公开(公告)号：US20120101157A1

公开(公告)日：2012-04-26

申请号：US13279519

申请日：2011-10-24

Applicant: AN-RONG LEE ,  WEN-HSIN HUANG ,  CHI-HONG CHU ,  WEN-LIANG CHANG ,  CHEN-WEN YAO ,  I-LING CHEN

Inventor： AN-RONG LEE ,  WEN-HSIN HUANG ,  CHI-HONG CHU ,  WEN-LIANG CHANG ,  CHEN-WEN YAO ,  I-LING CHEN

IPC: A61K31/245 ,  C07C233/54 ,  C07C231/14 ,  A61P31/16 ,  C07C277/08 ,  C07C279/18 ,  A61K31/196

CPC classification number: C07C233/54 ,  C07C279/18

Abstract: Disclosed are 4,5-diamino-3-halo-2-hydroxybenzoic acid derivatives and manufactures thereof. The 4,5-diamino-3-halo-2-hydroxybenzoic acid derivatives are presented by formula (I): wherein R1 group is H, CH3, or C2H5; R2 group is H, or Br; R3 group is CH3, or C3H7; and R4 group is H, or C(═NH)—NH2. 4,5-diamino-3-halo-2-hydroxybenzoic acid derivatives provided here were non-toxic to MDCK cells, particularly compounds 6a, 6b, 6c, 6e, 6f, 7a, 7b and 8 had better anti-H1N1 activity. In the future, these compounds can be used to focus on viral neuraminidases as targets to develop effective anti-influenza drugs.

Abstract translation: 公开了4,5-二氨基-3-卤代-2-羟基苯甲酸衍生物及其制造方法。 4,5-二氨基-3-卤代-2-羟基苯甲酸衍生物由式（I）表示：其中R 1基团是H，CH 3或C 2 H 5; R2组为H或Br; R3基团是CH3或C3H7; 和R 4基团是H或C（= NH）-NH 2。 本文提供的4,5-二氨基-3-卤代-2-羟基苯甲酸衍生物对MDCK细胞无毒，特别是化合物6a，6b，6c，6e，6f，7a，7b和8具有更好的抗H1N1活性。 未来，这些化合物可用于将病毒性神经氨酸酶作为靶点开发有效的抗流感药物。

公开(公告)号：US08414938B2

公开(公告)日：2013-04-09

申请号：US13298607

申请日：2011-11-17

Applicant: Wen-Liang Chang ,  Chen-Wen Yao ,  Chi-Hong Chu ,  An-Rong Lee ,  Ann Chen ,  Wen-Hsin Huang ,  Kuo-Yuan Hwa ,  Chiao-Ying Chien ,  Chien-Yi Pai

Inventor： Wen-Liang Chang ,  Chen-Wen Yao ,  Chi-Hong Chu ,  An-Rong Lee ,  Ann Chen ,  Wen-Hsin Huang ,  Kuo-Yuan Hwa ,  Chiao-Ying Chien ,  Chien-Yi Pai

IPC: A01N65/00

CPC classification number: A61K36/79 ,  A61K31/122 ,  A61K31/357 ,  A61K2236/35

Abstract: Disclosed are an Schisandrae fructus extract for inhibition or prevention of influenza and its application, wherein the Schisandrae fructus extract is obtained by water, methanol, or ethanol extraction process and the extract comprises compounds such as schisandrone, benzoylgomisin P, wulignan A1, epigomisin O, epiwulignan A1, and tigloylgomisin P. The extracts and purified compounds of Schisandrae fructus has anti-influenza virus H1N1 and H1N1-TR (a Tamiflu drug resistant virus strain) activities, therefore the extracts and the purified compounds of Schisandrae fructus can be applied as an inhitibory agent of a pharmaceutical composition for treatment or prevention agent for influenza infection.

Abstract translation: 公开了用于抑制或预防流感及其应用的五味子提取物，其中五味子提取物通过水，甲醇或乙醇提取方法获得，并且提取物包含化合物，例如五味子酮，苯甲酰基乳球菌素P，五味子胺A1，表不见素O， 五味子甙A和枸橼酸甘草聚糖P.提取物和纯化的五味子化合物具有抗流感病毒H1N1和H1N1-TR（达菲药物耐药病毒株）的活性，因此提取物和五味子的纯化化合物可以作为 用于流感感染的治疗或预防剂的药物组合物的生物剂。

公开(公告)号：US20120189719A1

公开(公告)日：2012-07-26

申请号：US13298607

申请日：2011-11-17

Applicant: WEN-LIANG CHANG ,  CHEN-WEN YAO ,  CHI-HONG CHU ,  AN-RONG LEE ,  ANN CHEN ,  WEN-HSIN HUANG ,  KUO-YUAN HWA ,  CHIAO-YING CHIEN ,  CHIEN-YI PAI

Inventor： WEN-LIANG CHANG ,  CHEN-WEN YAO ,  CHI-HONG CHU ,  AN-RONG LEE ,  ANN CHEN ,  WEN-HSIN HUANG ,  KUO-YUAN HWA ,  CHIAO-YING CHIEN ,  CHIEN-YI PAI

IPC: A61K36/00 ,  A61K31/343 ,  A61P31/16 ,  A61K31/122

CPC classification number: A61K36/79 ,  A61K31/122 ,  A61K31/357 ,  A61K2236/35

Abstract: Disclosed are an Schisandrae fructus extract for inhibition or prevention of influenza and its application, wherein the Schisandrae fructus extract is obtained by water, methanol, or ethanol extraction process and the extract comprises compounds such as schisandrone, benzoylgomisin P, wulignan A1, epigomisin O, epiwulignan A1, and tigloylgomisin P. The extracts and purified compounds of Schisandrae fructus has anti-influenza virus H1N1 and H1N1-TR (a Tamiflu drug resistant virus strain) activities, therefore the extracts and the purified compounds of Schisandrae fructus can be applied as an inhitibory agent of a pharmaceutical composition for treatment or prevention agent for influenza infection.

Abstract translation: 公开了用于抑制或预防流感及其应用的五味子提取物，其中五味子提取物通过水，甲醇或乙醇提取方法获得，并且提取物包含化合物，例如五味子酮，苯甲酰基乳球菌素P，五味子胺A1，表不见素O， 五味子甙A和枸橼酸甘草聚糖P.提取物和纯化的五味子化合物具有抗流感病毒H1N1和H1N1-TR（达菲药物耐药病毒株）的活性，因此五味子的提取物和纯化的化合物可以作为 用于流感感染的治疗或预防剂的药物组合物的生物剂。