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1. 发明授权

US07332615B2 Hydrophilic analogs of 4,8-dihydrobenzodithiophene-4,8-diones as anticancer agents 有权
标题翻译： 4,8-二氢苯并二噻吩-4,8-二酮的亲水类似物作为抗癌剂
公开(公告)号：US07332615B2
公开(公告)日：2008-02-19
申请号：US11236730
申请日：2005-09-28
申请人： Pi-Tsan Huang , Yen-Fang Wen , Wuu-Chian Shin , Mei-Hwai Chen , Sheng-Chu Kuo , Kuo-Hsiung Lee
发明人： Pi-Tsan Huang , Yen-Fang Wen , Wuu-Chian Shin , Mei-Hwai Chen , Sheng-Chu Kuo , Kuo-Hsiung Lee
IPC分类号： A61K31/38 , C07D333/74
CPC分类号： C07D495/04
摘要： The present invention discloses hydrophilic derivatives of 4,8-dihydrobenzodithiophene-4,8-diones, which are active as anticancer agents, along with pharmaceutical formulations containing the same.
摘要翻译：本发明公开了作为抗癌剂有活性的4,8-二氢苯并二噻吩-4,8-二氢discloses discloses的亲水性衍生物以及含有它们的药物制剂。

2. 发明申请

US20060069041A1 Novel hydrophilic analogs of 4,8-dihydrobenzodithiophene-4,8-diones as anticancer agents 有权
标题翻译： 4,8-二氢苯并二噻吩-4,8-二酮的新型亲水类似物作为抗癌剂
公开(公告)号：US20060069041A1
公开(公告)日：2006-03-30
申请号：US11236730
申请日：2005-09-28
申请人： Pi-Tsan Huang , Yen-Fang Wen , Wuu-Chian Shin , Mei-Hwai Chen , Sheng-Chu Kuo , Kuo-Hsiung Lee
发明人： Pi-Tsan Huang , Yen-Fang Wen , Wuu-Chian Shin , Mei-Hwai Chen , Sheng-Chu Kuo , Kuo-Hsiung Lee
IPC分类号： A61K31/7052 , A61K31/381 , C07D495/02
CPC分类号： C07D495/04
摘要： The present invention discloses hydrophilic derivatives of 4,8-dihydrobenzodithiophene-4,8-diones, which are active as anticancer agents, along with pharmaceutical formulations containing the same.
摘要翻译：本发明公开了作为抗癌剂有活性的4,8-二氢苯并二噻吩-4,8-二氢discloses discloses的亲水性衍生物以及含有它们的药物制剂。

3. 发明授权

US6071930A Method for treating tumors using 2-aryl-naphthyridin-4-ones 失效
标题翻译：使用2-芳基 - 萘啶-4-酮治疗肿瘤的方法
公开(公告)号：US6071930A
公开(公告)日：2000-06-06
申请号：US363101
申请日：1999-07-29
申请人： Kuo-Hsiung Lee , Ke Chen , Sheng-Chu Kuo
发明人： Kuo-Hsiung Lee , Ke Chen , Sheng-Chu Kuo
IPC分类号： A61K31/4375 , A61P17/06 , A61P19/06 , A61P35/00 , A61P43/00 , C07D213/74 , C07D471/04
CPC分类号： C07D213/74 , C07D471/04
摘要： The present invention provides compounds of Formula I: ##STR1## wherein A and R.sub.1 -R.sub.8 are defined herein. The compounds of Formula I inhibit the polymerization of tubulin and possess antimitotic activity. The compounds of Formula I may be useful for the treatment of psoriasis, gout, papiloma, warts, and a variety of tumors.
摘要翻译：本发明提供式I化合物：其中A和R 1 -R 8在本文中定义。式I的化合物抑制微管蛋白的聚合并具有抗生物活性。式I的化合物可用于治疗牛皮癣，痛风，乳头状瘤，疣和各种肿瘤。

4. 发明授权

US5789431A Naphthoquinone antitumor compound and method 失效
标题翻译：萘醌类抗肿瘤化合物及方法
公开(公告)号：US5789431A
公开(公告)日：1998-08-04
申请号：US601114
申请日：1996-02-16
申请人： Kuo-Hsiung Lee , Sheng-Chu Kuo , Toshiro Ibuka
发明人： Kuo-Hsiung Lee , Sheng-Chu Kuo , Toshiro Ibuka
IPC分类号： C07C233/32 , C07C233/42 , C07C233/43 , C07C233/44 , C07C233/76 , C07D235/02 , A61K31/415
CPC分类号： C07D235/02 , C07C233/32 , C07C233/42 , C07C233/43 , C07C233/44 , C07C233/76 , C07C2102/10
摘要： The invention provides 1,4-naphthoquinone compounds and a method for inhibiting tumor cell growth in a subject by administering such compounds. The compounds are represented by the structures: ##STR1## where R.sub.1 is lower alkyl, halogenated lower alkyl, phenyl, benzyl, phenethyl, or --(CH.sub.2).sub.m COOX where m is 2 or 3 and X is H, methyl, or ethyl; R.sub.2 is halo or NHY, where Y is hydrogen, lower alkyl, halogenated lower alkyl, hydroxylated lower alkyl, lower dialkylaminoalkyl, phenyl, benzyl, or phenethyl; R.sub.3 is lower alkyl, halogenated lower alkyl, phenyl, benzyl, phenethyl, or --(CH.sub.2).sub.m COOX, where m and X are as defined for R.sub.1 above; and R.sub.4 is hydrogen, lower alkyl, lower aminoalkyl, halogenated lower alkyl, phenyl, benzyl, or phenethyl.
摘要翻译：本发明提供1,4-萘醌化合物和通过施用这些化合物来抑制受试者的肿瘤细胞生长的方法。化合物由以下结构表示：其中R 1是低级烷基，卤代低级烷基，苯基，苄基，苯乙基或 - （CH 2）m COOX，其中m是2或3，以及 X是H，甲基或乙基; R2是卤素或NHY，其中Y是氢，低级烷基，卤代低级烷基，羟基化的低级烷基，低级二烷基氨基烷基，苯基，苄基或苯乙基; R3是低级烷基，卤代低级烷基，苯基，苄基，苯乙基或 - （CH2）mCOOX，其中m和X如上述R1所定义; 和R4是氢，低级烷基，低级氨基烷基，卤代低级烷基，苯基，苄基或苯乙基。

5. 发明授权

US06897316B2 Substituted 2-phenyl-4-quinolone-3-carboxylic acid compounds and their use as antitumor agents 失效
标题翻译：取代的2-苯基-4-喹诺酮-3-羧酸化合物及其作为抗肿瘤剂的用途
公开(公告)号：US06897316B2
公开(公告)日：2005-05-24
申请号：US10636603
申请日：2003-08-08
申请人： Sheng-Chu Kuo , Li-Jiau Huang , Ya-Yun Lai , Chun-Jen Chen , Mei-Hua Hsu , Ya-Ling Fang , Kuo-Hsiung Lee , Che-Ming Teng
发明人： Sheng-Chu Kuo , Li-Jiau Huang , Ya-Yun Lai , Chun-Jen Chen , Mei-Hua Hsu , Ya-Ling Fang , Kuo-Hsiung Lee , Che-Ming Teng
IPC分类号： A61K31/4355 , A61K31/47 , A61K31/4709 , A61P35/00 , C07D215/16 , C07D215/20 , C07D215/36 , C07D215/56 , C07D491/056
CPC分类号： C07D215/56
摘要： Substituted 2-phenyl-4-quinolone-3-carboxylic acid derivatives and their salts were synthesized. The results of preliminary screening revealed that these compounds are potent in killing solid tumor cancers.
摘要翻译：合成取代的2-苯基-4-喹诺酮-3-羧酸衍生物及其盐。初步筛选结果表明，这些化合物在杀死实体肿瘤中是有效的。

6. 发明申请

US20050032832A1 Substituted 2-phenyl-4-quinolone-3-carboxylic acid compounds and their use as antitumor agents 失效
公开(公告)号：US20050032832A1
公开(公告)日：2005-02-10
申请号：US10636603
申请日：2003-08-08
申请人： Sheng-Chu Kuo , Li-Jiau Huang , Ya-Yun Lai , Chun-Jen Chen , Mei-Hua Hsu , Ya-Ling Fang , Kuo-Hsiung Lee , Che-Ming Teng
发明人： Sheng-Chu Kuo , Li-Jiau Huang , Ya-Yun Lai , Chun-Jen Chen , Mei-Hua Hsu , Ya-Ling Fang , Kuo-Hsiung Lee , Che-Ming Teng
IPC分类号： A61K31/4355 , A61K31/47 , A61K31/4709 , A61P35/00 , C07D215/16 , C07D215/20 , C07D215/36 , C07D215/56 , C07D491/056
CPC分类号： C07D215/56
摘要： Substituted 2-phenyl-4-quinolone-3-carboxylic acid derivatives and their salts were synthesized. The results of preliminary screening revealed that these compounds are potent in killing solid tumor cancers.

7. 发明授权

US06337346B1 Naphtho- and dihydrobenzo-thiophene derivatives as cytotoxic antitumor agents 失效
标题翻译：萘并 - 二氢苯并噻吩衍生物作为细胞毒性抗肿瘤剂
公开(公告)号：US06337346B1
公开(公告)日：2002-01-08
申请号：US09651357
申请日：2000-08-30
申请人： Kuo-Hsiung Lee , Sheng-Chu Kuo
发明人： Kuo-Hsiung Lee , Sheng-Chu Kuo
IPC分类号： A61K3138
CPC分类号： C07D495/04 , C07D333/74
摘要： Compounds useful as cytotoxic agents are selected from the group consisting of compounds of Formula I and compounds of Formula II: wherein: R1, R2, R3 and R4 are each independently selected from the group consisting of: hydrogen, alkyl, carboxy, alkoxy, hydroxyalkyl, alkylcarbonyl; alkylcarbonyloxy; alkyl substituted with alkylcarbonyloxy, thiophenylcarbonyl; nitro and cyano; thiophenyl and thiophenylthiophenyl, each of which may be unsubstituted or substituted with alkyl, carboxy, alkoxy, hydroxyalkyl, alkylcarbonyl; alkylcarbonyloxy; alkyl substituted with alkylcarbonyloxy, nitro or cyano; subject to the proviso that at least one of R1, R2, R3 and R4 is not hydrogen; A1 and A2 are each selected from the group consisting of: ═O, alkyl, alkoxy, and alkylcarbonyloxy; and the pharmaceutically acceptable salts thereof. When A1 and A2 are ═O, the center ring has only two, and not three, double bonds.
摘要翻译：可用作细胞毒性剂的化合物选自式I化合物和式II化合物：其中：R 1，R 2，R 3和R 4各自独立地选自氢，烷基，羧基，烷氧基，羟基烷基，烷基羰基; 烷基羰氧基被烷基羰基氧基取代的烷基，硫代苯基羰基; 硝基和氰基; 硫代苯基和噻吩硫基苯基，其各自可以是未取代的或被烷基，羧基，烷氧基，羟烷基，烷基羰基取代; 烷基羰氧基被烷基羰基氧基，硝基或氰基取代的烷基; 条件是R 1，R 2，R 3和R 4中的至少一个不是氢; A1和A2各自选自：= O，烷基，烷氧基和烷基羰基氧基; 及其药学上可接受的盐。当A1和A2为= O时，中心环只有两个，而不是三个双键。

8. 发明授权

US06174918B1 Naphthoquinone antitumor compound and method 失效
标题翻译：萘醌类抗肿瘤化合物及方法
公开(公告)号：US06174918B1
公开(公告)日：2001-01-16
申请号：US09126624
申请日：1998-07-30
申请人： Kuo-Hsiung Lee , Sheng-Chu Kuo , Toshiro Ibuka
发明人： Kuo-Hsiung Lee , Sheng-Chu Kuo , Toshiro Ibuka
IPC分类号： A61K3121
CPC分类号： C07D235/02 , C07C233/32 , C07C233/42 , C07C233/43 , C07C233/44 , C07C233/76 , C07C2602/10
摘要： The invention provides 1,4-naphthoquinone compounds and a method for inhibiting tumor cell growth in a subject by administering such compounds. The compounds are represented by the structures: where R1 is lower alkyl, halogenated lower alkyl, phenyl, benzyl, phenethyl, or —(CH2)mCOOX, where m is 2 or 3 and X is H, methyl, or ethyl; R2 is halo or NHY, where Y is hydrogen, loweralkyl, halogenated lower alkyl, hydroxylated lower alkyl, lower dialkylaminoalkyl, phenyl, benzyl, or phenethyl; R3 is lower alkyl, halogenated lower alkyl, phenyl, benzyl, phenethyl, or —(CH2)mCOOX, where m and X are as defined for R1 above; and R4 is hydrogen, lower alkyl, lower aminoalkyl, halogenated lower alkyl, phenyl, benzyl, or phenethyl.
摘要翻译：本发明提供1,4-萘醌化合物和通过施用这些化合物来抑制受试者的肿瘤细胞生长的方法。化合物由以下结构表示：其中R1是低级烷基，卤代低级烷基，苯基，苄基，苯乙基或 - （CH2）mCOOX，其中m是2或3，X是H，甲基或乙基; R2是卤素或NHY，其中Y是氢，低级烷基，卤代低级烷基，羟基化的低级烷基，低级二烷基氨基烷基，苯基，苄基或苯乙基; R3是低级烷基，卤代低级烷基，苯基，苄基，苯乙基或 - （CH2）mCOOX，其中m和X如上述R1所定义; 和R4是氢，低级烷基，低级氨基烷基，卤代低级烷基，苯基，苄基或苯乙基。

9. 发明申请

US20120015908A1 SYNTHESIS AND ANTICANCER ACTIVITY OF ARYL AND HETEROARYL-QUINOLIN DERIVATIVES 有权
标题翻译：芳基和喹啉衍生物的合成和反应活性
公开(公告)号：US20120015908A1
公开(公告)日：2012-01-19
申请号：US13181978
申请日：2011-07-13
申请人： Sheng-Chu Kuo , Kuo-Hsiung Lee , Li-Jiau Huang , Li-Chen Chou , Tian-Shung Wu , Tzong-Der Way , Jing-Gung Chung , Jai-Sing Yang , Chi-Hung Huang , Meng-Tung Tsai
发明人： Sheng-Chu Kuo , Kuo-Hsiung Lee , Li-Jiau Huang , Li-Chen Chou , Tian-Shung Wu , Tzong-Der Way , Jing-Gung Chung , Jai-Sing Yang , Chi-Hung Huang , Meng-Tung Tsai
IPC分类号： A61K31/675 , A61K31/47 , C07D491/056 , A61K31/4741 , C07F9/60 , A61P35/00 , A61K31/5377 , C07D405/14 , A61K31/4709 , C07D413/10 , C07D401/10 , C07D215/233 , C07D413/14
CPC分类号： C07D493/04 , C07D215/22 , C07D215/233 , C07D215/38 , C07D401/04 , C07F9/60 , C07F9/65583 , C07F9/6561
摘要： A compound of Formula I is disclosed as follows: or a pharmaceutically acceptable salt, prodrug, solvate, or metabolite thereof, wherein R is hydrogen, P(═O)(OH)2, P(═O)(O(C1-C18)alkylene(C6-C20)aryl)2, P(═O)(OH)(OM), P(═O)(OM)2, P═O(O2M), S(═O)(OH)2, S(═O)(O(C1-C18)alkylene(C6-C20)aryl)2, S(═O)(OH)(OM), S(═O)(OM)2; M is a monovalent or divalent metal ion, or alkylammonium ion; W is (C6-C20)aryl, (C6-C20)heteroaryl, (C1-C18)alkyl(C6-C20)aryl, (C1-C18)alkyl(C6-C20)heteroaryl, hydroxy(C6-C20)aryl, hydroxy(C6-C20)heteroaryl, (C1-C18)alkoxy(C6-C20)aryl, (C1-C18)alkoxy(C6-C20)heteroaryl, (C1-C18)alkylenedioxy(C6-C20)aryl, (C1-C18)alkylenedioxy(C6-C20)heteroaryl, halo(C6-C20)aryl, halo(C6-C20)heteroaryl, (C1-C18)alkylamino(C6-C20)aryl, (C1-C18)alkylamino(C6-C20)heteroaryl, (C1-C18)cycloalkylamino(C6-C20)aryl, or (C1-C18)cycloalkylamino(C6-C20)heteroaryl, and their OR8 substutes; R5 is (C1-C18alkoxy, hydrogen, hydroxyl, O—(C1-C18)alkyl(C6-C20)aryl, halo or OR8, or R5 and R6 are (C1-C18)dioxy provided that R7 is hydrogen; R6 is hydroxyl, O—(C1-C18)alkyl(C6-C20)aryl, halo or ORR, (C1-C18)alkoxy, (C1-C18)alkylamino, or (C1-C18)cycloalkylamino, or R6 and R7 are (C1-C18)dioxy provided that R5 is hydrogen; R7 is hydrogen, halo or OR8, hydroxyl, or O—(C1-C18)alkyl(C6-C20)aryl; and R8 is P(═O)(OH)2, P(═O)(O(C1-C18)alkyl(C6-C20)aryl)2, P(═O)(OH)(OM), or P(═O)(OM)2, P═O(O2M).
摘要翻译：式I的化合物公开如下：或其药学上可接受的盐，前药，溶剂合物或代谢物，其中R是氢，P（= O）（OH）2，P（= O）（O（C 1 -C 18））亚烷基（C 6 -C 20）芳基）2，P（= O）（OH）（OM），P（= O）（OM）2，P = O（O 2 M） S（ΟO）（O（C1-C18）亚烷基（C6-C20）芳基）2，S（═0）（OH）（OM），S（ΟO）（OM） M是一价或二价金属离子或烷基铵离子; W是（C 6 -C 20）芳基，（C 6 -C 20）杂芳基，（C 1 -C 18）烷基（C 6 -C 20）芳基，（C 1 -C 18）烷基（C 6 -C 20）羟基（C 6 -C 20）杂芳基，（C 1 -C 18）烷氧基（C 6 -C 20）芳基，（C 1 -C 18）烷氧基（C 6 -C 20）杂芳基，（C 1 -C 18）亚烷基二氧基 C 1 -C 20烷基氨基（C 6 -C 20）芳基，（C 1 -C 20）芳基，（C 1 -C 20）芳基，杂芳基，（C1-C18）环烷基氨基（C6-C20）芳基或（C1-C18）环烷基氨基（C6-C20）杂芳基及其OR8分子; R5是（C1-C18烷氧基，氢，羟基，O-（C1-C18）烷基（C6-C20）芳基，卤素或OR8或R5和R6是（C1-C18）二氧基，条件是R7是氢; R6是羟基，（C 1 -C 18）烷基（C 6 -C 20）芳基，卤素或ORR，（C 1 -C 18）烷氧基，（C 1 -C 18）烷基氨基或（C 1 -C 18）环烷基氨基或R 6和R 7为其中R 5为氢，R 7为氢，卤素或OR 8，羟基或O-（C 1 -C 18）烷基（C 6 -C 20）芳基; R 8为P（= O）（OH）2，P （O）（O（C1-C18）烷基（C6-C20）芳基）2，P（= O）（OH）（OM）或P（= O）（OM）2，P = O（O2M）。

10. 发明授权

US06916831B2 Flavone acetic acid analogs and methods of use thereof 失效
标题翻译：黄酮乙酸类似物及其使用方法
公开(公告)号：US06916831B2
公开(公告)日：2005-07-12
申请号：US10373399
申请日：2003-02-24
申请人： Kuo-Hsiung Lee , Yi Xia , Zheng-Yu Yang , Kenneth F. Bastow , Sheng-Chu Kuo
发明人： Kuo-Hsiung Lee , Yi Xia , Zheng-Yu Yang , Kenneth F. Bastow , Sheng-Chu Kuo
IPC分类号： C07D215/22 , C07D215/233 , A61K31/445 , A61K31/35 , C07D211/06 , C07D257/04 , C07D311/82
CPC分类号： C07D215/233
摘要： Compounds are described having a structure according to Formula I or Formula II: wherein: X is selected from the group consisting of O, NH, and S; Y is selected from the group consisting of O and S; m is from 1 to 3; n is from 1 to 5; R1 and R3 are each independently selected from the group consisting of H, hydroxy, lower alky, lower alkoxy, halo, amino, aminoalkyl, nitro, heteroaryl, —OC(═O)R6, —O(C═O)OR6; and —O(C═O)N(R6)2; and R2 is side chain such as an acetic acid side chain, where p is O to 4, R5 is hydroxy, alkoxy or amino, and R6 is H or lower alkyl, or a pharmaceutically acceptable salt thereof. The compounds are useful for the treatment of cancer.
摘要翻译：描述具有根据式I或式II的结构的化合物：其中：X选自O，NH和S; Y选自O和S; m为1〜3; n为1〜5; R 1和R 3各自独立地选自H，羟基，低级烷基，低级烷氧基，卤素，氨基，氨基烷基，硝基，杂芳基，-OC （-O）R 6，-O（CO）OR 6; 和-O（C-O）N（R 6）2。并且R 2是侧链，例如乙酸侧链，其中p为0至4，R 5为羟基，烷氧基或氨基，R 6 或其低级烷基或其药学上可接受的盐。该化合物可用于治疗癌症。

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