公开(公告)号：US20140364595A1

公开(公告)日：2014-12-11

申请号：US14128281

申请日：2012-06-22

申请人： Abhijit S. Bapat ,  Gauthami Mahesh ,  Rajesh S. Gokhale ,  Sayali S. Shah ,  Shiladitya Sengupta ,  Sudhanand Prasad ,  Sumana Ghosh ,  Suresh R. Chawrai ,  Nidhi Arora ,  D. Sreedhar Reddy ,  Malika Mishra ,  Kirti Bajaj

发明人： Abhijit S. Bapat ,  Gauthami Mahesh ,  Rajesh S. Gokhale ,  Sayali S. Shah ,  Shiladitya Sengupta ,  Sudhanand Prasad ,  Sumana Ghosh ,  Suresh R. Chawrai ,  Nidhi Arora ,  D. Sreedhar Reddy ,  Malika Mishra ,  Kirti Bajaj

IPC分类号： A61K31/7056 ,  A61K47/48 ,  A61K31/085 ,  A61K31/496

CPC分类号： A61K31/7056 ,  A01N37/46 ,  A61K8/0241 ,  A61K8/347 ,  A61K8/361 ,  A61K8/362 ,  A61K8/368 ,  A61K8/37 ,  A61K8/375 ,  A61K8/39 ,  A61K8/49 ,  A61K8/4933 ,  A61K8/602 ,  A61K8/8129 ,  A61K31/085 ,  A61K31/496 ,  A61K47/54 ,  A61K47/542 ,  A61K47/552 ,  A61K47/60 ,  A61K2800/412 ,  A61K2800/413 ,  A61K2800/57 ,  A61Q5/006 ,  A61Q17/005

摘要： The invention provides conjugate-based antifungal or antibacterial prodrugs formed by coupling at least one anti-fungal agent or antibacterial agent with at least one linker and/or carrier. The prodrugs are of formula: (i) (AFA)m-X-(L)n; (ii) [(AFA)m′-X]p-L; (iii) AFA-[X-(L)n′]q; or (iv) (AFA)m″-X, wherein: AFA is an antifungal agent or an antibacterial agent; L is a carrier; X is a linker; m ranges from 1 to 10; n ranges from 2 to 10; m′ is 1 to 10; p is 1 to 10; n′ is 1 to 10; and q is 1 to 10, provided that q′ and n are not both 1; and m″ is 1 to 10. The invention also provides nanoparticles comprising the conjugate-based prodrugs. Additionally, the invention also provides non-conjugated antifungal and antibacterial agents in the form of nanoparticles.

摘要翻译： 本发明提供了通过将至少一种抗真菌剂或抗菌剂与至少一种接头和/或载体偶联而形成的基于缀合物的抗真菌或抗菌前药。 前药具有下式：（i）（AFA）m-X-（L）n; （ii）[（AFA）m'-X] p-L; （iii）AFA- [X-（L）n'] q; 或（iv）（AFA）m“-X，其中：AFA是抗真菌剂或抗菌剂; L是载体; X是一个连接子; m范围从1到10; n范围从2到10; m'为1〜10; p为1〜10; n'为1〜10; q为1〜10，条件是q'和n不同时为1; 并且m“为1至10.本发明还提供了包含基于缀合物的前药的纳米颗粒。 此外，本发明还提供纳米颗粒形式的非共轭抗真菌剂和抗菌剂。

公开(公告)号：US09907812B2

公开(公告)日：2018-03-06

申请号：US14128281

申请日：2012-06-22

申请人： Abhijit S. Bapat ,  Gauthami Mahesh ,  Rajesh S. Gokhale ,  Sayali S. Shah ,  Shiladitya Sengupta ,  Sudhanand Prasad ,  Sumana Ghosh ,  Suresh R. Chawrai ,  Nidhi Arora ,  D. Sreedhar Reddy ,  Mallika Mishra ,  Kirti Bajaj

发明人： Abhijit S. Bapat ,  Gauthami Mahesh ,  Rajesh S. Gokhale ,  Sayali S. Shah ,  Shiladitya Sengupta ,  Sudhanand Prasad ,  Sumana Ghosh ,  Suresh R. Chawrai ,  Nidhi Arora ,  D. Sreedhar Reddy ,  Mallika Mishra ,  Kirti Bajaj

IPC分类号： A61K31/7056 ,  A61K47/48 ,  A61K31/085 ,  A61K31/496 ,  A61K8/37 ,  A61Q17/00 ,  A61K8/34 ,  A61K8/36 ,  A61K8/362 ,  A61K8/368 ,  A61K8/39 ,  A61K8/49 ,  A61Q5/00 ,  A61K8/60 ,  A61K8/81 ,  A61K8/02 ,  A01N37/46 ,  A61K47/60 ,  A61K47/54 ,  A61K47/55

CPC分类号： A61K31/7056 ,  A01N37/46 ,  A61K8/0241 ,  A61K8/347 ,  A61K8/361 ,  A61K8/362 ,  A61K8/368 ,  A61K8/37 ,  A61K8/375 ,  A61K8/39 ,  A61K8/49 ,  A61K8/4933 ,  A61K8/602 ,  A61K8/8129 ,  A61K31/085 ,  A61K31/496 ,  A61K47/54 ,  A61K47/542 ,  A61K47/552 ,  A61K47/60 ,  A61K2800/412 ,  A61K2800/413 ,  A61K2800/57 ,  A61Q5/006 ,  A61Q17/005

摘要： The invention provides conjugate-based antifungal or antibacterial prodrugs formed by coupling at least one anti-fungal agent or antibacterial agent with at least one linker and/or carrier. The prodrugs are of formula: (i) (AFA)m-X-(L)n; (ii) [(AFA)m′-X]p-L; (iii) AFA-[X-(L)n′]q; or (iv) (AFA)m″-X, wherein: AFA is an antifungal agent or an antibacterial agent; L is a carrier; X is a linker; m ranges from 1 to 10; n ranges from 2 to 10; m′ is 1 to 10; p is 1 to 10; n′ is 1 to 10; and q is 1 to 10, provided that q′ and n are not both 1; and m″ is 1 to 10. The invention also provides nanoparticles comprising the conjugate-based prodrugs. Additionally, the invention also provides non-conjugated antifungal and antibacterial agents in the form of nanoparticles.