QUATERNARY AMMONIUM DIPHENYLMETHYL COMPOUNDS USED AS MUSCARINIC RECEPTOR ANTAGONISTS Russian patent published in 2012 - IPC C07D207/08 C07D207/09 C07D207/46 A61K31/40 A61P11/00 

Abstract RU 2452728 C2

FIELD: chemistry.

SUBSTANCE: invention relates to novel compounds of formula l , where a and b are independently equal to 0-5; R1 and R2 independently denote -C1-4alkyl, CN, halogen, -ORa, -CH2OH, Ra independently denotes H, C1-4alkyl; R3 denotes -C(O)NR3aR3b, -CN; R3a and R3b denote H; R5 denotes -C1-6alkyl; Q denotes -C0-5-alkylene-Q'-C0-1alkylene-, Q' denotes -CH2-, -CH=CH-, -C≡C-, -O-, -S-, -S(O)-, -SO2-, -C(O)-, -OC(O)-, -C(O)O-, -NRQ1C(O)-, -C(O)NRQ1-, -NRQ2-C(O)-NRQ3-, -C=N-O-, -S-S- and -C(=N-O-RQ4)-, RQ1 denotes H; RQ2 and RQ3 denote H; RQ4 denotes -C1-4alkyl, benzyl; e equals 0-5; R6 independently denotes halogen, -C1-4alkyl, -C0-4alkylene-OH, CN, -C (O)O-C1-4alkyl, -O-C1-4alkyl, -S-C1-4alkyl, -NH-C(O)-C1-4alkyl, -N (C1-4alkyl)2 and -N+(O)O; where the alkyl group in R6 is optionally substituted with 1-5 F atoms; one -CH2- group in Q is optionally substituted with one -OH; or a pharmaceutically acceptable salt or zwitterion form thereof.

EFFECT: compounds exhibit antagonistic activity towards muscarinic receptors, which enables their use to produce pharmaceutical compositions for treating lung diseases such as chronic obstructive pulmonary disease and asthma.

32 cl, 16 ex

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RU 2 452 728 C2

Authors

Tszi Ju-Khua

Khasfeld Krehjg

Lehndzh Kristofer

Li Rik

Mu Juntsi

Dates

2012-06-10Published

2008-02-21Filed