Korea Institute of Science and Technology

Korea Research Institute of Chemical Technology

Joo Hwan Cha

Ae Nim Pae

Yong Seo Cho

Hun Yeong Koh

Hyunah Choo

Kyung Il Choi

Sang Hee Kim

Sang Eun Chae

Jae Yang Kong

Hyewhon Rhim

Gildon Choi

Hee-Yoon Lee

Woo-Kyu Park

Heeyeong Cho

Ye Sun Han

Chul Soo Shin

Daeyoung Jeong

Wook Hwan Kim

Seon Hee Seo

Satish N Chavre

Hwa-Sil Kim

Hun Yeoung Koh

Jung Ho Back

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 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

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 invention is a gene coding for a quinone oxidoreductase fromand a protein having an amino acid sequence expressed therefrom, which can be advantageously used in a reduction reaction of a quinone compound and synthesis of intermediates for a biologically active compound.

Gene coding for quinone oxidoreductase of kluyveromyces marxianus and protein expressed therefrom

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Seoul, South Korea

Joo Hwan Cha