公开(公告)号：US07351843B2

公开(公告)日：2008-04-01

申请号：US10581799

申请日：2004-12-24

申请人： Kyu Yang Yi ,  Sun Kyung Lee ,  Nak Jeong Kim ,  Jee Hee Suh ,  Soon Hee Hwang ,  Byung Ho Lee ,  Ho Won Seo ,  Sun Kyung Hwang ,  Sung Eun Yoo ,  Kyung Hee Lee

发明人： Kyu Yang Yi ,  Sun Kyung Lee ,  Nak Jeong Kim ,  Jee Hee Suh ,  Soon Hee Hwang ,  Byung Ho Lee ,  Ho Won Seo ,  Sun Kyung Hwang ,  Sung Eun Yoo ,  Kyung Hee Lee

IPC分类号： C07D307/02 ,  A61K31/34 ,  A01N43/08

CPC分类号： C07D307/68

摘要： The present invention relates to furancarbonylguanidine derivatives, a preparation method thereof and a pharmaceutical composition comprising the same.Furancarbonylguanidine derivatives of the present invention inhibit NHE-1 (sodium-hydrogen exchanger isoform 1), which helps recovery of heart function damaged from ischemia/reperfusion and decreases myocardial infarction rate, indicating that they have protective effect on myocardial cells. Thus, furancarbonylguanidine derivatives of the present invention can be effectively used for the prevention and the treatment of ischemic heart diseases such as myocardial infarction, arrhythmia, angina pectoris, etc, and also a promising candidate for a heart protecting agent applied to reperfusion therapy including thrombolytics or cardiac surgery including coronary artery bypass graft, percutaneous transluminal coronary angioplasty, etc.

摘要翻译： 本发明涉及呋喃羰基胍衍生物，其制备方法和包含其的药物组合物。 本发明的呋喃羰基胍衍生物抑制NHE-1（钠氢交换异构体1），其有助于恢复从缺血/再灌注损伤的心脏功能，并降低心肌梗死率，表明它们对心肌细胞具有保护作用。 因此，本发明的呋喃羰基胍衍生物可以有效地用于预防和治疗心肌梗死，心律失常，心绞痛等缺血性心脏病，也是应用于再灌注治疗的心脏保护剂的有希望的候选物，包括溶栓剂 或心脏手术，包括冠状动脉旁路移植术，经皮腔内冠状动脉血管成形术等

公开(公告)号：US07309793B2

公开(公告)日：2007-12-18

申请号：US10558020

申请日：2004-05-28

申请人： Hong Lim ,  Dong Ha Lee ,  Sun Ok Kim ,  Sung-Eun Yoo ,  Kyu Yang Yi ,  Sun Kyung Lee ,  Jee Hee Suh ,  Nak Jeong Kim ,  Sun Kyung Hwang ,  Tae Mi Kim ,  Byung Ho Lee ,  Ho-Won Seo

发明人： Hong Lim ,  Dong Ha Lee ,  Sun Ok Kim ,  Sung-Eun Yoo ,  Kyu Yang Yi ,  Sun Kyung Lee ,  Jee Hee Suh ,  Nak Jeong Kim ,  Sun Kyung Hwang ,  Tae Mi Kim ,  Byung Ho Lee ,  Ho-Won Seo

IPC分类号： C07D235/26 ,  C07D235/28 ,  C07D235/30

CPC分类号： C07D405/04 ,  C07D405/14

摘要： The present invention relates to benzopyran derivatives substituted with a benzimidazole derivative, or pharmaceutically acceptable salts thereof, a preparation method of the same and pharmarceutical compositions containing them. Benzopyran derivatives substituted with a benzimidazole derivative, represented in Formula (1), have the function of protecting heart from ischemia-reperfusion without side effect like vasodilation, so that a pharmaceutical composition containing benzopyran derivatives substituted with a benzimidazole derivative or pharmaceutically acceptable salts thereof of the present invention as an effective ingredient can be effectively used for the protection of tissues influenced by ischemia-reperfusion, for example, for the protection of heart, nervous cells, brain, retinal cells, storage organs, etc. and for the treatment of diseases caused by ischemia-reperfusion.

摘要翻译： 本发明涉及用苯并咪唑衍生物取代的苯并吡喃衍生物或其药学上可接受的盐，其制备方法和含有它们的药物组合物。 由式（1）表示的苯并咪唑衍生物取代的苯并吡喃衍生物具有保护心脏免于缺血再灌注而无副作用如血管舒张的功能，因此含有苯并咪唑衍生物或其药学上可接受的盐取代的苯并吡喃衍生物的药物组合物 作为有效成分的本发明可以有效地用于保护受缺血再灌注影响的组织，例如用于保护心脏，神经细胞，脑，视网膜细胞，储存器官等，并用于治疗疾病 由缺血再灌注引起。

公开(公告)号：US06323238B1

公开(公告)日：2001-11-27

申请号：US09693082

申请日：2000-10-20

申请人： Sung-Eun Yoo ,  Kyu Yang Yi ,  Sun Kyung Lee ,  Nak-Jeong Kim ,  Jee Hee Suh ,  Young Sook Park ,  Sun Kyung Hwang ,  Hwa Sup Shin ,  Byung Ho Lee ,  Ho Won Seo ,  Hong Lim ,  Sun-Ok Kim ,  In Sun Cho ,  Miae Namgoong ,  Dongsoo Jang

发明人： Sung-Eun Yoo ,  Kyu Yang Yi ,  Sun Kyung Lee ,  Nak-Jeong Kim ,  Jee Hee Suh ,  Young Sook Park ,  Sun Kyung Hwang ,  Hwa Sup Shin ,  Byung Ho Lee ,  Ho Won Seo ,  Hong Lim ,  Sun-Ok Kim ,  In Sun Cho ,  Miae Namgoong ,  Dongsoo Jang

IPC分类号： C07D31174

CPC分类号： C07D407/04 ,  A61K31/155 ,  A61K31/352 ,  C07D311/68

摘要： The present invention relates to novel benzopyranyl guanidine derivatives of the formula 1, process for preparation therof and pharmaceutical use of the benzopyranyl guanidine derivatives. The benzopyranyl guanidine derivatives of the present invention can be used for protecting heart, neuronal cell or brain damage, preserving organs, and also the benzopyranyl guanidine derivatives are pharmacologically useful for inhibiting NO generation, and for suppressing lipid peroxidation, angiogenesis or restenosis. Wherein R1, R2, R3, R4, R5, R6, n and * are each defined in specification.

摘要翻译： 本发明涉及式1的新型苯并吡喃基胍衍生物，其制备方法和苯并吡喃基胍衍生物的药物用途。 本发明的苯并吡喃基胍衍生物可用于保护心脏，神经元细胞或脑损伤，保存器官，苯并吡喃基胍衍生物在药理学上可用于抑制NO产生，抑制脂质过氧化，血管生成或再狭窄。其中R1 ，R2，R3，R4，R5，R6，n和*各自在说明书中定义。

公开(公告)号：US07420060B2

公开(公告)日：2008-09-02

申请号：US10558111

申请日：2004-05-28

申请人： Hong Lim ,  Dong Ha Lee ,  Sun Ok Kim ,  Sung-Eun Yoo ,  Kyu Yang Yi ,  Sun Kyung Lee ,  Jee Hee Suh ,  Nak Jeong Kim ,  Sun Kyung Hwang ,  Tae Mi Kim ,  Byung Ho Lee ,  Ho-Won Seo

发明人： Hong Lim ,  Dong Ha Lee ,  Sun Ok Kim ,  Sung-Eun Yoo ,  Kyu Yang Yi ,  Sun Kyung Lee ,  Jee Hee Suh ,  Nak Jeong Kim ,  Sun Kyung Hwang ,  Tae Mi Kim ,  Byung Ho Lee ,  Ho-Won Seo

IPC分类号： C07D263/58

CPC分类号： C07D413/04

摘要： The present invention relates to benzopyran derivatives substituted with a thioxobenzoxazole derivative, or pharmaceutically acceptable salts thereof, processes for preparing the same and a pharmaceutical composition containing the above as an effective ingredient Benzopyran derivatives substituted with thioxobenzoxazole derivatives, represented in , have the function of protecting heart from ischemia-reperfusion both in vivo and in vitro, so that a pharmaceutical composition containing benzopyran derivatives substituted with thioxobenzoxoazole derivatives or pharmaceutically acceptable salts thereof of the present invention as an effective ingredient can be effectively used for the protection of tissues influenced by ischemia-reperfusion, for example, for the protection of heart, nervous cells, brain, retinal cells, storage organs, etc, and for the treatment of diseases caused by ischemia-reperfusion.

摘要翻译： 本发明涉及用硫代苯并恶唑衍生物取代的苯并吡喃衍生物或其药学上可接受的盐，其制备方法和含有上述作为有效成分的药物组合物用<式1>所示的噻吩并恶唑衍生物取代的苯并吡喃衍生物具有 在体内和体外保护心脏免于缺血 - 再灌注的功能，使得含有本发明的噻唑并苯并恶唑衍生物或其可药用盐取代的苯并吡喃衍生物的药物组合物作为有效成分可以有效地用于保护组织 受缺血再灌注的影响，例如保护心脏，神经细胞，脑，视网膜细胞，储存器官等，以及治疗由局部缺血 - 再灌注引起的疾病。

公开(公告)号：US07279497B2

公开(公告)日：2007-10-09

申请号：US10523015

申请日：2003-07-30

申请人： Kyu Yang Yi ,  Sun Kyung Lee ,  Sung-Eun Yoo ,  Jee Hee Suh ,  Nak Jeong Kim ,  Sun Kyung Hwang ,  Byung-Ho Lee ,  Ho Won Seo ,  Chong Ock Lee ,  Sang-Un Choi

发明人： Kyu Yang Yi ,  Sun Kyung Lee ,  Sung-Eun Yoo ,  Jee Hee Suh ,  Nak Jeong Kim ,  Sun Kyung Hwang ,  Byung-Ho Lee ,  Ho Won Seo ,  Chong Ock Lee ,  Sang-Un Choi

IPC分类号： A61K31/4164 ,  C07D233/54

CPC分类号： C07D405/12

摘要： The present invention relates to benzopyran derivatives substituted with secondary amines including imidazole, their preparation, and pharmaceutical compositions containing them. The present invention is pharmacologically useful for the treatment of cancer, rheumatoid arthritis, and diabetic retinopathies through anti-angiogenic properties, and also pharmacologically useful in the protection of heart and neuronal cells against ischemia-reperfusion injury or preserving organs.

摘要翻译： 本发明涉及被仲胺包括咪唑取代的苯并吡喃衍生物，其制备方法和含有它们的药物组合物。 本发明在药理学上可用于通过抗血管生成特性治疗癌症，类风湿性关节炎和糖尿病性视网膜病变，并且还可用于保护心脏和神经细胞免受缺血再灌注损伤或保存器官的药理作用。

公开(公告)号：US06413983B1

公开(公告)日：2002-07-02

申请号：US09724029

申请日：2000-11-28

申请人： Sung-Eun Yoo ,  Sun Kyung Lee ,  Kyu Yang Yi ,  Nak Jeong Kim ,  Jee Hee Suh ,  Hwa Sup Shin ,  Byung Ho Lee ,  Ho Won Seo ,  Hong Lim ,  Sun-Ok Kim ,  Dongha Lee ,  Insun Cho ,  Miae Namgung ,  Dongsoo Jang

发明人： Sung-Eun Yoo ,  Sun Kyung Lee ,  Kyu Yang Yi ,  Nak Jeong Kim ,  Jee Hee Suh ,  Hwa Sup Shin ,  Byung Ho Lee ,  Ho Won Seo ,  Hong Lim ,  Sun-Ok Kim ,  Dongha Lee ,  Insun Cho ,  Miae Namgung ,  Dongsoo Jang

IPC分类号： A01N4342

CPC分类号： C07D498/14 ,  C07D405/04

摘要： The present invention relates to novel benzopyranyl heterocycle derivatives of the formula 1, process for preparation thereof and pharmaceutical use of the benzopyranyl heterocycle derivatives. The benzopyranyl heterocycle derivatives of the present invention can be used for protecting heart, brain, retina and neuronal cell from “ischemia-reperfusion” injury, treatment for diseases related to it and suppressing lipid peroxidation. Wherein R1, R2, R3, R4, n and * are each defined in specification.

摘要翻译： 本发明涉及式1的新型苯并吡喃基杂环衍生物，其制备方法和苯并吡喃基杂环衍生物的药物用途。 本发明的苯并吡喃基杂环衍生物可用于保护心脏，脑，视网膜和神经元细胞免受“缺血再灌注”损伤，治疗与之相关的疾病和抑制脂质过氧化作用。其中R1，R2，R3，R4，n 和*各自在规范中定义。

公开(公告)号：US08143307B2

公开(公告)日：2012-03-27

申请号：US11794238

申请日：2005-12-27

申请人： Kyu Yang Yi ,  SunKyung Lee ,  Jee Hee Suh ,  Nak Jeong Kim ,  Hyunsuk Lee ,  Byung-Ho Lee ,  Sung-eun Yoo ,  Kyung-Hee Lee ,  Yong Oh Lee

发明人： Kyu Yang Yi ,  SunKyung Lee ,  Jee Hee Suh ,  Nak Jeong Kim ,  Hyunsuk Lee ,  Byung-Ho Lee ,  Sung-eun Yoo ,  Kyung-Hee Lee ,  Yong Oh Lee

IPC分类号： A61K31/381 ,  C07D333/56

CPC分类号： C07D333/70

摘要： The present invention is related to benzothiophen-2-carbonylguanidine derivatives, a preparation method thereof, and pharmaceutical compositions containing the same. The derivatives have potent inhibitory effect on the sodium/hydrogen exchanger NHE-I, improve the functional recovery of ischemia/reperfusion-induced heart injury in isolated ischemic heart models, and significantly reduce the myocardiac infarct size in in vivo ischemic animal models, thereby showing excellent cardioprotective effects. Also, the derivatives are protective of both neuronal cells and the brain as proven by their protective effects on neuronal cells from necrosis and apoptosis and by their ability to significantly reduce cerebral infarct sizes in in vivo ischemic brain models. The derivatives can be effectively used for the prevention and treatment of ischemic heart diseases such as myocardiac infarction, arrhythmia, angina pectoris and the like, and cerebrovascular diseases such as cerebral stroke and be used as cardioprotective agents to the patients undergoing reperfusion therapy including chemicals such as thrombolytic agents, or surgery such as coronary artery bypass and percutaneous transluminal coronary angioplasty.

摘要翻译： 本发明涉及苯并噻吩-2-羰基胍衍生物，其制备方法和含有它们的药物组合物。 该衍生物对钠/氢交换器NHE-1具有有效的抑制作用，改善了分离缺血心脏模型缺血/再灌注诱导的心脏损伤的功能恢复，并显着降低了体内缺血动物模型中的心肌梗死面积，从而显示 良好的心脏保护作用。 此外，衍生物保护神经元细胞和脑，如通过其对来自坏死和凋亡的神经元细胞的保护作用以及通过其在体内缺血性脑模型中显着降低脑梗塞大小的能力所证明的。 该衍生物可以有效地用于预防和治疗心肌梗塞，心律失常，心绞痛等缺血性心脏病，脑血管疾病如脑卒中，并用作心脏保护剂，用于接受再灌注治疗的患者，包括化学药剂 作为溶栓剂，或手术如冠状动脉旁路和经皮腔内冠状动脉成形术。

公开(公告)号：US20100004466A1

公开(公告)日：2010-01-07

申请号：US11794238

申请日：2005-12-27

申请人： Kyu Yang Yi ,  SunKyung Lee ,  Jee Hee Suh ,  Nak Jeong Kim ,  Hyunsuk Lee ,  Byung-Ho Lee ,  Sung-eun Yoo ,  Kyung-Hee Lee ,  Yong Oh Lee

发明人： Kyu Yang Yi ,  SunKyung Lee ,  Jee Hee Suh ,  Nak Jeong Kim ,  Hyunsuk Lee ,  Byung-Ho Lee ,  Sung-eun Yoo ,  Kyung-Hee Lee ,  Yong Oh Lee

IPC分类号： C07D333/54

CPC分类号： C07D333/70

摘要： The present invention is related to benzothiophen-2-carbonylguanidine derivatives, a preparation method thereof, and pharmaceutical compositions containing the same. The derivatives have potent inhibitory effect on the sodium/hydrogen exchanger NHE-I, improve the functional recovery of ischemia/reperfusion-induced heart injury in isolated ischemic heart models, and significantly reduce the myocardiac infarct size in in vivo ischemic animal models, thereby showing excellent cardioprotective effects. Also, the derivatives are protective of both neuronal cells and the brain as proven by their protective effects on neuronal cells from necrosis and apoptosis and by their ability to significantly reduce cerebral infarct sizes in in vivo ischemic brain models. The derivatives can be effectively used for the prevention and treatment of ischemic heart diseases such as myocardiac infarction, arrhythmia, angina pectoris and the like, and cerebrovascular diseases such as cerebral stroke and be used as cardioprotective agents to the patients undergoing reperfusion therapy including chemicals such as thrombolytic agents, or surgery such as coronary artery bypass and percutaneous transluminal coronary angioplasty.

摘要翻译： 本发明涉及苯并噻吩-2-羰基胍衍生物，其制备方法和含有它们的药物组合物。 该衍生物对钠/氢交换器NHE-1具有有效的抑制作用，改善了分离缺血心脏模型缺血/再灌注诱导的心脏损伤的功能恢复，并显着降低了体内缺血动物模型中的心肌梗死面积，从而显示 良好的心脏保护作用。 此外，衍生物保护神经元细胞和脑，如通过其对来自坏死和凋亡的神经元细胞的保护作用以及通过其在体内缺血性脑模型中显着降低脑梗塞大小的能力所证明的。 该衍生物可以有效地用于预防和治疗心肌梗塞，心律失常，心绞痛等缺血性心脏病，脑血管疾病如脑卒中，并用作心脏保护剂，用于接受再灌注治疗的患者，包括化学药剂 作为溶栓剂，或手术如冠状动脉旁路和经皮腔内冠状动脉成形术。

公开(公告)号：US08372862B2

公开(公告)日：2013-02-12

申请号：US12765363

申请日：2010-04-22

申请人： Nak Jeong Kim ,  Myung-Ae Bae ,  Sung-Eun Yoo ,  Namsook Kang ,  Jung Nyoung Heo ,  Kyu Yang Yi ,  Jee Hee Suh ,  Sung Youn Chang ,  Eun Sook Hwang ,  Jeong-Ho Hong

发明人： Nak Jeong Kim ,  Myung-Ae Bae ,  Sung-Eun Yoo ,  Namsook Kang ,  Jung Nyoung Heo ,  Kyu Yang Yi ,  Jee Hee Suh ,  Sung Youn Chang ,  Eun Sook Hwang ,  Jeong-Ho Hong

IPC分类号： A01N43/42 ,  A61K31/44

CPC分类号： C07D471/04 ,  A61K31/437 ,  C07D403/10

摘要： A phamaceutical composition comprising a phenyltetrazole derivative of formula (I) or a pharmaceutical acceptable salt thereof is effective in preventing or treating osteoporosis, obesity, diabetes, or hyperlipidemia, by regulating protein TAZ. wherein, A is ethyl or n-butyl; R1 is methyl, —CH2OH, —CO2CH3, —CH2F, —CH(OCH3)2, —CH2OC(═O)CH3, styryl or —CH2OCH2SCH3; R2 is H, Br, —CO2CH3, phenyl, pyridin-2-yl, pyridin-3-yl,  or styryl; R3 is H or methyl; X is CH or N; and P is H or —CH(CH3)OCH2CH3.

摘要翻译： 通过调节蛋白质TAZ，包含式（I）的苯基四唑衍生物或其药学上可接受的盐的药物组合物可有效预防或治疗骨质疏松症，肥胖症，糖尿病或高脂血症。 其中A为乙基或正丁基; R1是甲基，-CH2OH，-COO2CH3，-CH2F，-CH（OCH3）2，-CH2OC（= O）CH3，苯乙烯基或-CH2OCH2SCH3; R 2是H，Br，-CO 2 CH 3，苯基，吡啶-2-基，吡啶-3-基或苯乙烯基; R3是H或甲基; X是CH或N; 并且P是H或-CH（CH 3）OCH 2 CH 3。

公开(公告)号：US20100305324A1

公开(公告)日：2010-12-02

申请号：US12765363

申请日：2010-04-22

申请人： Nak Jeong KIM ,  Myung-Ae Bae ,  Sung-Eun Yoo ,  Namsook Kang ,  Jung Nyoung Heo ,  Kyu Yang Yi ,  Jee Hee Suh ,  Sung Youn Chang ,  Eun Sook Hwang ,  Jeong-Ho Hong

发明人： Nak Jeong KIM ,  Myung-Ae Bae ,  Sung-Eun Yoo ,  Namsook Kang ,  Jung Nyoung Heo ,  Kyu Yang Yi ,  Jee Hee Suh ,  Sung Youn Chang ,  Eun Sook Hwang ,  Jeong-Ho Hong

IPC分类号： C07D471/04 ,  C07D403/10

CPC分类号： C07D471/04 ,  A61K31/437 ,  C07D403/10

摘要： A phamaceutical composition comprising a phenyltetrazole derivative of formula (I) or a pharmaceutical acceptable salt thereof is effective in preventing or treating osteoporosis, obesity, diabetes, or hyperlipidemia, by regulating protein TAZ. wherein, A is ethyl or n-butyl; R1 is methyl, —CH2OH, —CO2CH3, —CH2F, —CH(OCH3)2, —CH2OC(═O)CH3, styryl or —CH2OCH2SCH3; R2 is H, Br, —CO2CH3, phenyl, pyridin-2-yl, pyridin-3-yl,  or styryl; R3 is H or methyl; X is CH or N; and P is H or —CH(CH3)OCH2CH3.

摘要翻译： 通过调节蛋白质TAZ，包含式（I）的苯基四唑衍生物或其药学上可接受的盐的药物组合物可有效预防或治疗骨质疏松症，肥胖症，糖尿病或高脂血症。 其中A为乙基或正丁基; R1是甲基，-CH2OH，-COO2CH3，-CH2F，-CH（OCH3）2，-CH2OC（= O）CH3，苯乙烯基或-CH2OCH2SCH3; R 2是H，Br，-CO 2 CH 3，苯基，吡啶-2-基，吡啶-3-基或苯乙烯基; R3是H或甲基; X是CH或N; 并且P是H或-CH（CH 3）OCH 2 CH 3。