公开(公告)号：US20190382390A1

公开(公告)日：2019-12-19

申请号：US16557180

申请日：2019-08-30

Applicant: DAEWOONG PHARMACEUTICAL CO., LTD. ,  GREEN CROSS CORPORATION

Inventor： Hee-kyoon YOON ,  Se-Hwan PARK ,  Ji-sung YOON ,  Soongyu CHOI ,  Hee Jeong SEO ,  Eun-Jung PARK ,  Younggyu KONG ,  Kwang-Seop SONG ,  Min Ju KIM ,  So Ok PARK

IPC: C07D409/04 ,  C07D407/04 ,  B01D9/00

Abstract: The present invention relates to an improved method for producing a diphenylmethane derivative which is effective as a sodium-dependent glucose cotransporter (SGLT) inhibitor, the method being carried out by means of a convergent synthesis method in which each major group is separately synthesized and then coupled. As such, in comparison to a linear synthesis method disclosed in existing documents, the synthesis pathway is compact and yield can be increased, and risk factors inherent in the linear synthesis pathway can be reduced. Furthermore, the crystal form of the compound produced according to the method has superb physicochemical characteristics, and thus can be effectively utilized in fields such as pharmaceutical manufacturing.

公开(公告)号：US20190169174A1

公开(公告)日：2019-06-06

申请号：US16310005

申请日：2017-06-15

Applicant: DAEWOONG PHARMACEUTICAL CO., LTD. ,  GREEN CROSS CORPORATION

Inventor： Hee-kyoon YOON ,  Se-Hwan PARK ,  Ji-Sung YOON ,  Soongyu CHOI ,  Hee Jeong SEO ,  Eun-Jung PARK ,  Younggyu KONG ,  Kwang-Seop SONG ,  Min Ju KIM ,  So Ok PARK

IPC: C07D409/04 ,  C07D407/04 ,  B01D9/00

Abstract: The present invention relates to an improved method for producing a diphenylmethane derivative which is effective as a sodium-dependent glucose cotransporter (SGLT) inhibitor, the method being carried out by means of a convergent synthesis method in which each major group is separately synthesized and then coupled. As such, in comparison to a linear synthesis method disclosed in existing documents, the synthesis pathway is compact and yield can be increased, and risk factors inherent in the linear synthesis pathway can be reduced. Furthermore, the crystal form of the compound produced according to the method has superb physicochemical characteristics, and thus can be effectively utilized in fields such as pharmaceutical manufacturing.

公开(公告)号：US20160311772A1

公开(公告)日：2016-10-27

申请号：US15134987

申请日：2016-04-21

Applicant: GREEN CROSS CORPORATION

Inventor： Soongyu CHOI ,  Eun-Jung PARK ,  Hee Jeong SEO ,  Younggyu KONG ,  Ickhwan SON ,  Sang-ho MA ,  Man-Young CHA ,  Mi-Soon KIM ,  Kisoo PARK

IPC: C07D209/46 ,  C07D403/04 ,  C07D401/04 ,  C07D403/14 ,  C07D409/12 ,  C07D405/12 ,  C07D409/04 ,  C07D413/04 ,  C07D409/14 ,  C07D403/12 ,  C07D405/06 ,  C07D409/06 ,  C07D471/04 ,  C07D217/24 ,  C07D401/12 ,  C07D417/04

CPC classification number: C07D209/46 ,  C07D209/48 ,  C07D217/24 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14 ,  C07D405/04 ,  C07D405/06 ,  C07D405/12 ,  C07D409/04 ,  C07D409/06 ,  C07D409/12 ,  C07D409/14 ,  C07D413/04 ,  C07D417/04 ,  C07D471/04

Abstract: Provided is a compound of formula (I) as a TNIK (Traf2- and NCK-interacting kinase), IKKε (I-kappa-B kinase epsilon) and TBK1 (TANK-binding kinase 1) inhibitor; the compound according to the present invention effectively inhibits TNIK, IKKε and TBK1, and thus is useful not only as an anticancer agent for the treatment of various cancers including colorectal cancer, breast cancer, CNS cancer, colon cancer, non-small cell lung cancer, kidney cancer, prostate cancer, ovarian cancer, uterus cancer, stomach cancer, liver cancer, skin cancer, lung cancer, brain cancer, bladder cancer, esophageal cancer, pancreatic cancer, thyroid cancer, head and neck cancer, squamous cell carcinoma, osteosarcoma, B-cell or T-cell lymphoma, acute or chronic leukemia and multiple myeloma, but as a therapeutic agent for chronic inflammation.

Abstract translation: 提供作为TNIK（Traf2-和NCK相互作用激酶），IKKε（I-κB激酶ε）和TBK1（TANK结合激酶1）抑制剂的式（I）化合物; 根据本发明的化合物有效地抑制TNIK，IKKε和TBK1，因此不仅可用作治疗各种癌症的抗癌剂，包括结肠直肠癌，乳腺癌，CNS癌，结肠癌，非小细胞肺癌 ，肾癌，前列腺癌，卵巢癌，子宫癌，胃癌，肝癌，皮肤癌，肺癌，脑癌，膀胱癌，食管癌，胰腺癌，甲状腺癌，头颈癌，鳞状细胞癌，骨肉瘤 ，B细胞或T细胞淋巴瘤，急性或慢性白血病和多发性骨髓瘤，但作为慢性炎症的治疗剂。

公开(公告)号：US20140274918A1

公开(公告)日：2014-09-18

申请号：US13845466

申请日：2013-03-18

Applicant: GREEN CROSS CORPORATION

Inventor： Soongyu CHOI ,  Jae Eun KIM ,  Kwang-Seop SONG ,  Suk Ho LEE ,  Kisoo PARK ,  Hee Jeong SEO ,  Min Ju KIM ,  Eun-Jung PARK ,  So Ok PARK ,  Younggyu KONG ,  Hyunku KANG ,  Ickhawn SON ,  Myung Eun JUNG ,  Man-Young CHA ,  Hyun Jung KIM ,  Jun Sung LEE ,  Mi-Soon KIM ,  Min Woo LEE ,  Kinam LEE

IPC: C07D309/10 ,  C07D409/04 ,  C07D409/14 ,  C07D407/04

CPC classification number: C07D309/10 ,  C07D407/04 ,  C07D409/04 ,  C07D409/14

Abstract: The present invention relates to a method for dual inhibition of sodium-dependent glucose cotransporter 1 (SGLT1) and sodium-dependent glucose cotransporter 2 (SGLT2) present in the intestine and kidney by using the compound of formula I or a pharmaceutically acceptable salt or a prodrug thereof: wherein ring A, ring B, X and Y have the same meanings as defined in the specification.

Abstract translation: 本发明涉及通过使用式I化合物或其药学上可接受的盐或其药学上可接受的盐或其药学上可接受的盐或其药学上可接受的盐或其盐 其前药：其中环A，环B，X和Y具有与说明书中定义相同的含义。

公开(公告)号：US20160297815A1

公开(公告)日：2016-10-13

申请号：US15080068

申请日：2016-03-24

Applicant: GREEN CROSS CORPORATION

Inventor： Soongyu CHOI ,  Kwang-Seop SONG ,  Hee Jeong SEO ,  Sang-ho MA ,  Eun-Jung PARK ,  Younggyu KONG ,  So Ok PARK ,  Kisoo PARK ,  Ickhwan SON ,  Min Ju KIM ,  Man-Young CHA ,  Mi-Soon KIM ,  Sang Mi KANG ,  Dong Hyuk JANG ,  Jangwon HONG

IPC: C07D471/04 ,  C07D519/00 ,  C07D487/04 ,  C07C53/18

CPC classification number: C07D471/04 ,  C07D487/04 ,  C07D519/00

Abstract: Provided are 7-azaindole or 4,7-diazaindole derivatives as an IKKε (I-kappa-B kinase epsilon) and TBK1 (TANK-binding kinase 1) inhibitor. The 7-azaindole or 4,7-diazaindole derivative effectively inhibits IKKε and TBK1, and thus is useful not only as an anticancer agent for the treatment of various cancers including colorectal cancer, breast cancer, CNS cancer, colon cancer, non-small cell lung cancer, kidney cancer, prostate cancer, ovarian cancer, uterus cancer, stomach cancer, liver cancer, skin cancer, lung cancer, brain cancer, bladder cancer, esophageal cancer, pancreatic cancer, thyroid cancer, head and neck cancer, squamous cell carcinoma, osteosarcoma, B-cell or T-cell lymphoma, acute or chronic leukemia and multiple myeloma, but as a therapeutic agent for chronic inflammation.

Abstract translation: 提供作为IKKε（I-kappa-B激酶ε）和TBK1（TANK结合激酶1）抑制剂的7-氮杂吲哚或4,7-二氮杂双环衍生物。 7-氮杂吲哚或4,7-二氮杂双环衍生物有效抑制IKKε和TBK1，因此不仅可用作治疗各种癌症的抗癌剂，包括结肠直肠癌，乳腺癌，CNS癌，结肠癌，非小细胞 肺癌，肾癌，前列腺癌，卵巢癌，子宫癌，胃癌，肝癌，皮肤癌，肺癌，脑癌，膀胱癌，食管癌，胰腺癌，甲状腺癌，头颈癌，鳞状细胞癌 ，骨肉瘤，B细胞或T细胞淋巴瘤，急性或慢性白血病和多发性骨髓瘤，但作为慢性炎症的治疗剂。

公开(公告)号：US20150152075A1

公开(公告)日：2015-06-04

申请号：US14593071

申请日：2015-01-09

Applicant: GREEN CROSS CORPORATION

Inventor： Soongyu CHOI ,  Kwang-Seop SONG ,  Suk Ho LEE ,  Min Ju KIM ,  Hee Jeong SEO ,  Eun-Jung PARK ,  Younggyu KONG ,  So Ok PARK ,  Hyunku KANG ,  Myung Eun JUNG ,  Kinam LEE ,  Hyun Jung KIM ,  Jun Sung LEE ,  Min Woo LEE ,  Mi-Soon KIM ,  Dong Ho HONG ,  Misuk KANG

IPC: C07D309/10 ,  C07D405/10 ,  C07D407/10 ,  C07D409/10 ,  C07D407/14 ,  C07D413/14 ,  C07D413/10 ,  C07D411/10 ,  C07D405/14 ,  C07D409/14 ,  C07D413/12 ,  C07D407/04 ,  C07D409/04

CPC classification number: C07D309/10 ,  C07D405/10 ,  C07D405/14 ,  C07D407/04 ,  C07D407/10 ,  C07D407/14 ,  C07D409/04 ,  C07D409/10 ,  C07D409/14 ,  C07D411/10 ,  C07D413/04 ,  C07D413/10 ,  C07D413/12 ,  C07D413/14

Abstract: A compound with a diphenylmethane moiety having an inhibitory activity against sodium-dependent glucose cotransporter 2 (SGLT2) being present in the intestine and kidney is disclosed. A pharmaceutical composition including the compound as an active ingredient, which is useful for preventing or treating metabolic disorders, particularly diabetes is disclosed. A method for preparing the compound, and a method for preventing or treating metabolic disorders, particularly diabetes, by using the compound is provided.

Abstract translation: 公开了具有对钠依赖性葡萄糖转运蛋白2（SGLT2）具有抑制活性的二苯基甲烷部分的化合物存在于肠和肾中。 公开了包含该化合物作为活性成分的药物组合物，其可用于预防或治疗代谢紊乱，特别是糖尿病。 提供了制备该化合物的方法，以及通过使用该化合物预防或治疗代谢紊乱，特别是糖尿病的方法。

公开(公告)号：US20180346588A1

公开(公告)日：2018-12-06

申请号：US15762885

申请日：2016-09-23

Applicant: MOGAM INSTITUTE FOR BIOMEDICAL RESEARCH ,  GREEN CROSS CORPORATION

Inventor： Dong-Sik KIM ,  Eun Jung SONG ,  Mijung LEE ,  Eun-Hee LEE ,  Miyoung OH ,  Jae Chan PARK ,  Kisu KIM ,  Sujeong KIM ,  Hyung-Kwon LIM ,  Kyuhyun LEE ,  Jongwha WON ,  Soongyu CHOI ,  Young Seoub PARK

IPC: C07K16/30

CPC classification number: C07K16/30 ,  C07K16/18 ,  C07K2317/21 ,  C07K2317/565 ,  C07K2317/92

Abstract: The present invention relates to an antibody specifically bound to mesothelin (MSLN), a nucleic acid encoding the antibody, a vector and a host cell including the nucleic acid, a method for producing the antibody, and a pharmaceutical composition for treating cancer or tumor including the antibody as an active ingredient. The antibody specifically bound to the mesothelin according to the present invention has high affinity and specificity to an antigen, such that it is possible to develop an antibody effectively usable for treatment or diagnosis of cancer or tumor diseases.

公开(公告)号：US20170152251A1

公开(公告)日：2017-06-01

申请号：US15325521

申请日：2014-07-18

Applicant: GREEN CROSS CORPORATION ,  LEGOCHEM BIOSCIENCES,INC.

Inventor： Soongyu CHOI ,  Jungsub CHOI ,  So-Hyun YOON ,  Yoo Hoon KIM ,  Jae Yeon KIM ,  Suk Ho LEE ,  Young Lag CHO ,  Ho Young SONG ,  Dae Yon LEE ,  Sung Yoon BAEK ,  Sang Eun CHAE ,  Tae Kyo PARK ,  Sung Ho WOO ,  Yong Zu KIM

IPC: C07D413/14

CPC classification number: C07D413/14 ,  A61K31/53 ,  A61P7/02 ,  A61P9/00 ,  A61P29/00 ,  C07B2200/13 ,  C07D253/065 ,  C07D409/10

Abstract: The present invention relates to a novel crystalline form of 5-chloro-N-({(5S)-2-oxo-3-[4-(5,6-dihydro-4H-[1,2,4]triazin-1-yl)phenyl]-1,3-oxazolidin-5-yl}methyl)thiophene-2-carboxamide methanesulfonate and a pharmaceutical composition containing the same. The novel crystalline form of a compound according to the present invention exhibits excellent stability even in high-temperature and humidity environments, and thus can be favorably used to prevent or treat diseases, such as thrombosis, myocardial infarction, atherosclerosis, inflammation, stroke, angina pectoris, restenosis after angioplasty, and thromboembolism.

公开(公告)号：US20160289196A1

公开(公告)日：2016-10-06

申请号：US15083503

申请日：2016-03-29

Applicant: GREEN CROSS CORPORATION

Inventor： Soongyu CHOI ,  Kisoo PARK ,  Hee Jeong SEO ,  Eun-Jung PARK ,  Younggyu KONG ,  Ickhwan SON ,  Sang-ho MA ,  Kwang-Seop SONG ,  Min Ju KIM ,  So Ok PARK ,  Man-Young CHA ,  Mi-Soon KIM ,  Sang Mi KANG ,  Dong Hyuk JANG ,  Jangwon HONG

IPC: C07D231/56 ,  C07D409/12 ,  C07D495/04 ,  C07D409/14 ,  C07D401/12 ,  C07D413/12 ,  C07C53/18 ,  C07D417/12 ,  C07D403/12 ,  C07D413/14 ,  C07D405/12 ,  C07D409/04

CPC classification number: C07D231/56 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/04 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D495/04

Abstract: Provided is pyrazole derivatives as a TNIK (Traf2- and NCK-interacting kinase), IKKε (I-kappa-B kinase epsilon) and TBK1 (TANK-binding kinase 1) inhibitor; the pyrazole derivative according to the present invention effectively inhibits TNIK, IKKε and TBK1, and thus is useful not only as an anticancer agent for the treatment of various cancers including colorectal cancer, breast cancer, CNS cancer, colon cancer, non-small cell lung cancer, kidney cancer, prostate cancer, ovarian cancer, uterus cancer, stomach cancer, liver cancer, skin cancer, lung cancer, brain cancer, bladder cancer, esophageal cancer, pancreatic cancer, thyroid cancer, head and neck cancer, squamous cell carcinoma, osteosarcoma, B-cell or T-cell lymphoma, acute or chronic leukemia and multiple myeloma, but as a therapeutic agent for chronic inflammation.

Abstract translation: 提供吡唑衍生物作为TNIK（Traf2-和NCK相互作用激酶），IKKε（I-κB激酶ε）和TBK1（TANK结合激酶1）抑制剂; 根据本发明的吡唑衍生物有效地抑制TNIK，IKKε和TBK1，因此不仅可用作治疗各种癌症的抗癌剂，包括结肠直肠癌，乳腺癌，CNS癌，结肠癌，非小细胞肺 癌症，肾癌，前列腺癌，卵巢癌，子宫癌，胃癌，肝癌，皮肤癌，肺癌，脑癌，膀胱癌，食管癌，胰腺癌，甲状腺癌，头颈癌，鳞状细胞癌， 骨肉瘤，B细胞或T细胞淋巴瘤，急性或慢性白血病和多发性骨髓瘤，但作为慢性炎症的治疗剂。