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11.发明专利
公开(公告)号：HRP20040489A2
公开(公告)日：2005-04-30
申请号：HRP20040489
申请日：2004-05-31
Applicant: JANSSEN PHARMACEUTICA NV
Inventor： MAO HUA , KOZLECKI TOMASZ , COMPERNOLLE FRANS JOSEF CORNEL , HOORNAERT GEORGES JOSEF CORNEL
IPC: A61K31/34 , A61K31/343 , A61P25/00 , A61P25/06 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/30 , 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
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12.发明专利
公开(公告)号：HU0402325A2
公开(公告)日：2005-02-28
申请号：HU0402325
申请日：2002-12-02
Applicant: JANSSEN PHARMACEUTICA NV
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
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
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13.发明专利
公开(公告)号：AU2002342926A1
公开(公告)日：2003-06-17
申请号：AU2002342926
申请日：2002-12-02
Applicant: JANSSEN PHARMACEUTICA NV
Inventor： LANG YOLANDE LYDIA , MEDAER BART PETRUS ANNA MARIA , HOORNAERT GEORGES JOSEPH CORNE , BROSSETTE THIERRY , COMPERNOLLE FRANS JOSEF CORNEL , GUILLAUME MICHEL JOSEPH MAURIC , MAO HUA , KOZLECKI TOMASZ
IPC: A61K31/34 , A61K31/343 , A61P25/06 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , C07D307/93
Abstract: The present invention concerns processes for the preparation of each of the 4 diastereomers of formula (I) in stereochemically pure form from either of two enantiomerically pure precursors. The tetracyclic ringsystem having trans-fused five and seven membered rings is formed in an acid-catalysed cyclization reaction. The invention further relates to the thus obtained cis-fused tetracyclic alcohol intermediates, the methanamine end-products, the methanamine end-products for use as a medicine, in particular as CNS active medicines.
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公开(公告)号：CA2468040A1
公开(公告)日：2003-06-12
申请号：CA2468040
申请日：2002-12-02
Applicant: JANSSEN PHARMACEUTICA NV
Inventor： MAO HUA , HOORNAERT GEORGES JOSEPH CORNE , COMPERNOLLE FRANS JOSEF CORNEL , KOZLECKI TOMASZ
IPC: A61K31/34 , A61K31/343 , A61P25/00 , A61P25/06 , A61P25/18 , A61P25/22 , A61P25/24 , A61P25/30 , 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 ci s- fused five and seven membered rings is formed in a base-catalysed cyclizatio n 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.
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15.发明专利
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.
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Patent Agency Ranking
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.
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17.发明专利
公开(公告)号：CA2588760A1
公开(公告)日：2006-06-15
申请号：CA2588760
申请日：2005-12-06
Applicant: JANSSEN PHARMACEUTICA NV
Inventor： HOORNAERT GEORGES JOSEPH CORNE , KOUKNI MOHAMED , COMPERNOLLE FRANS JOSEF CORNEL , KOZLECKI TOMASZ , MEGENS ANTONIUS ADRIANUS HENDR , JHA SUSHIL CHANDRA , CID-NUNEZ JOSE MARIA , TRABANCO-SUAREZ ANDRES AVELINO , MAO HUA , 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
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.
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公开(公告)号：DE60203937D1
公开(公告)日：2005-06-02
申请号：DE60203937
申请日：2002-12-02
Applicant: JANSSEN PHARMACEUTICA NV
Inventor： LANG YOLANDE LYDIA , MEDAER B P A M J , HOORNAERT G J , BROSSETTE THIERRY , COMPERNOLLE FRANS J C , GUILLAUME MICHEL JOSEPH MAURIC , MAO HUA , KOZLECKI TOMASZ
IPC: A61K31/34 , A61K31/343 , A61P25/06 , A61P25/22 , A61P25/24 , A61P25/28 , A61P25/30 , C07D307/93
Abstract: The present invention concerns processes for the preparation of each of the 4 diastereomers of formula (I) in stereochemically pure form from either of two enantiomerically pure precursors. The tetracyclic ringsystem having trans-fused five and seven membered rings is formed in an acid-catalysed cyclization reaction. The invention further relates to the thus obtained cis-fused tetracyclic alcohol intermediates, the methanamine end-products, the methanamine end-products for use as a medicine, in particular as CNS active medicines.
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19.发明专利
公开(公告)号：PL370440A1
公开(公告)日：2005-05-30
申请号：PL37044002
申请日：2002-12-02
Applicant: JANSSEN PHARMACEUTICA NV
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
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
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公开(公告)号：BR0214775A
公开(公告)日：2004-11-09
申请号：BR0214775
申请日：2002-12-02
Applicant: JANSSEN PHARMACEUTICA NV
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
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
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