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1. 发明申请

US20070269369A1 Modified Fc molecules 有权
标题翻译：修饰的Fc分子
公开(公告)号：US20070269369A1
公开(公告)日：2007-11-22
申请号：US11502761
申请日：2006-08-10
申请人： Colin Gegg , Kenneth Walker , Leslie Miranda , Fei Xiong
发明人： Colin Gegg , Kenneth Walker , Leslie Miranda , Fei Xiong
IPC分类号： A61K51/10 , C07H21/04 , A61K49/00
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

US20080020978A1 CGRP peptide antagonists and conjugates 失效
标题翻译： CGRP肽拮抗剂和缀合物
公开(公告)号：US20080020978A1
公开(公告)日：2008-01-24
申请号：US11584177
申请日：2006-10-19
申请人： Colin Gegg , Eileen Johnson , Leslie Miranda , Kenneth Walker , Jerry Holder , Marie Wright , Derin D'Amico
发明人： Colin Gegg , Eileen Johnson , Leslie Miranda , Kenneth Walker , Jerry Holder , Marie Wright , Derin D'Amico
IPC分类号： A61K38/00 , A61P43/00
CPC分类号： A61K38/225 , C07K14/57527
摘要： Disclosed is a composition of matter that involves a CGRP peptide antagonist. A pharmaceutical composition is disclosed that comprises the composition of matter and a pharmaceutically acceptable carrier, which can be configured for administration to a patient. Also disclosed is a method of producing the composition of matter. Methods of treating, preventing or mitigating migraine, are also disclosed.
摘要翻译：公开了涉及CGRP肽拮抗剂的物质组合物。公开了包含物质组合物和药学上可接受的载体的药物组合物，其可被配置用于给予患者。还公开了一种生产物质组合物的方法。还公开了治疗，预防或减轻偏头痛的方法。

3. 发明申请

US20070071764A1 Toxin peptide therapeutic agents 有权
公开(公告)号：US20070071764A1
公开(公告)日：2007-03-29
申请号：US11406454
申请日：2006-04-17
申请人： John Sullivan , Joseph McGivern , Leslie Miranda , Hung Nguyen , Kenneth Walker , Shaw-Fen Hu , Colin Gegg , Stefan McDonough
发明人： John Sullivan , Joseph McGivern , Leslie Miranda , Hung Nguyen , Kenneth Walker , Shaw-Fen Hu , Colin Gegg , Stefan McDonough
IPC分类号： A61K39/395 , C07K16/46
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.

4. 发明申请

US20060173159A1 Water-soluble thioester and selenoester compounds and methods for making and using the same 失效
标题翻译：水溶性硫酯和硒酯化合物及其制备和使用方法
公开(公告)号：US20060173159A1
公开(公告)日：2006-08-03
申请号：US10541078
申请日：2003-12-30
申请人： Leslie Miranda , Stephen Kent
发明人： Leslie Miranda , Stephen Kent
IPC分类号： C07K14/00
CPC分类号： C07K14/001 , C07C327/32 , C07C391/00 , C07K1/04 , C07K1/086 , C07K1/088 , C07K1/10
摘要： Water-soluble thioester and selenoester compounds, their generators, as well as methods for making and using the same, are provided. The subject thioester and selenoester compounds are characterized by including an amino acid synthon having a C-terminal group bonded to a water-soluble polymer through a thioester or selenoester linkage. Solid phase resins and protocols for generating the subject compounds are also provided. The subject water soluble thioester and selenoester compounds and generators find use in a variety of different applications, including thioester or selenoester mediated chemical ligation reactions.
摘要翻译：提供了水溶性硫酯和硒酯化合物，它们的发生剂，以及制备和使用它们的方法。受试者硫酯和硒酯化合物的特征在于包括具有通过硫酯或硒酸酯键与水溶性聚合物键合的C-端基的氨基酸合成子。还提供了用于产生本发明化合物的固相树脂和方案。本发明的水溶性硫酯和硒酯化合物和发生器可用于各种不同的应用，包括硫酯或硒酯介导的化学连接反应。

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