Abstract: Compounds of formula [I] in which: W may represent a —(CH2)2—, —(CH2)3—, —CH2—C≡C— or —CH2—CH═CH— group, R2 may in particular represent a piperidyl group, an optionally substituted 1,2,3,6-tetrahydropyridyl group, a hexahydro-1H-azepinyl group, an optionally substituted piperazinyl group or a morpholinyl group, R3 may in particular represent a group —COR1, A may in particular represent an optionally substituted phenyl group, a heterocycle or a cyclopentyl group, and B may in particular represent a pyridyl group, an aminopyrazinyl group, an aminopyridazinyl group, a pyrimidinyl group optionally substituted with an amino group, piperidyl group or an aminopyridyl group optionally substituted on the pyridine with a (C1-C4)alkyl or (C1-C4)alkoxy group, the amino group possibly also being substituted with a (C1-C4)alkyl group, their preparation and their therapeutic application.

Abstract: Generally, the present invention is directed to central nervous system dopamine transporter-imaging agents and methods of use thereof. In certain embodiments, the present invention relates to radiolabeled piperidine derivatives for use as imaging agents in the diagnosis of Parkinson's disease. Another aspect of the present invention relates to piperidine monoamine transporter ligands, comprising a functional group capable of chelating a radionuclide, e.g., technetium, and methods of use thereof.

Abstract: Piperidine derivatives, their manufacture and use as medicaments is described. The compounds are useful for treating diseases associated with restenosis, glaucoma, cardiac infarct, high blood pressure and end organ damage, e.g. cardiac insufficiency and kidney insufficiency.

Abstract: This invention relates to novel compounds of 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 or pharmaceutically acceptable acid addition salt thereof.

Abstract: A retroviral protease inhibiting compound of the formula: is disclosed.

Abstract: Novel compounds and methods for preparing same, immunopotentiating compositions, and a method for potentiating the immune system of a host animal. The method comprises administering to the animal an effective amount of an immunopotentiating compound of Formula I or Formula II, or a physiologically acceptable salt.

Abstract: A sulfonyl divalent aromatic or heteroaromatic ring hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a treatment process that comprises administering a contemplated sulfonyl divalent aromatic or heteroaromatic ring hydroxamic acid compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.

Abstract: Disclosed are carboxamide-substituted benzimidazole derivatives of general formula (I) wherein the groups X, R1, R2, R3 and R4 may have the meanings given in the claims and specification, processes for preparing them and the use of carboxamide-substituted benzimidazole derivatives as pharmaceutical compositions, particularly as pharmaceutical compositions with a tryptase-inhibiting activity.

Abstract: The present invention is directed to a novel crystalline hydrate of 6-hydroxy-3-(4-[2-(piperidin-1-yl)ethoxy]phenoxy)-2-(4-methoxyphenyl)benzo[b]thiophene hydrochloride and uses for same, including inhibition of disease states associated with estrogen deprivation including cardiovascular disease, hyperlipidemia, and osteoporosis; and inhibition of other pathological conditions such as endometriosis, uterine fibrosis, estrogen-dependent cancer (including breast and uterine cancer), prostate cancer, benign prostatic hyperplasia, CNS disorders including Alzheimer's disease, prevention of breast cancer, and up-regulating ChAT.

Abstract: This invention relates to the fields of pharmaceutical and organic chemistry and provides novel 3-benzyl-benzothiophenes which are &agr;-substituted with ether, thioether amino, cyano or halo that are useful for the treatment of the various medical indications associated with post-menopausal syndrome, as well as estrogen dependent diseases including cancer of the breast, uterus and cervix. The present invention further relates to intermediate compounds and processes useful for preparing the pharmaceutically active compounds of the present invention, and pharmaceutical compositions.

Abstract: Disclosed herein is a method for inhibiting the premature polymerization of ethylenically unsaturated monomers comprising adding to said monomers an effective amount of a mixture comprising: A) at least one stable hindered nitroxyl compound having the structural formula: wherein R1 and R4 are independently selected from the group consisting of hydrogen, alkyl, and heteroatom-substituted alkyl and R2 and R3 are independently selected from the group consisting of alkyl and heteroatom-substituted alkyl; and X1 and X2 (1) are independently selected from the group consisting of halogen, cyano, COOR7, —S—COR7, —OCOR7, (wherein R7 is alkyl or aryl), amido, —S—C6H5, carbonyl, alkenyl, or alkyl of 1 to 15 carbon atoms, or (2) taken together, form a ring structure with the nitrogen; and B) at least one inhibitor selected from the group consisting of ortho-quinone, ortho-hydroquinone, para-quinone, para-hydroquinone, and derivatives of the foregoing.

Abstract: N-[2-hydroxy-3-(1-piperidinyl)-propoxy]-pyridine-1-oxide-3-carboximidoyl chloride, its stereoisomers, and the addition salts thereof, pharmaceutical compositions containing the same, methods of treating pathological insulin resistance, methods of treating pathological insulin resistance and pathological conditions associated therewith, and methods of treating pathological insulin resistance by simultaneously treating diabetes-induced chronic complications, especially retinopathy, neuropathy and nephropathy, and/or by simultaneously increasing pathologically decreased peripheral neuroregeneration caused by diabetes.

Abstract: A method and apparatus for performing in situ measurement of etch uniformity within a semiconductor wafer processing system. Specifically, the apparatus and concomitant method analyzes optical emission spectroscopy (OES) data produced by an OES system. The analysis computes the first derivative of the OES data as the data is acquired. When the data meets a particular trigger criterion, the value of the first derivative is correlated with a particular uniformity value. As such, the system produces a uniformity value for a semiconductor wafer using an in situ measurement technique.

Abstract: This invention is directed to a method of retarding or preventing the transformation of a colonic adenoma to a colonic adenocarcinoma comprising the administration to a patient with FAP or a patient with one or more of said adenomas a non-toxic therapeutically effective amount of NSAID, said amount effective to inhibit the PGHS-2 in said adenoma. The preferred method comprises the administration of a specific PGHS-2 inhibiting agent as defined herein.

Abstract: Compounds of formula (I) and their salts, solvates and prodrugs, wherein the substituents have the values mentioned herein, are Procollagen C-Proteinase (PCP) inhibitors and have utility in conditions mediated by PCP.

Abstract: The present invention is directed to a process for the preparation of the mesylate trihydrate of the (1S,2S)-1-(4-hydroxyphenyl)-2-(4-hydroxy-4-phenylpiperidin-1-yl)-1-propanol compound having the formula (I): The present invention is also further comprises a process for enantiomeric resolution and isolation of the (D)-(−)-tartrate salt of the compound of the formula (I).

Abstract: A process for the synthesis of 2,2,6,6-tetramethyl-4-oxopiperidine is disclosed wherein the process comprises reacting in a liquid phase reaction mixture: A) at least one acetone compound, and B) at least one ammonia donor compound, in the presence of a catalytically effective amount of a crystalline aluminosilicate containing calcium.

Abstract: Hydroxy functional urethane compounds comprising the reaction product of a hydroxy functional urethane intermediate with a compound having at least 2 isocyanate groups, wherein the intermediate is represented by the formula: wherein R1 and R2=hydrogen, alkyl, cycloalkyl or a residue R6—O— or R6—CO—O— with R6; R6=an alkyl, cycloalkyl or benzylic group having up to 18 carbon atoms; R4 and R5=hydrogen or alkyl group containing eventually a hydroxyl group; and R3=alkyl, cycloalkyl or benzylic group eventually containing an ether linkage and/or a hydroxyl group, or HO—CH(R1)—CH(R2)—; and is prepared by reaction of a cyclic 5-ring carbonate with a beta-hydroxy functional, secondary amine. The hydroxy functional urethanes are useful in paints and coatings, particularly for automotive applications.

Abstract: A free-flowing, amorphous paroxetine hydrochloride composition suitable as a therapeutic agent for premature ejaculation can be prepared by dissolving paroxetine free base in a hydrochloric acid-ethanol solution followed by drying. The present compositions comprise amorphous paroxetine hydrochloride and at least one hydroxyl-bearing compound. In one preferred embodiment, the hydroxyl-bearing compound is ethanol and the amount of ethanol present in the amorphous product is in the range of 1 to 4 weight percent based on paroxetine hydrochloride. The amorphous product is stable and substantially non-hygroscopic.

Abstract: This invention relates to novel compounds of formula I wherein A, B, D, E, G, J, L, X, V are as defined in the specification, and the compounds are useful in the modulation of endogenous growth hormone levels in a mammal.