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US3985876A Expired / Lapsed US ⏱️ 0.0 years remaining

Chemotherapeutic solutions containing a sulphur and a salt of a 2,4-diamino-5-benzylpyrimidine

Assignee: SmithKline Beecham Corp
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Filing: 1975-05-07
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Granted: 1976-10-12
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Expires: 1995-05-07
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Abstract

Abstract A clear solution suitable for oral or parenteral chemotherapy of microbial, especially bacterial, infections containing a sulfonamide in an organic solvent and a mono acid addition salt of a sulfonamide potentiator (e.g. trimethoprim) in water, the solution having a pH in the range 2 to 7.

Inventors

  • 👤 John R. Hazlett
  • 👤 Elvin A. Holstius

Bibliographic Details

Application Number —
Jurisdiction US
Data Source google_patents
Last Synchronized 2026-11-03 13:41
CPC Classifications
A; A61; A61K; A61K9/00; A61K9/0012; A61K9/0019; A61K31/00; A61K31/63; A61K31/635; A61K47/00; A61K47/06; A61K47/08; A61K47/10; A61K47/16; A61K47/18; A61K47/20

Claims Analysis

Total Claims: 16
Claim 1
Independent Claim 127 words
A clear solution which includes 1 to 40 per cent (w/v) of sulfamethoxazole, 1 to 10 percent (w/v) of trimethoprim calculated as base in the form of a water soluble pharmaceutically acceptable acid addition mono salt, 10 to 60 percent water (v/v) and 30 to 90 percent (v/v) of a water miscible organic solvent for the sulfamethoxazole, the solution having a pH of 4.0 to 7.0, and a solution in which the organic solvent is selected from the class consisting of N, N-dimethylacetamide, polyethylene glycols having average molecular weights from about 190 to 7500 and containing 2 to 159 ethylene glycol monomer units, 1, 2-propylene glycol, glycerin, hexamethylene glycol, 1,3-butylene glycol, ethanol, diethylacetamide, dimethylsulfoxide, dimethylformamide, di 1,2-propylene glycol, glycerin formal, polyethylene-glycoethers of tetrahydrofurfuryl alcohol and diethylene glycol.
Claim 2
Dependent Claim 127 words
A clear solution which includes 1 to 40 per cent (w/v) of sulfamethoxazole, 1 to 10 percent (w/v) of trimethoprim calculated as base in the form of a water soluble pharmaceutically acceptable acid addition mono salt, 10 to 60 percent water (v/v) and 30 to 90 percent (v/v) of a water miscible organic solvent for the sulfamethoxazole, the solution having a pH of 4.0 to 7.0, and a solution in which the organic solvent is selected from the class consisting of N, N-dimethylacetamide, polyethylene glycols having average molecular weights from about 190 to 7500 and containing 2 to 159 ethylene glycol monomer units, 1, 2-propylene glycol, glycerin, hexamethylene glycol, 1,3-butylene glycol, ethanol, diethylacetamide, dimethylsulfoxide, dimethylformamide, di 1,2-propylene glycol, glycerin formal, polyethylene-glycoethers of tetrahydrofurfuryl alcohol and diethylene glycol.
Claim 3
Dependent Claim 14 words
A solution according to claim 1 in which the salt is the lactate salt.
Claim 4
Dependent Claim 19 words
A solution according to claim 1 wherein the ratio of sulfamethoxazole to trimethoprim as base is 20:1 to 0.1:1.
Claim 5
Dependent Claim 21 words
A solution according to claim 3 in which the solution contains from 0.5 to 3.5 percent of a pharmaceutically acceptable acid.
Claim 6
Dependent Claim 13 words
The solution of claim 1 which has a pH between 4 to 6.
Claim 7
Dependent Claim 13 words
The solution of claim 1 which has a pH of 4.5 to 5.5.
Claim 8
Dependent Claim 198 words
A clear solution for oral or parenteral use including (a) 1 to 40 per cent (w/v) of a sulphonamide selected from the group consisting of sulfadimethoxine, sulphadiazine, sulfadoxine, sulphadimethoxine, sulphamethoxazol, sulphaquinoxaline, sulphadimidine, sulfafurazole and sulfacetamide; (b) 30 to 90 percent (v/v) of a medicinally acceptable water miscible organic solvent for the sulphonamide, said organic solvent is selected from the class consisting of N,N-dimethylacetamide, polyethylene glycols having average molecular weights from about 190 to 7500 and containing 2 to 159 ethylene glycol monomer units, 1,2-propylene glycol, glycerin, hexamethylene glycol, 1,3-butylene glycol, ethanol, diethylacetamide, dimethylsulfoxide, dimethylformamide, di 1,2-propylene glycol, glycerin formal, polyethylene-glycoethers of tetrahydrofurfuryl alcohol and diethylene glycol; (c) 1 to 10 percent (w/v) of sulphonamide potentiator calculated as a base, in the form of a water soluble, pharmaceutically acceptable mono acid addition salt, said sulphonamide potentiator being of formula I ##SPC4## wherein R 1 is hydrogen or lower alkyl, wherein R 3 and R 4 are hydrogen, halogen, lower alkyl, lower alkoxy and wherein one or both R 5 and R 6 are halogen, lower alkyl and lower alkoxy; and (d) 10 to 60 percent water (v/v) said solution having a pH in the range of 2 to 7.
Claim 9
Dependent Claim 198 words
A clear solution for oral or parenteral use including (a) 1 to 40 per cent (w/v) of a sulphonamide selected from the group consisting of sulfadimethoxine, sulphadiazine, sulfadoxine, sulphadimethoxine, sulphamethoxazol, sulphaquinoxaline, sulphadimidine, sulfafurazole and sulfacetamide; (b) 30 to 90 percent (v/v) of a medicinally acceptable water miscible organic solvent for the sulphonamide, said organic solvent is selected from the class consisting of N,N-dimethylacetamide, polyethylene glycols having average molecular weights from about 190 to 7500 and containing 2 to 159 ethylene glycol monomer units, 1,2-propylene glycol, glycerin, hexamethylene glycol, 1,3-butylene glycol, ethanol, diethylacetamide, dimethylsulfoxide, dimethylformamide, di 1,2-propylene glycol, glycerin formal, polyethylene-glycoethers of tetrahydrofurfuryl alcohol and diethylene glycol; (c) 1 to 10 percent (w/v) of sulphonamide potentiator calculated as a base, in the form of a water soluble, pharmaceutically acceptable mono acid addition salt, said sulphonamide potentiator being of formula I ##SPC4## wherein R 1 is hydrogen or lower alkyl, wherein R 3 and R 4 are hydrogen, halogen, lower alkyl, lower alkoxy and wherein one or both R 5 and R 6 are halogen, lower alkyl and lower alkoxy; and (d) 10 to 60 percent water (v/v) said solution having a pH in the range of 2 to 7.
Claim 10
Dependent Claim 40 words
A solution as claimed in claim 7 wherein R 3 is hydrogen, and R 4 , R 5 and R 6 are the same or different and represent an alkyl or alkoxy group having from 1 to 4 carbon atoms.
Claim 11
Dependent Claim 46 words
A solution according to claim 7 in which the sulphonamide potentiator is represented by the formula: ##STR2## where R 1 , R 2 and R 3 are the same or different and can each represent alkyl or alkoxy groups having from 1 to 4 carbon atoms.
Claim 12
Dependent Claim 19 words
A solution according to claim 9 in which R 1 , R 2 , and R 3 are methoxy.
Claim 13
Dependent Claim 11 words
A solution according to claim 9 wherein the sulphonamide is sulfamethoxazole.
Claim 14
Dependent Claim 34 words
A solution according to claim 7 in which the sulphonamide is present in an effective antibacterial or antiprotozoal treatment amount and in which the sulphonamide potentiator is present in an effective sulphonamide potentiating amount.
Claim 15
Dependent Claim 36 words
A method of treating an animal or mammal suffering from bacterial or protazoal infections which comprises administering to said animal or mammal a therapeutically effective antibacterial or antiprotozoal treatment amount of the solution of claim 7.
Claim 16
Dependent Claim 17 words
A method according to claim 13 in which the sulphonamide is sulfamethoxazole and the potentiator is trimethoprim.

References Cited (Backward Citations)

US3551564A Cited
US3728452A Cited
US3881003A Cited

USPTO Annuity & Maintenance Windows

Annuity Stage Window Opens Payment Deadline Surcharge Period Until Estimated Fee Status
3.5 Years (Year 4) 1979-10-12 1980-04-12 1980-10-12 $2000.00 Window Closed / Lapsed
7.5 Years (Year 8) 1983-10-12 1984-04-12 1984-10-12 $3760.00 Window Closed / Lapsed
11.5 Years (Year 12) 1987-10-12 1988-04-12 1988-10-12 $7700.00 Window Closed / Lapsed

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