Abstract: Compounds of formula (I) wherein n1 is 0, 1, or 2; n2 is 0, 1, or 2; X is a bond, O, S, or NR1; and Ar1 is a 5-membered aromatic ring, 6-membered aromatic ring, or a fused bicycloheterocycle. The compounds are useful in treating conditions or disorders prevented by or ameliorated by ?7 nAChR ligands. Also disclosed are pharmaceutical compositions having compounds of formula (I) and methods for using such compounds and compositions.

Abstract: The present invention described the administration of halogenated flosequinan derivatives and the enantiomers of halogenated flosequinan derivatives for the treatment of sexual dysfunction (in males and females) and for the treatment of cardiovascular disease.

Abstract: The invention provides compounds of Formula I: wherein Azabicyclo is W is a six-membered heterocyclic ring system having 1–2 nitrogen atoms or a 10-membered bicyclic-six-six-fused-ring system having up to two nitrogen atoms within either or both rings, provided that no nitrogen is at a bridge of the bicyclic-six-six-fused-ring system, and further having 1–2 substitutents independently selected from R3. These compounds may be in the form of pharmaceutical salts or compositions, may be in pure enantiomeric form or racemic mixtures, and are useful in pharmaceuticals to treat diseases or conditions in which ?7 is known to be involved.

Abstract: Compounds of formula I: wherein A, D, Ar1, E and Ar2 are as defined in the specification, processes for preparing them, pharmaceutical compositions containing them and their use in therapy, especially in the treatment or prophylaxis of psychotic and intellectual impairment disorders.

Abstract: The present invention relates to 3-substituted-2-(arylalkyl)-1-azabicycloalkanes, methods of preparing the compounds and methods of treatment using the compounds. The azabicycloalkanes generally are azabicycloheptanes, azabicyclooctanes, or azabicyclononanes. The aryl group in the arylalkyl moiety is a 5- or 6-membered ring heteroaromatic, preferably 3-pyridinyl and 5-pyrimidinyl moieties, and the alkyl group is typically a C1-4 alkyl. The substituent at the 3-position of the 1-azabicycloalkane is a carbonyl group-containing moiety, such as an amide, carbamate, urea, thioamide, thiocarbamate, thiourea or similar functionality. The compounds exhibit activity at nicotinic acetylcholine receptors (nAChRs), particularly the ?7 nAChR subtype, and are useful towards modulating neurotransmission and the release of ligands involved in neurotransmission.

Abstract: The invention provides compounds of Formula I: wherein Azabicyclo is any of: 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 ?7 is known to be involved.

Abstract: The invention provides compounds of general formula (I) 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: The present invention provides novel compounds, corresponding to formulae I and II, respectively, which are able to reactivate the apoptosis-inducing function of mutant p53 proteins. This reactivation is provided by restoration of sequence-specific DNA-binding activity and transcriptional transactivation function to mutant p53 proteins, and modulation of the conformation-dependent epitopes of the p53 protein. Accordingly, the substances according to the invention will be used in pharmaceutical compositions and methods for treatment of patients suffering from various types of tumors.

Abstract: The invention relates to carbamates having general structure (I), wherein: R1, R2 and R3 are H, OH, SH, CN, F, Cl, Br, I, (C1-C4)-alkylthio, (C1-C4)-alkoxyl, (C1-C4)-alkoxyl substituted by one or several F radicals, carbamoylamine, (C1-C4)-alkyl and (C1-C4)-alkyl substituted by one or several F or OH radicals; R4 represents a substituted or non-substituted cycloalkyl or cycloaryl radical (a heteroalkyl radical or not). The amine of the quinuclidine ring can also be forming quatemary ammonium salts or in an oxidized state (N-oxide). Carbamates (I) are antagonists of the M3 muscarinic receptor, and selectively, the M2 receptor. Hence, they can be used in the treatment of urinary incontinence (particularly due to bladder instability), irritable bowel syndrome, diseases of the respiratory tract (particularly chronic obstructive pulmonary disease, chronic bronchitis, asthma, emphysema and rhinitis) and in ophthalmologic operations.

Abstract: The present invention relates to aryl olefinic azacyclic compounds and aryl acetylenic azacyclic compounds, including pyridyl olefinic cycloalkylamines and pyridyl acetylenic cycloalkylamines. The present invention also relates to prodrug derivatives of the compounds of the present invention.

Abstract: This invention relates to novel 3-substituted quinuclidine derivatives, which are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.

Abstract: The invention relates to substituted polycyclic aryl and heteroaryl pyridone compounds useful inhibitors of serine proteases of the coagulation cascade and compounds, compositions and methods for anticoagulant therapy for the treatment and prevention of a variety of thrombotic conditions including coronary artery and cerebrovascular diseases.

Abstract: The invention provides compounds of Formula I: wherein m1 is 0 or 1; m2 is 1 or 2; R1 is —H, alkyl, halogenated alkyl, substituted alkyl, cycloalkyl, or phenyl; R2 is —H, alkyl, halogenated alkyl, substituted alkyl, cycloalkyl, or phenyl, provided that when m1 is 1 at least one of R1 and R2 is —H; or a pharmaceutically acceptable salt, pharmaceutical composition, a pure enantiomer or racemic mixture thereof. The invention also provides a method for treating a disease or condition in a mammal, wherein the ?7 nicotinic acetylcholine receptor is implicated and for treating diseases where there is a sensory-gating deficit in a mammal comprising administering to a mammal a therapeutically effective amount of a compound of Formula I. These compounds may be in the form of pharmaceutical salts or compositions, and may be in pure enantiomeric form or may be racemic mixtures.

Abstract: The invention provides compounds of Formula I: These compounds may be in the form of pharmaceutical salts or compositions, may be in pure enantiomeric form or racemic mixtures, and are useful in pharmaceuticals to treat conditions or diseases in which ?7 is known to be involved.

Abstract: The invention provides compounds of Formula I: wherein Azabicyclo is W0 is a bicyclic moiety and is These compounds may be in the form of pharmaceutical salts or compositions, may be in pure enantiomeric form or racemic mixtures, and are useful in pharmaceuticals in which ?7 is known to be involved.

Abstract: The present invention provides methods for purifying, identifying and using optically active isomers of quinine and quinidine as well as compositions comprising such optically active isomers. Such optically active isomers having desired actions on cardiac sodium and potassium channel function substantially separable from undesirable effects on GI motility can be useful for more effective therapy of cardiac arrhythmias. Also disclosed are methods for assaying the levels of such isomers present in the biological fluids.

Abstract: A water solution of a mixture of quinine and camphor in preferably a ratio of 2 parts quinine to 1 part camphor is injected into hemorrhoidal tissue to effectuate a cure of the hemorrhoid. After a period of time, dependent upon the age and other aspects of the physical condition of the patient, the hemorrhoid will turn black, shrivel and flake off to yield a clean non-hemorrhoid area surrounding the anus.

Abstract: A compound which is a carbamate of formula: 1

Abstract: A method for treating fibromyalgia syndrome with an agonist of &agr;7 nicotinic acetylcholine receptors.

Abstract: This invention concerns the use of the brucine (2,3-dimethoxystrychnidin-10-one) or a dermatologically acceptable derivative thereof in the treatment of damaged mammalian skin.

Abstract: The invention provides compounds of Formula I: wherein W0 is a bicyclic moiety and is These compounds may be in the form of pharmaceutical salts or compositions, may be in pure enantiomeric form or racemic mixtures, and are useful to treat diseases or conditions in which &agr;7 is known to be involved.

Abstract: A compound which is a carbamate of formula: 1

Abstract: The present invention relates to injecting a high specificity p38 kinase inhibitor into a diseased intervertebral disc.

Abstract: The invention provides compounds of Formula I: 1

Abstract: Patients susceptible to or suffering from disorders, such as central nervous system disorders, which are characterized by an alteration in normal neurotransmitter release, such as dopamine release (e.g., Parkinsonism, Parkinson's Disease, Tourette's Syndrome, attention deficient disorder, or schizophrenia), are treated by administering a 1-aza-2-(3-pyridyl)bicyclo[2.2.1]heptane, a 1-aza-2-(3-pyridyl)bicyclo[2.2.2]octane, a 1-aza-2-(3-pyridyl)bicyclo[3.2.1]octane, a 1-aza-2-(3-pyridyl)bicyclo[3.2.2]nonane, a 1-aza-7-(3-pyridyl) bicyclo[2.2.1]heptane, a 1-aza-3-(3-pyridyl)bicyclo[3.2.2]nonane, or a 1-aza-7-(3-pyridyl)bicyclo[3.2.2]nonane. The compounds can exist as individual stereoisomers, racemic mixtures, diastereomers and the like.

Abstract: According to the subject invention, antimalarial drugs (including salts or isomers thereof) may be used to treat degenerative disease. Antimalarial drugs include mefloquine, the enantiomers of mefloquine, hydroxychloroquine, the enantiomers of hydroxychloroquine, chloroquine, primaquine and quinine, and also their metabolites.

Abstract: A composition useful for protecting and/or repairing DNA from oxidative damages said composition comprising redistilled cow's urine distillate (RCUD) having components benzoic acid, and hexanoic acid, with ammonia content of the composition ranging between 5-15 mg/L, and optionally along with anti-oxidants; and a method of protecting and/or repairing DNA from oxidative damages using composition of claim 1, said method comprising steps of estimating the amount of folded DNA in a sample, mixing the said composition to the said DNA either before or after the exposure of the DNA to the oxidatively DNA-damaging agent, and determining percentage folded DNA in the mixture showing protection and/or repair of DNA from oxidative damages.

Abstract: The present invention relates to the delivery of muscle relaxants through an inhalation route. Specifically, it relates to aerosols containing muscle relaxants that are used in inhalation therapy. In a method aspect of the present invention, a muscle relaxant is delivered to a patient through an inhalation route. The method comprises: a) heating a coating of a muscle relaxant, on a solid support, to form a vapor; and, b) passing air through the heated vapor to produce aerosol particles having less than 5% muscle relaxant degradation products. In a kit aspect of the present invention, a kit for delivering a muscle relaxant through an inhalation route is provided which comprises: a) a coating of a muscle relaxant and b) a device for dispensing said coating a muscle relaxant as a condensation aerosol.

Abstract: This invention relates to salts of guanidine derivatives of formula R—X—C(═NH)NH3+Z−, wherein X represents a valence bond, —CH2—NH—, —CH2—NH—NH— or —CH═N—NH—; R represents a linear or branched C1-C30 alkyl, C3-C20 cycloalkyl, adamantyl, norbornyl, tricyclodecyl, benzyl, furyl, pyridyl, anthracyl, naphthyl, phenanthryl, perinaphthyl or quinuclidinyl residue, which can be substituted by one or more hydroxyl groups, C1-C4 alkoxy groups, C1-C4 alkyl groups and/or one or more halogen atoms or one or more amino groups; Z represents O—CO—Y, O—S(O)2—Y, or O—P(O)(OH)—Y; and Y represents a linear or branched C1-C12 alkyl, C3-C8 cycloalkyl, benzyl, furyl or pyridyl residue, which can be substituted by one or more hydroxyl groups, carboxylic acid groups, C1-C4 alkoxy groups, C1-C4 alkyl groups and/or one or more halogen atoms or one or more amino groups.

Abstract: The present invention relates to the delivery of muscle relaxants through an inhalation route. Specifically, it relates to aerosols containing muscle relaxants that are used in inhalation therapy. In a method aspect of the present invention, a muscle relaxant is delivered to a patient through an inhalation route. The method comprises: a) heating a coating of a muscle relaxant, on a solid support, to form a vapor; and, b) passing air through the heated vapor to produce aerosol particles having less than 5% muscle relaxant degradation products. In a kit aspect of the present invention, a kit for delivering a muscle relaxant through an inhalation route is provided which comprises: a) a coating of a muscle relaxant and b) a device for dispensing said coating a muscle relaxant as a condensation aerosol.

Abstract: A pharmaceutical composition comprising therapeutically effective quantities of calcium channel blockers in combination with quinolines. In preferred embodiments, the invention further comprises quercetin. The components combine and interact in a manner to effectively treat viral infections.

Abstract: A water solution of a mixture of quinine and camphor in preferably a ratio of 2 parts quinine to 1 part camphor is injected into hemorrhoidal tissue to effectuate a cure of the hemorrhoid. After a period of time, dependent upon the age and other aspects of the physical condition of the patient, the hemorrhoid will turn black, shrivel and flake off to yield a clean non-hemorrhoid area surrounding the anus.

Abstract: The invention provides compounds of formula (I) wherein n, A, R1, R2 and R3 are as defined in the description, and the preparation thereof. The compounds of formula (I) are useful as pharmaceuticals.

Abstract: Radiolabeled ligands useful as probes for determining the relative abundance, receptor occupancy, and/or function of nicotinic acetylcholine receptors. The compounds of Formula I as described herein are labeled with a radioactive isotopic moiety such as 11C, 18F, 76Br, 123I or 125I. Disorders are diagnosed by administering to a mammal a detectably labeled compound and detecting the binding of that compound to the nAChR. The compounds that have been administered are detected using methods including, but not limited to, position emission topography and single-photon emission computed tomography. The present invention is useful in diagnosing a wide variety of diseases and disorders as discussed herein.

Abstract: The invention discloses compounds that are selective &agr;7 nAChR agonists and 5-HT3 antagonists. The compounds are useful for treating many CNS diseases.

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 pharmaceutical excipient, 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 pharmaceutical excipient. The invention still further provides for the use of a ferrous ion source as an anti-oxidant in pharmaceutical formulations.

Abstract: The invention features quaternary ammonium compounds of formula I, described herein, and their use in treating asthma, chronic obstructive pulmonary disorder, allergic rhinitis, and infectious rhinitis.

Abstract: A depressant of capsaicin-sensitive sensory nerve, containing quinuclidin-3′-yl 1-phenyl-1,2,3,4-tetrahydroisoquinoline-2-carboxylate or a salt thereof as an active ingredient, specifically a therapeutic drug of interstitial cystitis, hypersensitive disorder of the lower urinary tract, and/or abacterial prostatitis.

Abstract: A compound according to formula (I) 1

Abstract: A novel class of imidazo heterocyclic compounds, pharmaceutical compositions comprising them and use thereof in the treatment and/or prevention of diseases and disorders related to the histamine H3 receptor. More particularly, the compounds are useful for the treatment and/or prevention of diseases and disorders in which an interaction with the histamine H3 receptor is beneficial.

Abstract: A compound according to formula (I) wherein: is a phenyl ring, a C4 to C9 heteroaromatic compound containing one or more heteroatoms, or a naphthalenyl, 5,6,7,8-tetrahydronaphthalenyl or biphenyl group; which shows high affinity for muscarinic M3 receptors (Hm3).

Abstract: The use of [R-(Z)]-&agr;-(methoxyimino)-&agr;-(1-azabicyclo[2.2.2]oct-3-yl)acetonitrile or a pharmaceutically acceptable salt thereof for the treatment of neuropsychiatric symptoms in patients with Alzheimer's Disease is disclosed.

Abstract: This invention is directed towards substituted aminoquinuclidine compounds useful as delta-opioid receptor modulators, delta-opioid receptor agonists useful as analgesics and delta-opioid receptor antagonists useful as immunosuppressants, antiinflammatory agents, agents for the treatment of neurological and psychiatric conditions, medicaments for drug and alcohol abuse, agents for treating gastritis and diarrhea, cardiovascular agents and agents for the treatment of respiratory diseases.

Abstract: After refractive surgery to reduce ametropy (i.e. myopia, astigmatism or hypermetropia) an average percentage of patients between 15.8% after PRK (Photo Refractive Keratectomy) and 33% after LASIK (Laser in situ Keratomileusis) shows a poor night sight due to the presence of halos, glare and coma. A comparable disorder is present in a percentage of patients that underwent lensectomy (cataract or refractive lensectomy) with intra ocular lens (IOL) implant and IOL implants in phakic patients to reduce ametropy. Thanks to the effect on pupillary kinetics, diluted low concentrations (from 0.002% to 0.040%) of Aceclidine were surprisingly found to effectively reduce and/or eliminate night sight problems for about 6 hours.

Abstract: Disclosed are compounds of the formula and the pharmaceutically acceptable salts thereof wherein R, Ar, A, n, R1 and R2 are defined herein. These compounds are highly selective agonists, antagonists or inverse agonists for GABAA brain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAA brain receptors and are therefore useful in the diagnosis and treatment of anxiety, depression, Down Syndrome, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory. Pharmaceutical compositions, including packaged pharmaceutical compositions, are also disclosed.

Abstract: Squaric acid derivatives of formula (1) are described: wherein Het is an optionally substituted bicyclic fused ring heteroaromatic group; L2 is a covalent bond or an atom or group —O—, —S—, —C(O)—, —C(S)—, —S(O)—, —S(O)2, —N(R8)— or —C(R8)(R8a)—; Ar2 is an optionally substituted aromatic or heteroaromatic group; Alk is a chain  in which R is a carboxylic acid (—CO2H) or a derivative or biostere thereof; R1 is a hydrogen atom or a C1-6alkyl group; L1 is a covalent bond or a linker atom or group; Alk1 is an optionally substituted aliphatic chain; n is zero or the integer 1; R2 is a hydrogen atom or an optionally substituted heteroaliphatic, cycloaliphatic, heterocycloaliphatic, polycycloalphatic, heteropolycycloaliphatic, aromatic or heteroaromatic group other than a 2,6-naphthyridin-1-yl, isoquinolin-1-yl, 2,7-naphthyridin-1-yl or quinazolin-4-yl group; and the salt

Abstract: 5HT3-receptor-antagonists for the treatment of CFS (Chronic Fatigue Syndrome) are disclosed.

Abstract: The invention provides compounds of Formula I: 1

Abstract: Substituted isoquinolines, isochromanones and isothiochromanones that inhibit the pro-inflammatory cytokines tumor necrosis factor-alpha (TNF-alpha) and/or interleukin-6 (IL-6) and/or the enzyme cyclooxygenase-2 (COX-2) and/or interleukin-10 (IL-10). Compositions containing such compounds and methods of using such compounds for treatment and/or prevention of inflammation, inflammatory diseases, immunologic diseases and other diseases mediated by TNF-alpha, IL-6, COX-2 and/or IL-10 are also disclosed.

Abstract: A compound of formula (I), wherein B is a phenyl ring, a 5 to 10 membered heteroaromatic group containing one or more heteroatoms, or a naphthalenyl, 5,6,7,8-tetrahydronaphthalenyl, benzo[1,3]dioxolyl, or biphenyl group; R1, R2 and R3 each independently represent a hydrogen or halogen atom, or a hydroxy group, a phenyl group, —OR7, —SR7, —NR7R8, —NHCOR7, —CONR7R8, —CN, —NO2, —COOR7 or CF3 group, or a strait or branched, substituted or unsubstituted lower alkyl group, wherein R7 and R8 each independently represent a hydrogen atom, a straight or branched lower alkyl group, or together form an alicyclic ring; or R1 and R2 together form an aromatic or alicyclic ring or a heterocyclic group.