6-aryl-7-substituted-3-(1H-pyrazol-5-yl)-7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazines as inhibitors of the STAT3 pathway with anti-proliferative activity

A compound represented by the following formula:

• wherein:
• R is selected from the group consisting of a C1-C6 alkyl or aryl, optionally substituted by one or more selected from the group consisting of —OR′, —NR′R″,
• and an optionally substituted phenyl, wherein:
• (1) R′ and R″ are each independently selected from —H, C1-C6 alkyl and C1-C6 alkyl substituted by one or more fluoro groups, and when R′ and R″ are each alkyl they may form a ring, and
• (2) Y is selected from C1-C6 alkyl, and —NR′R″, wherein when the optionally substituted phenyl contains a substituent, the substituent is selected from —OR′, —NR′R″, and
• R1 is
• wherein:
• (1) each Z is independently selected from halogen, C1-C6 alkyl, C1-C6 alkyl substituted by one or more fluoro groups, —OR′, —NR′R″,
• (2) a is an integer of 0 to 4,
• (3) Y′ is selected from C1-C6 alkyl, C1-C6 alkyl substituted by one or more fluoro groups, —OR′, and —NR′R″,
• wherein R and R1 may form a 5 or 6 membered ring that is optionally substituted by one or more selected from the group consisting of —OR′, —NR′R″,
• and an optionally substituted phenyl,
• X is phenyl optionally substituted by one or more halogen, and
• R2 is absent or phenyl optionally substituted by one or more halogen or a pharmaceutically acceptable solvate or salt thereof, and
• wherein when R and R1 are both unsubstituted phenyl, then R2 cannot be unsubstituted phenyl.