Claims
- 1. A compound of formula I
- 2. A compound of claim 1 wherein R1 is methyl; X is —NR3; R3 is formyl or acetyl; R2 is methyl or ethyl; Y is —CH2—; W is sulfur, and n is 0 or 1.
- 3. A compound of claim 1 wherein R1 is methyl; X is —NR3; R3 is formyl or acetyl; R2 is methyl or ethyl; Y is —O—; W is sulfur; and n is 1.
- 4. A compound of claim 1 wherein W is sulfur, R1, R2, n, X and Y are the same as in claim 1.
- 5. A compound of claim 1 wherein X is —NR3—; R3 is 2-fluoroethyl, glycolyl, formyl, methoxyacetyl, oxoethylacetate, acetyl, or methylaminocarbothioyl, R1, R2, n, W and Y are the same as in claim 1.
- 6. A compound of claim 1 wherein X is —NR3—; R3 is is formyl or acetyl; R1, R2, n, W and Y are the same as in claim 1.
- 7. A compound of claim 1 wherein X is —NR3—; R3 is as defined in claim 1: R1, R2, n, W and Y are the same as in claim 1.
- 8. A compound of claim 1 wherein Y is —CH2—; R1, R2, n, W and X are the same as in claim 1.
- 9. A compound of claim 1 wherein Y is oxygen, R1,R2, n W and X are the same as in claim 1.
- 10. A compound of claim 1 which is
a) N-({(5S)-3-[(2R)-1-(2-fluoroethyl)-2-methyl-2,3-dihydro-1H-indol-5-yl]-2-oxo-1,3-oxazolidin-5-yl}methyl)acetamide; b) N-{[(5S)-3-((2R)-1-glycoloyl-2-methyl-2,3-dihydro-1H-indol-5-yl)-2-oxo-1,3-oxazolidin-5-yl]methyl}acetamide; c) N-({(5S)-3-[(2R)-1-glycoloyl-2-methyl-2,3-dihydro-1H-indol-5-yl]-2-oxo-1,3-oxazolidin-5-yl}methyl)acetamide; d) N-({(5S)-3-[(2R)-1-formyl-2-methyl-2,3-dihydro-1H-indol-5-yl]-2-oxo-1,3-oxazolidin-5-yl}methyl)acetamide; e) N-({(5S)-3-[(2R)-1-formyl-2-methyl-2,3-dihydro-1H-indol-5-yl]-2-oxo-1,3-oxazolidin-5-yl}methyl)propanamide; f) N-({(5S)-3-[(2R)-1-formyl-2-methyl-2,3-dihydro-1-indol-5-yl]-2-oxo-1,3-oxazolidin-5-yl}methyl)ethanethioamide; g) N-({(5S)-3-[(2R)-1-(2-methoxyacetyl)-2-methyl-2,3-dihydro-1H-indol-5-yl]-2-oxo-1,3-oxazolidin-5-yl}methyl)acetamide; h) 2-((2R)-5-{(5S)-5-[(acetylamino)methyl]-2-oxo-1,3-oxazolidin-3-yl}-2-methyl-2,3dihydro-1H-indol-1-yl)-2-oxoethyl acetate; i) N-({(5S)-3-[(2R)-1-acetyl-2-methyl-2,3-dihydro-1H-indol-5-yl]-2-oxo-1,3-oxazolidin-5-yl}methyl)acetamide; j) N-[((5S)-3-{(2R)-2-methyl-1-[(methylamnino)carbothioyl]-2,3-dihydro-1H-indol-5-yl}-2-oxo-1,3-oxazolidin-5-yl)methyl]acetamide; k) 2-((2R)-5-{(5S)-5-[(ethanethioylamino)methyl]-2-oxo-1,3-oxazolidin-3-yl}-2-methyl-2,3-dihydro-1H-indol-1-yl)-2-oxoethyl acetate; l) N-({(5S)-3-[(2R)-1-glycoloyl-2-methyl-2,3-dihydro-1H-indol-5-yl]-2-oxo-1,3-oxazolidin-5-yl}methyl)ethanethioamide; m) N-{[(5S)-3-[(2R)-1-formyl-2-methyl-1,2,3,4-tetrahydro-6-quinolinyl]-2-oxo-1,3oxazolidin-5-yl]methyl}acetamide; n) N-{[(5S)-3-[(2R)-1-glycoloyl-2-methyl-1,2,3,4-tetrahydro-6-quinolinyl]-2-oxo-1,3oxazolidin-5-yl]methyl}acetamide; o) N-({(5S)-3-[(2R)-1-formyl-2-methyl-1,2,3,4-tetrahydro-6-quinolinyl]-2-oxo-1,3-oxazolidin-5-yl}methyl)acetamide; p) N-({(5S)-3-[(2R)-1-formyl-2-methyl-1,2,3,4-tetrahydro-6-quinolinyl]-2-oxo-1,3oxazolidin-5-yl}methyl)ethanethioamide; q) N-{[(5S)-3-[(3R)4-Formyl-3-methyl-3,4-dihydro-2H-1,4-benzoxazin-7-yl]-2-1,3-oxazolidin-5-yl]methyl}acetamide; r) N-({(5S)-3-[(3R)-4-Formyl-3-methyl-3,4-dihydro-2H-1,4-benzoxazin-7-yl]-2-oxo-1,3-oxazolidin-5-yl}methyl)acetamiide; s) N-({(5S)-3-[(3R)-4-Formyl-3-methyl-3,4-dihydro-2H-1,4-benzoxazin-7-yl]-2-oxo-1,3-oxazolidin-5-yl}methyl)ethanethioamide; t) N-({(5S)-3-[(2R)2-(fluoromethyl)-1-formyl-2,3-dihydro-1H-indol-5-yl]-2-oxo-1,3-oxazolidin-5-yl}methyl)acetamide; u) N-{[(5R)-3-(2(+)-methyl-2,3-dihydro-1-benzothien-5-yl)-2-oxo-1,3-oxazolidin-5-yl]methyl}acetamide; or v) N-[[(5S)-3-[2-( 1,1-dimethylethyl)-1-formyl-2,3-dihydro-1H-indol-5-yl]-2-oxo-5-oxazolidinyl]methyl]ethanethioamide.
- 11. A compound of claim 1 which is
a) N-({(5S)-3-[(2R)-1-formyl-2-methyl-2,3-dihydro-1H-indol-5-yl]-2-oxo-1,3oxazolidin-5-yl}methyl)ethanethioamide; b) N-({(5S)-3-[(2R)-1-(2-methoxyacetyl)-2-methyl-2,3-dihydro-1H-indol-5-yl]-2-oxo-1,3-oxazolidin-5-yl}methyl)acetamide; c) 2-((2R)-5-{(5S)-5-[(acetylamino)methyl]-2-oxo-1,3-oxazolidin-3-yl}-2-methyl-2,3dihydro-1H-indol-1-yl)-2-oxoethyl acetate; d) N-({(5S)-3-[(2R)-1-acetyl-2-methyl-2,3-dihydro-1H-indol-5-yl]-2-oxo-1,3-oxazolidin-5-yl}methyl)acetamide; e) N-[((5S)-3-{(2R)-2-methyl-1-[(methylamino)carbothioyl]-2,3-dihydro-1H-indol-5-yl}-2-oxo-1,3-oxazolidin-5-yl)methyl]acetamide; f) 2-((2R)-5-{(5S)-5-[(ethanethioylamino)methyl]-2-oxo-1,3-oxazolidin-3-yl}-2-methyl-2,3-dihydro-1H-indol-1-yl)-2-oxoethyl acetate; g) N-({(5S)-3-[(2R)-1-glycoloyl-2-methyl-2,3-dihydro-1H-indol-5-yl]-2oxo-1,3-oxazolidin-5-yl}methyl)ethanethioamide; h) N-({(5S)-3-[(2R)-1-formyl-2-methyl-1,2,3,4-tetrahydro-6-quinolinyl]-2-oxo-1,3-oxazolidin-5-yl}methyl)acetamide; i) N-({(5S)-3-[(2R)-1-formyl-2-methyl-1,2,3,4-tetrahydro-6-quinolinyl]-2-oxo-1,3-oxazolidin-5-yl}methyl)ethanethioamide; j) N-({(5S)-3-[(3R)-4-Formyl-3-methyl-3,4-dihydro-2H-1,4-benzoxazin-7-yl]-2-oxo-1,3-oxazolidin-5-yl}methyl)acetamide; k) N-({(5S)-3-[(3R)-4-Formyl-3-methyl-3,4-dihydro-2H-1,4-benzoxazin-7-yl]-2-oxo-1,3-oxazolidin-5-yl}methyl)ethanethioamide; or l) N-[[(5S)-3-[2-(1,1-dimethylethyl)-1-formyl-2,3-dihydro-1H-indol-5-yl]-2-oxo-5-oxazolidinyl]methyl]ethanethioamide.
- 12. A compound of claim 1 which is
a) N-({(5S)-3-[(2R)-1-formyl-2-methyl-2,3-dihydro-1H-indol-5-yl]-2-oxo-1,3-oxazolidin-5-yl}methyl)ethanethioamide; b) N-({(5S)-3-[(2R)-1-glycoloyl-2-methyl-2,3-dihydro-1H-indol-5-yl]-2-oxo-1,3-oxazolidin-5-yl}methyl)ethanethioamide; c) N-({(5S)-3-[(2R)-1-formyl-2-methyl-1,2,3,4-tetrahydro-6-quinolinyl]-2-oxo-1,3-oxazolidin-5-yl}methyl)ethanethioamide; or e) N-({(5S)-3-[(3R)-4-Formyl-3-methyl-3,4-dihydro-2H-1,4-benzoxazin-7-yl]-2-oxo-1,3-oxazolidin-5-yl}methyl)ethanethioamide.
- 13. A compound of claim 1 which N-({(5S)-3 -[(2R)-1-formyl-2-methyl-1,2,3,4-tetrahydro-6-quinolinyl]-2-oxo-1,3-oxazolidin-5-yl}methyl)ethanethioamide.
- 14. A method for treating microbial infections in patients comprising: administering to a human or warn blood animals in need thereof an effective amount of a compound of formula I as shown in claim 1.
- 15. The method of claim 14 wherein said compound of formula I is administered orally, parenterally, transdermally, or topically in a pharmaceutical composition.
- 16. The method of claim 14 wherein said compound is administered in an amount of from about 0.1 to about 100 mg/kg of body weight/day.
- 17. The method of claim 14 wherein said compound is administered in an amount of from about 1 to about 50 mg/kg of body weight/day.
- 18. A method for treating microbial infections of claim 14 wherein the infection is skin infection.
- 19. A method for treating microbial infections of claim 14 wherein the infection is eye infection.
- 20. A pharmaceutical composition comprising a compound of claim 1 and a pharmaceutically acceptable carrier.
CROSS REFERENCE TO RELATED APPLICATIONS
[0001] This application claims the benefit of the following provisional application: U.S. Serial No. 60/136,250, filed May 27, 1999, under 35 USC § 119(e)(1).
Provisional Applications (1)
|
Number |
Date |
Country |
|
60136250 |
May 1999 |
US |
Divisions (1)
|
Number |
Date |
Country |
Parent |
09572167 |
May 2000 |
US |
Child |
10090400 |
Mar 2002 |
US |