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21. 发明公开

EP3310813A1 ANTIBODY DRUG CONJUGATES 审中-公开
公开(公告)号：EP3310813A1
公开(公告)日：2018-04-25
申请号：EP16732342.7
申请日：2016-06-17
申请人： Novartis AG
发明人： ABRAMS, Tinya , COHEN, Steven , D'ALESSIO, Joseph Anthony , DAMIANO, Jason , DURR, Clemens , GEIERSTANGER, Bernhard Hubert , HU, Qi-Ying , HUBER, Thomas , IMASE, Hidetomo , JIN, Yunho , MENEZES, Daniel , MILLER, Kathy , MOHSENI, Morvarid , OU, Weijia , RENDAHL, Katherine , UNO, Tetsuo , WAN, Yongqin , WANG, Xing
IPC分类号： C07K16/28 , A61K31/00 , A61K39/395 , A61P35/00
CPC分类号： C07K16/28 , A61K45/06 , A61K47/6803 , A61K47/6849 , A61K2039/505 , C07K2317/21 , C07K2317/24 , C07K2317/33 , C07K2317/34 , C07K2317/52 , C07K2317/522 , C07K2317/524 , C07K2317/526 , C07K2317/55 , C07K2317/73 , C07K2317/76 , C07K2317/92
摘要： This application discloses anti-P-cadherin antibodies, antigen binding fragments thereof, and antibody drug conjugates of said antibodies or antigen binding fragments, particularly antibody drug conjugates comprising anti-P-cadherin antibodies conjugated to auristatin analogs. The invention also relates to methods of treating cancer using the antibody drug conjugates. Also disclosed herein are methods of making the antibodies, antigen binding fragments, and antibody drug conjugates, and methods of using the antibodies and antigen binding fragments as diagnostic reagents.

22. 发明授权

EP2501678B1 ARYL-PYRIDINE DERIVATIVES AS ALDOSTERONE SYNTHASE INHIBITORS 有权
标题翻译：芳基吡啶衍生物AS醛固酮合酶抑制剂
公开(公告)号：EP2501678B1
公开(公告)日：2015-09-23
申请号：EP10785016.6
申请日：2010-11-16
申请人： Novartis AG
发明人： ALLAN, Martin , CHAMOIN, Sylvie , HU, Qi-Ying , IMASE, Hidetomo , PAPILLON, Julien
IPC分类号： C07D213/30 , C07D213/57 , C07D213/61 , C07D401/04 , C07D405/04 , C07D409/04 , A61K31/44 , A61K31/443 , A61K31/4436 , A61K31/4439 , A61P9/12
CPC分类号： C07D213/57 , C07D213/30 , C07D213/61 , C07D401/04 , C07D405/04 , C07D409/04

23. 发明授权

EP2049517B1 AMINO-PIPERIDINE DERIVATIVES AS CETP INHIBITORS 有权
标题翻译：氨基哌啶衍生物作为CETP抑制剂
公开(公告)号：EP2049517B1
公开(公告)日：2013-11-27
申请号：EP07786158.1
申请日：2007-07-18
申请人： Novartis AG
发明人： IMASE, Hidetomo , IWAKI, Yuki , KAWANAMI, Toshio , MIYAKE, Takahiro , MOGI, Muneto , OHMORI, Osamu , QIN, Hongbo , UMEMURA, Ichiro , YAMADA, Ken , YASOSHIMA, Kayo
IPC分类号： C07D401/12 , C07D311/30 , A61K31/455 , A61P9/00 , C07D211/58 , C07D401/14 , C07D413/14 , C07D417/14
CPC分类号： C07D211/58 , C07D401/12 , C07D401/14 , C07D413/14 , C07D417/14

24. 发明公开

EP2084149A1 ORGANIC COMPOUNDS 审中-公开
标题翻译：有机化合物
公开(公告)号：EP2084149A1
公开(公告)日：2009-08-05
申请号：EP07822551.3
申请日：2007-11-13
申请人： NOVARTIS AG
发明人： IMASE, Hidetomo , KISHIDA, Masashi
IPC分类号： C07D401/12 , C07D401/14 , A61K31/4439 , A61K31/4709 , A61P9/00 , A61P3/00
CPC分类号： C07D401/12 , C07D401/14
摘要： The present invention provides a compound of formula (I), said compound is an inhibitor of CETP, and thus can be employed for the treatment of a disorder or disease mediated by CETP or responsive to the inhibition of CETP.
摘要翻译：本发明提供了式（I）化合物，所述化合物是CETP抑制剂，因此可用于治疗由CETP介导的或响应于CETP抑制的病症或疾病。

26. 发明授权

EP3074048B1 METHODS FOR OXIME CONJUGATION TO KETONE-MODIFIED POLYPEPTIDES 有权
公开(公告)号：EP3074048B1
公开(公告)日：2019-03-06
申请号：EP14815051.9
申请日：2014-11-24
申请人： Novartis AG
发明人： HU, Qi-Ying , IMASE, Hidetomo
IPC分类号： A61K47/54 , A61K47/62 , A61K47/64

27. 发明公开

EP3074048A1 METHODS FOR OXIME CONJUGATION TO KETONE-MODIFIED POLYPEPTIDES 审中-公开
标题翻译：用于OXIME缀合至酮改性的多肽的方法
公开(公告)号：EP3074048A1
公开(公告)日：2016-10-05
申请号：EP14815051.9
申请日：2014-11-24
申请人： Novartis AG
发明人： HU, Qi-Ying , IMASE, Hidetomo
IPC分类号： A61K47/48
CPC分类号： C07K7/64 , A61K47/542 , A61K47/62 , A61K47/646 , A61K47/68 , A61K47/6803 , A61K47/6849 , C07K1/1133 , C07K2317/40
摘要： The invention provides improved methods to prepare protein conjugates from a ketone-modified protein. In one embodiment, the protein is prepared by linking two free cysteines by reaction with a 1,3-dihaloacetone or similar ketone-containing reactant, linking the sulfur atoms of the two cysteines together. The ketone inserted between the sulfur atoms is then used to form an oxime, thus conjugating the protein to a payload. In another embodiment, two cysteine residues are tied together by reaction with a 1,3-dihaloacetone or similar reactant, and the new ketone is used to form an oxime with a suitable payload molecule, thus conjugating the protein to a payload. The method provides improved reaction conditions for the oxime formation, whereby higher yields and improved product homogeneity are achieved.
摘要翻译：本发明提供了从酮修饰的蛋白质制备蛋白质缀合物的改进方法。在一个实施方案中，通过将两个游离半胱氨酸与1,3-二卤代丙酮或类似的含酮反应物反应，将两个半胱氨酸的硫原子连接在一起来制备蛋白质。插入硫原子之间的酮然后用于形成肟，从而将蛋白质缀合到有效载荷上。在另一个实施方案中，两个半胱氨酸残基通过与1,3-二卤代丙酮或类似的反应物反应而连接在一起，并且新的酮用于与合适的有效负载分子形成肟，由此将蛋白质偶联至有效负载。该方法为肟形成提供改进的反应条件，由此获得更高的收率和改进的产物均匀性。

28. 发明公开

EP2207775A1 4-BENZYLAMINO-1-CARBOXYACYL-PIPERIDINE DERIVATIVES AS CETP INHIBITORS USEFUL FOR THE TREATMENT OF DISEASES SUCH AS HYPERLIPIDEMIA OR ARTERIOSCLEROSIS 有权
标题翻译： 4-苄基氨基-1-羧酰基哌啶作为CETP抑制剂的治疗诸如高脂血症或动脉粥样硬化治疗
公开(公告)号：EP2207775A1
公开(公告)日：2010-07-21
申请号：EP08848438.1
申请日：2008-11-03
申请人： Novartis AG
发明人： MOGI, Muneto , YAMADA, Ken , YASOSHIMA, Kayo , KAWANAMI, Toshio , UMEMURA, Ichiro , IWAKI, Yuki , QIN, Hongbo , IMASE, Hidetomo
IPC分类号： C07D401/12 , C07D401/14 , C07D413/14 , A61K31/5377 , A61P3/06
CPC分类号： C07D401/14 , C07D413/14
摘要： The present invention provides a compound of formula (I): wherein the variants R1, R2, R3, R4, R5, R6, R7 are as defined herein, and wherein said compound is an inhibitor of CETP, and thus can be employed for the treatment of a disorder or disease mediated by CETP or responsive to the inhibition of CETP.

29. 发明公开

EP2049517A1 AMINO-PIPERIDINE DERIVATIVES AS CETP INHIBITORS 有权
标题翻译：氨基哌啶衍生物作为CETP抑制剂
公开(公告)号：EP2049517A1
公开(公告)日：2009-04-22
申请号：EP07786158.1
申请日：2007-07-18
申请人： NOVARTIS AG
发明人： IMASE, Hidetomo , IWAKI, Yuki , KAWANAMI, Toshio , MIYAKE, Takahiro , MOGI, Muneto , OHMORI, Osamu , QIN, Hongbo , UMEMURA, Ichiro , YAMADA, Ken , YASOSHIMA, Kayo
IPC分类号： C07D401/12 , C07D311/30 , A61K31/455 , A61P9/00 , C07D211/58 , C07D401/14 , C07D413/14 , C07D417/14
CPC分类号： C07D211/58 , C07D401/12 , C07D401/14 , C07D413/14 , C07D417/14
摘要： The present invention provides a compound of formula (I), wherein the variants R1, R2, R3, R4, R5, R6, R7 are as defined herein, and wherein said compound is an inhibitor of CETP, and thus can be employed for the treatment of a disorder or disease mediated by CETP or responsive to the inhibition of CETP.
摘要翻译：本发明提供了式（I）化合物，其中变体R1，R2，R3，R4，R5，R6，R7如本文所定义，并且其中所述化合物是CETP的抑制剂，因此可用于治疗由CETP介导的或响应于CETP抑制的病症或疾病。

30. 发明授权

EP2993169B1 ARYL-PYRIDINE DERIVATIVES AS ALDOSTERONE SYNTHASE INHIBITORS 失效
标题翻译：芳基 - 吡啶衍生物作为醛固酮合成酶抑制剂
公开(公告)号：EP2993169B1
公开(公告)日：2017-12-20
申请号：EP15182564.3
申请日：2010-11-16
申请人： Novartis AG
发明人： ALLAN, Martin , CHAMOIN, Sylvie , HU, Qi-Ying , IMASE, Hidetomo , PAPILLON, Julien
IPC分类号： C07D213/30 , C07D213/57 , C07D213/61 , C07D401/04 , C07D405/04 , C07D409/04 , A61K31/44 , A61K31/443 , A61K31/4436 , A61K31/4439 , A61P9/12
CPC分类号： C07D213/57 , C07D213/30 , C07D213/61 , C07D401/04 , C07D405/04 , C07D409/04
摘要： The present invention provides a compound of formula I; or a pharmaceutically acceptable salt thereof, wherein A, R 1 , R 2 , R 3 , R 4 , R 5 and n are as defined herein and the use of such compounds for the treatment of disorders or diseases mediated by aldosterone synthase. The invention also relates to pharmaceutical compositions and combinations comprising compounds of formula I.

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