公开(公告)号：US11840574B2

公开(公告)日：2023-12-12

申请号：US16492780

申请日：2018-02-08

申请人： DONG-A ST CO., LTD.

发明人： Hyounmie Doh ,  Dongsop Lee ,  Hanyoung Lee ,  Yoojin Kim ,  Kyungmi Han ,  Eunee Jung ,  Donghyeon Kim ,  Eongsup Song ,  Kum-Joo Shin ,  Soyon Woo

IPC分类号： C07K16/28 ,  A61P35/00 ,  C12N15/63

CPC分类号： C07K16/2878 ,  A61P35/00 ,  C12N15/63 ,  C07K2317/565 ,  C07K2317/73

摘要： The present invention relates to an antibody that specifically binds to death receptor 5 (DR5) and has a function of killing cancer cells. Specifically, provided are an anti-DR5 antibody or antigen-binding fragment thereof, and a use of the antibody or antigen-binding fragment for preventing or treating cancer. The present invention is characterized in that the anti-DR5 antibody or antigen-binding fragment thereof is improved in terms of affinity to DR5, stability, and an effect of killing cancer cells.

公开(公告)号：US20230117286A1

公开(公告)日：2023-04-20

申请号：US17905912

申请日：2021-03-10

申请人： DONG-A ST CO., LTD.

发明人： Mi-Kyung KIM ,  Hansu PARK ,  Seung Ho LEE

IPC分类号： A61K31/506 ,  A61K31/192 ,  A61K31/495 ,  A61K31/4985 ,  A61K31/575 ,  A61K31/55 ,  A61P1/16 ,  A61K31/519

摘要： The present invention relates to a pharmaceutical composition for preventing or treating nonalcoholic fatty liver disease. The pharmaceutical composition according to the present invention exhibits excellent effects of improving lipid metabolism, reducing fat accumulation in liver tissues and inhibiting histological damage caused by inflammation and fibrosis of liver tissues, and thus can be effectively used as a use of preventing or treating nonalcoholic fatty liver disease.

公开(公告)号：US10894768B2

公开(公告)日：2021-01-19

申请号：US16328492

申请日：2016-08-26

申请人： Dong-A St Co., Ltd.

发明人： Woo Young Kwak ,  Chang-Yong Shin ,  Punna Reddy Ullapu ,  Sun-Ho Choi ,  Min-Jung Lee ,  Ji-Su Kim

IPC分类号： C07D207/09 ,  A61K31/40 ,  C07D207/08

摘要： The present invention relates to a novel salt of (R)-(1-methylpyrrolidine-3-yl)methyl(3′-chloro-4′-fluoro-[1,1′-biphenyl]-2-yl)carbamate and a crystal form thereof. Also, the novel salt of (R)-(1-methylpyrrolidine-3-yl)methyl(3′-chloro-4′-fluoro-[1,1′-biphenyl]-2-yl)carbamate and the crystal form thereof according to examples of the present invention have remarkably excellent stability, hygroscopicity and solubility.

公开(公告)号：US20180086709A1

公开(公告)日：2018-03-29

申请号：US15718474

申请日：2017-09-28

申请人： Dong-A St Co., Ltd.

发明人： Sun-Ho Choi ,  Weon-Bin Im ,  Sung-Hak Choi ,  Chong-Hwan Cho ,  Ho-Sang Moon ,  Jung-Sang Park ,  Min-Jung Lee ,  Hyun-Jung Sung ,  Jun-Hwan Moon ,  Seung-Hyun Song ,  Hyung-Keun Lee ,  Ji-Hoon Choi ,  Cheon-Hyoung Park ,  Yoon-Jung Kim ,  Jin-Hyuk Kim

IPC分类号： C07D211/70 ,  C07D401/10 ,  C07D409/10 ,  C07D405/10 ,  C07D401/04

CPC分类号： C07D211/70 ,  C07D401/04 ,  C07D401/10 ,  C07D405/10 ,  C07D409/10

摘要： The present disclosure relates to a novel tetrahydropyridine derivative compound, a stereoisomer thereof, or a pharmaceutically acceptable salt thereof, methods for preparing the compounds, methods for inhibiting UDP-3-O—(R-3-hydroxymyristoyl)-N-acetylglucosamine deacetylase (LpxC), methods for treating Gram-negative bacterial infections, the use of the compounds for the preparation of therapeutic medicaments for treating Gram-negative bacterial infections, and pharmaceutical compositions for prevention or treatment of Gram-negative bacterial infections, which contain the compounds. The compounds represented by formula I, stereoisomers thereof or pharmaceutically acceptable salts thereof according to the present disclosure can exhibit excellent effects on the treatment bacterial infections.

公开(公告)号：US20170340638A1

公开(公告)日：2017-11-30

申请号：US15527246

申请日：2015-11-06

申请人： DONG-A ST CO., LTD

发明人： Mi-Won SOHN ,  Sun-Woo JANG ,  Dong-Han WON ,  Yong-Min KIM ,  Hyung-Don HWANG ,  Dong-Hun MIN

IPC分类号： A61K31/519 ,  A61K9/08 ,  A61K31/16 ,  A61K31/185

CPC分类号： A61K31/519 ,  A61K9/0019 ,  A61K9/08 ,  A61K31/16 ,  A61K31/185 ,  A61K47/02 ,  A61K47/18

摘要： Provided is a composition of a ready-to-use injectable solution comprising pemetrexed or pharmaceutically acceptable salts thereof, containing pemetrexed; anhydrous sodium sulfite; and N-acetyl-L-cystein. With respect to use as an injectable preparation. The ready-to-use injectable solution composition is suitable for effective administration of pemetrexed since a melting process of main ingredients is not necessary before administration, and the composition can be used by being diluted immediately in a perfusate. In addition, the properties of the composition do not change even in long-term storage, and pharmaceutical stability is significantly improved by inhibiting related substances below a reference, whereby the composition can be stored in a liquid preparation state.

公开(公告)号：US09163043B2

公开(公告)日：2015-10-20

申请号：US13863216

申请日：2013-04-15

申请人： DONG-A ST CO., LTD.

发明人： Jae Keol Rhee ,  Weon Bin Im ,  Chong Hwan Cho ,  Sung Hak Choi ,  Tae Ho Lee

IPC分类号： C07D263/32 ,  C07D413/14 ,  C07D417/10 ,  C07F9/6558 ,  C07D417/14 ,  C07F9/653

CPC分类号： A61K31/4439 ,  A61K31/675 ,  C07D263/32 ,  C07D413/14 ,  C07D417/10 ,  C07D417/14 ,  C07F9/653 ,  C07F9/65583

摘要： The present invention relates to novel derivatives of oxazolidinone, a method thereof and pharmaceutical compositions comprising the derivatives for use in an antibiotic. The oxazolidinone derivatives of the present invention show inhibitory activity against a broad spectrum of bacteria and lower toxicity. The prodrugs, prepared by reacting the compound having hydroxyl group with amino acid or phosphate, have an excellent efficiency on solubility thereof against water. Further, the derivatives of the present invention may exert potent antibacterial activity versus various human and animal pathogens, including Gram-positive bacteria such as Staphylococi, Enterococci and Streptococi, anaerobic microorganisms such as Bacteroides and Clostridia, and acid-resistant microorganisms such as Mycobacterium tuberculosis and Mycobacterium avium. Accordingly, the compositions comprising the oxazolidinone are used in an antibiotic.

摘要翻译： 本发明涉及恶唑烷酮的新衍生物，其方法和药物组合物，其包含用于抗生素的衍生物。 本发明的恶唑烷酮衍生物显示出对广谱细菌的抑制活性和较低的毒性。 通过使具有羟基的化合物与氨基酸或磷酸酯反应制备的前药在对水的溶解性方面具有优异的效果。 此外，本发明的衍生物可以对各种人和动物病原体（包括葡萄球菌，肠球菌和链球菌）等革兰阳性菌，拟杆菌和梭菌等厌氧微生物和结核分枝杆菌等耐酸微生物产生有效的抗菌活性 和鸟分枝杆菌。 因此，包含恶唑烷酮的组合​​物用于抗生素中。

公开(公告)号：US20130281492A1

公开(公告)日：2013-10-24

申请号：US13863216

申请日：2013-04-15

申请人： DONG-A ST CO., LTD.

发明人： Jae Keol Rhee ,  Weon Bin Im ,  Chong Hwan Cho ,  Sung Hak Choi ,  Tae Ho Lee

IPC分类号： C07D413/14

CPC分类号： A61K31/4439 ,  A61K31/675 ,  C07D263/32 ,  C07D413/14 ,  C07D417/10 ,  C07D417/14 ,  C07F9/653 ,  C07F9/65583

摘要： The present invention relates to novel derivatives of oxazolidinone, a method thereof and pharmaceutical compositions comprising the derivatives for use in an antibiotic. The oxazolidinone derivatives of the present invention show inhibitory activity against a broad spectrum of bacteria and lower toxicity. The prodrugs, prepared by reacting the compound having hydroxyl group with amino acid or phosphate, have an excellent efficiency on solubility thereof against water. Further, the derivatives of the present invention may exert potent antibacterial activity versus various human and animal pathogens, including Gram-positive bacteria such as Staphylococi, Enterococci and Streptococi, anaerobic microorganisms such as Bacteroides and Clostridia, and acid-resistant microorganisms such as Mycobacterium tuberculosis and Mycobacterium avium. Accordingly, the compositions comprising the oxazolidinone are used in an antibiotic.

摘要翻译： 本发明涉及恶唑烷酮的新衍生物，其方法和药物组合物，其包含用于抗生素的衍生物。 本发明的恶唑烷酮衍生物显示出对广谱细菌的抑制活性和较低的毒性。 通过使具有羟基的化合物与氨基酸或磷酸酯反应制备的前药在对水的溶解性方面具有优异的效果。 此外，本发明的衍生物可以对各种人和动物病原体（包括葡萄球菌，肠球菌和链球菌）等革兰阳性菌，拟杆菌和梭菌等厌氧微生物和结核分枝杆菌等耐酸微生物产生有效的抗菌活性 和鸟分枝杆菌。 因此，包含恶唑烷酮的组合​​物用于抗生素中。

公开(公告)号：US12115159B2

公开(公告)日：2024-10-15

申请号：US17275555

申请日：2019-09-11

申请人： DONG-A ST CO., LTD.

发明人： Mi-Kyung Kim ,  Bo Ram Lee ,  Hansu Park ,  Seung Ho Lee ,  Yu Na Chae

IPC分类号： A61K31/506 ,  A23L33/10 ,  A61P1/06

CPC分类号： A61K31/506 ,  A23L33/10 ,  A61P1/06

摘要： The present invention pertains to a pharmaceutical composition for preventing or treating non-alcoholic fatty liver disease, the composition containing G protein coupled receptor 119 (GPR119) ligand as an active ingredient. The pharmaceutical composition according to the present invention exhibits the excellent effects of improving lipid metabolism, reducing fat accumulation in liver tissues, and preventing histological damage caused by inflammation and fibrosis in liver tissues, and can thus be useful in preventing or treating non-alcoholic fatty liver disease.

公开(公告)号：US20230201131A1

公开(公告)日：2023-06-29

申请号：US17924781

申请日：2021-05-12

申请人： DONG-A ST CO., LTD. ,  KM TRANSDERM LTD.

发明人： Sun-Woo JANG ,  Chang-Yell SHIN ,  Hae-Sun KIM ,  Kwang-Ho CHA ,  Hyun-jung KIM ,  Sang-Min HYUN ,  Masaoki GOTO

IPC分类号： A61K9/70 ,  A61K31/445 ,  A61K47/16 ,  A61K47/20 ,  A61K47/22

CPC分类号： A61K9/7038 ,  A61K31/445 ,  A61K47/16 ,  A61K47/20 ,  A61K47/22

摘要： A percutaneous absorption preparation for the treatment of dementia wherein the drug-containing layer contains donepezil or a pharmaceutically acceptable salt thereof as an active ingredient and a stabilizer that is either (i) a mixture of a thiocyanate salt and a compound selected from the group consisting of tea catechin, (+)-catechin, epigallocatechin gallate, ascorbic acid, and isoascorbic acid, or (ii) a mixture of monothioglycerol and a compound selected from the group consisting of tea catechin, (+)-catechin, epigallocatechin gallate, and ascorbic acid is disclosed. The percutaneous absorption preparation meets the criteria of Procedure 1 and Procedure 2 of the U.S. Pharmacopoeia in short-term stress test (70° C. 48 hours storage), long-term accelerated test 1 (40° C. relative humidity 75% 1 month storage), and long-term accelerated test 2 (40° C. relative humidity 75% 3 months storage), and exhibits improved stability for long-term preservation.

公开(公告)号：US20230133381A1

公开(公告)日：2023-05-04

申请号：US16492780

申请日：2018-02-08

申请人： DONG-A ST CO., LTD.

发明人： Hyounmie DOH ,  Dongsop LEE ,  Hanyoung LEE ,  Yoojin KIM ,  Kyungmi HAN ,  Eunee JUNG ,  Donghyeon KIM ,  Eongsup SONG ,  Kum-Joo SHIN ,  Soyon WOO

IPC分类号： C07K16/28 ,  C12N15/63 ,  A61P35/00

摘要： The present invention relates to an antibody that specifically binds to death receptor 5 (DR5) and has a function of killing cancer cells. Specifically, provided are an anti-DR5 antibody or antigen-binding fragment thereof, and a use of the antibody or antigen-binding fragment for preventing or treating cancer. The present invention is characterized in that the anti-DR5 antibody or antigen-binding fragment thereof is improved in terms of affinity to DR5, stability, and an effect of killing cancer cells.