公开(公告)号：US20180193475A1

公开(公告)日：2018-07-12

申请号：US15329818

申请日：2015-07-27

Applicant: Novartis AG

Inventor： Tinya ABRAMS ,  Steven Bruce COHEN ,  Dylan DANIEL ,  Catrin FINNER ,  Bernhard Hubert GEIERSTANGER ,  Thomas HUBER ,  William MALLET ,  Matthew John MEYER ,  Weijia OU ,  Siew Ho SCHLEYER ,  Kathrin Ulrike TISSOT-DAGUETTE

IPC: A61K47/68 ,  A61K39/395 ,  C07K16/28 ,  A61P35/02

CPC classification number: A61K47/6803 ,  A61K39/39558 ,  A61K47/6849 ,  A61K49/00 ,  A61K51/103 ,  A61K51/1093 ,  A61K2039/505 ,  A61K2039/545 ,  A61P35/02 ,  C07K16/2803 ,  C07K2317/21 ,  C07K2317/24 ,  C07K2317/33 ,  C07K2317/34 ,  C07K2317/55 ,  C07K2317/565 ,  C07K2317/77 ,  C07K2317/92

Abstract: The present invention relates to anti-cKIT antibodies, antibody fragments, antibody drug conjugates, and their uses for the treatment of cancer.

公开(公告)号：US20190382441A1

公开(公告)日：2019-12-19

申请号：US16439204

申请日：2019-06-12

Applicant: NOVARTIS AG

Inventor： Bernhard Hubert GEIERSTANGER ,  Jan GRUNEWALD ,  Yunho JIN ,  Weijia OU ,  Tetsuo UNO ,  Yongqin WAN ,  Xing WANG

IPC: C07K5/02 ,  A61K47/68 ,  C07K7/02 ,  C07K16/32

Abstract: Disclosed herein are novel cytotoxic peptides of formula (I) as described herein: and the use of such peptides in making immunoconjugates (i.e Antibody Drug Conjugates) Also described herein are immunoconjugates (i.e Antibody Drug Conjugates) comprising such novel cytotoxic peptide linked to an antigen binding moiety, such as an antibody; where such immunoconjugates are useful for treating cell proliferative disorders. The invention further provides pharmaceutical compositions comprising these immunoconjugates, compositions comprising the immunoconjugates with a therapeutic co-agent, and methods to use these immunoconjugates and compositions for treating cell proliferation disorders.

公开(公告)号：US20170021033A1

公开(公告)日：2017-01-26

申请号：US15124606

申请日：2015-03-11

Applicant: NOVARTIS AG

Inventor： Bernhard Hubert GEIERSTANGER ,  Weijia OU

IPC: A61K47/48 ,  C07K16/24 ,  C07K16/32

CPC classification number: A61K47/48646 ,  A61K47/6803 ,  A61K47/6805 ,  A61K47/6809 ,  A61K47/6811 ,  A61K47/6845 ,  A61K47/6855 ,  A61K47/6871 ,  A61K2039/505 ,  C07K16/24 ,  C07K16/32 ,  C07K2317/522 ,  C07K2317/567

Abstract: The present application provides specific sites for modifying antibodies or antibody fragments by replacing at least one native amino acid in the constant region of a parental antibody or antibody fragment with cysteine, which can be used as a site of attachment for a payload or linker-payload combination. In one embodiment, the antibodies are modified with cysteines at positions 152 and 375 of the heavy chain constant region, as defined by EU numbering format. In another embodiment, the antibodies are modified with cysteines at position 360 of the heavy chain constant region, and position 107 of the kappa light chain constant region, as defined by EU numbering format.

Abstract translation: 本申请通过用亲本抗体或抗体片段的恒定区域中的至少一个天然氨基酸替代半胱氨酸来提供用于修饰抗体或抗体片段的特异性位点，其可用作有效载荷或连接体有效载荷的附着位点 组合。 在一个实施方案中，根据EU编号格式所定义的，在重链恒定区的位置152和375的半胱氨酸修饰抗体。 在另一个实施方案中，根据EU编号格式定义，抗体在重链恒定区的360位的半胱氨酸和κ轻链恒定区的位置107修饰。

公开(公告)号：US20210170043A1

公开(公告)日：2021-06-10

申请号：US16669291

申请日：2019-10-30

Applicant: NOVARTIS AG ,  ADURO BIOTECH, INC.

Inventor： Lisa BARNETT ,  Steven BENDER ,  Charles Y. CHO ,  Sarah COX ,  Jonathan Deane ,  Scott Martin GLASER ,  Xueshi Hao ,  Shailaja KASIBHATLA ,  Weijia OU ,  Tetsuo UNO ,  Yongqin WAN ,  Ben WEN ,  Tom Yao-Hsiang WU

IPC: A61K47/68 ,  C07K16/28 ,  A61K31/688 ,  A61P35/00

Abstract: Provided herein are immunoconjugates comprising an anti-DC-SIGN antibody conjugated to a STING agonist. Also disclosed are methods of making the immunoconjugates and methods of treating cancer using the immunoconjugates.

公开(公告)号：US20180244717A1

公开(公告)日：2018-08-30

申请号：US15961531

申请日：2018-04-24

Applicant: NOVARTIS AG

Inventor： Bernhard Hubert GEIERSTANGER ,  Jan GRUNEWALD ,  Yunho JIN ,  Weijia OU ,  Tetsuo UNO ,  Yongqin WAN ,  Xing WANG

IPC: C07K5/02 ,  C07K7/02 ,  A61K47/68 ,  C07K16/32

CPC classification number: C07K5/0205 ,  A61K47/6817 ,  A61K47/6851 ,  C07K7/02 ,  C07K16/32

Abstract: Disclosed herein are novel cytotoxic peptides of formula (I) as described herein: and the use of such peptides in making immunoconjugates (i.e Antibody Drug Conjugates) Also described herein are immunoconjugates (i.e Antibody Drug Conjugates) comprising such novel cytotoxic peptide linked to an antigen binding moiety, such as an antibody; where such immunoconjugates are useful for treating cell proliferative disorders. The invention further provides pharmaceutical compositions comprising these immunoconjugates, compositions comprising the immunoconjugates with a therapeutic co-agent, and methods to use these immunoconjugates and compositions for treating cell proliferation disorders.

公开(公告)号：US20180155281A1

公开(公告)日：2018-06-07

申请号：US15822930

申请日：2017-11-27

Applicant: NOVARTIS AG

Inventor： Bernhard Hubert Geierstanger ,  Jan Grunewald ,  Weijia OU ,  Shifeng Pan ,  Tetsuo Uno ,  Yongqin Wan ,  Xing Wang

IPC: C07D207/09 ,  C07D401/12 ,  A61K47/68 ,  C07K16/32 ,  C07D403/12 ,  C07D403/14 ,  C07D413/12

CPC classification number: C07D207/09 ,  A61K47/6803 ,  A61K47/6849 ,  A61K47/6851 ,  A61K47/6855 ,  C07D401/12 ,  C07D403/12 ,  C07D403/14 ,  C07D413/12 ,  C07K5/0205 ,  C07K16/32

Abstract: Disclosed herein are novel compounds of formula (I) as described herein: and the use of such peptides in making immunoconjugates (i.e Antibody Drug Conjugates) Also described herein are immunoconjugates (i.e Antibody Drug Conjugates) comprising such novel compound linked to an antigen binding moiety, such as an antibody; where such immunoconjugates are useful for treating cell proliferative disorders. The invention further provides pharmaceutical compositions comprising these immunoconjugates, compositions comprising the immunoconjugates with a therapeutic co-agent, and methods to use these immunoconjugates and compositions for treating cell proliferation disorders.