公开(公告)号：EP0805810A1

公开(公告)日：1997-11-12

申请号：EP96901309.0

申请日：1996-01-19

Applicant: SCHERING AKTIENGESELLSCHAFT

Inventor： SKUBALLA, Werner ,  BUCHMANN, Bernd ,  REHWINKEL, Hartmut ,  SCHNEIDER, Frank ,  FRÖHLICH, Wolfgang ,  GIESEN, Claudia ,  HENNEKES, Hartwig

IPC: A61K31 ,  C07D471 ,  C07D491

CPC classification number: C07D471/04

Abstract: Novel 9H-pyrido[3,4-b]indol derivatives of general formula (I), in which U, V and W are a carbon-carbon bond or a C1-C6 alkylene group, R1 is a hydrogen atom, a hydroxy group or a carboxyl group and R2 is a hydrogen atom, a hydroxy group, a C1-C4 alkoxy group, a C1-C6 alkanoyloxy group or a C1-C4-φ carboxyl alkoxy group, or R1 and R2 together are an oxycarbonyl group and in which X is a carbon-carbon bond or oxygen, Y is a carbon-carbon bond, the group -CONR'- with R' as a hydrogen atom or a C1-C7 alkyl group possibly substituted by a carboxyl group, or the grouping (a) where m and n are figures of a total of 3,4 or 5 and Z is a methylidine or an aza group, and R3 and R4 are a naphthyl group possibly substituted by halogen atoms, trifluoromethyl groups, a C1-C7 alkyl C1-C4 alkoxy group or carboxyl groups and, in the case of the carboxylic acids of general formula (I), their esters of physiologically acceptable alcohols, their amides of physiologically acceptable amines and their salts of physiologically acceptable bases with anti-leucotriene B4 action are described.

公开(公告)号：EP1456224B1

公开(公告)日：2006-02-08

申请号：EP02793067.6

申请日：2002-12-18

Applicant: Schering Aktiengesellschaft

Inventor： GEISLER, Jens ,  SCHNEIDER, Frank ,  LOVIS, Kai ,  LOPEZ HOLGUIN, Fernando

IPC: C01B21/093 ,  C07J41/00 ,  C07C303/34 ,  C07C307/02

CPC classification number: C01B21/096 ,  C07C303/34 ,  C07J41/0072 ,  C07C307/02

Abstract: This invention describes a safe method for the production of sulfamoyl chloride from chlorosulfonyl isocyanate and formic acid in the presence of a amide catalyst, taming the hazardous nature of this reaction by circumventing heat accumulation processes, as well as the sulfamoylation of alcohols and phenols with the resulting sulfamoyl chloride in N,N-dimethyl acetamide or N-methyl pyrrolidone thereby avoiding the formation of side-products which were inevitable with the methods of the prior art using dimethyl formamide or dichloromethane as a solvent. The current invention allows industrial scale applications and describes as an example the process of manufacture of the biologically active compound 17β-Hydroxyestra-1,3,5(10)-triene-3-yl sulfamate.

公开(公告)号：EP1456224A2

公开(公告)日：2004-09-15

申请号：EP02793067.6

申请日：2002-12-18

Applicant: Schering Aktiengesellschaft

Inventor： GEISLER, Jens ,  SCHNEIDER, Frank ,  LOVIS, Kai ,  LOPEZ HOLGUIN, Fernando

IPC: C07J41/00 ,  C07C303/34 ,  C07C307/02

CPC classification number: C01B21/096 ,  C07C303/34 ,  C07J41/0072 ,  C07C307/02

Abstract: This invention describes a safe method for the production of sulfamoyl chloride from chlorosulfonyl isocyanate and formic acid in the presence of a amide catalyst, taming the hazardous nature of this reaction by circumventing heat accumulation processes, as well as the sulfamoylation of alcohols and phenols with the resulting sulfamoyl chloride in N,N-dimethyl acetamide or N-methyl pyrrolidone thereby avoiding the formation of side-products which were inevitable with the methods of the prior art using dimethyl formamide or dichloromethane as a solvent. The current invention allows industrial scale applications and describes as an example the process of manufacture of the biologically active compound 17β-Hydroxyestra-1,3,5(10)-triene-3-yl sulfamate.