Check patentability & draft patents in minutes with Patsnap Eureka AI!

Benzo[b]thiophene compounds as sting agonists

A compound, SCH3 technology, applied in drug combination, organic chemistry, resistance to vector-borne diseases, etc., can solve the problem that the innate immune system does not have antigen specificity

Active Publication Date: 2022-03-22
MERCK SHARP & DOHME BV
View PDF21 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The innate immune system is not antigen specific but responds to many effector mechanisms

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Benzo[b]thiophene compounds as sting agonists
  • Benzo[b]thiophene compounds as sting agonists
  • Benzo[b]thiophene compounds as sting agonists

Examples

Experimental program
Comparison scheme
Effect test

no. 1 approach

[0036] The first embodiment relates to compounds of general formula (Ia):

[0037]

[0038] or a pharmaceutically acceptable salt thereof, wherein R 1 selected from H, halogen, OR 6 , N(R 6 ) 2 , C 1 -C 6 Alkyl, C 1 -C 6 haloalkyl, by OR 6 substituted C 1 -C 6 Alkyl, by N(R 6 ) 2 substituted C 1 -C 6 Alkyl, COOR 6 , and C(O)N(R 6 ) 2 ;R 2 Selected from halogen, CN, OR 6 , N(R 6 ) 2 , COOR 6 , C(O)N(R 6 ) 2 , SO 2 R 6 , C 1 -C 6 Alkyl, C 1 -C 6 haloalkyl, by OR 6 substituted C1 -C 6 Alkyl, C 2 -C 6 Alkenyl, C 2 -C 6 haloalkenyl, by OR 6 substituted C 2 -C 6 Alkenyl, C 2 -C 6 Alkynyl, C 2 -C 6 haloalkynyl, by OR 6 substituted C 2 -C 6 Alkynyl, C 3 -C 6 Cycloalkyl, and including 1 to 2 selected from O, S, and N(R 6 3- to 6-membered heterocycle of ring members in ); R 3 Selected from halogen, CN, OR 6 , N(R 6 ) 2 , COOR 6 , C(O)N(R 6 ) 2 , SO 2 R 6 , C 1 -C 6 Alkyl, C 1 -C 6 haloalkyl, by OR 6 substituted C 1 -C 6 A...

no. 3 approach

[0087] A third embodiment relates to compounds of general formula (Ib):

[0088]

[0089] or a pharmaceutically acceptable salt thereof, wherein R 1 selected from H, halogen, OR 6 , N(R 6 ) 2 , C 1 -C 6 Alkyl, C 1 -C 6 haloalkyl, by OR 6 substituted C 1 -C 6 Alkyl, by N(R 6 ) 2 substituted C 1 -C 6 Alkyl, COOR 6 , and C(O)N(R 6 ) 2 ;R 2 Selected from halogen, CN, OR 6 , N(R 6 ) 2 , COOR 6 , C(O)N(R 6 ) 2 , SO 2 R 6 , C 1 -C 6 Alkyl, C 1 -C 6 haloalkyl, by OR 6 substituted C 1 -C 6 Alkyl, C 2 -C 6 Alkenyl, C 2 -C 6 haloalkenyl, by OR 6 substituted C 2 -C 6 Alkenyl, C 2 -C 6 Alkynyl, C 2 -C 6 haloalkynyl, by OR 6 substituted C 2 -C 6 Alkynyl, C 3 -C 6 Cycloalkyl, and including 1 to 2 selected from O, S, and N(R 6 3- to 6-membered heterocycle of ring members in ); R 3 Selected from halogen, CN, OR 6 , N(R 6 ) 2 , COOR 6 , C(O)N(R 6 ) 2 , SO 2 R 6 , C 1 -C 6 Alkyl, C 1 -C 6 haloalkyl, by OR 6 substituted C 1 -C 6 A...

no. 4 approach

[0108] A fourth embodiment relates to compounds of general formula (Ib'):

[0109]

[0110] or a pharmaceutically acceptable salt thereof, wherein R 1 selected from H, halogen, OR 6 , N(R 6 ) 2 , SR 6 , C 1 -C 6 Alkyl, C 1 -C 6 haloalkyl, by OR 6 substituted C 1 -C 6 Alkyl, by SR 6 substituted C 1 -C 6 Alkyl, by N(R 6 ) 2 substituted C 1 -C 6 Alkyl, by OR 6 substituted C 1 -C 6 Haloalkyl, by SR 6 substituted C 1 -C 6 Haloalkyl, and N(R 6 ) 2 substituted C 1 -C 6 haloalkyl; R 2 Selected from H, halogen, CN, OR 6 , N(R 6 ) 2 , COOR 6 , C(O)N(R 6 ) 2 , SR 6 , SO 2 R 6 , C 1 -C 6 Alkyl, C 1 -C 6 haloalkyl, C 2 -C 6 Alkenyl, C 2 -C 6 haloalkenyl, C 2 -C 6 Alkynyl, C 2 -C 6 haloalkynyl, C 3 -C 6 Cycloalkyl, and including 1 to 2 selected from O, S, N and N(R 6 3- to 6-membered heterocycles of ring members in ), wherein the C 1 -C 6 Alkyl, C 1 -C 6 haloalkyl, C 2 -C 6 Alkenyl, C 2 -C 6haloalkenyl, C 2 -C 6 Alkynyl, C 2 -...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

No PUM Login to View More

Abstract

Provide the compound of general formula (Ia), the compound of general formula (Ia'), the compound of general formula (Ib), the compound of general formula (Ib'), the compound of general formula (I), the compound of general formula (I') Compounds, and their pharmaceutically acceptable salts, wherein, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 8 , R 9 、X 1 、X 2 , and X 3 As defined herein, it can be used as an inducer of type I interferon production, in particular as a STING active agent. Syntheses and uses of the disclosed compounds are also provided.

Description

technical field [0001] The present disclosure relates to compounds and derivatives thereof that may be useful as STING (interferon-stimulated gene) agonists that activate the STING pathway. The present disclosure also relates to methods of synthesizing such compounds and uses thereof. [0002] Reference to electronically filed sequence listings [0003] The sequence listing of this application is submitted via EFS-Web in the form of a sequence listing in ASCII format, the file name is "24170_SEQLIST-OCT2017", the date of creation is August 24, 2017, and the size is 25KB. The Sequence Listing submitted via EFS-Web is part of the specification and is incorporated herein by reference in its entirety. Background technique [0004] The immune system is involved in recognizing and neutralizing different types of threats, thereby maintaining homeostasis in the subject, and is generally divided into two categories: acquired and innate. The adaptive immune system specifically reco...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Patents(China)
IPC IPC(8): C07D333/60C07D409/12C07D498/04A61K31/381A61K31/385A61K31/424A61P35/00
CPCC07D333/60C07D333/62C07D409/12C07D498/04A61P35/00A61P37/00A61P37/04A61K31/385A61K31/424A61K31/381
Inventor M·D·阿尔特曼B·D·卡什W·常J·N·卡明A·M·海德勒T·J·亨德森J·P·杰威尔M·A·劳森梁睿J·利姆卢旻R·D·奥特T·萧B·W·特洛特S·特亚加亚詹
Owner MERCK SHARP & DOHME BV
Features
  • R&D
  • Intellectual Property
  • Life Sciences
  • Materials
  • Tech Scout
Why Patsnap Eureka
  • Unparalleled Data Quality
  • Higher Quality Content
  • 60% Fewer Hallucinations
Social media
Patsnap Eureka Blog
Learn More

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2025 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com