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11. 发明申请

WO2009042440A1 1-METHYL NICOTINAMIDE AND DERIVATIVES FOR TREATMENT OF GASTRIC INJURY 审中-公开
标题翻译：用于治疗胃肠损伤的1-甲基尼可苷和衍生物
公开(公告)号：WO2009042440A1
公开(公告)日：2009-04-02
申请号：PCT/US2008/076446
申请日：2008-09-15
申请人： CORTRIA CORPORATION , KRANTZ, Alexander , BRZOZOWSKI, Tomasz
发明人： KRANTZ, Alexander , BRZOZOWSKI, Tomasz
IPC分类号： A01N43/40 , A61K31/44
CPC分类号： A61K31/44
摘要： The present invention is directed to nicotinamide derivatives, and their use in treating gastrointestinal disorders.
摘要翻译：本发明涉及烟酰胺衍生物及其在治疗胃肠道疾病中的用途。

12. 发明申请

WO2007103540A2 COMBINATION THERAPY WITH NON-SELECTIVE COX INHIBITORS TO PREVENT COX-RELATED GASTRIC INJURIES 审中-公开
标题翻译：与非选择性COX抑制剂组合治疗以预防与相关的胃肠道损伤
公开(公告)号：WO2007103540A2
公开(公告)日：2007-09-13
申请号：PCT/US2007/006004
申请日：2007-03-08
申请人： PHARMENA NORTH AMERICA INC. , KRANTZ, Alexander
发明人： KRANTZ, Alexander
IPC分类号： C12Q1/00
CPC分类号： A61K45/06 , A61K31/138 , A61K31/352 , A61K2300/00
摘要： The present invention is directed to nicotinamide, nicotinamide derivatives and prostaglandin mimetics, alone or in combination with an NSAID, and their use in treating pain, inflammation, and/or gastrointestinal toxicty.
摘要翻译：本发明涉及单独或与NSAID组合的烟酰胺，烟酰胺衍生物和前列腺素模拟物，以及它们在治疗疼痛，炎症和/或胃肠道毒性中的用途。

13. 发明申请

WO9924076A9 SALICYLATE DERIVATIZED THERAPEUTIC AND DIAGNOSTIC AGENTS 审中-公开
标题翻译：盐酸衍生的治疗和诊断试剂
公开(公告)号：WO9924076A9
公开(公告)日：2000-06-08
申请号：PCT/US9823706
申请日：1998-11-06
申请人： CONJUCHEM INC , KRANTZ ALEXANDER , SONG YONG HONG , BRIDON DOMINIQUE P , HARDY MARGARET , CHEN QI QI , SETTINERI TINA
发明人： KRANTZ ALEXANDER , SONG YONG HONG , BRIDON DOMINIQUE P , HARDY MARGARET , CHEN QI QI , SETTINERI TINA
IPC分类号： A61K35/16 , A61K38/00 , A61K47/48 , A61K49/00 , A61P7/02 , A61P25/04 , A61P43/00 , C07K7/08 , C07K14/665 , C07K14/75 , C07K14/78
CPC分类号： C07K14/665 , A61K38/00 , A61K47/64 , A61K47/6901
摘要： The present invention relates to novel salicylate compounds which comprise a salicylate moiety and a biologically active agent of interest, where the compound binds and bonds specifically through reaction of the salicylate ester to serum albumin at Lys 199. Albumin is a long-lived moiety present in the blood. Novel salicylate compounds of the present invention provide for long-lived maintenance of the biologically active entity in the host. These compounds find broad applications in prophylactic and therapeutic applications, production of antibodies, reduction of the biologically effective concentration or activity of an endogenous or exogenous blood component, and in other situations where long term administration of a physiologically active compound is of interest.
摘要翻译：本发明涉及包含水杨酸酯部分和感兴趣的生物活性剂的新型水杨酸酯化合物，其中该化合物通过水杨酸酯在Lys 199处与血清白蛋白的反应而特异性地结合和键合。白蛋白是存在于血液。本发明的新型水杨酸酯化合物提供宿主中生物活性实体的长期维持。这些化合物在预防和治疗应用中广泛应用，产生抗体，降低内源或外源性血液成分的生物学有效浓度或活性，以及其他感兴趣的生理活性化合物的长期给药的情况。

14. 发明申请

WO2017139329A1 SITE-SELECTIVE FUNCTIONALIZATION OF PROTEINS USING TRACELESS AFFINITY LABLES 审中-公开
标题翻译：用无痕亲和试剂盒对蛋白质进行选择性功能化
公开(公告)号：WO2017139329A1
公开(公告)日：2017-08-17
申请号：PCT/US2017/016932
申请日：2017-02-08
申请人： KRANTZ, Alexander , WILCZYNSKI, Andrzej
发明人： KRANTZ, Alexander , WILCZYNSKI, Andrzej
IPC分类号： A61K47/66 , A61K47/68 , A61P35/00
CPC分类号： C07K1/13 , A61K31/55 , A61K47/48384 , A61K47/60 , A61K47/62 , A61K47/65 , A61K47/68 , C07K1/062 , C07K1/084 , C07K16/32 , C07K2317/24 , G01N33/532
摘要： The present disclosure relates to site-selective labeling compounds, and methods of using such compounds.
摘要翻译：本发明涉及位点选择标记化合物和使用这些化合物的方法。

15. 发明申请

WO2013170272A3 SITE-SPECIFIC LABELING AND TARGETED DELIVERY OF PROTEINS FOR THE TREATMENT OF CANCER 审中-公开
标题翻译：用于治疗癌症的特定标签和靶向递送蛋白质
公开(公告)号：WO2013170272A3
公开(公告)日：2014-02-27
申请号：PCT/US2013040823
申请日：2013-05-13
申请人： KRANTZ ALEXANDER
发明人： KRANTZ ALEXANDER
IPC分类号： C12P21/00 , C07K1/10 , C07K2/00
CPC分类号： A61K47/48246 , A61K38/17 , A61K38/38 , A61K38/40 , A61K45/06 , A61K47/64 , C07K14/435
摘要： The present invention relates to the formation of protein conjugates from proteins chemically modified for linkage to (1) anticancer drug pharmacophores, (2) ligands to biomarkers on cancer cell surfaces, (3) and/or another protein molecule. It provides and specifies new compositions, methods and combinations for tumor, and tumor vasculature targeting and cancer treatment.
摘要翻译：本发明涉及从化学修饰用于连接到（1）抗癌药物载体的蛋白质的蛋白质的形成，（2）癌细胞表面上生物标志物的配体，（3）和/或另一种蛋白质分子。它提供并指定肿瘤的新组合物，方法和组合以及肿瘤血管系统靶向和癌症治疗。

16. 发明申请

WO2013170272A2 SITE-SPECIFIC LABELING AND TARGETED DELIVERY OF PROTEINS FOR THE TREATMENT OF CANCER 审中-公开
标题翻译：用于治疗癌症的特定标签和靶向递送蛋白质
公开(公告)号：WO2013170272A2
公开(公告)日：2013-11-14
申请号：PCT/US2013/040823
申请日：2013-05-13
申请人： KRANTZ, Alexander
发明人： KRANTZ, Alexander
IPC分类号： A61K38/17
CPC分类号： A61K47/48246 , A61K38/17 , A61K38/38 , A61K38/40 , A61K45/06 , A61K47/64 , C07K14/435
摘要： The present invention relates to the formation of protein conjugates from proteins chemically modified for linkage to (1) anticancer drug pharmacophores, (2) ligands to biomarkers on cancer cell surfaces, (3) and/or another protein molecule. It provides and specifies new compositions, methods and combinations for tumor, and tumor vasculature targeting and cancer treatment.
摘要翻译：本发明涉及从化学修饰用于连接到（1）抗癌药物载体的蛋白质的蛋白质的形成，（2）癌细胞表面上生物标志物的配体，（3）和/或另一种蛋白质分子。它提供并指定肿瘤的新组合物，方法和组合以及肿瘤血管系统靶向和癌症治疗。

17. 发明申请

WO2011103409A1 SITE-SPECIFIC MODIFICATION OF PROTEINS THROUGH CHEMICAL MODIFICATION ENABLING PROTEIN CONJUGATES, PROTEIN DIMER FORMATION, AND STAPLED PEPTIDES 审中-公开
标题翻译：通过化学修饰使蛋白质的蛋白质特异性修饰使蛋白质结合蛋白，蛋白质二聚体形成和嵌段蛋白
公开(公告)号：WO2011103409A1
公开(公告)日：2011-08-25
申请号：PCT/US2011/025413
申请日：2011-02-18
申请人： ADVANCED PROTEOME THERAPEUTICS INC. , KRANTZ, Alexander , YU, Peng
发明人： KRANTZ, Alexander , YU, Peng
IPC分类号： A01N57/00
CPC分类号： A61K47/481 , A61K47/55
摘要： The present invention generally provides methods for the site-specific modification of peptides, polypeptides, and proteins, e.g., granulocyte macrophage colony-stimulating factor, human superoxide dismutase, annexin, leptin, antibodies and the like, cytokines and chemokines, at their N-termini and at sites at which unnatural aminoacids have been introduced along the protein framework. The modifications described herein can be used for the synthesis and application of the adducts in radio-labeling, molecular imaging and protein therapeutic applications, and the treatment of disorders such as rheumatoid arthritis, lupus erythematosus, psoriasis, multiple sclerosis, type-1 diabetes, Crohn's disease, and systemic sclerosis, Alzheimer disease, cancer, liver disease (e.g., alcoholic liver disease), and cachexia.
摘要翻译：本发明通常提供肽，多肽和蛋白质的位点特异性修饰的方法，例如粒细胞巨噬细胞集落刺激因子，人超氧化物歧化酶，膜联蛋白，瘦素，抗体等，细胞因子和趋化因子，并且沿着蛋白质框架引入非天然氨基酸的位点。本文所述的修饰可以用于加合物在放射性标记，分子成像和蛋白质治疗应用中的合成和应用，以及治疗疾病如类风湿性关节炎，红斑狼疮，牛皮癣，多发性硬化，1型糖尿病，克罗恩病和系统性硬化症，阿尔茨海默病，癌症，肝病（如酒精性肝病）和恶病质。

18. 发明申请

WO2007103540A3 COMBINATION THERAPY WITH NON-SELECTIVE COX INHIBITORS TO PREVENT COX-RELATED GASTRIC INJURIES 审中-公开
标题翻译：与非选择性COX抑制剂联合治疗以预防与相关的胃肠道损伤
公开(公告)号：WO2007103540A3
公开(公告)日：2008-12-18
申请号：PCT/US2007006004
申请日：2007-03-08
申请人： PHARMENA NORTH AMERICA INC , KRANTZ ALEXANDER
发明人： KRANTZ ALEXANDER
IPC分类号： A01N37/08 , A01N53/00 , A61K31/19
CPC分类号： A61K45/06 , A61K31/138 , A61K31/352 , A61K2300/00
摘要： The present invention is directed to nicotinamide, nicotinamide derivatives and prostaglandin mimetics, alone or in combination with an NSAID, and their use in treating pain, inflammation, and/or gastrointestinal toxicty.
摘要翻译：本发明涉及单独或与NSAID组合的烟酰胺，烟酰胺衍生物和前列腺素模拟物，以及它们在治疗疼痛，炎症和/或胃肠道毒性中的用途。

19. 发明申请

WO2004066917A3 TANDEM ANALYSES OF NONCOVALENTLY DRIVEN EFFECTORS FOR MODULATORY MAPPING OF ACTIVITIES OF PROTEIN SITES 审中-公开
标题翻译：用于调节蛋白质活性活性的非特异性驱动效应的分析仪
公开(公告)号：WO2004066917A3
公开(公告)日：2005-08-11
申请号：PCT/US2004001038
申请日：2004-01-16
申请人： ADVANCED PROTEOME THERAPEUTICS , KRANTZ ALEXANDER
发明人： KRANTZ ALEXANDER
IPC分类号： A61K20060101 , C07K14/52 , C07K14/575 , C07K14/705 , C07K16/00 , C07K16/46 , C12Q1/00 , G01N33/58 , G01N33/68
CPC分类号： G01N33/6845 , C07K14/52 , C07K16/00 , C12Q1/00 , G01N33/58 , G01N33/6842 , G01N2500/00
摘要： The present invention provides methods of discovering and mapping secondary binding sites on biological molecules (e.g., proteins), the effects, if any, of site occupancy on the primary function of the molecule, and the screening of small molecules against the secondary binding sites. The invention further provides novel complexes for modification of secondary binding sites and the resulting modified biological molecules.
摘要翻译：本发明提供发现和映射生物分子（例如蛋白质）上的二级结合位点，对分子的主要功能的位置占据的影响（如果有的话）以及针对二级结合位点筛选小分子的方法。本发明还提供用于修饰二级结合位点和所得修饰的生物分子的新型复合物。

20. 发明申请

WO1998011437A1 AFFINITY LABELING LIBRARIES WITH TAGGED LEAVING GROUPS 审中-公开
标题翻译：具有标签的组织的标志性标签图书馆
公开(公告)号：WO1998011437A1
公开(公告)日：1998-03-19
申请号：PCT/US1997016435
申请日：1997-09-16
申请人： REDCELL CANADA, INC. , KRANTZ, Alexander
发明人： REDCELL CANADA, INC. , HANEL, Arthur, M. , HUANG, Wolin
IPC分类号： G01N33/53
CPC分类号： C40B30/04 , B01J2219/00592 , G01N33/6845
摘要： Methods and compositions are provided for identifying compounds having affinity to a target site. The method provides for the affinity group to be a leaving group from a reactive functionality capable of forming a covalent bond to the target site. One can combine the compound comprising the target site with the library, and assay for the resulting composition of the leaving groups. The leaving groups having the highest concentration can be identified as the groups having the binding highest affinity for the target site. The selected compounds may then be used for labeling the target molecule, particularly where the target molecule is naturally found in a complex mixture, such as a physiological fluid, like blood. By affinity labeling in vivo, the lifetime of physiologically active entities can be greatly enhanced by becoming bound to long lived blood components. The covalently bound entity may also serve as an antagonist or agonist of a particular binding protein or as an enzyme inhibitor.
摘要翻译：提供方法和组合物用于鉴定对靶位点具有亲和性的化合物。该方法提供了亲和基团为能够与靶位点形成共价键的反应性官能团的离去基团。可以将包含靶位点的化合物与文库结合，并测定所得离去基团的组成。具有最高浓度的离去基团可以被鉴定为对靶位点具有最高亲和力的结合基团。然后可以将所选择的化合物用于标记靶分子，特别是当目标分子天然存在于复杂混合物如生理液体如血液中时。通过体内的亲和标记，通过与长寿命血液成分结合，可以大大提高生理活性物质的寿命。共价结合的实体也可以用作特异性结合蛋白的拮抗剂或激动剂或作为酶抑制剂。

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