公开(公告)号：US11479596B2

公开(公告)日：2022-10-25

申请号：US17256296

申请日：2019-07-24

申请人： YUHAN CORPORATION ,  INDUSTRY-ACADEMIC COOPERATION FOUNDATION, YONSEI UNIVERSITY

发明人： Moo Young Song ,  Taejin Yoon ,  Jung-Sun Lee ,  Byung Hyun Choi ,  In Hwan Lim ,  Man Sil Park ,  Jin-Hyoung Lee ,  Hyoung Sig Seo ,  Hyeon Woo Kang ,  Sung Ho Kim ,  Eun Jig Lee ,  Jin Sook Yoon ,  Cheol Ryong Ku

IPC分类号： A61K38/17 ,  A61K47/68 ,  C07K14/72 ,  C07K19/00 ,  A61K47/64 ,  A61K38/00

摘要： Disclosed are a fusion protein comprising a thyrotropin receptor (TSHR) fragment and the use thereof. More specifically, disclosed are a fusion protein comprising a TSHR fragment comprising an extracellular domain of a wild-type TSHR and having a substitution of an amino acid at specific position and an immunoglobulin Fc region or a carboxy-terminal cap (C-CAP), and the use thereof. The fusion protein has improved pharmaceutical efficacy, in-vivo persistence and protein stability and a pharmaceutical composition containing the fusion protein as an active ingredient is useful as a therapeutic agent or diagnostic reagent for the alleviation of Graves' disease and Graves' ophthalmopathy.

公开(公告)号：USD965985S1

公开(公告)日：2022-10-11

申请号：US29751733

申请日：2020-09-23

申请人： YUHAN CORPORATION

设计人： Sung Jin Lee

公开(公告)号：US20220144774A1

公开(公告)日：2022-05-12

申请号：US17594062

申请日：2020-04-03

申请人： YUHAN CORPORATION

发明人： Sang-Ho OH ,  Doo-Byung LEE ,  Kyoung-Chan KWON ,  Sang-Won KIM ,  Hyo-Ick HWANG ,  Kyeong-Sill LEE ,  Ik-Su JO ,  Ji-Hye CHOI ,  Sung-Hee CHO ,  Su-Young LEE

IPC分类号： C07D211/56 ,  C07D487/04

摘要： Provided are a novel process for preparing (3R,4R)-1-benzyl-N,4-dimethylpiperidin-3-amine or a salt thereof, which is an intermediate useful for the preparation of tofacitinib, an intermediate used in the process, i.e., isopropanol solvate of methyl ((3R,4R)-1-benzyl-4-methylpiperidin-3-yl)carbamate dibenzoyl-L-tartrate, an intermediate, having excellent stability, useful for the preparation of tofacitinib, i.e., (3R,4R)-1-benzyl-N,4-dimethylpiperidin-3-amine acetate, and a process for preparing tofacitinib or a pharmaceutically acceptable salt thereof.

公开(公告)号：US20220002367A1

公开(公告)日：2022-01-06

申请号：US17478600

申请日：2021-09-17

申请人： YUHAN CORPORATION

发明人： Jun Hwan KIM ,  Seyoung LIM ,  Minji SEO ,  Hyun Ho CHOI ,  Dohoon KIM ,  Mi Kyeong JU ,  Ju-Young PARK ,  Byung Hyun CHOI ,  Jun Kyung LEE ,  Jong Gyun KIM ,  Su Youn NAM

IPC分类号： C07K14/50 ,  A61P1/16 ,  A61P3/04 ,  A61P3/10

摘要： A fusion protein comprises an FGF21 mutant protein and an Fc region of an immunoglobulin. The fusion protein exhibits improved pharmacological efficacy, in vivo duration and protein stability. A pharmaceutical composition containing the fusion protein as an active ingredient may be effectively used as a therapeutic agent for diabetes, obesity, dyslipidemia, metabolic syndrome, non-alcoholic fatty liver disease or non-alcoholic steatohepatitis.

公开(公告)号：US11142557B2

公开(公告)日：2021-10-12

申请号：US15768616

申请日：2016-10-28

申请人： YUHAN CORPORATION

发明人： Jun Hwan Kim ,  Seyoung Lim ,  Minji Seo ,  Hyun Ho Choi ,  Dohoon Kim ,  Mi Kyeong Ju ,  Ju-Young Park ,  Byung Hyun Choi ,  Jun Kyung Lee ,  Jong Gyun Kim ,  Su Youn Nam

IPC分类号： A61K38/18 ,  C07K14/50 ,  A61P1/16 ,  A61P3/04 ,  A61P3/10

摘要： The present invention provides a fusion protein comprising an FGF21 mutant protein and an Fc region of an immunoglobulin. The fusion protein according to the present invention exhibits improved pharmacological efficacy, in vivo duration and protein stability, and a pharmaceutical composition comprising the fusion protein as an active ingredient may be effectively used as a therapeutic agent for diabetes, obesity, dyslipidemia, metabolic syndrome, non-alcoholic fatty liver disease or non-alcoholic steatohepatitis.

公开(公告)号：US20210269427A1

公开(公告)日：2021-09-02

申请号：US17115037

申请日：2020-12-08

申请人： Yuhan Corporation

发明人： Sang-Ho Oh ,  Ja-Heouk Khoo ,  Jong-Chul Lim ,  Seong-Ran Lee ,  Hyun Ju ,  Woo-Seob Shin ,  Dae-Gyu Park ,  Su-Min Park ,  Yoon-Ah Hwang

IPC分类号： C07D413/14

摘要： The present invention provides an improved process for preparing an aminopyrimidine derivative or pharmaceutically acceptable salt thereof having a selective inhibitory activity against protein kinases, especially against the protein kinases for mutant epidermal growth factor receptors. Additional, the present invention provides novel intermediates useful for said process and processes for preparing the same.

公开(公告)号：US11046742B2

公开(公告)日：2021-06-29

申请号：US16097572

申请日：2017-04-19

申请人： YUHAN CORPORATION

发明人： Su Youn Nam ,  Jong Gyun Kim ,  Byung Hyun Choi ,  June Hyung Lee ,  Ju Young Park ,  Jun Kyung Lee ,  Na Rae Lee ,  Ki Hong Kim ,  Seul Gi Kim ,  Se Woong Oh ,  Seung Yub Shin ,  Ho Woong Kang ,  Su Jin Ahn ,  Soo Yong Chung

IPC分类号： C07K14/52 ,  C07K19/00 ,  C12N15/09 ,  C12N15/11 ,  C12N15/63 ,  A61K38/19 ,  A61K47/68 ,  A61P35/00 ,  A61K38/00 ,  A61K47/50

摘要： Provided are a fusion protein having a CCL3 variant with improved in vivo persistency, protein stability and pharmacological activity and a use thereof, more particularly, a fusion protein comprising a CCL3 variant and an immunoglobulin Fc region and a use thereof as a therapeutic agent for lymphopenia, cancer or infection, in which an N-terminal amino acid of a wild-type CCL3α or CCL3β is deleted and an amino acid at a specific position is substituted with a different amino acid at the same position of the wild-type CCL3α or CCL3β in the CCL3 variant.

公开(公告)号：US20210147368A1

公开(公告)日：2021-05-20

申请号：US17104557

申请日：2020-11-25

申请人： YUHAN CORPORATION

发明人： Tae Dong HAN ,  Hee Jae TAK ,  Eun Kyung KIM ,  Su Bin CHOI ,  Dong Hoon KIM ,  Sol PARK ,  Eun Hye JUNG ,  Hyun Ho CHOI ,  Tae Wang KIM ,  Mi Kyeong JU ,  Na Ry HA

IPC分类号： C07D249/08 ,  C07D401/04 ,  C07D403/04 ,  C07D417/04 ,  C07D409/10 ,  C07D405/10 ,  C07D407/14 ,  C07D401/10 ,  C07D403/10 ,  C07D401/14 ,  C07D405/14 ,  C07D417/14 ,  C07D413/14 ,  C07D413/10 ,  C07D417/10 ,  C07D249/12 ,  C07D403/14

摘要： The present technology provides aryl or heteroaryl triazolone derivatives or pharmaceutically acceptable salts thereof, preparation processes thereof, pharmaceutical compositions comprising the same, and the use thereof. The aryl or heteroaryl triazolone derivatives or their pharmaceutically acceptable salts exhibit selective inhibitory activity on VAP-1 and therefore can be usefully applied, e.g., for the treatment and prophylaxis of nonalcoholic hepatosteatosis (NASH).

公开(公告)号：US20210139461A1

公开(公告)日：2021-05-13

申请号：US16605944

申请日：2018-04-18

申请人： Yuhan Corporation

发明人： Sang Ho OH ,  Jong Gyun KIM ,  Se-Woong OH ,  Tae Dong HAN ,  Soo Yong CHUNG ,  Seong Ran LEE ,  Kyeong Bae KIM ,  Young Sung LEE ,  Woo Seob SHIN ,  Hyun JU ,  Jeong Ki KANG ,  Su Min PARK ,  Dong Kyun KIM

IPC分类号： C07D403/04 ,  C07C309/04 ,  C07C303/22

摘要： The present invention relates to novel mesylate salt of N-(5-(4-(4-((dimethylamino)methyl)-3-phenyl-1H-pyrazol-1-yppyrimidine-2-ylamino)-4-methoxy-2-morpholinophenyl)acrylamide, a novel crystalline form thereof, and a process for preparing the same. More specifically, the present invention relates to mesylate salt of N-(5-(4-(4-((dimethylamino)methyl)-3-phenyl-1H-pyrazol-1-yl)pyrimidine-2-ylamino)-4-methoxy-2-morpholinophenyl)acrylamide, which is excellent in stability, solubility, and bioavailability when it is administered not only alone but also in combination with other drugs and which has a high purity, a crystalline form thereof, and a process for preparing the same.

公开(公告)号：US20210087268A1

公开(公告)日：2021-03-25

申请号：US16970351

申请日：2019-02-28

申请人： YUHAN CORPORATION

发明人： Kwang-Hoon LEE ,  June Hyung LEE ,  Na Rae LEE ,  Eunjeong JEONG ,  Young Bong PARK ,  Nakho CHANG ,  Eun-Jung LEE ,  Ki Hong KIM ,  Sunghyun CHOI ,  Byung Hyun CHOI ,  Ju Young PARK ,  Moo Young SONG ,  Jong-Seo LEE ,  Kyu-Tae KIM ,  Bong-Kook KO

IPC分类号： C07K16/28

摘要： Disclosed are a novel antibody specifically binding to the tumor-immunosuppressant, TIGIT (T cell immunoglobulin and immunoreceptor tyrosine-based inhibitory motif [ITIM] domain) or an antigen-binding fragment thereof, a nucleic acid encoding the antibody or the antigen-binding fragment thereof, a vector and a host cell including the nucleic acid, a method for producing the antibody or the antigen-binding fragment thereof, a pharmaceutical composition containing the antibody or the antigen-binding fragment thereof as an active ingredient, and uses of the pharmaceutical composition.
The antibody specifically binding to TIGIT or the antigen-binding fragment thereof and the pharmaceutical composition containing the same as an active ingredient are preferably used for the treatment of cancer or tumors.