|Title:||Benzene sulfonamide thiazole and oxazole compounds|
|Abstract:||The present invention provides thiazole sulfonamide and oxazole sulfonamide compounds, compositions containing the same, as well as processes for the preparation and methods for their use as pharmaceutical agents.|
|Inventor(s):||Rheault; Tara Renae (Durham, NC)|
|Assignee:||Novartis AG (Basel, CH)|
1. A method for treating a susceptible neoplasm selected from melanoma and non-small cell lung cancer in a mammal in need thereof comprising the steps of: (a) analyzing a
sample from said neoplasm to determine whether an activating mutation is present in the coding sequence for B-Raf in cells of said neoplasm; (b) selecting a mammal having said neoplasm with an activating mutation in the coding sequence for B-Raf; and
(c) administering a therapeutically effective amount the compound of formula ##STR00608## or a pharmaceutically acceptable salt thereof to the mammal selected in step (b).
2. The method of claim 1, wherein the activating mutation present in the coding sequence for BRAF results in a BRAF having an amino acid substitution selected from the group consisting of R462I, I463S, G464V, G464E, G466A, G466E, G466V, G469A, G469E, D594V, F595L, G596R, L597V, L597R, T599I, V600E, V600D, V600K, V600R, T119S, and K601E.
3. The method of claim 2, wherein the activating mutation present in the coding sequence for BRAF results in a BRAF having a V600E amino acid substitution.
4. The method of claim 1, wherein said neoplasm is melanoma.
5. The method of claim 4, wherein said neoplasm is metastatic melanoma.
6. The method of claim 1, wherein the activating mutation present in the coding sequence for BRAF results in the coding sequence of BRAF having a substitution of T1799A.
7. The method of claim 1, wherein said mammal is a human.