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1. 发明申请

WO2006094934A8 SUBSTITUTED OXA-DIAZA-SPIRO-[5.5]-UNDECANONE DERIVATIVES AND THEIR USE AS NEUROKININ ANTAGONISTS 审中-公开
标题翻译：取代的OXA-DIAZA-SPIRO- [5.5] - 十一酮衍生物及其作为神经激肽原拮抗剂的用途
公开(公告)号：WO2006094934A8
公开(公告)日：2006-12-07
申请号：PCT/EP2006060419
申请日：2006-03-03
申请人： JANSSEN PHARMACEUTICA NV , JANSSENS FRANS EDUARD , COUPA SOPHIE , PONCELET ALAIN PHILIPPE , SCHOENTJES BRUNO
发明人： JANSSENS FRANS EDUARD , COUPA SOPHIE , PONCELET ALAIN PHILIPPE , SCHOENTJES BRUNO
IPC分类号： C07D498/10 , A61K31/537 , A61P25/18 , A61P25/24
CPC分类号： C07D498/10 , B82Y5/00
摘要： This invention concerns substituted oxa-diaza-spiro-[5.5]-undecanone derivatives having neurokinin antagonistic activity, in particular an NK 1 antagonistic activity, an NK 3 antagonistic activity, a combined NK 1 /NK 2 antagonistic activity and a combined NK 1 /NK 2 /NK 3 antagonistic activity, their preparation, compositions comprising them and their use as a medicine, in particular for the treatment and/or prophylaxis of schizophrenia, emesis, anxiety and depression, irritable bowel syndrome (IBS), circadian rhythm disturbances, pre-eclampsia, nociception, pain, in particular visceral and neuropathic pain, pancreatitis, neurogenic inflammation, asthma, chronic obstructive pulmonary disease (COPD) and micturition disorders such as urinary incont inence. 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.
摘要翻译：本发明涉及具有神经激肽拮抗活性，特别是NK 1拮抗活性，NK 3拮抗活性，联合NK _{1 / NK _{2 拮抗活性和组合的NK _{1 / NK _{2 / NK _{3 拮抗活性，它们的制备，包含它们的组合物以及它们作为药物的用途，特别是用于治疗和/或预防精神分裂症，呕吐，焦虑和抑郁，肠易激综合征（IBS），昼夜节律紊乱， - 惊厥，疼痛，尤其是内脏和神经性疼痛，胰腺炎，神经原性炎症，哮喘，慢性阻塞性肺病（COPD）和排尿障碍如尿失禁。根据本发明的化合物可以由通式（I）表示并且还包含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。}}}}}

2. 发明申请

WO2009037308A1 INHIBITORS OF THE INTERACTION BETWEEN MDM2 AND P53 审中-公开
标题翻译： MDM2和P53之间相互作用的抑制剂
公开(公告)号：WO2009037308A1
公开(公告)日：2009-03-26
申请号：PCT/EP2008/062433
申请日：2008-09-18
申请人： JANSSEN PHARMACEUTICA NV , PONCELET, Virginie Sophie , COUPA, Sophie , STORCK, Pierre-Henri , SCHOENTJES, Bruno
发明人： PONCELET, Virginie Sophie , COUPA, Sophie , STORCK, Pierre-Henri , SCHOENTJES, Bruno
IPC分类号： C07D401/12 , A61K31/4045 , A61P35/00 , A61P29/00 , C07D401/14
CPC分类号： A61K31/4439 , A61K9/28 , A61K31/438 , A61K31/4709 , A61K31/5377 , A61K31/55 , A61K45/06 , C07D401/12 , C07D487/04
摘要： The present invention provides compounds of formula (I), their use as an inhibitor of a p53-MDM2 interaction as well as pharmaceutical compositions comprising said compounds; wherein n, m, p, s, t, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 20 , 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p53-MDM2相互作用的抑制剂的用途以及包含所述化合物的药物组合物; 其中n，m，p，s，t，R1，R2，R3，R4，R5，R6，R7，R20，X，Y，Q和Z具有定义的含义。

3. 发明申请

WO2007107543A1 INHIBITORS OF THE INTERACTION BETWEEN MDM2 AND P53 审中-公开
标题翻译： MDM2和P53之间相互作用的抑制剂
公开(公告)号：WO2007107543A1
公开(公告)日：2007-09-27
申请号：PCT/EP2007/052579
申请日：2007-03-19
申请人： JANSSEN PHARMACEUTICA N.V. , LACRAMPE, Jean, Fernand, Armand , MEYER, Christophe , SCHOENTJES, Bruno , LARDEAU, Delphine, Yvonne, Raymonde , PONCELET, Alain, Philippe , VAN HIJFTE, Luc
发明人： LACRAMPE, Jean, Fernand, Armand , MEYER, Christophe , SCHOENTJES, Bruno , LARDEAU, Delphine, Yvonne, Raymonde , PONCELET, Alain, Philippe , VAN HIJFTE, Luc
IPC分类号： C07D401/12 , C07D405/12 , C07D471/04 , A61K31/4409 , A61P35/00
CPC分类号： C07D405/12 , C07D401/12 , C07D471/04
摘要： The present invention provides compounds of formula (I), their use as an inhibitor of a p53-MDM2 interaction as well as pharmaceutical compositions comprising said compounds of formula (I) wherein n, m, p, s, t, R 1 , R 2 , A and Z have defined meanings.
摘要翻译：本发明提供式（I）化合物，其作为p53-MDM2相互作用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n，m，p，s，t， 1，R 2，A和Z具有定义的含义。

4. 发明申请

WO2006032631A1 INHIBITORS OF THE INTERACTION BETWEEN MDM2 AND P53 审中-公开
标题翻译： MDM2和P53之间相互作用的抑制剂
公开(公告)号：WO2006032631A1
公开(公告)日：2006-03-30
申请号：PCT/EP2005/054604
申请日：2005-09-16
申请人： JANSSEN PHARMACEUTICA N.V. , LACRAMPE, Jean, Fernand, Armand , MEYER, Christophe , LIGNY, Yannick, Aimé, Eddy , CSOKA, Imre, Christian, Francis , VAN HIJFTE, Luc , ARTS, Janine , SCHOENTJES, Bruno , WERMUTH, Camille, Georges , GIETHLEN, Bruno , CONTRERAS, Jean-Marie , JOUBERT, Muriel
发明人： LACRAMPE, Jean, Fernand, Armand , MEYER, Christophe , LIGNY, Yannick, Aimé, Eddy , CSOKA, Imre, Christian, Francis , VAN HIJFTE, Luc , ARTS, Janine , SCHOENTJES, Bruno , WERMUTH, Camille, Georges , GIETHLEN, Bruno , CONTRERAS, Jean-Marie , JOUBERT, Muriel
IPC分类号： C07D401/12 , A61K31/4709 , A61P35/00 , A61K31/4439 , C07D401/14 , C07D403/12 , C07D487/04 , C07D413/14 , A61K31/519 , A61K31/501
CPC分类号： C07D403/12 , C07D401/12 , C07D401/14 , C07D413/14 , C07D471/04 , C07D487/04
摘要： The present invention provides compounds of formula (I), their use as an inhibitor of a p53-MDM2 interaction as well as pharmaceutical compositions comprising said compounds of formula (I) wherein n, m, p, s, t, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , 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p53-MDM2相互作用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n，m，p，s，t，R

5. 发明申请

WO2010089327A3 INDOLE DERIVATIVES AS ANTICANCER AGENTS 审中-公开
公开(公告)号：WO2010089327A3
公开(公告)日：2010-08-12
申请号：PCT/EP2010/051316
申请日：2010-02-03
申请人： JANSSEN PHARMACEUTICA NV , SCHOENTJES, Bruno , DESCAMPS, Sophie , AMBLARD, Nathalie, Claudie, Isabelle
发明人： SCHOENTJES, Bruno , DESCAMPS, Sophie , AMBLARD, Nathalie, Claudie, Isabelle
IPC分类号： C07D401/12 , A61K31/435 , A61K31/44 , A61P35/00
摘要： The present invention provides compounds of formula (I), their use for the treatment of cancer as well as pharmaceutical compositions comprising said compounds of formula (I).

6. 发明申请

WO2010089327A2 INDOLE DERIVATIVES AS ANTICANCER AGENTS 审中-公开
标题翻译：吲哚衍生物作为抗癌剂
公开(公告)号：WO2010089327A2
公开(公告)日：2010-08-12
申请号：PCT/EP2010051316
申请日：2010-02-03
申请人： JANSSEN PHARMACEUTICA NV , SCHOENTJES BRUNO , DESCAMPS SOPHIE , AMBLARD NATHALIE CLAUDIE ISABELLE
发明人： SCHOENTJES BRUNO , DESCAMPS SOPHIE , AMBLARD NATHALIE CLAUDIE ISABELLE
IPC分类号： C07D401/12 , A61K31/435 , A61K31/44 , A61P35/00
CPC分类号： C07D401/12
摘要： The present invention provides compounds of formula (I), their use for the treatment of cancer as well as pharmaceutical compositions comprising said compounds of formula (I).
摘要翻译：本发明提供了式（I）化合物，它们用于治疗癌症的用途以及包含所述式（I）化合物的药物组合物。

7. 发明申请

WO2009037343A1 INHIBITORS OF THE INTERACTION BETWEEN MDM2 AND P53 审中-公开
标题翻译： MDM2和P53之间相互作用的抑制剂
公开(公告)号：WO2009037343A1
公开(公告)日：2009-03-26
申请号：PCT/EP2008/062551
申请日：2008-09-19
申请人： JANSSEN PHARMACEUTICA NV , STORCK, Pierre-Henri , SCHOENTJES, Bruno , PIETTRE, Arnaud Marcel Pierre , ERMERT, Philipp , PONCELET, Virginie Sophie , CSOKA, Imre Christian Francis
发明人： STORCK, Pierre-Henri , SCHOENTJES, Bruno , PIETTRE, Arnaud Marcel Pierre , ERMERT, Philipp , PONCELET, Virginie Sophie , CSOKA, Imre Christian Francis
IPC分类号： C07D413/14 , A61K31/538 , A61P35/00
CPC分类号： C07D413/14
摘要： The present invention provides compounds of formula (I), their use as an inhibitor of a p53-MDM2 interaction as well as pharmaceutical compositions comprising said compounds: wherein n, s, t, R 1 , R 2 , R 3 , R 4 , R 5 , X, Y, Q, Z, G, E and D have defined meanings.
摘要翻译：本发明提供式（I）化合物，其作为p53-MDM2相互作用抑制剂的用途以及包含所述化合物的药物组合物：其中n，s，t，R 1，R 2，R 3，R 4，R 5，X， Y，Q，Z，G，E和D具有定义的含义。

8. 发明申请

WO2006094948A1 DIAZA-SPIRO-[4.4]-NONANE DERIVATIVES AS NEUROKININ (NK1) ANTAGONISTS 审中-公开
标题翻译： DIAZA-SPIRO- [4.4] -NONANE衍生物作为神经营养因子（NK1）拮抗剂
公开(公告)号：WO2006094948A1
公开(公告)日：2006-09-14
申请号：PCT/EP2006/060458
申请日：2006-03-03
申请人： JANSSEN PHARMACEUTICA N.V. , JANSSENS, Frans, Eduard , COUPA, Sophie , PONCELET, Alain, Philippe , SIMONNET, Yvan, René, Ferdinand , SCHOENTJES, Bruno
发明人： JANSSENS, Frans, Eduard , COUPA, Sophie , PONCELET, Alain, Philippe , SIMONNET, Yvan, René, Ferdinand , SCHOENTJES, Bruno
IPC分类号： C07D487/08 , A61K31/435 , A61P25/00
CPC分类号： C07D487/08
摘要： This invention concerns substituted diaza-spiro-[4.4]-nonane derivatives having neurokinin antagonistic activity, in particular NK1 antagonist ic activity, their preparation, compositions comprising them and their use as a medicine, in particular for the treatment and/or prophylaxis of schizophrenia, emesis, anxiety and depression, irritable bowel syndrome (IBS), circadian rhythm disturbances, pre-eclampsia, nocicept ion, pain, in particular visceral and neuropathic pain, pancreatitis, neurogenic inflammation, asthma, chronic obstructive pulmonary disease (COPD) and micturition disorders such as urinary incont inence. 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.
摘要翻译：本发明涉及具有神经激肽拮抗活性的具有神经激肽拮抗活性的取代的二氮杂螺 - [4.4] - 壬烷衍生物，特别是NK1拮抗剂活性，其制备方法，包含它们的组合物及其作为药物的用途，特别是用于治疗和/或预防精神分裂症呕吐，焦虑和抑郁症，肠易激综合征（IBS），昼夜节律紊乱，先兆子痫，伤痛感染，疼痛，特别是内脏和神经性疼痛，胰腺炎，神经源性炎症，哮喘，慢性阻塞性肺病（COPD）和排尿疾病如尿不起。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。

9. 发明申请

WO0155134A2 NOVEL 1,3-DIHYDRO-2H-INDOL-2-ONE DERIVATIVES, PREPARATION METHOD AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 审中-公开
标题翻译：新型1,3-二氢-2H-吲哚-2-酮衍生物，制备方法和含有它们的药物组合物
公开(公告)号：WO0155134A2
公开(公告)日：2001-08-02
申请号：PCT/FR0100228
申请日：2001-01-24
申请人： SANOFI SYNTHELABO , SCHOENTJES BRUNO , SERRADEIL LE GAL CLAUDINE , WAGNON JEAN
发明人： SCHOENTJES BRUNO , SERRADEIL-LE GAL CLAUDINE , WAGNON JEAN
IPC分类号： A61K31/5377 , A61P1/00 , A61P1/04 , A61P1/08 , A61P1/16 , A61P3/04 , A61P3/06 , A61P3/10 , A61P5/00 , A61P9/00 , A61P9/04 , A61P9/10 , A61P9/12 , A61P11/00 , A61P11/06 , A61P13/12 , A61P15/08 , A61P17/06 , A61P19/02 , A61P25/00 , A61P25/06 , A61P25/14 , A61P25/16 , A61P25/22 , A61P25/24 , A61P25/28 , A61P27/06 , A61P27/12 , A61P29/00 , A61P35/00 , A61P37/04 , A61P43/00 , C07D413/04
CPC分类号： C07D413/04
摘要： The invention concerns compounds of formula (I), and their solvates and/or hydrates, having affinity and selectivity for V1b receptors or for both V1b and V1a arginine-vasopressin receptors. The invention also concerns their method of preparation, intermediate compounds of formula (II) used for preparing them, pharmaceutical compositions containing them and their use for preparing medicines.
摘要翻译：本发明涉及式（I）化合物及其溶剂合物和/或水合物，对V1b受体或V1b和V1a精氨酸 - 加压素受体具有亲和力和选择性。本发明还涉及它们的制备方法，用于制备它们的式（II）的中间体化合物，含有它们的药物组合物及其制备药物的用途。

10. 发明申请

WO2009133052A1 BENZOCYCLOHEPTANE AND BENZOXEPINE DERIVATIVES 审中-公开
标题翻译：苯并噻吩和苯并吡喃衍生物
公开(公告)号：WO2009133052A1
公开(公告)日：2009-11-05
申请号：PCT/EP2009/055034
申请日：2009-04-27
申请人： JANSSEN PHARMACEUTICA NV , SCHOENTJES, Bruno , PONCELET, Alain, Philippe , DOYON, Julien, Georges, Pierre-Olivier , LINDERS, Joannes, Theodorus, Maria , MEERPOEL, Lieven , VER DONCK, Luc, August, Laurentius
发明人： SCHOENTJES, Bruno , PONCELET, Alain, Philippe , DOYON, Julien, Georges, Pierre-Olivier , LINDERS, Joannes, Theodorus, Maria , MEERPOEL, Lieven , VER DONCK, Luc, August, Laurentius
IPC分类号： C07C215/44 , C07C217/52 , C07C313/08 , C07C213/02 , C07C213/08 , A61K31/135 , A61K31/335
CPC分类号： C07C215/42 , C07C35/52 , C07C43/192 , C07C215/64 , C07C217/08 , C07C217/74 , C07C2602/12 , C07D207/06 , C07D213/53 , C07D213/65 , C07D215/14 , C07D239/26 , C07D295/092 , C07D295/096 , C07D295/16 , C07D313/08 , C07D317/58 , C07D405/04 , C07D407/04
摘要： The present invention relates to a compound of formula (I), including any stereochemically isomeric form thereof, wherein the substituents are as defined in the specification and the claims; a N -oxide thereof, a pharmaceutically acceptable salt thereof or a solvate thereof; provided that the compound is other than formula (B) or a pharmaceutically acceptable salt thereof. The claimed compounds are useful for the treatment of a disease, the treatment of which is affected, mediated or facilitated by activating the GHS1A-r receptor. The invention also relates to pharmaceutical compositions thereof and processes for the preparation thereof.
摘要翻译：本发明涉及式（I）化合物，包括其任何立体化学异构形式，其中取代基如说明书和权利要求书中所定义; 其N-氧化物，其药学上可接受的盐或其溶剂合物; 条件是该化合物不是式（B）化合物或其药学上可接受的盐。要求保护的化合物可用于治疗通过激活GHS1A-r受体而影响，介导或促进的疾病的治疗。本发明还涉及其药物组合物及其制备方法。

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