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1. 发明申请

WO2008106248A1 METHOD OF CANCER TREATMENT WITH NAPHTHOL ANALOGS 审中-公开
标题翻译：用萘酚类似物治疗癌症的方法
公开(公告)号：WO2008106248A1
公开(公告)日：2008-09-04
申请号：PCT/US2008/051398
申请日：2008-01-18
申请人： BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM , KOO, Ja, Seok , BORNMANN, William , MAXWELL, David
发明人： KOO, Ja, Seok , BORNMANN, William , MAXWELL, David
IPC分类号： A61K31/661 , A61P35/00 , A61P35/02
CPC分类号： A61K31/661
摘要： In one embodiment, the present invention relates to a method of treating a cancer characterized by overexpression of cyclic adenosine monophosphate response element-binding protein (CREB) or phosphorylated CREB (p-CREB) by administering to a patient suffering from the cancer a pharmaceutically-effective amount of a composition comprising a compound selected from the group consisting of 2-{1-[3-(Amidinothio)propyl]-1H-indol-3-yl}-3-(1-methylindol-3-yl)maleimide, naphthol analogs having the structure (I), wherein R 1 is selected from the group consisting of -H, -F, -Cl, -Br, and -I; R 2 is selected from the group consisting of -H, -F, -Cl, -Br, -I, -C 1-6 alkyl, -C 1-6 alkenyl, and -C 1-6 alkynyl; R 3 is selected from the group consisting of -H and -NO 2 ; and R 4 is selected from the group consisting of -H, -C 1-6 alkyl, -C 1-6 alkenyl, -C 1-6 alkynyl, -OC 1-6 alkyl, -OC 1-6 alkenyl, and -OC 1-6 alkynyl; and salts and esters thereof.
摘要翻译：在一个实施方案中，本发明涉及一种治疗癌症的方法，其特征在于通过向患有癌症的患者施用药学上可接受的方法来过表达环腺苷一磷酸应答元件结合蛋白（CREB）或磷酸化CREB（p-CREB）有效量的包含选自2- {1- [3-（脒基硫代）丙基] -1H-吲哚-3-基} -3-（1-甲基吲哚-3-基）马来酰亚胺的化合物的组合物，具有结构（I）的萘酚类似物，其中R 1选自-H，-F，-Cl，-Br和-I; R 2选自-H，-F，-Cl，-Br，-I，-C 1-6 - 烷基，-C 1-6个烯基和-C 1-6个炔基; R 3选自-H和-NO 2 2; 和R 4选自-H，-C 1-6 - 烷基，-C 1-6 - 烯基，-C 1-6烷基，-OC 1-6烯基和-OC 1-6亚烷基，-OC 1-6，炔基; 及其盐和酯。

2. 发明申请

WO2008070350A2 METHODS AND COMPOSITIONS RELATED TO WRAPPING OF DEHYDRONS 审中-公开
标题翻译：与包裹脱水有关的方法和组合物
公开(公告)号：WO2008070350A2
公开(公告)日：2008-06-12
申请号：PCT/US2007/082893
申请日：2007-10-29
申请人： THE BOARD OF REGENTS OF THE UNIVERSITY OF TEXAS SYSTEM , RICE UNIVERSITY , FERNANDEZ, Ariel , BORNMANN, William , LOPEZ-BERESTEIN, Gabriel , SANGUINO, Angela , PENG, Zhenghong
发明人： FERNANDEZ, Ariel , BORNMANN, William , LOPEZ-BERESTEIN, Gabriel , SANGUINO, Angela , PENG, Zhenghong
IPC分类号： C07D401/04 , A61K31/506 , A61P35/00 , C07D401/14
CPC分类号： A61K31/506 , C07D401/04
摘要： This application describes a novel technology in drug discovery and drug-based imaging/detection: the wrapping technology. This technology is based on identified singularities in the structure of soluble proteins. In contrast with drug-design approaches based on standard structural considerations, the packing of a protein, or more precisely, its dehydron pattern, may be used as a selectivity filter to design small-molecule inhibitors. The wrapping technology described herein is a novel form of rational drug design for avoiding side effects in drug therapy and sharpening the inhibitory impact of drugs on the oncokinome.
摘要翻译：本申请描述了一种用于药物发现和基于药物的成像/检测的新技术：包装技术。这项技术是基于可溶性蛋白质结构中可识别的奇点。与基于标准结构考虑的药物设计方法相反，蛋白质的包装，或者更准确地说，其脱水模式可以用作设计小分子抑制剂的选择性过滤器。这里描述的包装技术是一种合理的药物设计的新形式，用于避免药物治疗中的副作用并且增强药物对癌生长因子的抑制作用。

3. 发明申请

WO2008024829A3 RADIOHALOIMATINIBS AND METHODS OF THEIR SYNTHESIS AND USE IN PET IMAGING OF CANCERS 审中-公开
公开(公告)号：WO2008024829A3
公开(公告)日：2008-05-02
申请号：PCT/US2007076501
申请日：2007-08-22
申请人： UNIV TEXAS , BORNMANN WILLIAM , ALAUDDIN MAIN , GELOVANI JURI , GHOSH PRADIP , GUO LIWEI , HAN DONGMEI , MAXWELL DAVID , MUKHOPADHYAY UDAY , PENG ZHENGHONG , SHAVRIN ALEKSANDR , YING YUNMING
发明人： BORNMANN WILLIAM , ALAUDDIN MAIN , GELOVANI JURI , GHOSH PRADIP , GUO LIWEI , HAN DONGMEI , MAXWELL DAVID , MUKHOPADHYAY UDAY , PENG ZHENGHONG , SHAVRIN ALEKSANDR , YING YUNMING
IPC分类号： A61K31/497
CPC分类号： A61K51/0491
摘要： We disclose methods of synthesizing radiohalidated organic compounds and their use in positron emission tomography (PET) imaging of cancer cells.

4. 发明申请

WO2008030795A2 COMPOSITIONS AND METHODS FOR INHIBITION OF TYROSINE KINASES 审中-公开
标题翻译：用于抑制酪氨酸激酶的组合物和方法
公开(公告)号：WO2008030795A2
公开(公告)日：2008-03-13
申请号：PCT/US2007/077511
申请日：2007-09-04
申请人： BOARDS OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM , BORNMANN, William , MAXWELL, David , PENG, Zhenghong , GUO, Liwei
发明人： BORNMANN, William , MAXWELL, David , PENG, Zhenghong , GUO, Liwei
IPC分类号： A61K31/506
CPC分类号： A61K31/506
摘要： Compositions for inhibiting the catalytic activity of tyrosine kinases comprising compounds represented by Formulas (I), (II), and (III). Methods for treating proliferative diseases comprising administering a therapeutically effective amount of the above compositions.
摘要翻译：用于抑制酪氨酸激酶的催化活性的组合物，其包含由式（I），（II）和（III）表示的化合物。治疗增殖性疾病的方法包括施用治疗有效量的上述组合物。

5. 发明申请

WO2008024826A2 RADIOHALOTHYMIDINES AND METHODS OF THEIR SYNTHESIS AND USE IN PET IMAGING OF CANCERS 审中-公开
标题翻译：放射线虫及其合成及其在PET成像中的应用
公开(公告)号：WO2008024826A2
公开(公告)日：2008-02-28
申请号：PCT/US2007/076498
申请日：2007-08-22
申请人： BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEM , BORNMANN, William , ALAUDDIN, Mian , GELOVANI, Juri , GHOSH, Pradip , GUO, Liwei , HAN, Dongmei , MAXWELL, David , MUKHOPADHYAY, Uday , PENG, Zhenghong , SHAVRIN, Aleksandr , YING, Yunming , PAL, Ashutosh
发明人： BORNMANN, William , ALAUDDIN, Mian , GELOVANI, Juri , GHOSH, Pradip , GUO, Liwei , HAN, Dongmei , MAXWELL, David , MUKHOPADHYAY, Uday , PENG, Zhenghong , SHAVRIN, Aleksandr , YING, Yunming , PAL, Ashutosh
IPC分类号： A61K51/00
CPC分类号： A61K51/0491
摘要： We disclose methods of synthesizing radiohalidated organic compounds and their use in positron emission tomography (PET) imaging of cancer cells. We also disclose specific N 3 -radiohaloalkyl thymidines and salts thereof.
摘要翻译：我们公开了合成放射性有机化合物的方法及其在癌细胞正电子发射断层扫描（PET）成像中的应用。我们还公开了具体的N 3 - 二卤代烷基胸苷及其盐。

6. 发明申请

WO2005044995A2 USES OF HUMAN PEPTIDE DEFORMYLASE 审中-公开
标题翻译：使用人类胃蛋白酶
公开(公告)号：WO2005044995A2
公开(公告)日：2005-05-19
申请号：PCT/US2004036866
申请日：2004-11-04
申请人： SLOAN KETTERING INST CANCER , SCHEINBERG DAVID A , LEE MONA D , SIROTNAK FRANCIS M , ANTCZAK CHRISTOPHE , BORNMANN WILLIAM G
发明人： SCHEINBERG DAVID A , LEE MONA D , SIROTNAK FRANCIS M , ANTCZAK CHRISTOPHE , BORNMANN WILLIAM G
IPC分类号： C12N20060101 , C12N
CPC分类号： C12N9/80 , A61K38/00 , C12N15/1137 , C12N2310/14 , C12Y305/01088
摘要： This invention provides a substance derived naturally or manufactured through chemical or genetic engineering that is capable of inhibiting the removal of N-formyl group from peptides by peptide deformylase. This invention also provides a nucleic acid molecule encoding the above fragment of human peptide deformylase or its functional equivalent. This invention provides methods of identifying (1) a compound that inhibits peptide deformylase or its functional equivalent, and (2) a compound that inhibits tumor growth. The invention further provides a method of identifying a compound that inhibits tumor growth comprising comparison of the inhibitory concentration or binding affinity of the compound to a bacterial peptide deformylase with a human peptide deformylase, and this inhibitory concentration or binding of the compound to human peptide deformylase indicates a better inhibition of tumor growth. This invention provides a composition comprising an effective amount of the compound identified by the above methods and a suitable carrier.
摘要翻译：本发明提供了一种天然产生的或通过化学或遗传工程制造的物质，其能够通过肽去甲酰化酶抑制从肽中去除N-甲酰基。本发明还提供了编码人肽脱甲酰酶的上述片段或其功能等同物的核酸分子。本发明提供鉴定（1）抑制肽脱甲酰酶或其功能等价物的化合物的方法，和（2）抑制肿瘤生长的化合物。本发明还提供了鉴定抑制肿瘤生长的化合物的方法，其包括将化合物与细菌肽变性酶与人肽脱甲酰酶的抑制浓度或结合亲和性与人肽变性酶的抑制浓度或结合作用表明更好地抑制肿瘤生长。本发明提供了包含有效量的通过上述方法鉴定的化合物和合适的载体的组合物。

7. 发明申请

WO2008030795A3 COMPOSITIONS AND METHODS FOR INHIBITION OF TYROSINE KINASES 审中-公开
标题翻译：抑制酪氨酸激酶的组合物和方法
公开(公告)号：WO2008030795A3
公开(公告)日：2008-11-27
申请号：PCT/US2007077511
申请日：2007-09-04
申请人： BOARDS OF REGENTS THE UNIVERSI , BORNMANN WILLIAM , MAXWELL DAVID , PENG ZHENGHONG , GUO LIWEI
发明人： BORNMANN WILLIAM , MAXWELL DAVID , PENG ZHENGHONG , GUO LIWEI
IPC分类号： A61K31/506
CPC分类号： A61K31/506
摘要： Compositions for inhibiting the catalytic activity of tyrosine kinases comprising compounds represented by Formulas (I), (II), and (III). Methods for treating proliferative diseases comprising administering a therapeutically effective amount of the above compositions.
摘要翻译：用于抑制包含由式（I），（II）和（III）表示的化合物的酪氨酸激酶的催化活性的组合物。治疗增殖性疾病的方法包括施用治疗有效量的上述组合物。

8. 发明申请

WO2008024826A3 RADIOHALOTHYMIDINES AND METHODS OF THEIR SYNTHESIS AND USE IN PET IMAGING OF CANCERS 审中-公开
标题翻译：放射线甲状腺素及其合成和用于癌症PET显像的方法
公开(公告)号：WO2008024826A3
公开(公告)日：2008-11-20
申请号：PCT/US2007076498
申请日：2007-08-22
申请人： UNIV TEXAS , BORNMANN WILLIAM , ALAUDDIN MIAN , GELOVANI JURI , GHOSH PRADIP , GUO LIWEI , HAN DONGMEI , MAXWELL DAVID , MUKHOPADHYAY UDAY , PENG ZHENGHONG , SHAVRIN ALEKSANDR , YING YUNMING , PAL ASHUTOSH
发明人： BORNMANN WILLIAM , ALAUDDIN MIAN , GELOVANI JURI , GHOSH PRADIP , GUO LIWEI , HAN DONGMEI , MAXWELL DAVID , MUKHOPADHYAY UDAY , PENG ZHENGHONG , SHAVRIN ALEKSANDR , YING YUNMING , PAL ASHUTOSH
IPC分类号： A61K51/00 , A61M36/14
CPC分类号： A61K51/0491
摘要： We disclose methods of synthesizing radiohalidated organic compounds and their use in positron emission tomography (PET) imaging of cancer cells. We also disclose specific N 3 -radiohaloalkyl thymidines and salts thereof.
摘要翻译：我们公开了合成放射性卤化有机化合物的方法及其在癌细胞的正电子发射断层摄影（PET）成像中的用途。我们还公开了具体的N 3 - 对 - 二卤代烷基胸腺嘧啶及其盐。

9. 发明申请

WO2008005877A3 INHIBITORS OF C-KIT AND USES THEREOF 审中-公开
标题翻译： C-kit及其用途的抑制剂
公开(公告)号：WO2008005877A3
公开(公告)日：2008-03-27
申请号：PCT/US2007072555
申请日：2007-06-29
申请人： UNIV TEXAS , BORNMANN WILLIAM , MAXWELL DAVID , PAL ASHUTOSH , PENG ZHENGHONG , ESTROV ZEEV
发明人： BORNMANN WILLIAM , MAXWELL DAVID , PAL ASHUTOSH , PENG ZHENGHONG , ESTROV ZEEV
IPC分类号： G01N33/574
CPC分类号： C07D471/04
摘要： Compounds and methods useful as inhibitors of c-Kit are presented. Pharmaceutical compositions containing these compounds, methods of using these compounds as inhibitors of c-Kit and processes for synthesizing these compounds are also described herein.
摘要翻译：提出了可用作c-Kit抑制剂的化合物和方法。含有这些化合物的药物组合物，使用这些化合物作为c-Kit抑制剂的方法以及合成这些化合物的方法也在本文中描述。

10. 发明申请

WO2005044995A3 USES OF HUMAN PEPTIDE DEFORMYLASE 审中-公开
公开(公告)号：WO2005044995A3
公开(公告)日：2005-05-19
申请号：PCT/US2004/036866
申请日：2004-11-04
申请人： SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCH , SCHEINBERG, David, A. , LEE, Mona, D. , SIROTNAK, Francis, M. , ANTCZAK, Christophe , BORNMANN, William, G.
发明人： SCHEINBERG, David, A. , LEE, Mona, D. , SIROTNAK, Francis, M. , ANTCZAK, Christophe , BORNMANN, William, G.
IPC分类号： C07K2/00 , A61K38/00
摘要： This invention provides a substance derived naturally or manufactured through chemical or genetic engineering that is capable of inhibiting the removal of N-formyl group from peptides by peptide deformylase. This invention also provides a nucleic acid molecule encoding the above fragment of human peptide deformylase or its functional equivalent. This invention provides methods of identifying (1) a compound that inhibits peptide deformylase or its functional equivalent, and (2) a compound that inhibits tumor growth. The invention further provides a method of identifying a compound that inhibits tumor growth comprising comparison of the inhibitory concentration or binding affinity of the compound to a bacterial peptide deformylase with a human peptide deformylase, and this inhibitory concentration or binding of the compound to human peptide deformylase indicates a better inhibition of tumor growth. This invention provides a composition comprising an effective amount of the compound identified by the above methods and a suitable carrier.

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