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1. 发明授权

US07825154B2 Small molecule inhibitors of botulinum neurotoxins 失效
标题翻译：肉毒杆菌神经毒素的小分子抑制剂
公开(公告)号：US07825154B2
公开(公告)日：2010-11-02
申请号：US11464007
申请日：2006-08-11
申请人： Sina Bavari , Rick Gussio , James C. Burnett
发明人： Sina Bavari , Rick Gussio , James C. Burnett
IPC分类号： A61K31/40 , A01N43/38 , A01N43/06 , A01N43/08 , C07D333/02
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 the activity of Botulinum neurotoxin A metalloprotease with the compounds disclosed herein. Also disclosed are methods of treating, inhibiting or preventing 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：本文公开的是使用本文公开的化合物抑制肉毒杆菌神经毒素A金属蛋白酶的活性的方法。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。

2. 发明授权

US07781183B2 Inhibition of anthrax lethal factor protease 失效
标题翻译：炭疽致死因子蛋白酶抑制
公开(公告)号：US07781183B2
公开(公告)日：2010-08-24
申请号：US11017771
申请日：2004-12-22
申请人： Sina Bavari , Rekha G. Panchal , Ann Hermone , Tam Nguyen , Rick Gussio
发明人： Sina Bavari , Rekha G. Panchal , Ann Hermone , Tam Nguyen , Rick Gussio
IPC分类号： C12Q1/37 , C12N9/50 , C07D233/00 , G01N33/53
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. 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 还公开了拟合药效团模型及其使用方法的小分子。

3. 发明授权

US08691859B2 Broad spectrum antibacterial compounds 失效
标题翻译：广谱抗菌化合物
公开(公告)号：US08691859B2
公开(公告)日：2014-04-08
申请号：US11464001
申请日：2006-08-11
申请人： Sina Bavari , Rekha G. Panchal , Rick Gussio
发明人： Sina Bavari , Rekha G. Panchal , Rick Gussio
IPC分类号： A01N43/52 , A61K31/415 , A01N43/76 , A61K31/42 , A01N43/78 , A61K31/425 , A01N43/38 , A61K31/405
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。

4. 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。

5. 发明授权

US07574340B2 Small molecules and a pharmacophore model for inhibition of botulinum toxin and methods of making and using thereof 失效
标题翻译：用于抑制肉毒杆菌毒素的小分子和药效团模型及其制备和使用方法
公开(公告)号：US07574340B2
公开(公告)日：2009-08-11
申请号：US10935622
申请日：2004-09-08
申请人： Sina Bavari , James J. Schmidt , James Burnett , Rick Gussio
发明人： Sina Bavari , James J. Schmidt , James Burnett , Rick Gussio
IPC分类号： G06G7/48
CPC分类号： A61K31/635 , A61K31/47 , A61K31/4706 , A61K45/06 , G06F19/705 , G06F19/706 , A61K2300/00
摘要： Disclosed herein is a pharmacophore model for inhibiting Botulinum neurotoxin A metalloprotease activity which comprises a first plane A, a second plane B, a first hydrophobic moiety C, a second hydrophobic moiety D and a positive ionizable substituent E. The pharmacophore model may further comprise a heteroatom in the first plane A. In some embodiments, the distance between the center of the first plane A and the center of the second plane B is about 6.5 to about 9.5 Å. In some embodiments, the distance between the center of the first hydrophobic moiety C and the center of the second hydrophobic moiety D is about 8.0 to about 16.0 Å. In some embodiments, the distance between the center of the first plane to the center of the first hydrophobic moiety C is about 3.0 to about 5.0 Å. In some embodiments, the distance between the center of the second plane to the center of the second hydrophobic moiety C is about 3.0 to about 5.0 Å. In some embodiments, the distance between the center of the first plane to the center of the positive ionizable substituent is about 6.5 to about 9.5 Å.
摘要翻译：本文公开了用于抑制肉毒杆菌神经毒素A金属蛋白酶活性的药效团模型，其包含第一平面A，第二平面B，第一疏水部分C，第二疏水部分D和可阳离子化取代基E.药效基团模型还可包含在一些实施例中，第一平面A的中心与第二平面B的中心之间的距离为约6.5至约9.5。在一些实施方案中，第一疏水部分C的中心与第二疏水部分D的中心之间的距离为约8.0至约16.0。在一些实施方案中，第一平面的中心与第一疏水部分C的中心之间的距离为约3.0至约5.0。在一些实施方案中，第二平面的中心与第二疏水部分C的中心之间的距离为约3.0至约5.0。在一些实施方案中，第一平面的中心与正电离取代基的中心之间的距离为约6.5至约9.5。

6. 发明申请

US20070112049A1 Small Molecule Inhibitors of Botulinum Neurotoxins 失效
标题翻译：肉毒杆菌神经毒素的小分子抑制剂
公开(公告)号：US20070112049A1
公开(公告)日：2007-05-17
申请号：US11464007
申请日：2006-08-11
申请人： Sina Bavari , Rick Gussio , James Burnett
发明人： Sina Bavari , Rick Gussio , James Burnett
IPC分类号： A61K31/427 , 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 the activity of Botulinum neurotoxin A metalloprotease with the compounds disclosed herein. Also disclosed are methods of treating, inhibiting or preventing 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：本文公开的是使用本文公开的化合物抑制肉毒杆菌神经毒素A金属蛋白酶的活性的方法。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。

7. 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。

8. 发明申请

US20050153945A1 Small molecules and a pharmacophore model for inhibition of botulinum toxin and methods of making and using thereof 失效
标题翻译：用于抑制肉毒杆菌毒素的小分子和药效团模型及其制备和使用方法
公开(公告)号：US20050153945A1
公开(公告)日：2005-07-14
申请号：US10935622
申请日：2004-09-08
申请人： Sina Bavari , James Schmidt , James Burnett , Rick Gussio
发明人： Sina Bavari , James Schmidt , James Burnett , Rick Gussio
IPC分类号： A61K31/4709 , A61K31/473 , A61K31/555 , A61K31/63 , C07K20060101 , G01N33/48 , G01N33/50 , G01N33/53 , G06F19/00
CPC分类号： A61K31/635 , A61K31/47 , A61K31/4706 , A61K45/06 , G06F19/705 , G06F19/706 , A61K2300/00
摘要： Disclosed herein is a pharmacophore model for inhibiting Botulinum neurotoxin A metalloprotease activity which comprises a first plane A, a second plane B, a first hydrophobic moiety C, a second hydrophobic moiety D and a positive ionizable substituent E. The pharmacophore model may further comprise a heteroatom in the first plane A. In some embodiments, the distance between the center of the first plane A and the center of the second plane B is about 6.5 to about 9.5 Å. In some embodiments, the distance between the center of the first hydrophobic moiety C and the center of the second hydrophobic moiety D is about 8.0 to about 16.0 Å. In some embodiments, the distance between the center of the first plane to the center of the first hydrophobic moiety C is about 3.0 to about 5.0 Å. In some embodiments, the distance between the center of the second plane to the center of the second hydrophobic moiety C is about 3.0 to about 5.0 Å. In some embodiments, the distance between the center of the first plane to the center of the positive ionizable substituent is about 6.5 to about 9.5 Å.
摘要翻译：本文公开了用于抑制肉毒杆菌神经毒素A金属蛋白酶活性的药效团模型，其包含第一平面A，第二平面B，第一疏水部分C，第二疏水部分D和可阳离子化取代基E.药效基团模型还可包含在一些实施例中，第一平面A的中心与第二平面B的中心之间的距离为约6.5至约9.5。在一些实施方案中，第一疏水部分C的中心与第二疏水部分D的中心之间的距离为约8.0至约16.0。在一些实施方案中，第一平面的中心与第一疏水部分C的中心之间的距离为约3.0至约5.0。在一些实施方案中，第二平面的中心与第二疏水部分C的中心之间的距离为约3.0至约5.0。在一些实施方案中，第一平面的中心与正电离取代基的中心之间的距离为约6.5至约9.5。

9. 发明申请

US20090012107A1 Antiviral Compounds and Methods of Using Thereof 有权
标题翻译：抗病毒化合物及其使用方法
公开(公告)号：US20090012107A1
公开(公告)日：2009-01-08
申请号：US12013640
申请日：2008-01-14
申请人： Mohammad Javad Aman , Sina Bavari , James C. Burnett , Kelly Lyn Warfield
发明人： Mohammad Javad Aman , Sina Bavari , James C. Burnett , Kelly Lyn Warfield
IPC分类号： A61K31/506 , C12N5/00 , A61K31/381 , A61K31/343 , A61K31/4184 , A61K31/416 , A61P31/12 , A61K31/122 , A61K31/404 , A61K31/42 , A61K31/4178 , A61K31/4745
CPC分类号： A61K31/505 , A61K31/12 , A61K31/16 , A61K31/343 , A61K31/381 , A61K31/404 , A61K31/4178 , A61K31/4184 , A61K31/421 , A61K31/4745 , A61K31/506
摘要： Disclosed herein are compounds which exhibit antiviral activity against a plurality of viruses belonging to different families such as Bornaviridae, Filoviridae, Paramyxoviridae, Rhabdoviridae, Arenaviridae, Bunyaviridae, Orthomyxoviridae, and Poxviridae. Thus, methods of preventing, inhibiting, or reducing the viral activity of various viruses are provided as well as methods of treating viral infections.
摘要翻译：本文公开了对属于不同家族的多种病毒如博拉维病毒，非螺病毒属，副粘病毒科，弹状病毒科，沙病毒科，布尼亚病毒科，正粘病毒科和痘病毒科的抗病毒活性的化合物。因此，提供了预防，抑制或降低各种病毒的病毒活性的方法以及治疗病毒感染的方法。

10. 发明申请

US20120035198A1 Antiviral Compounds and Methods of Using Thereof 审中-公开
标题翻译：抗病毒化合物及其使用方法
公开(公告)号：US20120035198A1
公开(公告)日：2012-02-09
申请号：US13179267
申请日：2011-07-08
申请人： Mohammad Javad Aman , Sina Bavari , James C. Burnett , Kelly Lyn Warfield
发明人： Mohammad Javad Aman , Sina Bavari , James C. Burnett , Kelly Lyn Warfield
IPC分类号： A61K31/506 , A61K31/4184 , A61K31/343 , A61K31/165 , A61K31/381 , A61P31/16 , A61K31/421 , A61K31/4178 , A61K31/4375 , A61P31/12 , A61P31/14 , A61P31/20 , C12N7/06 , A61K31/404
CPC分类号： A61K31/505 , A61K31/12 , A61K31/16 , A61K31/343 , A61K31/381 , A61K31/404 , A61K31/4178 , A61K31/4184 , A61K31/421 , A61K31/4745 , A61K31/506
摘要： Disclosed herein are compounds which exhibit antiviral activity against a plurality of viruses belonging to different families such as Bornaviridae, Filoviridae, Paramyxoviridae, Rhabdoviridae, Arenaviridae, Bunyaviridae, Orthomyxoviridae, and Poxviridae. Thus, methods of preventing, inhibiting, or reducing the viral activity of various viruses are provided as well as methods of treating viral infections.
摘要翻译：本文公开了对属于不同家族的多种病毒如博拉维病毒，非螺病毒属，副粘病毒科，弹状病毒科，沙病毒科，布尼亚病毒科，正粘病毒科和痘病毒科的抗病毒活性的化合物。因此，提供了预防，抑制或降低各种病毒的病毒活性的方法以及治疗病毒感染的方法。

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