1. A compound of formula I, having the structure:
wherein:
Q1 and Q2 are independently H, a modified or unmodified hexose residue or S(O)t\u2014OH, provided that Q1 and Q2 are not both H;
t is 0, 1 or 2;
R1 is alkenyl of 2-7 carbon atoms; wherein the alkenyl moiety is optionally substituted with hydroxyl, \u2014CN, halogen, trifluoroalkyl, trifluoroalkoxy, \u2014COR5, \u2014CO2R5, \u2014NO2, CONR5R6, NR5R6 or N(R5)COR6;
R2 and R2a are each, independently, hydrogen, hydroxyl, halogen, alkyl of 1-6 carbon atoms, alkoxy of 1-4 carbon atoms, alkenyl of 2-7 carbon atoms, alkynyl of 2-7 carbon atoms, trifluoroalkyl of 1-6 carbon atoms, or trifluoroalkoxy of 1-6 carbon atoms; wherein the alkyl, alkenyl, or alkynyl moieties are optionally substituted with hydroxyl, \u2014CN, halogen, trifluoroalkyl, trifluoroalkoxy, \u2014COR5, \u2014CO2R5, \u2014NO2, CONR5R6, NR5R6 or N(R5)COR6;
R3, and R3a are each, independently, hydrogen, alkyl of 1-6 carbon atoms, alkenyl of 2-7 carbon atoms, alkynyl of 2-7 carbon atoms, halogen, alkoxy of 1-4 carbon atoms, trifluoroalkyl of 1-6 carbon atoms, or trifluoroalkoxy of 1-6 carbon atoms; wherein the alkyl, alkenyl, or alkynyl moieties are optionally substituted with hydroxyl, \u2014CN, halogen, trifluoroalkyl, trifluoroalkoxy, \u2014COR5, \u2014CO2R5, \u2014NO2, CONR5R6, NR5R6 or N(R5)COR6;
R5, R6 are each, independently hydrogen, alkyl of 1-6 carbon atoms, aryl of 6-10 carbon atoms;
X is O, S, or NR7;
R7 is hydrogen, alkyl of 1-6 carbon atoms, aryl of 6-10 carbon atoms, \u2014COR5, \u2014CO2R5 or \u2014SO2R5;
or a pharmaceutically acceptable salt thereof.
2. The compound of claim 1 wherein t is 2.
3. The compound according to claim 2, wherein X is O; and R1 is alkenyl of 2-3 carbon atoms, which is optionally substituted with hydroxyl, \u2014CN, halogen, trifluoroalkyl, trifluoroalkoxy, \u2014COR5, \u2014CO2R5, \u2014NO2, CONR5R6, NR5R6 or N(R5)COR6.
4. The compound of claim 3 wherein Q1 and Q2 are independently selected from \u2014S(O)2\u2014OH and a modified or unmodified hexose residue.
5. The compound of claim 4 wherein the modified hexose residue is a glucuronide residue.
6. The compound of claim 3 wherein Q1 and Q2 are independently selected from \u2014S(O)2\u2014OH and H.
7. The compound of claim 3 wherein Q1 and Q2 are independently selected from H and a modified or unmodified hexose residue.
8. The compound of claim 7 wherein the modified hexose residue is a glucuronide residue.
9. (canceled)
10. The compound according to claim 1, which is 2-(3\u2032-fluoro-4\u2032-glucuronide phenyl)-7-vinyl-1,3-benzoxazol-5-ol or a pharmaceutically acceptable salt thereof.
11. The compound according to claim 1, which is 2-(3\u2032-fluoro-4\u2032-sulfate phenyl)-7-vinyl-1,3-benzoxazol-5-ol or a pharmaceutically acceptable salt thereof.
12. The compound according to claim 1, which is 2-(3\u2032-fluoro-4\u2032-hydroxy phenyl)-7-vinyl-1,3-benzoxazol-5-glucuronide or a pharmaceutically acceptable salt thereof.
13. The compound according to claim 1, which is 2-(3\u2032-fluoro-4\u2032-hydroxy phenyl)-7-vinyl-1,3-benzoxazol-5-sulfate or a pharmaceutically acceptable salt thereof.
14. The compound according to claim 1, which is 2-(3\u2032-fluoro-4\u2032-glucuronide phenyl)-7-vinyl-1,3-benzoxazol-5-glucuronide or a pharmaceutically acceptable salt thereof.
15. The compound according to claim 1, which is 2-(3\u2032-fluoro-4\u2032-glucuronide phenyl)-7-vinyl-1,3-benzoxazol-5-sulfate or a pharmaceutically acceptable salt thereof.
16. The compound according to claim 1, which is 2-(3\u2032-fluoro-4\u2032-sulfate phenyl)-7-vinyl-1,3-benzoxazol-5-glucuronide or a pharmaceutically acceptable salt thereof.
17. The compound according to claim 1, which is 2-(3\u2032-fluoro-4\u2032-sulfate phenyl)-7-vinyl-1,3-benzoxazol-5-sulfate or a pharmaceutically acceptable salt thereof.
18-106. (canceled)
107. A pharmaceutical composition comprising a compound according to claim 1 and a pharmaceutically acceptable carrier.
The claims below are in addition to those above.
All refrences to claim(s) which appear below refer to the numbering after this setence.
1. A device for opening a locked door or drawer, which device comprises;
a) means for facilitating the insertion of a key into a lock, said means comprising a rotatable guide having a slot for accommodating the shank of a key and facilitating the entry of said key into a lock, said rotatable guide being rotatable independently of said lock in the absence of a key;
b) means for rotating said key when inserted; and
c) alignment means which, in use, will either return said slot to a position in which it is aligned with said lock to facilitate insertion of a key therein or will index said slot in such a position.
2. A device as claimed in claim 1, wherein said rotatable guide comprises a concave cavity to facilitate the passage of a key to said slot.
3. A device as claimed in claim 1, wherein said alignment means includes means to bias said rotatable guide to a predetermined position.
4. A device as claimed in claim 3, wherein said alignment means comprises a spring.
5. A device as claimed in claim 4, further comprising a backing plate having an opening through which can pass the body of a cylinder latch but not the head thereof so that said device can be secured to a door via said cylinder latch.
6. A device as claimed in claim 5, further comprising a cover removeably mounted on said backing plate, and said rotatable guide is rotatably mounted between said backing plate and said cover.
7. A device as claimed in claim 1, including a handle displaceable to rotate said rotatable guide.
8. A device as claimed in claim 7, wherein said handle has a recess to accommodate at least part of the head of a key when inserted in a lock, whereby when said handle is depressed said rotatable guide rotates and said key also rotates as a result of the recess in the reversible handle engaging against the head of the key.
9. A device as claimed in claim 7, wherein said handle comprises an elongate member which can be attached to said rotatable guide in two positions, one extending to one side of said rotatable guide and the other to the other side of said rotatable guide.
10. A door fitted with a lock having a device as claimed in claim 1 operatively associated therewith.
11. A drawer fitted with a lock having a device as claimed in claim 1 operatively associated therewith.
12. A device as claimed in claim 2, wherein said slot is positioned at the bottom of said concave cavity and extends upwardly on one side thereof.