Abstract: The present invention relates to new salts and crystalline salt forms of an indolinone derivative which have valuable pharmacological properties, to a process for their manufacture, to pharmaceutical formulations containing them and to their use as medicament.

Abstract: Disclosed are hydrates and polymorphs of 4-[[(7R)-8-cyclopentyl-7-ethyl-5,6,7,8-tetrahydro-5-methyl-6-oxo-2-pteridinyl]amino]-3-methoxy-N-(1-methyl-4-piperidinyl)-benzamide, processes for preparing them and their use as pharmaceutical compositions.

Abstract: The present invention encompasses a process for preparing compounds of formula (1), wherein a compound of general formula (2) is reacted in the presence of a catalyst and a solvent under hydrogen pressure to form a compound of general formula (1) and wherein A and R1-R4 are defined as in claim 1.

Abstract: The present invention relates to indolinone derivatives substituted in the 6 position of general formula wherein R1 to R6 and X are defined as in claim 1, the tautomers, enantiomers, diastereomers, mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof, which have valuable pharmacological properties, in particular an inhibiting effect on various receptor tyrosine kinases and on the proliferation of endothelial cells and various tumour cells, pharmaceutical compositions containing these compounds, their use and processes for preparing them.

Abstract: 4-[4-(2-pyrrolylcarbonyl)-1-piperazinyl]-3-trifluoromethylbenzoylguanidine hydrochloride and its hydrates, processes for preparing this benzoylguanidine salt and its hydrates, pharmaceutical compositions containing this benzoylguanidine salt and its hydrates, and its use in treating diseases, particularly those in which inhibition of the cellular Na+/H+ exchange is of therapeutic benefit.

Abstract: A process for making a compound of formula 1 or a salt thereof, wherein: R1 and R2 are each independently H, halogen, or C1-4-alkyl, or R1 and R2 together are C1-6-alkylene; and R3 is H, halogen, OH, C1-4-alkyl, or O—C1-4-alkyl, the process comprising: (a) reacting a compound of formula 6 wherein R4 is benzyl, diphenylmethyl, or trityl, each optionally substituted at, if available, an aryl group or an aliphatic carbon atom, with a compound of formula 7 or a salt thereof, to obtain a compound of formula 5, or a salt thereof (b) reducing the nitro group of the compound of formula 5 to an amine group and mesylating this amine group and cleaving the protecting group during the reduction step or after the mesylation step to obtain the compound of formula 1.

Abstract: Crystalline forms of the compounds (R)-2-(4-amidinophenylaminomethyl)-1-methyl-5-[1-(carboxymethylamino)-1-(pyrrolidinocarbonyl)-ethyl]-benzimidazole and the monohydrochloride thereof, processes for the preparation thereof and the use thereof as pharmaceutical compositions.

Abstract: The present invention relates to a process for preparing compounds of general formula I wherein R1 and R2 are defined as in claim 1, the pharmaceutically acceptable salts and the solvates thereof, which may be prepared starting from compounds of general formula II wherein R1 is defined as in claim 1.

Abstract: 4-[4-(2-pyrrolylcarbonyl)-1-piperazinyl]-3-trifluoromethylbenzoylguanidine hydrochloride and its hydrates, processes for preparing this benzoylguanidine salt and its hydrates, pharmaceutical compositions containing this benzoylguanidine salt and its hydrates, and its use in treating diseases, particularly those in which inhibition of the cellular Na+/H+ exchange is of therapeutic benefit.

Abstract: Crystalline forms of the compounds (R)-2-(4-amidinophenylaminomethyl)-1-methyl-5-[1-(carboxymethylamino)-1-(pyrrolidinocarbonyl)-ethyl]-benzimidazole and the monohydrochloride thereof, processes for the preparation thereof and the use thereof as pharmaceutical compositions.

Abstract: 4-[4-(2-pyrrolylcarbonyl)-1-piperazinyl]-3-trifluoromethylbenzoylguanidine hydrochloride and its hydrates, processes for preparing this benzoylguanidine salt and its hydrates, pharmaceutical compositions containing this benzoylguanidine salt and its hydrates, and its use in treating diseases, particularly those in which inhibition of the cellular Na+/H+exchange is of therapeutic benefit.

Abstract: A process for making a compound of formula 1 or a salt thereof, wherein: R1 and R2 are each independently H, halogen, or C1-4-alkyl, or R1 and R2 together are C1-6-alkylene; and R3 is H, halogen, OH, C1-4-alkyl, or O—C1-4-alkyl, the process comprising: (a) reacting a compound of formula 6 wherein R4 is benzyl, diphenylmethyl, or trityl, each optionally substituted at, if available, an aryl group or an aliphatic carbon atom, with a compound of formula 7 or a salt thereof, to obtain a compound of formula 5, or a salt thereof (b) reducing the nitro group of the compound of formula 5 to an amine group and mesylating this amine group and cleaving the protecting group during the reduction step or after the mesylation step to obtain the compound of formula 1.

Abstract: Crystalline forms of the compounds (R)-2-(4-amidinophenylaminomethyl)-1-methyl-5-[1 -(carboxymethylamino)-1-(pyrrolidinocarbonyl)-ethyl]-benzimidazole and the monohydrochloride thereof, processes for the preparation thereof and the use thereof as pharmaceutical compositions.

Abstract: The present invention relates to a process for preparing betamimetics of formula 1, wherein n denotes 1 or 2; R1 denotes hydrogen, halogen, C1-4-alkyl or O—C1-4-alkyl; R2 denotes hydrogen, halogen, C1-4-alkyl or O—C1-4-alkyl; R3 denotes hydrogen, C1-4-alkyl, OH, halogen, O—C1-4-alkyl, O—C1-4-alkylene-COOH, O—C1-4-alkylene-COO—C1-4-alkyl.

Abstract: An improved process for preparing 4-[(3-chloro-4-fluorophenyl)amino]-6-{[4-(N,N-dimethylamino)-1-oxo-2-buten-1-yl]amino}-7-((S)-tetrahydrofuran-3-yloxy)-quinazoline and related aminocrotonyl compounds and the preparation of a suitable salt of 4-[(3-chloro-4-fluorophenyl)amino]-6-{[4-(N,N-dimethylamino)-1-oxo-2-buten-1-yl]amino}-7-((S)-tetrahydrofuran-3-yloxy)-quinazoline for use as a pharmaceutically active substance.

Abstract: Crystalline forms of the compounds (R)-2-(4-amidinophenylaminomethyl)-1-methyl-5-[1-(carboxymethylamino)-1-(pyrrolidinocarbonyl)-ethyl]-benzimidazole and the monohydrochloride thereof, processes for the preparation thereof and the use thereof as pharmaceutical compositions.

Abstract: The present invention relates to a process for preparing the compound 3-(4-piperidinyl)-2,3,4,5-tetrahydro-1,3-benzodiazepin-2(1H)-one of formula which is to be found as a structural element in CGRP-antagonists, which are particularly suitable for the oral treatment of migraine.

Abstract: The present invention relates to the compound 3-Z-[1-(4-(N-((4-methyl-piperazin-1-yl)-methylcarbonyl)-N-methyl-amino)-anilino)-1-phenyl-methylene]-6-methoxycarbonyl-2-indolinone-monoethanesulphonate of formula I and the use thereof as a pharmaceutical composition.

Abstract: The present invention relates to the compound 3-Z-[1-(4-(N-((4-methyl-piperazin-1-yl)-methylcarbonyl)-N-methyl-amino)-anilino)-1-phenyl-methylene]-6-methoxycabonyl-2-indolinone-monoethanesulphonate of formula I and the use thereof as a pharmaceutical composition

Abstract: 4-[4-(2-pyrrolylcarbonyl)-1-piperazinyl]-3-trifluoromethylbenzoylguanidine hydrochloride and its hydrates, processes for preparing this benzoylguanidine salt and its hydrates, pharmaceutical compositions containing this benzoylguanidine salt and its hydrates, and its use in treating diseases, particularly those in which inhibition of the cellular Na+/H+ exchange is of therapeutic benefit.