Thiazolopyrimidine modulators as immunosuppressive agents
US-9221822-B2 · Dec 29, 2015 · US
US9334272B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-9334272-B2 |
| Application number | US-201414339491-A |
| Country | US |
| Kind code | B2 |
| Filing date | Jul 24, 2014 |
| Priority date | Mar 30, 2007 |
| Publication date | May 10, 2016 |
| Grant date | May 10, 2016 |
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Novel N-acylated, O-acylated and (bis or tris)-N,O-acylated derivatives of purinic and pyrimidinic nucleoside analogs, pharmaceutical compositions containing same, and uses thereof for treating proliferative diseases or disorders are disclosed.
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What is claimed is: 1. A compound having Formula I: wherein: R 1 is H; R 2 is an acyl moiety selected from the group consisting of valproyl, 4-phenylbutyryl, cinnamoyl, 2-(4-isobutylphenyl)propionyl, 1-(butyryloxymethoxy)succinyl, 1-(valproyloxymethoxy)succinyl, 1-(4-phenylbutyryloxymethoxy)succinyl, 1-(cinnamoyloxymethoxy)succinyl, 1-(phenylacetoxymethoxy)succinyl and 1-(2-(4-isobutylphenyl)propionyloxymethoxy)succinyl; and R 3 and R 4 are each independently hydrogen or an acyl moiety selected from the group consisting of valproyl, 4-phenylbutyryl, cinnamoyl, 2-(4-isobutylphenyl)propionyl, 1-(butyryloxymethoxy)succinyl, 1-(valproyloxymethoxy)succinyl, 1-(4-phenylbutyryloxymethoxy)succinyl, 1-(cinnamoyloxymethoxy)succinyl, 1-(phenylacetoxymethoxy)succinyl and 1-(2-(4-isobutylphenyl)propionyloxymethoxy)succinyl. 2. The compound of claim 1 , wherein R 2 is selected from the group consisting of 4-phenylbutyryl, cinnamoyl and valproyl, and R 3 and R 4 are each independently selected from the group consisting of H, 4-phenylbutyryl, cinnamoyl and valproyl. 3. The compound of claim 1 , wherein R 4 is H. 4. The compound of claim 3 , wherein R 2 and R 3 are each cinnamoyl. 5. The compound of claim 3 , wherein R 2 is valproyl and R 3 is H. 6. The compound of claim 3 , wherein R 2 is 4-phenylbutyryl and R 3 is H. 7. The compound of claim 3 , wherein R 2 is 2-(4-isobutylphenyl) propionyl and R 3 is H. 8. The compound of claim 3 , wherein R 2 and R 3 are each valproyl. 9. N-valproyl-9-(2-valproyloxy) ethoxymethylguanine. 10. A pharmaceutical composition comprising the compound of claim 1 and a pharmaceutically acceptable carrier.
one oxygen and one nitrogen atom, e.g. guanine · CPC title
Antineoplastic agents · CPC title
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