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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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公开(公告)号：US20050203030A1
公开(公告)日：2005-09-15
申请号：US10727209
申请日：2003-12-02
IPC分类号： C07D295/18 , A61K31/40 , A61K31/425 , A61K31/426 , A61K31/427 , A61K31/495 , A61K38/00 , A61K45/06 , A61P3/06 , A61P3/10 , A61P13/12 , A61P43/00 , C07D207/34 , C07D277/04 , C07D295/185 , C07D417/00 , C07D417/12 , C07K5/06 , A61K38/04 , C07K5/04
CPC分类号： C07D295/185 , A61K31/40 , A61K31/425 , A61K31/426 , A61K31/427 , A61K45/06 , C07D277/04 , A61K2300/00
摘要： Dipeptide compounds and compounds analogous to dipeptide compounds that are formed from an amino acid and a thiazolidine or pyrrolidine group, and salts thereof used in the treatment of impaired glucose tolerance, glycosuria, hyperlipidaemia, metabolic acidoses, diabetes mellitus, diabetic neuropathy and nephropathy and also of sequelae of diabetes mellitus in mammals.
摘要翻译： 二肽化合物和类似于由氨基酸和噻唑烷或吡咯烷基组成的二肽化合物的化合物及其盐用于治疗葡萄糖耐量异常，糖尿病，高脂血症，代谢性酸痛，糖尿病，糖尿病性神经病变和肾病等 的哺乳动物糖尿病后遗症。
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公开(公告)号：US20080182798A1
公开(公告)日：2008-07-31
申请号：US11443389
申请日：2006-05-30
IPC分类号： A61K38/00 , C07C205/00 , A61P1/00
CPC分类号： C07D295/185 , A61K31/40 , A61K31/425 , A61K31/426 , A61K31/427 , A61K45/06 , C07D277/04 , A61K2300/00
摘要： Dipeptide compounds and compounds analogous to dipeptide compounds that are formed from an amino acid and a thiazolidine or pyrrolidine group, and salts thereof used in the treatment of impaired glucose tolerance, glycosuria, hyperlipidaemia, metabolic acidoses, diabetes mellitus, diabetic neuropathy and nephropathy and also of sequelae of diabetes mellitus in mammals.
摘要翻译： 二肽化合物和类似于由氨基酸和噻唑烷或吡咯烷基组成的二肽化合物的化合物及其盐用于治疗葡萄糖耐量异常，糖尿病，高脂血症，代谢性酸痛，糖尿病，糖尿病性神经病变和肾病等 的哺乳动物糖尿病后遗症。
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公开(公告)号：US06548481B1
公开(公告)日：2003-04-15
申请号：US09723638
申请日：2000-11-28
IPC分类号： A61K3805
CPC分类号： C07D295/185 , A61K31/40 , A61K31/425 , A61K31/426 , A61K31/427 , A61K45/06 , C07D277/04 , A61K2300/00
摘要： Dipeptide compounds and compounds analogous to dipeptide compounds that are formed from an amino acid and a thiazolidine or pyrrolidine group, and salts thereof used in the treatment of impaired glucose tolerance, glycosuria, hyperlipidaemia, metabolic acidoses, diabetes mellitus, diabetic neuropathy and nephropathy and also of sequelae of diabetes mellitus in mammals.
摘要翻译： 二肽化合物和类似于由氨基酸和噻唑烷或吡咯烷基组成的二肽化合物的化合物及其盐用于治疗葡萄糖耐量异常，糖尿病，高脂血症，代谢性酸痛，糖尿病，糖尿病性神经病变和肾病等 的哺乳动物糖尿病后遗症。
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公开(公告)号：US06559314B2
公开(公告)日：2003-05-06
申请号：US10012786
申请日：2001-12-10
申请人： Hans-Ulrich Demuth , Susanne Kruber
发明人： Hans-Ulrich Demuth , Susanne Kruber
IPC分类号： C07D22704
CPC分类号： C07D277/04
摘要： The invention relates to a simple and industrially readily executable method of producing thiazolidine base and salts thereof. In particular, the invention relates to a process for the production of thiazolidine base and salts thereof which is characterized in that hexamethylenetetramine of formula (I) is caused to react with cysteamine or salts thereof of formula (II) in which X(−) represents an acid residue, X(−) being preferably a halide or sulfate.
摘要翻译： 本发明涉及一种生产噻唑烷碱及其盐的简单且工业上易于执行的方法。 特别地，本发明涉及一种制备噻唑烷碱及其盐的方法，其特征在于使式（I）的六亚甲基四胺与式（II）的半胱胺或其盐反应，其中X（ - ）表示 酸残基X（ - ）优选为卤化物或硫酸盐。
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