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1. 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。

2. 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。

3. 发明申请

WO2005007091A3 HISTONE DEACETYLASE INHIBITORS AND METHODS OF USE THEREOF 审中-公开
标题翻译： HISTONE DEACETYLASE抑制剂及其使用方法
公开(公告)号：WO2005007091A3
公开(公告)日：2005-04-28
申请号：PCT/US2004021663
申请日：2004-07-07
申请人： UNIV GEORGETOWN , KOZIKOWSKI ALAN P , DRITSCHILO ANATOLY , JUNG MIRA , PETUKHOV PAVEL , CHEN BIN
发明人： KOZIKOWSKI ALAN P , DRITSCHILO ANATOLY , JUNG MIRA , PETUKHOV PAVEL , CHEN BIN
IPC分类号： A01N37/10 , A01N43/40 , A01N43/42 , A61K20060101 , C07C259/04 , C07C271/02 , C07C275/24 , C07C275/26 , C07C275/40 , C07C323/44 , C07C323/60 , C07D215/48 , C07D215/54
CPC分类号： C07D215/54 , C07C271/02 , C07C275/24 , C07C275/26 , C07C275/40 , C07C323/44 , C07C323/60 , C07C2603/74 , C07D215/48
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和治疗神经疾病的方法。此外，本发明进一步提供了包含本发明的HDAC抑制剂的药物组合物，以及包含含有本发明的HDAC抑制剂的容器的试剂盒。

4. 发明申请

WO2004024939A3 LIGANDS FOR THE PEROXISOME PROLIFERATOR-ACTIVATED RECEPTOR, AND METHODS OF USE THEREOF 审中-公开
标题翻译：过氧化物酶促增殖因子受体的配体及其使用方法
公开(公告)号：WO2004024939A3
公开(公告)日：2004-10-14
申请号：PCT/US0328931
申请日：2003-09-12
申请人： UNIV GEORGETOWN , KOZIKOWSKI ALAN P , GLAZER ROBERT I , PETUKHOV PAVEL , WEI ZHI-LIANG
发明人： KOZIKOWSKI ALAN P , GLAZER ROBERT I , PETUKHOV PAVEL , WEI ZHI-LIANG
IPC分类号： A61K31/381 , A61K31/4015 , A61K31/423 , A61K31/428 , A61K31/44 , A61K31/45 , C07D207/456 , C07D213/62 , C07D261/08 , C07D333/30 , C07D413/06 , C07D413/12 , C07D471/04 , C07D498/02 , C12Q20060101
CPC分类号： C07D471/04 , C07D261/08 , C07D413/06 , C07D413/12
摘要： One aspect of the present invention relates to compounds that are active at a peroxisome proliferator-activated receptor (PPAR). In certain embodiments, the compound has a isoxazole or indole core. Another aspect of the present invention relates to a method of treating a mammal afflicted with cancer or non-insulin-dependent (type II) diabetes by administering a therapeutic amount of the compounds of the invention. In certain embodiments, the invention relates to a method of treating prostrate, stomach, or breast cancer. Another aspect of the invention relates to a method of identifying ligands active at a PPAR subtype using X-ray structural information. In certain embodiments, the method of identifying the ligand comprises using molecular modeling approaches including: in silico screening of chemical databases, de novo/rational drug design in which the ligand will be created computationally, and/or in silico screening of virtual combinatorial libraries.
摘要翻译：本发明的一个方面涉及在过氧化物酶体增殖物激活受体（PPAR）上有活性的化合物。在某些实施方案中，化合物具有异恶唑或吲哚核。本发明的另一方面涉及通过施用治疗量的本发明化合物治疗患有癌症或非胰岛素依赖型（II型）糖尿病的哺乳动物的方法。在某些实施方案中，本发明涉及治疗前列腺癌，胃癌或乳腺癌的方法。本发明的另一方面涉及使用X射线结构信息鉴定在PPAR亚型上活性的配体的方法。在某些实施方案中，鉴定配体的方法包括使用分子模拟方法，包括：化学数据库的计算机筛选，计算地创建配体的重新/合理的药物设计，和/或虚拟组合文库的计算机筛选。

5. 发明申请

WO2004041211A3 INHIBITORS OF beta-SECRETASE, AND THEIR USE FOR THE PREVENTION OR TREATMENT OF ALZHEIMER'S DISEASE OR MILD COGNITIVE IMPAIRMENT 审中-公开
标题翻译： β-分泌酶抑制剂及其用于预防或治疗阿尔茨海默病或轻度认知障碍的用途
公开(公告)号：WO2004041211A3
公开(公告)日：2004-09-10
申请号：PCT/US0335219
申请日：2003-11-03
申请人： UNIV GEORGETOWN , KOZIKOWSKI ALAN P , AISEN PAUL S , PETUKHOV PAVEL
发明人： KOZIKOWSKI ALAN P , AISEN PAUL S , PETUKHOV PAVEL
IPC分类号： A61K20060101 , A61K31/34 , A61K31/38 , A61K31/40 , C07C233/00 , C07C275/14 , C07C275/16 , C07C275/20 , C07C275/24 , C07D207/10 , C07D307/02 , C07D307/66 , C07D333/36 , C07D405/00
CPC分类号： C40B40/04 , C07C275/14 , C07C275/16 , C07C275/20 , C07C275/24 , C07D307/66 , C07D333/36
摘要： One aspect of the present invention relates to urea-containing compounds. In certain embodiments, the urea-containing compounds of the present invention comprise a heteroaromatic moiety. Another aspect of the present invention relates to a method of inhibiting a beta-secretase using a urea-containing compound of the present invention. A third aspect of the present invention relates to a method of treating Alzheimer's Disease or mild cognitive impairment using a urea-containing compound of the present invention.
摘要翻译：本发明的一个方面涉及含脲化合物。在某些实施方案中，本发明的含脲化合物包含杂芳族部分。本发明的另一方面涉及使用本发明的含脲化合物来抑制β-分泌酶的方法。本发明的第三方面涉及使用本发明的含尿素化合物治疗阿尔茨海默氏病或轻度认知障碍的方法。

6. 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。

7. 发明公开

EP0944626A4 TROPANE DERIVATIVES AND METHOD FOR THEIR SYNTHESIS 失效
标题翻译：托烷衍生物的合成及方法
公开(公告)号：EP0944626A4
公开(公告)日：2002-09-04
申请号：EP97954023
申请日：1997-12-02
申请人： UNIV GEORGETOWN , KOZIKOWSKI ALAN P , ARALDI GIAN LUCA
发明人： KOZIKOWSKI ALAN P , ARALDI GIAN LUCA
IPC分类号： A61K31/46 , A61K51/00 , A61P3/04 , A61P25/00 , A61P25/16 , A61P25/24 , A61P43/00 , C07D451/02
CPC分类号： C07D451/02

8. 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。

9. 发明申请

WO2005041875A3 DOPAMINE-, NOREPINEPHRINE- AND SEROTONIN- TRANSPORTER- SELECTIVE HETEROCYCLIC COMPOUNDS AND THEIR THERAPEUTIC APPLICATIONS 审中-公开
标题翻译：多巴胺，肾上腺素和丝氨酸 - 转运体 - 选择性杂环化合物及其治疗应用
公开(公告)号：WO2005041875A3
公开(公告)日：2005-11-24
申请号：PCT/US2004035162
申请日：2004-10-22
申请人： UNIV GEORGETOWN , KOZIKOWSKI ALAN P , ZHOU JIA
发明人： KOZIKOWSKI ALAN P , ZHOU JIA
IPC分类号： A61K20060101 , A61K31/445 , C07D211/68 , C07D401/00
CPC分类号： C07D211/20 , C07D211/22 , C07D211/24 , C07D405/12 , C07D413/12
摘要： One aspect of the invention relates to piperidine compounds that are useful as inhibitors of monoamine transporters. The invention also relates to pharmaceutical compositions, comprising a piperidine compound of the invention. Another aspect of the present invention relates to the use of the aformentioned compounds in a method of treating a disorder of the central nervous system in a mammal.
摘要翻译：本发明的一个方面涉及可用作单胺转运蛋白抑制剂的哌啶化合物。本发明还涉及包含本发明的哌啶化合物的药物组合物。本发明的另一方面涉及上述化合物在治疗哺乳动物中的中枢神经系统疾病的方法中的用途。

10. 发明申请

WO2005000806A2 LIGANDS FOR NICOTINIC ACETYLCHOLINE RECEPTORS, AND METHODS OF MAKING AND USING THEM 审中-公开
标题翻译：尼古丁乙酰胆碱受体配体及其制备和使用方法
公开(公告)号：WO2005000806A2
公开(公告)日：2005-01-06
申请号：PCT/US2004018340
申请日：2004-06-09
申请人： UNIV GEORGETOWN , KOZIKOWSKI ALAN P , MUSACHIO JOHN L , KELLAR KENNETH J , XIAO YINGXIAN , WEI ZHI-LIANG
发明人： KOZIKOWSKI ALAN P , MUSACHIO JOHN L , KELLAR KENNETH J , XIAO YINGXIAN , WEI ZHI-LIANG
IPC分类号： A61K31/4375 , A61K31/439 , A61P25/00 , C07D20060101 , C07D471/18 , C07D487/08 , C07D
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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