Patent number: 8372844
Abstract: 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.
Type:
Grant
Filed:
April 24, 2012
Date of Patent:
February 12, 2013
Assignee:
Korea Research Institute of Chemical Technology
Inventors:
Jae Yang Kong, Woo-Kyu Park, Heeyeong Cho, Daeyoung Jeong, Gildon Choi, Hun Yeong Koh, Sang Hee Kim, Ae Nim Pae, Yong Seo Cho, Joo Hwan Cha, Hyunah Choo, Sang Eun Chae, Hee-Yoon Lee
Publication number: 20120209001
Abstract: 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.
Type:
Application
Filed:
April 24, 2012
Publication date:
August 16, 2012
Applicant:
KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY
Inventors:
Jae Yang KONG, Park Woo-Kyu, Heeyeong CHO, Daeyoung JEONG, Gildon CHOI, Hun Yeong KOH, Sang Hee KIM, Ae Nim PAE, Yong Seo CHO, Joo Hwan CHA, Hyunah CHOO, Sang Eun CHAE, Hee-Yoon LEE
Patent number: 8236806
Abstract: 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.
Type:
Grant
Filed:
July 13, 2007
Date of Patent:
August 7, 2012
Assignee:
Korea Research Institute of Chemical Technology
Inventors:
Jae Yang Kong, Woo-Kyu Park, Heeyeong Cho, Daeyoung Jeong, Gildon Choi, Hun Yeong Koh, Sang Hee Kim, Ae Nim Pae, Yong Seo Cho, Joo Hwan Cha, Hyunah Choo, Sang Eun Chae, Hee-Yoon Lee
Publication number: 20100286207
Abstract: The present invention is related to new 2-oxo-cyclic compound, the process for preparing them and a pharmaceutical composition comprising the same. The present invention provides a pharmaceutical composition for preventing and treating the inflammatory disease comprising the pain or inflammation caused by rheumatic disease, for example, rheumatoid arthritis, spondyloarthopathies, gout, osteoarthritis, systemic lupus erythematosus and juvenile arthritis, and inflammatory syndrome for example, from myositis, gingivitis, synovitis, ankylosing spondylitis, burstitis, burns and scar, inflammatory Crohn's disease, Types I diabetes. therefore, it can be used as the therapeutics for treating and preventing inflammatory diseases.
Type:
Application
Filed:
July 20, 2010
Publication date:
November 11, 2010
Applicant:
Korea Research Institute of Bioscience and Biotechnology
Inventors:
Yung Hee KHO, Gyoon Hee HAN, Ho Jae LEE, Bum Woo PARK, Hyo Kon CHUN, Hwan Mook KIM, Song Kyu PARK, Sang Bae HAN, Dong Kyu RYU, Tae Gyu CHUN, Jin Ha LEE, Chang Woo LEE, Ki Hoon LEE, Hee Yoon LEE
Publication number: 20100063286
Abstract: 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.
Type:
Application
Filed:
July 13, 2007
Publication date:
March 11, 2010
Applicant:
KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY
Inventors:
Jae Yang Kong, Woo-Kyu Park, Heeyeong Cho, Daeyoung Jeong, Gildon Choi, Hun Yeong Koh, Sang Hee Kim, Ae Nim Pae, Yong Seo Cho, Joo Hwan Cha, Hyunah Choo, Sang Eun Chae, Hee-Yoon Lee
Patent number: 5703246
Abstract: A process for the preparation of an oxirane, aziridine or cyclopropane of formula (I) wherein, X is oxygen, NR.sup.4 or CHR.sup.5 ; R.sup.1 is hydrogen, alkyl, aryl, heteroaromatic, heterocyclic or cycloalkyl; R.sup.2 is hydrogen, alkyl, aryl, heteroaromatic, CO.sub.2 R.sup.8, CHR.sup.14 NHR.sup.13, heterocyclic or cycloalkyl; or R.sup.1 and R.sup.2 join together to form a cycloalkyl ring; R.sup.3 is hydrogen, alkyl, aryl, heteroaromatic, CO.sub.2 R.sup.8, R.sup.8.sub.3 Sn, CONR.sup.8 R.sup.9 or trimethylsilyl; R.sup.4 and R.sup.5 are, independently, alkyl, cycloalkyl, aryl, heteroaromatic, SO.sub.2 R.sup.8, SO.sub.3 R.sup.8, COR.sup.8, CO.sub.2 R.sup.8, CONR.sup.8 R.sup.9 or CN, or R.sup.4 can also be P(O)(aryl).sub.2 ; R.sup.8 and R.sup.9 are independently alkyl, aryl or arylalkyl; R.sup.13 and R.sup.14 are independently hydrogen, alkyl or aryl; the process comprising reacting a mixture of a compound of formula (II), wherein R.sup.1, R.sup.2 and X are as defined above, and a sulphide of formula SR.sup.6 R.
Type:
Grant
Filed:
March 15, 1996
Date of Patent:
December 30, 1997
Assignee:
Zeneca Limited
Inventors:
Varinder Kumar Aggarwal, Hesham Nimer Hasan Abdel-Rahman, Hee Yoon Lee