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1. 发明申请

US20050251345A1 Small molecules and a pharmacophore model for inhibition of anthrax lethal factor 失效
标题翻译：小分子和抑制炭疽致死因子的药效团模型
公开(公告)号：US20050251345A1
公开(公告)日：2005-11-10
申请号：US11017771
申请日：2004-12-22
申请人： Sina Bavari , Rekha Panchal , Ann Hermone , Tam Nguyen , Rick Gussio
发明人： Sina Bavari , Rekha Panchal , Ann Hermone , Tam Nguyen , Rick Gussio
IPC分类号： C12Q1/18 , C12Q1/37 , C40B30/02 , G01N33/48 , G01N33/50 , G06F19/00 , G06G7/48 , G06G7/58
CPC分类号： C12Q1/18 , C12Q1/37 , C40B30/02 , G01N2333/32 , G06F19/705
摘要： Disclosed herein is a pharmacophore model for inhibiting anthrax lethal factor protease activity which comprises a first aromatic center A, a second aromatic center B, a first polar center C, a second polar center D, a third polar center E, and a neutral linker F. In some embodiments, the distance between the first aromatic center A and the neutral linker F is about 4.7 to about 6.7 Å, preferably about 5.7 Å. In some embodiments, the distance between the neutral linker F and the second aromatic center B is about 3.4 to about 4.4 Å, preferably about 3.9 Å. In some embodiments, the distance between first aromatic center A and the first polar center C is about 5.5 to about 7.5 Å, preferably about 6.5 Å. In some embodiments, the distance between the first aromatic center A and the second polar center D is about 4.6 to about 6.6 Å, preferably about 5.6 Å. In some embodiments, the distance between the second aromatic center B and the second polar center D is about 3.6 to about 4.6 Å, preferably about 4.1 Å. In some embodiments, the distance between the second aromatic center B and the third polar center E is about 2.6 to about 3.6 Å, preferably about 3.1 Å. In some embodiments, the distance between the first polar center C and the third polar center E is about 15.6 to about 19.6 Å, preferably about 17.6 Å. Also disclosed are small molecules fitting the pharmacophore model and compositions and methods of using thereof.
摘要翻译：本文公开了用于抑制炭疽致死因子蛋白酶活性的药效团模型，其包含第一芳族中心A，第二芳族中心B，第一极中心C，第二极中心D，第三极中心E和中性接头F 在一些实施方案中，第一芳族中心A和中性接头F之间的距离为约4.7至约6.7，优选约为5.7。在一些实施方案中，中性接头F和第二芳族中心B之间的距离为约3.4至约4.4，优选约为3.9。在一些实施方案中，第一芳族中心A和第一极性中心C之间的距离为约5.5至约7.5，优选约为6.5。在一些实施方案中，第一芳族中心A和第二极性中心D之间的距离为约4.6至约6.6，优选约为。在一些实施方案中，第二芳族中心B和第二极性中心D之间的距离为约3.6至约4.6，优选约为4.1。在一些实施方案中，第二芳族中心B和第三极性中心E之间的距离为约2.6至约3.6，优选约为。在一些实施方案中，第一极心C和第三极心E之间的距离为约15.6至约19.6，优选约17.6。还公开了拟合药效团模型及其使用方法的小分子。

2. 发明申请

US20070112048A1 Broad Spectrum Antibacterial Compounds 失效
标题翻译：广谱抗菌化合物
公开(公告)号：US20070112048A1
公开(公告)日：2007-05-17
申请号：US11464001
申请日：2006-08-11
申请人： Sina Bavari , Rekha Panchal , Rick Gussio
发明人： Sina Bavari , Rekha Panchal , Rick Gussio
IPC分类号： A61K31/428 , A61K31/423 , A61K31/4184
CPC分类号： A61K31/4184 , A61K31/423 , A61K31/427 , A61K31/428 , C07D209/10 , C07D209/12 , C07D209/14 , C07D333/56 , C07D333/60 , C07D401/06 , C07D401/12 , C07D403/04 , C07D405/06 , C07D405/14 , C07D407/06 , C07D409/04 , Y02A50/406 , Y02A50/473
摘要： Disclosed herein are methods of inhibiting, reducing or preventing growth of or destroying bacteria of at least one bacterial strain which comprises contacting the bacteria with the compounds disclosed herein. Also disclosed are methods of treating, inhibiting or preventing an infection or intoxication caused by bacteria of at least one bacterial strain in a subject and pharmaceutical and cosmetic compositions comprising the compounds disclosed herein.
摘要翻译：本文公开了抑制，减少或预防至少一种细菌菌株的生长或破坏细菌的方法，其包括使细菌与本文公开的化合物接触。还公开了治疗，抑制或预防受试者中至少一种细菌菌株的细菌引起的感染或中毒的方法，以及包含本文公开的化合物的药物和化妆品组合物。

3. 发明申请

US20120135013A1 CD45 and Methods and Compounds Related Thereto 审中-公开
标题翻译： CD45及其相关方法和化合物
公开(公告)号：US20120135013A1
公开(公告)日：2012-05-31
申请号：US12013648
申请日：2008-01-14
申请人： Rekha Panchal , Sina Bavari
发明人： Rekha Panchal , Sina Bavari
IPC分类号： A61K31/122 , A61P37/04 , A61P31/14 , A61P31/12 , A61P31/04 , A61K31/165 , C12N5/0786
CPC分类号： A61K45/06 , A61K31/13 , A61K31/7088 , C12N15/1138 , C12N2310/11 , C12N2310/3145 , C12N2310/3233 , C12N2310/3513 , A61K2300/00
摘要： Disclosed herein are compounds, compositions and methods for preventing, reducing or inhibiting an amount of protein tyrosine phosphatase receptor type C (CD45) expressed or activity of CD45 in a cell or a subject. Also disclosed are methods for preventing, inhibiting or treating an infection in a cell or a subject immunizing a subject or enhancing a subject's immune response against an infection preventing, reducing or inhibiting the susceptibility of a cell or a subject to an infection or subsequent pathogenesis and morbidity due to the infection and preventing, reducing, and inhibiting apoptosis caused by or resulting from a biological agent in a cell or a subject which comprises preventing, reducing or inhibiting an amount of protein tyrosine phosphatase receptor type C (CD45) expressed or activity of CD45 in the cell or the subject.
摘要翻译：本文公开了用于在细胞或受试者中预防，减少或抑制表达的C蛋白酪氨酸磷酸酶受体C型（CD45）或CD45活性的化合物，组合物和方法。还公开了用于预防，抑制或治疗免疫受试者的细胞或受试者感染的方法，或增强受试者针对预防，减少或抑制细胞或受试者对感染或随后发病的易感性的受试者的免疫应答，以及由于感染和预防，减少和抑制由细胞或受体中的生物制剂引起或由细胞或受试者产生的细胞凋亡的发病率，包括预防，减少或抑制表达的蛋白酪氨酸磷酸酶受体C（CD45）或活性 CD45在细胞或受试者。

4. 发明授权

US5777078A Triggered pore-forming agents 失效
标题翻译：触发成孔剂
公开(公告)号：US5777078A
公开(公告)日：1998-07-07
申请号：US478913
申请日：1995-06-07
申请人： Hagan Bayley , Barbara J. Walker , Chung-yu Chang , Brett Niblack , Rekha Panchal
发明人： Hagan Bayley , Barbara J. Walker , Chung-yu Chang , Brett Niblack , Rekha Panchal
IPC分类号： A61K38/00 , A61K41/00 , A61K47/48 , C07K14/31 , C07K16/18 , C12N15/62 , G01N33/50 , C07K14/195
CPC分类号： A61K47/48184 , A61K41/00 , C07K14/31 , C07K16/18 , C12N15/62 , G01N33/5008 , G01N33/5011 , G01N33/5014 , A61K38/00 , C07K2319/00 , C07K2319/50 , C07K2319/55 , Y10S530/82 , Y10S530/825
摘要： An inactive pore-forming agent which is activated to lytic function by a condition such as pH, light, heat, reducing potential, or metal ion concentration, or substance such as a protease, at the surface of a cell.
摘要翻译：在细胞表面通过pH，光，热，还原电位或金属离子浓度等条件或蛋白酶等物质活化成裂解功能的无活性成孔剂。

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