Abstract: Bicyclic heterocycles of general formula wherein: Ra to Rd, A to C and X are as defined herein, the tautomers, the stereoisomers and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable pharmacological properties, particularly an inhibitory effect on signal transduction mediated by tyrosine kinases, the use thereof for treating diseases, particularly tumoral diseases, diseases of the lungs and respiratory tract, and the preparation thereof.

Abstract: Disclosed are novel 2-(5-halopyridyl) and 2-(5-halopyrimidinyl) magnesium halides, processes of making and their use in the efficient synthesis in their respective 5-halo-2-substituted pyridines and pyrimidines.

Abstract: A process for preparing tropenol (I) or an acid addition salt thereof, the process comprising: (a) reducing a scopine ester of formula (II)  wherein R is C1-C4-alkyl or C1-C4-alkylene-phenyl, each optionally substituted by hydroxy or C1-C4-alkoxy, or an acid addition salt or hydrate thereof, using zinc in a suitable solvent in the presence of an activating metal salt; and (b) saponifying the product of (a) using a suitable base to obtain the tropenol of formula (I) or the acid addition salt thereof.

Abstract: This invention relates to the use of specifically attenuated live BVD (bovine viral diarrhea) viruses for the preparation of a vaccine for use in the prevention and/or treatment of BVDV infections in breeding stocks of cattle, pregnant cows and for fetal protection in pregnant cows.

Abstract: A compound of formula I or of formula II wherein: R1 is F, Cl, Br, CH2F, CF2H, or CF3; R2 is NR6R7, where R6 is Me, Et, Pr, or iPr, and R7 is Me, Et or Pr; and R3, R4, and R5 independently of one another each are H, Me, F, Cl, Br, CH2F, CF2H, or CF3, and if R4 is Me, F, Cl, Br, CH2F, CF2H, or CF3, then R1 is additionally H or Me, or a pharmacologically acceptable salt thereof. In addition, pharmaceutical compositions comprising an effective amount of these compounds, methods for the treatment or prophylaxis of urinary incontinence and diseases of the bladder using these compounds, and methods for making these compounds are disclosed.

Abstract: Compound of formula (I) wherein: R1 is hydrogen or C1-C6-alkyl optionally substituted by C3-C6-cycloylalkyl; R2 and R3 together with the nitrogen form a saturated or unsaturated 5- or 6-membered heterocyclic ring optionally containing nitrogen or oxygen as an additional heteroatom, wherein the heterocyclic ring thereof is substituted by a group selected from phenyl, benzyl, and diphenylmethyl, each optionally mono- or di-substituted by one or two groups selected from CF3, C1-C4-alkyl, C1-C4-alkoxy, phenyl, benzyl, halogen, and OH, or R2 and R3 together with the nitrogen form a saturated or unsaturated 5- or 6-membered heterocyclic ring optionally containing nitrogen or oxygen as an additional heteroatom, the heterocyclic ring thereof linked via a single bond, a methylene-bridge, or spiro-connected to another saturated or unsaturated heterocyclic group containing one or two heteroatoms selected from oxygen and nitrogen, the heterocyclic group being optionally mono- or di-substituted by a g

Abstract: Disclosed are novel processes and novel intermediate compounds for preparing aryl- and heteroaryl-substituted urea compounds of the formula (I) wherein Ar1, Ar2, L, Q and X are described herein. The product compounds are useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases.

Abstract: Methods of lowering the levels of A&bgr;40, A&bgr;42 and tau protein in a mammal comprising administering to the mammal an effective amount of talsaclidine, or a physiologically acceptable acid addition salt thereof, and methods of treating diseases associated with the formation of diffuse and senile plaques or A&bgr;40-, A&bgr;42- and tau-containing plaques are disclosed.

Abstract: A formulation comprising, and process for preparing, improved oral dosage forms of 1-(5-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl)-3-[4-(2-morpholin-4-yl-ethoxy)-naphthalen-1-yl]-urea, a chemical entity with anti-inflammatory properties. Granulation of 1-(5-tert-but l-2-p-tolyl-2H-pyrazol-3-yl)-3-[4-(2-morpholin-4-yl-ethoxy)-naphthalen-1-yl]-urea within specified ranges provides improved dissolution of 1-(5-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl)-3-[4-(2-morpholin-4-yl-ethoxy)-naphthalen-1-yl]-urea and oral bioavailability, as well as content uniformity. Incorporation into the formulation of an aqueous soluble inclusion compound capable of forming a complex with 1-(5-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl)-3-[4-(2-morpholin-4-yl-ethoxy)-naphthalen-1-yl]-urea, such as beta-cyclodextrin provides enhanced stability of 1-(5-tert-butyl-2-p-tolyl-2H-pyrazol-3-yl)-3-[4-(2-morpholin-4-yl-ethoxy)-naphthalen-1-yl]-urea, in particular in highly ionic environments.

Abstract: A compound of formula (I) wherein: R1 is C1-C6-alkyl substituted by a group selected from OH, C1-C6-alkoxy, —OCONHC1-C6-alkyl, —OCONHC1-C6-alkyl, —NHSO2C1-C6-alkyl, and —NHCOC1-C6-alkyl, or R1 is C1-C6-alkyl substituted by a saturated or unsaturated 5- or 6-membered heterocycle containing one or two heteroatoms selected from the group consisting of nitrogen and oxygen, the heterocycle optionally substituted by a group selected from C1-C4-alkyl, halogen, and benzyl; R2 and R3 together with the nitrogen form a saturated or unsaturated 5- or 6-membered heterocyclic ring optionally containing nitrogen or oxygen as an additional heteroatom, the heterocyclic ring thereof substituted by a group selected from phenyl, benzyl, and diphenylmethyl, each of these groups optionally mono- or di-substituted by one or two groups selected from CF3, C1-C4-alkyl, C1-C4-alkoxy, phenyl, benzyl, halogen, and OH, or R2 and R3 together with the nitrogen form a saturated or unsaturated 5-

Abstract: A method for treating menopausal hot flushes using CGRP antagonists and/or CGRP release inhibitors and the corresponding pharmaceutical compositions containing as active substance one or more CGRP antagonists and/or CGRP release inhibitors, and the preparation thereof.

Abstract: Compounds of general formula (I) wherein: A is —CH2—, —CH2—CH2—, —CH2—CH2—CH2—, —CH2—CH2—CH2—CH2—, —CH2—CO—, —CH2—CH2—CO—, or —CH═CH—CO—; Het is piperidinyl, piperazinyl, or dihydrobenzimidazolonyl; R1 is hydrogen or halogen; R2 is hydrogen, C1-C4-alkyl, CF3, or a phenyl group optionally substituted by halogen, C1-C4-alkyl, or C1-C4-alkyloxy; and R3 is hydrogen, C1-C4-alkyl, HO—C1-C4-alkyl, or C2-C4-alkenyl; or a group selected from phenyl, benzyl, and phenylethyl, each optionally substituted by halogen, CF3, C1-C4-alkyl, or C1-C4-alkyloxy; or a heterocycle selected from among morpholine, piperidine, piperazine, and dihydrobenzimidazolone, the heterocycle either linked directly or via a C1-C4-alkylene bridge, or an optical isomer, enantiomer, tautomer, free base, or pharmacologically acceptable acid addition salt thereof; methods of

Abstract: A process for the production of a container (1) comprising an outer container (2), an inner bag (3) disposed therein and a pressure equalisation opening (10) disposed in the outer container (2), and also a container (1) produced according to this process, is described, wherein firstly a pre-moulding, comprising two coaxial tubes, is first produced by co-extrusion with the help of a blow mould and with an outwardly-projecting base seam (5) being formed. The process is to form a pressure equalisation opening (10) in the outer container (2) of the container (1) without endangering the integrity of the container (1), wherein a lower wastage rate and higher productivity are to be achieved. This is attained by a process wherein the base seam (5) is partially cut off and a force which acts in the direction of the seam is introduced into the pre-moulding, which still has a temperature of 40° C. to 70°C.

Abstract: The invention relates to new arylglycinamide derivatives of general formula I and the pharmaceutically acceptable salts thereof, wherein R1 and R2 together with the N to which they are bound form a ring of the formula in which R3, R4, R5, Ar, R6, R7, R8, R9, R10, R11, r, s and t have the meanings given in the specification and the preparation and use thereof. The new compounds are valuable neurokinin (tachykinin) antagonists.

Abstract: A process for dynamically separating the enantiomers of a piperidone derivative of formula (1) wherein: R1 is aryl optionally mono- to polysubstituted, heteroaryl, which is linked to the chiral center via at least one carbon atom of its own or a carbon atom belonging to the methylene bridge, or straight-chain or branched C1-C8-alkyl optionally mono- to polysubstituted by halogen; R2 and R3, which are identical or different, are each straight-chain or branched C1-C6-alkyl; and n is 0, 1, 2 or 3, the process comprising: (a) dissolving an optically active acid and optionally catalytic amounts of a sulfonic acid in a solvent to make a first solution maintained at a desired temperature; (b) adding a second solution of the piperidone derivative to the first solution to precipitate out the desired enantiomer of the piperidone derivative as a salt of the optically active acid used while racemizing the unwanted enantiomer of the piperidone derivative in solution and further precipitating the de

Abstract: A method for treating a neurodegenerative disease or cerebral ischemia arising from conditions selected from the group consisting of Status epilepticus, hypoglycaemia, hypoxia, anoxia, brain trauma, brain oedema, amyotropic lateral sclerosis, Huntington's disease, Alzheimer's disease, hypotonia, cardiac infarction, brain pressure (elevated intracranial pressure), ischaemic and haemorrhagic stroke, global cerebral ischaemia with heart stoppage, diabetic polyneuropathy, tinnitus, perinatal asphyxia, psychosis, schizophrenia, depression, and Parkinson's disease, the method of treatment comprising administering to a host in need of such treatment a therapeutic amount of a compound of formula (I) wherein R1, R2, R3, R4, R5, R6, and R7 are as defined herein, or a pharmaceutically acceptable salt thereof, and pharmaceutical compositions containing a compound of formula (I).

Abstract: A process for purifying 20(S)-camptothecin, the process comprising: (a) combining an aqueous base and a starting material containing 20(S)-camptothecin to convert the lactone ring of the 20(S)-camptothecin into a carboxylate salt; (b) hydrogenating to the product of step (a) in the presence of a transition metal catalyst; (c) acidifying the aqueous phase of the product of step (b) to form 20(S)-camptothecin crystals; (d) adding at least one polar aprotic solvent to the product of step (c); and (e) separating off the purified 20(S)-camptothecin crystals.

Abstract: New disubstituted bicyclic heterocycles of general formula Ra—A—Het—B—Ar—E  (I) Compounds of the above general formula I, wherein E denotes an RbNH—C(═NH)— group, have valuable pharmacological properties, particularly a thrombin-inhibiting effect and the effect of prolonging thrombin time, and those wherein E denotes a cyano group, are valuable intermediates for preparing the other compounds of general formula I.

Abstract: Compounds of general formula I wherein X is a single bond, —O—, C-C4-alkylene, or an alkylene bridge having 1 to 8 carbon atoms which may be branched or unbranched and optionally have one or two oxygen atom(s) anywhere in the bridge; R1 is hydrogen, methyl, ethyl, or phenyl; R2 is hydrogen or methyl; R3 is hydrogen, fluorine, chlorine, bromine, hydroxy, methyl, or methoxy; R4 is hydrogen, methyl, or ethyl; R5 is hydrogen, methyl, or ethyl; R6 is hydrogen, methyl, or ethyl; R7 is tert-butyl, cyclohexyl, phenyl optionally substituted by R9 and R10, which may be identical or different, or; R8 is hydrogen or C1-C4-alkyl; Z is oxygen, NH, or sulfur; R9 is hydrogen, methyl, fluorine, chlorine, bromine, or methoxy; R10 is hydrogen, methyl, fluorine, chlorine, bromine, or methoxy; optionally in the form of the individual optical isomers, mixtures of the individual enantiomers or racemates as well as in the form of the free bases or the corresponding acid addition salts

Abstract: The present invention relates to new medicament compositions based on anticholinergic compounds, which have a long-lasting effect, and &bgr;-mimetics, which have a long-lasting effect, processes for their production and their use in the therapy of respiratory ailments.