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1. 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。

2. 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。

3. 发明申请

WO2007107545A1 CYCLIC-ALKYLAMINEDERIVATIVES AS INHIBITORS OF THE INTERACTION BETWEEN MDM2 AND P53 审中-公开
标题翻译：作为MDM2和P53之间相互作用的抑制剂的环丙基氨基亚胺
公开(公告)号：WO2007107545A1
公开(公告)日：2007-09-27
申请号：PCT/EP2007/052582
申请日：2007-03-19
申请人： JANSSEN PHARMACEUTICA N.V. , LACRAMPE, Jean, Fernand, Armand , MEYER, Christophe , SCHOENTJES, Bruno , PONCELET, Alain, Philippe , WERMUTH, Camille, Georges , GIETHLEN, Bruno , CONTRERAS, Jean-Marie , JOUBERT, Muriel , VAN HIJFTE, Luc
发明人： LACRAMPE, Jean, Fernand, Armand , MEYER, Christophe , SCHOENTJES, Bruno , PONCELET, Alain, Philippe , WERMUTH, Camille, Georges , GIETHLEN, Bruno , CONTRERAS, Jean-Marie , JOUBERT, Muriel , VAN HIJFTE, Luc
IPC分类号： C07D401/14 , A61K31/4439 , A61K31/4709 , A61P35/00
CPC分类号： C07D401/14
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 of formula (I) wherein n, m, p, t, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , Q, Y 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，t，R 1， R 2，R 3，R 4，R 5，R 6， R，Q，Y和Z具有定义的含义。

4. 发明申请

WO2005097794A1 SUBSTITUTED DIAZA-SPIRO-[4.5]-DECANE DERIVATIVES AND THEIR USE AS NEUROKININ ANTAGONISTS 审中-公开
标题翻译：取代的DIAZA-SPIRO- [4.5] - 衍生物及其作为神经营养因子拮抗剂的用途
公开(公告)号：WO2005097794A1
公开(公告)日：2005-10-20
申请号：PCT/EP2005/051506
申请日：2005-04-04
申请人： JANSSEN PHARMACEUTICA N.V. , JANSSENS, Frans, Eduard , SCHOENTJES, Bruno , COUPA, Sophie , PONCELET, Alain, Philippe , SIMONNET, Yvan, René, Ferdinand
发明人： JANSSENS, Frans, Eduard , SCHOENTJES, Bruno , COUPA, Sophie , PONCELET, Alain, Philippe , SIMONNET, Yvan, René, Ferdinand
IPC分类号： C07D471/10
CPC分类号： C07D471/10
摘要： This invention concerns substituted diaza-spiro-[4.5]-decane derivatives having neurokinin antagonistic activity, in particular NK 1 antagonistic activity, a combined NK 1 /NK 2 antagonist ic activity, a combined NK 1 /NK 3 antagonist ic 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 incontinence. 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NK1拮抗活性，组合的NK1 / NK2拮抗剂ic活性，组合的NK1 / NK3拮抗剂ic活性和组合的NK1 / NK2 / NK3的取代的二氮 - 螺 - [4.5] 拮抗活性，它们的制备，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，肠易激综合征（IBS），昼夜节律紊乱，先兆子痫，伤害感受疼痛，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。

5. 发明申请

WO2006094934A1 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] - 去氧胆碱衍生物及其作为神经营养因子拮抗剂的用途
公开(公告)号：WO2006094934A1
公开(公告)日：2006-09-14
申请号：PCT/EP2006/060419
申请日：2006-03-03
申请人： JANSSEN PHARMACEUTICA N.V. , 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的取代的氧杂二氮杂螺[5-] - 十一酮衍生物，特别是NK 1拮抗活性，NK 3拮抗活性，组合的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，肠易激综合征（IBS），昼夜节律紊乱，前期 - 癫痫，疼痛，疼痛，特别是内脏和神经性疼痛，胰腺炎，神经源性炎症，哮喘，慢性阻塞性肺疾病（COPD）和排尿障碍如尿不良。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。

6. 发明申请

WO2005097795A1 SUBSTITUTED DIAZA-SPIRO-[5.5]-UNDECANE DERIVATIVES AND THEIR USE AS NEUROKININ ANTAGONISTS 审中-公开
标题翻译：取代的DIAZA-SPIRO- [5.5] - 单克隆衍生物及其作为神经营养因子拮抗剂的用途
公开(公告)号：WO2005097795A1
公开(公告)日：2005-10-20
申请号：PCT/EP2005/051508
申请日：2005-04-04
申请人： JANSSEN PHARMACEUTICA N.V. , JANSSENS, Frans, Eduard , SCHOENTJES, Bruno , COUPA, Sophie , PONCELET, Alain, Philippe , SIMONNET, Yvan, René, Ferdinand
发明人： JANSSENS, Frans, Eduard , SCHOENTJES, Bruno , COUPA, Sophie , PONCELET, Alain, Philippe , SIMONNET, Yvan, René, Ferdinand
IPC分类号： C07D471/10
CPC分类号： C07D471/10 , C07D519/00
摘要： This invention concerns substituted diaza-spiro-[5.5]-undecane derivatives having neurokinin antagonistic activity, in particular NK 1 antagonistic activity, a combined NK 1 /NK 2 antagonistic activity, a combined NK 1 /NK 3 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, COPD and micturition disorders such as urinary incontinence. The compounds according to the invention can be represented by general Formula (I) (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NK1拮抗活性，组合的NK1 / NK2拮抗活性，组合的NK1 / NK3拮抗活性和组合的NK1 / NK2 / NK3拮抗活性的取代的二氮 - 螺 - [5.5] - 十一烷衍生物，它们的制剂，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，肠易激综合征（IBS），昼夜节律紊乱，先兆子痫，伤害感受，疼痛，特别是内脏和神经性疼痛，胰腺炎，神经源性炎症，哮喘，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）（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，其中所有取代基如权利要求1所述。

7. 发明授权

EP1999126B1 CYCLIC-ALKYLAMINEDERIVATIVES AS INHIBITORS OF THE INTERACTION BETWEEN MDM2 AND P53 有权
标题翻译： BETWEEN MDM2与p53相互作用的CYCLOALKYLAMINDERIVATE作为抑制剂
公开(公告)号：EP1999126B1
公开(公告)日：2010-06-09
申请号：EP07727060.1
申请日：2007-03-19
申请人： Janssen Pharmaceutica N.V.
发明人： LACRAMPE, Jean, Fernand, Armand , MEYER, Christophe , SCHOENTJES, Bruno , PONCELET, Alain, Philippe , WERMUTH, Camille, Georges , GIETHLEN, Bruno , CONTRERAS, Jean-Marie , JOUBERT, Muriel , VAN HIJFTE, Luc
IPC分类号： C07D401/14 , A61K31/4439 , A61K31/4709 , A61P35/00
CPC分类号： C07D401/14
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 of formula (I) wherein n, m, p, t, R1 , R2 , R3, R4, R5, R6, R7, Q, Y and Z have defined meanings.

8. 发明公开

EP2297089A1 BENZOCYCLOHEPTANE AND BENZOXEPINE DERIVATIVES 有权
标题翻译：苯并环庚烷和苯并哌嗪衍生物
公开(公告)号：EP2297089A1
公开(公告)日：2011-03-23
申请号：EP09738096.8
申请日：2009-04-27
申请人： Janssen Pharmaceutica, N.V.
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化物; 条件是该化合物不是式（B）或其药学上可接受的盐。要求保护的化合物可用于治疗疾病，其治疗受到激活GHS1A-r受体的影响，介导或促进。本发明还涉及其药物组合物及其制备方法。

9. 发明公开

EP2001868A1 INHIBITORS OF THE INTERACTION BETWEEN MDM2 AND P53 有权
标题翻译： BETWEEN MDM2与p53相互作用的抑制剂
公开(公告)号：EP2001868A1
公开(公告)日：2008-12-17
申请号：EP07727057.7
申请日：2007-03-19
申请人： Janssen Pharmaceutica, N.V.
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, R1, R2, A and Z have defined meanings.

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