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公开(公告)号：WO2008100601A3
公开(公告)日：2008-11-20
申请号：PCT/US2008002055
申请日：2008-02-15
Applicant: PROCTER & GAMBLE , SMETS JOHAN , VANSTEENWINCKEL PASCALE CLAIRE ANNICK , ARNAUT PIET ANDRE AN , VANRAES DAVID ARMAND JOSEPH , ENGELS CHRISTIAAN , METTEN BERT DENIS FERDINAND , MESSALI MOUSLIM , HARIRI MOUAFFAK AL , HOORNAERT GEORGES JOSEPH CORNELIUS
Inventor： SMETS JOHAN , VANSTEENWINCKEL PASCALE CLAIRE ANNICK , ARNAUT PIET ANDRE AN , VANRAES DAVID ARMAND JOSEPH , ENGELS CHRISTIAAN , METTEN BERT DENIS FERDINAND , MESSALI MOUSLIM , HARIRI MOUAFFAK AL , HOORNAERT GEORGES JOSEPH CORNELIUS
Abstract: Benefit agent delivery compositions, compositions, packaged products and displays comprising such benefit agent delivery compositions, and processes for making and using such benefit agent delivery compositions, compositions, packaged products and displays. Such compositions have improved deposition and retention properties that may impart improved benefit characteristics to a composition and/or situs.
Abstract translation: 包含此类有益剂递送组合物的有益剂递送组合物，组合物，包装产品和展示品，以及制造和使用此类有益剂递送组合物，组合物，包装产品和展示品的方法。 这种组合物具有改善的沉积和保留性能，可以赋予组合物和/或部位改善的有益特性。
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公开(公告)号：WO2006015985A1
公开(公告)日：2006-02-16
申请号：PCT/EP2005/053936
申请日：2005-08-10
Applicant: JANSSEN PHARMACEUTICA N.V. , ARTS, Frank, Xavier, Jozef, Herwig , HOORNAERT, Georges, Joseph, Cornelius , KILONDA, Amuri , HEERES, Jan , LEWI, Paulus, Joannes , DE JONGE, Marc, René , DAEYAERT, Frederik, Frans, Desiré , VINKERS, Hendrik, Maarten , KOYMANS, Lucien, Maria, Henricus
Inventor： HOORNAERT, Georges, Joseph, Cornelius , KILONDA, Amuri , HEERES, Jan , LEWI, Paulus, Joannes , DE JONGE, Marc, René , DAEYAERT, Frederik, Frans, Desiré , VINKERS, Hendrik, Maarten , KOYMANS, Lucien, Maria, Henricus
IPC: C07D253/06
CPC classification number: C07D253/075
Abstract: The present invention relates to HIV replication inhibitors of formula (I) a N -oxide, a pharmaceutically acceptable addition salt, a quaternary amine or a stereochemically isomeric form thereof, wherein ring A and ring B represent phenyl, pyridyl, pyridazinyl, pyrimidinyl or pyrazinyl; n and m are 1 to 4; R 1 represents hydrogen; aryl; formyl; C 1-6 alkylcarbonyl; C 1-6 alkyloxycarbonyl; optionally substituted C 1-6 alkyl; C 1-6 alkyloxy C 1-6 alkylcarbonyl substituted with C 1-6 alkyloxycarbonyl; their use as a medicine, their use for the manufacture of a medicament for the treatment or the prevention of HIV infection; their processes for preparation and pharmaceutical compositions comprising them.
Abstract translation: 本发明涉及式（I）的HIV复制抑制剂a
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公开(公告)号：WO2008100601A2
公开(公告)日：2008-08-21
申请号：PCT/US2008/002055
申请日：2008-02-15
Applicant: THE PROCTER & GAMBLE COMPANY , SMETS, Johan , VANSTEENWINCKEL, Pascale, Claire Annick , ARNAUT, Piet, Andre An , VANRAES, David, Armand Joseph , ENGELS, Christiaan , METTEN, Bert, Denis Ferdinand , MESSALI, Mouslim , HARIRI, Mouaffak, Al , HOORNAERT, Georges, Joseph Cornelius
Inventor： SMETS, Johan , VANSTEENWINCKEL, Pascale, Claire Annick , ARNAUT, Piet, Andre An , VANRAES, David, Armand Joseph , ENGELS, Christiaan , METTEN, Bert, Denis Ferdinand , MESSALI, Mouslim , HARIRI, Mouaffak, Al , HOORNAERT, Georges, Joseph Cornelius
Abstract: Benefit agent delivery compositions, compositions, packaged products and displays comprising such benefit agent delivery compositions, and processes for making and using such benefit agent delivery compositions, compositions, packaged products and displays. Such compositions have improved deposition and retention properties that may impart improved benefit characteristics to a composition and/or situs.
Abstract translation: 包含这种有益剂递送组合物的益处药递送组合物，组合物，包装产品和显示器，以及用于制备和使用这些有益试剂递送组合物，组合物，包装产品和显示器的方法。 这样的组合物具有改善的沉积和保留性能，其可赋予组合物和/或部位改善的益处特征。
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4.发明申请NOVEL SUBSTITUTED TETRACYCLIC TETRAHYDROFURAN, PYRROLIDINE AND TETRAHYDROTHIOPHENE DERIVATIVES AND THEIR USE AS A MEDICAMENT 审中-公开新型取代的四氢四氢呋喃，吡咯烷和四氢苯并噻吩衍生物及其作为药物的用途
公开(公告)号：WO2006125812A1
公开(公告)日：2006-11-30
申请号：PCT/EP2006/062612
申请日：2006-05-24
Applicant: JANSSEN PHARMACEUTICA N.V. , MEGENS, Antonius, Adrianus, Hendrikus, Petrus , TRABANCO-SUÁREZ, Andrés, Avelino , KOUKNI, Mohamed , HOORNAERT, Georges, Joseph, Cornelius , COMPERNOLLE, Frans, Josef, Cornelius , KOZLECKI, Tomasz , CID-NÚÑEZ, José, Maria , MAO, Hua , JHA, Sushil, Chandra , FERNÁNDEZ-GADEA, Francisco, Javier
Inventor： MEGENS, Antonius, Adrianus, Hendrikus, Petrus , TRABANCO-SUÁREZ, Andrés, Avelino , KOUKNI, Mohamed , HOORNAERT, Georges, Joseph, Cornelius , COMPERNOLLE, Frans, Josef, Cornelius , KOZLECKI, Tomasz , CID-NÚÑEZ, José, Maria , MAO, Hua , JHA, Sushil, Chandra , FERNÁNDEZ-GADEA, Francisco, Javier
IPC: C07D487/04 , C07D209/94 , C07D491/04 , C07D333/80 , C07D311/94 , C07D221/18 , C07D307/93 , A61K31/403 , A61K31/407 , A61P25/00
CPC classification number: C07D209/94 , C07D221/18 , C07D307/93 , C07D311/94 , C07D333/80 , 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-氧化物形式和其前药，其中所有取代基被定义 如权利要求1所述。
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Patent Agency Ranking
公开(公告)号：WO2004074266A1
公开(公告)日：2004-09-02
申请号：PCT/EP2004/050084
申请日：2004-02-05
Applicant: JANSSEN PHARMACEUTICA N.V. , ARTS, Theodora, Joanna, Francisca , JANSSEN, Graziella, Maria, Constantina , JANSSEN, Herwig, Josephus, Margareta , JANSSEN, Jasmine, Josée, Werner , JANSSEN, Paul, Peter, Maria , JANSSEN, Maroussia, Godelieve, Frank , LEWI, Paulus, Joannes , DE JONGE, Marc, René , KOYMANS, Lucien, Maria, Henricus , VINKERS, Hendrik, Maarten , DAEYAERT, Frederik, Frans, Desiré , HEERES, Jan , LEENDERS, Ruben, Gerardus, George , HOORNAERT, Georges, Joseph, Cornelius , KILONDA, Amuri , LUDOVICI, Donald, William
Inventor： LEWI, Paulus, Joannes , DE JONGE, Marc, René , KOYMANS, Lucien, Maria, Henricus , VINKERS, Hendrik, Maarten , DAEYAERT, Frederik, Frans, Desiré , HEERES, Jan , LEENDERS, Ruben, Gerardus, George , HOORNAERT, Georges, Joseph, Cornelius , KILONDA, Amuri , LUDOVICI, Donald, William
IPC: C07D253/06
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: 本发明涉及如本说明书中定义的式（I）的HIV复制抑制剂，其用作药物，其制备方法和包含它们的药物组合物。
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公开(公告)号：WO2002078708A1
公开(公告)日：2002-10-10
申请号：PCT/EP2002/002806
申请日：2002-03-13
Applicant: JANSSEN PHARMACEUTICA N.V. , JANSSEN, Paul, Adriaan, Jan , VAN AKEN, Koen, Jeanne, Alfons , LEWI, Paulus, Joannes , KOYMANS, Lucien, Maria, Henricus , DE JONGE, Marc, René , HEERES, Jan , DAEYAERT, Frederik, Frans, Desire , HOORNAERT, Georges, Joseph, Cornelius , COMPERNOLLE, Frans, Josef, Cornelius , KILONDA, Amuri
Inventor： JANSSEN, Paul, Adriaan, Jan , VAN AKEN, Koen, Jeanne, Alfons , LEWI, Paulus, Joannes , KOYMANS, Lucien, Maria, Henricus , DE JONGE, Marc, René , HEERES, Jan , DAEYAERT, Frederik, Frans, Desire , HOORNAERT, Georges, Joseph, Cornelius , COMPERNOLLE, Frans, Josef, Cornelius , KILONDA, Amuri
IPC: A61K31/4965
CPC classification number: C07D241/20
Abstract: This invention concerns compounds of formula (I) a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein R 1-4 and X are as defined in the claims; their use as a medicine for inhibiting HIV replication, their processes for preparation and pharmaceutical compositions comprising them.
Abstract translation: 本发明涉及式（I）的化合物，N-氧化物，药学上可接受的加成盐，季胺及其立体化学异构形式，其中R 1-4和X如权利要求中所定义; 它们用作抑制HIV复制的药物，其制备方法和包含它们的药物组合物。
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7.发明申请NOVEL SUBSTITUTED TETRACYCLIC TETRAHYDROFURAN, PYRROLIDINE AND TETRAHYDROTHIOPHENE DERIVATIVES 审中-公开新型取代的四氢四氢呋喃，吡咯烷和四氢苯并噻吩衍生物
公开(公告)号：WO2006061392A2
公开(公告)日：2006-06-15
申请号：PCT/EP2005/056544
申请日：2005-12-06
Applicant: JANSSEN PHARMACEUTICA N.V. , CID-NÚÑEZ, José, Maria , MEGENS, Antonius, Adrianus, Hendrikus, Petrus , TRABANCO-SUÁREZ, Andrés, Avelino , KOUKNI, Mohamed , HOORNAERT, Georges, Joseph, Cornelius , COMPERNOLLE, Frans, Josef, Cornelius , KOZLECKI, Tomasz , MAO, Hua , JHA, Sushil, Chandra , FERNÁNDEZ-GADEA, Francisco, Javier
Inventor： CID-NÚÑEZ, José, Maria , MEGENS, Antonius, Adrianus, Hendrikus, Petrus , TRABANCO-SUÁREZ, Andrés, Avelino , KOUKNI, Mohamed , HOORNAERT, Georges, Joseph, Cornelius , COMPERNOLLE, Frans, Josef, Cornelius , KOZLECKI, Tomasz , MAO, Hua , JHA, Sushil, Chandra , FERNÁNDEZ-GADEA, Francisco, Javier
IPC: C07D209/70 , C07D221/18 , C07D307/93 , C07D311/94 , C07D333/80 , C07D487/04 , C07D491/044 , A61K31/343 , A61K31/352 , A61K31/381 , A61K31/403 , A61K31/407 , A61K31/496 , A61K31/4188 , A61K31/4985 , A61K31/5377 , A61P25/00
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。
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8.发明申请
公开(公告)号：WO2003048147A3
公开(公告)日：2003-06-12
申请号：PCT/EP2002/013561
申请日：2002-12-02
Applicant: JANSSEN PHARMACEUTICA N.V. , MAO, Hua , KOZLECKI, Tomasz , COMPERNOLLE, Frans, Josef, Cornelius , HOORNAERT, Georges, Joseph, Cornelius
Inventor： MAO, Hua , KOZLECKI, Tomasz , COMPERNOLLE, Frans, Josef, Cornelius , HOORNAERT, Georges, Joseph, Cornelius
IPC: 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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9.发明申请PREPARATION OF TRANS-FUSED 3,3a,8,12b-TETRAHYDRO-2H-DIBENZO[3,4:6,7]CYCLOHEPTA[1,2-b]FURAN DERIVATIVES 审中-公开转化的3,3a，8,12b-四氢-2H-二苯并[3,4：6,7]环庚砜[1,2-b]呋喃衍生物的制备
公开(公告)号：WO2003048146A1
公开(公告)日：2003-06-12
申请号：PCT/EP2002/013560
申请日：2002-12-02
Applicant: JANSSEN PHARMACEUTICA N.V. , LANG, Yolande, Lydia , MEDAER, Bart, Petrus, Anna, Maria, Jozef , HOORNAERT, Georges, Joseph, Cornelius , BROSSETTE, Thierry , COMPERNOLLE, Frans, Josef, Cornelius , GUILLAUME, Michel, Joseph, Maurice, André , MAO, Hua , KOZLECKI, Tomasz
Inventor： LANG, Yolande, Lydia , MEDAER, Bart, Petrus, Anna, Maria, Jozef , HOORNAERT, Georges, Joseph, Cornelius , BROSSETTE, Thierry , COMPERNOLLE, Frans, Josef, Cornelius , GUILLAUME, Michel, Joseph, Maurice, André , MAO, Hua , KOZLECKI, Tomasz
IPC: C07D307/93
CPC classification number: 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.
Abstract translation: 本发明涉及制备式（I）的4种非对映异构体中的每一种的方法：以两种对映异构体纯的前体任一种的立体化学纯的形式。 在酸催化的环化反应中形成具有反式稠合的五元和七元环的四环体系。 本发明还涉及由此获得的顺式稠合四环醇中间体，甲胺终产物，用作药物的甲胺最终产物，特别是CNS活性药物。
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