| 摘要 |
A compound of the formula as shown are inhibitors of tumor necrosis factor alpha and phosphodiesterase and can be used to combat cachexia, endotoxic shock, retrovirus replication, asthma, and inflammatory conditions. A typical embodiment is 3-Phthalimido-3-(3,4-dimethoxyphenyl)propionitrile. Wherein; Y is-C=N or -C(O)-(CH2)mCH3; m is 0, 1, 2, or 3; R5 is (i) o-phenylene, unsubstituted or substituted with 1 to 3 substituents each selected independently from nitro, cyano, trifluoromethyl, carbethoxy, carbomethoxy, carbopropoxy, acetyl, carbamoyl, carbamoyl substituted with and alkyl of 1 to 3 carbon atoms, acetoxy, carboxy, hydroxy, amino, amino substituted with an alkyl of 1 to 3 carbon atoms, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, or halo; (ii) the divalent residue of pyridine, pyrrolidine, imidizole, naphthalene, or thiophene; (iii) a divalent cycloalkyl of 4-10 carbon atoms, substituted and unsubstituted, alkyl of 1-10 carbon atoms, alkoxy 1-10 carbon atoms, phenyl or halo; (iv) disubstituted vinylene, substituted with nitro, cyano, trifluromethyl, carbethoxy, carbomethoxy; R6 is -CO-, -CH2-, -CH2CO- or -SO2-; R7 is (i) cyclic or bicyclic alkyl of 4 to 12 carbon atoms; (ii) cyclic or bicyclic alkyl of 4 to12 carbon atoms; (iii) pyridyl; (iv) phenyl substituted with one or more substituents each selected independently of the other from nitro, cyano, trifluoromethyl, carbethoxy, carbomethoxy, carbopropoxy, acetyl, carbamoyl, acetoxy, carboxy, hydroxy, amino, straight or branched alkyl of 1 to 10 carbon atoms, straight or branched, alkoxy of 1 to 10 carbon atoms, or halo; (v) benzyl substituted with one to three substituents each selected independently from the group consisting of nitro, cyano, trifluoromethyl, carbethoxy, carbomethoxy, carbopropoxy, acetyl, carbamoyl, acetoxy, carboxy, hydroxy, amino, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 10 carbon atoms, or halo; (vi) naphthyl; or (vi) benzyloxy; and; n has a value of 0, 1, 2, or 3.
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