公开(公告)号：EP1663996B1

公开(公告)日：2012-06-20

申请号：EP04734301.7

申请日：2004-05-21

申请人： Richter Gedeon Nyrt.

发明人： AGAINE' CSONGOR, Eva ,  GALAMBOS, János ,  NOGRADI, Katalin ,  VAGO, István ,  GYERTYAN, István ,  KISS, Béla ,  LASZLOVSZKY, István ,  LASZY, Judit ,  SAGHY, Katalin

IPC分类号： C07D243/08 ,  C07D295/12 ,  C07D295/14 ,  C07D401/12 ,  A61K31/495 ,  A61P25/00 ,  C07D233/04 ,  C07D295/135 ,  C07D295/215

CPC分类号： C07D295/215 ,  C07D223/04 ,  C07D243/08 ,  C07D295/135

摘要： The present invention relates to new D3 and D2 dopamine receptor subtype preferring ligands of formula (I): wherein R1 and R2 represent independently a substituent selected from hydrogen, alkyl, aryl, cycloalkyl, aroyl, or R1 and R2 may form a heterocyclic ring with the adjacent nitrogen atom; X represents an oxygen or sulphur atom; n is an integer of from 1 to 2, and/or geometric isomers and/or stereoisomers and/or diastereomers and/or salts and/or hydrates and/or solvates thereof, to the processes for producing the same, to pharmaceutical compositions containing the same and to their use in therapy and/or prevention of a condition which requires modulation of dopamine receptors.

摘要翻译： 本发明涉及式（I）的新的D3和D2多巴胺受体亚型优选配体：其中R1和R2独立地表示选自氢，烷基，芳基，环烷基，芳酰基的取代基，或者R1和R2可以与 相邻的氮原子; X代表氧或硫原子; n为1至2的整数，和/或其几何异构体和/或立体异构体和/或非对映异构体和/或盐和/或水合物和/或溶剂合物，其制备方法，含有 并且涉及它们在治疗和/或预防需要调节多巴胺受体的病症中的用途。

公开(公告)号：EP2358690A1

公开(公告)日：2011-08-24

申请号：EP09797145.1

申请日：2009-12-17

申请人： Richter Gedeon Nyrt.

发明人： CZIBULA, Lászl ,  ÁGAINÉ CSONGOR, Éva ,  NOGRADI, Katalin ,  JUHASZ, Bálint ,  SEBOK, Ferenc ,  GALAMBOS, János ,  VAGO, István

IPC分类号： C07D295/135

CPC分类号： C07D295/135

摘要： The invention relates to novel trans N-{4-{2-[4-(2,3-dichlorophenyl)-piperazine-l-il]-ethyl}- cyclohexylamine dihydrochloride monohydrate and a process for the preparation of the trans N- {4- {2-[4-(2,3-dichlorophenyl)-piperazine-l -il]-ethyl}-cyclohexylamine dihydrochloride monohydrate, said process comprising the steps a) reacting trans 2-{l-[4-(N-tert-butoxycarbonyl)amino]- cyclohexyl} -acetic acid ester with sodium borohydride and aluminium trichloride to give trans 2-{l-[4-(N-tert-butoxycarbonyl)-amino]-cyclohexyl}-ethanol; b) reacting trans 2-{l-[4-(N-tert-butoxycarbonyl)-amino]cyclohexyl}-ethanol obtained with methanesulfonic acid chloride in the presence of an acid binding agent to give trans 2-{l-[4- (N-tert-butoxycarbonyl)-amino] -cyclohexyl} -ethyl methanesulfonate; c) reacting trans 2-{l-[4-(N-tert-butoxycarbonyl)-amino]-cyclohexyl}-ethyl methanesulfonate obtained with 2,3-dichlorophenyl-piperazine in the presence of an acid binding agent to give trans 2-{l-[4-(N-tert-butoxycarbonyl)-amino]-cyclohexyl}-carbamic acid tert-butylester; d) heating trans 2-{l-[4-(N-tert-butoxycarbonyl)-amino]-cyclohexyl}-carbamic acid tert- butylester obtained to a temperature between 40-100°C in a mixture of aqueous hydrochloric acid/methanol to give trans N-{4-{2-[4-(2,3-dichlorophenyl)piperazine-l-il]-ethyl}- cyclohexylamine dihydrochloride monohydrate.

公开(公告)号：EP2358690B1

公开(公告)日：2016-03-30

申请号：EP09797145.1

申请日：2009-12-17

申请人： Richter Gedeon Nyrt.

发明人： CZIBULA, Lászl ,  ÁGAINÉ CSONGOR, Éva ,  NOGRADI, Katalin ,  JUHASZ, Bálint ,  SEBOK, Ferenc ,  GALAMBOS, János ,  VAGO, István

IPC分类号： C07D295/135

CPC分类号： C07D295/135

公开(公告)号：EP1409477B1

公开(公告)日：2008-09-17

申请号：EP02753161.5

申请日：2002-07-23

申请人： Richter Gedeon NYRT

发明人： DOMANY, György ,  HORVATH, Csilla ,  FARKAS, Sándor ,  BARTANE SZALAI, Gizella ,  NAGY, József ,  KOLOK, Sándor ,  BOZO, Eva ,  BORZA, István ,  VAGO, István ,  BIELIK, Attila ,  IGNACZNE SZENDREI, Györgyi ,  KESERÜ, György

IPC分类号： C07D401/12 ,  C07D413/12 ,  C07D295/185 ,  C07D407/12 ,  C07D417/12 ,  C07D451/02 ,  A61K31/445 ,  A61P25/28

CPC分类号： C07D211/14 ,  C07D211/16 ,  C07D401/12 ,  C07D413/12 ,  C07D417/12

摘要： The present invention relates to new carboxylic acid amide derivatives of formula (I), wherein U, V, W, X, Y, Z, n and m are as defined as in Claim 1. A further object of the invention are the processes for producing of carboxylic acid amide compounds of formula (I), and the pharmaceutical manufacture of medicaments containing these compounds, as well as the process of treatments with these compounds, which means administering to a mammal to be treated including human - effective amount/amounts of compounds of formula (I) of the present invention as such or as medicament. The new carboxylic acid amide derivatives of formula (I) of the present invention are highly effective and selective antagonists of NMDA receptor, and moreover most of the compounds are selective antagonist of NR2B subtype of NMDA receptor.

公开(公告)号：EP1438302B1

公开(公告)日：2012-05-30

申请号：EP02765129.8

申请日：2002-09-25

申请人： Richter Gedeon Nyrt.

发明人： GALAMBOS, János ,  NOGRADI, Katalin ,  AGAINE CSONGOR, Eva ,  KESERU, György, Miklos ,  VAGO, István ,  DOMANY, György ,  KISS, Béla ,  GYERTYAN, István ,  LASZLOVSZKY, István ,  LASZY, Judit

IPC分类号： C07D211/14 ,  C07D211/18 ,  C07D211/44 ,  C07D295/04 ,  C07D295/12

CPC分类号： C07D295/135 ,  C07D211/14 ,  C07D211/18 ,  C07D211/28 ,  C07D211/44 ,  C07D211/46 ,  C07D211/58 ,  C07D213/71 ,  C07D295/04 ,  C07D295/12

摘要： The present invention relates to new D3 dopamine receptor subtype selectice ligands of formula (I) to pharmacological compositions containing the same and to their us in therapy and/or prevention of psychoses (e.g. schizophrenia, schizo-affective disorders, etc), drug (e.g. alcohol, cocaine and nicotine, opioids etc.) abuse, cognitive impairment accompanying schizophrenia, mild-to-moderate cognitive deficits, amnesia, eating disorders (e.g. bulimia nervosa, etc.), attention deficit disorders, hyperactivity disorders in children, psychotic depression, mania, paranoid and delusional disorders, dyskinetic disorders (e.g. Parkinson's diseases, neuroleptic induced Parkinson's desases, tardive dyskinesias) anxiety, sexual dysfunction, sleep disorders, emesis, aggression, autism, pain ophthalmological diseases (e.g. glaucoma etc.).