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1. 发明授权

US07378232B2 Assay for melanogenesis 失效
标题翻译：测定黑素生成
公开(公告)号：US07378232B2
公开(公告)日：2008-05-27
申请号：US10435439
申请日：2003-05-09
申请人： Seth J. Orlow , Prashiela Manga , Liliana Staleva
发明人： Seth J. Orlow , Prashiela Manga , Liliana Staleva
IPC分类号： C12Q1/00 , C12Q1/02
CPC分类号： G01N33/5011 , G01N33/5008 , G01N33/5014 , G01N33/5044 , G01N33/5097 , G01N33/6872 , G01N2510/00
摘要： The invention provides methods for the identification of agents that modify or mimic P protein function. Cells expressing a P protein are generally more sensitive to toxins, and changes in cell viability and/or cell death after exposure of P protein-expressing cells to an agent and a toxin is an indication that such an agent is a modifier of P protein expression. The invention also provides methods for the treatment of melanoma and other cancers.
摘要翻译：本发明提供用于鉴定修饰或模拟P蛋白功能的试剂的方法。表达P蛋白的细胞通常对毒素更敏感，并且将表达P蛋白的细胞暴露于药物和毒素后，细胞活力和/或细胞死亡的变化表明这样的试剂是P蛋白表达的调节剂。本发明还提供了治疗黑素瘤和其他癌症的方法。

2. 发明授权

US07604949B2 Methods and compositions that affect melanogenesis 失效
公开(公告)号：US07604949B2
公开(公告)日：2009-10-20
申请号：US11408108
申请日：2006-04-20
申请人： Seth J. Orlow , Andrea Hall , Prashiela Manga
发明人： Seth J. Orlow , Andrea Hall , Prashiela Manga
IPC分类号： G01N33/53
CPC分类号： A61K8/4906 , A61K8/72 , A61K31/56 , A61Q19/02 , C12Q1/26 , G01N33/5008 , G01N33/502 , G01N33/5035 , G01N33/5044 , G01N33/5076 , G01N33/5088 , G01N33/6881 , G01N2333/90219 , G01N2500/00 , G01N2500/10 , G01N2800/207
摘要： The invention provides methods of screening for compounds that affect melanogenesis and the function of P protein in organisms, cells, or cell-free systems. The invention further relates to pharmacologic and cosmetic uses of methods of inhibiting melanogenesis, methods of activating melanogenesis, and compounds and pharmacologic compositions useful for the inhibition or activation of melanogenesis and, therefore, for lightening or darkening the pigmentation of cells and tissue, i.e., skin.

3. 发明授权

US06749840B2 Inhibition of pigmentation by inhibition of fatty acid synthase 有权
标题翻译：通过抑制脂肪酸合酶抑制色素沉着
公开(公告)号：US06749840B2
公开(公告)日：2004-06-15
申请号：US10137632
申请日：2002-05-02
申请人： Seth J. Orlow , Andrea Hall
发明人： Seth J. Orlow , Andrea Hall
IPC分类号： A61K7135
CPC分类号： A61K31/00 , A61K31/34 , A61K31/365 , A61K31/38
摘要： The invention provides novel methods and pharmaceutical compositions designed to decrease melanin production by inhibiting fatty acid synthase in a melanocyte, thereby lightening skin pigmentation.
摘要翻译：本发明提供了通过抑制黑素细胞中的脂肪酸合成来减少黑色素产生的新方法和药物组合物，从而减轻皮肤色素沉着。

4. 发明申请

US20130302264A1 INDOLE ALKALOID COMPOUNDS AS MELANOGENESIS PROMOTERS AND USES THEREOF 有权
标题翻译：作为造血发酵剂的吲哚类化合物及其用途
公开(公告)号：US20130302264A1
公开(公告)日：2013-11-14
申请号：US13885685
申请日：2011-11-16
申请人： Seth J. Orlow , Li Ni Komatsu
发明人： Seth J. Orlow , Li Ni Komatsu
IPC分类号： A61K31/475 , A61K45/06 , A61K31/4375
CPC分类号： A61K31/475 , A61K8/4906 , A61K8/4926 , A61K31/437 , A61K31/4375 , A61K36/72 , A61K45/06 , A61Q17/04 , A61Q19/04 , C07D471/14 , C07D491/22 , A61K2300/00
摘要： Provided are indole alkaloid compounds of formula I, for example, pubescine, and the use of such compounds and compositions thereof to promote (e.g., enhance) melanogenesis and pigmentation. Also provided are plant extracts containing a compound of formula I, for example, pubescine, and the use of such a plant extract to promote (e.g., enhance) melanogenesis and pigmentation. The compound or plant extract may be prepared as pharmaceutical and cosmetic compositions, and may be used for the prevention and treatment of conditions that are related to aberrant melanogenesis activity.
摘要翻译：提供式I的吲哚生物碱化合物，例如，绒毛，以及这些化合物及其组合物用于促进（例如增强）黑素生成和色素沉着的用途。还提供了含有式I化合物，例如草丝的植物提取物，以及这种植物提取物用于促进（例如增强）黑素生成和色素沉着的用途。化合物或植物提取物可以制备为药物和化妆品组合物，并且可以用于预防和治疗与异常黑素生成活性相关的病症。

5. 发明授权

US08772252B2 Coumarin compounds as melanogenesis modifiers and uses thereof 有权
标题翻译：香豆素化合物作为黑素生成修饰剂及其用途
公开(公告)号：US08772252B2
公开(公告)日：2014-07-08
申请号：US13360619
申请日：2012-01-27
申请人： Seth J. Orlow , Li Ni Komatsu
发明人： Seth J. Orlow , Li Ni Komatsu
IPC分类号： A61K31/37 , A61K31/665 , A61K31/7048 , A61K45/06 , A61K36/48
CPC分类号： A61K31/37 , A61K8/498 , A61K8/97 , A61K9/0014 , A61K9/0019 , A61K9/06 , A61K9/08 , A61K9/2063 , A61K9/4866 , A61K36/48 , A61K45/06 , A61K47/20 , A61Q19/02 , A61K2300/00
摘要： Provided are coumarin compounds of formula I, for example, robustic acid methyl ether, and the use of such compounds and compositions thereof to modulate (e.g., inhibit) melanogenesis and pigmentation. wherein R3, R4, R5, R6, R7 and R8 are described herein. Also provided are plant extracts containing a compound of formula I, and the use of such a plant extract to modulate (e.g., inhibit) melanogenesis and pigmentation. The compound or plant extract may be prepared as pharmaceutical and cosmetic compositions, and may be used for the prevention and treatment of conditions that are related to aberrant melanogenesis activity.
摘要翻译：提供式I的香豆素化合物，例如强直性甲基醚，以及这些化合物及其组合物用于调节（例如抑制）黑素生成和色素沉着的用途。其中R3，R4，R5，R6，R7和R8如本文所述。还提供了含有式I化合物的植物提取物和这种植物提取物用于调节（例如抑制）黑素生成和色素沉着的用途。化合物或植物提取物可以制备为药物和化妆品组合物，并且可以用于预防和治疗与异常黑素生成活性相关的病症。

6. 发明申请

US20100093823A1 STEROIDAL COMPOUNDS AS MELANOGENESIS MODIFIERS AND USES THEREOF 审中-公开
标题翻译：作为造血剂改性剂的异种化合物及其用途
公开(公告)号：US20100093823A1
公开(公告)日：2010-04-15
申请号：US12433322
申请日：2009-04-30
申请人： Seth J. Orlow , Li Ni Komatsu
发明人： Seth J. Orlow , Li Ni Komatsu
IPC分类号： A61K31/403 , C12N5/071 , C07D209/56 , A61P17/00
CPC分类号： A61K31/56 , A61K8/63 , A61K31/58 , A61Q19/02
摘要： A method for the identification of compounds) that control melanin synthesis (melanogenesis), and the preparation and use of such compounds, and compositions and formulations thereof to modify (e.g., inhibit) melanin production are disclosed. A representative compound of the invention is defined by formula I: The compounds may be prepared as pharmaceutical and cosmetic compositions, and in one embodiment, may be prepared in combination with each other, and with other melanogenesis inhibiting formulations. The compounds, compositions and formulations of the invention may be used for the prevention and treatment of conditions that are causally related to aberrant melanogenesis activity including, by way of non-limiting example, hyperpigmentation and others.
摘要翻译：公开了控制黑色素合成（黑素生成）的化合物的鉴定方法，以及这些化合物及其组合物和制剂的制备和用途，以改变（例如抑制）黑色素的产生。本发明的代表性化合物由式I定义：化合物可以制备为药物和化妆品组合物，并且在一个实施方案中，可以彼此组合制备，并与其它黑素生成抑制制剂一起制备。本发明的化合物，组合物和制剂可用于预防和治疗与异常黑素生成活性有因果关系的病症，包括作为非限制性实例，色素沉着过度等。

7. 发明申请

US20090298868A1 QUINOLINE COMPOUNDS AS MELANOGENESIS MODIFIERS AND USES THEREOF 审中-公开
标题翻译：喹啉化合物作为成色剂改性剂及其用途
公开(公告)号：US20090298868A1
公开(公告)日：2009-12-03
申请号：US12433863
申请日：2009-04-30
申请人： Seth J. Orlow , Li Ni Komatsu
发明人： Seth J. Orlow , Li Ni Komatsu
IPC分类号： A61K31/4709 , A61K31/47
CPC分类号： A61K31/47 , A61K31/4706 , A61K31/4709 , A61K31/49 , A61K45/06 , A61K2300/00
摘要： A method of identification of quinoline compounds (formula I) that modify melanin synthesis (melanogenesis), and the use of such compounds and compositions thereof to control (e.g., inhibit) melanin production are disclosed. The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of conditions that are causally related to aberrant melanogenesis activity including by way of non-limiting example, pigmentation deficiencies (albinism) and hyperpigmentation and others.
摘要翻译：公开了一种鉴定修饰黑色素合成（黑素生成）的喹啉化合物（式I）的方法，以及这些化合物及其组合物用于控制（例如抑制）黑色素生成的方法。化合物可以制备成药物组合物，并且可以用于预防和治疗与异常黑素生成活性有因果关系的病症，包括作为非限制性实例，色素沉着缺失（白化病）和色素沉着过度等。

8. 发明授权

US09822125B2 Benzopyran compounds as melanogenesis modifiers and uses thereof 有权
公开(公告)号：US09822125B2
公开(公告)日：2017-11-21
申请号：US14457634
申请日：2014-08-12
申请人： Seth J. Orlow
发明人： Seth J. Orlow
IPC分类号： A61K31/335 , C07D493/04 , A61K31/352 , A61K36/60 , A61K45/06 , A61K8/49 , A61Q19/02 , A61K8/97 , A61K31/353 , A61Q5/00 , A61K31/357
CPC分类号： C07D493/04 , A61K8/498 , A61K8/97 , A61K31/352 , A61K31/353 , A61K31/357 , A61K36/60 , A61K45/06 , A61Q5/00 , A61Q19/02
摘要： Provided are benzopyran compounds of formula I, for example, pomiferin-3′,4′-dimethyl ether, and the use of such compounds and compositions thereof to modulate (e.g., inhibit) melanogenesis and pigmentation. wherein R3, R4, R5, R6, R7 and R8 are described herein. Also provided are plant extracts containing a compound of formula I, and the use of such a plant extract to modulate (e.g., inhibit) melanogenesis and pigmentation. The compound or plant extract may be prepared as pharmaceutical and cosmetic compositions, and may be used for the prevention and treatment of conditions that are related to aberrant melanogenesis activity.

9. 发明授权

US08563754B2 Compounds, compositions and methods for preventing skin darkening 失效
标题翻译：用于防止皮肤变黑的化合物，组合物和方法
公开(公告)号：US08563754B2
公开(公告)日：2013-10-22
申请号：US13015882
申请日：2011-01-28
申请人： Seth J. Orlow , Li Ni Komatsu
发明人： Seth J. Orlow , Li Ni Komatsu
IPC分类号： A61K31/37 , C07D309/38
CPC分类号： A61K31/37 , A61K31/35
摘要： A method for preventing hyperpigmented skin, undesired pigmentation disorder of skin, or undesired darkening of skin using coumarin compounds, the use of such compounds, and compositions and formulations thereof are disclosed. In a particular embodiment, the coumarin compounds are selected from robustic acid methyl ether, scandenin, and coumophos. The compounds may be prepared as additives to pharmaceutical and cosmetic compositions, and in personal care products such as antiperspirants. In a particular embodiment extends to an antiperspirant product containing a skin darkening inhibitory amount of a compound of the invention. Also, the present skin darkening compounds may be prepared in combination with each other. The compounds, compositions and formulations of the invention may be used for the prevention of the onset or progression of conditions characterized by unwanted skin darkening, including those that may be causally related to aberrant melanogenesis activity including, by way of non-limiting example, hyperpigmentation and others.
摘要翻译：公开了一种使用香豆素化合物防止皮肤色素沉着过多，皮肤不希望的色素沉着失调或皮肤不希望的变暗的方法，使用这些化合物及其组合物和制剂。在一个具体的实施方案中，香豆素化合物选自鲁西酸甲基醚，斯堪迪汀和香豆磷。化合物可以制备成药物和化妆品组合物的添加剂，以及个人护理产品如止汗剂。在一个具体实施方案中延伸至含有皮肤变暗抑制量的本发明化合物的止汗剂产品。此外，本发明的皮肤变色化合物可以彼此组合制备。本发明的化合物，组合物和制剂可用于预防特征在于不想要的皮肤变暗的病症的发作或进展，包括可能与异常黑素生成活性有因果关系的那些，包括作为非限制性实例的色素沉着过度和别的。

10. 发明申请

US20100040568A1 Steroidal compounds as melanogenesis modifiers and uses thereof 审中-公开
标题翻译：甾体化合物作为黑素生成修饰剂及其用途
公开(公告)号：US20100040568A1
公开(公告)日：2010-02-18
申请号：US12587882
申请日：2009-10-13
申请人： Seth J. Orlow , Li Ni Komatsu
发明人： Seth J. Orlow , Li Ni Komatsu
IPC分类号： A61K31/58 , A61K31/565 , A61P17/00 , A61K8/30
CPC分类号： A61K8/63 , A61K9/0014 , A61K9/0019 , A61K9/06 , A61K9/2063 , A61K9/4858 , A61K31/565 , A61K36/24 , A61K45/06 , A61K47/06 , A61Q19/02 , A61K2300/00
摘要： Provided are steroidal compounds of formula I, for example, conessine, and the use of such compounds and compositions thereof to modulate (e.g., inhibit) melanogenesis and pigmentation. Also provided are plant extracts containing a compound of formula I, for example, conessine, and the use of such a plant extract to modulate (e.g., inhibit) melanogenesis and pigmentation. The compound or plant extract may be prepared as pharmaceutical and cosmetic compositions, and may be used for the prevention and treatment of conditions that are related to aberrant melanogenesis activity.
摘要翻译：提供式I的类固醇化合物，例如conessine，以及这些化合物及其组合物用于调节（例如抑制）黑素生成和色素沉着的用途。还提供了含有式I化合物的植物提取物，例如conessine，以及使用这种植物提取物调节（例如抑制）黑素生成和色素沉着。化合物或植物提取物可以制备为药物和化妆品组合物，并且可以用于预防和治疗与异常黑素生成活性相关的病症。

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