Abstract: The present invention discloses novel cholinergic receptor ligands. The present invention also relates to the synthesis of substituted derivatives of aza-bridged bicyclic amines for use as muscarinic receptor ligands as well as methods of regulating function of certain cholinergic receptors, and hence acting as antagonists, agonists and partial agonists at certain specific cholinergic receptor subtypes. The present invention also relates to methods for treating disorders associated with cholinergic receptors.

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: Compounds of formula I wherein A represents: and R, R1, R2, R3 and R4 are as defined in the specification, pharmaceutically-cceptable salts thereof, processes for preparing them, pharmaceutical compositions containing them and their use in therapy, especially in the treatment or prophylaxis of psychotic disorders and intellectual impairment disorders.

Abstract: The invention relates to new heterocyclic compounds of general formula (I), and their salts with a base or an acid: 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 an endo or exo form of 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[3.2.2]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.

Abstract: The present invention comprises compounds, compositions thereof, and methods capable of delivering inositol hexaphospahte (IHP) to the cytoplasm of mammalian cells. In certain embodiments, the present invention relates to compounds, compositions thereof, and methods that enhance the ability of mammalian red blood cells to deliver oxygen, by delivering IHP to the cytoplasm of the red blood cells.

Abstract: The present invention provides an excellent squalene synthesizing enzyme inhibitor. Specifically, it provides a compound (I) represented by the following formula, a salt thereof or a hydrate of them.

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: A process for preparing compounds of formula (I), by nitrosating compounds of formula (II), compounds of formula (I) having pharmaceutical activity.

Abstract: The present invention relates compounds of the formula (I): wherein X represents hydrogen or a C1-4alkyl group optionally substituted by a hydroxy group; Y represents hydrogen, C1-6alkyl or C3-7cycloalkyl; Z is —CR9R10CH2— or —CH2CR9R10—; R represents hydrogen, fluorine, hydroxy, C1-6alkyl or C1-6alkoxy; and R1, R2, R3, R4, R5 and R6 are as defined herein. The compounds are of particular use in the treatment of depression, anxiety, pain, inflammation, migraine, emesis or postherpetic neuralgia.

Abstract: The present invention relates to novel cysteine protease inhibitors of Formula I: the pharmaceutically acceptable salts and N-oxide derivatives thereof, their use as therapeutic agents and methods of making them.

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 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 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: 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 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 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: 1

Abstract: A method of preparing carboxylic acid derivatives comprising mixing a quaternary ammonium salt having a particular triazine ring in the molecules thereof, a carboxylic acid compound and a compound having a nucleophilic functional group, to condense the carboxylic acid with the compound having the nucleophilic functional group. The invention further provides a condensing agent comprising the quaternary ammonium salt. The condensation is conducted under mild conditions to form carboxylic acid derivatives and, particularly, amide compounds or ester compounds maintaining high yields.

Abstract: A compound shown by the formula II, wherein Het is a mono- or polycyclic heterocyclic group comprising one or more hetero atoms selected from the group consisting of N, O and S which may be the same or different from each other; R1 is hydrogen, an optionally substituted lower alkyl or an optionally substituted lower alkenyl; A is an optionally substituted lower alkylene, an optionally substituted lower alkenylene or a single bond; B is an optionally substituted imino or a single bond; or A and B taken together may form a single bond; and D is a single bond or a group of the formula (a):

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: The present invention provides non-peptidic amino derivatives, their therapeutic use as well as pharmaceutical compositions that possess activity as Follicle Stimulating Hormone (FSH) agonists and are useful in the for treatment of infertility. In particular, the invention provides cyclic and acyclic alpha- and beta-aminocarboxamides, more particularly tetrahydroisoquinolinecarboxamides, piperidinecarboxamides, pyrrolidinecarboxamides, and 2-amino-3-carboxamidopyridine derivatives.

Abstract: The invention provides compounds of Formula I: 1

Abstract: There is provided a process for preparing a pharmacologically acceptable salt of N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl-amino acid which comprises condensing an amino acid and N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanine.

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: This invention provides a compound of general formula (I) 1

Abstract: The invention provides compounds of Formula I: 1

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: 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: A composition having the formula: wherein R is a linear alkyl, branched alkyl, cycloalkyl, polycyclic alkyl, alkylaminoalkyl, or alkyloxyalkyl group having 1 to 20 carbon atoms and at least one primary, secondary, or tertiary amino functional group. The composition is effective as a catalyst in the production of polyurethanes.

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

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: 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: 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: Compounds of the formula wherein R1 is methoxy and R2 is selected from the group consisting of methyl, ethyl, isopropyl, sec-butyl and tert-butyl; and the pharmaceutically acceptable salts of such compounds. These compounds are substance P antagonists and useful in the treatment of gastrointestinal disorders, inflammatory disorders, central nervous system disorders and pain.

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: This invention provides a compound of the formula (I): ##STR1## and its pharmaceutically acceptable salts, wherein A.sup.1 and A.sup.2 are each halo; R.sup.1 and R.sup.2 are independently C.sub.1-4 alkyl; R.sup.3 is substituted or unsubstituted, phenyl or naphthyl; Y is heterocyclic group selected from C.sub.5-10 azacycloalkyl, C.sub.6-10 diazacycloalkyl, C.sub.7-10 azabicycloalkyl and the like; and R.sup.4 is selected from (a) substituted or unsubstituted C.sub.1-8 alkyll; (b) substituted or unsubstituted amino; (c) substituted or unsubstituted C.sub.2-6 alkanoyl; (d) substituted or unsubstituted C.sub.3-8 cycloalkyl or C.sub.7-14 bicycloalkyl; (e) substituted or unsubstituted C.sub.5-10 azacycloalkyl or C.sub.6-10 diazacycloalkyl, and (f) substituted or unsubstituted C.sub.7-14 mono- or di-azabicycloalkyl. These compounds are useful for the treatment of medical conditions caused by bradykinin such as inflammation, cardiovascular disease, pain, etc.

Abstract: Compounds of formula (3), and pharmaceutically acceptable salts and derivatives thereof, in which R.sup.1 is vinyl or ethyl; and R.sup.2 is a group R.sup.3, R.sup.4 CH.sub.2 --, or R.sup.5 R.sup.6 C.dbd.CH--; wherein each of R.sup.3 and R.sup.4 is an azabicyclic ring system or R.sup.5 and R.sup.6 together with the carbon atom to which they are attached form an azabicyclic ring system, are useful in the prevention and treatment of microbial infections.

Abstract: The present invention provides heterocyclic compounds which are useful for modulating a muscarinic receptor.

Abstract: The present invention relates to therapeutically active quaternary azacyclic or azabicyclic compounds with formula I: ##STR1## wherein X is oxygen or sulfur and wherein G is selected from the group of azacyclic or azabicyclic ring systems consisting of: ##STR2## a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in treating a cholinergic deficit in the peripheral system.

Abstract: This invention relates to compounds of formula (I), or pharmaceutically acceptable acid addition salts thereof, wherein: (a) R.sup.2 and R.sup.5 are taken separately and R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are each independently hydrogen, (C.sub.1 -C.sub.6) alkyl, halo, CF.sub.3, OH or OR.sup.7 and R.sup.5 is methyl or ethyl; or (b) R.sup.2 and R.sup.5 are taken together, forming a chroman-4-ol ring, and R.sup.1, R.sup.3 and R.sup.4 are each independently hydrogen, (C.sub.1 -C.sub.6) alkyl, halo, CF.sub.3, OH or OR.sup.7 ; and R.sup.6 is a substituted piperidinyl, pyrrolidinyl or 8-azabicyclo(3.2.1)octanyl derivative; provided that (a) when R.sup.2 and R.sup.5 are taken separately, at least one of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 is not hydrogen; and (b) when R.sup.2 and R.sup.5 are taken together, at least one of R.sup.1, R.sup.3 and R.sup.

Abstract: The present invention relates to therapeutically active azacyclic or azabicyclic compounds, a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in treating diseases in the central nervous system caused by malfunctioning of the muscarinic cholinergic system.

Abstract: The present invention relates to therapeutically active azabicyclic compounds of formula I ##STR1## wherein X, R.sup.1, R.sup.2, R.sup.3, Ar, m and n are defined in the description, a method of preparing the same and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in treating a disease in the central nervous system caused by malfunctioning of the muscarinic cholinergic system.

Abstract: The invention relates to compounds of the formula ##STR1## in which: A is a divalent radical selected from:A.sub.1) --O--CO--A.sub.2) --CH.sub.2 --O--CO--A.sub.3) --O--CH.sub.2 --CO--A.sub.4) --O--CH.sub.2 --CH.sub.2 --A.sub.5) --N(R.sub.1)--CO--A.sub.6) --N(R.sub.1)--CO--CO--A.sub.7) --N(R.sub.1)--CH.sub.2 --CH.sub.2 --A.sub.8) --O--CH.sub.2 --in which:R.sub.1 is a hydrogen or a (C.sub.1 -C.sub.4)-alkyl; andAm is a nitrogen-containing heterocycle.