公开(公告)号：US09441005B2

公开(公告)日：2016-09-13

申请号：US14279416

申请日：2014-05-16

Applicant: The University of Kansas

Inventor： Sunil A. David ,  Nikunj M. Shukla

IPC: C07H15/26 ,  C07D471/04 ,  C07D495/04 ,  C07D519/00 ,  C07F5/02

CPC classification number: C07D471/04 ,  A61K39/385 ,  A61K39/39 ,  C07D495/04 ,  C07D519/00 ,  C07F5/022 ,  C07F5/025 ,  C07H15/26 ,  C07K17/02 ,  C08B37/00 ,  G01N21/64 ,  G01N33/53

Abstract: The present disclosure provides novel imidazoquinoline derived compounds, derivatives thereof, analogues thereof, and pharmaceutically acceptable salts thereof, and methods of making and using such compounds. The present disclosure also provides TLR7 agonists and TLR7/TLR8 dual agonists, probes, tissue-specific molecules, adjuvants, immunogenic compositions, therapeutic compositions, and self-adjuvanting vaccines including the imidazoquinoline derived compounds, derivatives thereof, analogues thereof, and pharmaceutically acceptable salts thereof. Derivatives of the imidazoquinoline derived compounds also include dendrimers and dimers of the imidazoquinoline derived compounds, and methods of making and using the dendrimeic and dimeric imidazoquinoline derived compounds. The present disclosure also provides dual TLR2/TLR7 hybrid agonists that include imidazoquinoline derived compounds of the present disclosure.

Abstract translation: 本公开提供了新的咪唑并喹啉衍生的化合物，其衍生物，其类似物及其药学上可接受的盐，以及制备和使用这些化合物的方法。 本公开还提供TLR7激动剂和TLR7 / TLR8双重激动剂，探针，组织特异性分子，佐剂，免疫原性组合物，治疗组合物和自我佐剂疫苗，包括咪唑并喹啉衍生的化合物，其衍生物，其类似物和药学上可接受的盐 其中。 咪唑并喹啉衍生化合物的衍生物还包括咪唑并喹啉衍生化合物的树枝状大分子和二聚体，以及制备和使用树枝状和二聚咪唑并喹啉衍生化合物的方法。 本公开还提供了包含本发明的咪唑并喹啉衍生化合物的双重TLR2 / TLR7混合激动剂。

公开(公告)号：US20180134701A1

公开(公告)日：2018-05-17

申请号：US15848349

申请日：2017-12-20

Applicant: The University of Kansas

Inventor： Sunil A. David ,  Nikunj M. Shukla

IPC: C07D471/04 ,  C07F5/02 ,  A61K39/39 ,  C07D495/04 ,  C07D519/00 ,  C07H15/26 ,  A61K39/385 ,  C07K17/02 ,  C08B37/00 ,  G01N21/64 ,  G01N33/53

CPC classification number: C07D471/04 ,  A61K39/385 ,  A61K39/39 ,  C07D495/04 ,  C07D519/00 ,  C07F5/022 ,  C07F5/025 ,  C07H15/26 ,  C07K17/02 ,  C08B37/00 ,  G01N21/64 ,  G01N33/53

Abstract: The present disclosure provides novel imidazoquinoline derived compounds, derivatives thereof, analogues thereof, and pharmaceutically acceptable salts thereof, and methods of making and using such compounds. The present disclosure also provides TLR7 agonists and TLR7/TLR8 dual agonists, probes, tissue-specific molecules, adjuvants, immunogenic compositions, therapeutic compositions, and self-adjuvanting vaccines including the imidazoquinoline derived compounds, derivatives thereof, analogues thereof, and pharmaceutically acceptable salts thereof. Derivatives of the imidazoquinoline derived compounds also include dendrimers and dimers of the imidazoquinoline derived compounds, and methods of making and using the dendrimeric and dimeric imidazoquinoline derived compounds. The present disclosure also provides dual TLR2/TLR7 hybrid agonists that include imidazoquinoline derived compounds of the present disclosure.

公开(公告)号：US20170029421A1

公开(公告)日：2017-02-02

申请号：US15230708

申请日：2016-08-08

Applicant: The University of Kansas

Inventor： Sunil A. David ,  Nikunj M. Shukla

IPC: C07D471/04 ,  C07H15/26 ,  C07D519/00 ,  C07F5/02

CPC classification number: C07D471/04 ,  A61K39/385 ,  A61K39/39 ,  C07D495/04 ,  C07D519/00 ,  C07F5/022 ,  C07F5/025 ,  C07H15/26 ,  C07K17/02 ,  C08B37/00 ,  G01N21/64 ,  G01N33/53

Abstract: The present disclosure provides novel imidazoquinoline derived compounds, derivatives thereof, analogues thereof, and pharmaceutically acceptable salts thereof, and methods of making and using such compounds. The present disclosure also provides TLR7 agonists and TLR7/TLR8 dual agonists, probes, tissue-specific molecules, adjuvants, immunogenic compositions, therapeutic compositions, and self-adjuvanting vaccines including the imidazoquinoline derived compounds, derivatives thereof, analogues thereof, and pharmaceutically acceptable salts thereof. Derivatives of the imidazoquinoline derived compounds also include dendrimers and dimers of the imidazoquinoline derived compounds, and methods of making and using the dendrimeic and dimeric imidazoquinoline derived compounds. The present disclosure also provides dual TLR2/TLR7 hybrid agonists that include imidazoquinoline derived compounds of the present disclosure.

Abstract translation: 本公开提供了新的咪唑并喹啉衍生的化合物，其衍生物，其类似物及其药学上可接受的盐，以及制备和使用这些化合物的方法。 本公开还提供TLR7激动剂和TLR7 / TLR8双重激动剂，探针，组织特异性分子，佐剂，免疫原性组合物，治疗组合物和自我佐剂疫苗，包括咪唑并喹啉衍生的化合物，其衍生物，其类似物和药学上可接受的盐 其中。 咪唑并喹啉衍生化合物的衍生物还包括咪唑并喹啉衍生化合物的树枝状大分子和二聚体，以及制备和使用树枝状和二聚咪唑并喹啉衍生化合物的方法。 本公开还提供了包含本发明的咪唑并喹啉衍生化合物的双重TLR2 / TLR7混合激动剂。

公开(公告)号：US10208037B2

公开(公告)日：2019-02-19

申请号：US15848349

申请日：2017-12-20

Applicant: The University of Kansas

Inventor： Sunil A. David ,  Nikunj M. Shukla

IPC: C07D471/04 ,  C07D519/00 ,  C07D495/04 ,  C07F5/02 ,  C07H15/26 ,  A61K39/385 ,  A61K39/39 ,  C07K17/02 ,  C08B37/00 ,  G01N21/64 ,  G01N33/53

Abstract: The present disclosure provides novel imidazoquinoline derived compounds, derivatives thereof, analogues thereof, and pharmaceutically acceptable salts thereof, and methods of making and using such compounds. The present disclosure also provides TLR7 agonists and TLR7/TLR8 dual agonists, probes, tissue-specific molecules, adjuvants, immunogenic compositions, therapeutic compositions, and self-adjuvanting vaccines including the imidazoquinoline derived compounds, derivatives thereof, analogues thereof, and pharmaceutically acceptable salts thereof. Derivatives of the imidazoquinoline derived compounds also include dendrimers and dimers of the imidazoquinoline derived compounds, and methods of making and using the dendrimeric and dimeric imidazoquinoline derived compounds. The present disclosure also provides dual TLR2/TLR7 hybrid agonists that include imidazoquinoline derived compounds of the present disclosure.

公开(公告)号：US20170260184A1

公开(公告)日：2017-09-14

申请号：US15607960

申请日：2017-05-30

Applicant: The University of Kansas

Inventor： Sunil A. David ,  Nikunj M. Shukla

IPC: C07D471/04 ,  C07D519/00 ,  A61K39/39 ,  C07H15/26 ,  A61K39/385 ,  C07D495/04 ,  C07F5/02

CPC classification number: C07D471/04 ,  A61K39/385 ,  A61K39/39 ,  C07D495/04 ,  C07D519/00 ,  C07F5/022 ,  C07F5/025 ,  C07H15/26 ,  C07K17/02 ,  C08B37/00 ,  G01N21/64 ,  G01N33/53

Abstract: The present disclosure provides novel imidazoquinoline derived compounds, derivatives thereof, analogues thereof, and pharmaceutically acceptable salts thereof, and methods of making and using such compounds. The present disclosure also provides TLR7 agonists and TLR7/TLR8 dual agonists, probes, tissue-specific molecules, adjuvants, immunogenic compositions, therapeutic compositions, and self-adjuvanting vaccines including the imidazoquinoline derived compounds, derivatives thereof, analogues thereof, and pharmaceutically acceptable salts thereof. Derivatives of the imidazoquinoline derived compounds also include dendrimers and dimers of the imidazoquinoline derived compounds, and methods of making and using the dendrimeic and dimeric imidazoquinoline derived compounds. The present disclosure also provides dual TLR2/TLR7 hybrid agonists that include imidazoquinoline derived compounds of the present disclosure.