阅读说明：本技术 作为ERK抑制剂的5,6-二氢-4H-噻吩并[2,3-c]吡咯-4-酮化合物的盐 (Salts of 5, 6-dihydro-4H-thieno [2,3-c ] pyrrol-4-one compounds as ERK inhibitors ) 是由 D·A·科亚茨 S·约瑟夫 M·A·波利齐 D·M·雷米克 于 2020-03-19 设计创作，主要内容包括：本发明提供了6,6-二甲基-2-{2-[(1-甲基-1H-吡唑-5-基)氨基]嘧啶-4-基}-5-[2-(吗啉-4-基)乙基]-5,6-二氢-4H-噻吩并[2,3-c]吡咯-4-酮的新结晶盐形式。(The present invention provides novel crystalline salt forms 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.)

1. A compound which is 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; methanesulfonic acid.

2. The compound of claim 1, wherein the compound is crystalline.

3. The compound of claim 2, characterized by an X-ray powder diffraction pattern comprising a peak at 20.2 and one or more peaks (2 θ +/-0.2 °) at 20.9, 16.9 and 23.8 (CuK α radiation, λ =1.54060 a).

4. A compound which is 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; methanesulfonic acid dihydrate.

5. The compound of claim 4, wherein the compound is crystalline.

6. The compound of claim 5, characterized by an X-ray powder diffraction pattern comprising a peak at 16.6 and one or more peaks (2 θ +/-0.2 °) at 15.9, 21.7 and 15.6 (CuK α radiation, λ = 1.54060A).

7. A compound which is 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; 4-methylbenzenesulfonic acid.

8. The compound of claim 7, wherein the compound is crystalline.

9. The compound of claim 8, characterized by an X-ray powder diffraction pattern comprising peaks at 4.4 and one or more peaks (2 θ +/-0.2 °) at 22.1, 11.6 and 17.3 (CuK α radiation, λ =1.54060 a).

10. A pharmaceutical composition comprising a compound according to any one of claims 1 to 9 and one or more pharmaceutically acceptable carriers, diluents or excipients.

11. The pharmaceutical composition of claim 10, wherein the composition comprises about 65wt% of the compound.

12. A method of treating melanoma, colorectal cancer, pancreatic cancer, non-small cell lung cancer, head and neck cancer, liver cancer, breast cancer, cholangiocarcinoma, leukemia, or thyroid cancer, comprising administering to a patient in need thereof an effective amount of a compound according to any one of claims 1 to 9.

13. A compound according to any one of claims 1 to 9 for use in therapy.

14. A compound according to any one of claims 1 to 9 for use in the treatment of cancer.

15. The compound of claim 14, wherein the cancer is melanoma, colorectal cancer, pancreatic cancer, non-small cell lung cancer, head and neck cancer, liver cancer, breast cancer, cholangiocarcinoma, leukemia, or thyroid cancer.