COMPOUNDS AND COMPOSITIONS AS c-Kit KINASE INHIBITORS

A compound represented by Formula I:

• or a pharmaceutically acceptable salt thereof;
• wherein:
• R1 represents independently for each occurrence, —CN, C1-6 alkyl, or C1-6 haloalkyl;
• R2 is a 3 membered saturated monocyclic carbocyclic ring wherein R2 is substituted with p occurrences of R6
• R6 represents independently for each occurrence oxo, halogen, C1-6 aliphatic, C1-6 haloaliphatic, —CN, —NO2, —OR, —OCR3, —SR, —NR2, —S(O)2R, —S(O)2NR2, —S(O)R, —S(O)NR2, —C(R)2OR, —C(O)R, —C(O)OR, —C(O)NR2, —C(O)N(R)OR, —OC(O)R, —OC(O)NR2, —N(R)C(O)OR, —N(R)C(O)R, —N(R)C(O)NR2, —N(R)C(NR)NR2, —N(R)NR2, —N(R)S(O)2NR2, —N(R)S(O)2R, —N═S(O)R2, —S(NR)(O)R, —N(R)S(O)R, —N(R)CN, or optionally substituted phenyl;
• RA is of any of the following structures:
• each of which is substituted by n occurrences of R3;
• R3 represents independently for each occurrence oxo, —CN, —NO2, —OR, —OCR3, —SR, —NR2, —S(O)2R, —S(O)2NR2, —S(O)R, —S(O)NR2, —C(R)2OR, —C(R)2OCR3—C(O)R, —C(O)OR, —C(O)NR2, —C(O)N(R)OR, —OC(O)R, —OC(O)NR2, —N(R)C(O)OR, —N(R)C(O)R, —N(R)C(O)NR2, —N(R)C(NR)NR2, —N(R)NR2, —N(R)S(O)2NR2, —N(R)S(O)2R, —N═S(O)R2, —S(NR)(O)R, —N(R)S(O)R, —N(R)CN, -L2-R5, or an optionally substituted group selected from C1-6 haloaliphatic, phenyl, naphthalenyl, a 3-7 membered saturated or partially unsaturated monocyclic carbocyclic ring;
• a 3-7 membered saturated or partially unsaturated monocyclic heterocyclic ring having 1-2 heteroatoms independently selected from nitrogen, oxygen, and sulfur;
• or a 5-6 membered monocyclic heteroaryl ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, and sulfur;
• an 8-10 membered bicyclic heteroaryl ring having 1-5 heteroatoms independently selected from nitrogen, oxygen, and sulfur;
• a 5-8 membered saturated or partially unsaturated bridged bicyclic ring having 0-3 heteroatoms independently selected from nitrogen, oxygen, and sulfur;
• a 6-11 membered saturated or partially unsaturated spirocyclic ring having 0-3 heteroatoms independently selected from nitrogen, oxygen, and sulfur;
• or a 6-11 membered saturated or partially unsaturated bicyclic heterocyclic ring having 1-3 heteroatoms independently selected from nitrogen, oxygen, and sulfur;
• each of which is substituted with r instances of R;
• or:
• two R3 groups on adjacent carbon atoms are taken together with the carbon atoms to which they attach to form an optionally substituted 4-7 membered saturated monocyclic ring having 0-3 heteroatoms independently selected from nitrogen, oxygen, and sulfur, substituted with r instances of R;
• L2 represents independently for each occurrence a C1-6 bivalent saturated or unsaturated, straight or branched hydrocarbon chain wherein one, two, or three methylene units of the chain are independently replaced by —N(R)—, —N(R)C(O)—, —C(O)N(R)—, —N(R)S(O)2—, —S(O)2N(R)—, —O—, —C(O)—, —OC(O)—, —C(O)O—, —S—, —S(O)—, —S(O)2— or -Cy-;
• Cy represents independently for each occurrence phenyl, a 3-7 membered saturated or partially unsaturated monocyclic carbocyclic ring or a 3-7 membered saturated or partially unsaturated monocyclic heterocyclic ring having 1-2 heteroatoms independently selected from nitrogen, oxygen, and sulfur;
• R5 represents independently for each occurrence hydrogen, OR, C1-6 aliphatic, C1-6 haloaliphatic, or phenyl fused to a 5-6 membered saturated heterocyclic ring having 1-2 heteroatoms independently selected from nitrogen, oxygen, and sulfur;
• each R is independently hydrogen, —CN, halogen, oxo, or an optionally substituted group selected from C1-6 aliphatic;
• C1-6 haloaliphatic;
• C1-3 hydroxyalkyl;
• phenyl;
• naphthalenyl;
• a 3-7 membered saturated or partially unsaturated monocyclic carbocyclic ring;
• a 3-7 membered saturated or partially unsaturated monocyclic heterocyclic ring having 1-2 heteroatoms independently selected from nitrogen, oxygen, and sulfur;
• a 5-6 membered monocyclic heteroaryl ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, and sulfur;
• an 8-10 membered bicyclic heteroaryl ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, and sulfur;
• a 7-12 membered saturated or partially unsaturated bicyclic heterocyclic ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, and sulfur;
• a 5-8 membered saturated or partially unsaturated bridged bicyclic ring having 0-3 heteroatoms independently selected from nitrogen, oxygen, and sulfur;
• a 6-10 membered saturated or partially unsaturated spirocyclic ring having 0-3 heteroatoms independently selected from nitrogen, oxygen, and sulfur;
• a 6-11 membered saturated or partially unsaturated bicyclic carbocyclic ring having 1-2 heteroatoms independently selected from nitrogen, oxygen, and sulfur;
• or:
• two R groups on the same nitrogen are taken together with the nitrogen to form an optionally substituted 4-7 membered monocyclic saturated, partially unsaturated, or heteroaryl ring having, in addition to the nitrogen, 0-3 heteroatoms independently selected from nitrogen, oxygen, and sulfur;
• an 8-10 membered bicyclic heteroaryl ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, and sulfur;
• a 7-12 membered saturated or partially unsaturated bicyclic heterocyclic ring having 1-4 heteroatoms independently selected from nitrogen, oxygen, and sulfur;
• m is 0 or 1;
• n is 1, 2, 3, 4, or 5;
• p is 0, 1, 2, 3, 4, or 5;
• and
• r is 0, 1, 2, 3, 4, or 5.