公开(公告)号：US07851654B2

公开(公告)日：2010-12-14

申请号：US12295669

申请日：2006-04-03

Applicant: Ki Hun Park ,  Jin Hyo Kim ,  Woo Duck Seo ,  Young Bae Ryu ,  Hyung Won Ryu ,  Woo Song Lee ,  Sang Wan Gal

Inventor： Ki Hun Park ,  Jin Hyo Kim ,  Woo Duck Seo ,  Young Bae Ryu ,  Hyung Won Ryu ,  Woo Song Lee ,  Sang Wan Gal

IPC: C07C211/00 ,  A61K31/13 ,  A61K31/135

CPC classification number: C07C49/796 ,  C07C45/74 ,  C07C49/835 ,  C07C225/22 ,  C07C311/08 ,  C07C311/21

Abstract: Disclosed relates to a novel chalcone derivative, pharmaceutically acceptable salt thereof, a method for preparing the same and uses thereof, the chalcone derivative being readily obtained through the steps of: reacting aminoacetophenone with sulfonylchloride under the presence of an appropriate salt; and reacting the compound prepared in the above step with hydroxybenzaldehide under the presence of an appropriate catalyst. The chalcone derivative of formula 1 in accordance with the present invention having strong enzyme inhibitory activities for glycosidase can be effectively used in preventing and treating various diseases induced by glycosidase, and the chalcone derivative of the invention having tyrosinase and melanin synthesis inhibitory activities can be effectively used as a skin-whitening compound.

Abstract translation: 本发明涉及一种新型查耳酮衍生物，其药学上可接受的盐，其制备方法及其用途，所述查耳酮衍生物通过以下步骤容易地获得：在适当的盐存在下使氨基苯乙酮与磺酰氯反应; 并在合适的催化剂存在下使上述步骤制备的化合物与羟基苯甲醛反应。 具有强糖酶抑制活性的本发明式1的查耳酮衍生物可有效地用于预防和治疗由糖苷酶诱导的各种疾病，具有酪氨酸酶和黑色素合成抑制活性的本发明查耳酮衍生物可以有效地 用作皮肤美白化合物。

公开(公告)号：US20090252694A1

公开(公告)日：2009-10-08

申请号：US12295669

申请日：2006-04-03

Applicant: Ki Hun Park ,  Jin Hyo Kim ,  Woo Duck Seo ,  Young Bae Ryu ,  Hyung Won Ryu ,  Woo Song Lee ,  Sang Wan Gal

Inventor： Ki Hun Park ,  Jin Hyo Kim ,  Woo Duck Seo ,  Young Bae Ryu ,  Hyung Won Ryu ,  Woo Song Lee ,  Sang Wan Gal

IPC: A61K8/35 ,  C07C211/27 ,  A61K31/137 ,  A61P3/10 ,  A61P3/04 ,  A61P35/00 ,  A61P31/12 ,  A61P31/18 ,  A61P31/14 ,  A61P31/20 ,  A61Q19/02 ,  C07C49/796 ,  A61K31/12

CPC classification number: C07C49/796 ,  C07C45/74 ,  C07C49/835 ,  C07C225/22 ,  C07C311/08 ,  C07C311/21

Abstract: Disclosed relates to a novel chalcone derivative, pharmaceutically acceptable salt thereof, a method for preparing the same and uses thereof, the chalcone derivative being readily obtained through the steps of: reacting aminoacetophenone with sulfonylchloride under the presence of an appropriate salt; and reacting the compound prepared in the above step with hydroxybenzaldehide under the presence of an appropriate catalyst. The chalcone derivative of formula 1 in accordance with the present invention having strong enzyme inhibitory activities for glycosidase can be effectively used in preventing and treating various diseases induced by glycosidase, and the chalcone derivative of the invention having tyrosinase and melanin synthesis inhibitory activities can be effectively used as a skin-whitening compound.

Abstract translation: 本发明涉及一种新型查耳酮衍生物，其药学上可接受的盐，其制备方法及其用途，所述查耳酮衍生物通过以下步骤容易地获得：在适当的盐存在下使氨基苯乙酮与磺酰氯反应; 并在合适的催化剂存在下使上述步骤制备的化合物与羟基苯甲醛反应。 具有强糖酶抑制活性的本发明式1的查耳酮衍生物可有效地用于预防和治疗由糖苷酶诱导的各种疾病，具有酪氨酸酶和黑色素合成抑制活性的本发明查耳酮衍生物可以有效地 用作皮肤美白化合物。