Abstract: A pharmaceutical composition comprising: (a) an active substance consisting of a compound of formula 1 wherein X? is an anion; (b) ethanol or a mixture of ethanol and water; (c) a pharmacologically acceptable acid.

Abstract: Soft anticholinergic esters of the formulas: wherein R1 and R2 are both phenyl or one of R1 and R2 is phenyl and the other is cyclopentyl; R is C1-C8 alkyl, straight or branched chain; and X? is an anion with a single negative charge; and wherein each asterisk marks a chiral center; said compound having the R, S or RS stereoisomeric configuration at each chiral center unless specified otherwise, or being a mixture thereof.

Abstract: Soft anticholinergic zwitterions of the formulas: wherein R1 and R2 are both phenyl or one of R1 and R2 is phenyl and the other is cyclopentyl; and wherein each asterisk marks a chiral center; said compound having the R, S or RS stereoisomeric configuration at each chiral center unless specified otherwise, or being a mixture thereof.

Abstract: The present invention relates to novel pharmaceutical compositions based on fluorene carboxylic acid ester derived anticholinergics of formula 1 and soluble TNF receptor fusion proteins, processes for preparing them and their use in the treatment of respiratory diseases.

Abstract: The present application describes deuterium-enriched tiotropium, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.

Abstract: Fluorenecarboxylic acid esters of general formula 1 wherein X? and the groups A, R, R1, R2, R3, R3?, R4, and R4? have the meanings given in the claims and in the specification, processes for the manufacture thereof and the use thereof as medicaments.

Abstract: Soft anticholinergic zwitterions of the formulas: wherein R1 and R2 are both phenyl or one of R1 and R2 is phenyl and the other is cyclopentyl; and wherein each asterisk marks a chiral center; said compound having the R, S or RS stereoisomeric configuration at each chiral center unless specified otherwise, or being a mixture thereof.

Abstract: A pharmaceutical composition comprising: (a) a salt of formula 1 wherein: X? is an anion with a single negative charge; and (b) a betamimetic 2, or a solvate or hydrate thereof, optionally in the form of the enantiomers, mixtures of the enantiomers, or in the form of the racemates thereof, processes for preparing them and their use in the treatment of respiratory complaints.

Abstract: Xanthenecarboxylates of formula 1 wherein: A is a group selected from X? is an anion with a single negative charge; R is hydroxy, methyl, hydroxymethyl, ethyl, —CF3, —CHF2, or fluorine; R1 and R2, which are identical or different, are each C1-C5-alkyl which is optionally substituted by C3-C6-cycloalkyl, hydroxy, or halogen, or R1 and R2 together denote a —C3-C5-alkylene-bridge; and R3, R4, R3?, and R4?, which are identical or different, are each hydrogen, —C1-C4-alkyl, —C4-alkyloxy, hydroxy, —CF3, —CHF2, —CN, —NO2, or halogen, or a physiologically acceptable salt thereof, processes for preparing, them and their use in pharmaceutical compositions.

Abstract: Soft anticholinergic esters of the formulas: wherein R1 and R2 are both phenyl or one of R1 and R2 is phenyl and the other is cyclopentyl; R is C1-C8 alkyl, straight or branched chain; and X? is an anion with a single negative charge; and wherein each asterisk marks a chiral center; said compound having the R, S or RS stereoisomeric configuration at each chiral center unless specified otherwise, or being a mixture thereof.

Abstract: This invention provides compounds of formula I: wherein R1, R2, R3, R4, R5, R6 and R7 are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The compounds of this invention possess both ?2 adrenergic receptor agonist and muscarinic receptor antagonist activity. Such compounds are useful for treating pulmonary disorders, such as chronic obstructive pulmonary disease and asthma.

Abstract: Methscopolamine Tannate is prepared from methscopolamine salt and tannic acid salt in aqueous medium. Methscopolamine salt is Methscopolamine bromide or nitrate, preferably methscopolamine bromide, whereas tannic acid salt is an alkali metal salt of tannic acid, preferably potassium salt of tannic acid. The preparation leads to methscopolamine tannate composition having a purity of about 93 wt. %, based on the weight of the composition, with the balance comprising primarily water.

Abstract: The invention relates to a crystalline micronisate of (1?,2?,4?,5?,7?)-7-[(hydroxydi-2-thienylacetyl)oxy]-9,9-dimethyl-3-oxa-9-azoniatricyclo[3.3.1.02,4]nonane-bromide, processes for preparing it and its use for preparing a pharmaceutical composition, particularly for preparing a pharmaceutical composition with an anticholinergic activity.

Abstract: An aerosol solution formulation comprising: (a) a salt of formula 1 wherein X? is an anion (b) an HFC propellant; (c) a cosolvent; and (d) an inorganic or an organic acid, wherein the concentration of the acid is in a range that corresponds with a pH range of 2.5 to 5.5 in aqueous solution.

Abstract: A pharmaceutical composition comprising: (a) an anticholinergic of formula 1 wherein X? is an anion with a single negative charge; (b) a corticosteroid; and (c) a betamimetic, wherein each component (a), (b), and (c) are optionally in the form of the solvates or hydrates thereof, processes for preparing them, and their use in the treatment of respiratory diseases.

Abstract: Fluorenecarboxylic acid esters of general formula 1 wherein X? and the groups A, R, R1, R2, R3, R3?, R4, and R4? have the meanings given in the claims and in the specification, processes for the manufacture thereof and the use thereof as medicaments.

Abstract: A compound of formula 1 wherein X?, A, R1, R2, R3, and R4 may have the meanings given in the claims and in the specification, processes for preparing them, their use in pharmaceutical compositions, and methods of treating patients using them.

Abstract: The present application is directed to a method of synthesis of a bicyclic or polycyclic compound of formula I or formula II: in which E, G, Y, n, m, R, R1, R2, R3, R6, R7, R8 and R9 are as defined.

Abstract: Fluorenecarboxylic acid esters of general formula 1 wherein X? and the groups A, R, R1, R2, R3, R3?, R4, and R4? have the meanings given in the claims and in the specification, processes for the manufacture thereof and the use thereof as medicaments.

Abstract: Crystalline monohydrate of (1?,2?,4?,5?,7?)-7-[(hydroxydi-2-thienylacetyl)oxy]-9,9-dimethyl-3-oxa-9-azoniatricyclo[3.3.1.02,4]nonane bromide (tiotropium bromide monohydrate), processes for the preparation thereof, pharmaceutical compositions thereof, and their use.

Abstract: The invention relates to a new industrially useable process for preparing tropenol, optionally in the form of the acid addition salts thereof.

Abstract: A compound of formula 1 wherein: A is a group selected from X? is an anion with a single negative charge; R1 and R2 are each independently a C1-C4-alkyl optionally substituted with hydroxy or halogen; and R3, R4, R5, R6, R7, and R8 are each independently hydrogen, C1-C4-alkyl, C1-C4-alkyloxy, hydroxy, CF3, CN, NO2, or halogen, with the proviso that at least one of the groups R3, R4, R5, R6, R7, and R8 is not hydrogen, processes for preparing these compounds, pharmaceutical compositions containing these compounds, and their use as pharmaceutical compositions.

Abstract: This invention provides compounds of formula I: 1

Abstract: Flourenecarboxylic acid esters of general formula 1 wherein X− and the groups A, R, R1, R2, R3, R3′, R4, and R4′ have the meanings given in the claims and in the specification, processes for the manufacture thereof and the use thereof as medicaments.

Abstract: Crystalline monohydrate of (1&agr;,2&bgr;,4&bgr;,5&agr;,7&bgr;)-7-[(hydroxydi-2-thienylacetyl)oxy]-9,9-dimethyl-3-oxa-9-azoniatricyclo[3.3.1.02,4]nonane bromide (tiotropium bromide monohydrate), processes for the preparation thereof, pharmaceutical compositions thereof, and their use.

Abstract: A compound of formula 1 1

Abstract: A process for preparing a compound of formula 1 from a compound of formula 2 the process comprising reacting in one step the compound of formula 2 with a compound of formula 3 wherein: X− is chlorine, bromine, iodine, methanesulfonate, or trifluoromethanesulfonate; R1 is hydroxy, C1-C4-alkyl, C1-C4-alkoxy, CF3, or fluorine; Ar is phenyl, naphthyl, thienyl, and furyl, each optionally mono- or disubstituted with one or two groups selected from C1-C4-alkyl, C1-C4-alkoxy, hydroxy, fluorine, chlorine, bromine, or CF3; Y− is chlorine, bromine, iodine, methanesulfonate, or trifluoromethanesulfonate; and R is hydroxy, methoxy, ethoxy, O—N-succinimide, O—N-phthalimide, phenyloxy, nitrophenyloxy, fluorophenyloxy, pentafluorophenyloxy, vinyloxy, 2-allyloxy, —S-methyl, —S-ethyl, or —S-phenyl.

Abstract: The invention relates to a new industrially useable process for preparing tropenol, optionally in the form of the acid addition salts thereof.

Abstract: Crystalline monohydrate of (1&agr;,2&bgr;,4&bgr;,5&agr;,7&bgr;)-7-[(hydroxydi-2-thienylacetyl)oxy]-9,9-dimethyl-3-oxa-9-azoniatricyclo[3.3.1.02,4]nonane bromide (tiotropium bromide monohydrate), processes for the preparation thereof, pharmaceutical compositions thereof, and their use.

Abstract: The present invention relates to new anticholinergics of general formula 1: wherein A, X− and the groups R1, R2, R3, R4, R5, R6 and R7 may have the meanings given in the claims and in the specification, processes for preparing them and their use as pharamaceutical compositions.

Abstract: The invention relates to a crystalline micronisate of (1&agr;,2&bgr;,4&bgr;,5&agr;,7&bgr;)-7-[(hydroxydi-2-thienylacetyl)oxy]-9,9-dimethyl-3-oxa-9-azoniatricyclo[3.3.1.02,4]nonane-bromide, processes for preparing it and its use for preparing a pharmaceutical composition, particularly for preparing a pharmaceutical composition with an anticholinergic activity.

Abstract: The invention relates to a new industrially useable process for preparing tropenol, optionally in the form of the acid addition salts thereof.

Abstract: A process for preparing a compound of formula 1 1

Abstract: Difurylglycolic acid esters of the formula 1 1

Abstract: Xanthenecarboxylates of formula 1 1

Abstract: Flourenecarboxylic acid esters of general formula 1 1

Abstract: Crystalline monohydrate of (1&agr;,2&bgr;,4&bgr;,5&agr;,7&bgr;)-7-[(hydroxydi-2-thienylacetyl)oxy]-9,9-dimethyl-3-oxa-9-azoniatricyclo[3.3.1.02,4]nonane bromide (tiotropium bromide monohydrate), processes for the preparation thereof, pharmaceutical compositions thereof, and their use.

Abstract: The invention relates to crystalline anhydrous (1&agr;,2&bgr;,4&bgr;,5&agr;,7&bgr;)-7-[(hydroxydi-2-thienylacetyl)oxy]-9,9-dimethyl-3-oxa-9-azoniatricyclo[3.3.1.022,4]nonane-bromide, processes for preparing it and its use for preparing a pharmaceutical composition, particularly for preparing a pharmaceutical composition with an anticholinergic activity.

Abstract: The invention relates to a new process for preparing a scopine ester useful as an intermediate in preparing (1&agr;,2&bgr;,4&bgr;,5&agr;,7&bgr;)-7-[(hydroxydi-2-thienylacetyl)oxy]-9,9-dimethyl-3-oxa-9-azoniatricyclo[3.3.1.02,4] nonane-bromide.

Abstract: Crystalline monohydrate of (1&agr;,2&bgr;,4&bgr;,5&agr;,7&bgr;)-7-[(hydroxydi-2-thienylacetyl)oxy]-9,9-dimethyl-3-oxa-9-azoniatricyclo[3.3.1.02,4]nonane bromide (tiotropium bromide monohydrate), processes for the preparation thereof, pharmaceutical compositions thereof, and their use.

Abstract: The invention relates to a method for extracting and preparing alkaloids from plants using supercritical fluid extracting technology and alkaloids prepared by said method. Specifically, the invention relates to a method of preparing alkaloids by mixing plants with carbon dioxide as a major solvent and 1 to 20 parts by weight of at least one alkaline cosolvent selected from a group consisting of methanol, ethanol, water or a mixture thereof wherein 2 to 18 (v/v) % of diethylamine or triethylamine is dissolved in the cosolvent based on 100 parts by weight of carbon dioxide at the temperature of 70 to 90° C. and under 4000 to 6000 PSI of pressure in a supercritical extracting apparatus to extract the alkaloid, and then separating, filtering and purifying the alkaloid using the chromatography, and to alkaloids prepared by said method.

Abstract: The invention relates to a new process for preparing (1&agr;,2&bgr;,4&bgr;,5&agr;,7&agr;)-7-[(hydroxydi-2-thienylacetyl)oxy]-9,9-dimethyl-3-oxa-9-azoniatricyclo[3.3.1.02,4]nonane-bromide.

Abstract: A compound of formula 1 1

Abstract: The present invention relates to 8-azabicyclo[3.2.1]oct-2-ene derivatives in their labelled form. Furthermore, the present invention relates to the use of said derivatives in their labelled or unlabelled form in diagnostic methods, in particular for in vivo receptor imaging (neuroimaging).

Abstract: The present invention is particularly directed to the use of a derivative of vinblastine, 3',4'-anhydrovinblastine (AHVB), which differs from vinblastine in that it possesses a double bond at the 3',4' position of the caranthine nucleus rather than the hydroxyl group that is present in the parent structure, as an antineoplastic agent in the therapeutic treatment of cancer. Specifically, the treatment of lymphoma with 3',4'-anhydrovinblastine is disclosed.

Abstract: Methylecgonidine (MEG; anhydroecgonine methylester), is produced when cocaine base ("crack") is heated. MEG alone and in combination with cocaine was tested for action on isolated tracheal rings stimulated to contact with acetylcholine. At micromolar concentrations, cocaine sensitized tracheal rings, increasing both the potency and efficacy of acetylcholine-induced contraction. Surprisingly, MEG, at nanomolar concentrations and above, non-competitively and irreversibly antagonized acetylcholine-induced contraction independently of the actions of cocaine. MEG also displayed antihistaminic activity. Therefore, MEG and anticholinergically active derivatives or analogues thereof are useful in the prevention or treatment of a disease or disorder treatable by an antimuscarinic anticholinergic agent, an anti-histaminic agent or a spasmolytic agent, in particular bronchoconstriction in a number of pulmonary diseases such as asthma.

Abstract: The new compounds of formulaA--O--CO--Z (I)(wherein A and Z are defined as explained in the specification) can be prepared by conventional methods; they are suitable as active substances for pharmaceutical compositions.

Abstract: Compounds of the formula ##STR1## of which, in exemplary compounds, the thienyl group is attached via the 2-position and:(a) A is 3.alpha.-(6.beta., 7.beta.-epoxy)-tropanyl methobromide and R.sub.1 is 2-thienyl;(b) A is 3.alpha.-(6, 7dehydro)-tropanyl methobromide and R.sub.1 is 2-thienyl;(c) A is 3.beta.-tropanyl methobromide and R.sub.1 is 2-thienyl; and,(d) A is 3.alpha.-(N-isopropyl)-nortropanyl methobromide and R.sub.1 is cyclopentyl.These are anticholinergics. Administered by inhalation, they are useful for the treatment of chronic obstructive bronchitis or slight to moderately severe asthma. Administered by the intravenous or oral routes, they are useful for the treatment of vagally induced sinus bradycardia.

Abstract: Methylecgonidine (MEG; anhydroecgonine methylester), is produced when cocaine base ("crack") is heated. MEG alone and in combination with cocaine was tested for action on isolated tracheal rings stimulated to contact with acetylcholine. At micromolar concentrations, cocaine sensitized tracheal rings, increasing both the potency and efficacy of acetylcholine-induced contraction. Surprisingly, MEG, at nanomolar concentrations and above, non-competitively and irreversibly antagonized acetylcholine-induced contraction independently of the actions of cocaine. MEG also displayed antihistaminic activity. Therefore, MEG and anticholinergically active derivatives or analogues thereof are useful in the prevention or treatment of a disease or disorder treatable by an antimuscarinic anticholinergic agent, an anti-histaminic agent or a spasmolytic agent, in particular bronchoconstriction in a number of pulmonary diseases such as asthma.

Abstract: Compounds of the formula of which, in exemplary compounds, the thienyl group is attached via the 2-position and; (a) A is 3?-(6?, 7?-epoxy)-tropanyl methobromide and R1 is 2-thienyl; (b) A is 3?-(6, 7dehydro)-tropanyl methobromide and R1 is 2-thienyl; (c) A is 3?-tropanyl methobromide and R1 is 2-thienyl; and, (d) A is 3?-(N-isopropyl)-nortropanyl methobromide and R1 is cyclopentyl. There are anticholinergics. Administered by inhalation, they are useful for the treatment of chronic obstructive bronchitis or slight to moderately severe asthma. Administered by the intravenous or oral routes, they are useful for the treatment of vagally induced sinus bradycardia.