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1. 发明申请

WO2004033428A1 SUBSTITUTED 1,4-DI-PIPERIDIN-4-YL-PIPERAZINE DERIVATIVES AND THEIR USE AS NEUROKININ ANTAGONISTS 审中-公开
标题翻译：取代的1,4-二哌啶-4-基哌嗪衍生物及其作为神经营养因子拮抗剂的用途
公开(公告)号：WO2004033428A1
公开(公告)日：2004-04-22
申请号：PCT/EP2003/050697
申请日：2003-10-07
申请人： JANSSEN PHARMACEUTICA N.V. , JANSSENS, Frans, Eduard , SOMMEN, François, Maria , DE BOECK, Benoît, Christian, Albert, Ghislain , LEENAERTS, Joseph, Elisabeth , VAN ROOSBROECK, Yves, Emiel, Maria , DIELS, Gaston, Stanislas, Marcella
发明人： JANSSENS, Frans, Eduard , SOMMEN, François, Maria , DE BOECK, Benoît, Christian, Albert, Ghislain , LEENAERTS, Joseph, Elisabeth , VAN ROOSBROECK, Yves, Emiel, Maria , DIELS, Gaston, Stanislas, Marcella
IPC分类号： C07D211/58
CPC分类号： C07D401/14 , C07D211/58 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04
摘要： The invention concerns substituted 1,4-di-piperidin-4-yl-piperazine derivatives having neurokinin antagonistic activity, in particular NK 1 antagonistic activity, their preparation, compositions comprising them and their use as a medicine, in particular for the treatment of emesis, anxiety, depression, pain, pancreatitis and IBS. 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. In view of their capability to antagonize the actions of neurokinins by blocking the neurokinin receptors, and in particular antagonizing the actions of substance P by blocking the NK 1 receptor, the compounds according to the invention are useful as a medicine, in particular in the prophylactic and therapeutic treatment of neurokinin-mediated conditions, such as, for instance CNS disorders, in particular depression, anxiety disorders, stress-related disorders, sleep disorders, cognitive disorders, personality disorders, schizoaffective disorders, eating disorders, neurodegenerative diseases, addiction disorders, mood disorders, sexual dysfunction, pain and other CNS-related conditions; inflammation; allergic disorders; emesis; gastrointestinal disorders, in particular irritable bowel syndrome (IBS); skin disorders; vasospastic diseases; fibrosing and collagen diseases; disorders related to immune enhancement or suppression and rheumatic diseases and body weight control.
摘要翻译：本发明涉及具有神经激肽拮抗活性的取代的1,4-二哌啶-4-基 - 哌嗪衍生物，特别是NK1拮抗活性，其制备方法，包含它们的组合物及其作为药物的用途，特别是用于治疗呕吐，焦虑，抑郁，疼痛，胰腺炎和IBS。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-氧化物形式和其前药，其中所有取代基被定义鉴于它们通过阻断神经激肽受体拮抗神经激肽的作用的能力，特别是通过阻断NK1受体拮抗物质P的作用，根据本发明的化合物可用作药物，在特别是在神经激肽介导的病症例如中枢神经系统疾病，特别是抑郁症，焦虑障碍，应激相关疾病，睡眠障碍，认知障碍，人格障碍，分裂情感障碍，进食障碍，神经变性疾病中的预防和治疗治疗中，成瘾症，情绪障碍，性功能障碍，疼痛等CNS相关c onditions; 炎; 过敏性疾病; 呕吐; 胃肠道疾病，特别是肠易激综合征（IBS）; 皮肤病; 血管痉挛性疾病; 纤维化和胶原病; 与免疫增强或抑制相关的疾病和风湿性疾病和体重控制。

2. 发明申请

WO2004056772A1 SUBSTITUTED 1,4-DI-PIPERIDIN-4-YL-PIPERAZINE DERIVATIVES AND THEIR USE AS TACHYKININ ANTAGONISTS 审中-公开
标题翻译：取代的1,4-二哌啶-4-基哌嗪衍生物及其作为TACHYKININ拮抗剂的用途
公开(公告)号：WO2004056772A1
公开(公告)日：2004-07-08
申请号：PCT/EP2002/014836
申请日：2002-12-23
申请人： JANSSEN PHARMACEUTICA N.V. , JANSSENS, Frans, Eduard , SOMMEN, François, Maria , DE BOECK, Benoît, Christian, Albert, Ghislain , LEENAERTS, Joseph, Elisabeth , VAN ROOSBROECK, Yves, Emiel, Maria
发明人： JANSSENS, Frans, Eduard , SOMMEN, François, Maria , DE BOECK, Benoît, Christian, Albert, Ghislain , LEENAERTS, Joseph, Elisabeth , VAN ROOSBROECK, Yves, Emiel, Maria
IPC分类号： C07D211/58
CPC分类号： C07D409/14 , C07D211/58 , C07D401/14 , C07D405/14 , C07D413/14 , C07D417/14 , C07D471/04
摘要： The invention concerns substituted 1,4-di-piperidin-4-yl-piperazine derivatives having tachykinin antagonistic activity, in particular NK 1 antagonistic activity, their preparation, compositions comprising them and their use as a medicine, in particular for the treatment of emesis, anxiety, depression and IBS. 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. In view of their capability to antagonize the actions of tachykinins by blocking the tachykinin receptors, and in particular antagonizing the actions of substance P by blocking the NK 1 receptor, the compounds according to the invention are useful as a medicine, in particular in the prophylactic and therapeutic treatment of tachykinin-mediated conditions, such as, for instance CNS disorders, in particular depression, anxiety disorders, stress-related disorders, sleep disorders, cognitive disorders, personality disorders, schizoaffective disorders, eating disorders, neurodegenerative diseases, addiction disorders, mood disorders, sexual dysfunction, pain and other CNS-related conditions; inflammation; allergic disorders; emesis; gastrointestinal disorders, in particular irritable bowel syndrome (IBS); skin disorders; vasospastic diseases; fibrosing and collagen diseases; disorders related to immune enhancement or suppression and rheumatic diseases and body weight control.
摘要翻译：本发明涉及具有速激肽拮抗活性的取代的1,4-二哌啶-4-基 - 哌嗪衍生物，特别是NK1拮抗活性，其制备方法，包含它们的组合物及其作为药物的用途，特别是用于治疗呕吐，焦虑，抑郁和IBS。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鉴于其通过阻断速激肽受体拮抗速激肽的作用的能力，特别是通过阻断NK1受体拮抗物质P的作用，本发明的化合物可用作药物，特别是作为药物在速激肽介导的病症例如中枢神经系统疾病，特别是抑郁症，焦虑症，压力相关疾病，睡眠障碍，认知障碍，人格障碍，分裂情感障碍，进食障碍，神经变性疾病中的预防和治疗性治疗中，成瘾症，情绪障碍，性功能障碍，疼痛等CNS相关公司 nditions; 炎; 过敏性疾病; 呕吐; 胃肠道疾病，特别是肠易激综合征（IBS）; 皮肤病; 血管痉挛性疾病; 纤维化和胶原病; 与免疫增强或抑制相关的疾病和风湿性疾病和体重控制。

3. 发明申请

WO2004110415A2 NOVEL FORMULATIONS FOR OPIOID-BASED TREATMENTS OF PAIN COMPRISING SUBSTITUTED 1,4-DI-PIPERIDIN-4-YL-PIPERAZINE DERIVATIVES 审中-公开
标题翻译：取代4-DI-PIPERIDIN-4-YL-哌啶衍生物与阿片样物质联用及其用于治疗与基于阿片类药物治疗相关的疼痛和副作用的用途
公开(公告)号：WO2004110415A2
公开(公告)日：2004-12-23
申请号：PCT/EP2004/051048
申请日：2004-06-07
申请人： JANSSEN PHARMACEUTICA N.V. , JANSSENS, Frans, Eduard , SOMMEN, François, Maria , DE BOECK, Benoît, Christian, Albert, Ghislain , LEENAERTS, Joseph, Elisabeth , VAN ROOSBROECK, Yves, Emiel, Maria , MEERT, Theo, Frans
发明人： JANSSENS, Frans, Eduard , SOMMEN, François, Maria , DE BOECK, Benoît, Christian, Albert, Ghislain , LEENAERTS, Joseph, Elisabeth , VAN ROOSBROECK, Yves, Emiel, Maria , MEERT, Theo, Frans
IPC分类号： A61K31/00
CPC分类号： A61K45/06 , A61K31/496 , A61K31/551 , A61K2300/00
摘要： This invention concerns novel formulations for opioid-based treatments of pain and/or nociception comprising opioid analgesics and 1,4-di-piperidin-4-yl-piperazine derivatives having neurokinin antagonistic activity, in particular NK 1 antagonistic activity, the use of said formulation for the manufacture of a medicament for the prevention and/or treatment of emesis, pain and/or nociception, in particular in opioidbased acute and chronic pain treatments, more in particular in inflammatory, postoperative, emergency room (ER), breakthrough, neuropathic and cancer pain treatments and the use of an NK 1 -receptor antagonist for the manufacture of a medicament for the prevention and/or treatment of respiratory depression in opioid-based treatments of pain. The pharmaceutical formulations according to the invention comprise a pharmaceutically acceptable carrier and, as active ingredients, a therapeutically effective amount of an opioid analgesic and NKI -antagonists according to the general Formula (I) the pharmaceutically acceptable acid or base addition salts thereof, the stereochernically isomeric forms thereof, the N -oxide form thereof and prodrugs thereof, wherein all substituents are defined as in Claim 1. The pharmaceutical composition according to the invention reduces to a large extent a number of unwanted sideeffects associated with opioid analgesics, in particular emesis, respiratory depression and tolerance, thereby increasing the total tolerability of said opioids in pain treatment.
摘要翻译：本发明涉及基于阿片样物质治疗疼痛和/或伤害感受的新制剂，其包括具有神经激肽拮抗活性的阿片类镇痛药和1,4-二哌啶-4-基 - 哌嗪衍生物，特别是NK1拮抗活性，所述制剂的用途用于制备用于预防和/或治疗呕吐，疼痛和/或伤害感受的药物，特别是在阿片样物质的急性和慢性疼痛治疗中，特别是在炎性，术后，急诊室（ER），突破性，神经性和癌症疼痛治疗和NK1受体拮抗剂在制备用于预防和/或治疗基于阿片样物质的疼痛治疗中的呼吸抑制的药物中的用途。根据本发明的药物制剂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根据通式（I）的阿片类镇痛药和NKI拮抗剂其药学上可接受的酸或碱加成盐，立体选择性其异构体形式，其N-氧化物形式和其前药，其中所有取代基如权利要求1中所定义。根据本发明的药物组合物在很大程度上降低了与阿片类镇痛药有关的多种不希望的副作用，特别是呕吐，呼吸抑制和耐受性，从而增加所述阿片样物质在疼痛治疗中的总耐受性。

4. 发明申请

WO2004056805A1 SUBSTITUTED 4-(4-PIPERIDIN-4-YL-PIPERAZIN-1-YL)-AZEPANE DERIVATIVES AND THEIR USE AS NEUROKININ ANTAGONISTS 审中-公开
标题翻译：取代的4-（4-哌啶-4-基 - 哌嗪-1-基） - 氨基衍生物及其作为神经营养因子拮抗剂的用途
公开(公告)号：WO2004056805A1
公开(公告)日：2004-07-08
申请号：PCT/EP2003/051043
申请日：2003-12-17
申请人： JANSSEN PHARMACEUTICA N.V. , JANSSENS, Frans, Eduard , SOMMEN, François, Maria , DE BOECK, Benoît, Christian, Albert, Ghislain , LEENAERTS, Joseph, Elisabeth
发明人： JANSSENS, Frans, Eduard , SOMMEN, François, Maria , DE BOECK, Benoît, Christian, Albert, Ghislain , LEENAERTS, Joseph, Elisabeth
IPC分类号： C07D401/14
CPC分类号： C07D401/12 , C07D401/14 , C07D405/14 , C07D413/14
摘要： The invention concerns substituted 4-(4-piperidin-4-yl-piperazin-1-yl)-azepane derivatives having neurokinin antagonistic activity, in particular NK 1 antagonistic activity, their preparation, compositions comprising them and their use as a medicine, in particular for the treatment of pain, emesis, anxiety, depression and IBS. 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. In view of their capability to antagonize the actions of tachykinins by blocking the neurokinin receptors, and in particular antagonizing the actions of substance P and Neurokinin B by blocking the NK 1 , NK 2 and NK 3 receptors, the compounds according to the invention are useful as a medicine, in particular in the prophylactic and therapeutic treatment of tachykinin-mediated conditions, such as, for instance CNS disorders, in particular schizoaffective disorders, depression, anxiety disorders, stress-related disorders, sleep disorders, cognitive disorders, personality disorders, eating disorders, neurodegenerative diseases, addiction disorders, mood disorders, sexual dysfunction, pain and other CNS-related conditions ; inflammation ; allergic disorders ; emesis ; gastrointestinal disorders, in particular irritable bowel syndrome (IBS); skin disorders ; vasospastic diseases ; fibrosing and collagen diseases ; disorders related to immune enhancement or suppression and rheumatic diseases and body weight control.
摘要翻译：本发明涉及具有神经激肽拮抗活性的取代的4-（4-哌啶-4-基 - 哌嗪-1-基） - 氮杂环庚烷衍生物，特别是NK1拮抗活性，其制备方法，包含它们的组合物及其作为药物的用途用于治疗疼痛，呕吐，焦虑，抑郁和IBS。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鉴于其通过阻断神经激肽受体拮抗速激肽的作用的能力，特别是通过阻断NK1，NK2和NK3受体拮抗物质P和神经激肽B的作用，本发明的化合物是可用作药物，特别是在速激肽介导的病症例如CNS疾病，特别是分裂情感障碍，抑郁症，焦虑症，压力相关疾病，睡眠障碍，认知障碍，人格障碍，进食障碍，神经变性疾病，成瘾症，情绪障碍，性功能障碍疼痛等CNS相关病情; 炎症; 过敏性疾病; 呕吐胃肠道疾病，特别是肠易激综合征（IBS）; 皮肤病; 血管痉挛性疾病; 纤维化和胶原病; 与免疫增强或抑制相关的疾病和风湿性疾病和体重控制。

5. 发明申请

WO2004056800A1 SUBSTITUTED 1-PIPERIDIN-4-YL-4-AZETIDIN-3-YL-PIPERAZINE DERIVATIVES AND THEIR USE AS NEUROKININ ANTAGONISTS 审中-公开
标题翻译：取代的1-哌啶-4-Y-4-AZETIDIN-3-Y-PIPERAZINE衍生物及其作为神经营养因子拮抗剂的用途
公开(公告)号：WO2004056800A1
公开(公告)日：2004-07-08
申请号：PCT/EP2003/051042
申请日：2003-12-17
申请人： JANSSEN PHARMACEUTICA N.V. , JANSSENS, Frans, Eduard , SOMMEN, François, Maria , DE BOECK, Benoît, Christian, Albert, Ghislain , LEENAERTS, Joseph, Elisabeth
发明人： JANSSENS, Frans, Eduard , SOMMEN, François, Maria , DE BOECK, Benoît, Christian, Albert, Ghislain , LEENAERTS, Joseph, Elisabeth
IPC分类号： C07D401/12
CPC分类号： C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D417/14
摘要： The invention concerns substituted 1-piperidin-4-yl-4-azefdin-3-yl-piperazine having neurokinin antagonistic activity, in particular NK 1 and NK 1 /NK 3 - antagonistic activity, their preparation, compositions comprising them and their use as a medicine, in particular for the treatment of schizophrenia, emesis, anxiety, depression, irritable bowel syndrome (IBS), circadian rhythm disturbances, pain, neurogenic inflammation, asthma, micturition disorders such as urinary incontinence and nociception. 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. In view of their capability to antagonize the actions of tachykinins by blocking the neurokinin receptors, and in particular antagonizing the actions of substance P by blocking the NK receptors, the compounds according to the invention are useful as a medicine, in particular in the prophylactic and therapeutic treatment of tachykininmediated conditions, such as, for instance CNS disorders, in particular depression, anxiety disorders, stress-related disorders, sleep disorders, cognitive disorders, personality disorders, schizoaffective disorders, eating disorders, neurodegenerative diseases, addiction disorders, mood disorders, sexual dysfunction, pain and other CNSrelated conditions ; inflammation ; allergic disorders ; emesis ; gastrointestinal disorders, in particular irritable bowel syndrome (IBS); skin disorders ; vasospastic diseases ; fibrosing and collagen diseases ; disorders related to immune enhancement or suppression and rheumatic diseases and body weight control.
摘要翻译：本发明涉及具有神经激肽拮抗活性，特别是NK1和NK1 / NK3拮抗活性的取代的1-哌啶-4-基-4-甲啡菲-3-基 - 哌嗪，其制备方法，包含它们的组合物及其作为药物的用途，特别是用于治疗精神分裂症，呕吐，焦虑症，抑郁症，肠易激综合征（IBS），昼夜节律紊乱，疼痛，神经源性炎症，哮喘，排尿障碍如尿失禁和伤害感受。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鉴于其通过阻断神经激肽受体拮抗速激肽的作用的能力，特别是通过阻断NK受体拮抗物质P的作用，本发明的化合物可用作药物，特别是作为药物在速激肽介导的病症例如CNS病症，特别是抑郁症，焦虑症，压力相关疾病，睡眠障碍，认知障碍，人格障碍，分裂情感障碍，进食障碍，神经变性疾病，成瘾疾病中的预防和治疗性治疗，情绪障碍，性功能障碍，疼痛等CNS相关性神话炎症; 过敏性疾病; 呕吐胃肠道疾病，特别是肠易激综合征（IBS）; 皮肤病; 血管痉挛性疾病; 纤维化和胶原病; 与免疫增强或抑制相关的疾病和风湿性疾病和体重控制。

6. 发明申请

WO2005097774A1 SUBSTITUTED 4-ALKYL- AND 4-ALKANOYL-PIPERIDINE DERIVATIVES AND THEIR USE AS NEUROKININ ANTAGONISTS 审中-公开
标题翻译：取代的4-烷基和4-烷基 - 哌啶衍生物及其作为神经营养因子拮抗剂的用途
公开(公告)号：WO2005097774A1
公开(公告)日：2005-10-20
申请号：PCT/EP2005/051509
申请日：2005-04-04
申请人： JANSSEN PHARMACEUTICA N.V. , JANSSENS, Frans, Eduard , SOMMEN, François, Maria , DE BOECK, Benoît, Christian, Albert, Ghislain , LEENAERTS, Joseph, Elisabeth
发明人： JANSSENS, Frans, Eduard , SOMMEN, François, Maria , DE BOECK, Benoît, Christian, Albert, Ghislain , LEENAERTS, Joseph, Elisabeth
IPC分类号： C07D401/02
CPC分类号： C07D409/14 , C07D401/02 , C07D401/04 , C07D401/14 , C07D405/14 , C07D413/14 , C07D417/14
摘要： The invention concerns substituted 4-alkyl- and 4-alkanoyl-piperidine derivatives having neurokinin antagonistic activity, in particular NK 1 antagonistic activity and a combined NK 1 /NK 3 antagonistic activity, 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的取代的4-烷基 - 和4-链烷酰基 - 哌啶衍生物，特别是NK1拮抗活性和组合的NK1 / NK3拮抗活性，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。

7. 发明申请

WO2004056799A2 SUBSTITUTED 1-PIPERIDIN-4-YL-4-PYRROLIDIN-3-YL-PIPERAZINE DERIVATIVES AND THEIR USE AS NEUROKININ ANTAGONISTS 审中-公开
标题翻译：取代的1-哌啶-4-基-4-吡咯烷-3-基 - 哌嗪衍生物及其作为神经激肽原拮抗剂的用途
公开(公告)号：WO2004056799A2
公开(公告)日：2004-07-08
申请号：PCT/EP2003/051041
申请日：2003-12-17
申请人： JANSSEN PHARMACEUTICA N.V. , JANSSENS, Frans, Eduard , SOMMEN, François, Maria , DE BOECK, Benoît, Christian, Albert, Ghislain , LEENAERTS, Joseph, Elisabeth
发明人： JANSSENS, Frans, Eduard , SOMMEN, François, Maria , DE BOECK, Benoît, Christian, Albert, Ghislain , LEENAERTS, Joseph, Elisabeth
IPC分类号： C07D401/08
CPC分类号： C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14
摘要： This invention concerns substituted I-piperidin-4-yl-4-pyrrolidin-3-yl-piperazine derivatives having neurokinin antagonistic activity, in particular NK 1 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 of schizophrenia, anxiety, depression, emesis and IBS. 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. In view of their capability to antagonize the actions of tachykinins by blocking the neurokinin receptors, and in particular antagonizing the actions of substance P and Neurokinin B by blocking the NK 1 , NK 2 and NK 3 receptors, the compounds according to the invention are useful as a medicine, in particular in the prophylactic and therapeutic treatment of tachykinin-mediated conditions, such as, for instance CNS disorders, in particular schizoaffective disorders, depression, anxiety disorders, stress-related disorders, sleep disorders, cognitive disorders, personality disorders, eating disorders, neurodegenerative diseases, addiction disorders, mood disorders, sexual dysfunction, pain and other CNS-related conditions ; inflammation ; allergic disorders ; emesis ; gastrointestinal disorders, in particular irritable bowel syndrome (IBS); skin disorders ; vasospastic diseases ; fibrosing and collagen diseases ; disorders related to immune enhancement or suppression and rheumatic diseases and body weight control.
摘要翻译：本发明涉及具有神经激肽拮抗活性，特别是NK1拮抗活性的取代的1-哌啶-4-基-4-吡咯烷-3-基 - 哌嗪衍生物，组合的NK1 / NK3拮抗活性和组合的NK1 / NK2 / NK3组合拮抗活性，它们的制备，包含它们的组合物以及它们作为药物的用途，特别是用于治疗精神分裂症，焦虑症，抑郁症，呕吐和IBS。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如权利要求1中所定义。鉴于它们通过阻断神经激肽受体拮抗速激肽作用的能力，特别是通过阻断NK1受体拮抗物质P和神经激肽B的作用， NK2和NK3受体的化合物，根据本发明的化合物可用作药物，特别是在预防和治疗速激肽介导的病症中，例如CNS障碍，特别是情感分裂性障碍，抑郁症，焦虑症，压力相关障碍，睡眠障碍，认知障碍，人格障碍，进食障碍，神经退行性疾病，成瘾性障碍情绪障碍，性功能障碍，疼痛和其他中枢神经系统相关病症; 炎症; 过敏性疾病; 呕吐胃肠疾病，特别是肠易激综合征（IBS）; 皮肤病; 血管痉挛性疾病; 纤维化和胶原病; 与免疫增强或抑制相关的疾病以及风湿性疾病和体重控制。

8. 发明申请

WO2004056364A1 SUBSTITUTED 1-PIPERIDIN-3-YL-4-PIPERIDIN-4-YL-PIPERAZINE DERIVATIVES AND THEIR USE AS NEUROKININ ANTAGONISTS 审中-公开
标题翻译：取代的1-哌啶-3-基-4-哌啶-4-基 - 哌嗪衍生物及其作为神经营养因子拮抗剂的用途
公开(公告)号：WO2004056364A1
公开(公告)日：2004-07-08
申请号：PCT/EP2003/051035
申请日：2003-12-17
申请人： JANSSEN PHARMACEUTICA N.V. , JANSSENS, Frans, Eduard , SOMMEN, François, Maria , DE BOECK, Benoît, Christian, Albert, Ghislain , LEENAERTS, Joseph, Elisabeth
发明人： JANSSENS, Frans, Eduard , SOMMEN, François, Maria , DE BOECK, Benoît, Christian, Albert, Ghislain , LEENAERTS, Joseph, Elisabeth
IPC分类号： A61K31/496
CPC分类号： C07D405/14 , C07D211/58 , C07D211/96 , C07D401/12 , C07D401/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D513/04
摘要： This invention concerns substituted 1-piperidin-3-yl-4-piperidin-4-yl-piperazine derivatives having neurokinin antagonistic activity, in particular NK 1 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 of schizophrenia, emesis, anxiety and depression, irritable bowel syndrom (IBS), circadian rhythm disturbances, visceral pain, neurogenic inflammation, asthma, micturition disorders such as urinary incontinence and nociception. 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. In view of their capability to antagonize the actions of tachykinins by blocking the neurokinin receptors, and in particular antagonizing the actions of substance P, Neurokinin A and Neurokinin B by blocking the NK 1 , NK 2 and NK 3 receptors, the compounds according to the invention are useful as a medicine, in particular in the prophylactic and therapeutic treatment of tachykinin-mediated conditions, such as, for instance CNS disorders, in particular schizoaffective disorders, depression, anxiety disorders, stress-related disorders, sleep disorders, cognitive disorders, personality disorders, eating disorders, neurodegenerative diseases, addiction disorders, mood disorders, sexual dysfunction, pain and other CNS-related conditions; inflammation; allergic disorders; emesis; gastrointestinal disorders, in particular irritable bowel syndrome (IBS); skin disorders; vasospastic diseases; fibrosing and collagen diseases; disorders related to immune enhancement or suppression and rheumatic diseases and body weight control.
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 / NK3拮抗活性和组合的NK1 / NK2 / NK3拮抗活性的取代的1-哌啶-3-基-4-哌啶-4-基 - 哌嗪衍生物，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，内脏痛，神经源性炎症，哮喘，排尿障碍作为尿失禁和伤害感受。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鉴于其通过阻断神经激肽受体拮抗速激肽的作用的能力，特别是通过阻断NK1，NK2和NK3受体拮抗物质P，神经激肽A和神经激肽B的作用，根据本发明可用作药物，特别是在速激肽介导的病症例如中枢神经系统疾病，特别是分裂情感障碍，抑郁症，焦虑症，压力相关疾病，睡眠障碍，认知障碍，人格障碍，进食障碍，神经变性疾病，成瘾症，情绪障碍，性别功能障碍，疼痛等CNS相关病症; 炎; 过敏性疾病; 呕吐; 胃肠道疾病，特别是肠易激综合征（IBS）; 皮肤病; 血管痉挛性疾病; 纤维化和胶原病; 与免疫增强或抑制相关的疾病和风湿性疾病和体重控制。

9. 发明申请

WO2004110451A1 COMBINATIONS FOR OPIOID-BASED TREATMENT OF PAIN COMPRISING 1-(1,2-DISUBSTITUTED PIPERIDINYL)-4-SUBSTITUTED PIPERAZINE DERIVATIVES 审中-公开
标题翻译：用于以包含1-（1,2-取代的哌啶子基）-4-取代的哌嗪衍生物的基于鸦片的治疗疼痛的组合
公开(公告)号：WO2004110451A1
公开(公告)日：2004-12-23
申请号：PCT/EP2004/051050
申请日：2004-06-07
申请人： JANSSEN PHARMACEUTICA N.V. , JANSSENS, Frans, Eduard , SOMMEN, François, Maria , LEENAERTS, Joseph, Elisabeth , VAN ROOSBROECK, Yves, Emiel, Maria , MEERT, Theo, Frans
发明人： JANSSENS, Frans, Eduard , SOMMEN, François, Maria , LEENAERTS, Joseph, Elisabeth , VAN ROOSBROECK, Yves, Emiel, Maria , MEERT, Theo, Frans
IPC分类号： A61K31/496
CPC分类号： A61K31/4468 , A61K31/485 , A61K31/496 , A61K2300/00
摘要： This invention concerns novel formulations for opioid-based treatments of pain and/or nociception comprising opioid analgesics and 1-(1,2-disubstituted piperidinyl)-4substituted piperazine derivatives having neurokinin antagonistic activity, in particular NKI antagonistic activity the use of said formulation for the manufacture of a medicament for the prevention and/or treatment of emesis, pain and/or nociception, in particular in acute and chronic pain treatments, more in particular in inflammatory, postoperative, emergency room (ER), breakthrough, neuropathic and cancer pain treatments and the use of an NKI -receptor antagonist for the manufacture of a medicament for the prevention and/or treatment of respiratory depression and tolerance in opioid-based treatments of pain. The pharmaceutical formulations according to the invention comprise NK 1 - antagonists according to the general Formula (I) 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. The pharmaceutical composition according to the invention reduces to a large extent a number of unwanted side-effects associated with opioid analgesics, in particular respiratory depression and tolerance, thereby increasing the total tolerability of said opioids in pain treatment.
摘要翻译：本发明涉及用于基于阿片样物质治疗疼痛和/或伤害感受的新制剂，其包含阿片类止痛剂和具有神经激肽拮抗活性的1-（1,2-二取代哌啶基）-4-取代哌嗪衍生物，特别是NKI拮抗活性，所述制剂用于制造用于预防和/或治疗呕吐，疼痛和/或伤害感受的药物，特别是在急性和慢性疼痛治疗中，特别是在炎性，术后，急诊室（ER），突破性，神经性和癌症疼痛治疗和使用NKI-受体拮抗剂在制备用于预防和/或治疗基于阿片样物质的疼痛治疗中的呼吸抑制和耐受的药物中的用途。根据本发明的药物制剂包含根据通式（I）的NK1-拮抗剂，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，其中所有取代基被定义如权利要求1所述。根据本发明的药物组合物在很大程度上降低了与阿片类镇痛药相关的许多不希望的副作用，特别是呼吸抑制和耐受性，从而增加所述阿片样物质在疼痛治疗中的总耐受性。

10. 发明申请

WO2002100862A2 NOVEL SUBSTITUTED TETRACYCLIC IMIDAZOLE DERIVATIVES, PROCESSES FOR THEIR PREPARATION, PHARMACEUTICAL COMPOSITIONS COMPRISING THEM AND THEIR USE AS A MEDICINE 审中-公开
标题翻译：新型取代的四唑咪唑衍生物，其制备方法，包含它们的药物组合物及其作为药物的用途
公开(公告)号：WO2002100862A2
公开(公告)日：2002-12-19
申请号：PCT/EP2002/006576
申请日：2002-06-11
申请人： JANSSEN PHARMACEUTICA N.V. , JANSSENS, Frans, Eduard , LEENAERTS, Joseph, Elisabeth , VAN ROSSEM, Koenraad, Arthur , ALCÁZAR-VACA, Manuel, Jesús , MARTÍNEZ-JIMÉNEZ, Pedro , BARTOLOMÉ-NEBREDA, José, Manuel , GÓMEZ-SÁNCHEZ, Antonio , FERNÁNDEZ-GADEA, Francisco, Javier , VAN REEMPTS, Jos
发明人： JANSSENS, Frans, Eduard , LEENAERTS, Joseph, Elisabeth , VAN ROSSEM, Koenraad, Arthur , ALCÁZAR-VACA, Manuel, Jesús , MARTÍNEZ-JIMÉNEZ, Pedro , BARTOLOMÉ-NEBREDA, José, Manuel , GÓMEZ-SÁNCHEZ, Antonio , FERNÁNDEZ-GADEA, Francisco, Javier , VAN REEMPTS, Jos
IPC分类号： C07D487/00
CPC分类号： C07D487/04 , C07D471/04
摘要： The invention concerns novel substituted tetracyclic imidazole derivatives useful for the treatment of elevated intracranial pressure (ICP) and/or secondary ischaemia, in particular caused by brain injury, more in particular caused by traumatic (TBI) and non-traumatic brain injury, processes for their preparation, pharmaceutical compositions comprising them and their use as a medicine. The novel compounds comprise compounds according to the general Formula (I), the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof and the N -oxide form thereof. In particular, the preferred compound is 3-[2-[4-(11,12-dihydro-6 H -benzimidazo[2,1-b][3]benzazepin-6-yl)-2-(phenylmethyl)-1-piperidinyl]ethyl]-2,10-dimethyl pyrimido[1,2- a ]benzimidazol-4(10 H )-one, the pharmaceutically acceptable acid or base addition salts thereof, the stereochemically isomeric forms thereof and the N -oxide form thereof.
摘要翻译：本发明涉及可用于治疗升高的颅内压（ICP）和/或继发性缺血的新型取代的四环咪唑衍生物，特别是由脑损伤引起的，特别是由创伤性（TBI）和非创伤性脑损伤引起的其制备方法，包含它们的药物组合物及其作为药物的用途。新化合物包括根据通式（I）的化合物，其药学上可接受的酸或碱加成盐，其立体化学异构形式和其N-氧化物形式。特别地，优选的化合物是3- [2- [4-（11,12-二氢-6H-苯并咪唑并[2,1-b] [3]苯并氮杂-6-基） - 2-（苯基甲基）-1-哌啶基]乙基] -2,10-二甲基嘧啶并[1,2-a]苯并咪唑-4（10H） - 酮，其药学上可接受的酸或碱加成盐，其立体化学异构形式和其N-氧化物形式。

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