Imidazolyl and pyridyl derivatives of phenyl substituted...

C - Chemistry – Metallurgy – 07 – D

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167/211, 260/278

C07D 401/10 (2006.01) A61K 31/44 (2006.01) C07D 401/14 (2006.01) C07D 521/00 (2006.01)

Patent

CA 2005490

A B S T R A C T The invention relates to imidazolyl and pyridyl derivatives of phenyl substituted 1,4-dihydropyridines of formula (I) Image (I) wherein Het is Image or Image ; A represents a direct linkage, -CH2-, -CH2-CH2- or, when Het is Image , A may also represent -CH=CH-; R is hydrogen, halogen, C1-C3 alkyl or C1-C3 alkoxy; each of R3 and R4, which may be the same or different, is a C1-C3 alkyl group; one of R1 and R2 is a group -OR' wherein R' is C1-C6 alkyl either unsubstituted or omega substituted by C1-C3 alkoxy or cyano, and the other is, independently a) a group -OR' as defined hereabove; or b) a group Image wherein each of R" and R''', which may be the same or different, is hydrogen or C1-C3 alkyl; or Abstract 2 c) a group -ORIV wherein RIV is hydrogen or a substituent selected from the group consisting of (i) -(CH2)m-CH=CH-Ph, wherein m is an integer of 1 to 3 and Ph is a phenyl group either unsubstituted or substituted by one to three substituents chosen among C1-C3 alkyl, C1-C3 alkoxy and halogen; (ii) Image wherein Ph is as defined above; Q is a C2-C5 alkylene radical; n is zero, 1 or 2; and each RV is, independently, hydrogen, C1-C3 alkyl or Ph, wherein Ph is as defined above; (iii) Image wherein m, n, RV and Ph are as defined above; and (iv) Image wherein p is 2 or 3 and Ph is as defined above, which are useful as Thromboxane A2 (TxA2) Synthase inhibitors and as calcium antagonists.

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