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1. 发明专利

JP2002193954A NEW ISOOXAZOLYLALKYLPIPERAZINE DERIVATIVE HAVING SELECTIVE ACTIVITY ON DOPAMINE D3 AND D4 RECEPTORS AND METHOD FOR PRODUCING THE SAME 失效
公开(公告)号：JP2002193954A
公开(公告)日：2002-07-10
申请号：JP2001121712
申请日：2001-04-19
申请人： KOREA INST SCI & TECH , KOREA RES INST CHEM TECH
发明人： KOH HUN YEONG , CHOI KYUNG IL , CHO YONG SEO , PAE AE NIM , KANG KYUNG HO , CHA MI YOUNG , KONG JAE YANG , JEONG DAE YOUNG , LEE HAE-YOON
IPC分类号： A61K31/454 , A61K31/496 , A61P25/00 , A61P25/18 , A61P43/00 , C07D261/08 , C07D413/04 , C07D413/06 , C07D413/14
摘要： PROBLEM TO BE SOLVED: To provide a method for producing a new compound which is useful in a field of medical treatment of mental disease and a dopamine antagonist having the same as an effective component. SOLUTION: This invention provides a new isooxazolylalkylpiperazine derivative represented by general formula 1, having a selective activity on dopamine D3 and D4 receptors and a method for producing the compound by using reducing amination reaction in the presence of a reducing agent.

2. 发明专利

JP2002193953A 4,5-DIHYDROISOOXAZOLYLALKYLPIPERAZINE DERIVATIVE AND METHOD FOR PRODUCING THE SAME 失效
公开(公告)号：JP2002193953A
公开(公告)日：2002-07-10
申请号：JP2001120229
申请日：2001-04-18
申请人： KOREA INST SCI & TECH , KOREA RES INST CHEM TECH , SEISHIN GAKUIN
发明人： KOH HUN YEONG , CHOI KYUNG IL , CHO YONG SEO , PAE AE NIM , KONG JAE YANG , JEONG DAE YOUNG , JUNG SUN HO , JUNG JI YOUNG , LEE HAE-YOON
IPC分类号： C07D261/04 , A61K31/454 , A61K31/496 , A61K31/506 , A61P25/00 , A61P25/18 , C07D261/08 , C07D413/04 , C07D413/06 , C07D413/12 , C07D413/14
摘要： PROBLEM TO BE SOLVED: To develope a new compound which is useful for medical treatment of mental disease, specially a compound which selectively effects on dopamine D3 and D4 receptors and provide a method for producing the same and dopamine antagonist having the same as an effective component. SOLUTION: The 4,5-dihydroisooxazolylalkylpiperazine derivative is a compound selected from compounds represented by formula (1) and their pharmacologically permissible salts. The compound is a dopamine antagonist which can be produced by using reducing amination reaction of the corresponding amine compound with an aldehyde compound in the presence of a reductant (wherein, R1 R2, R3, R4 and R5 are each independently H-atom, a halogen atom, alkyl, alkoxy, alkenyl, hydroxy, etc.; R6 is H-atom, a halogen atom, alkyl, 1-6C alkoxy, aryl, pyrimidine, or hetero ring; and X is CH or N-atom; n is 3 or 4).

3. 发明申请

WO2012115446A2 COMPOUND BASED ON 5-(SUBSTITUTED ALKYL-AMINOMETHYL) ISOXAZOLE ACTING AS A T-TYPE CALCIUM CHANNEL ANTAGONIST 审中-公开
标题翻译：基于5-（取代的烷基氨基甲酰基）异噻唑作为T型钙通道拮抗剂的化合物
公开(公告)号：WO2012115446A2
公开(公告)日：2012-08-30
申请号：PCT/KR2012001340
申请日：2012-02-22
申请人： KOREA INST SCI & TECH , CHOO HYUN AH , PAE AE NIM , CHO YONG SEO , LEE HYO SEON , LEE JIE EUN , CHO GYEONG HI , RHIM HYE WHON , SEO SEON HEE , SONG CHI MAN , CHUNG HYE JIN , NAM GHIL SOO , KEUM GYO CHANG , KIM DONG JIN , CHOI KYUNG IL , CHOI KEE HYUN , LEE JAE KYUN , KANG YONG KOO , PARK WOONG SEO , LEE JU HYEON , SHIN SUN MI , AHMED ABDUL WAHEED , KIM YOUNG SOO , MIN SUN JOON
发明人： CHOO HYUN AH , PAE AE NIM , CHO YONG SEO , LEE HYO SEON , LEE JIE EUN , CHO GYEONG HI , RHIM HYE WHON , SEO SEON HEE , SONG CHI MAN , CHUNG HYE JIN , NAM GHIL SOO , KEUM GYO CHANG , KIM DONG JIN , CHOI KYUNG IL , CHOI KEE HYUN , LEE JAE KYUN , KANG YONG KOO , PARK WOONG SEO , LEE JU HYEON , SHIN SUN MI , AHMED ABDUL WAHEED , KIM YOUNG SOO , MIN SUN JOON
IPC分类号： C07D413/12 , A61K31/497 , A61P25/00 , A61P35/00
CPC分类号： C07D413/12
摘要： The present invention relates to: a compound based on 5-(substituted alkyl-aminomethyl) isoxazole which exhibits pharmaceutical activity with respect to T-type calcium channels; a pharmaceutically acceptable salt thereof; a production method for such a compound; and to a pharmaceutical composition containing such a compound as an active ingredient.
摘要翻译：本发明涉及：基于相对于T型钙通道具有药物活性的基于5-（取代的烷基 - 氨基甲基）异恶唑的化合物; 其药学上可接受的盐; 这种化合物的制备方法; 以及含有这种化合物作为活性成分的药物组合物。

4. 发明申请

WO2011043519A3 SULFONAMIDE DERIVATIVES AS SEROTONIN RECEPTOR ANTAGONIST AND SEROTONIN REUPTAKE INHIBITOR 审中-公开
标题翻译：磺酰胺衍生物作为丝氨酸受体拮抗剂和丝氨酸还原抑制剂
公开(公告)号：WO2011043519A3
公开(公告)日：2011-10-20
申请号：PCT/KR2010001633
申请日：2010-03-17
申请人： KOREA INST SCI & TECH , PAE AE NIM , CHOO HYUNAH , CHO YONG SEO , JUN SUN AH , CHO HYE JIN , PARK WOO KYU , KIM JEONG MIN
发明人： PAE AE NIM , CHOO HYUNAH , CHO YONG SEO , JUN SUN AH , CHO HYE JIN , PARK WOO KYU , KIM JEONG MIN
IPC分类号： C07C311/16 , A61K31/18 , C07C303/38
CPC分类号： C07C311/18 , C07C2601/08 , C07D207/09 , C07D207/14 , C07D211/14 , C07D295/13 , C07D409/12
摘要： 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-HT2A and 5-HT2C 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.
摘要翻译：本发明涉及作为5-羟色胺受体拮抗剂和5-羟色胺再摄取抑制剂及其可药用盐的磺酰胺衍生物。磺酰胺衍生物具有5-羟色胺5-HT2A和5-HT2C受体拮抗和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，强迫症神经症，偏头痛，食欲障碍，睡眠障碍，中风和药物滥用引起的戒断症状。

5. 发明申请

WO2008093920A3 1,2-DIHYDRO-1-OXOPHTHALAZINYL DERIVATIVES HAVING BIOLOGICAL ACTIVITY ON SEROTONIN RECEPTORS 5-HT2A AND 5-HT2C, AND PREPARATION THEREOF 审中-公开
标题翻译：具有SEROTONIN受体5-HT2A和5-HT2C的生物活性的1,2-二氢-1-氧代吗啉衍生物及其制备方法
公开(公告)号：WO2008093920A3
公开(公告)日：2009-05-28
申请号：PCT/KR2007003198
申请日：2007-07-02
申请人： DONGBU HITEK CO LTD , KOREA INST SCI & TECH , 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
发明人： 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分类号： C07D401/12
CPC分类号： C07D237/32
摘要： 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.
摘要翻译：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。

6. 发明申请

WO2010005148A3 NOVEL ISOINDOLINONE DERIVATIVES HAVING INHIBITORY ACTIVITY AGAINST T-TYPE CALCIUM CHANNEL AND METHOD FOR PREPARATION THEREOF 审中-公开
标题翻译：具有对T型钙通道的抑制活性的新型异吲哚啉酮衍生物及其制备方法
公开(公告)号：WO2010005148A3
公开(公告)日：2010-07-01
申请号：PCT/KR2008005784
申请日：2008-10-01
申请人： KOREA INST SCI & TECH , 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
发明人： 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分类号： C07D403/12
CPC分类号： C07D401/12 , A61K31/454
摘要： 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.
摘要翻译：公开了具有抑制T-型钙通道活性的异吲哚啉酮衍生物，其药学上可接受的盐，其制备方法以及包含其作为活性成分的药物组合物。

7. 发明公开

KR20200126354A 진세노사이드 Rb2를 포함하는 신경세포 보호용 조성물 审中-公开
公开(公告)号：KR20200126354A
公开(公告)日：2020-11-06
申请号：KR20200138311
申请日：2020-10-23
申请人： KOREA INST SCI & TECH
发明人： LEE JAE WOOK , KIM DONG HOI , SELVARAJ BASKAR , LIM SANG MIN , JUNG SANG HOON , KWON HAK CHEOL , PAE AE NIM
IPC分类号： A61K31/704 , A23L33/125 , A61P25/16 , A61P25/28
摘要： 본명세서는진세노사이드 Rb2을유효성분으로서포함하는조성물에관한것이다. 이러한본 명세서의조성물은산화적스트레스로부터신경세포를보호하고, 신경세포의사멸을억제하는효과를나타낸다. 또한, 세포내에서산화적스트레스의증가로인해발생하는세포사멸을억제하는항산화효소의발현을증가시킬수 있다. 따라서, 본명세서의조성물은산화적스트레스로부터신경세포의사멸로인하여발생될수 있는 2차적질병을예방, 개선또는치료하는효과를나타낼수 있어약학또는식품조성물로서사용될수 있다.

8. 发明公开

KR20120021370A 2-AZACYCLICAMINO-4-PHENYLPYRIMIDINE DERIVATIVES AS IKK-β INHIBITORS 有权
标题翻译： 2-AZACYCLICAMINO-4-PHYYLPYRIMIDINE DERIVATIVES AS IKK-ßINHIBITORS
公开(公告)号：KR20120021370A
公开(公告)日：2012-03-09
申请号：KR20100073077
申请日：2010-07-28
申请人： KOREA INST SCI & TECH
发明人： CHOO HYUN AH , PAE AE NIM , SHIN KYE JUNG , NAM GHIL SOO , ROH EUN JOO , CHO YONG SEO , KIM SO RA , JUNG JIN KYO , CHUNG HYE JIN
IPC分类号： C07D401/12 , A61K31/506 , A61P29/00 , C07D403/12
摘要： PURPOSE: A 2-azacyclicamino-4-phenylpyrimidine derivative is provided to treat and prevent inflammatory disease such as rheumatoid arthritis and asthma. CONSTITUTION: A 2-azacyclic amino-4-phenylpyrimidine compound is denoted by chemical formula 1. A pharmaceutical composition for treating inflammatory diseases or cancer contains the compound of chemical formula 1 as an active ingredient. The inflammatory diseases are rheumatoid arthritis, degenerative arthritis, asthma, or chronic obstructive pulmonary disease.
摘要翻译：目的：提供2-氮杂环氨基-4-苯基嘧啶衍生物，以治疗和预防类风湿性关节炎和哮喘等炎性疾病。构成：2-氮杂环丁基-4-苯基嘧啶化合物由化学式1表示。用于治疗炎性疾病或癌症的药物组合物含有化学式1的化合物作为活性成分。炎性疾病是类风湿性关节炎，退行性关节炎，哮喘或慢性阻塞性肺疾病。

9. 发明授权

KR100743256B1 6-VINYLIDENE-HEXAHYDRO-PYRROLIZIN-3-ONE DERIVATIVES AND THEIR PREPARATION METHOD 无效
标题翻译： 6-乙烯基 - 六氢吡喃-3-酮衍生物及其制备方法
公开(公告)号：KR100743256B1
公开(公告)日：2007-07-20
申请号：KR20060046152
申请日：2006-05-23
申请人： KOREA INST SCI & TECH
发明人： CHO YONG SEO , CHOO HYUN AH , PAE AE NIM , CHA JOO HWAN , KIM SANG HEE , KIM HYUNG GYU
IPC分类号： C07D487/04
摘要： Novel 6-vinylidene-hexahydro-pyrrolizin-3-one derivatives and their preparation method are provided to serve intermediates for synthesis of various natural products and development of new drugs by introducing various substituents to the C-6 site. The 6-vinylidene-hexahydro-pyrrolizin-3-one derivatives represented by the formula(1) are provided, wherein R1 and R2 are each independently hydrogen, C1-C6 alkyl group or C1-C6 alkoxy group or form a 5- to 10-membered aliphatic or aromatic hydrocarbon ring together; and the 6-vinylidene-hexahydro-pyrrolizin-3-one derivatives are prepared by subjecting hydroxylactam containing trimethylsilylmethyl-allene to intramolecular acyliminium cyclization in the presence of Lewis acid selected from trimethylsilyl trifluoromethanesulfonate, borontrifluoride etherate and indium halide in a reaction solvent selected from dichloromethane, chloroform and diethylether at 0-25 deg.C.
摘要翻译：提供了新的6-亚乙烯基 - 六氢 - 吡咯烷-3-酮衍生物及其制备方法，为C-6位点引入各种取代基提供合成各种天然产物和开发新药的中间体。提供由式（1）表示的6-亚乙烯基 - 六氢 - 吡咯烷-3-酮衍生物，其中R 1和R 2各自独立地为氢，C 1 -C 6烷基或C 1 -C 6烷氧基或形成5-至10 一起形成脂族或芳族烃环; 6-亚乙烯基 - 六氢 - 吡咯烷-3-酮衍生物是通过在选自三氟甲磺酸三甲基甲硅烷基酯，三氟化硼醚合物和卤化铟的路易斯酸存在下，在含有三甲基甲硅烷基甲基 - 丙烯的三羟甲基甲硅烷基甲基 - ，氯仿和乙醚在0-25℃。

10. 发明公开

KR20070113384A RING-FUSED LACTAM DERIVATIVES WITH A DIEXOMETHYLENE MOIETY AND THEIR PREPARATION METHOD 无效
标题翻译：具有二甲基乙烯基环的环状乳糖衍生物及其制备方法
公开(公告)号：KR20070113384A
公开(公告)日：2007-11-29
申请号：KR20060046149
申请日：2006-05-23
申请人： KOREA INST SCI & TECH
发明人： CHO YONG SEO , CHOO HYUN AH , CHA JOO HWAN , PAE AE NIM , KIM SANG HEE , KIM HYUNG GYU
IPC分类号： C07D471/04
CPC分类号： C07D471/04 , C07D471/14
摘要： A ring-fused lactam derivative with a diexomethylene moiety is provided to be very useful in medicine as well as precision chemistry industries and be useful as an intermediate for preparing an important multicyclic compound through the Diels-Alder reaction. And a method for preparing the same is provided to mass-produce the desired product industrially through a relatively simple process. A ring-fused lactam derivative with a diexomethylene moiety is represented by the formula(1), wherein R1 is H or C1-6 alkyl; each R2 and R3 is H, C1-6 alkyl or C1-6 alkoxy, or the R2 and R3 are bound to each other to form a pentagonal to a decagonal aliphatic or an aromatic hydrocarbon ring; and n is 0 or 1. A method for preparing the compound of the formula(1) comprises a step of subjecting hydroxy lactam including trimethylsilylmethyl-allene represented by the formula(2) to the intramolecular acyliminium cyclization in the presence of Lewis acid.
摘要翻译：提供具有阴离子亚甲基部分的稠环内酰胺衍生物在医药和精密化学工业中非常有用，并且可用作通过Diels-Alder反应制备重要多环化合物的中间体。提供了制备该方法的方法，通过相对简单的方法在工业上大量生产所需的产物。具有阴离子亚甲基部分的环稠合内酰胺衍生物由式（1）表示，其中R 1是H或C 1-6烷基; 每个R 2和R 3是H，C 1-6烷基或C 1-6烷氧基，或者R 2和R 3彼此结合以形成五边形至十五烷基或芳族烃环; 并且n为0或1.制备式（1）化合物的方法包括在路易斯酸存在下，将包含式（2）表示的三甲基甲硅烷基甲基 - 丙烯的羟基内酰胺进行分子内酰基亚胺鎓环化的步骤。

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