| 摘要 |
The compound of formula (I) wherein: R1 is (C2-C9) heteroaryl optionally substituted or naphthalene-2-yl. R2 is phenyl-(CH2)m-, naphthyl-(CH2)m-, (C3-C10)cycloalkyl-(CH2)m-, (C1-C6)alkyl or (C2-C9)heteroaryl-(CH2)m-, wherein m is an integer from 0 to 4 wherein each of said phenyl, naphthyl, (C3-C10)cycloalkyl or (C2-C9)heteroaryl moieties may be optionally substituted. R3 is hydrogen, (C1-C10) alkyl, (C3-C10) cycloalkyl-(CH2)n-, (C2-C9)heterocycloalkyl-(CH2)n-, (C2-C9)heteroaryl-(CH2)n or aryl-(CH2)n wherein n is an integer from 0 to 6 and wherein the (C1-C10)alkyl group, the (C3-C10)cycloalkyl moiety, the (C2-C9)heterocycloalkyl moiety, the (C2-C9)heteroaryl moiety or the aryl moiety may be optionally substituted. R4 is hydrogen, (C1-C6) alkyl, hydroxy, (C1-C6) alkoxy, hydroxy (C1-C6 ) alkyl, (C1-C6)alkoxy(C=O)-, (C3-C10)cycloalkyl-(CH2)p-, (C2-C9)heterocycloalkyl-(CH2)p-, (C2-C9)heteroaryl-(CH2)p- phenyl-(CH2)p-, or naphthyl-(CH2)p wherein p is an integer 0 to 4 and the (C2-C9)heterocycloalkyl, (C2-C9)heteroaryl, phenyl and naphthyl groups may be optionally substituted. R4 and R5 together with the nitrogen atom to which they are attached form a (C2-C9)heterocycloalkyl group wherein any of the ring atoms may be optionally substituted. R5 is hydrogen, (C1-C6) alkyl or amino. R6 is hydrogen, (C1-C6)alkyl, (C1-C6)alkoxy-(CH2)g-, (C1-C6)alkoxy(C=O)-(CH2)g-, (C1-C6)alkyl-(SO2)-(CH2)g-, (C6-C10)aryloxy-(CH2)g-, (C6-C10)aryloxy(C=O)-(CH2)g-, and (C6-C10)aryl-(SO2)-(CH2)g-, wherein g is an integer from 1 to 4. Providing that when either R4 or R5 is hydrogen and the other of R4 or R5 is (C1-C6) alkyl or morpholinoethyl, R2 is (C3-C10) cycloalkyl or isopropyl and R3 is (C3-C5) alkyl, phenyl, methylvinyl, dimethylvinyl, halovinyl, hydroxy (C1-C3) alkyl or amino (C1-C4) alkyl or amino (C1-C4) alkyl then R1 must be other than indol-5-yl, 6-azaindol-2-yl, 2,3-dichloro-pyrol-5-yl, 4-hydroxyquinolin-3-yl, 2-hydroxyquinoxalin-3-yl, 6-azaindolin-3-yl or optionally substituted indol-2 or 3-yl. Providing that when R5 is hydrogen, then R4 must be other than pyrazolyl, isoxazolyl, imidazolylmethyl, thiazolyl, thiazolylmethyl, triazolyl, tetrazolyl or oxazolylmethyl. And the pharmaceutically acceptable salts of the compound. Also described are pharmaceutical composition comprising the compound of formula (I). The compounds of formula (I) are useful for autoimmune diseases, acute and chronic inflammatory conditions, allergic conditions, infection associated with inflammation, viral, transplantation tissue rejection, atherosclerosis, restenosis, HIV infectivity and glaucomatous.
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