Back to results
US 6,617,335 B1Granted
Preparation and drug composition of bis-benzyl-isoquinoline class alkaloids
AssigneeKanghong USA, Inc.
InventorsFengpeng Wang, Li Wang, Jinsong Yang, Donglin Chen, Xixian Jian
Life of this patent
Estimating the term…
Abstract
This invention relates to the preparation of bis-isoquinoline derivatives of general formula (I) and salts thereof, which possesses multi-drug resistance (MDR) reversal activities. Drug compositions and formulations comprising bis-isoquinoline derivatives of general formula (I) and salts thereof are provided for use as sensitivity enhancers in cancer chemotherapy. Methods for inhibiting MDR by treatment with bis-isoquinoline derivatives are also provided.
Claims12
A bis-isoquinoline alkaloid compound of formula (I) and salts thereof,
- wherein:
- R1 is hydrogen, straight chain or branched chain alkyl containing 1-10 carbon atoms;
- R2 and R3 are hydrogen, substituted acyl, straight chain or branched chain alkane in which the alkane is optionally interrupted by replacement with heterogeneous atoms O, N, or S, or R2 and R3 in combination comprise a ketone or thioketone;
- R4 and R5 are each selected from the group consisting of a hydrogen, a substituted acyl, a straight chain or branched chain alkyl in which the alkyl chain is optionally interrupted by replacement with a heterogeneous atom N or S, or R4 and R5 in combination consisting of a thioketone;
- X1, X2, X3 and X4 are same or different, and can be individually substituted by a halogen or substituted by straight or branched chain alkyloxy or acyloxy groups containing 1-10 carbon atoms, further wherein when R4 and R5 are both hydrogen, either (a) any one of X1, X2, X3 and X4 is a halogen or (b) X1 is a straight or branched chain alkyloxy or acyloxy group, the alkyloxy group containing at least 3 carbon atoms;
- C(1) and C(1′) are any possible combination of all stereoisomers of C(1) and C(1′);
- and
- n is an integer between 1 and 4 for X2, n is an integer between 0 and 4 for X4, and n is an integer between 1 and 3 for X1 and X3.
5 more elements
Dependencies are inferred from the claim text.