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1. 发明申请

WO2010045212A2 NICOTINIC ACETYLCHOLINE RECEPTOR LIGANDS AND THE USES THEREOF 审中-公开
标题翻译： NICOTINIC乙酰胆碱受体配体及其用途
公开(公告)号：WO2010045212A2
公开(公告)日：2010-04-22
申请号：PCT/US2009/060473
申请日：2009-10-13
申请人： PSYCHOGENICS, INCstatuts , CHANDRASEKHAR, Jayaraman , KOZIKOWSKI, Alan, P. , LIU, Jianhua , TUECKMANTEL, Werner , WALKER, Joel, R. , YUEN, Po-wai , THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOIS
发明人： CHANDRASEKHAR, Jayaraman , KOZIKOWSKI, Alan, P. , LIU, Jianhua , TUECKMANTEL, Werner , WALKER, Joel, R. , YUEN, Po-wai
IPC分类号： C07D401/12 , C07D401/04 , C07D401/02 , A61K31/44 , A61K31/4427 , A61P25/18 , A61P25/26
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和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。

2. 发明申请

WO2008019025A3 ISOFORM-SELECTIVE HDAC INHIBITORS 审中-公开
标题翻译： ISOFORM-SELECTIVE HDAC抑制剂
公开(公告)号：WO2008019025A3
公开(公告)日：2008-09-12
申请号：PCT/US2007017205
申请日：2007-08-02
申请人： UNIV GEORGETOWN , KOZIKOWSKI ALAN P , JUNG MIRA , DRITSCHILO ANTATOLY , GAYSIN ARSEN , PETUKHOV PAVEL , TUECKMANTEL WERNER , YUAN HONGBIN
发明人： KOZIKOWSKI ALAN P , JUNG MIRA , DRITSCHILO ANTATOLY , GAYSIN ARSEN , PETUKHOV PAVEL , TUECKMANTEL WERNER , YUAN HONGBIN
IPC分类号： C07D277/04 , A61K31/44 , C07D277/08
CPC分类号： C07D277/46 , C07C259/06 , C07C323/60
摘要： One aspect of the invention relates to isoform-selective HDAC inhibitors. Also provided are methods of sensitizing a cancer cell to the cytotoxic effects of radiotherapy. The invention also provides methods for treating cancer, methods for treating neurological diseases and methods for treating malaria. Additionally, the invention provides pharmaceutical compositions comprising an HDAC inhibitor of the invention; and kits comprising a an HDAC inhibitor of the invention.
摘要翻译：本发明的一个方面涉及同种型选择性HDAC抑制剂。还提供了使癌细胞对放射疗法的细胞毒性作用敏感的方法。本发明还提供治疗癌症的方法，治疗神经疾病的方法和治疗疟疾的方法。此外，本发明提供了包含本发明的HDAC抑制剂的药物组合物; 和包含本发明的HDAC抑制剂的试剂盒。

3. 发明申请

WO2007115092A3 10-SUBSTITUTED CYTISINE DERIVATIVES AND METHODS OF USE THEREOF 审中-公开
标题翻译： 10替代的CYTISINE衍生物及其使用方法
公开(公告)号：WO2007115092A3
公开(公告)日：2008-07-31
申请号：PCT/US2007065498
申请日：2007-03-29
申请人： UNIV GEORGETOWN , KOZIKOWSKI ALAN P , TUECKMANTEL WERNER , CHELLAPPAN SHEELA , KELLAR KENNETH J , XIAO YINGXIAN
发明人： KOZIKOWSKI ALAN P , TUECKMANTEL WERNER , CHELLAPPAN SHEELA , KELLAR KENNETH J , XIAO YINGXIAN
IPC分类号： A61K31/4375 , A61K31/439
CPC分类号： C07D471/18
摘要： The present invention relates to substituted cytisine compounds that are useful in treating diseases impacted by a nicotinic ACh receptor. One aspect of the invention relates to 10-substituted cytisine compounds. In certain instances, the cytisine is substituted in the 10-position by an alkyl, aryl or aralkyl group. The present invention also relates to a pharmaceutical composition comprises the substituted cytisine compound or the 10- substituted cytisine compound. The invention also relates to a method of modulation a nicotinic ACh receptor in a mammal, comprising the step of administering to a mammal in need thereof a therapeutically effective amount of a substituted cytisine. In certain instances, the substituted cytisine is a 10-substituted cytisine. Another aspect of the present invention relates a method of treating a disease impacted by a nicotinic ACh receptor, comprising the step of administering to a mammal in need thereof a therapeutically effective amount of a substituted cytisine. In certain instances, the substituted cytisine is a 10-substituted cytisine.
摘要翻译：本发明涉及可用于治疗受烟碱性ACh受体影响的疾病的取代的仙培酮化合物。本发明的一个方面涉及10-取代的仙客来化合物。在某些情况下，通过烷基，芳基或芳烷基在十位置替代赤藓酸。本发明还涉及一种药物组合物，其包含取代的赤藓苷化合物或10-取代的仙茅素化合物。本发明还涉及一种调节哺乳动物中烟碱性ACh受体的方法，其包括向有需要的哺乳动物施用治疗有效量的取代的氰尿酸的步骤。在某些情况下，取代的洋甘菊是一种10-取代的胞苷。本发明的另一方面涉及一种治疗由烟碱性ACh受体影响的疾病的方法，其包括向有需要的哺乳动物施用治疗有效量的取代的氰尿酸的步骤。在某些情况下，取代的洋甘菊是一种10-取代的胞苷。

4. 发明申请

WO2007008514A2 INHIBITORS OF GLYCOGEN SYNTHASE KINASE 3 审中-公开
标题翻译： GLYCOGEN SYNTHASE KINASE的抑制剂3
公开(公告)号：WO2007008514A2
公开(公告)日：2007-01-18
申请号：PCT/US2006/026137
申请日：2006-07-06
申请人： GEORGETOWN UNIVERSITY , KOZIKOWSKI, Alan, P. , GAYSINA, Irina , PETUKHOV, Pavel , SRIDHAR, Jayalakshmi , TUECKMANTEL, Werner
发明人： KOZIKOWSKI, Alan, P. , GAYSINA, Irina , PETUKHOV, Pavel , SRIDHAR, Jayalakshmi , TUECKMANTEL, Werner
IPC分类号： A61K31/426
CPC分类号： C07D403/14 , C07D403/04
摘要： One aspect of the present invention relates to heterocyclic compounds that inhibit mammalian or human glycogen synthase kinase 3. Another aspect of the invention relates to pharmaceutical compositions comprising such a heterocyclic compound. The present invention also relates to methods of treating a mammal or human suffering from a malady that is based at least in part on abnormal activity of glycogen synthase kinase 3. The present invention also relates to methods of treating a mammal or human suffering from diabetes, Alzheimer's disease, Huntington's disease, Parkinson's disease, AIDS-associated dementia, ALS, MS, or schizophrenia.
摘要翻译：本发明的一个方面涉及抑制哺乳动物或人糖原合成酶激酶3的杂环化合物。本发明的另一方面涉及包含这种杂环化合物的药物组合物。本发明还涉及治疗至少部分基于糖原合成酶激酶3的异常活性的患有疾病的哺乳动物或人的方法。本发明还涉及治疗患有糖尿病的哺乳动物或人的方法，阿尔茨海默病，亨廷顿氏病，帕金森病，AIDS相关性痴呆，ALS，MS或精神分裂症。

5. 发明申请

WO2010045212A3 NICOTINIC ACETYLCHOLINE RECEPTOR LIGANDS AND THE USES THEREOF 审中-公开
标题翻译：烟碱乙酰胆碱受体配体及其用途
公开(公告)号：WO2010045212A3
公开(公告)日：2010-07-29
申请号：PCT/US2009060473
申请日：2009-10-13
申请人： PSYCHOGENICS INC , CHANDRASEKHAR JAYARAMAN , KOZIKOWSKI ALAN P , LIU JIANHUA , TUECKMANTEL WERNER , WALKER JOEL R , YUEN PO-WAI , UNIV ILLINOIS
发明人： CHANDRASEKHAR JAYARAMAN , KOZIKOWSKI ALAN P , LIU JIANHUA , TUECKMANTEL WERNER , WALKER JOEL R , YUEN PO-WAI
IPC分类号： C07D401/12 , A61K31/44 , A61K31/4427 , A61P25/18 , A61P25/26 , C07D401/02 , C07D401/04
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：吡啶基烟碱乙酰胆碱受体配体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和治疗或预防例如抑郁症和尼古丁依赖性病症的方法，所述方法包括给予有需要的动物有效量的吡啶基烟碱乙酰胆碱受体配体。

6. 发明申请

WO2007115092A2 10-SUBSTITUTED CYTISINE DERIVATIVES AND METHODS OF USE THEREOF 审中-公开
标题翻译： 10替代的CYTISINE衍生物及其使用方法
公开(公告)号：WO2007115092A2
公开(公告)日：2007-10-11
申请号：PCT/US2007/065498
申请日：2007-03-29
申请人： GEORGETOWN UNIVERSITY , KOZIKOWSKI, Alan, P. , TUECKMANTEL, Werner , CHELLAPPAN, Sheela , KELLAR, Kenneth, J. , XIAO, Yingxian
发明人： KOZIKOWSKI, Alan, P. , TUECKMANTEL, Werner , CHELLAPPAN, Sheela , KELLAR, Kenneth, J. , XIAO, Yingxian
IPC分类号： H05B6/10
CPC分类号： C07D471/18
摘要： The present invention relates to substituted cytisine compounds that are useful in treating diseases impacted by a nicotinic ACh receptor. One aspect of the invention relates to 10-substituted cytisine compounds. In certain instances, the cytisine is substituted in the 10-position by an alkyl, aryl or aralkyl group. The present invention also relates to a pharmaceutical composition comprises the substituted cytisine compound or the 10- substituted cytisine compound. The invention also relates to a method of modulation a nicotinic ACh receptor in a mammal, comprising the step of administering to a mammal in need thereof a therapeutically effective amount of a substituted cytisine. In certain instances, the substituted cytisine is a 10-substituted cytisine. Another aspect of the present invention relates a method of treating a disease impacted by a nicotinic ACh receptor, comprising the step of administering to a mammal in need thereof a therapeutically effective amount of a substituted cytisine. In certain instances, the substituted cytisine is a 10-substituted cytisine.
摘要翻译：本发明涉及可用于治疗受烟碱性ACh受体影响的疾病的取代的仙培酮化合物。本发明的一个方面涉及10-取代的仙客来化合物。在某些情况下，通过烷基，芳基或芳烷基在十位置替代赤藓酸。本发明还涉及一种药物组合物，其包含取代的赤藓苷化合物或10-取代的仙茅素化合物。本发明还涉及一种调节哺乳动物中烟碱性ACh受体的方法，其包括向有需要的哺乳动物施用治疗有效量的取代的胞苷酸的步骤。在某些情况下，取代的洋甘菊是一种10-取代的胞苷。本发明的另一方面涉及治疗由烟碱性ACh受体影响的疾病的方法，其包括向有需要的哺乳动物施用治疗有效量的取代的洋甘菊的步骤。在某些情况下，取代的洋甘菊是一种10-取代的胞苷。

7. 发明申请

WO2007008514A3 INHIBITORS OF GLYCOGEN SYNTHASE KINASE 3 审中-公开
标题翻译：糖原合成酶激酶抑制剂3
公开(公告)号：WO2007008514A3
公开(公告)日：2007-10-04
申请号：PCT/US2006026137
申请日：2006-07-06
申请人： UNIV GEORGETOWN , KOZIKOWSKI ALAN P , GAYSINA IRINA , PETUKHOV PAVEL , SRIDHAR JAYALAKSHMI , TUECKMANTEL WERNER
发明人： KOZIKOWSKI ALAN P , GAYSINA IRINA , PETUKHOV PAVEL , SRIDHAR JAYALAKSHMI , TUECKMANTEL WERNER
IPC分类号： A01N43/56
CPC分类号： C07D403/14 , C07D403/04
摘要： One aspect of the present invention relates to heterocyclic compounds that inhibit mammalian or human glycogen synthase kinase 3. Another aspect of the invention relates to pharmaceutical compositions comprising such a heterocyclic compound. The present invention also relates to methods of treating a mammal or human suffering from a malady that is based at least in part on abnormal activity of glycogen synthase kinase 3. The present invention also relates to methods of treating a mammal or human suffering from diabetes, Alzheimer's disease, Huntington's disease, Parkinson's disease, AIDS-associated dementia, ALS, MS, or schizophrenia.
摘要翻译：本发明的一个方面涉及抑制哺乳动物或人糖原合酶激酶3的杂环化合物。本发明的另一方面涉及包含这种杂环化合物的药物组合物。本发明还涉及治疗患有至少部分基于糖原合酶激酶3的异常活性的疾病的哺乳动物或人的方法。本发明还涉及治疗患有糖尿病的哺乳动物或人的方法，阿尔茨海默氏病，亨廷顿舞蹈病，帕金森病，艾滋病相关性痴呆，ALS，MS或精神分裂症。

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