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1. 发明授权

US08524740B2 Synthesis and anticancer activity of aryl and heteroaryl-quinolin derivatives 有权
标题翻译：芳基和杂芳基 - 喹啉衍生物的合成和抗癌活性
公开(公告)号：US08524740B2
公开(公告)日：2013-09-03
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： A61K31/04 , C07D215/04
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 OR8, (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（= O）（O（C1-C18）亚烷基（C6-C20）芳基）2，S（= O）（OH）（OM），S（= O）（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OR 8，（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（C 1 -C 18）烷基（C 6 -C 20）芳基; R 8为P（= O）（OH）2，P（= O） = O）（O（C 1 -C 18）烷基（C 6 -C 20）芳基）2，P（= O）（OH）（OM）或P（= O）（OM）2，P = O（O 2 M）。

2. 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）。

3. 发明申请

US20130177661A1 Saussurea Involucrate Extract, Pharmaceutical Composition and Use for Anti-Fatigue and Anti-Aging 审中-公开
标题翻译： Saussurea Involucrate Extract，Pharmaceutical Composition and Use for Anti-Fatigue and Anti-Aging
公开(公告)号：US20130177661A1
公开(公告)日：2013-07-11
申请号：US13344019
申请日：2012-01-05
申请人： Yi-Lin Chen , Hsin-Sheng Tsay , Tzong-Der Way , Po-Lei Lee , Chao-Yuan Yu , Chien-Hsu Chen
发明人： Yi-Lin Chen , Hsin-Sheng Tsay , Tzong-Der Way , Po-Lei Lee , Chao-Yuan Yu , Chien-Hsu Chen
IPC分类号： A61K36/28 , A61P29/00
CPC分类号： A61K36/28 , A61K2236/30
摘要： Disclosed are a Saussurea involucrate extract, pharmaceutical composition and use thereof for anti-fatigue and anti-aging. In the embodiments of the present invention, a low dose of ethyl acetate fraction of Saussurea involucrate (preferably 30 mg/kg) and Rutin (preferably 30 mg/kg) can inhibit MDA expression level and increase GPx activity. Additionally, both decrease the expression of COX-2, PARP and caspase-3, via downregulation of NF-kappaB, resulting in neuroprotection. Further, syringe feeding of Saussurea involucrate extract is also performed in aging mouse model. In the future, Saussurea involucrate extract of the present invention can be used in neuroprotection, particularly in treatment or prevention of cerebral diseases, nerve diseases, neurodegenerative diseases, chronic neurodegenerative diseases, aging, and fatigue, caused by oxidative injury.
摘要翻译：公开了一种Saussurea通用提取物，药物组合物及其用于抗疲劳和抗衰老的用途。在本发明的实施方案中，低剂量的Saussurea比例（优选30mg / kg）和Rutin（优选30mg / kg）的乙酸乙酯级分可以抑制MDA表达水平并增加GPx活性。另外，通过下调NF-κB，都能降低COX-2，PARP和caspase-3的表达，从而导致神经保护作用。此外，老化小鼠模型也进行了Saussurea内rate提取物的注射器喂养。将来，本发明的Saussurea泛酸提取物可用于神经保护，特别是在由氧化损伤引起的脑疾病，神经疾病，神经变性疾病，慢性神经变性疾病，衰老和疲劳的治疗或预防中。

4. 发明授权

US08440692B2 Hydrophilic derivatives of 2-aryl-4-quinolones as anticancer agents 有权
标题翻译： 2-芳基-4-喹诺酮的亲水性衍生物作为抗癌剂
公开(公告)号：US08440692B2
公开(公告)日：2013-05-14
申请号：US12448088
申请日：2007-12-07
申请人： Sheng-Chu Kuo , Che-Ming Teng , Kuo-Hsiung Lee , Li-Jiau Huang , Li-Chen Chou , Chih-Shiang Chang , Chung-Ming Sun , Tian-Shung Wu , Shiow-Lin Pan , Tzong-Der Way , Jang-Chang Lee , Jing-Gung Chung , Jai-Sing Yang , Chien-Ting Chen , Ching-Che Huang , Shih-Ming Huang
发明人： Sheng-Chu Kuo , Che-Ming Teng , Kuo-Hsiung Lee , Li-Jiau Huang , Li-Chen Chou , Chih-Shiang Chang , Chung-Ming Sun , Tian-Shung Wu , Shiow-Lin Pan , Tzong-Der Way , Jang-Chang Lee , Jing-Gung Chung , Jai-Sing Yang , Chien-Ting Chen , Ching-Che Huang , Shih-Ming Huang
IPC分类号： A61K31/47 , C07F9/38
CPC分类号： C07F9/6561 , C07D215/233 , C07D421/04 , C07D491/056 , C07F9/60
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 Λ/, Λ/-dialkylaminoalkyl derivatives of 2-phenyl-4-quinolones are also synthesized. These novel intermediates exhibited significant anticancer activities.
摘要翻译： 2-芳基-4-喹诺酮通过与焦磷酸四苄酯反应而形成磷酸盐，形成其二苄基磷酸酯，然后进行氢化，用H代替二苄基，然后与Amberlite IR-120（Na +形式）反应形成二钠盐。初步筛选结果表明，这些磷酸盐显示出显着的抗癌活性。还合成了一种新的中间体2-硒吩-4-喹诺酮和2-苯基-4-喹诺酮的λ/，λ/二烷基氨基烷基衍生物。这些新型中间体显示出显着的抗癌活性。

5. 发明申请

US20100168064A1 NOVEL HYDROPHILIC DERIVATIVES OF 2-ARYL-4-QUINOLONES AS ANTICANCER AGENTS 有权
标题翻译：作为抗原剂的2-亚芳基-4-喹啉酮的新型疏水衍生物
公开(公告)号：US20100168064A1
公开(公告)日：2010-07-01
申请号：US12448088
申请日：2007-12-07
申请人： Sheng-Chu Kuo , Che-Ming Teng , Kuo-Hsiung Lee , Li-Jiau Huang , Li-Chen Chou , Chih-Shiang Chang , Chung-Ming Sun , Tian-Shung Wu , Shiow-Lin Pan , Tzong-Der Way , Jang-Chang Lee , Jing-Gung Chung , Jai-Sing Yang , Chien-Ting Chen , Ching-Che Huang , Shih-Ming Huang
发明人： Sheng-Chu Kuo , Che-Ming Teng , Kuo-Hsiung Lee , Li-Jiau Huang , Li-Chen Chou , Chih-Shiang Chang , Chung-Ming Sun , Tian-Shung Wu , Shiow-Lin Pan , Tzong-Der Way , Jang-Chang Lee , Jing-Gung Chung , Jai-Sing Yang , Chien-Ting Chen , Ching-Che Huang , Shih-Ming Huang
IPC分类号： A61K31/675 , C07F9/09 , A61K31/47 , A61P35/00 , A61P35/02 , C07D421/04 , C07D215/233
CPC分类号： C07F9/6561 , C07D215/233 , C07D421/04 , C07D491/056 , C07F9/60
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 Λ/, Λ/-dialkylaminoalkyl derivatives of 2-phenyl-4-quinolones are also synthesized. These novel intermediates exhibited significant anticancer activities.
摘要翻译： 2-芳基-4-喹诺酮通过与焦磷酸四苄酯反应而形成磷酸盐，形成其二苄基磷酸酯，然后进行氢化，用H代替二苄基，然后与Amberlite IR-120（Na +形式）反应形成二钠盐。初步筛选结果表明，这些磷酸盐显示出显着的抗癌活性。还合成2-苯基-4-喹诺酮的新型中间体2-硒吩-4-喹诺酮和Λ/，Λ/二烷基氨基烷基衍生物。这些新型中间体显示出显着的抗癌活性。

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