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1. 发明授权

US06913877B1 Methods for detecting bioactive compounds 失效
标题翻译：检测生物活性化合物的方法
公开(公告)号：US06913877B1
公开(公告)日：2005-07-05
申请号：US10024654
申请日：2001-12-17
申请人： Frank W. R. Chaplen , William H. Gerwick , Goran Jovanovic , Wojtek Kolodziej , Jim Liburdy , Phil McFadden , Brian Kevin Paul , Thomas K. Plant , Janine E. Trempy , Corwin Willard
发明人： Frank W. R. Chaplen , William H. Gerwick , Goran Jovanovic , Wojtek Kolodziej , Jim Liburdy , Phil McFadden , Brian Kevin Paul , Thomas K. Plant , Janine E. Trempy , Corwin Willard
IPC分类号： A61K9/14 , A61K35/60 , C12Q1/00 , C12Q1/02 , C12Q1/04 , G01N33/542
CPC分类号： G01N33/542 , C12Q1/04
摘要： Methods of detecting bioactive compounds include exposing compounds to one or more classes of chromatophores and measuring or sensing associated changes in one or more of the chromatophores. Representative methods permit identification and quantification of neurotransmitters, toxins, hormones, and chemical warfare agents with or without prior knowledge of the content of a sample. In some examples, chromatophores based on Betta fish are used. Cytosensor apparatus using such chromatophores include means for exposing chromatophores to a sample and optical detection systems for assessing changes in chromatophore optical properties. Compounds can be identified or quantified based on a red-green-blue or hue saturation-value representations of transmitted or reflected light or based on other characterizations of transmitted or reflected light.
摘要翻译：检测生物活性化合物的方法包括将化合物暴露于一类或多种色素，并测量或检测一种或多种色素中的相关变化。代表性的方法允许在有或没有样品内容的知识的情况下鉴定和定量神经递质，毒素，激素和化学战剂。在一些实例中，使用基于Betta鱼的色素。使用这种色素的细胞传感器装置包括用于将染色体暴露于样品的装置和用于评估染色质光学性质变化的光学检测系统。可以基于透射或反射光的红 - 绿 - 蓝或色相饱和度值表示或基于透射或反射光的其它表征来鉴定或量化化合物。

2. 发明申请

US20140248333A1 COMPOSITIONS AND METHODS FOR INHIBITING PROTEASES 有权
标题翻译：用于抑制蛋白质的组合物和方法
公开(公告)号：US20140248333A1
公开(公告)日：2014-09-04
申请号：US14131681
申请日：2012-07-12
申请人： William H. Gerwick , Alban R. Pereira-Badilla , Tara Byrum , Frederick A. Valeriote , Michael Kenneth Gilson , Andrew Fenley , Bradley S. Moore , Andrew Kale , Hosana M. Debonsi
发明人： William H. Gerwick , Alban R. Pereira-Badilla , Tara Byrum , Frederick A. Valeriote , Michael Kenneth Gilson , Andrew Fenley , Bradley S. Moore , Andrew Kale , Hosana M. Debonsi
IPC分类号： C07K5/083
CPC分类号： C07K5/0808 , A61K31/336 , C07K5/06052
摘要： In particular, in alternative embodiments, the invention provides pharmaceutical compounds and formulations comprising a family of epoxyketone compounds, which include racemic mixtures or racemates, isomers, stereoisomers, diastereoisomers, derivatives and analogs, and methods for making and using them. In alternative embodiments, pharmaceutical compositions and formulations of the invention are administered to an individual in need thereof in an amount sufficient to treat, prevent, reverse and/or ameliorate an infection, disease or condition that can be ameliorated, treated, prevented or reversed by partially or completely inhibiting a chymotrypsin-like protease or a proteasome activity, including e.g., a retroviral infection such as human immunodeficiency virus-1 (HIV-1) infection, an immune disorder, a neurodegenerative disease or condition, or a cancer such as a myeloma or multiple myeloma, an adenocarcinoma such as a lung adenocarcinoma, a pancreatic cancer, a B-cell related cancer, and lymphomas such as non-Hodgkin's lymphoma.
摘要翻译：特别地，在替代实施方案中，本发明提供包含一系列环氧酮化合物的药物化合物和制剂，其包括外消旋混合物或外消旋体，异构体，立体异构体，非对映异构体，衍生物和类似物，以及制备和使用它们的方法。在替代实施方案中，将本发明的药物组合物和制剂以足以治疗，预防，逆转和/或改善可被改善，治疗，预防或逆转的感染，疾病或病症的量施用于有需要的个体部分或完全抑制胰凝乳蛋白酶样蛋白酶或蛋白酶体活性，包括例如逆转录病毒感染如人免疫缺陷病毒-1（HIV-1）感染，免疫疾病，神经变性疾病或病症，或癌症如骨髓瘤或多发性骨髓瘤，腺癌如肺腺癌，胰腺癌，B细胞相关癌症，淋巴瘤如非霍奇金淋巴瘤。

3. 发明授权

US06495588B2 Scytonemin and methods of using thereof 失效
标题翻译： Scytonemin及其使用方法
公开(公告)号：US06495588B2
公开(公告)日：2002-12-17
申请号：US09960314
申请日：2001-09-24
申请人： Robert S. Jacobs , Lisa A. Marshall , William H. Gerwick , Christopher Stevenson
发明人： Robert S. Jacobs , Lisa A. Marshall , William H. Gerwick , Christopher Stevenson
IPC分类号： A61K4338
CPC分类号： A61K31/404 , Y02A50/409 , Y02A50/411 , Y02A50/414 , Y02A50/415 , Y02A50/419 , Y02A50/491
摘要： Disclosed are compounds having a scytoneman skeleton, such as scytonemin, and methods of using thereof. Methods of using a compound having a scytoneman skeleton to inhibit, modulate, attenuate, or prevent cell-cycle progression, cell proliferation, kinase activity, or induce apoptosis are disclosed. Also disclosed are methods of treating, preventing, or inhibiting diseases and disorders associated with cell cycle progression, cell proliferation, kinase activity, tissue hyperplasia or angiogenesis, such as cancer or an inflammatory disease.
摘要翻译：公开了具有scytoneman骨架的化合物，例如scytonemin，及其使用方法。公开了使用具有Scytoneman骨架的化合物抑制，调节，减弱或预防细胞周期进程，细胞增殖，激酶活性或诱导细胞凋亡的方法。还公开了治疗，预防或抑制与细胞周期进程，细胞增殖，激酶活性，组织增生或血管发生如癌症或炎性疾病相关的疾病和病症的方法。

4. 发明授权

US5461070A Anti-flammatory method using indole alkaloids 失效
标题翻译：使用吲哚生物碱的抗炎方法
公开(公告)号：US5461070A
公开(公告)日：1995-10-24
申请号：US297022
申请日：1994-08-29
申请人： William H. Gerwick , Robert S. Jacobs , Richard Castenholz , Ferran Garcia-Pichel , Krista J. S. Grace , Philip J. Proteau , James Rossi
发明人： William H. Gerwick , Robert S. Jacobs , Richard Castenholz , Ferran Garcia-Pichel , Krista J. S. Grace , Philip J. Proteau , James Rossi
IPC分类号： A61K31/404 , A61P29/00 , A61K31/40
CPC分类号： A61K31/404
摘要： Indole alkaloid compounds having the formula ##STR1## where R and R' are H, an alkyl group having up to 5 carbon atoms or --CO--(CH.sub.2).sub.n --CH.sub.3 where n=0 to 16. The indole alkaloid compounds and their reduction products are useful as both UV protective and anti-inflammatory agents.
摘要翻译：吲哚类生物碱化合物，其中R和R'为H，具有至多5个碳原子的烷基或-CO-（CH2）n-CH3，其中n = 0至16.吲哚生物碱化合物及其还原产品可用作紫外线防护剂和抗炎剂。

5. 发明授权

US4810424A Method for the recovery of 12-(S)-hydroxyeicosapentaenoic acid from the red alga murrayella periclados 失效
标题翻译：从红藻mur lad属中回收12-（S） - 羟基二十碳五烯酸的方法
公开(公告)号：US4810424A
公开(公告)日：1989-03-07
申请号：US107616
申请日：1987-10-09
申请人： William H. Gerwick , Matthew W. Bernart
发明人： William H. Gerwick , Matthew W. Bernart
IPC分类号： C11B1/10
CPC分类号： C11B1/10
摘要： 12-(S)-hydroxyeicosapentaenoic acid is chemically extracted from the red alga Murrayella periclados. Fresh or frozen quantities of Murrayella periclados are first macerated and combined with a 2:1 mixture of chloroform and methanol. This results in an organic fraction containing lipid isolates. After filtration to remove extraneous solids, the organic fraction is evaporated to produce a tar. The tar contains 12-(S)-HEPE which is further purified as desired.
摘要翻译：从红藻Murrayella periclados中化学提取12-（S） - 羟基二十碳五烯酸。首先将新鲜或冷冻的Murrayella periclados浸泡并与氯仿和甲醇的2:1混合物混合。这导致含有脂质分离物的有机部分。过滤除去外来固体后，蒸发有机级分以产生焦油。焦油含有12-（S）-HEPE，其根据需要进一步纯化。

6. 发明授权

US6057348A Curacin A analogs exhibiting antiproliferative activity against cells 失效
标题翻译：表现出对细胞抗增殖活性的库拉霉素A类似物
公开(公告)号：US6057348A
公开(公告)日：2000-05-02
申请号：US115582
申请日：1998-07-14
申请人： William H. Gerwick , John R. Falck , Brian L. Marquez
发明人： William H. Gerwick , John R. Falck , Brian L. Marquez
IPC分类号： C07D277/24 , C07D417/06 , A61K31/427
CPC分类号： C07D417/06 , C07D277/24
摘要： Isomers of a cytotoxic compound isolated and purified from a marine cyanobacterium Lyngbya majuscula are disclosed. The compound, termed "curacin D", exhibits substantial biological activity against proliferating cells. Analogs of curacin A also are described, as are formulations that include curacin D and the curacin A analogs. The curacins A-D and analogs of curacin A exhibit antimitotic behavior.
摘要翻译：公开了从海洋蓝杆菌Lyngbya大理石分离和纯化的细胞毒性化合物的异构体。称为“凝乳酶D”的化合物对增殖细胞表现出显着的生物活性。也描述了Curacin A的类似物，还包括包含Curacin D和Curacin A类似物的制剂。曲安素A-D和曲美素A的类似物显示抗有丝分裂的行为。

7. 发明授权

US5508026A Indole alkaloids useful as UV protective and anti-inflammatory agents 失效
标题翻译：吲哚生物碱可用作紫外线防护和抗炎剂
公开(公告)号：US5508026A
公开(公告)日：1996-04-16
申请号：US503448
申请日：1995-07-17
申请人： William H. Gerwick , Richard Castenholz , Ferran Garcia-Pichel , Philip J. Proteau
发明人： William H. Gerwick , Richard Castenholz , Ferran Garcia-Pichel , Philip J. Proteau
IPC分类号： A61K31/404 , A61P29/00 , A61K31/40 , C07D209/94
CPC分类号： A61K31/404
摘要： Indole alkaloid compounds having the formula ##STR1## where R and R' are H, an alkyl group having up to 5 carbon atoms or --CO--(CH.sub.2).sub.n --CH.sub.3 where n=0 to 16. The indole alkaloid compounds and their reduction products are useful as both UV protective and anti-inflammatory agents.
摘要翻译：吲哚类生物碱化合物，其中R和R'为H，具有至多5个碳原子的烷基或-CO-（CH2）n-CH3，其中n = 0至16.吲哚生物碱化合物及其还原产品可用作紫外线防护剂和抗炎剂。

8. 发明授权

US09409944B2 Compositions and methods for inhibiting proteases 有权
标题翻译：抑制蛋白酶的组合物和方法
公开(公告)号：US09409944B2
公开(公告)日：2016-08-09
申请号：US14131681
申请日：2012-07-12
申请人： William H. Gerwick , Alban R. Pereira-Badilla , Tara Byrum , Frederick A. Valeriote , Michael Kenneth Gilson , Andrew T. Fenley , Bradley S. Moore , Andrew Kale , Hosana Debonsi
发明人： William H. Gerwick , Alban R. Pereira-Badilla , Tara Byrum , Frederick A. Valeriote , Michael Kenneth Gilson , Andrew T. Fenley , Bradley S. Moore , Andrew Kale , Hosana Debonsi
IPC分类号： C07K5/083 , A61K31/336 , C07K5/062
CPC分类号： C07K5/0808 , A61K31/336 , C07K5/06052
摘要： In particular, in alternative embodiments, the invention provides pharmaceutical compounds and formulations comprising a family of epoxyketone compounds, which include racemic mixtures or racemates, isomers, stereoisomers, diastereoisomers, derivatives and analogs, and methods for making and using them. In alternative embodiments, pharmaceutical compositions and formulations of the invention are administered to an individual in need thereof in an amount sufficient to treat, prevent, reverse and/or ameliorate an infection, disease or condition that can be ameliorated, treated, prevented or reversed by partially or completely inhibiting a chymotrypsin-like protease or a proteasome activity, including e.g., a retroviral infection such as human immunodeficiency virus-1 (HIV-1) infection, an immune disorder, a neurodegenerative disease or condition, or a cancer such as a myeloma or multiple myeloma, an adenocarcinoma such as a lung adenocarcinoma, a pancreatic cancer, a B-cell related cancer, and lymphomas such as non-Hodgkin's lymphoma.
摘要翻译：特别地，在替代实施方案中，本发明提供包含一系列环氧酮化合物的药物化合物和制剂，其包括外消旋混合物或外消旋体，异构体，立体异构体，非对映异构体，衍生物和类似物，以及制备和使用它们的方法。在替代实施方案中，将本发明的药物组合物和制剂以足以治疗，预防，逆转和/或改善可被改善，治疗，预防或逆转的感染，疾病或病症的量施用于有需要的个体部分或完全抑制胰凝乳蛋白酶样蛋白酶或蛋白酶体活性，包括例如逆转录病毒感染如人免疫缺陷病毒-1（HIV-1）感染，免疫疾病，神经变性疾病或病症，或癌症如骨髓瘤或多发性骨髓瘤，腺癌如肺腺癌，胰腺癌，B细胞相关癌症，淋巴瘤如非霍奇金淋巴瘤。

9. 发明授权

US06495586B2 Scytonemin and methods of using thereof 失效
公开(公告)号：US06495586B2
公开(公告)日：2002-12-17
申请号：US09790640
申请日：2001-02-23
申请人： Robert S. Jacobs , Lisa A. Marshall , William H. Gerwick , Christopher Stevenson
发明人： Robert S. Jacobs , Lisa A. Marshall , William H. Gerwick , Christopher Stevenson
IPC分类号： A61K3140
CPC分类号： A61K31/404
摘要： Disclosed are compounds having a scytoneman skeleton, such as scytonemin, and methods of using thereof. Methods of using a compound having a scytoneman skeleton to inhibit, modulate, attenuate, or prevent cell-cycle progression, cell proliferation, kinase activity, or induce apoptosis are disclosed. Also disclosed are methods of treating, preventing, or inhibiting diseases and disorders associated with cell cycle progression, cell proliferation, kinase activity, tissue hyperplasia or angiogenesis, such as cancer or an inflammatory disease.

10. 发明授权

US4935529A Cytoxic substances from the marine cyanophyte hormothamnion enteromorphoides grunow 失效
标题翻译：来自海洋蓝藻激素的肠毒素物质
公开(公告)号：US4935529A
公开(公告)日：1990-06-19
申请号：US320007
申请日：1989-03-06
申请人： William H. Gerwick
发明人： William H. Gerwick
IPC分类号： C07D311/22 , C12P17/06
CPC分类号： C12R1/89 , C07D311/22 , C12P17/06
摘要： Several new, biologically active substances have been isolated from Hormothamnion enteromorphoides, a somewhat rare cyanophyte from Puerto Rico.Hormothamnion, a lipophilic metabolite from this alga, has the styrylchromone structure: ##STR1## Hormothamnion and, to a lesser extent, one of its homologs, are potent cytotoxins to some types of cancer cells and appear to exert this cytotoxic action by a selective inhibition of RNA synthesis.A peptide compound of about 11 to 12 amino acids has antimicrobial activity, particularly against Candida albicans. The peptide, which includes phenylalanine, serine and other aliphatic amino acids, has blocked carboxyl and amino termini.
摘要翻译：已经从波多黎各的一种有些罕见的蓝藻分离出了几种新的生物活性物质。来自该藻类的亲脂性代谢物ormothamion具有苯乙烯基色酮结构：在较小程度上，其同系物之一是对某些类型的癌细胞的有效细胞毒素，并且似乎通过选择性抑制发挥这种细胞毒性作用的RNA合成。约11至12个氨基酸的肽化合物具有抗微生物活性，特别是针对白色念珠菌。包括苯丙氨酸，丝氨酸和其他脂肪族氨基酸的肽已经封闭羧基和氨基末端。

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