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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Bibliographische Detailangaben
Hauptverfasser:	HIRKALA-SCHAEFER, Truman, BRANT, Michael G, BARNSCHER, Stuart Daniel, GARNETT, Graham Albert Edwin, DUAN, Zhuang, COLOMBO, Raffaele
Format:	Patent
Sprache:	eng ; fre
Schlagworte:	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
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Beschreibung
Zusammenfassung:	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.