公开(公告)号：US09321746B2

公开(公告)日：2016-04-26

申请号：US14768341

申请日：2014-02-12

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: A61K31/00 ,  C07D333/64 ,  A61K31/381 ,  A61K31/4196 ,  A61K31/422 ,  A61K31/4245 ,  A61K31/4436 ,  A61K31/506 ,  A61K45/06 ,  C07D333/66 ,  C07D409/12 ,  C07D413/04 ,  C07D413/12 ,  C07D409/04 ,  C07D409/10 ,  C07D417/12 ,  A61K31/397 ,  A61K31/4025 ,  A61K31/404 ,  A61K31/41 ,  A61K31/428 ,  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.

Abstract translation: 本发明涉及式I化合物：其中n，m，X，Y 1，R 1，R 2，R 3，R 4和R 5在发明概述中定义; 能够成为雌激素受体的有效拮抗剂和降解物。 本发明还提供了制备本发明化合物的方法，包含这些化合物的药物制剂以及使用这些化合物和组合物来管理与异常雌激素受体活性相关的疾病或病症的方法。

公开(公告)号：US10654828B2

公开(公告)日：2020-05-19

申请号：US16045993

申请日：2018-07-26

Applicant: NOVARTIS AG

Inventor： John Ryan Kerrigan ,  Natalie Dales ,  George Scott Tria ,  Daniel Palacios ,  Paul Gormisky

IPC: C07D401/14 ,  C07D405/14 ,  C07D403/14 ,  C07D471/04 ,  C07D487/04 ,  C07D403/04 ,  A61P25/28 ,  C07D471/08 ,  C07D491/04 ,  A61P21/00 ,  A61P27/16 ,  C07D403/12 ,  C07D498/04

Abstract: The present disclosure provides a compound of formula (I): or a pharmaceutically acceptable salt thereof, and its therapeutic uses for activating a growth factor pathway, promoting wound healing, promoting tissue repair, and treating hearing loss, skeletal muscle loss, organ degeneration, tissue damage, neurodegeneration, and muscular atrophy. The disclosure further provides pharmaceutical compositions and combinations. The present disclosure also relates to the use of such compounds for research or other non-therapeutic purposes.

公开(公告)号：US11098077B2

公开(公告)日：2021-08-24

申请号：US16315612

申请日：2017-07-01

Applicant: CHINOOK THERAPEUTICS, 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 ,  A61K45/06 ,  A61P35/00 ,  A61P17/06 ,  A61P31/00 ,  A61P37/06 ,  A61P3/10 ,  A61P1/00 ,  A61K9/00 ,  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：US10058534B2

公开(公告)日：2018-08-28

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 ,  A61K31/506 ,  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 ,  C07D409/04

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：US09931317B2

公开(公告)日：2018-04-03

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

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：US20190055219A1

公开(公告)日：2019-02-21

申请号：US16045993

申请日：2018-07-26

Applicant: NOVARTIS AG

Inventor： John Ryan Kerrigan ,  Natalie Dales ,  George Scott Tria ,  Daniel Palacios ,  Paul Gormisky

IPC: C07D401/14 ,  C07D405/14 ,  C07D403/12 ,  C07D471/04 ,  C07D498/04 ,  C07D403/14

Abstract: The present disclosure provides a compound of formula (I): or a pharmaceutically acceptable salt thereof, and its therapeutic uses for activating a growth factor pathway, promoting wound healing, promoting tissue repair, and treating hearing loss, skeletal muscle loss, organ degeneration, tissue damage, neurodegeneration, and muscular atrophy. The disclosure further provides pharmaceutical compositions and combinations. The present disclosure also relates to the use of such compounds for research or other non-therapeutic purposes.