N-substituted 3-hydroxy-4-pyridinones and pharmaceuticals containing thereof
AssigneeBristol-Myers Squibb Company
InventorShuang Liu
Life of this patent
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Abstract
N-substituted 3-hydroxy-4-pyridinones and metal chelates, methods of preparing N-substituted 3-hydroxy-4-pyridinones and metal chelates, and pharmaceutical compositions containing new N-substituted 3-hydroxy-4-pyridinones and/or their metal chelates. Use of N-substituted 3-hydroxy-4-pyridinones and their metal chelates as pharmaceutical agents for the treatment of diseases, such as parasitic and viral infections, conditions associated with inflammation and infection, and conditions mediated by cell-proliferation or collagen formation.
Claims28
An N-substituted 3-hydroxy-4-pyridinone compound of the formula (I):
- 10
- or a pharmaceutically acceptable salt thereof, or prodrug thereof, wherein:
- X is selected from the group:
- CH2, C(O), C(S), P(O)R3R4, SO2, C(═NH)NH, C(O)NH, and C(S)NH;
- R1 and R2 are independently selected from:
- H, C1-C10 alkyl substituted with 0-5 R5, C2-C10 alkenyl substituted with 0-5 R5, aryl substituted with 0-3 R5, and heteroaryl substituted with 0-3 R5;
- R3 and R4 are independently selected from:
- C1-C10 alkyl substituted with 0-5 R5, C2-C10 alkenyl substituted with 0-5 R5, aryl substituted with 0-3 R5, heteroaryl substituted with 0-3 R5, or R3 and R4 may be taken together to form a C5-C7 cyclic alkyl group optionally interrupted with O or NR6;
- R5 is elected from:
- OH, C(═O)R6, C(═O)OR6, C(═O)NR6R7, PO(OR6)(OR7), S(O)2OR6;
- R6 and R7 are independently selected from:
- H, C1-C10 alkyl, or aryl.
A radiopharmaceutical of the formula:
- M(Ch)n,
- and pharmaceutically acceptable salt thereof, wherein:
- M is a radionuclide selected from:
- 64Cu, 67Cu, 67Ga, 68Ga, 99mTc, 111In, 90Y, 149Pr, 153Sm, 159Gd, 166Ho, 169Yb, 177Lu, 186Re, and 188Re;
- n is 2 or 3;
- X is CH2;
- R1 is H;
- R2 is methyl;
- R3 and R4 are taken together form a 6-membered cyclic piperidine ring.
Dependencies are inferred from the claim text.