Derivatives of 3,4-dihydro - 2H - 1,4 benzo oxazine and thiazine as CETP inhibitors

摘要

Pharmaceutical compositions that contain them and uses to prevent or treat coronary heart disease, and as anticolesterol and antilipidemic agents. Claim 1: A compound of formula (1) in which: L is a covalent bond or O; X is O, or S; Q is C6-10 aryl or 5-6 membered heteroaryl, n is 0 to 3; m is from 0 to 3; R1 is C1-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, C3-10 cycloalkyl, 5- or 6-membered heteroaryl, wherein each of the C1-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, cycloalkyl C3-10, 5- or 6-membered heteroaryl may be optionally substituted; or R1 is phenyl optionally substituted with 1 or 2 members selected from Ra and Rb,where Ra and Rb are independently selected from the group consisting of optionally substituted C1-4 alkyl, halogenated C1-4 alkyl, optionally substituted C2-4 alkenyl, optionally substituted C2-4 alkynyl, C1- alkoxy 4 optionally substituted, halogenated C1-4 alkoxy, optionally substituted C1-4 alkylthio, halo, cyano and hydroxy, or Ra and Rb together with the carbon atoms of the phenyl ring to which they are attached form a heterocyclyl of 5 or 6 members optionally substituted fused to the phenyl ring; each R2 is independently selected from halo, hydroxy, cyano, C1-4 alkoxy, halogenated C1-4 alkoxy, C1-4 alkyl,halogenated C1-4 alkyl, C2-4 alkenyl, C2-4 alkynyl and -C (O) H; each R3 is independently selected from C1-4 alkyl, halogenated C1-4 alkyl, C2-4 alkenyl, C2-4 alkynyl, C1-4 alkoxy, halo, cyano and hydroxy; R4 is C1-10 alkyl optionally substituted with 1-3 members independently selected from halo, oxo, hydroxy, halogenated C1-4 alkyl, C1-4 alkoxy, C3-8 cycloalkyl, CN, tert-butyldimethylsilyloxy, substituted heterocyclyl optionally and -NRcRd, where Rc and Rd are independently selected from H, optionally substituted C1-3 alkyl, -C (O) C1-3 alkyl, - C (O) O-C1-3 alkyl, and -SO2 C1-3alkyl,O R4 refers to C1-6 tar, which is replaced by isomerization or phenyl, and consists of 1 to 3 independently selected halogenated, hydroxy, c1-3 tar, c1-3 halogenated tar, alcoxi C1-4 and alcoxi C1-4 halogenated, as well as acceptable salts of dwarfs, diacetylene, ceramics, solutions or drugs.