公开(公告)号：EP1615924A1

公开(公告)日：2006-01-18

申请号：EP04727566.4

申请日：2004-04-15

申请人： Synthon B.V.

发明人： GIELING, Reinerus, Gerardus ,  LAURANT, Désirée

IPC分类号： C07D471/04 ,  A61K31/505 ,  A61P25/00

CPC分类号： C07D471/04

摘要： The invention relates to a salt of risperidone in solid state having a water solubility of at least 10 mg/ml, to risperidone dihydrochloride, risperidone hydrogenmaleate, risperidone hernitartrate and risperidone (L)-hemimalate, to a process for making a solid state water soluble salt of risperidone, which comprises: contacting a risperidone donor with a suitable acid in an organic solvent to form a water soluble risperidone salt; and precipitating said risperidone salt from said solvent, and to the use for treating psychotic disorders in a mammal.

公开(公告)号：EP2981537B1

公开(公告)日：2017-05-10

申请号：EP13861489.6

申请日：2013-03-14

申请人： Synthon B.V.

发明人： GIELING, Reinerus, Gerardus ,  LINDEN VAN DER, Johannes, Bastiaan ,  VERKERK, Pascal, Renart ,  MELSA, Petr

IPC分类号： C07D487/04 ,  C07C279/14 ,  C07C279/18

CPC分类号： C07C279/14 ,  C07C279/18 ,  C07D487/04

公开(公告)号：EP1740545B1

公开(公告)日：2010-03-24

申请号：EP05735077.9

申请日：2005-04-14

申请人： Synthon B.V.

发明人： OVEREEM, Arjanne ,  GIELING, Reinerus, Gerardus ,  ZHU, Jie ,  LAMBERTUS, Thijs

IPC分类号： C07D215/18 ,  C07C67/00

CPC分类号： C07D215/18

摘要： A process for making montelukast, a pharmaceutically useful compound of the following formula and salts thereof: formula (1), using a compound of formula (20) and a compound of formula (5) is provided.

公开(公告)号：EP1740545A1

公开(公告)日：2007-01-10

申请号：EP05735077.9

申请日：2005-04-14

申请人： Synthon B.V.

发明人： OVEREEM, Arjanne ,  GIELING, Reinerus, Gerardus ,  ZHU, Jie ,  LAMBERTUS, Thijs

IPC分类号： C07D215/18 ,  C07C67/00

CPC分类号： C07D215/18

摘要： A process for making montelukast, a pharmaceutically useful compound of the following formula and salts thereof: formula (1), using a compound of formula (20) and a compound of formula (5) is provided.

公开(公告)号：EP2981537A1

公开(公告)日：2016-02-10

申请号：EP13861489.6

申请日：2013-03-14

申请人： Synthon B.V.

发明人： GIELING, Reinerus, Gerardus ,  LINDEN VAN DER, Johannes, Bastiaan ,  VERKERK, Pascal, Renart ,  MELSA, Petr

IPC分类号： C07D487/04 ,  C07C279/14 ,  C07C279/18

CPC分类号： C07C279/14 ,  C07C279/18 ,  C07D487/04

摘要： The present invention relates to an improved process for making anagrelide of formula (1), or an acid addition salt thereof, including any hydrated or solvated form thereof, comprising reacting a compound of formula (3), or an acid addition salt thereof, (3), wherein R is a C1-C4 alkyl group, with chloroformamidine hydrochloride of formula (8), in an inert solvent, followed by treatment of the reaction mixture with a base.

公开(公告)号：EP1740546A2

公开(公告)日：2007-01-10

申请号：EP05759120.8

申请日：2005-04-14

申请人： Synthon B.V.

发明人： OVEREEM, Arjanne ,  GIELING, Reinerus, Gerardus ,  ZHU, Jie ,  THIJS, Lambertus

IPC分类号： C07D215/18 ,  C07C67/00

CPC分类号： C07C303/28 ,  C07C67/08 ,  C07C67/39 ,  C07C319/02 ,  C07C2601/02 ,  C07D215/18 ,  C07C69/675 ,  C07C69/92 ,  C07C323/60 ,  C07C309/66

摘要： A process for making montelukast, a pharmaceutically useful compound of the following formula and salts thereof: formula (1), using a compound of formula (4), is provided.

摘要翻译： 本发明涉及制备式（5）化合物的方法，其中R是C1-C4烷基，L是离去基团。

公开(公告)号：EP1615923A1

公开(公告)日：2006-01-18

申请号：EP04727562.3

申请日：2004-04-15

申请人： Synthon B.V.

发明人： BARTL, Jiri ,  GIELING, Reinerus, Gerardus

IPC分类号： C07D471/04 ,  A61K31/505 ,  A61P25/00

CPC分类号： C07D471/04

摘要： Hydrochloride salts of risperidone have been found to have useful properties. A preferred form is crystalline risperidone monohydrochloride hemipentahydrate. The monohydrochloride salts can be used in pharmaceutical compositions and methods such as for use in treating psychotic disorders.