IP Library Granted Patent US 7,470,717
Granted Patent B2
US 7,470,717 · App. 10/548,475 · Granted Dec 30, 2008

Indazole derivatives

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Quick Facts
Patent No.
US 7,470,717
App. No.
10/548,475
Granted
Dec 30, 2008
Kind
B2
Abstract

The present invention provides a compound represented by Formula (I): [wherein R 1 represents CONR 1a R 1b (wherein R 1a and R 1b may be the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted aryl, substituted or unsubstituted ararkyl or a substituted or unsubstituted heterocyclic group, or R 1a and R 1b are combined together with the adjacent nitrogen atom thereto to form a substituted or unsubstituted heterocyclic group) or the like, R 2 represents a hydrogen atom, CONR 2a R 2b (wherein R 2a and R 2b may be the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted aryl, substituted or unsubstituted ararkyl or a substituted or unsubstituted heterocyclic group, or R 2a and R 2b are combined together with the adjacent nitrogen atom thereto to form a substituted or unsubstituted heterocyclic group), NR 2c R 2d (wherein R 2c and R 2d may be the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkanoyl, substituted or unsubstituted aroyl, substituted or unsubstituted heteroaroyl, substituted or unsubstituted ararkyl, substituted or unsubstituted lower alkylsulfonyl or substituted or unsubstituted lower arylsulfonyl) or the like].

Claims (20)

1. An indazole derivative represented by Formula (I)

wherein R 1 represents CONR 1a R 1b (wherein R 1a and R 1b may be the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted aryl, substituted or unsubstituted aralkyl, or a substituted or unsubstituted heterocyclic group, or R 1a and R 1b are combined together with the adjacent nitrogen atom thereto to form a substituted or unsubstituted heterocyclic group) or NR 1c R 1d (wherein R 1c represents substituted or unsubstituted lower alkylsulfonyl or substituted or unsubstituted arylsulfonyl and R 1d represents a hydrogen atom or substituted or unsubstituted lower alkyl); and

R 2 represents a hydrogen atom, halogen, cyano, nitro, hydroxy, carboxy, lower alkoxycarbonyl, substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkoxy, substituted or unsubstituted lower alkanoyl, CONR 2a R 2b (wherein R 2a and R 2b may be the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted aryl, substituted or unsubstituted aralkyl or a substituted or unsubstituted heterocyclic group, or R 2a and R 2b are combined together with the adjacent nitrogen atom thereto to form a substituted or unsubstituted heterocyclic group) or NR 2c R 2d (wherein R 2c and R 2d may be the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkanoyl, substituted or unsubstituted aroyl, substituted or unsubstituted heteroaroyl, substituted or unsubstituted aralkyl, substituted or unsubstituted lower alkylsulfonyl or substituted or unsubstituted arylsulfonyl),

or a pharmaceutically acceptable salt thereof.

2. The indazole derivative or the pharmaceutically acceptable salt thereof according to claim 1 , wherein R 1 is CONR 1a R 1b and R 2 is a hydrogen atom or substituted or unsubstituted lower alkoxy.

3. The indazole derivative or the pharmaceutically acceptable salt thereof according to claim 1 , wherein R 1 is NR 1c R 1d and R 2 is substituted or unsubstituted lower alkoxy.

4. The indazole derivative or the pharmaceutically acceptable salt thereof according to claim 1 , wherein R 1 is CONR 1a R 1b and R 2 is halogen or substituted or unsubstituted lower alkyl.

5. The indazole derivative or the pharmaceutically acceptable salt thereof according to claim 1 , wherein R 1 is NR 1c R 1d and R 2 is a hydrogen atom.

6. An indazole derivative represented by Formula (IA)

wherein R 1a and R 1b may be the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted aryl, substituted or unsubstituted aralkyl, or a substituted or unsubstituted heterocyclic group, or R 1a and R 1b are combined together with the adjacent nitrogen atom thereto to form a substituted or unsubstituted heterocyclic group,

or a pharmaceutically acceptable salt thereof.

7. The indazole derivative or the pharmaceutically acceptable salt thereof according to claim 6 , wherein R 1a and R 1b are combined together with the adjacent nitrogen atom thereto to form a substituted or unsubstituted heterocyclic group.

8. The indazole derivative or the pharmaceutically acceptable salt thereof according to claim 6 , wherein R 1a and R 1b are combined together with the adjacent nitrogen atom thereto to form a substituted or unsubstituted piperazinyl.

9. (E)-1-{4-[2-(1H-indazol-3-yl)vinyl]benzoyl}piperazine or a pharmaceutically acceptable salt thereof.

10. (E)-4-{4-[2-(1H-indazol-3-yl)vinyl]benzoyl}piperazine-2-one or a pharmaceutically acceptable salt thereof.

11. (E)-1-{4-[2-(1H-indazol-3-yl)vinyl]benzoyl}-3-aminopyrrolidine or a pharmaceutically acceptable salt thereof.

12. The indazole derivative or the pharmaceutically acceptable salt thereof according to claim 1 , wherein R 1 is CONR 1a R 1b , and R 1a and R 1b are combined together with the adjacent nitrogen atom thereto to form a substituted or unsubstituted heterocyclic group.

13. The indazole derivative or the pharmaceutically acceptable salt thereof according to claim 2 , wherein R 1a and R 1b are combined together with the adjacent nitrogen atom thereto to form a substituted or unsubstituted heterocyclic group.

14. The indazole derivative or the pharmaceutically acceptable salt thereof according to claim 4 , wherein R 1a and R 1b are combined together with the adjacent nitrogen atom thereto to form a substituted or unsubstituted heterocyclic group.

15. A pharmaceutical composition which comprises, as an active ingredient, the indazole derivative or the pharmaceutically acceptable salt thereof according to any of claims 1 - 5 or 6 - 14 together with a pharmaceutically acceptable carrier.

Assignments (2)
CHANGE OF NAME Recorded Apr 22, 2009
From: KYOWA HAKKO KOGYO CO., LTD.
To: KYOWA HAKKO KIRIN CO., LTD.
Reel/Frame 022579/0229 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Sep 12, 2005
From: OHTA, YOSHIHISA; KANAI, FUMIHIKO; NARA, SHINJI; KANDA, YUTAKA; UMCHARA, HIROSHI; SHIOTSU, YUKIMASA; NAOE, TOMOKI; KIYOI, HITOSHI; KAWASHIMA, KEIKO; ANDO, HIROMI; MIYAMA, MOTOKI
To: KYOWA HAKKO KOGYO CO., LTD.
Reel/Frame 017789/0354 →