Azaindenes

Details Azaindenes Azaindenes

C - Chemistry, Metallurgy

07

D

167/211, 260/273

C07D 471/04 (2006.01) A61K 31/435 (2006.01) A61K 31/495 (2006.01) C07D 473/00 (2006.01) C07D 487/04 (2006.01)

Patent

CA 2017066

The invention concerns novel azaindenes of the formula I (see formula I) wherein A, together with the adjacent vinylene group of the imidazole moiety completes an azene ring selected from pyridine, pyrimidine, pyridazine or pyrazine ring; R1 is (1-8C)alkyl, (3-8C)cycloalkyl, (3-8C)cycloalkyl-(1-4C)alkyl, phenyl or phenyl(1-4C)alkyl; R2 is hydrogen, (1-4C)alkyl, (1-4C)alkoxy, halogeno, trifluoromethyl, cyano or nitro; R3 and R4 are optional substituents on the said azene ring, independently selected from hydrogen, (1-4C)alkyl, (3-8C)cycloalkyl, (1-4C)alkoxy, halogeno, trifluoromethyl, cyano, hydroxy, hydroxymethyl, formyl, and nitro; or when A together with the imidazole moiety to which it is attached is an imidazo[4,5-b]pyridine or imidazo[4,5-c]pyridine group, R3 and R4 when they are on adjacent carbon atoms of A form a trimethylene or tetramethylene group, or together with the adjacent vinylene group of A complete a benzene ring, the latter optionally bearing a halogeno, (1-4C)alkyl or (1-4C)alkoxy substituent; or when A together with the imidazole moiety to which it is attached is other than a 1H-imidazo[4,5-c]pyridine ring, one of R3 or R4 is a carboxy or (1-6C)alkoxycarbonyl group and the other is as defined above; X is phenylene optionally bearing a substituent selected from (1-4C)alkyl, (1-4C)alkoxy and halogeno, or X is a direct bond between the adjacent phenyl and methylene moieties; and Z is 1H-tetrazol-5-yl or a group of the formula -CO.OR5 or -CO.NH.SO2.R6 in which R5 is hydrogen or a non-toxic, biodegradable residue of a physiologically acceptable alcohol or phenol, and R6 is (1-6C)alkyl, (3-8C)cycloalkyl or phenyl; and wherein any of said phenyl moieties may be unsubstituted or bear one or two substituents independently selected from (1-4C)alkyl, (1-4C)alkoxy, halogeno, cyano and trifluoromethyl; or a physiologically acceptable salt thereof except when R5 is other than hydrogen and R3 or R4 is other than carboxyl together with pharmaceutical compositions containing them. The azaindenes antagonise the actions of angiotensin II and are of value in treating conditions such as hypertension and congestive heart failure. The invention further includes processes for the manufacture of the novel compounds and their use in medical treatment.

Affiliated with

Also associated with

Rating

Azaindenes does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Azaindenes, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Azaindenes will most certainly appreciate the feedback.

Rate now

Comments { 0 }

Profile ID: LFCA-PAI-O-2069325