公开(公告)号：US20160102076A1

公开(公告)日：2016-04-14

申请号：US14881930

申请日：2015-10-13

Applicant: Yuhan Corporation

Inventor： Byung-Chul Suh ,  Paresh Devidas Salgaonkar ,  Jaekyoo Lee ,  Jong Sung Koh ,  Ho-Juhn Song ,  In Yong Lee ,  Jaesang Lee ,  Dong Sik Jung ,  Jung-Ho Kim ,  Se-Won Kim

IPC: C07D403/04 ,  C07D409/14 ,  C07D413/14 ,  C07D403/14

CPC classification number: C07D403/04 ,  A61K31/506 ,  C07D403/14 ,  C07D409/14 ,  C07D413/14

Abstract: The present invention provides a new group of protein kinase inhibitors, aminopyrimidine derivatives, and pharmaceutically acceptable salts thereof that are useful for treating cell proliferative disease and disorder such as cancer and immune disease. The present invention provides methods for synthesizing and administering the protein kinase inhibitor compounds. The present invention also provides pharmaceutical formulations comprising at least one of the protein kinase inhibitor compounds together with a pharmaceutically acceptable carrier, diluent or excipient therefore. The invention also provides useful intermediates generated during the syntheses of the aminopyrimidine derivatives.

Abstract translation: 本发明提供了一组可用于治疗细胞增殖性疾病和病症如癌症和免疫疾病的蛋白激酶抑制剂，氨基嘧啶衍生物及其药学上可接受的盐。 本发明提供了合成和施用蛋白激酶抑制剂化合物的方法。 本发明还提供了包含至少一种蛋白激酶抑制剂化合物以及药学上可接受的载体，稀释剂或赋形剂的药物制剂。 本发明还提供了在合成氨基嘧啶衍生物期间产生的有用的中间体。

公开(公告)号：US20020071864A1

公开(公告)日：2002-06-13

申请号：US10016821

申请日：2001-12-07

Applicant: Yuhan Corporation

Inventor： Hyun-Soo Kim ,  Young-Joon Park ,  Dae-Sik Kang

IPC: A61K009/20

CPC classification number: A61K31/4178 ,  A61K9/0007 ,  A61K9/0056 ,  A61K31/167 ,  A61K31/426 ,  A61K31/439 ,  A61K31/4422 ,  A61K31/4468 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/495 ,  A61K31/519

Abstract: The present invention relates to a rapidly disintegrable tablet for oral administration, which disintegrates in the oral cavity within 60 seconds, consisting essentially of (i) a therapeutically effective amount of an active ingredient, (ii) spray-dried mannitol, of which at least 80% has an average particle size over 100 nullm, (iii) crospovidone, and (iv) one or more pharmaceutically acceptable excipients, the tablet containing no microcrystalline cellulose.

Abstract translation: 本发明涉及用于口服给药的快速崩解片剂，其在60秒内在口腔内崩解，基本上由（i）治疗有效量的活性成分，（ii）喷雾干燥的甘露醇至少 80％的平均粒径超过100μm，（iii）交聚维酮，和（iv）一种或多种药学上可接受的赋形剂，该片不含微晶纤维素。

公开(公告)号：US20250066487A1

公开(公告)日：2025-02-27

申请号：US18935875

申请日：2024-11-04

Applicant: ABL Bio Inc. ,  YUHAN CORPORATION

Inventor： Yeryoung YONG ,  Ui-Jung JUNG ,  Hyejin CHUNG ,  Kyeongsu PARK ,  Wonjun SON ,  Yangsoon LEE ,  Yeunju KIM ,  Eunsil SUNG ,  Youngkwang KIM ,  Youngdon PAK ,  Minji PARK ,  Jaehyun EOM ,  Hyoju CHOI ,  Moo Young SONG ,  Na Rae LEE ,  Young Bong PARK ,  Eun-Jung LEE ,  Eun-Jung LEE

IPC: C07K16/28 ,  A61K39/00 ,  A61K39/395

Abstract: Provided are an anti-4-1BB/anti-EGFR bispecific antibody, and a pharmaceutical composition and a method for treating and/or preventing a cancer using the same.

公开(公告)号：US12227478B2

公开(公告)日：2025-02-18

申请号：US17594062

申请日：2020-04-03

Applicant: YUHAN CORPORATION

Inventor： 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: C07D211/56 ,  C07D487/04

Abstract: Provided are a 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：US12168690B2

公开(公告)日：2024-12-17

申请号：US16939472

申请日：2020-07-27

Applicant: ABL Bio Inc. ,  YUHAN CORPORATION

Inventor： Yeryoung Yong ,  Ui-Jung Jung ,  Hyejin Chung ,  Kyeongsu Park ,  Wonjun Son ,  Yangsoon Lee ,  Yeunju Kim ,  Eunsil Sung ,  Youngkwang Kim ,  Youngdon Pak ,  Minji Park ,  Jaehyun Eom ,  Hyoju Choi ,  Moo Young Song ,  Na Rae Lee ,  Young Bong Park ,  Eun-Jung Lee ,  Eun-Jung Lee

IPC: C07K16/28 ,  A61K39/00 ,  A61K39/395

Abstract: Provided are an anti-4-1BB/anti-EGFR bispecific antibody, and a pharmaceutical composition and a method for treating and/or preventing a cancer using the same.

公开(公告)号：US20240174636A1

公开(公告)日：2024-05-30

申请号：US18551894

申请日：2022-03-22

Applicant: YUHAN CORPORATION

Inventor： Gyu-Jin LEE ,  Eui-Chul LEE ,  Sol PARK ,  Dong-Hoon LEE ,  Su-Hwa KIM ,  Jong-Suk PARK ,  Ho-Woong KANG ,  Hyun-Sik YUN

IPC: C07D401/12 ,  A61K31/4709 ,  A61K31/517 ,  C07D215/18 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  C07D498/04 ,  C07D513/04

CPC classification number: C07D401/12 ,  A61K31/4709 ,  A61K31/517 ,  C07D215/18 ,  C07D405/12 ,  C07D413/12 ,  C07D417/12 ,  C07D498/04 ,  C07D513/04

Abstract: Provided are a compound having a cyclohexyl-(alkyl or cycloalkyl-substituted)ethylene-amino-heteroaryl moiety or pharmaceutically acceptable salt thereof, a process for the preparation thereof, a pharmaceutical composition comprising the same and a use thereof, wherein the compound or pharmaceutically acceptable salt thereof not only has excellent inhibitory activity against indoleamine 2,3-dioxygenase (IDO) but also exhibits remarkably high in vivo exposure upon oral administration and therefore the compound or pharmaceutically acceptable salt thereof can be usefully applied for preventing or treating various diseases associated with IDO.

公开(公告)号：US11981658B2

公开(公告)日：2024-05-14

申请号：US17822450

申请日：2022-08-26

Applicant: YUHAN CORPORATION ,  JANSSEN BIOTECH, INC.

Inventor： Byoungmoon Lee ,  Hyunjoo Lee ,  Gyu Jin Lee ,  Su Bin Choi ,  Sol Park ,  Heejun Kim ,  Misong Kim ,  Young Ae Yoon ,  Kwan Hoon Hyun ,  Tae Kyun Kim ,  Jae Young Sim ,  Marian C. Bryan ,  Scott Kuduk ,  James Campbell Robertson

IPC: C07D401/14

CPC classification number: C07D401/14

Abstract: Provided are aminopyridine compounds and pharmaceutically acceptable compositions thereof which exhibit inhibition activity against certain mutated forms of EGFR.

公开(公告)号：US11945798B2

公开(公告)日：2024-04-02

申请号：US17822438

申请日：2022-08-26

Applicant: YUHAN CORPORATION ,  JANSSEN BIOTECH, INC.

Inventor： Hyunjoo Lee ,  Su Bin Choi ,  Young Ae Yoon ,  Kwan Hoon Hyun ,  Jae Young Sim ,  Marian C. Bryan ,  Scott Kuduk ,  James Campbell Robertson ,  Jaekyoo Lee ,  Paresh Devidas Salgaonkar ,  Byung-Chul Suh ,  Jong Sung Koh ,  So Young Hwang

IPC: C07D401/14 ,  C07D413/14

CPC classification number: C07D401/14 ,  C07D413/14

Abstract: Provided are aminopyridine compounds and pharmaceutically acceptable compositions thereof which exhibit inhibition activity against certain mutated forms of EGFR.

公开(公告)号：US11850248B2

公开(公告)日：2023-12-26

申请号：US15931626

申请日：2020-05-14

Applicant: Janssen Biotech, Inc. ,  Yuhan Corporation

Inventor： Seonmi Kang ,  Sewoong Oh

IPC: A61K31/5377 ,  A61P35/00 ,  A61P35/04

CPC classification number: A61K31/5377 ,  A61P35/00 ,  A61P35/04

Abstract: The present invention relates to therapies with 3rd generation EGFR tyrosine kinase inhibitors. Embodiments of the invention relate to the administration of lazertinib to patients diagnosed with non-small cell lung cancer (NSCLC).

公开(公告)号：US11713308B2

公开(公告)日：2023-08-01

申请号：US17368738

申请日：2021-07-06

Applicant: YUHAN CORPORATION

Inventor： Tae Dong Han ,  Hee Jae Tak ,  Eun Kyung Kim ,  Eui Chul Lee ,  Sol Park ,  Hyok Jun Cho ,  Cheol Hee Lim ,  So Young Kim ,  Hyun Ho Choi ,  Da Na Jeong ,  Na Yeon Yang ,  Na Ry Ha

IPC: C07D403/10 ,  C07D249/12 ,  C07D401/04 ,  C07D401/10 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/10 ,  C07D405/14 ,  C07D409/06 ,  C07D409/14 ,  C07D413/14

CPC classification number: C07D403/10 ,  C07D249/12 ,  C07D401/04 ,  C07D401/10 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/10 ,  C07D405/14 ,  C07D409/06 ,  C07D409/14 ,  C07D413/14

Abstract: The present technology provides 3,3-difluoroallylamines or pharmaceutically acceptable salts thereof, preparation processes thereof, pharmaceutical compositions comprising the same, and uses thereof. The 3,3-difluoroallylamines or their pharmaceutically acceptable salts exhibit potent inhibitory activity on VAP-1 and therefore can be usefully applied, e.g., for the treatment and prophylaxis of nonalcoholic hepatosteatosis (NASH).