Claims
- 1. A method of treating a bacterial infection in a mammal in need thereof, comprising the step of administering to said mammal a therapeutically effective amount of a compound having the formula:
- 2. The method according to claim 1 wherein the compound has the formula IA:
- 3. The method according to claim 2 wherein the compound has one or more of the following features:
(a) R1 is selected from —C(R4)2NHCOR, —C(R4)2NHCO2R, —CO2R, and —CONHR where R is an optionally substituted C1-4 aliphatic group and each R4 is independently selected from hydrogen, a C1-3 alkyl group, or two R4 taken together with the carbon to which they are attached form a three or four membered aliphatic ring; and/or (b) R3 is a C1-8 aliphatic optionally substituted by alkoxy, alkylamino or dialkylamino, optionally substituted morpholinyl, piperazinyl, piperidinyl, pyridyl, phenyl or benzyl; and/or (c) Ar is an optionally substituted ring selected from phenyl, pyridyl, or pyrimidinyl.
- 4. The method according to claim 3 wherein the compound has the following features:
(a) R1 is selected from —C(R4)2NHCOR, —C(R4)2NHCO2R, —CO2R, and —CONHR where R is an optionally substituted C1-4 aliphatic group and each R4 is independently selected from hydrogen, a C1-3 alkyl group, or two R4 taken together with the carbon to which they are attached form a three or four membered aliphatic ring; (b) R3 is a C1-8 aliphatic optionally substituted by alkoxy, alkylamino or dialkylamino, optionally substituted morpholinyl, piperazinyl, piperidinyl, pyridyl, phenyl or benzyl; and (c) Ar is an optionally substituted ring selected from phenyl, pyridyl, or pyrimidinyl.
- 5. The method of claim 4 where R is selected from —C1-4 alkyl, —C1-4 haloalkyl, -allyl, —CH2C≡CR6, —CH(C1-3 alkyl)C≡CR6, and —C(Me)2C≡CR6, and R6 is selected from hydrogen, —C1-4 aliphatic, —CH2N(Me)2, or —CH2O(C1-3 alkyl).
- 6. The method of claim 5 where the compound is selected from those compounds listed in Table 1.
- 7. The method according to any one of claims 1-6 wherein the bacterial infection to be treated is characterized by the presence of one or more of the following organisms: Streptococcus pneumoniae, Streptococcus pyogenes, Enterococcus fecalis, Enterococcus faecium, Klebsiella pneumoniae, Enterobacter sps., Proteus sps., Pseudomonas aeruginosa, E. coli, Serratia marcesens, S. aureus, Coag. Neg. Staph., Acinetobacter sps., Salmonella sps, Shigella sps., Helicobacter pylori, Mycobacterium tuberculosis, Mycobacterium avium, Mycobacterium intracellulare, Mycobacterium fortuitum, Mycobacterium chelonae, Mycobacterium kansasii, Haemophilus influenzae, Stenotrophomonas maltophilia, and Streptococcus agalactiae.
- 8. The method according to any one of claims 1-6 wherein the bacterial infection to be treated is selected from one or more of the following: urinary tract infections, pneumonia, surgical wound infections, and bloodstream infections, prostatitis, skin and soft tissue infections, bone and joint infections, intra-abdominal infections, meningitis, brain abscess, infectious diarrhea, gastrointestinal infections, surgical prophylaxis, and therapy for febrile neutropenic patients.
- 9. A compound of formula IA:
- 10. The compound of claim 9 wherein said compound has one or more of the following features:
(a) R1 is selected from —C(R4)2NHCOR, —C(R4)2NHCO2R, —CO2R, and —CONHR where R is an optionally substituted C1-4 aliphatic group and each R4 is independently selected from hydrogen, a C1-3 alkyl group, or two R4 taken together with the carbon to which they are attached form a three or four membered aliphatic ring; and/or (b) R3 is a C1-8 aliphatic optionally substituted by alkoxy, alkylamino or dialkylamino, optionally substituted morpholinyl, piperazinyl, piperidinyl, pyridyl, phenyl or benzyl; and/or (c) Ar is an optionally substituted ring selected from phenyl, pyridyl, or pyrimidinyl.
- 11. The compound of claim 10 wherein said compound has the following features:
(a) R1 is selected from —C(R4)2NHCOR, —C(R4)2NHCO2R, —CO2R, and —CONHR where R is an optionally substituted C1-4 aliphatic group and each R4 is independently selected from hydrogen, a C1-3 alkyl group, or two R4 taken together with the carbon to which they are attached form a three or four membered aliphatic ring; (b) R3 is a C1-8 aliphatic optionally substituted by alkoxy, alkylamino or dialkylamino, optionally substituted morpholinyl, piperazinyl, piperidinyl, pyridyl, phenyl or benzyl; and (c) Ar is an optionally substituted ring selected from phenyl, pyridyl, or pyrimidinyl.
- 12. The compound of claim 11 where R is selected from —C1-4 alkyl, —C1-4 haloalkyl, -allyl, —CH2C≡CR6, —CH(C1-3 alkyl)C≡CR6, and —C(Me)2C≡CR6, and R6 is selected from hydrogen, —C1-4 aliphatic, —CH2N(Me)2, or —CH2O(C1-3 alkyl).
- 13. The compound of claim 12 wherein the compound is selected from compounds IA-1 through IA-70 listed in Table 1.
- 14. A pharmaceutical composition comprising a compound of claim 9 and a pharmaceutically acceptable carrier.
CROSS-REFERENCE TO RELATED APPLICATIONS
[0001] This application claims the benefit of International PCT application No. US/01/01374, filed, Jan. 16, 2001, which claims the benefit of U.S. Provisional Application serial No. 60/176,671, filed Jan. 18, 2000 and U.S. Provisional Application serial No. 60/254,331 filed Dec. 8, 2000, all three applications being incorporated herein by reference.
Divisions (1)
|
Number |
Date |
Country |
Parent |
10198407 |
Jul 2002 |
US |
Child |
10395331 |
Mar 2003 |
US |