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1. 发明授权

US07381745B2 Ligands for metabotropic glutamate receptors and inhibitors of NAALADase 有权
标题翻译：代谢型谷氨酸受体配体和NAALADase抑制剂
公开(公告)号：US07381745B2
公开(公告)日：2008-06-03
申请号：US10374765
申请日：2003-02-25
申请人： Alan P. Kozikowski , Jarda T. Wroblewski , Fajun Nan
发明人： Alan P. Kozikowski , Jarda T. Wroblewski , Fajun Nan
IPC分类号： A61K31/662 , C07F9/32 , C07F9/36
CPC分类号： C07D257/04 , C07C59/347 , C07C69/716 , C07C271/22 , C07C275/16 , C07C275/26 , C07C323/59 , C07C335/08 , C07F9/301 , C07F9/303
摘要： The present invention relates to novel compounds and formulations thereof which compounds are ligands, e.g., agonists or antagonists, for a metabotropic glutamate receptor or a NAALADase enzyme or both. The present invention also relates to methods of modulating the activity of a metabotropic glutamate receptor or a NAALADase enzyme or both, e.g., in a subject in need thereof, using a compound or formulation of the present invention. The present invention also relates to methods of treating a subject suffering from a chronic or acute disease, malady or condition due at least in part to an abnormality in the activity of an endogenous metabotropic glutamate receptor or a NAALADase enzyme or both, using a compound or formulation of the present invention.
摘要翻译：本发明涉及其化合物是代谢型谷氨酸受体或NAALADase酶或两者的配体，例如激动剂或拮抗剂的新化合物及其制剂。本发明还涉及使用本发明的化合物或制剂调节代谢型谷氨酸受体或NAALADase酶或两者的活性的方法，例如在有需要的受试者中。本发明还涉及使用化合物或至少部分由内源性代谢型谷氨酸受体或NAALADase酶或两者的活性异常而治疗患有慢性或急性疾病，疾病或病症的受试者的方法，本发明的制剂。

2. 发明授权

US08609721B2 Ligands for metabotropic glutamate receptors and inhibitors of NAALADase 有权
公开(公告)号：US08609721B2
公开(公告)日：2013-12-17
申请号：US12029367
申请日：2008-02-11
申请人： Alan P. Kozikowski , Jarda T. Wroblewski , Fajun Nan
发明人： Alan P. Kozikowski , Jarda T. Wroblewski , Fajun Nan
IPC分类号： A61K31/662 , C07F9/32 , C07F9/36
CPC分类号： C07D257/04 , C07C59/347 , C07C69/716 , C07C271/22 , C07C275/16 , C07C275/26 , C07C323/59 , C07C335/08 , C07F9/301 , C07F9/303
摘要： The present invention relates to novel compounds and formulations thereof which compounds are ligands, e.g., agonists or antagonists, for a metabotropic glutamate receptor or a NAALADase enzyme or both. The present invention also relates to methods of modulating the activity of a metabotropic glutamate receptor or a NAALADase enzyme or both, e.g., in a subject in need thereof, using a compound or formulation of the present invention. The present invention also relates to methods of treating a subject suffering from a chronic or acute disease, malady or condition due at least in part to an abnormality in the activity of an endogenous metabotropic glutamate receptor or a NAALADase enzyme or both, using a compound or formulation of the present invention.

3. 发明申请

US20080176821A1 LIGANDS FOR METABOTROPIC GLUTAMATE RECEPTORS AND INHIBITORS OF NAALADASE 有权
标题翻译：代谢谷氨酸受体和NAALADASE抑制剂的配体
公开(公告)号：US20080176821A1
公开(公告)日：2008-07-24
申请号：US12029367
申请日：2008-02-11
申请人： Alan P. Kozikowski , Jarda T. Wroblewski , Fajun Nan
发明人： Alan P. Kozikowski , Jarda T. Wroblewski , Fajun Nan
IPC分类号： A61K31/664 , A61K31/662 , A61K31/195 , A61K31/225 , A61P25/00 , A61P25/02 , A61P25/18
CPC分类号： C07D257/04 , C07C59/347 , C07C69/716 , C07C271/22 , C07C275/16 , C07C275/26 , C07C323/59 , C07C335/08 , C07F9/301 , C07F9/303
摘要： The present invention relates to novel compounds and formulations thereof which compounds are ligands, e.g., agonists or antagonists, for a metabotropic glutamate receptor or a NAALADase enzyme or both. The present invention also relates to methods of modulating the activity of a metabotropic glutamate receptor or a NAALADase enzyme or both, e.g., in a subject in need thereof, using a compound or formulation of the present invention. The present invention also relates to methods of treating a subject suffering from a chronic or acute disease, malady or condition due at least in part to an abnormality in the activity of an endogenous metabotropic glutamate receptor or a NAALADase enzyme or both, using a compound or formulation of the present invention.
摘要翻译：本发明涉及其化合物是代谢型谷氨酸受体或NAALADase酶或两者的配体，例如激动剂或拮抗剂的新化合物及其制剂。本发明还涉及使用本发明的化合物或制剂调节代谢型谷氨酸受体或NAALADase酶或两者的活性的方法，例如在有需要的受试者中。本发明还涉及使用化合物或至少部分由内源性代谢型谷氨酸受体或NAALADase酶或两者的活性异常而治疗患有慢性或急性疾病，疾病或病症的受试者的方法，本发明的制剂。

4. 发明授权

US06528499B1 Ligands for metabotropic glutamate receptors and inhibitors of NAALADase 有权
标题翻译：代谢型谷氨酸受体配体和NAALADase抑制剂
公开(公告)号：US06528499B1
公开(公告)日：2003-03-04
申请号：US09662767
申请日：2000-09-15
申请人： Alan P. Kozikowski , Jarda T. Wroblewski , Fajun Nan
发明人： Alan P. Kozikowski , Jarda T. Wroblewski , Fajun Nan
IPC分类号： A61K3166
CPC分类号： C07D257/04 , C07C59/347 , C07C69/716 , C07C271/22 , C07C275/16 , C07C275/26 , C07C323/59 , C07C335/08 , C07F9/301 , C07F9/303
摘要： The present invention relates to novel compounds and formulations thereof which compounds are ligands, e.g., agonists or antagonists, for a metabotropic glutamate receptor or a NAALADase enzyme or both. The present invention also relates to methods of modulating the activity of a metabotropic glutamate receptor or a NAALADase enzyme or both, e.g., in a subject in need thereof, using a compound or formulation of the present invention. The present invention also relates to methods of treating a subject suffering from a chronic or acute disease, malady or condition due at least in part to an abnormality in the activity of an endogenous metabotropic glutamate receptor or a NAALADase enzyme or both, using a compound or formulation of the present invention.
摘要翻译：本发明涉及其化合物是代谢型谷氨酸受体或NAALADase酶或两者的配体，例如激动剂或拮抗剂的新化合物及其制剂。本发明还涉及使用本发明的化合物或制剂调节代谢型谷氨酸受体或NAALADase酶或两者的活性的方法，例如在有需要的受试者中。本发明还涉及使用化合物或至少部分由内源性代谢型谷氨酸受体或NAALADase酶或两者的活性异常而治疗患有慢性或急性疾病，疾病或病症的受试者的方法，本发明的制剂。

5. 发明授权

US06479470B1 Ligands for metabotropic glutamate receptors and inhibitors of NAALAdase 有权
标题翻译：代谢型谷氨酸受体配体和NAALAdase抑制剂
公开(公告)号：US06479470B1
公开(公告)日：2002-11-12
申请号：US09559978
申请日：2000-04-27
申请人： Alan P. Kozikowski , Jarda T. Wroblewski , Fajun Nan
发明人： Alan P. Kozikowski , Jarda T. Wroblewski , Fajun Nan
IPC分类号： A61K3166
CPC分类号： C07C335/08 , C07C59/347 , C07C69/716 , C07F9/301
摘要： The present invention relates to novel compounds and formulations thereof which compounds are ligands, e.g., agonists or antagonists, for a metabotropic glutamate receptor or a NAALADase enzyme or both. The present invention also relates to methods of modulating the activity of a metabotropic glutamate receptor or a NAALADase enzyme or both, e.g., in a subject in need thereof, using a compound or formulation of the present invention. The present invention also relates to methods of treating a subject suffering from a chronic or acute disease, malady or condition due at least in part to an abnormality in the activity of an endogenous metabotropic glutamate receptor or a NAALADase enzyme or both, using a compound or formulation of the present invention.
摘要翻译：本发明涉及其化合物是代谢型谷氨酸受体或NAALADase酶或两者的配体，例如激动剂或拮抗剂的新化合物及其制剂。本发明还涉及使用本发明的化合物或制剂调节代谢型谷氨酸受体或NAALADase酶或两者的活性的方法，例如在有需要的受试者中。本发明还涉及使用化合物或至少部分由内源性代谢型谷氨酸受体或NAALADase酶或两者的活性异常而治疗患有慢性或急性疾病，疾病或病症的受试者的方法，本发明的制剂。

6. 发明授权

US4990504A Azetidine derivatives to treat memory and learning disorders 失效
标题翻译：氮杂环丁烷衍生物治疗记忆障碍和学习障碍
公开(公告)号：US4990504A
公开(公告)日：1991-02-05
申请号：US210917
申请日：1988-06-24
申请人： Alan P. Kozikowski , Jarda T. Wroblewski , Erminio Costa
发明人： Alan P. Kozikowski , Jarda T. Wroblewski , Erminio Costa
IPC分类号： C07D205/04 , C07K5/078
CPC分类号： C07K5/06139 , C07D205/04
摘要： This invention relates to novel azetidines and derivatives thereof, as well as to pharmaceutical compositions and methods of treating memory and learning disorders. Another aspect of the invention relates to a method of utilizing the compounds and compositions as biological tools and materials for characterizing excitatory amino acid receptor systems. A further aspect of the invention relates to a method of treating PCP toxicity and abuse.
摘要翻译：本发明涉及新的氮杂环丁烷及其衍生物，以及治疗记忆和学习障碍的药物组合物和方法。本发明的另一方面涉及一种利用化合物和组合物作为表征兴奋性氨基酸受体系统的生物工具和材料的方法。本发明的另一方面涉及一种治疗PCP毒性和滥用的方法。

7. 发明授权

US08445684B2 Nicotinic acetylcholine receptor ligands and the uses thereof 失效
标题翻译：烟碱乙酰胆碱受体配体及其用途
公开(公告)号：US08445684B2
公开(公告)日：2013-05-21
申请号：US12578020
申请日：2009-10-13
申请人： Jayaraman Chandrasekhar , Alan P. Kozikowski , Jianhua Liu , Werner Tueckmantel , Joel R. Walker , Po-wai Yuen
发明人： Jayaraman Chandrasekhar , Alan P. Kozikowski , Jianhua Liu , Werner Tueckmantel , Joel R. Walker , Po-wai Yuen
IPC分类号： C07D409/00 , C07D411/00 , C07D413/00 , C07D417/00 , C07D401/00 , C07D421/00
CPC分类号： C07D401/12 , C07D401/14 , C07D413/14 , C07D471/18
摘要： The invention relates to pyridinyl nicotinic acetylcholine receptor ligands, compositions comprising an effective amount of a pyridinyl nicotinic acetylcholine receptor ligand and methods to treat or prevent a condition, such as depression and nicotine dependence, comprising administering to an animal in need thereof an effective amount of a pyridinyl nicotinic acetylcholine receptor ligand.
摘要翻译：本发明涉及吡啶基烟碱乙酰胆碱受体配体，包含有效量的吡啶基烟碱乙酰胆碱受体配体的组合物以及治疗或预防诸如抑郁症和尼古丁依赖之类的病症的方法，包括向有需要的动物施用有效量的吡啶基烟碱乙酰胆碱受体配体。

8. 发明申请

US20120276007A1 IMAGING AGENTS AND METHODS OF IMAGING NAALADASE OR PSMA 审中-公开
标题翻译：成像剂及其形成方法NAALADASE或PSMA
公开(公告)号：US20120276007A1
公开(公告)日：2012-11-01
申请号：US13537789
申请日：2012-06-29
申请人： Martin Gilbert Pomper , Jiazhong Zhang , John L. Musachio , Alan P. Kozikowski
发明人： Martin Gilbert Pomper , Jiazhong Zhang , John L. Musachio , Alan P. Kozikowski
IPC分类号： A61K51/04 , C07C69/78 , C07C323/57
CPC分类号： A61K51/0402 , A61B6/508 , A61K49/0032 , A61K49/0052 , C07B2200/05 , C07C275/24 , C07C323/59 , C07F11/005 , C12Q1/37 , G01N33/5005 , G01N33/60 , G01N33/62 , G01N33/689 , G01N2333/705
摘要： The present invention relates to compounds particularly asymmetric urea compounds which are labeled with one or more radioisotopes and which are suitable for imaging or therapeutic treatment of tissues, organs, or tumors which express NAALADase and/or PSMA. In another embodiment, the invention relates to methods of imaging tissues, organs, or tumors using radiolabeled compounds of the invention, particularly tissues, organs, or tumors which express NAALADase and/or PSMA to which the compounds of the invention have an affinity.
摘要翻译：本发明涉及用一种或多种放射性同位素标记并且适用于表达NAALADase和/或PSMA的组织，器官或肿瘤的成像或治疗性治疗的化合物，特别是不对称的脲化合物。在另一个实施方案中，本发明涉及使用本发明的放射性标记的化合物，特别是表达本发明的化合物具有亲和力的NAALADase和/或PSMA的组织，器官或肿瘤来成像组织，器官或肿瘤的方法。

9. 发明授权

US08067600B2 Histone deacetylase inhibitors and methods of use thereof 有权
标题翻译：组蛋白脱乙酰酶抑制剂及其使用方法
公开(公告)号：US08067600B2
公开(公告)日：2011-11-29
申请号：US12339492
申请日：2008-12-19
申请人： Alan P. Kozikowski , Bin Chen
发明人： Alan P. Kozikowski , Bin Chen
IPC分类号： C07D217/12 , C07D215/14 , A61K31/47
CPC分类号： C07C271/02 , A61K31/19 , C07C259/06 , C07C275/24 , C07C275/26 , C07C275/40 , C07C323/44 , C07C323/60 , C07C2603/74 , C07D215/48 , C07D215/54
摘要： One aspect of the invention relates to HDAC inhibitors. Methods of sensitizing a cancer cell to the cytotoxic effects of radiotherapy are also provided. The invention also provides methods for treating cancer and methods for treating neurological diseases. Additionally, the invention further provides pharmaceutical compositions comprising an HDAC inhibitor of the invention, and kits comprising a container containing an HDAC inhibitor of the invention.
摘要翻译：本发明的一个方面涉及HDAC抑制剂。还提供了使癌细胞对放射治疗的细胞毒性作用敏感的方法。本发明还提供了治疗癌症的方法和治疗神经疾病的方法。另外，本发明还提供了包含本发明的HDAC抑制剂的药物组合物和包含含有本发明的HDAC抑制剂的容器的试剂盒。

10. 发明授权

US08030300B2 Ligands for nicotinic acetylcholine receptors, and methods of making and using them 有权
标题翻译：烟碱乙酰胆碱受体的配体，以及制造和使用它们的方法
公开(公告)号：US08030300B2
公开(公告)日：2011-10-04
申请号：US10558607
申请日：2004-06-09
申请人： Alan P. Kozikowski , John L. Musachio , Kenneth J. Kellar , Yingxian Xiao , Zhi-Liang Wei , Hong Fan
发明人： Alan P. Kozikowski , John L. Musachio , Kenneth J. Kellar , Yingxian Xiao , Zhi-Liang Wei , Hong Fan
IPC分类号： A61K31/4427 , C07D401/12
CPC分类号： C07D471/18 , C07D487/08
摘要： One aspect of the present invention relates to heterocyclic compounds that are ligands for nicotinic acetylcholine receptors. A second aspect of the invention relates to the use of a compound of the invention for modulation of a mammalian nicotinic acetylcholine receptor. The present invention also relates to the use of a compound of the invention for treating a mammal suffering from Alzheimer's disease, Parkinson's disease, dyskinesias, Tourette's syndrome, schizophrenia, attention deficit disorder, anxiety, pain, depression, obsessive compulsive disorder, chemical substance abuse, alcoholism, memory deficit, pseudodementia, Ganser's syndrome, migraine pain, bulimia, obesity, premenstrual syndrome or late luteal phase syndrome, tobacco abuse, post-traumatic syndrome, social phobia, chronic fatigue syndrome, premature ejaculation, erectile difficulty, anorexia nervosa, disorders of sleep, autism, mutism or trichtillomania.
摘要翻译：本发明的一个方面涉及作为烟碱乙酰胆碱受体配体的杂环化合物。本发明的第二方面涉及本发明化合物用于调节哺乳动物烟碱乙酰胆碱受体的用途。本发明还涉及本发明化合物用于治疗患有阿尔茨海默病，帕金森病，运动障碍，图雷特综合征，精神分裂症，注意力缺陷障碍，焦虑，疼痛，抑郁，强迫症，化学物质滥用的哺乳动物的用途酒精中毒，记忆缺陷，假性痴呆，甘ser综合征，偏头痛，贪食症，肥胖症，经前期综合征或晚期黄体期综合征，烟草滥用，创伤后综合征，社交恐惧症，慢性疲劳综合征，早泄，勃起障碍，神经性厌食症，睡眠障碍，自闭症，多发性或三叉神经痛。

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