3,4-disubstituted 1,2,5-oxadiazole 2-oxides, processes for...

C - Chemistry – Metallurgy – 07 – D

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C07D 271/08 (2006.01) A61K 31/42 (2006.01) A61K 31/475 (2006.01) A61K 31/50 (2006.01) A61K 31/505 (2006.01) A61K 31/54 (2006.01) A61K 31/55 (2006.01) C07D 413/14 (2006.01)

Patent

CA 1173034

ABSTRACT OF THE DISCLOSURE 3,4-Disubstituted 1,2,5-oxadiazole 2-oxides of the formula I Image (I) wherein, when R2 represents CH3, R1 denotes -CONHR3NR24, Image Image Image -CONHR3OR7, -CONHCH2CH=CH2, -CONHR8, -CONR9R10, -CONHR11CO2R4, -CONHR11CONH?2, Image -CONHR11-Het, Image , -CONHR11CONHR8, and when R2 is other than CH3 and has one of the meanings indicated above for R1, R1 denotes -CH3, R3 denotes an alkylene radical -CnH2n-, wherein ?? 2, 3 or 4, R4 denotes -CH3 or -C2H5, R5 and R6 denote -H, -CH3, -C2H5, -OCH3 or Cl, R7 denotes -H, -CH3 or -C2H5, R8 denotes C1-C6 alkyl or C3-C7 cycloalkyl, R9 and R10 denote C1-C4 alkyl, R11 denotes an alkylene radical -CmH2m wherein m = 1, 2 or 3, Het denotes a pyridyl, pyrimidinyl, thienyl, oxazolyl, imidazolyl, furanoyl or thiazolyl radical, X denotes -(CH2)p-, -(CH2)2-0-(CH2)2- or Image and R2 denotes -CH3 and, when R1 denotes -CH3, R2 has one of the meanings indicated for R1, with the exception of -CH3, and pharmacologically acceptable acid addition compounds thereof. These compounds may be used for curing, or preventing cardiovascular system diseases, such as antihypertensives.

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