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    Halogenated wang resins for combinatorial chemical synthesis
    35.
    发明授权
    Halogenated wang resins for combinatorial chemical synthesis 失效
    用于组合化学合成的卤化王树脂

    公开(公告)号：US06482898B1

    公开(公告)日：2002-11-19

    申请号：US09762780

    申请日：2001-04-12

    Applicant: Sung Eun Yoo ,  Young Dae Gong ,  Jin Soo Seo

    Inventor： Sung Eun Yoo ,  Young Dae Gong ,  Jin Soo Seo

    IPC: C08F818

    CPC classification number: C07C43/23 ,  C07B2200/11

    Abstract: The present invention relates to novel halogenated Wang resins for combinational chemical synthesis, more specifically to halogenated Wang resins expressed by formula (1) useful for the effective tracing of combinational chemical synthetic process on solid supports using X-ray photoelectron spectroscopy (XPS) element analysis method; in formula (1), P represents polystyrene-divinylbenzene; X and Y represent hydrogen atom or halogen atom, which may be identical or different, their total number being 1-4; and at least one of them is halogen atom.

    Abstract translation: 本发明涉及用于组合化学合成的新型卤化Wang树脂，更具体地说，涉及用于使用X射线光电子能谱（XPS）元素分析在固体支持物上有效追踪组合化学合成方法的式（1）表示的卤化Wang树脂 方法; 在式（1）中，P表示聚苯乙烯 - 二乙烯基苯; X和Y表示氢原子或卤素原子，其可以相同或不同，它们的总数为1-4; 并且其中至少一个是卤素原子。

    Pyridyl imidazole derivatives and processes for the preparation thereof
    36.
    发明授权
    Pyridyl imidazole derivatives and processes for the preparation thereof 失效
    吡啶基咪唑衍生物及其制备方法

    公开(公告)号：US5691348A

    公开(公告)日：1997-11-25

    申请号：US750460

    申请日：1996-12-08

    Applicant: Sung-Eun Yoo ,  Kyu-Yang Yi ,  Sang-Hee Lee ,  Hye-Ryung Kim ,  Jee-Hee Suh ,  Nak-Jeong Kim ,  Seon-Ju Kim ,  Ok-Ja Cha ,  Young-Ah Shin ,  Wha-Sup Shin ,  Sung-Hou Lee ,  Yi-Sook Jung ,  Byung-Ho Lee ,  Ho-Won Seo ,  Hye-Suk Lee

    Inventor： Sung-Eun Yoo ,  Kyu-Yang Yi ,  Sang-Hee Lee ,  Hye-Ryung Kim ,  Jee-Hee Suh ,  Nak-Jeong Kim ,  Seon-Ju Kim ,  Ok-Ja Cha ,  Young-Ah Shin ,  Wha-Sup Shin ,  Sung-Hou Lee ,  Yi-Sook Jung ,  Byung-Ho Lee ,  Ho-Won Seo ,  Hye-Suk Lee

    IPC: A61K31/435 ,  A61K31/44 ,  A61P9/12 ,  A61P43/00 ,  C07D471/04

    CPC classification number: C07D471/04

    Abstract: Novel pyridyl imidazole derivatives of formula(I) inhibit effectively the action of angiotensin II and have a superior antihypertensive activity: ##STR1## wherein: A is a straight, branched or cyclic C.sub.1 -C.sub.6 alkyl or alkenyl group, OR.sup.1 (wherein R.sup.1 is a hydrogen, or a straight, branched or cyclic C.sub.1 -C.sub.6 alkyl or alkenyl radical), or NR.sup.2 R.sup.3 (wherein R.sup.2 and R.sup.3 are independently a hydrogen, or a straight, branched or cyclic C.sub.1 -C.sub.6 alkyl radical); B is a group of the following formula ##STR2## D is a hydrogen; a halogen; a straight, branched or cyclic C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl or C.sub.2 -C.sub.6 alkynyl group which is optionally substituted with OH, a C.sub.1 -C.sub.4 alkoxy radical, CO.sub.2 R.sup.1, COR.sup.1, CON(R.sup.1).sub.2 or N(R.sup.1).sub.2, wherein R.sup.1 is the same as defined above; tetrazol-5-yl; a perfluoro-C.sub.1 -C.sub.4 alkyl group; or N(R.sup.1).sub.2, OR.sup.1, CO.sub.2 R.sup.1 or CON(R.sup.1).sub.2, wherein R.sup.1 is the same as defined above; E is a hydrogen; a halogen; a straight or branched C.sub.1 -C.sub.6 alkyl, C.sub.2 -C.sub.6 alkenyl or C.sub.2 -C.sub.6 alkynyl group which is optionally substituted with OH, a C.sub.1 -C.sub.4 alkoxy radical, CO.sub.2 R.sup.1, COR.sup.1, CON(R.sup.1).sub.2 or N(R.sup.1).sub.2, wherein R.sup.1 is the same as defined above; a perfluoro-C.sub.1 -C.sub.4 alkyl group; NO.sub.2 ; or N(R.sup.1).sub.2 or OR.sup.1, wherein R.sup.1 is the same as defined above; and n is 0 or an integer of 1 to 4.

    Abstract translation: PCT No.PCT / KR95 / 00075 Sec。 371日期1996年12月6日第 102（e）日期1996年12月6日PCT归档1995年6月7日PCT公布。 出版物WO95 / 34564 日期：1995年12月21日新型式（I）吡啶基咪唑衍生物有效抑制血管紧张素II的作用，具有优异的抗高血压活性：d或环状C 1 -C 6烷基或链烯基，OR 1（其中R 1为氢或直链 ，支链或环状的C 1 -C 6烷基或链烯基）或NR 2 R 3（其中R 2和R 3独立地是氢或直链，支链或环状的C 1 -C 6烷基）; B是一组下列公式： D是氢; 卤素 任选被OH，C 1 -C 4烷氧基，CO 2 R 1，COR 1，CON（R 1）2或N（R 1）2取代的直链，支链或环状C 1 -C 6烷基，C 2 -C 6烯基或C 2 -C 6炔基 其中R1与上述相同; 四唑-5-基; 全氟-C 1 -C 4烷基; 或N（R1）2，OR1，CO2R1或CON（R1）2，其中R1与上述定义相同; E是氢; 卤素 任选被OH，C 1 -C 4烷氧基，CO 2 R 1，COR 1，CON（R 1）2或N（R 1）2取代的直链或支链C 1 -C 6烷基，C 2 -C 6烯基或C 2 -C 6炔基，其中 R1与上述定义相同; 全氟-C 1 -C 4烷基; NO2; 或N（R1）2或OR1，其中R1与上述定义相同; n为0或1〜4的整数。

    Benzopyran derivatives and processes for the preparation thereof
    37.
    发明授权
    Benzopyran derivatives and processes for the preparation thereof 失效
    苯并吡喃衍生物及其制备方法

    公开(公告)号：US5236935A

    公开(公告)日：1993-08-17

    申请号：US886986

    申请日：1992-05-21

    Applicant: Sung-Eun Yoo ,  Kyu Y. Yi ,  Nak C. Jeong ,  Jee H. Suh ,  Seon-Ju Kim ,  Hwa-Sup Shin ,  Byung H. Lee ,  Kyu S. Jung

    Inventor： Sung-Eun Yoo ,  Kyu Y. Yi ,  Nak C. Jeong ,  Jee H. Suh ,  Seon-Ju Kim ,  Hwa-Sup Shin ,  Byung H. Lee ,  Kyu S. Jung

    IPC: C07D405/04

    CPC classification number: C07D405/04

    Abstract: The present invention relates to novel benzopyran derivatives of formula (I) which have superior selectivity in the treatment of hypertension by lowering blood pressure with a relaxation activity on vascular smooth muscle. The present invention also relates to processes for preparing such compounds; and to a pharmaceutical compositions containing such compounds as an active ingredient. ##STR1## wherein: R.sub.1 is --CN, --NO.sub.2, --OCX.sub.1 X.sub.2 X.sub.3, --NH.sub.2, --NHSO.sub.2 R.sup.A, ##STR2## --SO.sub.2 R.sup.C or --SO.sub.2 NR.sup.C R.sup.D wherein X.sub.1, X.sub.2 and X.sub.3 are, each independently, a fluorine, chlorine or hydrogen atom; R.sup.A and R.sup.B are, each independently, an amino, C.sub.1-6 alkoxy, C.sub.1-6 alkyl group or an optionally substituted phenyl group; and R.sup.C and R.sup.D are a hydrogen atom, or a C.sub.1-6 alkyl group or an optionally substituted phenyl group with a halogen atom, or a straight or branched C.sub.1-3 alkyl group;R.sub.2 is ##STR3## wherein R.sup.E is a hydrogen atom, or a C.sub.1-6 alkyl, cyclopropyl, cyclopropylmethyl or benzyl group; R.sup.F is --COR.sup.A or --CSR.sup.A ; X is O, S or NR.sup.C, and n is an integer from 0 to 3, wherein R.sup.A and R.sup.C have the same meanings as defined above;R.sub.3 is a C.sub.1-4 straight or branched alkyl group; andR.sub.4 is ##STR4## wherein R.sup.G and R.sup.H are, each independently, a C.sub.-16 alkyl group or an optionally substituted phenyl group; A and B are, each independently, S or O; and Z is a C.sub.1-3 straight or branched alkyl group.

    Abstract translation: 本发明涉及新型的式（I）的苯并吡喃衍生物，其通过降低血压以及对血管平滑肌的松弛活性而在治疗高血压方面具有优异的选择性。 本发明还涉及制备这些化合物的方法; 以及含有这些化合物作为活性成分的药物组合物。 （I）其中：R1是-CN，-NO2，-OCX1X2X3，-NH2，-NHSO2RA，-SO2RC或-SO2NRCRD，其中X1，X2和X3各自独立地是氟，氯或氢 原子; RA和RB各自独立地为氨基，C 1-6烷氧基，C 1-6烷基或任选取代的苯基; 和RC和RD是氢原子，或C 1-6烷基或任选取代的具有卤素原子的苯基，或直链或支链C 1-3烷基; R2是 其中RE是氢原子或C1-6烷基，环丙基，环丙基甲基或苄基; RF是-CORA或-CSRA; X是O，S或NRC，n是0-3的整数，其中RA和RC具有与上述相同的含义; R3是C1-4直链或支链烷基; 并且R 4是，其中RG和RH各自独立地是C 16-16烷基或任选取代的苯基; A和B各自独立地为S或O; Z为直链或支链的C1-3烷基。

    Benzothiophen-2-carbonylguanidine derivatives, preparation thereof, and pharmaceutical composition containing the same
    40.
    发明授权
    Benzothiophen-2-carbonylguanidine derivatives, preparation thereof, and pharmaceutical composition containing the same 有权
    苯并噻吩-2-羰基胍衍生物及其制备方法和含有它们的药物组合物

    公开(公告)号：US08143307B2

    公开(公告)日：2012-03-27

    申请号：US11794238

    申请日：2005-12-27

    Applicant: 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

    Inventor： 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: A61K31/381 ,  C07D333/56

    CPC classification number: C07D333/70

    Abstract: 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.

    Abstract translation: 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。

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