Mitotic kinesin inhibitor
View Patent ↗A mitotic kinesin Eg5 inhibitor which comprises a thiadiazoline derivative represented by the general formula (I) or a pharmacologically acceptable salt thereof as an active ingredient: [wherein R 1 represents a hydrogen atom and the like, R 2 represents a hydrogen atom, —C(═W)R 6 (wherein W represents an oxygen atom or a sulfur atom, and R 6 represents substituted or unsubstituted lower alkyl and the like) and the like, R 3 represents —C(═Z)R 19 (wherein Z represents an oxygen atom or a sulfur atom, and R 19 represents substituted or unsubstituted lower alkyl and the like) and the like, R 4 represents substituted or unsubstituted lower alkyl and the like, and R 5 represents substituted or unsubstituted aryl and the like] and the like are provided.
1. A thiadiazoline derivative represented by the following formulas (221) or (237),
or a pharmacologically acceptable salt thereof.
2. The thiadiazoline derivative according to claim 1 , wherein the thiadiazoline derivative is represented by formula (221),
or a pharmacologically acceptable salt thereof.
3. The thiadiazoline derivative according to claim 1 , wherein the thiadiazoline derivative is represented by formula (237),
or a pharmacologically acceptable salt thereof.
4. A medicament composition comprising the thiadiazoline derivative or a pharmaceutically acceptable salt thereof according to claim 1 as an active ingredient.
5. A medicament composition comprising the thiadiazoline derivative or a pharmaceutically acceptable salt thereof according to claim 2 as an active ingredient.
6. A medicament composition comprising the thiadiazoline derivative or a pharmaceutically acceptable salt thereof according to claim 3 as an active ingredient.
7. A method for inhibiting a mitotic kinesin Eg5 comprising administering an effective amount of a thiadiazoline derivative or a pharmacologically acceptable salt thereof according to claim 1 to inhibit the mitotic kinesin Eg5.
8. The method according to claim 7 wherein the thiadiazoline derivative or a pharmacologically acceptable salt thereof is administered to a human.
9. A method for inhibiting a mitotic kinesin Eg5 comprising administering an effective amount of a thiadiazoline derivative or a pharmacologically acceptable salt thereof according to claim 2 to inhibit the mitotic kinesin Eg5.
10. The method according to claim 9 wherein the thiadiazoline derivative or a pharmacologically acceptable salt thereof is administered to a human.
11. A method for inhibiting a mitotic kinesin Eg5 comprising administering an effective amount of a thiadiazoline derivative or a pharmacologically acceptable salt thereof according to claim 3 to inhibit the mitotic kinesin Eg5.
12. The method according to claim 11 wherein the thiadiazoline derivative or a pharmacologically acceptable salt thereof is administered to a human.