公开(公告)号：US08440692B2

公开(公告)日：2013-05-14

申请号：US12448088

申请日：2007-12-07

Applicant: 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

Inventor： 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: A61K31/47 ,  C07F9/38

CPC classification number: C07F9/6561 ,  C07D215/233 ,  C07D421/04 ,  C07D491/056 ,  C07F9/60

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US20100168064A1

公开(公告)日：2010-07-01

申请号：US12448088

申请日：2007-12-07

Applicant: 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

Inventor： 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: A61K31/675 ,  C07F9/09 ,  A61K31/47 ,  A61P35/00 ,  A61P35/02 ,  C07D421/04 ,  C07D215/233

CPC classification number: C07F9/6561 ,  C07D215/233 ,  C07D421/04 ,  C07D491/056 ,  C07F9/60

Abstract: 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.

Abstract translation: 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。

公开(公告)号：US07176230B2

公开(公告)日：2007-02-13

申请号：US11274436

申请日：2005-11-15

Applicant: Sheng-Chu Kuo ,  Fang-Yu Lee ,  Tsang-Miao Huang ,  Che-Ming Teng ,  On Lee ,  Chin-Yi Wu ,  Chrong-Shiong Hwang ,  Chi-Ying Hung

Inventor： Sheng-Chu Kuo ,  Fang-Yu Lee ,  Tsang-Miao Huang ,  Che-Ming Teng ,  On Lee ,  Chin-Yi Wu ,  Chrong-Shiong Hwang ,  Chi-Ying Hung

IPC: A61K31/405 ,  C07D209/04

CPC classification number: C07D209/12 ,  C07D405/04 ,  C07D409/04

Abstract: The present invention synthesizes a series of novel indole analogs of 1-benzyl-3-(5′-hydroxymethyl-2′-furyl)indazole (YC-1), and their anti-platelet activity.

Abstract translation: 本发明合成了一系列1-苄基-3-（5'-羟甲基-2'-呋喃基）吲唑（YC-1）的新吲哚类似物及其抗血小板活性。

公开(公告)号：US06946153B2

公开(公告)日：2005-09-20

申请号：US10438233

申请日：2003-05-14

Applicant: Tian-Shung Wu ,  Sheng-Chu Kuo ,  Che-Ming Teng ,  Feng-Nien Ko

Inventor： Tian-Shung Wu ,  Sheng-Chu Kuo ,  Che-Ming Teng ,  Feng-Nien Ko

IPC: A61K36/9066 ,  A61K35/78

CPC classification number: A61K36/9068 ,  A61K36/9066 ,  Y10S514/864

Abstract: A method of treating a patient suffering a disease associated with Trichophyton mentagrophytes or Pityrosporum ovale by applying topically an anti-fungal pharmaceutical composition which is prepared from Zingiber officinale, includes the following steps: preparing a crude liquid from rhizomes of ginger by extraction with an organic solvent or supercritical CO2, or by distillation with steam; introducing the crude liquid to a reverse phase chromatography column, and eluting the column with water, a first eluent and a second eluent having a polarity weaker than that of the first eluent but stronger than that of chloroform, so that a first eluate resulting from elution of the first eluent and a second eluate resulting from elution of the second eluent are obtained; removing the first eluent and the second eluent from the first eluate and the second eluate by evaporation, respectively, so that a first concentrated eluate and a second concentrated eluate are obtained as the potent extract.

Abstract translation: 通过局部施用由姜科药剂制备的抗真菌药物组合物治疗患有与毛癣菌相关的疾病的患者的方法包括以下步骤：通过用有机物提取从姜的根茎制备粗液体 溶剂或超临界CO 2，或通过蒸汽蒸馏; 将粗液体引入反相色谱柱，并用水洗脱柱，第一洗脱液和第二洗脱液，其极性弱于第一洗脱液的极性，但比氯仿强烈，使得从洗脱产生的第一洗脱液 的第一洗脱液和由第二洗脱液洗脱产生的第二洗脱液; 通过蒸发分别从第一洗脱液和第二洗脱液除去第一洗脱液和第二洗脱液，使得获得第一浓缩洗脱液和第二浓缩洗脱液作为有效提取物。

公开(公告)号：US20050119278A1

公开(公告)日：2005-06-02

申请号：US10930065

申请日：2004-08-30

Applicant: Che-Ming Teng ,  Sheng-Chu Kuo ,  Fang-Yu Lee ,  Shiow-Lin Pan ,  Jih-Hwa Guh

Inventor： Che-Ming Teng ,  Sheng-Chu Kuo ,  Fang-Yu Lee ,  Shiow-Lin Pan ,  Jih-Hwa Guh

IPC: A61K31/416 ,  A61K31/4745 ,  A61K31/519 ,  A61K31/4162 ,  A61K31/4439 ,  A61K31/506

CPC classification number: A61K31/4745 ,  A61K31/416 ,  A61K31/519

Abstract: A method for inhibiting cell proliferation, cell migration, or tube formation induced by an angiogenic factor. The method includes administrating to a subject in need thereof an effective amount of a compound of the formula: wherein A is H or in which n is 0, 1, 2, or 3; each of Ar1, Ar2, and Ar3, independently, is phenyl, thienyl, furyl, pyrrolyl, pyridinyl, or pyrimidinyl; each of R1, R2, R3, R4, R5, and R6, independently, is R, nitro, halogen, C(O)OR, C(O)SR, C(O)NRR′, (CH2)mOR, (CH2)mSR, (CH2)mNRR′, (CH2)mCN, (CH2)mC(O)OR, (CH2)mCHO, (CH2)mCH═NOR, or R1 and R2 together, R3 and R4 together, or R5 and R6 together are O(CH2)mO, in which each of R and R′, independently, is H, alkyl, aryl, heteroaryl, cyclyl, or heterocyclyl; and m is 0, 1, 2, 3, 4, 5, or 6, and n is 0, 1, 2, or 3.

Abstract translation: 一种抑制血管生成因子诱导的细胞增殖，细胞迁移或管形成的方法。 该方法包括向有需要的受试者施用有效量的下式化合物：其中A为H或其中n为0,1,2或3; Ar 1，Ar 2和Ar 3各自独立地是苯基，噻吩基，呋喃基，吡咯基，吡啶基或嘧啶基; R 1，R 2，R 3，R 4，R 5，和/或R 3中的每一个 >和R 6独立地是R，硝基，卤素，C（O）OR，C（O）SR，C（O）NRR'，（CH 2） （CH 2）m，或（CH 2）m SR，（CH 2 2）m， C（O）OR（CH 2 CH 2）m C（O）OR（CH 2） ，（CH 2 CH 2）m CHO，（CH 2 CH 2）m CH或NOR，或R 1， 1个和R 2个在一起，R 3和R 4一起，或者R 5和R 5 一起是O（CH 2）2 O，其中R和R'各自独立地是H，烷基，芳基， 杂芳基，环基或杂环基; m为0,1,2,3,4,5或6，n为0,1,2或3。

公开(公告)号：US5853731A

公开(公告)日：1998-12-29

申请号：US841053

申请日：1997-04-29

Applicant: Tian-Shung Wu ,  Che-Ming Teng ,  Sheu-Meei Yu

Inventor： Tian-Shung Wu ,  Che-Ming Teng ,  Sheu-Meei Yu

IPC: C07C43/23 ,  C07C59/64 ,  C07C69/017 ,  C07C69/734 ,  A01N65/00 ,  A61K35/78

CPC classification number: C07C59/64 ,  C07C43/23 ,  C07C69/017 ,  C07C69/734

Abstract: A pharmaceutical composition which possesses vasorelaxing effect of aortic contraction, relaxing effect of tracheal contraction, and antioxidative properties, is disclosed. It contains a pharmaceutical acceptable vehicle and an effective amount of any compound selected from those compounds represented by the following formula: ##STR1## where R.sub.1 represents H, C.sub.1-8 alkyl, or --OCOR, R.sub.2 represents OH, or COO.sup.--, and R represents H, or C.sub.1-8 alkyl.

Abstract translation: 公开了具有主动脉收缩的血管舒张作用，气管收缩的放松效果和抗氧化性质的药物组合物。 它含有药物可接受的载体和有效量的选自下列化学式表示的那些化合物的任何化合物：其中R1代表H，C1-8烷基或-OCOR，R2代表OH或COO-，R 表示H或C 1-8烷基。

公开(公告)号：US08501957B2

公开(公告)日：2013-08-06

申请号：US12635206

申请日：2009-12-10

Applicant: Chih-Shiang Chang ,  Jih-Hwa Guh ,  Che-Ming Teng ,  Shiow-Lin Pan ,  Wei-Ling Chang ,  Ju-Fang Liu ,  Kai-Wei Chang ,  Sheng-Chu Kuo

Inventor： Chih-Shiang Chang ,  Jih-Hwa Guh ,  Che-Ming Teng ,  Shiow-Lin Pan ,  Wei-Ling Chang ,  Ju-Fang Liu ,  Kai-Wei Chang ,  Sheng-Chu Kuo

IPC: A61K31/4184 ,  C07D235/18

CPC classification number: A61K31/4184 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/496 ,  A61K31/5377 ,  C07D235/06 ,  C07D235/10 ,  C07D235/18 ,  C07D401/04 ,  C07D401/12 ,  C07D403/06 ,  C07D403/12 ,  C07D405/04 ,  C07D405/14 ,  C07D409/04

Abstract: Benzimidazole compounds of formula (I): wherein R1, R2, R3, R4, R5, X, Y, Z1, and Z2 are defined herein. Also disclosed is a method for treating cancer with benzimidazole compounds.

Abstract translation: 式（I）的苯并咪唑化合物：其中R1，R2，R3，R4，R5，X，Y，Z1和Z2如本文所定义。 还公开了用苯并咪唑化合物治疗癌症的方法。

公开(公告)号：US20060106032A1

公开(公告)日：2006-05-18

申请号：US11274528

申请日：2005-11-15

Applicant: Sheng-Chu Kuo ,  Li-Jiau Huang ,  Fang-Yu Lee ,  Che-Ming Teng ,  Mei-Ling Shih ,  Hua-Sin Chen

Inventor： Sheng-Chu Kuo ,  Li-Jiau Huang ,  Fang-Yu Lee ,  Che-Ming Teng ,  Mei-Ling Shih ,  Hua-Sin Chen

IPC: A61K31/519 ,  A61K31/506 ,  A61K31/4745 ,  A61K31/4439 ,  A61K31/416 ,  C07D487/02 ,  C07D403/02

CPC classification number: C07D231/56 ,  C07D405/06

Abstract: Novel compounds of 2-(substituted arylmethyl)-3-(substituted phenyl)-2H-indazoles and 1-(substituted arylmethyl)-3-(substituted phenyl)-1H-indazoles are synthesized, and useful as anti-angiogenic agents.

Abstract translation: 合成2-（取代的芳基甲基）-3-（取代的苯基）-2H-吲唑和1-（取代的芳基甲基）-3-（取代的苯基）-1H-吲唑的新型化合物，可用作抗血管生成剂。

公开(公告)号：US20050209252A1

公开(公告)日：2005-09-22

申请号：US11132756

申请日：2005-05-18

Applicant: Che-Ming Teng ,  Sheng-Chu Kuo ,  Fang-Yu Lee ,  Shiow-Lin Pan ,  Jih-Hwa Guh

Inventor： Che-Ming Teng ,  Sheng-Chu Kuo ,  Fang-Yu Lee ,  Shiow-Lin Pan ,  Jih-Hwa Guh

IPC: C07D405/04 ,  A61K31/416 ,  A61K31/4162 ,  A61K31/4745 ,  A61K31/519 ,  A61P1/04 ,  A61P3/06 ,  A61P3/10 ,  A61P9/00 ,  A61P9/10 ,  A61P15/00 ,  A61P17/06 ,  A61P19/02 ,  A61P27/02 ,  A61P29/00 ,  A61P35/00

CPC classification number: A61K31/416 ,  A61K31/4162 ,  A61K31/4745 ,  A61K31/519

Abstract: This invention relates to a method for treating cancer including administrating to a subject in need thereof an effective amount of a compound of the formula: wherein, A is H or each of Ar1, Ar2, and Ar3, independently, is phenyl, thienyl, furyl, pyrrolyl, pyridinyl, or pyrimidinyl; each of R1, R2, R3, R4, R5, and R6, independently, is R, nitro, halogen, C(O)OR, C(O)SR, C(O)NRR′, (CH2)mOR, (CH2)mSR, (CH2)mNRR′, (CH2)mCN, (CH2)mC(O)OR, (CH2)mCHO, (CH2)mCH═NOR, (CH2)mC(O)N(OR)R′, N(OR)R′, or R1 and R2 together, R3 and R4 together, or R5 and R6 together are O(CH2)mO, in which each of R and R′, independently, is H or C1˜C6 alkyl; and m is 0, 1, 2, 3, 4, 5, or 6, and n is 0, 1, 2, or 3.

Abstract translation: 本发明涉及一种治疗癌症的方法，包括向有需要的受试者施用有效量的下式化合物：其中A为H或Ar 1，Ar 2的每一个 R 3和R 3独立地是苯基，噻吩基，呋喃基，吡咯基，吡啶基或嘧啶基; R 1，R 2，R 3，R 4，R 5，和/或R 3中的每一个 >和R 6独立地是R，硝基，卤素，C（O）OR，C（O）SR，C（O）NRR'，（CH 2） （CH 2）m，或（CH 2）m SR，（CH 2 2）m， C（O）OR（CH 2 CH 2）m C（O）OR（CH 2） ，（CH 2 CH 2）m CHO，（CH 2 CH 2）m CH，或CH 2，（CH 3） C（O）N（OR）R'，N（OR）R'或R 1和R 2' 一起，R 3和R 4一起，或者R 5和R 6一起是O（CH 其中R和R'各自独立地是H或C 1〜C 6， 烷基; m为0,1,2,3,4,5或6，n为0,1,2或3。

公开(公告)号：US06387942B2

公开(公告)日：2002-05-14

申请号：US09883742

申请日：2001-06-18

Applicant: Che-Ming Teng ,  Sheng-Chu Kuo ,  Fang Yu Lee

Inventor： Che-Ming Teng ,  Sheng-Chu Kuo ,  Fang Yu Lee

IPC: A61K3140

CPC classification number: C07D231/56 ,  A61K31/415 ,  C07D405/04 ,  C07D491/04 ,  C07D495/04

Abstract: A method of treating a disorder related to cell activation induced by protease-activated receptors. The method includes administering to a subject in need thereof a compound having a pyrazolyl core; an aryl group, via an via an alkylene linker, bonded to 1-N of the pyrazolyl core; a second aryl group fused at 4-C and 5-C of the pyrazolyl core; and a third aryl group bonded directly to 3-C of the pyrazolyl core.

Abstract translation: 治疗由蛋白酶激活受体诱导的细胞活化相关疾病的方法。 该方法包括向有需要的受试者施用具有吡唑基核心的化合物; 经由亚烷基接头的芳基与吡唑基核心的1-N键合; 在吡唑基核心的4℃和5℃熔化的第二个芳基; 和直接与吡唑基核心的3-C键合的第三个芳基。