AMINOTHIAZOLE COMPOUNDS AS C-KIT INHIBITORS

1 - 96 . (canceled)

97 . A compound of Formula (I):

or a pharmaceutically acceptable salt thereof,

wherein:

L is —C(O)NR 5 — or —NR 5 C(O)—;

A is (C 6 -C 10 ) aryl optionally substituted with one or more R 4 ;

R 1 is H, (C 1 -C 6 ) alkyl, —(CH 2 ) q C(O)OH, or —C(O)N(R 7 ) 2 ;

R 2 is (C 1 -C 6 ) alkyl, —C(O)R 8 , or —C(O)NR 9 R 10 ;

each R 3 is independently at each occurrence (C 1 -C 6 ) alkyl, (C 1 -C 6 ) alkoxy, (C 1 -C 6 ) haloalkyl, (C 1 -C 6 ) haloalkoxy, halogen, or OH;

each R 4 is independently at each occurrence (C 1 -C 6 ) alkyl, (C 1 -C 6 ) alkoxy, (C 1 -C 6 ) haloalkyl, (C 1 -C 6 ) haloalkoxy, halogen, —OH, CN, —(C(R 6 ) 2 ) p -heterocycloalkyl wherein the heterocycloalkyl comprises a 4- to 7-membered ring and 1 to 3 heteroatoms selected from N, O, and S, or —(C(R 6 ) 2 ) p -heteroaryl wherein the heteroaryl comprises a 5- or 6-membered ring and 1 to 3 heteroatoms selected from N, O, and S, and wherein the heterocycloalkyl or heteroaryl is optionally substituted with one or more substituents each independently selected from (C 1 -C 6 ) alkyl, —NH 2 , (C 1 -C 6 ) alkylamino, and (C 1 -C 6 ) dialkylamino;

R 5 is H, (C 1 -C 6 ) alkyl, or (C 1 -C 6 ) haloalkyl;

each R 6 is independently H or (C 1 -C 6 ) alkyl;

each R 7 is independently H or (C 1 -C 6 ) alkyl;

R 8 is (C 1 -C 6 ) alkyl, (C 3 -C 7 ) cycloalkyl, (C 2 -C 6 ) alkenyl, (C 1 -C 3 ) alkoxy, (C 1 -C 6 ) haloalkyl, (C 1 -C 6 ) haloalkoxy, or 4 to 7-membered heterocycloalkyl comprising 1 to 3 heteroatoms selected from N, O, and S;

R 9 is H, (C 1 -C 6 ) alkyl, (C 1 -C 6 ) haloalkyl, (C 3 -C 7 ) cycloalkyl, or 4 to 7-membered heterocycloalkyl comprising 1 to 3 heteroatoms selected from N, O, or S;

R 10 is H, (C 1 -C 6 ) alkyl, (C 1 -C 6 ) haloalkyl, (C 3 -C 7 ) cycloalkyl, or 4 to 7-membered heterocycloalkyl comprising 1 to 3 heteroatoms selected from N, O, or S, wherein the cycloalkyl or heterocycloalkyl is optionally substituted with one or more substituents each independently selected from (C 1 -C 6 ) alkyl, —NH 2 , (C 1 -C 6 ) alkylamino, (C 1 -C 6 ) dialkylamino, and —OH, and wherein the (C 1 -C 6 ) alkyl is optionally substituted with one or more R 11 ;

or R 9 and R 10 together with the nitrogen atom to which they are attached form a 4- to 7-membered heterocycloalkyl ring comprising 1 to 3 heteroatom selected from N, O, and S, optionally substituted with one or more substituent each independently selected from (C 1 -C 6 ) alkyl, (C 1 -C 6 ) hydroxyalkyl, —(CH 2 ) q —NH 2 , —(CH 2 ) q —(C 1 -C 6 ) alkylamino, —(CH 2 ) q —(C 1 -C 6 ) dialkylamino, —C(O)(C 1 -C 6 ) alkyl, —OH, and 4- to 7-membered heterocycloalkyl comprising 1 to 3 heteroatom selected from N, O, and S, and optionally substituted with one or more (C 1 -C 6 ) alkyl;

R 11 is (C 1 -C 6 ) alkoxy, —OH, —NH 2 , (C 1 -C 6 ) alkylamino, (C 1 -C 6 ) dialkylamino, 5- or 6-membered heteroaryl comprising 1 to 3 heteroatoms selected from N, O, or S, or 4- to 7-membered heterocycloalkyl comprising 1 to 3 heteroatoms selected from N, O, or S, wherein the heterocycloalkyl is optionally substituted with one or more substituents each independently selected from (C 1 -C 6 ) alkyl and OH; and

each p and q is independently 0, 1 or 2;

each n is 0 or 1;

and

provided that when A is phenyl and R 1 is H, then R 2 is not —C(O)CH 3 .

98 . The compound of claim 97 , wherein L is a —C(O)NR 5 —.

99 . The compound of claim 97 , wherein L is a —NR 5 C(O)—.

100 . The compound of claim 97 , wherein n is 1 and R 3 is methyl or F.

101 . The compound of claim 97 , wherein A is phenyl substituted with one or more R 4 .

102 . The compound of claim 97 , wherein R 5 is H.

103 . The compound of claim 97 , having one of the following formulae (Ia) or (Ib):

or a pharmaceutically acceptable salt thereof.

104 . The compound of claim 103 , having one of the following formulae (Ic) or (Id):

or a pharmaceutically acceptable salt tautomer thereof.

105 . The compound of claim 104 , having one of the following formulae (Ie) or (If):

or a pharmaceutically acceptable salt tautomer thereof.

106 . The compound of claim 105 , wherein one R 4 is (C 1 -C 6 ) haloalkyl and the other R 4 is (C 1 -C 6 ) alkoxy, CN, or —(C(R 6 ) 2 ) p -heterocycloalkyl wherein the heterocycloalkyl comprises a 4- to 7-membered ring and 1 to 3 heteroatoms selected from N, O, and S.

107 . The compound of claim 106 , wherein at least one R 4 is CF 3 and the other R 4 is (C 1 -C 6 ) alkoxy, CN, or —(C(R 6 ) 2 ) p -heterocycloalkyl wherein the heterocycloalkyl comprises a 4- to 7-membered ring and 1 to 3 heteroatoms selected from N, O, and S.

108 . The compound of claim 105 , wherein at least one R 4 is CF 3 and the other R 4 is —OCH 3 , CN, or —(CH 2 )-pyrrolyl.

109 . The compound of claim 105 , wherein R 1 is H and R 2 is —C(O)NR 9 R 10 .

110 . The compound of claim 109 , wherein R 9 is H and R 10 is (C 1 -C 6 ) alkyl or (C 1 -C 6 ) alkyl substituted with one R 11 .

111 . The compound of claim 110 , wherein R 11 is (C 1 -C 6 ) alkoxy.

112 . The compound of claim 111 , wherein the (C 1 -C 6 ) alkoxy is —OCH 3 .

113 . The compound of claim 109 , wherein R 9 is (C 1 -C 6 ) alkyl and R 10 is (C 1 -C 6 ) alkyl or (C 1 -C 6 ) alkyl substituted with one R 11 .

114 . The compound of claim 113 , wherein R 11 is (C 1 -C 6 ) alkoxy.

115 . The compound of claim 114 , wherein the (C 1 -C 6 ) alkoxy is —OCH 3 .

116 . The compound of claim 97 , wherein the compound is selected from:

3-((2-(3-(2-methoxyethyl)-3-methylureido)thiazol-5-yl)ethynyl)-4-methyl-N-(4-(pyrrolidin-1-ylmethyl)-3-(trifluoromethyl)phenyl)benzamide (I-46);

N-(2-methoxy-3-(trifluoromethyl)phenyl)-3-((2-(3-(2-methoxyethyl)-3-methylureido)thiazol-5-yl)ethynyl)-4-methylbenzamide (I-47);

N-(4-cyano-3-(trifluoromethyl)phenyl)-3-((2-(3-(2-methoxyethyl)-3-methylureido)thiazol-5-yl)ethynyl)-4-methylbenzamide (I-48);

3-((2-(cyclopropanecarboxamido)thiazol-5-yl)ethynyl)-4-methyl-N-(4-((4-methylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)benzamide (I-50); and

N-(3-((2-(3,3-dimethylureido)thiazol-5-yl)ethynyl)-4-methylphenyl)-3-(trifluoromethoxy)benzamide (I-56); and

or a pharmaceutically acceptable salt thereof.