|Title:||Pharmaceutical agents useful as leukotriene antagonists|
|Abstract:||The invention provides a pharmaceutical composition comprising a particular physical form of N-[4-[5-(cyclopentyloxycarbonyl)amino-1-methylindol-3-yl-methyl]-3-methoxy benzoyl]-2-methylbenzenesulphonamide and polyvinylpyrrolidone. It also provides methods for preparing this physical form, and another physical form of N-[4-[5-(cyclopentyloxycarbonyl)amino-1-methylindol-3-yl-methyl]-3-methoxy benzoyl]-2-methylbenzenesulphonamide useful in the preparation of the first mentioned physical form. The compositions are useful in the treatment of diseases in which leukotrienes are implicated, for example asthma.|
|Inventor(s):||Holohan; James J. (Macclesfield, GB2), Edwards; Ieuan J. (Congleton, GB2), Timko; Robert J. (West Chester, PA), Bradway; Randy J. (Downingtown, PA), Clements; Arlene (Turnersville, NJ)|
|Assignee:||Zeneca Limited (London, GB2)|
1. A pharmaceutical composition, which comprises, as active ingredient, an amorphous physical form of N-[4-[5-(cyclopentyloxycarbonyl)amino-1-methylindol-3-yl-methyl]-3methoxyb
enzoyl]-2-methylbenzenesulphonamide, which is substantially free of other physical forms and has an infra-red spectrum (0.5% in KBr) having sharp peaks at 1690, 1530, 1490, 1420, 1155, 1060, 862 and 550 cm.sup.-1, and polyvinylpyrrolidone.
2. A composition as claimed in claim 1, which further comprises a pharmaceutically acceptable carrier.
3. A composition as claimed in claim 1, in which the active ingredient is present in an amount of from 1 to 90% by weight, based upon the total weight of the composition.
4. A composition as claimed in claim 1 or claim 3, in which the polyvinylpyrrolidone is present in an amount of from 1 to 20% by weight, based upon the total weight of the composition.
5. A composition as claimed in claim 1 or claim 2, in which the pharmaceutically acceptable carrier is selected from mannitol, lactose, sorbitol, glucose, sucrose, dextrose, fructose, xylitol, microcrystalline cellulose, powdered cellulose and hydroxypropylmethylcellulose.
6. A composition as claimed in claim 1 or claim 2, which further comprises a processing adjuvant selected from croscarmellose sodium, sodium starch glycolate, starch, magnesium stearate, stearic acid, talc and powdered vegetable stearine.
7. A composition as claimed in claim 1 or claim 2, which is in the form of a tablet.
8. A method of antagonising one or more of the actions of leukotrienes in a living mammal, which comprises administering to said mammal an effective amount of a pharmaceutical composition as claimed in claim 1.
Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verifification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.