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。

公开(公告)号：AU2005313325A1

公开(公告)日：2006-06-15

申请号：AU2005313325

申请日：2005-12-06

Applicant: JANSSEN PHARMACEUTICA NV

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

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

Abstract: 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.

公开(公告)号：AU2011202995B2

公开(公告)日：2012-02-02

申请号：AU2011202995

申请日：2011-06-21

Applicant: JANSSEN PHARMACEUTICA NV

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

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

Abstract: This invention concerns novel substituted tetracyclic tetrahydrofuran, pyrrolidine and tetrahydrothiophene derivatives with binding affinities towards serotonin receptors, in particular 5-HT2A and 5-HT 2c receptors, and towards dopamine receptors, in particular dopamine D2 receptors and with norepinephrine reuptake inhibition 10 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 (1) (R9i A B (R9j 20 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.

公开(公告)号：BRPI0611408A2

公开(公告)日：2010-09-08

申请号：BRPI0611408

申请日：2006-05-24

Applicant: JANSSEN PHARMACEUTICA NV

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

IPC: C07D487/04 ,  A61K31/403 ,  A61K31/407 ,  A61P25/00 ,  C07D209/94 ,  C07D221/18 ,  C07D307/93 ,  C07D311/94 ,  C07D333/80 ,  C07D491/04

Abstract: 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.

公开(公告)号：CA2604165A1

公开(公告)日：2006-11-30

申请号：CA2604165

申请日：2006-05-24

Applicant: JANSSEN PHARMACEUTICA NV

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

IPC: C07D487/04 ,  A61K31/403 ,  A61K31/407 ,  A61P25/00 ,  C07D209/94 ,  C07D221/18 ,  C07D307/93 ,  C07D311/94 ,  C07D333/80 ,  C07D491/04

Abstract: 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 productio n. The compounds according to the invention can be represented by general Formu la (I), and comprises also the pharmaceutically acceptable acid or base additio n salts thereof, the stereochemically isomeric forms thereof, the N-oxide form thereof and prodrugs thereof, wherein all substituents are defined as in Cla im 1.

公开(公告)号：AU2006251166A1

公开(公告)日：2006-11-30

申请号：AU2006251166

申请日：2006-05-24

Applicant: JANSSEN PHARMACEUTICA NV

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

IPC: C07D487/04 ,  A61K31/403 ,  A61K31/407 ,  A61P25/00 ,  C07D209/94 ,  C07D221/18 ,  C07D307/93 ,  C07D311/94 ,  C07D333/80 ,  C07D491/04

Abstract: 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.

公开(公告)号：CA2588760C

公开(公告)日：2014-05-13

申请号：CA2588760

申请日：2005-12-06

Applicant: JANSSEN PHARMACEUTICA NV

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

IPC: C07D209/70 ,  A61K31/352 ,  A61K31/381 ,  A61K31/403 ,  A61K31/407 ,  A61K31/435 ,  A61P25/00 ,  C07D221/18 ,  C07D311/94 ,  C07D333/80 ,  C07D403/06 ,  C07D413/06 ,  C07D487/04 ,  C07D491/044

Abstract: This invention concerns 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. (see formula I)

公开(公告)号：NZ562008A

公开(公告)日：2010-03-26

申请号：NZ56200806

申请日：2006-05-24

Applicant: JANSSEN PHARMACEUTICA NV

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

IPC: C07D487/04 ,  A61K31/403 ,  A61K31/407 ,  A61P25/00 ,  C07D209/94 ,  C07D221/18 ,  C07D307/93 ,  C07D311/94 ,  C07D333/80 ,  C07D491/04

Abstract: Disclosed is a compound of formula (I), or an N-oxide, a pharmaceutically acceptable addition salt, or a stereochemically isomeric form thereof, wherein X is CH2 or O, ring C is either selected from formulas (c-1) or (c-2), wherein Y1 is S, S(=O), S(=O)2, or NR10, and R10 and R11 may together from a ring as described, or ring C is selected from (c-4) or (c-5), wherein Y2 is O or NH, and wherein the other substituents are as defined in the specification. Also disclosed is the use of the compound for treating conditions mediated through the 5-HT2 or D2 receptor, or for treating central nervous system disorders such anxiety, depression, psychosis schizophrenia, migraine, and addictive properties of drug abuse.

公开(公告)号：AU2005313325B2

公开(公告)日：2011-03-24

申请号：AU2005313325

申请日：2005-12-06

Applicant: JANSSEN PHARMACEUTICA NV

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

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

Abstract: 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.

公开(公告)号：MX2007014857A

公开(公告)日：2008-02-14

申请号：MX2007014857

申请日：2006-05-24

Applicant: JANSSEN PHARMACEUTICA NV

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

IPC: C07D487/04 ,  A61K31/403 ,  A61K31/407 ,  A61P25/00 ,  C07D209/94 ,  C07D221/18 ,  C07D307/93 ,  C07D311/94 ,  C07D333/80 ,  C07D491/04

Abstract: Esta invencion se refiere a derivados de tetrahidrofurano, pirrolidina y tetrahidrotiofeno tetraciclicos, sustituidos, novedosos con afinidades de union hacia receptores de serotonina, en particular receptores de 5-HT2A y 5-HT2C, y hacia receptores de dopamina, en particular receptores D2 de dopamina y con propiedades de inhibicion de reabsorcion de norepinefrina, composiciones farmaceuticas que comprenden los compuestos de acuerdo a la invencion, su uso como una medicina, en particular para la prevencion y/o tratamiento de un intervalo de trastornos psiquiatricos y neurologicos, en particular ciertos trastornos psicoticos, cardiovascular y gastrocineticos y procedimientos para su produccion: los compuestos de acuerdo con la invencion se pueden representar por la formula general (I), y comprenden tambien su acido farmaceuticamente aceptable o sus sales de adicion basica, sus formas estereoquimicamente isomericas, su forma de N-oxido y sus profarmacos, en donde todos los sustituyentes se definen como en la reivindicacion 1.