Modified Fc molecules
    7.
    发明授权
    Modified Fc molecules 有权
    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

    IPC分类号: C07K16/00 A61K38/00

    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。

    Toxin peptide therapeutic agents
    8.
    发明授权
    Toxin peptide therapeutic agents 有权
    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

    IPC分类号: A61K38/00 C07K14/00

    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。

    Modified Fc molecules
    10.
    发明授权
    Modified Fc molecules 有权
    修饰的Fc分子

    公开(公告)号:US09114175B2

    公开(公告)日:2015-08-25

    申请号:US13171233

    申请日:2011-06-28

    IPC分类号: C07K16/00 A61K47/48 A61K38/00

    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。