Patent ID: 11932636
Assignee: CYTEIR THERAPEUTICS, INC.
Field: Organic fine chemistry (Chemistry)
Classification: CPC C | IPC C

Claim 0:
1. A method of improving or partially ameliorating cancer, comprising administering to a subject in need thereof an effective amount, of a compound of Formula I:, , or a pharmaceutically acceptable salt or solvate thereof, wherein:
the thiazolyl ring, is optionally substituted with F or Cl;
the ring Cy is C3-C7 cycloalkyl, bridged C6-C12 cycloalkyl, or saturated heterocyclyl comprising one or two 3- to 7-membered rings and 1-3 heteroatoms selected from N, O, and S, wherein the cycloalkyl or heterocyclyl moiety is optionally substituted with one or more groups selected from halogen, OH, CN, NH2, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, and C1-C4 haloalkoxy;
X1 is NR8 or O, or, when X1 is bonded to a nitrogen atom in the ring Cy, X1 is absent;
X2 is NR8 or O;
R1 is H or C1-C6 alkyl optionally substituted with halogen, OH, C1-C6 alkoxy, or C6-C10 aryloxy;
R2 is H or C1-C6 alkyl optionally substituted with halogen, OH, C1-C6 alkoxy, or C6-C10 aryloxy;
or R1 and R2, together with the nitrogen atom to which they are attached, form a heterocyclyl comprising one or two 3- to 7-membered rings and 1-3 heteroatoms selected from N, O, and S;
R3 is C1-C6 alkyl optionally substituted with one or more groups selected from halogen, OH, and CN, phenyl, CH2-phenyl, C3-C7 cycloalkyl, CH2—(C3-C7) cycloalkyl, heterocyclyl, or CH2-heterocyclyl, wherein the heterocyclyl comprises one or two 3- to 7-membered rings and 1-3 heteroatoms selected from N, O, and S, wherein the cycloalkyl, phenyl, or heterocyclyl moiety is optionally substituted with one or more groups selected from halogen, OH, CN, C1-C4 alkyl, C1-C4 haloalkyl, C1-C4 alkoxy, and C1-C4 haloalkoxy;
A1, A2, A3, and A4 are each independently N or C(R4);
each R4 is independently H, halogen, CN, OH, N(R6′)2, C1-C6 alkoxy, C(═O)N(R6)2, C(═O)OR6, C(═O)R6, Q-T, C6-C10 aryl, or heteroaryl comprising one or two 5- or 6-membered rings and 1-3 heteroatoms selected from N, O, and S, wherein the aryl or heteroaryl moiety is optionally substituted with one or more R9;
each Q is independently C1-C4 alkylene or O—(C1-C4) alkylene wherein the oxygen atom is bonded to the ring, each T is independently C1-C4 alkoxy, OH, N(R6)2, N(R5)C(═O)R6, N(R5)C(═O)OR6, C(═O)N(R6)2, C(═O)OR6, C(═O)R6, C6-C10 aryl, or heteroaryl comprising one or two 5- or 6-membered rings and 1-3 heteroatoms selected from N, O, and S, wherein the aryl or heteroaryl moiety is optionally substituted with one or more R9;
each R5 is independently H or C1-C4 alkyl;
each R6′ is independently H, C1-C6 alkyl optionally substituted with one or more R7, C1-C6 haloalkyl, C3-C7 cycloalkyl, heterocyclyl comprising one or two 3- to 7-membered rings and 1-3 heteroatoms selected from N, O, and S, C6-C10 aryl, or heteroaryl comprising one or two 5- or 6-membered rings and 1-3 heteroatoms selected from N, O, and S, wherein the cycloalkyl, heterocyclyl, aryl, or heteroaryl moiety is optionally substituted with one or more R9, wherein at least one R6′ is not H;
or two R6′ together with the atoms to which they are attached form a 3- to 10-membered heterocyclyl comprising 1-3 heteroatoms selected from N, O, and S, wherein the heterocyclyl is optionally substituted with one or more R9;
each R6 is independently H, C1-C6 alkyl optionally substituted with one or more R7, C1-C6 haloalkyl, C6-C10 aryl, or heteroaryl comprising one or two 5- or 6-membered rings and 1-3 heteroatoms selected from N, O, and S, wherein the aryl or heteroaryl moiety is optionally substituted with one or more R9;
or two R6 together with the atoms to which they are attached form a 3- to 10-membered heterocyclyl comprising 1-3 heteroatoms selected from N, O, and S, wherein the heterocyclyl is optionally substituted with one or more R9;
each R7 is independently N(R8)2, OR8, C6-C10 aryl, or heteroaryl comprising one or two 5- or 6-membered rings and 1-3 heteroatoms selected from N, O, and S;
each R8 is independently H or C1-C6 alkyl; and
each R9 is independently oxo, halogen, OH, CN, NH2, N(C1-C4 alkyl)2, C1-C6 alkyl, C1-C6 haloalkyl, C1-C6 alkoxy, or C1-C6 haloalkoxy, wherein the C1-C6 alkyl is optionally substituted with one or more oxo, OH, O(C1-C4 alkyl), CN, NH2, NH(C1-C4 alkyl), or N(C1-C4 alkyl)2.