公开(公告)号：EP2640720A2

公开(公告)日：2013-09-25

申请号：EP11842404.3

申请日：2011-11-17

申请人： Yale University, Inc.

发明人： SPIEGEL, David ,  PARKER, Christopher

IPC分类号： C07D405/14 ,  A61K31/496 ,  A61P31/18

CPC分类号： C07D405/14 ,  A61K9/0014 ,  A61K31/496 ,  A61K45/06 ,  A61K2300/00

摘要： The present invention is directed to new bifunctional compounds and methods for treating HIV infections. The bifunctional small molecules, generally referred to as ARM- HI's, function through orthogonal pathways, by inhibiting the gpl20-CD4 interaction, and by recruiting anti-DNP antibodies to gpl20-expressing cells, thereby preventing cell infection and spread of HIV. It has been shown that ARM-HI's bind to gpl20 and gp-120 expressing cells competitively with CD4, thereby decreasing viral infectivity as shown by an MT-2 cell assay, the binding leading to formation of a ternary complex by recruiting anti-DNP antibodies to bind thereto, the antibodies present in the ternary complex promoting the complement-dependent destruction of the gpl20-expressing cells. Compounds and methods are described herein.

公开(公告)号：EP4294392A1

公开(公告)日：2023-12-27

申请号：EP22757120.5

申请日：2022-02-22

申请人： Yale University, Inc.

发明人： SPIEGEL, David ,  HOWELL, Rebecca ,  McDONALD, David

IPC分类号： A61K31/428 ,  C07D277/82 ,  C07D417/12

公开(公告)号：EP2640720B1

公开(公告)日：2018-10-17

申请号：EP11842404.3

申请日：2011-11-17

申请人： Yale University, Inc.

发明人： SPIEGEL, David ,  PARKER, Christopher

IPC分类号： C07D405/14 ,  A61K31/496 ,  A61P31/18 ,  A61K45/06

CPC分类号： C07D405/14 ,  A61K9/0014 ,  A61K31/496 ,  A61K45/06 ,  A61K2300/00

摘要： The present invention is directed to new bifunctional compounds and methods for treating HIV infections. The bifunctional small molecules, generally referred to as ARM-HI's, function through orthogonal pathways, by inhibiting the gp120-CD4 interaction, and by recruiting anti-DNP antibodies to gp120-expressing cells, thereby preventing cell infection and spread of HIV. It has been shown that ARM-HI's bind to gp120 and gp-120 expressing cells competitively with CD4, thereby decreasing viral infectivity as shown by an MT-2 cell assay, the binding leading to formation of a ternary complex by recruiting anti-DNP antibodies to bind thereto, the antibodies present in the ternary complex promoting the complement-dependent destruction of the gp120-expressing cells. Compounds and methods are described herein.

公开(公告)号：EP2291659A2

公开(公告)日：2011-03-09

申请号：EP09746950.6

申请日：2009-05-13

申请人： Yale University, Inc.

发明人： SPIEGEL, David ,  MURELLI, Ryan ,  ZHANG, Andrew

IPC分类号： G01N33/574

CPC分类号： C07K16/44 ,  A61K47/54 ,  A61K47/549 ,  A61K47/55 ,  A61K47/555 ,  A61K47/646 ,  A61K2039/505

摘要： The present invention relates to chimeric chemical compounds which are used to recruit antibodies to cancer cells, in particular, prostate cancer cells or metastasized prostate cancer cells. The compounds according to the present invention comprise an antibody binding terminus (ABT) moiety covalently bonded to a cell binding terminus (CBT) through a linker and optionally, a connector molecule.