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1. 发明申请

WO1997044040A1 HEXAHYDRO-PYRIDO(4,3-B)INDOLE DERIVATIVES AS ANTIPSYCHOTIC DRUGS 审中-公开
标题翻译：十六烷基吡啶（4,3-B）吲哚衍生物作为抗生素药物
公开(公告)号：WO1997044040A1
公开(公告)日：1997-11-27
申请号：PCT/EP1997002710
申请日：1997-05-15
申请人： JANSSEN PHARMACEUTICA N.V. , KENNIS, Ludo, Edmond, Josephine , MERTENS, Josephus, Carolus
发明人： JANSSEN PHARMACEUTICA N.V.
IPC分类号： A61K31/505
CPC分类号： C07D471/04
摘要： This invention concerns the compounds of formula (I), the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein Alk is C1-6alkanediyl; R is hydrogen, C1-6alkyl, aryl or arylC1-6alkyl; R , R and R are each independently selected from hydrogen, halo, hydroxy, nitro, cyano, C1-6alkyl, C1-6alkyloxy, trifluoromethyl, C1-6alkylthio, mercapto, amino, mono- and di(C1-6alkyl)amino, carboxyl, C1-6alkyloxycarbonyl or C1-6alkylcarbonyl; R is hydrogen, C1-6alkyl, phenyl or phenylC1-6alkyl; R is hydrogen, C1-6alkyl, C1-6alkyloxy, C1-6alkylthio, or a radical of formula -NR R , wherein R and R are each independently selected from hydrogen, C1-6alkyl, phenyl or phenylC1-6alkyl; R is hydrogen or C1-6alkyl; or R and R taken together may form a bivalent radical of formula -R -R -; having central dopamine and serotonin antagonistic activity; their preparation, compositions containing them and their use as a medecine.
摘要翻译：本发明涉及式（I）化合物，其药学上可接受的加成盐和立体化学异构形式，其中Alk是C1-6烷二基; R 1是氢，C 1-6烷基，芳基或芳基C 1-6烷基; R 2，R 3和R 4各自独立地选自氢，卤素，羟基，硝基，氰基，C 1-6烷基，C 1-6烷氧基，三氟甲基，C 1-6烷硫基，巯基，氨基，单 - 和二（C 1-6烷基）氨基，羧基，C 1-6烷氧基羰基或C 1-6烷基羰基; R 5是氢，C 1-6烷基，苯基或苯基C 1-6烷基; R 6是氢，C 1-6烷基，C 1-6烷氧基，C 1-6烷硫基或式-NR 8 R 9基团，其中R 8和R 9各自独立地选自氢，C 1-6烷基，苯基或苯基C 1-6烷基; R 7是氢或C 1-6烷基; 或R 6和R 7一起可以形成式-R 6 -R 7 - 的二价基团; 具有中枢多巴胺和5-羟色胺拮抗活性; 它们的制备，含有它们的组合物及其作为药物的用途。

2. 发明申请

WO2006003147A1 PHTHALAZINE DERIVATIVES AS PARP INHIBITORS 审中-公开
标题翻译：苯乙烯衍生物作为PARP抑制剂
公开(公告)号：WO2006003147A1
公开(公告)日：2006-01-12
申请号：PCT/EP2005/053030
申请日：2005-06-28
申请人： JANSSEN PHARMACEUTICA N.V. , MEVELLEC, Laurence, Anne , KENNIS, Ludo, Edmond, Josephine , MERTENS, Josephus, Carolus , VAN DUN, Jacobus, Alphonsus, Josephus , SOMERS, Maria, Victorina, Francisca , WOUTERS, Walter, Boudewijn, Leopold
发明人： MEVELLEC, Laurence, Anne , KENNIS, Ludo, Edmond, Josephine , MERTENS, Josephus, Carolus , VAN DUN, Jacobus, Alphonsus, Josephus , SOMERS, Maria, Victorina, Francisca , WOUTERS, Walter, Boudewijn, Leopold
IPC分类号： A61K31/502
CPC分类号： A61K31/55 , A61K31/502 , A61K31/506 , A61K31/517 , A61K31/542 , C07D237/34 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D417/14 , C07D451/04 , C07D471/04 , C07D513/04
摘要： The present invention provides compounds of formula (I), their use as PARP inhibitors as well as pharmaceutical compositions comprising said compounds of formula (I) wherein R 1 , R 2 , L 1 , L 2 , X, Y, Q and Z have defined meanings.
摘要翻译：本发明提供式（I）化合物，其作为PARP抑制剂的用途以及包含所述式（I）化合物的药物组合物，其中R

3. 发明申请

WO2006003146A1 QUINAZOLINONE DERIVATIVES AS PARP INHIBITORS 审中-公开
标题翻译：喹诺酮衍生物作为PARP抑制剂
公开(公告)号：WO2006003146A1
公开(公告)日：2006-01-12
申请号：PCT/EP2005/053029
申请日：2005-06-28
申请人： JANSSEN PHARMACEUTICA N.V. , GUILLEMONT, Jérôme, Emile, Georges , KENNIS, Ludo, Edmond, Josephine , MERTENS, Josephus, Carolus , VAN DUN, Jacobus, Alphonsus, Josephus , SOMERS, Maria, Victorina, Francisca , WOUTERS, Walter, Boudewijn, Leopold
发明人： GUILLEMONT, Jérôme, Emile, Georges , KENNIS, Ludo, Edmond, Josephine , MERTENS, Josephus, Carolus , VAN DUN, Jacobus, Alphonsus, Josephus , SOMERS, Maria, Victorina, Francisca , WOUTERS, Walter, Boudewijn, Leopold
IPC分类号： C07D239/91
CPC分类号： C07D403/12 , A61K31/517 , A61K45/06 , C07D401/12 , C07D401/14 , C07D405/14 , C07D413/14 , C07D417/12 , C07D417/14
摘要： The present invention provides compounds of formula (I), their use as PARP inhibitors as well as pharmaceutical compositions comprising said compounds of formula (I) wherein R 1 , R 2 , R 3 , L, X, Y and Z have defined meanings.
摘要翻译：本发明提供式（I）化合物，它们作为PARP抑制剂的用途以及包含所述式（I）化合物的药物组合物，其中R

4. 发明申请

WO9945011A8 GLYCINE TRANSPORT INHIBITORS 审中-公开
标题翻译：甘氨酸转运抑制剂
公开(公告)号：WO9945011A8
公开(公告)日：1999-10-14
申请号：PCT/EP9901308
申请日：1999-02-26
申请人： JANSSEN PHARMACEUTICA NV , LUYTEN WALTER HERMAN MARIA LOU , JANSSENS FRANS EDUARD , KENNIS LUDO EDMOND JOSEPHINE
发明人： LUYTEN WALTER HERMAN MARIA LOU , JANSSENS FRANS EDUARD , KENNIS LUDO EDMOND JOSEPHINE
IPC分类号： A61K31/4355 , A61K31/4427 , A61K31/443 , A61K31/4433 , A61K31/445 , A61K31/4468 , A61K31/451 , A61K31/4523 , A61K31/4525 , A61K31/454 , A61K31/4545 , A61K31/519 , A61K31/55 , A61P9/10 , A61P25/00 , A61P25/04 , A61P25/08 , A61P25/18 , A61P43/00 , C07D211/14 , C07D211/18 , C07D211/22 , C07D211/30 , C07D211/32 , C07D211/34 , C07D211/48 , C07D211/50 , C07D211/58 , C07D211/62 , C07D211/88 , C07D401/04 , C07D401/06 , C07D401/12 , C07D405/06 , C07D405/14 , C07D409/14 , C07D413/12 , C07D417/04 , C07D417/06 , C07D417/12 , C07D417/14 , C07D471/04 , C07D487/04 , C07D513/04 , A61K31/495
CPC分类号： C07D401/04 , A61K31/451 , A61K31/4523 , A61K31/519 , A61K31/55 , C07D211/14 , C07D211/18 , C07D211/22 , C07D211/30 , C07D211/34 , C07D211/58 , C07D211/88 , C07D401/06 , C07D401/12 , C07D405/06 , C07D405/14 , C07D409/14 , C07D413/12 , C07D417/04 , C07D417/06 , C07D417/12 , C07D417/14 , C07D471/04 , C07D487/04 , C07D513/04
摘要： The present invention is concerned with the use of glycine transport inhibiting alpha , alpha -diphenyl-1-piperidinebutanamides for the preparation of medicaments for treating disorders of the central and peripheral nervous system, in particular psychoses, pain, epilepsy, neurodegenerative diseases (Alzheimer's disease), stroke, head trauma, multiple sclerosis and the like. The invention further comprises novel compounds, their preparation and their pharmaceutical forms.
摘要翻译：本发明涉及甘氨酸转运抑制性α，α-二苯基-1-哌啶丁酰胺在制备用于治疗中枢和外周神经系统疾病，特别是精神病，疼痛，癫痫，神经退行性疾病（阿尔茨海默病），中风，头部创伤，多发性硬化症等。本发明还包括新化合物，它们的制备和它们的药物形式。

5. 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。

6. 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。

7. 发明申请

WO1996023784A1 ANTIPSYCHOTIC 4-(1H-INDOLYL-1-YL)-1-SUBSTITUTED PIPERIDINE DERIVATIVES 审中-公开
标题翻译：抗坏血酸4-（1H-吲哚-1-基）-1-取代的哌啶衍生物
公开(公告)号：WO1996023784A1
公开(公告)日：1996-08-08
申请号：PCT/EP1996000363
申请日：1996-01-23
申请人： JANSSEN PHARMACEUTICA N.V. , VANDENBERK, Jan , KENNIS, Ludo, Edmond, Josephine , MERTENS, Josephus, Carolus
发明人： JANSSEN PHARMACEUTICA N.V.
IPC分类号： C07D401/14
CPC分类号： C07D401/14 , C07D471/04 , C07D487/04 , C07D513/04
摘要： The present invention concerns the compounds of formula (I), the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein the dashed line designates an optional bond; R and R are each independently hydrogen, halogen, C1-6alkyl or C1-6alkyloxy; R and R are each independently hydrogen, C1-6alkyl, phenyl or phenyl substituted with one, two or three substituents selected from halo, hydroxy, nitro, cyano, trifluoromethyl, C1-6alkyl, C1-6alkyloxy, C1-6alkylthio, mercapto, amino, mono- and di(C1-6alkyl)-amino, carboxyl, C1-6alkyloxycarbonyl and C1-6alkylcarbonyl; Alk is C1-4alkanediyl; D is a pyrimidinone, piperidone or a benzimidozolidinone; having antipsychotic activity; their preparation, compositions containing them and their use as a medicine.
摘要翻译：本发明涉及式（I）化合物，其药学上可接受的加成盐和立体化学异构形式，其中虚线表示任选的键; R 1和R 2各自独立地为氢，卤素，C 1-6烷基或C 1-6烷氧基; R 3和R 4各自独立地为氢，C 1-6烷基，苯基或被一个，两个或三个取代基取代的苯基，所述取代基选自卤素，羟基，硝基，氰基，三氟甲基，C 1-6烷基，C 1-6烷氧基，C 1 巯基，氨基，单和二（C 1-6烷基） - 氨基，羧基，C 1-6烷氧基羰基和C 1-6烷基羰基; Alk是C1-4烷二基; D是嘧啶酮，哌啶酮或苯甲酰胺唑烷酮; 具有抗精神病活性; 其制剂，含有它们的组合物及其作为药物的用途。

8. 发明申请

WO1994001437A1 NOVEL 4-(3-BENZOFURANYL)PIPERIDINYL AND 4-(3-BENZOTHIENYL)PIPERIDINYL DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 审中-公开
标题翻译：新型4-（3-苯并呋喃）哌嗪和4-（3-苄基苯基）哌啶衍生物和含有它们的药物组合物
公开(公告)号：WO1994001437A1
公开(公告)日：1994-01-20
申请号：PCT/EP1993001776
申请日：1993-07-06
申请人： JANSSEN PHARMACEUTICA N.V. , VANDENBERK, Jan , KENNIS, Ludo, Edmond, Josephine , VAN HEERTUM, Albertus, Henricus, Maria, Theresia
发明人： JANSSEN PHARMACEUTICA N.V.
IPC分类号： C07D471/04
CPC分类号： C07D513/04 , A61K31/517 , A61K31/519 , C07D471/04
摘要： The invention is concerned with novel compounds of formula (I), the pharmaceutically acceptable acid addition salts thereof and the stereochemically isomeric forms thereof, wherein X is oxygen or sulphur; R1 is hydrogen or halo; R2 is hydrogen, C1-4alkyl, phenylmethyl or halophenylmethyl; Alk is C1-4alkanediyl; -Z-A- is a bivalent radical selected from the group consisting of -S-CH2-CH2, -S-CH2-CH2-CH2-, -S-CH=CH-, -CH=CH-CH=CH-, -C(=CHR3)-CH2-CH2-CH2-, -CH=CH-O-, -CHR4-CH2-CH2-, -CHR4-CH2-CH2-CH2-, -CHR4-CH2-CH2-CH2-CH2-; in said bivalent radicals one hydrogen may be replaced by C1-4alkyl; R3 is phenyl or halophenyl; each R4 independently represents hydrogen, hydroxy, phenylmethyl or halophenylmethyl. Pharmaceutical compositions of said compounds and use as a medicine.
摘要翻译：本发明涉及新的式（I）化合物，其药学上可接受的酸加成盐及其立体化学异构形式，其中X为氧或硫; R1是氢或卤素; R2是氢，C1-4烷基，苯基甲基或卤代苯基甲基; Alk是C1-4烷二基; -ZA是选自-S-CH2-CH2，-S-CH2-CH2-CH2-，-S-CH = CH-，-CH = CH-CH = CH-，-C （= CHR 3）-CH 2 -CH 2 -CH 2 - ，-CH = CH-O-，-CHR 4 -CH 2 -CH 2 - ， - CHR 4 -CH 2 -CH 2 - ， - CHR 4 -CH 2 -CH 2 -CH 2 - 在所述二价基团中，一个氢可被C 1-4烷基取代; R3是苯基或卤代苯基; 每个R 4独立地表示氢，羟基，苯基甲基或卤代苯基甲基。所述化合物的药物组合物并用作药物。

9. 发明申请

WO2007048779A1 PIPERIDIN-4-YL-PYRIDAZIN-3-YLAMINE DERIVATIVES AS FAST DISSOCIATING DOPAMINE 2 RECEPTOR ANTAGONISTS 审中-公开
标题翻译：作为快速分解多巴胺的受体拮抗剂PIPERIDIN-4-YL-吡啶-3-磺酰胺衍生物
公开(公告)号：WO2007048779A1
公开(公告)日：2007-05-03
申请号：PCT/EP2006/067696
申请日：2006-10-24
申请人： JANSSEN PHARMACEUTICA N.V. , DE BRUYN, Marcel, Frans, Leopold , MACDONALD, Gregor, James , KENNIS, Ludo, Edmond, Josephine , LANGLOIS, Xavier, Jean, Michel , VAN DEN KEYBUS, Frans, Alfons, Maria , VAN ROOSBROECK, Yves, Emiel, Maria
发明人： DE BRUYN, Marcel, Frans, Leopold , MACDONALD, Gregor, James , KENNIS, Ludo, Edmond, Josephine , LANGLOIS, Xavier, Jean, Michel , VAN DEN KEYBUS, Frans, Alfons, Maria , VAN ROOSBROECK, Yves, Emiel, Maria
IPC分类号： C07D401/12 , C07D409/14 , A61K31/501 , A61P25/00
CPC分类号： C07D401/12 , A61K31/501 , C07D409/14
摘要： The present invention relates to compounds that are fast dissociating dopamine 2 receptor antagonists, processes for preparing these compounds, pharmaceutical compositions comprising these compounds as an active ingredient. The compounds find utility as medicines for treating or preventing central nervous system disorders, for example schizophrenia, by exerting an antipsychotic effect without motor side effects.
摘要翻译：本发明涉及快速解离多巴胺2受体拮抗剂，制备这些化合物的方法，包含这些化合物作为活性成分的药物组合物。该化合物可用作治疗或预防中枢神经系统疾病（例如精神分裂症）的药物，通过发挥抗精神病作用而没有运动副作用。

10. 发明申请

WO2006003148A1 QUINAZOLINEDIONE DERIVATIVES AS PARP INHIBITORS 审中-公开
标题翻译：喹诺酮衍生物作为PARP抑制剂
公开(公告)号：WO2006003148A1
公开(公告)日：2006-01-12
申请号：PCT/EP2005/053031
申请日：2005-06-28
申请人： JANSSEN PHARMACEUTICA N.V. , KENNIS, Ludo, Edmond, Josephine , MERTENS, Josephus, Carolus , VAN DUN, Jacobus, Alphonsus, Josephus , SOMERS, Maria, Victorina, Francisca , WOUTERS, Walter, Boudewijn, Leopold
发明人： KENNIS, Ludo, Edmond, Josephine , MERTENS, Josephus, Carolus , VAN DUN, Jacobus, Alphonsus, Josephus , SOMERS, Maria, Victorina, Francisca , WOUTERS, Walter, Boudewijn, Leopold
IPC分类号： C07D401/14
CPC分类号： C07D401/04 , A61K31/517 , A61K45/06 , C07D401/06 , C07D401/14 , C07D403/12 , C07D405/14
摘要： The present invention provides compounds of formula (I), their use as PARP inhibitors as well as pharmaceutical compositions comprising said compounds of formula (I) wherein R', L', L 2 , X, Y and Z have defined meanings.
摘要翻译：本发明提供式（I）化合物，它们作为PARP抑制剂的用途以及包含所述式（I）化合物的药物组合物，其中R'，L'，L

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