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公开(公告)号：US20070197514A1
公开(公告)日：2007-08-23
申请号：US11636599
申请日：2006-12-11
申请人： Abraham Nudelman , Ada Rephaeli , Irit Gil-Ad , Abraham Weizman
发明人： Abraham Nudelman , Ada Rephaeli , Irit Gil-Ad , Abraham Weizman
IPC分类号： A61K31/5415 , C07D279/22
CPC分类号： C07D279/28 , A61K31/16 , A61K31/4172 , A61K31/5415 , A61K47/54 , A61K47/542 , A61K47/55
摘要： Novel chemical conjugates of psychotropic drugs and organic acids, uses thereof in the treatment of psychotic and/or proliferative disorders and diseases and as chemosensitizing agents, and their syntheses are disclosed. The organic acids are selected to reduce side effects induced by the psychotropic drugs and/or to exert an anti-proliferative activity.
摘要翻译： 公开了精神药物和有机酸的新型化学共轭物，其用于治疗精神病和/或增殖性疾病和疾病以及作为化学增敏剂的用途及其合成。 选择有机酸以减少由精神药物引起的副作用和/或发挥抗增殖活性。
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12.发明授权Conjugates comprising a psychotropic drug or a GABA agonist and an organic acid and their use in treating pain and other CNS disorders 失效包含精神药物或GABA激动剂和有机酸的缀合物及其在治疗疼痛和其它中枢神经系统疾病中的用途公开(公告)号：US08377990B2
公开(公告)日：2013-02-19
申请号：US12309361
申请日：2007-07-17
申请人： Abraham Nudelman , Ada Rephaeli , Irit Gil-Ad , Abraham Weizman
发明人： Abraham Nudelman , Ada Rephaeli , Irit Gil-Ad , Abraham Weizman
IPC分类号： A01N37/18 , A61K31/16 , C07C233/00 , C07C235/00 , C07C237/00 , C07C239/00
摘要： A novel use of conjugates of psychotropic drugs (e.g., antidepressants or anti-epileptic drugs) and organic acids such as GABA in the treatment of pain is disclosed. A novel GABA conjugate and uses thereof is also disclosed.
摘要翻译： 公开了一种在治疗疼痛中使用精神药物（例如抗抑郁药或抗癫痫药物）和有机酸（例如GABA）的新型用途。 还公开了一种新型的GABA缀合物及其用途。
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13.发明授权Crystalline forms of the tri-mesylate salt of perphenazine-GABA and process of producing the same 有权奋乃静-GABA三甲磺酸盐的结晶形式及其制备方法公开(公告)号：US08377929B2
公开(公告)日：2013-02-19
申请号：US13034453
申请日：2011-02-24
申请人： Abraham Nudelman , Ada Rephaeli , Irit Gil-Ad , Abraham Weizman , Mazal Shaul , Efrat Halbfinger
发明人： Abraham Nudelman , Ada Rephaeli , Irit Gil-Ad , Abraham Weizman , Mazal Shaul , Efrat Halbfinger
IPC分类号： A61K31/5415 , C07D417/06 , A61P25/28 , A61P25/00 , A61P25/18 , B32B5/16 , B65D79/00
CPC分类号： C07D417/06 , C07D279/28 , Y10T428/2982
摘要： Novel crystalline form of perphenazine 4-aminobutyrate trimesylate and a process of producing the same are disclosed. The novel crystalline form is characterized by a unique XRPD pattern and a DSC that exhibits an endothermic peak at a relatively high temperature (e.g., higher than 209° C.). Also disclosed are a process of preparing perphenazine 4-aminobutyrate trimesylate by in situ deprotection and salification, in a single-step synthesis, and a highly pure perphenazine 4-aminobutyrate trimesylate obtained thereby. Uses of any of the described perphenazine 4-aminobutyrate trimesylate are also disclosed.
摘要翻译： 公开了4-氨基丁酸三苯甲磺隆的奋乃静化新型结晶形式及其生产方法。 新型结晶形式的特征在于独特的XRPD图案和DSC，其在相对较高的温度（例如高于209℃）下显示出吸热峰。 还公开了通过在单步合成中原位去保护和成盐，以及由此得到的高纯度的奋乃静4-氨基丁酸三苯甲磺酸盐，制备4-氨基丁酸三苯甲基奋乃静化物的方法。 还公开了所述所述的所述4-氨基丁酸三苯甲磺酸激素的用途。
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公开(公告)号：US20120309748A1
公开(公告)日：2012-12-06
申请号：US13586913
申请日：2012-08-16
申请人： Abraham Nudelman , Ada Rephaeli , Irit Gil-ad , Abraham Weizman
发明人： Abraham Nudelman , Ada Rephaeli , Irit Gil-ad , Abraham Weizman
IPC分类号： C07D417/06 , A61P25/18 , A61P25/00 , A61P25/24 , A61P35/04 , A61P25/16 , A61P25/28 , A61P25/08 , A61P35/00 , A61K31/5415 , A61P25/22
CPC分类号： C07D279/28 , A61K31/16 , A61K31/4172 , A61K31/5415 , A61K47/54 , A61K47/542 , A61K47/55
摘要： Novel chemical conjugates of psychotropic drugs and organic acids, uses thereof in the treatment of psychotic and/or proliferative disorders and diseases and as chemosensitizing agents, and their syntheses are disclosed. The organic acids are selected to reduce side effects induced by the psychotropic drugs and/or to exert an anti-proliferative activity.
摘要翻译： 公开了精神药物和有机酸的新型化学共轭物，其用于治疗精神病和/或增殖性疾病和疾病以及作为化学增敏剂的用途及其合成。 选择有机酸以减少由精神药物引起的副作用和/或发挥抗增殖活性。
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公开(公告)号：US20100120755A1
公开(公告)日：2010-05-13
申请号：US12656048
申请日：2010-01-14
申请人： Abraham Nudelman , Ada Rephaeli , Irit Gil-Ad , Abraham Weizman
发明人： Abraham Nudelman , Ada Rephaeli , Irit Gil-Ad , Abraham Weizman
IPC分类号： A61K31/5415 , C07D513/00 , C07C229/08 , A61K31/225 , A61P25/18 , A61P35/00 , A61P35/04
CPC分类号： C07D279/28 , A61K31/16 , A61K31/4172 , A61K31/5415 , A61K47/54 , A61K47/542 , A61K47/55
摘要： Novel chemical conjugates of psychotropic drugs and organic acids, uses thereof in the treatment of psychotic and/or proliferative disorders and diseases and as chemosensitizing agents, and their syntheses are disclosed. The organic acids are selected to reduce side effects induced by the psychotropic drugs and/or to exert an anti-proliferative activity.
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16.发明申请Crystalline Forms of the Tri-Mesylate Salt of Perphenazine-Gaba and Process of Producing the Same 有权苯丙嗪Gaba的三甲磺酸盐的结晶形式及其生产方法公开(公告)号：US20110312948A1
公开(公告)日：2011-12-22
申请号：US13034453
申请日：2011-02-24
申请人： Abraham Nudelman , Ada Rephaeli , Irit Gil-Ad , Abraham Weizman , Mazal Shaul , Efrat Halbfinger
发明人： Abraham Nudelman , Ada Rephaeli , Irit Gil-Ad , Abraham Weizman , Mazal Shaul , Efrat Halbfinger
IPC分类号： A61K31/5415 , A61P25/28 , B65D79/00 , A61P25/18 , B32B5/16 , C07D417/06 , A61P25/00
CPC分类号： C07D417/06 , C07D279/28 , Y10T428/2982
摘要： Novel crystalline form of perphenazine 4-aminobutyrate trimesylate and a process of producing the same are disclosed. The novel crystalline form is characterized by a unique XRPD pattern and a DSC that exhibits an endothermic peak at a relatively high temperature (e.g., higher than 209° C.). Also disclosed are a process of preparing perphenazine 4-aminobutyrate trimesylate by in situ deprotection and salification, in a single-step synthesis, and a highly pure perphenazine 4-aminobutyrate trimesylate obtained thereby. Uses of any of the described perphenazine 4-aminobutyrate trimesylate are also disclosed.
摘要翻译： 公开了4-氨基丁酸三苯甲磺隆的奋乃静化新型结晶形式及其生产方法。 新型结晶形式的特征在于独特的XRPD图案和DSC，其在相对较高的温度（例如高于209℃）下显示出吸热峰。 还公开了通过在单步合成中原位去保护和成盐，以及由此得到的高纯度的奋乃静4-氨基丁酸三苯甲磺酸盐，制备4-氨基丁酸三苯甲基奋乃静化物的方法。 还公开了所述所述的所述4-氨基丁酸三苯甲磺酸激素的用途。
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17.发明申请Conjugates Comprising a gaba-or glycine compound, pharmaceutical compositions and combinations thereof as well as their use in treating cns disorders 失效缀合物包括gaba-或甘氨酸化合物，药物组合物及其组合以及它们在治疗cns病症中的用途公开(公告)号：US20100144869A1
公开(公告)日：2010-06-10
申请号：US12309361
申请日：2007-07-17
申请人： Abraham Nudelman , Ada Rephaeli , Irit Gil-Ad , Abraham Weizman
发明人： Abraham Nudelman , Ada Rephaeli , Irit Gil-Ad , Abraham Weizman
IPC分类号： A61K31/27 , A61K31/225 , A61K31/16 , C07C271/18 , C07C229/24 , C07C237/02 , A61P25/00 , A61P25/30
摘要： A novel use of conjugates of psychotropic drugs (e.g., antidepressants or anti-epileptic drugs) and organic acids such as GABA in the treatment of pain is disclosed. A novel GABA conjugate and uses thereof is also disclosed.
摘要翻译： 公开了一种在治疗疼痛中使用精神药物（例如抗抑郁药或抗癫痫药物）和有机酸（例如GABA）的新型用途。 还公开了一种新型的GABA缀合物及其用途。
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公开(公告)号：US20100063034A1
公开(公告)日：2010-03-11
申请号：US12585021
申请日：2009-09-01
申请人： Abraham Nudelman , Ada Rephaeli , Irit Gil-Ad , Abraham Weizman
发明人： Abraham Nudelman , Ada Rephaeli , Irit Gil-Ad , Abraham Weizman
IPC分类号： A61K31/5415 , C07D279/36 , A61P25/18 , A61P35/00
CPC分类号： C07D279/28 , A61K31/16 , A61K31/4172 , A61K31/5415 , A61K47/54 , A61K47/542 , A61K47/55
摘要： Novel chemical conjugates of psychotropic drugs and organic acids, uses thereof in the treatment of psychotic and/or proliferative disorders and diseases and as chemosensitizing agents, and their syntheses are disclosed. The organic acids are selected to reduce side effects induced by the psychotropic drugs and/or to exert an anti-proliferative activity.
摘要翻译： 公开了精神药物和有机酸的新型化学共轭物，其用于治疗精神病和/或增殖性疾病和疾病以及作为化学增敏剂的用途及其合成。 选择有机酸以减少由精神药物引起的副作用和/或发挥抗增殖活性。
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19.发明申请公开(公告)号：US20090298814A1
公开(公告)日：2009-12-03
申请号：US11921578
申请日：2006-06-07
申请人： Abraham Nudelman , Ada Rephaeli , Irit Gil-Ad , Abraham Weizman , Shlomit Halachmi , Eran J. Benjamin
发明人： Abraham Nudelman , Ada Rephaeli , Irit Gil-Ad , Abraham Weizman , Shlomit Halachmi , Eran J. Benjamin
IPC分类号： A61K31/5415 , C07D417/06
CPC分类号： C07D279/28 , A61K47/542
摘要： Novel chemical conjugates of a psychotropic drug residue and an amino-containing organic acid residue selected to reduce side effects induced by the psychotropic drug when administered per se, to enhance the therapeutic activity of the psychotropic drug and/or to exert anti-proliferative activity, in which the amino group is in the form of an acid addition salt thereof and which are characterized by high stability are disclosed. Further disclosed are processes for preparing the chemical conjugates and addition salts thereof, pharmaceutical compositions containing the chemical conjugates and methods utilizing the chemical conjugates for treating various medical conditions.
摘要翻译： 精神药物残基和含氨基的有机酸残基的新型化学共轭物被选择用于减少精神药物本身引起的副作用，以增强精神药物的治疗活性和/或发挥抗增殖活性， 其中氨基为其酸加成盐的形式，其特征在于高稳定性。 进一步公开的是制备化学共轭物及其加成盐的方法，含有化学共轭物的药物组合物和利用化学共轭物治疗各种医学病症的方法。
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公开(公告)号：US07544681B2
公开(公告)日：2009-06-09
申请号：US10808541
申请日：2004-03-25
申请人： Abraham Nudelman , Ada Rephaeli , Irit Gil-Ad , Abraham Weizman
发明人： Abraham Nudelman , Ada Rephaeli , Irit Gil-Ad , Abraham Weizman
IPC分类号： A61K31/54 , A61P25/18 , C07D417/06
CPC分类号： C07D279/28 , A61K31/16 , A61K31/4172 , A61K31/5415 , A61K47/54 , A61K47/542 , A61K47/55
摘要： Novel chemical conjugates of psychotropic drugs and organic acids, uses thereof in the treatment of psychotic and/or proliferative disorders and diseases and as chemosensitizing agents, and their syntheses are disclosed. The organic acids are selected to reduce side effects induced by the psychotropic drugs and/or to exert an anti-proliferative activity.
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