CLAIMS
What is claimed is:
1.
A compound selected from the group consisting of propane-1-sulfonic acid {2,4-difluoro-
3-[5-(2-methoxy-pyrimidin-5-yl)-1H-pyrrolo[2,3-b]pyridine-3-carbonyl]-phenyl}-amide, propane-1sulfonic acid [3-(5-cyano-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-difluoro-phenyl]-amide, propane-1sulfonic acid [3-(5-cyano-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2-fluoro-phenyl]-amide, N-[3-(5-cyano1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-difluoro-phenyl]-2,5-difluoro-benzenesulfonamide, N-[3-(5cyano-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-difluoro-phenyl]-3-fluoro-benzenesulfonamide,
pyrrolidine-1-sulfonic acid [3-(5-cyano-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-difluoro-phenyl]amide, N,N-dimethylamino-sulfonic acid [3-(5-cyano-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4difluoro-phenyl]-amide, and a pharmaceutically acceptable salt thereof.
2.
The compound of Claim 1 that is propane-1-sulfonic acid {2,4-difluoro-3-[5-(2-methoxy-
pyrimidin-5-yl)-1H-pyrrolo[2,3-b]pyridine-3-carbonyl]-phenyl}-amide, or a pharmaceutically acceptable
salt thereof.
3.
The compound of Claim 1 that is propane-1-sulfonic acid [3-(5-cyano-1H-pyrrolo[2,3-
b]pyridine-3-carbonyl)-2,4-difluoro-phenyl]-amide, or a pharmaceutically acceptable salt thereof.
4.
The compound of Claim 1 that is propane-1-sulfonic acid [3-(5-cyano-1H-pyrrolo[2,3-
b]pyridine-3-carbonyl)-2-fluoro-phenyl]-amide, or a pharmaceutically acceptable salt thereof.
5.
The compound of Claim 1 that is N-[3-(5-cyano-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-
2,4-difluoro-phenyl]-2,5-difluoro-benzenesulfonamide, or a pharmaceutically acceptable salt thereof.
6.
The compound of Claim 1 that is N-[3-(5-cyano-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-
2,4-difluoro-phenyl]-3-fluoro-benzenesulfonamide, or a pharmaceutically acceptable salt thereof.
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7.
The compound of Claim 1 that is pyrrolidine-1-sulfonic acid [3-(5-cyano-1H-pyrrolo[2,3-
b]pyridine-3-carbonyl)-2,4-difluoro-phenyl]-amide, or a pharmaceutically acceptable salt thereof.
8.
The compound of Claim 1 that is N,N-dimethylamino-sulfonic acid [3-(5-cyano-1H-
pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-difluoro-phenyl]-amide, or a pharmaceutically acceptable salt
thereof.
9.
A composition comprising the compound or salt thereof according to any one of claims
1-8 and one or more pharmaceutically acceptable excipients.
10.
A kit comprising the compound or salt thereof according to any one of claims 1-8 or a
composition according to claim 9.
11.
A compound or salt thereof according to any one of claims 1-8 for use as a medicament.
12.
Use of a compound or salt thereof according to any one of claims 1-8 or a composition
according to claim 9 in the preparation of a medicament for the treatment of a disease or condition for
which modulation of B-Raf V600E protein kinase activity provides a therapeutic benefit.
13.
Use of a compound or salt thereof according to any one of claims 1-8 or a composition
according to claim 9 in the preparation of a medicament for the treatment of a disease or condition
selected from the group consisting of melanoma, glioma, colorectal cancer, thyroid cancer, lung cancer,
ovarian cancer, prostate cancer, and biliary tract cancer.
14.
A method for treating a subject suffering from or at risk of a B-Raf V600E kinase-
mediated disease or condition, comprising administering a therapeutically effective amount of the
compound or salt thereof according to any one of claims 1-8 or the composition according to claim 9.
15.
A method for treating a subject suffering from or at risk of a disease selected from the
group consisting of melanoma, glioma, colorectal cancer, thyroid cancer, lung cancer, ovarian cancer,
prostate cancer, and biliary tract cancer, comprising administering a therapeutically effective amount of
the compound or salt thereof according to any one of claims 1-8 or the composition according to claim 9.
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ABSTRACT
Propane-1-sulfonic acid {2,4-difluoro-3-[5-(2-methoxy-pyrimidin-5-yl)-1H-pyrrolo[2,3b]pyridine-3-carbonyl]-phenyl}-amide, propane-1-sulfonic acid [3-(5-cyano-1H-pyrrolo[2,3-b]pyridine3-carbonyl)-2,4-difluoro-phenyl]-amide, propane-1-sulfonic acid [3-(5-cyano-1H-pyrrolo[2,3-b]pyridine3-carbonyl)-2-fluoro-phenyl]-amide, N-[3-(5-cyano-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-difluorophenyl]-2,5-difluoro-benzenesulfonamide, N-[3-(5-cyano-1H-pyrrolo[2,3-b]pyridine-3-carbonyl)-2,4difluoro-phenyl]-3-fluoro-benzenesulfonamide, pyrrolidine-1-sulfonic acid [3-(5-cyano-1H-pyrrolo[2,3b]pyridine-3-carbonyl)-2,4-difluoro-phenyl]-amide, N,N-dimethylamino-sulfonic acid [3-(5-cyano-1Hpyrrolo[2,3-b]pyridine-3-carbonyl)-2,4-difluoro-phenyl]-amide, and salts thereof, formulations thereof,
conjugates thereof, derivatives thereof, forms thereof and uses thereof are described. In certain aspects
and embodiments, the described compounds or salts thereof, formulations thereof, conjugates thereof,
derivatives thereof, and forms thereof are active on at least one Raf protein kinase. Also described are
methods of use thereof to treat diseases and conditions, including diseases and conditions associated with
activity of Raf protein kinases, including melanoma, glioma, colorectal cancer, thyroid cancer, lung
cancer, ovarian cancer, prostate cancer, and biliary tract cancer.
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