Abstract: The present invention relates to novel tricyclic derivative compounds, and more specifically to tricyclic derivative compounds, optical isomers thereof, racemates thereof, or pharmaceutically acceptable salts thereof, which have excellent activity against PARP-1, tankyrase-1 or tankyrase-2. The tricyclic derivative compounds, optical isomers thereof, racemates thereof or pharmaceutically acceptable salts thereof according to the present invention have inhibitory activity against PARP-1, tankyrase-1, or tankyrase-2, and thus can be effectively used for the prevention or treatment of neuropathic pain, neurodegenerative diseases, cardiovascular diseases, diabetic neuropathy, inflammatory diseases, osteoporosis, or cancer.
Type:
Grant
Filed:
June 3, 2016
Date of Patent:
November 5, 2019
Assignee:
Je Il Pharmaceutical Co., Ltd.
Inventors:
Hyunho Lee, Kwangwoo Chun, Bo-Young Joe, Eun Seon Kim, Eun Sung Jang, Hyeongchan Oh, Jeong-Min Kim, Jiseon Park, Hanchang Lee
Abstract: The present invention relates to a novel tricyclic derivative with efficient inhibitory activity against poly(ADP-ribose)polymerases (PARP) or pharmaceutically acceptable salts thereof, a preparation method thereof, and a pharmaceutical composition containing the same. The tricyclic derivative of the invention is useful for the prevention or treatment of diseases caused by excess PARP activity, especially neuropathic pain, neurodegenerative diseases, cardiovascular diseases, diabetic nephropathy, inflammatory diseases, osteoporosis, and cancer, by inhibiting the activity of poly(ADP-ribose)polymerases.
Type:
Grant
Filed:
November 11, 2009
Date of Patent:
August 26, 2014
Assignee:
Je Il Pharmaceutical Co., Ltd.
Inventors:
Myung-Hwa Kim, Seung-Hyun Kim, Sae-Kwang Ku, Chun-Ho Park, Bo-Young Joe, Kwang-Woo Chun, In-Hae Ye, Jong-Hee Choi, Dong-Kyu Ryu, Ji-Seon Park, Han-Chang Lee, Ji-So Choi, Young-Chul Kim
Abstract: The present invention relates to a method for preparing a tricyclic derivative, and more particularly, to a method for preparing a tricyclic derivative intermediate with high yield and purity, the method including: introducing a hydroxy group by esterifying and substituting 2-fluoroisophthalic acid compound; introducing a piperidyl group; introducing a hydroxy group through reduction reaction; and then hydrolyzing the resultant compound, and to a method for preparing the tricyclic derivative using said intermediate. According to the method of the present invention, it is possible to provide a tricyclic derivative and an intermediate thereof with high productivity and economic feasibility as well as high purity and yield, by purifying a compound using re-crystallization unlike typical methods of using column chromatography.
Type:
Grant
Filed:
June 29, 2010
Date of Patent:
June 3, 2014
Assignee:
JE IL Pharmaceutical Co., Ltd.
Inventors:
Myung-Hwa Kim, In-Hae Ye, Jong-Hee Choi
Abstract: The present invention relates to a method for inducing the differentiation of neural progenitors, neurons, and dopaminergic neurons from human embryonic stem cells with high efficiency, in which neural selection can be performed by the selected media and physical methods. The invention has advantages such as higher efficiency, the effect of lowering cost and time, and maintenance of neural progenitors for a longer period of time, as compared to the known methods for inducing the differentiation into neural progenitors, neurons, and dopaminergic neurons. Accordingly, the method can stably generate cells used for treating Parkinson's disease or other nervous system diseases.
Type:
Grant
Filed:
June 5, 2007
Date of Patent:
July 23, 2013
Assignee:
JE IL Pharmaceutical Co., Ltd.
Inventors:
Myung Soo Cho, Myung-Hwa Kim, Young-II Moon, Shin Yong Moon, Sun Kyung Oh, Hee Sun Kim, Dong-Wook Kim
Abstract: The present invention relates to a novel {4-[2-(dimethylamino)-1-(1-hydroxycyclohexyl)ethyl]phenoxy}phosphate or a pharmaceutically acceptable salt thereof, a production method therefor and a pharmaceutical composition for preventing and treating central nervous system disorders which contains the same as an active component. The novel {4-[2-(dimethylamino)-1-(1-hydroxycyclohexyl)ethyl]phenoxy}phosphate or a pharmaceutically acceptable salt thereof according to the present invention can beneficially be used to prevent and treat central nervous system disorders since it exhibits an equivalent biological and pharmacological activity to venlafaxine and salts thereof which are known in the field, it has very little toxicity, and, in particular, it is outstandingly soluble in water as compared with prior-art venlafaxine derivatives.
Type:
Grant
Filed:
May 8, 2009
Date of Patent:
December 18, 2012
Assignee:
JE IL Pharmaceutical Co., Ltd.
Inventors:
Seok Won Kang, Jong Soo Chun, Heung Mo Kang, Eui Seok Hong, Kwang-Woo Chun, Young Seok Byun, Myung-Hwa Kim, Young Il Moon, Jei Man Ryu
Abstract: The present invention relates to a method for preparing a tricyclic derivative, and more particulary, to a method for preparing a tricyclic derivative inetermediate with high yield and purity, the method including: introducing a hydroxy group by esterifying and substituting 2-fluoroisophthalic acid compound; introducing a piperidyl group; introducing a hydroxy group through reduction reaction; and then hydrolyzing the resultant compound, and to a method for preparing the tricyclic derivative using said intermediate. According to the method of the present invention, it is possible to provide a tricyclic derivative and an intermediate thereof with high productivity and economic feasibility as well as high purity and yield, by purifying a compound using re-crystallization unlike typical methods of using column chromatography.
Type:
Application
Filed:
June 29, 2010
Publication date:
April 26, 2012
Applicant:
JE IL PHARMACEUTICAL CO., LTD.
Inventors:
Myung-Hwa Kim, In-Hae Ye, Jong-Hee Choi
Abstract: The present invention relates to a novel tricyclic derivative with efficient inhibitory activity against poly(ADP-ribose)polymerases (PARP) or pharmaceutically acceptable salts thereof, a preparation method thereof, and a pharmaceutical composition containing the same. The tricyclic derivative of the invention is useful for the prevention or treatment of diseases caused by excess PARP activity, especially neuropathic pain, neurodegenerative diseases, cardiovascular diseases, diabetic nephropathy, inflammatory diseases, osteoporosis, and cancer, by inhibiting the activity of poly(ADP-ribose)polymerases.
Type:
Application
Filed:
November 11, 2009
Publication date:
September 8, 2011
Applicant:
JE IL PHARMACEUTICAL CO., LTD.
Inventors:
Myung-Hwa Kim, Seung-Hyun Kim, Sae-Kwang Ku, Chun-Ho Park, Bo-Young Joe, Kwang-Woo Chun, In-Hae Ye, Jong-Hee Choi, Dong-Kyu Ryu, Ji-Seon Park, Han-Chang Lee, Ji-So Choi, Young-Chul Kim
Abstract: The present invention relates to a novel {4-[2-(dimethylamino)-1-(1-hydroxycyclohexyl)ethyl]phenoxy}phosphate or a pharmaceutically acceptable salt thereof, a production method therefor and a pharmaceutical composition for preventing and treating central nervous system disorders which contains the same as an active component. The novel {4-[2-(dimethylamino)-1-(1-hydroxycyclohexyl)ethyl]phenoxy}phosphate or a pharmaceutically acceptable salt thereof according to the present invention can beneficially be used to prevent and treat central nervous system disorders since it exhibits an equivalent biological and pharmacological activity to venlafaxine and salts thereof which are known in the field, it has very little toxicity, and, in particular, it is outstandingly soluble in water as compared with prior-art venlafaxine derivatives.
Type:
Application
Filed:
May 8, 2009
Publication date:
March 10, 2011
Applicant:
JE IL PHARMACEUTICAL CO., LTD.
Inventors:
Seok Won Kang, Jong Soo Chun, Heung Mo Kang, Eui Seok Hong, Kwang-Woo Chun, Young Seok Byun, Myung-Hwa Kim, Young II Moon, Jei Man Ryu
Abstract: The present invention relates to a method for inducing the differentiation of neural progenitors, neurons, and dopaminergic neurons from human embryonic stem cells with high efficiency, in which neural selection can be performed by the selected media and physical methods. The invention has advantages such as higher efficiency, the effect of lowering cost and time, and maintenance of neural progenitors for a longer period of time, as compared to the known methods for inducing the differentiation into neural progenitors, neurons, and dopaminergic neurons. Accordingly, the method can stably generate cells used for treating Parkinson's disease or other nervous system diseases.
Type:
Application
Filed:
June 5, 2007
Publication date:
December 16, 2010
Applicant:
JE IL PHARMACEUTICAL CO., LTD.
Inventors:
Myung Soo Cho, Myung-Hwa Kim, Young-Il Moon, Shin Yong Moon, Sun Kyung Oh, Hee Sun Kim, Dong-Wook Kim
Abstract: The present invention relates to tricyclic derivatives or pharmaceutically acceptable salts thereof, their preparations and pharmaceutical compositions containing them. More precisely, the present invention relates to tricyclic derivatives as colchicine derivatives, pharmaceutically acceptable salts thereof, their preparations and pharmaceutical compositions containing them. Tricyclic derivatives of the present invention show very powerful cytotoxicity to cancer cell lines but were much less toxic than colchicine or taxol, confirmed through animal toxicity test. Tricyclic derivatives of the invention also decrease the volume and weight of a tumor and have a strong angiogenesis inhibiting activity in HUVEC cells. Thus, tricyclic derivatives of the present invention can effectively be used as an anticancer agent, anti-proliferation agent and an angiogenesis inhibitor.
Type:
Application
Filed:
June 23, 2004
Publication date:
August 2, 2007
Applicant:
JE IL Pharmaceutical CO., LTD.
Inventors:
Myung-Hwa Kim, Kwnagwoo Chun, Jae-Won Chol, Bo-Young Joe, Sang-Woo Park, Kwang Kim, Byung-Kyu Oh, Jong-Hee Chol
Abstract: Dehydroevodiamine-HCl, a constituent of Evodia rutaecarpa Benth. (DHED) exhibits anti-AChE activity and improves the memory impairment of animals produced by scopolamine in the passive avoidance test. Thus, DHED can be a potent, long term memory enhancing and anti-dementia agent if it is used together with a pharmaceutically acceptable carrier.
Type:
Grant
Filed:
March 12, 1997
Date of Patent:
January 12, 1999
Assignees:
JE IL Pharmaceutical Co., Ltd., Yoo-Hun Suh
Inventors:
Yoo-Hun Suh, Sam-Sik Kang, Seong-Hun Kim, Cheol-Hyoung Park, Woong Choi