公开(公告)号：US20240076301A1

公开(公告)日：2024-03-07

申请号：US18268795

申请日：2021-12-22

Applicant: Pfizer Inc. ,  EFFECTOR THERAPEUTICS, INC.

Inventor： Kapildev Kashmirilal Arora ,  Wesley Dewitt Clark ,  David Malcolm Crowe ,  Jason Gray

IPC: C07D519/00

CPC classification number: C07D519/00

Abstract: The present invention relates to solid forms of 7-(5-chloro-2-(3-(5-cyano-6-(1-(3,3-difluorocyclobutyl)piperidin-4-yl)(methyl)amino)-2-methyl-4-oxopyrido[3,4-d]pyrimidin-3(4H)-yl)prop-1-yn-1-yl)phenyl)-N-(methylsulfonyl)thieno[3,2-b]pyridine-3-carboxamide, to pharmaceutical compositions comprising such solid forms, and to methods of using such solid forms and pharmaceutical compositions for the treatment of cancer.

公开(公告)号：US20220378821A1

公开(公告)日：2022-12-01

申请号：US17624504

申请日：2020-06-30

Applicant: EFFECTOR THERAPEUTICS, INC.

Inventor： Kevin R. WEBSTER ,  Gary CHIANG

IPC: A61K35/13 ,  C12N15/10 ,  A61K31/519

Abstract: The present disclosure provides methods for the treatment of a subject having BRAF-mutated cancer cells comprising administering an effective amount of an eIF4E inhibitor, which may be optionally used in combination with other therapies, such as RAF inhibitors. Furthermore, BRAF mutational status can be used to select for patients that would clinically benefit from eIF4E inhibition, such as patient with BRAF-mutated cancer cells that are resistant to RAF kinase inhibitors.

公开(公告)号：US20220096472A1

公开(公告)日：2022-03-31

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 ,  A61P35/02

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：US20210338673A1

公开(公告)日：2021-11-04

申请号：US17308486

申请日：2021-05-05

Applicant: eFFECTOR Therapeutics Inc.

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

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

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：US11083727B2

公开(公告)日：2021-08-10

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: C07D471/04 ,  C07D471/10 ,  C07D471/20 ,  C07D487/04 ,  C07D491/20 ,  C07D495/20 ,  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：US11014926B2

公开(公告)日：2021-05-25

申请号：US16378809

申请日：2019-04-09

Applicant: EFFECTOR THERAPEUTICS, INC.

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

IPC: C07D487/04 ,  C07D519/00 ,  C07D471/04

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.

公开(公告)号：US10702526B2

公开(公告)日：2020-07-07

申请号：US15130538

申请日：2016-04-15

Applicant: eFFECTOR Therapeutics, Inc.

Inventor： Kevin R. Webster ,  Vikas Goel

IPC: A61K31/519 ,  A61K31/52 ,  A61K31/506 ,  A61K39/395 ,  A61K31/713 ,  A61K45/06 ,  A61K39/00

Abstract: The present disclosure relates to the use MNK-specific inhibitors to inhibit immunosuppression components, such as immune checkpoint proteins PD-1, PD-L1, LAG3, and/or immunosuppressive cytokines, such as IL-10, in order to inhibit or release immune suppression in certain diseases, such as cancer and infectious disease.

公开(公告)号：US20190330216A1

公开(公告)日：2019-10-31

申请号：US16378809

申请日：2019-04-09

Applicant: EFFECTOR THERAPEUTICS, INC.

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

IPC: C07D487/04 ,  C07D519/00 ,  C07D471/04

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.

公开(公告)号：US20180353545A1

公开(公告)日：2018-12-13

申请号：US15989098

申请日：2018-05-24

Applicant: eFFECTOR Therapeutics, Inc.

Inventor： Kevin R. WEBSTER ,  Rajesh SHARMA ,  Gary CHIANG

IPC: A61K35/17 ,  C07K14/74 ,  A61P35/00 ,  C07K14/725 ,  C07K14/705 ,  C07K14/73 ,  C07K14/16

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.

公开(公告)号：US20180298017A1

公开(公告)日：2018-10-18

申请号：US15917973

申请日：2018-03-12

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

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.