专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

1. 发明申请

US20060100179A1 Compositions and methods for use in targeting vascular destruction 审中-公开
公开(公告)号：US20060100179A1
公开(公告)日：2006-05-11
申请号：US11112055
申请日：2005-04-22
申请人： Ronald Pero , David Sherris , David Chaplin , George Pettit , John Lippert
发明人： Ronald Pero , David Sherris , David Chaplin , George Pettit , John Lippert
IPC分类号： A61K31/66 , A01N31/14
CPC分类号： A61K31/66
摘要： Treatment of warm-blooded animals having a tumor or non-malignant hypervascularation, by administering a sufficient amount of a cytotoxic agent formulated into a phosphate prodrug form having substrate specificity for microvessel phosphatases, so that microvessels are destroyed preferentially over other normal tissues, because the less cytotoxic prodrug form is converted to the highly cytotoxic dephosphorylated form.

2. 发明申请

US20050014849A1 Antifungal phenylethylene 审中-公开
标题翻译：抗真菌苯乙烯
公开(公告)号：US20050014849A1
公开(公告)日：2005-01-20
申请号：US10499958
申请日：2002-12-20
申请人： George Pettit , Robin Pettit
发明人： George Pettit , Robin Pettit
IPC分类号： A61K31/09 , C07C205/32 , A61K31/075
CPC分类号： A61K31/09 , C07C205/32
摘要： The antifungal and cancer cell growth inhibitory activities of 1-(3′,4′,5′-trimethoxyphenyl)-2-nitro-ethylene (TMPN) were examined. TMPN was fungicidal for the majority of 132 reference strains and clinical isolates tested, including those resistant to fluconazole, ketoconazole, amphotericin B or flucytosine. Minimum fungicidal concentration/minimum inhibitory concentration (MFC/MIC) ratios were ≦2 for 96% of Cryptococcus neoformans clinical isolates and 71% of Candida albicans clinical isolates. TMPN was fungicidal for a variety of other basidiomycetes, endomycetes and hyphomycetes, and its activity was unaffected by alterations in media pH. TMPN was slightly cytotoxic for murine and human cancer cell lines (GI50=1-4 μg/ml), and weakly inhibited mammalian tubulin polymerization (IC50=0.60 μg/ml). TMPN may also be used as a biochemical probe for tubulin and fungal dimorphism studies.
摘要翻译：检查1-（3'，4'，5'-三甲氧基苯基）-2-硝基 - 乙烯（TMPN）的抗真菌和癌细胞生长抑制活性。 TMPN对132个参考菌株和临床分离株进行了杀真菌处理，其中包括对氟康唑，酮康唑，两性霉素B或氟胞嘧啶耐药的参考菌株。对于96％的新型隐球菌临床分离株和71％的白念珠菌临床分离株，最低的杀真菌浓度/最小抑制浓度（MFC / MIC）比值<2。对于各种其他担子菌，内生菌和菌丝体，TMPN是杀真菌剂，其活性不受培养基pH变化的影响。 TMPN对鼠和人类癌细胞系（GI50 = 1-4mug / ml）略有细胞毒性，并且弱抑制哺乳动物微管蛋白聚合（IC50 = 0.60mug / ml）。 TMPN也可用作微管蛋白和真菌二态性研究的生物化学探针。

3. 发明申请

US20080119649A1 HALOCOMBSTATINS AND METHODS OF SYNTHESIS THEREOF 有权
标题翻译： HOCOCOMBSTATINS及其合成方法
公开(公告)号：US20080119649A1
公开(公告)日：2008-05-22
申请号：US12021246
申请日：2008-01-28
申请人： George Pettit , Mathew Minardi , Heidi Rosenberg
发明人： George Pettit , Mathew Minardi , Heidi Rosenberg
IPC分类号： C07D295/00 , C07D211/02 , C07F9/141
CPC分类号： C07C43/23 , C07F9/12
摘要： The invention relates to novel compounds denominated halocombstatins. The halocombstatins are derivatives of combretastatin A-3, and include compounds that exhibit cancer growth cell inhibition against a panel of human cancer cell lines and the murine P388 leukemia, as well as activity as inhibitors of tubulin polymerization and inhibitors of the binding of colchicine to tubulin.
摘要翻译：本发明涉及命名为卤代抑菌素的新化合物。卤代抑菌素是考布他汀A-3的衍生物，并且包括对人类癌细胞系和小鼠P388白血病显示出癌细胞生长细胞抑制作用的化合物，以及作为微管蛋白聚合抑制剂的活性以及秋水仙碱与微管蛋白

4. 发明申请

US20070135516A1 Irciniastatins a and b 失效
标题翻译：阿奇尼他他汀a和b
公开(公告)号：US20070135516A1
公开(公告)日：2007-06-14
申请号：US10580572
申请日：2004-11-17
申请人： George Pettit , Jun-Ping Xu
发明人： George Pettit , Jun-Ping Xu
IPC分类号： A61K31/366 , C07D405/02
CPC分类号： C07D407/06 , C07D405/06
摘要： The Indo-Pacific marine sponge Ircinia ramosa has been found to contain two powerful (GI50 0.001 to
摘要翻译：已经发现印度洋太平洋海绵茜草（Ircinia ramosa）含有两种功能强大的（GI50 0.001至<0.0001杯/毫升）鼠和人类癌细胞生长抑制剂，本文命名为irciniastatin A和irciniastatin B.两者均分离（10-3至 10-4％的产量）通过癌细胞系生物测定指导技术，并命名为irciniastatins A（1）和B（2）。通过光谱分析，主要是高分辨率质谱和2D-NMR（主要是APT，HMQC，HMBC和ROESY）的组合的结构阐明显示异常结构1和2。

5. 发明申请

US20070027439A1 Laser corneal flap cutting system and associated methods 有权
标题翻译：激光角膜切片系统及相关方法
公开(公告)号：US20070027439A1
公开(公告)日：2007-02-01
申请号：US11491636
申请日：2006-07-24
申请人： Daniel Durrie , George Pettit , John Campin
发明人： Daniel Durrie , George Pettit , John Campin
IPC分类号： A61F9/008 , A61B18/18
CPC分类号： A61F9/00802 , A61F9/008 , A61F9/00806 , A61F9/00836 , A61F2009/00846 , A61F2009/00872 , A61F2009/0088
摘要： A method for performing wavefront-guided laser surgery on a cornea includes the step of calculating a corneal flap configuration based upon collected anatomical information on an eye and wavefront data on a cornea of the eye. Such data may be collected by, for example, an aberrometer, although this is not intended as a limitation. The calculated configuration is transmitted to a processor in controlling relation to a corneal flap-cutting device. The flap-cutting device is used to create a corneal flap based upon the calculated configuration. A system for performing wavefront-guided laser surgery on a cornea includes a processor for receiving the anatomical information and wavefront data. A software package is adapted to calculate the corneal flap configuration and to control a corneal flap-cutting device to cut a corneal flap commensurate with the calculated corneal flap configuration.
摘要翻译：用于在角膜上进行波前引导激光手术的方法包括基于眼睛上收集的解剖信息和眼睛角膜上的波前数据计算角膜瓣构造的步骤。这样的数据可以通过例如像差计来收集，尽管这不是作为限制。所计算的配置在控制与角膜瓣切割装置的关系中被传送到处理器。根据计算出的结构，使用襟翼切割装置创建角膜瓣。用于在角膜上进行波前引导激光手术的系统包括用于接收解剖信息和波前数据的处理器。软件包适用于计算角膜瓣构造并控制角膜瓣切割装置以切割与计算出的角膜瓣构造相称的角膜。

6. 发明申请

US20060173032A1 Isolation and structure of cribrostatin 6 有权
标题翻译： cribrostatin的分离和结构6
公开(公告)号：US20060173032A1
公开(公告)日：2006-08-03
申请号：US10546468
申请日：2004-02-19
申请人： George Pettit , John Knight
发明人： George Pettit , John Knight
IPC分类号： C07D471/04 , A61K31/4745
CPC分类号： C07D471/04
摘要： Cribrostatin 6, a dark blue cancer cell growth inhibiting constituent of the Republic of Maldives marine sponge Cribrochalina sp. has been isolated, and its structure (shown below) elucidated, based on a combination of RMS, high field (500 MHz, HMBC, and GOESY experiments) 15N, 1H- and 13C NMR, and X-ray crystal structure analyses. Cribrostatin 6 also was found to inhibit the growth of a number of pathogenic bacteria and fungi.
摘要翻译： Cribrostatin 6，一种深蓝色的癌细胞生长抑制成分的马尔代夫海洋海绵Cribrochalina sp。已经被隔离，并且基于RMS，高场（500MHz，HMBC和GOESY实验）15N，1 H和13 C NMR的组合以及X 晶体结构分析。发现克雷司他汀6也抑制了许多病原菌和真菌的生长。

7. 发明授权

US06679606B2 Method for determining accommodation 有权
标题翻译：确定住宿的方法
公开(公告)号：US06679606B2
公开(公告)日：2004-01-20
申请号：US10338234
申请日：2003-01-08
申请人： John A. Campin , Gary P. Gray , George Pettit
发明人： John A. Campin , Gary P. Gray , George Pettit
IPC分类号： A61B310
CPC分类号： A61B3/1015 , A61B3/09
摘要： An automated, objective method for determining the accommodative range and aberration profile of an eye using a wavefront sensor that iteratively determines the change in accommodation of the lens of an eye.
摘要翻译：一种用于使用波前传感器确定眼睛的调节范围和像差轮廓的自动客观方法，所述波前传感器迭代地确定眼睛的镜片的适应性的变化。

8. 发明申请

US20050240062A1 Structural modification of resveratrol: Sodium resverastatin phosphate 失效
标题翻译：白藜芦醇的结构修饰：磷酸白藜芦醇钠
公开(公告)号：US20050240062A1
公开(公告)日：2005-10-27
申请号：US10510675
申请日：2003-04-10
申请人： George Pettit , Matthew Grealish
发明人： George Pettit , Matthew Grealish
IPC分类号： A61K31/66 , C07C41/26 , C07C43/20 , C07C43/215 , C07C43/23 , C07F9/12
CPC分类号： C07C43/23 , A61K31/66 , C07C41/26 , C07C41/30 , C07F9/12 , C07C43/215
摘要： Described herein are novel compounds having antineoplastic and antimicrobial activity, obtained via structural modifications of resveratrol and combretastatin A-4, methods for synthesis of these compounds, and their use in pharmaceutical composition and for use in the treatment of mammals having cancer. Examples of the novel compounds are: (Z)- and (E)-3,4′,5-trimethioxystilbene (4a, 4b); (Z)- and (E)-3,5-dimethoxy-4′-hydroxystilbene (14c, 14d); (Z)-and (E)-3-hydroxy-4′,5-dimethoxystilbene (14g, 14h);(Z)-and (E)-3,5-dihydroxy-4′-methoxy-stilbene (14k, 14l); sodium resverastatin dibenzyl phosphate ((Z)-3,5-dimethoxy-4-[O-bis(benzyl)phosphoryl]-stilbene) (14m); and sodium resverastatin phosphate (14n).
摘要翻译：本文描述了通过白藜芦醇和考布他汀A-4的结构修饰获得的具有抗肿瘤和抗微生物活性的新化合物，它们用于合成这些化合物的方法，以及它们在药物组合物中的用途以及用于治疗具有癌症的哺乳动物。新化合物的实例是：（Z） - 和（E）-3,4'，5-三甲基二氧噻吩（4a，4b）; （Z） - 和（E）-3,5-二甲氧基-4'-羟基茋（14c，14d）; （Z） - 和（E）-3-羟基-4'，5-二甲氧基茋（14g，14h）;（Z） - 和（E）-3,5-二羟基-4'-甲氧基 - 二苯乙烯（14k，14l ）; （（Z）-3,5-二甲氧基-4- [O-双（苄基）磷酰基] - 二苯乙烯钠（14m）; 和雷铂霉素磷酸钠（14n）。

9. 发明申请

US20050176688A1 Halocombstatins and methods of synthesis thereof 有权
标题翻译：卤虫抑制剂及其合成方法
公开(公告)号：US20050176688A1
公开(公告)日：2005-08-11
申请号：US10948926
申请日：2004-09-24
申请人： George Pettit , Mathew Minardi , Heidi Rosenberg
发明人： George Pettit , Mathew Minardi , Heidi Rosenberg
IPC分类号： A61K31/66 , C07C43/23 , C07F9/09 , C07F9/12
CPC分类号： C07C43/23 , C07F9/12
摘要： The invention relates to novel compounds denominated halocombstatins. The halocombstatins are derivatives of combretastatin A-3, and include compounds that exhibit cancer growth cell inhibition against a panel of human cancer cell lines and the murine P388 leukemia, as well as activity as inhibitors of tubulin polymerization and inhibitors of the binding of colchicine to tubulin.
摘要翻译：本发明涉及命名为卤代抑菌素的新化合物。卤代抑菌素是考布他汀A-3的衍生物，并且包括对人类癌细胞系和小鼠P388白血病显示出癌细胞生长细胞抑制作用的化合物，以及作为微管蛋白聚合抑制剂的活性以及秋水仙碱与微管蛋白

10. 发明申请

US20050075516A1 Synthesis of combretastatin a-2 prodrugs 有权
标题翻译：考布他汀a-2前药的合成
公开(公告)号：US20050075516A1
公开(公告)日：2005-04-07
申请号：US10499848
申请日：2002-12-20
申请人： George Pettit , Bryan Moser
发明人： George Pettit , Bryan Moser
IPC分类号： A61K31/665 , A61K31/36 , A61P9/00 , A61P35/00 , A61P43/00 , C07C43/23 , C07F9/12 , C07F9/655 , C07C43/20
CPC分类号： C07F9/65517 , C07C43/23 , C07F9/12 , Y02P20/55
摘要： The original synthesis of combretastatin A-2 (1a) was modified to provide an efficient scale-up procedure for obtaining this antineoplastic stilbene. Subsequent conversion to a useful prodrug was accomplished by phosphorylation employing in situ formation of dibenzylchlorophosphite followed 30 by cleavage of the benzyl ester protective groups with bromotrimethylsilane to afford phosphoric acid intermediate 11. The latter was immediately treated with sodium methoxide to complete a practical route to the disodium phosphate prodrug (2a). The phosphoric acid precursor (11) of phosphate 2a was employed in a parallel series of reactions to produce a selection of metal and ammonium cation prodrug candidates. Each of the phosphate salts (2a-q) was evaluated with respect to relative solubility behavior, cancer cell growth inhibition, and antimicrobial activity.
摘要翻译：改变了考布他汀A-2（1a）的原始合成方法，以获得这种抗肿瘤二萜烯的有效放大方法。随后转化为有用的前体药物是通过使用原位形成二氯苄基亚磷酸酯进行磷酸化，然后通过用溴代三甲基甲硅烷裂解苄酯保护基来提供磷酸中间体11来完成的。后者立即用甲醇钠处理以完成实际路线磷酸二钠前药（2a）。磷酸二烷基酯（11）以平行的一系列反应方式使用，以产生金属和铵阳离子前体药物候选物的选择。关于相对溶解行为，癌细胞生长抑制和抗微生物活性评估磷酸盐（2a-q）中的每一种。

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式