公开(公告)号：EP2925368A1

公开(公告)日：2015-10-07

申请号：EP13802452.6

申请日：2013-11-26

申请人： Novartis AG

发明人： HU, Qi-Ying ,  IMASE, Hidetomo

IPC分类号： A61K47/48

CPC分类号： A61F5/0006 ,  A61C5/90 ,  A61F5/566 ,  A61K47/542 ,  A61K47/6415 ,  A61K47/646 ,  A61K47/6803 ,  A61K47/6845 ,  A61K47/6849

摘要： The invention provides methods to prepare protein conjugates from proteins having at least two cysteines. In one embodiment, a protein with a disulfide linkage is reduced to provide two free cysteines for reaction with a 1,3-dihaloacetone or similar reactant, linking the sulfur atoms of the two cysteines together. The ketone inserted between the sulfur atoms is then used to form a Schiff base to an aminated payload molecule, 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. The linkage between the sulfur atoms in each case holds the protein or peptide in a constrained conformation, while also providing a convenient place for attaching a payload with good specificity and efficiency.

公开(公告)号：EP2229356A1

公开(公告)日：2010-09-22

申请号：EP08857355.5

申请日：2008-12-01

申请人： Novartis AG

发明人： MOGI, Muneto ,  KAWANAMI, Toshio ,  YAMADA, Ken ,  YASOSHIMA, Kayo ,  IMASE, Hidetomo ,  MIYAKE, Takahiro ,  OHMORI, Osamu

IPC分类号： C07D207/14 ,  C07D403/12 ,  C07D403/14 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  A61K31/40 ,  A61P3/06

CPC分类号： C07D207/14 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14

摘要： The present invention provides a compound of formula (I): wherein the variants R1, R2, R3, R4, 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.

公开(公告)号：EP1968941A1

公开(公告)日：2008-09-17

申请号：EP06829878.5

申请日：2006-12-27

申请人： Novartis AG

发明人： SAKAKI, Junichi ,  KISHIDA, Masashi ,  MATSUURA, Naoko ,  UMEMURA, Ichiro ,  KAWAHARA, Eiji ,  YAMADA, Ken ,  KONISHI, Kazuhide ,  IWAKI, Yuki ,  IMASE, Hidetomo ,  MIYAKE, Takahiro

IPC分类号： C07D213/38 ,  C07D213/40 ,  C07D401/12 ,  A61K31/44 ,  A61K31/4439 ,  A61P3/00 ,  A61P9/00

CPC分类号： C07D401/12 ,  C07D213/74 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14

摘要： The present invention relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein the variables are as defined, useful as inhibitors of chlosteryl ester transfer protein.

摘要翻译： 本发明涉及式（I）化合物或其药学上可接受的盐，其中变量如所定义，可用作氯代酯转移蛋白的抑制剂。

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.

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

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

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。

公开(公告)号：EP2925368B1

公开(公告)日：2019-03-27

申请号：EP13802452.6

申请日：2013-11-26

申请人： Novartis AG

发明人： HU, Qi-Ying ,  IMASE, Hidetomo

IPC分类号： A61K47/68 ,  A61K47/54 ,  A61K47/64

公开(公告)号：EP2807183B1

公开(公告)日：2018-02-28

申请号：EP13711953.3

申请日：2013-01-25

申请人： Novartis AG

发明人： GOLOSOV, Andrei ,  GROSCHE, Philipp ,  HU, Qi-Ying ,  IMASE, Hidetomo ,  PARKER, David, Thomas ,  YASOSHIMA, Kayo ,  ZECRI, Frederic ,  ZHAO, Hongjuan

IPC分类号： C07K7/56 ,  C07K14/47 ,  A61K38/12

CPC分类号： A61M16/0816 ,  A61K38/00 ,  A61K38/10 ,  A61M16/0066 ,  A61M16/201 ,  A61M2016/0027 ,  A61M2016/003 ,  A61M2205/35 ,  A61M2205/502 ,  C07K7/08 ,  C07K7/56 ,  C07K7/60

摘要： A pressure support system that comprises a patient circuit, a docking assembly, and a tank. The patient circuit delivers a pressurized flow of breathable gas to a patient. The docking assembly has an inlet and an outlet that is adapted to receive the pressurized flow of breathable gas, and is also adapted to be connected with the patient circuit. The tank is constructed and arranged to be removably connected with the docking assembly, and enables the pressurized flow of breathable gas to pass therethrough. The tank is also adapted to contain a liquid such that a humidity level of the pressurized flow of breathable gas is elevated as the pressurized flow of breathable gas passes therethrough.

公开(公告)号：EP2501678A1

公开(公告)日：2012-09-26

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

摘要： The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein R
1 , R
2 , R
3 , R
4 , R
5 and n are defined herein. The invention also relates to a method for manufacturing compounds of the invention, and their therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.