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Last Updated: April 2, 2026

Claims for Patent: 12,508,313


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Summary for Patent: 12,508,313
Title:Quinoline derivative-containing pharmaceutical composition
Abstract:A pharmaceutical composition comprising a compound represented by the formula (I) or pharmaceutically acceptable salt thereof or solvate thereof; and a basic substance is excellent in dissolution, is stable even after a long term storage, and is useful as a preventive or therapeutic agent against a tumor: wherein, R1 is a hydrogen atom, a C1-6 alkyl group or a C3-8 cycloalkyl group; and R2 is a hydrogen atom or a methoxy group.
Inventor(s):Masashi Bando
Assignee: Eisai R&D Management Co Ltd
Application Number:US17/228,025
Patent Claims: 1. A pharmaceutical composition, comprising: (1) 4-(3-chloro-4-(cyclopropylaminocarbonyl)aminophenoxy)-7-methoxy-6-quinolinecarboxamide methanesulfonate; (2) an alkaline earth metal carbonate wherein the weight ratio of 4-(3-chloro-4-(cyclopropylaminocarbonyl)aminophenoxy)-7-methoxy-6-quinolinecarboxamide methanesulfonate to the alkaline earth metal carbonate is from 1:0.25 to 1:26.4; and (3) a disintegrating agent, wherein the alkaline earth metal carbonate is magnesium carbonate or calcium carbonate.

2. The composition of claim 1, wherein the alkaline earth metal carbonate is magnesium carbonate.

3. The composition of claim 1, wherein the alkaline earth metal carbonate is calcium carbonate.

4. The composition of claim 2, wherein the disintegrating agent is carmellose sodium, carmellose calcium, carboxymethyl starch sodium, croscarmellose sodium, low-substituted hydroxypropylcellulose, or crospovidone.

5. The composition of claim 4, wherein the disintegrating agent is low-substituted hydroxypropylcellulose.

6. The composition of claim 2, wherein the weight ratio of 4-(3-chloro-4-(cyclopropylaminocarbonyl)aminophenoxy)-7-methoxy-6-quinolinecarboxamide methanesulfonate to the magnesium carbonate is from 1:1 to 1:25.

7. The composition of claim 2, wherein 4-(3-chloro-4-(cyclopropylaminocarbonyl)aminophenoxy)-7-methoxy-6-quinolinecarboxamide methanesulfonate is present in an amount from 1 wt % to 12.5 wt %.

8. The composition of claim 2, wherein the composition is in a capsule dosage form.

9. The composition of claim 2, wherein the composition is in a tablet dosage form.

10. The composition of claim 2, wherein the composition is in a granular form.

11. The composition of claim 3, wherein the disintegrating agent is carmellose sodium, carmellose calcium, carboxymethyl starch sodium, croscarmellose sodium, low-substituted hydroxypropylcellulose, or crospovidone.

12. The composition of claim 11, wherein the disintegrating agent is low-substituted hydroxypropylcellulose.

13. The composition of claim 12, wherein the composition further comprises mannitol, hydroxypropylcellulose, microcrystalline cellulose, and talc.

14. The composition of claim 3, wherein the weight ratio of 4-(3-chloro-4-(cyclopropylaminocarbonyl)aminophenoxy)-7-methoxy-6-quinolinecarboxamide methanesulfonate to the calcium carbonate is from 1:1 to 1:25.

15. The composition of claim 3, wherein 4-(3-chloro-4-(cyclopropylaminocarbonyl)aminophenoxy)-7-methoxy-6-quinolinecarboxamide methanesulfonate is present in an amount from 1 wt % to 12.5 wt %.

16. The composition of claim 15, wherein the calcium carbonate is present in an amount ranging from 10 to 40 wt %.

17. The composition of claim 3, wherein the composition is in a capsule dosage form.

18. The composition of claim 11, wherein the composition is in a capsule dosage form.

19. The composition of claim 12, wherein the composition is in a capsule dosage form.

20. The composition of claim 13, wherein the composition is in a capsule dosage form.

21. The composition of claim 14, wherein the composition is in a capsule dosage form.

22. The composition of claim 15, wherein the composition is in a capsule dosage form.

23. The composition of claim 16, wherein the composition is in a capsule dosage form.

24. The composition of claim 3, wherein the composition is in a tablet dosage form.

25. The composition of claim 11, wherein the composition is in a tablet dosage form.

26. The composition of claim 12, wherein the composition is in a tablet dosage form.

27. The composition of claim 3, wherein the composition is in a granular form.

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