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    MULTIVALENT MOLECULES COMPRISING DR5-BINDING DOMAINS
    1.
    发明申请
    MULTIVALENT MOLECULES COMPRISING DR5-BINDING DOMAINS 审中-公开
    包含DR5结合域的多重分子

    公开(公告)号：WO2016122702A1

    公开(公告)日：2016-08-04

    申请号：PCT/US2015/033099

    申请日：2015-05-29

    申请人： MACROGENICS, INC.

    发明人： MOORE, Paul, A. ,  JOHNSON, Leslie, S. ,  LI, Jonathan, C. ,  SHAH, Kalpana

    IPC分类号： C07K16/28

    CPC分类号： C07K16/2878 ,  A61K2039/505 ,  C07K16/30 ,  C07K2317/24 ,  C07K2317/35 ,  C07K2317/622 ,  C07K2317/73 ,  C07K2317/92

    摘要： The present invention is directed to multivalent DR5 -Binding Molecules that comprise Binding Domain(s) of anti-DR5 antibodies, and particularly Binding Domain(s) of anti-human DR5 antibodies. The DR5 -Binding Molecules of the present invention include bivalent and tetravalent molecules having two, three or four DR5-Binding Domains each capable of binding human DR5. In particular, the present invention is directed to multivalent DR5 -Binding Molecules that comprise diabodies, and more particularly, diabodies that comprise a covalently bonded complex of two or more polypeptide chains. The invention particularly pertains to such multivalent DR5 -Binding Molecules that comprise fragments of the anti-DR5 antibodies DR5 mAb 1 and/or DR5 mAb 2, and/or humanized and chimeric versions of such antibodies.

    摘要翻译： 本发明涉及包含抗DR5抗体的结合域，特别是抗人DR5抗体的结合结构域的多价DR5-结合分子。 本发明的DR5-结合分子包括具有两个，三个或四个能结合人DR5的DR5结合结构域的二价和四价分子。 特别地，本发明涉及包含双抗体的多价DR5-结合分子，更具体地，涉及包含两个或多个多肽链的共价键合复合物的双抗体。 本发明特别涉及包含抗DR5抗体DR5mAb1和/或DR5mAb2的片段，和/或这种抗体的人源化和嵌合形式的多价DR5-结合分子。

    COVALENTLY BONDED DIABODIES HAVING IMMUNOREACTIVITY WITH PD-1 AND LAG-3, AND METHODS OF USE THEREOF
    2.
    发明申请
    COVALENTLY BONDED DIABODIES HAVING IMMUNOREACTIVITY WITH PD-1 AND LAG-3, AND METHODS OF USE THEREOF 审中-公开
    具有PD-1和LAG-3的具有免疫反应性的双重结合的双歧杆菌及其使用方法

    公开(公告)号：WO2015200119A1

    公开(公告)日：2015-12-30

    申请号：PCT/US2015/036634

    申请日：2015-06-19

    申请人： MACROGENICS, INC.

    发明人： BONVINI, Ezio ,  JOHNSON, Leslie, S. ,  SHAH, Kalpana ,  LA MOTTE-MOHS, Ross ,  MOORE, Paul, A. ,  KOENIG, Scott

    IPC分类号： C07K16/28

    CPC分类号： C07K16/2803 ,  C07K16/2818 ,  C07K16/468 ,  C07K2317/31 ,  C07K2317/626 ,  C07K2317/74

    摘要： The present invention is directed to bi-specific diabodies that comprise two or more polypeptide chains and which possess at least one Epitope-Binding Site that is immunospecific for an epitope of PD-1 and at least one Epitope-Binding Site that is immunospecific for an epitope of LAG-3 (i.e., a "PD-I x LAG-3 bi-specific diabody"). More preferably, the present invention is directed to bi-specific diabodies that comprise four polypeptide chains and which possess two Epitope-Binding Sites that are immunospecific for one (or two) epitope(s) of PD-1 and two Epitope-Binding Site that are immunospecific for one (or two) epitope(s) of LAG-3 (i.e., a "PD-1 x LAG-3 bi-specific, tetra-valent diabody").

    摘要翻译： 本发明涉及包含两个或多个多肽链并且具有至少一个针对PD-1的表位具有免疫特异性的表位结合位点和至少一个对于一个或多个具有免疫特异性的表位结合位点的表位的双抗体 LAG-3表位（即，“PD-1×LAG-3双特异性双抗体”）。 更优选地，本发明涉及包含四个多肽链并且具有对PD-1的一个或两个表位和两个表位结合位点具有免疫特异性的两个表位结合位点的双特异性双抗体， 对于一个（或两个）LAG-3表位（即，“PD-1×LAG-3双特异性四价双抗体”）是免疫特异性的。

    PD-1-BINDING MOLECULES AND METHODS USE THEREOF
    4.
    发明申请
    PD-1-BINDING MOLECULES AND METHODS USE THEREOF 审中-公开
    PD-1结合分子及其使用方法

    公开(公告)号：WO2017019846A1

    公开(公告)日：2017-02-02

    申请号：PCT/US2016/044430

    申请日：2016-07-28

    申请人： MACROGENICS, INC.

    发明人： SHAH, Kalpana ,  SMITH, Douglas, H. ,  LA MOTTE-MOHS, Ross ,  JOHNSON, Leslie, S. ,  MOORE, Paul, A. ,  BONVINI, Ezio ,  KOENIG, Scott

    IPC分类号： A61K39/00 ,  A61K39/395 ,  C07K16/00

    CPC分类号： A61K39/00 ,  A61K39/395 ,  C07K16/2803 ,  C07K16/2818 ,  C07K2317/24 ,  C07K2317/31 ,  C07K2317/33 ,  C07K2317/76

    摘要： The present invention is directed to selected anti-PD-1 antibodies capable of binding to both cynomolgus monkey PD-1 and to human PD-1 : PD-1 mAb 1, PD-1 mAb 2, PD-1 mAb 3, PD-1 mAb 4, PD-1 mAb 5, PD-1 mAb 6, PD-1 mAb 7, PD-1 mAb 8, PD-1 mAb 9, PD-1 mAb 10, PD-1 mAb 11, PD-1 mAb 12, PD-1 mAb 13, PD-1 mAb 14, or PD-1 mAb 15, and to humanized and chimeric versions of such antibodies. The invention additionally pertains to PD-1 -binding molecules that comprise PD-1 binding fragments of such anti-PD-1 antibodies, immunocongugates, and to bispecific molecules, including diabodies, BiTEs, bispecific antibodies, etc., that comprise (i) such PD-1 -binding fragments, and (ii) a domain capable of binding an epitope of a molecule involved in regulating an immune check point present on the surface of an immune cells. The present invention also pertains to methods of using molecules that bind PD-1 for stimulating immune responses, as well as methods of detecting PD-1.

    摘要翻译： 本发明涉及能够结合食蟹猴PD-1和人PD-1的选择的抗PD-1抗体：PD-1mAb 1，PD-1mAb 2，PD-1mAb 3，PD- 1mAb 4，PD-1mAb 5，PD-1mAb 6，PD-1mAb 7，PD-1mAb 8，PD-1mAb 9，PD-1mAb 10，PD-1mAb 11，PD-1mAb 12，PD-1mAb 13，PD-1mAb 14或PD-1mAb 15，以及这些抗体的人源化和嵌合形式。 本发明还涉及包含PD-1结合片段的PD-1结合分子，所述PD-1结合片段包含抗PD-1抗体，免疫接种物以及双特异性分子，包括双抗体，BiTE，双特异性抗体等，其包含（i） 这样的PD-1结合片段，和（ii）能够结合涉及调节免疫细胞表面上存在的免疫检测点的分子表位的结构域。 本发明还涉及使用结合PD-1的分子刺激免疫应答的方法，以及检测PD-1的方法。

    BI-SPECIFIC MONOVALENT DIABODIES THAT ARE CAPABLE OF BINDING TO GPA33 AND CD3, AND USES THEREOF
    5.
    发明申请
    BI-SPECIFIC MONOVALENT DIABODIES THAT ARE CAPABLE OF BINDING TO GPA33 AND CD3, AND USES THEREOF 审中-公开
    可与GPA33和CD3结合的双特异性双价糖尿病及其应用

    公开(公告)号：WO2015026894A2

    公开(公告)日：2015-02-26

    申请号：PCT/US2014/051793

    申请日：2014-08-20

    申请人： MACROGENICS, INC.

    发明人： MOORE, Paul, A. ,  LI, Jonathan ,  CHEN, Francine, Zhifen ,  JOHNSON, Leslie, S. ,  SHAH, Kalpana ,  BONVINI, Ezio

    IPC分类号： B60Q1/00 ,  G06F7/00

    CPC分类号： C07K16/28 ,  A61K2039/505 ,  A61K2039/545 ,  C07K16/2803 ,  C07K16/2809 ,  C07K16/3046 ,  C07K2317/24 ,  C07K2317/31 ,  C07K2317/33 ,  C07K2317/35 ,  C07K2317/52 ,  C07K2317/524 ,  C07K2317/526 ,  C07K2317/56 ,  C07K2317/624 ,  C07K2317/626 ,  C07K2317/64 ,  C07K2317/73 ,  C07K2317/732 ,  C07K2317/92 ,  C07K2317/94 ,  C07K2319/31

    摘要： The present invention is directed to bi-specific monovalent diabodies that comprise two polypeptide chains and which possess at least one binding site specific for an epitope of CD3 and one binding site specific for an epitope of gpA33 (i.e., a "gpA33 x CD3 bi-specific monovalent diabody"). The present invention also is directed to bi-specific monovalent diabodies that comprise an immunoglobulin Fc Domain ("bi- specific monovalent Fc diabodies") and are composed of three polypeptide chains and which possess at least one binding site specific for an epitope of gpA33 and one binding site specific for an epitope of CD3 (i.e ., a "gpA33 x CD3 bi-specific monovalent Fc diabody"). The bi-specific monovalent diabodies and bi-specific monovalent Fc diabodies of the present invention are capable of simultaneous binding to gpA33 and CD3. The invention is directed to pharmaceutical compositions that contain such bi-specific monovalent diabodies or such bi-specific monovalent Fc diabodies. The invention is additionally directed to methods for the use of such diabodies in the treatment of cancer and other diseases and conditions.

    摘要翻译： 本发明涉及双特异性单价双抗体，其包含两条多肽链并且具有至少一个对CD3表位特异的结合位点和对gpA33表位特异的一个结合位点（即 ，“gpA33xCD3双特异性单价双抗体”）。 本发明还涉及包含免疫球蛋白Fc结构域的双特异性单价双抗体（“双特异性单价Fc双抗体”）并且由三条多肽链组成并且具有对gpA33的表位特异的至少一个结合位点 和一个对CD3表位特异的结合位点（即“gpA33xCD3双特异性单价Fc双抗体”）。 本发明的双特异性单价双抗体和双特异性单价Fc双抗体能够同时结合gpA33和CD3。 本发明涉及含有此类双特异性单价双抗体或此类双特异性单价Fc双抗体的药物组合物。 本发明另外涉及使用这种双抗体治疗癌症和其他疾病和病症的方法。

    BI-SPECIFIC MONOVALENT FC DIABODIES THAT ARE CAPABLE OF BINDING CD32B AND CD79B AND USES THEREOF
    7.
    发明申请
    BI-SPECIFIC MONOVALENT FC DIABODIES THAT ARE CAPABLE OF BINDING CD32B AND CD79B AND USES THEREOF 审中-公开
    具有结合CD32B和CD79B的双特异性单体FC二体及其用途

    公开(公告)号：WO2015021089A1

    公开(公告)日：2015-02-12

    申请号：PCT/US2014/049848

    申请日：2014-08-06

    申请人： MACROGENICS, INC.

    发明人： JOHNSON, Leslie, S. ,  HUANG, Ling ,  SHAH, Kalpana ,  BONVINI, Ezio ,  MOORE, Paul, A. ,  CHEN, Wei

    IPC分类号： A61K39/395

    CPC分类号： C07K16/283 ,  A61K2039/505 ,  C07K16/2803 ,  C07K16/468 ,  C07K2317/31 ,  C07K2317/52 ,  C07K2317/60 ,  C07K2317/624 ,  C07K2317/73 ,  C07K2317/74 ,  C07K2319/31 ,  C07K2319/73

    摘要： The present invention is directed to bi-specific monovalent diabodies that comprise an immunoglobulin Fc Domain ("bi-specific monovalent Fc diabodies") and are composed of three polypeptide chains and which possess at least one binding site specific for an epitope of CD32B and one binding site specific for an epitope of CD79b (i.e., a "CD32B x CD79b bi-specific monovalent Fc diabody"). The bi-specific monovalent Fc diabodies of the present invention are capable of simultaneous binding to CD32B and CD79b. The invention is directed to such compositions, to pharmaceutical compositions that contain such bi-specific monovalent Fc diabodies and to methods for their use in the treatment of inflammatory diseases or conditions, and in particular, systemic lupus erythematosus (SLE) and graft vs. host disease.

    摘要翻译： 本发明涉及包含免疫球蛋白Fc结构域（“双特异性单价Fc双抗体”）的双特异性单抗双抗体，并且由三条多肽链组成，并且具有至少一个对CD32B的表位有特异性的结合位点和一个 CD79b表位特异性结合位点（即“CD32B x CD79b双特异性单价Fc双抗体”）。 本发明的双特异性单价Fc双抗体能够同时结合CD32B和CD79b。 本发明涉及这样的组合物，含有这种双特异性单价Fc双抗体的药物组合物及其用于治疗炎性疾病或病症，特别是系统性红斑狼疮（SLE）和移植物抗宿主 疾病。

    LAG-3-BINDING MOLECULES AND METHODS OF USE THEREOF
    9.
    发明申请
    LAG-3-BINDING MOLECULES AND METHODS OF USE THEREOF 审中-公开
    LAG-3结合分子及其使用方法

    公开(公告)号：WO2016200782A1

    公开(公告)日：2016-12-15

    申请号：PCT/US2016/036172

    申请日：2016-06-07

    申请人： MACROGENICS, INC.

    发明人： LA MOTTE-MOHS, Ross ,  SHAH, Kalpana ,  SMITH, Douglas, H. ,  JOHNSON, Lesile, S. ,  MOORE, Paul, A. ,  BONVINI, Ezio ,  KOENIG, Scott

    IPC分类号： A61K39/395 ,  A61P31/00 ,  A61P35/00 ,  C07K16/28

    CPC分类号： C07K16/2803 ,  A61K2039/505 ,  C07K16/2818 ,  C07K2317/24 ,  C07K2317/76 ,  C07K2317/92

    摘要： The present invention is directed to the anti -LAG-3 antibodies, LAG-3 mAb 1, LAG-3 mAb 2, LAG-3 mAb 4, LAG-3 mAb 5, and LAG-3 mAb 6, and to humanized and chimeric versions of such antibodies. The invention additionally pertains to LAG-3 - binding molecules that comprise LAG-3 binding fragments of such anti-LAG-3 antibodies, immunocongugates, and to bispecific molecules, including diabodies, BiTEs, bispecific antibodies, etc. , that comprise (i) such LAG-3-binding fragments, and (ii) a domain capable of binding an epitope of a molecule involved in regulating an immune check point present on the surface of an immune cells. The present invention also pertains to methods of detecting LAG-3, as well as methods of using molecules that bind LAG-3 for stimulating immune responses.

    摘要翻译： 本发明涉及抗-LAG-3抗体，LAG-3mAb1，LAG-3mAb2，LAG-3mAb4，LAG-3mAb5和LAG-3mAb6，以及人源化和嵌合 这些抗体的版本。 本发明还涉及包含这种抗LAG-3抗体的LAG-3结合片段，免疫接种物以及双特异性分子（包括双抗体，BiTE，双特异性抗体等）的LAG-3结合分子，其包含（i） 这样的LAG-3结合片段，和（ii）能够结合涉及调节免疫细胞表面上存在的免疫检查点的分子表位的结构域。 本发明还涉及检测LAG-3的方法，以及使用结合LAG-3的分子刺激免疫应答的方法。