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US 2013/0158020 A1Published application
Indazole derivatives useful as erk inhibitors
AssigneeMerck Sharp & Dohme Corp.
InventorsYongqi Deng, Gerald W. Shipps, JR., Sie-Mun Lo, Liang Zhu, Alan B. Cooper, Kiran Muppalla
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Abstract
The present invention provides a compound of the Formula I: Formula I or a pharmaceutically acceptable salt, solvate or ester thereof, wherein R, R1, R2, R3, R4, X, m and n are as defined herein. The compounds are ERK inhibitors. Also disclosed are pharmaceutical compositions comprising the above compounds and methods of treating cancer using the same.
Claims19
A compound of Formula I
- or a pharmaceutically acceptable salt, solvate or ester thereof, wherein:
- R is H;
- R1 is selected from the group consisting of aryl, heterocyclyl and —C(═O)—NR5R6;
- R2 is H or alkyl;
- X is selected from the group consisting of —NR7, —C(R8)(R9)—, —O—, —S—, —S(═O)—, and —S(═O)2;
- each R3 independently is selected from the group consisting of alkyl, aryl, hydroxyl, and —S-alkyl, or wherein two R3 groups together with the same carbon atom to which both are attached form —C(═O)—;
- m is 0, 1, or 2;
- n is 0 or 1;
- R4 is selected from the group consisting of H, alkyl, aryl, —C(═O)-aryl, and —C(═O)—O-alkyl;
- R5, R6, and R7 independently are H or alkyl;
- R8 and R9 independently are H, alkyl or aryl;
- or —C(R8)(R9)— together is heterocyclyl.
9 more elements
The method of claim 25, wherein said cancer is selected from the group consisting of:
- lung cancer, pancreatic cancer, colon cancer, colorectal cancer, myeloid leukemias, acute myelogenous leukemia, chronic myelogenous leukemia, chronic myelomonocytic leukemia, thyroid cancer, myelodysplastic syndrome, bladder carcinoma, epidermal carcinoma, melanoma, breast cancer, prostate cancer, head and neck cancers, ovarian cancer, brain cancers, cancers of mesenchymal origin, sarcomas, tetracarcinomas, nuroblastomas, kidney carcinomas, hepatomas, non-Hodgkin's lymphoma, multiple myeloma, and anaplastic thyroid carcinoma.
Dependencies are inferred from the claim text.