公开(公告)号：US20090062358A1

公开(公告)日：2009-03-05

申请号：US11828446

申请日：2007-07-26

申请人： Ivan Collado Cano ,  Samuel James Dominianni ,  Garret Jay Etgen, JR. ,  Cristina Garcia-Paredes ,  Richard Duane Johnston ,  Michael Edward Letourneau ,  Nathan Bryan Mantlo ,  Michael John Martinelli ,  Daniel Ray Mayhugh ,  Ashraf Saeed ,  Richard Craig Thompson ,  Xiaodong Wang ,  David Scott Coffey ,  Christopher Randall Schmid ,  Jeffrey Thomas Vicenzi ,  Yanping Xu

发明人： Ivan Collado Cano ,  Samuel James Dominianni ,  Garret Jay Etgen, JR. ,  Cristina Garcia-Paredes ,  Richard Duane Johnston ,  Michael Edward Letourneau ,  Nathan Bryan Mantlo ,  Michael John Martinelli ,  Daniel Ray Mayhugh ,  Ashraf Saeed ,  Richard Craig Thompson ,  Xiaodong Wang ,  David Scott Coffey ,  Christopher Randall Schmid ,  Jeffrey Thomas Vicenzi ,  Yanping Xu

IPC分类号： A61K31/4196 ,  C07D249/12 ,  C07D405/02

CPC分类号： C07C281/06 ,  C07C257/22 ,  C07C281/04 ,  C07D249/12 ,  C07D401/06 ,  C07D405/06 ,  C07D409/06 ,  C07D409/12 ,  C07D413/06 ,  C07D417/12

摘要： The present invention is directed to compounds represented by the following structural formula, and pharmaceutically acceptable salts, solvates and hydrates thereof, R1 is a substituted or unsubstituted group selected from C1-C8 alkyl, aryl-C0-2-alkyl, heteroaryl-C0-2-alkyl, C3-C6 cycloalkylaryl-C0-2-alkyl or phenyl. W is O or S. R2 is H or a substituted or unsubstituted group selected from C1-C6 alkyl, C3-C6 cycloalkyl and heteroaryl. X is a C2-C5 alkylene linker wherein one carbon atom of the linker may be replaced with O, NH or S. Y is C, O, S, NH or a single bond. Furthermore, E is (CH2)nCOOH, wherein n is 0, 1, 2 or 3, or C(R3)(R4)A, wherein A is an acidic functional group such as carboxyl, carboxamide substituted or unsubstituted sulfonamide, or substituted or unsubstituted tetrazole. R3 is H, saturated or unsaturated C1-C5 alkyl, C1-C5 alkoxy. Additionally, R4 is H, halo, a substituted or unsubstituted group selected from C1-C5 alkyl, C1-C5 alkoxy, C3-C6 cycloalkyl, arylC0-C4alkyl and phenyl, or R3 and R4 are combined to form a C3-C4 cycloalkyl.

摘要翻译： 本发明涉及由以下结构式表示的化合物及其药学上可接受的盐，溶剂合物和水合物，R 1是选自C 1 -C 8烷基，芳基-C 0-2 - 烷基，杂芳基-C 0 - C 3 -C 6环烷基芳基-C 0-2 - 烷基或苯基。 W是O或S.R 2是H或选自C 1 -C 6烷基，C 3 -C 6环烷基和杂芳基的取代或未取代的基团。 X是C2-C5亚烷基连接体，连接体的一个碳原子可被O，NH或S取代.Y是C，O，S，NH或单键。 此外，E是（CH 2）n COOH，其中n是0,1,2或3或C（R3）（R4）A，其中A是酸性官能团如羧基，甲酰胺取代或未取代的磺酰胺，或取代或未取代的 未取代的四唑。 R3是H，饱和或不饱和的C1-C5烷基，C1-C5烷氧基。 另外，R 4为H，卤素，取代或未取代的选自C 1 -C 5烷基，C 1 -C 5烷氧基，C 3 -C 6环烷基，芳基C 0 -C 4烷基和苯基，或R 3和R 4的基团，形成C 3 -C 4环烷基。

公开(公告)号：US5977383A

公开(公告)日：1999-11-02

申请号：US934999

申请日：1997-09-22

申请人： Jeffrey Thomas Vicenzi ,  Tony Yantao Zhang

发明人： Jeffrey Thomas Vicenzi ,  Tony Yantao Zhang

IPC分类号： C07D333/52 ,  C07D333/56

CPC分类号： C07D333/56

摘要： The instant invention provides improved processes for preparing benzothiophenes utilizing cation exchange resins.

摘要翻译： 本发明提供了利用阳离子交换树脂制备苯并噻吩的改进方法。

公开(公告)号：US06590073B2

公开(公告)日：2003-07-08

申请号：US09944309

申请日：2001-08-30

申请人： Brian Weston Dalder ,  Michael Anthony Dotlich ,  Neil John Kallman ,  Samuel Dean Larsen ,  Sharon Van Den Berghe Snorek ,  Jeffrey Thomas Vicenzi

发明人： Brian Weston Dalder ,  Michael Anthony Dotlich ,  Neil John Kallman ,  Samuel Dean Larsen ,  Sharon Van Den Berghe Snorek ,  Jeffrey Thomas Vicenzi

IPC分类号： A61K3812

CPC分类号： C07K7/56 ,  A61K38/00 ,  Y10S977/898

摘要： A method is described for forming a crystalline Echinocandin nucleus salt from its mixed broth and/or partially purified process streams by the steps of nanofiltration to form a concentrate, addition of an aldehyde derivatizing agent which interacts with an aldehyde impurity, addition of an acid/metal salt to form a solubilized echinocandin nucleus salt having the desired anion, and subsequent cooling of the mixture to crystallize the salt.

摘要翻译： 描述了通过纳米过滤以形成浓缩物的步骤从其混合的肉汤和/或部分纯化的工艺流中形成结晶棘球in烷核盐的方法，加入与醛杂质相互作用的醛衍生化试剂，加入酸/ 形成具有所需阴离子的溶解的棘白菌素核盐，随后冷却混合物以使盐结晶。

公开(公告)号：US06506726B1

公开(公告)日：2003-01-14

申请号：US09857924

申请日：2001-12-10

申请人： John Robert Dobbins ,  Eugene Paul Kroeff ,  Jeffrey Thomas Vicenzi

发明人： John Robert Dobbins ,  Eugene Paul Kroeff ,  Jeffrey Thomas Vicenzi

IPC分类号： A61K3800

CPC分类号： C07K7/56 ,  A61K38/00

摘要： A method is described for separating and purifying a wide variety of fermentation cyclopeptide products containing at least one protonatable amino group (including the deacylated Echinocandin-type compounds) from their fermentation or mixed broths and partially purified process streams by adsorbing the mixture onto a hydrophobic, reversed phase chromatographic media and eluting with a continuous linear acetic acid gradient ranging from 0.1% acetic acid to 10.0% acetic acid by volume in water. A process for removing tripeptide-aldehyde by-products from the fermentation products by means of a derivatizing agent is also described.

摘要翻译： 描述了一种用于从其发酵或混合肉汤和部分纯化的工艺流中分离和纯化含有至少一个可质子化氨基（包括脱酰化棘皮菌素型化合物）的多种发酵环肽产物的方法，通过将混合物吸附到疏水， 反相色谱介质并用在水中的体积比为0.1％乙酸至10.0％乙酸的连续线性乙酸梯度洗脱。 还描述了通过衍生剂从发酵产物中除去三肽 - 醛副产物的方法。

公开(公告)号：US5969157A

公开(公告)日：1999-10-19

申请号：US972783

申请日：1997-11-18

申请人： Jeffrey Thomas Vicenzi

发明人： Jeffrey Thomas Vicenzi

IPC分类号： C07D333/52 ,  C07D333/56 ,  C07D405/00 ,  C07D409/00

CPC分类号： C07D333/56

摘要： The instant invention provides improved processes for preparing benzothiophenes utilizing methanesulfonic acid.

摘要翻译： 本发明提供了利用甲磺酸制备苯并噻吩的改进方法。