公开(公告)号：US20210024553A1

公开(公告)日：2021-01-28

申请号：US16989235

申请日：2020-08-10

Applicant: GLAXOSMITHKLINE BIOLOGICALS SA

Inventor： Helene G. BAZIN-LEE ,  Laura S. BESS ,  David A. JOHNSON

IPC: C07F9/6558 ,  C07F9/10 ,  C07F9/6561

Abstract: The present invention relates to a process for phospholipidation of imidazoquinolines and oxoadenines. More particularly, the present invention relates to a high-yielding and scalable procedure for the phospholipidation of imidazoquinolines and oxoadenines which obviates the need to isolate unstable phosphoramidite intermediates. This process may be used for the phospholipidation of toll-like receptor 7 (TLR7)-active and toll-like receptor (TLR8)-active imidazoquinolines and oxoadenines.

公开(公告)号：US20220144833A1

公开(公告)日：2022-05-12

申请号：US17582176

申请日：2022-01-24

Applicant: GLAXOSMITHKLINE BIOLOGICALS SA

Inventor： Helene G. BAZIN-LEE ,  Jay T. EVANS ,  David BURKHART ,  Michael COCHRAN ,  David A. JOHNSON

IPC: C07D471/04

Abstract: This invention relates inter alia to novel imidazoquinoline derivatives and their use in therapy, particularly as vaccine adjuvants.

公开(公告)号：US20180362560A1

公开(公告)日：2018-12-20

申请号：US15781905

申请日：2016-12-12

Applicant: GLAXOSMITHKLINE BIOLOGICALS, SA

Inventor： Helene G. BAZIN-LEE ,  David A. JOHNSON

IPC: C07F9/6561 ,  A61P31/14 ,  A61P31/20 ,  A61P35/00 ,  A61P17/12

CPC classification number: C07F9/6561 ,  A61P17/12 ,  A61P31/14 ,  A61P31/20 ,  A61P35/00

Abstract: The present invention provides novel phospholipidated imidazoquinolines of formula (I) as TLR7 and TLR8 agonists, pharmaceutical compositions, therapeutic uses and processes for preparing the same.

公开(公告)号：US20220144865A1

公开(公告)日：2022-05-12

申请号：US17582150

申请日：2022-01-24

Applicant: GLAXOSMITHKLINE BIOLOGICALS SA

Inventor： Helene G. BAZIN-LEE ,  Jay T. EVANS ,  David BURKHART ,  Michael COCHRAN ,  David A. JOHNSON

IPC: C07F9/6561

Abstract: This invention relates inter alia to novel imidazoquinoline derivatives and their use in therapy, particularly as vaccine adjuvants.

公开(公告)号：US20180273560A1

公开(公告)日：2018-09-27

申请号：US16060142

申请日：2016-12-12

Applicant: GLAXOSMITHKLINE BIOLOGICALS, SA

Inventor： Helene G. BAZIN-LEE ,  Laura S. BESS ,  David A. JOHNSON

IPC: C07F9/6558 ,  C07F9/6561 ,  C07F9/10

Abstract: The present invention relates to a process for phospholipidation of imidazoquinolines and oxoadenines. More particularly, the present invention relates to a high-yielding and scalable procedure for the phospholipidation of imidazoquinolines and oxoadenines which obviates the need to isolate unstable phosphoramidite intermediates. This process may be used for the phospholipidation of toll-like receptor 7 (TLR7)-active and toll-like receptor (TLR8)-active imidazoquinolines and oxoadenines.

公开(公告)号：US20220119428A1

公开(公告)日：2022-04-21

申请号：US17566247

申请日：2021-12-30

Applicant: GLAXOSMITHKLINE BIOLOGICALS SA

Inventor： Helene G. BAZIN-LEE ,  Laura S. BESS ,  David A. JOHNSON

IPC: C07F9/6558 ,  C07F9/10 ,  C07F9/6561

Abstract: The present invention relates to a process for phospholipidation of imidazoquinolines and oxoadenines. More particularly, the present invention relates to a high-yielding and scalable procedure for the phospholipidation of imidazoquinolines and oxoadenines which obviates the need to isolate unstable phosphoramidite intermediates. This process may be used for the phospholipidation of toll-like receptor 7 (TLR7)—active and toll-like receptor (TLR8)—active imidazoquinolines and oxoadenines.