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1. 发明授权

US06528487B1 Peptide inhibitors of inflammation mediated by selectins 失效
标题翻译：由选择素介导的炎症肽抑制剂
公开(公告)号：US06528487B1
公开(公告)日：2003-03-04
申请号：US08135319
申请日：1993-10-12
申请人： George A. Heavner , Rodger P. McEver , Jian-Guo Geng
发明人： George A. Heavner , Rodger P. McEver , Jian-Guo Geng
IPC分类号： A61K3808
CPC分类号： C07K14/70564
摘要： Peptides derived from three regions of the lectin domain of GMP-140 and the related selectins, ELAM-1 and the lymphocyte homing receptor, have seen found to inhibit neutrophil adhesion to GMP-140. These and additional peptides have been synthesized, having as their core region portions of the 56-60 amino acid sequence of GMP-140, with residue 1 defined as the N-terminus of the mature protein after the cleavage of the signal peptide. Examples demonstrate the inhibition of the binding of neutrophils to GMP-140 of peptides in concentrations ranging from 5 to 1500 &mgr;mol. It has been found that alterations within the core sequence, as well as N-terminal and C-terminal flanking regions, do not result in loss of biological activity. The peptides are useful as diagnostics and, in combination with a suitable pharmaceutical carrier, for clinical applications in the modulation or inhibition of coagulation processes or inflammatory processes.
摘要翻译：从GMP-140的凝集素结构域和相关选择素，ELAM-1和淋巴细胞归巢受体的三个区域衍生的肽已经发现抑制嗜中性粒细胞粘附到GMP-140。已经合成了这些和额外的肽，其具有作为GMP-140的56-60氨基酸序列的核心区域部分，残基1在信号肽切割后定义为成熟蛋白的N末端。实施例证明了嗜中性粒细胞与浓度范围为5-1500μmolol的肽的GMP-140的结合的抑制。已经发现，核心序列以及N-末端和C-末端侧翼区中的改变不会导致生物活性的丧失。肽可用作诊断，并且与合适的药物载体组合用于调节或抑制凝血过程或炎症过程中的临床应用。

2. 发明授权

US6111065A Peptide inhibitors of inflammation mediated by selectins 失效
标题翻译：由选择素介导的炎症肽抑制剂
公开(公告)号：US6111065A
公开(公告)日：2000-08-29
申请号：US233221
申请日：1994-04-26
申请人： George A. Heavner , Rodger P. McEver , Jian-Guo Geng , Douglas J. Riexinger , Marian Kruszynski , Leon A. Epps , Miljenko Mervic
发明人： George A. Heavner , Rodger P. McEver , Jian-Guo Geng , Douglas J. Riexinger , Marian Kruszynski , Leon A. Epps , Miljenko Mervic
IPC分类号： C07K7/06 , A61K38/00 , C07K7/08 , C07K14/645 , C07K14/705 , C07K14/00 , C07K7/04
CPC分类号： C07K14/70564 , A61K38/00
摘要： Peptides derived from three regions of the lectin domain of GMP-140 (P-selectin) and the related selectins, ELAM-1 (E-selectin) and the lymphocyte homing receptor (L-selectin), have been found to inhibit neutrophil adhesion to GMP-140. These and additional peptides have been synthesized, having as their core region portions of the 74-76 amino acid sequence of GMP-140, with residue 1 defined as the N-terminus of the mature protein after the cleavage of the signal peptide. Examples demonstrate the inhibition of the binding of neutrophils to GMP-140 of peptides in concentrations ranging from 30 to 1500 .mu.mol. It has been found that alterations within the core sequence, as well as N-terminal and C-terminal flanking regions, do not result in loss of biological activity. The peptides are useful as diagnostics and, in combination with a suitable pharmaceutical carrier, for clinical applications in the modulation or inhibition of coagulation processes or inflammatory processes.
摘要翻译：已经发现衍生自GMP-140（P-选择素）的凝集素结构域和相关选择素，ELAM-1（E-选择蛋白）和淋巴细胞归巢受体（L-选择蛋白））的三个区域的肽抑制嗜中性粒细胞粘附 GMP-140。已经合成了这些和额外的肽，其具有作为其核心区域的GMP-140的74-76氨基酸序列的部分，残基1在信号肽切割后定义为成熟蛋白的N末端。实施例证明嗜中性粒细胞与浓度范围为30至1500μmol的肽的GMP-140结合的抑制。已经发现，核心序列以及N-末端和C-末端侧翼区中的改变不会导致生物活性的丧失。肽可用作诊断，并且与合适的药物载体组合用于调节或抑制凝血过程或炎症过程中的临床应用。

3. 发明申请

US20100249032A1 Human EPO Mimetic Hinge Core Mimetibodies, Compositions, Methods and Uses 审中-公开
标题翻译：人类EPO模拟铰链核心模拟物，组合物，方法和用途
公开(公告)号：US20100249032A1
公开(公告)日：2010-09-30
申请号：US12718147
申请日：2010-03-05
申请人： George A. Heavner , David M. Knight , John Ghrayeb , Bernard J. Scallon , Thomas C. Nesspor , Chichi Huang
发明人： George A. Heavner , David M. Knight , John Ghrayeb , Bernard J. Scallon , Thomas C. Nesspor , Chichi Huang
IPC分类号： A61K38/10 , C07H21/04 , C07K7/00 , C07K16/00 , A61K38/08 , A61P19/00 , A61P9/00 , A61P5/00 , A61P3/00 , A61P1/00 , A61P15/00 , A61P17/00 , A61P21/00 , A61P13/00 , A61P25/00 , A61P11/00 , A61P27/16 , A61P31/00 , A61P37/00
CPC分类号： C07K14/505 , Y10S435/972
摘要： The present invention relates to at least one novel human EPO mimetic hinge core mimetibody or specified portion or variant, including isolated nucleic acids that encode at least one EPO mimetic hinge core mimetibody or specified portion or variant, EPO mimetic hinge core mimetibody or specified portion or variants, vectors, host cells, transgenic animals or plants, and methods of making and using thereof, including therapeutic compositions, methods and devices.
摘要翻译：本发明涉及至少一种新的人EPO模拟铰链核心模拟体或特定部分或变体，包括编码至少一个EPO模拟铰链核心模拟体或特定部分或变体的分离的核酸，EPO模拟铰链核心模拟体或特定部分或变体，载体，宿主细胞，转基因动物或植物，以及其制备和使用方法，包括治疗组合物，方法和装置。

4. 发明授权

US5602230A Peptide inhibitors of selectin binding 失效
标题翻译：选择蛋白结合肽抑制剂
公开(公告)号：US5602230A
公开(公告)日：1997-02-11
申请号：US438475
申请日：1995-05-10
申请人： George A. Heavner , Leon Epps , Marian Kruszynski
发明人： George A. Heavner , Leon Epps , Marian Kruszynski
IPC分类号： G01N33/53 , A61K38/00 , A61P29/00 , C07K7/06 , C07K14/705 , A61K38/08
CPC分类号： C07K14/70564 , A61K38/00
摘要： The present invention provides novel peptides derived from portions of the sequence of amino acids 23-26 and 27-30 of P-selectin. The invention also provides pharmaceutical compositions comprising the peptides of the invention, and diagnostic and therapeutic methods utilizing the peptides and pharmaceutical compositions of the invention. The peptides of this invention can be used in the modulation or inhibition of coagulation processes or inflammatory processes.
摘要翻译：本发明提供衍生自P-选择蛋白的氨基酸23-26和27-30的部分序列的新型肽。本发明还提供了包含本发明的肽的药物组合物，以及利用本发明的肽和药物组合物的诊断和治疗方法。本发明的肽可用于调节或抑制凝血过程或炎性过程。

5. 发明授权

US07718176B2 Human EPO mimetic hinge core mimetibodies, compositions, methods and uses 有权
标题翻译：人类EPO模拟铰链核心模拟物，组合物，方法和用途
公开(公告)号：US07718176B2
公开(公告)日：2010-05-18
申请号：US12031849
申请日：2009-03-27
申请人： George A. Heavner , David M. Knight , John Ghrayeb , Bernard J. Scallon , Thomas C. Nesspor , Chichi Huang
发明人： George A. Heavner , David M. Knight , John Ghrayeb , Bernard J. Scallon , Thomas C. Nesspor , Chichi Huang
IPC分类号： A61K39/00 , A61K38/00
CPC分类号： C07K14/505 , Y10S435/972
摘要： The present invention relates to at least one human EPO mimetic hinge core mimetibody or specified portion or variant, including isolated nucleic acids that encode at least one EPO mimetic hinge core mimetibody or specified portion or variant, EPO mimetic hinge core mimetibody or specified portion or variants, vectors, host cells, transgenic animals or plants, and methods of making and using thereof, including therapeutic compositions, methods and devices.
摘要翻译：本发明涉及至少一种人EPO模拟铰链核心模拟体或特定部分或变体，包括编码至少一种EPO模拟铰链核心模拟体或特定部分或变体的分离的核酸，EPO模拟铰链核心模拟体或特定部分或变体载体，宿主细胞，转基因动物或植物，及其制备和使用方法，包括治疗组合物，方法和装置。

6. 发明授权

US07393662B2 Human EPO mimetic hinge core mimetibodies, compositions, methods and uses 有权
标题翻译：人类EPO模拟铰链核心模拟物，组合物，方法和用途
公开(公告)号：US07393662B2
公开(公告)日：2008-07-01
申请号：US10935005
申请日：2004-09-03
申请人： George A. Heavner , David M. Knight , John Ghrayeb , Bernard J. Scallon , Thomas C. Nesspor , Chichi Huang
发明人： George A. Heavner , David M. Knight , John Ghrayeb , Bernard J. Scallon , Thomas C. Nesspor , Chichi Huang
IPC分类号： A61K38/24 , A61K39/00 , A61K38/16 , C07K1/00 , C07K14/00 , C07K16/00 , C07K19/00 , C12P21/00
CPC分类号： C07K14/505 , Y10S435/972
摘要： The present invention relates to at least one novel human EPO mimetic hinge core mimetibody or specified portion or variant, including isolated nucleic acids that encode at least one EPO mimetic hinge core mimetibody or specified portion or variant, EPO mimetic hinge core mimetibody or specified portion or variants, vectors, host cells, transgenic animals or plants, and methods of making and using thereof, including therapeutic compositions, methods and devices.
摘要翻译：本发明涉及至少一种新的人EPO模拟铰链核心模拟体或特定部分或变体，包括编码至少一个EPO模拟铰链核心模拟体或特定部分或变体的分离的核酸，EPO模拟铰链核心模拟体或特定部分或变体，载体，宿主细胞，转基因动物或植物，以及其制备和使用方法，包括治疗组合物，方法和装置。

7. 发明授权

US5753628A Peptide inhibitors of TNF containing predominantly D-amino acids 失效
标题翻译：主要含有D-氨基酸的TNF抑制剂
公开(公告)号：US5753628A
公开(公告)日：1998-05-19
申请号：US482009
申请日：1995-06-07
申请人： George A. Heavner , Marian Kruszynski , David Shealy
发明人： George A. Heavner , Marian Kruszynski , David Shealy
IPC分类号： A61K38/00 , C07K7/06 , C07K5/00 , C07K7/00 , C07K16/00
CPC分类号： C07K7/06 , A61K38/00
摘要： Peptides which consist of six to eight, predominately D-amino acids and which bind to tumor necrosis factor-alpha, prevent tumor necrosis factor-alpha from binding to its receptors and inhibit tumor necrosis factor-alpha activity are disclosed. Methods of inhibiting tumor necrosis factor-alpha activity and of treating individuals suffering from tumor necrosis factor-alpha-mediated diseases and disorders are disclosed.
摘要翻译：公开了由6-8个主要D-氨基酸组成并且与肿瘤坏死因子-α结合的肽，其阻止肿瘤坏死因子-α与其受体结合并抑制肿瘤坏死因子-α活性。公开了抑制肿瘤坏死因子-α活性和治疗患有肿瘤坏死因子-α介导的疾病和病症的个体的方法。

8. 发明授权

US4028401A (Substituted)ureidoacetohydroxamic acids 失效
标题翻译：（取代）脲基乙酰肟酸
公开(公告)号：US4028401A
公开(公告)日：1977-06-07
申请号：US701658
申请日：1976-07-01
申请人： Dyral C. Fessler , George A. Heavner , Thomas H. Massey
发明人： Dyral C. Fessler , George A. Heavner , Thomas H. Massey
IPC分类号： A61K31/195 , A61P9/12 , C07C67/00 , C07C239/00 , C07C275/16 , C07C119/00
CPC分类号： C07C275/16 , Y02P20/55
摘要： A series of (substituted)ureidoacetohydroxamic acids are useful as inhibitors of Angiotensin I converting enzyme.
摘要翻译：一系列（取代）脲基乙酰肟酸可用作血管紧张素I转化酶的抑制剂。

9. 发明授权

US5519000A Tumor necrosis factor inhibitors 失效
公开(公告)号：US5519000A
公开(公告)日：1996-05-21
申请号：US221580
申请日：1994-04-01
申请人： George A. Heavner , Marian Kruszynski , Miljenko Mervic , Robert W. Weber
发明人： George A. Heavner , Marian Kruszynski , Miljenko Mervic , Robert W. Weber
IPC分类号： A61K38/00 , C07K14/715 , C07K7/04 , C07K14/00
CPC分类号： C07K14/7151 , A61K38/00
摘要： Peptides which consist of 4-25 amino acids and which bind to tumor necrosis factor-alpha, prevent tumor necrosis factor-alpha from binding to its receptors and inhibit tumor necrosis factor-alpha activity are disclosed. Methods of inhibiting tumor necrosis factor-alpha activity and of treating individuals suffering from tumor necrosis factor-alpha-mediated diseases and disorders are disclosed.

10. 发明授权

US5506340A Tumor necrosis factor inhibitors 失效
公开(公告)号：US5506340A
公开(公告)日：1996-04-09
申请号：US221581
申请日：1994-04-01
申请人： George A. Heavner
发明人： George A. Heavner
IPC分类号： A61K38/00 , C07K14/715 , C07K5/00 , C07K7/00 , C07K17/00
CPC分类号： C07K14/7151 , A61K38/00
摘要： Peptides which consist of 4-25 amino acids and which bind to tumor necrosis factor-alpha, prevent tumor necrosis factor-alpha from binding to its receptors and inhibit tumor necrosis factor-alpha activity are disclosed. Methods of inhibiting tumor necrosis factor-alpha activity and of treating individuals suffering from tumor necrosis factor-alpha-mediated diseases and disorders are disclosed.

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