公开(公告)号：EP4192833A1

公开(公告)日：2023-06-14

申请号：EP21755582.0

申请日：2021-08-05

申请人： Richter Gedeon Nyrt.

发明人： BORZA, István ,  ÉLES, János ,  ROMÁN, Viktor ,  PETRÓ, József Levente ,  GEGÖ, Csaba Lehel ,  BÉNYEI, Gyula Attila

IPC分类号： C07D487/04 ,  A61K31/519 ,  A61P25/00 ,  A61P19/00

公开(公告)号：EP4192839A1

公开(公告)日：2023-06-14

申请号：EP21756058.0

申请日：2021-08-06

申请人： Richter Gedeon Nyrt.

发明人： BORZA, István ,  UJVÁRI, Viktor ,  BANA, Péter ,  PETRO, József Levente ,  ÉLES, János ,  BÓDI, József ,  VARRÓ, Gábor ,  KLADNI, László János ,  SPRÁNITZ, Péter ,  KRÁMOS, Balázs

IPC分类号： C07H1/00 ,  C07D487/04 ,  C07D519/00 ,  C07H15/18 ,  A61P31/12 ,  A61P31/14

公开(公告)号：EP3596080A1

公开(公告)日：2020-01-22

申请号：EP18713016.6

申请日：2018-03-12

申请人： Richter Gedeon Nyrt.

发明人： BORZA, István ,  ROMÁN, Viktor ,  ÉLES, János ,  HADADY, Zsuzsa

IPC分类号： C07D487/04 ,  A61K31/519 ,  A61P19/00 ,  A61P25/00

公开(公告)号：EP1963260B1

公开(公告)日：2010-11-03

申请号：EP06831516.7

申请日：2006-12-18

申请人： Richter Gedeon Nyrt.

发明人： BÓDI, József ,  ÉLES, János ,  SZÖKE, Katalin ,  VUKICS, Krisztina ,  GÁTI, Tamás ,  TEMESVÁRI, Krisztina ,  KISS-BARTOS, Dorottya

IPC分类号： C07D205/08 ,  C07D413/06 ,  C07D317/30 ,  C07D405/06 ,  C07F7/02

CPC分类号： C07D205/08 ,  C07D317/30 ,  C07D405/06 ,  C07D413/06 ,  C07F7/186 ,  C07F7/1892

摘要： This invention provides a novel, industrially easily realizable and economical process comprising only few steps, and built on new intermediates for the production of 1-(4-3(R)- [3(S)-(4-fluorophenyl)-3-hydroxypropyl]-4(S)-(4-hydroxyphenyl)-2-azetidinone (ezetimibe) according to the following reaction scheme: (I), (II), (III), (IV), (V), (VI), (VII), (VIII), (IX), (X), (XI) wherein, the substances of the general Formulas II, IV, VI, VIII, IX, X and XI are new, Formula III is a non-isolated intermediate, Rl, R2 and R3 are represented by the compounds of Formulas Va-Vd, (Va), (Vb), (Vc), (Vd) and R4 is a silil, e.g. tert.buthyl-dimethyl-silil, tert-buthyl-diphenyl-silil group.

公开(公告)号：EP2125772A1

公开(公告)日：2009-12-02

申请号：EP07858827.4

申请日：2007-12-20

申请人： Richter Gedeon Nyrt.

发明人： BÓDI, József ,  SZÖKE, Katalin ,  ÉLES, János ,  FOGASSY, Elemér ,  SCHINDLER, József ,  VUKICS, Krisztina ,  FARAGÓ, János ,  TEMESVÁRI, Krisztina ,  GÁTI, Tamás

IPC分类号： C07D333/20

CPC分类号： C07D333/20

摘要： The present invention relates to a process for the preparation of duloxetin. ((S)-(+)-N-methyl-N-(3-(l-naρhthalenyloxy)-3-(2-thienyl)propanamine) of formula (I) and pharmaceutically acceptable salts thereof, said process comprising the steps of a) resolving racemic 3-(N-methyl-N-berizylamino)-1-(2-thienyl)-1-propanol of formula (II) with a D-phenylglycine derivative to obtain a compound of formula (IV); and b) reacting (S)-3-(N-methyl-N-ben2yIamino)-1-(2-thienyl)-1-propanol of formula (IV) with 1-fluoronaphthalene to yield (S)-N-methyl-N-benzyl-3-(1-naphthalenyloxy)-3-(2- thienyl)propanamine of formula (V), reacting the compound of formula (V) obtained with 1-chloroethyl chloroformate to yield duloxetin of formula (I), and if desired converting the duloxetin of formula (I) obtained into an acid addition salt thereof.

公开(公告)号：EP2074083A1

公开(公告)日：2009-07-01

申请号：EP07824996.8

申请日：2007-10-27

申请人： Richter Gedeon Nyrt.

发明人： BOZÓ, Éva ,  BEKE, Gyula ,  ÉLES, János ,  FARKAS, Sándor ,  HORNOK, Katalin ,  KESERÜ, György ,  SCHMIDT, Éva ,  SZENTIRMAY, Éva ,  VÁGÓ, István ,  VASTAG, Mónika

IPC分类号： C07C311/21 ,  A61K31/18 ,  A61P29/00 ,  C07D207/26 ,  C07D211/26 ,  C07D211/34 ,  C07D211/56 ,  C07D211/62 ,  C07D211/76 ,  C07D213/38 ,  C07D213/74 ,  C07D213/75 ,  C07D233/54 ,  C07D239/04 ,  C07D239/42

CPC分类号： C07C311/21 ,  C07D207/26 ,  C07D211/26 ,  C07D211/34 ,  C07D211/56 ,  C07D211/62 ,  C07D211/76 ,  C07D213/38 ,  C07D213/74 ,  C07D213/75 ,  C07D233/54 ,  C07D239/04 ,  C07D239/42 ,  C07D241/20 ,  C07D243/08 ,  C07D295/12 ,  C07D295/20 ,  C07D401/04 ,  C07D401/06 ,  C07D401/12

摘要： The present invention relates to new sulfonamide derivatives of formula (I), wherein R1 -R5 and Z are as defined in the claims, and optical antipodes or racemates and/or salts and/or hydrates and/or solvates thereof, which are selective antagonists of bradykinin B1, to processes for producing these compounds, pharmacological compositions containing them and to their use in therapy or prevention of painful and inflammatory conditions.

公开(公告)号：EP3820869A1

公开(公告)日：2021-05-19

申请号：EP19744868.1

申请日：2019-07-12

申请人： Richter Gedeon Nyrt.

发明人： ÉLES, János ,  DUDÁSNÉ MOLNÁR, Katalin ,  LEDNECZKI, István ,  TAPOLCSÁNYI, Pál ,  HORVÁTH, Anita ,  NÉMETHY, Zsolt ,  LÉVAY, György István

IPC分类号： C07D471/04 ,  C07D491/107 ,  A61P25/18 ,  A61K31/397

公开(公告)号：EP3286193B1

公开(公告)日：2020-05-27

申请号：EP16718017.3

申请日：2016-04-14

申请人： Richter Gedeon Nyrt.

发明人： BEKE, Gyula ,  ÉLES, János ,  BOROS, András ,  FARKAS, Sándor ,  KESERÜ , György Miklós

IPC分类号： C07D487/04 ,  A61K31/551 ,  A61P3/00 ,  A61P25/00

公开(公告)号：EP1966142A2

公开(公告)日：2008-09-10

申请号：EP06831519.1

申请日：2006-12-19

申请人： Richter Gedeon NYRT

发明人： BEKE, Gyula ,  BOZÓ, Éva ,  CZÍRA, Gábor ,  ÉLES, János ,  FARKAS, Sándor ,  HORNOK, Katalin ,  SCHMIDT, Éva ,  SZENTIRMAY, Éva ,  VÁGÓ, István ,  VASTAG, Mónika

IPC分类号： C07D213/74 ,  C07D221/12 ,  C07D295/12 ,  C07D401/10 ,  C07D401/12 ,  C07D401/14 ,  A61K31/473 ,  A61P25/02

CPC分类号： C07D401/12 ,  C07D213/74 ,  C07D221/12 ,  C07D295/135 ,  C07D401/10 ,  C07D401/14

摘要： The present invention relates to new phenanthridine derivatives of formula (I), wherein the variables are as defined in the specificition, to processes for producing the same, to pharmacological compositions containing the same and to their use in therapy or prevention of painful and inflammatory processes.

公开(公告)号：EP1963260A1

公开(公告)日：2008-09-03

申请号：EP06831516.7

申请日：2006-12-18

申请人： Richter Gedeon NYRT

发明人： BÓDI, József ,  ÉLES, János ,  SZÖKE, Katalin ,  VUKICS, Krisztina ,  GÁTI, Tamás ,  TEMESVÁRI, Krisztina ,  KISS-BARTOS, Dorottya

IPC分类号： C07D205/08 ,  C07D413/06 ,  C07D317/30 ,  C07D405/06 ,  C07F7/02

CPC分类号： C07D205/08 ,  C07D317/30 ,  C07D405/06 ,  C07D413/06 ,  C07F7/186 ,  C07F7/1892

摘要： This invention provides a novel, industrially easily realizable and economical process comprising only few steps, and built on new intermediates for the production of 1-(4-3(R)- [3(S)-(4-fluorophenyl)-3-hydroxypropyl]-4(S)-(4-hydroxyphenyl)-2-azetidinone (ezetimibe) according to the following reaction scheme: (I), (II), (III), (IV), (V), (VI), (VII), (VIII), (IX), (X), (XI) wherein, the substances of the general Formulas II, IV, VI, VIII, IX, X and XI are new, Formula III is a non-isolated intermediate, Rl, R2 and R3 are represented by the compounds of Formulas Va-Vd, (Va), (Vb), (Vc), (Vd) and R4 is a silil, e.g. tert.buthyl-dimethyl-silil, tert-buthyl-diphenyl-silil group.