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公开(公告)号：US20120282172A1
公开(公告)日：2012-11-08
申请号：US13467178
申请日：2012-05-09
Applicant: João Nuno Sereno de Almeida Moreira , Vera Lúcia Dantas Nunes Caldeira de Moura , Sérgio Paulo de Magalhães Simões , Maria da Conceição Monteiro Pedroso de Lima
Inventor： João Nuno Sereno de Almeida Moreira , Vera Lúcia Dantas Nunes Caldeira de Moura , Sérgio Paulo de Magalhães Simões , Maria da Conceição Monteiro Pedroso de Lima
IPC: A61K9/127 , A61K9/00 , A61K9/107 , A61K31/704 , A61K51/12 , A61K31/675 , A61K31/196 , A61K31/198 , A61K31/255 , A61K31/175 , A61K31/131 , A61K31/565 , A61K31/047 , A61K31/519 , A61K31/513 , A61K31/7068 , A61K31/7076 , A61K31/517 , A61K31/52 , A61K31/475 , A61K33/24 , A61K31/337 , A61K31/4745 , A61K31/616 , A61K38/17 , A61K38/57 , A61P35/00 , A61P31/00 , A61P29/00 , A61P9/00 , G01N21/64 , A61K49/00
CPC classification number: A61K47/48246 , A61K9/0019 , A61K9/127 , A61K31/00 , A61K31/704 , A61K47/64 , A61K47/6911 , C07K14/4702 , C07K2319/33
Abstract: The present invention provides a system presenting site-specific accumulation through a ligand that specifically targets a receptor overexpressed on the surface of specific cells within a target organ, like, for example, tumor cells and/or vascular cells of tumor blood vessels. Moreover, this invention provides a method where, upon internalization of the previous-mentioned system by the target cells, triggered release at a high rate of the associated agent takes place, permitting efficient intracellular delivery and, thus, increased concentration of the transported cargo at the target site. Overall, this invention provides a method for the diagnosis, prevention and treatment of human diseases and disorders.
Abstract translation: 本发明提供了一种系统，其通过特异性靶向在靶器官（例如肿瘤细胞和/或肿瘤血管的血管细胞）中的特定细胞表面上过表达的受体的配体。 此外，本发明提供了一种方法，其中在靶细胞内部化先前提及的系统之后，以相关药剂的高速率触发释放，允许有效的细胞内递送，并因此使运送货物的浓度增加 目标网站。 总之，本发明提供了一种诊断，预防和治疗人类疾病和病症的方法。
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42.发明授权公开(公告)号：US08288345B2
公开(公告)日：2012-10-16
申请号：US12040851
申请日：2008-02-29
Applicant: Michael P. Belmares , Jonathan David Garman , Peter S. Lu , Michael W. Salter , Michael Tymianski
Inventor： Michael P. Belmares , Jonathan David Garman , Peter S. Lu , Michael W. Salter , Michael Tymianski
CPC classification number: A61K47/48246 , A61K38/00 , A61K47/645 , C07K7/06 , C07K14/70571 , C07K2319/10
Abstract: The invention provides methods for treating stroke and compositions for use in the same. The methods employ a chimeric peptide of an active peptide and an internalization peptide. The internalization peptide is a tat variant that promotes uptake of itself and a linked active peptide into a cell without substantial binding to N-type calcium channels. Use of the tat variant allows treating of stroke free of certain side effects associated with binding to N-type calcium channels. Tat variant peptides can also be linked to other active agent for use in treating other diseases.
Abstract translation: 本发明提供了治疗中风和组合物的方法。 该方法采用活性肽和内化肽的嵌合肽。 内化肽是一种tat变体，其促进其自身的摄取和连接的活性肽进入细胞，而不与N型钙通道基本结合。 使用tat变体允许治疗与结合N-型钙通道相关的某些副作用。 Tat变体肽也可以连接到其他活性剂以用于治疗其它疾病。
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43.发明申请HMGN2 PEPTIDES AND RELATED MOLECULES THAT SELECTIVELY HOME TO TUMOR BLOOD VESSELS AND TUMOR CELLS 有权HMGN2肽和相关分子选择性地选择肿瘤血管和肿瘤细胞公开(公告)号：US20120121501A1
公开(公告)日：2012-05-17
申请号：US13276237
申请日：2011-10-18
Applicant: Erkki Ruoslahti , Kimmo Porkka , Sven Christian
Inventor： Erkki Ruoslahti , Kimmo Porkka , Sven Christian
CPC classification number: A61K47/48246 , A61K47/64 , C07K7/06 , C07K14/4702 , C07K2319/00
Abstract: The present invention provides a conjugate which contains a therapeutic moiety linked to a homing molecule that selectively homes to tumor blood vessels and tumor cells and that specifically binds the receptor bound by peptide KDEPQRRSARLSAKPAPPKPEPKPKKAPAKK (SEQ ID NO: 9). Methods of directing a conjugate of the invention to tumor blood vessels and tumor cells and of using a conjugate to treat cancer also are provided.
Abstract translation: 本发明提供了一种缀合物，其包含与归巢分子连接的治疗部分，其选择性地归属于肿瘤血管和肿瘤细胞，并且特异性结合由肽KDEPQRRSARLSAKPAPPKPEPKPKKAPAKK（SEQ ID NO：9）结合的受体。 还提供了将本发明的缀合物引导到肿瘤血管和肿瘤细胞以及使用缀合物治疗癌症的方法。
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公开(公告)号：US20120058946A1
公开(公告)日：2012-03-08
申请号：US13219401
申请日：2011-08-26
Applicant: Hong M. Moulton , Ryszard Kole
Inventor： Hong M. Moulton , Ryszard Kole
CPC classification number: A61K47/48246 , A61K31/7088 , A61K47/64 , C07K2319/33 , C12N15/113 , C12N15/87 , C12N2310/11 , C12N2810/40
Abstract: An antisense compound for use in treating myotonic dystrophy DM1 or DM2, a method of enhancing antisense targeting to heart and quadricep muscles, and a method for treating DM1 or DM2 in a mammalian subject are disclosed. The oligonucleotide has 8-30 bases, with at least 8 contiguous bases being complementary to the polyCUG or polyCCUG repeats in the 3′UTR region of dystrophia myotonica protein kinase (DMPK) mRNA in DM1 or DM2, respectively. Conjugated to the oligonucleotide is a cell-penetrating peptide having the sequence (RXRR(B/X)R)2XB, where R is arginine; B is β-alanine; and each X is —C(O)—(CH2)n—NH—, where n is 4-6. The antisense compound is effective to selectively block the sequestration of muscleblind-like 1 protein (MBNL1) and/or CUGBP, in heart and quadricep muscle in a myotonic dystrophy animal model.
Abstract translation: 公开了用于治疗强直性营养不良DM1或DM2的反义化合物，增强对心脏和四头肌的反义靶向的方法，以及哺乳动物受试者中治疗DM1或DM2的方法。 寡核苷酸具有8-30个碱基，其中至少8个连续碱基分别与DM1或DM2中的肌营养不良肌群蛋白激酶（DMPK）mRNA的3'UTR区域中的polyCUG或polyCCUG重复序列互补。 与寡核苷酸共轭是具有序列（RXRR（B / X）R）2XB的细胞穿透肽，其中R是精氨酸; B是丙氨酸; 并且每个X是-C（O） - （CH 2）n -NH-，其中n是4-6。 反义化合物有效地选择性地阻断强直肌营养不良动物模型中心肌和四头肌中肌肉样蛋白样蛋白（MBNL1）和/或CUGBP的螯合。
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公开(公告)号：US20120046223A1
公开(公告)日：2012-02-23
申请号：US13145530
申请日：2010-01-27
Applicant: Todd C. Zion , Thomas M. Lancaster
Inventor： Todd C. Zion , Thomas M. Lancaster
CPC classification number: A61K47/4823 , A61K38/00 , A61K38/28 , A61K47/26 , A61K47/48092 , A61K47/48246 , A61K47/549 , A61K47/61 , A61K47/64
Abstract: The disclosure provides cross-linked materials that include multivalent cross-linking agents that bind an exogenous target molecule; and conjugates that include two or more separate affinity ligands bound to a conjugate framework, where in the two or more affinity ligands compete with the exogenous target molecule for binding with the cross-linking a agents and wherein conjugates are cross-linked within the material as a result of non-covalent interact ions between cross-linking agents and affinity ligands on different conjugates. The conjugates also include a drug.
Abstract translation: 本公开提供交联材料，其包括结合外源性靶分子的多价交联剂; 以及包含与缀合物框架结合的两个或更多个分离的亲和配体的缀合物，其中两个或更多个亲和配体与外源靶分子竞争与交联剂结合，并且其中缀合物在材料内交联 交联剂与不同共轭物上的亲和配体之间的非共价相互作用离子的结果。 缀合物还包括药物。
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Patent Agency Ranking
公开(公告)号：US20110294718A1
公开(公告)日：2011-12-01
申请号：US12671694
申请日：2008-07-23
Applicant: Hans-Georg Lerchen , Ursula Krenz , Joerg Keldenich , Nicole Diedrichs , Thomas Krahn , Claudia Hirth-Dietrich , Barbara Albrecht-Küpper
Inventor： Hans-Georg Lerchen , Ursula Krenz , Joerg Keldenich , Nicole Diedrichs , Thomas Krahn , Claudia Hirth-Dietrich , Barbara Albrecht-Küpper
IPC: A61K38/05 , A61P9/00 , C07D417/14 , C07D417/12 , A61K31/4439
CPC classification number: A61K47/48246 , A61K31/4439 , A61K47/542 , A61K47/64 , C07D417/12 , C07K5/06086
Abstract: The present application relates to prodrug derivatives of 2-amino-6-({[2-(4-chlorophenyl)-1,3-thiazol-4-yl]methyl}thio)-4-[4-(2-hydroxyethoxy)phenyl]pyridine-3,5-dicarbonitrile, processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, especially of cardiovascular disorders.
Abstract translation: 本申请涉及2-氨基-6 - （{[2-（4-氯苯基）-1,3-噻唑-4-基]甲基}硫基）-4- [4-（2-羟基乙氧基） 苯基]吡啶-3,5-二腈，其制备方法，它们用于治疗和/或预防疾病的用途，及其用于制备用于治疗和/或预防疾病，特别是心血管疾病的药物的用途。
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47.发明授权HMGN2 peptides and related molecules that selectively home to tumor blood vessels and tumor cells 有权HMGN2肽和相关分子，选择性地归属于肿瘤血管和肿瘤细胞公开(公告)号：US08048983B2
公开(公告)日：2011-11-01
申请号：US12288547
申请日：2008-10-20
Applicant: Erkki Ruoslahti , Kimmo Porkka , Sven Christian
Inventor： Erkki Ruoslahti , Kimmo Porkka , Sven Christian
IPC: C07K5/00 , C07K14/00 , G01N33/574
CPC classification number: A61K47/48246 , A61K47/64 , C07K7/06 , C07K14/4702 , C07K2319/00
Abstract: The present invention provides a conjugate which contains a therapeutic moiety linked to a homing molecule that selectively homes to tumor blood vessels and tumor cells and that specifically binds the receptor bound by peptide KDEPQRRSARLSAKPAPPKPEPKPKKAPAKK (SEQ ID NO: 9). Methods of directing a conjugate of the invention to tumor blood vessels and tumor cells and of using a conjugate to treat cancer also are provided.
Abstract translation: 本发明提供了一种缀合物，其包含与归巢分子连接的治疗部分，其选择性地归属于肿瘤血管和肿瘤细胞，并且特异性结合由肽KDEPQRRSARLSAKPAPPKPEPKPKKAPAKK（SEQ ID NO：9）结合的受体。 还提供了将本发明的缀合物引导到肿瘤血管和肿瘤细胞以及使用缀合物治疗癌症的方法。
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公开(公告)号：US07910088B2
公开(公告)日：2011-03-22
申请号：US11688968
申请日：2007-03-21
Applicant: Christophe Arbogast , Philippe Bussat , Hong Fan , Karen E. Linder , Edmund R. Marinelli , Palaniappa Nanjappan , Adrian D. Nunn , Radhakrishna K. Pillai , Sibylle Pochon , Kondareddiar Ramalingam , Ajay Shrivastava , Bo Song , Rolf E. Swenson , Mathew A. Von Wronski , Aaron K. Sato , Sharon Michele Walker , Daniel T. Dransfield , Feng Yan
Inventor： Christophe Arbogast , Philippe Bussat , Hong Fan , Karen E. Linder , Edmund R. Marinelli , Palaniappa Nanjappan , Adrian D. Nunn , Radhakrishna K. Pillai , Sibylle Pochon , Kondareddiar Ramalingam , Ajay Shrivastava , Bo Song , Rolf E. Swenson , Mathew A. Von Wronski , Aaron K. Sato , Sharon Michele Walker , Daniel T. Dransfield , Feng Yan
IPC: A61B8/00
CPC classification number: A61K47/48246 , A61K38/16 , A61K47/42 , A61K47/60 , A61K47/64 , A61K49/221 , A61K49/223 , C07K7/08 , C07K7/64 , Y02A50/411
Abstract: The invention provides compositions and methods for therapeutic and diagnostic applications.
Abstract translation: 本发明提供用于治疗和诊断应用的组合物和方法。
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公开(公告)号：US07906102B2
公开(公告)日：2011-03-15
申请号：US11183325
申请日：2005-07-15
Applicant: Dennis E. Hallahan , Shimian Qu , Zhaozhong Han
Inventor： Dennis E. Hallahan , Shimian Qu , Zhaozhong Han
CPC classification number: A61K41/00 , A61K38/03 , A61K38/08 , A61K41/0038 , A61K47/42 , A61K47/48246 , A61K47/48815 , A61K47/64 , A61K47/6911 , A61K49/0002 , A61K49/08 , A61K49/14 , A61K51/08 , A61K51/082 , A61K51/088 , A61K51/1255 , A61N5/10 , C07K2/00 , C07K7/06 , C07K7/08 , C07K16/18 , C07K16/44 , C07K2317/622
Abstract: A method for identifying a molecule that binds an irradiated tumor in a subject and molecules identified thereby. In some embodiments, the method includes the steps of (a) exposing a tumor to ionizing radiation; (b) administering to a subject a library of diverse molecules; and (c) isolating from the tumor one or more molecules of the library of diverse molecules, whereby a molecule that binds an irradiated tumor is identified. Also provided are targeting ligands that bind an irradiated tumor and therapeutic and diagnostic methods that employ the disclosed targeting ligands.
Abstract translation: 用于鉴定结合被照射的肿瘤的分子的方法和由此鉴定的分子。 在一些实施方案中，该方法包括以下步骤：（a）将肿瘤暴露于电离辐射; （b）向受试者施用不同分子的文库; 和（c）从肿瘤中分离不同分子文库的一个或多个分子，从而鉴定结合照射的肿瘤的分子。 还提供了结合照射的肿瘤的靶向配体和使用所公开的靶向配体的治疗和诊断方法。
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公开(公告)号：US20100292172A1
公开(公告)日：2010-11-18
申请号：US12785396
申请日：2010-05-21
Applicant: SOUMITRA S. GHOSH , JOSUE ALFARO-LOPEZ , LAWRENCE J. D'SOUZA , ODILE ESTHER LEVY , QING LIN , CHRISTOPHER J. SOARES
Inventor： SOUMITRA S. GHOSH , JOSUE ALFARO-LOPEZ , LAWRENCE J. D'SOUZA , ODILE ESTHER LEVY , QING LIN , CHRISTOPHER J. SOARES
CPC classification number: A61K47/48246 , A61K47/545 , A61K47/55 , A61K47/64
Abstract: Peptide-peptidase inhibitor conjugate molecules are disclosed. These conjugate molecules are useful as agents for the treatment and prevention of metabolic and cardiovascular diseases, disorders, and conditions. Such diseases, conditions and disorders include, but are not limited to, hypertension, dyslipidemia, cardiovascular disease, eating disorders, insulin-resistance, obesity, and diabetes mellitus of any kind, and other diabetes-related disorders.
Abstract translation: 公开了肽 - 肽酶抑制剂缀合物分子。 这些缀合物分子可用作治疗和预防代谢和心血管疾病，病症和病症的药剂。 这些疾病，病症和障碍包括但不限于高血压，血脂异常，心血管疾病，进食障碍，胰岛素抵抗，肥胖症和任何类型的糖尿病以及其它与糖尿病有关的疾病。
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