatives having activity against mammalian factor Xa are described. Compositions containing such compounds are also described. The compounds and compositions are useful in vitro or in vivo for preventing or treating conditions in mammals characterized by undesired thrombosis.

Abstract: The present invention provides compounds of Formula (I): 1

Abstract: The present application describes modulators of CCR3 of formula (I): 1

Abstract: Novel polyamines, their synthesis and use in pharmacological, cosmetic or agricultural applications are provided. The polyamines induce antizyme production which in turn down regulates both the production of polyamines by ornithine decarboxylase (ODC) and the transport of polyamines by its corresponding polyamine transporter. These compounds will preferably enter the cell independent of the polyamine transporter. As drugs, these compounds are used to treat any disease associated with cellular proliferation including but not limited to cancer.

Abstract: A process for preparing an amidine derivative represented by the following formula (II), wherein R represents a hydrogen atom or a phenyl group, which comprises reducing an amideoxime derivative represented by the following formula (I), wherein R represents a hydrogen atom or a phenyl group, with zinc in an acetic acid solvent, or a salt thereof.

Abstract: Compounds used for treating dependence on or withdrawal from a drug of abuse, for an eating disorder or for a CNS disease or pathology having the following formulas:

Abstract: The present invention is directed to novel compounds of the formula (I) 1

Abstract: Compounds of formula (I): wherein: X represents a heterocycle bonded to the remainder of the molecule by a nitrogen atom of the heterocycle, or an —NR2R3 group wherein R2 represents hydrogen or alkyl, and R3 represents aryl, 1,3 dihydro-2H-benzimidazolyl-2-one or alkyl substituted by a heterocycle, n represents zero or 1, R1 represents hydrogen or alkyl, Ra represents a single bond or an alkylene chain, A represents nitrogen or CH, E represents nitrogen or CRe, wherein Re is as defined in the description, Rb represents a single bond or an alkylene chain as defined in the description, W represents aryl or heteroaryl, Their optical isomers, and addition salts thereof with a pharmaceutically acceptable acid, and medicinal products containing the same which are useful for treatment of diseases or pathological conditions in which endothelial dysfunction is known.

Abstract: Compounds of general formula (I) are disclosed and claimed in the present application, as well as their pharmaceutically acceptable salts, pharmaceutical compositions comprising the novel compounds and their use in therapy, in particular in the management of pain.

Abstract: Compounds of formula I, or a salt thereof or a hydrate thereof, as follows: 1

Abstract: There are disclosed compounds of the formula I: 1

Abstract: Benzamidine derivatives of formula (I) or pharmaceutically acceptable salts thereof exhibit excellent inhibitory activity against factor Xa and are useful for treating or preventing blood coagulation disorders: 1

Abstract: Monomer compounds comprising several cationic groups are provided. The invention also relates to a process for making these monomer compounds. The process is highly selective and prevents unwanted reactions leading to undesired structures. The invention relates also to polymers, including copolymers, comprising units deriving from said monomer compounds. The monomer compounds comprise several cationic groups, e.g.

Abstract: A medicinal composition containing one or more compounds selected from the compounds represented by the following formula (I), salts of these compounds, solvates of these compounds and solvates of these salts and being capable of reducing the contact of the compounds with the components in the bile or pancreatic juice.

Abstract: The invention provides novel &bgr;2 adrenergic receptor agonist compounds of formula (I): wherein R1-R13 and w have any of the values described in the specification. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with &bgr;2 adrenergic receptor activity, and processes and intermediates useful for preparing such compounds.

Abstract: A compound having the formula (I) or its salt, hydrate, hydrate salt or solvate: 1

Abstract: The present invention discloses compounds, which are novel antagonists for melanin-concentrating hormone (MCH), as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such MCH antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.

Abstract: Disclosed are cyclic and acyclic amidines, pharmaceutical compositions containing such amidines, and their use in treating or preventing progesterone receptor mediated diseases or conditions, such as osteopenia and osteoporosis.

Abstract: The invention provides compounds of Formula (I): 1

Abstract: The invention provides novel selective estrogen receptor modulator compounds of the general formula: 1

Abstract: 1

Abstract: The compounds of formula 1, 1

Abstract: The present application describes modulators of MCP-1 of formula (I): 1

Abstract: The invention relates to acyl-3-carboxyphenylurea derivatives and to their physiologically tolerated salts and physiologically functional derivatives.

Abstract: The invention relates to liquid-crystalline compounds of the formula I 1

Abstract: This invention relates to novel compounds of Formula (I), and compositions thereof, useful in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).

Abstract: Compounds of the formula: 1

Abstract: Selected novel urea compounds are effective for prophylaxis and treatment of diseases, such as cell proliferation or apoptosis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving stoke, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.

Abstract: The invention relates to novel diphenylmethane derivatives, processes for their preparation and their use in medicaments, in particular for the indications of arteriosclerosis and hypercholesterolaemia.

Abstract: The present application describes modulators of CCR3 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma and other allergic diseases.