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1.发明授权1-(3-METHYL-2,4-DIMETHOXYPHENYL)-3-(2',4'-DIHYDROXYPHENYL)-PROPANE AS A POTENT TYROSINASE INHIBITOR 有权1-（3-甲基-2,4-二甲氧基苯基）-3-（2'，4'-二羟基苯基）丙酸酯HOCHWIRKSAMER酪氨酸酶抑制剂
公开(公告)号：EP1748767B1
公开(公告)日：2011-12-28
申请号：EP05762186.4
申请日：2005-05-27
申请人： Unigen, Inc. , Jia, Qi , Zhao, Ji-Fu
发明人： JIA, Qi , ZHAO, Ji-Fu
IPC分类号： A61K31/015 , A61K31/05 , A61K31/085 , A61K31/09 , A61K31/357 , A61K31/40 , A61P17/00 , A61P35/00 , C07D233/02 , C07D323/00
CPC分类号： A61K8/347 , A61K8/31 , A61K8/4973 , A61K8/97 , A61K31/015 , A61K31/05 , A61K31/085 , A61K31/09 , A61K31/357 , A61K31/40 , A61K31/704 , A61K2800/782 , A61Q19/02 , C07C39/15 , C07C39/367 , C07C41/26 , C07C41/32 , C07C43/23 , C07C45/673 , C07C49/835 , C07C215/74 , C07D321/12 , Y02A50/406 , Y02A50/411
摘要： The present invention implements a strategy that combines an enzyme inhibition assay with a chemical dereplication process to identify active plant extracts and the particular compounds—diarylalkanes and/or diarylalkanols within those extracts that specifically inhibit binuclear enzyme function. Included in the present invention are compositions of matter comprised of one or more of diarylalkanes and/or diarylalkanols, which inhibit the activity of binuclear enzymes, particularly tyrosinase and which prevent melanin overproduction. The present invention also provides a method for inhibiting the activity of a binuclear enzyme, particularly tyrosinase and a method for preventing and treating diseases and conditions related to binuclear enzyme function. The present invention further includes a method for preventing and treating melanin overproduction and diseases and conditions of the skin related thereto. The method for preventing and treating diseases and conditions related to binuclear enzyme function and melanin overproduction is comprised of administering to a host in need thereof an effective amount of a composition comprising one or more diarylalkanes and/or diarylalkanols synthesized and/or isolated from one or more plants together with a pharmaceutically acceptable carrier.
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2.发明公开DIARYLALKANES AS POTENT INHIBITORS OF BINUCLEAR ENZYMES 有权1-（3-甲基-2,4-二甲氧基苯基）-3-（2”，4'-二羟基苯基）丙烷作为有效酪氨酸酶抑制剂
公开(公告)号：EP1748767A1
公开(公告)日：2007-02-07
申请号：EP05762186.4
申请日：2005-05-27
发明人： JIA, Qi , ZHAO, Ji-Fu
IPC分类号： A61K31/015
CPC分类号： A61K8/347 , A61K8/31 , A61K8/4973 , A61K8/97 , A61K31/015 , A61K31/05 , A61K31/085 , A61K31/09 , A61K31/357 , A61K31/40 , A61K31/704 , A61K2800/782 , A61Q19/02 , C07C39/15 , C07C39/367 , C07C41/26 , C07C41/32 , C07C43/23 , C07C45/673 , C07C49/835 , C07C215/74 , C07D321/12 , Y02A50/406 , Y02A50/411
摘要： The present invention implements a strategy that combines an enzyme inhibition assay with a chemical dereplication process to identify active plant extracts and the particular compounds—diarylalkanes and/or diarylalkanols within those extracts that specifically inhibit binuclear enzyme function. Included in the present invention are compositions of matter comprised of one or more of diarylalkanes and/or diarylalkanols, which inhibit the activity of binuclear enzymes, particularly tyrosinase and which prevent melanin overproduction. The present invention also provides a method for inhibiting the activity of a binuclear enzyme, particularly tyrosinase and a method for preventing and treating diseases and conditions related to binuclear enzyme function. The present invention further includes a method for preventing and treating melanin overproduction and diseases and conditions of the skin related thereto. The method for preventing and treating diseases and conditions related to binuclear enzyme function and melanin overproduction is comprised of administering to a host in need thereof an effective amount of a composition comprising one or more diarylalkanes and/or diarylalkanols synthesized and/or isolated from one or more plants together with a pharmaceutically acceptable carrier.
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