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1. WO2020193660 - IMIDAZOLONYLQUINOLINE COMPOUNDS AND THERAPEUTIC USES THEREOF

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[ EN ]

CLAIMS

1. A compound, represented by the following formula


or pharmaceutically acceptable salt thereof.

2. A compound, represented by the following formula


Compound 2

or pharmaceutically acceptable salt thereof.

3. A pharmaceutically acceptable salt of Compound 1 according to claim 1 , which is selected from Compound 1 fumarate, Compound 1 napsylate, and Compound 1 edisylate.

4. A solid anhydrous form of Compound 1.

5. The solid anhydrous form of Compound 1 according to claim 4, which is characterized by one or more peaks in a powder X-ray diffraction pattern selected from those at about 7.3, about 9.6, about 1 1.1 , about 12.0, about 12.7, and about 16.2 degrees 2-theta ± 0.2 degrees 2-theta.

6. The solid anhydrous form of Compound 1 according to claim 4 or 5, which is characterized in that it has a monoclinic crystal system and a P2i space group and/or the following parameters of its unit cell:


7. A compound selected from:


Compound 5

and atropisomers and pharmaceutically acceptable salts thereof.

8. The compound according to claim 7, wherein the compound is selected from:


Compound 4-a Compound 4-b


Compound 5-a Compound 5-b

and pharmaceutically acceptable salts thereof.

9. A pharmaceutical composition comprising a compound, pharmaceutically acceptable salt, or solid anhydrous form thereof according to any one of claims 1 to 8, and a pharmaceutically acceptable excipient.

10. A method for treating cancer and/or tumours in a patient, comprising administering to the patient a compound, pharmaceutically acceptable salt, or solid form thereof according to any of claims 1 to 8, or a pharmaceutical composition according to claim 9.

1 1. The method according to claim 10, comprising administering the compound, pharmaceutically acceptable salt, solid anhydrous form or pharmaceutical composition thereof in combination with radiotherapy.

12. The method according to claim 10, comprising administering the compound, pharmaceutically acceptable salt, solid anhydrous form or pharmaceutical composition thereof in combination with a DNA-damaging agent.

13. The method according to any of claims 10 to 12, wherein the tumour is selected from the group of diseases of squamous epithelium, bladder, stomach, kidneys, head, neck, oesophagus, cervix, thyroid, intestine, bone, liver, brain, prostate, urogenital tract, lymphatic system, larynx, lung, skin, blood and immune system, and/or wherein the cancer is selected from monocytic leukaemia, lung adenocarcinoma, small-cell lung carcinoma, pancreatic cancer, glioblastoma, intestinal carcinoma, breast carcinoma, acute myeloid leukaemia, chronic myeloid leukaemia, acute lymphatic leukaemia, chronic lymphatic leukaemia, Hodgkin's lymphoma and non-Hodgkin's lymphoma.

14. Use of a compound, pharmaceutically acceptable salt, or solid anhydrous form thereof according to any of claims 1 to 8, in the manufacture of a medicament for the treatment of cancer and/or tumours according to any of claims 10 to 13.

15. Compound, pharmaceutically acceptable salt or solid form thereof according to any of claims 1 to 8, for use in the treatment of cancer and/or tumours, optionally in combination with radiotherapy and/or a DNA-damaging agent.