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US 2003/0119901 A1Published application
Pharmaceutical formulation containing an LTB4 antagonist
AssigneeBoehringer Ingelheim Pharma GmbH & Co. KG
InventorsRobert Becker, Thomas Bock, Siglinde Moll, Rene Roscher, Ulrich Roth, Achim Sauer, Karl Weber
Life of this patent
Estimating the term…
Abstract
The invention relates to a new pharmaceutical formulation containing an LTB4 antagonist of formula I 1 wherein A, R1, R2, R3 and R4 have the meanings as described herein, as well as the use thereof as pharmaceutical compositions for the treatment of disease.
Claims25
A pharmaceutical formulation in the form of a tablet comprising an LTB4 antagonist of formula I:
- 7
- wherein
- A denotes a group of formula
- —O—CmH2m—O—(PHE)n— (II)
- wherein
- m is an integer from 2 to 6,
- n is 0 or 1,
- PHE denotes a 1,4-phenylene group optionally substituted by one or two C1-C6 alkyl groups;
- or
- A denotes a group of formula
- 8
- R1 denotes H, OH, CN, COOR10, or CHO;
- R2 denotes H, Br, Cl, F, CF3, CHF2, OH, HO3—O, C1-C6-alkyl, C1-C6-alkoxy, C5-C7-cycloalkyl, CONR8R9, aryl, O-aryl, CH2-aryl, CR5R6-aryl, or C(CH3)2-R7,
- R3 denotes H, C1-C6-alkyl, C1-C6-alkoxy, OH, Cl or F,
- R4 denotes H or C1-C6-alkyl;
- R5 denotes C1-C4-alkyl, CF3, CH2OH, COOH or COO(C1-C4-alkyl);
- R6 denotes H, C1-C4-alkyl or CF3;
- R7 denotes CH2OH, COOH, COO(C1-C4-alkyl), CONR8R9 or CH2NR8R9;
- R8 denotes H, C1-C6-alkyl, phenyl, phenyl-(C1-C6-alkyl), COR10, COOR10, CHO, CONH2, CONHR10, SO2-(C1-C6-alkyl), or SO2-phenyl wherein the phenyl group may be mono- or disubstituted by Cl, F, CF3, C1-C4-alkyl, OH and/or C1-C4-alkoxy;
- R9 denotes H or C1-C6-alkyl;
- or
- R8 and R9 taken together represent a C4-C6-alkylene group;
- R10 denotes C1-C6-alkyl, C5-C7-cycloalkyl, aryl, heteroaryl, aralkyl or heteroaryl-(C1-C6-alkyl),
- wherein the aryl groups mentioned in groups R2 and R10 independently denote phenyl or naphthyl, and the heteroaryl groups independently denote pyrrolyl, pyrazolyl, imidazolyl, furanyl, thienyl, pyridinyl or pyrimidinyl and may each be mono- or polysubstituted by Cl, F, CF3, C1-C4-alkyl, OH, HSO3—O or C1-C4-alkoxy, or a pharmacologically acceptable acid addition salt or glycoside or 0-sulphate thereof;
- and at least one pharmacologically acceptable excipient, wherein the tablet contains at least one wetting agent.
22 more elements
Dependencies are inferred from the claim text.