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US 7,579,348 B2Granted
Derivatives of 8-substituted xanthines
AssigneePGxHealth, LLC
InventorsGuoquan Wang, Jayson M. Rieger, Robert D. Thompson
Life of this patent
Estimating the term…
Abstract
The present invention provides compounds and pharmaceutical compositions that are substituted pyridyl-linked-xantbines of formula I which are selective antagonists of A2B adenosine receptors (ARs). These compounds and compositions are useful as pharmaceutical agents.
Claims47
A compound of formula I:
- wherein:
- R is hydrogen or is selected from the group consisting of (C1-5)alkyl, halo(C1-8)alkyl, (C3-8)cycloalkyl, (C3-8)cycloalkyl(C1-8)alkyl-, (C3-5)alkenyl and (C3-5)alkynyl, each substituted or unsubstituted;
- R1 and R2 are each independently selected from the group consisting of hydrogen, substituted or unsubstituted (C1-8)alkyl, halo(C1-8)alkyl, (C3-8)alkenyl, (C3-8)alkenyl(C1-8)alkyl, (C3-8)alkynyl, (C3-8)alkynyl(C1-8)alkyl, (C1-8)alkoxy, (C3-8)cycloalkyl, (C3-8)cycloalkyl(C1-8)alkyl, (C4-10)heterocyclyl, (C4-10)heterocyclyl(C1-8)alkyl, (C6-10)aryl, (C6-10)aryloxy, (C6-10)aryl(C1-8)alkyl-, (C5-10)heteroaryl and (C5-10)heteroaryl(C1-8)alkyl-;
- L1 is a linker selected from the group consisting of substituted or unsubstituted——NRo—C(O)—, —NCH3—C(O)—, —C(O)NRo—, —C(O)NCH3—, —NRoC(O)CH2—, —NRoC(O)CH2CH2—, —C(O)NRoCH2—, —C(O)NRoCH2CH2—, —C(O)CH2NRo—, —C(O)CH2CH2NRo—, —CH2NRoC(O)—, —CH2CH2NRoC(O)—, —CH2C(O)NRo—, —CH2CH2C(O)NRo—, —NRoCH2C(O)—, and —NRoCH2CH2C(O)—, wherein each Ro is independently hydrogen or substituted or unsubstituted (C1-4)alkyl, (C1-4)alkylC(O)—, (C6-10)arylC(O)— and (C5-10)heteroarylC(O)—;
- Z is a 5-14 member substituted or unsubstituted heteroaryl ring selected from the group consisting of benzo[b]furan, benzo[b]thiophene, benzimidazole, imidazo[4,5-c]pyridine, quinazoline, thieno[2,3-c]pyridine, thieno[3,2-]pyridine, thieno[2,3-b]pyridine, indolizine, imidazo[1,2a]pyridine, quinoline, isoquinoline, phthalazine, quinoxaline, naphthyridine, quinolizine, indole, isoindole, indazole, indoline, benzoxazole, benzopyrazole, benzothiazole, imidazo[1,5-a]pyridine, pyrazolo[1,5-a]pyridine, pteridine, purine, carbazole, and acridine;
- Z1 is a 5-14 member substituted or unsubstituted aryl or heteroaryl ring;
- where n is 1 or 2;
- or
- a pharmaceutically acceptable salt thereof.
6 more elements
A compound selected from the group consisting of:
- or a pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.