IP Library › Granted Patent US 8,604,030
Granted Patent B2
US 8,604,030 · App. 13/260,711 · Granted Dec 10, 2013

Fused piperidine compound and pharmaceutical containing same

Inventors: Masanori Ashikawa (Tokyo, JP); Toshiharu Morimoto (Tokyo, JP); Hajime Yamada (Tokyo, JP); Shunji Takemura (Tokyo, JP); Tatsuaki Nishiyama (Tokyo, JP); Takeshi Doi (Tokyo, JP); Hiroyuki Ishiwata (Tokyo, JP)
Assignee: Kowa Company, Ltd.
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Quick Facts
Patent No.
US 8,604,030
App. No.
13/260,711
Granted
Dec 10, 2013
Kind
B2
Abstract

The present invention provides a low molecular weight compound having EPO production-promoting action and/or hemoglobin production-promoting action. The present invention relates to a fused piperidine compound represented by the following general formula (1): (wherein, ring A represents a C 10-14 aryl group or 5- to 10-membered heterocyclic group, X represents N—R 7 , a sulfur atom or an oxygen atom, R 1 , R 2 , R 2′ , R 3 and R 3′ independently represent a hydrogen atom, C 1-6 alkyl group or C 3-6 cycloalkyl group, and R 4 , R 5 and R 6 independently represent a hydrogen atom or halogen atom), or a salt thereof, or a solvate thereof.

Claims (31)

1. A fused piperidine compound represented by the following general formula (1):

wherein,

ring A represents a C 10-14 aryl group or 5- to 10-membered heterocyclic group,

X represents N—R 7 , a sulfur atom or an oxygen atom, where R 7 represents a hydrogen atom or a C 1-6 alkyl group,

R 1 , R 2 , R 2′ , R 3 and R 3′ independently represent a hydrogen atom, C 1-6 alkyl group or C 3-6 cycloalkyl group, and

R 4 , R 5 and R 6 independently represent a hydrogen atom or halogen atom, a salt thereof, or a solvate thereof.

2. The compound according to claim 1 , wherein the ring A moiety is selected from the group consisting of the following formulas:

a salt thereof, or a solvate thereof.

3. The compound according to claim 1 , wherein the compound represented by general formula (1) is selected from the group consisting of:

1-acetyl-4-[(4-chlorophenyl)amino]-2-methyl-3,4-dihydro-2H-[1,8]-naphthyridine (Compound 1),

1-acetyl-4-[(4-chlorophenyl)amino]-2-methyl-3,4-dihydro-2H-[1,6]-naphthyridine (Compound 2),

1-acetyl-4-[(4-chlorophenyl)amino]-2-methyl-3,4-dihydro-2H-[1,5]-naphthyridine (Compound 3),

1-(7-(4-chlorophenylamino)-5-methyl-6,7-dihydrothieno[3,2-b]pyridine-4(5H)-yl)ethanone (Compound 4),

1-acetyl-4-[(4-chlorophenyl)amino]-2-methyl-1,2,3,4-tetrahydro-benzo[h]quinoline (Compound 5),

1-[1-(4-chlorophenylamino)-3-methyl-2,3-dihydro-4,7-phenanthroline-4-(1H)-yl]ethanone (Compound 6),

6-acetyl-9-(4-chlorophenylamino)-7-methyl-6,7,8,9-tetrahydro-3H-pyrrolo[3,2-f]quinoline (Compound 7),

1-acetyl-9-[(4-chlorophenyl)amino]-7-methyl-6,7,8,9-dihydro-1H-imidazo[4,5-f]quinoline (Compound 8),

7-acetyl-10-[(4-chlorophenyl)amino]-8-methyl-7,8,9,10-tetrahydro-3H-pyrano[3,2-f]-quinolin-3-one (Compound 9),

1-[8-(4-chlorophenylamino)-6-methyl-7,8-dihydro-[1,3]dioxolo[4,5-g]quinolin-5(6H)-yl]ethanone (Compound 10),

6-acetyl-9-[(4-chlorophenyl)amino]-7-methyl-2,3,6,7,8,9-hexahydro-[1,4]dioxano[2,3-g]-quinoline (Compound 11), and

6-acetyl-9-(4-chlorophenylamino)-7-methyl-6,7,8,9-tetrahydro-2H-[1,4]oxazino[2,3-g]quinolin-3(4H)-one (Compound 12), or a salt thereof, or a solvate thereof.

4. A pharmaceutical composition comprising one or more compounds according to claim 1 , or a salt thereof, or a solvate thereof, and a pharmaceutically acceptable carrier.

5. The pharmaceutical composition according to claim 4 for promoting production of EPO.

6. The pharmaceutical composition according to claim 4 , for promoting the production of hemoglobin.

7. The pharmaceutical composition according to claim 4 , for the prevention and/or treatment of anemia.

8. An EPO production promoter having as an active ingredient thereof the compound according to claim 1 , a salt thereof, or a solvate thereof.

9. A hemoglobin production promoter having as an active ingredient thereof the compound according to claim 1 , a salt thereof, or a solvate thereof.

10. An anemia preventive and/or therapeutic agent having as an active ingredient thereof the compound according to claim 1 , a salt thereof, or a solvate thereof.

11. A method of promoting production of EPO, comprising administering an effective amount of the compound according to claim 1 , a salt thereof or a solvate thereof, to a patient requiring promotion of EPO production.

12. A method of promoting production of hemoglobin, comprising administering an effective amount of the compound according to claim 1 , a salt thereof or a solvate thereof, to a patient requiring promotion of hemoglobin production.

13. A method of preventing and/or treating anemia, comprising administering an effective amount of the compound according to claim 1 , a salt thereof or a solvate thereof, to an anemia patient.

Assignments (1)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 20, 2012
From: ASHIKAWA, MASANORI; MORIMOTO, TOSHIHARU; YAMADA, HAJIME; TAKEMURA, SHUNJI; NISHIYAMA, TAKSUAKI; DOI, TAKESHI; ISHIWATA, HIROYUKI
To: KOWA COMPANY, LTD.
Reel/Frame 027571/0391 →
Priority Claims (2)
JP 2009-079544 · Mar 27, 2009 · national
JP 2009-091484 · Apr 3, 2009 · national
Continuity (1)
Related Publication 20120108581A1 · May 3, 2012