- 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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Paragraph 0171
(2019/11/11)
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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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- Beta2-receptorexcitant and preparation method and application thereof
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The invention relates to a following formula I showed compound in a free form, a salt form or a solvated form and having a beta2-receptor exciting effect. II and III are contained in R1, Ar are following formula groups IV and V, definition of R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R13, R14, R15, R16, m and o is shown in the description. The invention further relates to a preparation method of the compound and application of a compound serving as a drug, in particular to treatment of diseases such as a chronic obstructive pulmonary disease, asthma and heart failure the aspects of a respiratory and cardiovascular system and a cardiovascular system.
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Paragraph 0115; 0116; 0117
(2017/08/25)
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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 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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- 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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- 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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- 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 16
(2008/06/13)
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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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