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1. 发明申请

WO2010042489A3 AMINOQUINOLINE DERIVED HEAT SHOCK PROTEIN 90 INHIBITORS, METHODS OF PREPARING SAME, AND METHODS FOR THEIR USE 审中-公开
标题翻译：氨基喹啉衍生的热休克蛋白90抑制剂，其制备方法及其使用方法
公开(公告)号：WO2010042489A3
公开(公告)日：2010-08-12
申请号：PCT/US2009059658
申请日：2009-10-06
申请人： UNIV EMORY , SUN AIMING , GANESH THOTA , MIN JAEKI , THEPCHATRI PAHK , DU YUHONG , SNYDER JAMES P , LIOTTA DENNIS C
发明人： SUN AIMING , GANESH THOTA , MIN JAEKI , THEPCHATRI PAHK , DU YUHONG , SNYDER JAMES P , LIOTTA DENNIS C
IPC分类号： C07D239/72 , A61K31/47 , A61P35/00 , C07D215/02 , C07D401/12 , C07D405/12 , C07D498/04
CPC分类号： C07D401/12 , A61K31/47 , C07D215/40 , C07D215/42 , C07D215/48 , C07D217/24 , C07D239/95 , C07D317/66 , C07D405/04 , C07D405/12 , C07D471/04
摘要： Novel classes of molecular chaperone Heat shock protein 90 (Hsp90) inhibitors and methods for making these classes are provided herein. These compounds are useful in treating and preventing cancer and other Hsp90-related diseases, such as inflammation and neurodegenerative disorders. Also provided herein are methods of treating and preventing cancer and other Hsp90 related disease. The methods include administering to a subject a therapeutically effective amount of an Hsp90 inhibitor.
摘要翻译：本文提供了新型的分子伴侣热休克蛋白90（Hsp90）抑制剂和制备这些类别的方法。这些化合物可用于治疗和预防癌症和其他Hsp90相关疾病，如炎症和神经变性疾病。本文还提供了治疗和预防癌症和其他Hsp90相关疾病的方法。该方法包括向受试者施用治疗有效量的Hsp90抑制剂。

2. 发明申请

WO2009146152A2 NON-MYELOSUPPRESSIVE COMPOUNDS, PHARMACEUTICAL COMPOSITIONS THEREOF, AND METHODS OF TREATMENT 审中-公开
标题翻译：非麻醉性化合物，其药物组合物及其治疗方法
公开(公告)号：WO2009146152A2
公开(公告)日：2009-12-03
申请号：PCT/US2009/039679
申请日：2009-04-06
申请人： EMORY UNIVERSITY , VIRGINIA TECH INTELLECTUAL PROPERTIES, INC. , CORNELL UNIVERSITY , RESEARCH FOUNDATION OF STATE UNIVERSITY OF NEW YORK , SNYDER, James, P. , ALCARAZ, Ana, A. , KINGSTON, David, George Ian , CHEN, Qiao-hong , GANESH, Thota , GIANNAKAKOU, Paraskevi , BANE, Susan
发明人： SNYDER, James, P. , ALCARAZ, Ana, A. , KINGSTON, David, George Ian , CHEN, Qiao-hong , GANESH, Thota , GIANNAKAKOU, Paraskevi , BANE, Susan
IPC分类号： C07D305/14
CPC分类号： C07D305/14
摘要： The present invention provides microtubule targeting compounds that are myelo-sparing. Particularly, the MTCs of the invention are structurally designed to exhibit specificity for inhibiting β-tubulin isotypes that are not related to the myelosuppression associated with other known MTCs. The invention further provides pharmaceutical compositions incorporating the inventive MTCs and methods of treating cancer using the MTCs. The invention still further provides various assays for identifying myelo-sparing compounds and determining whether such compounds are indicated for use with specific patients.
摘要翻译：本发明提供了作为骨髓保护的微管靶向化合物。特别地，本发明的MTC在结构上设计为表现出抑制与其他已知MTC相关的骨髓抑制无关的β-微管蛋白同种型的特异性。本发明还提供掺入本发明MTC的药物组合物和使用MTCs治疗癌症的方法。本发明还进一步提供用于鉴定骨髓保护化合物的各种测定法，并确定这些化合物是否指示用于特定患者。

3. 发明申请

WO2008008854A8 CXCR4 ANTAGONISTS INCLUDING DIAZINE AND TRIAZINE STRUCTURES FOR THE TREATMENT OF MEDICAL DISORDERS 审中-公开
标题翻译： CXCR4拮抗剂包括用于治疗医疗障碍的DIAZINE和TRIAZINE结构
公开(公告)号：WO2008008854A8
公开(公告)日：2009-02-19
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，药物组合物和使用作为趋化因子CXCR4受体的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化合物，药物组合物和方法。所提供的化合物干扰SDF1与受体的结合。这些化合物特别可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的能力来治疗或降低过度增殖性疾病的严重性。这些化合物可用于长期治疗方案。

4. 发明申请

WO2009006437A1 NMDA RECEPTOR ANTAGONISTS FOR NEUROPROTECTION 审中-公开
标题翻译： NMDA受体拮抗剂神经保护
公开(公告)号：WO2009006437A1
公开(公告)日：2009-01-08
申请号：PCT/US2008/068843
申请日：2008-06-30
申请人： EMORY UNIVERSITY , NEUROP, INC. , LIOTTA, Dennis, C. , SNYDER, James, P. , TRAYNELIS, Stephen, F. , WILSON, Lawrence , MOSLEY, Cara , DINGLEDINE, Raymond, J. , MYERS, Scott , TAHIROVIC, Yesim, Altas
发明人： LIOTTA, Dennis, C. , SNYDER, James, P. , TRAYNELIS, Stephen, F. , WILSON, Lawrence , MOSLEY, Cara , DINGLEDINE, Raymond, J. , MYERS, Scott , TAHIROVIC, Yesim, Altas
IPC分类号： A61K31/497 , A61K31/4965
CPC分类号： C07D209/34 , C07C217/20 , C07C235/20 , C07C311/08 , C07D211/52 , C07D213/74 , C07D215/227 , C07D233/32 , C07D233/34 , C07D235/26 , C07D263/58 , C07D295/088
摘要： Provided are compounds, pharmaceutical compositions and methods of treatment or prophylaxis of disorders associated with NMDA receptor activity, including neuropathic pain, stroke, traumatic brain injury, epilepsy, and related neurologic events or neurodegeneration. Compounds are of the general Formula I, or a pharmaceutically acceptable salt, ester, prodrug or derivative thereof are provided: Formula I wherein: each (L)k-Ar1 is a substituted or unsubstituted, mono or bicyclic aryl or heteroaryl; W is a bond, alkyl, or alkenyl; X is a bond, NR1 or O and each R 1 and R 2 is independently H, alkyl, alkenyl or aralkyl or R 1 and R 2 taken together form a 5-8 membered ring; R 3 R 6 are selected from certain specific substituents or a carbonyl; Y is a bond, O, S, SO, SO 2 , CH2, NH, N(alkyl), or NHC(=0); and Z is OH, NR 6 R 7 , NR8SO2(alkyl), NR 8 C(O)NR 6 R 7 , NR 8 C(O)O(alkyl), NR 8 - dihydrothiazole, or NR 8 -dihydroimidazole or wherein Z can fuse with Ar 2 to form selected heterocycles.
摘要翻译：提供了治疗或预防与NMDA受体活性相关的病症的化合物，药物组合物和方法，包括神经性疼痛，中风，创伤性脑损伤，癫痫以及相关的神经系统事件或神经变性。化合物具有通式I，或其药学上可接受的盐，酯，前药或衍生物：式I其中：（L）k-Ar1各自为取代或未取代的单或双环芳基或杂芳基; W是键，烷基或烯基; X是键，NR 1或O，并且每个R 1和R 2独立地是H，烷基，烯基或芳烷基，或者R 1和R 2一起形成5-8元环; R3 R6选自某些特定取代基或羰基; Y是键，O，S，SO，SO 2，CH 2，NH，N（烷基）或NHC（= O）; 并且Z是OH，NR 6 R 7，NR 8 SO 2（烷基），NR 8 C（O）NR 6 R 7，NR 8 C（O）O（烷基），NR 8 - 二氢噻唑或NR 8 - 二氢咪唑，或其中Z可与Ar 2融合形成选定的杂环。

5. 发明申请

WO2008098239A2 PARAMYXOVIRUS FAMILY INHIBITORS AND METHODS OF USE THEREOF 审中-公开
标题翻译：寄生虫家族抑制剂及其使用方法
公开(公告)号：WO2008098239A2
公开(公告)日：2008-08-14
申请号：PCT/US2008/053560
申请日：2008-02-11
申请人： EMORY UNIVERSITY , PLEMPER, Richard, K. , SNYDER, James, P. , SUN, Aiming
发明人： PLEMPER, Richard, K. , SNYDER, James, P. , SUN, Aiming
IPC分类号： C12N7/00 , A61K35/00 , C12N15/85
CPC分类号： A61K31/635 , A61K31/4155 , A61K31/454
摘要： Embodiments of the present disclosure include methods for identifying a compound or compounds useful as therapeutic agents in the treatment of paramyxovirus infections, compounds for the treatment of measles, and high throughput screening methods for identifying compounds capable of inhibiting the proliferation of a paramyxovirus.
摘要翻译：本公开的实施方案包括用于鉴定用于治疗副粘病毒感染的治疗剂的化合物或化合物的方法，用于治疗麻疹的化合物和用于鉴定能够抑制副粘病毒增殖的化合物的高通量筛选方法。

6. 发明申请

WO2008008852A2 CXCR4 ANTAGONISTS INCLUDING HETEROATOMS FOR THE TREATMENT OF MEDICAL DISORDERS 审中-公开
标题翻译： CXCR4拮抗剂，包括用于治疗医学病症的杂合子
公开(公告)号：WO2008008852A2
公开(公告)日：2008-01-17
申请号：PCT/US2007073282
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： A61K31/506
CPC分类号： C07D239/42 , C07D213/64 , C07D213/74 , C07D241/20 , C07D413/12
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. Certain compounds provided can 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. The compounds provided can also be useful for the treatment or prophylaxis of an HIV infection in a host.
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的方法。提供的某些化合物可以干扰SDF1与受体的结合。这些化合物特别适用于通过抑制转移来治疗或减轻过度增殖性疾病的严重程度。所提供的化合物也可用于治疗或预防宿主中的HIV感染。

7. 发明申请

WO2006074428A3 CXCR4 ANTAGONISTS FOR THE TREATMENT OF MEDICAL DISORDERS 审中-公开
标题翻译： CXCR4治疗医疗障碍的拮抗剂
公开(公告)号：WO2006074428A3
公开(公告)日：2007-01-11
申请号：PCT/US2006000604
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： A61K31/4402 , A61K31/505 , A61K31/506
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. 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.
摘要翻译：本发明提供化合物，药物组合物和使用作为趋化因子CXCR4受体的拮抗剂的某些化合物用于治疗CXCR4受体介导的增殖性病症的化合物，药物组合物和方法。所提供的化合物干扰SDF1与受体的结合。这些化合物特别可用于通过抑制转移来治疗或降低过度增殖性疾病的严重性。

8. 发明申请

WO2006017761A3 EPOTHILONE ANALOGUES AS THERAPEUTIC AGENTS 审中-公开
标题翻译：埃坡霉素类似物作为治疗剂
公开(公告)号：WO2006017761A3
公开(公告)日：2006-06-15
申请号：PCT/US2005027942
申请日：2005-08-05
申请人： UNIV EMORY , VIRGINIA POLYTECHNIC INST , SNYDER JAMES P , NETTLES JAMES , LIOTTA DENNIS C , KINGSTON DAVID GEORGE IAN , THOTA GANESH
发明人： SNYDER JAMES P , NETTLES JAMES , LIOTTA DENNIS C , KINGSTON DAVID GEORGE IAN , THOTA GANESH
IPC分类号： A61K31/336
CPC分类号： C07D493/08
摘要： Epothilone analogues represented by Formulas I-IX useful as microtubule stabilizing agents and in the treatment of abnormal cellular proliferation diseases and disorders are disclosed. Methods of making the compounds, compositions containing the compounds, 3D binding models of the binding of epothilone analogues on a,ß-tubulin, and methods for its use in predicting, designing, or selecting therapeutically useful epothilone analogues are also provided.
摘要翻译：公开了可用作微管稳定剂并用于治疗异常细胞增殖疾病和病症的由式I-IX表示的埃坡霉素类似物。还提供了制备所述化合物的方法，含有所述化合物的组合物，埃坡霉素类似物在β-微管蛋白上的结合的3D结合模型，以及其用于预测，设计或选择治疗上有用的埃坡霉素类似物的方法。

9. 发明申请

WO2006017761A2 EPOTHILONE ANALOGUES AS THERAPEUTIC AGENTS 审中-公开
标题翻译： EPOTHILONE类似物作为治疗药物
公开(公告)号：WO2006017761A2
公开(公告)日：2006-02-16
申请号：PCT/US2005/027942
申请日：2005-08-05
申请人： EMORY UNIVERSITY , VIRGINIA POLYTECHNIC INSTITUTE AND STATE UNIVERSITY , SNYDER, James, P. , NETTLES, James , LIOTTA, Dennis, C. , KINGSTON, David, George, Ian , THOTA, Ganesh
发明人： SNYDER, James, P. , NETTLES, James , LIOTTA, Dennis, C. , KINGSTON, David, George, Ian , THOTA, Ganesh
IPC分类号： A61K31/427 , C07D417/02
CPC分类号： C07D493/08
摘要： Epothilone analogues represented by Formulas I-IX useful as microtubule stabilizing agents and in the treatment of abnormal cellular proliferation diseases and disorders are disclosed. Methods of making the compounds, compositions containing the compounds, 3D binding models of the binding of epothilone analogues on α,β-tubulin, and methods for its use in predicting, designing, or selecting therapeutically useful epothilone analogues are also provided.
摘要翻译：公开了用作微管稳定剂和用于治疗异常细胞增殖疾病和病症的由式I-IX表示的埃坡霉酚类似物。还提供了制备化合物的方法，含有化合物的组合物，埃坡霉素类似物与β-微管蛋白结合的3D结合模型，以及用于预测，设计或选择治疗有用的埃坡霉素类似物的方法。

10. 发明申请

WO2005025623A3 EF-24-FACTOR VII CONJUGATES 审中-公开
公开(公告)号：WO2005025623A3
公开(公告)日：2005-03-24
申请号：PCT/US2004/024490
申请日：2004-07-28
申请人： EMORY UNIVERSITY , 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
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-tether-linker-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.

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