公开(公告)号：US10112955B2

公开(公告)日：2018-10-30

申请号：US15337184

申请日：2016-10-28

Applicant: eFFECTOR THERAPEUTICS, INC.

Inventor： Paul A. Sprengeler ,  Siegfried H. Reich ,  Justin T. Ernst ,  Stephen E. Webber ,  Mike Shaghafi ,  Douglas Murphy ,  Chinh Tran

IPC: C07D498/04 ,  C07D403/12 ,  C07D401/12 ,  C07D403/14 ,  C07D239/42 ,  C07D239/49 ,  C07D409/12 ,  C07D417/12 ,  C07D487/04 ,  C07D239/48 ,  C07D409/14 ,  C07D471/04 ,  C07D471/10 ,  C07D473/34 ,  C07D491/107

Abstract: The present invention provides synthesis, pharmaceutically acceptable formulations and uses of compounds in accordance with Formula I, or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof. For Formula I compounds A1, A2, A3, A4, A5, W1, Y, R1, R2, R3, R4, R5, R6a, R6b, R7, R8, R8a, R8b, R9, R9a, R9b, and R10 and subscript “n” are as defined in the specification. The inventive Formula I compounds are inhibitors of Mnk and find utility in any number of therapeutic applications, including but not limited to treatment of inflammation and various cancers.

公开(公告)号：US10000487B2

公开(公告)日：2018-06-19

申请号：US15355271

申请日：2016-11-18

Applicant: eFFECTOR Therapeutics, Inc.

Inventor： Paul A. Sprengeler ,  Seigfried H. Reich ,  Stephen E. Webber ,  Justin T. Ernst

IPC: C07D471/04

CPC classification number: C07D471/04 ,  C07D471/10

Abstract: The present invention provides synthesis, pharmaceutically acceptable formulations and uses of compounds in accordance with Formula IA or Formula IB, as well as stereoisomers, tautomers or pharmaceutically acceptable salts thereof. For Formula IA and Formula IB compounds A1, A2, A3, A4, W1, W2, Y, X, R1, R2, R3, R4a, R4b, R5a, R5b, R6, R7, R8, R9, R9a, R9b, R10 and subscript n are as defined in the specification. The inventive Formula IA and Formula IB compounds are inhibitors of Mnk and find utility in any number of therapeutic applications, including but not limited to treatment of inflammation and various cancers.

公开(公告)号：US09814718B2

公开(公告)日：2017-11-14

申请号：US15611966

申请日：2017-06-02

Applicant: eFFECTOR Therapeutics, Inc.

Inventor： Siegfried H. Reich ,  Paul A. Sprengeler ,  Stephen E. Webber ,  Alan X. Xiang ,  Justin T. Ernst

IPC: C07D471/04 ,  A61K31/506 ,  A61K31/52 ,  A61K31/519 ,  C07D487/04 ,  A61K31/551 ,  C07D519/00 ,  C07D495/20 ,  C07D491/20 ,  C07D471/20 ,  C07D471/10 ,  C07D473/34

CPC classification number: A61K31/506 ,  A61K31/519 ,  A61K31/52 ,  A61K31/551 ,  C07D471/04 ,  C07D471/10 ,  C07D471/20 ,  C07D473/34 ,  C07D487/04 ,  C07D491/20 ,  C07D495/20 ,  C07D519/00

Abstract: The present invention relates to compounds according to Formula (I): or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4a, R4b, R5, R6, R7, R8, W1, W2, Y and n are as defined herein. Also described are pharmaceutically acceptable compositions of Formula I compounds as well as methods for utilizing the compounds of Formula I and the pharmaceutically acceptable compositions of Formula I compounds as inhibitors of Mnk as well as therapeutics for the treatment of diseases such as cancer.

公开(公告)号：US09669031B2

公开(公告)日：2017-06-06

申请号：US15187854

申请日：2016-06-21

Applicant: eFFECTOR Therapeutics, Inc.

Inventor： Siegfried H. Reich ,  Paul A. Sprengeler ,  Stephen E. Webber ,  Alan X. Xiang ,  Justin T. Ernst

IPC: A61K31/506 ,  C07D471/04 ,  C07D471/10 ,  C07D471/20 ,  C07D491/20 ,  C07D495/20 ,  C07D519/00 ,  C07D473/34 ,  C07D487/04 ,  A61K31/519 ,  A61K31/52 ,  A61K31/551

CPC classification number: A61K31/506 ,  A61K31/519 ,  A61K31/52 ,  A61K31/551 ,  C07D471/04 ,  C07D471/10 ,  C07D471/20 ,  C07D473/34 ,  C07D487/04 ,  C07D491/20 ,  C07D495/20 ,  C07D519/00

Abstract: The present invention relates to compounds according to Formula (I): or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4a, R4b, R5, R6, R7, R8, W1, W2, Y and n are as defined herein. Also described are pharmaceutically acceptable compositions of Formula I compounds as well as methods for utilizing the compounds of Formula I and the pharmaceutically acceptable compositions of Formula I compounds as inhibitors of Mnk as well as therapeutics for the treatment of diseases such as cancer.

公开(公告)号：US09382248B2

公开(公告)日：2016-07-05

申请号：US14748990

申请日：2015-06-24

Applicant: eFFECTOR Therapeutics, Inc.

Inventor： Siegfried H. Reich ,  Paul A. Sprengeler ,  Stephen E. Webber ,  Alan X. Xiang ,  Justin T. Ernst

IPC: C07D471/04 ,  C07D471/10 ,  C07D471/20 ,  C07D491/20 ,  C07D495/20 ,  C07D519/00 ,  C07D473/34 ,  C07D487/04

CPC classification number: A61K31/506 ,  A61K31/519 ,  A61K31/52 ,  A61K31/551 ,  C07D471/04 ,  C07D471/10 ,  C07D471/20 ,  C07D473/34 ,  C07D487/04 ,  C07D491/20 ,  C07D495/20 ,  C07D519/00

Abstract: The present invention relates to compounds according to Formula (I): or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4a, R4b, R5, R6, R7, R8, W1, W2, Y and n are as defined herein. Also described are pharmaceutically acceptable compositions of Formula I compounds as well as methods for utilizing the compounds of Formula I and the pharmaceutically acceptable compositions of Formula I compounds as inhibitors of Mnk as well as therapeutics for the treatment of diseases such as cancer.

Abstract translation: 本发明涉及式（I）化合物或其立体异构体，互变异构体或其药学上可接受的盐，其中R1，R2，R3，R4a，R4b，R5，R6，R7，R8，W1，W2，Y和n 如本文所定义。 还描述了式I化合物的药学上可接受的组合物以及利用式I化合物和式I化合物的药学上可接受的组合物作为Mnk抑制剂以及用于治疗诸如癌症的疾病的治疗剂的方法。

公开(公告)号：US20150376181A1

公开(公告)日：2015-12-31

申请号：US14748990

申请日：2015-06-24

Applicant: eFFECTOR Therapeutics, Inc.

Inventor： Siegfried H. Reich ,  Paul A. Sprengeler ,  Stephen E. Webber ,  Alan X. Xiang ,  Justin T. Ernst

IPC: C07D471/04 ,  C07D495/20 ,  C07D519/00 ,  C07D491/20 ,  C07D471/10 ,  C07D471/20

CPC classification number: A61K31/506 ,  A61K31/519 ,  A61K31/52 ,  A61K31/551 ,  C07D471/04 ,  C07D471/10 ,  C07D471/20 ,  C07D473/34 ,  C07D487/04 ,  C07D491/20 ,  C07D495/20 ,  C07D519/00

Abstract: The present invention relates to compounds according to Formula (I): or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4a, R4b, R5, R6, R7, R8, W1, W2, Y and n are as defined herein. Also described are pharmaceutically acceptable compositions of Formula I compounds as well as methods for utilizing the compounds of Formula I and the pharmaceutically acceptable compositions of Formula I compounds as inhibitors of Mnk as well as therapeutics for the treatment of diseases such as cancer.

Abstract translation: 本发明涉及式（I）化合物或其立体异构体，互变异构体或其药学上可接受的盐，其中R1，R2，R3，R4a，R4b，R5，R6，R7，R8，W1，W2，Y和n 如本文所定义。 还描述了式I化合物的药学上可接受的组合物以及利用式I化合物和式I化合物的药学上可接受的组合物作为Mnk抑制剂以及用于治疗诸如癌症的疾病的治疗剂的方法。

公开(公告)号：US11878015B2

公开(公告)日：2024-01-23

申请号：US17396187

申请日：2021-08-06

Applicant: eFFECTOR Therapeutics Inc.

Inventor： Justin T Ernst ,  Paul A. Sprengeler ,  Siegfried H. Reich ,  Samuel Sperry

IPC: A61K31/506 ,  A61P29/00 ,  A61P35/00 ,  A61P35/02

CPC classification number: A61K31/506 ,  A61P29/00 ,  A61P35/02

Abstract: The present invention relates to compounds according to Formula (I):




or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof wherein X1, X2, R1, R2, R3 and n are as defined herein. Also described are pharmaceutically acceptable compositions of Formula (I) compounds as well as methods for utilizing the compounds of Formula (I) and the pharmaceutically acceptable compositions of Formula (I) compounds as inhibitors of Mnk as well as therapeutics for the treatment of diseases such as cancer.

公开(公告)号：US20230295179A1

公开(公告)日：2023-09-21

申请号：US18324616

申请日：2023-05-26

Applicant: eFFECTOR Therapeutics, Inc.

Inventor： Justin T. ERNST ,  Siegfried H. REICH ,  Paul A. SPRENGELER ,  Chinh Viet TRAN ,  Garrick Kenneth PACKARD ,  Alan X. XIANG ,  Christian NILEWSKI ,  Theo MICHELS

IPC: C07D491/048 ,  C07D307/93 ,  C07D333/78 ,  C07D491/153 ,  C07D491/16 ,  C07D491/20 ,  C07D498/14 ,  C07D519/00

CPC classification number: C07D491/048 ,  C07D307/93 ,  C07D333/78 ,  C07D491/153 ,  C07D491/16 ,  C07D491/20 ,  C07D498/14 ,  C07D519/00

Abstract: The present invention provides synthesis, pharmaceutically acceptable formulations and uses of compounds in accordance with Formula I, or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof.




For Formula I compounds X, Y, R1, R2, R3a, R3b, R4a, R4b and R5 are as defined in the specification. The inventive Formula I compounds are inhibitors of eIF4A and find utility in any number of therapeutic applications, including but not limited to treatment of inflammation and various cancers.

公开(公告)号：US11576933B2

公开(公告)日：2023-02-14

申请号：US16616087

申请日：2018-05-24

Applicant: EFFECTOR THERAPEUTICS, INC.

Inventor： Peggy A. Thompson ,  Kevin R. Webster

IPC: A61K35/17 ,  A61P35/00 ,  A61K31/343 ,  A61K31/4355 ,  A61K45/06 ,  C07D471/12

Abstract: The present disclosure provides compositions and methods for improving an antitumor response against non-inflamed solid tumors. Methods of this disclosure include use of an eIF4A inhibitor to promote infiltration of antitumor lymphocytes into a non inflamed solid tumor. Methods of treating cancer associated with a non-inflamed solid tumor are also provided.

公开(公告)号：US11564947B2

公开(公告)日：2023-01-31

申请号：US17025607

申请日：2020-09-18

Applicant: eFFECTOR Therapeutics, Inc.

Inventor： Kevin R. Webster ,  Rajesh Sharma ,  Gary Chiang

IPC: C07H21/04 ,  A61K35/17 ,  C07K14/74 ,  A61P35/00 ,  C07K14/725 ,  C07K14/73 ,  C07K14/16 ,  C07K14/705 ,  C12N5/0783 ,  C07D471/04 ,  C07D487/04 ,  C07D495/20 ,  C07D491/20 ,  C07D471/20 ,  A61K31/501 ,  A61K45/06

Abstract: The present disclosure relates to genetically modified T cells comprising a transgene encoding an engineered antigen specific receptor, wherein expression of an endogenous gene selected from MNK1, MNK2, or both are inhibited in the genetically modified T cell in order to enhance central memory T cell subsets in cellular immunotherapy compositions.