公开(公告)号：US11248012B2

公开(公告)日：2022-02-15

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：US10882876B2

公开(公告)日：2021-01-05

申请号：US16459776

申请日：2019-07-02

Applicant: GlaxoSmithKline Biologicals SA

Inventor： Helene G. Bazin-Lee ,  David A. Johnson

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

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

公开(公告)号：US10351582B2

公开(公告)日：2019-07-16

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 ,  A61P17/12 ,  A61P31/20 ,  A61P31/14 ,  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：US11274115B2

公开(公告)日：2022-03-15

申请号：US16330599

申请日：2017-09-05

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：US10774099B2

公开(公告)日：2020-09-15

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: C07F9/10 ,  C07F9/6558 ,  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.