| 摘要 |
<p>5-Phenoxy-2,2-dimethyl- 1-oxopentylaminobenzene derivs. of formula (I) are new (only 1 AB gp. is present; R1 is H, OH, 1-6C alkyl, 1-6 alkoxy, benzyloxy or CF3; R2 is H, OH, halogen, 1-6C alkyl or 1-6C alkoxy; A is (CH2)m or CR4:CR5; m is 1-3; R4 and R5 are H or 1-6C alkyl and are trans to each other; B is COOX; X is H, 1-6C alkyl, NH4 or a metal or organic amine cation; and k is 0 or 1. When k is 0, then R1 is not alkyl and when k is 1, then R1 the 4-position). - (I) are antiarteriosclerotic agents, as they cause an elevation in the high density lipoprotein fraction of cholesterol and some cpds. reduce the low density lipoprotein fraction of cholesterol. Dose is 10-250 mg/kg daily. (0/0) EPAB- EP-134337 B A cpd. having the salt, general structural formula (I) wherein R1 is hydrogen atom, a hydroxyl gp., an alkyl radical having from 1 to 6 carbon atoms, an alkoxy having from 1 to 6 carbon atoms, a benzyloxy radical or a trifluoromethyl radical; R2 is hydrogen atom, a hydroxy gp., a halogen atom, an alkyl radical having from 1 to 6 carbon atoms, or an alkoxy radical having from 1 to 6 carbon atoms, A is (CH2)m wherein m is 0, 1, 2, or 3, or A is (CR4=CR5)n wherein R4 and R5 are trans to each other and are hydrogen atoms or alkyl radicals having from 1 to 6 carbon atoms and n is 0 or 1, and the dotted lines indicate the presence of only one substit. A which must be located at one of the specified positions; B is either 1) CH2OH, CHO, COR3 wherein R3 is an alkyl radical having from 1 to 6 carbon atoms, or CO2X wherein X is a hydrogen atom, an alkyl radical having from 1 to 6 carbon atoms, an ammonium ion or a pharmaceutically acceptable metal or organic amine cation; or 2) SO2NHR6 wherein R6 is a hydrogen atom; an alkyl radical having from 1 to 6 carbon atoms; or (II) wherein D is a bond or an alkylene radical having from 1 to 6 carbon atoms, E is CH or N and R7 is hydrogen atom, an alkyl radical having from 1 to 6 carbon atoms, an alkoxy radical having from 1 to 6 carbon atoms, or a halogen, atom; and k is 0 or 1 with the provisos that, when k is 0, R1 may not be an alkyl radical having from 1 to 6 carbon atoms, and, when k is 1, R1 must be in the 4-position; or a pharmaceutically acceptable salt of the cpd. of formula I. (20pp) - EP-134337 B A cpd. having the salt, general structural formula (I) wherein R1 is hydrogen atom, a hydroxyl gp., an alkyl radical having from 1 to 6 carbon atoms, an alkoxy having from 1 to 6 carbon atoms, a benzyloxy radical or a trifluoromethyl radical; R2 is hydrogen atom, a hydroxy gp., a halogen atom, an alkyl radical having from 1 to 6 carbon atoms, or an alkoxy radical having from 1 to 6 carbon atoms, A is (CH2)m wherein m is 0, 1, 2, or 3, or A is (CR4 =CR5)n wherein R4 and R5 are trans to each other and are hydrogen atoms or alkyl radicals having from 1 to 6 carbon atoms and n is 0 or 1, and the dotted lines indicate the presence of only one substit. A which must be located at one of the specified positions; B is either 1) CH2OH, CHO, COR3 wherein R3 is an alkyl radical having from 1 to 6 carbon atoms, or CO2X wherein X is a hydrogen atom, an alkyl radical having from 1 to 6 carbon atoms, an ammonium ion or a pharmaceutically acceptable metal or organic amine cation; or 2) SO2NHR6 wherein R6 is a hydrogen atom; an alkyl radical having from 1 to 6 carbon atoms; or (II) wherein D is a bond or an alkylene radical having from 1 to 6 carbon atoms, E is CH or N and R7 is hydrogen atom, an alkyl radical having from 1 to 6 carbon atoms, an alkoxy radical having from 1 to 6 carbon atoms, or a halogen, atom; and k is 0 or 1 with the provisos that, when k is 0, R1 may not be an alkyl radical having from 1 to 6 carbon atoms, and, when k is 1, R1 must be in the 4-position; or a pharmaceutically acceptable salt of the cpd. of formula I. (20pp)</p> |
