IP Library › Granted Patent US 12,508,313
Granted Patent B2
US 12,508,313 · App. 17/228,025 · Granted Dec 30, 2025

Quinoline derivative-containing pharmaceutical composition

Inventor: Masashi Bando (Kakamigahara, JP)
Assignee: Eisai R&D Management Co., Ltd.
A61K47/02A61K9/1611A61K9/1652A61K9/485A61K9/4866A61K31/47C07D215/48
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Quick Facts
Patent No.
US 12,508,313
App. No.
17/228,025
Granted
Dec 30, 2025
Kind
B2
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, R 1 is a hydrogen atom, a C 1-6 alkyl group or a C 3-8 cycloalkyl group; and R 2 is a hydrogen atom or a methoxy group.

Claims (31)

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.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 13, 2022
From: BANDO, MASASHI
To: EISAI R&D MANAGEMENT CO., LTD.
Reel/Frame 058645/0049 →
Priority Claims (1)
JP 2009-190145 · Aug 19, 2009 · national
Continuity (3)
Continuation 13923858 · Jun 21, 2013
Continuation 13322961
Related Publication 20210228722A1 · Jul 29, 2021
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