公开(公告)号：US20160310611A1

公开(公告)日：2016-10-27

申请号：US15104388

申请日：2014-12-16

申请人： GENENTECH INC. ,  MEDIMMUNE LIMITED

发明人： John FLYGARE ,  Janet GUNZNER-TOSTE ,  Thomas PILLOW ,  Brian SAFINA ,  Vishal VERMA ,  Binqing WEI ,  Guiling ZHAO ,  Leanna STABEN ,  Philip Wilson HOWARD ,  Luke MASTERSON

IPC分类号： A61K47/48 ,  C07K16/30 ,  A61K31/5517 ,  C07K16/28

摘要： This invention relates to peptidomimetic linkers and anti-body drug conjugates thereof, pharmaceutical compositions containing them, and to their use in therapy for the prevention treatment of cancer.

摘要翻译： 本发明涉及肽模拟接头及其抗体药物偶联物，含有它们的药物组合物及其在预防癌症治疗中的用途。

公开(公告)号：US20200157240A1

公开(公告)日：2020-05-21

申请号：US16696455

申请日：2019-11-26

申请人： GENENTECH INC. ,  MEDIMMUNE LIMITED

发明人： John FLYGARE ,  Janet GUNZNER-TOSTE ,  Thomas PILLOW ,  Brian SAFINA ,  Vishal VERMA ,  Binqing WEI ,  Guiling ZHAO ,  Leanna STABEN ,  Philip Wilson HOWARD ,  Luke MASTERSON

IPC分类号： C07K16/30 ,  C07K16/28 ,  A61K31/5517 ,  A61K47/68

摘要： This invention relates to peptidomimetic linkers and anti-body drug conjugates thereof pharmaceutical compositions containing them, and to their use in therapy for the prevention treatment of cancer.

公开(公告)号：US20200085965A1

公开(公告)日：2020-03-19

申请号：US16689286

申请日：2019-11-20

申请人： GENENTECH, INC.

发明人： Peter DRAGOVICH ,  Zhonghua PEI ,  Thomas PILLOW ,  Jack SADOWSKY ,  Vishal VERMA ,  Donglu ZHANG

IPC分类号： A61K47/68 ,  A61K31/5517 ,  A61P35/00

摘要： The invention relates generally to pyrrolobenzodiazepine monomer and dimer prodrugs having a glutathione-activated disulfide prodrug moiety, a DT-diaphorase-activated quinone prodrug moiety or a reactive oxygen species-activated aryl boronic acid or aryl boronic ester prodrug moiety. The invention further relates to pyrrolobenzodiazepine prodrug dimer-antibody conjugates.

公开(公告)号：US20190175749A1

公开(公告)日：2019-06-13

申请号：US16271549

申请日：2019-02-08

申请人： GENENTECH, INC.

发明人： Peter DRAGOVICH ,  Zhonghua PEI ,  Thomas PILLOW ,  Jack SADOWSKY ,  Vishal VERMA ,  Donglu ZHANG

IPC分类号： A61K47/68 ,  A61P35/00 ,  A61K31/5517

摘要： The invention relates generally to pyrrolobenzodiazepine monomer and dimer prodrugs having a glutathione-activated disulfide prodrug moiety, a DT-diaphorase-activated quinone prodrug moiety or a reactive oxygen species-activated aryl boronic acid or aryl boronic ester prodrug moiety. The invention further relates to pyrrolobenzodiazepine prodrug dimer-antibody conjugates.

公开(公告)号：US20200048197A1

公开(公告)日：2020-02-13

申请号：US16657102

申请日：2019-10-18

申请人： Genentech, Inc.

发明人： Huifen CHEN ,  Yanyan CHU ,  Steven DO ,  Anthony ESTRADA ,  Baihua HU ,  Aleksandr KOLESNIKOV ,  Xingyu LIN ,  Joseph P. LYSSIKATOS ,  Daniel SHORE ,  Vishal VERMA ,  Lan WANG ,  Guosheng WU ,  Po-wai YUEN

IPC分类号： C07D207/48 ,  C07D403/12 ,  C07D401/14 ,  C07D401/12 ,  C07D403/14 ,  C07D417/12 ,  C07D451/02 ,  C07D491/048 ,  C07D405/14

摘要： The invention is concerned with the compounds of formula I or II: and salts thereof. In addition, the present invention relates to methods of manufacturing and methods of using the compounds of formula I or II as well as pharmaceutical compositions containing such compounds. The compounds may be useful in treating diseases and conditions mediated by TRPA1, such as pain.

公开(公告)号：US20190144430A1

公开(公告)日：2019-05-16

申请号：US16247995

申请日：2019-01-15

申请人： Genentech, Inc.

发明人： Baihua HU ,  Vishal VERMA ,  Matthew VOLGRAF ,  Anthony ESTRADA ,  Joseph LYSSIKATOS

IPC分类号： C07D403/04 ,  C07D231/12 ,  C07D401/04 ,  C07D231/20 ,  C07D239/26 ,  C07D231/16 ,  C07D213/61

摘要： The invention is concerned with the compounds of formula I: and pharmaceutically acceptable salts thereof. In addition, the present invention relates to methods of manufacturing and methods of using the compounds of formula I as well as pharmaceutical compositions containing such compounds. The compounds may be useful in treating diseases and conditions mediated by TRPA1, such as pain.

公开(公告)号：US20190167681A1

公开(公告)日：2019-06-06

申请号：US16269973

申请日：2019-02-07

申请人： Genentech, Inc.

发明人： Vishal VERMA ,  Matthew VOLGRAF ,  Baihua HU

IPC分类号： A61K31/506 ,  A61P11/00

摘要： The invention provides compounds of formula I: and pharmaceutically acceptable salts thereof where R1 is a substituted or unsubstituted phenyl or a fused bicyclic comprising a substituted or unsubstituted phenyl. In addition, the present invention relates to methods of manufacturing and methods of using the compounds of formula I as well as pharmaceutical compositions containing such compounds. The compounds may be useful in treating diseases and conditions mediated by TRPA1, such as pain.

公开(公告)号：US20180282272A1

公开(公告)日：2018-10-04

申请号：US16001770

申请日：2018-06-06

申请人： Genentech, Inc.

发明人： Huifen CHEN ,  Yanyan CHU ,  Steven DO ,  Anthony ESTRADA ,  Baihua HU ,  Aleksandr KOLESNIKOV ,  Xingyu LIN ,  Joseph P. LYSSIKATOS ,  Daniel SHORE ,  Vishal VERMA ,  Lan WANG ,  Guosheng WU ,  Po-wai YUEN

IPC分类号： C07D207/48 ,  C07D451/02 ,  C07D491/048 ,  C07D401/14 ,  C07D405/14 ,  C07D403/14 ,  C07D403/12 ,  C07D417/12 ,  C07D401/12

摘要： The invention is concerned with the compounds of formula I or II: and salts thereof. In addition, the present invention relates to methods of manufacturing and methods of using the compounds of formula I or II as well as pharmaceutical compositions containing such compounds. The compounds may be useful in treating diseases and conditions mediated by TRPA1, such as pain.

公开(公告)号：US20160221945A1

公开(公告)日：2016-08-04

申请号：US15095467

申请日：2016-04-11

申请人： Genentech, Inc.

发明人： Huifen CHEN ,  Yanyan CHU ,  Steven DO ,  Anthony ESTRADA ,  Baihua HU ,  Aleksandr KOLESNIKOV ,  Xingyu LIN ,  Joseph P. LYSSIKATOS ,  Daniel SHORE ,  Vishal VERMA ,  Lan WANG ,  Guosheng WU ,  Po-wai YUEN

IPC分类号： C07D207/48 ,  C07D403/12 ,  C07D403/14 ,  C07D417/12 ,  C07D405/14 ,  C07D491/048 ,  C07D451/02 ,  C07D401/14 ,  C07D401/12

摘要： The invention is concerned with the compounds of formula I or II: and salts thereof. In addition, the present invention relates to methods of manufacturing and methods of using the compounds of formula I or II as well as pharmaceutical compositions containing such compounds. The compounds may be useful in treating diseases and conditions mediated by TRPA1, such as pain.

摘要翻译： 本发明涉及式I或II化合物及其盐。 此外，本发明涉及制备方法和使用式I或II化合物的方法以及含有这些化合物的药物组合物。 该化合物可用于治疗TRPA1介导的疾病和病症，例如疼痛。

公开(公告)号：US20190144428A1

公开(公告)日：2019-05-16

申请号：US16250230

申请日：2019-01-17

申请人： Genentech, Inc.

发明人： Vishal VERMA ,  Daniel SHORE ,  Matthew VOLGRAF ,  Anthony A. ESTRADA ,  Joseph LYSSIKATOS

IPC分类号： C07D401/14 ,  C07D403/14 ,  C07D403/12 ,  C07D405/14

CPC分类号： C07D401/14 ,  C07D401/12 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14

摘要： The invention is concerned with the compounds of formula I: and salts thereof. In addition, the present invention relates to methods of manufacturing and methods of using the compounds of formula I as well as pharmaceutical compositions containing such compounds. The compounds may be useful in treating diseases and conditions mediated by TRPA1, such as pain.