公开(公告)号：WO2010056590A3

公开(公告)日：2010-05-20

申请号：PCT/US2009/063381

申请日：2009-11-05

Applicant: UNIVERSITY OF MARYLAND, BALTIMORE ,  UNIVERSITY OF MARYLAND, COLLEGE PARK ,  YU, Yihua, Bruce ,  JIANG, Zhong-Xing

Inventor： YU, Yihua, Bruce ,  JIANG, Zhong-Xing

IPC: A61K49/06

Abstract: Compositions for producing multi-chromic ("color") magnetic resonance images (MRI). The compositions for use as MRI imaging agents include a magnetic resonance imaging tracer having a signal emitter, such as a 19 F imaging tracer ( 19 FIT), conjugated with a magnetic signal modulator, such as a paramagnetic functional group or a paramagnetic ion. The 19 FIT and the signal modulator (M) are joined covalently by a chelator such as DOTA, forming a nanometer-sized fluorinated paramagnetic complex 19 FIT-DOTA-M. Other signal emitters, such as 31 P imaging tracer ( 31 PIT), can also be modulated using this strategy (i.e., 31 PIT-DOTA-M) to generate multi-chromic 31 P MRI or MRS.

公开(公告)号：WO2010056590A2

公开(公告)日：2010-05-20

申请号：PCT/US2009063381

申请日：2009-11-05

Applicant: UNIV MARYLAND ,  YU YIHUA BRUCE ,  JIANG ZHONG-XING

Inventor： YU YIHUA BRUCE ,  JIANG ZHONG-XING

IPC: A61K49/06

CPC classification number: A61K49/085 ,  A61K47/55 ,  A61K47/56 ,  A61K47/60 ,  A61K49/0002 ,  A61K49/122

Abstract: Compositions for producing multi-chromic ("color") magnetic resonance images (MRI). The compositions for use as MRI imaging agents include a magnetic resonance imaging tracer having a signal emitter, such as a 19F imaging tracer (19FIT), conjugated with a magnetic signal modulator, such as a paramagnetic functional group or a paramagnetic ion. The 19FIT and the signal modulator (M) are joined covalently by a chelator such as DOTA, forming a nanometer-sized fluorinated paramagnetic complex 19FIT-DOTA-M. Other signal emitters, such as 31P imaging tracer (31PIT), can also be modulated using this strategy (i.e., 31PIT-DOTA-M) to generate multi-chromic 31P MRI or MRS.

Abstract translation: 用于制造多色（“彩色”）磁共振图像（MRI）的组合物。 用作MRI成像剂的组合物包括磁共振成像示踪剂，其具有与磁性信号调节剂（例如顺磁性官能团或顺磁性离子）共轭的信号发射体，例如19F成像示踪剂（19FIT）。 19FIT和信号调节剂（M）通过诸如DOTA的螯合剂共价结合，形成纳米尺寸的氟化顺磁复合物19FIT-DOTA-M。 其他信号发射器，例如31P成像示踪剂（31PIT），也可以使用该策略（即31PIT-DOTA-M）来调制以产生多重31P MRI或MRS。

公开(公告)号：WO2007112100A2

公开(公告)日：2007-10-04

申请号：PCT/US2007/007459

申请日：2007-03-26

Applicant: THE UNIVERSITY OF UTAH RESEARCH FOUNDATION ,  YU, Yihua ,  JIANG, Zhong-xing

Inventor： YU, Yihua ,  JIANG, Zhong-xing

IPC: A61K49/10

CPC classification number: A61K51/065 ,  A61K41/0038 ,  A61K47/6905 ,  A61K47/6953 ,  A61K49/0002 ,  A61K49/085 ,  A61K49/124 ,  A61K49/14 ,  A61K49/1809 ,  A61K49/1818 ,  A61K51/122 ,  B82Y5/00 ,  C08G83/003 ,  C08G83/004

Abstract: Disclosed are compounds comprising the structure (I): In one aspect, the compounds exhibit maximum symmetric branching. Also disclosed are bilayers, micelles, coatings, and nanoparticles comprising the disclosed compounds. Also disclosed are processes for the preparation of the disclosed compounds and methods of using the disclosed compounds. Also disclosed are highly fluorinated dendrons and methods for making same. Also disclosed are methods for Fluorous Mixture Synthesis and tagging. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

Abstract translation: 公开了包含结构（I）的化合物：在一个方面，所述化合物表现出最大的对称分支。 还公开了包含所公开的化合物的双层，胶束，包衣和纳米颗粒。 还公开了用于制备所公开的化合物的方法和使用所公开的化合物的方法。 还公开了高度氟化的树突及其制造方法。 还公开了用于含氟混合物合成和标记的方法。 本摘要旨在作为用于在特定领域中进行搜索的目的的扫描工具，并且不旨在限制本发明。

公开(公告)号：WO2008034093A3

公开(公告)日：2008-03-20

申请号：PCT/US2007/078549

申请日：2007-09-14

Applicant: UNIVERSITY OF UTAH RESEARCH FOUNDATION ,  YU, Bruce ,  JIANG, Zhong-xing

Inventor： YU, Bruce ,  JIANG, Zhong-xing

IPC: A61K38/00 ,  A61K38/04

Abstract: Disclosed are compounds having the structure: wherein R la and R lb are independently H, alkyl, F, or fluoroalkyl; wherein R 2a , R 2b , R 2a' , and R 2b are independently H, alkyl, F, fluoroalkyl, aryl, or alkenyl; wherein R 3 is OH, alkoxyl, NH 2 , alkylamino, or dialkylamino; wherein R 4a and R 4b are independently H, alkyl, acyl, or alkyloxycarbonyl; wherein R 11 , R 12 , R 13 , R 21 , R 22 , and R 23 are independently H, alkyl, F, or fluoroalkyl; and wherein CO, Cl, C2, and C2' are independently chiral or achiral. Also disclosed are processes for making a fluorinated β-amino acid comprising the steps of: providing a diol; treating the diol with a thionyl halide with oxidative workup; reacting the product with an azide salt to yield an azido group; oxidizing the product to yield a carboxyl group; and reducing the azido group to yield an amino group. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

公开(公告)号：WO2008034095A3

公开(公告)日：2008-03-20

申请号：PCT/US2007/078552

申请日：2007-09-14

Applicant: UNIVERSITY OF UTAH RESEARCH FOUNDATION ,  YU, Bruce ,  JIANG, Zhong-Xing ,  XIAO, Nu

Inventor： YU, Bruce ,  JIANG, Zhong-Xing ,  XIAO, Nu

IPC: C07C261/00 ,  C07K1/00

Abstract: Disclosed are processes for preparing a protected trifluorothreonine, or salt thereof or carboxylate derivative thereof, the process comprising: dihydroxylation of an alkene to yield a dihydroxyl compound; conversion of the dihydroxyl compound to a monohydroxyl compound; protection of the monohydroxyl compound to yield an azide compound; transformation of the azide compound to yield an amino compound; protection of the amino compound to yield a protected amine compound; and oxidation of the protected amine compound to yield the protected trifluorothreonine. Also disclosed are compounds having the structure: or salt thereof or carboxylate derivative thereof, wherein P 2 is a hydroxyl protecting group, and wherein P 3 is an amine protecting group. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

公开(公告)号：WO2008034095A2

公开(公告)日：2008-03-20

申请号：PCT/US2007078552

申请日：2007-09-14

Applicant: UNIV UTAH RES FOUND ,  YU BRUCE ,  JIANG ZHONG-XING ,  XIAO NU

Inventor： YU BRUCE ,  JIANG ZHONG-XING ,  XIAO NU

IPC: C07C227/12

CPC classification number: C07C271/22 ,  A61K38/00 ,  C07B2200/07 ,  C07C29/147 ,  C07C41/16 ,  C07C41/26 ,  C07C43/176 ,  C07C67/14 ,  C07C67/29 ,  C07C67/31 ,  C07C67/317 ,  C07C271/16 ,  C07C2603/18 ,  C07K7/06 ,  Y02P20/55 ,  C07C69/78 ,  C07C69/675 ,  C07C69/65 ,  C07C43/1786

Abstract: Disclosed are processes for preparing a protected trifluorothreonine, or salt thereof or carboxylate derivative thereof, the process comprising: dihydroxylation of an alkene to yield a dihydroxyl compound; conversion of the dihydroxyl compound to a monohydroxyl compound; protection of the monohydroxyl compound to yield an azide compound; transformation of the azide compound to yield an amino compound; protection of the amino compound to yield a protected amine compound; and oxidation of the protected amine compound to yield the protected trifluorothreonine. Also disclosed are compounds having the structure: or salt thereof or carboxylate derivative thereof, wherein P 2 is a hydroxyl protecting group, and wherein P 3 is an amine protecting group. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

Abstract translation: 公开了制备受保护的三氟苏糖酸或其盐或其羧酸酯衍生物的方法，所述方法包括：将烯烃二羟基化以产生二羟基化合物; 将二羟基化合物转化成单羟基化合物; 保护单羟基化合物以产生叠氮化合物; 叠氮化合物转化成氨基化合物; 保护氨基化合物以产生受保护的胺化合物; 并将受保护的胺化合物氧化以产生受保护的三氟苏氨酸。 还公开了具有以下结构的化合物或其盐或其羧酸酯衍生物：其中P 2是羟基保护基，并且其中P 3是胺保护基。 该摘要旨在作为用于在特定领域中进行搜索的目的的扫描工具，并且不旨在限制本发明。

公开(公告)号：WO2008034093A2

公开(公告)日：2008-03-20

申请号：PCT/US2007078549

申请日：2007-09-14

Applicant: UNIV UTAH RES FOUND ,  YU BRUCE ,  JIANG ZHONG-XING

Inventor： YU BRUCE ,  JIANG ZHONG-XING

IPC: A61K38/08

CPC classification number: A61K38/08 ,  C07C229/22 ,  C07C247/04 ,  C07C271/22 ,  C07C2603/18

Abstract: Disclosed are compounds having the structure: wherein R la and R lb are independently H, alkyl, F, or fluoroalkyl; wherein R 2a , R 2b , R 2a' , and R 2b are independently H, alkyl, F, fluoroalkyl, aryl, or alkenyl; wherein R 3 is OH, alkoxyl, NH 2 , alkylamino, or dialkylamino; wherein R 4a and R 4b are independently H, alkyl, acyl, or alkyloxycarbonyl; wherein R 11 , R 12 , R 13 , R 21 , R 22 , and R 23 are independently H, alkyl, F, or fluoroalkyl; and wherein CO, Cl, C2, and C2' are independently chiral or achiral. Also disclosed are processes for making a fluorinated ß-amino acid comprising the steps of: providing a diol; treating the diol with a thionyl halide with oxidative workup; reacting the product with an azide salt to yield an azido group; oxidizing the product to yield a carboxyl group; and reducing the azido group to yield an amino group. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

Abstract translation: 公开了具有以下结构的化合物：其中R 1a和R 1b独立地为H，烷基，F或氟烷基; 其中R 2a，R 2b，R 2a，R 2a和R 2b独立地为H，烷基，F， 氟代烷基，芳基或链烯基; 其中R 3是OH，烷氧基，NH 2，烷基氨基或二烷基氨基; 其中R 4a和R 4b独立地为H，烷基，酰基或烷氧基羰基; 其中R 11，R 12，R 13，R 21，R 22， 和R 23独立地为H，烷基，F或氟烷基; 并且其中CO，Cl，C2和C2'独立地是手性或非手性的。 还公开了制备氟化β-氨基酸的方法，包括以下步骤：提供二醇; 用亚硫酰卤用氧化后处理二醇; 使产物与叠氮盐反应以产生叠氮基; 氧化产物以产生羧基; 并还原叠氮基得到氨基。 该摘要旨在作为用于在特定领域中进行搜索的目的的扫描工具，并且不旨在限制本发明。

公开(公告)号：WO2007112100A3

公开(公告)日：2007-12-21

申请号：PCT/US2007007459

申请日：2007-03-26

Applicant: UNIV UTAH RES FOUND ,  YU YIHUA ,  JIANG ZHONG-XING

Inventor： YU YIHUA ,  JIANG ZHONG-XING

IPC: A61B5/055 ,  C07C43/12

CPC classification number: A61K51/065 ,  A61K41/0038 ,  A61K47/6905 ,  A61K47/6953 ,  A61K49/0002 ,  A61K49/085 ,  A61K49/124 ,  A61K49/14 ,  A61K49/1809 ,  A61K49/1818 ,  A61K51/122 ,  B82Y5/00 ,  C08G83/003 ,  C08G83/004

Abstract: Disclosed are compounds comprising the structure (I): In one aspect, the compounds exhibit maximum symmetric branching. Also disclosed are bilayers, micelles, coatings, and nanoparticles comprising the disclosed compounds. Also disclosed are processes for the preparation of the disclosed compounds and methods of using the disclosed compounds. Also disclosed are highly fluorinated dendrons and methods for making same. Also disclosed are methods for Fluorous Mixture Synthesis and tagging. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

Abstract translation: 公开了包含结构（I）的化合物：一方面，化合物表现出最大对称支化。 还公开了包含所公开的化合物的双层，胶束，涂层和纳米颗粒。 还公开了制备所公开的化合物的方法和使用所公开的化合物的方法。 还公开了高度氟化的树枝状体及其制造方法。 还公开了氟混合物合成和标记的方法。 该摘要旨在作为用于在特定技术中进行搜索的扫描工具，而不意在限制本发明。