公开(公告)号：US09249186B2

公开(公告)日：2016-02-02

申请号：US14793942

申请日：2015-07-08

Applicant: PFIZER INC.

Inventor： Matthew David Doroski ,  Andreas Maderna ,  Christopher John O'Donnell ,  Chakrapani Subramanyam ,  Beth Vetelino ,  Russell George Dushin ,  Pavel Strop ,  Edmund Idris Graziani

IPC: C07K7/02 ,  C07K5/02 ,  C07K16/00 ,  C07K7/06

CPC classification number: C07K7/06 ,  A61K38/06 ,  A61K38/07 ,  A61K38/08 ,  A61K47/6803 ,  A61K47/6811 ,  A61K47/6851 ,  A61K47/6855 ,  A61K47/6863 ,  A61K47/6889 ,  C07K5/0205 ,  C07K5/0808 ,  C07K7/02 ,  C07K16/00 ,  C07K2319/30

Abstract: The present invention is directed to cytotoxic pentapeptides, to antibody drug conjugates thereof, and to methods for using the same to treat cancer.

公开(公告)号：US09138486B2

公开(公告)日：2015-09-22

申请号：US14322262

申请日：2014-07-02

Applicant: PFIZER INC.

Inventor： Matthew David Doroski ,  Andreas Maderna ,  Christopher John O'Donnell ,  Chakrapani Subramanyam ,  Beth Vetelino ,  Russell George Dushin ,  Pavel Strop ,  Edmund Idris Graziani

IPC: A61K47/48 ,  A61K38/06 ,  A61K38/08 ,  A61K38/07 ,  C07K7/02 ,  C07K5/083 ,  C07K5/02 ,  C07K16/00

CPC classification number: C07K7/06 ,  A61K38/06 ,  A61K38/07 ,  A61K38/08 ,  A61K47/6803 ,  A61K47/6811 ,  A61K47/6851 ,  A61K47/6855 ,  A61K47/6863 ,  A61K47/6889 ,  C07K5/0205 ,  C07K5/0808 ,  C07K7/02 ,  C07K16/00 ,  C07K2319/30

Abstract: The present invention is directed to cytotoxic pentapeptides, to antibody drug conjugates thereof, and to methods for using the same to treat cancer.

Abstract translation: 本发明涉及细胞毒性五肽，其抗体药物偶联物及其用于治疗癌症的方法。

公开(公告)号：US20150072990A1

公开(公告)日：2015-03-12

申请号：US14543020

申请日：2014-11-17

Applicant: Pfizer Inc.

Inventor： Martin Youngjin Pettersson ,  Douglas Scott Johnson ,  Chakrapani Subramanyam ,  Christopher John O'Donnell ,  Christopher William am Ende ,  Michael Eric Green ,  Nandini Chaturbhai Patel ,  Cory Michael Stiff ,  Tuan Phong Tran ,  Gregory Wayne Kauffman ,  Antonia Friederike Stepan ,  Patrick Robert Verhoest

IPC: C07D471/04

CPC classification number: C07D471/04

Abstract: Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

Abstract translation: 公开了化合物的化合物和药学上可接受的盐，其中化合物具有说明书中定义的式I的结构。 还公开了相应的药物组合物，治疗方法，合成方法和中间体。

公开(公告)号：US10391182B2

公开(公告)日：2019-08-27

申请号：US16053344

申请日：2018-08-02

Applicant: PFIZER INC.

Inventor： Andreas Maderna ,  Matthew David Doroski ,  Zecheng Chen ,  Hud Lawrence Risley ,  Jeffrey Michael Casavant ,  Christopher John O'Donnell ,  Alexander M. Porte ,  Chakrapani Subramanyam

IPC: C07D487/04 ,  C07D487/06 ,  A61K47/68 ,  A61K31/404 ,  A61K31/407 ,  A61K31/433 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/675 ,  A61K31/7056 ,  A61K38/05 ,  A61K38/06 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D417/14 ,  C07F9/6561 ,  C07H17/02 ,  C07K5/06 ,  C07K5/08 ,  C07K9/00

Abstract: Cytotoxic dimers comprising CBI-based and/or CPI-based sub-units, antibody drug conjugates comprising such dimers, and to methods for using the same to treat cancer and other conditions.

公开(公告)号：US09169264B2

公开(公告)日：2015-10-27

申请号：US14069057

申请日：2013-10-31

Applicant: PFIZER INC.

Inventor： Chakrapani Subramanyam ,  Frank Erich Koehn ,  Kenneth John Dirico ,  Alessandra S. Eustaquio ,  Michael Eric Green ,  Haiyin He ,  Min He ,  Christopher John O'Donnell ,  Sujiet Puthenveetil ,  Anokha Ratnayake ,  Jesse Alexander Teske ,  Hui Yu Yang

IPC: A61K38/00 ,  C07K16/00 ,  C07D493/10 ,  C07D309/10 ,  C07D405/12 ,  C07D493/20 ,  A61K45/06 ,  A61K47/48 ,  C07D309/14 ,  C07D405/14

CPC classification number: A61K47/6855 ,  A61K31/35 ,  A61K31/351 ,  A61K31/397 ,  A61K31/4025 ,  A61K31/453 ,  A61K31/496 ,  A61K31/501 ,  A61K45/06 ,  A61K47/6803 ,  A61K47/6869 ,  A61K47/6889 ,  C07D309/10 ,  C07D309/14 ,  C07D405/12 ,  C07D405/14 ,  C07D493/10 ,  C07D493/20

Abstract: The present invention is directed to novel cytotoxic spliceostatin analogs and derivatives, to antibody drug conjugates thereof, and to methods for using the same to treat medical conditions including cancer.

Abstract translation: 本发明涉及新颖的细胞毒素剪接抑制物类似物及其衍生物，其抗体药物偶联物及其用于治疗包括癌症在内的医学病症的方法。

公开(公告)号：US09067934B2

公开(公告)日：2015-06-30

申请号：US14053924

申请日：2013-10-15

Applicant: Pfizer Inc.

Inventor： Martin Youngjin Pettersson ,  Douglas Scott Johnson ,  Chakrapani Subramanyam ,  Christopher John O'Donnell ,  Christopher William am Ende ,  Benjamin Adam Fish ,  Michael Eric Green ,  Patrick Bradley Mullins ,  Cory Michael Stiff ,  Tuan Phong Tran ,  Thayalan Navaratnam

IPC: C07D471/04 ,  C07D401/04 ,  A61K31/4985 ,  A61K31/695 ,  A61K45/06 ,  C07D491/048 ,  C07F7/08

CPC classification number: C07D471/04 ,  A61K31/4985 ,  A61K31/695 ,  A61K45/06 ,  C07D401/04 ,  C07D491/048 ,  C07F7/0812

Abstract: Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I as defined herein. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

Abstract translation: 公开了化合物的化合物和药学上可接受的盐，其中所述化合物具有如本文所定义的式I的结构。 还公开了相应的药物组合物，治疗方法，合成方法和中间体。

公开(公告)号：US10086085B2

公开(公告)日：2018-10-02

申请号：US14605697

申请日：2015-01-26

Applicant: Pfizer Inc.

Inventor： Andreas Maderna ,  Matthew David Doroski ,  Zecheng Chen ,  Hud Lawrence Risley ,  Jeffrey Michael Casavant ,  Christopher John O'Donnell ,  Alexander M. Porte ,  Chakrapani Subramanyam

IPC: C07D487/04 ,  C07D487/06 ,  C07D209/30 ,  A61K31/404 ,  A61K31/407 ,  A61K47/48 ,  A61K31/433 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/675 ,  A61K31/7056 ,  A61K38/05 ,  A61K38/06 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D417/14 ,  C07F9/6561 ,  C07H17/02 ,  C07K5/06 ,  C07K5/08 ,  C07K9/00 ,  A61K47/68

Abstract: Cytotoxic dimers comprising CBI-based and/or CPI-based sub-units, antibody drug conjugates comprising such dimers, and to methods for using the same to treat cancer and other conditions.

公开(公告)号：US20160022626A1

公开(公告)日：2016-01-28

申请号：US14818455

申请日：2015-08-05

Applicant: PFIZER INC.

Inventor： Chakrapani SUBRAMANYAM ,  Frank Erich Koehn ,  Kenneth John Dirico ,  Alessandra S. Eustaquio ,  Michael Eric Green ,  Haiyin He ,  Min He ,  Christopher John O'Donnell ,  Sujiet Puthenveetil ,  Anokha Ratnayake ,  Jesse Alexander Teske ,  Hui Yu Yang

IPC: A61K31/351 ,  A61K47/48 ,  A61K31/496 ,  A61K31/501 ,  A61K31/453 ,  A61K31/397

CPC classification number: A61K47/6855 ,  A61K31/35 ,  A61K31/351 ,  A61K31/397 ,  A61K31/4025 ,  A61K31/453 ,  A61K31/496 ,  A61K31/501 ,  A61K45/06 ,  A61K47/6803 ,  A61K47/6869 ,  A61K47/6889 ,  C07D309/10 ,  C07D309/14 ,  C07D405/12 ,  C07D405/14 ,  C07D493/10 ,  C07D493/20

Abstract: The present invention is directed to novel cytotoxic spliceostatin analogs and derivatives, to antibody drug conjugates thereof, and to methods for using the same to treat medical conditions including cancer.

Abstract translation: 本发明涉及新颖的细胞毒素剪接抑制物类似物及其衍生物，其抗体药物偶联物及其用于治疗包括癌症在内的医学病症的方法。

公开(公告)号：US20140045790A1

公开(公告)日：2014-02-13

申请号：US14053924

申请日：2013-10-15

Applicant: Pfizer Inc.

Inventor： Martin Youngjin Pettersson ,  Douglas Scott Johnson ,  Chakrapani Subramanyam ,  Christopher John O'Donnell ,  Christopher William am Ende ,  Benjamin Adam Fish ,  Michael Eric Green ,  Patrick Bradley Mullins ,  Cory Michael Stiff ,  Tuan Phong Tran ,  Thayalan Navaratnam

IPC: C07D471/04 ,  C07D401/04 ,  C07F7/08 ,  C07D491/048 ,  A61K31/695 ,  A61K31/4985 ,  A61K45/06

CPC classification number: C07D471/04 ,  A61K31/4985 ,  A61K31/695 ,  A61K45/06 ,  C07D401/04 ,  C07D491/048 ,  C07F7/0812

Abstract: Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I as defined herein. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

Abstract translation: 公开了化合物的化合物和药学上可接受的盐，其中所述化合物具有如本文所定义的式I的结构。 还公开了相应的药物组合物，治疗方法，合成方法和中间体。