Ewha University-Industry Collaboration Foundation

Other

Korea Research Institute of Chemical Technology

Korea Advanced Institute of Science and Technology

Hee-Yoon Lee

Ae Nim Pae

Yong Seo Cho

Jae Yang Kong

Hun Yeong Koh

Hwang Suk Kim

Je Jin Lee

Hongsoo Lee

Kong Joo Lee

Kyung Il Choi

Sang Hee Kim

Hyunah Choo

Sang Eun Chae

Ji Soo Shin

Gildon Choi

Joo Hwan Cha

Dae Young Jeong

Heeyeong Cho

Woo-Kyu Park

Daeyoung Jeong

Ji-wan Seo

Bo-kyung Kim

Ji Young Jung

Mi Young Cha

Kyung Ho Kang

Hee-Sung Park

Sun Ho Jung

Eun Sun Lee

Aerin Yang

Eun-Kyoung Seo

Sura Ha

The present disclosure provides a novel biphenyl derivative compound, an optical isomer thereof or a pharmaceutically acceptable salt thereof. The biphenyl derivative compound, optical isomer thereof or pharmaceutically acceptable salt thereof according to the present disclosure may induce cancer cell death by damaging mitochondria and inducing ATP depletion in cells which are in a nutrient-starved state such as a glucose-starved state, which is the normal environment of cancer cells. In addition, it is an Nm23-H1/NDPK activity-increasing substance that may suppress cancer metastasis and growth. Thus, it exhibits excellent effects not only on the prevention, alleviation and treatment of cancer, but also on the suppression of cancer metastasis.

Biphenyl derivative compound and use thereof

The present disclosure provides a novel biphenyl derivative compound or a pharmaceutically acceptable salt thereof. The biphenyl derivative compound or pharmaceutically acceptable salt thereof according to the present disclosure is a compound that increases Nm23-H1/NDPK activity and can inhibit cancer metastasis and growth. Thus, it exhibits excellent effects not only on the prevention, alleviation and treatment of cancer, but also on the suppression of cancer metastasis.

The present disclosure relates to a pharmaceutical composition for suppressing cancer metastasis containing, as an active ingredient, an activator compound of the cancer metastasis inhibitor Nm23, a stereoisomer thereof, or a pharmaceutically acceptable salt thereof. The compound according to the present disclosure may suppress the metastasis of cancer cells by promoting the activity of Nm23 associated with cancer metastasis, and thus may be useful as a pharmaceutical composition for suppressing cancer metastasis.

Pharmaceutical composition, containing NM23 activator, for inhibiting cancer metastasis

A method for producing a site-specifically modified protein based on new carbon-carbon bond formation is disclosed, including the following three steps (marking, activation, and coupling steps): (a) marking of the modification site by incorporating a specific amino acid into a selected position of a target protein; (b) activation of the marked site; and (c) coupling of various post-translational modification (PTM) moieties or other chemical groups onto the activated site to obtain a site-specifically modified protein. The method for producing a site-specifically modified protein can incorporate desired diverse chemical groups including post-translational modification (PTM) moieties into a designated site in a target protein through a new carbon-carbon bond. Furthermore, the modified protein having a site-specific PTM exhibits the same chemical and functional properties as that of a target protein present in cells. Thus, the present invention is useful for studies of cellular proteins, human diseases including cancers and neurodegenerative diseases, and new drug discovery.

Method for preparing site-specifically modified protein based on novel carbon-carbon bond formation

The present invention relates to a novel piperazinyl-propyl-pyrazole derivative, a method of its preparation and a pharmaceutically acceptable composition comprising the same. The novel piperazinyl-propyl-pyrazole derivative of the present invention has superior selective affinity for dopamine Dreceptor, can effectively inhibit psychotic behavior (cage climbing) induced by apomorphine, and has relatively low adverse effects in mouse rotarod test. Therefore, it can be developed as a therapeutic agent for the treatment and prevention of central nervous system (CNS) disorders, in particular, schizophrenia, attention deficit hyperactivity disorder, depression, stress diseases, panic disorder, phobia, obsessive-compulsive disorder, posttraumatic stress disorder, cognitive disorder, Alzheimer's disease, Parkinson's disease, anxiety, paraphrenia, mania, seizure disorder, personality disorder, migraine, drug addiction, alcohol addiction, obesity, eating disorder, and sleeping disorder.

Piperazinyl-propyl-pyrazole derivatives as dopamine D4 receptor antagonists, and pharmaceutical compositions containing the same

The present invention relates to a novel piperazinyl-propyl-pyrazole derivative, a method of its preparation and a pharmaceutically acceptable composition comprising the same. The novel piperazinyl-propyl-pyrazole derivative of the present invention has superior selective affinity for dopamine D4 receptor, can effectively inhibit psychotic behavior (cage climbing) induced by apomorphine, and has relatively low adverse effects in mouse rotarod test. Therefore, it can be developed as a therapeutic agent for the treatment and prevention of central nervous system (CNS) disorders, in particular, schizophrenia, attention deficit hyperactivity disorder, depression, stress diseases, panic disorder, phobia, obsessive-compulsive disorder, posttraumatic stress disorder, cognitive disorder, Alzheimer's disease, Parkinson's disease, anxiety, paraphrenia, mania, seizure disorder, personality disorder, migraine, drug addiction, alcohol addiction, obesity, eating disorder, and sleeping disorder.

Isoxazolylalkylpiperazine derivatives having selective biological activity at dopamine D3 or D4 receptor, and preparation thereof

4,5,-dihydroisoxazolylakylpiperazine derivatives having selective biological activity at dopamine D3 or D4 receptor, and preparation thereof

Growing community of inventors

Daejeon, South Korea

Hee-Yoon Lee