公开(公告)号：US20220017612A1

公开(公告)日：2022-01-20

申请号：US17465247

申请日：2021-09-02

申请人： Tilos Therapeutics, Inc. ,  Merck Sharp & Dohme Corp.

发明人： Randall Burton ,  Jessie M. English ,  Barbara S. Fox ,  Stavros Kopsiaftis ,  Yacob Gomez Llorente ,  Renee Moore ,  Patricia Rao ,  Giovanna Scapin ,  Kenneth J. Simon ,  Haihong Zhou

IPC分类号： C07K16/18 ,  A61P35/04 ,  A61P35/00 ,  G01N33/574 ,  G01N33/68

摘要： Provided herein are anti-LAP antibodies (e.g., recombinant humanized, chimeric, and human anti-LAP antibodies) or antigen binding fragments thereof which have therapeutically beneficial properties, such as binding specifically to LAP-TGFβ1 on cells but not to LAP-TGFβ1 in extracellular matrix, as well as compositions including the same. Also provided are uses of these antibodies or antigen binding fragments in therapeutic applications, such as in the treatment of cancer, and diagnostic applications.

公开(公告)号：US20180237524A1

公开(公告)日：2018-08-23

申请号：US15553254

申请日：2016-02-22

申请人： Paul REICHERT ,  Winifred W. PROSISE ,  Giovanna SCAPIN ,  Xiaoyu YANG ,  Ramesh KASHI ,  Corey STRICKLAND ,  Merck Sharp & Dohme Corp.

发明人： Paul Reichert ,  Winifred W. Prosise ,  Giovanna Scapin ,  Xiaoyu Yang ,  Ramesh Kashi ,  Corey Strickland

IPC分类号： C07K16/28 ,  C07K16/00

摘要： Crystals of pembrolizumab and structurally similar anti-PD-1 monoclonal antibodies are provided, as well as methods of producing such crystals, and uses of compositions comprising such antibody crystals, e.g. in treatment of cancers. The present invention satisfies these needs and more by providing pembrolizumab crystals and a method producing pembrolizumab crystals. One embodiment of the method of the invention produces crystals suitable for X-ray diffraction, and the inventors herein used such crystals to solve the three-dimensional structure of pembrolizumab to 2.3 A resolution.

公开(公告)号：US20140336222A1

公开(公告)日：2014-11-13

申请号：US14339925

申请日：2014-07-24

申请人： Merck Sharp & Dohme Corp.

发明人： Stephane L. Bogen ,  Yao Ma ,  Yaolin Wang ,  Brian Robert Lahue ,  Latha G. Nair ,  Manami Shizuka ,  Matthew E. Voss ,  Margarita Kirova-Snover ,  Weidong Pan ,  Yuan Tian ,  Bheemashankar A. Kulkarni ,  Craig R. Gibeau ,  Yuan Liu ,  Giovanna Scapin ,  Diane Rindgen ,  Ronald J. Doll ,  Timothy J. Guzi ,  Danny J. Hicklin ,  Amin Nomeir ,  Cynthia Seidel-Dugan ,  Gerald W. Shipps, JR. ,  Malcolm MacCoss

IPC分类号： C07D401/14 ,  C07D409/14

CPC分类号： C07D401/14 ,  C07D409/14

摘要： The present invention provides a compound of Formula 1 as described herein or a pharmaceutically acceptable salt, solvate or ester thereof. The compounds are useful as inhibitors of the HDM2 protein. Also disclosed are pharmaceutical compositions comprising the above compounds and methods of treating cancer using the same.

摘要翻译： 本发明提供本文所述的式1的化合物或其药学上可接受的盐，溶剂合物或酯。 该化合物可用作HDM2蛋白的抑制剂。 还公开了包含上述化合物的药物组合物和使用其治疗癌症的方法。

公开(公告)号：US11014986B2

公开(公告)日：2021-05-25

申请号：US15553254

申请日：2016-02-22

申请人： Paul Reichert ,  Winifred W. Prosise ,  Giovanna Scapin ,  Xiaoyu Yang ,  Ramesh Kashi ,  Corey Strickland ,  Merck Sharp & Dohme Corp.

发明人： Paul Reichert ,  Winifred W. Prosise ,  Giovanna Scapin ,  Xiaoyu Yang ,  Ramesh Kashi ,  Corey Strickland

IPC分类号： C07K16/28 ,  C07K16/00

摘要： Crystals of pembrolizumab and structurally similar anti-PD-1 monoclonal antibodies are provided, as well as methods of producing such crystals, and uses of compositions comprising such antibody crystals, e.g. in treatment of cancers. The present invention satisfies these needs and more by providing pembrolizumab crystals and a method producing pembrolizumab crystals. One embodiment of the method of the invention produces crystals suitable for X-ray diffraction, and the inventors herein used such crystals to solve the three-dimensional structure of pembrolizumab to 2.3 A resolution.