INHIBITOR OF A THEROSCLEROTIC THICKENING OF INTIMA

• Main Authors: SAITO YASUSHI, KITAHARA MASAKI, TOYODA KYOMI, SAKASHITA MITSUAKI, SHIBAZAKI TASHIE
• Format: Patent
• Language: English
• Published: 08.11.1995
• Edition: 6
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

An inhibitor of atherosclerotic intimal thickening, which contains an effective amount of a compound of the formula (I): wherein ring X is phenyl, substituted phenyl or 5- or 6-membered heterocyclic aryl; each of R and R which are independent of each other, is hydrogen, C PI 3/4 alkyl, C PI 1/2 cycloalkyl, C PI alkoxy, n-butoxy, i-butoxy, sec-butoxy, tert-butoxy, R 0R N- (wherein each of R 0 and R which are independent of each other, is hydrogen or C PI alkyl), trifluoromethyl, trifluoromethoxy, difluoromethoxy, fluoro, chloro, bromo, phenyl, phenoxy, benzyloxy, hydroxy, trimethylsilyloxy, diphenyl-tert-butylsilyloxy, hydroxymethyl or -O(CH )POR (wherein R is hydrogen or C PI alkyl, and P is 1, 2, or 3); or R and R together form -CH=CH-CH=CH- or methylenedioxy, when they are at the o-position to each other; R is hydrogen, C PI 3/4 alkyl, C PI 1/4 alkenyl, C PI 1/2 cycloalkyl, C psi PI 1/2 cycloalkenyl or (wherein R7 is hydrogen, C PI 3/4 alkyl, C PI 3/4 alkoxy, C PI alkylthio, chloro, bromo, fluoro, chloromethyl, trichloromethyl, trifluoromethyl, trifluoromethoxy, trichloromethoxy, difluoromethoxy, phenoxy, benzyloxy, hydroxy, trimethylsilyloxy, diphenyl-tert-butylsilyloxy or hydroxymethyl); or C PI alkyl substituted by one (wherein R7 is as defined above) and zero, one or two C PI alkyl; Y is -CH -, -CH CH -, -CH=CH-, -CH -CH=CH-, -CH=CH-CH -, -C(CH )=CH- or -CH=C(CH )-; Z is -Q-CH -W-CH -CO R , (wherein Q is -C(O)-, -C(OR ) - or -CH(OH)-, W is -C(O), -C(OR ) - or -C(R )(OH)-, R is hydrogen or C PI alkyl, R is hydrogen, R 4 (wherein R 4 is alkyl of a chemically or physiologically hydrolyzable alkyl ester moiety, NHR R 4R 5 (wherein each of R , R 4 and R 5 is hydrogen or C PI alkyl), sodium, potassium or 1/2 calcium), each R is independently primary or secondary C PI 1/4 alkyl, or two R together form -(CH ) - or -(CH ) -, and each of R 5 and R 6 which are independent of each other, is hydrogen atom or C PI alkyl, or R 5 and R 6 together form -(CH ) - or -(CH ) -.