Boron-containing small molecules as anti-inflammatory agents
First Claim
Patent Images
1. A compound having a structure according to the formula:
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Abstract
Compounds and methods of treating anti-inflammatory conditions are disclosed.
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Citations
40 Claims
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1. A compound having a structure according to the formula:
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2. The compound of claim 1, wherein Rh is fluoro.
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3. The compound of claim 1, wherein Rh chloro.
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4. A pharmaceutical formulation comprising:
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a) the compound of claim 1, or a pharmaceutically acceptable salt thereof; and b) a pharmaceutically acceptable excipient.
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5. The compound of claim 1, or a salt thereof, wherein X is N, and Rb is OR4, and R4 is a member selected from H, substituted or unsubstituted alkyl, substituted or unsubstituted heteroalkyl, substituted or unsubstituted cycloalkyl, substituted or unsubstituted heterocycloalkyl, substituted or unsubstituted aryl, and substituted or unsubstituted heteroaryl.
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6. The compound of claim 1, or a salt thereof, wherein X is N, and Rb is OR4, and R4 is alkyl optionally substituted with at least one halogen, hydroxyl, ether, carboxy or ester moiety.
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7. The compound of claim 1, or a salt thereof, wherein X is N, and Rb is OH or methoxy or ethoxy or n-propoxy or isopropoxy or n-butoxy or isobutoxy or sec-butoxy or tert-butoxy or n-pentoxy or iso-pentoxy or neo-pentoxy or sec-pentoxy or n-hexoxy or iso-hexoxy or sec-hexoxy.
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8. The compound of claim 1, or a salt thereof, wherein X is N, and Rb is methoxy or ethoxy or isobutoxy.
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9. The compound of claim 1, or a salt thereof, wherein X is N, and Rb is OR4, and R4 is substituted or unsubstituted cycloalkyl.
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10. The compound of claim 1, or a salt thereof, wherein X is N, and Rb is cyclopropoxy or cyclobutoxy or cyclopentyloxy or cyclohexyloxy or cycloheptyloxy or cyclooctyloxy or cyclopropylmethoxy or cyclobutylmethoxy or cyclopentylmethoxy or cyclohexylmethoxy or cycloheptylmethoxy or cyclooctylmethoxy or 2-cyclopropylethoxy or 2-cyclobutylethoxy or 2-cyclopentylethoxy or 2-cyclohexylethoxy or 2-cycloheptylethoxy or 2-cyclooetylethoxy or 3-cyclopropyipropoxy or 3-cyclobutylpropoxy or 3-cyclopentylpropoxy or 3-cyclohexylpropoxy or 3-cycloheptylpropoxy or 3-cyclooctylpropoxy.
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11. The compound of claim 1, or a salt thereof, wherein X is N, and R is cyclopentyloxy.
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12. The compound of claim 1, or a salt thereof, wherein X is N, and Rb is OR4, and R4 is alkyl substituted with unsubstituted alkoxy.
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13. The compound of claim 1, or a salt thereof, wherein X is N, and Rb is —
- O(CH2)m5OR30, wherein m5 is 1 or 2 or 3 or 4 or 5 or 6 and R30 is H or unsubstituted alkyl or unsubstituted tetrahydropyran.
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14. The compound of claim 1, or a salt thereof, wherein X is N, and Rb is —
- O(CH2)m5OR30, wherein m5 is 1 or 2 or 3 or 4 or 5 or 6 and R30 is C1 or C2 or C3 or C1 or C5 or C6 alkyl.
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15. The compound of claim 1, or a salt thereof, wherein X is N, and Rb is OH or 2-hydroxyethoxy or 2-methoxyethoxy or 2-ethoxyethoxy or 2-n-propoxyethoxy or 2-isopropoxyethoxy or 2-n-butoxyethoxy or 2-isobutoxyethoxy or 2-sec-butoxyethoxy or 2-tert-butoxyethoxy or 2-n-pentoxyethoxy or 2-iso-pentoxyethoxy or 2-neo-pentoxyethoxy or 2-sec-pentoxyethoxy or 2-n-hexyloxyethoxy or 2-iso-hexoxyethoxy or 2-sec-hexoxyethoxy or 3-hydroxypropoxy or 3-methoxypropoxy or 3-ethoxypropoxy or 3-n-propoxypropoxy or 3-isopropoxypropoxy or 3-n-butoxypropoxy or 3-isobutoxypropoxy or 3-sec-butoxypropoxy or 3-tert-butoxypropoxy or 3-n-pentoxypropoxy or 3-iso-pentoxypropoxy or 3-neo-pentoxypropoxy or 3-sec-pentoxypropoxy or 3-n-hexyloxypropoxy or 3-iso-hexoxypropoxy or 3-sec-hexoxypropoxy or 4-hydroxybutoxy or 4-methoxybutoxy or 4-ethoxybutoxy or 4-n-propoxybutoxy or 4-isopropoxybutoxy or 4-n-butoxybutoxy or 4-isobutoxybutoxy or 4-see-butoxybutoxy or 4-tert-hutoxybutoxy or 4-n-pentoxybutoxy or 4-iso-pentoxybutoxy or 4-neo-pentoxybutoxy or 4-see-pentoxybutoxy or 4-n-hexyloxybutoxy or 4-iso-hexoxybutoxy or 4-see-hexoxybutoxy or 5-hydroxypentyloxy or 5-methoxypentyloxy or 5-ethoxypentyloxy or 5-n-propoxypentyloxy or 5-isopropoxypentyloxy or 5-n-butoxypentyloxy or 5-isobutoxypentyloxy or 5-sec-butoxypentyloxy or 5-tert-butoxypentyloxy or 5-n-pentoxypentyloxy or 5-iso-pentoxypentyloxy or 5-neo-pentoxypentyloxy or 5-sec-pentoxypentyloxy or 5-n-hexyloxypentyloxy or 5-iso-hexoxypentyloxy or 5-see-hexoxypentyloxy or 6-hydroxyhexyloxy or 6-methoxyhexyloxy or 6-ethoxyhexyloxy or 6-n-propoxyhexyloxy or 6-isopropoxyhexyloxy or 6-n-butoxyhexyloxy or 6-isobutoxyhexyloxy or 6-sec-butoxyhexyloxy or 6-tert-butoxyhexyloxy or 6-n-pentoxyhexyloxy or 6-iso-pentoxyhexyloxy or 6-neo-pentoxyhexyloxy or 6-sec-pentoxyhexyloxy or 6-n-hexyloxyhexyloxy or 6-iso-hexoxyhexyloxy or 6-sec-hexoxyhexyloxy.
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16. The compound of claim 1, or a salt thereof, wherein X is N, and Rb is 2-hydroxyethoxy or 2-methoxyethoxy or 2-ethoxyethoxy or 2-n-propoxyethoxy or 2-isopropoxyethoxy or 2-n-butoxyethoxy or 2-isobutoxyethoxy or 2-sec-butoxyethoxy or 2-tert-butoxyethoxy or 2-n-pentoxyethoxy or 2-iso-pentoxyethoxy or 2-neo-pentoxyethoxy or 2-sec-pentoxyethoxy or 2-n-hexyloxyethoxy or 2-iso-hexoxyethoxy or 2-sec-hexoxyethoxy or 3-hydroxypropoxy or 3-methoxypropoxy or 3-ethoxypropoxy or 3-n-propoxypropoxy or 3-isopropoxypropoxy or 3-n-butoxypropoxy or 3-isobutoxypropoxy or 3-sec-butoxypropoxy or 3-tert-butoxypropoxy or 3-n-pentoxypropoxy or 3-iso-pentoxypropoxy or 3-neo-pentoxypropoxy or 3-sec-pentoxypropoxy or 3-n-hexyloxypropoxy or 3-iso-hexoxypropoxy or 3-see-hexoxypropoxy.
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17. The compound of claim 1, or a salt thereof, wherein X is N, and Rb is 2-hydroxyethoxy or 2-methoxyethoxy or 2-ethoxyethoxy or 2-isopropoxyethoxy or 2-isobutoxyethoxy or 3-hydroxypropoxy or 3-methoxypropoxy or 3-ethoxypropoxy or 3-isopropoxypropoxy or 3-isobutoxypropoxy.
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18. The compound of claim 1, or a salt thereof, wherein X is N, and Rb is 2-methoxyethoxy.
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19. The compound of claim 1, or a salt thereof, wherein X is N, and Rb is 2-hydroxyethoxy.
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20. The compound of claim 1, or a salt thereof, wherein X is N, and Rb is 2-isopropoxyethoxy.
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21. The compound of claim 1, or a salt thereof, wherein X is N, and Rv is 3-isopropoxypropoxy.
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22. The compound of claim 1, or a salt thereof, wherein X is N, and Rb is —
- O(CH2)m1C(O)R4d, wherein m1 is a number selected from 1 or 2 or 3 or 4 or 5 or 6 and R4d is unsubstituted alkyl.
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23. The compound of claim 1, or a salt thereof, wherein X is N, and Rh is —
- O(CH2)m1C(O)R4d, wherein m1 is 1 or 2 or 3 or 4 or 5 or 6 and R4d is C or C2 or C3 or C4 or C5 or C6 alkyl.
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24. The compound of claim 1, or a salt thereof, wherein X is N, and Rb is 2-oxopropoxy or 2-oxobutoxy or 2-oxopentyloxy or 4-methyi-2-oxopentyloxy or 2-oxohexyloxy or 4-methyl-2-oxopentyloxy or 3-methyl-2-oxopentyloxy or 3,3-dimethyl-2-oxobutoxy or 2-oxoheptyloxy or 5-methyl-2-oxohexyloxy or 4,4-dimethyl-2-oxopentyloxy or 3-methyl-2-oxohexyloxy or 2-oxooctyloxy or 6-methyl-2-oxoheptyloxy or 3-methyl-2-oxoheptyloxy or 3-oxobutoxy or 3-oxopentyloxy or 3-oxohexyloxy or 4-methyl-3-oxopentyloxy or 3-oxoheptyloxy or 5-methyl-3-oxohexyloxy or 4-methyl-3-oxohexyloxy or 4,4-dimethyl-3-oxopentyloxy or 3-oxooctyloxy or 6-methyl-3-oxoheptyloxy or 5,5-dimethyl-3-oxohexyloxy or 4-ethyl-3-oxoheptyloxy or 3-oxononyloxy or 7-methyl-3-oxooctyloxy or 4-methyl-3-oxooctyloxy or 4-oxopentyloxy or 4-oxohexyloxy or 4-oxoheptyloxy or 5-methyl-4-oxohexyloxy or 4-oxooctyloxy or 6-methyl-4-oxoheptyloxy or 5-methyl-4-oxoheptyloxy or 5,5-dimethyl-4-oxohexyloxy or 4-oxononyloxy Or 7-methyl-4-oxooctyloxy or 6,6-dimethyl-4-oxoheptyloxy or 5-methyl-4-oxooctyloxy or 4-oxodecyloxy or 8-methyl-4-oxononyloxy or 5-methyl-4-oxononyloxy or 5-oxohexyloxy or 5-oxoheptyloxy or 5-oxooctyloxy or 6-methyl-5-oxoheptyloxy or 5-oxononyloxy or 7-methyl-5-oxooctyloxy 6-methyl-5-oxooctyloxy or 6,6-dimethyl-5-oxoheptyloxy or 5-oxodecyloxy 8-methyl-5-oxononyloxy or 7,7-dimethyl-5-oxooctyloxy or 6-methyl-5-oxononyloxy or 5-oxoundecyloxy or 9-methyl-5-oxodecyloxy or 6-methyl-5-oxodecyloxy or 6-oxoheptyloxy or 6-oxooctyloxy or 6-oxononyloxy or 8-methyl-6-oxononyloxy 6-oxodecyloxy or 8-methyl-6-oxononyloxy or 9-methyl-6-oxononyloxy or 7,7-dimethyl-6-oxooctyloxy or 6-oxoundecyloxy or 9-methyl-6-oxodecyloxy or 8,8-dimethyl-6-oxononyloxy 7-methyl-6-oxodecyloxy or 6-oxododecyloxy or 10-methyl-6-oxoundecyloxy or 7-methyl-6-oxoundecyloxy or 7-oxooctyloxy or 7-oxononyloxy or 7-oxodecyloxy or 8-methyl-7-oxononyloxy or 7-oxoundecyloxy 9-methyl-7-oxodecyloxy or 8-methyl-7-oxodecyloxy or 8,8-dimethyl-7-oxononyloxy or 7-oxododecyloxy or 10-methyl-7-oxoundecyloxy or 9,9-dimethyl-7-oxodecyloxy or 8-methyl-7-oxoundecyloxy or 7-oxotridecyloxy or 11-methyl-7-oxododecyloxy, or 8-methyl-7-oxododecyloxy.
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25. The compound of claim 1, or a salt thereof, wherein X is N, and Rb is 3-oxobutoxy or 3-oxopentyloxy or 3-oxohexyloxy or 4-methyl-3-oxopentyloxy or 3-oxoheptyloxy or 5-methyl-3-oxohexyloxy or 4-methyl-3-oxohexyloxy or 4,4-dimethyl-3-oxopentyloxy or 3-oxooctyloxy 6-methyl-3-oxoheptyloxy or 5,5-dimethyl-3-oxohexyloxy or 4-methyl-3-oxoheptyloxy or 3-oxononyloxy 7-methyl-3-oxooctyloxy or 4-methyl-3-oxooctyloxy or 4-oxopentyloxy or 4-oxohexyloxy or 4-oxoheptyloxy or 5-methyl-4-oxohexyloxy or 4-oxooctyloxy or 6-methyl-4-oxoheptyloxy 5-methyl-4-oxoheptyloxy or 5,5-dimethyl-4-oxohexyloxy or 4-oxononyloxy or 7-methyl-4-oxooctyloxy or 6,6-dimethyl-4-oxoheptyloxy 5-methyl-4-oxooctyloxy or 4-oxodecyloxy or 8-methyl-4-oxononyloxy or 5-methyl-4-oxononyloxy or 5-oxohexyloxy or 5-oxoheptyloxy or 5-oxooctyloxy or 6-methyl-5-oxoheptyloxy or 5-oxononyloxy or 7-methyl-5-oxooctyloxy or 6-methyl-5-oxooctyloxy or 6,6-dimethyl-5-oxoheptyloxy or 5-oxodecyloxy or 8-methyl-5-oxononyloxy or 7,7-dimethyl-5-oxooctyloxy or 6-methyl-5-oxononyloxy or 5-oxoundecyloxy or 9-methyl-5-oxodecyloxy or 6-methyl-5-oxodecyloxy.
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26. The compound of claim 1, or a salt thereof, wherein X is N, and Rb is 2-oxopropoxy or 2-oxobutoxy or 3-oxobutoxy or 3-oxopentyloxy or 4-oxopentyloxy or 4-oxohexyloxy or 5-oxohexyloxy or 5-oxoheptyloxy or 6-oxoheptyloxy or 6-oxooctyloxy.
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27. The compound of claim 1, or a salt thereof, wherein X is N, and Rb is 3-oxobutoxy or 3-oxopentyloxy or 3-oxohexyloxy or 4-methyl-3-oxopentyloxy or 3-oxoheptyloxy or 5-methyl-3-oxohexyloxy or 4-methyl-3-oxohexyloxy or 4,4-dimethyl-3-oxopentyloxy or 4-oxopentyloxy or 4-oxohexyloxy or 4-oxoheptyloxy or 5-methyl-4-oxohexyloxy or 4-oxooctyloxy or 6-methyl-4-oxoheptyloxy or 5-methyl-4-oxoheptyloxy or 5,5-dimethyl-4-oxohexyloxy or 5-oxohexyloxy or 5-oxoheptyloxy or 5-oxooctyloxy or 6-methyl-5-oxoheptyloxy or 5-oxononyloxy or 7-methyl-5-oxooctyloxy or 6-methyl-5-oxooctyloxy or 6,6-dimethyl-5-oxoheptyloxy.
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28. The compound of claim 1, or a salt thereof, wherein X is N, and Rb is 4-oxopentyloxy or 4-oxohexyloxy or 4-oxoheptyloxy or 5-methyl-4-oxohexyloxy.
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29. The compound of claim 1, or a salt thereof, wherein X is N, and Rb is 4-oxopentyloxy.
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30. The compound of claim 1, or a salt thereof, wherein X is N, and Rb is —
- O(CH2)m1OC(O)R4d, wherein m1 is a number selected from 1 or 2 or 3 or 4 or 5 or 6 and R4d is unsubstituted alkyl.
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31. The compound of claim 1, or a salt thereof, wherein X is N, and Rh is —
- O(CH2)m1(O)R4d, wherein m1 is 1 or 2 or 3 or 4 or 5 or 6 and R4d is C1 or C2 or C3 or C4 or C5 or C6 alkyl.
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32. The compound of claim 1, or a salt thereof, wherein X is N, and Rb is —
- O(CH2)m1OC(O)R4d, wherein m5 is 1 and R4d is C1 or C2 or C3 or C4 or C5 or C6 alkyl.
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33. The compound of claim 1, or a salt thereof, wherein X is N, and Rb is 2-acetoxyethoxy or 2-(propionyloxy)ethoxy or 2-(butyryloxy)ethoxy or 2-(isobutyryloxy)ethoxy or 2-(pentanoyloxy)ethoxy or 2-(3-methylbutanoyloxy)ethoxy or 2-(2-methylbutanoyloxy)ethoxy or 2-(pivaloyloxy)ethoxy or 2-(hexanoyloxy)ethoxy or 2-(4-methylpentanoyloxy)ethoxy or 2-(3,3-dimethylbutanoyloxy)ethoxy or 2-(2-methylpentanoyloxy)ethoxy or 2-(heptanoyloxy)ethoxy or 2-(5-methyl-hexanoyloxy)ethoxy or 2-(2-methylhexanoyloxy)ethoxy or 3-acetoxypropoxy or 3-(propionyloxy)propoxy or 3-(butyryloxy)propoxy or 3-(isobutyryloxy)propoxy or 3-(pentanoyloxy)propoxy or 3-(3-methylbutanoyloxy)propoxy or 3-(2-methylbutanoyloxy)propoxy or 3-(pivaloyloxy)propoxy or 3-(hexanoyloxy)propoxy or 3-(4-methyipentanoyloxy)propoxy or 3-(3,3-dimethylbutanoyloxy)propoxy or 3-(2-methylpentanoyloxy)propoxy or 3-(heptanoyloxy)propoxy or 3-(5-methylhexanoyloxy)propoxy or 3-(2-methylhexanoyloxy)propoxy or 4-acetoxybutoxy or 4-(propionyloxy)butoxy or 4-(butyryloxy)butoxy or 4-(isobutyryloxy)butoxy or 4-(pentanoyloxy)butoxy or 4-(3-methylbutanoyloxy)butoxy or 4-(2-methylbutanoyloxy)butoxy or 4-(pivaloyloxy)butoxy or 4-(hexanoyloxy)butoxy or 4-(4-methylpentanoyloxy)butoxy or 4-(3,3-dimethylbutanoyloxy)butoxy or 4-(2-methylpentanoyloxy)butoxy or 4-(heptanoyloxy)butoxy or 4-(5-methylhexanoyloxy)butoxy or 4-(2-methylhexanoyloxy)butoxy or 5-acetoxypentyloxy or 5-(propionyloxy)pentyloxy or 5-(butyryloxy)pentyloxy or 5-(isobutyryloxy)pentyloxy or 5-(pentanoyloxy)pentyloxy or 5-(3-methylbutanoyloxy)pentyloxy or 542-methylbutanoyloxy)pentyloxy or 5-(pivaloyloxy)pentyloxy or 5-(hexanoyloxy)pentyloxy or 5-(4-methylpentanoyloxy)pentyloxy or 5-(3,3-dimethylbutanoyloxy)pentyloxy or 5-(2-methylpentanoyloxy)pentyloxy or 5-(heptanoyloxy)pentyloxy or 5-(5-methylhexanoyloxy)pentyloxy or 5-(2-methylhexanoyloxy)pentyloxy or 6-acetoxyhexyloxy or 6-(propionyloxy)hexyloxy or 6-(butyryloxy)hexyloxy or 6-(isobutyryloxy)hexyloxy or 6-(pentanoyloxy)hexyloxy or 6-(3-methylbutanoyloxy)hexyloxy or 6-(2-methylbutanoyloxy)hexyloxy or 6-(pivaloyloxy)hexyloxy or 6-(hexanoyloxy)hexyloxy or 6-(4-methylpentanoyloxy)hexyloxy or 6-(3,3-dimethylbutanoyloxy)hexyloxy or 6-(2-methylpentanoyloxy)hexyloxy or 6-(heptanoyloxy)hexyloxy or 6-(5-methylhexanoyloxy)hexyloxy or 6-(2-methylhexanoyloxy)hexyloxy.
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34. The compound of claim 1, or a salt thereof, wherein X is N, and Rb is 2-acetoxyethoxy or 2-(propionyloxy)ethoxy or 2-(butyryloxy)ethoxy or 2-(isobutyryloxy)ethoxy or 2-(pentanoyloxy)ethoxy or 2-(3-methylbutanoyloxy)ethoxy or 2-(2-methylbutanoyloxy)ethoxy or 2-(pivaloyloxy)ethoxy or 2-(hexanoyloxy)ethoxy or 2-(4-methylpentanoyloxy)ethoxy or 2-(3,3-dimethylbutanoyloxy)ethoxy or 2-(2-methylpentanoyloxy)ethoxy or 2-(heptanoyloxy)ethoxy or 2-(5-methyl-hexanoyloxy)ethoxy or 2-(2-methylhexanoyloxy)ethoxy or 3-acetoxypropoxy or 3-(propionyloxy)propoxy or 3-(butyryloxy)propoxy or 3-(isobutyryloxy)propoxy or 3-(pentanoyloxy)propoxy or 3-(3-methylbutanoyloxy)propoxy or 3-(2-methylbutanoyloxy)propoxy or 3-(pivaloyloxy)propoxy or 3-(hexanoyloxy)propoxy or 3-(4-methylpentanoyloxy)propoxy or 3-(3,3-dimethylbutanoyloxy)propoxy or 3-(2-methylpentanoyloxy)propoxy or 3-(heptanoyloxy)propoxy or 3-(5-methythexanoyloxy)propoxy or 3-(2-methylhexanoyloxy)propoxy or 4-acetoxybutoxy or 4-(propionyloxy)butoxy or 4-(butyryloxy)butoxy or 4-(isobutyryloxy)butoxy or 4-(pentanoyloxy)butoxy or 4-(3-methylbutanoyloxy)butoxy or 4-(2-methylbutanoyloxy)butoxy or 4-(pivaloyloxy)butoxy or 4-(hexanoyloxy)butoxy or 4-(4-methylpentanoyloxy)butoxy or 4-(3,3-dimethylbutanoyloxy)butoxy or 4-(2-methylpentanoyloxy)butoxy or 4-(heptanoyloxy)butoxy or 4-(5-methylhexanoyloxy)butoxy or 4-(2-methylhexanoyloxy)butoxy.
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35. The compound of claim 1, or a salt thereof, wherein X is N, and Rb is 2-acetoxyethoxy or 2-(propionyloxy)ethoxy or 3-acetoxypropoxy or 3-(propionyloxy)propoxy or 4-acetoxybutoxy or 4-(propionyloxy)butoxy or 5-acetoxypentyloxy or 5-(propionyloxy)pentyloxy.
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36. The compound of claim 1, or a salt thereof, wherein X is N, and Rh is 2-acetoxyethoxy or 2-(propionyloxy)ethoxy or 2-(butyryloxy)ethoxy or 2-(isobutyryloxy)ethoxy or 2-(pentanoyloxy)ethoxy or 2-(3-methylbutanoyloxy)ethoxy or 2-(2-methylbutanoyloxy)ethoxy or 2-(pivaloyloxy)ethoxy or 3-acetoxypropoxy or 3-(propionyloxy)propoxy or 3-(butyryloxy)propoxy or 3-(isobutyryloxy)propoxy or 3-(pentanoyloxy)propoxy or 3-(3-methylbutanoyloxy)propoxy or 3-(2-methylbutanoyloxy)propoxy or 3-(pivaloyloxy)propoxy or 4-acetoxybutoxy or 4-(propionyloxy)butoxy or 4-(butyryloxy)butoxy or 4-(isobutyryloxy)butoxy or 4-(pentanoyloxy)butoxy or 4-(3-methylbutanoyloxy)butoxy or 4-(2-methylbutanoyloxy)butoxy or 4-(pivaloyloxy)butoxy.
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37. The compound of claim 1, wherein X is N, and Rb is 3-acetoxypropoxy or 3-(propionyloxy)propoxy or 3-(butyryloxy)propoxy or 3-(isobutyryloxy)propoxy.
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38. The compound of claim 1, wherein X is N, and Rb is 3-acetoxypropoxy.
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39. The compound of claim 1, which is 6-(4-fluoro-1-hydroxy-1,3-dihydrobenzo[e][1,2]oxaborol-5-yloxy)-2-methoxynicotinonitrile.
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40. The compound of claim 1, which is 6-(6-fluoro-1-hydroxy-1,3-dihydrobenzo[c][1,2]oxaborol-5-yloxy)-2-methoxynicotinonitrile.
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2. The compound of claim 1, wherein Rh is fluoro.
Specification
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Current AssigneeAnacor Pharmaceuticals, Inc. (Pfizer Inc.)
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Original AssigneeAnacor Pharmaceuticals, Inc. (Pfizer Inc.)
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InventorsAkama, Tsutomu, Zhang, Yong-Kang, Ding, Charles Z., Plattner, Jacob J., Maples, Kirk R., Freund, Yvonne, Sanders, Virginia, Xia, Yi, Baker, Stephen J., Nieman, James A., Lu, Xiaosong, Sales, Marcelo, Sharma, Rashmi, Singh, Rajeshwar, Jacobs, Robert T., Chen, Daitao, Alley, Michael Richard Kevin
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Primary Examiner(s)Aulakh, Charanjit
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Application NumberUS13/236,543Publication NumberTime in Patent Office631 DaysField of Search514/64, 546/13, 549/213, 558/288US Class Current514/64CPC Class CodesA61K 31/69 Boron compoundsA61P 1/00 Drugs for disorders of the ...A61P 19/00 Drugs for skeletal disordersA61P 19/02 for joint disorders, e.g. a...A61P 25/00 Drugs for disorders of the ...A61P 27/02 Ophthalmic agentsA61P 29/00 Non-central analgesic, anti...A61P 3/00 Drugs for disorders of the ...A61P 37/00 Drugs for immunological or ...A61P 9/00 Drugs for disorders of the ...C07F 5/025 Boronic and borinic acid co...C07F 5/04 Esters of boric acidsY02A 50/30 Against vector-borne diseas...