公开(公告)号：WO2004074266A8

公开(公告)日：2004-11-11

申请号：PCT/EP2004050084

申请日：2004-02-05

Applicant: JANSSEN PHARMACEUTICA NV ,  LEWI PAULUS JOANNES ,  ARTS THEODORA JOANNA FRANCISCA ,  JANSSEN GRAZIELLA MARIA CONSTA ,  JANSSEN HERWIG JOSEPHUS MARGAR ,  JANSSEN JASMINE JOSEE WERNER H ,  JANSSEN PAUL PETER MARIA HM ,  JANSSEN MAROUSSIA GODELIEVE FR ,  DE JONGE MARC RENE ,  KOYMANS LUCIEN MARIA HENRICUS ,  VINKERS HENDRIK MAARTEN ,  DAEYAERT FREDERIK FRANS DESIRE ,  HEERES JAN ,  LEENDERS RUBEN GERARDUS GEORGE ,  HOORNAERT GEORGES JOSEPH CORNE ,  KILONDA AMURI ,  LUDOVICI DONALD WILLIAM

Inventor： LEWI PAULUS JOANNES ,  JANSSEN PAUL ADRIAAN JAN DI ,  DE JONGE MARC RENE ,  KOYMANS LUCIEN MARIA HENRICUS ,  VINKERS HENDRIK MAARTEN ,  DAEYAERT FREDERIK FRANS DESIRE ,  HEERES JAN ,  LEENDERS RUBEN GERARDUS GEORGE ,  HOORNAERT GEORGES JOSEPH CORNE ,  KILONDA AMURI ,  LUDOVICI DONALD WILLIAM

IPC: A61K31/53 ,  C07D253/06 ,  C07D253/07 ,  C07D253/075

CPC classification number: A61K31/53 ,  C07D253/07 ,  C07D253/075

Abstract: The present invention relates to HIV replication inhibitors of formula (I) as defined in the specification their use as a medicine, their processes for preparation and pharmaceutical compositions comprising them.

Abstract translation: 本发明涉及如说明书中所定义的式（I）的HIV复制抑制剂作为药物的用途，它们的制备方法和包含它们的药物组合物。

公开(公告)号：WO03048147A2

公开(公告)日：2003-06-12

申请号：PCT/EP0213561

申请日：2002-12-02

Applicant: JANSSEN PHARMACEUTICA NV ,  MAO HUA ,  KOZLECKI TOMASZ ,  COMPERNOLLE FRANS JOSEF CORNEL ,  HOORNAERT GEORGES JOSEPH CORNE

Inventor： MAO HUA ,  KOZLECKI TOMASZ ,  COMPERNOLLE FRANS JOSEF CORNEL ,  HOORNAERT GEORGES JOSEPH CORNE

IPC: A61K31/34 ,  A61K31/343 ,  A61P25/00 ,  A61P25/06 ,  A61P25/18 ,  A61P25/22 ,  A61P25/24 ,  A61P25/30 ,  C07D307/93

CPC classification number: C07D307/93

Abstract: The present invention concerns a process for preparing each of the 4 individual diastereomers of formula (I) in stereochemically pure form from a single enantiomerically pure precursor. The tetracyclic ringsystem having cis-fused five and seven membered rings is formed in a base-catalysed cyclization reaction. The invention further relates to the thus obtained cis-fused tetracyclic alcohol intermediates and methanamine end-products, and the methanamine end-products for use as a medicine, in particular as CNS active medicines.

Abstract translation: 本发明涉及从单一对映异构体纯的前体以立体化学纯的形式制备式（I）的4种单独的非对映异构体的方法。 在碱催化的环化反应中形成具有顺式稠合的五元和七元环的四环环系。 本发明还涉及由此获得的顺式稠合四环醇中间体和甲胺终产物，以及用作药物的甲胺最终产物，特别是CNS活性药物。

公开(公告)号：WO2006061392A3

公开(公告)日：2006-11-02

申请号：PCT/EP2005056544

申请日：2005-12-06

Applicant: JANSSEN PHARMACEUTICA NV ,  CID-NUNEZ JOSE MARIA ,  MEGENS ANTONIUS ADRIANUS HENDR ,  TRABANCO-SUAREZ ANDRES AVELINO ,  KOUKNI MOHAMED ,  HOORNAERT GEORGES JOSEPH CORNE ,  COMPERNOLLE FRANS JOSEF CORNEL ,  KOZLECKI TOMASZ ,  MAO HUA ,  JHA SUSHIL CHANDRA ,  FERNANDEZ-GADEA FRANCISCO JAVI

Inventor： CID-NUNEZ JOSE MARIA ,  MEGENS ANTONIUS ADRIANUS HENDR ,  TRABANCO-SUAREZ ANDRES AVELINO ,  KOUKNI MOHAMED ,  HOORNAERT GEORGES JOSEPH CORNE ,  COMPERNOLLE FRANS JOSEF CORNEL ,  KOZLECKI TOMASZ ,  MAO HUA ,  JHA SUSHIL CHANDRA ,  FERNANDEZ-GADEA FRANCISCO JAVI

IPC: C07D209/70 ,  A61K31/343 ,  A61K31/352 ,  A61K31/381 ,  A61K31/403 ,  A61K31/407 ,  A61K31/4188 ,  A61K31/496 ,  A61K31/4985 ,  C07D221/18 ,  C07D307/93 ,  C07D311/94 ,  C07D333/80 ,  C07D487/04 ,  C07D491/044

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

Abstract: This invention concerns novel substituted tetracyclic tetrahydrofuran, pyrrolidine and tetrahydrothiophene derivatives with binding affinities towards serotonin receptors, in particular 5-HT 2A and 5-HT 2C 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.

Abstract translation: 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。