Mibefradil-based compounds as calcium channel blockers...

Details Mibefradil-based compounds as calcium channel blockers... Mibefradil-based compounds as calcium channel blockers...

C - Chemistry, Metallurgy

07

D

C07D 235/08 (2006.01) A61K 31/415 (2006.01) C07C 211/43 (2006.01) C07C 233/08 (2006.01) C07C 317/14 (2006.01) C07D 235/14 (2006.01)

Patent

CA 2462913

The subject invention provides novel calcium channel blockers based upon mibefradil: (I) wherein: X = a bond, (CH2)n, O, S, or O(CH2)n wherein = 1-6; R1 = C1-6 alkyl, optionally substituted with OH or NH2; R2 = F or COOR5, wherein R5 is C1-6 alkyl, optionally substituted with OH or NH2; R3 = CH3 or (CH2)~ - COOR6, wherein n =1-6 and R6 is C1-6 alkyl, optionally substituted with OH or NH2; R4 = (CH2)n - COR7R8 -(CH2)n -R10R11 or (II) R7 = 0, NH, or NR9, R8 = optionally substituted aryl or heterocycle, R9 = C1-6 alkyl, R10 = 0, S, SO, S02, NH, NR12 or N(CH2 )m COOR13 R11 = aryl of heterocyclyl optionally substituted with (CH2)n, COOR14, R12 = C1-6 alkyl, optionally substituted with OH or NH2, R13 = C1-6 alkyl, optionally substituted with OH or NH2, R14 = C1-6 alkyl, optionally substituted with OH or NH2, R15 = (CH2)n COOR16, R16 = C1-6 alkyl, optionally substituted with OH or NH2, R17 = not present or COOR18 wherein R18 is C1-6 alkyl, optionally substituted with OH or NH2, and wherein n =1-6, useful in the treatment of hypertension, angina pectoris, ischemia, arrhythmias and cardiaq, insufficiency.

L'invention concerne de nouveaux bloqueurs de canaux calciques à base de mibefradil: (I) formule dans laquelle : X = désigne une liaison , (CH¿2?)¿n?, O, S, ou O(CH¿2?)¿n? où = 1-6; R¿1? = C¿1-6? alkyl, éventuellement substitué par OH ou NH¿2?; R¿2? = F ou COOR¿5?, où R¿5? désigne C¿1-6? alkyle, éventuellement substitué par OH ou NH¿2?; R¿3? = CH¿3? ou (CH¿2?)~ - COOR¿6?, où n =1-6 et R¿6 ?désigne C¿1-6? alkyle, éventuellement substitué par OH ou NH¿2?; R¿4? = (CH¿2?)¿n? - COR¿7?R¿8? -(CH¿2?)¿n ?-R¿10?R¿11? ou (II) R¿7? = 0, NH, ou NR¿9?, R¿8? = éventuellement substitué par un aryle ou un hétérocycle , R¿9? = C¿1-6? alkyle, R¿10? = 0, S, SO, S0¿2?, NH, NR¿12? ou N(CH¿2? )¿m? COOR¿13? R¿11? = aryle ou hétérocyclyle éventuellement substitué par (CH¿2?)¿n,? COOR¿14?, R¿12? = C¿1-6? alkyl, éventuellement substitué par OH ou NH¿2?, R¿13? = C¿1-6? alkyle, éventuellement substitué par OH ou NH¿2?, R¿14? = C¿1-6? alkyle, éventuellement substitué par OH ou NH¿2?, R¿15? = (CH¿2?)¿n? COOR¿16?, R¿16? = C¿1-6? alkyle, éventuellement substitué par OH NH¿2?, R¿17? = soit inexistant, soit désigne COOR¿18? où R¿18? désigne C¿1-6? alkyle, éventuellement substitué par OH ou NH¿2?, et où n =1-6. Les composés selon l'invention sont utilisés pour le traitement de l'hypertension, angine de poitrine, ischémie, arythmie et insuffisance cardiaque.

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