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1. 发明申请

WO9402145A2 2-ARYL-4-QUINOLONES AS ANTITUMOR COMPOUNDS 审中-公开
标题翻译： 2-ARYL-4-QUINOLONES作为抗菌化合物
公开(公告)号：WO9402145A2
公开(公告)日：1994-02-03
申请号：PCT/US9306893
申请日：1993-07-22
申请人： GENELABS TECH INC , UNIV NORTH CAROLINA , LEE KUO HSIUNG , KUO SHENG CHU , WU TIAN SHUNG , LIU SU YING , HWANG KOU M , WENG HUI KANG , LI LE PENG
发明人： LEE KUO-HSIUNG , KUO SHENG-CHU , WU TIAN-SHUNG , LIU SU-YING , HWANG KOU M , WENG HUI KANG , LI LE PENG
IPC分类号： C07D215/22 , C07D215/233 , C07D215/26 , C07D215/38 , C07D215/40 , C07D401/04 , C07D405/04 , C07D409/04 , C07D491/04 , C07D491/056 , A61K31/47 , A61K31/495 , A61K31/535 , C07D215/220
CPC分类号： C07D215/233 , C07D215/26 , C07D215/38 , C07D215/40 , C07D401/04 , C07D405/04 , C07D409/04 , C07D491/04
摘要： A method of inhibiting tumor-cell growth, by administering a pharmaceutically effective amount of a 2-aryl-4-quinolone compound, is disclosed. The 2-aryl-4-quinolone compound is effective to inhibit tumor cell growth in tumors in which multiple drug resistance is encountered. Also disclosed are novel 2-aryl-4-quinolone anti-tumor compounds.
摘要翻译：公开了通过施用药学上有效量的2-芳基-4-喹诺酮化合物来抑制肿瘤细胞生长的方法。 2-芳基-4-喹诺酮化合物有效抑制其中遇到多重耐药性的肿瘤中的肿瘤细胞生长。还公开了新的2-芳基-4-喹诺酮抗肿瘤化合物。

2. 发明专利

CA2670292A1 NOVEL HYDROPHILIC DERIVATIVES OF 2-ARYL-4-QUINOLONES AS ANTICANCER AGENTS 未知
公开(公告)号：CA2670292A1
公开(公告)日：2008-06-12
申请号：CA2670292
申请日：2007-12-07
申请人： CHOU LI-CHEN , HUANG SHIH-MING , TENG CHE-MING , CHEN CHIEN-TING , CHANG CHIH-SHIANG , HUANG CHING-CHE , WAY TZONG-DER , LEE JANG-CHANG , YANG JAI-SING , CHUNG JING-GUNG , KUO SHENG-CHU , SUN CHUNG-MING , LEE KUO-HSIUNG , PAN SHIOW-LIN , WU TIAN-SHUNG , HUANG LI-JIAU
发明人： CHOU LI-CHEN , HUANG SHIH-MING , TENG CHE-MING , CHEN CHIEN-TING , CHANG CHIH-SHIANG , HUANG CHING-CHE , WAY TZONG-DER , LEE JANG-CHANG , YANG JAI-SING , CHUNG JING-GUNG , KUO SHENG-CHU , SUN CHUNG-MING , LEE KUO-HSIUNG , PAN SHIOW-LIN , WU TIAN-SHUNG , HUANG LI-JIAU
IPC分类号： A01N57/00 , A61K31/675
摘要： 2-aryl-4-quinolones are converted into phosphates by reacting with tetrab enzyl pyrophosphate to form dibenzyl phosphates thereof, which are then subj ect to hydrogenation to replace dibenzyl groups with H, followed by reacting with Amberlite IR-120(Na+ form) to form disodium salts. The results of prel iminary screening revealed that these phosphates showed significant anti-can cer activity. A novel intermediate, 2-selenophene 4-quinolone and .LAMBDA./, .LAMBDA./-dialkylaminoalkyl derivatives of 2-phenyl-4-quinolones are also s ynthesized. These novel intermediates exhibited significant anticancer activ ities.

3. 发明专利

CA2670292C NOVEL HYDROPHILIC DERIVATIVES OF 2-ARYL-4-QUINOLONES AS ANTICANCER AGENTS 未知
公开(公告)号：CA2670292C
公开(公告)日：2012-01-31
申请号：CA2670292
申请日：2007-12-07
申请人： KUO SHENG-CHU , TENG CHE-MING , LEE KUO-HSIUNG , HUANG LI-JIAU , CHOU LI-CHEN , CHANG CHIH-SHIANG , SUN CHUNG-MING , WU TIAN-SHUNG , PAN SHIOW-LIN , WAY TZONG-DER , LEE JANG-CHANG , CHUNG JING-GUNG , YANG JAI-SING , CHEN CHIEN-TING , HUANG CHING-CHE , HUANG SHIH-MING
发明人： KUO SHENG-CHU , TENG CHE-MING , LEE KUO-HSIUNG , HUANG LI-JIAU , CHOU LI-CHEN , CHANG CHIH-SHIANG , SUN CHUNG-MING , WU TIAN-SHUNG , PAN SHIOW-LIN , WAY TZONG-DER , LEE JANG-CHANG , CHUNG JING-GUNG , YANG JAI-SING , CHEN CHIEN-TING , HUANG CHING-CHE , HUANG SHIH-MING
IPC分类号： C07F9/6558 , A61K31/47 , A61K31/4709 , A61K31/675 , A61P35/00 , C07D215/233 , C07D421/04 , C07D491/056 , C07D517/04
摘要： 2-aryl-4-quinolones are converted into phosphates by reacting with tetrabenzyl pyrophosphate to form dibenzyl phosphates thereof, which are then subject to hydrogenation to replace dibenzyl groups with H, followed by reacting with Amberlite IR-120(Na+ form) to form disodium salts. The results of preliminary screening revealed that these phosphates showed significant anti-cancer activity. A novel intermediate, 2-selenophene 4-quinolone and .LAMBDA./, .LAMBDA./-dialkylaminoalkyl derivatives of 2-phenyl-4-quinolones are also synthesized. These novel intermediates exhibited significant anticancer activities.

4. 发明申请

WO9962909A2 NAPHTHO- AND DIHYDROBENZO-THIOPHENE DERIVATIVES AS CYTOTOXIC ANTITUMOR AGENTS 审中-公开
标题翻译：萘普生和二氢苯并噻吩衍生物作为细胞毒性抗菌剂
公开(公告)号：WO9962909A2
公开(公告)日：1999-12-09
申请号：PCT/US9912647
申请日：1999-06-04
申请人： UNIV NORTH CAROLINA , LEE KUO HSIUNG , KUO SHENG CHU
发明人： LEE KUO-HSIUNG , KUO SHENG-CHU
IPC分类号： A61K31/381 , A61P35/00 , C07D333/74 , C07D495/04 , A61K31/38
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）的化合物和式（II）的化合物，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; 羰; 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; 羰; 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。

5. 发明申请

WO2004075858A3 FLAVONE ACETIC ACID ANALOGS AND METHODS OF USE THEREOF 审中-公开
标题翻译： FLAVONE ACE酸类似物及其使用方法
公开(公告)号：WO2004075858A3
公开(公告)日：2005-01-20
申请号：PCT/US2004005826
申请日：2004-02-24
申请人： UNIV NORTH CAROLINA , LEE KUO-HSIUNG , XIA YI , YANG ZHENG-YU , BASTOW KENNETH F , KUO SHENG-CHU
发明人： LEE KUO-HSIUNG , XIA YI , YANG ZHENG-YU , BASTOW KENNETH F , KUO SHENG-CHU
IPC分类号： C07D215/22 , C07D215/233 , A61K31/525 , A61K31/44 , A61K31/47 , C07D215/16 , C07D311/04 , C07D491/00
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 alkyl, 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（C = O）OR 6; 和-O（C = O）N（R 6）2; R2是侧链如乙酸侧链，其中p为0至4，R5为羟基，烷氧基或氨基，R6为H或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。

6. 发明申请

WO9962909A9 NAPHTHO- AND DIHYDROBENZO-THIOPHENE DERIVATIVES AS CYTOTOXIC ANTITUMOR AGENTS 审中-公开
标题翻译：萘酚和二氢苯并噻吩衍生物作为细胞毒性抗肿瘤药物
公开(公告)号：WO9962909A9
公开(公告)日：2000-04-27
申请号：PCT/US9912647
申请日：1999-06-04
申请人： UNIV NORTH CAROLINA , LEE KUO HSIUNG , KUO SHENG CHU
发明人： LEE KUO-HSIUNG , KUO SHENG-CHU
IPC分类号： A61K31/381 , A61P35/00 , C07D333/74 , C07D495/04 , A61K31/38
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，羟烷基，烷基羰基; 羰; 被烷基羰基氧基取代的烷基，噻吩基羰基; 硝基和氰基; 噻吩基和噻吩基硫代苯基，它们中的每一个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; 羰; 被烷基羰氧基，硝基或氰基取代的烷基; 条件是R1，R2，R3和R4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 = O时，中心环只有两个，而不是三个双键。

7. 发明专利

AU4780793A 2-aryl-4-quinolones as antitumor compounds 未知
公开(公告)号：AU4780793A
公开(公告)日：1994-02-14
申请号：AU4780793
申请日：1993-07-22
申请人： GENELABS TECH INC , UNIV NORTH CAROLINA
发明人： LEE KUO-HSIUNG , KUO SHENG-CHU , WU TIAN-SHUNG , LIU SU-YING , HWANG KOU M , WENG HUI KANG , LI LE PENG
IPC分类号： C07D215/22 , C07D215/233 , C07D215/26 , C07D215/38 , C07D215/40 , C07D401/04 , C07D405/04 , C07D409/04 , C07D491/04 , C07D491/056 , A61K31/47 , A61K31/495 , A61K31/535 , C07D215/20

8. 发明申请

WO0226730A3 FLUORINATED QUINOLONES AS ANTIMITOTIC AND ANTITUMOR AGENTS 审中-公开
标题翻译：氟化喹诺酮作为抗肿瘤和抗肿瘤药物
公开(公告)号：WO0226730A3
公开(公告)日：2002-09-19
申请号：PCT/US0129916
申请日：2001-09-25
申请人： UNIV NORTH CAROLINA
发明人： LEE KUO-HSIUNG , XIA YI , YANG ZHENG-YU , KUO SHENG-CHU
IPC分类号： A61K31/4709 , A61K31/4741 , A61P35/00 , A61P43/00 , C07D215/38 , C07D491/04 , C07D491/056 , C07D215/22 , C07D493/04
CPC分类号： C07D491/04 , C07D215/38
摘要： The present invention provides fluorinated quinolones which are fluorinated on the phenyl group thereof, along with pharmaceutical formulations containing the same, methods of treating tumors or cancer by the administration of such compounds, and methods of inhibiting cellular mitosis by the administration of such compounds.
摘要翻译：本发明提供在其苯基上氟化的氟化喹诺酮，以及含有其的药物制剂，通过施用这些化合物治疗肿瘤或癌症的方法，以及通过施用这些化合物抑制细胞有丝分裂的方法。

9. 发明专利

AU4548899A Naphtho- and dihydrobenzo-thiophene derivatives as cytotoxic antitumor agents 未知
公开(公告)号：AU4548899A
公开(公告)日：1999-12-20
申请号：AU4548899
申请日：1999-06-04
申请人： UNIV NORTH CAROLINA
发明人： LEE KUO-HSIUNG , KUO SHENG-CHU
IPC分类号： A61K31/381 , A61P35/00 , C07D333/74 , C07D495/04 , A61K31/38
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.

10. 发明专利

AU2129397A Naphthoquinone antitumor compound and method 未知
公开(公告)号：AU2129397A
公开(公告)日：1997-09-02
申请号：AU2129397
申请日：1997-02-14
申请人： UNIV NORTH CAROLINA
发明人： LEE KUO HSIUNG , KUO SHENG-CHU , IBUKA TOSHIRO
IPC分类号： C07C233/32 , C07C233/42 , C07C233/43 , C07C233/44 , C07C233/76 , C07D235/02 , C07C233/74 , A61K31/165 , A61K31/415
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.

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