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公开(公告)号：US20120202706A1
公开(公告)日：2012-08-09
申请号：US13306772
申请日：2011-11-29
CPC分类号： C08B37/0063 , C08B37/0075 , C12N9/13 , C12N2510/02 , C12P19/26
摘要： Disclosed are methods of 6-O sulfating glucosaminyl N-acetylglucosamine residues (GlcNAc) in a polysaccharide preparation and methods of converting anticoagulant-inactive heparan sulfate to anticoagulant-active heparan sulfate and substantially pure polysaccharide preparations made by such methods. Also disclosed is a mutant CHO cell which hyper-produces anticoagulant-active heparan sulfate. Methods for elucidating the sequence of activity of enzymes in a biosynthetic pathway are provided.
摘要翻译： 公开了多糖制剂中6-O硫酸化葡糖胺酰基N-乙酰葡糖胺残基（GlcNAc）的方法和将抗凝血剂无活性硫酸乙酰肝素转化为抗凝血活性硫酸乙酰肝素的方法和通过这些方法制备的基本上纯的多糖制剂。 还公开了超生产抗凝血活性硫酸肝素的突变型CHO细胞。 提供了阐明生物合成途径中酶活性顺序的方法。
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公开(公告)号：US08067196B2
公开(公告)日：2011-11-29
申请号：US10473180
申请日：2002-03-28
CPC分类号： C08B37/0063 , C08B37/0075 , C12N9/13 , C12N2510/02 , C12P19/26
摘要： Disclosed are methods of 6-O-sulfating glucosaminyl N-acetylglucosamine residues (GlcNAc) in a polysaccharide preparation and methods of converting anticoagulant-inactive heparan sulfate to anticoagulant-active heparan sulfate and substantially pure polysaccharide preparations may by such methods. Also disclosed is a mutant CHO cell which hyper-produces anticoagulant-active heparan sulfate. Methods for elucidating the sequence of activity of enzymes in a biosynthetic pathway are provided.
摘要翻译： 公开了多糖制剂中6-O-硫酸化葡糖胺酰基N-乙酰葡糖胺残基（GlcNAc）的方法和将抗凝血剂无活性硫酸乙酰肝素转化为抗凝血活性硫酸乙酰肝素和基本上纯的多糖制剂的方法。 还公开了超生产抗凝血活性硫酸肝素的突变型CHO细胞。 提供了阐明生物合成途径中酶活性顺序的方法。
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3.发明授权公开(公告)号：US06861254B1
公开(公告)日：2005-03-01
申请号：US09557262
申请日：2000-04-24
申请人： Robert D. Rosenberg , Nicholas W. Shworak , Jian Liu , Linda M. S. Fritze , John J. Schwartz , Lijuan Zhang
发明人： Robert D. Rosenberg , Nicholas W. Shworak , Jian Liu , Linda M. S. Fritze , John J. Schwartz , Lijuan Zhang
CPC分类号： C12N9/13 , C07K2319/20
摘要： Disclosed are novel isolated nucleic acids and substantially pure protein preparations for naturally occurring and synthetic or chimeric heparan sulfate D-glicosaminyl 3-O-sulfo-transferases (3-OSTs). Also disclosed are uses for these genes and proteins, including uses for the modification and sequencing of glycosaminoglycans.
摘要翻译： 公开了用于天然存在和合成或嵌合的硫酸乙酰肝素D-葡糖胺基3-O-磺基转移酶（3-OST）的新型分离的核酸和基本上纯的蛋白质制剂。 还公开了这些基因和蛋白质的用途，包括用于糖胺聚糖修饰和测序的用途。
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4.发明授权公开(公告)号：US08575115B2
公开(公告)日：2013-11-05
申请号：US12097321
申请日：2006-08-28
申请人： Hui Kang , Jinhua Zhao , Guanghui Yao , Weizhen Zeng , Milai Yin , Yong Li , Cunfang Wang , Lijuan Zhang , Dan Zhu , Hong Chen , Chuangui Huang , Yu Man , Jing Li , Hanlin Feng , Lin Yu
发明人： Hui Kang , Jinhua Zhao , Guanghui Yao , Weizhen Zeng , Milai Yin , Yong Li , Cunfang Wang , Lijuan Zhang , Dan Zhu , Hong Chen , Chuangui Huang , Yu Man , Jing Li , Hanlin Feng , Lin Yu
CPC分类号： C07H15/20
摘要： The present invention relates to a novel crystalline form of a Compound 3,4′,5-trihydroxy-stilbene-3-β-D-glucoside (polydatin) and a method of preparation and use thereof, and to a pharmaceutical composition containing crystalline form I of 3,4′,5-trihydroxy-stilbene-3-β-D-glucoside. Crystalline form I of 3,4′,5-trihydroxy-stilbene-3-β-D-glucoside of the present invention has a stable crystalline morphology, a definite melting point and a good chemical stability. Such a novel form of 3,4′,5-trihydroxy-stilbene-3-β-D-glucoside possesses the properties required for the preparation of solid formulations and is easily tabletable and readily formable when formulated, which allows for substantial decrease in raw materials costs, more facile operations in production and easier control over quality in industrial drug production, and moreover, better convenience in storage.
摘要翻译： 本发明涉及化合物3,4'，5-三羟基 - 二苯乙烯-3-β-D-葡萄糖苷（多聚糖）的新结晶形式及其制备和应用的方法，以及含有结晶形式的药物组合物 I的3,4'，5-三羟基 - 二苯乙烯-3-β-D-葡萄糖苷。 本发明的3,4'，5-三羟基 - 二苯乙烯-3-β-D-葡萄糖苷的结晶形式I具有稳定的结晶形态，确定的熔点和良好的化学稳定性。 这种3,4'，5-三羟基 - 二苯乙烯-3-β-D-葡萄糖苷的新形式具有制备固体制剂所需的性质，并且在配制时易于制成并易于成型，这允许原料 材料成本较高，生产操作更加容易，工业药品生产质量更易于控制，而且储存更方便。
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5.发明申请N-ACYL AMINO ACID DERIVATIVES FOR TREATING SKIN CONDITIONS SUCH AS CELLULITE 有权用于治疗皮肤病症的N-亚氨基氨基酸衍生物如细胞公开(公告)号：US20130096143A1
公开(公告)日：2013-04-18
申请号：US13703292
申请日：2011-06-28
申请人： Timothy J. Falla , Lijuan Zhang
发明人： Timothy J. Falla , Lijuan Zhang
IPC分类号： A61K31/198 , A61K45/06 , A61Q19/06 , C07C237/12 , A61K8/44
CPC分类号： A61K31/198 , A61K8/42 , A61K8/44 , A61K31/20 , A61K45/06 , A61Q19/06 , C07C237/12
摘要： The invention relates to small molecules having biological and therapeutic activity. Particularly, the invention relates to small molecules having lipolytic and anti-adipogenic activity. Two examples of such molecules are 4-methyl-2-(octanoylamino) pentanoic acid and N-isopentyloctanamide. The invention further relates to methods of preventing or treating skin conditions such as cellulite using small molecules having lipolytic and anti-adipogenic activity.
摘要翻译： 本发明涉及具有生物和治疗活性的小分子。 特别地，本发明涉及具有脂肪分解和抗脂肪生成活性的小分子。 这些分子的两个实例是4-甲基-2-（辛酰氨基）戊酸和N-异戊基辛酰胺。 本发明还涉及使用具有脂肪分解和抗脂肪生成活性的小分子预防或治疗皮肤病症如脂肪团的方法。
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6.发明授权公开(公告)号：US08110658B2
公开(公告)日：2012-02-07
申请号：US11811876
申请日：2007-06-12
申请人： Scott M. Harris , Timothy J. Falla , Lijuan Zhang
发明人： Scott M. Harris , Timothy J. Falla , Lijuan Zhang
IPC分类号： C07K5/10
CPC分类号： A61K38/07 , A61K8/64 , A61K9/0014 , A61K9/06 , A61K38/00 , A61K2121/00 , A61K2300/00 , A61Q19/00 , A61Q19/08 , C07K5/1002 , C07K5/1008 , C07K5/1024 , C07K14/78
摘要： Short biologically active tetrapeptides are disclosed that are comprised of the sequences GxxG and PxxP where G (glycine) and P (proline) are maintained and x is a variable amino acid. The peptides can be used singly or in combination to stimulate production of extracellular matrix proteins in skin. A rapid, low-cost method of producing heterogenous formulations of tetrapeptides is disclosed.
摘要翻译： 公开了由保持G（甘氨酸）和P（脯氨酸）并且x是可变氨基酸的序列GxxG和PxxP组成的短生物活性四肽。 肽可单独使用或组合使用以刺激皮肤中细胞外基质蛋白的产生。 公开了生产四肽的异源制剂的快速，低成本的方法。
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公开(公告)号：US08071555B2
公开(公告)日：2011-12-06
申请号：US12290236
申请日：2008-10-28
申请人： Lijuan Zhang , Scott M. Harris , Timothy J. Falla
发明人： Lijuan Zhang , Scott M. Harris , Timothy J. Falla
CPC分类号： C07K5/1024 , A61K8/64 , A61K38/00 , A61K2800/782 , A61Q19/08
摘要： The disclosed invention provides tetrapeptides with the amino acid sequence proline-glutamine-glutamate-X (P-Q-E-X), where X can be either lysine (K) or isoleucine (I). These tetrapeptides inhibit ultraviolet light (UV)-induced expression of the pro-inflammatory cytokine interleukin-6 (IL-6) by skin epithelial cells and fibroblasts. Furthermore, the tetrapeptides repress the upregulation of matrix metalloproteinase-1 (MMP-1) by skin fibroblasts induced by either direct exposure to UV rays or treatment with media conditioned by UV-treated keratinocytes. The small size and bio-activity of the tetrapeptides render them suitable for use in therapies directed to inflammatory skin disorders and as active ingredients in skin care products.
摘要翻译： 所公开的发明提供四肽与氨基酸序列脯氨酸 - 谷氨酰胺 - 谷氨酸酯-X（P-Q-E-X），其中X可以是赖氨酸（K）或异亮氨酸（I）。 这些四肽通过皮肤上皮细胞和成纤维细胞抑制紫外线（UV）诱导的促炎细胞因子白细胞介素-6（IL-6）的表达。 此外，四肽通过直接暴露于紫外线诱导的皮肤成纤维细胞抑制基质金属蛋白酶-1（MMP-1）的上调或通过经紫外线处理的角质形成细胞调节的培养基来治疗。 四肽的小尺寸和生物活性使其适合用于治疗炎症性皮肤病症和作为皮肤护理产品中的活性成分。
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公开(公告)号：US20090142280A1
公开(公告)日：2009-06-04
申请号：US12290236
申请日：2008-10-28
申请人： Lijuan Zhang , Scott Harris , Timothy J. Falla
发明人： Lijuan Zhang , Scott Harris , Timothy J. Falla
CPC分类号： C07K5/1024 , A61K8/64 , A61K38/00 , A61K2800/782 , A61Q19/08
摘要： The disclosed invention provides tetrapeptides with the amino acid sequence proline-glutamine-glutamate-X (P-Q-E-X), where X can be either lysine (K) or isoleucine (I). These tetrapeptides inhibit ultraviolet light (UV)-induced expression of the pro-inflammatory cytokine interleukin-6 (IL-6) by skin epithelial cells and fibroblasts. Furthermore, the tetrapeptides repress the upregulation of matrix metalloproteinase-1 (MMP-1) by skin fibroblasts induced by either direct exposure to UV rays or treatment with media conditioned by UV-treated keratinocytes. The small size and bio-activity of the tetrapeptides render them suitable for use in therapies directed to inflammatory skin disorders and as active ingredients in skin care products.
摘要翻译： 所公开的发明提供四肽与氨基酸序列脯氨酸 - 谷氨酰胺 - 谷氨酸酯-X（P-Q-E-X），其中X可以是赖氨酸（K）或异亮氨酸（I）。 这些四肽通过皮肤上皮细胞和成纤维细胞抑制紫外线（UV）诱导的促炎细胞因子白细胞介素-6（IL-6）的表达。 此外，四肽通过直接暴露于紫外线诱导的皮肤成纤维细胞抑制基质金属蛋白酶-1（MMP-1）的上调或通过经紫外线处理的角质形成细胞调节的培养基来治疗。 四肽的小尺寸和生物活性使其适合用于治疗炎症性皮肤病症和作为皮肤护理产品中的活性成分。
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9.发明申请公开(公告)号：US20080293643A1
公开(公告)日：2008-11-27
申请号：US12097321
申请日：2006-08-28
申请人： Hui Kang , Jinhua Zhao , Guanghui Yao , Weizhen Zeng , Milai Yin , Yong Li , Cunfang Wang , Lijuan Zhang , Dan Zhu , Hong Chen , Chuangui Huang , Yu Man , Jing Li , Hanlin Feng , Lin Yu
发明人： Hui Kang , Jinhua Zhao , Guanghui Yao , Weizhen Zeng , Milai Yin , Yong Li , Cunfang Wang , Lijuan Zhang , Dan Zhu , Hong Chen , Chuangui Huang , Yu Man , Jing Li , Hanlin Feng , Lin Yu
IPC分类号： A61K31/7048 , C07G3/00 , A61P43/00
CPC分类号： C07H15/20
摘要： The present invention relates to a novel crystalline form of a Compound 3,4′,5-trihydroxy-stilbene-3-β-D-glucoside (polydatin) and a method of preparation and use thereof, and to a pharmaceutical composition containing crystalline form I of 3,4′,5-trihydroxy-stilbene-3-β-D-glucoside. Crystalline form I of 3,4′,5-trihydroxy-stilbene-3-β-D-glucoside of the present invention has a stable crystalline morphology, a definite melting point and a good chemical stability. Such a novel form of 3,4′,5-trihydroxy-stilbene-3-β-D-glucoside possesses the properties required for the preparation of solid formulations and is easily tabletable and readily formable when formulated, which allows for substantial decrease in raw materials costs, more facile operations in production and easier control over quality in industrial drug production, and moreover, better convenience in storage.
摘要翻译： 本发明涉及化合物3,4'，5-三羟基 - 二苯乙烯-3-β-D-葡萄糖苷（多聚糖）的新结晶形式及其制备和应用的方法，以及含有结晶形式的药物组合物 I的3,4'，5-三羟基 - 二苯乙烯-3-β-D-葡萄糖苷。 本发明的3,4'，5-三羟基 - 二苯乙烯-3-β-D-葡萄糖苷的结晶形式I具有稳定的晶体形态，确定的熔点和良好的化学稳定性。 这种新型形式的3,4'，5-三羟基 - 二苯乙烯-3-β-D-葡萄糖苷具有制备固体制剂所需的性质，并且在配制时易于制成并容易形成，这允许原料 材料成本较高，生产操作更加容易，工业药品生产质量更易于控制，而且储存更方便。
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公开(公告)号：US07407940B2
公开(公告)日：2008-08-05
申请号：US11350192
申请日：2006-02-08
申请人： Timothy J. Falla , Lijuan Zhang , Scott M. Harris
发明人： Timothy J. Falla , Lijuan Zhang , Scott M. Harris
CPC分类号： C07K7/06 , A61K38/00 , Y02A50/473
摘要： The invention encompasses hexapeptides consisting of alternating hydrophobic residues (B) at positions 2, 4, and 6, hydrophilic, charged residues (X) at positions 1 and 3, and a naphthylalanine (Nal), an aliphatic or aromatic residue (O) at position five, represented generally by the formula XBXBOB, which exhibit antimicrobial activity against infections caused by a variety of pathogens. These pathogens may include gram positive or negative bacteria, acid-fast bacteria such as mycobacteria, parasites, dermatophytes, or fungal pathogens. Typical fungal pathogens include Candida albicans and typical dermatophytes include Trichophyton rubrum and Trichophyton mentagrophytes. The hexapeptides of the present invention exhibit antifungal activity, antibacterial activity, desirable stability, and lack toxicity to the mammal receiving treatment.
摘要翻译： 本发明包括由位置2,4和6处的交替的疏水性残基（B），位置1和3的亲水性带电残基（X）和萘丙氨酸（Nal），脂族或芳族残基（O））组成的六肽 位置5，通常由式XBXBOB表示，其表现出针对由各种病原体引起的感染的抗微生物活性。 这些病原体可以包括革兰氏阳性或阴性细菌，耐酸细菌如分枝杆菌，寄生虫，皮肤真菌或真菌病原体。 典型的真菌病原体包括白色念珠菌和典型的皮肤癣菌包括红色毛癣菌和引发毛癣菌。 本发明的六肽对接受治疗的哺乳动物具有抗真菌活性，抗菌活性，理想的稳定性和缺乏毒性。
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