IMMUNOMODULATOR PURINE-DERIVED COMPOUNDS, CONJUGATES THEREOF, AND METHODS OF USE THEREOF

Disclosed are purine-derived compounds of general Formula (I), wherein X is O or NH; Y is CH or N; R1 is an optionally substituted alkyl; n is 1 to 4; m is 0 to 4, R2 is H, halogen, alkyl or alkoxy; each of R3 and R1 is H, OH, NR6R7, optionally substituted alkyl, alkenyl, cycloalkyl, heterocycloalky...

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Hauptverfasser: HIRKALA-SCHAEFER, Truman, BRANT, Michael G, BARNSCHER, Stuart Daniel, GARNETT, Graham Albert Edwin, DUAN, Zhuang, COLOMBO, Raffaele
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creator HIRKALA-SCHAEFER, Truman
BRANT, Michael G
BARNSCHER, Stuart Daniel
GARNETT, Graham Albert Edwin
DUAN, Zhuang
COLOMBO, Raffaele
description Disclosed are purine-derived compounds of general Formula (I), wherein X is O or NH; Y is CH or N; R1 is an optionally substituted alkyl; n is 1 to 4; m is 0 to 4, R2 is H, halogen, alkyl or alkoxy; each of R3 and R1 is H, OH, NR6R7, optionally substituted alkyl, alkenyl, cycloalkyl, heterocycloalkyl, aryl or heteroaryl; or R3, R4 and N together may form a ring. Also disclosed are immunostimulatory antibody conjugates (ISACs) comprising such compounds, as well as methods for producing and using such compounds, e.g., for the treatment of diseases such as cancer. L'invention concerne des composés dérivés de purine de formule générale (I), dans laquelle X est O ou NH ; Y est CH ou N ; R1 est un alkyle éventuellement substitué ; n est compris entre 1 et 4 ; m est compris entre 0 et 4, R2 est H, halogène, alkyle ou alcoxy ; chacun de R3 et R1 est H, OH, NR6R7, alkyle, alcényle, cycloalkyle, hétérocycloalkyle, aryle ou hétéroaryle éventuellement substitué ; ou R3, R4 et N peuvent former ensemble un cycle. L'invention concerne également des conjugués d'anticorps immunostimulateurs (ISAC) comprenant de tels composés, ainsi que des procédés de production et d'utilisation de tels composés, par exemple, pour le traitement de maladies telles que le cancer.
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Also disclosed are immunostimulatory antibody conjugates (ISACs) comprising such compounds, as well as methods for producing and using such compounds, e.g., for the treatment of diseases such as cancer. L'invention concerne des composés dérivés de purine de formule générale (I), dans laquelle X est O ou NH ; Y est CH ou N ; R1 est un alkyle éventuellement substitué ; n est compris entre 1 et 4 ; m est compris entre 0 et 4, R2 est H, halogène, alkyle ou alcoxy ; chacun de R3 et R1 est H, OH, NR6R7, alkyle, alcényle, cycloalkyle, hétérocycloalkyle, aryle ou hétéroaryle éventuellement substitué ; ou R3, R4 et N peuvent former ensemble un cycle. L'invention concerne également des conjugués d'anticorps immunostimulateurs (ISAC) comprenant de tels composés, ainsi que des procédés de production et d'utilisation de tels composés, par exemple, pour le traitement de maladies telles que le cancer.</description><language>eng ; fre</language><subject>CHEMISTRY ; HETEROCYCLIC COMPOUNDS ; HUMAN NECESSITIES ; HYGIENE ; MEDICAL OR VETERINARY SCIENCE ; METALLURGY ; ORGANIC CHEMISTRY ; PEPTIDES ; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES ; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS</subject><creationdate>2024</creationdate><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&amp;date=20240201&amp;DB=EPODOC&amp;CC=WO&amp;NR=2024020684A1$$EHTML$$P50$$Gepo$$Hfree_for_read</linktohtml><link.rule.ids>230,308,776,881,25543,76294</link.rule.ids><linktorsrc>$$Uhttps://worldwide.espacenet.com/publicationDetails/biblio?FT=D&amp;date=20240201&amp;DB=EPODOC&amp;CC=WO&amp;NR=2024020684A1$$EView_record_in_European_Patent_Office$$FView_record_in_$$GEuropean_Patent_Office$$Hfree_for_read</linktorsrc></links><search><creatorcontrib>HIRKALA-SCHAEFER, Truman</creatorcontrib><creatorcontrib>BRANT, Michael G</creatorcontrib><creatorcontrib>BARNSCHER, Stuart Daniel</creatorcontrib><creatorcontrib>GARNETT, Graham Albert Edwin</creatorcontrib><creatorcontrib>DUAN, Zhuang</creatorcontrib><creatorcontrib>COLOMBO, Raffaele</creatorcontrib><title>IMMUNOMODULATOR PURINE-DERIVED COMPOUNDS, CONJUGATES THEREOF, AND METHODS OF USE THEREOF</title><description>Disclosed are purine-derived compounds of general Formula (I), wherein X is O or NH; Y is CH or N; R1 is an optionally substituted alkyl; n is 1 to 4; m is 0 to 4, R2 is H, halogen, alkyl or alkoxy; each of R3 and R1 is H, OH, NR6R7, optionally substituted alkyl, alkenyl, cycloalkyl, heterocycloalkyl, aryl or heteroaryl; or R3, R4 and N together may form a ring. Also disclosed are immunostimulatory antibody conjugates (ISACs) comprising such compounds, as well as methods for producing and using such compounds, e.g., for the treatment of diseases such as cancer. L'invention concerne des composés dérivés de purine de formule générale (I), dans laquelle X est O ou NH ; Y est CH ou N ; R1 est un alkyle éventuellement substitué ; n est compris entre 1 et 4 ; m est compris entre 0 et 4, R2 est H, halogène, alkyle ou alcoxy ; chacun de R3 et R1 est H, OH, NR6R7, alkyle, alcényle, cycloalkyle, hétérocycloalkyle, aryle ou hétéroaryle éventuellement substitué ; ou R3, R4 et N peuvent former ensemble un cycle. 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subjects CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PEPTIDES
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
title IMMUNOMODULATOR PURINE-DERIVED COMPOUNDS, CONJUGATES THEREOF, AND METHODS OF USE THEREOF
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