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    MODIFIED Fc MOLECULES
    2.
    发明申请
    MODIFIED Fc MOLECULES 审中-公开
    改良的Fc分子

    公开(公告)号：US20160000932A1

    公开(公告)日：2016-01-07

    申请号：US14796502

    申请日：2015-07-10

    Applicant: AMGEN INC.

    Inventor： Colin V. GEGG ,  Kenneth W. WALKER ,  Leslie P. MIRANDA ,  Fei XIONG

    IPC: A61K47/48 ,  C07K16/00 ,  A61K38/02 ,  C07K17/00

    CPC classification number: A61K38/02 ,  A61K47/60 ,  A61K47/68 ,  A61K47/6817 ,  C07K16/00 ,  C07K17/00 ,  C07K2317/40 ,  C07K2317/52

    Abstract: 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.

    Abstract translation: 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。

    POTENT AND SELECTIVE INHIBITORS OF NAV1.3 AND NAV1.7
    5.
    发明申请
    POTENT AND SELECTIVE INHIBITORS OF NAV1.3 AND NAV1.7 有权
    NAV1.3和NAV1.7的POTENT和选择性抑制剂

    公开(公告)号：US20160304570A1

    公开(公告)日：2016-10-20

    申请号：US15134305

    申请日：2016-04-20

    Applicant: AMGEN INC.

    Inventor： Justin K. MURRAY ,  Leslie P. MIRANDA ,  Stefan I. MCDONOUGH

    IPC: C07K14/435 ,  C07K16/44 ,  A61K47/48

    CPC classification number: C07K14/43518 ,  A61K38/00 ,  A61K47/60 ,  A61K47/68 ,  A61K47/6817 ,  C07K14/00 ,  C07K16/44 ,  C07K2317/35 ,  C07K2317/76 ,  C07K2319/30

    Abstract: Disclosed is a composition of matter comprising an isolated polypeptide, which is a peripherally-restricted NaV1.7 inhibitor. In some disclosed embodiments, the isolated polypeptide is an inhibitor of NaV1.7 and/or NaV1.3. Other embodiments are conjugated embodiments of the inventive composition of matter and pharmaceutical compositions containing the inventive composition of matter. Isolated nucleic acids encoding some embodiments of inventive polypeptides and expression vectors, and recombinant host cells containing them are disclosed. A method of treating or preventing pain is also disclosed.

    Abstract translation: 公开了包含分离的多肽的物质组合物，其是外周受限制的NaV1.7抑制剂。 在一些公开的实施方案中，分离的多肽是NaV1.7和/或NaV1.3的抑制剂。 其它实施方案是本发明组合物和包含本发明组合物的药物组合物的共轭实施方案。 公开了编码本发明多肽和表达载体的一些实施方案的分离的核酸，以及含有它们的重组宿主细胞。 还公开了治疗或预防疼痛的方法。

    POTENT AND SELECTIVE INHIBITORS OF NAV1.7
    6.
    发明申请
    POTENT AND SELECTIVE INHIBITORS OF NAV1.7 有权
    NAV1.7的POTENT和选择性抑制剂

    公开(公告)号：US20150023988A1

    公开(公告)日：2015-01-22

    申请号：US14207445

    申请日：2014-03-12

    Applicant: AMGEN INC.

    Inventor： Justin K. MURRAY ,  Jerry Ryan HOLDER ,  Malgorzata WANSKA ,  Christopher M. TEGLEY ,  James R. FALSEY ,  Elizabeth M. DOHERTY ,  Leslie P. MIRANDA

    IPC: A61K47/48 ,  C07K16/00 ,  A61K38/17 ,  C07K14/435

    CPC classification number: A61K47/48438 ,  A61K38/00 ,  A61K47/60 ,  A61K47/68 ,  A61K47/6817 ,  C07K14/43518 ,  C07K14/705 ,  C07K16/44

    Abstract: Disclosed is a composition of matter comprising an isolated polypeptide, which is a peripherally-restricted Nav1.7 inhibitor. In some disclosed embodiments, the isolated polypeptide is an inhibitor of Nav1.7. Other embodiments are conjugated embodiments of the inventive composition of matter and pharmaceutical compositions containing the inventive composition of matter. Isolated nucleic acids encoding some embodiments of inventive polypeptides and expression vectors, and recombinant host cells containing them are disclosed. A method of treating or preventing pain is also disclosed.

    Abstract translation: 公开了包含分离的多肽的物质组合物，其是外周限制的Nav1.7抑制剂。 在一些公开的实施方案中，分离的多肽是Nav1.7的抑制剂。 其它实施方案是本发明组合物和包含本发明组合物的药物组合物的共轭实施方案。 公开了编码本发明多肽和表达载体的一些实施方案的分离的核酸，以及含有它们的重组宿主细胞。 还公开了治疗或预防疼痛的方法。

    MODIFIED Fc MOLECULES
    10.
    发明申请
    MODIFIED Fc MOLECULES 审中-公开

    公开(公告)号：US20190151463A1

    公开(公告)日：2019-05-23

    申请号：US16206899

    申请日：2018-11-30

    Applicant: AMGEN INC.

    Inventor： Colin V. GEGG ,  Kenneth W. WALKER ,  Leslie P. MIRANDA ,  Fei XIONG

    IPC: A61K47/68 ,  C07K16/00 ,  C07K17/00 ,  A61K47/60 ,  A61K38/02

    Abstract: 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.

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