公开(公告)号：US20190185511A1

公开(公告)日：2019-06-20

申请号：US16315612

申请日：2017-07-01

Applicant: ADURO BIOTECH, INC. ,  NOVARTIS AG

Inventor： David Braun KANNE ,  Chudi Obioma NDUBAKU ,  Jacob Robert BRUML ,  Thanh Ngoc Lan LE ,  Jeffrey MCKENNA ,  George Scott TRIA ,  Stephen CANHAM

IPC: C07H21/00 ,  C12N15/113 ,  A61P35/00 ,  A61K9/00 ,  A61P1/00 ,  A61P17/06 ,  A61P3/10 ,  A61P37/06 ,  A61P31/00

CPC classification number: C07H21/00 ,  A61K9/0019 ,  A61K45/06 ,  A61P1/00 ,  A61P3/10 ,  A61P17/06 ,  A61P31/00 ,  A61P35/00 ,  A61P37/06 ,  C12N15/113

Abstract: The present invention provides highly active locked nucleic acid cyclic-dinucleotide (LNA-CDN) immune stimulators that activate DCs via the cytoplasmic receptor known as STING (Stimulator of Interferon Genes). In particular, the LNA-CDNs of the present invention are provided in the form of a composition comprising one or more cyclic dinucleotides that induce human STING-dependent type I interferon production, wherein the cyclic dinucleotides present in the composition have at least one 2′, 4′ locked nucleic acids within the cyclic dinucleotide.

公开(公告)号：US20180169063A1

公开(公告)日：2018-06-21

申请号：US15898561

申请日：2018-02-17

Applicant: NOVARTIS AG

Inventor： Heather Elizabeth BURKS ,  Michael A. DECHANTSREITER ,  Guo HE ,  Jill NUNEZ ,  Stefan PEUKERT ,  Clayton SPRINGER ,  Yingchuan SUN ,  Noel Marie-France THOMSEN ,  George Scott TRIA ,  Bing YU

IPC: A61K31/381 ,  A61K45/06 ,  C07D409/04 ,  A61K31/4436 ,  A61K31/4245 ,  A61K31/422 ,  A61K31/4196 ,  C07D413/12 ,  C07D413/04 ,  C07D409/12 ,  C07D333/66 ,  C07D333/64 ,  A61K31/5377 ,  A61K31/404 ,  A61K31/41 ,  A61K31/428 ,  A61K31/397 ,  A61K31/4025 ,  A61K31/4745 ,  C07D417/12 ,  C07D409/10 ,  A61K31/506

CPC classification number: A61K31/381 ,  A61K31/397 ,  A61K31/4025 ,  A61K31/404 ,  A61K31/41 ,  A61K31/4196 ,  A61K31/422 ,  A61K31/4245 ,  A61K31/428 ,  A61K31/4436 ,  A61K31/4745 ,  A61K31/506 ,  A61K31/5377 ,  A61K45/06 ,  A61P35/00 ,  C07D333/64 ,  C07D333/66 ,  C07D409/04 ,  C07D409/10 ,  C07D409/12 ,  C07D413/04 ,  C07D413/12 ,  C07D417/12

Abstract: The present invention relates to compounds of formula I: in which n, m, X, Y1, R1, R2, R3, R4 and R5 are defined in the Summary of the Invention; capable of being both potent antagonists and degraders of estrogen receptors. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of diseases or disorders associated with aberrant estrogen receptor activity.

公开(公告)号：US20170112805A1

公开(公告)日：2017-04-27

申请号：US15399562

申请日：2017-01-05

Applicant: NOVARTIS AG

Inventor： Heather Elizabeth BURKS ,  Michael A. DECHANTSREITER ,  Guo HE ,  Jill NUNEZ ,  Stefan PEUKERT ,  Clayton SPRINGER ,  Yingchuan SUN ,  Noel Marie-France THOMSEN ,  George Scott TRIA ,  Bing YU

IPC: A61K31/381 ,  A61K31/4745 ,  A61K45/06 ,  A61K31/5377

CPC classification number: A61K31/381 ,  A61K31/397 ,  A61K31/4025 ,  A61K31/404 ,  A61K31/41 ,  A61K31/4196 ,  A61K31/422 ,  A61K31/4245 ,  A61K31/428 ,  A61K31/4436 ,  A61K31/4745 ,  A61K31/506 ,  A61K31/5377 ,  A61K45/06 ,  A61P35/00 ,  C07D333/64 ,  C07D333/66 ,  C07D409/04 ,  C07D409/10 ,  C07D409/12 ,  C07D413/04 ,  C07D413/12 ,  C07D417/12

Abstract: The present invention relates to compounds of formula I: in which n, m, X, Y1, R1, R2, R3, R4 and R5 are defined in the Summary of the Invention; capable of being both potent antagonists and degraders of estrogen receptors. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of diseases or disorders associated with aberrant estrogen receptor activity.