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21. 发明申请

US20110263659A1 Analogs of 1-Methylnicotinamide 审中-公开
标题翻译： 1-甲基烟酰胺的类似物
公开(公告)号：US20110263659A1
公开(公告)日：2011-10-27
申请号：US12991056
申请日：2009-05-05
申请人： Alexander Krantz
发明人： Alexander Krantz
IPC分类号： A61K31/4406 , A61P9/00 , A61P3/10 , A61P35/00 , A61P19/10 , A61P3/04 , A61P17/00 , A61P9/10 , A61P9/04 , A61P25/28 , A61P9/12 , A61P11/16 , A61P15/10 , A61P1/00 , C07D213/56
CPC分类号： A61K31/44 , A61K31/4425 , A61K31/535
摘要： The present invention is directed to derivatives and analogs of 1-methyl-nicotinamide useful for elevating the blood levels of 1-methylnicotinamide or deuterated species in a subject.
摘要翻译：本发明涉及用于提高受试者中1-甲基烟酰胺或氘化物质的血液水平的1-甲基 - 烟酰胺的衍生物和类似物。

22. 发明授权

US07927579B2 Tandem analyses of noncovalently driven effectors for modulatory mapping of activities of protein sites 有权
标题翻译：用于非蛋白质驱动效应物的串联分析用于蛋白质位点活性的调节作图
公开(公告)号：US07927579B2
公开(公告)日：2011-04-19
申请号：US10759513
申请日：2004-01-16
申请人： Alexander Krantz
发明人： Alexander Krantz
IPC分类号： A61K51/00
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。

23. 发明授权

US6013792A Matrix metalloprotease inhibitors 失效
标题翻译：基质金属蛋白酶抑制剂
公开(公告)号：US6013792A
公开(公告)日：2000-01-11
申请号：US382818
申请日：1995-02-03
申请人： Arlindo Lucas Castelhano , Teng Jiam Liak , Stephen Horne , Alexander Krantz , Zhengyu Yuan
发明人： Arlindo Lucas Castelhano , Teng Jiam Liak , Stephen Horne , Alexander Krantz , Zhengyu Yuan
IPC分类号： A61K31/40 , A61K31/437 , A61K31/66 , A61P1/02 , A61P3/14 , A61P19/10 , A61P29/00 , A61P35/00 , A61P43/00 , C07D487/04 , C07D487/08 , C07D498/08 , C07F9/30 , C07F9/645 , C07F9/6561 , C07D245/00
CPC分类号： C07D487/04 , C07D487/08 , C07F9/6561
摘要： Compounds of formula (I): ##STR1## as single stereoisomers or mixtures thereof and their pharmaceutically acceptable salts inhibit matrix metalloproteases, such as interstitial collagenases, and are useful in the treatment of mammals having disease states alleviated by the inhibition of such matrix metalloproteases, for example arthritic diseases or bone resorption disease, such as osteoporosis.
摘要翻译：式（I）化合物：作为单一立体异构体或其混合物及其药学上可接受的盐抑制基质金属蛋白酶，例如间质胶原酶，并且可用于治疗具有通过抑制此类基质金属蛋白酶（例如关节炎）减轻的疾病状态的哺乳动物疾病或骨吸收疾病，如骨质疏松症。

24. 发明授权

US5942620A Methods for producing novel conjugates of thrombin inhibitors 失效
标题翻译：生产凝血酶抑制剂新型缀合物的方法
公开(公告)号：US5942620A
公开(公告)日：1999-08-24
申请号：US108534
申请日：1998-07-01
申请人： Alexander Krantz , Alan M. Ezrin , Yonghong Song
发明人： Alexander Krantz , Alan M. Ezrin , Yonghong Song
IPC分类号： C12N5/06 , A61K38/00 , A61K47/48 , A61P7/02 , C07K5/068 , C07K14/765 , C07K16/18 , C07D215/02
CPC分类号： A61K47/48007 , A61K47/48238 , A61K47/48384
摘要： Novel compounds comprising chemically reactive intermediates which can react with available reactive functionalities on blood components to form covalent linkages, where the resulting covalently-bound conjugates are found to have thrombin inhibition activity are provided. Specifically, the thrombin inhibitor compounds of the present invention are derivatives of the known thrombin inhibitor argatroban, which can be covalently linked to chemically reactive functionalities on various blood components. The conjugated thrombin inhibitors thereby have extended lifetimes in the bloodstream, as compared to the unconjugated parent drug, and are, therefore, capable of maintaining thrombin inhibitory activity for extended periods of time as compared to the unconjugated parent drug. Also provided herein are methods for inhibiting thrombin activity in vivo comprising administering to the bloodstream of a mammalian host the novel compounds of the present invention.
摘要翻译：提供了包含化学反应中间体的新型化合物，其可与血液成分上的可用反应性官能团反应以形成共价键，其中发现所得的共价结合的缀合物具有凝血酶抑制活性。具体地，本发明的凝血酶抑制剂化合物是已知的凝血酶抑制剂阿加曲班的衍生物，其可以与各种血液成分上的化学反应性官能团共价连接。与未缀合的母体药物相比，缀合的凝血酶抑制剂在血液中的寿命延长，因此与未缀合的母体药物相比，能够延长凝血酶抑制活性。本文还提供用于抑制体内凝血酶活性的方法，包括向哺乳动物宿主的血流施用本发明的新化合物。

25. 发明授权

US5773428A Matrix metalloprotease inhibitors 失效
标题翻译：基质金属蛋白酶抑制剂
公开(公告)号：US5773428A
公开(公告)日：1998-06-30
申请号：US597062
申请日：1996-02-05
申请人： Arlindo Lucas Castelhano , Teng Jiam Liak , Stephen Horne , Alexander Krantz , Zhengyu Yuan , Jian Jeffrey Chen , Paul David Cannon , Hal Van Wart
发明人： Arlindo Lucas Castelhano , Teng Jiam Liak , Stephen Horne , Alexander Krantz , Zhengyu Yuan , Jian Jeffrey Chen , Paul David Cannon , Hal Van Wart
IPC分类号： C07D487/04 , C07D487/08 , C07D498/08 , C07F9/6561 , A61K31/395
CPC分类号： C07D487/04 , C07D487/08 , C07F9/6561
摘要： Compounds of formula (I): ##STR1## as single stereoisomers or mixtures thereof and their pharmaceutically acceptable salts inhibit matrix metalloproteases, such as interstitial collagenases, and are useful in the treatment of mammals having disease states alleviated by the inhibition of such matrix metalloproteases, for example arthritic diseases or bone resorption diseases, such as osteoporosis.
摘要翻译：式（I）的化合物：作为单一立体异构体或其混合物的式（I）化合物及其药学上可接受的盐抑制基质金属蛋白酶，例如间质胶原酶，并且可用于治疗具有通过抑制这种作用而减轻的疾病状态的哺乳动物基质金属蛋白酶，例如关节炎疾病或骨吸收疾病，如骨质疏松症。

26. 发明申请

US20200095275A1 SITE-SELECTIVE FUNCTIONALIZATION OF PROTEINS USING TRACELESS AFFINITY LABELS 审中-公开
公开(公告)号：US20200095275A1
公开(公告)日：2020-03-26
申请号：US16403971
申请日：2019-05-06
申请人： Alexander Krantz , Andrzej Wilczynski
发明人： Alexander Krantz , Andrzej Wilczynski
IPC分类号： C07K1/13 , A61K47/65 , A61K47/60 , A61K47/62 , A61K31/55 , C07K1/06 , C07K1/08 , C07K16/32 , G01N33/532 , A61K47/68
摘要： The present disclosure relates to site-selective labeling compounds, and methods of using such compounds.

27. 发明授权

US08927485B2 Site-specific modification of proteins through chemical modification enabling protein conjugates, protein dimer formation, and stapled peptides 有权
标题翻译：通过化学修饰实现蛋白质的位点特异性修饰，使蛋白质缀合物，蛋白质二聚体形成和装订肽
公开(公告)号：US08927485B2
公开(公告)日：2015-01-06
申请号：US13030772
申请日：2011-02-18
申请人： Alexander Krantz , Peng Yu
发明人： Alexander Krantz , Peng Yu
IPC分类号： A61K38/00 , C07K16/00 , C07K17/00 , C07K17/14 , C12P21/08 , A61K38/24 , A61K38/27 , C07K1/00 , C07K14/00 , A61K47/48
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。

28. 发明申请

US20110263832A1 SITE-SPECIFIC MODIFICATION OF PROTEINS THROUGH CHEMICAL MODIFICATION ENABLING PROTEIN CONJUGATES, PROTEIN DIMER FORMATION, AND STAPLED PEPTIDES 有权
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：US20110263832A1
公开(公告)日：2011-10-27
申请号：US13030772
申请日：2011-02-18
申请人： Alexander Krantz , Peng Yu
发明人： Alexander Krantz , Peng Yu
IPC分类号： C07K16/46 , C07K14/575
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。

29. 发明申请

US20090118225A1 1-Methyl Nicotinamide and Derivatives for Treatment of Gastric Injury 审中-公开
公开(公告)号：US20090118225A1
公开(公告)日：2009-05-07
申请号：US12210952
申请日：2008-09-15
申请人： Alexander Krantz , Tomasz Brzozowski
发明人： Alexander Krantz , Tomasz Brzozowski
IPC分类号： A61K31/737 , A61K31/455 , A61K31/727 , A61P1/04
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。

30. 发明申请

US20070259861A1 Combination therapy with non-selective COX inhibitors to prevent COX-related gastric injuries 审中-公开
标题翻译：联合治疗与非选择性COX抑制剂预防COX相关的胃损伤
公开(公告)号：US20070259861A1
公开(公告)日：2007-11-08
申请号：US11715660
申请日：2007-03-08
申请人： Alexander Krantz
发明人： Alexander Krantz
IPC分类号： A61K31/4439 , A61K31/19 , A61K31/192 , A61K31/196 , A61P29/00 , A61K31/5415 , A61K31/235 , A61K31/40
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，

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