Korea Institute of Science and Technology

Other

Korea Research Institute of Chemical Technology

Hun Yeong Koh

Ae Nim Pae

Yong Seo Cho

Joo Hwan Cha

Jae Yang Kong

Hee-Yoon Lee

Kyung Il Choi

Hyunah Choo

Sang Hee Kim

Sang Eun Chae

Hyewhon Rhim

Gildon Choi

Dae Young Jeong

Heeyeong Cho

Woo-Kyu Park

Chul Soo Shin

Hyun Jung Kang

Daeyoung Jeong

Moon Ho Chang

Ji Young Jung

Seon Hee Seo

In-sung Choi

Mi Young Cha

Kyung Ho Kang

Ye Sun Han

Ghilsoo Nam

Sun Ho Jung

Kyung-Il Choi

Hwa-Sil Kim

Hong Chul Yun

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.

The present invention provides for novel piperazinylalkylpyrazole derivatives, the preparation method thereof and the selective T-type calcium channel blocking activity thereof. Particularly, it provides a piperazinylalkylpyrazole derivative as represented by the formula set forth below or its pharmaceutically acceptable salts, and its preparation method thereof. The compound of Formula 1 is a novel piperazinylalkylpyrazole derivative, which particulary has T-type Cachannel blocking effect and thus can be useful as a therapeutic agent for nerve and muscle pain.

Piperazinylalkylpyrazole derivatives useful as selective T-type calcium channel blockers and preparation method thereof

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

The present invention relates to a synthesis of a 7-membered carbocyclic compound having diexomethylene groups, more particularly to a synthesis of a 7-membered carbocyclic compound having diexomethylene groups, a novel compound having the structure represented by the following Chemical Formula 1, from trimethylsilanylmethyl-allenol derivative by the intramolecular Prins cyclization using Lewis acid. The 7-membered carbocyclic compound is a useful intermediate for synthesis of other multicyclic compounds.  In Chemical Formula 1, Ris a Cto Calkyl group, and Rand Ris respectively a hydrogen atom, or R, Rand Rmay be connected with neighboring substituents to form a 5 to 10-membered aliphatic or aromatic ring.

Synthesis of 7-membered carbocyclic compound having diexomethylene groups

A compound represented by a general formula (Ia) or (Ib) and a stereo-selective preparation method thereof using a carbonyl reductase which is separated from. The compound can be prepared by reduction of substituted &#x3b2;-keto ester and can be used as an intermediate in preparing &#x3b2;-lactam group antibiotics. 

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The present invention relates to a synthesis of an 8-membered carbocyclic compound having diexomethylene groups, more particularly to a synthesis of an 8-membered carbocyclic compound having diexomethylene groups, a novel compound having the structure represented by the following Chemical Formula 1, from trimethylsilanylmethyl-allenol derivative by the intramolecular Prins cyclization using Lewis acid. The 8-membered carbocyclic compound is a useful intermediate for synthesis of other multicarbocyclic compounds. In Chemical Formula 1, Ris a phenyl group, and Rand Ris a hydrogen atom, or R, Rand Rmay be connected with neighboring substituents to form a 5 to 10-membered aliphatic or aromatic ring.

Synthesis of 8-membered carbocyclic compound having diexomethylene groups

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

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Seoul, South Korea

Hun Yeong Koh