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1. 发明申请

WO2010059142A1 ANTHRAQUINONE DIOXIMES AND USES THEREOF 审中-公开
标题翻译：蒽醌二氧化物及其用途
公开(公告)号：WO2010059142A1
公开(公告)日：2010-05-27
申请号：PCT/US2008/012995
申请日：2008-11-21
申请人： AVALON PHARMACEUTICALS , CHOLODY, Wieslaw, M. , ZANG, Yi , ZUCK, Karina , WATTHEY, Jeffrey, W.H. , OHLER, Zoe , STROVEL, Jeffrey , OHLER, Norman, E. , CHELLAPPAN, Sheela , PADIA, Janak
发明人： CHOLODY, Wieslaw, M. , ZANG, Yi , ZUCK, Karina , WATTHEY, Jeffrey, W.H. , OHLER, Zoe , STROVEL, Jeffrey , OHLER, Norman, E. , CHELLAPPAN, Sheela , PADIA, Janak
IPC分类号： A61K31/54
CPC分类号： C07D295/26 , C07D211/96 , C07D215/58 , C07D221/20 , C07D225/04
摘要： Anthraquinone dioximes and their derivatives are disclosed for use in treatment of diseases, especially cancer, such as colon and colorectal cancer. Methods of preparing such derivatives are also presented. Compositions of these compounds, as well as metabolites of said compounds and their use in gene modulation are also described.
摘要翻译：公开了蒽醌二肟及其衍生物用于治疗疾病，特别是癌症，例如结肠和结肠直肠癌。还提出了制备此类衍生物的方法。还描述了这些化合物的组合物，以及所述化合物的代谢物及其在基因调节中的用途。

2. 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。

3. 发明申请

WO2010082912A1 DERIVATIVES OF MULTI-RING AROMATIC COMPOUNDS AND USES AS ANTI-TUMOR AGENTS 审中-公开
标题翻译：多环芳烃化合物的衍生物和作为抗肿瘤剂的用途
公开(公告)号：WO2010082912A1
公开(公告)日：2010-07-22
申请号：PCT/US2009/000257
申请日：2009-01-15
申请人： AVALON PHARMACEUTICALS , CHOLODY, Wieslaw, M. , ZANG, Yi , ZUCK, Karina , WATTHEY, Jeffrey, W. H. , OHLER, Zoe , STROVEL, Jeffrey , OHLER, Norman, E. , CHELLAPPAN, Sheela , PADIA, Janak
发明人： CHOLODY, Wieslaw, M. , ZANG, Yi , ZUCK, Karina , WATTHEY, Jeffrey, W. H. , OHLER, Zoe , STROVEL, Jeffrey , OHLER, Norman, E. , CHELLAPPAN, Sheela , PADIA, Janak
IPC分类号： A01N35/00 , A01N41/06 , A61K31/18
CPC分类号： C07D219/08
摘要： Chemical agents, such as disulfonamide derivatives of fluorene, anthracene, xanthene, dibenzosuberone and acridine, and similar heterocyclic ring structures, including salts thereof, that act as anti-cancer and anti-tumor agents, are disclosed, along with methods for preparing such agents, as well as pharmaceutical compositions containing such agents as active ingredients and methods of using these as therapeutic agents.
摘要翻译：公开了作为抗癌剂和抗肿瘤剂的化学试剂，例如芴，蒽，呫吨，二苯并西泮和吖啶的二磺酰胺衍生物，以及类似的杂环结构，包括其盐，以及制备这些试剂的方法，以及含有活性成分的药剂和使用它们作为治疗剂的方法的药物组合物。

4. 发明申请

WO2008140792A1 DERIVATIVES OF FLUORENE, ANTHRACENE, XANTHENE, DIBENZOSUBERONE AND ACRIDINE AND USES THEREOF 审中-公开
标题翻译：荧光素，蒽醌，呫吨酮，二苯唑酮和吖啶的衍生物及其用途
公开(公告)号：WO2008140792A1
公开(公告)日：2008-11-20
申请号：PCT/US2008/006015
申请日：2008-05-09
申请人： AVALON PHARMACEUTICALS , CHOLODY, Wieslaw, M. , ZANG, Yi , ZUCK, Karina , WATTHEY, Jeffrey, W.H. , OHLER, Zoe , STROVEL, Jeffrey , OHLER, Gene , CHELLAPPAN, Sheela , PADIA, Janak
发明人： CHOLODY, Wieslaw, M. , ZANG, Yi , ZUCK, Karina , WATTHEY, Jeffrey, W.H. , OHLER, Zoe , STROVEL, Jeffrey , OHLER, Gene , CHELLAPPAN, Sheela , PADIA, Janak
IPC分类号： A61K31/185 , A61K31/135
CPC分类号： A61K31/395 , A61K31/18 , A61K31/409 , A61K31/435 , A61K31/4545 , A61K31/4709 , A61K31/4725 , A61K31/496 , A61K31/5377 , A61K31/55 , A61K31/551 , A61K31/553 , C07C311/20 , C07C2601/14 , C07D211/96 , C07D295/26
摘要： Chemical agents, such as disulfonamide derivatives of fluorene, anthracene, xanthene, dibenzosuberone and acridine, and similar heterocyclic ring structures, including salts thereof, that act as anti-cancer and anti-tumor agents, especially where such agents modulate the activity of the Wnt/β-catenin signaling pathway, and serve to reduce β-catenin levels present in cells, such as cancer cells, or where the agents modulate levels of gene expression in cellular systems, including cancer cells, are disclosed, along with methods for preparing such agents, as well as pharmaceutical compositions containing such agents as active ingredients and methods of using these as therapeutic agents.
摘要翻译：化学试剂，如芴，蒽，呫吨，二苯并uber酮和吖啶的二磺酰胺衍生物，以及类似的杂环结构（包括其盐），其作为抗癌剂和抗肿瘤剂，特别是当这些试剂调节Wnt的活性时并且用于降低存在于细胞中的β-连环蛋白水平，例如癌细胞，或其中调节细胞系统（包括癌细胞）中基因表达水平的那些，以及其制备方法试剂，以及含有这些试剂的活性成分的药物组合物和使用它们作为治疗剂的方法。

5. 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。

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