Abstract: The invention provides compounds of Formula I: These compounds may be in the form of pharmaceutical salts or compositions, and racemic mixtures or pure enantiomers thereof. The compounds of Formula I are useful in pharmaceuticals in which &agr;7 is known to be involved.

Abstract: The invention provides compounds of general formula in which m, A, R1 and Ar have the meanings defined in the specification; a process for their preparation; pharmaceutical compositions containing them; a process for preparing the pharmaceutical compositions; and their use in therapy.

Abstract: Compositions and methods are provided for prophylactic or therapeutic treatment of a mammal for hearing impairments involving neuronal damage, loss, or degeneration, preferably of spinal ganglion neurons, by administration of a therapeutically effective amount of a trkB or trkC agonist, particularly a neurotrophin, more preferably NT-4/5. Also provided are improved compositions and methods for treatments requiring administration of a pharmaceutical having an ototoxic side-effect, wherein the improvement includes administering a therapeutically effective amount of a trkB or trkC agonist to treat the ototoxicity.

Abstract: The invention provides compounds of Formula I: These compounds may be in the form of pharmaceutical salts or compositions, and racemic mixtures or pure enantiomers thereof. The compounds of Formula I are useful in pharmaceuticals in which &agr;7 is known to be involved.

Abstract: Compositions comprising antimuscarinic compounds that have been modified to render them substantially irreversible, such as by quaternization of the heterocyclic ring nitrogen, have improved properties when administered intravesically for treatment of bladder diseases, particularly urinary incontinence. Pharmaceutical compositions and methods of treatment using these improved compounds or improved routes of administration re disclosed.

Abstract: The invention provides compounds of Formula I: These compounds may be in the form of pharmaceutical salts or compositions, and racemic mixtures or pure enantiomers thereof. The compounds of Formula I are useful in pharmaceuticals in which &agr;7 is known to be involved.

Abstract: The invention provides 2, 3-, 4- or 5-substituted-N1-(arylsulfonyl)indole and (heteroaryl)indole compounds of the general formula (I): 1

Abstract: The present invention relates to aryl olefinic azacyclic compounds and aryl acetylenic azacylic compounds. The present invention relates in particular to five-membered heteroaromatic olefinic azacyclic compounds and five-membered heteroaromatic acetylenic azacylic compounds, including isoxazolyl olefinic cycloalkylamines and isoxazolyl acetylenic cycloalkylamines.

Abstract: Gamma aminobutyric acid (GABA) is a potent inhibitory neurotransmitter that binds to hetero-oligomeric receptors in the mammalian brain. In a previous study, we documented specific GABA binding to isolated rat hepatocytes which resulted in inhibition of hepatocyte proliferation. The purpose of the present study was to define the nature of hepatic GABAA receptors and document their expression during rapid liver growth (post-partial hepatectomy). Polymerase chain reactions (PCR) with gene-specific primers derived from published sequences were performed with marathon-ready human and rat liver cDNA. Two GABAA receptor subunit types (&bgr;3 and &egr;) were expressed in the human liver and one (&bgr;3) in the rat liver. PCR amplification of the human GABAA receptor &bgr;3 subunit produced a single product (m.w. 53-59 kDa). In the case of the &egr; subunit, two PCR products were identified.

Abstract: Methods for the simple, reliable application and local controlled release of selected anti-arrhythmia drugs from a hydrogel applied to or polymerized on the tissues of the heart or its vessels, especially in conjunction with cardiac bypass or other cardiac surgery, have been developed. The anti-arrhythmia drugs are incorporated into hydrogels that biodegrade and adhere to the tissues to which the anti-arrhythmic drugs are to be delivered. The hydrogels may be formed in vitro or in vivo. In a preferred embodiment, the drugs are effective to lengthen atrial effective refractory period. A particularly preferred drug is amiodarone.

Abstract: The present invention relates to bicylic 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: This invention relates to the treatment of antibiotic-resistant infections, including particularly infections caused by bacteria, Mycobacteria and fungi. A preferred group of compositions of the invention contain as active agents compounds containing pyridyl, quinolyl or benzoquinolyl ring systems substituted on the nitrogen-containing ring at the carbon opposite the nitrogen by a carbon bound to an oxygen which is also bound to a nitrogen through a saturated carbon or carbon chain, or, in the case of the pyridyl ring system, the substituent at the 4 position of the pyridyl ring may be an alkyl which may be substituted with halo, hydroxy, alkoxy, amino or alkylamino.

Abstract: Pharmaceutical compositions include aryl substituted amine compounds, and in particular, carbon-linked aromatic azabicyclo compounds, and in particular, aromatic alkylene azabicyclo compounds and aromatic alkyl azabicyclo compounds.

Abstract: This invention relates to the use of 5-HT3 receptor antagonists in the treatment of nonconstipated female IBS patients.

Abstract: The invention provides methods for inhibiting oxidative degradation of pharmaceutical formulations comprising at least one oxidation-susceptible active drug ingredient which methods comprise adding an oxidation-inhibiting amount of a ferrous ion source, preferably in the form of a pharmaceuticalexcipient, to the formulation. The invention further provides pharmaceutical formulations comprising at least one oxidation-susceptible active drug ingredient and an oxidation-inhibiting amount of a ferrous iron source, preferably in the form of a pharmaceuticalexcipient. The invention still further provides for the use of a ferrous ion source as an anti-oxidant in pharmaceutical formulations.

Abstract: The invention provides compounds of Formula I: 1

Abstract: Novel dry skin remedies useful for treatment dry skin, containing as the active ingredient spiro [oxathiolane-quinuclidine] derivatives represented by general formula (I) or acid addition salts thereof, desirably cis-2-methylspiro [1,3-oxathiolane-5,3′-quinuclidine] hydrochloride. The remedies promote the secretion of sebaceous and sweat glands through oral or parenteral administration to treat dry skin, thus being useful as drugs.

Abstract: A method of increasing the bioavailability upon oral administration of a pharmacologically active target agent, particularly an antitumor or antineoplastic agent which exhibits poor or inconsistent oral bioavailability (e.g., paclitaxel, docetaxel or etoposide), comprises the oral co-administration to a mammalian patient of the target agent and an oral bioavailability-enhancing agent (e.g., cyclosporin A, cyclosporin D, cyclosporin F or ketoconazole). The enhancing agent may be administered orally from 0.5-24 hrs. prior to the oral administration of one or more doses of the target agent, substantially simultaneously with the target agent or both prior to and substantially simultaneously with the target agent.

Abstract: Two crystalline polymorphic forms of (2-Benzhydryl-1-azo-bicyclo[2.2.2]oct-3-yl)-(5-isopropyl-2-methoxybenzyl)-amine citrate monohydrate (the monohydrates) are Form A and Form B. The pharmaceutical composition containing at least one of these polymorphs has advantageous stability for formulation to treat acute emesis in patient receiving chemotherapy. The administration of this pharmaceutical composition is conventional oral by preferably tablet or capsule and intravenous. A method of making A and B Forms is also disclosed.

Abstract: The invention provides compounds of Formula I: 1

Abstract: The invention provides compounds of Formula I: 1

Abstract: The present invention relates to a method of treating or preventing a disorder selected from stroke, epilepsy, head trauma, spinal cord trauma, ischemic neuronal damage such as cerebral ischemic damage from stroke or vascular occlusion (e.g., during open heart surgery), excitotoxic neuronal damage (e.g., in stroke or epilepsy) and amyotrophic lateral sclerosis in mammals, including humans, using an NK-1 antagonist. It also relates to a method of treating or preventing such disorders in mammals, including humans, using certain quinuclidine derivatives, piperidine derivatives, pyrrolidine derivatives, azanorbornane derivatives, ethylene diamine derivatives and related compounds that are substance P receptor antagonists.

Abstract: The invention provides compounds of Formula I: 1

Abstract: The invention provides compounds of Formula I: 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: Compounds of formula (I) wherein the groups are as defined in the description are disclosed. The compounds of formula (I) are endowed with reversible inhibiting activity of carnitine palmitoyl-transferase and are useful in the preparation of medicaments useful in the pathologies related to a hyperactivity of carnitine palmitoyl-transferase, such as hyperglycemia, diabetes and pathologies related thereto, heart failure, ischemia.

Abstract: The invention provides compounds of Formula I: 1

Abstract: A method of treating glaucoma or ocular hypertension in a patient, which comprises administering to the patient a pharmaceutically effective amount of a compound of formula I:

Abstract: A substance P antagonist is used in a cosmetic composition to treat sensitive skin. More specifically, a cosmetic composition containing a substance P antagonist is used to prevent and/or combat skin irritations, desquamation, erythermas, sensations of dysesthesia/overheating, or pruritus of the skin.

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: in which X is CH or N, R is H, Cl or OR1 in which R1 is H or an alkyl group having from 1 to 3 carbon atoms, Het is the 3-endotropyl group (that is, the 8-methyl-8-azadicyclo[3.2.1]oct-3-yl group) or the 3-quinuclidyl group (that is, the 1-azadicyclo[2.2.2]oct-3-yl group); these compounds have been found to be potent and selective antagonists of the 5-HT3 serotonin-like receptor and can therefore be used, for example, as anti-emetics as well as in various pathological conditions of the central nervous system, and as antitussives.

Abstract: The present invention relates to the different roles inorganic ion receptors have in cellular and body processes. The present invention features: (1) molecules which can modulate one or more inorganic ion receptor activities, preferably the molecule can mimic or block an effect of an extracellular ion on a cell having an inorganic ion receptor, more preferably the extracellular ion is Ca2+ and the effect is on a cell having a calcium receptor; (2) inorganic ion receptor proteins and fragments thereof, preferably calcium receptor proteins and fragments thereof; (3) nucleic acids encoding inorganic ion receptor proteins and fragments thereof, preferably calcium receptor proteins and fragments thereof; (4) antibodies and fragments thereof, targeted to inorganic ion receptor proteins, preferably calcium receptor protein; and (5) uses of such molecules, proteins, nucleic acids and antibodies.

Abstract: Methods are disclosed for correcting biological information transfer in a patient in need of such therapy which comprise administration to a patient of a composition comprising a therapeutically effective amount of a biocomplex comprising at least one bioactive agent from each of the three informational blocks of biological information transfer, each agent being present in an amount sufficient to correct the biological information transfer of the patient under treatment and resulting in the resumption of normal cell metabolism, said amount being less than the buffering amount of said agent; together with a carrier therefor.

Abstract: The pharmaceutical formulations according to the invention contain from 0.5 to 50% by weight of a cyclic quaternary ammonium compound and pharmaceutically appropriate excipients and are formulated by wet granulation, preferably with polysorbate 80.

Abstract: The invention concerns new guanidine derivatives of formula (I), methods of preparing them and their use in drugs containing such compounds.

Abstract: The invention concerns new guanidine derivatives of formula (I), methods of preparing them and their use in drugs containing such compounds.

Abstract: This invention relates to the use of 5-HT3 receptor antagonists in the treatment of nonconstipated female IBS patients.

Abstract: The present invention provides a method for treating a condition selected from the group consisting of schizophrenia, schizoaffective disorder, and schizophreniform disorder in a patient using a Compound (I).

Abstract: The present invention relates to pleuromutilin derivatives, to processes for their preparation, to pharmaceutical compositions containing them and to their use in medical therapy, particularly antibacterial therapy.

Abstract: The present invention relates to a novel method for treating a mammal suffering from gastrointestinal motility disorders.

Abstract: The present invention relates to a novel method for treating a mammal suffering from gastrointestinal motility disorders.

Abstract: The present invention relates to a novel method for treating a mammal suffering from gastrointestinal motility disorders.

Abstract: Two crystalline polymorphic forms of (2-Benzhydryl-1-azo-bicyclo(2.2.2]Octyl-3-yl)-(5-iso-propyl-2-methoxybenzyl)amine dihydrochloride dihydrate are Form I and Form II. The pharmaceutical composition containing at least are of these polymorphs has advantageous stability for formulation to treat emesis in patients receiving chemotherapy. The administration of this pharmaceutical composition is conventional oral by preferably tablet or capsule or intravenous. A method of making Forms I and II is also disclosed.

Abstract: The present invention relates to a method of treating or preventing symptoms of irritable bowel syndrome in a mammal, including a human, using a compound that is an NK-1 receptor antagonist, in particular a substance P receptor antagonist.

Abstract: A single crystalline polymorphic form (2S,3S)-N-(methoxy-5-t-butylphenylmethyl-2-diphenylmethyl-1-azobicyclo[2,2,2] octan-3-amine citrate(citrate monohydrate) and its pharmaceutical composition. The pharmaceutical composition of the polymorphic form if the citrate monohydrate has advantageous stability for formulation to treat emesis. The administration of this pharmaceutical composition is immediate release, oral dosage form preferably by tablet or capsule or intravenous.

Abstract: Derivatives of mutiline of formula (1A) and pharmaceutically acceptable salts and derivatives thereof, in which R1 is ethyl or vinyl, Y is a carbamoyloxy group, in which the N-atom is unsubstituted, or mono- or di-substituted, are useful in the treatment of bacterial infections.

Abstract: The present invention is concerned with the use of 5HT3 antagonists for promoting intestinal lavage, especially in combination with an osmotic agent.

Abstract: The present invention provides a compound of formula (I) wherein R is phenyl, C3-C7 cycloalkyl or heteroaryl, each of which being optionally benzo- or C3-C7 cycloalkyl-fused and optionally substituted, including in the benzo- or C3-C7 cycloalkyl-fused portion, by from 1 to 3 substituents each independently selected from C1-C4 alkyl, fluoro(C1-C4)alkyl, C1-C4 alkoxy, fluoro(C1-C4)alkoxy, phenoxy, C2-C4 alkanoyl, halo, C1-C4 alkoxycarbonyl, C3-C7 cycloalkyl, —S(O)m(C1-C4 alkyl), cyano, —NR2R3, —S(O)mNR2R3, —NR4(C1-C4 alkanoyl) and —CONR2R3, or R is 2,3-dihydrobenzo[b]furanyl or chromanyl; R1 is H or C1-C6 alkyl; W is a direct link, methylene or ethylene; X is unbranched C2-C4 alkylene; Y is phenyl, naphthyl, benzyl, pyridyl, thienyl or C3-C7 cycloalkyl, each of which being optionally substituted by from 1 to 3 substituents each independently selected from C1-C4 alkyl, fluoro(C1-C4)alkyl, C1-C4 alkoxy, fluoro(C1-C4)alkoxy, halo and cyano; Ar is phenyl, naphthyl, benzyl, th

Abstract: The cycloalkano-pyridines are prepared by reacting corresponding cycloalkano-pyridine-aldehydes with suitable organometallic compounds or Wittig or Grignard reagents or reacting compounds of the cycloalkano-pyridine alcohols type with suitable bromine compounds, and optionally varying the functional groups accordingly. The cycloalkanopyridines are suitable as active compounds in medicaments, in particular in medicaments for the treatment of hypertipoproteinaemia and arteriosclerosis.

Abstract: Patients can be helped to break free of addictive or habit-forming narcotics and anti-depressants, by treatment using two drugs. One drug is dextromethorphan (DM), which has been used for decades as an anti-tussive (cough-suppressing) drug in cough syrups. The other drug is an oxidase inhibitor which suppresses activity of a liver enzyme called cytochrome P450-2D6 (also called debrisoquin hydroxylase, sparteine monooxygenase, cytochrome P450-DB, and CYP2D6). In most patients, this oxidase enzyme rapidly degrades DM and converts it into a metabolite called dextrorphan. An oxidase inhibitor (such as quinidine) which suppresses cytochrome P450-2D6 activity increases the half-life and concentration of DM in the circulating blood. When this combined treatment was administered orally to patients who had become dependent on morphine and anti-depressant drugs because of chronic intractable pain, it initially helped the patients reduce their dosages of morphine and other drugs, including anti-depressants.

Abstract: A compound of formula (I) the process of preparing compounds of formula (I), their pharmaceutical compositions, and the method of treating diseases associated with M3 muscarinic and/or S—HT4 serotoninergic receptors.