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1. 发明授权

US08008453B2 Modified Fc molecules 有权
标题翻译：修饰的Fc分子
公开(公告)号：US08008453B2
公开(公告)日：2011-08-30
申请号：US11502761
申请日：2006-08-10
申请人： Colin V. Gegg , Kenneth W. Walker , Leslie P. Miranda , Fei Xiong
发明人： Colin V. Gegg , Kenneth W. Walker , Leslie P. Miranda , Fei Xiong
IPC分类号： C07K16/00 , A61K38/00
CPC分类号： A61K47/48369 , A61K38/02 , A61K47/60 , A61K47/68 , A61K47/6817 , C07K16/00 , C07K17/00 , C07K2317/40 , C07K2317/52
摘要： Disclosed is a process for preparing a pharmacologically active compound, in which at least one internal conjugation site of an Fc domain sequence is selected that is amenable to conjugation of an additional functional moiety by a defined conjugation chemistry through the side chain of an amino acid residue at the conjugation site. An appropriate amino acid residue for conjugation may be present in a native Fc domain at the conjugation site or may be added by insertion (i.e., between amino acids in the native Fc domain) or by replacement (i.e., removing amino acids and substituting different amino acids). In the latter case, the number of amino acids added need not correspond to the number of amino acids removed from the previously existing Fc domain. This technology may be used to produce useful compositions of matter and pharmaceutical compositions containing them. A DNA encoding the inventive composition of matter, an expression vector containing the DNA, and a host cell containing the expression vector are also disclosed.
摘要翻译：公开了制备药理活性化合物的方法，其中选择Fc结构域序列的至少一个内部缀合位点，其适于通过定义的缀合化学通过氨基酸残基的侧链与另外的功能部分缀合在共轭位点。用于缀合的合适的氨基酸残基可以在缀合位点处的天然Fc结构域中存在，或者可以通过插入（即天然Fc结构域中的氨基酸之间）或替换（即，除去氨基酸并用不同的氨基酸）。在后一种情况下，加入的氨基酸数不需要对应于从先前存在的Fc结构域去除的氨基酸的数目。该技术可用于生产含有它们的物质和药物组合物的有用组合物。还公开了编码本发明组合物的DNA，含有该DNA的表达载体和含有表达载体的宿主细胞。

2. 发明申请

US20110195895A1 FGF21 MUTANTS AND USES THEREOF 有权
标题翻译： FGF21突变体及其用途
公开(公告)号：US20110195895A1
公开(公告)日：2011-08-11
申请号：US13123205
申请日：2009-10-08
申请人： Kenneth W. Walker , Colin V. Gegg, JR. , Randy I. Hecht , Edward J. Belousky , Yue-Sheng Li , Mark L. Michaels , Jing Xu , Murielle M. Ellison
发明人： Kenneth W. Walker , Colin V. Gegg, JR. , Randy I. Hecht , Edward J. Belousky , Yue-Sheng Li , Mark L. Michaels , Jing Xu , Murielle M. Ellison
IPC分类号： A61K38/18 , C12N15/63 , C12N1/00 , C07H21/00 , C12P21/02 , C07K14/50 , C08F8/32 , C07K19/00 , A61P3/10 , A61P3/04 , A61P3/00
CPC分类号： C07K14/50 , A61K38/00 , A61K47/60
摘要： The invention provides nucleic acid molecules encoding FGF21 mutant polypeptides, FGF21 mutant polypeptides, pharmaceutical compositions comprising FGF21 mutant polypeptides, and methods for treating metabolic disorders using such nucleic acids, polypeptides, or pharmaceutical compositions.
摘要翻译：本发明提供编码FGF21突变体多肽，FGF21突变体多肽，包含FGF21突变体多肽的药物组合物的核酸分子，以及使用此类核酸，多肽或药物组合物治疗代谢紊乱的方法。

3. 发明授权

US07833979B2 Toxin peptide therapeutic agents 有权
标题翻译：毒素肽治疗剂
公开(公告)号：US07833979B2
公开(公告)日：2010-11-16
申请号：US11406454
申请日：2006-04-17
申请人： John K. Sullivan , Joseph G. McGivern , Leslie P. Miranda , Hung Q. Nguyen , Kenneth W. Walker , Shaw-Fen Sylvia Hu , Colin V. Gegg , Stefan I. McDonough
发明人： John K. Sullivan , Joseph G. McGivern , Leslie P. Miranda , Hung Q. Nguyen , Kenneth W. Walker , Shaw-Fen Sylvia Hu , Colin V. Gegg , Stefan I. McDonough
IPC分类号： A61K38/00 , C07K14/00
CPC分类号： A61K47/48215 , A61K38/00 , A61K47/60 , C07K14/43504 , C07K2319/30 , C07K2319/55
摘要： Disclosed is a composition of matter of the formula (X1)a—(F1)d—(X2)b—(F2)e—(X3)c (I) and multimers thereof, in which F1 and F2 are half-life extending moieties, and d and e are each independently 0 or 1, provided that at least one of d and e is 1; X1, X2, and X3 are each independently -(L)f-P-(L)g-, and f and g are each independently 0 or 1; P is a toxin peptide of no more than about 80 amino acid residues in length, comprising at least two intrapeptide disulfide bonds; L is an optional linker; and a, b, and c are each independently 0 or 1, provided that at least one of a, b and c is 1. Linkage to the half-life extending moiety or moieties increases the in vivo half-life of the toxin peptide, which otherwise would be quickly degraded. A pharmaceutical composition comprises the composition and a pharmaceutically acceptable carrier. Also disclosed are a DNA encoding the inventive composition of matter, an expression vector comprising the DNA, and a host cell comprising the expression vector. Methods of treating an autoimmune disorder, such as, but not limited to, multiple sclerosis, type 1 diabetes, psoriasis, inflammatory bowel disease, contact-mediated dermatitis, rheumatoid arthritis, psoriatic arthritis, asthma, allergy, restinosis, systemic sclerosis, fibrosis, scleroderma, glomerulonephritis, Sjogren syndrome, inflammatory bone resorption, transplant rejection, graft-versus-host disease, and lupus and of preventing or mitigating a relapse of a symptom of multiple sclerosis are also disclosed.
摘要翻译：公开了式（X1）a-（F1）d-（X2）b-（F2）e-（X3）c（Ⅰ）及其多元素的物质组成，其中F1和F2是半衰期延长部分，d和e各自独立地为0或1，条件是d和e中的至少一个为1; X1，X2和X3各自独立地为 - （L）f-P-（L）g-，f和g各自独立地为0或1; P是长度不超过约80个氨基酸残基的毒素肽，其包含至少两个肽内二硫键; L是可选的接头; 并且a，b和c各自独立地为0或1，条件是a，b和c中的至少一个为1.与半衰期延长部分或部分的连接增加毒素肽的体内半衰期，否则会很快退化。药物组合物包含该组合物和药学上可接受的载体。还公开了编码本发明组合物的DNA，包含DNA的表达载体和包含表达载体的宿主细胞。治疗自身免疫性疾病，例如但不限于多发性硬化，1型糖尿病，牛皮癣，炎性肠病，接触介导性皮炎，类风湿性关节炎，银屑病关节炎，哮喘，过敏，再狭窄，系统性硬化，纤维化，还公开了硬皮病，肾小球肾炎，干燥综合征，炎性骨吸收，移植排斥反应，移植物抗宿主病和狼疮以及预防或减轻多发性硬化症状的复发。

4. 发明申请

US20090299044A1 DNA encoding chimeric toxin peptide fusion proteins and vectors and mammalian cells for recombinant expression 失效
标题翻译：编码嵌合毒素肽融合蛋白的DNA和用于重组表达的载体和哺乳动物细胞
公开(公告)号：US20090299044A1
公开(公告)日：2009-12-03
申请号：US11978104
申请日：2007-10-25
申请人： John K. Sullivan , Joseph G. McGivern , Leslie P. Miranda , Hung Q. Nguyen , Kenneth W. Walker , Shaw-Fen Sylvia Hu , Colin V. Gegg, JR. , Taruna Arora Khare , Beverly S. Adler , Francis H. Martin
发明人： John K. Sullivan , Joseph G. McGivern , Leslie P. Miranda , Hung Q. Nguyen , Kenneth W. Walker , Shaw-Fen Sylvia Hu , Colin V. Gegg, JR. , Taruna Arora Khare , Beverly S. Adler , Francis H. Martin
IPC分类号： C07H21/04
CPC分类号： C07K14/43522 , A61K38/00 , A61K47/60 , C07K2319/30 , C07K2319/31
摘要： Disclosed is a composition of matter comprising an OSK1 peptide analog, and in some embodiments, a pharmaceutically acceptable salt thereof. A pharmaceutical composition comprises the composition and a pharmaceutically acceptable carrier. Also disclosed are DNAs encoding the inventive composition of matter, an expression vector comprising the DNA, and host cells comprising the expression vector. Methods of treating an autoimmune disorder and of preventing or mitigating a relapse of a symptom of multiple sclerosis are also disclosed.
摘要翻译：公开了包含OSK1肽类似物的物质组合物，并且在一些实施方案中为其药学上可接受的盐。药物组合物包含该组合物和药学上可接受的载体。还公开了编码本发明组合物的DNA，包含DNA的表达载体和包含表达载体的宿主细胞。还公开了治疗自身免疫性疾病和预防或减轻多发性硬化症状的复发的方法。

5. 发明申请

US20090297520A1 Methods of using conjugated toxin peptide therapeutic agents 失效
标题翻译：使用缀合毒素肽治疗剂的方法
公开(公告)号：US20090297520A1
公开(公告)日：2009-12-03
申请号：US11978111
申请日：2007-10-25
申请人： John K. Sullivan , Joseph G. McGivern , Leslie P. Miranda , Hung Q. Nguyen , Kenneth W. Walker , Shaw-Fen Sylvia Hu , Colin V. Gegg, JR. , Taruna Arora Khare , Beverly S. Adler , Francis H. Martin
发明人： John K. Sullivan , Joseph G. McGivern , Leslie P. Miranda , Hung Q. Nguyen , Kenneth W. Walker , Shaw-Fen Sylvia Hu , Colin V. Gegg, JR. , Taruna Arora Khare , Beverly S. Adler , Francis H. Martin
IPC分类号： A61K39/395 , A61K38/16
CPC分类号： C07K14/43522 , A61K38/00 , A61K47/60 , C07K2319/30 , C07K2319/31
摘要： Disclosed is a composition of matter comprising an OSK1 peptide analog, and in some embodiments, a pharmaceutically acceptable salt thereof. A pharmaceutical composition comprises the composition and a pharmaceutically acceptable carrier. Also disclosed are DNAs encoding the inventive composition of matter, an expression vector comprising the DNA, and host cells comprising the expression vector. Methods of treating an autoimmune disorder and of preventing or mitigating a relapse of a symptom of multiple sclerosis are also disclosed.
摘要翻译：公开了包含OSK1肽类似物的物质组合物，并且在一些实施方案中为其药学上可接受的盐。药物组合物包含该组合物和药学上可接受的载体。还公开了编码本发明组合物的DNA，包含DNA的表达载体和包含表达载体的宿主细胞。还公开了治疗自身免疫性疾病和预防或减轻多发性硬化症状的复发的方法。

6. 发明授权

US09102731B2 Human CGRP receptor binding proteins 有权
标题翻译：人CGRP受体结合蛋白
公开(公告)号：US09102731B2
公开(公告)日：2015-08-11
申请号：US12642711
申请日：2009-12-18
申请人： Thomas C. Boone , David W. Brankow , Colin V. Gegg, Jr. , Shaw-Fen Sylvia Hu , Chadwick T. King , Hsieng Sen Lu , Licheng Shi , Cen Xu
发明人： Thomas C. Boone , David W. Brankow , Colin V. Gegg, Jr. , Shaw-Fen Sylvia Hu , Chadwick T. King , Hsieng Sen Lu , Licheng Shi , Cen Xu
IPC分类号： C07K16/00 , C12P21/08 , C07K16/28
CPC分类号： C07K16/2869 , A61K39/395 , A61K39/39533 , A61K2039/505 , C07K2317/21 , C07K2317/32 , C07K2317/56 , C07K2317/565 , C07K2317/76 , C07K2317/92 , C07K2319/30
摘要： Antigen binding proteins that bind to human CGRP receptor (CGRP R) are provided. Nucleic acids encoding the antigen binding protein, vectors, and cells encoding the same are also provided. The antigen binding proteins can inhibit binding of CGRP R to CGRP, and are useful in a number of CGRP R related disorders, including the treatment and/or prevention of migraine headaches.
摘要翻译：提供了结合人CGRP受体（CGRP R）的抗原结合蛋白。还提供编码抗原结合蛋白，载体和编码抗原结合蛋白的核酸的核酸。抗原结合蛋白可以抑制CGRP R与CGRP的结合，并且可用于多种CGRP R相关疾病，包括治疗和/或预防偏头痛。

7. 发明授权

US08420779B2 Compositions and methods for producing bioactive fusion proteins 失效
公开(公告)号：US08420779B2
公开(公告)日：2013-04-16
申请号：US12154507
申请日：2008-05-22
申请人： Kenneth W. Walker , Colin V. Gegg, Jr.
发明人： Kenneth W. Walker , Colin V. Gegg, Jr.
IPC分类号： A61K38/16 , C07K14/00 , C07K17/00 , C07K19/00 , C07H21/04 , C12N15/63 , C12N5/10 , C12N1/21 , C12N15/09
CPC分类号： C07K14/78 , A61K47/60 , C07K14/43504 , C07K14/43522 , C07K14/524 , C07K16/18 , C07K2319/00 , C07K2319/30 , C07K2319/31 , C07K2319/35
摘要： Disclosed is a composition of matter involving a recombinant fusion protein comprising a a pharmacologically active protein partner, and a small pharmacologically inactive protein domain partner of human origin, such as but not limited to, a 10th fibronectin III domain, a SH3 domain, a SH2 domain, a CH2 domain of IgG1, a PDZ domain, a thrombospondin repeat domain, an ubiquitin domain, a leucine-rich repeat domain, a villin headpiece HP35 domain, a villin headpiece HP76 domain, or a fragment or modification of any of these. Also disclosed are nucleic acids (e.g., DNA constructs) encoding the fusion protein, expression vectors and recombinant host cells for expression of the fusion protein, and pharmaceutical compositions containing the recombinant fusion protein and a pharmaceutically acceptable carrier, and method of producing a pharmacologically active recombinant fusion protein.

8. 发明授权

US08288351B2 Antagonists of the bradykinin B1 receptor 失效
标题翻译：缓激肽B1受体的拮抗剂
公开(公告)号：US08288351B2
公开(公告)日：2012-10-16
申请号：US12082224
申请日：2008-04-08
申请人： Gordon Ng , Yue-Sheng Li , Colin V. Gegg , Benny C. Askew, Jr. , Thomas Storz , Yuelie Lu , Derin C. D'Amico , Mark A. Jarosinski , Chuan-Fa Liu , Qi Huang
发明人： Gordon Ng , Yue-Sheng Li , Colin V. Gegg , Benny C. Askew, Jr. , Thomas Storz , Yuelie Lu , Derin C. D'Amico , Mark A. Jarosinski , Chuan-Fa Liu , Qi Huang
IPC分类号： C07K7/18
CPC分类号： A61K38/08 , A61K38/10 , C07K7/06 , C07K7/08 , C07K7/18
摘要： The present invention relates to composition of matter involving bradykinin B1 receptor antagonist peptides conjugated to a univalent vehicle, including peptides conjugated to univalent PEG. These compositions can be used as therapeutics or prophylactics against diseases or conditions, such as inflammation or pain, linked to the bradykinin B1 receptor.
摘要翻译：本发明涉及与单价载体缀合的缓激肽B1受体拮抗剂肽的物质组合物，包括与一价PEG缀合的肽。这些组合物可用作与缓激肽B1受体连接的疾病或病症例如炎症或疼痛的治疗剂或预防剂。

9. 发明申请

US20110045587A1 TOXIN PEPTIDE THERAPEUTIC AGENTS 有权
标题翻译：毒素代谢治疗药物
公开(公告)号：US20110045587A1
公开(公告)日：2011-02-24
申请号：US12938294
申请日：2010-11-02
申请人： JOHN K. SULLIVAN , JOSEPH G. MCGIVERN , LESLIE P. MIRANDA , HUNG Q. NGUYEN , KENNETH W. WALKER , SHAW-FEN SYLVIA HU , COLIN V. GEGG , STEFAN I. MCDONOUGH
发明人： JOHN K. SULLIVAN , JOSEPH G. MCGIVERN , LESLIE P. MIRANDA , HUNG Q. NGUYEN , KENNETH W. WALKER , SHAW-FEN SYLVIA HU , COLIN V. GEGG , STEFAN I. MCDONOUGH
IPC分类号： C12N5/10 , C07H21/04 , C12N15/63 , C12N1/00 , C12N1/21
CPC分类号： A61K47/48215 , A61K38/00 , A61K47/60 , C07K14/43504 , C07K2319/30 , C07K2319/55
摘要： Disclosed is a DNA encoding a composition of matter of the formula (X1)a—(F1)d—(X2)b—(F2)e—(X3)c (I) and multimers thereof, in which F1 and F2 are half-life extending moieties, and d and e are each independently 0 or 1, provided that at least one of d and e is 1; X1, X2, and X3 are each independently -(L)f-P-(L)g-, and f and g are each independently 0 or 1; P is a ShK peptide analog of no more than about 80 amino acid residues in length; L is an optional linker; and a, b, and c are each independently 0 or 1, provided that at least one of a, b and c is 1. A DNA encoding the ShK peptide analog is disclosed. Also disclosed are an expression vector comprising the DNA, and a host cell comprising the expression vector.
摘要翻译：公开了编码式（X1）a-（F1）d-（X2）b-（F2）e-（X3）c（Ⅰ）及其多聚体的物质组成的DNA，其中F1和F2为一半并且d和e各自独立地为0或1，条件是d和e中的至少一个为1; X1，X2和X3各自独立地为 - （L）f-P-（L）g-，f和g各自独立地为0或1; P是长度不超过约80个氨基酸残基的ShK肽类似物; L是可选的接头; 和a，b和c各自独立地为0或1，条件是a，b和c中的至少一个为1.编码ShK肽类似物的DNA。还公开了包含DNA的表达载体和包含表达载体的宿主细胞。

10. 发明授权

US07834164B2 DNA encoding OSK1 toxin peptide analogs and vectors and cells for combinant expression 有权
标题翻译：编码OSK1毒素肽类似物的DNA和用于组合表达的载体和细胞
公开(公告)号：US07834164B2
公开(公告)日：2010-11-16
申请号：US11978105
申请日：2007-10-25
申请人： John K. Sullivan , Joseph G. McGivern , Leslie P. Miranda , Hung Q. Nguyen , Kenneth W. Walker , Shaw-Fen Sylvia Hu , Colin V. Gegg, Jr.
发明人： John K. Sullivan , Joseph G. McGivern , Leslie P. Miranda , Hung Q. Nguyen , Kenneth W. Walker , Shaw-Fen Sylvia Hu , Colin V. Gegg, Jr.
IPC分类号： C07H21/04 , C12N1/21 , C12N5/10 , C12N15/63
CPC分类号： C07K14/43522 , A61K38/00 , A61K47/60 , C07K2319/30 , C07K2319/31
摘要： Disclosed is a composition of matter comprising an OSK1 peptide analog, and in some embodiments, a pharmaceutically acceptable salt thereof. A pharmaceutical composition comprises the composition and a pharmaceutically acceptable carrier. Also disclosed are DNAs encoding the inventive composition of matter, an expression vector comprising the DNA, and host cells comprising the expression vector. Methods of treating an autoimmune disorder and of preventing or mitigating a relapse of a symptom of multiple sclerosis are also disclosed.
摘要翻译：公开了包含OSK1肽类似物的物质组合物，并且在一些实施方案中为其药学上可接受的盐。药物组合物包含该组合物和药学上可接受的载体。还公开了编码本发明组合物的DNA，包含DNA的表达载体和包含表达载体的宿主细胞。还公开了治疗自身免疫性疾病和预防或减轻多发性硬化症状的复发的方法。

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