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Last Updated: March 29, 2024

Claims for Patent: 9,526,733


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Summary for Patent: 9,526,733
Title:ERK inhibitors
Abstract: The present invention provides thieno[2,3-c]pyrrol-4-one compounds that inhibit activity of extracellular-signal-regulated kinase (ERK) and may be useful in the treatment of cancer.
Inventor(s): Bhagwat; Shripad Venkatraman (Carmel, IN), Joseph; Sajan (Carmel, IN)
Assignee: Eli Lilly and Company (Indianapolis, IN)
Application Number:15/259,381
Patent Claims:1. A method of treating non-small cell lung cancer in a patient, comprising administering to the patient an effective amount of 6,6-dimethyl-2-{2-[(1-methyl-1H-pyrazol-5-yl)amino]pyrimidin-4-yl}-5-[2-(- morpholin-4-yl)ethyl]-5,6-dihydro-4H-thieno[2,3-c]pyrrol-4-one, or a pharmaceutically acceptable salt thereof, in combination with an effective amount of ramucirumab.

2. A method of treating non-small cell lung cancer in a patient, comprising administering to the patient an effective amount of 6,6-dimethyl-2-{2-[(1-methyl-1H-pyrazol-5-yl)amino]pyrimidin-4-yl}-5-[2-(- morpholin-4-yl)ethyl]-5,6-dihydro-4H-thieno[2,3-c]pyrrol-4-one, or a pharmaceutically acceptable salt thereof, in combination with an effective amount of [5-(4-ethyl-piperazin-1-ylmethyl)-pyridin-2-yl]-[5-fluoro-4-(7-fluoro-3-i- sopropyl-2-methyl-3H-benzoimidazol-5-yl)-pyrimidin-2-yl]-amine, or a pharmaceutically acceptable salt thereof.

3. The method according to claim 1 wherein the non-small cell lung cancer is KRAS mutant non-small cell lung cancer.

4. The method according to claim 1 wherein the non-small cell lung cancer is KRAS mutant non-small cell lung cancer.

5. A method of treating colorectal cancer in a patient, comprising administering to the patient an effective amount of 6,6-dimethyl-2-{2-[(1-methyl-1H-pyrazol-5-yl)amino]pyrimidin-4-yl}-5-[2-(- morpholin-4-yl)ethyl]-5,6-dihydro-4H-thieno[2,3-c]pyrrol-4-one, or a pharmaceutically acceptable salt thereof, in combination with an effective amount of [5-(4-ethyl-piperazin-1-ylmethyl)-pyridin-2-yl]-[5-fluoro-4-(7-fluoro-3-i- sopropyl-2-methyl-3H-benzoimidazol-5-yl)-pyrimidin-2-yl]-amine, or a pharmaceutically acceptable salt thereof.

6. A method of treating colorectal cancer in a patient, comprising administering to the patient an effective amount of 6,6-dimethyl-2-{2-[(1-methyl-1H-pyrazol-5-yl)amino]pyrimidin-4-yl}-5-[2-(- morpholin-4-yl)ethyl]-5,6-dihydro-4H-thieno[2,3-c]pyrrol-4-one, or a pharmaceutically acceptable salt thereof, in combination with an effective amount of 1-(3,3-dimethylbutyl)-3-(2-fluoro-4-methyl-5-(7-methyl-2-(methylamino)pyr- ido[2,3-d]pyrimidin-6-yl)phenyl)urea), or a pharmaceutically acceptable salt thereof.

7. The method according to claim 5 wherein the colorectal cancer is KRAS mutant colorectal cancer.

8. The method according to claim 6 wherein the colorectal cancer is KRAS mutant colorectal cancer.

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