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11. 发明公开

KR1020070065654A ＰＯＣｌ３와 벤질트리에틸암모늄 클로라이드를 이용한염소화 방법 无效
标题翻译：使用磷酰氯和苄基氯化铵氯化物的杂环化合物的氯化
公开(公告)号：KR1020070065654A
公开(公告)日：2007-06-25
申请号：KR1020050126304
申请日：2005-12-20
申请人： 에스케이케미칼주식회사
发明人： 이남규 , 이준원 , 이석호
IPC分类号： C07D495/04 , C07D239/86 , C07D239/95
摘要： A method for chlorinating a nitrogen containing-heterocyclic compound is provided to obtain a chloride with high yield and high purity through a simplified post-treating step and a purification step by using POCl3 and benzyltriethylammonium chloride. In the chlorinating method of substituting an oxygen atom in a carbonyl group existent in an alpha-position of a nitrogen-containing heterocyclic compound with a chlorine atom, the chlorination is performed using 2-25 equivalents of POCl3 as a chlorinating agent and 1-3 equivalents of benzyltriethylammonium chloride as an acid binder. The product obtained by the chlorination is further purified by washing it with water or recrystallizing it using hexane.
摘要翻译：提供含氮杂环化合物的氯化方法，通过简单的后处理步骤和通过使用POCl 3和苄基三乙基氯化铵的纯化步骤获得高产率和高纯度的氯化物。在含有氯原子的含氮杂环化合物的α位存在的羰基中的氧原子的氯化方法中，使用2-25当量的POCl 3作为氯化剂和1-3 苄基三乙基氯化铵作为酸性粘合剂。通过氯化获得的产物通过用水洗涤或使用己烷重结晶进一步纯化。

12. 发明公开

KR1020060079498A 간섬유화 및 간경화 억제 활성을 나타내는Ν-(2,2-이중치환-2Η-크로멘-6-일)싸이오우레아 유도체 有权
标题翻译：用于治疗肝纤维化和闭塞性的N-（2,2-取代的2H-克隆-6-YL）硫脲的衍生物
公开(公告)号：KR1020060079498A
公开(公告)日：2006-07-06
申请号：KR1020040117711
申请日：2004-12-31
申请人： 에스케이케미칼주식회사 , 한국화학연구원
发明人： 공영대 , 서진수 , 전문국 , 곽의종 , 조용백 , 이남규 , 이은주 , 이정범 , 이준원 , 이석호 , 동미숙 , 김정란
IPC分类号： C07D311/70
摘要： 본 발명은 TGFβ 수용체 길항활성이 우수하여 간질환 예방 및 치료제로서는 물론 여러 섬유 증식성 질환 예를 들면 간섬유화, 간경화, 폐섬유증, 피부경화증, 신사구체 섬유증 등의 예방 및 치료제로서 유효한
N- (2,2-이중치환-2H-크로멘-6-일)싸이오우레아 유도체의 의약적 용도에 관한 것이다.

TGFβ 수용체 길항, 간경화, 콜라겐, 싸이오우레아, 고체상합성, 조합화학

13. 发明公开

KR1020060079121A 당뇨 및 비만 치료예방에 유효한 퀴나졸린 유도체 无效
标题翻译：治疗或预防糖尿病和肥胖的喹唑啉衍生物
公开(公告)号：KR1020060079121A
公开(公告)日：2006-07-05
申请号：KR1020050134722
申请日：2005-12-30
申请人： 에스케이케미칼주식회사 , 한소 주식회사 , 경희대학교 산학협력단
发明人： 이남규 , 이준원 , 이석호 , 임광진 , 한혜영 , 김태곤 , 김용혁 , 곽의종 , 김상웅 , 하주헌 , 김언겸 , 이정규 , 유충열 , 이대연
IPC分类号： C07D239/74
CPC分类号： C07D413/12 , C07D239/88 , C07D239/93 , C07D239/94 , C07D401/12 , C07D403/04 , C07D403/12 , C07D405/06 , C07D405/12
摘要： 본 발명은 혈당 강하, 체중 감소를 나타내는 신규의 퀴나졸린 유도체와, 이 화합물을 유효성분으로 함유하는 당뇨 및 비만 치료예방제에 관한 것이다.
당뇨병 치료제, 비만 치료제, 퀴나졸린

14. 发明公开

KR1020060073834A 당뇨 치료예방에 유효한 크로멘-4-온 유도체 有权
标题翻译：用于治疗或预防糖尿病的化合物4-一种衍生物
公开(公告)号：KR1020060073834A
公开(公告)日：2006-06-29
申请号：KR1020040112268
申请日：2004-12-24
申请人： 에스케이케미칼주식회사
发明人： 문창규 , 이남규 , 임광진 , 이준원 , 이석호 , 김남호 , 한혜영 , 이주영 , 김형욱 , 류제호 , 정재윤 , 김태곤 , 곽의종
IPC分类号： C07D311/56
摘要： 본 발명은 혈당 강하 작용을 나타내는 크로멘-4-온 유도체와, 이 화합물을 유효성분으로 함유하는 당뇨병 치료제 조성물에 관한 것이다.

크로멘-4-온, 혈당 강하, 당뇨병 치료제

15. 发明公开

KR1020080091948A 락탐형 피리딘 화합물을 포함하는 허혈성 질환의 예방 및치료용 약학조성물 无效
标题翻译：含有LACTAM型吡啶衍生物的药物组合物作为预防和治疗异位症的有效成分
公开(公告)号：KR1020080091948A
公开(公告)日：2008-10-15
申请号：KR1020070035074
申请日：2007-04-10
申请人： 에스케이케미칼주식회사
发明人： 조용백 , 이준원 , 이정범 , 이남규 , 이봉용 , 황기철 , 임소연 , 장우철 , 정지형 , 이병호 , 서호원
IPC分类号： A61K31/4375 , A61P9/10
CPC分类号： A61K31/4375
摘要： A lactam-type pyridine compound or a pharmaceutically acceptable salt thereof is provided to show excellent cell protecting activity, calcium homeostasis, and HSP(heat shock protein) expression controlling activity, thereby being useful as a composition for preventing and treating ischemic diseases. A pharmaceutical composition for treating and preventing ischemic diseases such as ischemic heart diseases and ischemia damage comprises a lactam-type pyridine compound represented by a formula(1) or a pharmaceutically acceptable salt thereof. In the formula(1), * is a single bond or a double bond; each R1, R2, R3, R4, R5, R6, and R7 is independently H, halo, nitro, C2-7 acyl, hydroxy, amino, C1-6 alkyl, C3-9 cycloalkyl, C2-6 alkenyl, C1-6 alkoxy, C1-6 alkylthio, C1-10 alkylamino, C4-9 cycloalkylamino, C4-9 heterocycloalkylamino, arylamino, C1-6 acylamino, C1-6 acyloxy, C1-6 alkylsulfinyl, C1-6 alkylsulfonylamino, arylsulfinyl, arylsulfonyl, arylsulfonylamino, aryl, heteroaryl, saturated heterocycle, aryl C1-10 alkyl, heteroaryl C1-10 alkyl, aryloxy or heteroaryloxy, or each of them together with an adjacent substitutent may form a ring; and R8 is H, C1-6 alkyl, C3-9 cycloalkyl, amino, C1-6 aminoalkyl, C1-6 alkylamino C1-6 alkyl, C1-6 hydroxyalkyl, C1-6 alkoxyalkyl, carboxyl, carboxy C1-6 alkyl, C1-6 alkoxycarbonyl, C1-6 alkoxycarbonyl C1-6 alkyl, C2-7 acyl, C2-7 acyl C1-6 alkyl, aryl, heteroaryl, saturated hetero-cycle, aryl C1-6 alkyl or heteroaryl C1-6 alkyl, or R8 may form a ring together with R6 or R7.
摘要翻译：提供内酰胺型吡啶化合物或其药学上可接受的盐以显示优异的细胞保护活性，钙稳态和HSP（热休克蛋白）表达控制活性，从而可用作预防和治疗缺血性疾病的组合物。用于治疗和预防缺血性疾病如缺血性心脏病和缺血损伤的药物组合物包含由式（1）表示的内酰胺型吡啶化合物或其药学上可接受的盐。在式（1）中，*是单键或双键; 每个R1，R2，R3，R4，R5，R6和R7独立地是H，卤素，硝基，C2-7酰基，羟基，氨基，C1-6烷基，C3-9环烷基，C2-6烯基，C1-6 烷氧基，C 1-6烷硫基，C 1-10烷基氨基，C 4-9环烷基氨基，C 4-9杂环烷基氨基，芳基氨基，C 1-6酰基氨基，C 1-6酰氧基，C 1-6烷基亚磺酰基，C 1-6烷基磺酰基氨基，芳基亚磺酰基，芳基磺酰基，芳基磺酰基氨基，芳基，杂芳基，饱和杂环，芳基C 1-10烷基，杂芳基C 1-10烷基，芳氧基或杂芳氧基，或它们各自与相邻取代基一起形成环; 且R 8为H，C 1-6烷基，C 3-9环烷基，氨基，C 1-6氨基烷基，C 1-6烷基氨基C 1-6烷基，C 1-6羟基烷基，C 1-6烷氧基烷基，羧基，羧基C 1-6烷基，C 1 -6烷氧基羰基，C 1-6烷氧基羰基C 1-6烷基，C 2-7酰基，C 2-7酰基C 1-6烷基，芳基，杂芳基，饱和杂环，芳基C 1-6烷基或杂芳基C 1-6烷基，或R 8 可与R6或R7一起形成环。

16. 发明公开

KR1020080088764A 허혈성 질환의 예방 및 치료에 유효한 크로멘-4-온 화합물 无效
标题翻译：用于治疗或预防ISCHEMIA的化合物4-一种衍生物
公开(公告)号：KR1020080088764A
公开(公告)日：2008-10-06
申请号：KR1020070031466
申请日：2007-03-30
申请人： 에스케이케미칼주식회사
发明人： 조용백 , 이준원 , 이정범 , 이남규 , 이봉용 , 황기철 , 임소연 , 장우철 , 정지형 , 이병호 , 서호원
IPC分类号： A61K31/353 , A61P9/10
摘要： Chromen-4-one derivatives are provided to protect cells in the ischemic area by controlling calcium homeostasis and HSP(heat shock protein) expression, so that the compounds are useful for the treatment or prevention of ischemic diseases including angina pectoris, myocardial infarction, cerebral apoplexy and cerebral vascular dementia. Chromen-4-one derivatives represented by the formula(1) are useful for treatment or prevention of ischemic diseases, wherein X is single bond, O, S, S(O), SCH2, Se, NH, CH2, CH2CH2 or CH=CH; R1 is C1-C6 alkyl group; phenyl group optionally substituted by halogen atom, hydroxyl, C1-C6 alkyl, C1-C6 alkoxy, C1-C6 alkylcarbonate or amino C1-C6 alkylcarbonate; pyridine group; or piperidine group optionally substituted by C1-C6 alkyl or C1-C6 alkoxy group; R2 is hydrogen atom or C1-C6 alkyl group; R3 is hydrogen atom, hydroxyl, C1-C6 alkoxy group, or C1-C6 alkylcarbonate group; R4 is hydrogen atom, halogen atom, hydroxyl group, C1-C6 alkyl group or C1-C6 alkoxy group; R5 is halogen atom; C1-C6 alkyl group, C1-C6 alkylcarbonate group, C1-C6 alkylhydroxy C1-C6 alkanoate group; hydroxyl group; C1-C6 alkoxy group; hydroxyl C1-C6 alkoxy group; benzyl C1-C6 alkoxy group optionally substituted by halogen atom, C1-C6 alkyl or C1-C6 alkoxy group; phenyl C1-C6 alkoxy group optionally substituted by C1-C6 alkyl or C1-C6 alkoxy group; pyridinyl C1-C6 alkoxy group; oxypyridinyl C1-C6 alkoxy group; piperidinyl C1-C6 alkoxy group; or morpholinyl C1-C6 alkoxy group; and R6 is hydrogen atom, halogen atom, C1-C6 alkyl group or C2-C6 alkenyl group.
摘要翻译：通过控制钙稳态和HSP（热休克蛋白）表达来提供色素-4-酮衍生物以保护缺血区域中的细胞，使得该化合物可用于治疗或预防缺血性疾病，包括心绞痛，心肌梗死，脑部中风和脑血管性痴呆。由式（1）表示的色素-4-酮衍生物可用于治疗或预防缺血性疾病，其中X为单键，O，S，S（O），SCH2，Se，NH，CH2，CH2CH2或CH = CH; R1是C1-C6烷基; 任选被卤素原子取代的苯基，羟基，C 1 -C 6烷基，C 1 -C 6烷氧基，C 1 -C 6烷基碳酸酯或氨基C 1 -C 6烷基碳酸酯; 吡啶基; 或任选被C 1 -C 6烷基或C 1 -C 6烷氧基取代的哌啶基; R2是氢原子或C1-C6烷基; R3是氢原子，羟基，C1-C6烷氧基或C1-C6烷基碳酸酯基; R4是氢原子，卤素原子，羟基，C1-C6烷基或C1-C6烷氧基; R5是卤素原子; C1-C6烷基，C1-C6烷基碳酸酯基，C1-C6烷基羟基C1-C6链烷酸酯基; 羟基; C1-C6烷氧基; 羟基C1-C6烷氧基; 任选被卤素原子取代的C1-C6烷氧基，C1-C6烷基或C1-C6烷氧基; 任选被C 1 -C 6烷基或C 1 -C 6烷氧基取代的苯基C 1 -C 6烷氧基; 吡啶基C 1 -C 6烷氧基; 氧基吡啶基C 1 -C 6烷氧基; 哌啶基C1-C6烷氧基; 或吗啉基C1-C6烷氧基; R6为氢原子，卤素原子，C1-C6烷基或C2-C6烯基。

17. 发明公开

KR1020030058858A 피리티온염의 제조 방법 有权
标题翻译：制备硫酸盐的方法
公开(公告)号：KR1020030058858A
公开(公告)日：2003-07-07
申请号：KR1020020000091
申请日：2002-01-02
申请人： 에스케이케미칼주식회사
发明人： 이준원 , 박기만 , 이남규 , 김진만 , 박정호
IPC分类号： C07F19/00
CPC分类号： C07F1/08 , C07F3/06
摘要： PURPOSE: A process for preparing pyrithione salt is provided, thereby simply preparing pyrithione salt in higher yield and purity. CONSTITUTION: A process for preparing pyrithione salt of the formula 1 comprises the steps of: (a) oxidation reacting 2-halopyridine of the formula 2 with a monopersulfate containing compound in solvent to prepare 2-halopyridine-N-oxide of the formula 3; (b) mercapto reacting the 2-halopyridine-N-oxide of the formula 3 with sulfide salt in the presence of base to prepare 2-mercaptopyridine-N-oxide of the formula 4; and (c) reacting the 2-mercaptopyridine-N-oxide of the formula 4 with metal salt in the presence of base, wherein M is Cu or Zn; X is halogen atom; and A is H, Na or K.
摘要翻译：目的：提供吡啶硫酮盐的制备方法，从而以更高的产率和纯度简单地制备吡啶硫酮盐。构成：制备式1的吡啶硫酮盐的方法包括以下步骤：（a）将式2的2-卤代吡啶与含有单过硫酸盐的化合物在溶剂中氧化反应制备式3的2-卤代吡啶-N-氧化物; （b）在碱存在下将式3的2-卤代吡啶-N-氧化物与硫化物盐进行巯基反应以制备式4的2-巯基吡啶-N-氧化物; 和（c）在碱的存在下使式4的2-巯基吡啶-N-氧化物与金属盐反应，其中M是Cu或Zn; X为卤素原子; A为H，Na或K.

18. 发明公开

KR1020080091949A 락톤형 피리딘 화합물을 포함하는 허혈성 질환의 예방 및치료용 약학조성물 无效
标题翻译：含有Lacton型吡啶衍生物的药物组合物作为预防和治疗异位症的有效成分
公开(公告)号：KR1020080091949A
公开(公告)日：2008-10-15
申请号：KR1020070035075
申请日：2007-04-10
申请人： 에스케이케미칼주식회사
发明人： 조용백 , 이준원 , 이정범 , 이남규 , 이봉용 , 황기철 , 임소연 , 장우철 , 정지형 , 이병호 , 서호원
IPC分类号： A61K31/436 , A61P9/10
CPC分类号： A61K31/436
摘要： A lacton-type pyridine compound or a pharmaceutically acceptable salt thereof is provided to control HSP(heat shock protein) expression and show cardiomyocyte protecting activity through controlling intracellular calcium homeostasis and heat protecting activity, thereby being useful as a composition for preventing and treating ischemic diseases. A pharmaceutical composition for treating and preventing ischemic diseases such as angina pectoris, myocardial infarction, stroke and cerebrovascular dementia comprises a lacton-type pyridine compound represented by a formula(1) or a pharmaceutically acceptable salt thereof. In the formula(1), * is a single bond or a double bond; X is O or S; and each R1, R2, R3, R4, R5, R6, and R7 is independently H, halo, nitro, C2-7 acyl, hydroxy, amino, C1-6 alkyl, C3-9 cycloalkyl, C2-6 alkenyl, C1-6 alkoxy, C1-6 alkoxyalkyl, C1-6 alkylthio, C1-10 alkylamino, C1-6 alkoxyalkylamino, C4-9 cycloalkylamino, C4-9 heterocycloalkylamino, aryl C1-6 alkylamino, arylamino, heteroayl C1-6 alkylamino, C2-7 acylamino, saturated heterocyclic, C2-7 acyloxy, C1-6 alkylsulfinyl, C1-6 alkylsulfonylamino, arylsulfinyl, arylsulfonyl, arylsulfonylamino, aryl, heteroaryl, aryl C1-6 alkyl, heteroaryl C1-6 alkyl, aryloxy or heteroaryloxy, or each of them together with an adjacent substitutent may form a ring.
摘要翻译：提供内酯型吡啶化合物或其药学上可接受的盐以控制HSP（热休克蛋白）表达，并通过控制细胞内钙稳态和热保护活性显示心肌细胞保护活性，从而可用作预防和治疗缺血性疾病的组合物。用于治疗和预防心绞痛，心肌梗塞，中风和脑血管性痴呆等缺血性疾病的药物组合物包含由式（1）表示的内酯型吡啶化合物或其药学上可接受的盐。在式（1）中，*是单键或双键; X是O或S; 并且每个R 1，R 2，R 3，R 4，R 5，R 6和R 7独立地为H，卤素，硝基，C 2-7酰基，羟基，氨基，C 1-6烷基，C 3-9环烷基，C 2-6烯基， C 1-6烷氧基，C 1-6烷氧基烷基，C 1-6烷硫基，C 1-10烷基氨基，C 1-6烷氧基烷基氨基，C 4-9环烷基氨基，C 4-9杂环烷基氨基，芳基C 1-6烷基氨基，芳基氨基，杂芳基C 1-6烷基氨基，C 2-7 酰基氨基，饱和杂环，C 2-7酰氧基，C 1-6烷基亚磺酰基，C 1-6烷基磺酰基氨基，芳基亚磺酰基，芳基磺酰基，芳基磺酰基氨基，芳基，杂芳基，芳基C 1-6烷基，杂芳基C 1-6烷基，芳氧基或杂芳氧基，与相邻的取代基一起形成环。

19. 发明公开

KR1020060079496A 간섬유화 및 간경화 억제 활성을 나타내는Ｎ-(2,2-이중치환-2Ｈ-크로멘-6-일)-Ｎ,Ｎ'-이중치환구아니딘 유도체 有权
标题翻译：用于治疗肝硬化和闭塞性的N-（2,2-取代的2H-克隆-6-YL）-N，N'-去离子的胍衍生物的衍生物
公开(公告)号：KR1020060079496A
公开(公告)日：2006-07-06
申请号：KR1020040117707
申请日：2004-12-31
申请人： 에스케이케미칼주식회사 , 한국화학연구원
发明人： 공영대 , 서진수 , 전문국 , 곽의종 , 조용백 , 이남규 , 이은주 , 이정범 , 이준원 , 이석호 , 동미숙 , 김정란
IPC分类号： A61K31/353 , A61K31/352
摘要： 본 발명은 TGFβ 수용체 길항활성이 우수하여 간질환 예방 및 치료제로서는 물론 여러 섬유 증식성 질환 예를 들면 간섬유화, 간경화, 폐섬유증, 피부경화증, 신사구체 섬유증 등의 예방 및 치료제로서 유효한
N- (2,2-이중치환-2H-크로멘-6-일)-
N,N' -이중치환 구아니딘 유도체의 의약적 용도에 관한 것이다.

간경화, 콜라겐합성, 구아니딘계 벤조피란, 고체상합성, 조합화학

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