公开(公告)号：US10392422B2

公开(公告)日：2019-08-27

申请号：US15312614

申请日：2015-05-19

Applicant: RQX PHARMACEUTICALS, INC. ,  GENENTECH, INC.

Inventor： Tucker Curran Roberts ,  Peter Andrew Smith ,  Robert I. Higuchi ,  Prasuna Paraselli ,  Philippe Bergeron ,  Michael F. T. Koehler ,  Huiyong Hu ,  Jacob Bradley Schwarz ,  Cuong Ly ,  James John Crawford

IPC: A61K38/00 ,  C07K5/103 ,  C07K7/06 ,  C07K7/08 ,  C07K5/02 ,  C07K5/087 ,  C07K5/09 ,  C07K5/11 ,  A61K45/06 ,  A61K31/395 ,  A61K31/407 ,  A61K31/4196 ,  A61K31/43 ,  A61K31/431 ,  A61K31/496 ,  A61K31/545 ,  A61K31/546 ,  A61K38/06 ,  A61K38/07 ,  A61K38/08 ,  C07K5/083 ,  A61K38/12

Abstract: Provided herein are antibacterial compounds, wherein the compounds in some embodiments have broad spectrum bioactivity. In various embodiments, the compounds act by inhibition of bacterial type 1 signal peptidase (SpsB), an essential protein in bacteria. Pharmaceutical compositions and methods for treatment using the compounds described herein are also provided.

公开(公告)号：US11072635B2

公开(公告)日：2021-07-27

申请号：US15777509

申请日：2016-11-21

Applicant: RQX PHARMACEUTICALS, INC. ,  GENENTECH, INC.

Inventor： Yongsheng Chen ,  Peter Andrew Smith ,  Tucker Curran Roberts ,  Robert I. Higuchi ,  Prasuna Paraselli ,  Michael F. T. Koehler ,  Jacob Bradley Schwarz ,  James John Crawford ,  Cuong Q. Ly ,  Huiyong Hu ,  Zhiyong Yu

IPC: C07K7/06 ,  A61P31/04 ,  A61K9/00 ,  A61K45/06

Abstract: Provided herein are antibacterial compounds, wherein the compounds in some embodiments have broad spectrum bioactivity. In various embodiments, the compounds act by inhibition of bacterial type 1 signal peptidase (SpsB), an essential protein in bacteria. Pharmaceutical compositions and methods for treatment using the compounds described herein are also provided.

公开(公告)号：US09790183B2

公开(公告)日：2017-10-17

申请号：US15015586

申请日：2016-02-04

Applicant: GENENTECH, INC. ,  CURIS, INC.

Inventor： Janet L. Gunzner-Toste ,  Daniel Sutherlin ,  Mark S. Stanley ,  Liang Bao ,  Georgette M. Castanedo ,  Rebecca L. Lalonde ,  Shumei Wang ,  Mark E. Reynolds ,  Scott J. Savage ,  Kimberly Malesky ,  Michael S. Dina ,  Michael F. T. Koehler

IPC: C07D213/16 ,  C07D401/12 ,  A61K31/44 ,  C07D213/38 ,  C07D213/40 ,  C07D213/56 ,  C07D213/70 ,  C07D213/75 ,  C07D213/81 ,  C07D213/82 ,  C07D401/14 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/04 ,  C07D417/12 ,  C07F9/58

CPC classification number: C07D213/16 ,  C07D213/38 ,  C07D213/40 ,  C07D213/56 ,  C07D213/70 ,  C07D213/75 ,  C07D213/81 ,  C07D213/82 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/04 ,  C07D417/12 ,  C07F9/58

Abstract: The invention provides novel inhibitors of hedgehog signaling that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula I: wherein A, X, Y R1, R2, R3, R4, m and n are as described herein.

公开(公告)号：US11208387B2

公开(公告)日：2021-12-28

申请号：US16884679

申请日：2020-05-27

Applicant: Genentech, Inc.

Inventor： Michael F. T. Koehler ,  Peter Andrew Smith ,  Dana Winter ,  Boubacar Sow ,  Claudio Sturino ,  Guillaume Pelletier ,  Jonathan Boudreault

IPC: A61K31/505 ,  C07D239/28 ,  C07D239/42 ,  A61K45/06 ,  A61P31/04 ,  A61K31/702 ,  A61K31/4709 ,  A61K38/14 ,  A61K31/497 ,  A61K31/165 ,  A61K31/351 ,  A61K38/12 ,  A61K31/5377 ,  A61K31/545

Abstract: Provided herein are antibacterial compounds, wherein the compounds in some embodiments have broad spectrum bioactivity. In various embodiments, the compounds act by inhibition of bacterial type 1 signal peptidases SpsB and/or LepB, an essential protein in bacteria. Pharmaceutical compositions and methods for treatment using the compounds described herein are also provided.

公开(公告)号：US10351595B2

公开(公告)日：2019-07-16

申请号：US15312614

申请日：2015-05-19

Applicant: RQX PHARMACEUTICALS, INC. ,  GENENTECH, INC.

Inventor： Tucker Curran Roberts ,  Peter Andrew Smith ,  Robert I. Higuchi ,  Prasuna Paraselli ,  Philippe Bergeron ,  Michael F. T. Koehler ,  Huiyong Hu ,  Jacob Bradley Schwarz ,  Cuong Ly ,  James John Crawford

IPC: A61K38/00 ,  C07K5/103 ,  C07K7/06 ,  C07K7/08 ,  C07K5/02 ,  C07K5/087 ,  C07K5/09 ,  C07K5/11 ,  A61K45/06 ,  A61K31/395 ,  A61K31/407 ,  A61K31/4196 ,  A61K31/43 ,  A61K31/431 ,  A61K31/496 ,  A61K31/545 ,  A61K31/546 ,  A61K38/06 ,  A61K38/07 ,  A61K38/08 ,  C07K5/083 ,  A61K38/12

Abstract: Provided herein are antibacterial compounds, wherein the compounds in some embodiments have broad spectrum bioactivity. In various embodiments, the compounds act by inhibition of bacterial type 1 signal peptidase (SpsB), an essential protein in bacteria. Pharmaceutical compositions and methods for treatment using the compounds described herein are also provided.

公开(公告)号：US09321761B2

公开(公告)日：2016-04-26

申请号：US14575018

申请日：2014-12-18

Applicant: GENENTECH, INC. ,  CURIS, INC.

Inventor： Janet L. Gunzner-Toste ,  Daniel Sutherlin ,  Mark S. Stanley ,  Liang Bao ,  Georgette M. Castanedo ,  Rebecca L. LaLonde ,  Shumei Wang ,  Mark E. Reynolds ,  Scott J. Savage ,  Kimberly Malesky ,  Michael S. Dina ,  Michael F. T. Koehler

IPC: C07D413/12 ,  C07D417/04 ,  C07D417/12 ,  C07D213/38 ,  C07D213/40 ,  C07D213/56 ,  C07D213/70 ,  C07D213/75 ,  C07D213/81 ,  C07D213/82 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D409/12 ,  C07F9/58

CPC classification number: C07D213/16 ,  C07D213/38 ,  C07D213/40 ,  C07D213/56 ,  C07D213/70 ,  C07D213/75 ,  C07D213/81 ,  C07D213/82 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/04 ,  C07D417/12 ,  C07F9/58

Abstract: The invention provides novel inhibitors of hedgehog signaling that are useful as a therapeutic agents for treating malignancies where the compounds have the general formula I: wherein A, X, Y R1, R2, R3, R4, m and n are as described herein.

Abstract translation: 本发明提供了可用作治疗恶性肿瘤的治疗剂的刺猬蛋白信号传导的新型抑制剂，其中化合物具有通式I：其中A，X，Y R1，R2，R3，R4，m和n如本文所述。

公开(公告)号：US20230133667A1

公开(公告)日：2023-05-04

申请号：US18047624

申请日：2022-10-18

Applicant: RQx Pharmaceuticals, Inc. ,  Genentech, Inc.

Inventor： Peter Andrew Smith ,  Tucker Curran Roberts ,  Robert I. Higuchi ,  Prasuna Paraselli ,  Michael F. T. Koehler ,  Jacob Bradley Schwarz ,  James John Crawford ,  Cuong Q. Ly ,  Emily J. Hanan ,  Huiyong Hu ,  Yongsheng Chen ,  Zhiyong Yu ,  Paul Colin Michael Winship ,  Calum MacCleod ,  Toby Blench

IPC: C07K5/11 ,  A61P31/04 ,  A61K9/00 ,  A61K38/06 ,  A61K38/07 ,  A61K38/08 ,  A61K45/06 ,  C07K5/083 ,  C07K5/097 ,  C07K5/107 ,  C07K7/06

Abstract: Provided herein are antibacterial compounds, wherein the compounds in some embodiments have broad spectrum bioactivity. In various embodiments, the compounds act by inhibition of bacterial type 1 signal peptidase (SpsB), an essential protein in bacteria. Pharmaceutical compositions and methods for treatment using the compounds described herein are also provided.