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    Piperazine derivatives and process for the preparation thereof
    1.
    发明授权
    Piperazine derivatives and process for the preparation thereof 有权
    哌嗪衍生物及其制备方法

    公开(公告)号：US06683184B2

    公开(公告)日：2004-01-27

    申请号：US10105936

    申请日：2002-03-26

    申请人： Eui-Hwan Cho ,  Sun-Gan Chung ,  Sun-Hwan Lee ,  Ho-Seok Kwon ,  Dong-Wook Kang ,  Jeong-Ho Joo ,  Young-Hee Lee

    发明人： Eui-Hwan Cho ,  Sun-Gan Chung ,  Sun-Hwan Lee ,  Ho-Seok Kwon ,  Dong-Wook Kang ,  Jeong-Ho Joo ,  Young-Hee Lee

    IPC分类号： C07D40112

    CPC分类号： C07D213/74 ,  C07D213/75 ,  C07D241/20 ,  C07D295/215

    摘要： The present invention relates to a novel compound of formula (I) and its pharmaceutically acceptable acid addition salt, and process for the preparation thereof, which have strong antitumor activities and very low toxicity: wherein R1 and R2 are independently hydrogen, C1-C4 alkyl, C1-C4 alkylcarboxyl, C1-C4 alkylcarbonyl, C1-C4 alkoxy, C1-C4 hydroxyalkyl, C1-C4 aminoalkyl or C1-C4 hydroxyiminoalkyl, or R1 and R2 are fused to form C3-C4 unsaturated ring; R3, R4, R5, R6 and R7 are independently hydrogen, halogen, hydroxy, nitro, amino, C1-C4 alkyl, C1-C4 alkylcarboxyl, C1-C4 alkylcarbonyl, C1-C4 alkoxy, C1-C4 thioalkoxy; R8 is C1-C4 alkyl; Y is oxygen, sulphur, amino, subsitituted amino or C1-C4 thioalkyl; Z is C1-C4 alkoxy, C1-C4 alkyl, C1-C4 alkylamino or C1-C4 thioalkoxy; X1 and X2 are independently CH or nitrogen; and —N═C— and —C═Y— may form a single bond or a double bond provided that if —N═C— forms a single bond, —C═Y— forms a double bond, and if —C═Y— forms a single bond, —N═C— forms a double bond and R8 is nonexistent.

    摘要翻译： 本发明涉及一种新的式（I）化合物及其药学上可接受的酸加成盐及其制备方法，其具有强的抗肿瘤活性和极低的毒性：其中R1和R2独立地为氢，C1-C4烷基 ，C1-C4烷基羧基，C1-C4烷基羰基，C1-C4烷氧基，C1-C4羟基烷基，C1-C4氨基烷基或C1-C4羟基亚氨基烷基，或R1和R2稠合形成C3-C4不饱和环; R3，R4，R5 ，R6和R7独立地是氢，卤素，羟基，硝基，氨基，C1-C4烷基，C1-C4烷基羧基，C1-C4烷基羰基，C1-C4烷氧基，C1-C4硫代烷氧基; R8是C1-C4烷基; Y是氧，硫，氨基，取代的氨基或C1-C4硫代烷基; Z是C1-C4烷氧基，C1-C4烷基，C1-C4烷基氨基或C1-C4硫代烷氧基; X1和X2独立地是CH或氮; 并且-N = C-和-C = Y-可以形成单键或双键，条件是如果-N = C-形成单键，则-C = Y-形成双键，并且如果-C = Y - 形成单键，-N = C-形成双键，R8不存在。

    Piperazine derivatives and process for the preparation thereof
    2.
    发明授权
    Piperazine derivatives and process for the preparation thereof 失效

    公开(公告)号：US6028195A

    公开(公告)日：2000-02-22

    申请号：US29660

    申请日：1998-02-27

    申请人： Eui-Hwan Cho ,  Sun-Gan Chung ,  Sun-Hwan Lee ,  Ho-Seok Kwon ,  Jae-Eung Lee ,  Dong-Wook Kang ,  Jeong-Ho Joo ,  Young-Hee Lee

    发明人： Eui-Hwan Cho ,  Sun-Gan Chung ,  Sun-Hwan Lee ,  Ho-Seok Kwon ,  Jae-Eung Lee ,  Dong-Wook Kang ,  Jeong-Ho Joo ,  Young-Hee Lee

    IPC分类号： C07D295/104 ,  A61K31/44 ,  A61K31/47 ,  A61K31/495 ,  A61P35/00 ,  C07D213/74 ,  C07D213/75 ,  C07D215/38 ,  C07D221/04 ,  C07D295/112 ,  C07D295/215 ,  C07D401/04 ,  C07D409/04 ,  C07D401/12

    CPC分类号： C07D213/75 ,  C07D215/38 ,  C07D221/04 ,  C07D295/215 ,  C07D401/04 ,  C07D409/04 ,  Y02P20/582

    摘要： The present invention relates to novel compound having strong antimumor activities of the general formula(I) ##STR1## wherein R.sub.1 and R.sub.2 are independently hydrogen, substituted or unsubstituted C.sub.1 -C.sub.8 alkyl, substituted or unsubstituted C.sub.3 -C.sub.6 cycloalkyl, substituted or unsubstituted C.sub.2 -C.sub.8 unsaturated alkyl, ketone, substituted or unsubstituted aryl, substituted or unsubstituted C.sub.1 -C.sub.4 alkoxy, substituted or unsubstituted arylhydroxy, substituted or unsubstituted amino, C.sub.1 -C.sub.4 lower ester, C.sub.1 -C.sub.4 lower thioester, thiol, substituted or unsubstituted carboxyl, epoxy, substituted or unsubstituted C.sub.1 -C.sub.4 lower thioalkoxy; or R.sub.1 and R.sub.2 are fused to form C.sub.3 -C.sub.4 saturated or unsaturated chain; R.sub.3, R.sub.4, R.sub.5, R.sub.6 and R.sub.7 are independently hydrogen, halogen, hydroxy, nitro, C.sub.1 -C.sub.4 lower ester, C.sub.1 -C.sub.4 lower alkyl, C.sub.1 -C.sub.4 lower thioalkyl, substituted or unsubstituted C.sub.3 -C.sub.6 cycloalkyl, C.sub.1 -C.sub.4 lower alkoxy, C.sub.1 -C.sub.4 lower thioalkoxy, substituted or unsubstituted aryl, substituted or unsubstituted lower arylalkoxy, substituted or unsubstituted lower alkylamino, or lower alkyl substituted or unsubstituted carbamate; or among R.sub.3, R.sub.4, R.sub.5, R.sub.6 and R.sub.7, two adjacent groups are bonded with each other to form 1,2-phenylene or 2,3-naphthylene; X is oxygen, sulfur, or substituted or unsubstituted imino; Y is bonded at the 3-position or 4-position of the aromatic ring part wherein Y is oxygen or --NR.sub.8 -- (wherein, R.sub.8 is the same with the above-mentioned R.sub.3.); Z is hydroxy, C.sub.1 -C.sub.4 lower alkoxy, C.sub.1 -C.sub.4 lower thioalkoxy, substituted or unsubstituted aryloxy, C.sub.1 -C.sub.4 lower alkylamino, substituted or unsubstituted cycloamino containing 1-5 nitrogen atoms; A is nitrogen or --CH.dbd.; its pharmaceutically acceptable acid addition salts and process for the preparation thereof.

    Piperazine derivatives and methods for the preparation thereof and compositions containing the same
    9.
    发明授权
    Piperazine derivatives and methods for the preparation thereof and compositions containing the same 失效
    哌嗪衍生物及其制备方法和含有它们的组合物

    公开(公告)号：US5780472A

    公开(公告)日：1998-07-14

    申请号：US676174

    申请日：1996-07-15

    申请人： Eui-Hwan Cho ,  Sun-Gan Chung ,  Joong-Ypoung Kim ,  Sun-Hwan Lee ,  Ho-Seok Kwon ,  Byung-Chul Kim ,  Jae-Myeong Kong ,  Jea-Eung Lee ,  Dong-Wook Kang

    发明人： Eui-Hwan Cho ,  Sun-Gan Chung ,  Joong-Ypoung Kim ,  Sun-Hwan Lee ,  Ho-Seok Kwon ,  Byung-Chul Kim ,  Jae-Myeong Kong ,  Jea-Eung Lee ,  Dong-Wook Kang

    IPC分类号： A61K31/00 ,  A61K31/44 ,  A61K31/495 ,  A61K31/496 ,  A61P35/00 ,  C07D213/38 ,  C07D213/40 ,  C07D213/64 ,  C07D213/75 ,  C07D215/22 ,  C07D401/12 ,  C07D401/14

    CPC分类号： C07D213/40 ,  C07D213/38 ,  C07D213/64

    摘要： The present invention relates to novel compound of the general formula(I) and acid addition salt thereof. ##STR1## wherein R.sub.1 and R.sub.2 are independently hydrogen, C.sub.1 -C.sub.8 alkyl or optionally substituted C.sub.3 -C.sub.6 membered cycloalkyl containing C.sub.3 -C.sub.8 ; R.sub.3, R.sub.4, R.sub.5, R.sub.6 and R.sub.7 are independently hydrogen, halogen, hydroxy, nitro, C.sub.1 -C.sub.4 lower ester, C.sub.1 -C.sub.4 lower alkyl, C.sub.1 -C.sub.4 lower alkoxy, aryl, arylalkoxy or unsaturated amine; l is an integer of 0-7; m and n are independently an integer of 0-1; W is carbon or nitrogen; X is oxygen, sulfur, optionally substituted imine; Y is nitrogen or oxygen; and Z is hydrogen, C.sub.1 -C.sub.8 alkoxy, aryloxy, C.sub.1 -C.sub.4 alkylamine, cycloamine containing N.sub.1 -N.sub.5 or oxo group. The present compounds of the above formula (I) has no only strong antimumor activities but lower toxicities, and accordingly are expected as novel antitumor agents.

    摘要翻译： PCT No.PCT / KR96 / 00005 Sec。 371日期：1996年7月15日 102（e）1996年7月15日PCT PCT 1996年1月10日PCT公布。 WO90 / 21648 PCT出版物 日期：1996年7月18日本发明涉及通式（I）的新型化合物及其酸加成盐。 （I）其中R1和R2独立地是氢，C1-C8烷基或含有C3-C8的任选取代的C3-C6元环烷基; R3，R4，R5，R6和R7独立地是氢，卤素，羟基，硝基，C1-C4低级酯，C1-C4低级烷基，C1-C4低级烷氧基，芳基，芳基烷氧基或不饱和胺; l是0-7的整数; m和n独立地为0-1的整数; W是碳或氮; X是氧，硫，任选取代的亚胺; Y是氮或氧; Z为氢，C1-C8烷氧基，芳氧基，C1-C4烷基胺，含有N1-N5的环胺或氧代基。 上述式（I）的本发明化合物不仅具有较强的抗肿瘤活性，而且具有较低的毒性，因此被认为是新的抗肿瘤剂。

    Antiviral substituted pyrimidinedione homocarbocyclic nucleoside derivatives and methods for the preparation thereof and compositions containing the same as active ingredients
    10.
    发明授权
    Antiviral substituted pyrimidinedione homocarbocyclic nucleoside derivatives and methods for the preparation thereof and compositions containing the same as active ingredients 失效
    抗病毒取代的嘧啶二酮同型碳环核苷衍生物及其制备方法和含有活性成分的组合物

    公开(公告)号：US5922727A

    公开(公告)日：1999-07-13

    申请号：US945121

    申请日：1998-01-21

    申请人： Eui-Hwan Cho ,  Sun-Gan Chung ,  Joong-Young Kim ,  Sun-Hwan Lee ,  Ho-Seok Kwon ,  Jae-Eung Lee ,  Jeong-Ho Joo ,  Byung-Chul Kim ,  Dong-Wook Kang

    发明人： Eui-Hwan Cho ,  Sun-Gan Chung ,  Joong-Young Kim ,  Sun-Hwan Lee ,  Ho-Seok Kwon ,  Jae-Eung Lee ,  Jeong-Ho Joo ,  Byung-Chul Kim ,  Dong-Wook Kang

    IPC分类号： A61K31/505 ,  A61K31/506 ,  A61K31/695 ,  A61P31/12 ,  A61P31/14 ,  A61P31/18 ,  C07D239/54 ,  C07D239/60

    CPC分类号： C07D239/54 ,  C07D239/60

    摘要： The present invention relates to novel compound of general formula (I) and pharmaceutically acceptable salts thereof, and process for the preparation of such derivatives and to pharmaceutical compositions containing the same as active ingredients. ##STR1## wherein R.sub.1, R.sub.2, and R.sub.3 represents independently hydrogen atom, halogen atom, C.sub.1 -C.sub.10 alkyl, C.sub.1 -C.sub.10 thioalkyl, C.sub.3 -C.sub.8 optionally substituted cyclicalkyl, unsaturated alkyl, substituted alkyl hydroxyl or aryl hydroxyl, C.sub.1 -C.sub.10 alkylamine, nitro, C.sub.1 -C.sub.4 lower ester, C.sub.1 -C.sub.4 lower alkoxy, C.sub.1 -C.sub.4 lower thioalkoxy; Z represents oxygen atom, sulfur atom, carbon atom and carbonyl group; X represents oxygen atom, sulfur atom; n represents an integer of 1-3; and (sub)cycloalk(en)yl represents ##STR2## in which R.sub.4 and R.sub.5 represents independently hydrogen atom, hydroxymethyl, protected hydroxymethyl, benzyl, substituted carbonyl, substituted alkylsulfonyl or arylsulfonyl, substituted silyl or the like.

    摘要翻译： PCT No.PCT / KR96 / 00265 Sec。 371日期1998年1月21日 102（e）1998年1月21日PCT PCT 1996年12月30日PCT公布。 公开号WO97 / 30979 日期：1997年8月28日本发明涉及通式（I）的新型化合物及其药学上可接受的盐，以及制备该衍生物的方法以及含有活性成分的药物组合物。 其中R1，R2和R3独立地表示氢原子，卤素原子，C1-C10烷基，C1-C10硫代烷基，C3-C8任意取代的环烷基，不饱和烷基，取代的烷基羟基或芳基羟基，C1-C10烷基胺，硝基，C1 -C4低级酯，C1-C4低级烷氧基，C1-C4低级硫代烷氧基; Z表示氧原子，硫原子，碳原子和羰基; X表示氧原子，硫原子; n表示1-3的整数; 和（亚）环烷基（en）代表其中R 4和R 5独立地表示氢原子，羟甲基，保护的羟甲基，苄基，取代的羰基，取代的烷基磺酰基或芳基磺酰基，取代的甲硅烷基等。