A pharmaceutical composition comprising: (a) a salt of formula 1 wherein: X- is an anion with a single negative charge; and (b) a betamimetic 2, or a solvate or hydrate thereof, optionally in the form of the enantiomers, mixtures of the enantiomers, or in the form of the racemates thereof, p
A pharmaceutical composition comprising: (a) a salt of formula 1 wherein: X- is an anion with a single negative charge; and (b) a betamimetic 2, or a solvate or hydrate thereof, optionally in the form of the enantiomers, mixtures of the enantiomers, or in the form of the racemates thereof, processes for preparing them and their use in the treatment of respiratory complaints.
대표청구항▼
We claim: 1. A pharmaceutical composition comprising: (a) a salt of formula 1 wherein: X- is an anion with a single negative charge; and (b) a betamimetic 2 wherein the betamimetic 2 is a salmeterol salt, formoterol salt, or acid addition salt of a compound of formula 2a' wherein: R1 and R2
We claim: 1. A pharmaceutical composition comprising: (a) a salt of formula 1 wherein: X- is an anion with a single negative charge; and (b) a betamimetic 2 wherein the betamimetic 2 is a salmeterol salt, formoterol salt, or acid addition salt of a compound of formula 2a' wherein: R1 and R2, which are identical or different, are each hydrogen or C1-C4-alkyl; and R3 and R4, which are identical or different, are each hydrogen, C1-C4-alkyl,--O--C1-C4-alkyl,--C1-C4-alkylene-O--C1-C4-alkyl, or R3 and R4 together are C1-C4-alkylene-or--O--C1-C4-alkylene-O--, or a solvate or hydrate thereof, optionally in the form of the enantiomers, mixtures of the enantiomers, or in the form of the racemates thereof. 2. The pharmaceutical composition according to claim 1, further comprising a pharmaceutically acceptable excipient. 3. The pharmaceutical composition according to claim 1, wherein X- is selected from chloride, bromide, iodide, sulfate, phosphate, methanesulfonate, nitrate, maleate, acetate, citrate, fumarate, tartrate, oxalate, succinate, benzoate, and p-toluenesulfonate. 4. The pharmaceutical composition according to claim 1, wherein pharmaceutical composition comprises more than one betamimetic 2. 5. The pharmaceutical composition of claim 1, wherein the betamimetic 2 is a salt of hydrochloric acid, hydrobromic acid, sulfuric acid, phosphoric acid, methanesulfonic acid, acetic acid, fumaric acid, succinic acid, lactic acid, citric acid, tartaric acid, 1-hydroxy-2-naphthalenecarboxylic acid, 4-phenylcinnamic acid, 5-(2,4-difluorophenyl)salicylic acid, or maleic acid. 6. The pharmaceutical composition of claim 1, wherein the betamimetic 2 is salmeterol xinafoate, salmeterol-4-phenylcinnamate, or salmeterol-5-(2,4-difluorophenyl)salicylate. 7. The pharmaceutical composition according to claim 1, wherein the betamimetic 2 is an acid addition salt of a compound of formula 2a' wherein: R1 and R2, which are identical or different, are each hydrogen, methyl, or ethyl; and R3 and R4, which are identical or different, are each hydrogen, methyl, ethyl, propyl, butyl, methoxy, ethoxy, methoxymethyl, or methoxyethyl, or R3 and R4 together are propylene, butylene,--O-ethylene-O--, or--O-propylene-O--. 8. The pharmaceutical composition according to claim 7, wherein: R1 and R2, which are identical or different, are each hydrogen or ethyl; and R3 and R4, which are identical or different, are each hydrogen, methyl, ethyl, propyl, butyl, or methoxyethyl, or R3 and R4 together are butylene or--O-ethylene-O--. 9. The pharmaceutical composition according to claim 7, wherein the betamimetic 2 is a salt of the compound of formula 2a' wherein: (a) R1 and R2 are each hydrogen and R3 and R4 are each ethyl; (b) R1 and R2 are each hydrogen and R3 and R4 are each methyl; (c) R1 and R2 are each ethyl and R3 and R4 are each hydrogen; (d) R1 and R2 are each hydrogen and R3 and R4 together are butylene; (e) R1 and R2 are each hydrogen and R3 and R4 together are--O-ethylene-O--; (f) R1 and R2 are each hydrogen and R3 and R4 are each tert-butyl; (g) R1 and R2 are each hydrogen and R3 and R4 are each isopropyl; or (h) R1 and R2 are each hydrogen and R3 and R4 are each methoxymethyl. 10. A pharmaceutical composition comprising: (a) a cation of 1' (b) salmetrol 2', wherein the weight ratio of 1' to 2' is in a range from about 1:30 to 400:1. 11. The pharmaceutical composition according to claim 10, wherein the weight ratio of 1' to the salmeterol 2' is in a range from about 1:25 to 200:1. 12. The pharmaceutical composition according to claim 1, wherein the betamimetic 2 is formoterol hydrochloride, formoterol sulfate, or formoterol fumarate. 13. A pharmaceutical composition comprising: (a) a cation of 1' (b) formoterol 2', wherein the weight ratio of 1' to 2' is in a range from about 1:10 to 300:1. 14. The pharmaceutical composition according to claim 13, wherein the weight ratio of 1' to the formoterol 2' is in a range from about 1:5 to 200:1. 15. The pharmaceutical composition according to claim 1, wherein the pharmaceutical composition is an inhalable powder, a propellant-containing metered-dose aerosol, or a propellant-free inhalable solution or suspension. 16. The pharmaceutical composition according to claim 15, wherein the pharmaceutical composition is an inhalable powder comprising the compound of formula 1 and the betamimetic 2 in admixture with a physiologically acceptable excipient selected from monosaccharides, disaccharides, oligo-and polysaccharides, polyalcohols, salts, or mixtures thereof. 17. The pharmaceutical composition according to claim 16, wherein the excipient has a maximum average particle size of 250 μm or less. 18. The pharmaceutical composition according to claim 17, wherein the excipient has a maximum average particle size of between 10 μm and 150 μm. 19. A pharmaceutical composition consisting essentially of: (a) a salt of formula 1 wherein: X- is an anion with a single negative charge; and (b) a betamimetic 2 wherein the betamimetic 2 is a salmeterol salt, formoterol salt, or acid addition salt of a compound of formula 2a' wherein: R1 and R2, which are identical or different, are each hydrogen or C1-C4-alkyl; and R3 and R4, which are identical or different, are each hydrogen, C1-C4-alkyl,--O--C1-C4-alkyl,--C1-C4-alkylene-O--C1-C4-alkyl, or R3 and R4 together are C1-C4-alkylene-or--O--C1-C4-alkylene-O--. 20. The pharmaceutical composition according to claim 15, wherein the pharmaceutical composition is a propellant-containing metered-dose aerosol comprising the salt of formula 1 and the steroid 2 in dissolved or dispersed form. 21. The pharmaceutical composition according to claim 20, wherein the propellant gas is a hydrocarbon or halohydrocarbon. 22. The pharmaceutical composition according to claim 21, wherein the propellant gas is selected from n-propane; n-butane; isobutane; or the chlorinated and/or fluorinated derivatives of methane, ethane, propane, butane, cyclopropane, or cyclobutane. 23. The pharmaceutical composition according to claim 21, wherein the propellant gas is selected from TG11, TG12, TG134a, TG227, or a mixture thereof. 24. The pharmaceutical composition according to claim 20, wherein the pharmaceutical composition comprises 5% by weight or less of active substance 1 and 2 . 25. The pharmaceutical composition according to claim 15, wherein the pharmaceutical composition is a propellant-free inhalable solution or suspension further comprising a solvent selected from water, ethanol, or a mixture thereof. 26. The pharmaceutical composition according to claim 25, further comprising a cosolvent or excipient. 27. The pharmaceutical composition according to claim 26, wherein the cosolvent is selected from an alcohol, a glycol, glycerol, a polyoxyethylene alcohol, and a polyoxyethylene fatty acid ester. 28. The pharmaceutical composition according to claim 27, wherein the cosolvent is selected from isopropyl alcohol, propyleneglycol, polyethyleneglycol, polypropyleneglycol, or glycol ether. 29. The pharmaceutical composition according to claim 26, wherein the excipient is selected from a surfactant, a stabilizer, a complexing agent, an antioxidant, a preservative, a flavoring, and a vitamin. 30. The pharmaceutical composition according to claim 29, wherein the excipient is edetic acid or a salt of edetic acid.
연구과제 타임라인
LOADING...
LOADING...
LOADING...
LOADING...
LOADING...
이 특허에 인용된 특허 (11)
Meissner, Helmut; Morschhaeuser, Gerd; Pieper, Michael Paul; Pohl, Gerald; Reichl, Richard; Speck, Georg; Banholzer, Rolf, Anticholinergics which may be used as medicaments as well as processes for preparing them.
Banholzer Rolf,DEX ; Bauer Rudolf,DEX ; Reichl Richard,DEX, Esters of bi- and tricyclic amino alcohols, their preparation and their use in pharmaceutical compositions.
Banholzer Rolf (Ingelheim am Rhein DEX) Bauer Rudolf (Ockenheim DEX) Reichl Richard (Gau-Algesheim DEX), Esters of bi-and tricyclic amino alcohols and their use in pharmaceutical compositions.
Banholzer Rolf (Ingelheim am Rheim DEX) Bauer Rudolf (Wiesbaden DEX) Reichl Richard (Ingelheim am Rheim DEX), Esters of thienyl carboxylic acids and amino alcohols and their quaternization products.
Rolf Banholzer DE; Manfred Graulich DE; Sven Luettke DE; Andreas Mathes DE; Helmut Meissner DE; Peter Specht DE; Wolfgang Broeder DE, Process for preparing an anticholinergic.
Banholzer Rolf (Ingelheim am Rhein DT) Bauer Rudolf (Wiesbaden DT) Heusner Alex (Gau-Algesheim DT) Schulz Werner (Ingelheim am Rhein DT), Quaternary N-b
상세보기
이 특허를 인용한 특허 (24)
Wachtel, Herbert, Adapter, inhalation device, and atomizer.
Lustenberger, Philipp; Konetzki, Ingo; Sieger, Peter, Enantiomerically pure beta agonists, process for the manufacture thereof and use thereof as medicaments.
Fairhurst, Robin Alec; Sandham, David Andrew; Beattie, David; Bruce, Ian; Cuenoud, Bernard; Madden, Reamonn; Press, Neil John; Taylor, Roger John; Turner, Katharine Louise; Watson, Simon James, Quinoline-2-one derivatives for the treatment of airways diseases.
※ AI-Helper는 부적절한 답변을 할 수 있습니다.