Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Novel agents targeting inhibitor of apoptosis proteins

A kind of technology of prodrugs, compounds, applied in the field of -3 and methods

Pending Publication Date: 2020-08-18
RGT UNIV OF CALIFORNIA
View PDF4 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Broad and selective inhibition of the BIR3 or BIR2 domains of proteins XIAP, cIAP1 or cIAP2 remains an elusive challenge

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
  • Novel agents targeting inhibitor of apoptosis proteins
  • Novel agents targeting inhibitor of apoptosis proteins
  • Novel agents targeting inhibitor of apoptosis proteins

Examples

Experimental program
Comparison scheme
Effect test

Embodiment approach 1

[0563] Embodiment 1: According to an embodiment of the present invention, there is provided a compound having the general structure I listed below or a pharmaceutically acceptable salt thereof, including the form of a prodrug:

[0564]

[0565] Among them, R 1 is any of the following: -CH 3 、-C 2 h 5 、-CF 3 、-CH 2 F, -CHF 2 、-CH 2 CF 3 、-CF 2 CH 3 、-CH 2 OH, -CF 2 OH, -CHFOH; R 2 is the following group which is monosubstituted, disubstituted or trisubstituted: -CH 2 SO 3 - 、-PO 3 -2 、-SO 3 - 、-SO 2 NH 2 、-CH 2 PO 3 -2 、-CH 2 SO 2 NH 2 、-CF 3 , -Cl, -F, -CH 3 , -NO 2 、-C 2 h 5 、-OCH 3 、-OCF 3 , Guanidino, Acrylamide, -2-Chloroacetamide, -B(OH) 2 、-SO 2 F, -SO 2 CH=CH 2 , –COH, -CO-epoxide, -CO-aziridine; R 3 Represents monosubstitution, disubstitution or trisubstitution of the following groups: -F, -Cl, -CH 3 、-C 2 h 5 , -OH, -OCH 3 、-OCF 3 ;X,Y=C or N;R 4 and R 5 Can independently be –H, -F, -OH, -OCH 3 、-OCF 3 , Guanidine, -OC...

Embodiment approach 1-i

[0566] Embodiment 1-i: According to an embodiment of the present invention, there is provided a compound having the general structure I-i listed below or a pharmaceutically acceptable salt thereof, including the form of a prodrug:

[0567]

[0568] Among them, R 1 is any of the following: -CH 3 、-C 2 h 5 、-CF 3 、-CH 2 F, -CHF 2 、-CH 2 CF 3 、-CF 2 CH 3 、-CH 2 OH, -CF 2 OH, -CHFOH; R 2 is the following group which is monosubstituted, disubstituted or trisubstituted: -CH 2 SO 3 - 、-PO 3 -2 、-SO 3 - 、-SO 2 NH 2 、-CH 2 PO 3 -2 、-CH 2 SO 2 NH 2 、-CF 3 , -Cl, -F, -CH 3 , -NO 2 、-C 2 h 5 、-OCH 3 、-OCF 3 , Guanidino, Acrylamide, -2-Chloroacetamide, -B(OH) 2 、-SO 2 F. -OSO 2 F. -NHSO 2 F, -SO 2 CH=CH 2 , –NHSO 2 CH=CH 2 , –COH, -CO-epoxide, -CO-aziridine, epoxide, aziridine, oxaziridine; R 3 Represents monosubstitution, disubstitution or trisubstitution of the following groups: -F, -Cl, -CH 3 、-C 2 h 5 , -OH, -OCH 3 、-OCF 3 、-SO2 F, -SO ...

Embodiment approach 2

[0569] Embodiment 2: According to an embodiment of the present invention, there is provided a compound having the general formula II listed below or a pharmaceutically acceptable salt thereof, including the form of a prodrug:

[0570]

[0571] Among them, R 1 is any of the following: -CH 3 、-C 2 h 5 、-CF 3 、-CH 2 F, -CHF 2 、-CH 2 CF 3 、-CF 2 CH 3 、-CH 2 OH, -CF 2 OH, -CHFOH; R 2 is the following group which is monosubstituted, disubstituted or trisubstituted: -CH 2 SO 3 - 、-PO 3 -2 、-SO 3 - 、-SO 2 NH 2 、-CH 2 PO 3 -2 、-CH 2 SO 2 NH 2 、-CF 3 , -Cl, -F, -CH 3 , -NO 2 、-C 2 h 5 、-OCH 3 、-OCF 3 , Guanidino, Acrylamide, -2-Chloroacetamide, -B(OH) 2 、-SO 2 F, -SO 2 CH=CH 2 , –COH, -CO-epoxide, -CO-aziridine; R 3 Represents monosubstitution, disubstitution or trisubstitution of the following groups: -F, -Cl, -CH 3 、-C 2 h 5 , -OH, -OCH 3 、-OCF 3 ;X,Y=C or N;R 4 and R 5 Can independently be –H, -F, -OH, -OCH 3 、-OCF 3 , Guanidine, -OC ...

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

Disclosed herein, inter alia, are methods of use and composition of novel inhibitors that target the Smac binding site of a variety of inhibitor of apoptosis proteins that contain a Bir domain, including XIAP, cIAP1, cIAP2, or other IAP proteins.

Description

[0001] Cross References to Related Applications [0002] This application claims priority to U.S. Provisional Application No. 62 / 580,328, filed November 1, 2017, which is incorporated herein by reference in its entirety for all purposes. [0003] Citations attached to "sequence listings," tables, or computer program listings filed as ASCII files [0004] The sequence listing written in the file 054156-501001WO_Sequence_Listing_ST25.txt is incorporated into this article by reference, which was created on October 16, 2018, 15,359 bytes, machine format IBM-PC, MS Windows operating system. Background technique [0005] Inhibitors of apoptosis proteins (IAPs) are an important class of apoptosis regulators, characterized by the presence of 1 to 3 baculovirus IAP repeat (BIR) domains. Cellular inhibitor of apoptosis protein 1 (cIAP1) and cellular inhibitor of apoptosis protein 2 (cIAP2) are involved in tumor necrosis factor receptor-mediated apoptosis. X-linked inhibitor of apoptos...

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
IPC IPC(8): A61K31/395C07K5/06C07K5/08C07K5/097A61K31/40A61K31/401
CPCC07K5/0202C07K5/0215C07K5/06C07K5/06026C07K5/06191C07K5/08C07K5/0806C07K5/0827C07K5/1027A61P35/00A61K45/06A61K31/635A61K31/7068A61K31/337A61K2300/00C07K5/10A61K38/05A61K38/06A61K38/07A61K31/496A61K38/08A61N5/10C07K5/06104C07K5/0819C07K5/1021C07K7/06
Inventor M·佩莱齐亚C·巴吉奥L·甘比尼P·尤多福尔库尔
Owner RGT UNIV OF CALIFORNIA
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

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

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com