Abstract: Tricyclic nitrogen containing compounds, having anxiolytic and anti-depressant activity and central nervous system activity of the following structural formula: 1

Abstract: This invention relates to non-steroidal tricyclic compounds that are modulators of androgen receptors and to methods for making and using such compounds.

Abstract: The present invention relates to tricyclic compounds of formula (I): 1

Abstract: Compounds of formula (I) are matrix metalloprotemase inhibitors wherein X represents a carboxylic acid group —COOH, or a hydroxamic acid group —CONHOH;R2 represents a radical of formula (II): R3—(ALK)m—(Q)p—(ALK)n.

Abstract: The present invention relates to novel imidazolidinone derivatives thereof, their synthesis, and their use as &agr;v integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors &agr;v&bgr;3 and/or &agr;v&bgr;5 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation, inflammatory arthritis, viral disease, cancer, and metastatic tumor growth.

Abstract: The present invention relates to methods for preparing a variety of Lamellarin compounds and analogues via a synthetic intermediate, which methods involved the step of performing an intramolecular cyclization of a compound of Formula (I) to produce compounds of Formula(II), wherein the variables are given in the specification.

Abstract: The present invention relates to compounds of the general formula (I) The compounds are useful in the treatment and/or prevention of conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR).

Abstract: Benzo[f]naphthyridine derivatives of formula (I): 1

Abstract: In accordance with the present invention, nanometer-scale reversible electronic switches are provided that can be assembled to make cross-bar circuits that provide memory, logic, and communications functions. The electronic switches, or crossed-wire devices, comprise a pair of crossed wires that form a junction where one wire crosses another at an angle other than zero degrees and at least one connector species connecting the pair of crossed wires in the junction. The junction has a functional dimension in nanometers, wherein at least one connector species and the pair of crossed wires forms an electrochemical cell.

Abstract: In accordance with the present invention, nanometer-scale reversible electronic switches are provided that can be assembled to make cross-bar circuits that provide memory, logic, and communications functions. The electronic switches, or crossed-wire devices, comprise a pair of crossed wires that form a junction where one wire crosses another at an angle other than zero degrees and at least one connector species connecting the pair of crossed wires in the junction. The junction has a functional dimension in nanometers, wherein at least one connector species and the pair of crossed wires forms an electrochemical cell.

Abstract: Compounds according to the formula: 1

Abstract: Disclosed are novel compounds and a method of treating a disease associated with aberrant leukocyte recruitment and/or activation.

Abstract: Compounds of the formula I, in which R1, R2, R3 and R4 have the meanings indicated in the description, are novel active bronchial therapeutics.

Abstract: Disclosed are compounds of the formula: 1

Abstract: A novel naphthyridine derivative showing high activity as a tachykinin receptor antagonist can be produced at high efficiency by reacting an acylating agent such as a carboxylic acid derivative with a compound represented by the formula (1): wherein R1, R2 and R3 represent independently a hydrogen atom, a lower alkyl group, a lower alkoxyl group, an aryl group, a heteroaryl group, an amino group, etc., and X1 and X2 represent respectively a halogen atom.

Abstract: The present invention relates to tricyclic 2-pyridone compounds of formula (I): 1

Abstract: The present invention concerns the compounds of formula 1

Abstract: Pharmaceutical compounds comprising bridged nicotine analogs of N-octylnicotinium iodide (NONI) having selective antagonist properties at &agr;3&bgr;2-containing nicotinic receptor subtypes, and compositions containing these compounds. The compounds and compositions are used to treat central nervous system pathologies.

Abstract: 1 Compounds having formula (I) wherein R3, R4, R7, and R8 are independently selected from the group consisting of hydrogen, lower alkyl, halogen, amine, mono(lower)alkylamine, di(lower)alkylamine, phenyl, or substituted phenyl possess antitumor activity and are new with the exception of the compound in which R3, R4, R7, R8 are all hydrogen and the compound in which R3 and R7 are hydrogen, R4 chlorine, and R8 is a 2-nitrophenyl group.

Abstract: Compounds are provided that, by way of their selective neurotransmitter binding useful for the treatment of various neurological and psychological disorders, e.g., ADHD. Such compounds are 4-phenyl substituted tetrahydroisoquinolines having the Formula IA, IB, IIA, IIB, IIIA or IIIC as set forth herein.

Abstract: The present invention discloses novel substituted imidazole compounds which have dual histamine-H1 and H3 receptor antagonist activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such imidazoles as well as methods of using them to treat allergy, inflammatory and CNS-related diseases and others.

Abstract: The present invention discloses novel substituted imidazole compounds which have H3 receptor antagonist activity or dual histamine-H1 and H3 receptor antagonist activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such imidazoles as well as methods of using them to treat allergy, congestion, inflammatory and CNS-related diseases and others.

Abstract: Cycloalcanoindole and -azaindole derivatives are prepared by reaction of appropriately substituted carboxylic acids with anmines. The cycloahloanindole and -azaindole derivatives are suitable as active compounds for medicaments, preferably antiatherosclerotic medicaments.

Abstract: This invention provides cancer-active tricyclic and tetracyclic oxypyrones and a method of synthesizing these compounds. Preferred compounds have aryl groups at the 3-position of the oxypyrone ring. The tricyclic oxypyrone synthetic method is a simple condensation reaction of pyrones with cyclohexenecarboxaldehydes, providing high yields and using few steps. The tetracyclic oxypyrone synthetic method is a simple condensation reaction of carvones with pyrones.

Abstract: Compounds 8,9-diethoxy-2-methyl-6-[4(p-toluenesulfonamide) phenyl]-1,2,3,4,4a,10b-hexahydrobenzo[c][1,6]naphthyridine and 9-ethoxy-8-methoxy-2-methyl-6-[4-(p-toluenesulfonamido)phenyl]-1,2,3,4,4a,10b-hexahydrobenzo[c][1,6]naphthyridine and medicament compositions based thereon are useful for treating airway disorders, high blood pressure disorders and concomitant disorders connected therewith.

Abstract: A compound of formula I: or a pharmaceutically acceptable salt, hydrate, ester, solvate, prodrug, metabolite, stereoisomer, or mixtures thereof.

Abstract: This invention concerns compounds of formula 1

Abstract: Novel basic derivatives of benz[e]isoindol-1-ones and pyrrolo[3,4-c]quinolin-1-ones which can be represented by the general formula (I) indicated below are described: 1

Abstract: Novel 1,8-benzo-naphthyridine derivatives of general formula (I): 1

Abstract: The present invention provides chemical compounds, pharmaceutical compositions, and methods for increasing the therapeutic efficacy of drugs. Specifically, the invention provides compounds and compositions for inhibiting drug transport proteins that efflux therapeutic agents from cells, and to methods for using these compounds and pharmaceutical compositions to increase the efficacy of the therapeutic agents that are effluxed by these drug transport proteins.

Abstract: The present invention relates to compounds of the general formula (I) 1

Abstract: The invention relates to novel pyrrolopyridinone derivatives of the formula (I) or (II): 1

Abstract: Tricyclic compound of the formula: 1

Abstract: Disclosed are novel compounds and a method of treating a disease associated with aberrant leukocyte recruitment and/or activation. The method comprises administering to a subject in need an effective amount of a compound represented by the following structural formula: and physiologically acceptable salts thereof.

Abstract: N-oxides of formula 1 wherein R1, R2, R3 and R4 have the meanings given in the description, are selective inhibitors of types 3 and 4 of cyclic nucleotide phosphodiesterase (PDE3, PDE4); they are useful on the one hand as bronchial therapeutics but on the other hand especially for the treatment of disorders of inflammatory nature.

Abstract: The present invention relates to compounds of formula (I) wherein A, B, Q, T, X, Y, Z, R5, R6, R7, R8, Ar, k, m, n and p are as defined in the specification. These compounds are useful in treating or preventing conditions mediated by nuclear receptors, in particular the Peroxisome Proliferator-Activated Receptors (PPAR).

Abstract: A novel naphthyridine compound represented by the general formula (1): wherein R1, R2 and R3 are independently a hydrogen atom, a lower alkyl group or the like, or R1 and R2, or R2 and R3, when taken together, form a cyclic group; each of X and Y is a methylene or ethylene group; Z is a phenyl group, a substituted phenyl group or the like; A is a hydrogen atom, a lower alkyl group or the like; and G is an acyl group, shows antagonism for tachykinin receptors and is useful as a prophylactic or therapeutic agent for diseases for which the tachykinin receptors are considered to be responsible. A specific example of such a compound is 2-[(−)-4-(N-benzoyl-N-methyl)amino-3-(3,4-dichlorophenyl)butyl]-10-acetylamino-1,2,3,4-tetrahydro-benzo[b][1,6]naphthyridine.

Abstract: The invention relates to the use of quinolone- and naphthyridonecarboxylic acid derivatives which are substituted in position 7 by a 1-aminomethyl-2-oxa-7-azabicyclo[3.3.0]oct-7-yl radical, and of their salts for the therapy of Helicobacter pylori infections and associated gastroduodenal disorders.

Abstract: This invention involves optionally substituted 1,2,3,4,5,6-hexahydro-1,5-methano-pyrido[1,2a][1,5]diazocin-8-one derivatives, their preparation, compositions containing same and method of treating addictive disorders and neurological or mental disorders related to a decrease in cholinergic function.

Abstract: Novel compounds of formula are disclosed. Also disclosed is a method of inhibiting farnesyl protein transferase function and therefore inhibiting the abnormal growth of cells. The method comprises administering a compound of the above formula to a biological system. In particular, the method inhibits the abnormal growth of cells in a mammal such as a human being. Also disclosed is a method of effecting an anti-allergic response by administering the compounds.

Abstract: Disclosed are nitrosated and/or nitrosylated phosphodiesterase inhibitors having the formula NOn-PDE inhibitor where n is 1 or 2. The invention also provides compositions comprising such compounds in a pharmaceutically acceptable carrier. The invention also provides a composition comprising a therapeutically effective amount of an phosphodiesterase inhibitor (PDE inhibitor), which can optionally be substituted with at least one NO or NO2 moiety, and one to ten fold molar excess of a compound that donates, transfers or releases nitrogen monoxide as a charged species, i. e., nitrosonium (NO+) or nitroxyl (NO−), or as the neutral species, nitric oxide (NO.) or which stimulates endogenous EDRF production. The invention also provides compositions comprising such compounds in a pharmaceutically acceptable carrier. The invention also provides methods for treating sexual dysfunctions in males and females.

Abstract: The present invention provides novel compounds of formula I which may be useful in hyperpolarizing cell membranes, opening potassium channels, relaxing smooth muscle cells, and inhibiting bladder contractions.

Abstract: The present invention provides methods and pharmaceutical preparations that inhibit the growth of bacterial microorganisms. Additionally, the present invention provides methods and pharmaceutical preparations that kill bacterial microorganisms.

Abstract: Fluorinated phenanthrene derivatives and their use in liquid-crystalline mixtures Fluorinated phenanthrene derivatives of the formula (I) in which G is —CHF—CH2— or —CF═CH—, E1, E2, E3, E4, E5 and E6 are identical or different and are —CH—, —CF— or —N— and R1(—A1—M1)a(—A2—M2)b, (M3—A3—)c(M4—A4—)d R2 denote mesogenic radicals are suitable as components for liquid-crystalline mixtures, especially ferroelectric mixtures.

Abstract: Compounds of formula (I) in which R.sup.4 is a phenyl radical substituted by R.sup.5, where R.sup.5 is a tetrazole-5-yl-radical optionally substituted by a radical R.sup.6, are novel efficacious PDE3/4 inhibitiors.

Abstract: A compound of formula I: ##STR1## or a pharmaceutically acceptable salt, hydrate, ester, solvate, prodrug, metabolite, stereoisomer, or mixtures thereof, wherein:Y represents the atoms necessary to form a fused 5- to 6-membered, aromatic or non-aromatic, heterocyclic ring containing at least one nitrogen heteroatom in a 1,3-relationship with the nitrogen atom depicted in formula I, wherein Y may be unsubstituted or substituted with at least one alkyl, alkenyl, cycloalkyl, cycloalkenyl, aralkyl, aryl, double bonded oxygen, or --COOR.sup.5 group, or a moiety selected from the group consisting of: ##STR2## wherein R.sup.5 and R.sup.7 are independently hydrogen or alkyl, alkenyl, cycloalkyl, cycloalkenyl, aralkyl, or aryl.

Abstract: Non-steroidal compounds which are high affinity, high selectivity modulators for steroid receptors are disclosed. Also disclosed are pharmaceutical compositions incorporating such compounds, methods for employing the disclosed compounds and compositions for treating patients requiring steroid receptor agonist or antagonist therapy, intermediates useful in the preparation of the compounds and processes for the preparation of the steroid receptor modulator compounds.

Abstract: The present invention relates to the use of 4a, 5a, 8a, 8b-tetrahydro-6H-pyrrolo[3',4':4,5]furo[3,2-b]pyridine-6,8(7H)-dione derivatives of the general formula (I) and salts thereof, ##STR1## in which the radicals R.sup.1 to R.sup.5 have the meaning given in the description, and to novel 4a, 5a, 8a, 8b-tetrahydro-6H-pyrrolo[3',4':4,5]furo[3,2-b]pyridine-6,8(7H)-dione derivatives and processes for their preparation.

Abstract: An immunogen/vaccine adjuvant composition containing an immunogen in an amount effective to stimulate an immune response and as a vaccine adjuvant a 1H-imidazo[4,5-c]quinolin-4-amine in an amount effective to increase the immune response to the immunogen.

Abstract: A class of benzopyrans, benzothiopyrans, dihydroquinolines, dihydronaphthalenes, and analogs thereof, is described for use in treating cyclooxygenase-2 mediated disorders. Compounds of particular interest are defined by Formula I'wherein X, A.sup.1, A.sup.2, A.sup.3, A.sup.4, R, R", R.sup.1 and R.sup.2 are as described in the specification.