Korea Institute of Science and Technology

Other

Korea Research Institute of Chemical Technology

Yong Seo Cho

Ae Nim Pae

Hyunah Choo

Hun Yeong Koh

Joo Hwan Cha

Kyung Il Choi

Jae Kyun Lee

Jae Yang Kong

Hyewhon Rhim

Hee-Yoon Lee

Seon Hee Seo

Woo-Kyu Park

Youngsoo Kim

Dong Jin Kim

Sang Hee Kim

Sang Eun Chae

Hee Sup Shin

Eun Joo Roh

Gyo Chang Keum

Gildon Choi

Yong Koo Kang

Dae Young Jeong

Kye Jung Shin

Heeyeong Cho

Eunice Eun-Kyeong Kim

Sun Joon Min

Hesson Chung

Key-Sun Kim

Chul Soo Shin

Ghilsoo Nam

Hoh Gyu Hahn

Kee Dal Nam

Hye Jin Chung

Dong Yun Shin

Yoon Jee Kim

Hye Ran Kim

Moon Ho Chang

Woong Seo Park

Hyun Jung Kang

Chan Seong Cheong

Kee Hyun Choi

Daeyoung Jeong

Youngjae Kim

Hoon Ryu

Yun Kyung Kim

Ji Young Jung

Soon Bang Kang

Ghil Soo Nam

Mi Young Cha

Kyung Ho Kang

You Seung Kim

Ye Sun Han

Chi Man Song

Sun Ho Jung

Younghee Kim

Jihye Seong

Sun-Joon Min

Yu Jin Hwang

Ji Yeong Kim

Cheolju Lee

Myung Hee Son

Sungsu Lim

Hong Chul Yun

Ahmed Asif

You Na Oh

Satish N Chavre

Hyemyung Seo

Young Wook Son

Eun Jeong Lim

Juhyeon Kim

Jihoon Jang

Hwa-Sil Kim

Azepine derivatives acting on 5-HTreceptors and pharmaceutically acceptable salts thereof are disclosed. The azepine derivatives and the pharmaceutically acceptable salts thereof have high binding affinities for and high antagonistic activities on 5-HTreceptors. Due to these advantages, the azepine derivatives and the pharmaceutically acceptable salts thereof can be applied to therapeutic or prophylactic agents for central nervous system diseases, such as depression, migraine, anxiety, pain, inflammatory pain, neuropathic pain, body temperature dysregulation, biorhythm dysregulation, sleep disturbance, and smooth muscle diseases where 5-HTreceptors antagonistic activity is required.

Azepine derivatives as 5-HTreceptor modulators

The present disclosure relates to a quinoline derivative which inhibits the activity of histone methyltransferases (ESET/SETDB1) specific for the histone molecule H3K9 or a pharmaceutically acceptable salt thereof and a use thereof.

Quinoline derivatives for inhibiting histone methyltransferases and use thereof

The present invention relates to a method for preparing tetrabenazine (TBZ) and dihydrotetrabenazine (DTBZ), and more specifically to a method for preparing tetrabenazine (TBZ) and dihydrotetrabenazine (DTBZ) by using simple and short reaction processes of using 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline and 4-methyl-2-(3-(trimethylsilyl)prop-1-ene-2-yl)pentane as starting materials to sequentially perform an alkylation reaction, an Aza-Prins cyclization reaction in the presence of an oxidant and an oxidation reaction.

Method of preparing tetrabenazine and dihydrotetrabenazine

Provided is a 2-(substituted ethynyl)quinoline derivative having an mGluR5 antagonistic activity and pharmaceutically acceptable salts thereof. The compound of the present invention can be useful as a medicament for treating and preventing mGluR5 receptor-mediated diseases such as Alzheimer's disease, senile dementia, Parkinson's disease, L-DOPA-induced dyskinesia, Huntington's chorea, amyotrophic lateral sclerosis, multiple sclerosis, schizophrenia, anxiety disorder, depression, neuropathic pain, drug dependence, fragile X syndrome, autism, migraine and gastroesophageal reflux disease (GERD).

2-(substituted ethynyl)quinoline derivatives as mGLUr5 antagonists

Disclosed are novel imidazolylalkylcarbonyl derivatives useful as calcium channel modulators and a preparation method of the same. Also disclosed is a method for the treatment of diseases by administering the above compounds based on their inhibitory activity against calcium channel.

Imidazolylalkylcarbonyl derivatives as calcium channel modulators and preparation method thereof

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 pyrazolylmethylamine-piperazine derivatives and their pharmaceutically acceptable salts effective as calcium channel modulators and a method of manufacturing the same. The present invention also relates to the medicinal use of the above compounds as therapeutic treatment of diseases due to their effect as calcium channel modulators.

Pyrazolylmethylamine compounds as calcium channel modulators and preparation method thereof

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.

The present invention relates to a novel medicinal use of pyrazolopyrimidine compounds having superior effect as serotonin 5-HTreceptor ligand thus being useful for the prevention and treatment of central nervous system (CNS) diseases. Accordingly, the pharmaceutical composition comprising pyrazolopyrimidine compounds and their pharmaceutically acceptable salts as active ingredients are useful for the prevention and treatment of serotonin 5-HT-related central nervous system diseases such as obesity, depression, anxiety and withdrawal symptoms due to drug abuse.

Pyrazolopyrimidine derivatives having biological activity on serotonin receptor 5-HT2c

Disclosed are isoindolinone derivatives, represented by Chemical Formula 1, having inhibitory activity against T-type calcium channels, pharmaceutically acceptable salts thereof, a preparation method thereof, and a pharmaceutical composition comprising the same as an active ingredient. 

Isoindolinone derivatives having inhibitory activity against T-type calcium channel and method for preparation thereof

Disclosed are cis-2,6-disubstituted tetrahydropyran derivatives represented by Chemical Formula 1 and a preparation method thereof. The tetrahydropyran derivatives can be prepared by Prins-reacting tetrahydropyran derivatives with homopargylicalcohol derivatives in the presence of trimethylsilyltriflate. The tetrahydropyran derivatives with cis-substituents at both C2 and C6 positions of the tetrahydropyran ring are useful as intermediates for use in the synthesis and development of therapeutically effective, naturally occurring compounds.  (wherein, R, Rand Rare as defined in the specification.).

Cis-2, 6-disubstituted tetrahydropyran derivatives and preparation method thereof

The present invention relates to a tetrahydrofuran compound having cis substituents, the derivatives thereof and a process for preparing the same, and in particular relates to a dihydrofuran-3-ylidene triflate compound having cis substituents at Cand Cpositions prepared through Prins-type cyclization using a homopropargylic alcohol derivative as a starting material in the presence of Lewis acid catalyst, a tetrahydrofuran compound having cis substituents at C, Cand Cpositions prepared through the hydrolysis of triflate group in the derivatives of the dihydrofuran-3-ylidene triflate compound, and a preparation method thereof. The derivatives and the target tetrahydrofuran compound prepared according to the present invention are hydrofuran compounds with novel structures having cis substituents at C, Cand/or Cpositions, which are useful as a derivative for synthesizing drugs such as an antagonist for neurokinin receptor.

Tetrahydrofuran derivatives having cis substituent, their intermediates, and their preparation method

The present invention relates to 1,3-dioxoisoindole derivatives of Formula (1) or pharmaceutically acceptable salts thereof, a preparation method thereof and use thereof as a T-type calcium channel antagonist, based on the fact that 1,3-dioxoisoindole derivatives of Formula (1) show selective antagonistic activity against T-type calcium channel, thus being effective in treating brain diseases, cardiac diseases and neurogenic pains: wherein Ris a phenyl or a benzyl group, optionally substituted with a moiety selected from the group consisting of a halogen atom, a C-Calkoxy, a C-Calkyl, and a cyano group; Ris a heterocyclic group selected from the group consisting of piperidinyl, pyrrolidinyl, morpholinyl, and piperazinyl groups, wherein the heterocyclic group is optionally substituted with a C-Calkyl group; and n is 1 or 2.

1,3-dioxoisoindole derivatives having selective antagonism of T-type calcium channel

The present invention relates to bicyclic tetrahydrofuran derivatives of Formula (1) and a preparation method thereof, and particularly it relates to a process of preparing compounds of Formula (1) by performing an intramolecular cyclization of tetrahydrofuran-allenol derivatives in the presence of alcohol compound, transitional metal catalyst and carbon monoxide: wherein n is 1 or 2; R is phenyl optionally substituted with C-Calkyl, C-Calkoxy, hydroxyl or C-Chydroxyalkyl group; and Ris C-Calkyl group.

Bycyclic tetrahydrofuran derivatives and process for the preparation thereof

The present invention relates to bicyclic tetrahydrofuran lactone derivatives of Formula (1) and a preparation method thereof, and particularly it relates to a process of preparing compounds of Formula (1) by performing an intramolecular cyclization of tetrahydrofuran-allenic acid derivatives in the presence of a phenyl halide, a palladium catalyst and a base: wherein n is 1 or 2, and R is phenyl optionally substituted with C&#x2013;Calkyl, C&#x2013;Calkoxy, hydroxyl or C&#x2013;Chydroxyalkyl group.

Bicyclic tetrahydrofuran lactone derivatives and process for the preparation thereof

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Seoul, South Korea

Yong Seo Cho