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公开(公告)号：US20170119719A1
公开(公告)日：2017-05-04
申请号：US15351042
申请日：2016-11-14
CPC分类号： A61K31/22 , A61K9/0014 , A61K9/06
摘要： The present invention relates to novel crystalline forms of ingenol ingenol-3-angelate and methods of preparation and use thereof. More specifically, the invention relates to a novel crystalline form and purified forms of the compound of Formula 1 (ingenol-3-mebutate; ingenol-3-angelate; isoform ‘b’; PEP005), which is characterized by, for example, attenuated total reflectance Fourier transform infrared (FTIR-ATR) spectroscopy, single crystal X-Ray crystallography (XRC), X-ray powder diffraction, and, Differential Scanning calorimetry (DSC), and methods of preparation and use thereof.
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公开(公告)号：US20160317486A1
公开(公告)日：2016-11-03
申请号：US15131851
申请日：2016-04-18
IPC分类号： A61K31/22
CPC分类号： A61K31/22 , A61K31/222 , A61K31/235
摘要： The present invention relates generally to methods and compositions for promoting wound healing in a subject. In particular, the invention relates to the use of ingenol compounds, particularly ingenol angelates, in wound healing and compositions thereof which contain such compounds.
摘要翻译： 本发明一般涉及用于促进受试者中伤口愈合的方法和组合物。 特别地，本发明涉及在含有这些化合物的伤口愈合中使用美烯酸酯化合物，特别是当归酸烯雌酚，及其组合物。
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公开(公告)号：US09440906B2
公开(公告)日：2016-09-13
申请号：US14182274
申请日：2014-02-17
IPC分类号： C07C67/52 , C07C69/533 , A61K9/00 , A61K9/06
CPC分类号： C07C67/52 , A61K9/0014 , A61K9/0034 , A61K9/06 , C07B2200/13 , C07C69/533 , C07C2603/86 , Y02A50/463
摘要： The present invention relates to a novel crystalline form of ingenol mebutate, methods of preparation thereof, and to its use. More specifically, the invention relates to the conversion of amorphous ingenol mebutate (ingenol-3-angelate, PEP005) to a crystalline form, which was characterized by single crystal X-Ray crystallography (XRC), attenuated total reflectance Fourier transform infrared (FTIR-ATR) spectroscopy and Differential Scanning calorimetry (DSC).
摘要翻译： 本发明涉及新戊烯酮甲酸酯的结晶形式，其制备方法及其用途。 更具体地说，本发明涉及以单结晶X射线晶体学（XRC），衰减全反射傅里叶变换红外（FTIR-3）为特征的无定形内酯酚酸酯（茚满醇-3-当归，PEP005）转化为结晶形式， ATR）光谱和差示扫描量热法（DSC）。
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公开(公告)号：US20150025265A1
公开(公告)日：2015-01-22
申请号：US14182274
申请日：2014-02-17
IPC分类号： C07C67/52
CPC分类号： C07C67/52 , A61K9/0014 , A61K9/0034 , A61K9/06 , C07B2200/13 , C07C69/533 , C07C2603/86 , Y02A50/463
摘要： The present invention relates to a novel crystalline form of ingenol mebutate, methods of preparation thereof, and to its use. More specifically, the invention relates to the conversion of amorphous ingenol mebutate (ingenol-3-angelate, PEP005) to a crystalline form, which was characterized by single crystal X-Ray crystallography (XRC), attenuated total reflectance Fourier transform infrared (FTIR-ATR) spectroscopy and Differential Scanning calorimetry (DSC).
摘要翻译： 本发明涉及新戊烯酮甲酸酯的结晶形式，其制备方法及其用途。 更具体地说，本发明涉及以单结晶X射线晶体学（XRC），衰减全反射傅立叶变换红外（FTIR-3）为特征的无定形内酯酚酸酯（茚满醇-3-当归，PEP005）转化为结晶形式， ATR）光谱和差示扫描量热法（DSC）。
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5.发明申请METHODS FOR TREATING UV-DAMAGED SKIN AND SCC TUMORS AND FOR REMOVING TATTOOS WITH TOPICAL INGENOL MEBUTATE 审中-公开用于治疗紫外线损伤的皮肤和SCC肿瘤的方法，以及用局部INGENOL MEBUTAT去除TATTOOS的方法公开(公告)号：US20140242012A1
公开(公告)日：2014-08-28
申请号：US14139869
申请日：2013-12-23
CPC分类号： A61K31/22 , A61K8/375 , A61K9/0014 , A61Q19/004 , A61Q19/02
摘要： The present invention is directed to the prophylatic field treatment of photodamaged skin with topical ingenol mebutate. More specifically, the present invention concerns field-directed treatment of UV-damaged skin with topical ingenol mebutate for reducing the number of skin lesions that emerge from the UV-damaged skin over time. In addition, the present invention concerns field-directed treatment for removing photodamaged skin, mutated keratinocytes, cutaneous immunosuppressive environments and/or p53+ patches caused by UV with topical ingenol mebutate. By way of example, the present invention is directed to treating photodamaged skin with topical ingenol mebutate at about 0.05% concentration.The present invention is also concerned with the treatment of SCC tumors with topical ingenol mebutate for reducing the number of SCC tumors. By example, the present invention is directed to treating and curing SCC xenografts with topical ingenol mebutate at about 0.25% concentration.The present invention is further directed to a topical field-directed treatment for the removal of tattoos from skin with ingenol mebutate. By way of example, the present invention is directed to removing tattoos with topical ingenol mebutate at concentrations of up to about 0.25%.
摘要翻译： 本发明涉及用局部西梅替丁配方对光损伤皮肤进行预防性治疗。 更具体地说，本发明涉及用局部用异麦芽酮甲酸酯配制的UV损伤皮肤的现场定向治疗，以减少随时间推移从UV损伤的皮肤中出现的皮肤病变的数量。 此外，本发明涉及用于去除光损伤的皮肤，突变的角质形成细胞，皮肤免疫抑制环境和/或由局部西梅洛尔配方产生的UV引起的p53 +斑块的场定向治疗。 作为实例，本发明涉及以约0.05％浓度处理外用西来诺梅酸甲酯处理光损伤皮肤。 本发明还涉及用局部西梅替丁治疗SCC肿瘤以减少SCC肿瘤的数量。 例如，本发明涉及以约0.25％浓度处理和固化SCC异种移植物，其中外用西ing酚甲酸酯。 本发明进一步涉及用内酯醇甲酸酯从皮肤去除纹身的局部场地定向治疗。 举例来说，本发明旨在以高达约0.25％的浓度去除外用西en酚甲酸酯的纹身。
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