Abstract: Intermediate compounds are described herein and which are used to manufacture a crystalline compound 1-cyano-2-(4-cyclopropyl-benzyl)-4-(?-D-glucopyranos-1-yl)-benzene L-proline monohydrate.

Abstract: Intermediate compounds are described herein and which are used to manufacture a crystalline compound 1-cyano-2-(4-cyclopropyl-benzyl)-4-(?-D-glucopyranos-1-yl)-benzene L-proline monohydrate.

Abstract: The invention relates to a process for the manufacture of the crystalline compound according to formula (I) comprising the steps (a) deacetylating the final intermediate (FI), (b) forming the crystalline compound according to formula (I) by reacting the deacetylated final intermediate of step (a) with L-proline and water and isolating the final reaction product; processes of manufacturing intermediates thereof; process intermediates and their uses in the processes according to the present invention.

Abstract: The invention relates to a process for the manufacture of the crystalline compound according to formula (I) comprising the steps (a) deacetylating the final intermediate (FI), (b) forming the crystalline compound according to formula (I) by reacting the deacetylated final intermediate of step (a) with L-proline and water and isolating the final reaction product; processes of manufacturing intermediates thereof; process intermediates and their uses in the processes according to the present invention.

Abstract: The invention relates to novel liquid pharmaceutical compositions comprising (8?)-8-[(methylthio)methyl]-6-propylergoline (pergolide) as well as corresponding processes of manufacturing such liquid pharmaceutical compositions and their medical uses.

Abstract: This invention relates to a process for the hydrogenation of a ketooxime to selectively form an aminoalcohol stereoisomer, and, in particular, to a process for the hydrogenation of 4,5-dihydro-imidazo[4,5,1-jk][1]benzazepin-2,6,7[1H]-trione-6-oxime or a salt thereof to selectively form a stereoisomer of 6-amino-7-hydroxy-4,5,6,7-tetrahydro-imidazo[4,5,1-jk][1]-benzazepin-2[1H]-one or a salt thereof. This invention also relates to the use of the 6-amino-7-hydroxy-4,5,6,7-tetrahydro-imidazo[4,5,1-jk][1]-benzazepin-2[1H]-one hydrogenation product or a salt thereof to selectively make a stereoisomer of zilpaterol or a salt thereof, as well as the use of such a zilpaterol stereoisomer or salt in methods of treatment and medicaments for animals.

Abstract: Polymorphs of 3-chloro-4[(2R)-2-(4-chlorophenyl)-4-[(1R)-1-(4-cyanophenyl)ethyl]-1-piperazinyl]-benzonitrile are disclosed, as well as pharmaceutical compositions comprising said polymorphs, methods of using the polymorphs, and a process for preparing them.

Abstract: This invention relates to a method for making macrolides, and, in particular, a method for making optionally substituted 20,23-dipiperidinyl-5-O-mycaminosyl-tylonolide and derivatives thereof, as well as uses of macrolides to make medicaments, methods of treatment using macrolides, and methods for making intermediates that, inter alia, may be used to make macrolides. This invention also relates to solvated and non-solvated crystalline forms of 20,23-dipiperidinyl-5-O-mycaminosyl-tylonolide, as well as methods for making such crystalline forms, medicaments comprising (or derived from) such crystalline forms, methods for making medicaments comprising (or derived from) such crystalline forms, methods of treatment using such crystalline forms, and kits comprising such crystalline forms.

Abstract: This invention relates to a method for making macrolides, and, in particular, a method for making optionally substituted 20,23-dipiperidinyl-5-O-mycaminosyl-tylonolide and derivatives thereof, as well as uses of macrolides to make medicaments, methods of treatment using macrolides, and methods for making intermediates that, inter alia, may be used to make macrolides. This invention also relates to solvated and non-solvated crystalline forms of 20,23-dipiperidinyl-5-O-mycaminosyl-tylonolide, as well as methods for making such crystalline forms, medicaments comprising (or derived from) such crystalline forms, methods for making medicaments comprising (or derived from) such crystalline forms, methods of treatment using such crystalline forms, and kits comprising such crystalline forms.

Abstract: This invention relates to a process for the hydrogenation of a ketooxime to selectively form an aminoalcohol stereoisomer, and, in particular, to a process for the hydrogenation of 4,5-dihydro-imidazo[4,5,1-jk][1]benzazepin-2,6,7[1H]-trione-6-oxime or a salt thereof to selectively form a stereoisomer of 6-amino-7-hydroxy-4,5,6, 7-tetrahydro-imidazo[4,5,1-jk][1]-benzazepin-2[1H]-one or a salt thereof. This invention also relates to the use of the 6-amino-7-hydroxy-4,5,6,7-tetrahydro-imidazo[4,5,1-jk][1]-benzazepin-2[1H]-one hydrogenation product or a salt thereof to selectively make a stereoisomer of zilpaterol or a salt thereof, as well as the use of such a zilpaterol stereoisomer or salt in methods of treatment and medicaments for animals.

Abstract: The invention relates to a process for the preparation of pyridylcarboxylic amides and esters I, Formula (I) wherein Hal, X and R1 have the meanings given in claim 1, which comprises the following steps: (a) heating a mixture consisting essentially of trichloromethylpyridine II, Formula (II), wherein Hal has the meaning given, and 1.0 to 1.5 equivalents of concentrated sulfuric acid, characterized in that the trichloromethylpyridine II in a liquid form is added to the concentrated sulfuric acid at a temperature from 110° C. to 160° C.; and (b) reacting the intermediate product obtained in step (a) with an amine or alcohol III, HXR1, wherein X and R1 have the meaning given, optionally in the presence of a solvent and/or a base.

Abstract: This invention relates to a method for making macrolides, and, in particular, a method for making optionally substituted 20,23-dipiperidinyl-5-O-mycaminosyl-tylonolide and derivatives thereof, as well as uses of macrolides to make medicaments, methods of treatment using macrolides, and methods for making intermediates that, inter alia, may be used to make macrolides. This invention also relates to solvated and non-solvated crystalline forms of 20,23-dipiperidinyl-5-O-mycaminosyl-tylonolide, as well as methods for making such crystalline forms, medicaments comprising (or derived from) such crystalline forms, methods for making medicaments comprising (or derived from) such crystalline forms, methods of treatment using such crystalline forms, and kits comprising such crystalline forms.

Abstract: The invention relates to a process for the preparation of pyridylcarboxylic amides and esters I, Formula (I) wherein Hal, X and R1 have the meanings given in claim 1, which comprises the following steps: (a) heating a mixture consisting essentially of trichloromethylpyridine II, Formula (II), wherein Hal has the meaning given, and 1.0 to 1.5 equivalents of concentrated sulfuric acid, characterized in that the trichloromethylpyridine II in a liquid form is added to the concentrated sulfuric acid at a temperature from 110° C. to 160° C.; and (b) reacting the intermediate product obtained in step (a) with an amine or alcohol III, HXR1, wherein X and R1 have the meaning given, optionally in the presence of a solvent and/or a base.

Abstract: The invention relates to a process for the preparation of hetero)aryloxyheteroarylcarboxylic amide or ester of formula VI wherein A1, A2, A3, A4, A5 Hal, X, R1, and R4 are defined within, which process comprises preparing the heteroarylcarboxylic amide or ester of formula I or a salt thereof,  from a trichoromethyl-heteroaromatic compound of formula II and reacting the compound of formula I with an aromatic or heteroaromatic hydroxyl compound of formula VII, R4—OH  VII optionally in the presence of a base.

Abstract: The invention relates to a process for the preparation of heteroarylcarboxylic amides and esters of formula I ##STR1## in which one or two of the groups A.sup.1, A.sup.2, A.sup.3, A.sup.4, and A.sup.5 represent a nitrogen atom and the other groups each independently represent CR.sup.3,Hal represent s a halogen atom,X represents oxygen or NR.sup.2,R.sup.1 represents an optionally substituted alkyl, aryl, heteroaryl or cycloalkyl group,R.sup.2 represents a hydrogen atom or an alkyl group, orR.sup.1 and R.sup.2 together with the interjacent ring form a heterocyclic group, andR.sup.3 each independently represent a hydrogen atom or an alkyl group,which comprises heating a mixture of a compound of formula II, ##STR2## and concentrated sulfuric acid, and reacting the resulting intermediate with in alcohol or amine of formula IIIHXR.sup.1 III.

Abstract: An effective and efficient process for the preparation of chloro-benzoylchlorides of formula I, ##STR1## (n is defined in the specification). In this process a a chloro-trichloromethylbenzene of formula II ##STR2## is treated with water acid in the presence of a Lewis at temperatures below 80.degree. C. The compounds obtained according to this process can be used to prepare certain chloro-substituted benzophenones.

Abstract: An effective and efficient process for the preparation of chloro-benzoylchlorides of formula I, ##STR1## (n is defined in the specification). In this process a a chloro-trichloromethylbenzene of formula II ##STR2## is treated with water acid in the presence of a Lewis at temperatures below 80.degree. C. The compounds obtained according to this process can be used to prepare certain chloro-substituted benzophenones.