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US 2008/0167270 A1Published application
Anti-infective phosphonate analogs
OwnerConstantine G. Boojamra, Aesop Cho +1inventors
InventorsConstantine G. Boojamra, Aesop Cho, William J. Watkins
Life of this patent
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Abstract
The invention is related to phosphorus substituted anti-infective compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.
Claims98
(canceled)
A conjugate or a pharmaceutically acceptable salt or solvate thereof, that is a compound of formula 504:
- substituted with one or more groups A0, wherein:
- A0 is A1, A2 or W3 with the proviso that the conjugate includes at least one A1;
- Y1 is independently O, S, N(Rx), N(O)(Rx), N(ORx), N(O)(ORx), or N(N(Rx)(Rx));
- Y2 is independently a bond, O, N(Rx), N(O)(Rx), N(ORx), N(O)(ORx), N(N(Rx)(Rx)), —S(O)M2—, or —S(O)M2—S(O)M2—;
- and when Y2 joins two phosphorous atoms Y2 can also be C(R2)(R2);
- Rx is independently H, R1, R2, W3, a protecting group, or the formula:
- R1 is independently H, W3, R2 or a protecting group;
- R1 is independently H or alkyl of 1 to 18 carbon atoms;
- R2 is independently H, R1, R3 or R4 wherein each R4 is independently substituted with 0 to 3 R3 groups or taken together at a carbon atom, two R2 groups form a ring of 3 to 8 carbons and the ring may be substituted with 0 to 3 R3 groups;
- R3 is R3a, R3b, R3c or R3d, provided that when R3 is bound to a heteroatom, then R3 is R3c or
- R3d
- R3a is F, Cl, Br, I, —CN, N3 or —NO2;
- R3b is Y1;
- R3c is —Rx, —N(Rx)(Rx), —SRx, —S(O)Rx, —S(O)2Rx, —S(O)(ORx), —S(O)2(ORx), —OC(Y1)Rx, —OC(Y1)ORx, —OC(Y1)(N(Rx)(Rx)), —SC(Y1)Rx, —SC(Y1)ORx, —SC(Y1)(N(Rx)(Rx)), —N(Rx)C(Y1)Rx, —N(Rx)C(Y1)ORx, or —N(Rx)C(Y1)(N(Rx)(Rx));
- R3d is —C(Y1)Rx, —C(Y1)ORx or —C(Y1)(N(Rx)(Rx));
- R4 is an alkyl of 1 to 18 carbon atoms, alkenyl of 2 to 18 carbon atoms, or alkynyl of 2 to 18 carbon atoms;
- R5 is R4 wherein each R4 is substituted with 0 to 3 R3 groups;
- W3 is W4 or W5;
- W4 is R5, —C(Y1)R5, —C(Y1)W5, —SOM2R5, or —SOM2W5;
- W5 is carbocycle wherein W5 is independently substituted with 0 to 3 R2 groups;
- W6 is W3 independently substituted with 1, 2, or 3 A3 groups;
- M2 is 0, 1 or 2;
- M12a is 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11 or 12;
- M12b is 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11 or 12;
- M1a, M1c, and M1d are independently 0 or 1;
- and
- M12c is 0, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11 or 12.
24 more elements
(canceled)
91-102. (canceled)
(canceled)
108-109. (canceled)
The compound:
- or a pharmaceutically acceptable salt or solvate thereof.
Dependencies are inferred from the claim text.