公开(公告)号：US20240239790A1

公开(公告)日：2024-07-18

申请号：US18279379

申请日：2022-03-10

申请人： adMare Therapeutics Society ,  LifeArc ,  Provincial Health Services Authority

发明人： Stephen Paul Arns ,  Tom Han Hsiao Hsieh ,  Fahimeh S. Shidmoossavee ,  Jason Samuel Tan ,  Leanna Yee ,  Jay John Paquette ,  James Brian Jaquith ,  Simon Andrew Osborne ,  Ela Smiljanic-Hurley ,  Callum Hamby ,  Elliott Smyth ,  Martin Ambler ,  Andrew I. Minchinton ,  Alastair H. Kyle ,  Jennifer H.E. Baker

IPC分类号： C07D471/04 ,  A61K31/5377 ,  A61K31/5386 ,  A61K31/541 ,  A61K31/55 ,  A61K45/06 ,  A61K48/00 ,  A61P35/00 ,  C07D519/00 ,  C12N9/22 ,  C12N15/11 ,  C12N15/63

CPC分类号： C07D471/04 ,  A61K31/5377 ,  A61K31/5386 ,  A61K31/541 ,  A61K31/55 ,  A61K45/06 ,  A61K48/005 ,  A61P35/00 ,  C07D519/00 ,  C12N9/22 ,  C12N15/111 ,  C12N15/63 ,  C12N2310/20

摘要： The present disclosure provides compounds and methods for inhibiting DNA-dependent protein kinase (DNA-PK). Aspects of the present disclosure also include methods of using the compounds to treat diseases, including, but not limited to, cancer. In certain embodiments, the compounds inhibit DNA-PK and thus sensitize cancers to therapies such as chemotherapy and radiotherapy. Certain compounds of the present disclosure are in the form of prodrugs that release the DNA-PK inhibitor in hypoxic tissue such as is known to occur in cancers. Aspects of the present disclosure also include methods of using the compounds for repairing a DNA break in a target genomic region or for modifying expression of one or more genes or proteins. Compounds provided are of formula: (II)

公开(公告)号：US20240246960A1

公开(公告)日：2024-07-25

申请号：US18279377

申请日：2022-03-10

申请人： adMare Therapeutics Society ,  LifeArc ,  Provincial Health Services Authority

发明人： Stephen Paul Arns ,  Tom Han Hsiao Hsieh ,  Fahimeh S. Shidmoossavee ,  Jason Samuel Tan ,  Leanna Yee ,  Jay John Paquette ,  James Brian Jaquith ,  Simon Andrew Osborne ,  Ela Smiljanic-Hurley ,  Callum Hamby ,  Elliott Smyth ,  Martin Ambler ,  Andrew I. Minchinton ,  Alastair H. Kyle ,  Jennifer H.E. Baker

IPC分类号： C07D471/04 ,  A61K31/5377 ,  A61K45/06 ,  A61P35/00 ,  C07D519/00 ,  C12N9/22 ,  C12N9/99 ,  C12N15/11

CPC分类号： C07D471/04 ,  A61K31/5377 ,  A61K45/06 ,  A61P35/00 ,  C07D519/00 ,  C12N9/22 ,  C12N9/99 ,  C12N15/111 ,  C12N2310/20

摘要： The present disclosure provides compounds and methods for inhibiting DNA-dependent protein kinase (DNA-PK). Aspects of the present disclosure also include methods of using the compounds to treat diseases, including, but not limited to, cancer. In certain embodiments, the compounds inhibit DNA-PK and thus sensitize cancers to therapies such as chemotherapy and radiotherapy. Certain compounds of the present disclosure are in the form of prodrugs that release the DNA-PK inhibitor in hypoxic tissue such as is known to occur in cancers. Aspects of the present disclosure also include methods of using the compounds for repairing a DNA break in a target genomic region or for modifying expression of one or more genes or proteins. Compounds provided are of formula.