Indole derivatives with antiviral activity
AssigneeShionogi & Co., Ltd.
InventorsToshio Fujishita, Tomokazu Yoshinaga
Life of this patent
Estimating the term…
Abstract
A compound of the formula: wherein R1 is hydrogen, lower alkyl, or optionally substituted arylsulfonyl, or the like, R2 is hydrogen, lower alkyl, or optionally substituted aralklyl, or the like, R3, R4, R5, and R6 each is independently hydrogen, halogen, trihalogenated lower alkyl, or the like, X is hydroxy or optionally substituted amino, Y is COOR R is hydrogen or an ester residue), optionally substituted aryl, or optionally substituted heteroaryl, has integrase inhibition activity, and is useful as an anti-HIV drug.
Claims20
A compound of the formula:
- wherein
- R1 is hydrogen, lower alkyl, cycloalkyl lower alkyl, lower alkylsulfonyl, lower alkylcarbonyl, substituted or unsubstituted aryl, substituted or unsubstituted aralkyl, substituted or unsubstituted arylsulfonyl, substituted or unsubstituted arylcarbonyl, substituted or unsubstituted heteroaryl, substituted or unsubstituted heteroaralkyl, substituted or unsubstituted heteroarylsulfonyl, lower alkoxycarbonyl, substituted or unsubstituted sulfamoyl, or substituted or unsubstituted carbamoyl;
- R2 is hydrogen, lower alkyl, lower alkylcarbonyl, substituted or unsubstituted aryl, substituted or unsubstituted aralkyl, substituted or unsubstituted arylcarbonyl, substituted or unsubstituted heteroaryl, substituted or unsubstituted heteroaralkyl, substituted or unsubstituted arylthio, substituted or unsubstituted arylsulfinyl, substituted or unsubstituted arylsulfonyl, substituted or unsubstituted heterocyclyl lower alkyl, or substituted or unsubstituted heterocyclyl sulfonyl;
- R3, R4, R5, and R6 each is independently hydrogen, halogen, trihalogenated lower alkyl, hydroxy, lower alkoxy, nitro, amino, esterified or unesterified carboxy, substituted or unsubstituted aralkyloxy, or substituted or unsubstituted arylsulfonyloxy;
- X is hydroxy or substituted or unsubstituted amino;
- Y is COOH, an ester, substituted or unsubstituted aryl, or substituted or unsubstituted heteroaryl,
- provided that a compound wherein R1, R2, R3, R5, and R6 each is hydrogen;
- R4 is hydrogen, methoxy, or chloro;
- X is hydroxy;
- and Y is COOC2H5 is excluded,
- a tautomer, or a pharmaceutically acceptable salt, or a hydrate thereof.
A pharmaceutical composition containing, as an active ingredient, an indole derivative having a group of the formula:
- —C(O)CH═C(X)Y, wherein X and Y are as defined above, at the 3-position.
Dependencies are inferred from the claim text.