Abstract: The present invention provides various processes for the preparation of (R)-&agr;-(2,3-dimethoxyphenyl)-1-[2-(4-fluorophenyl)ethyl]-4-piperidinemethanol.

Abstract: The instant invention provides an amorphous form of a compound of formula I Methods of preparing an amorphous form of a compound of formula I, pharmaceutical formulations containing same, and methods of using same are also provided.

Abstract: This invention relates to amide compounds having the potentiation of the cholinergic activity and represented by formula (I) wherein R1 is acyl, R2 is lower alkyl, A is a single bond, —CO— or —SO2—, E is lower alkylene, X is CH or N, Y is a single bond, Q is —CH2— etc. and R3 and R4 are taken together to form lower alkylene etc., pharmaceutically acceptable salts and processes fro preparation thereof and a pharmaceutical composition comprising the same.

Abstract: The present invention relates to a compound represented by the following formula (I) or a salt thereof, or a pharmaceutical composition containing the compound as an effective ingredient: (wherein A represents, for example, phenyl group substituted with R1 and R2 or unsubstituted thienyl group; R1 and R2 each independently represent, for example, hydrogen atom, halogen atom or lower alkoxycarbonyl group; R3 represents, for example, hydrogen atom; R4 represents, for example, lower alkyl group; R5 represents, for example, lower alkoxy group; R6 represents, for example, hydrogen atom; R7 and R8 each represent, for example, hydrogen atom, respectively; X represents, for example, a single bond; Y represents, for example, methylene group or benzylidene group substituted with R1; and Z represents, for example, methylene group.

Abstract: The present invention provides novel, reduced benzothiophenes of formula I wherein R is —H, —OH, —O(C1-C4 alkyl), —O—CO—(C1-C6 alkyl), —O—CO—Ar in which Ar is optionally substituted phenyl, or —O—SO2—(C4-C6 alkyl); R1 is —H, —OH, —O(C1-C4 alkyl), —O—CO—(C1-C6 alkyl), —O—CO—Ar in which Ar is optionally substituted phenyl, —O—SO2—(C4-C6 alkyl) chloro or bromo; n is 2 or 3; and R2 and R3 each are independently C1-C4 alkyl, or combine to form 1-piperidinyl, 1-pyrrolidino, methyl-1-pyrrolidino, dimethyl-1-pyrrolidino, 4-morpholino or 1-hexamethyleneimino; or a pharmaceutically acceptable salt thereof. Further provided are methods for alleviating the symptoms of post-menopausal syndrome, and inhibiting endometriosis, uterine fibrosis, and aortal smooth muscle cell proliferation.

Abstract: A compound or composition comprising N-formyl paroxetine of formula (1) is useful as a pharmaceutical and as a synthetic intermediate. The N-formyl paroxetine can be an impurity in paroxetine substances and methods of assaying for such an impurity are also useful.

Abstract: This invention relates to the compounds represented by the general formula [I], [in which A—D signify optionally substituted methine group(s) or nitrogen atom; E signifies oxygen or sulfur atom; signify optionally substituted mono- or bi-cyclic aliphatic nitrogen-containing heterocyclic group(s); R1 signifies lower alkenyl, lower alkynyl, cyclo(lower alkyl), lower alkanoyl, lower alkoxycarbonyl, optionally substituted lower alkyl and the like; and R2 signifies lower alkyl].

Abstract: This invention relates to compounds of the formula: wherein R1 is H or C1-C6alkyl and the C1-C6alkyl moiety is straight or branched; R2 and R3 are each independently C1-C6alkyl and the C1-C6alkyl moiety is straight or branched; or stereoisomers thereof.

Abstract: Paroxetine is adsorbed on a carrier to form a free-flowing powder useful for capsule filling or for tablet formulation; and used in therapy to treat depression.

Abstract: The present invention provides a pharmaceutical composition for use as an NPY Y5 receptor antagonist comprising a compound of the formula (I): wherein R1 is lower alkyl, cycloalkyl or the like, R2 is hydrogen, lower alkyl or the like, n is 1 or 2, X is lower alkylene, lower alkenylene, arylene, cycloalkylene or the like, Y is CONR7, CSNR7, NR7CO, NR7CS or the like, Z is lower alkyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl or the like and R7 is hydrogen or lower alkyl, prodrug, pharmaceutically acceptable salt or solvate thereof.

Abstract: This invention is directed to sulfonyl aromatic hydroxamic acid compounds and salts thereof that, inter alia, inhibit matrix metalloprotease (MMP) activity and/or aggrecanase activity. In some particularly preferred embodiments, the compound corresponds in structure to one of the following formulas: wherein W2, the R groups, and —A—R—E—Y are described in more detail in Applicants' specification. This invention also is directed to a process that comprises administering such a compound or pharmaceutically acceptable salt thereof to a host animal having a condition associated with MMP activity.

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: This invention relates to novel compounds of the formula: wherein R1 is H or C1-C6alkyl and the C1-C6alkyl moiety is straight or branched; R2 and R3 are each independently C1-C6alkyl and the C1-C6alkyl moiety is straight or branched; X is Cl, Br or I; or stereoisomers thereof.

Abstract: The present invention is directed to derivatives of piperidinylethyl, phenoxyethyl, and fluorophenethyl bromopyridyl thioureas, which have been found to be effective non-nucleoside inhibitors (NNRTI) of NNI-resistant and multi-drug resistant human immunodeficiency virus (HIV)-1 reverse transcriptase (RT). The present invention is further directed to methods of using the above derivatives to treat patients with NNI-resistant or multi-drug resistant human immunodeficiency virus (HIV)-1.

Abstract: The synthesis of paroxetine can be made more convenient by using a solvent system comprising an aliphatic alcohol and a hydrocarbon co-solvent. The solvent system is used particularly in the hydrolysis of paroxetine phenylcarbamate and preferably uses butanol and toluene as the system.

Abstract: This invention relates to novel piperidine derivatives of formula (I) and a process for the preparation thereof. wherein R1 is H or C1-C6alkyl wherein the C1-C6alkyl moiety is straight or branched; R2 is —COOH or —COOalkyl wherein the alkyl moiety has from 1 to 6 carbon atoms and is straight or branched; or stereoisomers or pharmaceutically acceptable acid addition salt thereof.

Abstract: The present invention relates to 1-alkoxy-polyalkyl-piperidine derivatives containing a structural element of formula (I) wherein G1, G2, G3, G4 are independently C1-C6alkyl with the proviso that at least one is not methyl or G1 and G2 or G3 and G4, or G1 and G2 and G3 and G4 together form a C5-C12cycloalkyl group; G5, G6 independently are H, C1-C18alkyl, phenyl, naphthyl or a group COOC1-C18alkyl and X represents a group such that the free radical X. derived from X is capable of initiating polymerization of ethylenically unsaturated monomers, with the proviso that compounds A1 and A2 are excluded Further subjects of the invention are a polymerizable composition comprising a) at least one ethylenically unsaturated monomer and b) a 1-alkoxy-polyalkyl-piperidine derivative, a process for polymerizing ethylenically unsaturated monomers, and the use of 1-alkoxy-polyalkyl-piperidine derivatives for controlled polymerization.

Abstract: This invention is directed to aromatic sulfone hydroxamates (also known as aromatic sulfone hydroxamic acids) and salts thereof that, inter alia, tend to inhibit matrix metalloproteinase (also known as matrix metalloprotease or MMP) activity and/or aggrecanase activity. This invention also is directed to a treatment method that comprises administering such a compound or salt in an MMP-inhibiting and/or aggrecanase-inhibiting effective amount to an animal, particularly a mammal having (or disposed to having) a pathological condition associated with MMP activity and/or aggrecanase activity.

Abstract: The invention concerns a novel method for preparing chiral amino acids of formula (I) characterised in that it consists in contracting a racemic hydantoin of formula (II) with an enantiomeric splitting agent.

Abstract: Indolylpiperidine compounds of formula (I) wherein: A1 represents an alkylene, alkyleneoxy, alkylenethio, alkanoyl or hydroxyalkylene group; A2 represents a single bond, an alkylene or alkenylene group; W represents a single bond or a phenylene or furanylene group which is unsubstituted or substituted by one or more halogen atoms, alkoxy groups and/or alkyl groups; R2 represents a hydrogen or halogen atom or an alkyl or alkoxy group; and R3 represents a carboxyl group or a tetrazolyl group. The present invention provides novel indolylpiperidine compounds having imporved antihistamine and antiallergic activity.