公开(公告)号：WO2011043519A2

公开(公告)日：2011-04-14

申请号：PCT/KR2010/001633

申请日：2010-03-17

Applicant: KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY ,  PAE, Ae Nim ,  CHOO, Hyunah ,  CHO, Yong Seo ,  JUN, Sun Ah ,  CHO, Hye Jin ,  PARK, Woo Kyu ,  KIM, Jeong Min

Inventor： PAE, Ae Nim ,  CHOO, Hyunah ,  CHO, Yong Seo ,  JUN, Sun Ah ,  CHO, Hye Jin ,  PARK, Woo Kyu ,  KIM, Jeong Min

IPC: C07C311/16

CPC classification number: C07C311/18 ,  C07C2601/08 ,  C07D207/09 ,  C07D207/14 ,  C07D211/14 ,  C07D295/13 ,  C07D409/12

Abstract: The present invention relates to sulfonamide derivatives as a serotonin receptor antagonist and serotonin reuptake inhibitor and a pharmaceutically acceptable salt thereof. The sulfonamide derivatives have serotonin 5-HT 2A and 5-HT 2C receptor antagonizing and serotonin reuptake inhibiting functions, and thus may be efficiently applied to a CNS-related disease such as depression, obesity, psychosis, schizophrenia, suicidal tendency, anxiety, obsessional neurosis, migraine, appetite disorders, sleep disorders, stroke, and withdrawal symptoms caused by drug abuse.

Abstract translation: 本发明涉及作为血清素受体拮抗剂和血清素再摄取抑制剂的磺酰胺衍生物及其药学上可接受的盐。 磺酰胺衍生物具有血清素5-HT 2A和5-HT 2C受体拮抗作用和5-羟色胺再摄取抑制功能，因此可以有效地应用于CNS相关疾病，例如 抑郁症，肥胖症，精神病，精神分裂症，自杀倾向，焦虑症，强迫症，偏头痛，食欲不振，睡眠障碍，中风和药物滥用引起的戒断症状。

公开(公告)号：WO2007007939A1

公开(公告)日：2007-01-18

申请号：PCT/KR2005/004325

申请日：2005-12-15

Applicant: KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY ,  CHO, Yong Seo ,  PAE, Ae Nim ,  CHA, Joo Hwan ,  KOH, Hun Yeong ,  SHIN, Chul

Inventor： CHO, Yong Seo ,  PAE, Ae Nim ,  CHA, Joo Hwan ,  KOH, Hun Yeong ,  SHIN, Chul

IPC: C07D493/02

CPC classification number: C07D493/04

Abstract: The present invention relates to bicyclic tetrahydrofuran derivatives and a preparation method thereof. Particularly the present invention relates to a process of preparing the above compounds by performing an intramolecular cyclization of tetrahydrofuran-allenol derivatives in the presence of alcohol compound, transitional metal catalyst and carbon monoxide.

Abstract translation: 本发明涉及二环四氢呋喃衍生物及其制备方法。 特别地，本发明涉及通过在醇化合物，过渡金属催化剂和一氧化碳的存在下进行四氢呋喃 - 聚烯醇衍生物的分子内环化来制备上述化合物的方法。

公开(公告)号：WO2008093919A1

公开(公告)日：2008-08-07

申请号：PCT/KR2007/003197

申请日：2007-07-02

Applicant: DONGBU HITEK CO., LTD. ,  KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY ,  PAE, Ae Nim ,  CHO, Yong Seo ,  CHOO, Hyunah ,  KIM, Hye-jung ,  KOH, Hun Yeong ,  PARK, Woo-Kyu ,  KONG, Jae Yang ,  CHAE, Myeong Yun ,  CHO, Insun ,  HWANG, Bong Woon ,  LEE, Dong Ha

Inventor： PAE, Ae Nim ,  CHO, Yong Seo ,  CHOO, Hyunah ,  KIM, Hye-jung ,  KOH, Hun Yeong ,  PARK, Woo-Kyu ,  KONG, Jae Yang ,  CHAE, Myeong Yun ,  CHO, Insun ,  HWANG, Bong Woon ,  LEE, Dong Ha

IPC: A61K31/18 ,  A61P25/28

CPC classification number: A61K31/18

Abstract: The present invention relates to N-benzyl-N-(2-dimethylamino-ethyl)-benzenesulfonamide compounds useful for the treatment of central nervous system (CNS) disorders.

Abstract translation: 本发明涉及可用于治疗中枢神经系统（CNS）病症的N-苄基-N-（2-二甲基氨基 - 乙基） - 苯磺酰胺化合物。

公开(公告)号：WO2007007938A1

公开(公告)日：2007-01-18

申请号：PCT/KR2005/004303

申请日：2005-12-14

Applicant: KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY ,  CHO, Yong Seo ,  CHA, Joo Hwan ,  PAE, Ae Nim ,  KOH, Hun Yeong ,  SHIN, Chul

Inventor： CHO, Yong Seo ,  CHA, Joo Hwan ,  PAE, Ae Nim ,  KOH, Hun Yeong ,  SHIN, Chul

IPC: C07D493/02

CPC classification number: C07D493/04

Abstract: The present invention relates to tricyclic tetrahydrofuran lactone derivatives and a preparation method thereof. Particularly, the present invention relates to a process of preparing the above compounds 'tetrahydrofuran lactone derivatives' by performing an intramolecular cyclization of tetrahydrofuran-allenic acid derivatives in the presence of a phenyl halide, a palladium catalyst and a base.

Abstract translation: 本发明涉及三环四氢呋喃内酯衍生物及其制备方法。 特别地，本发明涉及通过在苯基卤化物，钯催化剂和碱的存在下进行四氢呋喃 - 烯酸衍生物的分子内环化来制备上述化合物的四氢呋喃内酯衍生物的方法。

公开(公告)号：WO2007136197A1

公开(公告)日：2007-11-29

申请号：PCT/KR2007/002431

申请日：2007-05-18

Applicant: KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY ,  CHO, Yong Seo ,  CHOO, Hyunah ,  CHA, Joo Hwan ,  PAE, Ae Nim ,  KIM, Sang Hee ,  KIM, Hyung-Gyu

Inventor： CHO, Yong Seo ,  CHOO, Hyunah ,  CHA, Joo Hwan ,  PAE, Ae Nim ,  KIM, Sang Hee ,  KIM, Hyung-Gyu

IPC: C07D471/04 ,  C07D471/12

CPC classification number: C07D471/04 ,  C07D471/14

Abstract: The present invention relates to ring-fused lactam derivatives with diexomethylene groups and a method of their preparation thereof, more particularly to a novel ring-fused lactam derivatives with diexomethylene groups which is prepared by intramolecular acyliminium cyclization of a hydroxylactam having a trimethylsilylmethyl-allene group in the presence of a Lewis acid and is useful as an intermediate for synthesis of other polycyclic compounds by the Diels-Alder reaction, and a method of their preparation thereof.

Abstract translation: 本发明涉及具有阴离子亚甲基的环稠合内酰胺衍生物及其制备方法，更具体地涉及一种新颖的具有阴离子亚甲基的环稠合内酰胺衍生物，其通过分子内酰基亚胺鎓环化具有三甲基甲硅烷基甲基 - 全烯基的羟基内酰胺 在路易斯酸存在下，可用作通过Diels-Alder反应合成其它多环化合物的中间体及其制备方法。

公开(公告)号：WO2007007937A1

公开(公告)日：2007-01-18

申请号：PCT/KR2005/004302

申请日：2005-12-14

Applicant: KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY ,  CHO, Yong Seo ,  CHA, Joo Hwan ,  PAE, Ae Nim ,  KOH, Hun Yeong ,  SHIN, Chul

Inventor： CHO, Yong Seo ,  CHA, Joo Hwan ,  PAE, Ae Nim ,  KOH, Hun Yeong ,  SHIN, Chul

IPC: C07D307/93

CPC classification number: C07D307/93

Abstract: The present invention relates to tricyclic tetrahydrofuran derivatives and a preparation method thereof. Particularly, the present invention relates to a process of preparing the above compounds by performing an intramolecular cyclization of tetrahydrofuran-allene derivatives in the presence of metal catalyst and sodium azide (NaN 3 ).

Abstract translation: 本发明涉及三环四氢呋喃衍生物及其制备方法。 特别地，本发明涉及通过在金属催化剂和叠氮化钠（NaN 3 N 3）的存在下进行四氢呋喃 - 全烯衍生物的分子内环化来制备上述化合物的方法。

公开(公告)号：WO2010005148A2

公开(公告)日：2010-01-14

申请号：PCT/KR2008/005784

申请日：2008-10-01

Applicant: KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY ,  CHO, Yong Seo ,  PAE, Ae Nim ,  CHOO, Hyunah ,  LEE, Jae Kyun ,  OH, You Na ,  SHIN, Hee Sup ,  KIM, Dong Jin ,  HAHN, Hoh Gyu ,  CHOI, Kyung Il ,  NAM, Ghilsoo ,  SHIN, Kye Jung ,  KANG, Soon Bang ,  ROH, Eun Joo ,  SHIN, Dong Yun ,  SEO, Seon Hee ,  RHIM, Hyewhon ,  KEUM, Gyo Chang ,  KIM, Key-Sun ,  CHEONG, Chan Seong ,  KIM, Eunice Eun-Kyeong ,  LEE, Cheolju ,  KIM, Youngsoo ,  CHOI, Kee Hyun ,  NAM, Kee Dal ,  PARK, Woong Seo ,  KANG, Yong Koo ,  CHUNG, Hye Jin

Inventor： CHO, Yong Seo ,  PAE, Ae Nim ,  CHOO, Hyunah ,  LEE, Jae Kyun ,  OH, You Na ,  SHIN, Hee Sup ,  KIM, Dong Jin ,  HAHN, Hoh Gyu ,  CHOI, Kyung Il ,  NAM, Ghilsoo ,  SHIN, Kye Jung ,  KANG, Soon Bang ,  ROH, Eun Joo ,  SHIN, Dong Yun ,  SEO, Seon Hee ,  RHIM, Hyewhon ,  KEUM, Gyo Chang ,  KIM, Key-Sun ,  CHEONG, Chan Seong ,  KIM, Eunice Eun-Kyeong ,  LEE, Cheolju ,  KIM, Youngsoo ,  CHOI, Kee Hyun ,  NAM, Kee Dal ,  PARK, Woong Seo ,  KANG, Yong Koo ,  CHUNG, Hye Jin

IPC: C07D403/12

CPC classification number: C07D401/12 ,  A61K31/454

Abstract: Disclosed are isoindolinone derivatives 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.

Abstract translation: 公开了对T型钙通道具有抑制活性的异吲哚啉酮衍生物，其药学上可接受的盐，其制备方法和包含其的作为活性成分的药物组合物。

公开(公告)号：WO2009104849A1

公开(公告)日：2009-08-27

申请号：PCT/KR2008/005331

申请日：2008-09-10

Applicant: KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY ,  CHO, Yong Seo ,  KIM, You Seung ,  LEE, Jae Kyun ,  CHOO, Hyunah ,  PAE, Ae Nim

Inventor： CHO, Yong Seo ,  KIM, You Seung ,  LEE, Jae Kyun ,  CHOO, Hyunah ,  PAE, Ae Nim

IPC: C07D309/04

CPC classification number: C07D309/06

Abstract: Disclosed are cis-2,6-disubstituted tetrahydropyran derivatives 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.

Abstract translation: 公开了顺式-2,6-二取代四氢吡喃衍生物及其制备方法。 四氢吡喃衍生物可以通过Prins-在三甲基甲硅烷基三氟甲磺酸酯存在下将四氢吡喃衍生物与高官能醇衍生物反应来制备。 在四氢吡喃环的C2和C6位上具有顺式取代基的四氢​​吡喃衍生物可用作合成和开发治疗有效的天然存在的化合物的中间体。

公开(公告)号：WO2008093920A2

公开(公告)日：2008-08-07

申请号：PCT/KR2007/003198

申请日：2007-07-02

Applicant: DONGBU HITEK CO., LTD. ,  KOREA INSTITUTE OF SCIENCE AND TECHNOLOGY ,  PAE, Ae Nim ,  CHO, Yong Seo ,  CHOO, Hyunah ,  CHA, Joo Hwan ,  KIM, Ji Hye ,  KOH, Hun Yeong ,  PARK, Woo-Kyu ,  KONG, Jae Yang ,  CHAE, Myeong Yun ,  CHO, Insun ,  HWANG, Bong Woon ,  LEE, Dong Ha

Inventor： PAE, Ae Nim ,  CHO, Yong Seo ,  CHOO, Hyunah ,  CHA, Joo Hwan ,  KIM, Ji Hye ,  KOH, Hun Yeong ,  PARK, Woo-Kyu ,  KONG, Jae Yang ,  CHAE, Myeong Yun ,  CHO, Insun ,  HWANG, Bong Woon ,  LEE, Dong Ha

IPC: C07D401/12

CPC classification number: C07D237/32

Abstract: The present invention relates to a novel 1,2-dihydro-1-oxophthalazinyl piperazine compound having biological activity as serotonin receptor antagonist, a preparation method of the compound and a pharmaceutical composition for the treatment and prevention of central nervous system diseases comprising the compound.

Abstract translation: 本发明涉及具有生物活性作为血清素受体拮抗剂的新型1,2-二氢-1-氧代嗪嗪哌嗪化合物，该化合物的制备方法和用于治疗和预防包含该化合物的中枢神经系统疾病的药物组合物。

公开(公告)号：EP3560927A1

公开(公告)日：2019-10-30

申请号：EP17811428.6

申请日：2017-11-06

Applicant: Korea Institute of Science and Technology

Inventor： CHOO, Hyunah ,  KIM, Youngjae ,  SEONG, Jihye ,  NAM, Ghil Soo ,  CHO, Yong Seo

IPC: C07D487/04 ,  A61K31/55

Abstract: Azepine derivatives acting on 5-HT 7 receptors 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-HT 7 receptors. 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-HT 7 receptors antagonistic activity is required.