公开(公告)号：US06392055B1

公开(公告)日：2002-05-21

申请号：US09909076

申请日：2001-07-19

申请人： Peter Wipf ,  Jonathan T. Reeves ,  Billy W. Day ,  Raghavan Balachandran

发明人： Peter Wipf ,  Jonathan T. Reeves ,  Billy W. Day ,  Raghavan Balachandran

IPC分类号： C07D27722

CPC分类号： C07D277/20 ,  C07C43/23 ,  C07D263/32 ,  C07D277/10 ,  C07D307/42 ,  C07D307/80 ,  C07D333/16

摘要： The present invention provides an efficient synthetic strategy for the preparation of analogs that incorporate important structural elements of the marine natural product curacin A, the compositions and various uses of the compositions. The most active of these compounds at nanomolar concentrations inhibit tubulin polymerization, show growth inhibition activity, inhibited colchicines binding to tubulin and block mitotic progression. The compounds of the present invention represent some of the most potent synthetic curacin A analogs synthesized, with an activity profile rivaling that of the natural product despite the simplified structure, greater water solubility, and increased chemical stability.

公开(公告)号：US07122686B2

公开(公告)日：2006-10-17

申请号：US10655916

申请日：2003-09-05

申请人： Dennis P. Curran ,  Youseung Shin ,  Nakyen Choy ,  Billy W. Day ,  Raghavan Balachandran ,  Charitha Madiraju ,  Tiffany Turner

发明人： Dennis P. Curran ,  Youseung Shin ,  Nakyen Choy ,  Billy W. Day ,  Raghavan Balachandran ,  Charitha Madiraju ,  Tiffany Turner

IPC分类号： C07D313/00

CPC分类号： C07D407/06 ,  C07B2200/07 ,  C07C33/02 ,  C07C59/10 ,  C07C59/42 ,  C07C69/732 ,  C07C69/734 ,  C07D309/10 ,  C07D309/30 ,  C07D313/00 ,  C07D319/06 ,  C07F7/1804

摘要： A compound of the following structure: wherein R1 is H, an alkyl group, an aryl group, an alkenyl group, an alkynyl group, or a halogen atom; R2 is H, an alkyl group, an aryl group, a benzyl group, a trityl group, —SiRaRbRc, CH2ORd, or CORe; Ra, Rb and Rc are independently an alkyl group or an aryl group; Rd is an alkyl group, an aryl group, an alkoxylalkyl group, —RiSiRaRbRc or a benzyl group, wherein Ri is an alkylene group; Re is an alkyl group, an allyl group, a benzyl group, an aryl group, an alkoxy group, or —NRgRh, wherein Rg and Rh are independently H, an alkyl group or an aryl group; R3 is (CH2)n where n is and integer in the range of 0 to 5, —CH2CH(CH3)—, —CH═CH—, —CH═C(CH3)—, or —C≡C—; R4 is (CH2)p where p is an integer in the range of 4 to 12, —(CHRk1)y1(CHRk2)y2(CHRk3)y3(CHRk4)y4(CHRk5)y5C(Rs1)═C(Rs2)C(Rs3)═C(Rs4)—, —(CHRk1)y1(CHRk2)y2(CHRk3)y3(CHRk4)y4(CHRk5)y5CH(Rs1) CH(Rs2)C(Rs3)═C(Rs4)—, —(CHRk1)y1(CHRk2)y2(CHRk3)y3(CHRk4)y4(CHRk5)y5C(Rs1)═C(Rs2)CH(Rs3)CH(Rs4)—, —(CHRk1)y1(CHRk2)y2(CHRk3)y3(CHRk4)y4(CHRk5)y5CH(Rs1) CH(Rs2)CH(Rs3)CH(Rs4)—, wherein y1 and y2 are 1 and y3, y4 and y5 are independently 0 or 1, Rk1, Rk2, Rk3, Rk4 and Rk5 are independently H, CH3, or OR2a, and Rs1, Rs2, Rs3, and Rs4 are independently H or CH3, wherein R2a is H, an alkyl group, an aryl group, a benzyl group, a trityl group, —SiRaRbRc, CH2ORd, or CORe; and R5 is H or OR2b, wherein R2b is H, an alkyl group, an aryl group, an aryl group, a benzyl group, a trityl group, —SiRaRbRc, CH2ORd, or CORe; provided that the compound is not dictyostatin 1.

公开(公告)号：US06673937B2

公开(公告)日：2004-01-06

申请号：US09910195

申请日：2001-07-19

申请人： John S. Lazo ,  Peter Wipf ,  Billy W. Day

发明人： John S. Lazo ,  Peter Wipf ,  Billy W. Day

IPC分类号： C07D40500

CPC分类号： C07D317/72 ,  A61K31/357 ,  A61K31/426 ,  C07D319/08 ,  C07D403/12 ,  C07D405/06 ,  C07D405/12 ,  C07D493/10

摘要： Oxidative cyclization of bis-naphthyl ethers allows concise total syntheses of palmarumycin CP1 and deoxypreussomerin A in 8-9 steps and 15-35% overall yield from 5-hydroxy-8-methoxy-1-tetralone. A small library of palmarumycin analogs was created. Biological evaluation of these naphthoquinone spiroketals against MCF-7 and MDA-MB-231 human breast cancer cells revealed several low-micromolar growth inhibitors. A number of the analogs inhibit the thioredoxin—thioredoxin reductase system.

摘要翻译： 双萘基醚的氧化环化允许8-9步骤中棕榈霉素CP1和脱氧阿司咪霉素A的简明综合，5-羟基-8-甲氧基-1-四氢萘酮的总产率为15-35％。 创建了一个古老的棕榈霉素类似物库。 这些萘醌螺旋酮对MCF-7和MDA-MB-231人乳腺癌细胞的生物学评价显示出几种低微摩尔生长抑制剂。 许多类似物抑制硫氧还蛋白硫氧还蛋白还原酶系统。

公开(公告)号：US20140161877A1

公开(公告)日：2014-06-12

申请号：US14234133

申请日：2012-07-19

申请人： Paul Edward Floreancig ,  Billy W. Day ,  Shuangyi Wan ,  Fanghui Wu

发明人： Paul Edward Floreancig ,  Billy W. Day ,  Shuangyi Wan ,  Fanghui Wu

IPC分类号： A61K47/48

CPC分类号： A61K47/48384 ,  C07D407/06 ,  C07D407/12 ,  C07D407/14

摘要： Compounds that include a pederin, psymberin or pederin/psymberin chimera scaffold. The pederin scaffold includes a substituent at the C10 and/or C13 position that may include a linker that may be conjugated to a targeting moiety. The psymberin scaffold includes a substituent at the C8 and/or C11 positions that may include a linker that may be conjugated to a targeting moiety. The pederin/psymberin chimera scaffold includes a substituent at the C10 and/or C13 position that may include a linker that may be conjugated to a targeting moiety. The pederin, psymberin or pederin/psymberin chimera scaffold may be modified to include substituents at positions other than the C10 or C13 of pederin, or the C8 and C11 of psymberin.

摘要翻译： 化合物包括pederin，psymberin或pederin / psymberin嵌合体支架。 er脚骨架在C10和/或C13位置包含可以与可能与靶向部分缀合的接头的取代基。 精神分裂素支架在C8和/或C11位置包括可以包含可以与靶向部分缀合的接头的取代基。 pederin / psymberin嵌合体支架包括在C10和/或C13位置的取代基，其可以包括可以与靶向部分缀合的连接体。 可以修饰pederin，psymberin或pederin / psymberin嵌合体支架，以在除Pederin的C10或C13之外的位置或psymberin的C8和C11中包含取代基。

公开(公告)号：US5015666A

公开(公告)日：1991-05-14

申请号：US410938

申请日：1989-09-22

申请人： Robert A. Magarian ,  Joseph T. Pento ,  Billy W. Day

发明人： Robert A. Magarian ,  Joseph T. Pento ,  Billy W. Day

IPC分类号： A61K31/03 ,  C07C309/66 ,  C07D295/092

CPC分类号： C07D295/088 ,  A61K31/03 ,  C07C309/66 ,  C07C2101/02

摘要： Triarylcyclopropane derivatives in which one or more of the aryl groups includes a hydroxy as a substituted or unsubstituted or alkoxy or side chain substituent. The compounds are useful as antiestrogens and anti-tumor agents.

摘要翻译： 其中一个或多个芳基包括羟基作为取代或未取代的烷氧基或侧链取代基的三芳基环丙烷衍生物。 该化合物可用作抗雌激素和抗肿瘤剂。

公开(公告)号：US10160705B2

公开(公告)日：2018-12-25

申请号：US13982512

申请日：2012-02-10

申请人： Billy W. Day ,  Neil Hukriede

发明人： Billy W. Day ,  Neil Hukriede

IPC分类号： C07C29/80 ,  B01D15/18 ,  C07C317/44 ,  C07C323/52 ,  C07C323/56 ,  C07C323/60 ,  C07C323/62 ,  C07C229/18

摘要： Compounds and compositions are provided that inhibit histone deacylase activity and which expand renal progenitor cell populations and improve kidney function in a damaged kidney. Methods of use of the compounds and compositions are provided.

公开(公告)号：US09364555B2

公开(公告)日：2016-06-14

申请号：US14234133

申请日：2012-07-19

申请人： Paul Edward Floreancig ,  Billy W. Day ,  Shuangyi Wan ,  Fanghui Wu

发明人： Paul Edward Floreancig ,  Billy W. Day ,  Shuangyi Wan ,  Fanghui Wu

IPC分类号： A61K47/48 ,  C07D407/06 ,  C07D407/12 ,  C07D407/14

CPC分类号： A61K47/48384 ,  C07D407/06 ,  C07D407/12 ,  C07D407/14

摘要： Compounds that include a pederin, psymberin or pederin/psymberin chimera scaffold. The pederin scaffold includes a substituent at the C10 and/or C13 position that may include a linker that may be conjugated to a targeting moiety. The psymberin scaffold includes a substituent at the C8 and/or C11 positions that may include a linker that may be conjugated to a targeting moiety. The pederin/psymberin chimera scaffold includes a substituent at the C10 and/or C13 position that may include a linker that may be conjugated to a targeting moiety. The pederin, psymberin or pederin/psymberin chimera scaffold may be modified to include substituents at positions other than the C10 or C13 of pederin, or the C8 and C11 of psymberin.

摘要翻译： 化合物包括pederin，psymberin或pederin / psymberin嵌合体支架。 er脚骨架在C10和/或C13位置包含可以与可能与靶向部分缀合的接头的取代基。 精神分裂素支架在C8和/或C11位置包括可以包含可以与靶向部分缀合的接头的取代基。 pederin / psymberin嵌合体支架包括在C10和/或C13位置的取代基，其可以包括可以与靶向部分缀合的连接体。 可以修饰pederin，psymberin或pederin / psymberin嵌合体支架，以在除Pederin的C10或C13之外的位置或psymberin的C8和C11中包含取代基。

公开(公告)号：US20140081054A1

公开(公告)日：2014-03-20

申请号：US13982512

申请日：2012-02-10

申请人： Billy W. Day ,  Neil Hukriede

发明人： Billy W. Day ,  Neil Hukriede

IPC分类号： C07C29/80 ,  B01D15/18

CPC分类号： C07C29/80 ,  B01D15/1821 ,  C07C229/18 ,  C07C317/44 ,  C07C323/52 ,  C07C323/56 ,  C07C323/60 ,  C07C323/62

摘要： The invention concerns separation methods and systems including those comprising a continuous chromatographic simulated moving bed integrated with vapor compression distillation to create a high efficiency separations platform applicable to a broad range of separation functions.

摘要翻译： 本发明涉及分离方法和系统，包括包括与蒸气压缩蒸馏一体化的连续色谱模拟移动床的分离方法和系统，以产生适用于宽范围分离功能的高效分离平台。

公开(公告)号：US08541415B2

公开(公告)日：2013-09-24

申请号：US12988501

申请日：2009-05-14

申请人： Lori Emert-Sedlak ,  Toshiaki Kodama ,  Billy W. Day ,  Weixiang Dai ,  Ronald P. Trible ,  Thomas E. Smithgall

发明人： Lori Emert-Sedlak ,  Toshiaki Kodama ,  Billy W. Day ,  Weixiang Dai ,  Ronald P. Trible ,  Thomas E. Smithgall

IPC分类号： A01N43/58 ,  A01N43/60 ,  A61K31/50 ,  A61K31/495 ,  C07D241/36

CPC分类号： C07D491/048 ,  C07D241/44 ,  C07D405/12 ,  C07D491/04

摘要： Drug candidates for inhibition of HIV-I replication can target Src family kinases (SFK), such as Hck, that interact with Nef protein of the virus. Compounds characterized by such inhibitory activity were identified via an assay for kinase activity of an SFK in a Nef:SFK complex. Illustrative of inhibitors identified using the kinase assay are various 2,3-diaminoquinaxolines and furo[2,3-d]pyrimidines. The inventive inhibitors were found to arrest HIV-I viral replication in vitro.

摘要翻译： 用于抑制HIV-1复制的药物候选物可以靶向与病毒的Nef蛋白相互作用的Src家族激酶（SFK），例如Hck。 通过对Nef：SFK复合物中的SFK的激酶活性的测定来鉴定以这种抑制活性为特征的化合物。 使用激酶测定法鉴定的抑制剂的实例是各种2,3-二氨基鸟苷和呋喃并[2,3-d]嘧啶。 发现本发明的抑制剂在体外阻止HIV-1病毒复制。

公开(公告)号：US20120122992A1

公开(公告)日：2012-05-17

申请号：US13256584

申请日：2010-03-19

申请人： Billy W. Day ,  Waikok Michael Tsang ,  Vasiliy N. Korotchenko

发明人： Billy W. Day ,  Waikok Michael Tsang ,  Vasiliy N. Korotchenko

IPC分类号： A61K31/135 ,  C12N5/071 ,  C07C211/42

CPC分类号： C07C225/20 ,  A61K31/135 ,  C07C211/42 ,  C07D495/04

摘要： Compounds that stimulate fibroblast growth factor production, and thus cell growth are provided. Also provided are compositions comprising the compounds and methods of using the compounds. The compounds can be used to treat wounds, to expand cell populations, such as hematopoietic cells, or to grow tissue in vitro, among other uses.

摘要翻译： 提供了刺激成纤维细胞生长因子生成，从而促进细胞生长的化合物。 还提供了包含该化合物的组合物和使用该化合物的方法。 这些化合物可以用于治疗伤口，扩大细胞群体，如造血细胞，或者在体外培养组织以及其他用途。