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1.发明申请Modulation of central nervous system (CNS) dipeptidyl peptidase IV (DPIV)-like activity for the treatment of neurological and neuropsychological disorders 有权调节中枢神经系统（CNS）二肽基肽酶IV（DPIV）样活性用于治疗神经和神经心理障碍公开(公告)号：US20060252701A1
公开(公告)日：2006-11-09
申请号：US11397281
申请日：2006-04-04
申请人： Stephan von Hoersten , Ants Kask , Hans-Ulrich Demuth , Huu Nguyen , Susanne Kruber , Matthias Hoffmann
发明人： Stephan von Hoersten , Ants Kask , Hans-Ulrich Demuth , Huu Nguyen , Susanne Kruber , Matthias Hoffmann
IPC分类号： A61K38/04
CPC分类号： A61K31/426 , A61K31/40 , A61K38/2271 , A61K45/06 , A61K2300/00
摘要： The present invention discloses a method for therapeutically treating an animal, including a human, for psychosomatic, depressive and neuropsychiatric diseases, such as anxiety, depression, insomnia, schizophrenia, epilepsy, spasm and chronic pain. Administration of a suitable DP IV inhibitor causes the reduction of activity in the enzyme dipeptidyl peptidase (DP IV or CD 26) or of DP IV—like enzyme activity in the brain of mammals and leads as a causal consequence to a reduced degradation of the neuropeptide Y (NPY) and similar substrates by DP IV and DP IV-like enzymes. Such treatment will result in a reduction or delay in the decrease of the concentration of functionally active neuronal NPY (1-36). As a consequence of the resulting enhanced stability of the endogenous NPY (1-36) caused by the inhibition of DP IV activity, NPY activity is prolonged thereby resulting among other things in functionally active NPY Y1 receptor activity thereby facilitating antidepressive, anxiolytic, analgesic, antihypertension and other neurological effects.
摘要翻译： 本发明公开了一种治疗性处理动物（包括人）用于心身，抑郁和神经精神疾病如焦虑，抑郁，失眠，精神分裂症，癫痫，痉挛和慢性疼痛的方法。 施用合适的DP IV抑制剂导致哺乳动物脑中的酶二肽基肽酶（DP IV或CD 26）或DP IV样酶活性的活性降低，并导致神经肽降低的降低的因果结果 Y（NPY）和类似底物的DP IV和DP IV样酶。 这种治疗将导致功能活跃的神经元NPY（1-36）的浓度降低或延迟。 由于由抑制DP IV活性引起的内源性NPY（1-36）的增强的稳定性，NPY活性延长，从而导致功能活性的NPY Y1受体活性，从而促进抗抑郁，抗焦虑，止痛， 抗高血压等神经功能。
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2.发明授权Dipeptidyl peptidase IV inhibitors for the treatment of schizophrenia and depression 有权二肽基肽酶IV抑制剂用于治疗精神分裂症和抑郁症公开(公告)号：US08168199B2
公开(公告)日：2012-05-01
申请号：US12202774
申请日：2008-09-02
申请人： Hans-Ulrich Demuth , Ants Kask , Huu Phuc Nguyen , Stephan von Hoersten , Susanne Kruber , Matthias Hoffmann
发明人： Hans-Ulrich Demuth , Ants Kask , Huu Phuc Nguyen , Stephan von Hoersten , Susanne Kruber , Matthias Hoffmann
CPC分类号： A61K31/426 , A61K31/40 , A61K38/2271 , A61K45/06 , A61K2300/00
摘要： A method for therapeutically treating an animal, including a human, for psychosomatic, depressive and neuropsychiatric diseases, such as anxiety, depression, insomnia, schizophrenia, epilepsy, spasm and chronic pain. Administration of a suitable DP IV inhibitor causes the reduction of activity in the enzyme dipeptidyl peptidase (DP IV or CD 26) or of DP IV-like enzyme activity in the brain of mammals and leads as a causal consequence to a reduced degradation of the neuropeptide Y (NPY) and similar substrates by DP IV and DP IV-like enzymes. Such treatment will result in a reduction or delay in the decrease of the concentration of functionally active neuronal NPY (1-36). As a consequence of the resulting enhanced stability of the endogenous NPY (1-36) caused by the inhibition of DP IV activity, NPY activity is prolonged thereby resulting among other things in functionally active NPY Y1 receptor activity thereby facilitating antidepressive, anxiolytic, analgesic, antihypertension and other neurological effects.
摘要翻译： 用于治疗性处理动物，包括人的用于心身，抑郁和神经精神疾病如焦虑，抑郁，失眠，精神分裂症，癫痫，痉挛和慢性疼痛的方法。 施用合适的DP IV抑制剂导致哺乳动物脑中的酶二肽基肽酶（DP IV或CD 26）或DP IV样酶活性的活性降低，并导致神经肽降低的降低的因果结果 Y（NPY）和类似底物的DP IV和DP IV样酶。 这种治疗将导致功能活跃的神经元NPY（1-36）的浓度降低或延迟。 由于由抑制DP IV活性引起的内源性NPY（1-36）的增强的稳定性，NPY活性延长，从而导致功能活性的NPY Y1受体活性，从而促进抗抑郁，抗焦虑，止痛， 抗高血压等神经功能。
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3.发明申请DIPEPTIDYL PEPTIDASE IV INHIBITORS FOR THE TREATMENT OF SCHIZOPHRENIA AND DEPRESSION 有权用于治疗精神分裂症和抑郁症的替代肽第四剂抑制剂公开(公告)号：US20090062203A1
公开(公告)日：2009-03-05
申请号：US12202774
申请日：2008-09-02
申请人： Hans-Ulrich Demuth , Ants Kask , Huu Phuc Nguyen , Stephan von Hoersten , Susanne Kruber , Matthias Hoffmann
发明人： Hans-Ulrich Demuth , Ants Kask , Huu Phuc Nguyen , Stephan von Hoersten , Susanne Kruber , Matthias Hoffmann
CPC分类号： A61K31/426 , A61K31/40 , A61K38/2271 , A61K45/06 , A61K2300/00
摘要： A method for therapeutically treating an animal, including a human, for psychosomatic, depressive and neuropsychiatric diseases, such as anxiety, depression, insomnia, schizophrenia, epilepsy, spasm and chronic pain. Administration of a suitable DP IV inhibitor causes the reduction of activity in the enzyme dipeptidyl peptidase (DP IV or CD 26) or of DP IV-like enzyme activity in the brain of mammals and leads as a causal consequence to a reduced degradation of the neuropeptide Y (NPY) and similar substrates by DP IV and DP IV-like enzymes. Such treatment will result in a reduction or delay in the decrease of the concentration of functionally active neuronal NPY (1-36). As a consequence of the resulting enhanced stability of the endogenous NPY (1-36) caused by the inhibition of DP IV activity, NPY activity is prolonged thereby resulting among other things in functionally active NPY Y1 receptor activity thereby facilitating antidepressive, anxiolytic, analgesic, antihypertension and other neurological effects.
摘要翻译： 用于治疗性处理动物，包括人的用于心身，抑郁和神经精神疾病如焦虑，抑郁，失眠，精神分裂症，癫痫，痉挛和慢性疼痛的方法。 施用合适的DP IV抑制剂导致哺乳动物脑中的酶二肽基肽酶（DP IV或CD 26）或DP IV样酶活性的活性降低，并导致神经肽降低的降低的因果结果 Y（NPY）和类似底物的DP IV和DP IV样酶。 这种治疗将导致功能活跃的神经元NPY（1-36）的浓度降低或延迟。 由于由抑制DP IV活性引起的内源性NPY（1-36）的增强的稳定性，NPY活性延长，从而导致功能活性的NPY Y1受体活性，从而促进抗抑郁，抗焦虑，止痛， 抗高血压等神经功能。
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公开(公告)号：US07435420B2
公开(公告)日：2008-10-14
申请号：US11397281
申请日：2006-04-04
申请人： Stephan von Hoersten , Ants Kask , Hans-Ulrich Demuth , Huu Phuc Nguyen , Susanne Kruber , Matthias Hoffmann
发明人： Stephan von Hoersten , Ants Kask , Hans-Ulrich Demuth , Huu Phuc Nguyen , Susanne Kruber , Matthias Hoffmann
CPC分类号： A61K31/426 , A61K31/40 , A61K38/2271 , A61K45/06 , A61K2300/00
摘要： The present invention discloses a method for therapeutically treating an animal, including a human, for psychosomatic, depressive and neuropsychiatric diseases, such as anxiety, depression, insomnia, schizophrenia, epilepsy, spasm and chronic pain.Administration of a suitable DP IV inhibitor causes the reduction of activity in the enzyme dipeptidyl peptidase (DP IV or CD 26) or of DP IV—like enzyme activity in the brain of mammals and leads as a causal consequence to a reduced degradation of the neuropeptide Y (NPY) and similar substrates by DP IV and DP IV-like enzymes. Such treatment will result in a reduction or delay in the decrease of the concentration of functionally active neuronal NPY (1-36). As a consequence of the resulting enhanced stability of the endogenous NPY (1-36) caused by the inhibition of DP IV activity, NPY activity is prolonged thereby resulting among other things in functionally active NPY Y1 receptor activity thereby facilitating antidepressive, anxiolytic, analgesic, antihypertension and other neurological effects.
摘要翻译： 本发明公开了一种治疗性处理动物（包括人）用于心身，抑郁和神经精神疾病如焦虑，抑郁，失眠，精神分裂症，癫痫，痉挛和慢性疼痛的方法。 施用合适的DP IV抑制剂导致哺乳动物脑中的酶二肽基肽酶（DP IV或CD 26）或DP IV样酶活性的活性降低，并导致神经肽降低的降低的因果结果 Y（NPY）和类似底物的DP IV和DP IV样酶。 这种治疗将导致功能活跃的神经元NPY（1-36）的浓度降低或延迟。 由于由抑制DP IV活性引起的内源性NPY（1-36）的增强的稳定性，NPY活性延长，从而导致功能活性的NPY Y1受体活性，从而促进抗抑郁，抗焦虑，止痛， 抗高血压等神经功能。
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5.发明授权Modulation of central nervous system (CNS) dipeptidyl peptidase IV (DPIV) -like activity for the treatment of neurological and neuropsychological disorders 有权调节中枢神经系统（CNS）二肽基肽酶IV（DPIV）样活性用于治疗神经和神经心理障碍公开(公告)号：US07132104B1
公开(公告)日：2006-11-07
申请号：US10014291
申请日：2001-10-26
申请人： Stephan von Horsten , Ants Kask , Hans-Ulrich Demuth , Huu Phuc Nguyen , Susanne Kruber , Matthias Hoffmann
发明人： Stephan von Horsten , Ants Kask , Hans-Ulrich Demuth , Huu Phuc Nguyen , Susanne Kruber , Matthias Hoffmann
CPC分类号： A61K31/426 , A61K31/40 , A61K38/2271 , A61K45/06 , A61K2300/00
摘要： The present invention discloses a method for therapeutically treating an animal, including a human, for psychosomatic, depressive and neuropsychiatric diseases, such as anxiety, depression, insomnia, schizophrenia, epilepsy, spasm and chronic pain. Administration of a suitable DP IV inhibitor causes the reduction of activity in the enzyme dipeptidyl peptidase (DP IV or CD 26) or of DP IV-like enzyme activity in the brain of mammals and leads as a causal consequence to a reduced degradation of the neuropeptide Y (NPY) and similar substrates by DP IV and DP IV-like enzymes. Such treatment will result in a reduction or delay in the decrease of the concentration of functionally active neuronal NPY (1–36). As a consequence of the resulting enhanced stability of the endogenous NPY (1–36) caused by the inhibition of DP IV activity, NPY activity is prolonged thereby resulting among other things in functionally active NPY Y1 receptor activity thereby facilitating anti-depressive, anxiolytic, analgesic, anti-hypertension and other neurological effects.
摘要翻译： 本发明公开了一种治疗性处理动物（包括人）用于心身，抑郁和神经精神疾病如焦虑，抑郁，失眠，精神分裂症，癫痫，痉挛和慢性疼痛的方法。 施用合适的DP IV抑制剂导致哺乳动物脑中的酶二肽基肽酶（DP IV或CD 26）或DP IV样酶活性的活性降低，并导致神经肽降低的降低的因果结果 Y（NPY）和类似底物的DP IV和DP IV样酶。 这种治疗将导致功能活跃的神经元NPY（1-36）的浓度降低或延迟。 由于由抑制DP IV活性引起的内源性NPY（1-36）的增强的稳定性，NPY活性延长，从而导致功能活性的NPY Y1受体活性，从而促进抗抑郁，抗焦虑， 止痛，抗高血压等神经功能。
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