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1. 发明申请

WO0140188A8 CURCUMIN ANALOGUES FOR TREATING CANCER 审中-公开
标题翻译：用于治疗癌症的CURCUMIN ANALOGUES
公开(公告)号：WO0140188A8
公开(公告)日：2003-11-13
申请号：PCT/US0032870
申请日：2000-12-04
申请人： UNIV EMORY , SNYDER JAMES P , DAVIS MATTHEW C , ADAMS BRIAN , SHOJI MAMORU , LIOTTA DENNIS C , FERSTL EVA M , SUNAY USTUN B
发明人： SNYDER JAMES P , DAVIS MATTHEW C , ADAMS BRIAN , SHOJI MAMORU , LIOTTA DENNIS C , FERSTL EVA M , SUNAY USTUN B
IPC分类号： C07D317/54 , A61K31/065 , A61K31/10 , A61K31/121 , A61K31/122 , A61K31/15 , A61K31/351 , A61K31/352 , A61K31/36 , A61K31/404 , A61K31/4439 , A61K31/45 , A61K31/4545 , A61K31/46 , A61P35/00 , A61P43/00 , C07C33/28 , C07C33/48 , C07C43/23 , C07C45/29 , C07C45/62 , C07C45/74 , C07C49/233 , C07C49/235 , C07C49/248 , C07C49/255 , C07C49/697 , C07C49/747 , C07C49/753 , C07C225/22 , C07C235/34 , C07C251/40 , C07C275/24 , C07C317/10 , C07C317/18 , C07C321/20 , C07D209/34 , C07D213/63 , C07D213/68 , C07D295/205 , C07D309/20 , C07D309/22 , C07D309/38 , C07D311/58 , C07D317/50 , C07D401/06 , C07D401/14 , C07D451/02 , C07D451/06
CPC分类号： C07D295/205 , C07C45/292 , C07C45/62 , C07C45/74 , C07C49/233 , C07C49/235 , C07C49/248 , C07C49/255 , C07C49/697 , C07C49/747 , C07C49/753 , C07C225/22 , C07C235/34 , C07C251/40 , C07C275/24 , C07C317/10 , C07C321/20 , C07D209/34 , C07D213/63 , C07D317/50 , C07D451/02
摘要： The present invention is directed to curcumin analogs (I), wherein Y is OH, halogen, or CF3; Z is H, OH, OR1, halogen, or CF3; X1 and X2 are independently C or N; and A is as defined in the application; exhibiting anti-tumor and anti-angiogenic properties, pharmaceutical formulations including such compounds and methods of using such compounds.
摘要翻译：本发明涉及姜黄素类似物（I），其中Y是OH，卤素或CF 3; Z是H，OH，OR 1，卤素或CF 3; X1和X2独立地为C或N; 和A如申请中所定义; 显示抗肿瘤和抗血管生成性质，包括这些化合物的药物制剂和使用这些化合物的方法。

2. 发明申请

WO0140188A9 CURCUMIN ANALOGUES FOR TREATING CANCER 审中-公开
标题翻译：用于治疗癌症的CURCUMIN ANALOGUES
公开(公告)号：WO0140188A9
公开(公告)日：2002-07-25
申请号：PCT/US0032870
申请日：2000-12-04
申请人： UNIV EMORY , SNYDER JAMES P , DAVIS MATTHEW C , ADAMS BRIAN , SHOJI MAMORU , LIOTTA DENNIS C , FERSTL EVA M , SUNAY USTUN B
发明人： SNYDER JAMES P , DAVIS MATTHEW C , ADAMS BRIAN , SHOJI MAMORU , LIOTTA DENNIS C , FERSTL EVA M , SUNAY USTUN B
IPC分类号： C07D317/54 , A61K31/065 , A61K31/10 , A61K31/121 , A61K31/122 , A61K31/15 , A61K31/351 , A61K31/352 , A61K31/36 , A61K31/404 , A61K31/4439 , A61K31/45 , A61K31/4545 , A61K31/46 , A61P35/00 , A61P43/00 , C07C33/28 , C07C33/48 , C07C43/23 , C07C45/29 , C07C45/62 , C07C45/74 , C07C49/233 , C07C49/235 , C07C49/248 , C07C49/255 , C07C49/697 , C07C49/747 , C07C49/753 , C07C225/22 , C07C235/34 , C07C251/40 , C07C275/24 , C07C317/10 , C07C317/18 , C07C321/20 , C07D209/34 , C07D213/63 , C07D213/68 , C07D295/205 , C07D309/20 , C07D309/22 , C07D309/38 , C07D311/58 , C07D317/50 , C07D401/06 , C07D401/14 , C07D451/02 , C07D451/06
CPC分类号： C07D295/205 , C07C45/292 , C07C45/62 , C07C45/74 , C07C49/233 , C07C49/235 , C07C49/248 , C07C49/255 , C07C49/697 , C07C49/747 , C07C49/753 , C07C225/22 , C07C235/34 , C07C251/40 , C07C275/24 , C07C317/10 , C07C321/20 , C07D209/34 , C07D213/63 , C07D317/50 , C07D451/02
摘要： The present invention is directed to curcumin analogs (I), wherein Y is OH, halogen, or CF3; Z is H, OH, OR1, halogen, or CF3; X1 and X2 are independently C or N; and A is as defined in the application; exhibiting anti-tumor and anti-angiogenic properties, pharmaceutical formulations including such compounds and methods of using such compounds.
摘要翻译：本发明涉及姜黄素类似物（I），其中Y是OH，卤素或CF 3; Z是H，OH，OR 1，卤素或CF 3; X1和X2独立地为C或N; 和A如申请中所定义; 显示抗肿瘤和抗血管生成性质，包括这些化合物的药物制剂和使用这些化合物的方法。

3. 发明申请

WO2005025623A2 CYTOTOXIC COMPOUND-PROTEIN CONJUGATES AS SUPPRESSORS OF TUMOR GROWTH AND ANGIOGENESIS 审中-公开
标题翻译：作为肿瘤生长和血管生成抑制因子的细胞毒素化合物 - 蛋白质结合蛋白
公开(公告)号：WO2005025623A2
公开(公告)日：2005-03-24
申请号：PCT/US2004024490
申请日：2004-07-28
申请人： UNIV EMORY , SHOJI MAMORU , SNYDER JAMES P , LIOTTA DENNIS C , SUN AIMING
发明人： SHOJI MAMORU , SNYDER JAMES P , LIOTTA DENNIS C , SUN AIMING
IPC分类号： A61K47/48
CPC分类号： A61K47/6849 , A61K47/642
摘要： Compositions and methods are provided for delivering cytotoxic compounds, such as natural curcumoids and synthetic curcumin analogs, specifically to cancer cells and to blood vessels that nourish solid tumors. The compositions include a cytotoxic drug tethered to a protein, such as factor VIIa, which can bind with high affinity to a receptor, such as tissue factor, expressed on the surface of cancer cells and vascular endothelial cells within the tumor microenvironment. Upon binding, the drug-protein-receptor complex is endocytosed and the drug is subsequently liberated inside the target cell via proteolytic cleavage. The compositions and methods may increase the efficacy of the cytotoxic agets and decrease their side effects by delivering the agents to specific target cells, such as cancer cells, vascular endothelial cells in a tumor, and metastatic foci anywhere in the body, providing the target cells express surface bound tissue factor. Additionally, methods of synthesis of cytotoxic compound-protein conjugates are provided, for example, curcuminoid-tetherlinker-factor VIIa composition, as well as pharmaceutically acceptable compositions and methods for delivering a therapeutically-effective amount of a cytotoxic compound-protein conjugate together with one or more pharmaceutically acceptable carriers (additives) and/or diluents to an animal or human patient.
摘要翻译：提供组合物和方法用于递送细胞毒性化合物，例如天然的姜黄素和合成的姜黄素类似物，特别是癌细胞和滋养实体瘤的血管。组合物包括与诸如因子VIIa结合的蛋白质的细胞毒性药物，其可以高度亲和力结合到在肿瘤微环境中在癌细胞表面和血管内皮细胞表面上的受体，例如组织因子。结合后，药物 - 蛋白 - 受体复合物被内吞，并且药物随后通过蛋白水解切割在靶细胞内释放。组合物和方法可以通过将药物递送到特定靶细胞，例如肿瘤中的癌细胞，血管内皮细胞和体内任何地方的转移灶，来增加细胞毒性作用的功效并降低其副作用，提供靶细胞表达结合组织因子。此外，提供了合成细胞毒性化合物 - 蛋白质缀合物的方法，例如，姜黄素 - tetherlinker-factor VIIa组合物，以及用于将治疗有效量的细胞毒性化合物 - 蛋白质缀合物与一种或更多的药学上可接受的载体（添加剂）和/或稀释剂给动物或人类患者。

4. 发明申请

WO0247679A3 NONPEPTIDE AGONISTS AND ANTAGONISTS OF VASOPRESSIN RECEPTORS 审中-公开
标题翻译：血管收缩素的非肽类激动剂和拮抗剂
公开(公告)号：WO0247679A3
公开(公告)日：2003-06-12
申请号：PCT/US0149303
申请日：2001-12-17
申请人： UNIV EMORY , SNYDER JAMES P , LIOTTA DENNIS C , VENKATESAN HARIHARAN , WANG MINMIN , DAVIS MATTHEW C
发明人： SNYDER JAMES P , LIOTTA DENNIS C , VENKATESAN HARIHARAN , WANG MINMIN , DAVIS MATTHEW C
IPC分类号： A61P13/12 , C07C311/10 , C07D211/46 , C07D223/16 , C07D295/088 , C07D295/108 , C07D295/13 , C07D295/135 , C07D295/26 , C07D401/12 , C07D471/10 , C07D487/04 , A61K31/35 , A61K31/015 , A61K31/382 , A61K31/439 , A61K31/55 , C07C311/08 , C07C311/21 , C07C311/49 , C07D211/22 , C07D311/00 , C07D335/02
CPC分类号： C07D223/16 , C07C311/10 , C07C2602/42 , C07D211/46 , C07D295/088 , C07D295/108 , C07D295/13 , C07D295/135 , C07D295/26 , C07D401/12 , C07D471/10 , C07D487/04
摘要： The disclosed invention is a composition agonists and/or antagonists of V2, V1a or both receptors, in a host, including animals, and especially humans, using a small molecule or its pharmaceutically acceptable salt or prodrug.
摘要翻译：所公开的发明是使用小分子或其药学上可接受的盐或前药在宿主（包括动物，尤其是人）中的组合物激动剂和/或拮抗剂V2，V1a或两种受体。

5. 发明申请

WO0247679A8 NONPEPTIDE AGONISTS AND ANTAGONISTS OF VASOPRESSIN RECEPTORS 审中-公开
标题翻译：非吸收激素和血管紧张素受体拮抗剂
公开(公告)号：WO0247679A8
公开(公告)日：2003-01-30
申请号：PCT/US0149303
申请日：2001-12-17
申请人： UNIV EMORY , SNYDER JAMES P , LIOTTA DENNIS C , VENKATESAN HARIHARAN , WANG MINMIN , DAVIS MATTHEW C
发明人： SNYDER JAMES P , LIOTTA DENNIS C , VENKATESAN HARIHARAN , WANG MINMIN , DAVIS MATTHEW C
IPC分类号： A61P13/12 , C07C311/10 , C07D211/46 , C07D223/16 , C07D295/088 , C07D295/108 , C07D295/13 , C07D295/135 , C07D295/26 , C07D401/12 , C07D471/10 , C07D487/04 , A61K31/35 , A61K31/015 , A61K31/382 , A61K31/439 , A61K31/55 , C07D211/22 , C07D311/00 , C07D335/02
CPC分类号： C07D223/16 , C07C311/10 , C07C2602/42 , C07D211/46 , C07D295/088 , C07D295/108 , C07D295/13 , C07D295/135 , C07D295/26 , C07D401/12 , C07D471/10 , C07D487/04
摘要： The disclosed invention is a composition agonists and/or antagonists of V2, V1a or both receptors, in a host, including animals, and especially humans, using a small molecule or its pharmaceutically acceptable salt or prodrug.
摘要翻译：所公开的发明是使用小分子或其药学上可接受的盐或前药，在宿主中包括V2，V1a或两种受体的组合物激动剂和/或拮抗剂，包括动物，特别是人类。

6. 发明申请

WO2006074426A3 CXCR4 ANTAGONISTS FOR THE TREATMENT OF HIV INFECTION 审中-公开
标题翻译： CXCR4治疗艾滋病毒感染的拮抗剂
公开(公告)号：WO2006074426A3
公开(公告)日：2006-12-07
申请号：PCT/US2006000600
申请日：2006-01-09
申请人： UNIV EMORY , SHIM HYUNSUK , LIOTTA DENNIS C , SNYDER JAMES P , ZHAN WEIQIANG , LIANG ZHONGXING
发明人： SHIM HYUNSUK , LIOTTA DENNIS C , SNYDER JAMES P , ZHAN WEIQIANG , LIANG ZHONGXING
IPC分类号： A61K31/505 , A61K31/44
CPC分类号： C07D239/42 , A61K31/4402 , A61K31/444 , A61K31/505 , A61K31/506 , C07C51/412
摘要： The invention provides compounds, pharmaceutical compositions and methods of use of certain compounds that are antagonists of the chemokine CXCR4 receptor, and in particular to inhibit viral entry of certain viruses. Certain compounds in particular can reduce entry of immunodeficiency virus (HIV) into a cell while not reducing the capacity of stem cells to proliferate, and therefore can be useful for long term treatment regimes. The compounds are useful in particular in the treatment or prevention of HIV infections.
摘要翻译：本发明提供化合物，药物组合物和使用某些化合物作为趋化因子CXCR4受体的拮抗剂的方法，特别是抑制病毒进入某些病毒。某些化合物特别可以减少免疫缺陷病毒（HIV）进入细胞，而不会降低干细胞增殖的能力，因此可用于长期治疗方案。该化合物特别用于治疗或预防HIV感染。

7. 发明申请

WO2008008854A3 CXER4 ANTAGONISTS INCLUDING DIAZINE AND TRIAZINE STRUCTURES FOR THE TREATMENT OF MEDICAL DISORDERS 审中-公开
标题翻译： CXER4拮抗剂，包括用于治疗医疗失调的双嗪和三嗪结构
公开(公告)号：WO2008008854A3
公开(公告)日：2008-09-25
申请号：PCT/US2007073285
申请日：2007-07-11
申请人： UNIV EMORY , LIOTTA DENNIS C , SNYDER JAMES P , ZHAN WEIQIANG
发明人： LIOTTA DENNIS C , SNYDER JAMES P , ZHAN WEIQIANG
IPC分类号： C07C211/27 , A61K31/136 , A61K31/137 , A61K31/44 , A61K31/4965 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/53 , A61P31/18 , C07D401/06 , C07D403/06
CPC分类号： C07D239/42 , C07D239/47 , C07D239/52 , C07D401/12 , C07D403/06 , C07D403/12
摘要： The invention provides compounds, pharmaceutical compositions and methods of use of certain compounds that are antagonists of the chemokine CXCR4 receptor for the treatment of proliferative conditions mediated by CXCR4 receptors or for the treatment of viral infections. The compounds provided interfere with the binding of SDFl to the receptor. These compounds are particularly useful for treating or reducing the severity of hyperproliferative diseases by inhibiting metastasis, or for reducing entry of HIV in to a cell while not reducing the capacity of the stem cells to proliferate. The compounds may be useful for long term treatment regimes.
摘要翻译：本发明提供化合物，药物组合物和作为趋化因子CXCR4受体拮抗剂的某些化合物用于治疗由CXCR4受体介导的增殖性病症或用于治疗病毒感染的方法。提供的化合物干扰SDF1与受体的结合。这些化合物特别适用于通过抑制转移或减少HIV进入细胞而不降低干细胞增殖能力来治疗或减轻过度增殖性疾病的严重程度。该化合物可用于长期治疗方案。

8. 发明申请

WO0228862A2 TRIPTOLIDE ANALOGS FOR THE TREATMENT OF AUTOIMMUNE AND INFLAMMATORY DISORDERS 审中-公开
标题翻译：用于治疗自身免疫和炎症性疾病的三苯吡啶类似物
公开(公告)号：WO0228862A2
公开(公告)日：2002-04-11
申请号：PCT/US0130951
申请日：2001-10-02
申请人： UNIV EMORY , VENKATESAN HARIHARAN , SNYDER JAMES P , LIOTTA DENNIS C , WANG SUSHENG
发明人： VENKATESAN HARIHARAN , SNYDER JAMES P , LIOTTA DENNIS C , WANG SUSHENG
IPC分类号： A61K31/336 , A61K45/00 , A61P29/00 , A61P37/00 , A61P43/00 , C07D301/02 , C07D303/04 , C07D303/32 , C07D493/10 , C07D493/20 , C07C39/04
CPC分类号： C07D303/04 , C07C37/002 , C07C45/46 , C07C2601/14 , C07D303/14 , C07D303/32 , C07D493/10 , C07C47/565 , C07C39/11 , C07C39/17
摘要： The present invention provides synthetic methods and compositions for treatment of autoimmune and anti-inflammatory disorders comprising administering an effective amount of a derivative of triptolide alone or in combination or alternation with other anti-autoimmune or anti-inflammatory compounds.
摘要翻译：本发明提供用于治疗自身免疫和抗炎症病症的合成方法和组合物，包括单独给药有效量的雷公藤内酯衍生物或与其它抗自身免疫或抗炎化合物组合或替代。

9. 发明申请

WO2010068838A3 PROCESSES FOR PREPARING 5,7 DIAMINOPYRAZOLO[1,5-a] PYRIMIDINE COMPOUNDS 审中-公开
标题翻译：制备5,7二氨基吡唑并[1,5-a]吡啶化合物的方法
公开(公告)号：WO2010068838A3
公开(公告)日：2010-10-14
申请号：PCT/US2009067627
申请日：2009-12-11
申请人： UNIV EMORY , IMPERIAL COLLEGE , LIOTTA DENNIS C , SNYDER JAMES P , JOGALEKAR ASHUTOSH S , BARRETT ANTHONY G M , FUCHTER MATTHEW JOHN , COOK MATTHEW J , KROLL SEBASTIAN H B
发明人： LIOTTA DENNIS C , SNYDER JAMES P , JOGALEKAR ASHUTOSH S , BARRETT ANTHONY G M , FUCHTER MATTHEW JOHN , COOK MATTHEW J , KROLL SEBASTIAN H B
IPC分类号： C07D487/04 , C07D487/02
CPC分类号： C07D487/04
摘要： Processes for the preparation of certain 5,7-diaminopyrazolo[1,5-a]pyrimidine compounds comprising the reaction of a primary or secondary amine and a protected 5-halo-7-aminopyrazolo[1,5-a]pyrimidine compound in solvent system comprising water and one or more organic solvents, optionally in the presence of an exogenous base.
摘要翻译：制备某些5,7-二氨基吡唑并[1,5-a]嘧啶化合物的方法，包括将伯胺或仲胺与受保护的5-卤代-7-氨基吡唑并[1,5-a]嘧啶化合物在溶剂系统，其包含水和一种或多种有机溶剂，任选地在外源性碱的存在下。

10. 发明申请

WO2008151304A8 SELECTIVE INHIBITORS FOR CYCLIN-DEPENDENT KINASES 审中-公开
标题翻译：选择性抑制剂用于循环依赖型动物
公开(公告)号：WO2008151304A8
公开(公告)日：2010-01-07
申请号：PCT/US2008065988
申请日：2008-06-05
申请人： UNIV EMORY , IMPERIAL COLLEGE , JOGALEKAR ASHUTOSH S , SNYDER JAMES P , LIOTTA DENNIS C , BARRETT ANTHONY G M , COOMBES RCDS , ALI SIMAK , SIWICKA ALEKSANDRA , BRACKOW JAN , SCHEIPER BODO
发明人： JOGALEKAR ASHUTOSH S , SNYDER JAMES P , LIOTTA DENNIS C , BARRETT ANTHONY G M , COOMBES RCDS , ALI SIMAK , SIWICKA ALEKSANDRA , BRACKOW JAN , SCHEIPER BODO
IPC分类号： A01N43/90 , A61K31/519
CPC分类号： A61K31/519 , C07D487/04
摘要： This invention provides a class of compounds which are useful for specifically inhibiting cyclin-dependent kinases. This class of compounds finds use in treating diseases resulting from inappropriate activity of cyclin-dependent kinases, including cancer, viral infections (e.g., HIV) neurodegenerative disorders (e.g. Alzheimer's disease), and cardiovascular disorders (e.g. atherosclerosis). Moreover, certain members of this class are particularly useful for inhibiting cyclin-dependent kinase 7 and are especially useful for the treatment of breast cancer.
摘要翻译：本发明提供一类可用于特异性抑制细胞周期蛋白依赖性激酶的化合物。这类化合物可用于治疗由细胞周期蛋白依赖性激酶（包括癌症，病毒感染（例如HIV））神经变性疾病（例如阿尔茨海默病）和心血管疾病（例如动脉粥样硬化）的不适当活动引起的疾病。此外，该类的某些成员特别可用于抑制细胞周期蛋白依赖性激酶7，并且特别可用于治疗乳腺癌。

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