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公开(公告)号：US10973826B2
公开(公告)日：2021-04-13
申请号：US15333285
申请日：2016-10-25
申请人： Alex Cortez , Bernhard Hubert Geierstanger , Timothy Z. Hoffman , Shailaja Kasibhatla , Tetsuo Uno , Xing Wang , Tom Yao-Hsiang Wu
发明人： Alex Cortez , Bernhard Hubert Geierstanger , Timothy Z. Hoffman , Shailaja Kasibhatla , Tetsuo Uno , Xing Wang , Tom Yao-Hsiang Wu
摘要： Provided herein are antibody conjugates comprising toll-like receptor agonists and the use of such conjugates for the treatment of cancer. In some embodiments, the conjugates comprise anti-HER2 antibodies.
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公开(公告)号：US09884817B2
公开(公告)日：2018-02-06
申请号：US15317532
申请日：2015-06-11
申请人： Bernhard Hubert Geierstanger , Jan Grunewald , Weijia Ou , Shifeng Pan , Tetsuo Uno , Yongqin Wan , Xing Wang
发明人： Bernhard Hubert Geierstanger , Jan Grunewald , Weijia Ou , Shifeng Pan , Tetsuo Uno , Yongqin Wan , Xing Wang
IPC分类号： C07D207/09 , A61K47/48 , C07D403/12 , C07D401/12 , C07D413/12 , C07D403/14 , C07K16/32
CPC分类号： C07D207/09 , A61K47/6803 , A61K47/6849 , A61K47/6851 , A61K47/6855 , C07D401/12 , C07D403/12 , C07D403/14 , C07D413/12 , C07K5/0205 , C07K16/32
摘要： Disclosed herein are novel compounds of formula (I) as described herein: and the use of such peptides in making immunoconjugates (i.e Antibody Drug Conjugates) Also described herein are immunoconjugates (i.e Antibody Drug Conjugates) comprising such novel compound linked to an antigen binding moiety, such as an antibody; where such immunoconjugates are useful for treating cell proliferative disorders. The invention further provides pharmaceutical compositions comprising these immunoconjugates, compositions comprising the immunoconjugates with a therapeutic co-agent, and methods to use these immunoconjugates and compositions for treating cell proliferation disorders.
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公开(公告)号：US09988420B2
公开(公告)日：2018-06-05
申请号：US15104727
申请日：2014-12-17
申请人： Bernhard Hubert Geierstanger , Jan Grunewald , Weijia Ou , Tetsuo Uno , Yongqin Wan , Xing Wang , Yunho Jin
发明人： Bernhard Hubert Geierstanger , Jan Grunewald , Weijia Ou , Tetsuo Uno , Yongqin Wan , Xing Wang , Yunho Jin
CPC分类号： C07K5/0205 , A61K47/6817 , A61K47/6851 , C07K7/02 , C07K16/32
摘要： Disclosed herein are novel cytotoxic peptides of formula (I) as described herein: and the use of such peptides in making immunoconjugates (i.e Antibody Drug Conjugates) Also described herein are immunoconjugates (i.e Antibody Drug Conjugates) comprising such novel cytotoxic peptide linked to an antigen binding moiety, such as an antibody; where such immunoconjugates are useful for treating cell proliferative disorders. The invention further provides pharmaceutical compositions comprising these immunoconjugates, compositions comprising the immunoconjugates with a therapeutic co-agent, and methods to use these immunoconjugates and compositions for treating cell proliferation disorders.
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公开(公告)号：US20170121282A1
公开(公告)日：2017-05-04
申请号：US15317532
申请日：2015-06-11
申请人： Bernhard Hubert Geierstanger , Jan Grunewald , Weijia OU , Shifeng Pan , Tetsuo Uno , Yongqin Wan , Xing Wang
发明人： Bernhard Hubert Geierstanger , Jan Grunewald , Weijia OU , Shifeng Pan , Tetsuo Uno , Yongqin Wan , Xing Wang
IPC分类号： C07D207/09 , C07K16/32 , C07D413/12 , C07D403/14 , C07D403/12 , C07D401/12
CPC分类号： C07D207/09 , A61K47/6803 , A61K47/6849 , A61K47/6851 , A61K47/6855 , C07D401/12 , C07D403/12 , C07D403/14 , C07D413/12 , C07K5/0205 , C07K16/32
摘要： Disclosed herein are novel compounds of formula (I) as described herein: and the use of such peptides in making immunoconjugates (i.e Antibody Drug Conjugates) Also described herein are immunoconjugates (i.e Antibody Drug Conjugates) comprising such novel compound linked to an antigen binding moiety, such as an antibody; where such immunoconjugates are useful for treating cell proliferative disorders. The invention further provides pharmaceutical compositions comprising these immunoconjugates, compositions comprising the immunoconjugates with a therapeutic co-agent, and methods to use these immunoconjugates and compositions for treating cell proliferation disorders.
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公开(公告)号：US20200338207A1
公开(公告)日：2020-10-29
申请号：US16701576
申请日：2019-12-03
摘要： The present invention provides specific sites for modifying antibodies or antibody fragments by replacing at least one native amino acid in the constant region of a parental antibody or antibody fragment with cysteine, which can be used as a site of attachment for a payload or linker-payload combination.
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公开(公告)号：US20150104468A1
公开(公告)日：2015-04-16
申请号：US14402808
申请日：2013-05-31
CPC分类号： C07K16/32 , A61K47/6815 , A61K47/6817 , A61K47/6851 , A61K47/6889 , C07K16/00 , C07K16/30 , C07K2317/24 , C07K2317/94 , C07K2318/10 , C07K2319/90
摘要： The present disclosure provides methods of site-specific labeling of antibodies, using proteins having 4′-phosphopantetheinyl transferase activity that catalyze post-translational modification of peptide sequences (“peptide tags”) incorporated into one or more specific sites of an antibody of interest. Enzymatic labeling enables quantitative and irreversible covalent modification of a specific serine residue within the peptide tags incorporated into the antibody, and thus creates desirable antibody conjugates.
摘要翻译： 本公开提供使用具有4'-磷酸泛酰乙酰转移酶活性的蛋白质的抗体的位点特异性标记方法，所述蛋白质催化并入感兴趣抗体的一个或多个特定位点的肽序列（“肽标签”）的翻译后修饰。 酶标记可以使掺入抗体的肽标记内的特定丝氨酸残基进行定量和不可逆共价修饰，从而产生所需的抗体缀合物。
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7.发明授权公开(公告)号：US10669323B2
公开(公告)日：2020-06-02
申请号：US15248712
申请日：2016-08-26
申请人： Brian R. Boettcher , Shari Lynn Caplan , Susan E. Cellitti , Douglas S. Daniels , Norio Hamamatsu , Bernhard Hubert Geierstanger , Stuart Licht , Andreas Loew , Stephen Craig Weldon
发明人： Brian R. Boettcher , Shari Lynn Caplan , Susan E. Cellitti , Douglas S. Daniels , Norio Hamamatsu , Bernhard Hubert Geierstanger , Stuart Licht , Andreas Loew , Stephen Craig Weldon
IPC分类号： A61K38/18 , A61K38/26 , C07K14/605 , C07K14/50
摘要： The present invention relates to the identification of dual function fusion proteins comprising fibroblast growth factor 21 (FGF21) and Exenatide, Exendin-4, or GLP-1. Also disclosed are methods for treating metabolic, cardiovascular, and endocrine conditions related to glucose and/or lipid homeostasis.
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公开(公告)号：US09585970B2
公开(公告)日：2017-03-07
申请号：US13906584
申请日：2013-05-31
IPC分类号： A61K39/395 , C07K16/30 , A61K47/48 , C07K16/00 , C07K16/32
CPC分类号： C07K16/32 , A61K47/6815 , A61K47/6817 , A61K47/6851 , A61K47/6889 , C07K16/00 , C07K16/30 , C07K2317/24 , C07K2317/94 , C07K2318/10 , C07K2319/90
摘要： The present invention provides methods of site-specific labeling of antibodies, using proteins having 4′-phosphopantetheinyl transferase activity that catalyze post-translational modification of peptide sequences (“peptide tags”) incorporated into one or more specific sites of an antibody of interest. Enzymatic labeling enables quantitative and irreversible covalent modification of a specific serine residue within the peptide tags incorporated into the antibody, and thus creates desirable antibody conjugates.
摘要翻译： 本发明提供使用具有4'-磷酸泛酰乙酰转移酶活性的蛋白质的抗体的位点特异性标记方法，所述蛋白质催化并入感兴趣抗体的一个或多个特定位点的肽序列（“肽标签”）的翻译后修饰。 酶标记可以使掺入抗体的肽标记内的特定丝氨酸残基进行定量和不可逆共价修饰，从而产生所需的抗体缀合物。
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