Thiadiazoline derivative
View Patent ↗(wherein R 1 and R 4 are the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkynyl, substituted or unsubstituted lower alkenyl, or the like; R 5 represents a substituted or unsubstituted heterocyclic group, substituted or unsubstituted aryl, or the like; R 2 represents —C(═W)R 6 or the like; R 3 represents a hydrogen atom, —C(═W A )R 6A , or the like) Antitumor agents which comprises a thiadiazoline derivative represented by the aforementioned general formula (I) or a pharmacologically acceptable salt thereof as an active ingredient are provided.
1. A compound of formula
wherein
R 2A is —COC(CH 3 ) 3 , R 3A is —COCH 3 and R 4A is —CH 2 NHSO 2 CH 3 ;
R 2A is —COC(CH 3 ) 3 , R 3A is —COCH 3 and R 4A is —CH 2 NHSO 2 CH 2 Cl;
R 2A is —COCH 3 , R 3A is —COCH 3 and R 4A is —CH 2 NHSO 2 CH 2 Cl;
R 2A is —COC(CH 3 ) 3 , R 3A is —COCH 3 and R 4A is —CH 2 NHSO 2 CH═CH 2 ;
R 2A is —COC(CH 3 ) 3 , R 3A is —COC(CH 3 ) 3 and R 4A is —CH 2 NHSO 2 CH═CH 2 ;
R 2A is —COC(CH 3 ) 3 , R 3A is —COCH 3 and R 4A is
R 2A is —COC(CH 3 ) 3 , R 3A is —COCH 3 and R 4A is —CH 2 NHSO 2 (CH 2 ) 2 NHCH 2 CH 3 ;
R 2A is —COC(CH 3 ) 3 , R 3A is —COCH 3 and R 4A is —CH 2 NHSO 2 (CH 2 ) 2 N(CH 3 ) 2 ;
R 2A is —COC(CH 3 ) 3 , R 3A is —COCH 3 and R 4A is —CH 2 NHSO 2 (CH 2 ) 2 NH(CH 2 ) 2 OH;
R 2A is —COC(CH 3 ) 3 , R 3A is —COC(CH 3 ) 3 and R 4A is —CH 2 NHSO 2 (CH 2 ) 2 NHCH 2 CH 3 ;
R 2A is —COC(CH 3 ) 3 , R 3A is —COC(CH 3 ) 3 and R 4A is —CH 2 NHSO 2 (CH 2 ) 2 N(CH 3 ) 2 ;
R 2A is —COC(CH 3 ) 3 , R 3A is —COCH(CH 3 ) 2 and R 4A is —(CH 2 ) 2 NHSO 2 CH 3 ;
R 2A is —COCH 2 CH 3 , R 3A is —COCH 2 CH 3 and R 4A is —(CH 2 ) 2 NHSO 2 CH 3 ; or
R 2A is —COC(CH 3 ) 3 , R 3A is —COCH 2 CH 3 and R 4A is —(CH 2 ) 2 NHSO 2 CH 3 ;
or a pharmacologically acceptable salt thereof.
2. A compound according to claim 1 of formula
wherein
R 2A is —COC(CH 3 ) 3 , R 3A is —COCH 3 and R 4A is —CH 2 NHSO 2 CH═CH 2 ;
R 2A is —COC(CH 3 ) 3 , R 3A is —COC(CH 3 ) 3 and R 4A is —CH 2 NHSO 2 CH═CH 2 ;
R 2A is —COC(CH 3 ) 3 , R 3A is —COCH 3 and R 4A is —CH 2 NHSO 2 (CH 2 ) 2 NHCH 2 CH 3 ;
R 2A is —COC(CH 3 ) 3 , R 3A is —COC(CH 3 ) 3 and R 4A is —CH 2 NHSO 2 (CH 2 ) 2 NHCH 2 CH 3 ; or
R 2A is —COC(CH 3 ) 3 , R 3A is —COCH(CH 3 ) 2 and R 4A is —(CH 2 ) 2 NHSO 2 CH 3 ;
or a pharmacologically acceptable salt thereof.
3. A compound according to claim 2 of formula
wherein
R 2A is —COC(CH 3 ) 3 , R 3A is —COC(CH 3 ) 3 and R 4A is —CH 2 NHSO 2 (CH 2 ) 2 NHCH 2 CH 3 ;
or a pharmacologically acceptable salt thereof.
4. A compound according to claim 2 of formula
wherein
R 2A is —COC(CH 3 ) 3 , R 3A is —COCH(CH 3 ) 2 and R 4A is —(CH 2 ) 2 NHSO 2 CH 3
or a pharmacologically acceptable salt thereof.
5. A pharmaceutical composition comprising a compound of formula
wherein
R 2A is —COC(CH 3 ) 3 , R 3A is —COC(CH 3 ) 3 and R 4A is —CH 2 NHSO 2 (CH 2 ) 2 NHCH 2 CH 3 ;
or a pharmacologically acceptable salt thereof.
6. A pharmaceutical composition comprising a compound of formula
wherein
R 2A is —COC(CH 3 ) 3 , R 3A is —COCH(CH 3 ) 2 and R 4A is —(CH 2 ) 2 NHSO 2 CH 3
or a pharmacologically acceptable salt thereof.
7. A method of treating colon cancer in a patient in need thereof comprising administering a compound according to claim 3 .
8. A method of treating colon cancer in a patient in need thereof comprising administering a compound according to claim 4 .