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US 2010/0305165 A1Published application
Thiocolchicine derivatives, method of making and methods of use thereof
AssigneeTakeda Pharmaceuticals U.S.A., Inc.
InventorRajesh Manchanda
Life of this patent
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Abstract
Disclosed herein are thiocolchicine derivatives suitable for use as muscle relaxants, methods of making the derivatives, and compositions comprising the derivatives.
Claims20
A compound according to structure (I)
- wherein R is
- a.) —C(═O)-(G)-C(═O)OR1 where R1 is C1-C6 alkyl and G is C1-C6 alkylene or C2-C6 alkenylene;
- b.) an amino acid derivative linked through the carboxylate group with the proviso that the amino acid is not glycine;
- c.) —CH2—O(C═O)R2 where R2 is C1-C6 alkyl or C1-C6 alkoxy;
- d.) —C(═O)R3, where R3 is a heteroaryl or a substituted phenyl substituted with 1, 2, or 3 substituents independently chosen from hydroxy, amino, cyano, halogen, C1-C6alkyl, C3-C7cycloalkyl, C1-C6alkoxy, mono- and di-(C1-C4alkyl)amino, —COOH, C2-C6alkoxycarbonyl, C1-C6haloalkyl, or C1-C6haloalkoxy;
- e.) —C(═O)-(G)-C(═O)R1 where R1 is C1-C6 alkyl and G is C1-C6 alkylene or C2-C6 alkenylene;
- f.) —C(═O)-(G)-SO3R4 where R4 is hydrogen or C1-C3 alkyl and G is C1-C6 alkylene or C2-C6 alkenylene;
- g.) —C(═O)-(G)-N(R5)2 where each individual R5 is hydrogen or C1-C6 alkyl and G is C2-C6 alkylene or C2-C6 alkenylene;
- or
- h.) —C(═O)O-(G)-OC(═O)R6 where R6 is C1-C6 alkyl and G is C1-C6 alkylene or C2-C6 alkenylene;
- or a pharmaceutically acceptable salt, solvate, hydrate, crystalline form, non-crystalline form, or stereoisomer thereof.
8 more elements
Dependencies are inferred from the claim text.