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US 2013/0172353 A1Published application
3-phenyl-5-ureidoisothiazole-4-carboximide and 3-amino-5-phenylisothiazole derivatives as kinase inhibitors
AssigneeAllergan, Inc.
InventorsThomas C. Malone, C. Eugene Hull, Sougato Boral, Julie A. Wurster, Michael R. Robinson, Jeffrey L. Edelman
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Abstract
This invention is directed to a compound of Formula I or a pharmaceutically acceptable salt thereof, wherein R, R1, R2, R3, n, X1, X2, L1, and L2 are as defined herein. The compounds of Formula I are useful as receptor tyrosine kinase (RTK) inhibitors and can be used to treat such diseases as cancer, blood vessel proliferative disorders, fibrotic disorders, mesangial cell proliferative disorders and metabolic diseases.
Claims20
A compound of Formula I:
- or a pharmaceutically acceptable salt thereof, wherein:
- each of X1 and X2 is independently N or S, with the proviso that X1 and X2 are not simultaneously S;
- L1 is selected from the group consisting of —N(R)—, —N(R)—C(═O)—N(R)—, —O—C(═O)—N(R)—, —N(R)—C(═O)— and —C(═O)—N(R)—;
- L2 is selected from the group consisting of a covalent bond, —N(R)—, —N(R)—C(═O)—, —C(═O)—N(R)— and —N(R)—C(═O)—N(R)—;
- each R independently is H or C1-6 alkyl;
- each R1 independently is selected from the group consisting of C1-6 alkyl, C1-6 haloalkyl, halogen, and OR;
- or wherein two adjacent R1 groups taken together with the carbon atoms to which they are attached form a six-membered aryl or a five- or six-membered heteroaryl;
- n is 0, 1, or 2;
- R2 is selected from the group consisting of:
- a) H;
- b) C1-6 alkyl that is unsubstituted or substituted with one or two substituents selected from the group consisting of heterocyclyl, —C(═O)OR, hydroxy, O1-6 alkoxy, and aryl;
- and
- and
- R3 is selected from the group consisting of H, hydroxy, —NO2, aryl, and heteroaryl, wherein said aryl or heteroaryl is unsubstituted or substituted with one to three substituents selected from the group consisting of halo, C1-6 haloalkyl, and C1-6 alkyl.
11 more elements
Dependencies are inferred from the claim text.