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1. 发明申请

WO2008068272A2 ANTIBACTERIAL QUINOLINE DERIVATIVES 审中-公开
标题翻译：抗生素喹啉衍生物
公开(公告)号：WO2008068272A2
公开(公告)日：2008-06-12
申请号：PCT/EP2007/063319
申请日：2007-12-04
申请人： JANSSEN PHARMACEUTICA N.V. , GUILLEMONT, Jérôme, Emile, Georges , DORANGE, Ismet , LANÇOIS, David, Francis, Alain , VILLALGORDO-SOTO, José, Manuel , SIMONNET, Yvan, René, Ferdinand , MOTTE, Magali, Madeleine, Simone , ANDRIES, Koenraad, Jozef, Lodewijk, Marcel , KOUL, Anil
发明人： GUILLEMONT, Jérôme, Emile, Georges , DORANGE, Ismet , LANÇOIS, David, Francis, Alain , VILLALGORDO-SOTO, José, Manuel , SIMONNET, Yvan, René, Ferdinand , MOTTE, Magali, Madeleine, Simone , ANDRIES, Koenraad, Jozef, Lodewijk, Marcel , KOUL, Anil
IPC分类号： C07D215/22 , C07D401/12 , C07D487/08 , A61K31/47 , C07D401/14 , C07D417/06
CPC分类号： C07D401/06 , C07D215/227 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/14 , C07D417/06 , C07D487/08
摘要： The present invention relates to novel subst ituted quinoline derivatives according to the general Formula (Ia) or Formula (Ib): including any stereochemically isomeric form thereof, a pharmaceutically acceptable salt thereof, a N -oxide form thereof or a solvate thereof. The claimed compounds are useful for the treatment of a bacterial infection. Also claimed is a composition comprising a pharmaceutically acceptable carrier and, as active ingredient, a therapeutically effective amount of the claimed compounds, the use of the claimed compounds or composit ions for the manufacture of a medicament for the treatment of a bacterial infection and a process for preparing the claimed compounds.
摘要翻译：本发明涉及根据通式（Ia）或式（Ib）的新的取代的喹啉衍生物：包括其任何立体化学异构形式，其药学上可接受的盐，其N-氧化物形式或其溶剂合物。所要求保护的化合物可用于治疗细菌感染。还要求保护的是包含药学上可接受的载体和作为活性成分的治疗有效量的所要求保护的化合物的组合物，所要求保护的化合物或复合离子在制备用于治疗细菌感染和方法的药物中的用途用于制备所要求保护的化合物。

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

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。

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

US20100063026A1 ANTIBACTERIAL QUINOLINE DERIVATIVES 审中-公开
标题翻译：抗生素喹啉衍生物
公开(公告)号：US20100063026A1
公开(公告)日：2010-03-11
申请号：US12516420
申请日：2007-12-04
申请人： Jérôme Emile Georges Guillemont , Ismet Dorange , David Francis Alain Lançois , José Manuel Villalgordo-Soto , Yvan René Ferdinand , Magali Madeleine Simone Motte , Koenraad Jozef Lodewijk Marcel Andries , Anil Koul
发明人： Jérôme Emile Georges Guillemont , Ismet Dorange , David Francis Alain Lançois , José Manuel Villalgordo-Soto , Yvan René Ferdinand , Magali Madeleine Simone Motte , Koenraad Jozef Lodewijk Marcel Andries , Anil Koul
IPC分类号： A61K31/4709 , C07D215/227 , C07D401/06 , C07D401/14 , C07D487/04 , C07D417/06 , A61K31/551 , A61K31/541 , A61P31/04
CPC分类号： C07D401/06 , C07D215/227 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/14 , C07D417/06 , C07D487/08
摘要： The present invention relates to novel substituted quinoline derivatives according to the general Formula (Ia) or Formula (Ib): including any stereochemically isomeric form thereof, a pharmaceutically acceptable salt thereof, a N-oxide form thereof or a solvate thereof. The claimed compounds are useful for the treatment of a bacterial infection. Also claimed is a composition comprising a pharmaceutically acceptable carrier and, as active ingredient, a therapeutically effective amount of the claimed compounds, the use of the claimed compounds or compositions for the manufacture of a medicament for the treatment of a bacterial infection and a process for preparing the claimed compounds.
摘要翻译：本发明涉及根据通式（Ia）或式（Ib）的新的取代喹啉衍生物：包括其任何立体化学异构形式，其药学上可接受的盐，其N-氧化物形式或其溶剂合物。所要求保护的化合物可用于治疗细菌感染。还要求保护的是包含药学上可接受的载体和作为活性成分的治疗有效量的要求保护的化合物的组合物，所要求保护的化合物或组合物在制备用于治疗细菌感染的药物中的用途和制备所要求保护的化合物。

6. 发明授权

US07544694B2 Substituted diaza-spiro-[5.5]-undecane derivatives and their use as neurokinin antagonists 失效
标题翻译：取代的双 - 螺 - [5.5] - 十一烷衍生物及其作为神经激肽拮抗剂的用途
公开(公告)号：US07544694B2
公开(公告)日：2009-06-09
申请号：US11547889
申请日：2005-04-04
申请人： Frans Eduard Janssens , Bruno Schoentjes , Sophie Coupa , Alain Philippe Poncelet , Yvan René Ferdinand Simonnet
发明人： Frans Eduard Janssens , Bruno Schoentjes , Sophie Coupa , Alain Philippe Poncelet , Yvan René Ferdinand Simonnet
IPC分类号： A61K31/438 , 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 NK1 antagonistic activity, a combined NK1/NK2 antagonistic activity, a combined NK1/NK3 antagonistic activity and a combined NK1/NK2/NK3 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) 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NK1 / NK2拮抗活性，组合NK1 / NK3拮抗活性和组合NK1 / NK2 / NK3拮抗活性的取代二氮 - 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）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。

7. 发明授权

US07612056B2 Substituted diaza-spiro-[4.5]-decane derivatives and their use as neurokinin antagonists 失效
标题翻译：取代的二氮 - 螺 - [4.5] - 癸烷衍生物及其作为神经激肽拮抗剂的用途
公开(公告)号：US07612056B2
公开(公告)日：2009-11-03
申请号：US11547705
申请日：2005-04-04
申请人： Frans Eduard Janssens , Bruno Schoentjes , Sophie Coupa , Alain Philippe Poncelet , Yvan René Ferdinand Simonnet
发明人： Frans Eduard Janssens , Bruno Schoentjes , Sophie Coupa , Alain Philippe Poncelet , Yvan René Ferdinand Simonnet
IPC分类号： A61K31/44
CPC分类号： C07D471/10
摘要： This invention concerns substituted diaza-spiro-[4.5]-decane derivatives having neurokinin antagonistic activity, in particular NK1 antagonistic activity, a combined NK1/NK2 antagonistic activity, a combined NK1/NK3 antagonistic activity and a combined NK1/NK2/NK3 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NK1 / NK2拮抗活性，组合NK1 / NK3拮抗活性和组合NK1 / NK2 / NK3拮抗活性的取代的二氮 - 螺 - [4.5] - 癸烷衍生物，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，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。

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