公开(公告)号：US11440917B2

公开(公告)日：2022-09-13

申请号：US16804937

申请日：2020-02-28

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

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：US20210299111A1

公开(公告)日：2021-09-30

申请号：US17210062

申请日：2021-03-23

Applicant: eFFECTOR Therapeutics Inc.

Inventor： Peggy A. Thompson ,  Kevin R. Webster

IPC: A61K31/4355 ,  A61K9/00 ,  A61K45/06 ,  A61P35/04

Abstract: The present disclosure relates to methods for ameliorating or treating an eIF4A dependent condition or disease in a subject in need thereof. The methods of the disclosure comprise administering to the subject a therapeutically effective amount of at least one eukaryotic translation initiation factor 4A (eIF4A) inhibitor and a therapeutically effective amount of at least one cyclin-dependent kinase (CDK) inhibitor.

公开(公告)号：US20200147135A1

公开(公告)日：2020-05-14

申请号：US16616087

申请日：2018-05-24

Applicant: EFFECTOR THERAPEUTICS, INC.

Inventor： Peggy A. THOMPSON ,  Kevin R. WEBSTER

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

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：US10576098B2

公开(公告)日：2020-03-03

申请号：US15973281

申请日：2018-05-07

Applicant: eFFECTOR Therapeutics, Inc.

Inventor： James Appleman ,  Peggy A. Thompson

IPC: A61K31/713 ,  A61K31/155 ,  A61K31/16 ,  A61K31/357 ,  A61K31/4245 ,  A61K31/436 ,  A61K31/4418 ,  A61K31/496 ,  A61K31/519 ,  A61K31/706 ,  A61K45/06

Abstract: The present disclosure relates to compositions and methods for treating or preventing a fibrotic disorder or disease.

公开(公告)号：US20190275039A1

公开(公告)日：2019-09-12

申请号：US16233507

申请日：2018-12-27

Applicant: eFFECTOR Therapeutics Inc.

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

IPC: 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：US20190152988A1

公开(公告)日：2019-05-23

申请号：US16171606

申请日：2018-10-26

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

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：US20190119256A1

公开(公告)日：2019-04-25

申请号：US16162459

申请日：2018-10-17

Applicant: eFFECTOR Therapeutics, Inc.

Inventor： Justin T. ERNST ,  Siegfried H. REICH ,  Paul A. SPRENGELER ,  Alan X. XIANG

IPC: C07D403/04 ,  C07D401/14 ,  A61P35/00

Abstract: The present invention provides synthesis, pharmaceutically acceptable formulations and uses of compounds in accordance with Formula I or Formula II, or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof. For Formula I compounds X1, X2, X3, X4, X5, Y1, Y2, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12 and R13 are as defined in the specification. The inventive Formula I and Formula II 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：US20190038657A1

公开(公告)日：2019-02-07

申请号：US15973281

申请日：2018-05-07

Applicant: eFFECTOR Therapeutics, Inc.

Inventor： James APPLEMAN ,  Peggy A. THOMPSON

IPC: A61K31/713 ,  A61K31/4418 ,  A61K31/16 ,  A61K31/357 ,  A61K31/4245 ,  A61K31/436 ,  A61K31/155 ,  A61K31/496 ,  A61K31/519 ,  A61K31/706 ,  A61K45/06

CPC classification number: A61K31/713 ,  A61K31/155 ,  A61K31/16 ,  A61K31/165 ,  A61K31/357 ,  A61K31/4245 ,  A61K31/436 ,  A61K31/4418 ,  A61K31/496 ,  A61K31/519 ,  A61K31/706 ,  A61K45/06 ,  A61K2300/00

Abstract: The present disclosure relates to compositions and methods for treating or preventing a fibrotic disorder or disease.

公开(公告)号：US20180085368A1

公开(公告)日：2018-03-29

申请号：US15809011

申请日：2017-11-10

Applicant: eFFECTOR Therapeutics, Inc.

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

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

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.

公开(公告)号：US20170121339A1

公开(公告)日：2017-05-04

申请号：US15337237

申请日：2016-10-28

Applicant: EFFECTOR THERAPEUTICS, INC.

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

IPC: C07D487/04 ,  C07D519/00

CPC classification number: C07D487/04 ,  C07D471/04 ,  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 A1, A2, A3, A4, A5, A6, A7, W1, R1, R2, R3, R4, R5a, R5b, R6, R7, R7a, R7b, R8, R8a, R8b, R9, R9a, R9b and R10 and subscripts “m” and “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.