公开(公告)号：EP1942944A2

公开(公告)日：2008-07-16

申请号：EP06850076.8

申请日：2006-10-26

申请人： Genentech, Inc.

发明人： JACKSON, David Y.

IPC分类号： A61K47/48 ,  A61P35/00 ,  A61K38/15

CPC分类号： A61K47/6851 ,  A61K47/6803 ,  A61K47/6811

摘要： The present invention relates to antibody-drug conjugate compounds of Formula I: Ab (L D)p I where one or more macrocyclic depsipeptide drug moieties (D), selected from Aplidin, Didemnin B, Kahalalide F, and analogs and derivatives therefrom, are covalently attached by a linker (L) to an antibody (Ab) which binds to one or more tumor-associated antigens or cell-surface receptors. These compounds may be useful in methods of diagnosis or treatment of cancer, and other diseases and disorders.

公开(公告)号：EP1633731A2

公开(公告)日：2006-03-15

申请号：EP04752856.7

申请日：2004-05-19

申请人： GENENTECH, INC.

发明人： JACKSON, David Y.

IPC分类号： C07D295/20 ,  A61K31/5375 ,  C07D217/14 ,  C07D491/08

CPC分类号： C07D295/21 ,  C07D217/14 ,  C07D491/08

摘要： The invention provides novel thiocarbamate alpha-4 inhibitors of the general formula (I) wherein L is -C(S)-O- or -C(O)-S-; that are resistant to metabolism having improved half-life and/or clearance properties compared to corresponding carbamate compounds wherein substituents L, X, Y, Z, R1-R4, m, n, o and p are as defined herein. Also provided are compositions comprising compounds of formula I and a carrier, diluent or excipient as well as methods of treating a disease or condition mediated by the binding interaction of alpha-4 integrins to its ligands such as inflammatory diseases.