发明名称 NEW CYCLOHEXYLAMINE DERIVATIVES HAVING BETA2 ADRENERGIC AGONIST AND M3 MUSCARINIC ANTAGONIST ACTIVITIES
摘要 Abstract - 602556 Disclosed are cyclohexyl amine derivatives as represented by the general formula (I), or pharmaceutically acceptable salts or N-oxides or solvates or deuterated derivatives thereof, wherein: both X and Y represents a hydrogen atom or, X together with Y form the group -CH=CH-, -CH2-O- or -S-, wherein in the case of -CH2-O- the methylene group is bound to the carbon atom in the amido substituent holding X and the oxygen atom is bound to the carbon atom in the phenyl ring holding Y; R1 and R2 independently represent a hydrogen atom or an alkyl group; R3 represents a C(Ra)(Rb)(Rc) group, a 9-(Ra)-fluoren-9-yl group or a 9-(Ra)-xanthen-9-yl group; and wherein the remaining substituents are as defined herein. Representative compounds include formic acid - trans-4-[(9-{ [(2R)-2-hydroxy-2-(8-hydroxy-2-oxo-1,2-dihydroquinolin-5-yl)ethyl]amino} nonyl)(methyl)amino]cyclohexyl hydroxy(di-2-thienyl)acetate, trans-4-[{ 2-[({ [2-chloro-4-({ [(2R)-2-hydroxy-2-(5-hydroxy-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-8-yl)ethyl]amino} methyl)-5-methoxyphenyl]amino} carbonyl)oxy]-ethyl} (methyl)amino]cyclohexyl hydroxy(di-2-thienyl)acetate and trans-4-[{ 2-[({ [2-chloro-4-({ [(2R)-2-hydroxy-2-(8-hydroxy-2-oxo-1,2-dihydroquinolin-5-yl)ethyl]amino} methyl)-5-methoxyphenyl]amino} carbonyl)oxy]ethyl} -(methyl) amino]cyclohexyl (2S)-cyclopentyl(hydroxy)2-thienylacetate. Also disclosed is a pharmaceutical composition comprising a compound as defined above in association with a pharmaceutically acceptable diluent or carrier, for the treatment of a pathological condition or disease pulmonary diseases, pre-labor, glaucoma, neurological disorders, cardiac disorders, inflammation and gastrointestinal disorders, asthma and/or chronic obstructive pulmonary disease.
申请公布号 NZ602556(A) 申请公布日期 2013.10.25
申请号 NZ20110602556 申请日期 2011.05.13
申请人 ALMIRALL, S.A. 发明人 PRAT QUINONES, MARIA;FONQUERNA POU, SILVIA;PUIG DURAN, CARLOS;LUMERAS AMADOR, WENCESLAO;AIGUADE BOSCH, JOSE;CATURLA JAVALOYES, JUAN FRANCISCO
分类号 C07D409/14;A61K31/381;A61K31/428;A61K31/4709;A61K31/538;A61P11/00;C07D215/22;C07D215/24;C07D215/26;C07D265/36;C07D277/68 主分类号 C07D409/14
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