The Green Cross Corporation

Daewoong Pharmaceutical Co., Ltd.

So Ok Park

Hee Jeong Seo

Min Ju Kim

Soongyu Choi

Eun-Jung Park

Younggyu Kong

Kwang-Seop Song

Mi-Soon Kim

Hyun Jung Kim

Min Woo Lee

Kisoo Park

Suk Ho Lee

Myung Eun Jung

Ickhwan Son

Man-Young Cha

Hyunku Kang

Kinam Lee

Jun Sung Lee

Se-Hwan Park

Dong Hyuk Jang

Hee-kyoon Yoon

Dong Ho Hong

Sang-ho Ma

Jangwon Hong

Misuk Kang

Sang Mi Kang

Ji-sung Yoon

Ji-Sung Yoon

Jae Eun Kim

Kwang Seop Song

Hee-Kyoon Yoon

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.

Method for producing diphenylmethane derivative

Provided is pyrazole derivatives as a TNIK (Traf2- and NCK-interacting kinase), IKK&#x3b5; (I-kappa-B kinase epsilon) and TBK1 (TANK-binding kinase 1) inhibitor; the pyrazole derivative according to the present invention effectively inhibits TNIK, IKK&#x3b5; 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.

Pyrazole derivatives as TNIK, IKK&#x3f5; and TBK1 inhibitor and pharmaceutical composition comprising same

Provided are 7-azaindole or 4,7-diazaindole derivatives as an IKK&#x3b5; (I-kappa-B kinase epsilon) and TBK1 (TANK-binding kinase 1) inhibitor. The 7-azaindole or 4,7-diazaindole derivative effectively inhibits IKK&#x3b5; 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.

7-azaindole or 4,7-diazaindole derivatives as IKK&#x3f5; epsilon and TBK1 inhibitor and pharmaceutical composition comprising same

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.

Diphenylmethane derivatives as SGLT2 inhibitors

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.

Method for dual inhibition of SGLT1 and SGLT2 using diphenylmethane derivatives

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Yongin-si, South Korea

So Ok Park