公开(公告)号：EP2132185A2

公开(公告)日：2009-12-16

申请号：EP08737283.5

申请日：2008-04-10

申请人： Richter Gedeon Nyrt.

发明人： BARTÁNÉ SZALAI, Gizella ,  ÁGAINÉ CSONGOR, Éva ,  DOMÁNY, György ,  GYERTYÁN, István ,  KISS, Béla ,  LASZY, Judit ,  SÁGHY, Katalin ,  SCHMIDT, Éva ,  FARKAS, Sándor ,  KOMLÓDI, Zsolt

IPC分类号： C07D239/48 ,  A61K31/506 ,  A61P25/00

CPC分类号： C07D239/48

摘要： The present invention relates to new dopamine D3 and D2 ligands of formula (I): wherein Rl, R2 and Q are as described herein, and/or geometric isomers and/or stereoisomers and/or diastereomers and/or salts and/or hydrates and/or solvates and/or polymorphs thereof. The invention also relates to processes for preparing the same, to compositions containing the same and to their use in the treatment and/or prevention of conditions which requires modulation of dopamine receptors.

公开(公告)号：EP2964613B1

公开(公告)日：2018-07-18

申请号：EP14712780.7

申请日：2014-03-06

申请人： Richter Gedeon Nyrt.

发明人： BARTÁNÉ SZALAI, Gizella ,  WÁGNER, Gábor András ,  KISS, Béla ,  SCHMIDT, Éva ,  BALÁZS, Ottília ,  NAGY, Noémi

IPC分类号： C07D211/44 ,  C07D401/12 ,  A61K31/4465 ,  A61K31/454 ,  A61P25/28

CPC分类号： C07D211/46 ,  A61K9/0019 ,  A61K9/0095 ,  A61K9/02 ,  A61K9/2059 ,  A61K9/4866 ,  A61K31/27 ,  A61K31/445 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/473 ,  A61K31/55 ,  A61K45/06 ,  C07D211/44 ,  C07D401/12 ,  A61K2300/00

摘要： The present invention relates to new histamine H3 (H3) receptor subtype selective ligands of the general formula (I) and/or geometric isomers and/or stereoisomers and/or diastereomers and/or salts and/or hydrates and/or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds and the use of these compounds as medicaments for treatment and/or prevention of conditions which require modulation of H3 receptors. The invention also cover the combinations of a compound of the general formula (I) and an acetylcholinesterase inhibitor.

公开(公告)号：EP2964613A1

公开(公告)日：2016-01-13

申请号：EP14712780.7

申请日：2014-03-06

申请人： Richter Gedeon Nyrt.

发明人： BARTÁNÉ SZALAI, Gizella ,  WÁGNER, Gábor András ,  KISS, Béla ,  SCHMIDT, Éva ,  BALÁZS, Ottília ,  NAGY, Noémi

IPC分类号： C07D211/44 ,  C07D401/12 ,  A61K31/4465 ,  A61K31/454 ,  A61P25/28

CPC分类号： C07D211/46 ,  A61K9/0019 ,  A61K9/0095 ,  A61K9/02 ,  A61K9/2059 ,  A61K9/4866 ,  A61K31/27 ,  A61K31/445 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/473 ,  A61K31/55 ,  A61K45/06 ,  C07D211/44 ,  C07D401/12 ,  A61K2300/00

摘要： The present invention relates to new histamine H3 (H3) receptor subtype selective ligands of the general formula (I) and/or geometric isomers and/or stereoisomers and/or diastereomers and/or salts and/or hydrates and/or solvates thereof. The invention further relates to pharmaceutical compositions containing such compounds and the use of these compounds as medicaments for treatment and/or prevention of conditions which require modulation of H3 receptors. The invention also cover the combinations of a compound of the general formula (I) and an acetylcholinesterase inhibitor.

摘要翻译： 本发明涉及通式（I）的新组胺H3（H3）受体亚型选择性配体和/或几何异构体和/或立体异构体和/或非对映异构体和/或其盐和/或水合物和/或溶剂化物。 本发明还涉及含有这些化合物的药物组合物以及这些化合物作为治疗和/或预防需要调节H3受体的病症的药物的用途。 本发明还涵盖通式（I）的化合物与乙酰胆碱酯酶抑制剂的组合。

公开(公告)号：EP2922825A1

公开(公告)日：2015-09-30

申请号：EP13805593.4

申请日：2013-11-20

申请人： Richter Gedeon Nyrt.

发明人： SZAVICSKÓ, Krisztina ,  DOMÁNY, György ,  CZIBULA, László ,  BARTÁNÉ SZALAI, Gizella ,  DOBAY, László ,  PAPP, Éva

IPC分类号： C07D239/48 ,  A61K31/506 ,  A61P25/00

CPC分类号： C07D239/48

摘要： Our invention relates to trans-(4-{4-[2-(4-amino-cyclohexyl)-ethyl]-piperazin-1-yl}-5,6- dichloro-pyrimidin-2-yl)-methylamine dihydrochloride monohydrate, the process for the synthesis of this compound, the new (4,5-dichloro-6-piperazin-1-yl-pyirimidin-2-yl)- methylamine monohydrochlorid used as starting material in this synthesis, as well as the industrial process for the synthesis of trans-N-(4-{2-[4-(5,6-dichloro-2-methyl-amino- pyirimidin-4-yl)-piperazin-1-yl]-ethyl}cyclohexyl-propionamide starting from trans-(4-{4-[2-(4- amino-cyclohexyl)-ethyl]-piperazin-1-yl}-5,6-dichloro-pyrimidin-2-yl)-methylamine dihydrochloride monohydrate.

公开(公告)号：EP2132185B1

公开(公告)日：2011-08-03

申请号：EP08737283.5

申请日：2008-04-10

申请人： Richter Gedeon Nyrt.

发明人： BARTÁNÉ SZALAI, Gizella ,  ÁGAINÉ CSONGOR, Éva ,  DOMÁNY, György ,  GYERTYÁN, István ,  KISS, Béla ,  LASZY, Judit ,  SÁGHY, Katalin ,  SCHMIDT, Éva ,  FARKAS, Sándor ,  KOMLÓDI, Zsolt

IPC分类号： C07D239/48 ,  A61K31/506 ,  A61P25/00

CPC分类号： C07D239/48

摘要： The present invention relates to new dopamine D3 and D2 ligands of formula (I): wherein Rl, R2 and Q are as described herein, and/or geometric isomers and/or stereoisomers and/or diastereomers and/or salts and/or hydrates and/or solvates and/or polymorphs thereof. The invention also relates to processes for preparing the same, to compositions containing the same and to their use in the treatment and/or prevention of conditions which requires modulation of dopamine receptors.