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1. 发明申请

WO03011115A3 PEPTIDE-BASED MULTIMERIC TARGETED CONTRAST AGENTS 审中-公开
标题翻译：基于肽的多靶点造影剂
公开(公告)号：WO03011115A3
公开(公告)日：2003-05-22
申请号：PCT/US0224261
申请日：2002-07-30
申请人： EPIX MEDICAL INC , ZHANG ZHAODA , CARAVAN PETER D , MCMURRY THOMAS J , KOLODZIEJ ANDREW , NAIR SHRIKUMAR , AMEDIO JOHN C , DUMAS STEPHANE , WANG XIFANG , SUN WEI-CHUAN , NIVOROZHKIN ALEXANDER L , KOERNER STEFFI K
发明人： ZHANG ZHAODA , CARAVAN PETER D , MCMURRY THOMAS J , KOLODZIEJ ANDREW , NAIR SHRIKUMAR , AMEDIO JOHN C , DUMAS STEPHANE , WANG XIFANG , SUN WEI-CHUAN , NIVOROZHKIN ALEXANDER L , KOERNER STEFFI K
IPC分类号： A61K49/00 , A61K47/48 , A61K49/08 , C07K5/117 , C07K7/06 , C07K7/08 , A61B5/055
CPC分类号： C07K7/08 , A61K47/64 , A61K49/0039 , A61K49/0041 , A61K49/0043 , A61K49/0056 , A61K49/085 , A61K49/122 , A61K49/124 , A61K49/14 , A61K51/088 , C07K1/1077 , C07K7/06
摘要： Peptides and peptide-targeted multimeric contrast agents are described, as well as methods of making and using the contrast agents.
摘要翻译：描述了肽和靶向肽的多聚体造影剂，以及制造和使用造影剂的方法。

2. 发明申请

WO0108712A2 TARGETING MULTIMERIC IMAGING AGENTS THROUGH MULTILOCUS BINDING 审中-公开
标题翻译：通过多重绑定来定位多元成像剂
公开(公告)号：WO0108712A2
公开(公告)日：2001-02-08
申请号：PCT/US0020536
申请日：2000-07-28
申请人： EPIX MEDICAL INC , LAUFFER RANDALL B , MCMURRY THOMAS J , DUMAS STEPHANE , KOLODZIEJ ANDREW , AMEDIO JOHN , CARAVAN PETER , ZHANG ZHAODA , NAIR SHRIKUMAR
发明人： LAUFFER RANDALL B , MCMURRY THOMAS J , DUMAS STEPHANE , KOLODZIEJ ANDREW , AMEDIO JOHN , CARAVAN PETER , ZHANG ZHAODA , NAIR SHRIKUMAR
IPC分类号： A61K49/04 , A61K49/00 , A61K49/06 , A61K49/08 , A61K49/14
CPC分类号： A61K49/0021 , A61K49/0032 , A61K49/0052 , A61K49/085 , A61K49/10 , A61K49/124 , A61K49/128 , A61K49/14
摘要： The present invention relates to contrast agents for diagnostic imaging. In particular, this invention relates to novel multimeric compounds which exhibit improved relaxivity properties upon binding to endogenous proteins or other physiologically relevant sites. The compounds consist of: a) two or more Image Enhancing Moieties (IEMs) (or signal-generating moiety) comprising multiple subunits; b) two or more Target Binding Moieties (TBMs), providing for in vivo localization and multimer rigidification; c) a scaffold framework for attachment of the above moieties; and d) optional linkers for attachment of the IEMs to scaffold. This invention also relates to pharmaceutical compositions comprising these compounds and to methods of using the compounds and compositions for contrast enhancement of diagnostic imaging.
摘要翻译：本发明涉及用于诊断成像的造影剂。特别地，本发明涉及新颖的多聚体化合物，其在结合内源蛋白质或其他生理学相关位点时表现出改善的松弛性能。该化合物包括：a）包含多个亚基的两个或更多个图像增强部分（IEM）（或产生信号的部分）; b）两个或多个目标结合部分（TBM），用于体内定位和多聚体硬化; c）用于连接上述部分的支架框架; 和d）用于将IEM连接到脚手架的可选接头。本发明还涉及包含这些化合物的药物组合物以及使用化合物和组合物用于诊断成像的对比度增强的方法。

3. 发明申请

WO2007047608A3 FIBRIN TARGETED THERAPEUTICS 审中-公开
标题翻译： FIBRIN目标治疗
公开(公告)号：WO2007047608A3
公开(公告)日：2007-09-20
申请号：PCT/US2006040430
申请日：2006-10-16
申请人： EPIX PHARM INC , MCMURRY THOMAS J , KOLODZIEJ ANDREW , CARPENTER ALAN P JR , JONES SIMON , GRAHAM PHILIP , LOOBY RICHARD , SHRIKUMAR A NAIR , WANG XIFANG , OVEROYE-CHEN KIRSTEN , BARRETT JOHN A
发明人： MCMURRY THOMAS J , KOLODZIEJ ANDREW , CARPENTER ALAN P JR , JONES SIMON , GRAHAM PHILIP , LOOBY RICHARD , SHRIKUMAR A NAIR , WANG XIFANG , OVEROYE-CHEN KIRSTEN , BARRETT JOHN A
IPC分类号： A61K38/37
CPC分类号： C07K7/08 , A61K38/00 , A61K47/62 , A61K47/64 , A61K47/6911 , A61K49/14 , A61K51/088 , C07K7/06
摘要： Fibrin targeted therapeutic agents for the treatment of thromboembolism, infection, and cancer are provided.
摘要翻译：提供了用于治疗血栓栓塞，感染和癌症的纤维蛋白靶向治疗剂。

4. 发明专利

JP2005224589A Detection and treatment of intravascular lesions 审中-公开
标题翻译：检测和治疗血管内皮生长因子
公开(公告)号：JP2005224589A
公开(公告)日：2005-08-25
申请号：JP2004233953
申请日：2004-08-10
申请人： Epix Medical Inc , エピックスメディカル, インコーポレイテッド
发明人： MCMURRY THOMAS J , WEISSKOFF ROBERT M
IPC分类号： A61B18/20 , A61B17/00 , A61B17/22 , A61K38/48 , A61K45/00 , A61K49/00 , A61P7/02 , A61P9/10
CPC分类号： A61K49/0056 , A61K38/08 , A61K38/12 , A61K38/49 , A61K49/0039 , A61K49/0041 , A61K49/0043
摘要： PROBLEM TO BE SOLVED: To enhance the sensitivity and facilitate the administration of therapies in a timely fashion in the detection and treatment of intravascular lesions.
SOLUTION: An optical agent which contains a fibrin binding moiety covalently linked to an optical dye as well as a method of treating intravascular lesions in a patient by using such an optical agent are described. The method includes the following processes: (a) a process of administering the optical agent that includes a fibrin binding moiety and an optical dye and can form a fibrin-optical agent complex at the site of the lesion; (b) a process of detecting a signal from the fibrin-optical agent complex by using a device inserted near the lesion; (c) a process of acquiring data about the lesion on the basis of the signal of the fibrin-optical agent complex; and (d) a process of delivering a therapy, on the basis of the acquired data, to at least a portion of the lesion.
COPYRIGHT: (C)2005,JPO&NCIPI
摘要翻译：要解决的问题：为了提高灵敏度，并且有助于及时管理血管内病变的检测和治疗。解决方案：描述了包含与光学染料共价连接的纤维蛋白结合部分的光学剂以及通过使用这种光学剂治疗患者的血管内损伤的方法。该方法包括以下过程：（a）施用包含纤维蛋白结合部分和光学染料的光学剂的方法，并且可以在损伤部位形成纤维蛋白 - 光学剂复合物; （b）通过使用插入病变附近的装置检测来自纤维蛋白 - 光学剂复合物的信号的过程; （c）基于纤维蛋白 - 光学剂复合物的信号获取关于病变的数据的过程; 和（d）基于所获取的数据将治疗递送至至少一部分病变的过程。版权所有（C）2005，JPO＆NCIPI

5. 发明专利

JP2004210796A Bioactivated contrast agent for diagnostic imaging 审中-公开
公开(公告)号：JP2004210796A
公开(公告)日：2004-07-29
申请号：JP2004055545
申请日：2004-02-27
申请人： Epix Medical Inc , エピックスメディカル, インコーポレイテッド
发明人： LAUFFER RANDALL B , MCMURRY THOMAS J , DUNHAM STEPHEN O , SCOTT DANIEL M , PARMELEE DAVID J , DUMAS STEPHANE
IPC分类号： A61K49/00 , A61B5/055 , A61K49/06 , A61K49/08 , A61K49/14 , G01R33/28
CPC分类号： A61K49/14 , A61K49/0002 , A61K49/0017 , A61K49/0019 , A61K49/085 , A61K49/10 , A61K49/103 , A61K49/106
摘要： PROBLEM TO BE SOLVED: To obtain a compound useful for diagnostic contrast agents for Magnetic Resonance Imaging (MRI) and optical imaging. SOLUTION: The magnetic resonance imaging or optical imaging prodrug contrast agent has a lower affinity for a tissue protein than a bioactivated form of the contrast agent. In one embodiment, the prodrug contrast agent comprises:(a) an image-enhancing moiety (IEM); (b) a protein binding moiety (PBM); and (c) a modification site (MS). COPYRIGHT: (C)2004,JPO&NCIPI

6. 发明专利

JP2004026793A Diagnostic imaging contrast agent with prolonged blood retention 审中-公开
公开(公告)号：JP2004026793A
公开(公告)日：2004-01-29
申请号：JP2002369062
申请日：2002-12-19
申请人： Epix Medical Inc , エピックスメディカル, インコーポレイテッド
发明人： MCMURRY THOMAS J , SAJIKI HIRONAO , SCOTT DANIEL M , LAUFFER RANDALL B
IPC分类号： A61K49/00 , A61B5/055 , A61B6/00 , A61B8/00 , A61K49/04 , A61K49/08 , A61K49/18 , A61K51/00 , C07F9/09 , G01R33/28
CPC分类号： A61K49/085 , A61B6/507 , A61K49/0002 , A61K49/10 , A61K49/103 , A61K49/106 , C07F9/091
摘要： PROBLEM TO BE SOLVED: To provide a contrast agent for diagnostic imaging with prolonged blood retention. SOLUTION: This imaging contrast agent for diagnostic use contains (a) an image enhancing moiety (IEM), (b) a protein plasma binding moiety (PPBM) and (c) a blood half-life extending moiety (BHEM). The agent is bonded to plasma proteins in an amount of at least about 10%. In the pharmacokinetic experiment of rat plasma, the area under the curve of plasma concentration to time (0-10 min) is larger than the area observed by the combination of IEM and PPBM and free from BHEM by at least about 20%. COPYRIGHT: (C)2004,JPO

7. 发明专利

JP2003201258A TARGETING MULTIMERIC IMAGING AGENT THROUGH MULTILOCUS BINDING 审中-公开
公开(公告)号：JP2003201258A
公开(公告)日：2003-07-18
申请号：JP2002341392
申请日：2002-11-25
申请人： EPIX MEDICAL INC
发明人： LAUFFER RANDALL B , MCMURRY THOMAS J , DUMAS STEPHANE , KOLODZIEJ ANDREW , AMEDIO JOHN , CARAVAN PETER , ZHANG ZHAODA , NAIR SHRIKUMAR
IPC分类号： A61K49/04 , A61K49/00 , A61K49/06 , A61K49/08 , A61K49/14
摘要： PROBLEM TO BE SOLVED: To provide a method for improving a signal contrast in a specific target. SOLUTION: The present invention provides a method for increasing contrast using MRI or optical imaging, wherein (a) a multilocus contrast agent binds to a target, (b) contrast at the target is enhanced when the contrast agent is bound to the target, (c) the contrast enhancement improves with either of the number of IEMs, the rigidity of the molecule, or both. In one embodiment, the relaxivity is at least 10 mM -1 s -1 per IEM. COPYRIGHT: (C)2003,JPO

8. 发明申请

WO2010053550A3 CXCR4 RECEPTOR COMPOUNDS 审中-公开
标题翻译： CXCR4受体化合物
公开(公告)号：WO2010053550A3
公开(公告)日：2010-07-15
申请号：PCT/US2009005979
申请日：2009-11-04
申请人： ANCHOR THERAPEUTICS INC , KULIOPULOS ATHAN , MCMURRY THOMAS J , COVIC LIDIJA , TCHERNYCHEV BORIS
发明人： KULIOPULOS ATHAN , MCMURRY THOMAS J , COVIC LIDIJA , TCHERNYCHEV BORIS
IPC分类号： A61K38/00
CPC分类号： C07K7/08 , A61K38/00 , C07K7/06 , C07K14/7158
摘要： The invention relates generally to compounds which are allosteric modulators (e.g., positive and negative allosteric modulators, and allosteric agonists) of the G protein coupled receptor for stromal derived factor 1 (SDF-I), also known as the CXCR4 receptor. The CXCR4 receptor compounds are derived from the intracellular loops and domains of the CXCR4 receptor. The invention also relates to the use of these CXCR4 receptor compounds and pharmaceutical compositions comprising the CXCR4 receptor compounds in the treatment of diseases and conditions associated with CXCR4 modulation such as bone marrow transplantation, chemosensitization, cancer, metastatic disease, inflammatory diseases, HIV infection and stem cell-based regenerative medicine.
摘要翻译：本发明一般涉及作为基质衍生因子1（SDF-1）的G蛋白偶联受体（也称为CXCR4受体）的变构调节剂（例如正向和负向变构调节剂和变构激动剂）。 CXCR4受体化合物来源于CXCR4受体的细胞内环和结构域。本发明还涉及这些CXCR4受体化合物和包含CXCR4受体化合物的药物组合物在治疗与CXCR4调节相关的疾病和病症如骨髓移植，化学敏化，癌症，转移性疾病，炎性疾病，HIV感染和干细胞为基础的再生医学。

9. 发明申请

WO2010053545A3 APJ RECEPTOR COMPOUNDS 审中-公开
标题翻译： APJ受体化合物
公开(公告)号：WO2010053545A3
公开(公告)日：2010-07-15
申请号：PCT/US2009005974
申请日：2009-11-04
申请人： ANCHOR THERAPEUTICS INC , JANZ JAY , KULIOPULOS ATHAN , MCMURRY THOMAS J
发明人： JANZ JAY , KULIOPULOS ATHAN , MCMURRY THOMAS J
IPC分类号： C07K7/00
CPC分类号： C07K14/7158 , A61K38/00 , A61K47/542 , A61K47/554
摘要： The invention relates generally to compounds which are allosteric modulators (e.g., negative and positive allosteric modulators, allosteric agonists, and ago-allosteric modulators) of the G protein coupled receptor apelin, also known as the APJ receptor. The APJ receptor compounds are derived from the intracellular loops and domains of the the APJ receptor. The invention also relates to the use of these APJ receptor compounds and pharmaceutical compositions comprising the APJ receptor compounds in the treatment of diseases and conditions associated with APJ receptor modulation, such as heart diseases (e.g., hypertension and heart failure, such as congestive heart failure), cancer, diabetes, stem cell trafficking, fluid homeostasis, cell proliferation, immune function, obesity, metastatic disease, and HIV infection.
摘要翻译：本发明一般涉及G蛋白偶联受体apelin（也称为APJ受体）的变构调节剂（例如，负变构和正变构调节剂，变构兴奋剂和前变体调节剂）的化合物。 APJ受体化合物衍生自APJ受体的细胞内环和结构域。本发明还涉及这些APJ受体化合物和包含APJ受体化合物的药物组合物在治疗与APJ受体调节相关的疾病和病症（例如心脏病（例如，高血压和心力衰竭，例如充血性心力衰竭）），癌症，糖尿病，干细胞运输，流体稳态，细胞增殖，免疫功能，肥胖，转移性疾病和HIV感染。

10. 发明申请

WO2010053548A3 PTHR1 RECEPTOR COMPOUNDS 审中-公开
标题翻译： PTHR1受体化合物
公开(公告)号：WO2010053548A3
公开(公告)日：2010-07-15
申请号：PCT/US2009005977
申请日：2009-11-04
申请人： ANCHOR THERAPEUTICS INC , REN YONG , KULIOPULOS ATHAN , MCMURRY THOMAS J
发明人： REN YONG , KULIOPULOS ATHAN , MCMURRY THOMAS J
IPC分类号： C07K1/00 , C07K17/00
CPC分类号： C07K14/72 , A61K38/00 , A61K47/542
摘要： The invention relates generally to compounds which are allosteric modulators (e.g., negative and positive allosteric modulators, allosteric agonists, and ago-allosteric modulators) of the G protein coupled receptor PTHRl, also known as parathyroid hormone/parathyroid hormone related protein receptor. The PTHRl compounds are derived from the intracellular loops and domains of the PTHRl receptor. The invention also relates to the use of these PTHRl receptor compounds and pharmaceutical compositions comprising the PTHRl receptor compounds in the treatment of diseases and conditions associated with PTHRl receptor modulation, such as osteoporosis; humoral hypercalcemia of malignancy; osteolytic and osteoblastic metastasis to bone; primary and secondary hyperparathyroidism associated increase in bone absorption; vascular calcification; psychiatric disorders and cognitive disorders associated with hyperparathyroidism; dermatological disorders; and excess hair growth.
摘要翻译：本发明一般涉及G蛋白偶联受体PTHR1（也称为甲状旁腺激素/甲状旁腺激素相关蛋白受体）的变构调节剂（例如，负变构和正变构调节剂，变构兴奋剂和前变体调节剂）的化合物。 PTHR1化合物衍生自PTHR1受体的细胞内环和结构域。本发明还涉及这些PTHR1受体化合物和包含PTHR1受体化合物的药物组合物在治疗与PTHR1受体调节如骨质疏松症有关的疾病和病症中的用途; 体液高钙血症恶性肿瘤; 骨质疏松和成骨细胞转移; 原发性和继发性甲状旁腺功能亢进相关的骨吸收增加; 血管钙化; 与甲状旁腺功能亢进相关的精神疾病和认知障碍; 皮肤病; 和头发生长过多。

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