Benzoquinolizine-2-carboxylic acid arginine salt tetrahydrate
AssigneeWockhardt Limited
InventorsPrasad Deshpande, Vijaya Desai, Ravindra Yeole, Shrikant Gupte, Mahesh Patel, Noel de Souza
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Abstract
The invention relates to crystalline S-(−)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidin-1-yl)-5-methyl-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acid L-arginine salt tetrahydrate, a process for its preparation and pharmaceutical formulations incorporating it as the active ingredient for use in treating microbial infections.
Claims28
1-11. (canceled)
A composition comprising S-(−)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidin-1-yl)-5-methyl-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acid L-arginine salt tetrahydrate of the formula I
- and a carrier or excipient.
A composition comprising S-(−)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidin-1-yl)-5-methyl-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acid L-arginine salt tetrahydrate having the following X-ray powder diffraction data:
- (2θ):
- 4.86±0.2, 14.10±0.2, 14.90±0.2, 19.35±0.2, 22.20±0.2, 23.04±0.2, 23.54±0.2, 28.44±0.2, 39.44±0.2 and a carrier or excipient.
A composition comprising S-(−)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidin-1-yl)-5-methyl-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acid L-arginine salt tetrahydrate having the following X-ray powder diffraction data:
- (2θ):
- 4.86±0.2, 14.10±0.2, 14.90±0.2, 19.35±0.2, 22.20±0.2, 23.04±0.2, 23.54±0.2, 28.44±0.2, 39.44±0.2;
- a DSC exotherm at 194.93° C. (onset at 189.42° C.) and one endotherm at 87.83° C., 144.03° C. and 251.26° C. and a water content of between 11.0 to 12.5% by weight as determined by titration according to Karl Fischer and a carrier or excipient.
A method for treating a disease caused by a microbial infection in a mammal comprising administering an effective amount of S-(−)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidin-1-yl)-5-methyl-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acid L-arginine salt tetrahydrate of the formula I
- to the mammal in need thereof.
A method for treating a disease caused by a microbial infection in a mammal comprising administering an effective amount of S-(−)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidin-1-yl)-5-methyl-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acid L-arginine salt tetrahydrate having the following X-ray powder diffraction data:
- (2θ):
- 4.86±0.2, 14.10±0.2, 14.90±0.2, 19.35±0.2, 22.20±0.2, 23.04±0.2, 23.54±0.2, 28.44±0.2, 39.44±0.2 to the mammal in need thereof.
A method for treating a disease caused by a microbial infection in a mammal comprising administering an effective amount of S-(−)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidin-1-yl)-5-methyl-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acid L-arginine salt tetrahydrate having the following X-ray powder diffraction data:
- (2θ):
- 4.86±0.2, 14.10±0.2, 14.90±0.2, 19.35±0.2, 22.20±0.2, 23.04±0.2, 23.54±0.2, 28.44±0.2, 39.44±0.2;
- a DSC exotherm at 194.93° C. (onset at 189.42° C.) and one endotherm at 87.83° C., 144.03° C. and 251.26° C. and a water content of between 11.0 to 12.5% by weight as determined by titration according to Karl Fischer to the mammal in need thereof.
A method for preventing a disease caused by a microbial infection in a mammal comprising administering an effective amount of S-(−)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidin-1-yl)-5-methyl-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acid L-arginine salt tetrahydrate of the formula I
- to the mammal at risk of being infected.
A method for preventing a disease caused by a microbial infection in a mammal comprising administering an effective amount of S-(−)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidin-1-yl)-5-methyl-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acid L-arginine salt tetrahydrate having the following X-ray powder diffraction data:
- (2θ):
- 4.86±0.2, 14.10±0.2, 14.90±0.2, 19.35±0.2, 22.20±0.2, 23.04±0.2, 23.54±0.2, 28.44±0.2, 39.44±0.2 to the mammal at risk of being infected.
A method for preventing a disease caused by a microbial infection in a mammal comprising administering an effective amount of S-(−)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidin-1-yl)-5-methyl-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acid L-arginine salt tetrahydrate having the following X-ray powder diffraction data:
- (2θ):
- 4.86±0.2, 14.10±0.2, 14.90±0.2, 19.35±0.2, 22.20±0.2, 23.04±0.2, 23.54±0.2, 28.44±0.2, 39.44±0.2;
- a DSC exotherm at 194.93° C. (onset at 189.42° C.) and one endotherm at 87.83° C., 144.03° C. and 251.26° C. and a water content of between 11.0 to 12.5% by weight as determined by titration according to Karl Fischer to the mammal at risk of being infected.
A method for treating a bacterial infection in a mammal comprising administering an effective amount of S-(−)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidin-1-yl)-5-methyl-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acid L-arginine salt tetrahydrate of the formula I
- to the mammal in need thereof.
A method for treating a bacterial infection in a mammal comprising administering an effective amount of S-(−)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidin-1-yl)-5-methyl-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acid L-arginine salt tetrahydrate having the following X-ray powder diffraction data:
- (2θ):
- 4.86±0.2, 14.10±0.2, 14.90±0.2, 19.35±0.2, 22.20±0.2, 23.04±0.2, 23.54±0.2, 28.44±0.2, 39.44±0.2 to the mammal in need thereof.
A method for treating a bacterial infection in a mammal comprising administering an effective amount of S-(−)-9-fluoro-6,7-dihydro-8-(4-hydroxypiperidin-1-yl)-5-methyl-1-oxo-1H,5H-benzo[i,j]quinolizine-2-carboxylic acid L-arginine salt tetrahydrate having the following X-ray powder diffraction data:
- (2θ):
- 4.86±0.2, 14.10±0.2, 14.90±0.2, 19.35±0.2, 22.20±0.2, 23.04±0.2, 23.54±0.2, 28.44±0.2, 39.44±0.2;
- a DSC exotherm at 194.93° C. (onset at 189.42° C.) and one endotherm at 87.83° C., 144.03° C. and 251.26° C. and a water content of between 11.0 to 12.5% by weight as determined by titration according to Karl Fischer to the mammal in need thereof.
Dependencies are inferred from the claim text.