公开(公告)号：US20120157371A1

公开(公告)日：2012-06-21

申请号：US13323556

申请日：2011-12-12

申请人： Chongxi YU ,  Lina Xu ,  Yuhua Chen ,  Binbing Yan ,  Shiqian Tu

发明人： Chongxi YU ,  Lina Xu ,  Yuhua Chen ,  Binbing Yan ,  Shiqian Tu

IPC分类号： A61K38/12 ,  A61K31/431 ,  C07D499/46 ,  A61K31/43 ,  C07D499/64 ,  C07D499/68 ,  C07D499/70 ,  C07D501/60 ,  A61K31/546 ,  A61K31/545 ,  A61K31/675 ,  C07F9/6561 ,  C07F9/40 ,  C07F9/6506 ,  C12Q1/02 ,  C07K7/64 ,  A61P31/00 ,  A61P31/04 ,  A61P31/16 ,  A61P31/10 ,  A61P31/12 ,  A61P1/16 ,  A61P11/00 ,  A61P1/00 ,  A61P25/00 ,  A61P13/12 ,  A61P9/00 ,  A61P27/02 ,  A61P17/00 ,  A61P1/18 ,  C07D499/76

CPC分类号： C07D499/21

摘要： The invention provides compositions of novel high penetration compositions (HPC) or high penetration prodrugs (HPP) of antimicrobials and antimicrobial-related compounds, which are capable of crossing biological barriers with high penetration efficiency. The HPCs/HPPs are capable of being converted to parent active drugs or drug metabolites after crossing the biological barrier and thus can render treatments for the conditions that the parent drugs or metabolites can. Additionally, the HPPs are capable of reaching areas that parent drugs may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. The HPCs/HPPs can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.

摘要翻译： 本发明提供能够跨越具有高穿透效率的生物屏障的新型高渗透组合物（HPC）或抗高血压前药（HPP）的抗微生物剂和抗微生物相关化合物的组合物。 HPC / HPP能够在穿过生物屏障之后转化为亲本活性药物或药物代谢物，因此可以对母体药物或代谢物可以进行的处理。 此外，HPP能够达到母体药物可能无法进入或在目标区域提供足够浓度的区域，从而进行新的治疗。 HPC / HPP可以通过各种施用途径施用于受试者，例如局部递送至具有高浓度或系统地施用于生物受试者的病症的作用部位并以更快的速率进入总体循环。

公开(公告)号：US20130131100A1

公开(公告)日：2013-05-23

申请号：US13732256

申请日：2012-12-31

申请人： Chongxi YU

发明人： Chongxi YU

IPC分类号： C07D471/04

CPC分类号： C07D471/04 ,  A61K9/0014 ,  A61K31/44 ,  A61K31/4745

摘要： The invention provides compositions of novel high penetration compositions (HPC) or high penetration prodrugs (HPP) of 1H-imidazo[4,5-c]quinolin-4-amines and 1H-imidazo[4,5-c]quinolin-4-amine-related compounds, which are capable of crossing biological barriers with high penetration efficiency. The HPPs are capable of being converted to parent active drugs or drug metabolites after crossing the biological barrier and thus can render treatments for the conditions that the parent drugs or metabolites can. Additionally, the HPPs are capable of reaching areas that parent drugs may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. The HPPs can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.

摘要翻译： 本发明提供了1H-咪唑并[4,5-c]喹啉-4-胺和1H-咪唑并[4,5-c]喹啉-4-胺的新型高渗透组合物（HPC）或高渗透前药（HPP） 胺相关化合物，其能够穿过具有高穿透效率的生物屏障。 HPP在穿过生物屏障后能够转化为亲本活性药物或药物代谢物，因此可以对母体药物或代谢物可以进行的处理。 此外，HPP能够达到母体药物可能无法进入或在目标区域提供足够浓度的区域，从而进行新的治疗。 HPP可以通过各种施用途径施用于受试者，例如局部递送至具有高浓度或系统地施用于生物受试者的病症的作用部位并以更快的速率进入总体循环。

公开(公告)号：US20130018029A1

公开(公告)日：2013-01-17

申请号：US13550361

申请日：2012-07-16

申请人： Chongxi YU

发明人： Chongxi YU

IPC分类号： A61K31/43 ,  A61K31/546 ,  A61P31/00 ,  A61P25/00 ,  A61P31/04 ,  A61K31/431 ,  A61K31/545

CPC分类号： C07D499/00 ,  A61P31/04

摘要： The invention provides compositions of novel high penetration compositions (HPC) or high penetration prodrugs (HPP) of antimicrobials and antimicrobial-related compounds, which are capable of crossing biological barriers with high penetration efficiency. The HPPs are capable of being converted to parent active drugs or drug metabolites after crossing the biological barrier and thus can render treatments for the conditions that the parent drugs or metabolites can. Additionally, the HPPs are capable of reaching areas that parent drugs may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. The HPPs can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.

摘要翻译： 本发明提供能够跨越具有高穿透效率的生物屏障的新型高渗透组合物（HPC）或抗高血压前药（HPP）的抗微生物剂和抗微生物相关化合物的组合物。 HPP在穿过生物屏障后能够转化为亲本活性药物或药物代谢物，因此可以对母体药物或代谢物可以进行的处理。 此外，HPP能够达到母体药物可能无法进入或在目标区域提供足够浓度的区域，从而进行新的治疗。 HPP可以通过各种施用途径施用于受试者，例如局部递送至具有高浓度或系统地施用于生物受试者的病症的作用部位并以更快的速率进入总体循环。

公开(公告)号：US20100021394A1

公开(公告)日：2010-01-28

申请号：US12534096

申请日：2009-07-31

申请人： Chongxi YU

发明人： Chongxi YU

IPC分类号： A61K9/12 ,  C07D471/04 ,  A61K31/437 ,  A61K49/00 ,  A61P35/00 ,  A61P31/00

CPC分类号： C07D471/04 ,  A61K9/0014 ,  A61K31/44 ,  A61K31/4745

摘要： The invention provides compositions of novel high penetration compositions (HPC) or high penetration prodrugs (HPP) of 1H-imidazo[4,5-c]quinolin-4-amines and 1H-imidazo[4,5-c]quinolin-4-amine-related compounds, which are capable of crossing biological barriers with high penetration efficiency. The HPPs are capable of being converted to parent active drugs or drug metabolites after crossing the biological barrier and thus can render treatments for the conditions that the parent drugs or metabolites can. Additionally, the HPPs are capable of reaching areas that parent drugs may not be able to access or to render a sufficient concentration at the target areas and therefore render novel treatments. The HPPs can be administered to a subject through various administration routes, e.g., locally delivered to an action site of a condition with a high concentration or systematically administered to a biological subject and enter the general circulation with a faster rate.

摘要翻译： 本发明提供了1H-咪唑并[4,5-c]喹啉-4-胺和1H-咪唑并[4,5-c]喹啉-4-胺的新型高渗透组合物（HPC）或高渗透前药（HPP） 胺相关化合物，其能够穿过具有高穿透效率的生物屏障。 HPP在穿过生物屏障后能够转化为亲本活性药物或药物代谢物，因此可以对母体药物或代谢物可以进行的处理。 此外，HPP能够达到母体药物可能无法进入或在目标区域提供足够浓度的区域，从而进行新的治疗。 HPP可以通过各种施用途径施用于受试者，例如局部递送至具有高浓度或系统地施用于生物受试者的病症的作用部位并以更快的速率进入总体循环。