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.

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.

公开(公告)号：HRP20040490A2

公开(公告)日：2004-10-31

申请号：HRP20040490

申请日：2004-05-31

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： YOLANDE ,  BART ,  GEORGES ,  BROSSETTE THIERRY ,  MICHEL ,  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.

公开(公告)号：NZ532806A

公开(公告)日：2006-01-27

申请号：NZ53280602

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: A process for preparing each individual diastereoisomer of formula (I) wherein the substituents on carbon atoms 3a and 12b have the trans configuration, the substituent on carbon atom 2 may have the R or the S configuration, comprising the step of cyclizing a compound of formula (II) wherein R represents C1-3 alkylcarbonyl; OR1 represents a leaving group and the substituents -OR and -CH2-CHOH-CH2OR1 have the cis configuration, in a reaction inert solvent in the presence of an acid.

公开(公告)号：HK1076461A1

公开(公告)日：2006-01-20

申请号：HK05108415

申请日：2005-09-23

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: C07D20060101 ,  A61K20060101 ,  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.

公开(公告)号：PL369585A1

公开(公告)日：2005-05-02

申请号：PL36958502

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.

公开(公告)号：DE60203937T2

公开(公告)日：2006-05-11

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: C07D307/93 ,  A61K31/34 ,  A61K31/343 ,  A61P25/06 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30

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.

公开(公告)号：ES2242076T3

公开(公告)日：2005-11-01

申请号：ES02779576

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

IPC: A61K31/34 ,  A61K31/343 ,  A61P25/06 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  C07D307/93

Abstract: Procedimiento para preparar cada diastereoisómero individual de fórmula (I): en la que los sustituyentes en los átomos de carbono 3a y 12b tienen la configuración trans, el sustituyente en el átomo de carbono 2 puede tener la configuración R o S, que comprende la etapa de ciclar un compuesto de fórmula (II) en la que R representa (alquil C1-3)carbonilo; OR1 representa un grupo saliente y los sustituyentes -OR y - CH2-CHOH-CH2OR1 tienen la configuración cis, en un disolvente inerte en la reacción en presencia de un ácido, por el cual

公开(公告)号：MXPA04005400A

公开(公告)日：2004-10-11

申请号：MXPA04005400

申请日：2002-12-02

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： BROSSETTE THIERRY

IPC: A61K31/34 ,  A61K31/343 ,  A61P25/06 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30 ,  C07D307/93

Abstract: La presente invencion se refiere a procedimientos para la preparacion de cada uno de los 4 diastereomeros de formula (I)(ver formula I)en forma estereoquimicamente pura de cualquiera de dos precursores enantiomericamente puros; el sistema de anillo tetracilcio que tiene anillos de cinco y siete elementos trans-fusionados se forma en una reaccion de ciclizacion catalizada con acido, la invencion se refiere ademas a los intermedios de alcohol tetraciclico cis-fusionados asi obtenidos, los productos finales de metanamina, los productos finales de metanamina para uso como una medicina, en particular como medicinas activas para el CNS.

公开(公告)号：CA2468038C

公开(公告)日：2011-04-26

申请号：CA2468038

申请日：2002-12-02

Applicant: JANSSEN PHARMACEUTICA NV

Inventor： LANG YOLANDE LYDIA ,  MEDAER BART PETRUS ANNA MARIA JOZEF ,  HOORNAERT GEORGES JOSEPH CORNELIUS ,  BROSSETTE THIERRY ,  COMPERNOLLE FRANS JOSEF CORNELIUS ,  GUILLAUME MICHEL JOSEPH MAURICE ANDRE ,  MAO HUA ,  KOZLECKI TOMASZ

IPC: C07D307/93 ,  A61K31/34 ,  A61K31/343 ,  A61P25/06 ,  A61P25/22 ,  A61P25/24 ,  A61P25/28 ,  A61P25/30

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.