- CLASS OF BIFUNCTIONAL COMPOUNDS WITH QUATERNARY AMMONIUM SALT STRUCTURE
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The invention provides a class of compounds represented by formula (I), having bifunctional active quaternary ammonium salt structure of a β2-adrenoreceptor agonist and an M receptor antagonist, a pharmaceutically acceptable salt, solvate, and optical isomer thereof. A pharmaceutical composition comprising such a compound with quaternary ammonium salt structure, a method for preparing such a compound with quaternary ammonium salt structure and an intermediate thereof, and uses thereof in treating pulmonary disorders are also provided. The compounds of the invention have high selectivity to the M receptor subtype, and have less adverse reaction and lower toxic and side effects in the treatment of pulmonary diseases such as COPD and asthma.
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- Benzoxazine compound and its preparation methods and application
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The invention relates to a benzoxazine compound represented in the following formula 1. The benzoxazine compound can serve as a beta 2 receptor agonist. The formula can be seen from the description.
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- PROCESS FOR THE MANUFACTURING OF BETA MIMETICS
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The invention relates to a method for producing betamimetics of formula (1), wherein in which n represents 1 or 2; R1 represents hydrogen, halogen, C1-4-alkyl or O—C1-4-alkyl; R2 represents hydrogen, halogen, C
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Page/Page column 6
(2010/02/17)
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- Discovery of olodaterol, a novel inhaled β2-adrenoceptor agonist with a 24 h bronchodilatory efficacy
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Compound 4p was identified from a series of 6-hydroxy-4H-benzo[1,4]oxazin-3-ones as potent agonist of the human β2-adrenoceptor with a high β1/β2-selectivity. A complete reversal of acetylcholine-induced bronchoconstrictio
- Bouyssou, Thierry,Hoenke, Christoph,Rudolf, Klaus,Lustenberger, Philipp,Pestel, Sabine,Sieger, Peter,Lotz, Ralf,Heine, Claudia,Büttner, Frank H.,Schnapp, Andreas,Konetzki, Ingo
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scheme or table
p. 1410 - 1414
(2010/07/10)
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- PROCESS FOR THE MANUFACTURING OF BETAMIMETICS
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The present invention relates to a process for preparing betamimetics of formula 1, wherein n denotes 1 or 2; R1 denotes hydrogen, halogen, C1-4-alkyl or O—C1-4-alkyl; R2 denotes hydrogen, halogen, C1-4/su
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Page/Page column 11
(2008/06/13)
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- Novel Enantiomeric Pure Beta Agonists, Manufacturing and Use as a Medicament Thereof
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The present invention relates to enantiomerically pure compounds of formula 1 wherein the groups m, n, B, X, R1, m and Ym- may have the meanings given in the claims and specification, methods for preparing them and their use as pharmaceutical compositions, particularly as pharmaceutical compositions for the treatment of respiratory complaints.
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Page/Page column 11
(2008/06/13)
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- Medicament Combinations for the Treatment of Respiratory Diseases
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The present invention relates to new medicament combinations which contain in addition to one or more, preferably one compound of general formula 1 wherein A, B, R1, X, n and m may have the meanings given in the claims and in the specification, at least one other active substance 2, processes for preparing them and their use as pharmaceutical compositions.
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Page/Page column 33
(2010/11/28)
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- New betamimetics for the treatment of respiratory complaints
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The present invention relates to compounds of formula 1 wherein the groups n, m, B, X and R1 may have the meanings given in the claims and specification, processes for preparing them and their use as pharmaceutical compositions, particularly as pharmaceutical compositions for the treatment of respiratory complaints.
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Page/Page column 10
(2010/10/20)
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- New enentiomerically pure beta agonists, process for the manufacture thereof and use thereof as medicaments
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The present invention relates to enantiomerically pure compounds of general formula 1 wherein the groups R1, R2, R3, R4 and X? may have the meanings given in the claims and in the specification, proce
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Page/Page column 7
(2008/06/13)
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- NOVEL ENANTIOMERICALLY PURE BETA-AGONISTS, METHOD FOR THE PRODUCTION AND THE USE THEREOF IN THE FORM OF A DRUG
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The invention relates to enantiomerically pure compounds of formula (1), wherein the radicals R1, R2, R3, R4and X are defined as in claims and a description. A method for producing said compounds and the use thereof
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Page/Page column 15-16
(2008/06/13)
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- HYDROXY-SUBSTITUTED BENZO-CONDENSED HETEROCYCLES FOR USE AS BETA AGONISTS IN THE TREATMENT OF RESPIRATORY DISEASES
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The invention relates to the compounds of general formula (1), wherein the groups n, A, B, R1, R2 and R3 are defined as in the claims and in the description, and to methods for producing the same. The invention also relates to the use of these compounds as drugs, especially as drugs for use in the treatment of respiratory diseases.
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Page/Page column 21-22
(2010/02/14)
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- Beta agonists for the treatment of respiratory diseases
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The present invention relates to compounds of general formula 1 wherein the groups n, A, B, R1, R2 and R3 may have the meanings given in the claims and in the specification, processes for preparing them, and their use as pharmaceutical compositions, particularly as pharmaceutical compositions for the treatment of respiratory complaints.
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Page/Page column 9
(2010/02/15)
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- Powder formulations for inhalation, comprising enantiomerically pure beta agonists
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The present invention relates to powder formulations for inhalation containing enantiomerically pure compounds of general formula 1 wherein the groups R1, R2, R3 and R4 may have the meanings given in the claims
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