13-aza-14-oxo-txa.sub.2 analogues

Details 13-aza-14-oxo-txa.sub.2 analogues 13-aza-14-oxo-txa.sub.2 analogues

C - Chemistry, Metallurgy

07

C

260/477, 260/515

C07C 59/11 (2006.01) C07C 33/14 (2006.01) C07C 51/367 (2006.01) C07C 405/00 (2006.01) C07D 209/18 (2006.01)

Patent

CA 1261826

ABSTRACT OF THE DISCLOSURE This invention discloses a novel 13-aza-14-oxo- TXA2 analogue of the general formula (III): Image (III) wherein A represents -CH2CH2-(CH2)m-, cis-CH=CH-(CH2)m-, -CH2O-(CH2)m-, -S-(CH2)m- or Image (wherein m is 1 to 6); R1 is hydrogen or C1-12 alkyl; R2 is a bond or C1-10 alkenylene; R3 is phenyl, phenoxy, phenylthio, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkyloxy or cycloalkylthio, naphthyl, indolyl, indanyl or amino group; and R4 represents a hydrogen atom or a methyl group, and cyclodextrin clathrates thereof and non- toxic salts thereof. These compounds are useful for the prevention and/or treatment of inflammation, hypertension, thrombus, cerebral apoplexy, asthma, cardiac infarction, angina pectoris, cerebral infarction and death by acute cardiac diseases. When compared to the prior art compound, they exhibit improved pharmaceutical formulation with the equivalent antagonistic activity on TXA2.

483112

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