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US 2017/0360780 A1Published application
Pharmaceutical composition comprising bicyclic nitrogen-containing aromatic heterocyclic amide compound as active ingredient
AssigneeAstellas Pharma Inc.
InventorsTakeyuki NAGASHIMA, Susumu TSUJIMOTO
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Abstract
[Problem] Provided is a pharmaceutical composition for treating multiple myeloma. [Means for Solution] The inventors of the present invention conducted examinations on a compound having an effect of inhibiting mitochondrial Complex I, and confirmed that a bicyclic nitrogen-containing aromatic heterocyclic amide compound of the present invention has the effect of inhibiting mitochondrial Complex I and that this compound exhibits the effect of inhibiting growth of multiple myeloma, and therefore completed the present invention.
Claims11
1:
- A pharmaceutical composition for treating multiple myeloma, the composition comprising:
- a compound selected from (5-{1-[(6-methoxypyridin-3-yl)methyl]piperidin-4-yl}-1H-benzimidazol-2-yl){4-[4-(trifluoromethyl)benzyl]piperazin-1-yl}methanone, (5-{1-[(5-methoxypyrazin-2-yl)methyl]piperidin-4-yl}-1H-benzimidazol-2-yl){4-[4-(trifluoromethyl)benzyl]piperazin-1-yl}methanone, 4-({4-[(6-{1-[(5-ethoxypyrazin-2-yl)methyl]piperidin-4-yl}-1-methyl-1H-indol-2-yl)carbonyl]piperazin-1-yl}methyl)benzonitrile, and 4-({4-[(5-{1-[(5-methoxypyrazin-2-yl)methyl]piperidin-4-yl}-1-methyl-1H-indol-2-yl)carbonyl]piperazin-1-yl}methyl)benzonitrile, or a pharmaceutically acceptable salt thereof as an active ingredient.
2:
- The pharmaceutical composition according to claim 1,
- wherein the multiple myeloma is a multiple myeloma in which the PI3K/Akt/mTOR pathway is enhanced.
3:
- The pharmaceutical composition according to claim 1, comprising:
- (5-{1-[(6-methoxypyridin-3-yl)methyl]piperidin-4-yl}-1H-benzimidazol-2-yl){4-[4-(trifluoromethyl)benzyl]piperazin-1-yl}methanone or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable excipient.
4:
- The pharmaceutical composition according to claim 1, comprising:
- (5-{1-[(5-methoxypyrazin-2-yl)methyl]piperidin-4-yl}-1H-benzimidazol-2-yl){4-[4-(trifluoromethyl)benzyl]piperazin-1-yl}methanone or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable excipient.
5:
- The pharmaceutical composition according to claim 1, comprising:
- 4-({4-[(6-{1-[(5-ethoxypyrazin-2-yl)methyl]piperidin-4-yl}-1-methyl-1H-indol-2-yl)carbonyl]piperazin-1-yl}methyl)benzonitrile or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable excipient.
6:
- The pharmaceutical composition according to claim 1, comprising:
- 4-({4-[(5-{1-[(5-methoxypyrazin-2-yl)methyl]piperidin-4-yl}-1-methyl-1H-indol-2-yl)carbonyl]piperazin-1-yl}methyl)benzonitrile or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable excipient.
7:
- The pharmaceutical composition according to claim 1, comprising:
- (5-{1-[(6-methoxypyridin-3-yl)methyl]piperidin-4-yl}-1H-benzimidazol-2-yl){4-[4-(trifluoromethyl)benzyl]piperazin-1-yl}methanone ditosylate, and a pharmaceutically acceptable excipient thereof.
8:
- The pharmaceutical composition according to claim 1, comprising:
- (5-{1-[(5-methoxypyrazin-2-yl)methyl]piperidin-4-yl}-1H-benzimidazol-2-yl){4-[4-(trifluoromethyl)benzyl]piperazin-1-yl}methanone ditosylate, and a pharmaceutically acceptable excipient thereof.
9:
- The pharmaceutical composition according to claim 1, comprising:
- 4-({4-[(6-{1-[(5-ethoxypyrazin-2-yl)methyl]piperidin-4-yl}-1-methyl-1H-indol-2-yl)carbonyl]piperazin-1-yl}methyl)benzonitrile ditosylate, and a pharmaceutically acceptable excipient thereof.
10:
- The pharmaceutical composition according to claim 1, comprising:
- 4-({4-[(5-{1-[(5-methoxypyrazin-2-yl)methyl]piperidin-4-yl}-1-methyl-1H-indol-2-yl)carbonyl]piperazin-1-yl}methyl)benzonitrile ditosylate, and a pharmaceutically acceptable excipient thereof.
11:
- The pharmaceutical composition according to claim 1,
- wherein lenalidomide is used in combination.