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.

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：US09434725B2

公开(公告)日：2016-09-06

申请号：US13927278

申请日：2013-06-26

Applicant: Genentech, Inc.

Inventor： Steven Do ,  Huiyong Hu ,  Aleksandr Kolesnikov ,  Vickie H. Tsui ,  Xiaojing Wang

IPC: C07D471/04 ,  C07D471/10 ,  C07D487/10 ,  C07D491/052 ,  A61K31/496 ,  A61K31/551 ,  A61K31/4545 ,  A61K31/497 ,  A61K31/513 ,  A61K31/444 ,  A61K31/55 ,  A61K45/06 ,  A61K31/501

CPC classification number: C07D471/04 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/497 ,  A61K31/501 ,  A61K31/513 ,  A61K31/55 ,  A61K31/551 ,  A61K45/06 ,  C07D471/10 ,  C07D487/10 ,  C07D491/052

Abstract: 5-Azaindazole compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, are useful for inhibiting Pim kinase, and for treating disorders such as cancer mediated by Pim kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.

公开(公告)号：US20160159797A1

公开(公告)日：2016-06-09

申请号：US15044231

申请日：2016-02-16

Applicant: Genentech, Inc.

Inventor： Steven Do ,  Huiyong Hu ,  Aleksandr Kolesnikov ,  Wendy Lee ,  Vickie Hsiao-Wei Tsui ,  Xiaojing Wang ,  Zhaoyang Wen

IPC: C07D471/04 ,  A61K31/497 ,  A61K31/506 ,  A61K45/06 ,  A61K31/55 ,  A61K31/551 ,  C07D519/00 ,  A61K31/4995 ,  A61K31/437 ,  A61K31/496

CPC classification number: C07D471/04 ,  A61K31/437 ,  A61K31/496 ,  A61K31/497 ,  A61K31/4995 ,  A61K31/506 ,  A61K31/55 ,  A61K31/551 ,  A61K45/06 ,  C07D231/00 ,  C07D519/00

Abstract: Pyrazolo[3,4-c]pyridine compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, wherein R1 and R2 are as defined herein, are useful for inhibiting Pim kinase, and for treating disorders such as cancer mediated by Pim kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.

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：US20140005168A1

公开(公告)日：2014-01-02

申请号：US13927278

申请日：2013-06-26

Applicant: Genentech, Inc.

Inventor： Steven Do ,  Huiyong Hu ,  Aleksandr Kolesnikov ,  Vickie H. Tsui ,  Xiaojing Wang

IPC: C07D471/04 ,  A61K31/551 ,  A61K31/4545 ,  A61K31/497 ,  A61K31/513 ,  C07D491/052 ,  A61K31/55 ,  C07D471/10 ,  C07D487/10 ,  A61K45/06 ,  A61K31/501 ,  A61K31/496 ,  A61K31/444

CPC classification number: C07D471/04 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/497 ,  A61K31/501 ,  A61K31/513 ,  A61K31/55 ,  A61K31/551 ,  A61K45/06 ,  C07D471/10 ,  C07D487/10 ,  C07D491/052

Abstract: 5-Azaindazole compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, are useful for inhibiting Pim kinase, and for treating disorders such as cancer mediated by Pim kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.

Abstract translation: 式I的5-氮杂吲唑化合物，包括立体异构体，几何异构体，互变异构体及其药学上可接受的盐，可用于抑制Pim激酶和用于治疗由Pim激酶介导的癌症等疾病。 公开了使用式I化合物在体外，原位和体内诊断，预防或治疗哺乳动物细胞或相关病理状况中的这种病症的方法。

公开(公告)号：US20230133817A1

公开(公告)日：2023-05-04

申请号：US18063173

申请日：2022-12-08

Applicant: RQX Pharmaceuticals, Inc. ,  Genentech, Inc.

Inventor： Yongsheng Chen ,  Peter Andrew Smith ,  Tuker 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 ,  Zhiyong Yu

IPC: C07D245/04 ,  C07K5/02 ,  A61K38/06 ,  A61K38/07 ,  A61K38/08 ,  A61K45/06 ,  A61K31/496 ,  A61K31/546 ,  C07K5/087 ,  C07K5/103 ,  C07K5/11 ,  C07K7/06 ,  C07K7/08 ,  C07K5/113 ,  C07K9/00 ,  C07K5/117 ,  A61K31/395 ,  A61K31/431 ,  A61K31/407 ,  A61K31/43 ,  A61K31/4196 ,  A61K31/545 ,  C07K5/09 ,  A61P31/04 ,  A61K9/00

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：US09850239B2

公开(公告)日：2017-12-26

申请号：US15044231

申请日：2016-02-16

Applicant: Genentech, Inc.

Inventor： Steven Do ,  Huiyong Hu ,  Aleksandr Kolesnikov ,  Wendy Lee ,  Vickie Hsiao-Wei Tsui ,  Xiaojing Wang ,  Zhaoyang Wen

IPC: C07D471/04 ,  A61K31/437 ,  A61K31/496 ,  A61K31/497 ,  A61K31/4995 ,  A61K31/506 ,  A61K31/55 ,  A61K31/551 ,  A61K45/06 ,  C07D519/00 ,  C07D231/00

CPC classification number: C07D471/04 ,  A61K31/437 ,  A61K31/496 ,  A61K31/497 ,  A61K31/4995 ,  A61K31/506 ,  A61K31/55 ,  A61K31/551 ,  A61K45/06 ,  C07D231/00 ,  C07D519/00

Abstract: Pyrazolo[3,4-c]pyridine compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, wherein R1 and R2 are as defined herein, are useful for inhibiting Pim kinase, and for treating disorders such as cancer mediated by Pim kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.