公开(公告)号：US20080287450A1

公开(公告)日：2008-11-20

申请号：US11815726

申请日：2005-12-06

申请人： Jose Maria Cid-Nunez ,  Antonius Adrianus Hendrikus Petrus Megens ,  Andres Avelino Trabanco-Suarez ,  Mohamed Koukni ,  Georges Joseph Cornelius Hoornaert ,  Frans Josef Cornelius Compernolle ,  Tomasz Kozlecki ,  Hua Mao ,  Sushil Chandra Jha ,  Francisco Javier Fernandez-Gadea

发明人： Jose Maria Cid-Nunez ,  Antonius Adrianus Hendrikus Petrus Megens ,  Andres Avelino Trabanco-Suarez ,  Mohamed Koukni ,  Georges Joseph Cornelius Hoornaert ,  Frans Josef Cornelius Compernolle ,  Tomasz Kozlecki ,  Hua Mao ,  Sushil Chandra Jha ,  Francisco Javier Fernandez-Gadea

IPC分类号： A61K31/403 ,  C07D487/04 ,  C07D209/56 ,  C07D491/044 ,  A61K31/4985 ,  A61K31/352 ,  A61P3/04 ,  A61P25/00 ,  A61K31/381 ,  A61K31/407 ,  C07D333/50 ,  C07D311/94

CPC分类号： C07D333/80 ,  C07D209/70 ,  C07D221/18 ,  C07D307/93 ,  C07D311/94 ,  C07D487/04 ,  C07D491/04

摘要： This invention concerns novel substituted tetracyclic tetrahydrofuran, pyrrolidine and tetrahydrothiophene derivatives with binding affinities towards serotonin receptors, in particular 5-HT2A and 5-HT2C receptors, and towards dopamine receptors, in particular dopamine D2 receptors and with norepinephrine reuptake inhibition properties, pharmaceutical compositions comprising the compounds according to the invention, the use thereof as a medicine, in particular for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic, cardiovascular and gastrokinetic disorders and processes for their production.The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in Claim 1.

摘要翻译： 本发明涉及对5-羟色胺受体，特别是5-HT 2A和5-HT 2C受体具有结合亲和力的新型取代四环四氢呋喃，吡咯烷和四氢噻吩衍生物，并且涉及多巴胺受体 ，特别是多巴胺D2受体和去甲肾上腺素再摄取抑制性质，包含根据本发明的化合物的药物组合物，其作为药物的用途，特别是用于预防和/或治疗一系列精神和神经障碍，特别是 某些精神病，心血管和胃肠功能障碍及其生产过程。 根据本发明的化合物可以由通式（I）表示，并且还包括其药学上可接受的酸或碱加成盐，其立体化学异构形式，其N-氧化物形式及其前药，其中所有取代基定义为 在权利要求1中。

公开(公告)号：US20090023721A1

公开(公告)日：2009-01-22

申请号：US11915202

申请日：2006-05-24

申请人： Antonius Adrianus Hendrikus Petrus Megens ,  Andres Avelino Trabanco-Suarez ,  Jose Maria Cid-Nunez ,  Hua Mao ,  Sushil Chandra Jha ,  Francisco Javier Fernandez-Gadea ,  Mohamed Koukni ,  Georges Joseph Cornelius Hoornaert ,  Frans Josef Cornelius Compernolle ,  Tomasz Kozlecki

发明人： Antonius Adrianus Hendrikus Petrus Megens ,  Andres Avelino Trabanco-Suarez ,  Jose Maria Cid-Nunez ,  Hua Mao ,  Sushil Chandra Jha ,  Francisco Javier Fernandez-Gadea ,  Mohamed Koukni ,  Georges Joseph Cornelius Hoornaert ,  Frans Josef Cornelius Compernolle ,  Tomasz Kozlecki

IPC分类号： A61K31/4184 ,  C07D235/02 ,  C07D241/36 ,  C07D333/50 ,  A61K31/498 ,  A61K31/35 ,  A61K31/5377 ,  A61P25/00 ,  A61K31/403 ,  A61K31/381 ,  C07D311/02 ,  C07D209/56 ,  C07D413/12

CPC分类号： C07D209/94 ,  C07D221/18 ,  C07D307/93 ,  C07D311/94 ,  C07D333/80 ,  C07D487/04 ,  C07D491/04

摘要： This invention concerns novel substituted tetracyclic tetrahydrofuran, pyrrolidine and tetrahydrothiophene derivatives with binding affinities towards serotonin receptors, in particular 5-HT2A and 5-HT2C receptors, and towards dopamine receptors, in particular dopamine D2 receptors and with norepinephrine reuptake inhibition properties, pharmaceutical compositions comprising the compounds according to the invention, the use thereof as a medicine, in particular for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic, cardiovascular and gastrokinetic disorders and processes for their production.The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in Claim 1.

摘要翻译： 本发明涉及对5-羟色胺受体，特别是5-HT2A和5-HT2C受体以及对多巴胺受体，特别是多巴胺D2受体和去甲肾上腺素再摄取抑制性质具有结合亲和力的新型取代四环四氢呋喃，吡咯烷和四氢噻吩衍生物，包含 根据本发明的化合物，其用作药物，特别是用于预防和/或治疗一系列精神和神经障碍，特别是某些精神病性，心血管和胃肠功能障碍及其生产方法。 根据本发明的化合物可以由通式（I）表示，并且还包括其药学上可接受的酸或碱加成盐，其立体化学异构形式，其N-氧化物形式及其前药，其中所有取代基定义为 在权利要求1中。

公开(公告)号：US08415347B2

公开(公告)日：2013-04-09

申请号：US12850958

申请日：2010-08-05

申请人： José Maria Cid-Núñez ,  Antonius Adrianus Hendrikus Petrus Megens ,  Andrés Avelino Trabanco-Suárez ,  Mohamed Koukni ,  Georges Joseph Cornelius Hoornaert ,  Frans Josef Cornelius Compernolle ,  Tomasz Kozlecki ,  Hua Mao ,  Sushil Chandra Jha ,  Francisco Javier Fernández-Gadea

发明人： José Maria Cid-Núñez ,  Antonius Adrianus Hendrikus Petrus Megens ,  Andrés Avelino Trabanco-Suárez ,  Mohamed Koukni ,  Georges Joseph Cornelius Hoornaert ,  Frans Josef Cornelius Compernolle ,  Tomasz Kozlecki ,  Hua Mao ,  Sushil Chandra Jha ,  Francisco Javier Fernández-Gadea

IPC分类号： A61K31/5377 ,  A61K31/403 ,  A61K31/496 ,  A61K31/381 ,  A61K31/4985 ,  A61K31/352 ,  A61K31/435 ,  C07D491/044 ,  C07D209/58 ,  C07D413/04 ,  C07D333/80 ,  C07D487/04

CPC分类号： C07D333/80 ,  C07D209/70 ,  C07D221/18 ,  C07D307/93 ,  C07D311/94 ,  C07D487/04 ,  C07D491/04

摘要： This invention concerns novel substituted tetracyclic tetrahydrofuran, pyrrolidine and tetrahydrothiophene derivatives with binding affinities towards serotonin receptors, in particular 5-HT2A and 5-HT2C receptors, and towards dopamine receptors, in particular dopamine D2 receptors and with norepinephrine reuptake inhibition properties, pharmaceutical compositions comprising the compounds according to the invention, the use thereof as a medicine, in particular for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic, cardiovascular and gastrokinetic disorders and processes for their production.The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in Claim 1.

摘要翻译： 本发明涉及对5-羟色胺受体，特别是5-HT2A和5-HT2C受体以及对多巴胺受体，特别是多巴胺D2受体和去甲肾上腺素再摄取抑制性质具有结合亲和力的新型取代四环四氢呋喃，吡咯烷和四氢噻吩衍生物，包含 根据本发明的化合物，其用作药物，特别是用于预防和/或治疗一系列精神和神经障碍，特别是某些精神病性，心血管和胃肠功能障碍及其生产方法。 根据本发明的化合物可以由通式（I）表示，并且还包括其药学上可接受的酸或碱加成盐，其立体化学异构形式，其N-氧化物形式及其前药，其中所有取代基定义为 在权利要求1中。

公开(公告)号：US07799785B2

公开(公告)日：2010-09-21

申请号：US11815726

申请日：2005-12-06

申请人： José Maria Cid-Núñez ,  Antonius Andrianus Hendrikus Petrus Megens ,  Andrés Avelino Trabanco-Suárez ,  Mohamed Koukni ,  Georges Joseph Cornelius Hoornaert ,  Frans Josef Cornelius Compernolle ,  Tomasz Kozlecki ,  Hua Mao ,  Sushil Chandra Jha ,  Francisco Javier Fernández-Gadea

发明人： José Maria Cid-Núñez ,  Antonius Andrianus Hendrikus Petrus Megens ,  Andrés Avelino Trabanco-Suárez ,  Mohamed Koukni ,  Georges Joseph Cornelius Hoornaert ,  Frans Josef Cornelius Compernolle ,  Tomasz Kozlecki ,  Hua Mao ,  Sushil Chandra Jha ,  Francisco Javier Fernández-Gadea

IPC分类号： A61K31/403 ,  A61K31/4985 ,  A61K31/352 ,  A61P3/04 ,  A61P25/00 ,  A61K31/381 ,  A61K31/407 ,  C07D487/04 ,  C07D209/56 ,  C07D491/044

CPC分类号： C07D333/80 ,  C07D209/70 ,  C07D221/18 ,  C07D307/93 ,  C07D311/94 ,  C07D487/04 ,  C07D491/04

摘要： This invention concerns novel substituted tetracyclic tetrahydrofuran, pyrrolidine and tetrahydrothiophene derivatives with binding affinities towards serotonin receptors, in particular 5-HT2A and 5-HT2C receptors, and towards dopamine receptors, in particular dopamine D2 receptors and with norepinephrine reuptake inhibition properties, pharmaceutical compositions comprising the compounds according to the invention, the use thereof as a medicine, in particular for the prevention and/or treatment of a range of psychiatric and neurological disorders, in particular certain psychotic, cardiovascular and gastrokinetic disorders and processes for their production.The compounds according to the invention can be represented by general Formula (I) and comprises also the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in Claim 1.

摘要翻译： 本发明涉及对5-羟色胺受体，特别是5-HT2A和5-HT2C受体以及对多巴胺受体，特别是多巴胺D2受体和去甲肾上腺素再摄取抑制性质具有结合亲和力的新型取代四环四氢呋喃，吡咯烷和四氢噻吩衍生物，包含 根据本发明的化合物，其用作药物，特别是用于预防和/或治疗一系列精神和神经障碍，特别是某些精神病性，心血管和胃肠功能障碍及其生产方法。 根据本发明的化合物可以由通式（I）表示，并且还包括其药学上可接受的酸或碱加成盐，其立体化学异构形式，其N-氧化物形式及其前药，其中所有取代基定义为 在权利要求1中。

公开(公告)号：US20110224208A1

公开(公告)日：2011-09-15

申请号：US13129311

申请日：2009-11-16

申请人： Dorothée Bardiot ,  Emilie Blanche ,  Patrick Chaltin ,  Mohamed Koukni ,  Pieter Leyssen ,  Johan Neyts ,  Arnaud Marchand ,  Inge Vliegen

发明人： Dorothée Bardiot ,  Emilie Blanche ,  Patrick Chaltin ,  Mohamed Koukni ,  Pieter Leyssen ,  Johan Neyts ,  Arnaud Marchand ,  Inge Vliegen

IPC分类号： A61K31/4725 ,  C07D409/04 ,  C07D409/14 ,  C07D405/04 ,  C07D217/22 ,  A61K31/472 ,  C07D401/04 ,  C07D413/14 ,  A61K31/5377 ,  C07D417/04 ,  A61K31/506 ,  A61K31/497 ,  A61P31/14

CPC分类号： C07D409/04 ,  A61K31/472 ,  A61K31/4725 ,  A61K31/497 ,  C07D217/24 ,  C07D217/26 ,  C07D401/04 ,  C07D401/12 ,  C07D405/04 ,  C07D405/12 ,  C07D409/14 ,  C07D413/04 ,  C07D413/14 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14

摘要： The present invention relates to a series of Isoquinolone derivatives which are suitable to treat infections with viruses belonging to the family of the Flaviviridae and more preferably infections with Hepatitis C virus (HCV). The present invention also relates to Isoquinolone compounds for use as a medicine for the prevention or treatment of viral infections, preferably infections with viruses belonging to the family of the Flaviviridae.

摘要翻译： 本发明涉及一系列适用于治疗属于黄病毒科病毒感染的异喹诺酮衍生物，更优选丙型肝炎病毒（HCV）感染。 本发明还涉及用作预防或治疗病毒感染的药物的异喹诺酮化合物，优选为属于黄病毒科的病毒感染。