公开(公告)号：US10947315B2

公开(公告)日：2021-03-16

申请号：US16229028

申请日：2018-12-21

申请人： IMMUNOGEN, INC.

发明人： Wei Li ,  Nathan Elliott Fishkin ,  Robert Yongxin Zhao ,  Michael Louis Miller ,  Ravi V. J. Chari

IPC分类号： C07D487/04 ,  C07D498/04 ,  C07D519/00 ,  A61K47/60 ,  A61P35/00 ,  C07K16/28 ,  A61K47/68 ,  A61K45/06 ,  A61K31/5517 ,  A61K38/07 ,  C07K5/103 ,  C07K5/02 ,  C07K16/46 ,  C07K19/00

摘要： The invention relates to novel benzodiazepine derivatives with antiproliferative activity and more specifically to novel benzodiazepines of formula (I) and (II), in which the diazepine ring (B) is fused with a heterocyclic ring (CD), wherein the heterocyclic ring is bicyclic or a compound of formula (III), in which the diazepine ring (B) is fused with a heterocyclic ring (C), wherein the heterocyclic ring is monocyclic. The invention provides cytotoxic dimers of these compounds. The invention also provides conjugates of the monomers and the dimers. The invention further provides compositions and methods useful for inhibiting abnormal cell growth or treating a proliferative disorder in a mammal using the compounds or conjugates of the invention. The invention further relates to methods of using the compounds or conjugates for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.

公开(公告)号：US09974867B2

公开(公告)日：2018-05-22

申请号：US15476770

申请日：2017-03-31

申请人： IMMUNOGEN, INC.

发明人： Ravi V. J. Chari ,  Michael Louis Miller ,  Manami Shizuka

IPC分类号： A61K47/68 ,  C07D487/04 ,  C07D519/00 ,  A61K45/06 ,  C07K16/28 ,  A61K39/00

CPC分类号： A61K47/6803 ,  A61K45/06 ,  A61K47/6845 ,  A61K47/6849 ,  A61K47/6851 ,  A61K47/6857 ,  A61K2039/505 ,  C07D487/04 ,  C07D519/00 ,  C07K16/28 ,  C07K16/2863 ,  C07K16/2866 ,  C07K2317/21 ,  C07K2317/24 ,  C07K2317/73 ,  C07K2317/92

摘要： The invention relates to novel benzodiazepine derivatives with antiproliferative activity and more specifically to novel benzodiazepine compounds of formula (I)-(VII). The invention also provides conjugates of the benzodiazepine compounds linked to a cell-binding agent. The invention further provides compositions and methods useful for inhibiting abnormal cell growth or treating a proliferative disorder in a mammal using the compounds or conjugates of the invention.

公开(公告)号：US09617270B2

公开(公告)日：2017-04-11

申请号：US14621813

申请日：2015-02-13

申请人： ImmunoGen, Inc.

发明人： Wei Li ,  Michael Louis Miller ,  Ravi V. J. Chari

IPC分类号： C07D487/04 ,  A61K47/48

CPC分类号： C07D487/04 ,  A61K47/60 ,  A61K47/6849

摘要： The invention relates to novel benzodiazepine derivatives with antiproliferative activity and more specifically to novel benzodiazepine compounds of formula (I)-(VII). The invention also provides conjugates of the benzodiazepine compounds linked to a cell-binding agent. The invention further provides compositions and methods useful for inhibiting abnormal cell growth or treating a proliferative disorder in a mammal using the compounds or conjugates of the invention.

公开(公告)号：US10570212B2

公开(公告)日：2020-02-25

申请号：US16205609

申请日：2018-11-30

申请人： IMMUNOGEN, INC.

发明人： Wei Li ,  Michael Louis Miller ,  Nathan Elliott Fishkin ,  Ravi V. J. Chari

IPC分类号： C07D487/04 ,  C07K16/30 ,  A61K47/68 ,  A61P35/00 ,  C07D519/00 ,  A61K45/06 ,  A61K31/5517 ,  A61K47/54 ,  A61K39/00

摘要： The invention relates to novel benzodiazepine derivatives with antiproliferative activity and more specifically to novel benzodiazepine compounds of formula (I)-(VII). The invention also provides conjugates of the benzodiazepine compounds linked to a cell-binding agent. The invention further provides compositions and methods useful for inhibiting abnormal cell growth or treating a proliferative disorder in a mammal using the compounds or conjugates of the invention.

公开(公告)号：US09669102B2

公开(公告)日：2017-06-06

申请号：US14843520

申请日：2015-09-02

申请人： ImmunoGen, Inc.

发明人： Ravi V. J. Chari ,  Michael Louis Miller ,  Manami Shizuka

IPC分类号： C07D487/04 ,  A61K47/48 ,  C07K16/28 ,  C07D519/00 ,  C07K5/093 ,  C07K5/113 ,  C07K5/02 ,  A61K39/00

CPC分类号： A61K47/64 ,  A61K2039/505 ,  C07D487/04 ,  C07D519/00 ,  C07K5/0202 ,  C07K5/0819 ,  C07K5/1021 ,  C07K16/28 ,  C07K16/2863 ,  C07K16/2866 ,  C07K2317/24 ,  C07K2317/92

摘要： The invention relates to novel benzodiazepine derivatives with antiproliferative activity and more specifically to novel benzodiazepine compounds of formula (I)-(VI). The invention also provides conjugates of the benzodiazepine compounds linked to a cell-binding agent. The invention further provides compositions and methods useful for inhibiting abnormal cell growth or treating a proliferative disorder in a mammal using the compounds or conjugates of the invention.

公开(公告)号：US09265841B2

公开(公告)日：2016-02-23

申请号：US14316105

申请日：2014-06-26

申请人： ImmunoGen, Inc.

发明人： Wei Li ,  Nathan Elliott Fishkin ,  Robert Yongxin Zhao ,  Michael Louis Miller ,  Ravi V. J. Chari

IPC分类号： C07D413/12 ,  A61K47/48 ,  C07D487/04 ,  C07D498/04 ,  C07D519/00 ,  A61K45/06 ,  A61K31/5517 ,  A61K38/07 ,  C07K5/103 ,  C07K16/28

CPC分类号： C07K16/2896 ,  A61K31/5517 ,  A61K38/07 ,  A61K45/06 ,  A61K47/60 ,  A61K47/6835 ,  A61K47/6849 ,  A61K47/6863 ,  A61P35/00 ,  C07D487/04 ,  C07D498/04 ,  C07D519/00 ,  C07K5/0202 ,  C07K5/1008 ,  C07K16/2803 ,  C07K16/46 ,  C07K19/00

摘要： The invention relates to novel benzodiazepine derivatives with antiproliferative activity and more specifically to novel benzodiazepines of formula (I) and (II), in which the diazepine ring (B) is fused with a heterocyclic ring (CD), wherein the heterocyclic ring is bicyclic or a compound of formula (III), in which the diazepine ring (B) is fused with a heterocyclic ring (C), wherein the heterocyclic ring is monocyclic. The invention provides cytotoxic dimers of these compounds. The invention also provides conjugates of the monomers and the dimers. The invention further provides compositions and methods useful for inhibiting abnormal cell growth or treating a proliferative disorder in a mammal using the compounds or conjugates of the invention. The invention further relates to methods of using the compounds or conjugates for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.

公开(公告)号：USRE49918E1

公开(公告)日：2024-04-16

申请号：US17316241

申请日：2021-05-10

申请人： IMMUNOGEN, INC.

发明人： Wei Li ,  Michael Louis Miller ,  Nathan Elliott Fishkin ,  Ravi V. J. Chari

IPC分类号： C07K16/30 ,  A61K31/5517 ,  A61K39/00 ,  A61K45/06 ,  A61K47/54 ,  A61K47/68 ,  A61P35/00 ,  C07D487/04 ,  C07D519/00

CPC分类号： C07K16/30 ,  A61K31/5517 ,  A61K45/06 ,  A61K47/545 ,  A61K47/6803 ,  A61K47/6849 ,  A61K47/6851 ,  A61K47/6867 ,  A61P35/00 ,  C07D487/04 ,  C07D519/00 ,  A61K2039/505 ,  C07K2317/24 ,  C07K2317/92 ,  C07K2317/94

摘要： The invention relates to novel benzodiazepine derivatives with antiproliferative activity and more specifically to novel benzodiazepine compounds of formula (I)-(VII). The invention also provides conjugates of the benzodiazepine compounds linked to a cell-binding agent. The invention further provides compositions and methods useful for inhibiting abnormal cell growth or treating a proliferative disorder in a mammal using the compounds or conjugates of the invention.

公开(公告)号：US11229639B2

公开(公告)日：2022-01-25

申请号：US17032219

申请日：2020-09-25

申请人： IMMUNOGEN, INC.

发明人： Ravi V. J. Chari ,  Wayne C. Widdison ,  Wei Li ,  David P. Pleynet

IPC分类号： A61K31/4745 ,  A61K47/68 ,  A61P35/00 ,  A61K39/395 ,  C07D491/22

摘要： Disclosed herein are novel cytotoxic compounds, and cytotoxic conjugates comprising these cytotoxic compounds and cell-binding agents. More specifically, this disclosure relates to novel camptothecin derivatives thereof, intermediates thereof, conjugates thereof, and pharmaceutically acceptable salts thereof, which are useful as medicaments, in particular as anti-proliferative agents (anticancer agents).

公开(公告)号：US10722588B2

公开(公告)日：2020-07-28

申请号：US16274665

申请日：2019-02-13

申请人： IMMUNOGEN, INC.

发明人： Ravi V. J. Chari ,  Michael Louis Miller ,  Manami Shizuka

IPC分类号： C07D487/04 ,  A61K47/64 ,  C07K16/28 ,  C07D519/00 ,  C07K5/02 ,  C07K5/093 ,  C07K5/113 ,  A61K39/00

摘要： The invention relates to novel benzodiazepine derivatives with antiproliferative activity and more specifically to novel benzodiazepine compounds of formula (I)-(VI). The invention also provides conjugates of the benzodiazepine compounds linked to a cell-binding agent. The invention further provides compositions and methods useful for inhibiting abnormal cell growth or treating a proliferative disorder in a mammal using the compounds or conjugates of the invention.

公开(公告)号：US10208127B2

公开(公告)日：2019-02-19

申请号：US15974089

申请日：2018-05-08

申请人： ImmunoGen, Inc.

发明人： Wei Li ,  Nathan Elliott Fishkin ,  Robert Yongxin Zhao ,  Michael Louis Miller ,  Ravi V. J. Chari

IPC分类号： C07D487/04 ,  C07K16/28 ,  C07K5/103 ,  A61K31/5517 ,  A61K45/06 ,  C07D519/00 ,  C07D498/04 ,  A61K47/68 ,  A61K47/60 ,  C07K19/00 ,  C07K16/46 ,  C07K5/02 ,  A61P35/00 ,  A61K38/07

摘要： The invention relates to novel benzodiazepine derivatives with antiproliferative activity and more specifically to novel benzodiazepines of formula (I) and (II), in which the diazepine ring (B) is fused with a heterocyclic ring (CD), wherein the heterocyclic ring is bicyclic or a compound of formula (III), in which the diazepine ring (B) is fused with a heterocyclic ring (C), wherein the heterocyclic ring is monocyclic. The invention provides cytotoxic dimers of these compounds. The invention also provides conjugates of the monomers and the dimers. The invention further provides compositions and methods useful for inhibiting abnormal cell growth or treating a proliferative disorder in a mammal using the compounds or conjugates of the invention. The invention further relates to methods of using the compounds or conjugates for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.