Back to results
US 2004/0002502 A1Published application
Medicament combinations comprising heterocyclic compounds and a novel anticholinergic
AssigneeBoehringer Ingelheim Pharma GmbH & Co. KG
InventorsRolf Banholzer, Helmut Meissner, Gerd Morschhaeuser, Michael P. Pieper, Gerald Pohl, Richard Reichl, Georg Speck, Christopher John Montague Meade, Michel Pairet
Life of this patent
Estimating the term…
Abstract
The present invention relates to novel pharmaceutical compositions based on a new anticholinergic 1 and heterocyclic compounds 2, processes for preparing them and their use in the treatment of respiratory complaints.
Claims20
1) A pharmaceutical composition of matter comprising, as an active substance one or more, salt of formula 1
- 195
- wherein
- X− denotes an anion with a single negative charge,
- in combination with, also as active substance, one or more compound of formula (2)
- 196
- wherein
- R1 denotes hydrogen, methyl, ethyl, n-butyl, i-butyl, phenyl, 2-ethylphenyl, 2-i-propylphenyl, benzyl, 4-pyridyl, 2-pyridyl, —CO-phenyl, CN, or
- together with R2 denotes a butylene or pentylene bridge;
- R2 denotes hydrogen, methyl, ethyl, or
- together with R1 denotes a butylene or pentylene bridge, or
- together with R13 denotes a single bond or a butylene bridge;
- R3 denotes hydrogen;
- R4 denotes methoxy;
- R5 denotes cyclohexyl, phenyl, 3-methoxycarbonylphenyl, 4-methoxycarbonylphenyl, 3-carboxyphenyl, 4-carboxyphenyl, CN, —COOH, —COOMe, —COOEt, 3,5-dichloro-pyridin-4-yl, 4-pyridyl or 4-pyridyl-N-oxide;
- A denotes oxygen or —CH2—;
- B denotes oxygen or one of the groups —C(R12)(R13) or —CH(R15)—CH(R17);
- D denotes a group selected from —CH2—CH2—, —CH(Ph)—CH2—, —CONH—, —CO—CH2—, —CH═CH—, —C(Ph)═CH—, —C(CR18)(CR19)—X—, —C(R19a)═Y—, —C═C— or phenylene;
- R12 denotes hydrogen, methyl, ethyl, i-propyl, phenyl or —CH2—CORx;
- R13 denotes hydrogen or
- together with R2 denotes a single bond or a butylene bridge
- R15 denotes hydrogen or
- together with R17 denotes a single bond;
- R17 denotes hydrogen or
- together with R15 denotes a single bond;
- R18 denotes hydrogen or methyl;
- R19 denotes hydrogen, methoxy, phenyl or CN;
- R19a denotes hydrogen, methyl or phenyl;
- Rx denotes hydroxy, ethoxy, benzyloxy, 2-phenylethyloxy, 4-methylpiperazin-1-yl, 4-phenylpiperazin-1-yl, N-tetrahydroisoquinolinyl, —NH-phenyl, —NH-benzyl, —NH—CH2-(4-methoxyphenyl), —NH—CH2-(4-fluorophenyl), —NH—CH2-(4-chlorophenyl), —NH—CH2-(2-chlorophenyl), —NH-(3-pyridyl), —NH—CH2-(2-pyridyl), —NH—CH2-(3-pyridyl), —NH—CH2-(4-pyridyl), —NH-(3,5-dichloropyridin-4-yl) or —NH-(2-pyrimidinyl);
- X denotes —CH2—, —S— or —NH—
- Y denotes CH, CCN, CCOOEt or CHCONH,
- optionally in the form of the individual optical isomers, mixtures thereof or racemates and optionally in the form of the pharmacologically acceptable acid addition salts thereof, optionally in the form of the solvates or hydrates thereof, and a pharmaceutically acceptable carrier or excipient.
28 more elements
Dependencies are inferred from the claim text.