IP Library Granted Patent US 7,122,543
Granted Patent B2
US 7,122,543 · App. 10/416,755 · Granted Oct 17, 2006

Substituted benzoic acid derivatives having NF-κB inhibiting action

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Quick Facts
Patent No.
US 7,122,543
App. No.
10/416,755
Granted
Oct 17, 2006
Kind
B2
Abstract

A substituted benzoic acid derivative which is represented by the following formula (I) and has an NF-κB inhibiting action (in the formula, R 3 , R 4 and R 5 each independently represents a hydrogen atom, an alkyl group having 1 to 6 carbon(s) or an alkoxy group having 1 to 6 carbon(s); R 9 and R 10 each independently represents a hydrogen atom, an alkyl group having 1 to 6 carbon(s) or an acyl group having 2 to 11 carbons); R 2 represents an optionally-substituted aromatic hydrocarbon group or an optionally-substituted heterocyclic group; and X represents a carboxyl group which may be esterified or amidated)

Claims (19)

1. A substituted benzoic acid derivative represented by the following formula (I):

wherein R 1 is the following formula (II):

or the following formula (III):

wherein R 3 , R 4 and R 5 each independently represents a hydrogen atom, an alkyl group having 1 to 6 carbon(s) or an alkoxy group having 1 to 6 carbon(s); R 9 and R 10 each independently represents a hydrogen atom, an alkyl group having 1 to 6 carbon(s) or an acyl group having 2 to 11 carbons;

R 2 represents an optionally-substituted aromatic hydrocarbon group or an optionally-substituted heterocyclic group; and

X represents a carboxyl group which may be esterified or amidated.

2. The substituted benzoic acid derivative according to claim 1 , wherein R 1 is the following formula (II):

wherein R 3 and R 4 each independently represents a hydrogen atom, a methyl group or a methoxy group.

3. The substituted benzoic acid derivative according to claim 1 , wherein R 1 is the following formula (II):

wherein R 5 represents a hydrogen atom or a methyl group.

4. The substituted benzoic acid derivative according to claim 1 , wherein R 2 is an optionally substituted aryl group having 6 to 12 carbons or an optionally substituted heteroaryl group having 4 to 11 carbons.

5. The substituted benzoic acid derivative according to claim 1 , wherein R 2 is a phenyl group, a 4-methoxyphenyl group, a 3-methoxyphenyl group, a 2-methoxyphenyl group, a 3,4-dimethoxyphenyl group, a 4-pyridyl group, a 3-pyridyl group, a 2-pyridyl group, a 2-furanyl group or a 3-furanyl group.

6. The substituted benzoic acid derivative according to claim 1 , wherein X is a group —COOR 6 , wherein R 6 represents a hydrogen atom, an optionally substituted alkyl group having 1 to 6 carbon(s) or an optionally substituted aralkyl group having 7 to 14 carbons.

7. The substituted benzoic acid derivative according to claim 1 , wherein X is a group —CONR 7 R 8 , wherein R 7 and R 8 each independently represents a hydrogen atom, an optionally-substituted alkyl group having 1 to 6 carbon(s), an optionally-substituted aryl group having 6 to 12 carbons, an optionally-substituted heteroaryl group having 4 to 11 carbons, an optionally-substituted aralkyl group having 7 to 14 carbons or an optionally-substituted heteroarylalkyl group having 5 to 13 carbons, or R 7 and R 8 together with the nitrogen atom to which they are attached, represents a heterocyclic ring which may further contain a nitrogen atom, oxygen atom or sulfur atom or may be condensed.

8. The substituted benzoic acid derivative according to claim 1 , wherein X is a group —CONR 7 R 8 , wherein R 7 and R 8 together with the nitrogen atom to which they are attached, represents a five to eight-membered nitrogen-containing heterocyclic ring which may further contain 1 to 3 hetero atom(s) selected from nitrogen atom, oxygen atom and sulfur atom where carbon atom or sulfur atom on the ring may be in a form of an oxide.

9. The substituted benzoic acid derivative according to claim 1 , which is represented by the following formula (I):

wherein R 1 is the following formula (II):

wherein R 3 and R 4 each represents a methyl group or a methoxy group and R 5 represents a methyl group; R 2 represents a phenyl group, a 4-methoxyphenyl group, a 3-methoxyphenyl group, a 2-methoxyphenyl group, a 3,4-dimethoxyphenyl group, a 4-pyridyl group, a 3-pyridyl group, a 2-pyridyl group, a 2-furanyl group or a 3-furanyl group; and X represents a carboxyl group which may be esterified or amidated.

10. A pharmaceutical composition of matter comprising a substituted benzoic acid derivative according to claim 1 , or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier.

Assignments (4)
CHANGE OF NAME Recorded Dec 21, 2005
From: DAIICHI SUNTORY PHARMA CO., LTD.
To: DAIICHI ASUBIO PHARMA CO., LTD.
Reel/Frame 017384/0499 →
CHANGE OF ASSIGNEE FROM JOINT TO SOLE DUE TO ABSORPTION Recorded Jun 13, 2005
From: DAIICHI SUNTORY PHARMA CO., LTD.; DAIICHI SUNTORY BIOMEDICAL RESEARCH CO., LTD.
To: DAIICHI SUNTORY PHARMA CO., LTD.
Reel/Frame 016332/0513 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 12, 2004
From: SUZUKI, KENJI; NUNOKAWA, YOICHI
To: DAIICHI SUNTORY PHARMA CO., LTD.
Reel/Frame 015982/0177 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded May 15, 2003
From: SUZUKI, KENJI; NUNOKAWA, YOICHI
To: DAIICHI SUNTORY PHARMA CO., LTD.; DAIICHI SUNTORY BIOMEDICAL RESEARCH LTD.
Reel/Frame 014644/0849 →