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1. 发明申请

WO2011051342A8 IMIDAZO[1,2-b]PYRIDAZINE DERIVATIVES AND THEIR USE AS PDE10 INHIBITORS 审中-公开
标题翻译：咪唑并[1,2-b]哒嗪衍生物及其作为PDE10抑制剂的用途
公开(公告)号：WO2011051342A8
公开(公告)日：2011-07-07
申请号：PCT/EP2010066264
申请日：2010-10-27
申请人： JANSSEN PHARMACEUTICA NV , PASTOR-FERNANDEZ JOAQUIN , BARTOLOME-NEBREDA JOSE MANUEL , MACDONALD GREGOR JAMES , CONDE-CEIDE SUSANA , DELGADO-GONZALEZ OSCAR , VANHOOF GRETA CONSTANTIA PETER , VAN GOOL MICHIEL LUC MARIA , MARTIN-MARTIN MARIA LUZ , ALONSO-DE DIEGO SERGIO-ALVAR , SWINNEY KELLY ANN , LEYS CARINA , WEERTS JOHAN ERWIN EDMOND
发明人： PASTOR-FERNANDEZ JOAQUIN , BARTOLOME-NEBREDA JOSE MANUEL , MACDONALD GREGOR JAMES , CONDE-CEIDE SUSANA , DELGADO-GONZALEZ OSCAR , VANHOOF GRETA CONSTANTIA PETER , VAN GOOL MICHIEL LUC MARIA , MARTIN-MARTIN MARIA LUZ , ALONSO-DE DIEGO SERGIO-ALVAR , SWINNEY KELLY ANN , LEYS CARINA , WEERTS JOHAN ERWIN EDMOND
IPC分类号： C07D487/04 , A61K31/5025 , A61P3/00 , A61P25/00
CPC分类号： C07D487/04
摘要： The present invention relates to novel imidazo[1,2-b]pyridazine derivatives which are inhibitors of the phosphodiesterase 10 enzyme (PDE10) and which are useful for the treatment or prevention of neurological, psychiatric and metabolic disorders in which the PDE10 enzyme is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, to the use of such compounds or pharmaceutical compositions for the prevention or treatment of neurological, psychiatric and metabolic disorders and diseases.
摘要翻译：本发明涉及作为磷酸二酯酶10酶（PDE10）抑制剂的新型咪唑并[1,2-b]哒嗪衍生物，其可用于治疗或预防其中涉及PDE10酶的神经病学，精神病学和代谢病症。本发明还涉及包含此类化合物的药物组合物，涉及制备此类化合物和组合物的方法，涉及此类化合物或药物组合物用于预防或治疗神经病学，精神病学和代谢病症和疾病的用途。

2. 发明申请

WO2004056745A2 ADAMANTYL ACETAMIDES AS 11-BETA HYDROXYSTEROID DEHYDROGENASE INHIBITORS 审中-公开
标题翻译： ADAMANTYL ACETAMIDES as 11-BETA HYDROXYSTERIDID DEHYDROGENASE INHIBITORS
公开(公告)号：WO2004056745A2
公开(公告)日：2004-07-08
申请号：PCT/EP2003/051021
申请日：2003-12-16
申请人： JANSSEN PHARMACEUTICA N.V. , LINDERS, Joannes, Theodorus, Maria , WILLEMSENS, Gustaaf, Henri, Maria , GILISSEN, Ronaldus, Arnodus, Hendrika, Joseph , BUYCK, Christophe, Francis, Robert, Nestor , VANHOOF, Greta, Constantia, Peter , VAN DER VEKEN, Louis, Jozef, Elisabeth , JAROSKOVA, Libuse
发明人： LINDERS, Joannes, Theodorus, Maria , WILLEMSENS, Gustaaf, Henri, Maria , GILISSEN, Ronaldus, Arnodus, Hendrika, Joseph , BUYCK, Christophe, Francis, Robert, Nestor , VANHOOF, Greta, Constantia, Peter , VAN DER VEKEN, Louis, Jozef, Elisabeth , JAROSKOVA, Libuse
IPC分类号： C07C233/11
CPC分类号： C07D207/27 , C07C233/11 , C07C233/14 , C07C233/22 , C07C233/23 , C07C233/32 , C07C233/41 , C07C233/58 , C07C235/36 , C07C235/40 , C07C237/20 , C07C237/22 , C07C255/41 , C07C255/57 , C07C271/22 , C07C2601/02 , C07C2601/14 , C07C2601/18 , C07C2601/20 , C07C2602/06 , C07C2602/08 , C07C2602/10 , C07C2602/12 , C07C2602/18 , C07C2602/42 , C07C2602/46 , C07C2603/62 , C07C2603/66 , C07C2603/70 , C07C2603/74 , C07D209/08 , C07D209/18 , C07D213/56 , C07D215/08 , C07D215/48 , C07D217/06 , C07D217/26 , C07D243/08 , C07D257/04 , C07D277/40 , C07D277/48 , C07D295/088 , C07D295/155 , C07D295/185 , C07D309/12 , C07D311/58 , C07D311/64 , C07D317/60 , C07D317/72 , C07D333/24 , C07D333/68 , C07D335/06
摘要： The N -oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n represents an integer being 1 or 2; R 1 and R 2 each independently represents hydrogen C 1-4 alkyl, NR 9 R 10 , C 1-4 alkyloxy; or R 1 and R 2 taken together with the carbon atom with which they are attached form a C 3-6 cycloalkyl; and where n is 2, either R 1 or R 2 may be absent to form an unsaturated bond; R 3 represents a C 6-12 cycloalkyl, preferably selected from cylo-octanyl and cyclohexyl or R 3 represents a monovalent radical having one of the following formulae, wherein said C 6-12 cycloalkyl or monovalent radical may optionally be substituted with one, or where possible two, three or more substituents selected from the group consisting of C 1-4 alkyl, C 1-4 alkyloxy, halo or hydroxy; Q represents Het 1 or Ar 2 wherein said C 3-8 cycloalkyl, Het 1 or Ar 2 are optionally substituted with one or where possible two or more substituents selected from halo, C 1-4 alkyl, C 1-4 alkyloxy, hydroxy, nitro, NR 5 R 6 , C 1-4 alkyloxy substituted with one or where possible two, three or more substituents each independently selected from hydroxycarbonyl, Het 2 and NR 7 R 8 , and C 1-4 alkyl substituted with one or where possible two or three halo substituents, preferably trifluoromethyl; R 5 and R 6 each independently represent hydrogen, C 1-4 alkyl, or C 1-4 alkyl substituted with phenyl; R 1 and R 8 each independently represent hydrogen or C 1-4 alkyl; R 9 and R 10 each independently represent hydrogen, C 1-4 alkyl or C l-4 alkyloxycarbonyl; L represents C 1-4 alkyl; Het 1 represents a heterocycle selected from pyridinyl, thiophenyl, or 1,3-benzodioxolyl; Het 2 represents piperidinyl, pyrrolidinyl or morpholinyl; Ar 2 represents phenyl, naphtyl or indenyl.
摘要翻译： N-氧化物形式，其药学上可接受的加成盐及其立体化学异构形式，其中n表示1或2的整数; R 1和R 2各自独立地表示氢，C 1-4烷基，NR 9 R 10，C 1-4烷氧基，或R 1和R 2与它们所连接的碳原子一起形成C 3-6环烷基; 并且其中n为2时，R 1或R 2可以不存在以形成不饱和键; R 3表示C6-12环烷基，优选选自环辛基和环己基，或R 3表示具有下式之一的一价基团，其中所述C 6-12环烷基或一价基团可任选地被一个或在可能的情况下可能有两个，三个或更多个选自C 1-4烷基，C 1-4烷氧基，卤素或羟基的取代基; Q表示Het 1或Ar 2，其中所述C 3-8环烷基，Het 1或Ar 2任选被一个或可能的两个或多个选自卤素，C 1-4烷基，C 1-4烷氧基，羟基，硝基，NR 5 R 6，被一个或可能的两个，三个或更多个各自独立地选自羟基羰基，Het 2和NR 7 R 8的取代基取代的C 1-4烷氧基，和C 1 被一个或两个或三个卤素取代基取代的4-烷基，优选三氟甲基; R 5和R 6各自独立地表示氢，C 1-4烷基或被苯基取代的C 1-4烷基; R 1和R 8各自独立地表示氢或C 1-4烷基; R 9和R 10各自独立地表示氢，C 1-4烷基或C 1-4烷氧基羰基; L表示C 1-4烷基; Het 1表示选自吡啶基，噻吩基或1,3-苯并二恶唑基的杂环; Het 2表示哌啶基，吡咯烷基或吗啉基; Ar 2表示苯基，萘基或茚基。

3. 发明申请

WO2011110545A1 IMIDAZO [1, 2 -A] PYRAZINE DERIVATIVES AND THEIR USE FOR THE PREVENTION OR TREATMENT OF NEUROLOGICAL, PSYCHIATRIC AND METABOLIC DISORDERS AND DISEASES 审中-公开
标题翻译：咪唑并[1,2-A]吡嗪衍生物及其用于预防或治疗神经，心理和代谢障碍和疾病的用途
公开(公告)号：WO2011110545A1
公开(公告)日：2011-09-15
申请号：PCT/EP2011/053445
申请日：2011-03-08
申请人： JANSSEN PHARMACEUTICA NV , BARTOLOMÉ-NEBREDA, José, Manuel , CONDE-CEIDE, Susana , MACDONALD, Gregor, James , PASTOR-FERNÁNDEZ, Joaquin , VAN GOOL, Michiel, Luc, Maria , MARTÍN-MARTÍN, María, Luz , VANHOOF, Greta, Constantia, Peter
发明人： BARTOLOMÉ-NEBREDA, José, Manuel , CONDE-CEIDE, Susana , MACDONALD, Gregor, James , PASTOR-FERNÁNDEZ, Joaquin , VAN GOOL, Michiel, Luc, Maria , MARTÍN-MARTÍN, María, Luz , VANHOOF, Greta, Constantia, Peter
IPC分类号： C07D487/04 , A61K31/4985 , A61P3/00 , A61P25/00
CPC分类号： C07D487/04 , A61K31/5377
摘要： The present invention relates to novel imidazo[1,2-a]pyrazine derivatives which are inhibitors of the phosphodiesterase 10 enzyme (PDE10) and which are useful for the treatment or prevention of neurological, psychiatric and metabolic disorders in which the PDE10 enzyme is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, to the use of such compounds or pharmaceutical compositions for the prevention or treatment of neurological, psychiatric and metabolic disorders and diseases.
摘要翻译：本发明涉及作为磷酸二酯酶10酶（PDE10）的抑制剂的新的咪唑并[1,2-a]吡嗪衍生物，其可用于治疗或预防涉及PDE10酶的神经，精神和代谢紊乱。本发明还涉及包含这些化合物的药物组合物，以制备这些化合物和组合物以使用这些化合物或药物组合物来预防或治疗神经，精神和代谢疾病和疾病。

4. 发明申请

WO2011051342A1 IMIDAZO[1,2-b]PYRIDAZINE DERIVATIVES AND THEIR USE AS PDE10 INHIBITORS 审中-公开
标题翻译：咪唑并[1,2-b]吡啶衍生物及其用作PDE10抑制剂
公开(公告)号：WO2011051342A1
公开(公告)日：2011-05-05
申请号：PCT/EP2010/066264
申请日：2010-10-27
申请人： JANSSEN PHARMACEUTICA NV , PASTOR-FERNÁNDEZ, Joaquin , BARTOLOMÉ-NEBREDA, José, Manuel , MACDONALD, Gregor, James , CONDE-CEIDE, Susana , DELGADO-GONZÁLEZ, Óscar , VANHOOF, Greta, Constantia, Peter , VAN GOOL, Michiel, Luc, Maria , MARTÍN-MARTÍN, María, Luz , ALONSO-DE DIEGO, Sergio-Alvar
发明人： PASTOR-FERNÁNDEZ, Joaquin , BARTOLOMÉ-NEBREDA, José, Manuel , MACDONALD, Gregor, James , CONDE-CEIDE, Susana , DELGADO-GONZÁLEZ, Óscar , VANHOOF, Greta, Constantia, Peter , VAN GOOL, Michiel, Luc, Maria , MARTÍN-MARTÍN, María, Luz , ALONSO-DE DIEGO, Sergio-Alvar
IPC分类号： C07D487/04 , A61K31/5025 , A61P3/00 , A61P25/00
CPC分类号： C07D487/04
摘要： The present invention relates to novel imidazo[1,2-b]pyridazine derivatives which are inhibitors of the phosphodiesterase 10 enzyme (PDE10) and which are useful for the treatment or prevention of neurological, psychiatric and metabolic disorders in which the PDE10 enzyme is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, to the use of such compounds or pharmaceutical compositions for the prevention or treatment of neurological, psychiatric and metabolic disorders and diseases.
摘要翻译：本发明涉及作为磷酸二酯酶10酶（PDE10）的抑制剂的新的咪唑并[1,2-b]哒嗪衍生物，其可用于治疗或预防涉及PDE10酶的神经，精神和代谢紊乱。本发明还涉及包含这些化合物的药物组合物，以制备这些化合物和组合物以使用这些化合物或药物组合物来预防或治疗神经，精神和代谢疾病和疾病。

5. 发明申请

WO2004056744A1 ADAMANTYL ACETAMIDES AS HYDROXYSTEROID DEHYDROGENASE INHIBITORS 审中-公开
标题翻译：作为羟肟酸脱氢酶抑制剂的ADAMANTYL ACETAMIDES
公开(公告)号：WO2004056744A1
公开(公告)日：2004-07-08
申请号：PCT/EP2002/014832
申请日：2002-12-23
申请人： JANSSEN PHARMACEUTICA N.V. , LINDERS, Joannes, Theodorus, Maria , WILLEMSENS, Gustaaf, Henri, Maria , GILISSEN, Ronaldus, Arnodus, Hendrika, Joseph , BUYCK, Christophe, Francis, Robert, Nestor , VANHOOF, Greta, Constantia, Peter , VAN DER VEKEN, Louis, Jozef, Elisabeth , JAROSKOVA, Libuse
发明人： LINDERS, Joannes, Theodorus, Maria , WILLEMSENS, Gustaaf, Henri, Maria , GILISSEN, Ronaldus, Arnodus, Hendrika, Joseph , BUYCK, Christophe, Francis, Robert, Nestor , VANHOOF, Greta, Constantia, Peter , VAN DER VEKEN, Louis, Jozef, Elisabeth , JAROSKOVA, Libuse
IPC分类号： C07C233/11
CPC分类号： C07D207/27 , C07C233/11 , C07C233/14 , C07C233/22 , C07C233/23 , C07C233/32 , C07C233/41 , C07C233/58 , C07C235/36 , C07C235/40 , C07C237/20 , C07C237/22 , C07C255/41 , C07C255/57 , C07C271/22 , C07C2601/02 , C07C2601/14 , C07C2601/18 , C07C2601/20 , C07C2602/06 , C07C2602/08 , C07C2602/10 , C07C2602/12 , C07C2602/18 , C07C2602/42 , C07C2602/46 , C07C2603/62 , C07C2603/66 , C07C2603/70 , C07C2603/74 , C07D209/08 , C07D209/18 , C07D213/56 , C07D215/08 , C07D215/48 , C07D217/06 , C07D217/26 , C07D243/08 , C07D257/04 , C07D277/40 , C07D277/48 , C07D295/088 , C07D295/155 , C07D295/185 , C07D309/12 , C07D311/58 , C07D311/64 , C07D317/60 , C07D317/72 , C07D333/24 , C07D333/68 , C07D335/06
摘要： formulae (I)the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n represents an integer being 1 or 2; R 1 and R 2 each independently represents hydrogen C 1-4 alkyl, NR 9 R 10 , C 1-4 alkyloxy; or R 1 and R 2 taken together with the carbon atom with which they are attached form a C 3-6 cycloalkyl; and where n is 2, either R 1 or R 2 may be absent to form an unsaturated bond; R 3 represents a C 6-12 cycloalkyl, preferably selected from cylo-octanyl and cyclohexyl or R 3 represents a monovalent radical having one of the following formulae(a) (b) (c) (l) (q) (r) (g) (u) (o) (w) (j) (k) (t) wherein said C 6-12 cycloalkyl or monovalent radical may optionally be substituted with one, or where possible two, three or more substituents selected from the group consisting of C 1-4 alkyl, C 1-4 alkyloxy, halo or hydroxy; Q represents Het 1 or Ar 2 wherein said C 3-8 cycloalkyl, Het 1 or Ar 2 are optionally substituted with one or where possible two or more substituents selected from halo, C 1-4 alkyl, C 1-4 alkyloxy, hydroxy, nitro, NR 5 R 6 , C 1-4 alkyloxy substituted with one or where possible two, three or more substituents each independently selected from hydroxycarbonyl, Het 2 and NR 7 R 8 , and C 1-4 alkyl substituted with one or where possible two or three halo substituents, preferably trifluoromethyl; R 5 and R 6 each independently represent hydrogen, C 1-4 alkyl, or C 1-4 alkyl substituted with phenyl; R 7 and R 8 each independently represent hydrogen or C 1-4 alkyl; R 9 and R 10 ? each independently represent hydrogen, C 1-4 alkyl or C 1-4 alkyloxycarbonyl; L represents C 1-4 alkyl; Het 1 represents a heterocycle selected from pyridinyl, thiophenyl, or 1,3-benzodioxolyl; Het 2 represents piperidinyl, pyrrolidinyl or morpholinyl; Ar 2 represents phenyl, naphtyl or indenyl.
摘要翻译：式（I）N-氧化物形式，其药学上可接受的加成盐和立体化学异构形式，其中n表示1或2的整数; R 1和R 2各自独立地表示氢C 1-4烷基，NR 9 R 10，C 1-4烷氧基，或R 1和R 2与它们所连接的碳原子一起形成C 3-6环烷基; 并且其中n为2时，R 1或R 2可以不存在以形成不饱和键; R 3表示C 12-12环烷基，优选选自环辛基和环己基，或R 3表示具有下式（a）（b）（c）（1）（q）（r））（g）（u）（o）（w）（j）（k）（t）其中所述C 6-12环烷基或一价基团可以任选地被一个或可能的两个，三个或更多个选自由C 1-4烷基，C 1-4烷氧基，卤素或羟基组成; Q表示Het 1或Ar 2，其中所述C 3-8环烷基，Het 1或Ar 2任选被一个或可能的两个或多个选自卤素，C 1-4烷基，C 1-4烷氧基，羟基，硝基，NR 5 R 6，被一个或可能的两个，三个或更多个各自独立地选自羟基羰基，Het 2和NR 7 R 8的取代基取代的C 1-4烷氧基，和C 1 被一个或两个或三个卤素取代基取代的4-烷基，优选三氟甲基; R 5和R 6各自独立地表示氢，C 1-4烷基或被苯基取代的C 1-4烷基; R 7和R 8各自独立地表示氢或C 1-4烷基; R 9和R 10各自独立地表示氢，C 1-4烷基或C 1-4烷氧基羰基; L表示C 1-4烷基; Het 1表示选自吡啶基，噻吩基或1,3-苯并二恶唑基的杂环; Het 2表示哌啶基，吡咯烷基或吗啉基; Ar 2表示苯基，萘基或茚基。

6. 发明申请

WO2013000924A1 1-ARYL-4-METHYL-[1,2,4]TRIAZOLO[4,3-a]QUINOXALINE DERIVATIVES 审中-公开
标题翻译： 1-芳基-4-甲基 - [1,2,4]三唑并[4,3-a]喹啉衍生物
公开(公告)号：WO2013000924A1
公开(公告)日：2013-01-03
申请号：PCT/EP2012/062381
申请日：2012-06-26
申请人： JANSSEN PHARMACEUTICA NV , ANDRÉS-GIL, José, Ignacio , ROMBOUTS, Frederik, Jan, Rita , TRABANCO-SUÁREZ, Andrés, Avelino , VANHOOF, Greta, Constantia, Peter , DE ANGELIS, Meri , BUIJNSTERS, Peter, Jacobus, Johannes, Antonius , GUILLEMONT, Jerôme, Emile, Georges , BORMANS, Guy, Maurits R. , CELEN, Sofie, Jeanne, Leopoldine , VLIEGEN, Maarten
发明人： ANDRÉS-GIL, José, Ignacio , ROMBOUTS, Frederik, Jan, Rita , TRABANCO-SUÁREZ, Andrés, Avelino , VANHOOF, Greta, Constantia, Peter , DE ANGELIS, Meri , BUIJNSTERS, Peter, Jacobus, Johannes, Antonius , GUILLEMONT, Jerôme, Emile, Georges , BORMANS, Guy, Maurits R. , CELEN, Sofie, Jeanne, Leopoldine , VLIEGEN, Maarten
IPC分类号： C07D487/04 , A61K31/4985 , A61P25/00
CPC分类号： C07D487/04 , A61K31/4985 , A61K45/06 , A61K51/0463 , G01N33/60
摘要： The present invention relates to novel l-aryl-4-methyl-[l,2,4]triazolo[4,3-a]- quinoxaline derivatives as inhibitors of phosphodiesterase 2 (PDE2) and to a lesser extent of phosphodiesterase 10 (PDE10) or as inhibitors of both, phosphodiesterases 2 and 10. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which PDE2 is involved, or disorders in which both PDE2 and PDE10 are involved, such as neurological and psychiatric disorders, and endocrinological or metabolic diseases. The present invention also relates to radiolabeled compounds which may be useful for imaging and quantifying the PDE2 enzyme in tissues, using positron- emission tomography (PET). The invention is also directed to compositions comprising such compounds, to processes for preparing such compounds and compositions, to the use of such compounds and compositions for imaging a tissue, cells or a host, in vitro or in vivo and to precursors of said compounds.
摘要翻译：本发明涉及新的1-芳基-4-甲基 - [1,2,4]三唑并[4,3-a] - 喹喔啉衍生物作为磷酸二酯酶2（PDE2）的抑制剂，而较少程度的磷酸二酯酶10（PDE10 ）或作为磷酸二酯酶2和10两者的抑制剂。本发明还涉及包含这些化合物的药物组合物，制备此类化合物和组合物的方法，以及用于预防和治疗疾病的化合物和组合物其中涉及PDE2，或PDE2和PDE10都涉及的疾病，如神经和精神疾病，以及内分泌或代谢疾病。本发明还涉及放射性标记的化合物，其可用于使用正电子发射断层摄影（PET）在组织中成像和定量PDE2酶。本发明还涉及包含这些化合物的组合物，用于制备此类化合物和组合物的方法，以使用这些化合物和组合物用于在体外或体内成像组织，细胞或宿主以及所述化合物的前体。

7. 发明申请

WO2005089753A3 DAAO INHIBITING B?NZISOXAZOLES AND THEIR USE FOR THE TREATMENT OF MENTAL DISORDERS 审中-公开
标题翻译： DAAO抑制B？NZISOXAZOLES及其用于治疗精神疾病的用途
公开(公告)号：WO2005089753A3
公开(公告)日：2006-11-30
申请号：PCT/EP2005051105
申请日：2005-03-11
申请人： JANSSEN PHARMACEUTICA NV , KENNIS LUDO EDMOND JOSEPHINE , VANHOOF GRETA CONSTANTIA PETER , BONGARTZ JEAN-PIERRE ANDRE MAR , LUYCKX MARCEL GEREBERNUS MARIA , MINKE WENDA EVELINE
发明人： KENNIS LUDO EDMOND JOSEPHINE , VANHOOF GRETA CONSTANTIA PETER , BONGARTZ JEAN-PIERRE ANDRE MAR , LUYCKX MARCEL GEREBERNUS MARIA , MINKE WENDA EVELINE
IPC分类号： A61K31/423 , A61P25/18 , C07D261/20 , C07D413/12
CPC分类号： A61K31/423 , A61K31/42 , A61K31/425 , A61K31/426 , A61K31/428 , C07D261/20
摘要： The present invention concerns the compounds of formula (I) , the substituents being specified in the description, (I) the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemical Iy isomeric forms thereof , and their use for the manufacture of a medicament for the treatment of mental disorders, preferably schizophrenia.
摘要翻译：本发明涉及式（I）化合物，其描述中指定的取代基，（I）N-氧化物形式，其药学上可接受的加成盐和立体化学异构体形式及其在制备用于治疗精神障碍，优选精神分裂症的药物。

8. 发明申请

WO2005089753A2 BENZISOXAZOLES 审中-公开
标题翻译：苯并异恶唑
公开(公告)号：WO2005089753A2
公开(公告)日：2005-09-29
申请号：PCT/EP2005/051105
申请日：2005-03-11
申请人： JANSSEN PHARMACEUTICA N.V. , KENNIS, Ludo, Edmond, Josephine , VANHOOF, Greta, Constantia, Peter , BONGARTZ, Jean-Pierre, André, Marc , LUYCKX, Marcel, Gerebernus, Maria , MINKE, Wenda, Eveline
发明人： KENNIS, Ludo, Edmond, Josephine , VANHOOF, Greta, Constantia, Peter , BONGARTZ, Jean-Pierre, André, Marc , LUYCKX, Marcel, Gerebernus, Maria , MINKE, Wenda, Eveline
IPC分类号： A61K31/423
CPC分类号： A61K31/423 , A61K31/42 , A61K31/425 , A61K31/426 , A61K31/428 , C07D261/20
摘要： The present invention concerns the compounds of formula (I), the N -oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein m represents an integer from 1 to 3; X represents amino, hydroxy, -oxo or -Z-R 1 ; Y is absent when X represents -Z-R 1 and -(C=O)-R 6 when X represents oxo; Z represents carbonyl, -oxy-carbonyl- or -NR 5 -carbonyl-; R 1 represents C 1 - 4 alkyl, Ar 1 , Ar 1 -C 1-4 a1ky1-, -NR 3 R 4 or -Het 1 ; R 2 represents hydrogen, halo, nitro, hydroxycarbonyl-, C 1-4 alkyloxy or C 1-4 alkyl; R 3 and R 4 are each independently selected from hydrogen, Ar 3 or C 1-4 alkyl; R 5 represents hydrogen, C 1-4 alkylcarbonyl- or Ar 4 -carbonyl-; R 6 represents a substituent selected from the group consisting of C 1 . 4 alkyl, Ar 5 , Ar 6 -C 1-4 alkyl- or NR 7 R 8 ; R 7 and R 8 are each independently selected from hydrogen, Het 4 or C 1-4 alkyl; Het 1 represents a heterocycle selected from oxazolyl, isoxazolyl, imidazolyl or pyrazolyl wherein said heterocycle is optionally substituted with one, two or three substituents selected from the group consisting of amino, C 1-4 alkyl, hydroxy-C 1-4 alkyl, phenyl, phenyl-C 1-4 alkyl- and phenyl substituted with one or more halo substituents; Het 4 represents a heterocycle selected from oxazolyl or isoxazolyl, wherein said heterocycle is optionally substituted with one or more substituents selected from the group consisting of amino, C 1-4 alkyl, hydroxy-C 1-4 alkyl-, phenyl, phenyl-C l-4 alkyl and phenyl substituted with one or more halo substituents; and Ar 1 , Ar 2 , Ar 3 , Ar 4 , Ar 5 or Ar 6 each independently represents phenyl optionally substituted one or where possible two or more substituents selected from halo, nitro, C 1-4 alkyl, hydroxy or C 1-4 alkyloxy-.
摘要翻译：本发明涉及式（I）化合物，N-氧化物形式，其药学上可接受的加成盐和立体化学异构形式，其中m表示1至3的整数; X代表氨基，羟基，-oxo或-Z-R 1; 当X表示氧代时，当X表示-Z-R 1和 - （C = O）-R 6时，Y不存在; Z表示羰基， - 氧基 - 羰基 - 或-NR 5 - 羰基 - ; R 1表示C 1-4烷基，Ar 1，Ar 1 -C 1-4烷基，-NR 3 R 4或-Het 1; R 2表示氢，卤素，硝基，羟基羰基 - ，C 1-4烷氧基或C 1-4烷基; R 3和R 4各自独立地选自氢，Ar 3或C 1-4烷基; R 5表示氢，C 1-4烷基羰基 - 或Ar 4 - 羰基 - ; R 6表示选自C 1-4烷基，Ar 5，Ar 6 -C 1-4烷基或NR 7 R 8中的取代基。 R 7和R 8各自独立地选自氢，Het 4或C 1-4烷基; Het 1表示选自恶唑基，异恶唑基，咪唑基或吡唑基的杂环，其中所述杂环任选被一个，两个或三个选自以下的取代基取代：氨基，C 1-4烷基，羟基-C 1-4烷基，苯基，苯基 C 1-4烷基 - 和被一个或多个卤素取代基取代的苯基; Het 4表示选自恶唑基或异恶唑基的杂环，其中所述杂环任选被一个或多个选自以下的取代基取代：氨基，C 1-4烷基，羟基-C 1-4烷基 - ，苯基，苯基-C 1-4烷基和被一个或多个卤素取代基取代的苯基; Ar 1，Ar 2，Ar 3，Ar 4，Ar 5或Ar 6各自独立地表示任选被取代的苯基，或者可能的两个或多个选自卤素，硝基， C 1-4烷基，羟基或C 1-4烷氧基。

9. 发明申请

WO2004056745A3 ADAMANTYL ACETAMIDES AS 11-BETA HYDROXYSTEROID DEHYDROGENASE INHIBITORS 审中-公开
标题翻译：作为11-β羟基类固醇脱氢酶抑制剂的酰胺乙酰胺
公开(公告)号：WO2004056745A3
公开(公告)日：2004-11-11
申请号：PCT/EP0351021
申请日：2003-12-16
申请人： JANSSEN PHARMACEUTICA NV , LINDERS JOANNES THEODORUS MARI , WILLEMSENS GUSTAAF HENRI MARIA , GILISSEN RONALDUS ARNODUS HEND , BUYCK CHRISTOPHE FRANCIS ROBER , VANHOOF GRETA CONSTANTIA PETER , VAN DER VEKEN LOUIS JOZEF ELIS , JAROSKOVA LIBUSE
发明人： LINDERS JOANNES THEODORUS MARI , WILLEMSENS GUSTAAF HENRI MARIA , GILISSEN RONALDUS ARNODUS HEND , BUYCK CHRISTOPHE FRANCIS ROBER , VANHOOF GRETA CONSTANTIA PETER , VAN DER VEKEN LOUIS JOZEF ELIS , JAROSKOVA LIBUSE
IPC分类号： A61K31/165 , A61K31/335 , A61K31/40 , A61K31/44 , A61P3/04 , A61P3/10 , C07C233/11 , C07C233/14 , C07C233/22 , C07C233/23 , C07C233/32 , C07C233/41 , C07C233/58 , C07C235/36 , C07C235/40 , C07C237/20 , C07C237/22 , C07C255/41 , C07C255/57 , C07C271/22 , C07D207/12 , C07D207/26 , C07D207/27 , C07D209/08 , C07D209/18 , C07D213/56 , C07D215/08 , C07D215/48 , C07D217/06 , C07D217/26 , C07D243/08 , C07D257/04 , C07D277/40 , C07D277/48 , C07D295/088 , C07D295/092 , C07D295/155 , C07D295/185 , C07D309/12 , C07D311/58 , C07D311/64 , C07D317/60 , C07D317/72 , C07D333/24 , C07D333/68 , C07D335/06
CPC分类号： C07D207/27 , C07C233/11 , C07C233/14 , C07C233/22 , C07C233/23 , C07C233/32 , C07C233/41 , C07C233/58 , C07C235/36 , C07C235/40 , C07C237/20 , C07C237/22 , C07C255/41 , C07C255/57 , C07C271/22 , C07C2601/02 , C07C2601/14 , C07C2601/18 , C07C2601/20 , C07C2602/06 , C07C2602/08 , C07C2602/10 , C07C2602/12 , C07C2602/18 , C07C2602/42 , C07C2602/46 , C07C2603/62 , C07C2603/66 , C07C2603/70 , C07C2603/74 , C07D209/08 , C07D209/18 , C07D213/56 , C07D215/08 , C07D215/48 , C07D217/06 , C07D217/26 , C07D243/08 , C07D257/04 , C07D277/40 , C07D277/48 , C07D295/088 , C07D295/155 , C07D295/185 , C07D309/12 , C07D311/58 , C07D311/64 , C07D317/60 , C07D317/72 , C07D333/24 , C07D333/68 , C07D335/06
摘要： The N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n represents an integer being 1 or 2; R and R each independently represents hydrogen C1-4alkyl, NR R , C1-4alkyloxy; or R and R taken together with the carbon atom with which they are attached form a C3-6cycloalkyl; and where n is 2, either R or R may be absent to form an unsaturated bond; R represents a C6-12cycloalkyl, preferably selected from cylo-octanyl and cyclohexyl or R represents a monovalent radical having one of the following formulae, wherein said C6-12cycloalkyl or monovalent radical may optionally be substituted with one, or where possible two, three or more substituents selected from the group consisting of C1-4alkyl, C1-4alkyloxy, halo or hydroxy; Q represents Het or Ar wherein said C3-8cycloalkyl, Het or Ar are optionally substituted with one or where possible two or more substituents selected from halo, C1-4alkyl, C1-4alkyloxy, hydroxy, nitro, NR R , C1-4alkyloxy substituted with one or where possible two, three or more substituents each independently selected from hydroxycarbonyl, Het and NR R , and C1-4alkyl substituted with one or where possible two or three halo substituents, preferably trifluoromethyl; R and R each independently represent hydrogen, C1-4alkyl, or C1-4alkyl substituted with phenyl; R and R each independently represent hydrogen or C1-4alkyl; R9 and R10 each independently represent hydrogen, C1-4alkyl or Cl-4alkyloxycarbonyl; L represents C1-4alkyl; Het represents a heterocycle selected from pyridinyl, thiophenyl, or 1,3-benzodioxolyl; Het represents piperidinyl, pyrrolidinyl or morpholinyl; Ar represents phenyl, naphtyl or indenyl.
摘要翻译： N-氧化物形式，其药学上可接受的加成盐和立体化学异构形式，其中n代表1或2的整数; R 1和R 2各自独立地表示氢C 1-4烷基，NR 9 R 10，C 1-4烷氧基; 或者R 1和R 2与它们所连接的碳原子一起形成C 3-6环烷基; 并且其中n是2时，可以不存在R 1或R 2以形成不饱和键; R 3代表C 6-12环烷基，优选选自环辛基和环己基，或者R 3代表具有下式之一的一价基团，其中所述C 6-12环烷基或一价基团可以任选被一个，或者在可能的情况下两个，三个或更多个选自C 1-4烷基，C 1-4烷氧基，卤素或羟基的取代基; Q代表Het 1或Ar 2，其中所述C 3-8环烷基，Het 1或Ar 2任选被一个或在可能的情况下被两个或更多个选自卤素，C 1-4烷基，C 1-4烷氧基，羟基，硝基，NR 5 R 6，被一个或在可能的情况下被两个，三个或更多个取代基取代的C 1-4烷氧基，所述取代基各自独立地选自羟基羰基，Het 2和NR 7 R 8，以及C1 被一个或在可能的情况下被两个或三个卤素取代基取代的芳基， R 5和R 6各自独立地表示氢，C 1-4烷基或被苯基取代的C 1-4烷基; R 1和R 8各自独立地表示氢或C 1-4烷基; R9和R10各自独立地表示氢，C1-4烷基或C1-4烷氧基羰基; L代表C 1-4烷基; Het 1表示选自吡啶基，噻吩基或1,3-苯并二氧杂环戊烯基的杂环; Het 2代表哌啶基，吡咯烷基或吗啉基; Ar 2代表苯基，萘基或茚基。

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