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1. 发明授权

US10973826B2 Antibody conjugates comprising toll-like receptor agonist 有权
公开(公告)号：US10973826B2
公开(公告)日：2021-04-13
申请号：US15333285
申请日：2016-10-25
申请人： Alex Cortez , Bernhard Hubert Geierstanger , Timothy Z. Hoffman , Shailaja Kasibhatla , Tetsuo Uno , Xing Wang , Tom Yao-Hsiang Wu
发明人： Alex Cortez , Bernhard Hubert Geierstanger , Timothy Z. Hoffman , Shailaja Kasibhatla , Tetsuo Uno , Xing Wang , Tom Yao-Hsiang Wu
IPC分类号： A61K31/52 , A61K47/68 , C07D487/04 , C07H15/26 , C07K16/28 , C07K16/32
摘要： Provided herein are antibody conjugates comprising toll-like receptor agonists and the use of such conjugates for the treatment of cancer. In some embodiments, the conjugates comprise anti-HER2 antibodies.

2. 发明授权

US09884817B2 Auristatin derivatives and conjugates thereof 有权
公开(公告)号：US09884817B2
公开(公告)日：2018-02-06
申请号：US15317532
申请日：2015-06-11
申请人： Bernhard Hubert Geierstanger , Jan Grunewald , Weijia Ou , Shifeng Pan , Tetsuo Uno , Yongqin Wan , Xing Wang
发明人： Bernhard Hubert Geierstanger , Jan Grunewald , Weijia Ou , Shifeng Pan , Tetsuo Uno , Yongqin Wan , Xing Wang
IPC分类号： C07D207/09 , A61K47/48 , C07D403/12 , C07D401/12 , C07D413/12 , C07D403/14 , C07K16/32
CPC分类号： C07D207/09 , A61K47/6803 , A61K47/6849 , A61K47/6851 , A61K47/6855 , C07D401/12 , C07D403/12 , C07D403/14 , C07D413/12 , C07K5/0205 , C07K16/32
摘要： 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.

3. 发明授权

US09988420B2 Cytotoxic peptides and conjugates thereof 有权
公开(公告)号：US09988420B2
公开(公告)日：2018-06-05
申请号：US15104727
申请日：2014-12-17
申请人： Bernhard Hubert Geierstanger , Jan Grunewald , Weijia Ou , Tetsuo Uno , Yongqin Wan , Xing Wang , Yunho Jin
发明人： Bernhard Hubert Geierstanger , Jan Grunewald , Weijia Ou , Tetsuo Uno , Yongqin Wan , Xing Wang , Yunho Jin
IPC分类号： A61K38/00 , C07K5/02 , C07K7/02 , C07K16/32 , A61K47/68
CPC分类号： C07K5/0205 , A61K47/6817 , A61K47/6851 , C07K7/02 , C07K16/32
摘要： 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.

4. 发明申请

US20170121282A1 AURISTATIN DERIVATIVES AND CONJUGATES THEREOF 有权
公开(公告)号：US20170121282A1
公开(公告)日：2017-05-04
申请号：US15317532
申请日：2015-06-11
申请人： Bernhard Hubert Geierstanger , Jan Grunewald , Weijia OU , Shifeng Pan , Tetsuo Uno , Yongqin Wan , Xing Wang
发明人： Bernhard Hubert Geierstanger , Jan Grunewald , Weijia OU , Shifeng Pan , Tetsuo Uno , Yongqin Wan , Xing Wang
IPC分类号： C07D207/09 , C07K16/32 , C07D413/12 , C07D403/14 , C07D403/12 , C07D401/12
CPC分类号： C07D207/09 , A61K47/6803 , A61K47/6849 , A61K47/6851 , A61K47/6855 , C07D401/12 , C07D403/12 , C07D403/14 , C07D413/12 , C07K5/0205 , C07K16/32
摘要： 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.

5. 发明申请

US20200338207A1 SPECIFIC SITES FOR MODIFYING ANTIBODIES TO MAKE IMMUNOCONJUGATES 审中-公开
公开(公告)号：US20200338207A1
公开(公告)日：2020-10-29
申请号：US16701576
申请日：2019-12-03
申请人： Bernhard Hubert Geierstanger , Weijia Ou , Tetsuo Uno
发明人： Bernhard Hubert Geierstanger , Weijia Ou , Tetsuo Uno
IPC分类号： A61K47/68 , C07K16/32
摘要： The present invention 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.

6. 发明申请

US20110262963A1 BIOSYNTHETICALLY GENERATED PYRROLINE-CARBOXY-LYSINE AND SITE SPECIFIC PROTEIN MODIFICATIONS VIA CHEMICAL DERIVATIZATION OF PYRROLINE-CARBOXY-LYSINE AND PYRROLYSINE RESIDUES 失效
标题翻译：通过化学衍生化吡咯烷 - 羧酸 - 赖氨酸和吡咯啉残基的生物活性生成的吡咯烷 - 羧酸 - 赖氨酸和位点特异性蛋白质修饰
公开(公告)号：US20110262963A1
公开(公告)日：2011-10-27
申请号：US13125547
申请日：2009-10-23
申请人： Bernhard Geierstanger , Weijia Ou , Susan E. Cellitti , Tetsuo Uno , Tiffany Crossgrove , Hsien-Po Chiu , Jan Grunewald , Xueshi Hao
发明人： Bernhard Geierstanger , Weijia Ou , Susan E. Cellitti , Tetsuo Uno , Tiffany Crossgrove , Hsien-Po Chiu , Jan Grunewald , Xueshi Hao
IPC分类号： C12P21/02 , C07D207/22 , C07K16/00 , C12P21/08 , C07K14/485 , C12N11/18 , C12N9/90 , C07K14/50 , C07K14/525 , C07K14/435 , C07K14/505
CPC分类号： C12P21/00 , C07D207/20 , C07D207/48 , C07K5/0215
摘要： Disclosed herein is pyrroline-carboxy-lysine (PCL), a pyrrolysine analogue, which is a natural, biosynthetically generated amino acid, and methods for biosynthetically generating PCL. Also disclosed herein are proteins, polypeptides and peptides that have PCL incorporated therein and methods for incorporating PCL into such proteins, polypeptides and peptides. Also disclosed herein is the site-specific derivatization of proteins, polypeptides and peptides having PCL or pyrrolysine incorporated therein. Also disclosed herein is the crosslinking of proteins, polypeptides and peptides having PCL or pyrrolysine incorporated therein.
摘要翻译：本文公开的是吡咯啉 - 羧基赖氨酸（PCL），吡咯赖氨酸类似物，其是天然的，生物合成产生的氨基酸，以及用于生物合成生成PCL的方法。本文还公开了具有并入其中的PCL的蛋白质，多肽和肽以及将PCL并入此类蛋白质，多肽和肽的方法。本文还公开了具有并入其中的PCL或吡咯赖胺的蛋白质，多肽和肽的位点特异性衍生化。本文还公开了具有并入其中的PCL或吡咯赖氨酸的蛋白质，多肽和肽的交联。

7. 发明申请

US20110257154A1 COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHIBITORS 有权
公开(公告)号：US20110257154A1
公开(公告)日：2011-10-20
申请号：US13172357
申请日：2011-06-29
申请人： Pierre-Yves Michellys , Wei Pei , Thomas H. Marsilje , Wenshuo Lu , Bei Chen , Tetsuo Uno , Yunho Jin , Tao Jiang
发明人： Pierre-Yves Michellys , Wei Pei , Thomas H. Marsilje , Wenshuo Lu , Bei Chen , Tetsuo Uno , Yunho Jin , Tao Jiang
IPC分类号： A61K31/397 , A61K31/506 , C07D239/48 , A61K31/505 , C07D413/14 , A61K31/5377 , C07D413/12 , C07D403/12 , A61K31/496 , C07D487/04 , A61K31/519 , A61K31/52 , A61P31/00 , A61P35/00 , C12N5/09 , C07D401/14
CPC分类号： A61K31/506 , A61K31/5377 , A61K45/06 , C07D213/74 , C07D239/48 , C07D239/95 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/14 , C07D413/12 , C07D417/12 , C07D451/02 , C07D453/02 , C07D471/04 , C07D473/16 , C07D487/04 , C07D487/08
摘要： The invention provides novel pyrimidine and pyridine derivatives and pharmaceutical compositions thereof, and methods for using such compounds. For example, the pyrimidine and pyridine derivatives of the invention may be used to treat, ameliorate or prevent a condition which responds to inhibition of anaplastic lymphoma kinase (ALK) activity, focal adhesion kinase (FAK), zeta-chain-associated protein kinase 70 (ZAP-70), insulin-like growth factor (IGF-1R), or a combination thereof.

8. 发明申请

US20110053897A1 COMPOUNDS AND COMPOSITIONS AS SYK KINASE INHIBITORS 审中-公开
标题翻译：作为SYK激酶抑制剂的化合物和组合物
公开(公告)号：US20110053897A1
公开(公告)日：2011-03-03
申请号：US12843771
申请日：2010-07-26
申请人： Jianwei CHE , Bei Chen , Qiang Ding , Xueshi Hao , Xiaohui He , Songchun Jiang , Qihui Jin , Yunho Jin , Hong Liu , Yahua Liu , Barun Okram , Tetsuo Uno , Xu Wu , Kunyong Yang , Xuefeng Zhu
发明人： Jianwei CHE , Bei Chen , Qiang Ding , Xueshi Hao , Xiaohui He , Songchun Jiang , Qihui Jin , Yunho Jin , Hong Liu , Yahua Liu , Barun Okram , Tetsuo Uno , Xu Wu , Kunyong Yang , Xuefeng Zhu
IPC分类号： A61K31/635 , C07D471/04 , A61K31/497 , A61K31/5377 , A61K31/506 , A61K31/444 , A61P11/06 , A61P19/02 , A61P35/00 , A61P7/06 , A61P25/00
CPC分类号： C07D471/04 , A61K31/4375
摘要： Provided herein area novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated Syk kinase activity.
摘要翻译：本文提供了区域新颖的化合物类，包含这些化合物的药物组合物和使用这些化合物治疗或预防与异常或失调的Syk激酶活性相关的疾病或病症的方法。

9. 发明申请

US20080108616A1 COMPOUNDS AND COMPOSITIONS AS PROTEIN KINASE INHIBITORS 审中-公开
标题翻译：作为蛋白激酶抑制剂的化合物和组合物
公开(公告)号：US20080108616A1
公开(公告)日：2008-05-08
申请号：US11970278
申请日：2008-01-07
申请人： Qiang Ding , Nathanael Gray , Bing Li , Yi Liu , Tetsuo Uno
发明人： Qiang Ding , Nathanael Gray , Bing Li , Yi Liu , Tetsuo Uno
IPC分类号： C07D487/04 , A61K31/5377 , A61K31/496 , C07D413/14 , C07D403/14 , A61K31/519 , A61P35/00
CPC分类号： C07D487/04
摘要： The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly diseases or disorders that involve abnormal activation of the Abl, BCR-Abl, Bmx, CSK, TrkB, FGFR3, Fes, Lck, B-RAF, C-RAF, MKK6, SAPK2α and SAPK2β kinases.
摘要翻译：本发明提供了一类新颖的化合物，包含这些化合物的药物组合物和使用这些化合物治疗或预防与异常或失调的激酶活性相关的疾病或病症的方法，特别是涉及Abl，BCR-Abl异常活化的疾病或病症，Bmx，CSK，TrkB，FGFR3，Fes，Lck，B-RAF，C-RAF，MKK6，SAPK2alpha和SAPK2β激酶。

10. 发明申请

US20080068410A1 Driving apparatus of inkjet head 有权
标题翻译：喷墨头驱动装置
公开(公告)号：US20080068410A1
公开(公告)日：2008-03-20
申请号：US11901193
申请日：2007-09-14
申请人： Hiroaki Arakawa , Tetsuo Uno , Masakazu Mori
发明人： Hiroaki Arakawa , Tetsuo Uno , Masakazu Mori
IPC分类号： B41J29/38
CPC分类号： B41J2/04581 , B41J2/04521 , B41J2/04541 , B41J2/04573 , B41J2/0458
摘要： An inkjet head driving apparatus, wherein serial data indicating emission or non emission of nozzles respectively for a plurality of heads, is latched and memorized, and the nozzles are driven respectively based on the data memorized, the inkjet head driving apparatus having: an emission timing signal outputting device disposed in common for a plurality of heads so as to output a plurality of emission timing signals in one emission cycle; a setting device disposed respectively for the plurality of the heads so as to select the sequential emission timing signals at which emission starts synchronously, among the emission timing signals outputted from the emission timing signal outputting device in one emission cycle.
摘要翻译：一种喷墨头驱动装置，其中分别指示用于多个头的喷嘴的发射或不发射的串行数据被锁存和存储，并且基于所记录的数据分别驱动喷嘴，该喷墨头驱动装置具有：发射定时信号输出装置，用于多个头共用，以便在一个发射周期中输出多个发射定时信号; 在一个发射周期中，从发射定时信号输出装置输出的发射定时信号中，分别设置用于多个磁头的设定装置，以选择同步发射的顺序发射定时信号。

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