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Inhalation formulation comprising a glucocorticoid and a? 2-adrenoceptor agonist.
专利权人:
GLAXO GROUP LIMITED
发明人:
BIGGADIKE, KEITH,JONES, PAUL,PAYNE, JEREMY JOHN
申请号:
ES03702732
公开号:
ES2305438T5
申请日:
2003.02.04
申请国别(地区):
ES
年份:
2012
代理人:
摘要:
A pharmaceutical formulation for administration by inhalation comprising a compound of formula (I), (See formula) in which the compound of formula (I) is S-fluoromethyl ester of 6alpha, 9alpha-difluoro-11beta-hydroxy-16alpha- methyl-17alpha - [(4-methyl-1,3-thiazol-5-carbonyl) oxy] -3-oxo-androsta-1,4-diene-17beta-carbothioic acid or a salt or solvate thereof together with an agonist long-acting beta2-adreno-receptor which is salmeterol or formoterol or a compound of formula (M): (See formula) or a salt or solvate thereof, in which: m is an integer from 2 to 8; n is an integer from 3 to 11, with the proviso that m + n is from 5 to 19, R 11 is -XSO2NR 16 R 17 where X is - (CH2) p - or C2-6 alkenylene; R 16 and R 17 are independently selected from hydrogen, C 1-6 alkyl, C 3-7 cycloalkyl, C (O) NR 18 R 19, phenyl, and phenyl (C 1-4 alkyl) -, or R 18 and R 17, together with the nitrogen to which they are attached, they form a ring containing 5, 6, or 7-membered nitrogen, and R 18 and R 17 are each optionally substituted by one or two groups selected from halo, C1-6 alkyl, C1 haloalkyl - 6, C1-6 alkoxy, hydroxy-substituted C1-6 alkoxy, -CO2R 18, -SO2NR 18 R 19, -CONR 18 R 19, -NR 18 C (O) R 19, or a 5-6 heterocyclic ring or 7 members; R 18 and R 19 are independently selected from hydrogen, C 1-6 alkyl, C 3-6 cycloalkyl, phenyl, and phenyl (C 1-4 alkyl) -; and p is an integer from 0 to 6, preferably from 0 to 4; R 12 and R 13 are independently selected from hydrogen, C 1-6 alkyl, C 1-6 alkoxy, halo, phenyl, and C 1-6 haloalkyl; and R 14 and R 15 are independently selected from hydrogen and C1-4 alkyl with the proviso that the total amount of carbon atoms in R 14 and R 15 is not more than 4, said formulation having a therapeutically useful effect in the treatment of asthma or COPD for a period of 24 hours or more.Una formulación farmacéutica para administración por inhalación que comprende un compuesto de fórmula (I), (Ver fórmula) en la que el compuesto de fórmula (I) es
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