Carbapenem Antibacterials with Gram-Negative Activity
AssigneeFOB Synthesis, Inc.
InventorsWoo-Baeg CHOI, Ewa GRUSZECKA-KOWALIK, Hyung-Yeul JOO, Shuangpei LIU, Shuli MAO, Yongfeng LI, Deog-Il KIM
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Abstract
The present invention provides β-methyl carbapenem compounds and pharmaceutical compositions useful in the treatment of bacterial infections and methods for treating such infections using such compounds and/or compositions. The invention includes administering an effective amount of a carbapenem compound or salt and/or prodrug thereof to a host in need of such a treatment.
Claims35
A compound of Formula I:
- or a pharmaceutically acceptable salt, ester or prodrug thereof,
- wherein
- R1 and R2 are each independently selected from H or alkyl;
- P is H, OH, halogen, or hydroxyl protected by a hydroxyl protecting group;
- n is 0, 1 or 2;
- X is —(CR2)m— or —C(═O)—;
- m is 0, 1 or 2;
- Y is CN, OR, SR′ or NRR′;
- each R is independently selected from H, alkyl or haloalkyl;
- R′ is H, alkyl, NR2;
- C(═O)R;
- SO2R;
- SO2NR2;
- C(═NR)NR2;
- C(═O)NR2;
- CR2C(═O)NR2;
- C(═NR)R;
- C(═NR)NRSO2R;
- C(═NR)NRC(═O)R;
- C(═O)CR2NRSO2NR2;
- or
- C(═O)CR2NRC(═NR)NR2;
- and
- Z is H, alkyl, halo, CN, OR, SR′ or NRR′.
A compound of Formula IV:
- or a pharmaceutically acceptable salt, ester or prodrug thereof,
- wherein
- R1, R2 and R3 are each independently selected from H or alkyl;
- P is H, OH, halogen, or hydroxyl protected by a hydroxyl protecting group;
- n is 0, 1, or 2
- X is —(CR2)m— or —C(═O)—;
- m is 0, 1 or 2;
- Y is CN, OR, SR′ or NRR′;
- each R is independently selected from H, alkyl or haloalkyl;
- R′ is H, alkyl, NR2;
- C(═O)R;
- SO2R;
- SO2NR2;
- C(═NR)NR2;
- C(═O)NR2;
- CR2C(═O)NR2;
- C(═NR)R;
- C(═NR)NRSO2R;
- C(═NR)NRC(═O)R;
- C(═O)CR2NRSO2NR2;
- or
- C(═O)CR2NRC(═NR)NR2;
- and
- Z is H, alkyl, halo, CN, OR, SR′ or NRR′.
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Dependencies are inferred from the claim text.