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US 7,405,232 B2Granted
Long acting beta-2 agonists and their use as medicaments
AssigneeBoehringer Ingelheim International GmbH
InventorsThierry Bouyssou, Christoph Hoenke, Ingo Konetzki, Juergen Mack, Andreas Schnapp
Life of this patent
Estimating the term…
Abstract
A compound of formula 1 wherein the groups R1, R2, R3, R4 and n may have the meanings given in the claims and in the specification, and methods for preparing a pharmaceutical composition for the treatment of inflammatory and obstructive respiratory complaints.
Claims16
A method for preparing a pharmaceutical composition comprising the steps of
- (a) providing a compound of formula 1
- wherein
- R1 is hydrogen, —C1-6-alkyl, —C1-6-haloalkyl, —OH, —O—C1-6-alkyl, halogen, aryl, or a heterocycle, wherein R1 may be substituted by 1, 2, 3, 4, or 5 identical or different groups R5;
- R5 is halogen, —CN, —NO2, —C1-6-alkyl, —C3-6-cycloalkyl, —C1-6-haloalkyl, —CO—R6, —COO—R6, —CON—R6−R7, —O—R6, —N—R6—R7, —N—R6−CO—R7, —N—R6—SO2—R7, —S—R6, —SO—R6, —SO2—R6 or —SO2N—R6—R7, —C2-6-alkylene, —C2-6-alkenylene, or —O—C1-6-alkylene-O—;
- wherein R6 and R7 are individually hydrogen, —C1-6-alkyl, or —C3-6-cycloalkyl;
- R2 is hydrogen, —C1-6-alkyl, -or C1-6-haloalkyl;
- R3 is —C1-6-alkyl;
- R4 is —OH, —NH2, or halogen;
- and
- n is 0, 1, 2, or 3;
- or an isomer, enantiomer, or racemate thereof, in the form of a free base or an acid addition salt, and
- (b) combining said compound of the formula I with at least one excipient or additive to obtain the pharmaceutical composition.
9 more elements
A compound of formula 1
- wherein
- R1 is hydrogen, —C1-6-alkyl, —C1-6-haloalkyl, —OH, —O—C1-6-alkyl, halogen, aryl or a heterocycle, wherein R1 may be substituted by 1, 2, 3, 4, or 5 identical or different groups R5;
- R5 is halogen, —CN, —NO2, —C1-6-alkyl, —C3-6-cycloalkyl, —C1-6-haloalkyl, —CO—R6, —COO—R6, —CON—R6−R7, —O—R6, —N—R6−R7, —N—R6−CO—R7, —N—R6—SO2——R7, —S—R6, —SO—R6 or —SO2N—R7, —C2-6-alkylene, —C2-6-alkenylene, or —O—C1-6-alkylene-O—;
- R6 and R7 is hydrogen, —C1-6-alkyl, or —C3-6-cycloalkyl;
- R2 is hydrogen, —C1-6-alkyl, -or C1-6-haloalkyl;
- R3 is methyl;
- R4 is OH;
- and
- n is 0, 1, 2, or 3;
- or an isomer, enantiomer, or racemate thereof, in the form of a free base or an acid addition salt.
7 more elements
A pharmaceutical formulation comprising a compound of formula 1
- wherein
- R1 is hydrogen, —C1-6-alkyl, —C1-6-haloalkyl, —OH, —O—C1-6-alkyl, halogen, aryl or a heterocycle, wherein R1 may be substituted by 1, 2, 3, 4, or 5 identical or different groupsR5;
- R5 is halogen, —CN, —NO2, —C1-6-alkyl, —C3-6-cycloalkyl, —C1-6-haloalkyl, —CO—R6, —COO—R6, —CON—R6−R7, —O—R6, —N—R6−R7, —N—R6−R6−CO—R7, —N—R6—SO2—R7, —S—R6, —SO—R6, —SO2—R6 or —SO2N—R6—R7, —C2-6-alkylene, —C2-6-alkenylene, or —O—C1-6-alkylene-O—;
- R6 and R7 are individually hydrogen, —C1-6-alkyl, or —C3-6-cycloalkyl;
- R2 is hydrogen, —C1-6-alkyl, -or C1-6-haloalkyl;
- R3 is methyl;
- R4 is OH;
- and
- n is 0, 1, 2, or 3;
- or an isomer, enantiomer, or racemate thereof, in the form of a free base or an acid addition salt.
7 more elements
Dependencies are inferred from the claim text.