| 主权项 |
1. A method of inhibiting one or more activities in a cell, said method comprising administering to a subject in need thereof a compound having a structure according to Formula I:or a pharmaceutically acceptable salt, a hydrate or a solvate thereof,
wherein: n is an integer from 1 to 6, wherein when n is 1, Cn, Bn, Rn, and Y are absent, and C1 is attached to Bn; each of B1, B2, . . . Bn−1 and Bn is independently selected from the group consisting of oxygen, sulfur, nitrogen, phosphorus and silicon, whereby each of said nitrogen, phosphorus and silicon is substituted by at least one substituent selected from the group consisting of hydrogen, lone pair electrons, alkyl, halo, cycloalkyl, aryl, hydroxy, thiohydroxy, alkoxy, aryloxy, thioaryloxy, thioalkoxy and oxo; each of A1, A2, . . . An−1 and An is independently selected from the group consisting of CR″R′″, C═O and C═S, Y is selected from the group consisting of hydrogen, acyl, alkyl, aryl, cycloalkyl, carboxy, saccharide, phosphoric acid, phosphoryl choline, phosphoryl ethanolamine, phosphoryl serine, phosphoryl cardiolipin, phosphoryl inositol, ethylphosphocholine, phosphorylmethanol, phosphorylethanol, phosphorylpropanol, phosphorylbutanol, phosphorylethanolamine-N-lactose, phosphoethanolamine-N-glutaric acid, phosphoethanolamine-N-[methoxy(propylene glycol)], phosphoinositol-4-phosphate, phosphoinositol-4,5-biphosphonate, phosphoinositol-4,5-bisphosphate, pyrophosphate, phosphoethanolamine-diethylenetriamine-pentaacetate, dinitrophenyl-phosphoethanolamine, phosphoglycerol and a moiety having the general formula: wherein: each of B′ and B″ is independently selected from the group consisting of sulfur and oxygen; and each of D′ and D″ is independently selected from the group consisting of hydrogen, alkyl, amino substituted alkyl, cycloalkyl, phosphonate and thiophosphonate; and each of X1, X2, . . . Xn−1 is independently a saturated or unsaturated hydrocarbon having the general Formula II: wherein m is an integer from 1 to 7; and Z is selected from the group consisting of:
H, and —OR, wherein W is selected from the group consisting of oxygen and sulfur; wherein at least one of X1, X2, . . . Xn−1 comprises a Z other than hydrogen, and wherein: each of R1, R′1, R2, . . . Rn−1, Rn, R′n, each of R″ and R′″ and each of Ra, R′a, Rb, R′b, . . . Rm−1, R′m−1, Rm and R′m is independently selected from the group consisting of hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl, halo, trihalomethyl, hydroxy, alkoxy, aryloxy, thiohydroxy, thioalkoxy, thioaryloxy, phosphonate, phosphate, phosphinyl, sulfonyl, sulfinyl, sulfonamide, amide, carbonyl, thiocarbonyl, C-carboxy, O-carboxy, C-carbamate, N-carbamate, C-thiocarboxy, S-thiocarboxy and amino, or, alternatively, at least two of R1, R′1, R2, . . . Rn−1, Rn and R′n and/or at least two of Ra, R′a, Rb, R′b, . . . Rm−1, R′m−1, Rm and R′m form at least one four-, five- or six-membered aromatic, heteroaromatic, alicyclic or heteroalicyclic ring, or a pharmaceutically acceptable salt, a hydrate or a solvate thereof, in combination with another agent; wherein said one or more activities that are inhibited are one or more of TLR2 activity, CD14 activity, and monocyte chemotaxis activity. |
